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)  
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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