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Analgesic & Antimigraine

 Butorphanol  Naloxone
 Dihydroergotamine  Propoxyphene
 Fentanyl  Sumatriptan
 Meperidine  Tramadol
 Methadone
 Morphine
Butorphanol
 Opioid analgesic  Dysphoria
 Mixed opioid agonist-antagonist  Nightmares
 w/drawal in pts dependent on full
opioid agonists
 Partial agonist or antagonist @
opioid µ receptors  AVOID MAOI
 Agonist @ κ receptors @ spinal &  Potentially fatal
supraspinal sites
 Inhibits spinothalamic pain
neurotransmission

 Moderate-severe pain
 Admin intranasally

 ↓ respiratory depression, constipation,


dependence than full µ receptor
agonists
Dihydroergotamine
 Antimigraine  N, V
 Ergot alkaloid  Stiff neck, shoulder, extremities
 5-HT 1B/1D receptor agonist  Leg weakness
 Numbness & tingling in fingers &
toes
 Activates 5-HT 1B/1D receptors
 Pial & dural vessel constriction
 Presynaptic inhibition of trigeminal
peptide neurotransmitter release
 Inhibitions brainstem activation of
trigeminal neurons

 Vascular HA
 Migraine & cluster

 Injection or nasal spray


Fentanyl
 Opioid analgesic  Sedation
 Phenylpiperidine  Confusion
 Respiratory depression
 Activates opioid µ receptors  Anorexia
 Inhibits pain transmission @  N, V
spinal & supraspinal sites  Constipation

 Chronic pain  AVOID MAOI in past 14d


 Breakthrough for cancer pain

 Transdermal patch
Meperidine
 Opioid analgesic  Confusion
 Sedation
 Strong opioid agonist  Constipation
 N, V
 Activates opioid receptors  Dependence
 Inhibits pain transmission  Toxic metabolite  CNS
excitation, convulsions, tremors
 Generalized CNS depression
 AVOID MAOI
 Moderate-severe pain  Potentially fatal
 Analgesia during labor
 Preoperative sedation

 Lacks antitussive activity


Methadone
 Opioid analgesic  Respiratory depression
 Constipation
 Strong opioid agonist  Confusion
 Sedation
 Activates opioid receptors
 Inhibits pain transmission  AVOID MAOI
 Suppresses opioid w/drawl
Sx w/ euphoria or
dependence

 Moderate-severe pain
 Prevention of opioid abuse

 Orally, once per day


Morphine
 Opioid analgesic  Sedation
 Strong opioid µ receptor agonist  Confusion
 Hypotension
 Constipation
 Activates µ receptors
 Respiratory depression
 ↑ cAMP
 Opens K & closes Ca channels
 ↓ release substance P  AVOID MAOI w/ 14 d
 Potentially fata
 Inhibits pain @ spinal & supraspinal
sites

 Severe pain w/ MI
 Pulmonary edema

 Active metabolite
 Morphine glucuronate
Naloxone
 Opioid antagonist
 Opioid receptor antagonist

 Blocks opioid µ, δ, κ
receptors
 Rapidly reverses effects of
opioid agonists

Opioid OD, dependence

Short half-life needs


repeated doses
Propoxyphene
 Opioid analgesic  Dizziness
 Weak opioid agonist  Weakness
N
 dependence
 Activates opioid receptors
 Inhibits pain transmission

 Mid-moderate pain

 Combined w/
acetaminophen or aspirin
Sumatriptan
 Antimigraine  Dizziness
 5-HT 1B/1D receptor agonist  Vertigo
 Tingling
 Warm sensation
 Activates 5-HT 1B/1D receptors
 Tight feeling head & chest
 Pial & dural vessel constriction
 Coronary vasospasm
 Presynaptic inhibition of trigeminal
peptide neurotransmitter release
 AVOID
 Inhibitions brainstem activation of  MAOI
trigeminal neurons  SSRI

 Vascular HA
 Migraine & cluster

 Oral, nasal, & subQ


Tramadol
 Analgesic  Dizziness
 Dual action  HA
 Constipation
 Activates µ opioid receptors  Lowers seizure threshold
 Inhibits neuronal reuptake 5-
HT & NE  AVOID MAOI
 ↑ inhibition of pain
 ↑ risk seizures w/ high doses
 Moderate pain  Penicillins
 Chronic pain  Phenothiazines

 Naloxone reverses some but


NOT all Sx
Anesthetics
 Benzocaine  Midazolam
 Bupivacaine  Nitrous oxide
 Halothane  Propofol
 Ketamine  Sevoflurane
 Lidocaine
Benzocaine
 Local anesthetic  Cross-sensitivity w/ other ester-type
anesthetics
 Ester-type

 Blocks Na channels & nerve conduction

 Topical anesthetic
 Pain
 Itching
 Inflammation
 Burns
 Insect bites
 Contact dermatitis
 Wounds

 Irritates skin when 1st applied


 Use caution w/ sunburn & large areas of
skin
Bupivacaine
 Local anesthetic  Cross-sensitivity w/ amide-
type anesthetics
 Amide-type

 Blocks Na channels &


nerve conduction

 Local or regional anesthetic


 Surgical
 Diagnostic
 Obstetrical
 therapeutic
Halothane
 General anesthetic  Sensitizes heart to catecholamine-
induced cardiac arrhythmia
 Inhalational, halogenated  Hepatotoxic
hydrocarbon  Fluoride metabolites

 Potentiates GABA binding to


GABA-A Cl ion channel
 Suppresses sensory processing
in thalamus

 General anesthetic

 High blood:gas partition


coefficient
 Slow rate of induction &
recovery
Ketamine
 IV anesthetic  Delirium
 Glutamate antagonist  Hallucination
 Irrational behavior during recovery
 ↑ BP
 Blocks glutamate NMDA receptors
 Dissociate anesthesia
 Analgesia
 Immobility
 Amnesia

 Does NOT depression respiration


or cause LOC

 Anesthesia
 Minor surgical & diagnostic
procedures
 Children
Lidocaine
 Local anesthetic  Cross-reactivity w/ amide-type
 Amide-type anesthetics

 Blocks Na channels & nerve


conduction

 Topical
 Infiltration
 Nerve block
 Epidural
 Spinal anesthesia
 Eutectic mixture
 Lidocaine & prilocaine
 Anesthetize intact skin for
venipuncture
 IV cannulation
 Circumcism
Midazolam
 Sedative-hypnotic-anxiolytic  Apnea
 Short-acting BZDP  Laryngospasm
 Respiratory depression
 Cardiac arrest
 Potentiates GABA binding to
GABA-A Cl ion channel
 Sedation
 Hypnosis
 Amnesia

 Preoperative sedation &


anxiolysis
 Sedation of mechanically vented
pts
Nitrous Oxide
 Inhalation general anesthetic
 Anesthetic gas

 Potentiates GABA binding


to GABA-A Cl ion channel
 Suppresses sensory
processing in thalamus

 Minor surgery & dental


procedures

 Rapid induction & recovery


 Euphoria – laughing gas
Propofol
 General anesthesia  Bradycardia
 IV anesthetic  Hypotension
 Diisopropyl phenol

 Potentiates GABA binding


GABA-A Cl ion channel
 Hypnosis
 Anesthesia
 Amnesia

 NO analgesic effect

 Intubation & maintenance of


general anesthesia
 Sedation of intubated pts in ICU
Sevoflurane
 General anesthetic
 Inhalation anesthetic

 Potentiates GABA binding


to GABA-A Cl channel
 Suppresses sensory
processing in thalamus
 Causes LOC

 General anesthesia
Anti-infective
 Acyclovir  Cefepime
 Albendazole  Cetriaxone
 Amantadine  Ciprofloxacin
 Amoxicillin-clavulanate  Clindamycin
 Amphotericin B  Doxycycline
 Azithromycin  Efavirenz
 Aztreonam  Enfuvirtide
 Caspofungin  Erythromycin
 Cefazolin  Ethambutol
 Foscarnet  Linezolid
 Fosfomycin  Mefloquine
 Ganciclovir  Metronidazole
 Gentamicin  Mupirocin
 Griseofulvin  Nafcillin
 Imipenem-cilastatin  Nitrofurantoin
 Isoniazid  Oseltamivir
 Itraconazole  Paromomycin
 Ivermectin  Penicillin G
 Levofloxacin
 Pentamidine  Rifampin
 Piperacillin-tazobactam  Ritonavir-lopinavir
 Praziquantel  Streptomycin
 Primaquine  Terbinafine
 Pyrimethamine  Trifluridine
 Pyrantel  TMP-SMX
 Quinine  Vancomycin
 Quinpristein-dalfopristin  Zidovudine
 Ribavirin
Acyclovir
 Antiviral  Dizziness
 Nucleoside analogue  Diarrhea
 N
 Converted to acyclovir  Nephrotoxicity
triphosphate by viral & host
cell kinases  Probenecid ↑ serum levels
 Incorporated into DNA by
viral DNA polymerase causing
DNA chain termination

 HSV2
 Herpes zoster
• Shingles
• Chickenpox – varicella

 ↓ viral shedding, pain, &


healing time
Albendazole
 Antihelmintic  GI distress
 Benzimidazole  Constipation or diarrhea
 Hepatitis & hematologic toxicity
w/ high doses
 Binds & inhibits polymerization of
tubulin dimmers to form
cytoplasmic microtubules
 Impairs glucose uptake &
deplete glycogen stores

 Intestinal nematode infections


• Hookworm
• Pinworm
• Whipworm
• Ascariasis
• Capillariasis
 Trichinosis
• Use w/ corticosteroid
 Cysticercosis & echinococcus
 Microsporidiosis
Amantadine
 Anti-influenza,  Ataxia
antiparkinson  Dizziness
 Tricyclic amine  Insomnia
 Skin mottling & livedo
reticularis
 Inhibits influenza-A M2
proton channel &  Blurred vision
acidification of virus  Dry mouth
particle
 Prevents viral protein-
protein dissociation &
uncoating of viral
particles

 Influenza A
Amoxicillin-clavulanate
 β-lactam ABX  Diarrhea
 Extended spectrum aminopenicillin  Superinfection
& β-lactamase inhibitor  Pseudomembranous colitis
 Allergic rxn
 Amoxicillin • Rash
• Serum sickness
 Binds PBP
• anaphylaxis
• Inhibits cross-linking of cell
wall peptidoglycan
 Clavulanate  Probenecid inhibits renal tubular
 Inhibits class-A β-lactamase excretion
• ↑ serum levels
• Protects amoxicillin from
destruction
 NOT antimicrobial by itself

 Respiratory tract infections


• Otitis, sinusitis, pneumonia
 Skin or skin structure infections
• Bite wounds
Amphotericin B
 Antifungal  Chills
 Polyene ABX  Fever
 Diarrhea
 N, V
 Binds ergosterol & ↑  Nephrotoxicity
membrane permeability  Hypokalemia
 Leakage of cell contents
 ↑ toxicity w/ cyclosporine,
 Candidiasis antineoplastics
 Cryptococcal meningitis  Thiazides, &
 Aspergillosis corticosteroids ↑
hypokalemia
 Blastomycosis
 Coccidioidomycosis
 Histoplasmosis
 Mucormycosis
Azithromycin
 Macrolide
 Protein synthesis inhibitor

 Binds 50s ribosome


 Prevents peptide elongation &
translocation from acceptor
site to peptidyl site

 Respiratory infections d/t


strep, pneumo, H. influenzae,
Legionella
• Otitis media, sinusitis
 Single-dose Tx for chlamydial
urethritis, chancroid, MAI
infections
Aztreonam
 β-lactam ABX  Thrombophlebitis
 Monobactam  Allergic rxn

 Binds PBP including


transpeptidase
 Inhibits cross-linking of
cell wall peptidoglycan

 Drug resistant gram (-)


infections including
Pseudomonas
aeruginosa &
Enterobacteriaceae
Caspofungin
 Antifungal  HA
 Echinocandin  Fever
 Phlebitis
 Inhibits synthesis of cell  Abnormal LFTs
wall component
 β-1,3-D-glucan

 Candida albicans
 Invasive aspergillosis

 IV admin
• Not absorbed well by
gut
Cefazolin
 β-lactam ABX  Rash
 2nd generation cephalosporin  Diarrhea
 Pseudomembranous colitis
 Binds PBP including  Superinfection
transpeptidase
 Inhibits cross-linking of cell  Probenecid inhibits excretion
wall peptidoglycan & ↑ serum levels

 Surgical wound infections


 Infections d/t
• Staph, strep, E. coli,
Klebsiella pneumoniae,
Proteus mirabilis

 NOT active against MRSA


Cefepime
 β-lactam ABX  Rash
 4th generation  Diarrhea
cephalosporin  Pseudomembranous
colitis
 Superinfection
 Binds multiple PBP
 Inhibits cross-linking of  Probenecid inhibits
cell wall peptidoglycan excretion & ↑ serum levels
 Resistant to many β-
lactamases

 Drug-resistant gram (-)


bacteria
• Citrobacter
• Enterobacter
Ceftazidime
 β-lactam ABX  Rash
 3rd generation cephalosporin  Diarrhea
 Pseudomembranous colitis
 Binds PBP including  Superinfection
transpeptidase
 Inhibits cross-linking of cell  Probenecid inhibits excretion
wall peptidoglycan & ↑ serum levels

 Gram (+), gram (-), &


anaerobics – Pseudomonas
aeruginosa

 Pneumonia, meningitis, UTI,


skin structures, bones, jts
Cetriaxone
 β-lactam ABX  Rash
 3rd generation cephalosporin  Diarrhea
 Pseudomembranous colitis
 Binds PBP including  Superinfection
transpeptidase
 Inhibits cross-linking of cell  Probenecid inhibits excretion
wall peptidoglycan & ↑ serum levels

 Infection d/t
• Pneumococci, gonococci,
meningococci, H. influenzae,
Moraxella catarrhalis,
Borrelia burgdorferi

 Single IM injection Tx acute


otitis media or gonorrhea
Ciprofloxacin
 Antibacterial  Insomnia
 Fluoroquinolone  Diarrhea
 N
 Inhibits bacterial DNA
topoisomerase type II (DNA  Absorption ↓ by cations
gyrase) & type IV • Antacids
 Prevents DNA replication & • Iron
separation of chromosomes • Zinc
• bismuth

 Urinary tract, prostate,


intraabdominal w/ metronidazole,
bone or jt, skin
 Inhalational anthrax
 Gonorrhea
 Infectious diarrhea

 Gram (+), gram (-), Pseudomonas


aeruginosa
Clindamycin
 Aminosugar ABX  C. difficile superinfection
 Protein synthesis inhibitor  Diarrhea
 Pseudomembranous colitis
 Binds 50s ribosome
 Prevents translocation of
nascent peptide from
acceptor site to peptidyl
site

 Strep, staph, gram (+)


 Acne vulgaris
 Anaerobes including
Bacteroides
Doxycycline
 Tetracycline ABX  AVOID
 Protein synthesis inhibitor • Pregnancy & children > 8
y/o
• Outdated preparations are
 Binds 30s ribosome nephrotoxic
 Reversibly inhibits binding of
transfer RNA to acceptor site  Permanent teeth
discoloration
 Rickettsia, Chlamydia,  Photosensitivity
Mycoplasma, Borrelia  Diarrhea
 Acne  N, V
 Cholera
 Gonorrhea & syphilis in
PCN allergic pts
 Brucellosis & ehrlichiosis
Efavirenz
 Antiretroviral  N
 Non-nucleoside reverse  Rash
transcriptase inhibitor  Drowsiness
 Depression
 Binds reverse
transcriptase & disrupts
catalytic site

 HIV in combo w/
nucleoside reverse
transcriptase inhibitor –
synergistic

 High fat meal ↑ absorption


Enfuvirtide

 Antiretroviral  Injection site rxn


 HIV fusion inhibitor • Rotate sites daily

 Binds HIV virus gp41 &


blocks fusion of HIV w/
host cells CD4 Thelper
lymphocytes

 Drug-resistant HIV
Erythromycin
 Macrolide ABX  Activates motilin receptors
 Protein synthesis inhibitor causing uncoordinated
peristalsis
• Anorexia
 Binds 50s ribosome • N, V
 Prevents peptide elongation
& translocation from
acceptor site to peptidyl site

 Pharyngitis, otitis media,


sinusitis, pneumonia d/t
• Strep, pneumococci,
Mycoplasma, Chlamydia,
Legionella, MAI
Ethambutol

 Antitubercular  Dose-related
 Synthetic butanol retrobulbar optic
neuritis
derivative
 Impaired red-green
color discrimination
 Bacteriostatic against • Monitor pts color
mycobacteria discrimination
regularly
 Inhibits RNA synthesis
 Gouty arthritis

 M. tuberculosis
 MAI
Foscarnet
 Antiviral  HA
 Pyrophosphate  Diarrhea
 V
 Renal failure
 Blocks pyrophosphate-  Hypocalcemia
binding site on viral  Hypokalemia
DNA polymerase  Hypomagnesemia
 Prevents attachment of  Anemia
nucleotide precursors to  Arthralgia
DNA
 Myalgia
 CMV retinitis in HIV pts
 Acyclovir-resistant HSV in  Pentamidine causes life-
immunocompromised threatening
hypocalcemia
Fosfomycin
 ABX
 Cell wall synthesis
inhibitor

 Inhibits enopyruvyl
transferase & addition of
phosphenolpyruvate to N-
acetylglucosamine to form
N-acetylmuramic acid

 Cystitis d/t E. coli or


Enterococcus faecalis

 Single dose Tx for UTI


Ganciclovir

 Antiviral  ↓ visual acuity


 Neutropenia
 Nucleoside analogue
 Thrombocytopenia
 Anemia
 Converted to
ganciclovir
triphosphate
 Inhibits viral DNA
polymerase

 CMV infection in
immunocompromised &
transplants
Gentamicin
 Aminoglycoside ABX  Nephrotoxicity
 Protein synthesis inhibitor  Ototoxicity
• Vestibular & cochlear
• ↑ w/ loop diuretics
 Binds 30s ribosome
 Prevents initiation of protein
synthesis
 Misreading of genetic code

 Gram (-) bacilli including


Enterobacteriaceace & P.
aeruginosa
 Strep, enterococcal, & staph
infections

 Monitor serum levels


Griseofulvin
 Antifungal  HA
 Fungistatic ABX
 Induces CYP450
• Reduces plasma
 Deposits in keratin levels warfarin &
precursor cells of skin, OCP
hair, & nails
 Disrupts microtubules
& mitotis of
dermatophytes

 Dermatophyte
infections
 NOT Candida
Imipenem-cilastatin
 β-lactam ABX  Allergic rxns
 Carbapenem ABX &  Diarrhea
dehydropeptidase inhibitor  V
 Seizures
 Imipenem • ↑ risk w/ ganciclovir or
cyclosporine
 Binds PBP & inhibits cross-
linking cell wall
peptidoglycan  Probenecid inhibits secretion
& ↑ serum levels
 Cilastatin
 Inhibits renal
dehydropeptidase &
degradation of imipenem

 Endocarditis, pneumonia,
UTI, pelvic, abdominal d/t
aerobic & anaerobic
Isoniazid
 Antitubercular  Hepatitis
 Nicotinic acid derivative • Toxic metabolite acetyl-
hydrazine
 Peripheral neuropathy
 Reduces catalase- • Vit. B6 deficiency
peroxidase
 Inhibits synthesis of
mycolic acid component
of cell wall

 TB

 Bimodal distribution d/t


fast & slow acetylation
 Inactivates vit. B6
Itraconazole
 Antifunal  GI distress
 Synthetic triazole  Rash
 Hepatitis
 Inhibits 14-α-demethylase
 CYP450 enzyme that
converts lanosterol 
ergosterol

 Blastomycosis,
candidiasis,
coccidioidomycosis,
histoplasmosis
 Onychomycosis – nail
beds
Ivermectin
 Antiparasitic  Vertigo
 Antihelmintic ABX  Sedation

 Activates glutamate-gated
Cl ion channel
 Pharyngeal m.
hyperpolarization &
paralysis

 Strongyloidiasis
 Cutaneous larva migrans
 Onchocerciasis filiariasis
• W. bancrofti
Levofloxacin
 Antibacterial
 Fluoroquinolone

 Inhibits bacterial DNA


topoisomerase type II (DNA
gyrase) & type IV
 Prevents DNA replication &
separation of chromosomes

 Community-acquired
pneumonia
 UTI
 Gynecologic & skin infections

 Gram (+), gram (-), P.


aeruginosa, Mycoplasma,
Mycobacterium
Linezolid

 Antibacterial  Inhibits MAO


 Oxazolidinone protein
synthesis inhibitor

 Binds 23s ribosomal


RNA of 50S subunit
 Prevents formation of
70s initiation complex

 VRE, MS/MRSA, PCN-


sensitive pneumococci
Mefloquine
 Antimalarial  Neuropsychiatric syn
 4-quinolone methanol • Hallucination
derivative • Anxiety
• Confusion
• Seizure
 Inhibits erythrocytic • Coma
schizogony
 Inhibit nucleic acid synthesis

 Malaria
 Chloroquine-
susceptible/resistant trains
of P. falciparum & P. vivax

 Perform CBC during


chronic prophylactic Tx
Metronidazole
 Antiprotozoal  GI pain
 Nitroimidazole  Anorexia
 N
 Reduced by  Dizziness
pyruvate:ferredoxin to
form nitro-free radicals  Alcohol causes
that attack DNA & disulfiram-like effect
proteins

 Amebiasis, giardiasis,
trichomoniasis
 Balantidium coli, C.
difficile, B. fragilis
Mupirocin
 ABX
 Protein synthesis inhibitor

 Competes w/ isoleucine for


binding bacterial isoleucyl
tRNA synthetase
 Prevents addition of
isoleucine during protein
synthesis

 Impetigo by staph or strep


 Eradicate nasal
colonization of MRSA
 Infected traumatic skin
lesions
Nafcillin
 β-lactam ABX  Diarrhea
 Antistaphylococcal,  Superinfection
penicillinase-resistant  Pseudomembranous
colitis
penicillin  Allergic rxn
• Rash
 Binds PBP • Serum sickness
 Inhibits cross-linking of • Anaphylaxis
cell wall peptidoglycan
 Probenecid inhibits renal
 Methicillin-sensitive tubular secretion & ↑
penicillinase producing serum levels
staph
• Bone, jt, UTI,
respiratory, skin,
endocarditis, meningitis
Nitrofurantoin

 Urinary tract  Anorexia


antibacterial  N, V
 Nitrofuran  Neurotoxicity
 Pneumonitis
 Inhibits bacterial
enzymes  Probenecid inhibits
urinary excretion
 UTI
• E. coli, S.
saprophyticus
Oseltamivir

 Antiviral
 Neuraminidase
inhibitor

 Inhibits influenza A &


B neuraminidase
 Prevents release &
spreading of viral
particles

 Influenza A & B
Paromomycin

 Antiprotozoal  Nephrotoxic &


 Aminoglycoside ABX ototoxic if given IV

 Inhibits protein
synthesis

 Intestinal amebiasis
 Cryptosporidiosis in
immunocompromised
pts
Penicillin G
 β-lactam ABX  Diarrhea
 Narrow-spectrum  Superinfection
penicillin  Pseudomembranous
colitis
 Allergic rxn
 Binds PBP
• Rash
 Inhibits cross-linking • Serum sickness
of cell wall
• Anaphylaxis
peptidoglycan

 Probenecid inhibits
 Strep, pneumococcal, renal tubular secretion
meningococcal
 Syphilis
Pentamidine

 Antiprotozoal  Nephrotoxic
 Amidino-pentane  Hematologic toxicity
derivative  Hypoglycemia
 Allergic rxn
• Anaphylaxis
 Disrupts nucleic acid
synthesis in protozoa
 Erythromycin ↑ fatal
arrhythmias
 P. carinii
 Early stage African
trypanosimiasis –
sleeping sickness
Piperacillin-tazobactam
 β-lactam ABX  Diarrhea
 Antipseudomonal penicillin  Superinfection
& β-lactamase inhibitor  Pseudomembranous colitis
 Allergic rxn
• Rash
 Piperacillin • Serum sickness
 Binds PBP • Anaphylaxis
• Inhibits cross-linking of
cell wall peptidoglycan
 Probenecid inhibits renal
 Tazobactam tubular secretion
 Inhibits class A β-lactamases

 Gram (-) bacilli, P. aeruginosa


Praziquantel
 Antihelmintic  Malaise
 Isoquinoline derivative  Anorexia
 Drowsiness
 ↑ Ca permeability of  dizziness
schistosome tegument
 Contraction &
exposing antigens to
host immunity

 Schistosomiasis
 Chinese liver fluke
 Lung fluke
 Cestodes – tapeworms
Primaquine

 Antimalarial  Hemolytic anemia in


 8-aminoquinoline G6PD deficiency
 methemoglobinemia

 Converted to oxidizing
quinoline-quinone
intermediates

 Eradicate exo-
erythrocytic forms of P.
vivax & P. ovale
Pyrimethamine
 Antiprotozoal  N
 Folate reductase inhibitor  Anorexia
 Hypersensitivity rxn
 Inhibits folate reductase
 Folate deficiency in protozoa

 Malaria in combo w/
sulfadoxine
 Toxoplasmosis in combo w/
sulfadoxine

 NOT effective against P.


vivax
Pyrantel
 Antihelmintic  Abdominal cramps
 Pyrimidine analogue  Anorexia
 Diarrhea
 Activates cholinergic  V
nicotinic receptors in
somatic m. of
nematodes
 Produces depolarizing
NM blockade

 Ascariasis
 Hookworm & pinworm
Quinine
 Antimalarial  Abdominal cramps
 4-aminoquinoline  Diarrhea
 V
 Binds plasmodial DNA &
prevents replication &  Cinchonism
transcription during • Tinnitus
erythrocytic schizogony • Blurred vision

 Metabolism
 Chloroquine-resistant • Cimetidine inhibits
malaria
• Rifampin induce

 Admin w/ doxycycline or
pyrimethamine-
sulfadoxine
Quinupristin-dalfopristin
 Streptogramin ABX  Infusion site rxn
 Protein synthesis inhibitor

 Binds 50s ribosomal


subunit
 Quinupristin
 Inhibits aminoacyl tRNA
synthesis & addition of
AA
 Dalfopristin
 Inhibits peptidyl
transferase

 VRE, MS/MRSA
Ribavirin
 Broad-spectrum antiviral  Anemia
 Guanosine analogue  Hypotension
 Cardiac arrest
 Converted to ribavirin
triphosphate
 Depletes guanosine
triphosphate
 Inhibits viral RNA &
protein synthesis

 RSV in infants or children


 Chronic hepatitis C
 Viral hemorrhagic fever –
Lass fever
Rifampin
 Antitubercular  Red discoloration of tears,
 Rifampin derivative urine, saliva, sweat
 Abdominal pain
 V
 Inhibits DNA-dependent RNA
polymerase  Diarrhea
 Hepatitis
 TB
 Leprosy  Induces CYP450
 Prophylaxis meningococcal  ↓ levels
meningitis & H. flu B • Warfarin
infections • Theophylline
• Itraconazole
• Steroids
• Opioids
• Phenytoin
• Verapamil
Ritonavir-lopinavir
 Antiretroviral  Anorexia
 HIV protease inhibitor  V
 Altered taste
 Inhibits HIV protease  Abnormal thinking
& conversion of gag-pol  Hyperlipidemia
polyprotein to  Hyperlgycemia
functional proteins
 Ritonavir
 ↑ lopinavir levels

 HIV in combo w/
nucleoside reverse
transcriptase inhibitor
Streptomycin
 Aminoglycoside  Nephrotoxic
 Protein synthesis inhibitor  Ototoxic
• ↑ w/ loop diuretics

 Binds 30s ribosome


 Prevents initiation of
protein synthesis
 Misreading of genetic
code

 Drug-resistant TB
 Plague
 Tularemia

 IV admin
Terbinafine
 Antifungal  Itching
 Allylamine  Rash
 Diarrhea
 Inhibits squalene  Anorexia
oxygenase & formation of
squalene epoxide during  Metabolism
fungal membrane • Cimetidine inhibits
ergosterol synthesis • Rifampin induce

 Topical
• Tinea corporis, cruris,
pedis, versicolor
 Oral
• Onychomycosis – fungal
nail infection
Trifluridine

 Antiviral  Ocular irritation


 Thymidine analogue • Redness
• Itching

 Inhibits HSV DNA


polymerase

 Herpetic keratitis
 Keratoconjunctivitis

 Topical ocular admin


Trimethoprim-
sulfamethoxazole
 Antibacterial  N, V
 Folate antagonist  Rash
 Stevens-Johnson syn
 Allergic rxn
 Sulfamethoxazole  Anemia
 Inhibits folate synthesis • Hemolytic anemia
 Trimethoprim • Megalobalstic anemia
 Inhibits folate reduction  Leukopenia
 Thrombocytopenia
 UTI, traveler’s diarrhea  Crystalluria
 Shigella enteritis
 P. carinii & Nocardia  Added folate deficiency w/
pneumonia phenytoin or MTX
Vancomycin
 Glycopeptide ABX  Red man syn
 Cell wall synthesis • Extensive rate of
infusion
inhibitor
• Erythematous rash on
face & upper body
 Binds D-alanyl-D-alanine  Ototoxicity
portion of peptidoglycan • Vestibular & cochlear
 Prevents cross-linking of
D-alanine & pentaglycine
chain

 MRSA, penicillin-resistant
enterococci, C. difficile
Zidovudine
 Antiretroviral  Anemia
 Nucleoside reverse
transcriptase inhibitor

 Activated nucleotide
triphosphate incorporated into
DNA causing chain
termination

 HIV
 Prevent maternal-fetal HIV
transmission

 1st line Tx for HIV infections


• Zidovudine w/ lamivudine
or emtricitabine &
efavirenz or lapinavir-
ritonavir
Antineoplastic
 Anastrozole  Imatinib
 Bleomycin  Leuprolide
 Busulfan  Meraptopurine
 Carmustine  Methotrexate
 Cisplatin  Paclitaxel
 Cyclophosphamide  Tamoxifen
 Doxorubicin  Trastuzumab
 Etoposide  Vincristine
 Fluorouracil
 Gemtuzumab ozogamicin
Anastrozole
 Estrogen antagonist  N
 Nonsteroidal aromatase  HA
inhibitor  Hot flashes
 Back pain
 Inhibits aromatase &
conversion to estrone
precursor to estradiol
 Lowers estrogen levels
 Halts progression of
estrogen-sensitive breast
cancers

 Breast cancer in
postmenopausal women
Bleomycin
 Antitumor  Pneumonitis & pulmonary
 DNA intercalating fibrosis
 Hyperpigmentation
 Mucocutaneous toxicity
 Complexes iron-forming
 Hematology toxicity
oxygen free radicals that
cause single strand breaks
 G2 phase specific

 Lymphomas
 SCC
 Testicular carcinoma
 Choriocarcinoma
Busulfan
 Antineoplastic  N, V
 Alkyl sulfonate bifunctional  Myelosuppression
alkylating agent  Pulmonary fibrosis

 Cross-links DNA strands by


covalently bonding guanine
residues
 Prevents DNA replication &
transcription

 CML

 Use w/ cyclophosphamide prior


allogenic hematopoietic
progenitor cell transplant for
CML
Carmustine
 Antineoplastic  N, V
 Nitrosurea bifunctional  Hepatotoxicity
akylating agent  Anemia
 Leucopenia
 Cross-links DNA strands by  Thrombocytopenia
covalently bonding guanine  Pulmonary fibrosis
residues
 Prevents DNA replication &
transcription

 Brain tumors
 Myeloma
 Lymphoma

 Causes prolonged
myelosuppression
Cisplatin
 Antineoplastic  Severe N, V
 Platinum compound  Ototoxicity & tinnitus
 Hypocalcemia
 Forms reactive metabolites  Hypokalemia
that covalently bond DNA  Hypomagnesemia
bases & cross-link DNA  Anemia
strands

 Testicular, ovarian, cervical,


bladder, lung, head/neck
cancers

 Less bone marrow suppression


Cyclophosphamide
 Antineoplastic  Anorexia
 Nitrogen mustard bifunctional  N, V
akylating agent  Hemorrhagic cystitis & hematuria
 Alopecia
 Thrombocytopenia
 Cross-links DNA strands by  Leukopenia
covalently bonding guanine residues  Anemia
 Prevents DNA replication &
transcription  Rifampin induces CYP & ↑ toxicity

 Hodgkin’s ds
 Lymphomas, myeloma
 Leukemia
 Ovarian & breast tumors
 RA

 Converted to active metabolites by CYP


enzymes
Doxorubicin
 Antitumor  Colors urine red
 DNA intercalating agent
 Cardiomyopathy – dose-limiting
 Inserts b/w DNA bases  Anemia
 Causes deformation & uncoupling  Leukopenia
 Complexes iron forming hydroxyl  Thrombocytopenia
free radicals that cause strand  Diarrhea
breaks  V
 Inhibits topoisomerase II  Stomatitis
 Causes strand breaks  Alopecia
 S phase specific

 Breast, ovarian, bladder tumors


 Bronchogenic carcinoma
 Lymphoma & leukemia
Etoposide
 Antineoplastic  N, V
 Podophyllotoxin,  Leukopenia
topoisomerase inhibitor  Thrombocytopenia
 Alopecia
 Inhibits mammalian
topoisomerase II & prevents
resealing of nicked DNA
strands
 G2 phase specific

 Testicular, small cell lung


carcinoma
 Lymphoma
 Leukemia
Fluorouracil
 Antineoplastic  Diarrhea
 Pyrimidine antimetabolite  V
 Stomatitis
 Converted to active  Alopecia
nucleotide form  Maculopapular rash
 Inhibits thymidylate  Anemia
synthetase  Leukopenia
 S phase specific  Thrombocytopenia

 Colon, breast, rectal, gastric,


pancreatic cancer
 Topical for basal cell
carcinoma & actinic keratosis
Gemtuzumab ozogamicin
 Antineoplastic  Severe myelosuppression &
 Monoclonal Ab & cytotoxic hypersensitivity rxn
 anaphylaxis
ABX calicheamicin
 Severe pulmonary rxns
 Chills
 Gemtuzumab
 Fever
 Binds CD33 Ag on
 N
hematopoietic cells & sequesters
lysosomes where calicheamicin  Dyspnea
is released
 Calicheamicin
 Causes DNA dbl strand breaks

 CD33 (+) AML


Imatinib
 Antineoplastic  Cough
 Tyrosine kinase inhibitor  Dyspnea
 Pharyngitis
 Inhibits oncoprotein bcr-abl  Pneumonia
tyrosine kinase expressed by  Abdominal pain
Philadelphia chromosome  V
 Inhibits leukemic cell  Petechiae
proliferation & induced  Pruritis
apoptosis  Rash
 Night sweats
 CML  Myalgia
 Cause hematologic &  Arthralgia
cytogenetic remission  Thrombocytopenia
 Neutropenia
Leuprolide
 Antineoplastic, agent for precocious  Transient ↑ in testosterone w/ 1st dose
puberty  Use flutamide or other androgen
antagonist
 GnRH analogue
 Hot flashes

 Pulsatile admin ↑ FSH & LH release


 Continuous admin down-regulates
GnRH receptors & ↓ FSH & LH

 Central precocious puberty


 Advanced prostate cancer
 Endometriosis
 Uterine fibroids

 IM depot & implants for prostate cancer


Mercaptopurine
 Antineoplastic  Cross-react w/ thioguanine
 Purine antimetabolite
 Myelosuppression
 Hyperuricemia
 Converted to nucleotide triphosphate  Hepatotoxicity
by phosphoribosyl transferase
 Inhibits purine biosynthesis &  Allopurinol inhibits degradation
salvage pathways
 S phase specific

 Acute leukemia
 CML
 Lymphomas

 Tumors that delete phosphoribosyl-


transferase acquire resistance
Methotrexate
 Antineoplastic  N, V
 Folate reductase inhibitor  Stomatitis
 Hepatotoxicity
 Anemia
 Inhibits dihydrofolate reductase  Leukopenia
 Prevents formation of active folate &  Thrombocytopenia
addition of single carbon units to  Nephropathy
DNA base precursors
 S phase specific

 Choriocarcinoma, trophoblastic tumors


 Leukemia
 Breast, head, neck, lung cancers
 Severe psoriasis
 RA
 Mycosis fungoides

 Leucovorin used to minimized


hematologic toxicity & Tx OD
Paclitaxel
 Antineoplastic  D
 Mitotic inhibitor  N, V
 Alopecia
 Binds tubulin & prevents  Anemia
depolymerization of  Leukopenia
microtubules of mitotic  Thrombocytopenia
spindle  Peripheral neuropathy
 M phase specific  Arthralgia
 Myalgia
 Advanced ovarian cancer w/
cisplatin
 Non-small-cell lung cancer
 Metastatic ovarian or breast
cancer
Tamoxifen
 Antineoplastic  CI during pregnancy &
 Estrogen receptor antagonist lactation
& partial agonist
 N
 Hot flashes
 Competes w/ estrogen for
receptors in breast & other  Menstrual irregularities
tissues
 Suppresses breast tumor
growth

 Breast cancer & ductal


carcinoma following surgery
& radiation
 Advanced breast cancer
Trastuzumab
 Antineoplastic  Abdominal pain
 Monoclonal Ab  Anorexia
 Diarrhea
 Binds human epidermal growth  V
factor-2 (HER2) receptor on  Back pain
breast cancer cells  Chills
 Prevents receptor stim. & cell  Fever
proliferation  Allergic rxns
 Regression of breast cancer
metastases  Doxorubicin ↑ risk of
cardiotoxicity
 Metastatic breast cancer w/
overexpression HER2

 Combined w/ paclitaxel
 ↑ blood levels
Vincristine
 Antineoplastic  N, V
 Vinca alkaloid, mitotic inhibitor  Alopecia
 Peripheral neuropathy
 Binds tubulin & prevents
polymerization of tubulin
dimers forming microtubules of
mitotic spindle
 M phase specific

 Hodgkin’s ds
 Lymphoma
 Leukemia
 Neuroblastoma
 Rhabdomyosarcoma
 Wilm’s tumor
Autonomic & Neuromuscular
 Atenolol  Pralidoxime
 Atropine  Propranolol
 Dobutamine  Pseudoephrine
 Edrophonium  Pyridostigmine
 Epinephrine  Rocuronium
 Phenoxybenzamine  Sildenafil
 Phentolamine  Succinylcholine
 Phenylephrine  Tamsulosin
 Pilocarpine  Terazosin
Atenolol

 Sympatholytic, Bronchoconstriction w/
antihypertensive high doses b/c β1
blockade
 Β1 receptor antagonist
Additive hypotension w/
 β1 receptor antagonist nitrates

Angina
Post MI
Hypertension
Atropine
 Anticholinergic  Mydriasis & cycloplegia
 Muscarinic receptor  Warm, dry, flushed skin
antagonist  Tachycardia
 Delirium
 Hallucinations
 Muscarinic receptor
blocker

 Bradycardia
 IBS
 Anticholinesterase poisoning
 Antisecretory agent
Dobutamine
 Sympathomimetic, cardiac  Tachycardia
stimulant  Arrhythmia
 β1 receptor agonist

 Selective β1 receptor agonist


 β1 > β2 > α1

 Cardiac contractility & output


 Acute heart failure
 Cardiogenic shock

 Synergistic on cardiac output w/


nitroprusside
Edrophonium

 Diagnostic agent Muscarinic effects


 Miosis
 Cholinesterase
 Salivation
inhibitor

 Reversible
cholinesterase
inhibitor

Dx myasthenia gravis


Epinephrine
 Sympathomimetic,  HTN
bronchodilator, vasopressor  Tachycardia
 Nonselective adrenergic agonist  Ischemia
 Hyperglycemia
 Activates α & β receptors
 ↑ IP3 & cAMP
 α1 – vasoconstrict & ↑ BP
 β1 – ↑ HR, conduction, &
contractility
 β2 – vasodilate, ↓ BP,
bronchodilate

 Cardiac arrest, V fib


 Shock, asthma
 COPD
Phenoxybenzamine

 Vasodilator Postural hypotension

 Irreversible α receptor
Hypotension w/ β
antagonist blockers & Ca channel
blockers
 α receptor antagonist
α1 > α2

 Presurgical Tx of HTN d/t


pheochromocytoma
Phentolamine
 Vasodilator  Hypotension

 α receptor antagonist  Severe hypotension w/ Epi

 Blocks α1 & α2
receptors

Control BP during
surgical removal of
pheochromocytoma

IV admin only


Phenylephrine
 Vasocontrictor, decongestant  Rebound nasal congestion
 Selective α1 receptor agonist  HTN

 MAOI cause severe HTN


 Activates α1 receptor
 Increase IP3 causing
contraction of vascular smooth
m.

 Nasal & ocular decongestant


 Dilate pupil for opthalmoscopy
 Mydriasis w/o cycloplegia
 Paralysis of accommodation
Pilocarpine
 Antiglaucoma, sialogogue  Miosis
 Muscarinic receptor  Blurred vision
agonist  Accommodative spasm

 Activates muscarinic
receptors in ciliary m. &
salivary gland

 Sjogren’s syn
 Glaucoma
• Ciliary m. ↑ aqueous
humor
 Xerostomia
• Salivary gland ↑ salivation
Pralidoxime
 Organophosphate antidote
 Cholinesterase reactivator

 Binds phosphorous &


breaks organophosphate
bond w/ cholinesterase

 Organophosphate toxicity
 Reverses muscle weakness
Propranolol
 Sympatholytic, antihypertensive  Bronchoconstriction
 Nonselective β receptor  Inhibits glycogenolysis
antagonist  Nightmares & depression

 Blocks β1 & β2 receptors

 Angina
 HTN
 Benign tremor
 Migraine prophylaxis
 thyrotoxicosis
 Post-MI

 Highly lipophilic  CNS effects


Pseudoephedrine
 Decongestant  Tachycardia
 Indirect/direct-acting  CNS stim.
adrenergic receptor  ↑ BP
agonist
 MAOI cause severe HTN
 ↑ release NE directly
activates adrenergic
receptors causing
vasoconstriction & cardiac
stim.

 Allergic & viral rhinitis


Pyridostigmine
 Antimyasthenic  Muscarinic effects
 Miosis
 Cholinesterase inhibitor,
 Salivation
cholinergic agonist
 Prolongs effects of
 Reversibly inhibits succinylcholine
cholinesterase

 Tx myasthenia gravis
 Reverse nondepolarizing
NM blockers
Rocuronium
 Paralytic agent  Respiratory m. paralysis
 Nondepolarizing NM  Apnea
blockade

 Blocks nicotinic receptors in


skeletal m.

 Skeletal m. relaxation for


intubation, surgery, ECT

 Effects reversed by
neostigmine & edrophonium
Sildenafil
 Vasodilator  HA
 Phosphodiesterase  Nasal congestion
inhibitor  Back pain
 Visual disturbances
 Inhibits type 5
phosphodiesterase &
degradation of cGMP
 vasodilation in corpus
cavernosum d/t Ach
release from sacral PNS
neurons

 Erectile dysfunction
Succinylcholine
 Paralytic agent  Respiratory m. paralysis
 Depolarizing NM blockade  Apnea

 Binds nicotinic receptors


causing prolonged
depolarization of skeletal
m. & paralysis

 Skeletal m. relaxation for


intubation & surgery

 Transient m. fasciculations
Tamsulosin

 Urologic agent Dizziness


HA
 Uroselective α1
Postural hypotension
receptor antagonist
Cimetidine increases
 Blocks α1A receptors blood levels & effects
in prostate

Tx urinary outflow


obstruction d/t prostatic
hyperplasia
Terazosin
 Antihypertensive, 1st dose syncope
urologic agent
 Selective α1 receptor
antagonist

 Blocks α1 receptors

HTN
Outflow obstruction d/t
prostate hyperplasia
Cardiovascular
 Acetazolamide Hydrochlorothiazide
 Adenosine  Labetalol
 Amiloride  Mannitol
 Amiodarone  Methyldopa
 Amlodipine  Minoxidil
 Carvedilol  Nesiritide
 Clonidine  Nitroglycerin
 Digoxin  Nitroprusside
 Diltiazem  Propafenone
 Dofetilide  Quinidine
 Enalapril  Sotalol
 Esmolol  Spironolactone
 Fenoldopam  Valsartan
 Furosemide  verapamil
 Hydralazine
Acetazolamide
 Diuretic – Parasthesia
 Carbonic anhydrase inhibitor – Urinary stone formation
 Inhibits interconversion of
carbonic acid & bicarbonate
 ↑ NaHCO3 excretion
 Inhibit aqueous humor
formation
 Hyperchloremic metabolic
acidosis

– Tx open-angle glaucoma
– Mtn sickness
– Metabolic alkalosis
Adenosine

 Antiarrhythmic – Transient asystole


 Purine nucleoside, cardiac
node membrane stabilizer

 Opens K channels & blocks


Ca influx in SA & AV nodes
 Slows AV conduction
 ↑ AV refractory period

– Terminate SVT
Amiloride

 K-sparring diuretic – Hyperkalemia


 Epithelial Na channel blocker

 Blocks Na Channel distal


tubule & collecting duct
– Inhibits Na reabsorption &
K excretion

– Prevent & Tx hypokalemia


Amidarone

 Antiarrhythmic – Hypo/hyperthyroidism
 Cardiac ion channel blocker – Photosensitivity
– Blue-gray skin
– Corneal microdeposits
 Blocks K, Na, Ca channels &
β receptors – Pulmonary fibrosis
– Prolongs repolarization
– ↑ refractory period
– Slows HR
– ↑ PR & QT intervals

– SVT, VT, VF
Amlodipine

 Antihypertensive, antianginal – HA
 Dihydropyridine Ca channel – Edema
blocker – Hypotension

 Ca channel blocker in – Effects ↑ w/ grapefruit juice


vascular smooth m.
– Arteriolar vasodilation & ↑
coronary blood flow

– HTN
– Angina pectoris
Carvedilol

 Antihypertensive & heart – Orthostatic hypotension


failure Tx – Dizziness
 Nonselective adrenergic – Bradycardia
receptor agonist

 Blocks β1, β2, α1 receptors


– Cause vasodilation

– HTN
– Heart failure
 ↓ remodeling
Clonidine

 Antihypertensive – Abrupt w/drawal  severe


 α2 receptor agonist rebound HTN
– Sedation
– Dry mouth
 Central α2 receptor agonist
– ↓ sympathetic outflow from
vasomotor center
– Inhibits pain
neurotransmission in spinal
cord

– HTN
– Opioid w/drawal
Digoxin

 Cardiac stimulant – Arrhythmias


 Digitalis glycoside – N, V
– Blurred vision
 Inhibits Na/K ATPase – Yellow vision
– ↑ IC Ca & cardiac
contractility
– ↓ AV conduction
– ↑ AV refractory period

– Heart failure
– Serum levels assess dosage &
toxicity
Diltiazem
 Vasodilator, antiarrhythmic – Dizziness
 Non-dihydropyridine Ca – Hypotension
channel blocker – Peripheral edema
– Constipation
 Block Ca channels in cardiac – Gingival hyperplasia
tissue & vascular smooth m.
– Vasodilation
– Grapefruit juice ↑ serum levels
– ↓ HR & conduction
– ↓ contractility

– HTN
– Angina pectoris
– SVT
Dofetilide
 Antiarrhythmic – QT prolongation
 K channel blocker – Torsade de pointes

 Blocks delayed K channels in


cardiac tissue
– Slows repolarization &
prolongs refractory period
– ↑ QT interval

– AF, A flutter

– Monitor QT interval during


initial dose titration
Enalapril
 Antihypertensive – Cough & angioedema
 ACE inhibitor  Inhibits bradykinin
degradation
 Inhibits ACE & formation of AT II
– Hypotension
– Vasodilation
– ↓ aldosterone secretion – Taste disturbances
– ↑ CO
– ↓ V remodeling
– ↑ survival in heart failure

– HTN
– Heart failure
– Post-MI
– ↓ progression of diabetic nephropathy
Esmolol
 Antiarrhythmic – Hypotension
 Class II
 Selective β1 blocker – Bradycardia

 Blocks SNS stim. SA & AV nodes


– ↓ HR
– ↓ AV conduction
– ↑ AV refractory period

– Sinus tachycardia & SVT during/after


surgery

– Rapidly metabolized by plasma


esterase
Fenoldopam

 Antihypertensive – ↓ serum K levels


 Monitor for hypokalemia
 D1-like receptor agonist

 D1 receptor agonist
– Arteriolar vasodilation
 Afferent & efferent renal
arterioles
– ↑ renal blood flow

– Hypertensive emergencies
Furosemide
 Loop-acting diuretic – Hypokalemia
 Membrane ion transport inhibitor – Metabolic alkalosis
– Hyperuricemia
 Inhibits Na/K/2Cl cotransporter in – Hypomagnesemia
ascending loop of Henle
– Blocks NaCl reabsorption – ↑ ototoxicity of aminoglycoside
ABX
– Edema
– Heart failure
– HTN
– Hypercalcemia

– ↑ Ca excretion
– ↑ Na/K exchange in collecting duct
Hydralazine
 Antihypertensive. heart failure – Edema
 Vasodilator – Reflex tachycardia & MI
– Lupus syndrome
 Alters IC Ca metabolism
– Relaxes arteriolar smooth m.
 vasodilation
– ↓ afterload

– Heart failure in combo w/


isosorbide dinitrate
 More effective than ACEI in
black people
– Moderate-severe HTN
Hydrochlorothiazide

 Antihypertensive – Hypokalemia
 Thiazide diuretic – Metabolic alkalosis
– Hyperuricemia & gout
 Inhibits NaCl transporter in
distal tubule – ↓ excretion of lithium
– ↑ excretion Na, K, Cl
– ↓ Ca excretion

– HTN
– Nephrogenic DI
– Nephrolithiasis
Labetolol

 Antihypertensive – Postural hypotension


 Adrenergic α & β – Abrupt w/drawal cause
life-threatening HTN,
receptor antagonist arrhythmias, or MI

 Selective α1 &
nonselective β1, β2
blockers

– HTN
Mannitol

 Diuretic – Electrolyte imbalances


 Osmotic Diuretic – Transient volume expansion
 Pulmonary edema or heart
failure
 Osmotic attraction of
edematous & ocular fluid
 Filtered by glomerulus
– ↑ electrolyte excretion

– Oliguric renal failure


– Cerebral edema – ↑ ICP
– Acute glaucoma
Methyldopa
 Antihypertensive – Positive direct Coomb’s test
 Adrenergic α2 receptor
agonist

 Converted to active form


methyl-norepinephrine which
activates central α2 receptor
agonist
– ↓ SNS outflow from
vasomotor center

– HTN
– HTN in pregnancy
Minoxidil
 Antihypertensive, hair growth – Systemic admin.
stimulant  Reflex tachycardia
 Vasodilator, K channel opener  Angina pericarditis
 Pulmonary HTN
 Opens K channels in vascular  hypertrichosis
smooth m.
– Hyperpolarization
– m. relaxation
– vasodilation
 Stim. resting hair follicle 
growth follicles

– Severe HTN
– Topical for alopecia
Nesiritide
 Heart failure Tx – Hypotension
 Recombinant human B-type
natriuretic peptide

 Activate guanylate cyclase 


↑ cGaMP
– Dilates venous & arterial
smooth m.
– ↓ venous pressure, cardiac
preload, vascular congestion,
& dyspnea

– Decompensated heart failure


Nitroglycerin
 Antianginal – HA
 Organic nitrate – Hypotension
– Syncope
– Reflex tachycardia
 Releases NO in vascular
smooth m.
– Vasodilation – ↑ vasodilative effect of
– ↑ coronary blood flow sildenafil, tadalafil, vardenafil
– ↓ myocardial O2 demand

– Angina pectoris
 Sublingual or lingual admin.
 Short half-life
Nitroprusside
 Antihypertensive – CN toxicity
 Vasodilator – Hypotension
– HA
 Relaxes venous & arteriolar
smooth m.
– Metabolized to CN & thiocyanate
 Tx toxicity w/ sodium nitrite &
sodium thiosulfate

– HTN crisis
– Acute heart failure or cardiogenic
shock
– Controlled hypotension during
pregnancy
Propafenone

 Antiarrhythmic – Proarrhythmic 1st 2 wks


 Class IC Na channel blocker  Monitor ECG when starting
Tx
– GI disturbances
 Blocks Na channel in cardiac
tissue – ↑ digoxin levels
– ↓ conduction & prevent re-
entry
– ↑ PR, QRS, & QT duration

– SVT & life-threatening V


arrhythmias
Quinidine

 Antiarrhythmic – Cinchonism
 Class IA Na channel blocker  Blurred vision
 Tinnitus
 Photophobia
 Blocks Na & K channels in
cardiac tissue – ↑ levels w/
– ↓ conduction  Amiodarone
– ↑ QRS & QT duration  Cimetidine
 Diltiazem
– SVT & VT  Verapamil
 Grapefruit juice
– D-isomer = quinine, used to
treat malaria pts
Sotalol

 Antiarrhythmic – Torsades de pointes


 Class III K channel blocker

 Blocks K channels in cardiac


tissue
– Prolongs repol.
– ↑ refractory period & ↑ QT
interval
 Blocks adrenergic β receptors

– SVT & life-threatening


arrhythmias
Spironolactone

 K-sparring diuretic – Gynecomastia


 Aldosterone antagonist – Impotence
– Hyperkalemia
 Blocks aldosterone receptors
– ↑ Na excretion
– ↓ K excretion

– Primary hyperaldosteronism
– HTN
– hypokalemia
Valsartan
 Antihypertensive
 Angiotensin receptor antagonist

 Blocks AT II receptor in
vascular smooth m. & adrenal
cortex
– Vasodilation & ↓ aldosterone
secretion

– HTN
– Nephropathy

– Less cough & angioedema than


ACEI
Verapamil
 Antihypertensive, antianginal – Peripheral edema
 Non-dihydropyridine Ca channel – Constipation
blocker
– Gingival hyperplasia
 Blocks Ca channels in cardiac m. &
vascular smooth m.
– Vasodilation
– ↓ HR & conduction
– ↓ contractility
 Suppress contractility more than
other Ca channel blockers

– HTN
– Angina pectoris
– SVT
– Prevent migraine HA
CNS Depressants
• Buspirone • Lorazepam
• Carbamazepine • Phenobarbital
• Diazepam • Phenytoin
• Disulfiram • Topiramate
• Ethosuximide • Valproate
• Flumazeil • Zolpidem
• Gabapentin
• Lamotrigine
Busprione
• Antianxiety – Dizziness
• 5-HT1A partial agonist – Drowsiness
– Fatigue
– HA
• Activates presynaptic 5-HT1A
receptors in dorsal raphe nucleus – Excitement
– ↓ firing serotonergic neurons – Nervousness
– Blurred vision
– Generalized anxiety disorder – Tachycardia
– N
– NO – Rash
• Drug dependence – Myalgia
• Significant sedation – Sweating
• Muscle relaxation
• Anticonvulsant effects – ↑ levels by
• Erythromycin
• Itraconazole
• Grapefruit juice
Carbamazepine
• Anticonvulsant – Ataxia
• Neuronal Na channel blocker – Drowsiness
– Blurred vision
• Blocks Na channels in CNS – Agranulocytosis
– Aplastic anemia
– ↓ firing of ectopic foci & spread
of epileptic seizures – Thrombocytopenia

– Partial seizures & generalized – Induces its own metabolism


tonic-clonic seizures
– Bipolar disorders
– Trigeminal neuralgia
– Neuropathic pain
Diazepam
• Antianxiety – Drowsiness
• Benzodiazepine – Lethargy
– Physical/psychological dependence
– Tolerance
• Binds ω receptors on GABA
operated Cl ion channel
– ↑ channel affinity for GABA &
frequency of channel opening
– Potentiates inhibitory effects of
GABA

– Anxiety
– Status epilepticus
– Muscle spasm
– Alcohol w/drawal
– Anterograde amnesia

– Long-lasting active metabolites


Disulfiram
• Alcohol abuse Tx – Drowsiness
• Acetaldehyde dehydrogenase
inhibitor

• Inhibits acetaldehyde degradation


following alcohol ingestion
– Blurred vision
– Chest pain
– Dizziness
– Palpitations
– N, V
– HA
– Weakness

– Reinforcement of alcohol abstinence


Ethosuximide
• Anticonvulsant – Dizziness
• Succimide – Drowsiness
– Gastric distress
– N
• Binds T-type Ca channels
in thalamic neurons
– Suppresses nerve
transmissions to motor
cortex

– Generalized absence seizures


• Petit mal epilepsy
Flumazenil
• Antidote – Seizures
• Benzodiazepine receptor – Dizziness
antagonist – Emotional lability

• Blocks benzodiazepine
receptors

– Counteract adverse effects of


benzodiazepines
• Respiratory depression d/t IV
OD

– CI in status epilepticus
Gabapentin
• Anticonvulsant – Ataxia
• GABA analogue – Dizziness
– Drowsiness
– Nystagmus
• ↑ GABA release from – Tremor
central neurons
– Inhibits neuronal discharges
from seizure foci
– Inhibits pain
neurotransmission

– Partial seizures
– Chronic pain
– Migraine prophylaxis
Lamotrigine
• Anticonvulsant – Skin rash in 1st 8 wk of Tx
• Can progress to Stevens-
• Phenyltriazine Johnson syn

– Ataxia
• Blocks voltage-sensitive
– Dizziness
Na channels – Drowsiness
– Release of glutamate – Photosensitivity
– Prevents spread of seizure foci
discharges – ↓ metabolism & ↑ ADR w/
valproate
– Adjunct/monotherapy for
partial seizures in adults
Lorazepam
• Sedative-hypnotic, anxiolytic – Dizziness
– Drowsiness
• Benzodiazepine – Apnea & cardiac arrest w/ rapid IV
admin
• Binds benzodiazepine ω receptors
on GABA operate Cl ion channel – Additive depression w/ alcohol & other
depressants
– ↑ channel affinity for GABA &
frequency of channel opening
– Potentiates inhibitory effects of
GABA

– Anxiety
– Insomnia
– Preoperative sedation
– Light anesthesia
– Anterograde amnesia

– Flumazenil used to counteract severe


OD
Phenobarbital
• Sedative-hypnotic, anticonvulsant – Drowsiness
• Barbiturate – Lethargy
– Delirium
– Hangover
• Binds GABA operated Cl ion – Physical & psychological dependence
channel increasing duration of
channel opening – Induces CYP P450 ↑ metabolism of
– ↑ Cl influx in absence of GABA drugs

– Tonic-clonic & partial seizures


– Febrile seizures in children
– Preoperative sedation
– Short-term hypnotic

– ↑ folate requirement during long-


term Tx
Phenytoin
• Anticonvulsant – Ataxia
• Hydantoin – Diplopia
– Nystagmus
– Gingival hyperplasia
• Blocks voltage-sensitive Na
channels
– Release glutamate
– Prevents spread of seizure foci
discharges

– Partial seizures
– Generalized tonic-clone seizures
– Status epilepticus following IV
diazepam

– Zero-order @ high doses


– Fosphenytoin for IV use
Topiramate
• Anticonvulsant – Ataxia
• Monosaccharide derivative – Dizziness
– Drowsiness
• Block voltage-sensitive Na – Fatigue
channels – Impaired concentration &
memory
– Augments GABA activation of
GABA receptors – Psychomotor slowing
• Blocks glutamate receptors – Speech problems
– Diplopia
– Partial & tonic-clonic seizures – Nystagmus

– Decrease dose in pts w/ renal


impairment
Valproate
• Anticonvulsant – Indigestion
• Branched-chain FA – N, V
– Dizziness
• ↑ GABA levels by ↑ release or ↓ – Sedation
metabolism or reuptake – Hepatotoxicity
– Reduced Na dependent action
potentials

– Simple & complex absence


seizures
– Complex partial seizures
– Tonic-clonic seizures
– Myoclonic seizures
– Migraine prevention
– Manic phase of bipolar
Zolpidem
• Non-benzodiazepine hypnotic
• Imidazopyridine

• Activates ω BZBP receptors on


GABA operated Cl ion channel
– ↑ channel affinity for GABA &
frequency of channel opening
• Neuronal hyperpolarization

– Insomnia
Endocrine
 Acarbose  Insulin
 Alendronate  Levothyroxine
 Calcitonin  Medroxyprogesterone
 Danazol  Metformin
 Desmopressin  Methimazole
 Ergocalciferol  Mifepristone
 Ethinyl estradiol & drospirenone  Octreotide
 Ethinyl estradiol & norethindrone  Oxytocin
 Finasteride  Pioglitazone
 Fludrocortisone  Prednisone
 Glyburide  Raloxifene
 Hydrocortisone  Repaglinide
 Somatropin
 Testosterone
Acarbose
 Antidiabetic  Intestinal bloating
 α-glucosidase inhibitor  Flatulence

 ↑ oral bioavailability of
 Inhibits intestinal enzyme that
metformin
converts oligosaccharides &
 ↓ iron absorption
disaccharides to glucose
 ↓ digestion of starch & sucrose
 ↓ postprandial blood glucose &
HbA1c

 Type II DM
Alendronate
 Bone resorption inhibitor  Absorption ↓ by Ca supplements,
 Bisphosphonate antacids, foods, beverages
(except water)

 Prevents attachment of
osteoclast precursor cells to
bone
 ↓ metabolic activity of
osteoclasts & ability to resorb
bone

 Prevent/Tx
 Osteoporosis
 Corticosteroid-induced
osteoporosis
 Paget’s ds of bone
 hypercalcemia
Calcitonin
 Ca hormone
 Thyroid gland hormone

 Binds calcitonin receptor on


osteoclasts
 ↑ cAMP & inhibits osteoclast
activity
 ↓ bone resorption, bone pain, &
serum [Ca]

 Postmenopausal osteoporosis
 Paget’s ds of bone
 hypercalcemia
Danazol
 Ovarian inhibitor  CI in pregnancy – androgenic
 Synthetic androgen, effects on female fetus
antiestrogen
 Emotional lability
 Deepening voice
 Feedback inhibits pituitary FSH
 Acne
& LH secretion ↓ ovarian
estrogen secretion & stim.  Hirsutism
endometrial & breast tissue.  Amenorrhea
 ↓ breast size
 Endometriosis
 Fibrocystic breast ds
 Hereditary angioedema
 ↑ C1 esterase inhibitor & C4
complement component
Desmopressin
 Posterior pituitary hormone
 Vasopressin, ADH analogue

 Mimics natural vasopression


 Increases water reabsorption in
kidneys
 Vasoconstriction

 DI
 Nocturnal enuresis
 Control bleeding in hemophilia
& wWF’s ds

 Intranasal, oral, or IV
Ergocalciferol
 Vit. D  Hypercalcemia
 Fat-soluble  Hypercalciuria

 Activated in liver & kidneys to  Cholestyramine inhibits vit. D


absorption
form calcitriol
 Induce vit. D metabolism
 ↑ Ca & phosphorus absorption  Phenytoin
from gut
 Barbiturates

 Vit. D deficiency
 Rickets, osteomalacia
 Chronic renal failure
 Familial hypophosphatemia
 Hypocalcemia d/t
hypoparathyroidism
 Postoperative & idiopathic tetany
Ethinyl estradiol & drospirenone
 OCP  Drospirenone
 Estrogen & progesterone  Antiandrogenic
 Blocks aldosterone
 ↓ salt & water retention
 Feedback inhibit GnRH
 ↓ BP
 Estrogen
 ↓ FSH secretion & maturation
of dominant follicle  Thromboembolism
 ↑ risk w/ smoking
 Progesterone
 Inhibits midcycle LH surge &  Edema
ovulation
 Efficacy ↓ w/
 Contraception  ABX
 Regulate menstrual cycle  Carbamazepine
 Acne in women  phenytoin
Ethinyl estradiol & norethindrone
 OCP  Norethidrone
 Estrogen & progesterone  Slightly androgenic

 Feedback inhibit GnRH  Thromboembolism


 Estrogen  Edema
 ↓ FSH secretion & maturation  Depression
of dominant follicle  Gallbladder ds
 Progesterone
 Inhibits midcycle LH surge &
ovulation

 Contraception
 Regulate menstrual cycle
 Acne in women
Finasteride
 Androgen synthesis inhibitor  CI pregnancy
 5-α-reductase inhibitor  Risk to male fetus
 Do NOT handle tablets

 Inhibits conversion testosterone


 Impotence
 dihydrotestosterone & ↓
androgenic stimulation of
prostate & skin
 ↓ prostate size & promotes hair
growth

 BPH
 Male pattern baldness
Fludrocortisone
 Corticosteroid  Hypokalemia
 Mineralocorticoid  ↑ by thiazide & loop diuretics

 Activates aldosterone receptors


in renal distal tubule
 ↑ Na reabsorption
 ↑ K & H excretion

 Adrenal insufficiency
 Addison’s ds
 Congenital adrenogenital syn

 Tx idiopathic orthostatic
hypotension w/ ↑ Na intake
Glyburide
 Antidiabetic  Photosensitivity
 Sulfonylurea hypoglycemia  Hypoglycemia

 Closes ATP-sensitive K
channels preventing K efflux &
depolarizing pancreas B cells
 Influx Ca & relaxing insulin
 ↑ amount of insulin secreted
during each pulse

 Type II DM
Hydrocortisone
 Short-acting corticosteroid, low-
potency topical corticosteroid
 Glucocorticoid

 Replaces endogenous cortisol in


deficiency states
 Suppresses inflammation &
immune response – topical

 Adrenocortical insufficiency
 Topical
 Insect bites
 Contact dermatitis
Insulin
 Antidiabetic  Hypoglycemia
 Pancreatic hormone
 β-blockers mask signs of
hypoglycemia & prolong
 Replaces endogenous recovery
insulin

 DM

 Rapid acting – lispro


 Intermediate acting – lente
 Long acting – ultralente
Levothyroxine
 Thyroid hormone  Insomnia
 Tetraiodothyronine  Irritability
 Tachycardia
 Wt loss
 Binds nuclear receptors &
↑ gene transcription  Bile acid sequestrants ↓
 ↑ metabolic rate, protein absorption
synthesis, gluconeogenesis,
cell growth &
differentiation, & CNS
development
 Converted to T3 in tissues

 Hypothyroidism
Medroxyprogesterone
 Progestin, contraceptive  Amenorrhea
 Progesterone analogue  Breakthrough bleeding
 Dysmenorrhea
 ↓ endometrial hyperplasia in
women receiving estrogen
 Prevents conception by
thickening cervical mucus

 Estrogen-progestin HRT
 Injectable contraceptive
 Progestin-only injectable
contraceptive

 IM depot injection lasts 3mo


Metformin
 Antidiabetic  N, V, D
 Biguanide, antihyperglycemic  Abdominal bloating

 ↑ # & affinity of insulin


receptors in peripheral tissues
 ↓ hepatic glucose output
 ↓glucose absorption from gut
 ↑ glucose uptake & utilization in
skeletal m. & adipose tissue

 Type II DM

 Used in combo w/ sulfonylureas


Methimazole
 Antithyroid  Rash
 Thiourea, thyroid  Agranulocytosis
hormone synthesis
inhibitor

 Inhibits peroxidase &


iodination & coupling of
tyrosine residue of
thyroglobulin
 ↓ thyroxine secretion

 Hyperthyroidism – Grave’s ds
Mifepristone
 Abortificient  Abdominal pain
 Progesterone antagonist  Diarrhea
 N, V
 Uterine bleeding
 Partial agonist or antagonist
progesterone receptors  Cramping

 Medical termination of
pregnancy through 49d gestation

 Single dose + prostaglandin for


48hr stim. uterine contractions
Octreotide
 GH inhibitor, antidiarrheal  Arrhythmias
 Somatostatin analogue w/ greater  Hyperglycemia
effects on GH than insulin secretion  Hypoglycemia
 Constipation
 Suppresses secretion of GH,  Diarrhea
insulin-like growth factors, 5-HT &  Flatulence
GI peptides – gastrin, motilin,  N
secretin, & VIP

 Acromegaly
 Severe diarrhea & flushing d/t
carcinoid tumors & VIP tumors
 Bleeding GE varices
 Complications of pancreatic surgery
Oxytocin
 Oxytocic  Excessive & painful uterine
 Posterior pituitary hormone contractions

 Stim. Uterine smooth m. &


induce labor
 Stim. mammary gland smooth
m. & lactation

 Induce labor @ term


 Facilitate uterine contractions
 Postpartum control of uterine
bleeding
 Promote milk let-down

 IV for uterine stim.


 Nasal for milk let-down
Pioglitazone
 Antidiabetic
 Thiazolidinedione
antihyperglycemic

 Activates peroxisome proliferator-


activated receptor-γ in adipose
tissue, skeletal m., & liver
 ↑ gene transcription, insulin
sensitivity, & glucose transports in
muscle & adipose tissue
 Suppresses hepatic glucose output

 Type II DM

 Used w/ metformin
Prednisone
 Anti-inflammatory  Depression or euphoria
 Corticosteroid  HTN
 Acne
 Impaired wound healing
 Suppresses inflammation  Adrenal suppression
& immune response  Muscle wasting
 Osteoporosis
 Inflammatory, allergic,  Cushingoid appearance
autoimmune, & neoplastic ds  Moon facies
 Prevent organ transplant  Buffalo hump
rejection  ↑ susceptibility to infection
 Asthma
Raloxifene
 Bone resorption inhibitor  Hot flashes
 Selective estrogen receptor
modulator – SERM  Cholestyramine inhibits
absorption
 Estrogen-like effect on bone &
lipid metabolism
 Estrogen antagonist in breast &
uterine tissue
 ↑ bone mineral density & ↓
vertebral fractures

 Osteoporosis in postmenopausal
women

 Used in woman @ risk for


breast cancer
Repaglinide
 Antidiabetic  Hypoglycemia
 Meglitinide hypoglycemic

 Closes ATP-sensitive K
channels & ↑ insulin secretion
 ↓ postprandial blood glucose &
[HbA1c]

 Taken before meals to control


postprandial hyerglycemia

 Used w/ metformin
 NOT sulfonylureas
Somatropin
 GH
 Recombinant somatotropin

 ↑ release of insulin-like growth


factors in liver & cartilage
 Stim. skeletal growth, AA
transport, protein synthesis,
nucleic acid synthesis & cell
prolif.

 Short stature in children d/t GH


deficiency
 Turner syn
 Chronic renal failure
 Prader-Will syn
Testosterone
 Androgen  Edema
 Gonadal steroid  Acne
 Gynecomastia
 Impotence
 Activated gene transcription &
development of male sex organs &  Oligospermia
secondary sex characteristics  Priapism
 ↑ lean body mass
 Stim. skeletal growth
 Accelerates epiphyseal closure
 ↑ sebaceous gland sebum
production
 ↑ EPO secretion
 ↓ HDL levels

 Hypogonadism in androgen-deficient
men
 Delayed puberty in males
Gastrointestinal
 Bisacodyl  Misoprostol
 Calcium carbonate  Omeprazole
 Dicyclomine  Ondansetron
 Docusate  Promethazine
 Lactulose  Ranitidine
 Loperamide  Sucralfate
 Mesalamine  Tegaserod
 Metoclopramide
Bisacodyl
 Stimulant laxative  Cramping
N
 Fluid & electrolyte
 Inhibits GI fluid depletion
reabsorption &  Hypokalemia
stimulates peristalsis

 Bowel evacuation prior


colonoscopy or surgery
 Acute constipation
Calcium carbonate
 Antacid, Ca supplement  Constipation
 Ca salt
 ↓ absorption of drugs
 Tetracyclines
 Neutralizes gastric acid  Fluoroquinolones
 Provides Ca supplementation  Phenytoin
 Iron salts
 Dyspepsia
 Hypocalcemia
 Prevention of osteoporosis

 Admin 1-1.5hr after meals & @


bedtime
Dicyclomine
 Antispasmodic  Constipation
 Muscarinic receptor  Dyspepsia
antagonist  Dry mouth
 Urinary retention
 Blurred vision
 Blocks PNS stim. intrinsic  Decreased sweating
nervous system & ↓ GI
tone & motility
 Directly relaxes GI smooth
m.

 IBS – cramping & pain


Docusate
 Stool softener, laxative
 Surface-active agent

 Facilitates hydration of
fecal material & softens
feces

 Constipation
 Fecal impaction – rectal
enema
Lactulose
 Laxative  Cramping
 Osmotic agent  Abdominal distention
 Flatulence
 ↑ water content & softens feces
 Lowers pH of colon
 Converts ammonia 
ammonium ion & ↓ ammonia
absorption & blood levels

 Chronic constipation
 Hepatic encephalopathy
 Improves mental status
Loperamide
 Antidiarrheal  Constipation
 Opioid analogue  Drowsiness

 Additive effects
 Activates opioid receptors in GI smooth  Kava
m.  Chamomile
 Segmental contraction & inhibits  Valerian
peristalsis

 Mild-moderate acute diarrhea


 Chronic diarrhea d/t IBD
 ↓ volume of ileostomy drainage

 AVOID
 Pregnancy
 Lactation
 Children < 2 y/o
Mesalamine
 GI anti-inflammatory
 Salicylate – 5-ASA

 Inhibits prostaglandin synthesis &


migration of inflammatory cells
into bowel wall
 Scavenges superoxide-free radicals

 IBD
 UC
 Proctitis

 Sulfasalazine  mesalamine &


sulfapyridine
Metoclopramide
 Promotility & antiemetic  CI in Parkinson’s ds & seizure
 D2 receptor antagonist disorders

 Drowsiness
 Blocks relaxant effect of D on GI  EPS rxns
smooth m.  restlessness
 Blocks presynaptic D receptors & ↑
Ach release & stim. smooth m.
 Blocks D2 receptors in
chemoreceptor trigger zone &
vomiting center

 Chemotherapy-induced emesis
 Gastric stasis – postsurgical &
diabetic
 GE reflux
Misoprostol
 Cytoprotective  CI in pregnancy
 Synthetic PGE1 analogue
 Abdominal pain
 D
 ↓ gastric mucosal secretion  Miscarriage
& ↑ secretion of
bicarbonate & mucus

 Prevent gastric mucosal injury


from NSAIDs
 Abortificient in combo w/
mifepristone
Omeprazole
 Antiulcer  Abdominal pain
 Proton pump inhibitor
 Inhibits metabolism
 Diazepam
 Irreversibly inhibits H/K ATP  Cyclosporine
pump in gastric parietal cells  Phenytoin
 Prevents gastric acid secretion

 Peptic ulcer ds
 GE reflux
 Zollinger-Ellison syn
 dyspepsia
Ondansetron
 Antiemetic  HA
 5-HT3 receptor antagonist  Constipation
 D
 Blocks 5-HT3 receptors in GI
vagal afferent nerves, solitary
tract nucleus, & chemoreceptor
trigger zone

 Prevent N, V from chemotherapy


& radiation therapy
 Postoperative N, V
Promethazine
 Antiemetic, antihistamine,  Neuroleptic malignant syn
sedative
 H1 receptor antagonist,  Sedation
phenothiazine  Confusion
 Disorientation
 Blocks H1 & M1 receptors
 Inhibits stim. chemoreceptor
trigger zone & vomiting center

 N, V
 Preoperative sedation
 Allergic rxns
Ranitidine
 Antiulcer
 H2 receptor antagonist

 Blocks H2 receptors in
gastric parietal cells
 ↓ gastric acid secretion

 Peptic ulcer ds
 GE reflux
 Dyspepsia
Sucralfate
 Antiulcer  Constipation
 Cytoprotective, sulfated
polysaccharide  ↓ absorption
 Fat soluble vitamins
 fluoroquinolones
 Adheres ulcer crater & forms
protective barrier
 Prevents acid secretion & pepsin
hydrolysis of mucosal proteins
 Stim. prostaglandin synthesis

 Peptic ulcer ds
 GE reflux
 Prevent NSAID-induced gastric
injury
Tegaserod
 GI motility agent  Diarrhea
 Partial agonist @ 5-HT4  Ischemic colitis
receptors

 Activates 5-HT4 receptors


on sensory neurons in
enteric nervous system
 Release neurotransmitters
& ↑ peristalsis

 IBS in women w/ constipation


Hematologic
 Abciximab  Epoetin
 Alteplase  Eptifibatide
 Aspirin  Ezetimibe
 Atorvastatin  Filgrastim
 Bivalirudin  Folic acid
 Cholestyramine  Gemfibrozil
 Cilostazol  Heparin
 Clopidogrel  Niacin
 Cyclosporine  Sirolimus
 Enoxaparin  Warfarin
Abciximab
 Antithrombotic  Bleeding
 Monoclonal Ab  Thrombocytopenia

 Inactivates platelet gp
llb/llla receptors
 Prevents platelet
aggregation

 Prevent thrombosis during


coronary angioplasty &
stent placement
Alteplase
 Thrombolytic  Reperfusion arrhythmia
 Plasminogen activator
 Contraindications
 Internal bleeding
 Converts plasminogen   Recent CNS surgery or
plasmin trauma
 Degrades fibrin & fibrinogen

 AMI
 Acute ischemic stroke
 Occluded central venous
access devices

 Streptokinase & urokinase for


pulmonary embolism
Atorvastatin
 Cholesterol lowering agent  Myalgia
 HMG-CoA reductase  Myositis
inhibitor  Rhabdomyolysis
 Hepatitis
 HMG-CoA reductase, rate-  GI distress
limiting enzyme for
cholesterol  Effects ↑ w/
 ↑ hepatic cholesterol uptake  Grapefruit juice
 ↓ LDL levels  Azole antifungals
 cyclosporine
 Hypercholesterolemia

 Cholesterol-lowering effects ↑
w/ ezetimibe & bile acid-
binding agents
Bivalirudin
 Anticoagulant  Bleeding
 Hirudin analogue

 Inhibits thrombin
 Prevents blood coagulation

 Thrombosis in unstable angina


 AMI
 Stent insertion

 Used in pts w/ heparin-induced


thrombocytopenia
Cholestyramine
 Cholesterol-lowering  Constipation
agent  Abdominal discomfort
 Bile-acid binding resin

 Binds intestinal bile


acids
 Prevents reabsorption
 ↑ cholesterol utilization
 ↓ LDL levels

 Hypercholesterolemia
 Diarrhea d/t excess bile
acids
Cilostazol
 Antiplatelet  HA
 Platelet aggregation inhibitor
 Effects ↑ w/ CYP3A4
 Inhibits phosphodiesterase III inhibitors
& ↑ cAMP in platelet & blood  Azole antifungals
vessels  Erythromycin
 Inhibit platelet aggregation  Grapefruit juice
 Causes vasodilation

 Intermittent claudication
 Improves blood flow &
walking distance

 Additive effects w/ aspirin


Clopidogrel
 Antiplatelet  Hypersensitivity reaction
 Platelet aggregation inhibitor

 Irreversibly inhibits binding


of ADP to platelet receptors
 ↓ gp IIb/IIIa mediated
aggregation

 Stroke
 MI
 Peripheral vascular ds

 Additive effects w/ aspirin


Cyclosprine
 Immunosuppressant  HTN
 IL2 expression inhibitor  Nephrotoxic
 Gingival hyperplasia
 Hirsutism
 Bind immunophilins  Tremor
 Complex binds
calcineurin  inhibits
transcription of IL2 gene  Induce metabolism
 Rifampin
 Barbiturates
 Prevent rejection of renal,  Carbamazepine
cardiac or hepatic allografts
 Severe RA & psoriasis
 Inhibits metabolism
 Grapefruit juice
Enoxaparin
 Parenteral anticoagulant  Thrombocytopenia
 LMWH

 Binds/potentiates antithrombin
III on factor Xa

 Prevent
 DVT
 Pulmonary embolism after knee,
hip, or abdominal surgery
 Thrombosis in unstable angina &
non Q-wave MI

 Effects reversed w/ protamine


sulfate
 NO monitoring w/ PTT
Epoetin
 Hematopoietic growth factor  HTN
 Recombinant human EPO

 Binds receptors on erythroid


progenitor cells & stim. cell
maturation & prolif.
 Reticulocytosis & ↑ Hct

 Anemia d/t
 CRF
 Chemotherapy
 Zidovudine therapy
 Hematologic malignancy
 lymphoma

 Used as performance-enhancing
drug by athletes
Eptifibatide
 Antiplatelet  Bleeding
 GP IIb/IIIa receptor
antagonist

 Reversibly inhibits fibrinogen


binding to gp IIb/IIIa
receptors
 Prevents platelet aggregation

 Prevent coronary thrombosis in


 Unstable angina or non-ST
segment elevation MI
 Coronary angioplasty or stent
placement
Ezetimibe
 Cholesterol-lowering agent
 Cholesterol absorption inhibitor

 Disrupts annexin-caveolin
complex mediating cholesterol
transport intestinal brush border
 Inhibits absorption of biliary
dietary cholesterol

 Pro-drug converted to active


glucuronide metabolite

 Hypercholesterolemia

 Additive effect w/ statins


Filgrastim
 Hematopoietic growth factor  Bone pain
 Recombinant human GCSF

 Binds receptors on myeloid


progenitor cells & stim.
maturation & prolif.
 Accelerates neutrophil recovery
after myelosuppressive
chemotherapy
 ↓ infection incidence

 Neutropenia assoc/ w/
chemotherapy & bone marrow
transplants

 Avoid 24 hrs prior & after


chemotherapy
Folic acid
 Vitamin, hematologic agent  Absorption ↓ by
 Metabolic cofactor for DNA  Phenytoin
synthesis  Cholestyramine

 Folate reductase inhibited by


 Activated folate transfer one- MTX
carbon units to purine &
pyrimidine precursors

 Megaloblastic anemia
 Fetal neural tube defects
 Coronary artery ds

 Pregnant woman have ↑


requirements
Gemfibrozil
 Lipid-lowering agent  GI distress
 Fibric acid derivative  Myositis

 Activates peroxisome  Statins ↑ risk


rhabdomyolisys
proliferator activated
receptor-α
 Oxidizes FA & apo-AI & AII
 ↓ plasma triglycerides
 ↑ HDL

 Hypertriglyceridemia
 ↓ HDL levels

 Monitor LFTs throughout Tx


Heparin
 Parenteral anticoagulant Thrombocytopenia
 Antithrombotic

 Binds/potentiates antithrombin
III
 ↑ inactivation factor Xa &
thrombin

 Venous thromboembolism
 Pulmonary embolism
 AF w/ embolism
 Consumptive coagulopathies
 In vitro & catheter coagulation

 Monitor PTT
 Protamine sulfate for OD
Niacin
 Vitamin, lipid-lowering agent  Flushing
 G-protein coupled receptor  Pruritis
ligand  GI distress, peptic ulcer
 Hyperglycemia
 Activates G-protein coupled  Hepatotoxicity
receptor
 Inhibits lipolysis & release of  Statins ↑ risk
FA rhabdomyolysis
 ↓ hepatic triglyceride
synthesis & VLDL secretion

 Hypertriglyceridemia
 ↑ HDL
 Hypercholesterolemia
 Pellagra
Sirolimus
 Immunosuppressant  Leukopenia
 T-lymphocyte inhibitor  Thrombocytopenia
 Hyperlipidemia
 Rash
 Inhibits regulatory
kinase in cytokine-  ↑↑ blood levels
driven T-cell prolif.  Cyclosporine
 Combo w/ corticosteroid &  Azole antifungals
cyclosporine  Erythromycin
 Grapefruit juice
 Prevent  Cimetidine
 Rejection renal allograph
 Coronary stent restenosis
Warfarin
 Oral anticoagulant  Fetal malformations
 Coumarin vit. K antagonist  Abnormal bone development

 Inhibits reduction of oxidized


vit. K
 Prevents vit. K dependent
carboxylation of glutamate
residues of factors II, VII,
IX, X, proteins C & S

 Delayed onset d/t circulating


coagulation factors

 Monitor INR
 Give vit. K if bleeding
Musculoskeletal
 Acetaminophen  Indomethacin
 Allopurinol  Infliximab
 Celecoxib  Ketorolac
 Cyclobenaprine  Probenecid &
 Etanercept colchicine
 Ibuprofen
Acetaminophen
 Analgesic, antipyretic  OD cause fatal hepatic
 COX-3 inhibitor failure

 ↑ hepatotoxicity w/ alcohol
 Inhibits COX-3 selectively
 ↑ renal toxicity w/ salicylates
 Inhibits synthesis of PG & NSAIDs
causing pain & fever

 Mild-moderate pain
 Fever

 Lacks anti-inflammatory
& antiplatelet activity
Allopurinol
 Antigout  Rash
 Xanthine oxidase
inhibitor  Inhibits metabolism
 Mercaptopurine

 Inhibits xanthine
oxidase & catabolism of
purines  xanthine &
uric acid
 ↓ uric acid levels

 Prevent hyperuricemia &


gout
Celecoxib
 NSAID  GI bleeding
 COX-2 inhibitor  ↑ risk stroke & MI

 Inhibits COX-2 &


synthesis of PG causing
pain, fever, &
inflammation

 OA
 RA
 Inflammatory jt ds
Cyclobenzaprine
 Skeletal m. relaxant  Dizziness
 Tricyclic central-acting  Drowsiness
m. relaxant  Dry mouth

 AVOID MAOI
 Acts on brainstem &
spinal cord to reduce
tonic somatic m.
activity via γ & α motor
neurons

 Acute muscle spasm


Etanercept
 Antirheumatic agent,  URI
antitumor necrosis factor  HA
 Antitumor necrosis
factor – p57 combined  ↓ Ab response to live
w/ Fc of IgG virus vaccines

 Binds TNF-α & ↓ jt


inflammation & pain
 Slows progression of
RA

 RA
Ibuprofen
 NSAID  GI bleeding
 Nonselective COX inhibitor  N, V
 Dyspepsia
 Inhibits COX-1 & COX-2 &  Allergic rxns
synthesis of PG causing  Hepatitis & renal failure
pain, fever, & inflammation

 Mild-moderate pain or
dysmenorrhea
 Inflammatory disorders
 OA
 RA

 ↓ risk colon, breast, lung, &


prostate cancers
Indomethacin
 NSAID  GI bleeding
 Nonselective COX inhibitor  N, V
 Dyspepsia
 Allergic rxns
 Inhibits COX-1 & COX-2
 Dizziness
 Drowsiness
 Inflammatory disorders
 HA
 Gouty arthritis
 OA
 RA
 Ankylosing spondylitis
 PDA in premature
neonates
Infliximab
 Ds modifying  Fatigue
antirheumatic  N, V
 Monoclonal Ab to  URI
TNF-α

 Inactivates TNF-α & ↓


jt inflammation, pain,
& destruction
 ↓ Sx of Crohn’s ds

 RA
 Crohn’s ds
Ketorolac
 NSAID  Aspirin-allergy
 Nonselective COX inhibitor  Allergic rxn in pt w/ asthma
 Nasal polyps
 Inhibits COX-1 & COX-2 &
synthesis of PG causing
pain, fever, & inflammation

 Short-term pain management

 Prolongs bleeding time


 Limit use to < 5d
Probenecid & Colchicine
 Antigout  Probenecid
 Uricosuric – probenicid  Inhibits renal tubular
secretion of Penicillins
 Anti-inflammatory – colchicine  Used to ↑ penicillin serum
levels
 Probenecid  Colchicine
 Inhibits renal reabsorption of  D
uric acid & ↑ uric acid  N, V
secretion  Agranulocytosis & aplastic
 Colchicine anemia
 Inhibits leukocyte response to
monosodium urate crystals in
jt

 Acute gouty arthritis


 Prevent gouty arthritis
Neurodegenerative
 Baclofen  Levodopa-carbidopa
 Benztropine  Memantine
 Donepezil  Pergolide
 Entacapone  Selegiline
 Interferon-beta-1b
Baclofen
 Antispasticity • Drowsiness
 GABA-B receptor agonist • Dizziness
• Fatigue
 ↓ neuronal cAMP & Ca • Weakness
influx
• ↑ K influx • Additive effects
• ↓ motor neuron excitability • Alcohol
& inhibits spinal reflexes • Kava
• Valerian
• Spasticity
• Chamomile
• MS
• Spinal cord injury
• ALS
Benztropine
 Anti-Parkinson • Blurred vision
 Central anticholinergic • Dry eyes
• Constipation
 Blocks cholinergic receptors • Dry mouth
& restores neurotransmitter • Urinary retention
balance in basal ganglia

• Parkinson’s ds
• Drug-induced EPS

• ↓ tremor > bradykinesia &


rigidity
Donepezil
 Anti-Alzheimer • N, D
 Cholinesterase inhibitor • HA

 Inhibits cholinesterase in
CNS
• ↑ Ach neurotransmission
• Slows decline in cognitive
function

• Alzheimer’s ds

• Does NOT prevent ds


progression
Entacapone
 Anti-Parkinson • Rhabdomyolysis
• Neuroleptic malignant syndrome
 Catechol-O-
methyltransferase inhibitor

 Inhibits catechol-o-
methyltransferase
inactivation of levodopa
• ↑ levodopa in CNS
• Prolongs response to levodopa
& ↓ S/Sx Parkinson’s ds

• Adjunct to levodopa/carbidopa for


Parkinson’s ds

• AVOID nonselective MAOI


Interferon-beta-1b
 Anti-multiple sclerosis • HA
 Interferon • Weakness
• GI distress
 Binds cell surface
• Sweating
receptors producing • Neutropenia
immuno-suppressive • Myalgia
effects • Chills
• ↓ relapse & slows physical • Fever
disability in MS

• Relapsing-remitting MS

• SubQ daily
Levodopa-carbidopa
 Anti-Parkinson • Dyskinesia – involuntary movements
 Dopamine precursor, decarboxylase • N, V
inhibitor • Hallucinations

• ↑ arrhythmia w/ halothane
 Levodopa
• Converted to D in CNS
• Augments neurotransmission in
basal ganglia
 Carbidopa
• Inhibits peripheral dopa-decarboxylase
• ↑ levodopa availability in CNS

• Parkinson’s ds

• HTN crisis w/ MAOI


Memantine
 Anti-Alzheimer
 Glutamate antagonist

 Glutamate NMDA
receptor antagonist
• Prevent excitotoxic effects
of glutamate causing
neuronal loss
• Slows decline in cognitive
function

• Alzheimer’s ds
Pergolide
 Anti-Parkinson • Dyskinesia
 Dopamine receptor • Hallucination
agonist • Orthostatic hypotension
• Constipation

 Activates D receptors in
basal ganglia

• Parkinson’s ds in
conjunction w/
levodopa/carbidopa
Selegiline
 Anti-Parkinson • AVOID
• Meperidine & opioids
 Type B MAOI • Fatal rxn
• Excitation
• Rigidity
 Converted to active form by • HTN
• coma
MAO • SSRI
 Irreversibly inhibits D • Serotonin syn
degradation by MAO • Tricyclics
• Asystole
• ↑ response to levodopa/carbidopa • HTN
Tx • Syncope
• Rigidity
• Parkinson’s ds w/ • seizures
levodopa/carbidopa

• Slows progression of Parkinson’s


ds
Other Drugs
• Alprostadil • Latanoprost
• Bosentan • Mesna
• Epoprostenol • Succimer
Alprostadil
• Vasodilator – IV infusion
• Prostaglandin E1 • Apnea
• Hypotension
• Arrhythmia
• Activates PG EP receptors – Local products
– Vascular smooth m. • Prolonged/painful erection
relaxation & vasodilation • lightheadedness

– Maintain PDA in neonates


awaiting surgery
• IV infusion
– Male erectile dysfunction
• Local injection or pellets
Bosentan
• Vasodilator – CI in pregnancy
• Endothelin-1 receptor • Causes birth defects
antagonist
– ↑ serum aminotransferase
levels
• Blocks endothelin A & B
receptors
• ↓ pulmonary vascular
resistance & dyspnea
• Improves walking distance

– Pulmonary arterial HTN


Epoprostenol
• Vasodilator – Flushing
• Naturally occurring – Hypotension
prostacyclin (PGI2) – Tachycardia
– Diarrhea
• Activated prostaglandin IP – N, V
receptors
– Vascular smooth m.
relaxation
• ↑ pulmonary blood flow &
reduces dyspnea

– Pulmonary arterial HTN


Latanoprost
• Ocular hypotensive agent – Alters color of iris causing
• Prostaglandin F2α analogue permanent eye color change
by ↑ amount of melanin in
melanocytes
• Activates prostaglandin FP
receptors
• ↑ aqueous humor outflow via
uveoscleral pathways
• Lowers intraocular pressure

– Chronic open-angle glaucoma

– Topical ocular admin


Mesna
• Antidote
• Sulfhydryl compound

• Detoxifies urotoxic
metabolites acrolein of
ifosfamide &
cyclophosphamide

– Hemorrhagic cystitis d/t


ifosfamide &
cyclophosphamide
Succimer
• Antidote
• Metal chelating agent –
dimercaptosuccinic acid

• Chelates lead
– Water-soluble chelates to
excreted in urine
• ↓ blood lead levels
Pharmacology
Analgesic & Antimigraine
 Butorphanol  Naloxone
 Dihydroergotamine  Propoxyphene
 Fentanyl  Sumatriptan
 Meperidine  Tramadol
 Methadone
 Morphine
Butorphanol
 Opioid analgesic  Dysphoria
 Mixed opioid agonist-antagonist  Nightmares
 w/drawal in pts dependent on full
opioid agonists
 Partial agonist or antagonist @
opioid µ receptors  AVOID MAOI
 Agonist @ κ receptors @ spinal  Potentially fatal
& supraspinal sites
 Inhibits spinothalamic pain
neurotransmission

 Moderate-severe pain
 Admin intranasally

 ↓ respiratory depression,
constipation, dependence than full
µ receptor agonists
Dihydroergotamine
 Antimigraine  N, V
 Ergot alkaloid  Stiff neck, shoulder, extremities
 5-HT 1B/1D receptor agonist  Leg weakness
 Numbness & tingling in fingers
& toes
 Activates 5-HT 1B/1D receptors
 Pial & dural vessel constriction
 Presynaptic inhibition of
trigeminal peptide
neurotransmitter release
 Inhibitions brainstem activation
of trigeminal neurons

 Vascular HA
 Migraine & cluster

 Injection or nasal spray


Fentanyl
 Opioid analgesic  Sedation
 Phenylpiperidine  Confusion
 Respiratory depression
 Activates opioid µ receptors  Anorexia
 Inhibits pain transmission  N, V
@ spinal & supraspinal  Constipation
sites
 AVOID MAOI in past 14d
 Chronic pain
 Breakthrough for cancer
pain

 Transdermal patch
Meperidine
 Opioid analgesic  Confusion
 Strong opioid agonist  Sedation
 Constipation
 N, V
 Activates opioid receptors  Dependence
 Inhibits pain transmission  Toxic metabolite  CNS
 Generalized CNS excitation, convulsions,
depression tremors

 AVOID MAOI
 Moderate-severe pain
 Potentially fatal
 Analgesia during labor
 Preoperative sedation

 Lacks antitussive activity


Methadone
 Opioid analgesic  Respiratory depression
 Strong opioid agonist  Constipation
 Confusion
 Sedation
 Activates opioid receptors
 Inhibits pain transmission  AVOID MAOI
 Suppresses opioid w/drawl
Sx w/ euphoria or
dependence

 Moderate-severe pain
 Prevention of opioid abuse

 Orally, once per day


Morphine
 Opioid analgesic  Sedation
 Strong opioid µ receptor  Confusion
agonist  Hypotension
 Constipation
 Activates µ receptors  Respiratory depression
 ↑ cAMP
 Opens K & closes Ca  AVOID MAOI w/ 14 d
channels  Potentially fata
 ↓ release substance P
 Inhibits pain @ spinal &
supraspinal sites

 Severe pain w/ MI
 Pulmonary edema

 Active metabolite
 Morphine glucuronate
Naloxone
 Opioid antagonist
 Opioid receptor antagonist

 Blocks opioid µ, δ, κ
receptors
 Rapidly reverses effects of
opioid agonists

 Opioid OD, dependence

 Short half-life needs


repeated doses
Propoxyphene
 Opioid analgesic  Dizziness
 Weak opioid agonist  Weakness
N
 dependence
 Activates opioid
receptors
 Inhibits pain transmission

 Mid-moderate pain

 Combined w/
acetaminophen or aspirin
Sumatriptan
 Antimigraine  Dizziness
 5-HT 1B/1D receptor agonist  Vertigo
 Tingling
 Warm sensation
 Activates 5-HT 1B/1D receptors
 Tight feeling head & chest
 Pial & dural vessel constriction
 Coronary vasospasm
 Presynaptic inhibition of
trigeminal peptide
neurotransmitter release  AVOID
 MAOI
 Inhibitions brainstem activation  SSRI
of trigeminal neurons

 Vascular HA
 Migraine & cluster

 Oral, nasal, & subQ


Tramadol
 Analgesic  Dizziness
 Dual action  HA
 Constipation
 Activates µ opioid receptors  Lowers seizure threshold
 Inhibits neuronal reuptake
5-HT & NE  AVOID MAOI
 ↑ inhibition of pain
 ↑ risk seizures w/ high
 Moderate pain doses
 Chronic pain  Penicillins
 Phenothiazines

 Naloxone reverses some


but NOT all Sx
Anesthetics
 Benzocaine  Midazolam
 Bupivacaine  Nitrous oxide
 Halothane  Propofol
 Ketamine  Sevoflurane
 Lidocaine
Benzocaine
 Local anesthetic  Cross-sensitivity w/ other ester-
 Ester-type type anesthetics

 Blocks Na channels & nerve


conduction

 Topical anesthetic
 Pain
 Itching
 Inflammation
 Burns
 Insect bites
 Contact dermatitis
 Wounds

 Irritates skin when 1st applied


 Use caution w/ sunburn & large
areas of skin
Bupivacaine
 Local anesthetic Cross-sensitivity w/
 Amide-type amide-type anesthetics

 Blocks Na channels &


nerve conduction

 Local or regional
anesthetic
 Surgical
 Diagnostic
 Obstetrical
 therapeutic
Halothane
 General anesthetic  Sensitizes heart to
 Inhalational, halogenated catecholamine-induced
cardiac arrhythmia
hydrocarbon
 Hepatotoxic
 Fluoride metabolites
 Potentiates GABA binding to
GABA-A Cl ion channel
 Suppresses sensory
processing in thalamus

 General anesthetic

 High blood:gas partition


coefficient
 Slow rate of induction &
recovery
Ketamine
 IV anesthetic  Delirium
 Glutamate antagonist  Hallucination
 Irrational behavior during
 Blocks glutamate NMDA recovery
receptors  ↑ BP
 Dissociate anesthesia
 Analgesia
 Immobility
 Amnesia

 Does NOT depression


respiration or cause LOC

 Anesthesia
 Minor surgical & diagnostic
procedures
 Children
Lidocaine
 Local anesthetic  Cross-reactivity w/ amide-type
 Amide-type anesthetics

 Blocks Na channels & nerve


conduction

 Topical
 Infiltration
 Nerve block
 Epidural
 Spinal anesthesia
 Eutectic mixture
 Lidocaine & prilocaine
 Anesthetize intact skin for
venipuncture
 IV cannulation
 Circumcism
Midazolam
 Sedative-hypnotic-anxiolytic  Apnea
 Short-acting BZDP  Laryngospasm
 Respiratory depression
 Potentiates GABA binding to  Cardiac arrest
GABA-A Cl ion channel
 Sedation
 Hypnosis
 Amnesia

 Preoperative sedation &


anxiolysis
 Sedation of mechanically
vented pts
Nitrous Oxide
 Inhalation general anesthetic
 Anesthetic gas

 Potentiates GABA binding to


GABA-A Cl ion channel
 Suppresses sensory
processing in thalamus
 Minor surgery & dental
procedures

 Rapid induction & recovery


 Euphoria – laughing gas
Propofol
 General anesthesia  Bradycardia
 IV anesthetic  Hypotension
 Diisopropyl phenol

 Potentiates GABA binding


GABA-A Cl ion channel
 Hypnosis
 Anesthesia
 Amnesia

 NO analgesic effect

 Intubation & maintenance of


general anesthesia
 Sedation of intubated pts in
ICU
Sevoflurane
 General anesthetic
 Inhalation anesthetic

 Potentiates GABA
binding to GABA-A Cl
channel
 Suppresses sensory
processing in thalamus
 Causes LOC

 General anesthesia
Anti-infective
 Acyclovir  Cefepime
 Albendazole  Cetriaxone
 Amantadine  Ciprofloxacin
 Amoxicillin-clavulanate  Clindamycin
 Amphotericin B  Doxycycline
 Azithromycin  Efavirenz
 Aztreonam  Enfuvirtide
 Caspofungin  Erythromycin
 Cefazolin  Ethambutol
 Foscarnet  Linezolid
 Fosfomycin  Mefloquine
 Ganciclovir  Metronidazole
 Gentamicin  Mupirocin
 Griseofulvin  Nafcillin
 Imipenem-cilastatin  Nitrofurantoin
 Isoniazid  Oseltamivir
 Itraconazole  Paromomycin
 Ivermectin  Penicillin G
 Levofloxacin
 Pentamidine  Rifampin
 Piperacillin-tazobactam  Ritonavir-lopinavir
 Praziquantel  Streptomycin
 Primaquine  Terbinafine
 Pyrimethamine  Trifluridine
 Pyrantel  TMP-SMX
 Quinine  Vancomycin
 Quinpristein-dalfopristin  Zidovudine
 Ribavirin
Acyclovir
 Antiviral  Dizziness
 Nucleoside analogue  Diarrhea
 N
 Nephrotoxicity
 Converted to acyclovir
triphosphate by viral & host cell
kinases  Probenecid ↑ serum levels
 Incorporated into DNA by viral
DNA polymerase causing DNA
chain termination

 HSV2
 Herpes zoster
 Shingles
 Chickenpox – varicella

 ↓ viral shedding, pain, & healing


time
Albendazole
 Antihelmintic  GI distress
 Benzimidazole  Constipation or diarrhea
 Hepatitis & hematologic toxicity w/ high
doses
 Binds & inhibits polymerization of
tubulin dimmers to form
cytoplasmic microtubules
 Impairs glucose uptake & deplete
glycogen stores

 Intestinal nematode infections


 Hookworm
 Pinworm
 Whipworm
 Ascariasis
 Capillariasis
 Trichinosis
 Use w/ corticosteroid
 Cysticercosis & echinococcus
 Microsporidiosis
Amantadine
 Anti-influenza,  Ataxia
antiparkinson  Dizziness
 Tricyclic amine  Insomnia
 Skin mottling & livedo
reticularis
 Inhibits influenza-A M2  Blurred vision
proton channel &  Dry mouth
acidification of virus
particle
 Prevents viral protein-
protein dissociation &
uncoating of viral
particles

 Influenza A
Amoxicillin-clavulanate
 β-lactam ABX  Diarrhea
 Extended spectrum aminopenicillin  Superinfection
& β-lactamase inhibitor  Pseudomembranous colitis
 Allergic rxn
 Rash
 Amoxicillin  Serum sickness
 Binds PBP  anaphylaxis
 Inhibits cross-linking of cell wall
peptidoglycan
 Probenecid inhibits renal tubular
 Clavulanate excretion
 Inhibits class-A β-lactamase  ↑ serum levels
 Protects amoxicillin from
destruction
 NOT antimicrobial by itself

 Respiratory tract infections


 Otitis, sinusitis, pneumonia
 Skin or skin structure infections
 Bite wounds
Amphotericin B
 Antifungal  Chills
 Fever
 Polyene ABX  Diarrhea
 N, V
 Binds ergosterol & ↑  Nephrotoxicity
membrane permeability  Hypokalemia
 Leakage of cell contents
 ↑ toxicity w/ cyclosporine,
antineoplastics
 Candidiasis
 Thiazides, & corticosteroids ↑
 Cryptococcal meningitis hypokalemia
 Aspergillosis
 Blastomycosis
 Coccidioidomycosis
 Histoplasmosis
 Mucormycosis
Azithromycin
 Macrolide
 Protein synthesis inhibitor

 Binds 50s ribosome


 Prevents peptide elongation &
translocation from acceptor site
to peptidyl site

 Respiratory infections d/t strep,


pneumo, H. influenzae, Legionella
 Otitis media, sinusitis
 Single-dose Tx for chlamydial
urethritis, chancroid, MAI
infections
Aztreonam
 β-lactam ABX  Thrombophlebitis
 Monobactam  Allergic rxn

 Binds PBP including


transpeptidase
 Inhibits cross-linking of
cell wall peptidoglycan

 Drug resistant gram (-)


infections including
Pseudomonas aeruginosa
& Enterobacteriaceae
Caspofungin
 Antifungal  HA
 Echinocandin  Fever
 Phlebitis
 Abnormal LFTs
 Inhibits synthesis of
cell wall component
 β-1,3-D-glucan

 Candida albicans
 Invasive aspergillosis

 IV admin
 Not absorbed well by gut
Cefazolin
 β-lactam ABX  Rash
 2nd generation cephalosporin  Diarrhea
 Pseudomembranous colitis
 Superinfection
 Binds PBP including
transpeptidase
 Probenecid inhibits excretion & ↑
 Inhibits cross-linking of cell serum levels
wall peptidoglycan

 Surgical wound infections


 Infections d/t
 Staph, strep, E. coli, Klebsiella
pneumoniae, Proteus mirabilis

 NOT active against MRSA


Cefepime
 β-lactam ABX  Rash
 4th generation  Diarrhea
cephalosporin  Pseudomembranous colitis
 Superinfection

 Binds multiple PBP  Probenecid inhibits excretion


 Inhibits cross-linking of & ↑ serum levels
cell wall peptidoglycan
 Resistant to many β-
lactamases

 Drug-resistant gram (-)


bacteria
 Citrobacter
 Enterobacter
Ceftazidime
 β-lactam ABX  Rash
 3rd generation cephalosporin  Diarrhea
 Pseudomembranous colitis
 Superinfection
 Binds PBP including
transpeptidase
 Probenecid inhibits excretion & ↑
 Inhibits cross-linking of cell serum levels
wall peptidoglycan

 Gram (+), gram (-), & anaerobics


– Pseudomonas aeruginosa

 Pneumonia, meningitis, UTI, skin


structures, bones, jts
Cetriaxone
 β-lactam ABX  Rash
 3rd generation cephalosporin  Diarrhea
 Pseudomembranous colitis
 Superinfection
 Binds PBP including
transpeptidase
 Probenecid inhibits excretion & ↑
 Inhibits cross-linking of cell serum levels
wall peptidoglycan

 Infection d/t
 Pneumococci, gonococci,
meningococci, H. influenzae,
Moraxella catarrhalis, Borrelia
burgdorferi

 Single IM injection Tx acute


otitis media or gonorrhea
Ciprofloxacin
 Antibacterial  Insomnia
 Fluoroquinolone  Diarrhea
 N
 Inhibits bacterial DNA  Absorption ↓ by cations
topoisomerase type II (DNA gyrase)  Antacids
& type IV
 Iron
 Prevents DNA replication &  Zinc
separation of chromosomes  bismuth

 Urinary tract, prostate, intraabdominal


w/ metronidazole, bone or jt, skin
 Inhalational anthrax
 Gonorrhea
 Infectious diarrhea

 Gram (+), gram (-), Pseudomonas


aeruginosa
Clindamycin
 Aminosugar ABX  C. difficile superinfection
 Protein synthesis  Diarrhea
inhibitor  Pseudomembranous colitis

 Binds 50s ribosome


 Prevents translocation of
nascent peptide from
acceptor site to peptidyl
site

 Strep, staph, gram (+)


 Acne vulgaris
 Anaerobes including
Bacteroides
Doxycycline
 Tetracycline ABX  AVOID
 Protein synthesis inhibitor  Pregnancy & children > 8 y/o
 Outdated preparations are
nephrotoxic
 Binds 30s ribosome
 Reversibly inhibits binding of  Permanent teeth discoloration
transfer RNA to acceptor site  Photosensitivity
 Diarrhea
 Rickettsia, Chlamydia,  N, V
Mycoplasma, Borrelia
 Acne
 Cholera
 Gonorrhea & syphilis in PCN
allergic pts
 Brucellosis & ehrlichiosis
Efavirenz
 Antiretroviral  N
 Non-nucleoside reverse  Rash
transcriptase inhibitor  Drowsiness
 Depression

 Binds reverse
transcriptase & disrupts
catalytic site

 HIV in combo w/ nucleoside


reverse transcriptase inhibitor
– synergistic

 High fat meal ↑ absorption


Enfuvirtide
 Antiretroviral  Injection site rxn
 HIV fusion inhibitor  Rotate sites daily

 Binds HIV virus gp41 &


blocks fusion of HIV w/
host cells CD4 Thelper
lymphocytes

 Drug-resistant HIV
Erythromycin
 Macrolide ABX  Activates motilin receptors
causing uncoordinated
 Protein synthesis inhibitor peristalsis
 Anorexia
 Binds 50s ribosome  N, V

 Prevents peptide elongation


& translocation from
acceptor site to peptidyl site

 Pharyngitis, otitis media,


sinusitis, pneumonia d/t
 Strep, pneumococci,
Mycoplasma, Chlamydia,
Legionella, MAI
Ethambutol
 Antitubercular  Dose-related
retrobulbar optic
 Synthetic butanol
neuritis
derivative
 Impaired red-green
color discrimination
 Bacteriostatic against  Monitor pts color
mycobacteria discrimination
regularly
 Inhibits RNA synthesis  Gouty arthritis

 M. tuberculosis
 MAI
Foscarnet
 Antiviral  HA
 Diarrhea
 Pyrophosphate  V
 Renal failure
 Blocks pyrophosphate-  Hypocalcemia
binding site on viral  Hypokalemia
DNA polymerase  Hypomagnesemia
 Prevents attachment of  Anemia
nucleotide precursors to  Arthralgia
DNA  Myalgia

 CMV retinitis in HIV pts  Pentamidine causes life-


 Acyclovir-resistant HSV in threatening hypocalcemia
immunocompromised
Fosfomycin
 ABX
 Cell wall synthesis
inhibitor

 Inhibits enopyruvyl
transferase & addition of
phosphenolpyruvate to N-
acetylglucosamine to
form N-acetylmuramic
acid

 Cystitis d/t E. coli or


Enterococcus faecalis

 Single dose Tx for UTI


Ganciclovir
 Antiviral  ↓ visual acuity
 Nucleoside  Neutropenia
analogue  Thrombocytopenia
 Anemia
 Converted to
ganciclovir
triphosphate
 Inhibits viral DNA
polymerase

 CMV infection in
immunocompromise
d & transplants
Gentamicin
 Aminoglycoside ABX  Nephrotoxicity
 Protein synthesis inhibitor  Ototoxicity
 Vestibular & cochlear
 ↑ w/ loop diuretics
 Binds 30s ribosome
 Prevents initiation of protein
synthesis
 Misreading of genetic code

 Gram (-) bacilli including


Enterobacteriaceace & P.
aeruginosa
 Strep, enterococcal, & staph
infections

 Monitor serum levels


Griseofulvin
 Antifungal  HA
 Fungistatic ABX
 Induces CYP450
 Reduces plasma levels
 Deposits in keratin warfarin & OCP
precursor cells of skin,
hair, & nails
 Disrupts microtubules
& mitotis of
dermatophytes

 Dermatophyte infections
 NOT Candida
Imipenem-cilastatin
 β-lactam ABX  Allergic rxns
 Carbapenem ABX &  Diarrhea
dehydropeptidase inhibitor  V
 Seizures
 ↑ risk w/ ganciclovir or
 Imipenem cyclosporine
 Binds PBP & inhibits cross-
linking cell wall peptidoglycan
 Probenecid inhibits secretion & ↑
 Cilastatin serum levels
 Inhibits renal dehydropeptidase
& degradation of imipenem

 Endocarditis, pneumonia, UTI,


pelvic, abdominal d/t aerobic &
anaerobic
Isoniazid
 Antitubercular  Hepatitis
 Toxic metabolite acetyl-
 Nicotinic acid derivative hydrazine
 Peripheral neuropathy
 Reduces catalase-  Vit. B6 deficiency
peroxidase
 Inhibits synthesis of
mycolic acid component of
cell wall

 TB

 Bimodal distribution d/t fast


& slow acetylation
 Inactivates vit. B6
Itraconazole
 Antifunal  GI distress
 Synthetic triazole  Rash
 Hepatitis

 Inhibits 14-α-demethylase
 CYP450 enzyme that
converts lanosterol 
ergosterol

 Blastomycosis, candidiasis,
coccidioidomycosis,
histoplasmosis
 Onychomycosis – nail beds
Ivermectin
 Antiparasitic  Vertigo
 Antihelmintic ABX  Sedation

 Activates glutamate-gated
Cl ion channel
 Pharyngeal m.
hyperpolarization &
paralysis

 Strongyloidiasis
 Cutaneous larva migrans
 Onchocerciasis filiariasis
 W. bancrofti
Levofloxacin
 Antibacterial
 Fluoroquinolone

 Inhibits bacterial DNA


topoisomerase type II (DNA
gyrase) & type IV
 Prevents DNA replication &
separation of chromosomes

 Community-acquired pneumonia
 UTI
 Gynecologic & skin infections

 Gram (+), gram (-), P. aeruginosa,


Mycoplasma, Mycobacterium
Linezolid
 Antibacterial  Inhibits MAO
 Oxazolidinone protein
synthesis inhibitor

 Binds 23s ribosomal


RNA of 50S subunit
 Prevents formation of
70s initiation complex

 VRE, MS/MRSA, PCN-


sensitive pneumococci
Mefloquine
 Antimalarial  Neuropsychiatric syn
 4-quinolone methanol  Hallucination
derivative  Anxiety
 Confusion
 Seizure
 Inhibits erythrocytic  Coma
schizogony
 Inhibit nucleic acid synthesis

 Malaria
 Chloroquine-
susceptible/resistant trains of
P. falciparum & P. vivax

 Perform CBC during chronic


prophylactic Tx
Metronidazole
 Antiprotozoal  GI pain
 Nitroimidazole  Anorexia
N
 Dizziness
 Reduced by
pyruvate:ferredoxin to
form nitro-free radicals  Alcohol causes
disulfiram-like effect
that attack DNA &
proteins

 Amebiasis, giardiasis,
trichomoniasis
 Balantidium coli, C.
difficile, B. fragilis
Mupirocin
 ABX
 Protein synthesis
inhibitor

 Competes w/ isoleucine
for binding bacterial
isoleucyl tRNA
synthetase
 Prevents addition of
isoleucine during protein
synthesis

 Impetigo by staph or strep


 Eradicate nasal colonization of
MRSA
 Infected traumatic skin lesions
Nafcillin
 β-lactam ABX  Diarrhea
 Superinfection
 Antistaphylococcal,  Pseudomembranous colitis
penicillinase-resistant  Allergic rxn
penicillin  Rash
 Serum sickness
 Anaphylaxis
 Binds PBP
 Inhibits cross-linking of cell
wall peptidoglycan  Probenecid inhibits renal
tubular secretion & ↑ serum
levels
 Methicillin-sensitive
penicillinase producing
staph
 Bone, jt, UTI, respiratory,
skin, endocarditis,
meningitis
Nitrofurantoin
 Urinary tract Anorexia
antibacterial N, V
 Nitrofuran Neurotoxicity
Pneumonitis

 Inhibits bacterial Probenecid inhibits


enzymes urinary excretion

UTI
 E. coli, S.
saprophyticus
Oseltamivir
 Antiviral
 Neuraminidase inhibitor

 Inhibits influenza A & B


neuraminidase
 Prevents release &
spreading of viral
particles

 Influenza A & B
Paromomycin
 Antiprotozoal  Nephrotoxic & ototoxic
if given IV
 Aminoglycoside ABX

 Inhibits protein
synthesis

 Intestinal amebiasis
 Cryptosporidiosis in
immunocompromised pts
Penicillin G
 β-lactam ABX  Diarrhea
 Narrow-spectrum  Superinfection
penicillin  Pseudomembranous
colitis
 Allergic rxn
 Binds PBP  Rash
 Inhibits cross-linking of  Serum sickness
cell wall peptidoglycan  Anaphylaxis

 Strep, pneumococcal,  Probenecid inhibits


meningococcal renal tubular secretion
 Syphilis
Pentamidine
 Antiprotozoal  Nephrotoxic
 Amidino-pentane  Hematologic toxicity
derivative  Hypoglycemia
 Allergic rxn
 Anaphylaxis
 Disrupts nucleic acid
synthesis in protozoa
 Erythromycin ↑ fatal
arrhythmias
 P. carinii
 Early stage African
trypanosimiasis –
sleeping sickness
Piperacillin-tazobactam
 β-lactam ABX  Diarrhea
 Antipseudomonal penicillin & β-  Superinfection
lactamase inhibitor  Pseudomembranous colitis
 Allergic rxn
 Rash
 Piperacillin
 Serum sickness
 Binds PBP
 Anaphylaxis
 Inhibits cross-linking of cell
wall peptidoglycan
 Tazobactam  Probenecid inhibits renal tubular
secretion
 Inhibits class A β-lactamases

 Gram (-) bacilli, P. aeruginosa


Praziquantel
 Antihelmintic  Malaise
 Isoquinoline derivative  Anorexia
 Drowsiness
 dizziness
 ↑ Ca permeability of
schistosome tegument
 Contraction & exposing
antigens to host
immunity

 Schistosomiasis
 Chinese liver fluke
 Lung fluke
 Cestodes – tapeworms
Primaquine
 Antimalarial  Hemolytic anemia in
G6PD deficiency
 8-aminoquinoline
 methemoglobinemia

 Converted to oxidizing
quinoline-quinone
intermediates

 Eradicate exo-erythrocytic
forms of P. vivax & P.
ovale
Pyrimethamine
 Antiprotozoal  N
 Folate reductase inhibitor  Anorexia
 Hypersensitivity rxn
 Inhibits folate reductase
 Folate deficiency in protozoa

 Malaria in combo w/ sulfadoxine


 Toxoplasmosis in combo w/
sulfadoxine

 NOT effective against P. vivax


Pyrantel
 Antihelmintic  Abdominal cramps
 Pyrimidine analogue  Anorexia
 Diarrhea
V
 Activates cholinergic
nicotinic receptors in
somatic m. of
nematodes
 Produces depolarizing
NM blockade

 Ascariasis
 Hookworm & pinworm
Quinine
 Antimalarial  Abdominal cramps
 4-aminoquinoline  Diarrhea
V

 Binds plasmodial DNA &  Cinchonism


prevents replication &  Tinnitus
transcription during  Blurred vision
erythrocytic schizogony
 Metabolism
 Chloroquine-resistant malaria  Cimetidine inhibits
 Rifampin induce
 Admin w/ doxycycline or
pyrimethamine-sulfadoxine
Quinupristin-dalfopristin
 Streptogramin ABX  Infusion site rxn
 Protein synthesis
inhibitor

 Binds 50s ribosomal


subunit
 Quinupristin
 Inhibits aminoacyl tRNA
synthesis & addition of AA
 Dalfopristin
 Inhibits peptidyl transferase

 VRE, MS/MRSA
Ribavirin
 Broad-spectrum antiviral  Anemia
 Guanosine analogue  Hypotension
 Cardiac arrest

 Converted to ribavirin
triphosphate
 Depletes guanosine
triphosphate
 Inhibits viral RNA &
protein synthesis

 RSV in infants or children


 Chronic hepatitis C
 Viral hemorrhagic fever – Lass
fever
Rifampin
 Antitubercular  Red discoloration of tears,
 Rifampin derivative urine, saliva, sweat
 Abdominal pain
 V
 Inhibits DNA-dependent RNA  Diarrhea
polymerase  Hepatitis

 TB  Induces CYP450
 Leprosy  ↓ levels
 Prophylaxis meningococcal  Warfarin
meningitis & H. flu B infections  Theophylline
 Itraconazole
 Steroids
 Opioids
 Phenytoin
 Verapamil
Ritonavir-lopinavir
 Antiretroviral  Anorexia
 HIV protease inhibitor V
 Altered taste
 Abnormal thinking
 Inhibits HIV protease &
 Hyperlipidemia
conversion of gag-pol
polyprotein to  Hyperlgycemia
functional proteins
 Ritonavir
 ↑ lopinavir levels

 HIV in combo w/
nucleoside reverse
transcriptase inhibitor
Streptomycin
 Aminoglycoside  Nephrotoxic
 Protein synthesis  Ototoxic
inhibitor  ↑ w/ loop diuretics

 Binds 30s ribosome


 Prevents initiation of
protein synthesis
 Misreading of genetic code

 Drug-resistant TB
 Plague
 Tularemia

 IV admin
Terbinafine
 Antifungal  Itching
 Allylamine  Rash
 Diarrhea
 Anorexia
 Inhibits squalene
oxygenase & formation of  Metabolism
squalene epoxide during  Cimetidine inhibits
fungal membrane  Rifampin induce
ergosterol synthesis

 Topical
 Tinea corporis, cruris,
pedis, versicolor
 Oral
 Onychomycosis – fungal
nail infection
Trifluridine
 Antiviral  Ocular irritation
 Thymidine analogue  Redness
 Itching

 Inhibits HSV DNA


polymerase

 Herpetic keratitis
 Keratoconjunctivitis

 Topical ocular admin


Trimethoprim-sulfamethoxazole
 Antibacterial  N, V
 Rash
 Folate antagonist  Stevens-Johnson syn
 Allergic rxn
 Sulfamethoxazole  Anemia
 Inhibits folate synthesis  Hemolytic anemia
 Megalobalstic anemia
 Trimethoprim  Leukopenia
 Inhibits folate reduction  Thrombocytopenia
 Crystalluria
 UTI, traveler’s diarrhea
 Shigella enteritis  Added folate deficiency w/
 P. carinii & Nocardia phenytoin or MTX
pneumonia
Vancomycin
 Glycopeptide ABX  Red man syn
 Extensive rate of infusion
 Cell wall synthesis
 Erythematous rash on
inhibitor face & upper body
 Ototoxicity
 Binds D-alanyl-D-alanine  Vestibular & cochlear
portion of peptidoglycan
 Prevents cross-linking of
D-alanine & pentaglycine
chain

 MRSA, penicillin-resistant
enterococci, C. difficile
Zidovudine
 Antiretroviral  Anemia
 Nucleoside reverse
transcriptase inhibitor

 Activated nucleotide
triphosphate incorporated into
DNA causing chain termination

 HIV
 Prevent maternal-fetal HIV
transmission

 1st line Tx for HIV infections


 Zidovudine w/ lamivudine or
emtricitabine & efavirenz or
lapinavir-ritonavir
Antineoplastic
 Anastrozole  Imatinib
 Bleomycin  Leuprolide
 Busulfan
 Meraptopurine
 Carmustine
 Cisplatin  Methotrexate
 Cyclophosphamide  Paclitaxel
 Doxorubicin  Tamoxifen
 Etoposide  Trastuzumab
 Fluorouracil  Vincristine
 Gemtuzumab
ozogamicin
Anastrozole
 Estrogen antagonist N
 Nonsteroidal aromatase  HA
inhibitor  Hot flashes
 Back pain
 Inhibits aromatase &
conversion to estrone
precursor to estradiol
 Lowers estrogen levels
 Halts progression of
estrogen-sensitive breast
cancers

 Breast cancer in
postmenopausal women
Bleomycin
 Antitumor  Pneumonitis &
 DNA intercalating pulmonary fibrosis
 Hyperpigmentation
 Complexes iron-  Mucocutaneous toxicity
forming oxygen free  Hematology toxicity
radicals that cause
single strand breaks
 G2 phase specific

Lymphomas
SCC
Testicular carcinoma
Choriocarcinoma
Busulfan
 Antineoplastic  N, V
 Alkyl sulfonate bifunctional  Myelosuppression
alkylating agent  Pulmonary fibrosis

 Cross-links DNA strands by


covalently bonding guanine
residues
 Prevents DNA replication &
transcription

 CML

 Use w/ cyclophosphamide prior


allogenic hematopoietic
progenitor cell transplant for
CML
Carmustine
 Antineoplastic  N, V
 Nitrosurea bifunctional  Hepatotoxicity
akylating agent  Anemia
 Leucopenia
 Cross-links DNA strands by  Thrombocytopenia
covalently bonding guanine  Pulmonary fibrosis
residues
 Prevents DNA replication &
transcription

 Brain tumors
 Myeloma
 Lymphoma

 Causes prolonged
myelosuppression
Cisplatin
 Antineoplastic  Severe N, V
 Platinum compound  Ototoxicity & tinnitus
 Hypocalcemia
 Forms reactive metabolites  Hypokalemia
that covalently bond DNA
bases & cross-link DNA
 Hypomagnesemia
strands  Anemia

 Testicular, ovarian, cervical,


bladder, lung, head/neck
cancers

 Less bone marrow


suppression
Cyclophosphamide
 Antineoplastic  Anorexia
 Nitrogen mustard bifunctional  N, V
akylating agent  Hemorrhagic cystitis & hematuria
 Alopecia
 Thrombocytopenia
 Cross-links DNA strands by  Leukopenia
covalently bonding guanine  Anemia
residues
 Prevents DNA replication &  Rifampin induces CYP & ↑ toxicity
transcription

 Hodgkin’s ds
 Lymphomas, myeloma
 Leukemia
 Ovarian & breast tumors
 RA

 Converted to active metabolites


by CYP enzymes
Doxorubicin
 Antitumor  Colors urine red
 DNA intercalating agent
 Cardiomyopathy – dose-
 Inserts b/w DNA bases limiting
 Causes deformation & uncoupling  Anemia
 Complexes iron forming  Leukopenia
hydroxyl free radicals that  Thrombocytopenia
cause strand breaks  Diarrhea
 Inhibits topoisomerase II V
 Causes strand breaks  Stomatitis
 S phase specific  Alopecia

 Breast, ovarian, bladder tumors


 Bronchogenic carcinoma
 Lymphoma & leukemia
Etoposide
 Antineoplastic  N, V
 Podophyllotoxin,  Leukopenia
topoisomerase inhibitor  Thrombocytopenia
 Alopecia
 Inhibits mammalian
topoisomerase II & prevents
resealing of nicked DNA
strands
 G2 phase specific

 Testicular, small cell lung


carcinoma
 Lymphoma
 Leukemia
Fluorouracil
 Antineoplastic  Diarrhea
 Pyrimidine antimetabolite V
 Stomatitis
 Converted to active  Alopecia
nucleotide form
 Maculopapular rash
 Inhibits thymidylate
synthetase  Anemia
 S phase specific  Leukopenia
 Thrombocytopenia
 Colon, breast, rectal, gastric,
pancreatic cancer
 Topical for basal cell
carcinoma & actinic
keratosis
Gemtuzumab ozogamicin
 Antineoplastic  Severe myelosuppression &
 Monoclonal Ab & cytotoxic hypersensitivity rxn
ABX calicheamicin  anaphylaxis
 Severe pulmonary rxns
 Gemtuzumab  Chills
 Binds CD33 Ag on  Fever
hematopoietic cells &
sequesters lysosomes where N
calicheamicin is released
 Dyspnea
 Calicheamicin
 Causes DNA dbl strand breaks

 CD33 (+) AML


Imatinib
 Antineoplastic  Cough
 Tyrosine kinase inhibitor  Dyspnea
 Pharyngitis
 Inhibits oncoprotein bcr-abl  Pneumonia
tyrosine kinase expressed  Abdominal pain
by Philadelphia V
chromosome  Petechiae
 Inhibits leukemic cell  Pruritis
proliferation & induced  Rash
apoptosis
 Night sweats
 Myalgia
 CML
 Cause hematologic &
 Arthralgia
cytogenetic remission  Thrombocytopenia
 Neutropenia
Leuprolide
 Antineoplastic, agent for  Transient ↑ in testosterone w/
precocious puberty 1st dose
 GnRH analogue  Use flutamide or other
androgen antagonist
 Hot flashes
 Pulsatile admin ↑ FSH & LH
release
 Continuous admin down-
regulates GnRH receptors & ↓
FSH & LH

 Central precocious puberty


 Advanced prostate cancer
 Endometriosis
 Uterine fibroids

 IM depot & implants for prostate


cancer
Mercaptopurine
 Antineoplastic  Cross-react w/ thioguanine
 Purine antimetabolite
 Myelosuppression
 Hyperuricemia
 Converted to nucleotide  Hepatotoxicity
triphosphate by phosphoribosyl
transferase  Allopurinol inhibits degradation
 Inhibits purine biosynthesis &
salvage pathways
 S phase specific

 Acute leukemia
 CML
 Lymphomas

 Tumors that delete


phosphoribosyl-transferase
acquire resistance
Methotrexate
 Antineoplastic  N, V
 Folate reductase inhibitor  Stomatitis
 Hepatotoxicity
 Inhibits dihydrofolate reductase  Anemia
 Prevents formation of active folate  Leukopenia
& addition of single carbon units to  Thrombocytopenia
DNA base precursors  Nephropathy
 S phase specific

 Choriocarcinoma, trophoblastic tumors


 Leukemia
 Breast, head, neck, lung cancers
 Severe psoriasis
 RA
 Mycosis fungoides

 Leucovorin used to minimized


hematologic toxicity & Tx OD
Paclitaxel
 Antineoplastic D
 Mitotic inhibitor  N, V
 Alopecia
 Binds tubulin & prevents  Anemia
depolymerization of  Leukopenia
microtubules of mitotic  Thrombocytopenia
spindle  Peripheral neuropathy
 M phase specific  Arthralgia
 Myalgia
 Advanced ovarian cancer w/
cisplatin
 Non-small-cell lung cancer
 Metastatic ovarian or breast
cancer
Tamoxifen
 Antineoplastic  CI during pregnancy &
 Estrogen receptor lactation
antagonist & partial agonist
N
 Competes w/ estrogen for  Hot flashes
receptors in breast & other  Menstrual irregularities
tissues
 Suppresses breast tumor
growth

 Breast cancer & ductal


carcinoma following surgery &
radiation
 Advanced breast cancer
Trastuzumab
 Antineoplastic  Abdominal pain
 Monoclonal Ab  Anorexia
 Diarrhea
 Binds human epidermal growth
factor-2 (HER2) receptor on V
breast cancer cells  Back pain
 Prevents receptor stim. & cell  Chills
proliferation  Fever
 Regression of breast cancer
metastases  Allergic rxns

 Metastatic breast cancer w/  Doxorubicin ↑ risk of


overexpression HER2 cardiotoxicity
 Combined w/ paclitaxel
 ↑ blood levels
Vincristine
 Antineoplastic  N, V
 Vinca alkaloid, mitotic inhibitor  Alopecia
 Peripheral neuropathy
 Binds tubulin & prevents
polymerization of tubulin dimers
forming microtubules of mitotic
spindle
 M phase specific

 Hodgkin’s ds
 Lymphoma
 Leukemia
 Neuroblastoma
 Rhabdomyosarcoma
 Wilm’s tumor
Autonomic & Neuromuscular
 Atenolol  Pralidoxime
 Atropine  Propranolol
 Dobutamine  Pseudoephrine
 Edrophonium  Pyridostigmine
 Epinephrine  Rocuronium
 Phenoxybenzamine  Sildenafil
 Phentolamine  Succinylcholine
 Phenylephrine  Tamsulosin
 Pilocarpine  Terazosin
Atenolol
 Sympatholytic, Bronchoconstriction w/
antihypertensive high doses b/c β1
 Β1 receptor antagonist blockade

Additive hypotension w/
 β1 receptor antagonist
nitrates

 Angina
 Post MI
 Hypertension
Atropine
 Anticholinergic  Mydriasis & cycloplegia
 Muscarinic receptor  Warm, dry, flushed skin
antagonist  Tachycardia
 Delirium
 Muscarinic receptor
blocker  Hallucinations

Bradycardia
IBS
Anticholinesterase
poisoning
Antisecretory agent
Dobutamine
 Sympathomimetic, cardiac  Tachycardia
stimulant  Arrhythmia
 β1 receptor agonist

 Selective β1 receptor
agonist
 β1 > β2 > α1

 Cardiac contractility &


output
 Acute heart failure
 Cardiogenic shock

 Synergistic on cardiac output


w/ nitroprusside
Edrophonium
 Diagnostic agent Muscarinic effects
 Miosis
 Cholinesterase
 Salivation
inhibitor

 Reversible
cholinesterase
inhibitor

Dx myasthenia gravis


Epinephrine
 Sympathomimetic,  HTN
bronchodilator, vasopressor  Tachycardia
 Nonselective adrenergic  Ischemia
agonist  Hyperglycemia

 Activates α & β receptors


 ↑ IP3 & cAMP
 α1 – vasoconstrict & ↑ BP
 β1 – ↑ HR, conduction, &
contractility
 β2 – vasodilate, ↓ BP,
bronchodilate

 Cardiac arrest, V fib


 Shock, asthma
 COPD
Phenoxybenzamine
 Vasodilator Postural hypotension

 Irreversible α
Hypotension w/ β
receptor antagonist blockers & Ca channel
blockers
 α receptor
antagonist
α1 > α2

 Presurgical Tx of HTN d/t


pheochromocytoma
Phentolamine
 Vasodilator  Hypotension
 α receptor antagonist
 Severe hypotension w/
Epi
 Blocks α1 & α2
receptors

 Control BP during surgical


removal of
pheochromocytoma

 IV admin only
Phenylephrine
 Vasocontrictor, decongestant  Rebound nasal congestion
 HTN
 Selective α1 receptor
agonist  MAOI cause severe HTN

 Activates α1 receptor
 Increase IP3 causing
contraction of vascular
smooth m.

 Nasal & ocular decongestant


 Dilate pupil for opthalmoscopy
 Mydriasis w/o cycloplegia
 Paralysis of accommodation
Pilocarpine
 Antiglaucoma, sialogogue  Miosis
 Muscarinic receptor  Blurred vision
agonist  Accommodative spasm

 Activates muscarinic
receptors in ciliary m. &
salivary gland

 Sjogren’s syn
 Glaucoma
• Ciliary m. ↑ aqueous
humor
 Xerostomia
• Salivary gland ↑
salivation
Pralidoxime
 Organophosphate antidote
 Cholinesterase reactivator

 Binds phosphorous &


breaks organophosphate
bond w/ cholinesterase

 Organophosphate toxicity
 Reverses muscle weakness
Propranolol
 Sympatholytic,  Bronchoconstriction
antihypertensive  Inhibits glycogenolysis
 Nonselective β receptor  Nightmares & depression
antagonist

 Blocks β1 & β2 receptors

 Angina
 HTN
 Benign tremor
 Migraine prophylaxis
 thyrotoxicosis
 Post-MI

 Highly lipophilic  CNS


effects
Pseudoephedrine
 Decongestant  Tachycardia
 Indirect/direct-acting  CNS stim.
adrenergic receptor  ↑ BP
agonist
 MAOI cause severe HTN
 ↑ release NE directly
activates adrenergic
receptors causing
vasoconstriction &
cardiac stim.

 Allergic & viral rhinitis


Pyridostigmine
 Antimyasthenic  Muscarinic effects
 Cholinesterase  Miosis
 Salivation
inhibitor, cholinergic
agonist
 Prolongs effects of
succinylcholine
 Reversibly inhibits
cholinesterase

 Tx myasthenia gravis
 Reverse nondepolarizing
NM blockers
Rocuronium
 Paralytic agent  Respiratory m. paralysis
 Nondepolarizing NM blockade  Apnea

 Blocks nicotinic receptors in


skeletal m.

 Skeletal m. relaxation for


intubation, surgery, ECT

 Effects reversed by
neostigmine & edrophonium
Sildenafil
 Vasodilator  HA
 Phosphodiesterase  Nasal congestion
inhibitor  Back pain
 Visual disturbances
 Inhibits type 5
phosphodiesterase &
degradation of cGMP
 vasodilation in corpus
cavernosum d/t Ach
release from sacral PNS
neurons

 Erectile dysfunction
Succinylcholine
 Paralytic agent  Respiratory m. paralysis
 Depolarizing NM blockade  Apnea

 Binds nicotinic receptors


causing prolonged
depolarization of skeletal m.
& paralysis

 Skeletal m. relaxation for


intubation & surgery

 Transient m. fasciculations
Tamsulosin
 Urologic agent Dizziness
 Uroselective α1 HA
receptor antagonist Postural hypotension

 Blocks α1A Cimetidine increases


blood levels & effects
receptors in
prostate

Tx urinary outflow


obstruction d/t prostatic
hyperplasia
Terazosin
 Antihypertensive, 1st dose syncope
urologic agent
 Selective α1
receptor antagonist

 Blocks α1 receptors

HTN
Outflow obstruction d/t
prostate hyperplasia
Cardiovascular
 Acetazolamide Hydrochlorothiazide
 Adenosine  Labetalol
 Amiloride  Mannitol
 Amiodarone  Methyldopa
 Amlodipine  Minoxidil
 Carvedilol  Nesiritide
 Clonidine  Nitroglycerin
 Digoxin  Nitroprusside
 Diltiazem  Propafenone
 Dofetilide  Quinidine
 Enalapril  Sotalol
 Esmolol  Spironolactone
 Fenoldopam  Valsartan
 Furosemide  verapamil
 Hydralazine
Acetazolamide
 Diuretic  Parasthesia
 Carbonic anhydrase
inhibitor  Urinary stone formation

 Inhibits interconversion of
carbonic acid & bicarbonate
 ↑ NaHCO3 excretion
 Inhibit aqueous humor
formation
 Hyperchloremic metabolic
acidosis

 Tx open-angle glaucoma
 Mtn sickness
 Metabolic alkalosis
Adenosine
 Antiarrhythmic  Transient asystole
 Purine nucleoside,
cardiac node membrane
stabilizer

 Opens K channels &


blocks Ca influx in SA &
AV nodes
 Slows AV conduction
 ↑ AV refractory period

Terminate SVT
Amiloride
 K-sparring diuretic  Hyperkalemia
 Epithelial Na channel
blocker

 Blocks Na Channel
distal tubule &
collecting duct
 Inhibits Na reabsorption
& K excretion

 Prevent & Tx hypokalemia


Amidarone
 Antiarrhythmic  Hypo/hyperthyroidism
 Cardiac ion channel  Photosensitivity
blocker  Blue-gray skin
 Corneal microdeposits
 Pulmonary fibrosis
 Blocks K, Na, Ca
channels & β receptors
 Prolongs repolarization
 ↑ refractory period
 Slows HR
 ↑ PR & QT intervals

 SVT, VT, VF
Amlodipine
 Antihypertensive, HA
antianginal Edema
 Dihydropyridine Ca Hypotension
channel blocker

 Ca channel blocker in Effects ↑ w/ grapefruit


vascular smooth m. juice
Arteriolar vasodilation
& ↑ coronary blood
flow

HTN
Angina pectoris
Carvedilol
 Antihypertensive & heart Orthostatic hypotension
failure Tx Dizziness
 Nonselective Bradycardia
adrenergic receptor
agonist

 Blocks β1, β2, α1


receptors
Cause vasodilation

HTN
Heart failure
 ↓ remodeling
Clonidine
 Antihypertensive  Abrupt w/drawal 
 α2 receptor agonist severe rebound HTN
 Sedation
 Central α2 receptor agonist  Dry mouth
 ↓ sympathetic outflow from
vasomotor center
 Inhibits pain
neurotransmission in spinal
cord

 HTN
 Opioid w/drawal
Digoxin
 Cardiac stimulant  Arrhythmias
 Digitalis glycoside  N, V
 Blurred vision
 Inhibits Na/K ATPase  Yellow vision
 ↑ IC Ca & cardiac
contractility
 ↓ AV conduction
 ↑ AV refractory period

 Heart failure
 Serum levels assess
dosage & toxicity
Diltiazem
 Vasodilator, antiarrhythmic  Dizziness
 Non-dihydropyridine Ca  Hypotension
channel blocker  Peripheral edema
 Constipation
 Block Ca channels in cardiac
tissue & vascular smooth m.
 Gingival hyperplasia
 Vasodilation
 ↓ HR & conduction  Grapefruit juice ↑ serum
 ↓ contractility levels

 HTN
 Angina pectoris
 SVT
Dofetilide
 Antiarrhythmic  QT prolongation
 K channel blocker  Torsade de pointes

 Blocks delayed K channels


in cardiac tissue
 Slows repolarization &
prolongs refractory period
 ↑ QT interval

 AF, A flutter

 Monitor QT interval during


initial dose titration
Enalapril
 Antihypertensive  Cough & angioedema
 ACE inhibitor  Inhibits bradykinin
degradation
 Inhibits ACE & formation of AT
II  Hypotension
 Vasodilation  Taste disturbances
 ↓ aldosterone secretion
 ↑ CO
 ↓ V remodeling
 ↑ survival in heart failure

 HTN
 Heart failure
 Post-MI
 ↓ progression of diabetic
nephropathy
Esmolol
 Antiarrhythmic  Hypotension
 Class II
 Selective β1 blocker  Bradycardia

 Blocks SNS stim. SA & AV


nodes
 ↓ HR
 ↓ AV conduction
 ↑ AV refractory period

 Sinus tachycardia & SVT


during/after surgery

 Rapidly metabolized by plasma


esterase
Fenoldopam
 Antihypertensive ↓ serum K levels
 D1-like receptor agonist  Monitor for
hypokalemia

 D1 receptor agonist
 Arteriolar vasodilation
 Afferent & efferent renal
arterioles
 ↑ renal blood flow

 Hypertensive
emergencies
Furosemide
 Loop-acting diuretic  Hypokalemia
 Membrane ion transport  Metabolic alkalosis
inhibitor  Hyperuricemia
 Hypomagnesemia
 Inhibits Na/K/2Cl cotransporter
in ascending loop of Henle  ↑ ototoxicity of
 Blocks NaCl reabsorption aminoglycoside ABX
 Edema
 Heart failure
 HTN
 Hypercalcemia

 ↑ Ca excretion
 ↑ Na/K exchange in collecting duct
Hydralazine
 Antihypertensive. heart failure  Edema
 Vasodilator  Reflex tachycardia & MI
 Lupus syndrome
 Alters IC Ca metabolism
 Relaxes arteriolar smooth m.
 vasodilation
 ↓ afterload

 Heart failure in combo w/


isosorbide dinitrate
 More effective than ACEI in
black people
 Moderate-severe HTN
Hydrochlorothiazide
 Antihypertensive  Hypokalemia
 Thiazide diuretic  Metabolic alkalosis
 Hyperuricemia & gout
 Inhibits NaCl
 ↓ excretion of lithium
transporter in distal
tubule
 ↑ excretion Na, K, Cl
 ↓ Ca excretion

 HTN
 Nephrogenic DI
 Nephrolithiasis
Labetolol
 Antihypertensive Postural hypotension
Abrupt w/drawal
 Adrenergic α & β
cause life-threatening
receptor antagonist HTN, arrhythmias, or
MI
 Selective α1 &
nonselective β1, β2
blockers

HTN
Mannitol
 Diuretic  Electrolyte imbalances
 Osmotic Diuretic  Transient volume
expansion
 Pulmonary edema or
 Osmotic attraction of heart failure
edematous & ocular
fluid
 Filtered by glomerulus
 ↑ electrolyte excretion

 Oliguric renal failure


 Cerebral edema – ↑ ICP
 Acute glaucoma
Methyldopa
 Antihypertensive  Positive direct Coomb’s
 Adrenergic α2 receptor test
agonist

 Converted to active
form methyl-
norepinephrine which
activates central α2
receptor agonist
 ↓ SNS outflow from
vasomotor center

 HTN
 HTN in pregnancy
Minoxidil
 Antihypertensive, hair growth  Systemic admin.
stimulant  Reflex tachycardia
 Vasodilator, K channel  Angina pericarditis
opener  Pulmonary HTN
 hypertrichosis
 Opens K channels in
vascular smooth m.
 Hyperpolarization
 m. relaxation
 vasodilation
 Stim. resting hair follicle 
growth follicles

 Severe HTN
 Topical for alopecia
Nesiritide
 Heart failure Tx  Hypotension
 Recombinant human B-type
natriuretic peptide

 Activate guanylate cyclase


 ↑ cGaMP
 Dilates venous & arterial
smooth m.
 ↓ venous pressure, cardiac
preload, vascular
congestion, & dyspnea

 Decompensated heart failure


Nitroglycerin
 Antianginal  HA
 Organic nitrate  Hypotension
 Syncope
 Reflex tachycardia
 Releases NO in vascular
smooth m.
 Vasodilation  ↑ vasodilative effect of
 ↑ coronary blood flow sildenafil, tadalafil,
 ↓ myocardial O2 demand vardenafil

 Angina pectoris
 Sublingual or lingual admin.
 Short half-life
Nitroprusside
 Antihypertensive  CN toxicity
 Vasodilator  Hypotension
 HA
 Relaxes venous & arteriolar
smooth m.
 Metabolized to CN &
thiocyanate
 Tx toxicity w/ sodium nitrite
& sodium thiosulfate

 HTN crisis
 Acute heart failure or
cardiogenic shock
 Controlled hypotension during
pregnancy
Propafenone
 Antiarrhythmic  Proarrhythmic 1st 2 wks
 Class IC Na channel  Monitor ECG when
blocker starting Tx
 GI disturbances
 Blocks Na channel in
cardiac tissue  ↑ digoxin levels
↓ conduction & prevent
re-entry
↑ PR, QRS, & QT
duration

SVT & life-threatening


V arrhythmias
Quinidine
 Antiarrhythmic  Cinchonism
 Class IA Na channel  Blurred vision
blocker  Tinnitus
 Photophobia
 Blocks Na & K channels
in cardiac tissue  ↑ levels w/
↓ conduction  Amiodarone
↑ QRS & QT duration  Cimetidine
 Diltiazem
SVT & VT  Verapamil
D-isomer = quinine,  Grapefruit juice
used to treat malaria
pts
Sotalol
 Antiarrhythmic  Torsades de pointes
 Class III K channel blocker

 Blocks K channels in cardiac


tissue
 Prolongs repol.
 ↑ refractory period & ↑ QT
interval
 Blocks adrenergic β
receptors

 SVT & life-threatening


arrhythmias
Spironolactone
 K-sparring diuretic Gynecomastia
 Aldosterone antagonist Impotence
Hyperkalemia
 Blocks aldosterone
receptors
↑ Na excretion
↓ K excretion

Primary
hyperaldosteronism
HTN
hypokalemia
Valsartan
 Antihypertensive
 Angiotensin receptor
antagonist

 Blocks AT II receptor in
vascular smooth m. &
adrenal cortex
 Vasodilation & ↓ aldosterone
secretion

 HTN
 Nephropathy

 Less cough & angioedema


than ACEI
Verapamil
 Antihypertensive, antianginal  Peripheral edema
 Non-dihydropyridine Ca  Constipation
channel blocker
 Gingival hyperplasia
 Blocks Ca channels in cardiac
m. & vascular smooth m.
 Vasodilation
 ↓ HR & conduction
 ↓ contractility
 Suppress contractility more
than other Ca channel
blockers

 HTN
 Angina pectoris
 SVT
 Prevent migraine HA
CNS Depressants
 Buspirone  Lorazepam
 Carbamazepine  Phenobarbital
 Diazepam  Phenytoin
 Disulfiram  Topiramate
 Ethosuximide  Valproate
 Flumazeil  Zolpidem
 Gabapentin
 Lamotrigine
Busprione
 Antianxiety  Dizziness
 5-HT1A partial agonist  Drowsiness
 Fatigue
 HA
 Activates presynaptic 5-HT1A
receptors in dorsal raphe  Excitement
nucleus  Nervousness
 ↓ firing serotonergic neurons  Blurred vision
 Tachycardia
 Generalized anxiety disorder  N
 Rash
 NO  Myalgia
 Drug dependence  Sweating
 Significant sedation
 Muscle relaxation  ↑ levels by
 Anticonvulsant effects  Erythromycin
 Itraconazole
 Grapefruit juice
Carbamazepine
 Anticonvulsant  Ataxia
 Neuronal Na channel blocker  Drowsiness
 Blurred vision
 Blocks Na channels in CNS  Agranulocytosis
 Aplastic anemia
 ↓ firing of ectopic foci &
spread of epileptic seizures  Thrombocytopenia

 Partial seizures & generalized  Induces its own metabolism


tonic-clonic seizures
 Bipolar disorders
 Trigeminal neuralgia
 Neuropathic pain
Diazepam
 Antianxiety  Drowsiness
 Benzodiazepine  Lethargy
 Physical/psychological
dependence
 Binds ω receptors on GABA  Tolerance
operated Cl ion channel
 ↑ channel affinity for GABA &
frequency of channel opening
 Potentiates inhibitory effects of
GABA

 Anxiety
 Status epilepticus
 Muscle spasm
 Alcohol w/drawal
 Anterograde amnesia

 Long-lasting active metabolites


Disulfiram
 Alcohol abuse Tx  Drowsiness
 Acetaldehyde dehydrogenase
inhibitor

 Inhibits acetaldehyde
degradation following alcohol
ingestion
 Blurred vision
 Chest pain
 Dizziness
 Palpitations
 N, V
 HA
 Weakness

 Reinforcement of alcohol
abstinence
Ethosuximide
 Anticonvulsant  Dizziness
 Succimide  Drowsiness
 Gastric distress
 Binds T-type Ca N
channels in thalamic
neurons
Suppresses nerve
transmissions to
motor cortex

Generalized absence
seizures
 Petit mal epilepsy
Flumazenil
 Antidote  Seizures
 Benzodiazepine  Dizziness
receptor antagonist  Emotional lability

 Blocks benzodiazepine
receptors

 Counteract adverse
effects of
benzodiazepines
 Respiratory depression
d/t IV OD

 CI in status epilepticus
Gabapentin
 Anticonvulsant  Ataxia
 GABA analogue  Dizziness
 Drowsiness
 Nystagmus
 ↑ GABA release from
 Tremor
central neurons
 Inhibits neuronal
discharges from seizure
foci
 Inhibits pain
neurotransmission

 Partial seizures
 Chronic pain
 Migraine prophylaxis
Lamotrigine
 Anticonvulsant  Skin rash in 1st 8 wk of
Tx
 Phenyltriazine  Can progress to
Stevens-Johnson syn

 Blocks voltage-
 Ataxia
sensitive Na channels
 Dizziness
 Release of glutamate
 Drowsiness
 Prevents spread of  Photosensitivity
seizure foci discharges
 ↓ metabolism & ↑ ADR w/
 Adjunct/monotherapy for valproate
partial seizures in adults
Lorazepam
 Sedative-hypnotic, anxiolytic  Dizziness
 Drowsiness
 Benzodiazepine  Apnea & cardiac arrest w/ rapid IV
admin
 Binds benzodiazepine ω
receptors on GABA operate Cl  Additive depression w/ alcohol & other
depressants
ion channel
 ↑ channel affinity for GABA &
frequency of channel opening
 Potentiates inhibitory effects of
GABA

 Anxiety
 Insomnia
 Preoperative sedation
 Light anesthesia
 Anterograde amnesia

 Flumazenil used to counteract


severe OD
Phenobarbital
 Sedative-hypnotic,  Drowsiness
anticonvulsant  Lethargy
 Barbiturate  Delirium
 Hangover
 Physical & psychological
 Binds GABA operated Cl ion dependence
channel increasing duration
of channel opening  Induces CYP P450 ↑ metabolism
of drugs
 ↑ Cl influx in absence of
GABA

 Tonic-clonic & partial seizures


 Febrile seizures in children
 Preoperative sedation
 Short-term hypnotic

 ↑ folate requirement during


long-term Tx
Phenytoin
 Anticonvulsant  Ataxia
 Hydantoin  Diplopia
 Nystagmus
 Gingival hyperplasia
 Blocks voltage-sensitive Na
channels
 Release glutamate
 Prevents spread of seizure foci
discharges

 Partial seizures
 Generalized tonic-clone seizures
 Status epilepticus following IV
diazepam

 Zero-order @ high doses


 Fosphenytoin for IV use
Topiramate
 Anticonvulsant  Ataxia
 Monosaccharide derivative  Dizziness
 Drowsiness
 Block voltage-sensitive Na  Fatigue
channels  Impaired concentration &
memory
 Augments GABA activation
of GABA receptors  Psychomotor slowing
 Blocks glutamate  Speech problems
receptors  Diplopia
 Nystagmus
 Partial & tonic-clonic seizures

 Decrease dose in pts w/ renal


impairment
Valproate
 Anticonvulsant  Indigestion
 Branched-chain FA  N, V
 Dizziness
 ↑ GABA levels by ↑ release  Sedation
or ↓ metabolism or reuptake  Hepatotoxicity
 Reduced Na dependent
action potentials

 Simple & complex absence


seizures
 Complex partial seizures
 Tonic-clonic seizures
 Myoclonic seizures
 Migraine prevention
 Manic phase of bipolar
Zolpidem
 Non-benzodiazepine hypnotic
 Imidazopyridine

 Activates ω BZBP receptors


on GABA operated Cl ion
channel
 ↑ channel affinity for GABA
& frequency of channel
opening
 Neuronal
hyperpolarization

 Insomnia
Endocrine
 Acarbose  Insulin
 Alendronate  Levothyroxine
 Calcitonin  Medroxyprogesterone
 Danazol  Metformin
 Desmopressin  Methimazole
 Ergocalciferol  Mifepristone
 Ethinyl estradiol &  Octreotide
drospirenone  Oxytocin
 Ethinyl estradiol &  Pioglitazone
norethindrone  Prednisone
 Finasteride  Raloxifene
 Fludrocortisone  Repaglinide
 Glyburide  Somatropin
 Hydrocortisone  Testosterone
Acarbose
 Antidiabetic  Intestinal bloating
 α-glucosidase inhibitor  Flatulence

 Inhibits intestinal enzyme


that converts  ↑ oral bioavailability of
oligosaccharides & metformin
disaccharides to glucose  ↓ iron absorption
 ↓ digestion of starch &
sucrose
 ↓ postprandial blood
glucose & HbA1c

 Type II DM
Alendronate
 Bone resorption inhibitor  Absorption ↓ by Ca
 Bisphosphonate supplements, antacids,
foods, beverages (except
water)
 Prevents attachment of
osteoclast precursor cells to
bone
 ↓ metabolic activity of
osteoclasts & ability to
resorb bone

 Prevent/Tx
 Osteoporosis
 Corticosteroid-induced
osteoporosis
 Paget’s ds of bone
 hypercalcemia
Calcitonin
 Ca hormone
 Thyroid gland hormone

 Binds calcitonin receptor on


osteoclasts
 ↑ cAMP & inhibits osteoclast
activity
 ↓ bone resorption, bone
pain, & serum [Ca]

 Postmenopausal osteoporosis
 Paget’s ds of bone
 hypercalcemia
Danazol
 Ovarian inhibitor  CI in pregnancy –
 Synthetic androgen, androgenic effects on
antiestrogen female fetus

 Feedback inhibits pituitary


FSH & LH secretion ↓  Emotional lability
ovarian estrogen secretion &  Deepening voice
stim. endometrial & breast
tissue.  Acne
 Hirsutism
 Endometriosis  Amenorrhea
 Fibrocystic breast ds  ↓ breast size
 Hereditary angioedema
 ↑ C1 esterase inhibitor &
C4 complement
component
Desmopressin
 Posterior pituitary hormone
 Vasopressin, ADH analogue

 Mimics natural vasopression


 Increases water
reabsorption in kidneys
 Vasoconstriction

 DI
 Nocturnal enuresis
 Control bleeding in
hemophilia & wWF’s ds

 Intranasal, oral, or IV
Ergocalciferol
 Vit. D  Hypercalcemia
 Fat-soluble  Hypercalciuria

 Activated in liver & kidneys  Cholestyramine inhibits


to form calcitriol vit. D absorption
 ↑ Ca & phosphorus  Induce vit. D
absorption from gut
metabolism
 Vit. D deficiency  Phenytoin
 Rickets, osteomalacia  Barbiturates
 Chronic renal failure
 Familial hypophosphatemia
 Hypocalcemia d/t
hypoparathyroidism
 Postoperative & idiopathic
tetany
Ethinyl estradiol & drospirenone
 OCP  Drospirenone
 Estrogen & progesterone Antiandrogenic
Blocks aldosterone
 Feedback inhibit GnRH  ↓ salt & water retention
 Estrogen  ↓ BP
 ↓ FSH secretion &
maturation of dominant Thromboembolism
follicle
 ↑ risk w/ smoking
 Progesterone
 Inhibits midcycle LH Edema
surge & ovulation
Efficacy ↓ w/
 Contraception  ABX
 Regulate menstrual cycle  Carbamazepine
 Acne in women  phenytoin
Ethinyl estradiol & norethindrone
 OCP  Norethidrone
 Estrogen & progesterone
 Slightly androgenic

 Feedback inhibit GnRH


 Estrogen  Thromboembolism
 ↓ FSH secretion &  Edema
maturation of dominant
follicle  Depression
 Progesterone  Gallbladder ds
 Inhibits midcycle LH
surge & ovulation
 Contraception

 Regulate menstrual cycle


 Acne in women
Finasteride
 Androgen synthesis inhibitor  CI pregnancy
 5-α-reductase inhibitor  Risk to male fetus
 Do NOT handle tablets
 Inhibits conversion
testosterone 
dihydrotestosterone & ↓  Impotence
androgenic stimulation of
prostate & skin
 ↓ prostate size & promotes
hair growth

 BPH
 Male pattern baldness
Fludrocortisone
 Corticosteroid  Hypokalemia
 Mineralocorticoid  ↑ by thiazide & loop
diuretics
 Activates aldosterone
receptors in renal distal
tubule
 ↑ Na reabsorption
 ↑ K & H excretion

 Adrenal insufficiency
 Addison’s ds
 Congenital adrenogenital syn

 Tx idiopathic orthostatic
hypotension w/ ↑ Na intake
Glyburide
 Antidiabetic  Photosensitivity
 Sulfonylurea hypoglycemia  Hypoglycemia

 Closes ATP-sensitive K
channels preventing K efflux
& depolarizing pancreas B
cells
 Influx Ca & relaxing insulin
 ↑ amount of insulin secreted
during each pulse

 Type II DM
Hydrocortisone
 Short-acting corticosteroid,
low-potency topical
corticosteroid
 Glucocorticoid

 Replaces endogenous
cortisol in deficiency states
 Suppresses inflammation &
immune response – topical

 Adrenocortical insufficiency
 Topical
 Insect bites
 Contact dermatitis
Insulin
 Antidiabetic Hypoglycemia
 Pancreatic hormone
β-blockers mask signs
 Replaces endogenous of hypoglycemia &
insulin prolong recovery

 DM

 Rapid acting – lispro


 Intermediate acting –
lente
 Long acting – ultralente
Levothyroxine
 Thyroid hormone Insomnia
 Tetraiodothyronine Irritability
Tachycardia
 Binds nuclear receptors Wt loss
& ↑ gene transcription
 ↑ metabolic rate, protein
synthesis, Bile acid sequestrants ↓
gluconeogenesis, cell absorption
growth & differentiation,
& CNS development
 Converted to T3 in
tissues

 Hypothyroidism
Medroxyprogesterone
 Progestin, contraceptive  Amenorrhea
 Progesterone analogue  Breakthrough bleeding
 Dysmenorrhea
 ↓ endometrial hyperplasia in
women receiving estrogen
 Prevents conception by
thickening cervical mucus

 Estrogen-progestin HRT
 Injectable contraceptive
 Progestin-only injectable
contraceptive

 IM depot injection lasts 3mo


Metformin
 Antidiabetic  N, V, D
 Biguanide, antihyperglycemic
 Abdominal bloating
 ↑ # & affinity of insulin
receptors in peripheral tissues
 ↓ hepatic glucose output
 ↓glucose absorption from gut
 ↑ glucose uptake & utilization in
skeletal m. & adipose tissue

 Type II DM

 Used in combo w/ sulfonylureas


Methimazole
 Antithyroid Rash
 Thiourea, thyroid Agranulocytosis
hormone synthesis
inhibitor

 Inhibits peroxidase &


iodination & coupling of
tyrosine residue of
thyroglobulin
 ↓ thyroxine secretion

 Hyperthyroidism –
Grave’s ds
Mifepristone
 Abortificient  Abdominal pain
 Progesterone antagonist  Diarrhea
 N, V
 Partial agonist or antagonist
progesterone receptors  Uterine bleeding
 Cramping
 Medical termination of
pregnancy through 49d
gestation

 Single dose + prostaglandin


for 48hr stim. uterine
contractions
Octreotide
 GH inhibitor, antidiarrheal  Arrhythmias
 Somatostatin analogue w/  Hyperglycemia
greater effects on GH than  Hypoglycemia
insulin secretion  Constipation
 Diarrhea
 Suppresses secretion of GH,  Flatulence
insulin-like growth factors,
5-HT & GI peptides – gastrin,  N
motilin, secretin, & VIP

 Acromegaly
 Severe diarrhea & flushing d/t
carcinoid tumors & VIP
tumors
 Bleeding GE varices
 Complications of pancreatic
surgery
Oxytocin
 Oxytocic  Excessive & painful
 Posterior pituitary hormone uterine contractions

 Stim. Uterine smooth m. &


induce labor
 Stim. mammary gland
smooth m. & lactation

 Induce labor @ term


 Facilitate uterine contractions
 Postpartum control of uterine
bleeding
 Promote milk let-down

 IV for uterine stim.


 Nasal for milk let-down
Pioglitazone
 Antidiabetic
 Thiazolidinedione
antihyperglycemic

 Activates peroxisome
proliferator-activated receptor-γ
in adipose tissue, skeletal m., &
liver
 ↑ gene transcription, insulin
sensitivity, & glucose
transports in muscle & adipose
tissue
 Suppresses hepatic glucose
output

 Type II DM

 Used w/ metformin
Prednisone
 Anti-inflammatory  Depression or euphoria
 Corticosteroid  HTN
 Acne
 Suppresses  Impaired wound healing
inflammation & immune
response  Adrenal suppression
 Muscle wasting
 Inflammatory, allergic,  Osteoporosis
autoimmune, & neoplastic  Cushingoid appearance
ds
 Moon facies
 Prevent organ transplant
rejection  Buffalo hump
 Asthma  ↑ susceptibility to infection
Raloxifene
 Bone resorption inhibitor  Hot flashes
 Selective estrogen receptor
modulator – SERM  Cholestyramine inhibits
absorption
 Estrogen-like effect on bone
& lipid metabolism
 Estrogen antagonist in
breast & uterine tissue
 ↑ bone mineral density & ↓
vertebral fractures

 Osteoporosis in
postmenopausal women

 Used in woman @ risk for


breast cancer
Repaglinide
 Antidiabetic  Hypoglycemia
 Meglitinide hypoglycemic

 Closes ATP-sensitive K
channels & ↑ insulin
secretion
 ↓ postprandial blood
glucose & [HbA1c]

 Taken before meals to control


postprandial hyerglycemia

 Used w/ metformin
 NOT sulfonylureas
Somatropin
 GH
 Recombinant somatotropin

 ↑ release of insulin-like
growth factors in liver &
cartilage
 Stim. skeletal growth, AA
transport, protein synthesis,
nucleic acid synthesis & cell
prolif.

 Short stature in children d/t


GH deficiency
 Turner syn
 Chronic renal failure
 Prader-Will syn
Testosterone
 Androgen  Edema
 Gonadal steroid  Acne
 Gynecomastia
 Activated gene transcription &
development of male sex organs &  Impotence
secondary sex characteristics  Oligospermia
 ↑ lean body mass  Priapism
 Stim. skeletal growth
 Accelerates epiphyseal closure
 ↑ sebaceous gland sebum
production
 ↑ EPO secretion
 ↓ HDL levels

 Hypogonadism in androgen-deficient
men
 Delayed puberty in males
Gastrointestinal
 Bisacodyl  Misoprostol
 Calcium carbonate  Omeprazole
 Dicyclomine  Ondansetron
 Docusate  Promethazine
 Lactulose  Ranitidine
 Loperamide  Sucralfate
 Mesalamine  Tegaserod
 Metoclopramide
Bisacodyl
 Stimulant laxative Cramping
N
Fluid & electrolyte
 Inhibits GI fluid depletion
reabsorption &  Hypokalemia
stimulates
peristalsis

Bowel evacuation prior


colonoscopy or surgery
Acute constipation
Calcium carbonate
 Antacid, Ca supplement  Constipation
 Ca salt
 ↓ absorption of drugs
 Tetracyclines
 Neutralizes gastric acid
 Fluoroquinolones
 Provides Ca  Phenytoin
supplementation  Iron salts

 Dyspepsia
 Hypocalcemia
 Prevention of osteoporosis

 Admin 1-1.5hr after meals &


@ bedtime
Dicyclomine
 Antispasmodic  Constipation
 Muscarinic receptor  Dyspepsia
antagonist  Dry mouth
 Urinary retention
 Blurred vision
 Blocks PNS stim.
intrinsic nervous  Decreased sweating
system & ↓ GI tone &
motility
 Directly relaxes GI
smooth m.

 IBS – cramping & pain


Docusate
 Stool softener, laxative
 Surface-active agent

 Facilitates hydration of
fecal material & softens
feces

 Constipation
 Fecal impaction – rectal
enema
Lactulose
 Laxative  Cramping
 Osmotic agent  Abdominal distention
 Flatulence
 ↑ water content & softens
feces
 Lowers pH of colon
 Converts ammonia 
ammonium ion & ↓ ammonia
absorption & blood levels

 Chronic constipation
 Hepatic encephalopathy
 Improves mental status
Loperamide
 Antidiarrheal  Constipation
 Opioid analogue  Drowsiness

 Additive effects
 Activates opioid receptors in GI  Kava
smooth m.  Chamomile
 Segmental contraction & inhibits  Valerian
peristalsis

 Mild-moderate acute diarrhea


 Chronic diarrhea d/t IBD
 ↓ volume of ileostomy drainage

 AVOID
 Pregnancy
 Lactation
 Children < 2 y/o
Mesalamine
 GI anti-inflammatory
 Salicylate – 5-ASA

 Inhibits prostaglandin synthesis


& migration of inflammatory
cells into bowel wall
 Scavenges superoxide-free
radicals

 IBD
 UC
 Proctitis

 Sulfasalazine  mesalamine &


sulfapyridine
Metoclopramide
 Promotility & antiemetic  CI in Parkinson’s ds & seizure
 D2 receptor antagonist disorders

 Drowsiness
 Blocks relaxant effect of D on  EPS rxns
GI smooth m.  restlessness
 Blocks presynaptic D receptors
& ↑ Ach release & stim. smooth
m.
 Blocks D2 receptors in
chemoreceptor trigger zone &
vomiting center

 Chemotherapy-induced emesis
 Gastric stasis – postsurgical &
diabetic
 GE reflux
Misoprostol
 Cytoprotective  CI in pregnancy
 Synthetic PGE1
analogue  Abdominal pain
D
 Miscarriage
 ↓ gastric mucosal
secretion & ↑ secretion
of bicarbonate & mucus

 Prevent gastric mucosal


injury from NSAIDs
 Abortificient in combo w/
mifepristone
Omeprazole
 Antiulcer  Abdominal pain
 Proton pump inhibitor
 Inhibits metabolism
 Diazepam
 Irreversibly inhibits H/K ATP
 Cyclosporine
pump in gastric parietal cells
 Phenytoin
 Prevents gastric acid
secretion

 Peptic ulcer ds
 GE reflux
 Zollinger-Ellison syn
 dyspepsia
Ondansetron
 Antiemetic  HA
 5-HT3 receptor antagonist  Constipation
D
 Blocks 5-HT3 receptors in GI
vagal afferent nerves,
solitary tract nucleus, &
chemoreceptor trigger zone

 Prevent N, V from
chemotherapy & radiation
therapy
 Postoperative N, V
Promethazine
 Antiemetic, antihistamine,  Neuroleptic malignant syn
sedative
 H1 receptor antagonist,  Sedation
phenothiazine  Confusion
 Disorientation
 Blocks H1 & M1 receptors
 Inhibits stim. chemoreceptor
trigger zone & vomiting
center

 N, V
 Preoperative sedation
 Allergic rxns
Ranitidine
 Antiulcer
 H2 receptor antagonist

 Blocks H2 receptors in
gastric parietal cells
 ↓ gastric acid secretion

 Peptic ulcer ds
 GE reflux
 Dyspepsia
Sucralfate
 Antiulcer  Constipation
 Cytoprotective, sulfated
polysaccharide  ↓ absorption
 Fat soluble vitamins
 fluoroquinolones
 Adheres ulcer crater & forms
protective barrier
 Prevents acid secretion &
pepsin hydrolysis of mucosal
proteins
 Stim. prostaglandin synthesis

 Peptic ulcer ds
 GE reflux
 Prevent NSAID-induced gastric
injury
Tegaserod
 GI motility agent  Diarrhea
 Partial agonist @ 5-HT4  Ischemic colitis
receptors

 Activates 5-HT4
receptors on sensory
neurons in enteric
nervous system
 Release
neurotransmitters & ↑
peristalsis

 IBS in women w/
constipation
Hematologic
 Abciximab  Epoetin
 Alteplase  Eptifibatide
 Aspirin  Ezetimibe
 Atorvastatin  Filgrastim
 Bivalirudin  Folic acid
 Cholestyramine  Gemfibrozil
 Cilostazol  Heparin
 Clopidogrel  Niacin
 Cyclosporine  Sirolimus
 Enoxaparin  Warfarin
Abciximab
 Antithrombotic  Bleeding
 Monoclonal Ab  Thrombocytopenia

 Inactivates platelet gp
llb/llla receptors
 Prevents platelet
aggregation

 Prevent thrombosis during


coronary angioplasty &
stent placement
Alteplase
 Thrombolytic  Reperfusion arrhythmia
 Plasminogen activator
 Contraindications
 Internal bleeding
 Converts plasminogen 
 Recent CNS surgery or
plasmin trauma
 Degrades fibrin & fibrinogen

 AMI
 Acute ischemic stroke
 Occluded central venous
access devices

 Streptokinase & urokinase for


pulmonary embolism
Atorvastatin
 Cholesterol lowering agent  Myalgia
 HMG-CoA reductase  Myositis
inhibitor  Rhabdomyolysis
 Hepatitis
 HMG-CoA reductase, rate-  GI distress
limiting enzyme for
cholesterol  Effects ↑ w/
 ↑ hepatic cholesterol uptake  Grapefruit juice
 ↓ LDL levels  Azole antifungals
 cyclosporine
 Hypercholesterolemia

 Cholesterol-lowering effects ↑
w/ ezetimibe & bile acid-
binding agents
Bivalirudin
 Anticoagulant  Bleeding
 Hirudin analogue

 Inhibits thrombin
 Prevents blood coagulation

 Thrombosis in unstable
angina
 AMI
 Stent insertion

 Used in pts w/ heparin-


induced thrombocytopenia
Cholestyramine
 Cholesterol-lowering  Constipation
agent  Abdominal discomfort
 Bile-acid binding resin

 Binds intestinal bile


acids
 Prevents reabsorption
 ↑ cholesterol utilization
 ↓ LDL levels

 Hypercholesterolemia
 Diarrhea d/t excess bile
acids
Cilostazol
 Antiplatelet  HA
 Platelet aggregation
inhibitor  Effects ↑ w/ CYP3A4 inhibitors
 Azole antifungals
 Inhibits phosphodiesterase  Erythromycin
III & ↑ cAMP in platelet &  Grapefruit juice
blood vessels
 Inhibit platelet aggregation
 Causes vasodilation

 Intermittent claudication
 Improves blood flow &
walking distance

 Additive effects w/ aspirin


Clopidogrel
 Antiplatelet  Hypersensitivity reaction
 Platelet aggregation
inhibitor

 Irreversibly inhibits binding


of ADP to platelet receptors
 ↓ gp IIb/IIIa mediated
aggregation

 Stroke
 MI
 Peripheral vascular ds

 Additive effects w/ aspirin


Cyclosprine
 Immunosuppressant  HTN
 IL2 expression inhibitor  Nephrotoxic
 Gingival hyperplasia
 Hirsutism
 Bind immunophilins
 Tremor
 Complex binds
calcineurin  inhibits
transcription of IL2  Induce metabolism
gene  Rifampin
 Barbiturates
 Prevent rejection of renal,  Carbamazepine
cardiac or hepatic
allografts  Inhibits metabolism
 Severe RA & psoriasis  Grapefruit juice
Enoxaparin
 Parenteral anticoagulant  Thrombocytopenia
 LMWH

 Binds/potentiates antithrombin
III on factor Xa

 Prevent
 DVT
 Pulmonary embolism after
knee, hip, or abdominal surgery
 Thrombosis in unstable angina
& non Q-wave MI

 Effects reversed w/ protamine


sulfate
 NO monitoring w/ PTT
Epoetin
 Hematopoietic growth factor  HTN
 Recombinant human EPO

 Binds receptors on erythroid


progenitor cells & stim. cell
maturation & prolif.
 Reticulocytosis & ↑ Hct

 Anemia d/t
 CRF
 Chemotherapy
 Zidovudine therapy
 Hematologic malignancy
• lymphoma

 Used as performance-enhancing
drug by athletes
Eptifibatide
 Antiplatelet
 GP IIb/IIIa receptor  Bleeding
antagonist

 Reversibly inhibits
fibrinogen binding to gp
IIb/IIIa receptors
 Prevents platelet
aggregation

 Prevent coronary thrombosis


in
 Unstable angina or non-ST
segment elevation MI
 Coronary angioplasty or
stent placement
Ezetimibe
 Cholesterol-lowering agent
 Cholesterol absorption inhibitor

 Disrupts annexin-caveolin
complex mediating cholesterol
transport intestinal brush
border
 Inhibits absorption of biliary
dietary cholesterol

 Pro-drug converted to active


glucuronide metabolite

 Hypercholesterolemia

 Additive effect w/ statins


Filgrastim
 Hematopoietic growth factor  Bone pain
 Recombinant human GCSF

 Binds receptors on myeloid


progenitor cells & stim.
maturation & prolif.
 Accelerates neutrophil recovery
after myelosuppressive
chemotherapy
 ↓ infection incidence

 Neutropenia assoc/ w/
chemotherapy & bone marrow
transplants

 Avoid 24 hrs prior & after


chemotherapy
Folic acid
 Vitamin, hematologic agent  Absorption ↓ by
 Metabolic cofactor for DNA  Phenytoin
synthesis  Cholestyramine

 Activated folate transfer  Folate reductase inhibited by


MTX
one-carbon units to purine &
pyrimidine precursors

 Megaloblastic anemia
 Fetal neural tube defects
 Coronary artery ds

 Pregnant woman have ↑


requirements
Gemfibrozil
 Lipid-lowering agent  GI distress
 Fibric acid derivative  Myositis

 Activates peroxisome  Statins ↑ risk


rhabdomyolisys
proliferator activated
receptor-α
 Oxidizes FA & apo-AI & AII
 ↓ plasma triglycerides
 ↑ HDL

 Hypertriglyceridemia
 ↓ HDL levels

 Monitor LFTs throughout Tx


Heparin
 Parenteral anticoagulant Thrombocytopenia
 Antithrombotic

 Binds/potentiates antithrombin
III
 ↑ inactivation factor Xa &
thrombin

 Venous thromboembolism
 Pulmonary embolism
 AF w/ embolism
 Consumptive coagulopathies
 In vitro & catheter coagulation

 Monitor PTT
 Protamine sulfate for OD
Niacin
 Vitamin, lipid-lowering agent  Flushing
 G-protein coupled receptor  Pruritis
ligand  GI distress, peptic ulcer
 Hyperglycemia
 Activates G-protein coupled  Hepatotoxicity
receptor
 Inhibits lipolysis & release  Statins ↑ risk
of FA rhabdomyolysis
 ↓ hepatic triglyceride
synthesis & VLDL secretion

 Hypertriglyceridemia
 ↑ HDL
 Hypercholesterolemia
 Pellagra
Sirolimus
 Immunosuppressant  Leukopenia
 T-lymphocyte inhibitor  Thrombocytopenia
 Hyperlipidemia
 Rash
 Inhibits regulatory
kinase in cytokine-
driven T-cell prolif.  ↑↑ blood levels
 Cyclosporine
 Combo w/ corticosteroid
& cyclosporine  Azole antifungals
 Erythromycin
 Grapefruit juice
 Prevent  Cimetidine
 Rejection renal allograph
 Coronary stent
restenosis
Warfarin
 Oral anticoagulant  Fetal malformations
 Coumarin vit. K antagonist  Abnormal bone
development
 Inhibits reduction of
oxidized vit. K
 Prevents vit. K dependent
carboxylation of glutamate
residues of factors II, VII, IX,
X, proteins C & S

 Delayed onset d/t circulating


coagulation factors

 Monitor INR
 Give vit. K if bleeding
Musculoskeletal
 Acetaminophen  Indomethacin
 Allopurinol  Infliximab
 Celecoxib  Ketorolac
 Cyclobenaprine  Probenecid &
 Etanercept colchicine
 Ibuprofen
Acetaminophen
 Analgesic, antipyretic  OD cause fatal hepatic failure
 COX-3 inhibitor
 ↑ hepatotoxicity w/ alcohol
 ↑ renal toxicity w/ salicylates &
 Inhibits COX-3 selectively
NSAIDs
 Inhibits synthesis of PG
causing pain & fever

 Mild-moderate pain
 Fever

 Lacks anti-inflammatory &


antiplatelet activity
Allopurinol
 Antigout  Rash
 Xanthine oxidase
inhibitor  Inhibits metabolism
 Mercaptopurine
 Inhibits xanthine
oxidase & catabolism of
purines  xanthine &
uric acid
 ↓ uric acid levels

 Prevent hyperuricemia &


gout
Celecoxib
 NSAID  GI bleeding
 COX-2 inhibitor  ↑ risk stroke & MI

 Inhibits COX-2 &


synthesis of PG
causing pain, fever, &
inflammation

 OA
 RA
 Inflammatory jt ds
Cyclobenzaprine
 Skeletal m. relaxant  Dizziness
 Tricyclic central-acting  Drowsiness
m. relaxant  Dry mouth

 AVOID MAOI
 Acts on brainstem &
spinal cord to reduce
tonic somatic m.
activity via γ & α motor
neurons

 Acute muscle spasm


Etanercept
 Antirheumatic agent,  URI
antitumor necrosis factor  HA
 Antitumor necrosis
factor – p57 combined  ↓ Ab response to live
w/ Fc of IgG virus vaccines

 Binds TNF-α & ↓ jt


inflammation & pain
 Slows progression of
RA

 RA
Ibuprofen
 NSAID  GI bleeding
 Nonselective COX inhibitor  N, V
 Dyspepsia
 Inhibits COX-1 & COX-2 &  Allergic rxns
synthesis of PG causing  Hepatitis & renal failure
pain, fever, & inflammation

 Mild-moderate pain or
dysmenorrhea
 Inflammatory disorders
 OA
 RA

 ↓ risk colon, breast, lung, &


prostate cancers
Indomethacin
 NSAID  GI bleeding
 Nonselective COX inhibitor  N, V
 Dyspepsia
 Allergic rxns
 Inhibits COX-1 & COX-2
 Dizziness
 Drowsiness
 Inflammatory disorders
 HA
 Gouty arthritis
 OA
 RA
 Ankylosing spondylitis
 PDA in premature neonates
Infliximab
 Ds modifying  Fatigue
antirheumatic  N, V
 Monoclonal Ab to TNF-  URI
α

 Inactivates TNF-α & ↓ jt


inflammation, pain, &
destruction
 ↓ Sx of Crohn’s ds

 RA
 Crohn’s ds
Ketorolac
 NSAID  Aspirin-allergy
 Nonselective COX inhibitor  Allergic rxn in pt w/ asthma
 Nasal polyps
 Inhibits COX-1 & COX-2 &
synthesis of PG causing
pain, fever, & inflammation

 Short-term pain management

 Prolongs bleeding time


 Limit use to < 5d
Probenecid & Colchicine
 Antigout  Probenecid
 Uricosuric – probenicid  Inhibits renal tubular secretion
of Penicillins
 Anti-inflammatory – colchicine
 Used to ↑ penicillin serum
levels
 Probenecid  Colchicine
 Inhibits renal reabsorption of  D
uric acid & ↑ uric acid secretion  N, V
 Colchicine  Agranulocytosis & aplastic
 Inhibits leukocyte response to anemia
monosodium urate crystals in jt

 Acute gouty arthritis


 Prevent gouty arthritis
Neurodegenerative
 Baclofen  Levodopa-carbidopa
 Benztropine  Memantine
 Donepezil  Pergolide
 Entacapone  Selegiline
 Interferon-beta-1b
Baclofen
 Antispasticity  Drowsiness
 GABA-B receptor agonist  Dizziness
 Fatigue
 ↓ neuronal cAMP & Ca  Weakness
influx
 ↑ K influx  Additive effects
 Alcohol
 ↓ motor neuron excitability
& inhibits spinal reflexes  Kava
 Valerian
 Chamomile
 Spasticity
 MS
 Spinal cord injury
 ALS
Benztropine
 Anti-Parkinson  Blurred vision
 Central anticholinergic  Dry eyes
 Constipation
 Dry mouth
 Blocks cholinergic
receptors & restores  Urinary retention
neurotransmitter balance
in basal ganglia

 Parkinson’s ds
 Drug-induced EPS

 ↓ tremor > bradykinesia &


rigidity
Donepezil
 Anti-Alzheimer  N, D
 Cholinesterase inhibitor  HA

 Inhibits cholinesterase in
CNS
 ↑ Ach neurotransmission
 Slows decline in cognitive
function

 Alzheimer’s ds

 Does NOT prevent ds


progression
Entacapone
 Anti-Parkinson  Rhabdomyolysis
 Neuroleptic malignant syndrome
 Catechol-O-
methyltransferase inhibitor

 Inhibits catechol-o-
methyltransferase
inactivation of levodopa
 ↑ levodopa in CNS
 Prolongs response to levodopa &
↓ S/Sx Parkinson’s ds

 Adjunct to levodopa/carbidopa for


Parkinson’s ds

 AVOID nonselective MAOI


Interferon-beta-1b
 Anti-multiple sclerosis  HA
 Interferon  Weakness
 GI distress
 Sweating
 Binds cell surface  Neutropenia
receptors producing  Myalgia
immuno-suppressive  Chills
effects  Fever
 ↓ relapse & slows
physical disability in MS

 Relapsing-remitting MS

 SubQ daily
Levodopa-carbidopa
 Anti-Parkinson  Dyskinesia – involuntary movements
 Dopamine precursor,  N, V
decarboxylase inhibitor  Hallucinations

 ↑ arrhythmia w/ halothane
 Levodopa
 Converted to D in CNS
 Augments neurotransmission in
basal ganglia
 Carbidopa
 Inhibits peripheral dopa-
decarboxylase
 ↑ levodopa availability in CNS

 Parkinson’s ds

 HTN crisis w/ MAOI


Memantine
 Anti-Alzheimer
 Glutamate antagonist

 Glutamate NMDA
receptor antagonist
 Prevent excitotoxic
effects of glutamate
causing neuronal loss
 Slows decline in
cognitive function

 Alzheimer’s ds
Pergolide
 Anti-Parkinson  Dyskinesia
 Dopamine receptor  Hallucination
agonist  Orthostatic hypotension
 Constipation

 Activates D receptors
in basal ganglia

 Parkinson’s ds in
conjunction w/
levodopa/carbidopa
Selegiline
 Anti-Parkinson  AVOID
 Meperidine & opioids
 Type B MAOI • Fatal rxn
• Excitation
• Rigidity
• HTN
 Converted to active form • coma
by MAO  SSRI
 Irreversibly inhibits D • Serotonin syn
 Tricyclics
degradation by MAO • Asystole
 ↑ response to • HTN
levodopa/carbidopa Tx • Syncope
• Rigidity
• seizures
 Parkinson’s ds w/
levodopa/carbidopa

 Slows progression of
Parkinson’s ds
Other Drugs
 Alprostadil  Latanoprost
 Bosentan  Mesna
 Epoprostenol  Succimer
Alprostadil
 Vasodilator  IV infusion
 Prostaglandin E1  Apnea
 Hypotension
 Arrhythmia
 Activates PG EP receptors
 Local products
 Vascular smooth m.
 Prolonged/painful erection
relaxation & vasodilation
 lightheadedness

 Maintain PDA in neonates


awaiting surgery
 IV infusion
 Male erectile dysfunction
 Local injection or pellets
Bosentan
 Vasodilator  CI in pregnancy
 Endothelin-1 receptor  Causes birth defects
antagonist
 ↑ serum aminotransferase
levels
 Blocks endothelin A & B
receptors
 ↓ pulmonary vascular
resistance & dyspnea
 Improves walking distance

 Pulmonary arterial HTN


Epoprostenol
 Vasodilator  Flushing
 Naturally occurring  Hypotension
prostacyclin (PGI2)  Tachycardia
 Diarrhea
 Activated prostaglandin IP  N, V
receptors
 Vascular smooth m.
relaxation
 ↑ pulmonary blood flow &
reduces dyspnea

 Pulmonary arterial HTN


Latanoprost
 Ocular hypotensive agent  Alters color of iris causing
 Prostaglandin F2α analogue permanent eye color change
by ↑ amount of melanin in
melanocytes
 Activates prostaglandin FP
receptors
 ↑ aqueous humor outflow via
uveoscleral pathways
 Lowers intraocular pressure

 Chronic open-angle glaucoma

 Topical ocular admin


Mesna
 Antidote
 Sulfhydryl compound

 Detoxifies urotoxic
metabolites acrolein of
ifosfamide &
cyclophosphamide

 Hemorrhagic cystitis d/t


ifosfamide &
cyclophosphamide
Succimer
 Antidote
 Metal chelating agent –
dimercaptosuccinic
acid

 Chelates lead
 Water-soluble chelates
to excreted in urine
 ↓ blood lead levels
Psychotherapeutics
 Amitriptyline
 Amphetamine &  Methylphenidate
dextroamphetamine  Mirtazapine
 Atomoxetine  Olanzapine
 Buproprion  Phenelzine
 Desipramine  Risperidone
 Fluoxetine  Thioridazine
 Haloperidol  Venlafaxine
 Lithium
Amitriptyline
 Antidepressant  Lethargy
 Sedation
 Tricyclic  Blurred vision
 Constipation
 Blocks neuronal reuptake of  Urinary retention
serotonin > norepinephrine  ↑ appetite & wt gain
 Blocks muscarinic & α-
adrenergic receptors  OD wide QRS complex VT

 Altered effects by drugs that


 Chronic pain inhibit/induce CYP450
 Depression  Carbamazepine
 Quinidine
 Rifampin
 Delayed onset of antidepressant
effect >4 wks

 AVOID
 MAOI
 SSRI
Amphetamine
 CNS stimulant  Tachycardia
 HTN
 Sympathomimetic  Anorexia
amine  Irritability
 Insomnia
 ↑ neuronal release of  Tremor
norepinephrine  Growth inhibition
 Drug dependence

 ADHD  HTN crisis w/ MAOI


 ↑ attention span
 ↓ motor restlessness
 Narcolepsy
 ↑ mental alertness
 ↓ drowsiness & fatigue
Atomoxetine
 ADHD agent  ↓ appetite
 Selective NE reuptake  Insomnia
inhibitor
 Levels & effects altered by
drugs that inhibit/induce
 Inhibits neuronal CYP2D6
reuptake of NE in CNS

 ADHD in children/adults

 ↑ levels & effect in slow


metabolizers – CYP2D6
Bupropion
 Antidepressant  Agitation
 Neuronal reuptake  HA
inhibitor  Dry mouth
N
 Inhibits neuronal  Tremor
reuptake of DA > 5-HT &  Impaired motor &
NE cognitive skills

 Depression  MAOI ↑ adverse effects


 Smoking cessation  Seizure risks w/
phenothiazines
 Delayed onset for
antidepressant effects
Desipramine
 Antidepressant  Lethargy
 Tricyclic  Sedation
 Blurred vision
 Constipation
 Blocks neuronal reuptake NE >
5-HT  Urinary retention
 ↑ appetite & wt gain
 Blocks muscarinic & α-
adrenergic receptors
 OD wide QRS complex VT
 Depression
 Chronic pain

 Delayed onset for antidepressant


effects

 AVOID
 MAOI
 SSRI
Fluoxetine
 Antidepressant  Anxiety
 SSRI  Drowsiness
 Insomnia
 Nervousness
 Inhibits neuronal reuptake of  Sexual dysfunction
serotonin
 Sweating
 Tremor
 Depression
 OCD  ↑ levels metabolized by CYP2D6
 Bulimia nervosa
 Anorexia nervosa
 Fibromyalgia
 Panic attacks
 Phobias
 Prementsrual dysmorphic disorder

 Active metabolite 5-7d half-life


 AVOID MAOI
Haloperidol
 Typical antipsychotic  Neuroleptic malignant syn
 Fever
 Butyrophenone
 Respiratory distress
 Tachycardia
 Blocks D2 receptors in  Seizures
mesolimbic area,  Severe m. stiffness
chemoreceptor trigger  Altered BP
zone, solitary tract, &  Extrapyramidal rxns
basal ganglia  Tardive dyskinesia
 Blocks muscarinic & α-  Blurred vision
adrenergic receptors  Constipation
 Dry mouth
 Urinary retention
 Psychotic disorders
 Hypotension
 Schizophrenia
 Tourette’s syn
Lithium
 Mood stabilizer, antimanic  Polyuria
 Impaired memory
 Inorganic cation  Acne
 Tremor
 ↓ noradrenergic  ECG changes
neurotransmission or effects  GI distress
b/c of ↓ cAMP  Hypothyroidism
 Inhibition of inositol-1-  Leukocytosis
phosphatase
 NM toxicity w/ haloperidol
 Depletion of inositol & IP3  ↑ toxicity
 Improved Na transport via Na  Diuretics
pump  NSAIDS
 Fluoxetine
 Bipolar affective disorder

 Monitor serum levels


 Toxicity > 2.5
Methyphenidate
 CNS stimulant  Tachycardia
 Sympathomimetic  HTN
amine  Anorexia
 Irritability
 ↑ neuronal release NE  Insomnia
 Tremor
 ADHD  Growth inhibition
 ↑ attention span
 Dependence
 ↓ motor restlessness
 Narcolepsy
 ↑ mental alertness  HTN crisis w/ MAOI
 ↓ drowsiness & fatigue
Mirtazapine
 Antidepressant  ↑ appetite & wt gain
 Constipation
 Tetracyclic  Dry mouth
 Drowsiness
 Inhibits presynaptic α2
autoreceptors &
heteroreceptors
 ↑ NE & 5-HT release

 Depression
 Appetite stimulation

 AVOID MAOI
 HTN, seizure, death
Olanzapine
 Atypical antipsychotic  Agitation
 Thienobenzodiazepine  Dizziness
 Restlessness
 Sedation
 Blocks D2 & 5-HT2 receptors in
CNS  Amblyopia
 Orthostatic hypotension
 Blocks H1, muscarinic, & α-
adrenergic receptors  Tachycardia
 Constipation
 Dry mouth
 Schizophrenia
 Wt gain
 Manic episodes of biploar
 Tremor
 Anorexia nervosa

 Oral tablets contain aspartame


 Avoid in phenylketonuria
Phenelzine
 Antidepressant  Dizziness
 MAOI  Insomnia
 Restlessness
 Blurred vision
 Inhibits MAO & ↑ CNS levels of
NE & 5-HT  Orthostatic hypotension
 Diarrhea
 Neurotic & atypical depression
 Potentially fatal
 SSRI
 Avoid  Tricyclics
 Fluoxetine
 Tyramine
 HTN crisis
 Tyramine
 Amphetamines
 Methyldopa
 Levodopa
Risperidone
 Atypical antipsychotic  Aggressive behavior
 Benzisoxazole  Extrapyramidal rxns
 Sleep disturbances
 Insomnia
 Blocks 5-HT2 > D2  Sedation
receptors in CNS  Constipation or diarrhea
 Blocks H1 & α-adrenergic  Wt gain
receptors

 Schizophrenia
 Psychotic disorders

 Monitor pt for neuroleptic


malignant syn
Thioridazine
 Typical antipsychotic  Extrapyramidal rxns
 Phenothiazine  Tardive dyskinesia
 Photosensitivity
 Potential for V
 Blocks D2 receptors in arrhythmias & sudden
mesolimbic area, death
chemoreceptor trigger  Retinal pigmentation w/
zone, solitary tract, & high doses
basal ganglia  melanosis
 Blocks muscarinic
receptors

 Psychotic disorders
 Schizophrenia
Venlafaxine
 Antidepressant  Sexual dysfunction
 Phenethylamine  GI distress
 Dizziness
 Insomnia
 Inhibits neuronal
 Nervousness
reuptake 5-HT & NE

 Depression
 Generalized anxiety
disorder

 AVOID MAOI
Respiratory
 Albuterol  Montelukast
 Cromolyn  Omalizumab
 Diphenhydramine  Salmeterol
 Fluticasone  Theophylline
 Ipratropium  Zileuton
 Loratadine
Albuterol
 Bonchodilator  Muscle tremor
 β2 receptor agonist  Nervousness
 Restlessness
 Activates β2 receptors in  Tachycardia
bronchial smooth m.
 ↑ cAMP  activating kinases  HTN crisis w/ MAOI
 Inhibiting myosin
phosphorylase  m. relaxation

 Asthma
 Acute bronchospasm
 Prevent exercise-induced
asthma
 Chronic bronchitis & emphysema
 Reversible airway obstruction
Cromolyn
 Antiasthmatic & antiallergy  Nasal & throat irritation
 Mast cell stabilizer

 Prevents Ca influx &


stabilizes mast cell &
eosinophil membranes
 Prevents degranulation &
release of histamine,
leukotrienes

 Asthma prophylaxis
 Exercise-induced
bronchospasm
 Allergic disorders

 Oral or nasal inhalation


Diphenhydramine
 Antihistamine, sedative,  Drowsiness
antiemetic  Blurred vision
 H1 receptor antagonist  Dry mouth
 Urinary retention
 Anorexia
 Blocks H1 & muscarinic
receptors
 Prevents histamine-
induced allergic rxns
 Prevents vestibular stim.
of vomiting center
 Sedation

 Allergic rxns
 Prevent motion sickness
 Insomnia
Fluticasone
 Anti-inflammatory  Nasal & throat irritation
 Corticosteroid  Oral candidiasis

 Inhibits cytokine production


by Thelper cells
 Prevents mediator release
from mast cells, basophils,
eosinophils
 Stabilizes lysosomal
membranes
 Vasoconstriction & ↓
capillary permeability

 Allergic rhinitis
 Chronic nasal inflammation
 Chronic asthma
Ipratropium
 Bronchodilator  Cough
 Muscarinic receptor  Nasal dryness & irritation
antagonist

 Blocks muscarinic receptors


in bronchial smooth m. &
nasal mucosa
 Prevents vagal-stimulated
bronchoconstriction

 COPD
 Rhinitis
 Asthma

 Inhalation admin
Loratadine
 Antihistamine
 H1 receptor antagonist

 Blocks H1 receptors in
nasal mucosa
 Prevents allergic rxns

Seasonal rhinitis
Chronic idiopathic
urticaria

Less sedating than


diphenhydramine
Montelukast
 Antiasthmatic
 Leukotriene antagonist

 Blocks cysteinyl leukotriene-


1 receptor for leukotrienes
C4, D4, E4
 Prevent airway inflammation,
edema, bronchoconstriction,
& secretion viscous mucus
 Inhibits early/late phase
bronchoconstriction

 Long-term asthma control

 Oral admin
Omalizumab
 Antiasthmatic Allergic rxns
 IgE antagonist  anaphylaxis

 Blocks IgE

Severe asthma in
combo w/ corticosteroid
therapy

SubQ every 2-4 wks


Salmeterol
 Bronchodilator  Tachycardia
 β2 agonist  Nervousness
 HA
 ↑ cAMP
 Relaxes bronchial smooth
m.
 Inhibits late phase allergen-
induced
bronchoconstriction

 Asthma
 Prevent nocturnal attacks
 Exercise-induced asthma

 NOT acute bronchospasm

 Inhalation admin
Theophylline
 Bronchodilator  N, V
 Methylxanthine  Anxiety
 Insomnia
 Inhibits phosphodiesterase  Tachycardia
isoenzymes & ↑ cAMP
 Relaxes bronchial smooth m.
 Inhibits T-lymphocyte proliferation
& cytokine production

 Chronic asthma
 Obstructive pulmonary ds
 Neonatal apnea – respiratory stim.

 Half-life
 Shorter in smokers & children
 Longer in elderly
 Monitor blood levels
Zileuton
 Antiasthmatic Flu-like syn
 Leukotriene synthesis HA
inhibitor Drowsiness
Dyspepsia
↑ serum
 Inhibits 5-lipoxygenase aminotransferase levels
& leukotriene synthesis & hepatitis
 Prevents airway
inflammation &
Inhibits CYP450 & 3A4
bronchoconstriction
 ↑ theophylline &
warfarin levels
 Long-term asthma control
Psychotherapeutics
 Amitriptyline
 Amphetamine &  Methylphenidate
dextroamphetamine  Mirtazapine
 Atomoxetine  Olanzapine
 Buproprion  Phenelzine
 Desipramine  Risperidone
 Fluoxetine  Thioridazine
 Haloperidol  Venlafaxine
 Lithium
Amitriptyline
 Antidepressant  Lethargy
 Tricyclic  Sedation
 Blurred vision
 Constipation
 Blocks neuronal reuptake of  Urinary retention
serotonin > norepinephrine  ↑ appetite & wt gain
 Blocks muscarinic & α-
adrenergic receptors  OD wide QRS complex VT

 Chronic pain  Altered effects by drugs that


inhibit/induce CYP450
 Depression • Carbamazepine
• Quinidine
• Rifampin
 Delayed onset of
antidepressant effect >4 wks

 AVOID
• MAOI
• SSRI
Amphetamine
 CNS stimulant  Tachycardia
 Sympathomimetic  HTN
amine  Anorexia
 Irritability
 Insomnia
 ↑ neuronal release of  Tremor
norepinephrine  Growth inhibition
 Drug dependence
 ADHD
• ↑ attention span  HTN crisis w/ MAOI
• ↓ motor restlessness
 Narcolepsy
• ↑ mental alertness
• ↓ drowsiness & fatigue
Atomoxetine
 ADHD agent  ↓ appetite
 Selective NE reuptake  Insomnia
inhibitor
 Levels & effects altered by
drugs that inhibit/induce
 Inhibits neuronal CYP2D6
reuptake of NE in CNS

 ADHD in children/adults

 ↑ levels & effect in slow


metabolizers – CYP2D6
Bupropion
 Antidepressant  Agitation
 Neuronal reuptake  HA
inhibitor  Dry mouth
 N
 Inhibits neuronal  Tremor
reuptake of DA > 5-HT  Impaired motor &
& NE
cognitive skills
 Depression
 MAOI ↑ adverse effects
 Smoking cessation
 Seizure risks w/
phenothiazines
 Delayed onset for
antidepressant effects
Desipramine
 Antidepressant  Lethargy
 Tricyclic  Sedation
 Blurred vision
 Blocks neuronal reuptake NE  Constipation
> 5-HT  Urinary retention
 Blocks muscarinic & α-  ↑ appetite & wt gain
adrenergic receptors
 OD wide QRS complex VT
 Depression
 Chronic pain

 Delayed onset for


antidepressant effects

 AVOID
• MAOI
• SSRI
Fluoxetine
 Antidepressant  Anxiety
 SSRI  Drowsiness
 Insomnia
 Inhibits neuronal reuptake of  Nervousness
serotonin  Sexual dysfunction
 Sweating
 Depression  Tremor
 OCD
 Bulimia nervosa  ↑ levels metabolized by CYP2D6
 Anorexia nervosa
 Fibromyalgia
 Panic attacks
 Phobias
 Prementsrual dysmorphic disorder

 Active metabolite 5-7d half-life


 AVOID MAOI
Haloperidol
 Typical antipsychotic  Neuroleptic malignant
 Butyrophenone syn
• Fever
• Respiratory distress
 Blocks D2 receptors in • Tachycardia
mesolimbic area, • Seizures
chemoreceptor trigger • Severe m. stiffness
zone, solitary tract, & • Altered BP
basal ganglia  Extrapyramidal rxns
 Blocks muscarinic & α-  Tardive dyskinesia
adrenergic receptors  Blurred vision
 Constipation
 Psychotic disorders  Dry mouth
• Schizophrenia  Urinary retention
 Tourette’s syn  Hypotension
Lithium
 Mood stabilizer, antimanic  Polyuria
 Inorganic cation  Impaired memory
 Acne
 Tremor
 ↓ noradrenergic  ECG changes
neurotransmission or effects  GI distress
b/c of ↓ cAMP  Hypothyroidism
 Inhibition of inositol-1-  Leukocytosis
phosphatase
 Depletion of inositol & IP3  NM toxicity w/ haloperidol
 Improved Na transport via Na  ↑ toxicity
• Diuretics
pump • NSAIDS
• Fluoxetine
 Bipolar affective disorder

 Monitor serum levels


• Toxicity > 2.5
Methyphenidate
 CNS stimulant  Tachycardia
 Sympathomimetic  HTN
amine  Anorexia
 Irritability
 ↑ neuronal release NE  Insomnia
 Tremor
 ADHD
 Growth inhibition
• ↑ attention span
• ↓ motor restlessness  Dependence
 Narcolepsy
• ↑ mental alertness  HTN crisis w/ MAOI
• ↓ drowsiness &
fatigue
Mirtazapine
 Antidepressant  ↑ appetite & wt gain
 Tetracyclic  Constipation
 Dry mouth
 Drowsiness
 Inhibits presynaptic α2
autoreceptors &
heteroreceptors
 ↑ NE & 5-HT release

 Depression
 Appetite stimulation

 AVOID MAOI
• HTN, seizure, death
Olanzapine
 Atypical antipsychotic  Agitation
 Thienobenzodiazepine  Dizziness
 Restlessness
 Blocks D2 & 5-HT2 receptors  Sedation
in CNS  Amblyopia
 Blocks H1, muscarinic, & α-  Orthostatic hypotension
adrenergic receptors  Tachycardia
 Constipation
 Schizophrenia  Dry mouth
 Manic episodes of biploar  Wt gain
 Anorexia nervosa  Tremor

 Oral tablets contain


aspartame
• Avoid in phenylketonuria
Phenelzine
 Antidepressant  Dizziness
 MAOI  Insomnia
 Restlessness
 Inhibits MAO & ↑ CNS levels  Blurred vision
of NE & 5-HT  Orthostatic hypotension
 Diarrhea
 Neurotic & atypical
depression  Potentially fatal
• SSRI
 Avoid • Tricyclics
• Fluoxetine
• Tyramine  HTN crisis
• Tyramine
• Amphetamines
• Methyldopa
• Levodopa
Risperidone
 Atypical antipsychotic  Aggressive behavior
 Benzisoxazole  Extrapyramidal rxns
 Sleep disturbances
 Blocks 5-HT2 > D2  Insomnia
receptors in CNS  Sedation
 Blocks H1 & α-adrenergic  Constipation or diarrhea
receptors  Wt gain

 Schizophrenia
 Psychotic disorders

 Monitor pt for
neuroleptic malignant
syn
Thioridazine
 Typical antipsychotic  Extrapyramidal rxns
 Phenothiazine  Tardive dyskinesia
 Photosensitivity
 Blocks D2 receptors in  Potential for V
arrhythmias & sudden
mesolimbic area, death
chemoreceptor trigger
zone, solitary tract, &  Retinal pigmentation
w/ high doses
basal ganglia • melanosis
 Blocks muscarinic
receptors

 Psychotic disorders
 Schizophrenia
Venlafaxine
 Antidepressant  Sexual dysfunction
 Phenethylamine  GI distress
 Dizziness
 Inhibits neuronal  Insomnia
reuptake 5-HT & NE  Nervousness

 Depression
 Generalized anxiety
disorder

 AVOID MAOI
Respiratory
 Albuterol  Montelukast
 Cromolyn  Omalizumab
 Diphenhydramine  Salmeterol
 Fluticasone  Theophylline
 Ipratropium  Zileuton
 Loratadine
Albuterol
 Bonchodilator  Muscle tremor
 β2 receptor agonist  Nervousness
 Restlessness
 Tachycardia
 Activates β2 receptors in
bronchial smooth m.
 ↑ cAMP  activating kinases  HTN crisis w/ MAOI
 Inhibiting myosin
phosphorylase  m. relaxation

 Asthma
 Acute bronchospasm
 Prevent exercise-induced asthma
 Chronic bronchitis & emphysema
 Reversible airway obstruction
Cromolyn
 Antiasthmatic & antiallergy  Nasal & throat irritation
 Mast cell stabilizer

 Prevents Ca influx & stabilizes


mast cell & eosinophil
membranes
 Prevents degranulation &
release of histamine,
leukotrienes

 Asthma prophylaxis
 Exercise-induced bronchospasm
 Allergic disorders

 Oral or nasal inhalation


Diphenhydramine
 Antihistamine, sedative,  Drowsiness
antiemetic  Blurred vision
 H1 receptor antagonist  Dry mouth
 Urinary retention
 Blocks H1 & muscarinic  Anorexia
receptors
 Prevents histamine-induced
allergic rxns
 Prevents vestibular stim. of
vomiting center
 Sedation

 Allergic rxns
 Prevent motion sickness
 Insomnia
Fluticasone
 Anti-inflammatory  Nasal & throat irritation
 Corticosteroid  Oral candidiasis

 Inhibits cytokine production by


Thelper cells
 Prevents mediator release from
mast cells, basophils,
eosinophils
 Stabilizes lysosomal membranes
 Vasoconstriction & ↓ capillary
permeability

 Allergic rhinitis
 Chronic nasal inflammation
 Chronic asthma
Ipratropium
 Bronchodilator  Cough
 Muscarinic receptor antagonist  Nasal dryness & irritation

 Blocks muscarinic receptors in


bronchial smooth m. & nasal
mucosa
 Prevents vagal-stimulated
bronchoconstriction

 COPD
 Rhinitis
 Asthma

 Inhalation admin
Loratadine
 Antihistamine
 H1 receptor antagonist

 Blocks H1 receptors in nasal


mucosa
 Prevents allergic rxns

 Seasonal rhinitis
 Chronic idiopathic urticaria

 Less sedating than


diphenhydramine
Montelukast
 Antiasthmatic
 Leukotriene antagonist

 Blocks cysteinyl leukotriene-1


receptor for leukotrienes
C4, D4, E4
 Prevent airway inflammation,
edema, bronchoconstriction, &
secretion viscous mucus
 Inhibits early/late phase
bronchoconstriction

 Long-term asthma control

 Oral admin
Omalizumab
 Antiasthmatic  Allergic rxns
 anaphylaxis
 IgE antagonist

 Blocks IgE

 Severe asthma in combo w/


corticosteroid therapy

 SubQ every 2-4 wks


Salmeterol
 Bronchodilator  Tachycardia
 β2 agonist  Nervousness
 HA
 ↑ cAMP
 Relaxes bronchial smooth m.
 Inhibits late phase allergen-
induced bronchoconstriction

 Asthma
 Prevent nocturnal attacks
 Exercise-induced asthma

 NOT acute bronchospasm

 Inhalation admin
Theophylline
 Bronchodilator  N, V
 Methylxanthine  Anxiety
 Insomnia
 Tachycardia
 Inhibits phosphodiesterase
isoenzymes & ↑ cAMP
 Relaxes bronchial smooth m.
 Inhibits T-lymphocyte proliferation
& cytokine production

 Chronic asthma
 Obstructive pulmonary ds
 Neonatal apnea – respiratory stim.

 Half-life
 Shorter in smokers & children
 Longer in elderly
 Monitor blood levels
Zileuton
 Antiasthmatic  Flu-like syn
 Leukotriene synthesis  HA
inhibitor  Drowsiness
 Dyspepsia
 ↑ serum aminotransferase
 Inhibits 5-lipoxygenase levels & hepatitis
& leukotriene synthesis
 Prevents airway  Inhibits CYP450 & 3A4
inflammation &  ↑ theophylline &
bronchoconstriction warfarin levels

 Long-term asthma control

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