Janeirah Q.

Manalundong – Mamowalas, RN
Assistant Professor IV
College of Health Sciences
Mindanao State University – Marawi City
Chemotherapeutic Drugs
§ Drugs used to destroy both organisms that invade the body and abnormal cells
within the body.
§ Affect cells by altering cellular function or
§ Disrupting cellular integrity causing cell death or
§ Preventing cellular reproduction eventually leading to cell death.

§ Anti-Infectives
§ Antineoplastics

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Anti-Infectives
§ Drugs designed to target foreign organisms that have invaded and infected the
body of a human host.

Antineoplastics
§ Drugs used for treating diseases caused by abnormal human cells such as cancers.
§ Specifically affect human cells to cause cell death or
§ Prevent cell growth and reproduction

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§ Bactericidal
§ Substance that causes the death of the bacteria

§ Bacteriostatic
§ Substance that prevent the replication of bacteria

§ Prophylaxis
§ Treatment to prevent an infection before it occurs

§ Resistance
§ Ability of pathogens over time to adapt to an anti-infective to produce cells that
are no longer affected by a particular drug
§ Spectrum
§ Range of bacteria against which antibiotic is effective
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1. Antibiotics
2. Antivirals
3. Antifungals
4. Antiprotozoals
5. Anthelminthics

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§Do not possess total selective toxicity.
§No anti-infective drug has yet been
developed that does not affect the host.

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GOALS:
§ Interference with the normal function of the invading
organism to prevent it from reproducing
§ To cause cell death without affecting host cells.

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ACTION EFFECT DRUGS

Inhibition of cell-wall synthesis Bactericidal effect Penicillins, Cephalosporins

Alteration in membrane Bacteriostatic or bactericidal Some antibiotics, antifungals,

permeability effect. antiprotozoals

Inhibition of protein synthesis Bacteriostatic or bactericidal Aminoglycosides, macrolides,

chloramphenicol

Inhibition of synthesis of Leads to inability to divide and cell Fluroquinolones

bacterial RNA and DNA death

Interference with cellular Bacteriostatic effect Sulfonamides, antimycobacterial

metabolism drugs, trimethoprim-
sulfamethoxazole

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§ Anti-infectives vary in spectrum.
Narrow spectrum
§ Selective action, are effective against only a few microorganisms
Broad spectrum
§ Interfere with biochemical reactions in many different kinds of microorganisms
§ Useful in treatment of a wide variety of infections
“cidal”
§ Cause death of the cells the drugs affect
“static”
§ Interference with the ability of the cells to reproduce or divide.

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GOAL of therapy:
§ Reduction of the population of invading organism to a point at which the human
immune response can take care of the infection.
§ If a person is immunocompromised for any reason à immune system may be
incapable of dealing effectively with the invading organisms.
Treatment in such patients is difficult due to the following:
§ Anti-infective drugs cannot totally eliminate the pathogen without causing severe
toxicity in the host
§ These patients do not have inflammatory or immune response in place to deal with
even a few invading organisms.

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§ Refers to the ability over time to adapt to an anti-infective drug and produce cells
that are no longer affected by a particular drug.
§ Innate resistance of microorganisms should be anticipated when prescribing a
drug for treatment.
Microorganisms develop resistance in the following:
§ Producing enzyme that deactivates the antimicrobial drug.
§ Changing cellular permeability to prevent the drug from entering the cell.
§ Altering binding sites on the membranes or ribosomes which then longer accept
the drug.
§ Producing a chemical that acts as an antagonist to the drug.

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§ Important to limit the use of antimicrobial agents to the treatment of specific
pathogens.
§ Drug dosing.

§ Duration of the drug use.

§ Being cautious about indiscriminate use of anti-infectives.
§ Ex.: antibiotics are not effective in the treatment of viral infections.

§ Doses should be high enough and long enough to eradicate even slightly resistance
microorganisms.
§ Around-the-clock dosing eliminates the peaks and valleys in drug concentration and
helps maintain a constant therapeutic level.

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Anti-infective agents are used to:
ü Treat systemic infections
ü Prophylaxis

TREATMENT OF SYSTEMIC INFECTIONS

§ Identification of pathogen
§ Done by culturing a tissue sample from the infected area.

§ Sensitivity of the pathogen

§ Sensitivity testing on cultured microbes to evaluate bacteria and determine which drugs
are capable of controlling the particular microorganism
§ Combination therapy

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COMBINATION THERAPY
§ Used for the following reasons:
üEncourage use of smaller dose of each drug, leading to fewer
adverse effects.
üSome drugs are synergistic.
üMany microbial infection are caused by >1 organism, and each
pathogen may react to a different anti-infective agent.
üCombined effects may delay the emergence of resistant strains.

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PROPHYLAXIS
§ To prevent infections before they occur.
Examples:
§ Travellingto area where malaria is endemic, may begin antimalarial
drugs before the journey.
§ Patients undergoing GI and GU surgeries
§ Patientswith known cardiac valve disease, valve replacements, and
other conditions because of the vulnerability of their heart valves.

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§ It is always possible that the host cells will also be damaged.
§ No anti-infective agent has been developed that is completely free of adverse
effects.
§ Most commonly encountered adverse effects are direct toxic effects on the:
ü Kidney

ü GI tract
ü Nervous system

§ Hypersensitivity reactions and superinfections can also occur.

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§ Chemicals that inhibit specific bacteria

Made in three ways:

§ Living microorganisms
§ Synthetic manufacture
§ Genetic engineering

§ Either bacteriostatic or bactericidal.

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1. Aminoglycosides
2. Carbapenems
3. Cephalosporins
4. Fluoroquinolones
5. Penicillin and Penicillinase-resistant drugs
6. Sulfonamides
7. Tetracyclines
8. Disease-specific antimycobacterials (antitubercular and
leprostatic)

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1. Ketolides
2. Lincosamides
3. Lipoglycopeptides
4. Macrolides
5. Monobactams
6. Oxazolidinones

7. Vancomycin

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1. Clavulanic Acid
2. Thalidomide
3. Sulbactam

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§ Bacteria can invade the body through many routes.

§ Human inflammatory response is activated and S/Sx of infection occur as the body
tries to rid itself of foreign cells.
§ The body becomes the host for the bacteria and supplies proteins and enzymes the
bacteria needs for reproduction.
§ The bacteria can multiply and send out other bacteria to further invade the tissue if
unchallenged.
GOAL of antibiotic therapy:
“To decrease the population of invading bacteria to a point at which the
human immune system can effectively deal with the invader. “
§ Culture and sensitivity testing are done.

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 GRAM-POSITIVE BACTERIA
Those whose cell wall retains a
stain known as Gram’s stain or
resists decolorization with alcohol
during C/S.
Commonly associated with
infections of:
1. Respiratory tract
2. Soft tissues
Example:
Streptococcus pneumoniae à
common cause of pneumonia
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GRAM-NEGATIVE BACTERIA
Those whose cell wall lose a
stain or are decolorized by
alcohol.
Commonly associated with
infections of:
1. Genitourinary tract
2. Gastrointestinal tract
Example:
Escherichia coli à common
cause of cystitis
§ “-CIN”
§ A group
of powerful antibiotics used to treat serious infections caused
by gram-negative aerobic bacilli.
§ Include:
1. AmikaCIN
2. GentamiCIN
3. NeomyCIN
4. StreptomyCIN
5. TobramyCIN
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§ Bactericidal à susceptible strains of gram-negative bacteria.
§ Include:
§ Pseudomonas aeruginosa
§ Escherichia coli
§ Proteus spp. , Klebsiella-Enterobacter-Serratia group
§ Staphylococcus spp. (such as staphylococcus aureus)

§ Indicated for the treatment of serious infections that are susceptible to

penicillin when penicillin is contraindicated.
§ Can be used in severe infections before C/S results have been obtained.

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§ Poorly absorbed from the GI § Amikacin: short-term IM or IV
tract use.
§ Rapidly absorbed after IM, peak § Gentamicin: ophthalmic,
levels after 1 hr. topical, IV, IM, intrathecal
§ Ave. half-life: 2 to 3 hrs. § Neomycin: topical and oral
forms
§ Widely distributed all over the
body. § Streptomycin: only available
for IM use.
§ Cross placenta
§ Tobramycin: short-term IM or
§ Enter breastmilk
IV treatment, ophthalmic and
§ Excreted unchanged in the nebulizer solution.
urine.
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§ Known allergy to any of the § CAUTION: pregnancy
aminoglycosides § Test urine function frequently
§ Renal or hepatic disease
§ AMIKACIN: Very high
§ Pre-existing hearing loss potential for nephrotoxicity and
ototoxicity.
§ Active infection with herpes or
mycobacterial infections. § STREPTOMYCIN: reserved
for use in special situations à
§ Myastheniagravis or
very toxic to 8th CN and kidney.
parkinsonism
§ Lactation

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§ Come with a black box warning: serious risk of ototoxicity and nephrotoxicity.

§ Ototoxicity possibly leading to irreversible deafness

§ Vestibular paralysis, numbness, tingling, weakness; depression, disorientation

§ Renal failure
§ Bone marrow depression à superinfections

§ Nausea & vomiting, diarrhea, weight loss

§ Stomatitis
§ Hepatic toxicity

§ Palpitations, hypotension and hypertension

§ Hypersensitivity

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§Most aminoglycosides have a synergistic
bactericidal effect when given with
penicillins or cephalosporins.
§Avoid combining with potent diuretics:
üIncreased incidence of ototoxicity,
nephrotoxicity, neurotoxicity

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§ Neuromuscular blockade
ü May produce respiratory depression.
ü Check anesthesia record (succinylcholine or pancuronium bromide)

§ Heparin

ü Gentamicin and heparin are physically incompatible. à DO NOT MIX

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 PENEMS
§ “-PENEMS”
§ New class of broad-spectrum antibiotics
§ Effective against gram-positive and gram-negative bacteria.
§ DoriPENEM
§ ErtaPENEM
§ ImiPENEM-Cilastatin
§ MeroPENEM

§ Meropenem, the first drug, has limited use because of the severe risk for
potentially fatal GI toxicities.

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§ Bactericidal.
§ Used to treat serious infections caused by:
Ø Streptococcus pneumoniae, Haemophilus Influenzae, Streptococcus aureus
Ø Escherichia coli, Klebsiella pneumoniae, Clostridium clostridioforme, Acinetobacter
baumanii
§ Indications: serious infections on
1. Intra-abdominal
2. Urinary tract
3. Skin and skin structure
4. Bone and joint
5. Gynecological
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§ IM: Rapidly absorbed
§ IV: reach peak levels after infusion
§ Ave. half life: 1 to 4 hours.

§ Imipenem-cilastatin:
ü Combination: imipenem (bactericidal) and cilastatin (increased urinary excretion &
decreased renal toxicity)
ü Can be given IV or IM
ü Approved for use in children

§ Meropenem: given IV for 1 hour, every 8 hrs for 5 to 14 days.

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Contraindications: Meropenem
§ Known allergy § Should be used with caution
with inflammatory bowel
§ Seizure disorders disorders
§ Meningitis § Associated with
§ Lactation pseudomembranous colitis

CAUTION:
§ Pregnancy

§ Test urine function regularly

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Toxic effects on GI tract
üPseudomembranous colitis (severe diarrhea, blood and mucus in the
stool)
üClostridium difficile diarrhea
üNausea and vomiting à serious DHN and electrolyte imbalances
§ Superinfections
§ CNS effects: dizziness, headache, altered mental state
üSeizures have been reported when combined with other drugs

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Probenecid
§ Should not be combined with meropenem
§ Can lead to toxic levels of meropenem

§ Inhibits urinary excretion of carbapenems

Valproic acid
§ Consider alternative antibiotic
§ Combination can cause serum levels to fall and increase risk of seizures
Ganciclovir
§ Avoid concurrent use with imipenem: can cause seizures

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CEPH
§ “-CEFs”
§ Similar to penicillins in structure and activity
§ Four generations

1st Generation
§ Largely effective against gram-positive bacteria (affected by Pen G)

§ Gram-negative bacteria Proteus mirabilis, E. coli, Klebsiella pneumoniae (PEcK)

2nd Generation
§ Less effective against gram-positive bacteria

§ Haemophilus influenzae, Enterobacter aerogenes, Neisseria spp. (HENPeCK)

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3rd Generation
§ Effective against all previously mentioned strains
§ Relatively weak agains gram(+) bacteria but more potent against gram(-)
bacilli
§ Serratia marcecens (HENPeCKS)

4th Generation
§ In development
§ First drug: Cefepime
§ Active against
gram (-) and gram (+) organisms including
cephalosporin-resistant staphylococci and Pseudomonas aeruginosa.

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1st Generation 3rd Generation
§ Cefadroxil § Cefotaxime
§ Cephalexin § Ceftazidime
§ Cefazolin § Ceftriaxone

2nd Generation 4th Generation

§ Cefaclor § Cefepime
§ Cefuroxime

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§ Bactericidal and bacteriostatic
§ Selection depends on:
1. The sensitivity of the involved organism
2. The route of choice
3. The cost involved
§ Important to reserve cephalosporins for appropriate situations
§ Before therapy: C&S test should be performed

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§ Primarily metabolized in the liver
§ Excreted in urine
§ Cross placenta and breast milk
Well-absorbed in GI tract:
1. First gen: cefadroxil, cephalexin
2. 2nd gen: cefaclor
3. 4th gen: cefepime
§ Others: IM, IV

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§ Known allergies to cephalosporins or penicillins
§ Caution: hepatic and renal impairment
§ Caution: pregnancy and lactation

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§ Most common: GI tract
§ Nausea & vomiting, diarrhea, anorexia, abdominal pain, flatulence
§ Pseudomembranous colitis
§ CNS: headache, dizziness, lethargy, paresthesias
§ Nephrotoxicity
§ Superinfections
§ Possibility of phlebitis with IV
§ Local abscess at the site of IM injection

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§ With aminoglycosides à increase risk of nephrotoxicity
§ Oral anticoagulants à increase risk of bleeding
§ Avoid alcohol for up to 72 hours after discontinuation to
prevent a disulfiram-like reaction.
§ Flushing, throbbing headache, nausea and vomiting
§ Chest pain, palpitations, dyspnea
§ Syncope, vertigo, blurred vision
§ In extreme reactions: cardiovascular collapse, convulsions, or
even death.

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FLUO
§ “-floxacin”
§ New synthetic class of antibiotics with broad spectrum of
activity
§ CiproFLOXACIN – most widely used
§ levoFLOXACIN
§ moxiFLOXACIN
§ oFLOXACIN

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§ Bactericidal

§ Misuse of drugs lead to resistant strains of bacteria

§ Gram (-) bacteria (E. coli, Kleb. Pneumoniae, Pseudomonas aeruginosa, H. influenzae,
Staph aureus, some Neisseria gonorrhoeae)
ü Urinary tract

ü Respiratory tract

ü Skin infections
§ Ciprofloxacin: wide spectrum of gram(-) bacteria

ü Approved for prevention of anthrax infection

ü Also effective against typhoid fever.
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§ Absorbed from GI tract
§ Metabolized in the liver
§ Excreted in urine and feces
§ Cross the placenta and enter breastmilk
§ Ciprofloxacin: injectable, oral and topical
§ Levefloxacin: oral and IV forms
ü May be preferred for severe infections or use when patient cannot take oral drugs
§ Ofloxacin: IV or oral
ü Ocular infections
§ Finafloxacin (new drug): otic drops for topical treatment of swimmer’s ears.

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Contraindications:
§ Known allergy
§ Pregnant or lactating patients
Caution:
§ Presence of renal dysfunction

ØAlways perform culture and

sensitivity tests of infected tissue
ØNot recommended for use in patients younger than 18 years of
age.

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§ Generally mild adverse reactions.
§ CNS: headache, dizziness, insomnia, depression.
§ GI: nausea, vomiting, diarrhea, dry mouth

§ Immunological: bone marrow depression

§ Fever, rash, photosensitivity

§ Warning: risk of tendinitis and tendon rupture

ü Increased in patients over age of 60, concurrent steroids, and
ü Those with renal, heart, or lung transplants.

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§ Decreased therapeutic effects with:

ü Iron salts, sucralfate, mineral supplements, antacids

ü Should be separated by at least 4 hours.

§ Severe-to-fatal cardiac reactions possible: taken with drugs that increase QTc
interval or torsaides de pointes.
ü Continual cardiac monitoring.

§ Increased CNS stimulation: NSAIDs

ü Closely monitor especially with history of seizures or CNS problems

§ Corticosteroids: increased risk of tendonitis and tendon rupture.

ü Instruct patient to report any tendon pain or weakness

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 CILLINS
§ “-cillins” Extended-Spectrum
Penicillins:
§ Penicillin: first antibiotic
introduced for clinical use. § Amoxicillin
PENICILLINS: § Ampicillin
§ Penicillin G benzathine Penicillinase-Resistant
Antibiotics:
§ Penicillin G potassium
§ Nafcillin
§ Penicillin G procaine
§ Oxacillin
§ Penicillin V
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§ Bactericidal § Diphtheria
§ Treatment of streptococcal § Anthrax
infections: § Syphilis
ØPharyngitis, tonsillitis,
§ Uncomplicated
scarlet fever, endocarditis gonococcal infections
§ Pneumococcal infections
§ High doses:
§ Staphylococcal infections
ØMeningococcal infections
§ Ratbite fever
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§ Rapidly absorbed from the GI tract, reaching peak
levels in 1 hr.
§ Sensitive to gastric acid levels in the stomach à
should be taken with empty stomach to ensure
adequate absorption.
§ Excreted unchanged in the urine.
§ Enter breastmilk.

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Contraindications:
§ Allergies to penicillins, cephalosporins, or other allergens
Caution:
§ Renal disease
§ Pregnancy and lactation

§ Culture and sensitivity tests

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§ Major adverse effect: GI tract
ØNausea, vomiting, diarrhea, abdominal pain
ØGlossitis, stomatitis, gastritis, sore mouth, and furry tongue.
§ Superinfections
§ Pain and inflammation at injection site
§ Hypersensitivity reactions: rash, fever, wheezing, with repeated
exposure anaphylaxis à anaphylactic shock and death.

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§ Tetracyclines: decrease in the effectiveness of
penicillins

§ With any parenteral aminoglycosides:

üInactivation of aminoglycosides occurs.

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SULF
§ Sulfa drugs
§ Aka Sulfa drugs
§ Inhibit folic acid synthesis
§ Sulfadiazine
§ Sulfasalazine
§ cotrimoxazole (Septra, Bactrim)
üCombi: sulfamethoxazole + trimethoprim

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§ Folic acid is necessary for the synthesis of precursors of RNA and
DNA.
§ Gram (+) and gram (-) bacteria
§ Remain inexpensive and effective treatment for UTIs and trachoma
especially in developing countries.
§ Used to treat:
üUTIs, STDs

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§ Teratogenic

§ Distributed into breastmilk.

§ PO: absorbed from GI tract, metabolized in the liver, excreted in urine.

§ Sulfadiazine: oral agent; slowly absorbed in GIT.

§ Peak levels in 3 – 6 hrs.

§ Sulfasalazine: rapidly absorbed in GIT.

§ Peak levels in 2 – 6 hrs.

ü Metabolized in liver à excreted in urine with half-life 5 to 10 hrs.

§ Cotrimoxazole: rapidly absorbed in GI.
§ Peak levels: 2 hrs.

ü Metabolized in liver à excreted in urine with half-life 7 to 12 hrs.

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Contraindications:
§ Any known allergy
§ Pregnancy

§ Lactation

Caution:
§ Patients with renal disease or Hx of kidney stones
§ Elderly à due to increased incidence of CNS effects

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§ GI effects
ü Nausea, vomiting, diarrhea, abdominal pain, anorexia, stomatitis, hepatic injury
§ Renal effects

ü Crystaluria, hematuria, proteinuria

§ CNS effects

ü Headache, dizziness, vertigo, ataxia, convulsions, depression

§ Bone marrow depression
§ Dermatological effects

ü Photosensitivity, rashes

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§ Antidiabetic agents (e.g. glyburide, glipizide)
à ↑ risk of hypoglycemia.
§ Cyclosporine
à ↑ nephrotoxicity

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 CYCLINES
§ “-cyclines”
§ Developed as semisynthetic antibiotics
§ Composed of 4 rings, based on the structure of a common soil mold.

§ tetraCYCLINE
§ demecloCYCLINE

§ doxyCYCLINE
§ minoCYCLINE

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§ Bacteriostatic.
§ Can be toxic at high concentrations.
§ Used when penicillin is contraindicated in susceptible infections.

§ Treatment of acne
§ Treatment of uncomplicated GU infections caused by Chlamydia trachomatis.

§ Can be used as adjuncts in treatment of certain protozoal infections.

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Drug Usual Indications
Doxycycline Wide variety of infections:
1. Sexually transmitted diseases
2. Periodontal disease

Tetracycline 1. When penicillin is contraindicated

2. Acne vulgaris and minor skin infections
3. Ophthalmic agent: superficial ocular lesions
4. Prophylactic agent: ophthalmia neonatorum caused by
Neisseria gonorrhoeae and Chlamydia trachomatis

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§ Absorption in GIT is affected by food, iron, calcium, and other drugs in the
stomach.
§ Concentrated in the liver.

§ Excreted unchanged in the urine.

§ Half-lives: 12 to 25 hrs.

§ Cross placenta and pass breastmilk.

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Contraindications:
§ Known allergy to tetracyclines and tartrazine.
§ Pregnancy and lactation

§ Ophthalmic preparation: patients with fungal, mycobacterial or viral ocular

infections.

Caution:
§ Children younger than 18 y/o

§ With hepatic or renal dysfunction

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§ Direct irritation of the GIT.
ü Nausea, vomiting, diarrhea, abdominal pain, glossitis, dysphagia.
§ Fatal hepatotoxicity
§ Skeletal effects à damage to teeth and bones
§ Dermatological effects à rash and photosensitivity
§ Superinfections
§ Local effects
ü Pain and stinging with topical or ocular application
§ Hematological effects (less frequent) à hemolytic anemia, bone marrow depression
§ Hypersensitivity

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§ Pen G effectiveness decreases § ↓ tetracycline effectiveness
when combined. results from oral combinations
with:
§ Oral contraceptives:
1. Calcium salts
↓effectiveness
2. Magnesium salts
§ ↑ Digoxin toxicity
3. Zinc salts
4. Aluminum salts
5. Bismuth salts
6. Iron
7. Urinary alkalinizers
8. Charcoal
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§Not absorbed effectively if taken with food or
dairy products.
§Administered on an empty stomach 1 hr
before or 2 to 3 hrs after any meal or
medication.

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Mycobacteria
ü Group of bacteria that cause tuberculosis and leprosy
ü “acid-fast” bacteria
ü Have outer coat of mycolic acid à protects them from many disinfectants
§ Mycobacterium tuberculosis à Causes tuberculosis
§ Mycobacterium leprae à Causes leprosy
ü Aka Hansen’s disease
ü Characterized by disfiguring skin lesions and destructive effects on the respiratory
tract.
§ Mycobacterium avium-intracellulare à seen in patients with AIDS, or in severely
immunocompromised.
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§ Slow growing à treatment must be continued for 6 months to 2 years.
§ Use of drugs in combination:
ü ↓ emergence of resistant strains and

ü to affect bacteria at various phases during their long and slow life cycle.
§ Drugs from other antibiotic classes are found effective in second-line treatment:

ü Ciprofloxacin
ü Ofloxacin
ü Levofloxacin

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First-Line Drugs Second-Line Drugs
Rifampin, Rifapentin Bedaquiline
INH (Isoniazid) Capreomycin
Pyrazinamide Cycloserine
Ethambutol Ethionamide
Streptomycin Rifabutin

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Dapsone
§ Mainstay of leprosy treatment
§ Inhibits folate synthesis

§ Used to treat Pneumocystic jiroveci pneumonia in AIDS patients

Thalidomide (hypnotic drug)

§ Treatment for erythema nodosum leprosum
à occurs after treatment for leprosy.

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§ Bactericidal (affects DNA and/or RNA)
§ Isoniazid (INH) à specifically affects the mycolic acid coat around
bacterium.
Drugs are always used in combination:
§ To affect the bacteria at various stages
§ To decrease the emergence of resistant strains

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§ Generally well-absorbed in GIT.
§ PO: metabolized in liver, excreted in urine
§ Cross placenta and enter breastmilk.

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Contraindications:
§ Known allergy
§ Hepatic and renal failure

§ With severe CNS dysfunction

§ Pregnancy

If necessary during pregnancy, the safest combination:

§ Rifampin + Isoniazid (INH) + Ethambutol.

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§ CNS effects
ü Neuritis, dizziness, headache, malaise, drowsiness, hallucinations
§ GIT irritation

ü Nausea, vomiting, anorexia, stomach upset, abdominal pain.

§ Rifampin, Rifabutin, Rifapentine

ü Cause discoloration of body fluids from urine to sweat and tears.

ü ALERT patients: orange-tinged urine, sweat, and tears may stain clothing and
permanently stain contact lenses.

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§ Rifampin + INH: toxic liver reaction increases.
§ Decrease drug effectiveness in combination with Rifampin or rifabutin:
1. Metoprolol, propranolol
2. Oral antidiabetic agents
3. Phenytoin
4. Ketoconazole

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§ Antibiotics that do not fit into the large antibiotic classes.
§ Include:
1. Ketolides
2. Lincosamides
3. Lipoglycopeptides
4. Macrolides
5. Oxazolidinones
6. Monobactams

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Telithromycin: only approved drug in the class.
§ Approved for use in treating mild to moderate CAP.
§ Bactericidal.

§ Effective against:
1. Streptococcus pneumoniae
2. Multidrug-resistant strains
3. Haemophilus influenzae
4. Chlamydophila pneumoniae
5. Mycoplasma pneumoniae

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§ Similar to macrolides but are more toxic.
§ Include:
1. Clindamycin
2. Lincomycin
§ Used in the treatment of severe infections when a less toxic antibiotic cannot be
used.

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§ Synthetic derivatives of vancomycin.
§ Effective against gram(+) organisms.
§ The only approved use for these drugs is treating complicated skin and skin
structure infections in adults.
§ IV drugs only.

§ Include:
1. Televancin
2. Dalbavancin
3. Oritavancin

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§ “-thromycin”

§ May be bactericidal or bacteriostatic.

§ Include:

1. Erythromycin
2. Azithromycin
3. Clarithromycin
§ May be used as prophylaxis for endocarditis before dental procedures in high-risk
patients with valvular heart disease who are allergic to penicillin.
§ Topical: indicated for ocular infections and for acne vulgaris.
§ Prophylaxis against infection in minor skin abrasions

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§Has direct and indirect antiviral activity in
bronchial epithelial cells and other host cells.
§Anti-inflammatory effect and modulation of
macrophage action.
§Prophylaxis against bacterial superinfection

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§ Cross placenta and enter breastmilk.
§ Absorbed in GIT
§ Azithromycin and clarithromycin: excreted unchanged in the urine.

Azithromycin
§ Half-life: 68 hrs
§ Can be given once a day
§ Useful for patients who have trouble remembering to take pills.

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§Food in the stomach decreases
absorption
§Should be taken on an empty stomach
with a full 8-oz glass water 1 hr before or
at least 2 – 3 hrs after meals.

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 ZOLID
§ “-zolid”
§ Currently two antibiotics available:
1. Tedizolid
2. Linezolid
§ Effective against:

ü Vancomycin-resistant strains of enterococci (VRE)

ü Staphylococcus and Methicillin-resistant Staphylococcus aureus (MRSA)
ü Penicillin-resistant pneumococci and S. aureus.

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Linezolid
§ Used in pneumonia

§ Skin and skin structure infections

§ Diabetic foot infections without osteomyelitis

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§ CNS effects
ü Headache, insomnia, dizziness
§ GI effects

ü Dry mouth, nausea, vomiting, diarrhea

ü Potential for pseudomembraneous colitis

§ Thrombocytopenia
§ Hypertension

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§ Risk of hypertension if combined with drugs that increase
blood pressure.
§ Increased risk for bleeding and further thrombocytopenia
à Combined with drugs that affect bleeding including
NSAIDS and platelet inhibitors.

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§ Tyramine-containing foods (large amounts)
àPotential for serious life-threatening hypertension
àExample: cheese and red wine

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Adjuncts:
1. Clavulanic acid and sulbactam
2. Thalidomide
Tigecycline
§ First drug of a new class called glycycyclines.
§ Approved for use in the treatment of complicated:
ü Skin and skin structure infections
ü Intra-abdominal infections
§ Caution: known allergy to tetracycline.
§ Women should be advised to use a barrier form of contraceptive

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Clavulanic Acid
§ Protects certain beta-lactam antibiotics from breakdown in the presence of
penicillinase enzymes.

Combination of amoxicillin and clavulanic acid (Augmentin)

§ Commonly used to allow amoxicillin to remain effective against certain
strains of resistant bacteria

Sulbactam
§ Increases the effectiveness of antibiotics against certain resistant bacteria.
§ Used in the systemic treatment of infections (e.g. Ampicillin + Sulbactam)

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§ Prevents synthesis of bacterial walls.
§ Glycopeptide antibiotic
§ Effective against ONLY gram-positive bacteria such as:

streptococci, staphylococci, Clostridium difficile, and Corynebacterium that

may cause endocarditis, osteomyelitis, meningitis, pneumonia, or
septicemia.
§ May be used orally against staphylococcal enterocolitis and antibiotic-associated
pseudomembranous colitis produced by C. difficile.
§ Reserved for potentially life-threatening infections who cannot be treated with less
toxic agents such as penicillins or cephalosporins.
§ Most prominent adverse effects: nephrotoxicity and ototoxicity.

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Red Man Syndrome
§ Rapid IV administration may result in severe
hypotensive episode.
§ Characteristic of vancomycin.
§ Manifested by sudden and profound
hypotension with or without a maculopapular
rash over the face, neck, upper chest and
extremities.
§ Rash generally resolves after few hours after
terminating the infusion.

§ Monitor blood pressure during infusion.

§ Serum trough levels should be routinely ordered
to minimize these adverse effects.

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Ototoxicity
§ Dizziness, tinnitus, and progressive hearing loss.
Nephrotoxicity
§ Secondary infections: oral thrush, genital and anal pruritus, vaginitis, and vaginal
discharge.

Drug interactions:
§ Concurrent use of other ototoxic or nephrotoxic agents such as streptomycin.

§ Neuromuscular blockade: may produce respiratory depression.

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§ A fungus is a cellular organism with a hard cell wall that is made up of chitin and
various polysaccharides.
§ Cell membrane contains ergosterol.

§ Any infection with a fungus is called a mycosis.

§ Systemic fungal infections (which can be life-threatening) are increasing with the
rise in the number of immunocompromised patients.

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§ Can be toxic to host and are not to be used indiscriminately.
§ Important to get a culture of the fungus.
§ Are associated with many drug-drug interactions because of their effects on the
liver.
§ Monitor a patient closely when adding or removing a drug from a drug regimen if
the patient is receiving a systemic antifungal.

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AZOLE
§ Large group of antifungals used to treat systemic and topical fungal infections.
§ Include:
Fluconazole, itraconazole, ketoconazole, terbinafine, voriconazole.
§ Are considered less toxic than some other antifungals, they may also be less
effective in very severe and progressive infections.

Therapeutic Action:
§ Fungicidal effect or fungistatic effect, depending on the type of fungus being
affected and the concentration of the drug.

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Ketoconazole
§ Associated with severe hepatic toxicity, should be avoided in patients
with hepatic dysfunction.
§ Notthe drug of choice for patients with endocrine or fertility
problems.
Fluconazole
§ Should be used in caution in the presence of liver or renal toxicity.
§ Not associated with the endocrine problems seen with ketoconazole.

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§ Many azoles are associated with liver toxicity
§ Can cause severe effects on fetus or a nursing baby.

DRUG – DRUG Interactions

§ Increased serum levels of the following agents:
§ Digoxin, oral hypoglycemics, warfarin, oral anticoagulants and
phenytoin.
§ Closely monitor patients and anticipate for dose adjustments.

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§ Anidulafungin, caspofungin, and micafungin.
§ Work by inhibiting glucan synthesis.
§ Glucan is an enzyme present in the fungal cell wall
but not in human cell walls.
§ If enzyme is inhibited, fungal cell wall cannot form,
leading to death of the cell wall.

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Anidulafungin
ØMay cross placenta and enter breastmilk, should not be used by
pregnant or lactating women.
ØCaution must be used in the presence of hepatic impairment.
Caspofungin
§ Can be toxic to liver, reduced dose must be used if known hepatic
impairment.
§ Embryotoxic in animal studies and is known to enter breastmilk, it
should be used with great caution during pregnancy and lactation.

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§Amphotericin B, flucytosine, and nystatin
§Work to cause fungal cell death or to prevent
fungal cell reproduction
§Because of the many adverse effects
associated with this agent, its use is reserved
for progressive, potentially fatal infections.

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§ Amphotericin B has been used successfully during
pregnancy, but it should be used cautiously.
§ Crosses into breastmilk and should not be used during
lactation.
§ Nystatin: not known whether it crosses the placenta or
enters breast milk, so it should not be used during
pregnancy or lactation, unless the benefits clearly
outweigh the potential risks.

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Amphotericin B:
§Associated with severe renal impairment,
bone marrow suppression, GI irritation with
nausea and vomiting, and potentially severe
diarrhea, anorexia, and weight loss.

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§ For treatment of a variety of mycoses of the skin and mucous membranes.
§ Fungi that cause these mycoses are called dermatophytes.
§ Include a variety of tinea infections, often referred to as ringworm.
§ Athelete’s foot (tinea pedis), jock itch (tinea cruris), and yeast infections of the
mouth and vagina often caused by Candida albicans.
§ Care is necessary when using near open or draining wounds that might permit
systemic absorption.
Topical antifungals include:
§ Azole-type antifungals-–butoconazole, clotrimazole, ketoconazole, miconazole,
econazole
§ Other antifungals-butenafine, gentian violet

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§ Work to alter the cell permeability of the fungus, causing prevention
of replication.
§ Indicated only for local treatment of mycoses, including tinea
infections.

Pharmacokinetics:
These drugs are not absorbed systematically and do not undergo
metabolism or excretion in the body.

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For athlete's foot:
§ The powder is most effective in intertriginous areas and in patients for whom a dry
environment may enhance the therapeutic response.
§ Instruct patients to wear cotton socks (avoid nylon), change them two to three times
daily if possible.
For jock itch or ringworm, wear well-fitting, non-constrictive, ventilated clothing.
Intravaginal:
§ Refrain from sexual intercourse during therapy (or the male should wear a condom
to avoid reinfection)
§ Contraception other than a diaphragm or condom should be used when the patient
is being treated with vaginal ointment.
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§ Contraindications are limited to a known allergy to any of
these drugs and open lesions.
§ Econazole can cause intense, local burning and irritation.
§ Gentian violet stains skin and clothing bright purple.
Very toxic when absorbed, so it cannot be used near
active lesions.

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