Pharmacology - Antimicrobials

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)
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
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
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
Amoxicillin	aminopenicillin b-lactam	G+	(blank)	(blank)	(blank)
Ampicillin	(blank)	(blank)	(blank)	(blank)	(blank)
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
Augmentin (amoxicillin + clauvulanic acid)	b-lactams penicillin	(blank)	PO drug of choice when switching from IV unasyn	(blank)	PO only
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
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
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
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
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)
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
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
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
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)	IV
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
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
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
Cefepime (Maxipime)	b-lactam, 4th gen. cephalosporin	PSEUDOMONAS and expanded G- goverage	**Reserve for resistant infections	(blank)	IV only, renally adjust
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)
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
Azithromycin	Macrolides	S. pneumonia, "atypical G-s" Chlamidia 1xdose	(respiratory infx, pneumonia, bronchitis, pharyngitis, sinusitis, otitis media, MAC)	(blank)	(blank)
Clarithromycin	Macrolides	S. pneumonia, "atypical G-s", H. pylori	S. pneumonia, "atypical G-s" (respiratory infx, pneumonia, bronchitis, pharyngitis, sinusitis, otitis media, MAC)	(blank)	(blank)
Telithromycin	Ketolides	S. pneumonia, "atypical G-s"	(blank)	drug interactions d/t -3A4 interactions	overcame macrolide resistance
Clindamycin	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)	(blank)
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)	(blank)
Tetracycline	Tetracyclines	H. pylori	acne	(blank)	Don't give w/milk products (binds Ca)
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)	(blank)
Minocycline	Tetracyclines	Staph	Rheumatoid arthritis	limited use d/t side effects	(blank)
Tigecycline	Glycycyclines	(blank)	cSSSI, intra-abdominal infx	(blank)	recently approved
Chloramphenicol	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
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
(blank)	Metronidazole	(blank)	(blank)	(blank)	(blank)
(blank)	Rifampin	(blank)	(blank)	(blank)	(blank)
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
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
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)	(blank)
Isoniazid or Rifampin	Latent TB	preventative/chemoprophylaxic therapy of walled off/dormant TB	Isoniazid (9mo, 6mo) or Rifampin (4mo)	(blank)	(blank)
Isoniazid (INH)	(blank)	(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)	(blank)	(blank)	hepatotoxicity, ARTHRALGIAS, Gouty arthritis; contraindicated in gout	PO only; dependent on presence of pyrazinamidase; renal excretion mostly, adj dose
Ethambutol	(blank)	(blank)	best with rapidly dividing M. tuberculosis	retrobulbar neuritis (visual disturbance with colors: red/green); NO HEPATOTOXICITY	PO only; renal excretion, adj dose
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)
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
Ethionamide	second line drugs for Active TB	resistant strains	(blank)	GI, hepatotoxicity, NEUROTOXICITY (peripheral and optic)!!	(blank)
P-aminosalicylic acid (PAS)	(blank)	(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
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)	(blank)
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)	(blank)
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)	(blank)	(blank)

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