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Pharmacology Flash Cards 2017
Pharmacology Flash Cards 2017
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
Vascular HA
Migraine & cluster
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
Moderate-severe pain
Prevention of opioid abuse
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
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
Topical anesthetic
Pain
Itching
Inflammation
Burns
Insect bites
Contact dermatitis
Wounds
General anesthetic
Anesthesia
Minor surgical & diagnostic
procedures
Children
Lidocaine
Local anesthetic Cross-reactivity w/ amide-type
Amide-type anesthetics
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
NO analgesic effect
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
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
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
Infection d/t
• Pneumococci, gonococci,
meningococci, H. influenzae,
Moraxella catarrhalis,
Borrelia burgdorferi
HIV in combo w/
nucleoside reverse
transcriptase inhibitor –
synergistic
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
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
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
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
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
Community-acquired
pneumonia
UTI
Gynecologic & skin infections
Malaria
Chloroquine-
susceptible/resistant trains
of P. falciparum & P. vivax
Amebiasis, giardiasis,
trichomoniasis
Balantidium coli, C.
difficile, B. fragilis
Mupirocin
ABX
Protein synthesis inhibitor
Antiviral
Neuraminidase
inhibitor
Influenza A & B
Paromomycin
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
Schistosomiasis
Chinese liver fluke
Lung fluke
Cestodes – tapeworms
Primaquine
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
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
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
HIV in combo w/
nucleoside reverse
transcriptase inhibitor
Streptomycin
Aminoglycoside Nephrotoxic
Protein synthesis inhibitor Ototoxic
• ↑ w/ loop diuretics
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
Herpetic keratitis
Keratoconjunctivitis
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
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
CML
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
Hodgkin’s ds
Lymphomas, myeloma
Leukemia
Ovarian & breast tumors
RA
Acute leukemia
CML
Lymphomas
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
Reversible
cholinesterase
inhibitor
Irreversible α receptor
Hypotension w/ β
antagonist blockers & Ca channel
blockers
α receptor antagonist
α1 > α2
Blocks α1 & α2
receptors
Control BP during
surgical removal of
pheochromocytoma
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
Organophosphate toxicity
Reverses muscle weakness
Propranolol
Sympatholytic, antihypertensive Bronchoconstriction
Nonselective β receptor Inhibits glycogenolysis
antagonist Nightmares & depression
Angina
HTN
Benign tremor
Migraine prophylaxis
thyrotoxicosis
Post-MI
Tx myasthenia gravis
Reverse nondepolarizing
NM blockers
Rocuronium
Paralytic agent Respiratory m. paralysis
Nondepolarizing NM Apnea
blockade
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
Transient m. fasciculations
Tamsulosin
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
– Terminate SVT
Amiloride
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
– HTN
– Angina pectoris
Carvedilol
– HTN
– Heart failure
↓ remodeling
Clonidine
– HTN
– Opioid w/drawal
Digoxin
– 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
– AF, A flutter
– HTN
– Heart failure
– Post-MI
– ↓ progression of diabetic nephropathy
Esmolol
Antiarrhythmic – Hypotension
Class II
Selective β1 blocker – Bradycardia
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
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
Selective α1 &
nonselective β1, β2
blockers
– HTN
Mannitol
– 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
– 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 – 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
– Primary hyperaldosteronism
– HTN
– hypokalemia
Valsartan
Antihypertensive
Angiotensin receptor antagonist
Blocks AT II receptor in
vascular smooth m. & adrenal
cortex
– Vasodilation & ↓ aldosterone
secretion
– HTN
– Nephropathy
– 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
– Anxiety
– Status epilepticus
– Muscle spasm
– Alcohol w/drawal
– Anterograde amnesia
• Blocks benzodiazepine
receptors
– 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
– Partial seizures
– Generalized tonic-clone seizures
– Status epilepticus following IV
diazepam
– 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
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
DI
Nocturnal enuresis
Control bleeding in hemophilia
& wWF’s ds
Intranasal, oral, or IV
Ergocalciferol
Vit. D Hypercalcemia
Fat-soluble Hypercalciuria
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
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
BPH
Male pattern baldness
Fludrocortisone
Corticosteroid Hypokalemia
Mineralocorticoid ↑ by thiazide & loop diuretics
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
Adrenocortical insufficiency
Topical
Insect bites
Contact dermatitis
Insulin
Antidiabetic Hypoglycemia
Pancreatic hormone
β-blockers mask signs of
hypoglycemia & prolong
Replaces endogenous recovery
insulin
DM
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
Type II DM
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
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
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
Closes ATP-sensitive K
channels & ↑ insulin secretion
↓ postprandial blood glucose &
[HbA1c]
Used w/ metformin
NOT sulfonylureas
Somatropin
GH
Recombinant somatotropin
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
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
AVOID
Pregnancy
Lactation
Children < 2 y/o
Mesalamine
GI anti-inflammatory
Salicylate – 5-ASA
IBD
UC
Proctitis
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
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
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
Inactivates platelet gp
llb/llla receptors
Prevents platelet
aggregation
AMI
Acute ischemic stroke
Occluded central venous
access devices
Cholesterol-lowering effects ↑
w/ ezetimibe & bile acid-
binding agents
Bivalirudin
Anticoagulant Bleeding
Hirudin analogue
Inhibits thrombin
Prevents blood coagulation
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
Stroke
MI
Peripheral vascular ds
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
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
Disrupts annexin-caveolin
complex mediating cholesterol
transport intestinal brush border
Inhibits absorption of biliary
dietary cholesterol
Hypercholesterolemia
Neutropenia assoc/ w/
chemotherapy & bone marrow
transplants
Megaloblastic anemia
Fetal neural tube defects
Coronary artery ds
Hypertriglyceridemia
↓ HDL levels
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
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
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
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
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
• Parkinson’s ds
• Drug-induced EPS
Inhibits cholinesterase in
CNS
• ↑ Ach neurotransmission
• Slows decline in cognitive
function
• Alzheimer’s ds
Inhibits catechol-o-
methyltransferase
inactivation of levodopa
• ↑ levodopa in CNS
• Prolongs response to levodopa
& ↓ S/Sx Parkinson’s ds
• 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
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
• Detoxifies urotoxic
metabolites acrolein of
ifosfamide &
cyclophosphamide
• 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
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
Moderate-severe pain
Prevention of opioid abuse
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
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
Topical anesthetic
Pain
Itching
Inflammation
Burns
Insect bites
Contact dermatitis
Wounds
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
Anesthesia
Minor surgical & diagnostic
procedures
Children
Lidocaine
Local anesthetic Cross-reactivity w/ amide-type
Amide-type anesthetics
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
NO analgesic effect
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
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
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
Infection d/t
Pneumococci, gonococci,
meningococci, H. influenzae,
Moraxella catarrhalis, Borrelia
burgdorferi
Binds reverse
transcriptase & disrupts
catalytic site
Drug-resistant HIV
Erythromycin
Macrolide ABX Activates motilin receptors
causing uncoordinated
Protein synthesis inhibitor peristalsis
Anorexia
Binds 50s ribosome N, V
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
Inhibits enopyruvyl
transferase & addition of
phosphenolpyruvate to N-
acetylglucosamine to
form N-acetylmuramic
acid
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
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
TB
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
Community-acquired pneumonia
UTI
Gynecologic & skin infections
Malaria
Chloroquine-
susceptible/resistant trains of
P. falciparum & P. vivax
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
UTI
E. coli, S.
saprophyticus
Oseltamivir
Antiviral
Neuraminidase inhibitor
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
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
Ascariasis
Hookworm & pinworm
Quinine
Antimalarial Abdominal cramps
4-aminoquinoline Diarrhea
V
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
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
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
Herpetic keratitis
Keratoconjunctivitis
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
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
CML
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
Hodgkin’s ds
Lymphomas, myeloma
Leukemia
Ovarian & breast tumors
RA
Acute leukemia
CML
Lymphomas
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
Reversible
cholinesterase
inhibitor
Irreversible α
Hypotension w/ β
receptor antagonist blockers & Ca channel
blockers
α receptor
antagonist
α1 > α2
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.
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
Organophosphate toxicity
Reverses muscle weakness
Propranolol
Sympatholytic, Bronchoconstriction
antihypertensive Inhibits glycogenolysis
Nonselective β receptor Nightmares & depression
antagonist
Angina
HTN
Benign tremor
Migraine prophylaxis
thyrotoxicosis
Post-MI
Tx myasthenia gravis
Reverse nondepolarizing
NM blockers
Rocuronium
Paralytic agent Respiratory m. paralysis
Nondepolarizing NM blockade Apnea
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
Transient m. fasciculations
Tamsulosin
Urologic agent Dizziness
Uroselective α1 HA
receptor antagonist Postural hypotension
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
Terminate SVT
Amiloride
K-sparring diuretic Hyperkalemia
Epithelial Na channel
blocker
Blocks Na Channel
distal tubule &
collecting duct
Inhibits Na reabsorption
& K excretion
SVT, VT, VF
Amlodipine
Antihypertensive, HA
antianginal Edema
Dihydropyridine Ca Hypotension
channel blocker
HTN
Angina pectoris
Carvedilol
Antihypertensive & heart Orthostatic hypotension
failure Tx Dizziness
Nonselective Bradycardia
adrenergic receptor
agonist
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
AF, A flutter
HTN
Heart failure
Post-MI
↓ progression of diabetic
nephropathy
Esmolol
Antiarrhythmic Hypotension
Class II
Selective β1 blocker Bradycardia
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
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
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
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
Primary
hyperaldosteronism
HTN
hypokalemia
Valsartan
Antihypertensive
Angiotensin receptor
antagonist
Blocks AT II receptor in
vascular smooth m. &
adrenal cortex
Vasodilation & ↓ aldosterone
secretion
HTN
Nephropathy
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
Anxiety
Status epilepticus
Muscle spasm
Alcohol w/drawal
Anterograde amnesia
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
Partial seizures
Generalized tonic-clone seizures
Status epilepticus following IV
diazepam
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
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
Postmenopausal osteoporosis
Paget’s ds of bone
hypercalcemia
Danazol
Ovarian inhibitor CI in pregnancy –
Synthetic androgen, androgenic effects on
antiestrogen female fetus
DI
Nocturnal enuresis
Control bleeding in
hemophilia & wWF’s ds
Intranasal, oral, or IV
Ergocalciferol
Vit. D Hypercalcemia
Fat-soluble Hypercalciuria
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
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
Type II DM
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
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
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
Closes ATP-sensitive K
channels & ↑ insulin
secretion
↓ postprandial blood
glucose & [HbA1c]
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.
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
Dyspepsia
Hypocalcemia
Prevention of osteoporosis
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
AVOID
Pregnancy
Lactation
Children < 2 y/o
Mesalamine
GI anti-inflammatory
Salicylate – 5-ASA
IBD
UC
Proctitis
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
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
AMI
Acute ischemic stroke
Occluded central venous
access devices
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
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
Stroke
MI
Peripheral vascular ds
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
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
Disrupts annexin-caveolin
complex mediating cholesterol
transport intestinal brush
border
Inhibits absorption of biliary
dietary cholesterol
Hypercholesterolemia
Neutropenia assoc/ w/
chemotherapy & bone marrow
transplants
Megaloblastic anemia
Fetal neural tube defects
Coronary artery ds
Hypertriglyceridemia
↓ HDL levels
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
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
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
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
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
Parkinson’s ds
Drug-induced EPS
Inhibits cholinesterase in
CNS
↑ Ach neurotransmission
Slows decline in cognitive
function
Alzheimer’s ds
Inhibits catechol-o-
methyltransferase
inactivation of levodopa
↑ levodopa in CNS
Prolongs response to levodopa &
↓ S/Sx Parkinson’s ds
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
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
Detoxifies urotoxic
metabolites acrolein of
ifosfamide &
cyclophosphamide
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
AVOID
MAOI
SSRI
Amphetamine
CNS stimulant Tachycardia
HTN
Sympathomimetic Anorexia
amine Irritability
Insomnia
↑ neuronal release of Tremor
norepinephrine Growth inhibition
Drug dependence
ADHD in children/adults
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
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
Schizophrenia
Psychotic disorders
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
Asthma prophylaxis
Exercise-induced
bronchospasm
Allergic disorders
Allergic rxns
Prevent motion sickness
Insomnia
Fluticasone
Anti-inflammatory Nasal & throat irritation
Corticosteroid Oral candidiasis
Allergic rhinitis
Chronic nasal inflammation
Chronic asthma
Ipratropium
Bronchodilator Cough
Muscarinic receptor Nasal dryness & irritation
antagonist
COPD
Rhinitis
Asthma
Inhalation admin
Loratadine
Antihistamine
H1 receptor antagonist
Blocks H1 receptors in
nasal mucosa
Prevents allergic rxns
Seasonal rhinitis
Chronic idiopathic
urticaria
Oral admin
Omalizumab
Antiasthmatic Allergic rxns
IgE antagonist anaphylaxis
Blocks IgE
Severe asthma in
combo w/ corticosteroid
therapy
Asthma
Prevent nocturnal attacks
Exercise-induced asthma
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
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
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
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
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
Asthma prophylaxis
Exercise-induced bronchospasm
Allergic disorders
Allergic rxns
Prevent motion sickness
Insomnia
Fluticasone
Anti-inflammatory Nasal & throat irritation
Corticosteroid Oral candidiasis
Allergic rhinitis
Chronic nasal inflammation
Chronic asthma
Ipratropium
Bronchodilator Cough
Muscarinic receptor antagonist Nasal dryness & irritation
COPD
Rhinitis
Asthma
Inhalation admin
Loratadine
Antihistamine
H1 receptor antagonist
Seasonal rhinitis
Chronic idiopathic urticaria
Oral admin
Omalizumab
Antiasthmatic Allergic rxns
anaphylaxis
IgE antagonist
Blocks IgE
Asthma
Prevent nocturnal attacks
Exercise-induced asthma
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