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Cell Wall Agents
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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