Pharmacology - Antimicrobials

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Antimicrobial Agent

Drug Class

Coverage

Place in Therapy

Adverse Effects

MOA

Penicillin G

beta-lactam

G+ (strep and staph) VERY limited G-

Tx of syphilis (endocarditis, neurosyphilis, susceptible OB-Gyn infections)

Rash, anaphylactic shock

Binds PBP (transpeptidase)

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Penicillin V

beta-lactam

Good G+, limited G-

Strep throat, dental infections

rash, anaphylaxis

binds PBP (transpeptidase); PO only; don't give with food; renal/fecal excretion

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Nafcillin/Oxacillin

beta-lactam

Penicillinase resistant; antistaphylococcal

Staph infections (not for MRSA), (endocarditis, bacteremia, cellulitis, osteomyelitis)

rash, anaphylaxis, neutropenia

alteration of b-lactam ring protects against b-lactamase; IV (PO possible), metabolized in liver; adjust for liver fxn

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Dicloxacillin/Cloxacillin

beta-lactam

G+ (non-MRSA)

Staph infections (not for MRSA), (endocarditis, bacteremia, cellulitis, osteomyelitis)

rash, anaphylaxis, neutropenia

Altered b-lactam ring, binds PBP; PO only; renal excretion; no adjustments

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Amoxicillin

aminopenicillin b-lactam

G+

(blank)

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Ampicillin

(blank)

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Unasyn (ampicillin + sulbactam)

b-lactams penicillin

G+s (staph/strep), Lesser G-s, most anaerobes, B. fragilis, peptostreptococcus

bacteremia, cellulitis, osteomyelitis, HEENT infx, pneumonia

(blank)

IV only

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Augmentin (amoxicillin + clauvulanic acid)

b-lactams penicillin

(blank)

PO drug of choice when switching from IV unasyn

(blank)

PO only

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Zosyn (Piperacillin + Tazobactam)

b-lactam extended spectrum penicillin

PSEUDOMONAS!!, G+ (non-MRSA), G-s, anaerobes

Nosocomial pneumonia, cellulitis/osteomyelitis, diabetic foot, intra-abdominal, bacteremia, complicated UTI, febrile neutropenia

(blank)

IV only, renal excretion, dose modification needed

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Timentin (Ticarcillin + Clauvulanic Acid)

b-lactam extended spectrum penicillin

PSEUDOMONAS!!, G+ (non-MRSA), G-s, anaerobes

Nosocomial pneumonia, cellulitis/osteomyelitis, diabetic foot, intra-abdominal, bacteremia, complicated UTI, febrile neutropenia

(blank)

IV only, renal excretion, dose modification needed

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Imipenem-Cilastatin (Primaxin)

b-lactam; carbapenem

PSEUDOMONAS, Greater G-s

nosocomial pneumonia, bacteremia, febrile neutropenia, intra-abdominal infx, complicated UTI

seizures, don't use in ped. CNS infx, infusion-related hypersensitivity

IV (gastric acid destroys it); cleared renally, dose adjust

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Meropenem (Merrem)

b-lactam; carbapenem

PSEUDOMONAS, Greater G-s

nosocomial pneumonia, bacteremia, febrile neutropenia, intra-abdominal infx, complicated UTI

seizures, don't use in ped. CNS infx, infusion-related hypersensitivity, hepatotoxicity

IV (gastric acid destroys it); cleared renally, dose adjust

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Ertapenam (Invanz)

b-lactam; carbapenem

G+ (strep, staph, non-MRSA), G-s (not pseudomonas)

intra-abdominal infx, cSSSI, complicated UTI

seizures, don't use in ped. CNS infx, infusion-related hypersensitivity

IV (gastric acid destroys it); cleared renally, dose adjust; Once daily IM available (allows for outpt tx)

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Aztreonam

b-lactam; monobactam

PSEUDOMONAS!!, G-s (except Acinetobacter); stable against b-lactamase

Good for b-lactam allergic pts

hypersensitivity, hepatotoxicity

IV or IM, cleared renally, needs adjustment

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Cefazolin (Ancef/Kefzol)

b-lactam; 1st gen. cephalosporin

G+s (staph, strep, non-MRSA); SS-PEK (staph, strep, proteus, e. coli, klebsiella)

cellulitis, puncture wounds, bacteremia, surgical prophylaxis, G- UTIs

allergies similar to penicillin, thrombocytopenia, neutropenia, hemolysis, hepatotoxicity

IV, short 1/2-life, renal clearance, dose adjust

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Cephalexin (Keflex)

b-lactam; 1st gen. cephalosporin

G+s (staph, strep, non-MRSA); SS-PEK (staph, strep, proteus, e. coli, klebsiella)

PO drug of choice when switching from IV Cefazolin; cellulitis, puncture wounds, bacteremia, surgical prophylaxis, G- UTIs

allergies similar to penicillin, thrombocytopenia, neutropenia, hemolysis, hepatotoxicity

PO, short 1/2-life, renal clearance, dose adjust

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Cefoxitin (Mefoxin), Cefotetan (Cefotan)

b-lactam; 2nd generation cephalosporin

Weaker G+, but Expanded G-; HNM-PEK (H. influenzae, e. coli, n. gonorrhea, proteus, klebsiella, m. catarhalis); anaerobic (B.fragilis)

intra-abdominal, pelvic inflam. disease, surgical prophylaxis

(blank)

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Cefuroxime (Ceftin, Zinacef)

b-lactam; 2nd generation cephalosporin

Weaker G+, but Expanded G-; HNM-PEK (H. influenzae, e. coli, n. gonorrhea, proteus, klebsiella, m. catarhalis); anaerobic (B.fragilis)

Pulmonary/HEENT infx, (otitis media, pneumonia, pharyngitis, tonsilitis, bronchitis)

(blank)

PO and IV, stable against b-lactamase

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Cefotaxime (Claforan), Ceftriaxone (Rocephin), Ceftazidime (Fortaz)

b-lactam, 3rd gen. cephalosporin

Ceftazidime has PSEUDOMONAS coverage; HENS PECK MA (h. influenza, e. coli, n. meningitides, salmonella, serratia, proteus, enterobacter, citrobacter, klebsiella, m. catarrhalis, acinetobacter)

meningitis, pneumonia, bacteremia, intra-abdominal infx

ceftriaxone - sludging of bladder

IV, biliary excretion

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Cefixime (Suprax), Cefpodoxime (Vantin)

b-lactam, 3rd gen. cephalosporin

HENS PECK MA (h. influenza, e. coli, n. meningitides, salmonella, serratia, proteus, enterobacter, citrobacter, klebsiella, m. catarrhalis, acinetobacter)

PO drug of choice when switching from IV cephalosporin

(blank)

PO, renally cleared, dose adjust

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Cefepime (Maxipime)

b-lactam, 4th gen. cephalosporin

PSEUDOMONAS and expanded G- goverage

**Reserve for resistant infections

(blank)

IV only, renally adjust

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Vancomycin

glycopeptide

MRSA/MRSE!!, G+s ONLY, enterococcus, listeria

nosocomial pneumonia, bacteremia, cellulitis/osteomyelitis, meningitis, endocarditis; b-lactam allergic pts

OTOTOXICITY, neprhotoxicity, Red Man's syndrome (1g/hr max)

blocks glycosidic bond (PBP; transglycosidase) and peptide bond (transpeptidase); causes weak cell wall and bacterial lysis; IV (po given only for colitis), DOSE DEPENDENT on total body weight, dose adjust, Narrow therapeutic index (monitor troughs)

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Daptomycin

b-lactam; cyclic lipopetide

MRSA G+ (strep, staph aureus), enterococcus faecalis and faecium, including VRE

Complicated skin and skin structure infx (cSSSI), surgical sites, traumatic wounds, ulcers, abscesses, cellulitis...NEVER for PNEUMONIA

Muscle pain and weakness, CPK elevations (monitor weekly)

IV only, renal excretion, dose adjust; binds and depolarizes cell causing efflux of K+ and cell death; low risk of cross-resistance with other b-lactams b/c of unique mechanism

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Azithromycin

Macrolides

S. pneumonia, "atypical G-s" Chlamidia 1xdose

(respiratory infx, pneumonia, bronchitis, pharyngitis, sinusitis, otitis media, MAC)

(blank)

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Clarithromycin

Macrolides

S. pneumonia, "atypical G-s", H. pylori

S. pneumonia, "atypical G-s" (respiratory infx, pneumonia, bronchitis, pharyngitis, sinusitis, otitis media, MAC)

(blank)

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Telithromycin

Ketolides

S. pneumonia, "atypical G-s"

(blank)

drug interactions d/t -3A4 interactions

overcame macrolide resistance

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Clindamycin

G+s, anaerobics

common choice for penicillin allergic pts (bacteremia, cellulitis/osteomyelitis, aspiration pneumonia (anaerobes), dental infx, endocarditis prophylaxis, diabetic foot - mixed infx)

(blank)

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Linezolid

Oxazolidinones

MRSA, VRE

1st line agent for MRSA; pneumonia, bacteremia, cellulitis/osteomyelitis, diabetic foot

(blank)

PO, high bioavailability,

🗑

Synercid (Quinupristin + dalfopristin; 2 drugs in 1)

Streptogramins

G+ VRE enterococcus faecium (not E. faecalis)

endocarditis, peritonitis, pneumonia, bacteremia, cellulitis/osteomyelitis, UTIs

(blank)

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Tetracycline

Tetracyclines

H. pylori

acne

(blank)

Don't give w/milk products (binds Ca)

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Doxycycline

Tetracyclines

"atypicals," rickettsial infx

better choice w/poor kidney fxn; Lyme disease, Q Fever, Rocky mountain spotted fever, ehrlichiosis; 2nd line agent for CAP and COPD exacerbations, acne

(blank)

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Minocycline

Tetracyclines

Staph

Rheumatoid arthritis

limited use d/t side effects

(blank)

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Tigecycline

Glycycyclines

(blank)

cSSSI, intra-abdominal infx

(blank)

recently approved

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Chloramphenicol

(blank)

CNS infx, rickettsial infx in children as last resort

aplastic anemia, Gray Baby syndrome

(blank)

🗑

Gentamicin

Aminoglycosides

G-s (best for serratia mercasens); pseudomonas

Extended interval of 1qd high peak with low trough

(similar to Vancomycin) OTOTOXICITY and Nephrotoxicity (related to dose/duration of therapy; low peaks and high troughs increase risk)

synergistic with b-lactams against enterococcus

🗑

Tobramycin

Aminoglycosides

G-s (best for PSEUDOMONAS and acinetobacter)

(blank)

(similar to Vancomycin) OTOTOXICITY and Nephrotoxicity (related to dose/duration of therapy; low peaks and high troughs increase risk)

synergistic with b-lactams against enterococcus

🗑

Amikacin

Aminoglycosides

G-s (Useful in Gentra/Tobra-resistant strains)

(blank)

(similar to Vancomycin) OTOTOXICITY and Nephrotoxicity (related to dose/duration of therapy; low peaks and high troughs increase risk)

synergistic with b-lactams against enterococcus

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Gemifloxacin, Moxifloxacin, Gatifloxacin, Levofloxacin

3rd gen. Fluoroquinolones

G+ (staph non-MRSA, strep/s. pneumoniae, E. faecalis), G-s (Levofloxacin for PSEUDOMONAS); some anaerobes (not C. dificile), "atypicals"

Pneumonia; respiratory "above the waist" infx; ok for UTIs, STDs

must separate from food w/complex metallic ions; hypo/hyperglycemia, CNS, QT prolongation, tendon rupture; Gemifloxacin - rash

IV, PO (gemifloxacin only PO); inhibit topoisomerase (DNA gyrase) preventing supercoiling of DNA; resistance by target site modification and efflux pump; Mefloxacin hepatically metabolized; the rest need renal adjustment

🗑

Ciprofloxacin

2nd gen. Fluoroquinolones

1st choice FQ for PSEUDOMONAS; G-s, "atypicals"

Anthrax; "below the waist" UTIs, STDs (gonnorrhea); poor S. pneumonia coverage

metabolized by CYP-1A2; must separate from food w/complex metallic ions; hypo/hyperglycemia, CNS, QT prolongation, tendon rupture

inhibit topoisomerase (DNA gyrase) preventing supercoiling of DNA; resistance by target site modification and efflux pump

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(blank)

Metronidazole

(blank)

🗑

(blank)

Rifampin

(blank)

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Sulfonamides (sulfasalazine, dapsone, silver sulfadiazine)

Antifolates/bacterial nucleic acid synthesis inhibitors

(blank)

(blank)ulderative colitis (Crohn's disease), leprosy and brown recluse spider bite, burns respectively

(blank)

blocks THF, a cofactor needed by bacteria to produce nucleotide bases

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Sulfonamide and Trimethoprim (Diaminopyrimidines)

Antifolates/bacteiral nucleic acid synthesis inhibitors

Drug of choice for: stenotropomonas multiphilia nocardia sp.; some lesser G-s (e. coli, klebsiella (resistance: altered target site AND overproduction of PABA) First line for: acute cystitis (bladder UTI), traveler's diarrhea, Pneumocystis jiroveci

rarely used as a single agent b/c of synergistic effects (except TMP in UTIs)

highly bound ptn displaces unconjugated bilirubin from albumin causes kernicterus allergies, rash can be fatal if SJS, GI symptoms, myelosuppression, hyperkalemia

step 1: PABA converted by folic acid sythetase to dihydroflic acid (sulfonamides mimic PABA and compete for enzyme) step 2: dihydrofolate acid converted to tetrahydrofolic acid by DHA reductase step 3: tetrahydrofolate helps produce nucleotide

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Isoniazid (INH), Rifampin (RIF), Pyrazinamide (PZA), Ethambutol (EMB)

First line drugs for Active TB

mycobacterium

Initial phase (2mo with 4 drugs) then "continuation phase" (4-7mo with 2 drugs)

(blank)

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Isoniazid or Rifampin

Latent TB

preventative/chemoprophylaxic therapy of walled off/dormant TB

Isoniazid (9mo, 6mo) or Rifampin (4mo)

(blank)

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Isoniazid (INH)

(blank)

First line monotherapy for LTBI and 1 of 4 drugs used for first line active TB tx; safe in pregnancy

liver (asymptomatic elevation of aminotransferases --> clinical hepatitis --> fatal hepatitis)

PO, (IV); competitive antagonism; inhibits mycolic acid synthesis for cell wall; no renal adj.. avoid liver pts

🗑

Rifampin

(blank)

G+s

safe in pregnancy

CYP450 induction...MOST DRUG INTERACTION OF ALL TB agents; hepatotoxicity, discoloration of body fluids!

inhibits DNA-dependent RNA polymerases

🗑

Pyrazinimide

(blank)

hepatotoxicity, ARTHRALGIAS, Gouty arthritis; contraindicated in gout

PO only; dependent on presence of pyrazinamidase; renal excretion mostly, adj dose

🗑

Ethambutol

(blank)

best with rapidly dividing M. tuberculosis

retrobulbar neuritis (visual disturbance with colors: red/green); NO HEPATOTOXICITY

PO only; renal excretion, adj dose

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Fluoroquinolones/Aminoglycosides

ptn synthesis inhibitors

(blank)

1. moxifloxacin, levofloxacin gatifloxacin --> resistant to all or none; 2. amikacin/kanamyxin (cross resistance 100%, less vestibular dysf than streptomycin); 3. streptomycin (works w/ strains resistant to amikacin/kanamycin with less nephrotoxicity)

Pregnancy restrictions

(blank)

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Cycloserine

second line drugs for Active TB

resistant strains

try to avoid in pregnancy if possible

CNS (headache restlessness --> psychosis, seizures)

celll wall; inhibits alanine racemase preventing peptide bond

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Ethionamide

second line drugs for Active TB

resistant strains

(blank)

GI, hepatotoxicity, NEUROTOXICITY (peripheral and optic)!!

(blank)

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P-aminosalicylic acid (PAS)

(blank)

avoid in pregnancy if possible

Hypothyroidism, GI, hepatotoxicity

similar to sulfonamides; competes with PABA; no renal adj

🗑

Chloroquine

antiparasitic

malaria (P. falciparum tx); active against sensitive malarial infections in blood stage

Prophylaxis/Tx of Malaria

Screen for G6PD; pruritis, GI

somehow prevents conversion from heme to hemozoin (buildup kills parasite); PO rapidly absorbed with large vol distribution; 1/2-life 1-2 months; urine excretion; DOES NOT work on hepatic stage

🗑

Primaquine

antiparasitic

Malaria (P. vivax and P. ovale) in hepatic stage

Mararia prophylaxis/Tx

Check G6PD - hemolysis; GI; leukopenia

PO rapidly absorbed large vol distribution; urine excretion; DOES NOT work on blood stage

🗑

Mefloquine

antiparasitic

Mararia (P. falciparum and P. vivax); choroquine resistant strains; blood stage

Prophylaxis for chloroquine resistant malaria

Neuropsychiatric toxicity; myelosuppression; GI

PO good absorption large vol of distribution; terminal 1/2-life is 20days allowing weekly dosing

🗑

Quinine/Quinidine

antiparasitic

Malaria (P. faliparum) blood stage

Tx only choice for severe P. falciparin (after chloroquine)...no prophylaxis because of adverse effects

Check G6PD; Cinchonism: visual changes headache, dizziness, tinnitus, flushing; hypersensitivity; myelosuppression; Quinidine - arrhythmias/hypotension

Quinine: PO only; Quinidine: IV only; not active against hepatic stage

🗑

Doxycycline/Clindamycin

antibiotics

malaria

Doxycyclin: prophylactic drug of choice in SE Asia for blood stage; usually combined with quinine/quinidine; Clindamycin is safe for children/pregnant/breastfeeding mothers

(blank)

not active against hepatic stage

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Atovaquone-Proguanil (Malarone)

antifolate agent

Malaria (P. falciparum only)

Prophylaxis only

(blank)

inhibits bacterial DNA synthesis; expensive; shorter pre/post exposure Tx

🗑

Sulfadoxine

antifolate

malaria (P. falciparum only)

Standard cost-effective single dose Tx in Africa

(blank)

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Iodoquinolol

(blank)

trophozoites in bowel lumen

Amebiasis therapy - luminal agent

contraindicated for pts with iodine allergy; diarrhea

PO only; 10% absorbed so it is not active in intestinal wall or extraintestinal tissue; excreted in feces

🗑

Paromomycin

aminoglycoside antibiotic

trophozoites in bowel lumen

amebiasis therapy - luminal agent

Caution with renal insufficiency (avoid if serious); diarrhea, GI

PO only; little absorption; 7-day therapy; better tolerated than iodoquinol

🗑

Metronidazole (Flagyl)

nitroimidazole

C. dificile-associated diarrhea; anaerobics; amebiasis; giardiasis; trichomoniasis; bacterial vaginosis

amebiasis therapy - tissue agent; anaerobes; parasites; active against intestinal wall and extraintestinal infections

alcohol intolerance; peripheral neuoropathy; metallic taste; GI

PO 100% bioavailable; high penetration to most sites; hepatic metabolism/renal elimination

🗑

Tindazole (Tindamax)

(blank)

Giardiasis; trichomoniasis

amebiasis therapy - tissue agent

(blank)

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Stibogluconate sodium (pentavalent antimony)

(blank)

Leishmaniasis

First-line for all leishmaniasis infx (except in certain parts of India)

GI; myalgias/arthralgias; QT prolongation

IV, (IM)

🗑

Pentamidine

(blank)

Leishmaniasis; African sleeping sickness

Leishmaniasis; African sleepin sickness; last-line for PCP pneumonia

Very Toxic; pancreatitis; renal damage; bronchospasm (inhaled)

IV or inhaled; alternative to Stibogluconate Sodium

🗑

Albendazole, Mebendazole, Thiabendazole

Helminth agents

worms (primarily nematodes)

nematodes

short term: GI; long term: increased LFTs, pancytopenia; Thiabendazole rarely used d/t toxicity

PO only; fatty meals increase absorption; inhibits microtubule synthesis in parasites

🗑

Praziquantel

Helminth agent

Flukes, tapeworms

primarily tremadotes and cestodes

headache, dizziness, fatigue

PO only (swallow tablets whole); excreted renally; increases parasitic cell membrane permeability to Ca

🗑

bacitracin and gramicidin

antibacterial

G+ (strep, pneumo, staph), anaerobic cocci; neisseriae, tetanus bacilli; diptheria bacilli

"temporary" decrease in staph nares colonization; use in combo with other antibiotics

allergic contact dermatitis

inhibits bacterial wall synthesis

🗑

Mupirocin

antibacterial

MRSA G+s; aerobic

"eradicates" nasal MRSA colonization; Tx of impetigo due to Staph. aureus, Grp a hemolytic strep, S. pyogenes

irritation of mucous membrane; pruritis; rash; taste perversion; URI

topical; inhibits ptn synthesis (binds t-RNA); not absorbed into systemic circulation

🗑

Polymyxin B Sulfate

antibacterial

G-s; Pseudomonas, e. coli, enterobacter klebsiella

prevent infxn in minor cuts/burns; Tx of ocular infx

Neuorotoxic, Nephrotoxic

ointment or solution; alters permeability

🗑

Neomycin and Gentamicin

antibacterial

G-s: e.coli, proteus klebsiella, enterobacter (gentamicin is better for Pseudomonas, staph, and GAS)

Tx of minor skin or eye infx

Neurotoxic, Nephrotoxic; Ototoxic

ptn synth (binds 30s); ointment, cream, solution

🗑

Clindamycin

antibacterial

P. acnes

Tx of acne

dry skin irritation; BLOODY diarrhea and pseudomembranous colitis

binds 50s; gel or lotion

🗑

Erythromycin

antibacterial

P.acnes

Tx of acne vulgaris

allergies; skin irritation; antibiotic resistance

gel or topical

🗑

Metronidazole

antibacterial

P. acnes

Tx of skin infxn and acne rosacea

dry/burning/stinging skin

inhibitory effects on neutrophil cellular fxn; gel or cream

🗑

Sodium sulfacetamide

antibacterial

P. acnes

seborrheic scaling dermatosis; bacterial infx of skin; acne vulgaris/acne rosacea

local irritation; Risk of SJS, exfoliative dermatitis, toxic epidermal necrolysis; contraindicated in pts w/ hypersensitivity to sulfonamides

inhibits p.acnes by competitive inhibition of PABA

🗑

Clotrimazole, econazole, ketoconazole, miconazole, oxiconazole, sulconazole

imidazoles; antifungal agents

dermatophytes, candidiasis

tinea pedis, cruris, corporis, versicolor; Cutaneous candidiasis

skin irritation

alters membrane permeability

🗑

Cilopirox olamine

antimycotic/antifungal agent

dermatophytes, candidiasis

dermatomycosis candidiasis, tinea versicolor; mild to moderate onychomycosis of nails

skin irritation/worsening;

inhibits uptake of molecules for cell membrane synth; cream, lotion, nail polish

🗑

Naftifine and Terbinafine

allylamine class antifungals

dermatophytes, candidiasis

(blank)

🗑

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