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51 Cards in this Set
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- Back
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Penicillin G |
Mechanism -beta lactam which binds PBP -inhibits cell wall synthesis -CIDAL Resistance -beta-lactamases Indications -GAS pyogenes pharyngitis (RF prophylaxis) -GBS agalactiae (intrapartum) -Clostridium perfringens -Pasteurella (dog bites) -Syphillis (single dose) -Strep viridans -Staph aureus -Actinomyces israelii -Neisseria meningitidis Adverse -T1 (IgE) HSR (90% of "allergic" aren't) -10% X-reactivity with Cephalosporins -autoimmune hemolytic anemia w/ positive Direct Coombs (RBC IgG) -interstitial nephritis |
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Nafcillin Oxacillins |
Mechanism -beta lactam which binds PBP -resistant to beta-lactamases due to BULKY R GROUPS -inhibits cell wall synthesis -CIDAL Resistance -altered PBPs Indications -PCN resistant MSSA (mild-moderate LOCALIZED) -empirical PO Tx of SKIN and SOFT-TISSUE infections (folliculitis and abscesses) -given IV for serious SYTEMIC Staph (tricuspid endocarditis, osteomyelitis) -no activity against MRSA! Adverse -T1 (IgE) HSR (90% of "allergic" aren't) -10% X-reactivity with Cephalosporins -autoimmune hemolytic anemia w/ positive Direct Coombs (RBC IgG) -interstitial nephritis |
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Amoxicillin (PO) (aminoPCN) |
Mechanism -beta lactam which binds PBP -improved GN activity (penetration of GN outer membrane) "broad spectrum" -inhibits cell wall synthesis -CIDAL Resistance -beta-lactamases -often given with BL inhibitor like Clavulonate (Augmentin), Sulbactam, Tazobactam Indications -Staph -GAS pyogenes (pharyngitis) -sinusitis, acute otitis media, respiratory (Strep pneumo, H. influenza, M. catarrhalis -pneumonia (S. pneumo and H. influenza) -H. pylori triple therapy (Amoxicillin, Clarithromycin, PPI) -Lyme (Borrelia burgdorferi by Ixodes tick) if in early stage or pediatric -prophylaxis against encapsulated bacteria (S. pneumo and H. flu) in asplenic pts -prophylaxis before DENTAL procedures in pts at high risk for endocarditis (S. viridans) Adverse -Stevens-Johnson -Liver injury -rash when given in viral infection (EBV) |
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Ampicillin (IV) (aminoPCN) |
Mechanism -beta lactam which binds PBP -improved GN activity (penetration of GN outer membrane) "broad spectrum" -inhibits cell wall synthesis -CIDAL Resistance -beta-lactamases -often given with BL inhibitor like Clavulonate (Augmentin), Sulbactam, Tazobactam Indications -serious ANAEROBE infections (aspiration pneumonia) -enterococcus UTI and endocarditis -Listeria meningitis (infants and elderly) -second line GNR GI infections and UTI (e.g. E. coli) Adverse -Stevens-Johnson -rash when given in viral infection (EBV) |
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Piperacillin-tazobactam Ticarcillin-clavulonate |
Mechanism -beta lactam which binds PBP -improved GN activity (penetration of GN outer membrane) "broad spectrum" -inhibits cell wall synthesis -CIDAL Resistance -NOT beta-lactamases (combined with BL inhibitors) Indications -Broad spec -serious ANAEROBE infections (aspiration pneumonia) -PSEUDOMONAS -serious infections (HA Pneumonia, Sepsis) |
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Cephalexin Cephazolin (1st Gen Cephalosporins) (contain "ph" in name instead of "f") |
Mechanism -beta lactam which binds PBP -inhibits cell wall synthesis -CIDAL Indications -PO for GP cocci (Staph and Strep) cellulitis, abscess, pharyngitis (2nd line) -UTI GNRs (E. coli, Proteus, Klebsiella) -surgical prophylaxis (good tissue penetration) Adverse -T1 (IgE) HSR (90% of "allergic" aren't) -10% X-reactivity with PCN allergy -autoimmune hemolytic anemia w/ positive Direct Coombs (RBC IgG) -interstitial nephritis |
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Cefuroxime Cefotetan Cefoxitin (2nd Gen Cephalosporins) |
Mechanism -beta lactam which binds PBP -inhibits cell wall synthesis -CIDAL Indications (1st gen ceph PLUS HNS GNRs) -sinusitis -otitis -LRI -peritonitis, diverticulitis (2nd line) -H. influenza -Neisseria -Serratia -PO for GP cocci (Staph and Strep) cellulitis, abscess, pharyngitis (2nd line) -UTI GNRs (E. coli, Proteus, Klebsiella) Adverse -T1 (IgE) HSR (90% of "allergic" aren't) -10% X-reactivity with PCN allergy -autoimmune hemolytic anemia w/ positive Direct Coombs (RBC IgG) -interstitial nephritis |
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Ceftriaxone Ceftazidime Cefotaxime (3rd Gen Cephalosporins) |
Mechanism -beta lactam which binds PBP -inhibits cell wall synthesis -CIDAL Indications (2nd gen ceph PLUS MORE GNR) -IV can cross BBB -1st line for MENINGITIS (empiric, targets S. pneumo, H. flu, N. meningitidis)(but add Vanco for resistant S. pneumo and in infants/elderly add Ampicillin for Listeria coverage) -CEFTAZIDIME for CA and HA/VA Pneumonia (required for Pseudomonas coverage) -Ceftriaxone for endocarditis (S. viridans) -Ceftriaxone empirically for Sepsis -Ceftriaxone single IM dose for Gonorrhea -Ceftriaxone for Lyme (BB/Ixodes) arthritis and neurologic disease NO MRSA COVERAGE Adverse -T1 (IgE) HSR (90% of "allergic" aren't) -10% X-reactivity with PCN allergy -autoimmune hemolytic anemia w/ positive Direct Coombs (RBC IgG) -interstitial nephritis |
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Cefepime (4th Gen Cephalosporins) |
Mechanism -beta lactam which binds PBP -inhibits cell wall synthesis -CIDAL Indications -Broad spectrum -BBB penetration (meningitis) -Pseudomonas -serious systemic MDR-risk infection -H. flu -Neisseria -Staph and Strep NO MRSA COVERAGE Adverse -T1 (IgE) HSR (90% of "allergic" aren't) -10% X-reactivity with PCN allergy -autoimmune hemolytic anemia w/ positive Direct Coombs (RBC IgG) -interstitial nephritis |
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Ceftaroline (5th Gen Cephalosporin) |
Mechanism -beta lactam which binds PBP -inhibits cell wall synthesis -CIDAL Indications -MRSA (can bind altered PBPs) Adverse -T1 (IgE) HSR (90% of "allergic" aren't) -10% X-reactivity with PCN allergy -autoimmune hemolytic anemia w/ positive Direct Coombs (RBC IgG) -interstitial nephritis |
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Aztreonam (Monobactams) |
Mechanism -single beta lactam ring which binds PBP -resistant to beta-lactamases -inhibits cell wall synthesis -CIDAL Indications -AEROBIC GNRs (PSEUDOMONAS) -CSF penetration (good for serious/systemic pneumonia, meningitis, sepsis) -use in pts with Hx of PCN anaphylaxis |
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Imipenem-Cilastin Ertapenem Meropenem Doripenem (Carbapenems) |
Mechanism -beta lactam which binds PBP -resistant to extended spectrum beta-lactamases -inhibits cell wall synthesis -CIDAL Imipenem given with Cilastin to inhibit degradation by dihydropeptidases in Renal Tubule Indications -Broad spectrum (anaerobes, GP, GNRs including Pseudomonas) -Anaerobic coverage good for Aspiration pneumonia and intra-abdominal infection -good tissue penetration (incl. CSF meningitis) -Big Gun for MDR, HAP, empiric sepsis Tx Adverse (especially Imipenem) -skin rash -GI (N/V/D) -lowered seizure threshold |
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Vancomycin |
Mechanism -Glycopeptide binds to D-ala-D-ala in GP cell wall -inhibits cell wall synthesis -CIDAL Resistance -conversion to d-ala-D-lac Indications -GP (Staph, Strep, Enterococcus) -bloodstream MRSA -empiric meningitis due to resistant S. pneumo coverage (with Ceftriaxone, and with Listeria in infant/elderly) -MRSA osteomyelitis -Staph epidermidis (prosthetics, valves) -empiric endocarditis -enterococcus -PO for C. diff (2nd line for Metro resistance) Adverse -Red Man Syndrome (infusion rxn histamine release from mast cells); prolong infusion or treat with anti-histamines -thrombophlebitis at injection site -oto/nephrotoxicity ONLY when administered with other toxic agent (e.g. aminoglycosides) -DRESS Syndrome (Drug Rxn w/ Eosinophilia and Systemic Symptoms) -Renally excreted (must monitor plasma levels in AKI/CKD) |
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Daptomycin |
Mechanism -cyclic lipopeptide that inserts into GP cell MEMBRANE leading to DEPOLARIZATION -CIDAL Indication -GP (Staph, Strep, Enterococcus) -MRSA (even Vanco-resistant MRSA) -activity against Vanco-resistant GP (especially enterococcus) -MRSA bacteremia, tricuspid endocarditis, skin/soft tissue ANTAGONIZED BY SURFACTANT (not for pneumonia!!!) Adverse -myopathy/rhabdomyelysis (monitor CPK levels weekly) |
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Tetracyclin (Doxycycline, Minocycline) |
Mechanism -reversible binding of 30S ribosome -block tRNA binding, halt peptide formation -STATIC Indication: MRSA, outdoors, atypicals, acne -Broad (GP and GN) -MRSA -consider for "outdoorsy infections" -tick borne bacteria (RICKETTSIA, Ehrlichia, Francisella, Borellia) -Brucellosis (most common zoonotic worldwide) -Coxiella -Yersinia -atypicals (CHLAMYDIA) (pair with Ceftriaxone for Neisseria coverage) -Mycoplasma -ACNE anaerobes -fecal elimination (safe for RENAL pts) Adverse -chelates multivalent metals, thus absorption is reduced when given with Ca2+, Mg2+, Fe2+ -do NOT give with milk, antacids, ferrous sulfates -NOT FOR CHILDREN less than 8 or PREGNANT (deposition in teeth, cause discoloration) -N/V/D -skin photosensitivity -Fanconi T2 RTA with expired tetracyclines Resistance -efflux pumps -altered ribosome binding site |
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Azithromycin and Clarithromycin |
Mechanism -macrolide -bind 50S ribosome, block translocation -STATIC Indication -Bordatella pertussis (and family prophylaxis) -CAP: S. pneumo, H.ib, M. catarrhalis (especially in PCN allergy) -atypical PNA (Myco, Legio, Chlam) -Bartonella (cat scratch) -Mycobacterium avium (HIV CD4 < 50) -Clarithromycin, Amoxicillin, PPI for H. pylori Adverse -increased GI motility -acute cholestatic hepatitis/jaundice -long QT/torsade -Clarithromycin reduces P450 activity |
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Erythromycin |
Mechanism -bind 50S ribosome, block translocation -macrolide -STATIC Indication -NEONATAL Chlamydia conjunctivitis/PNA -NEONATAL Gonorrhea conjunctivitis -Diptheria (bull neck LAD) -constipation Adverse -increased GI motility -acute cholestatic hepatitis/jaundice -long QT/torsade |
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Clindamycin |
Mechanism -bind 50S ribosome, inhibit translocation -very similar to macrolides -STATIC -great tissue penetration (cellulitis, etc) Indication -ANAEROBIC -especially ANAEROBE LUNG ABSCESSES (think aspiration PNA, bacteroides, fusobacterium) -Clinda for anaerobes above the diaphragm (Metro for anaerobes below) -severe acne due to skin anaerobes -Gentamycin/Clindamycin for polymicrobial endometritis especially with retained products of delivery, septic abortion, pelvic abscess, foreign object like IUD (but think Dox/Cef first for Chlam/Gon) -GP -Staph and Strep skin & soft tissue infection -MRSA CAP -babesiosis -Clostridium perfringens (road rash, myonecrosis) |
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Chloramphenicol |
Mechanism -reversible binding to 50S ribosome, inhibit translocation -STATIC Indications -primarily used in developing countries -empiric tx of meningitis (IM) (covers S. pneumo, Neisseria, H.flu) -tick-borne disease (Rickettsia) especially in PREGNANT WOMEN (Doxy contraindication) Adverse -dose-dependent reversible RBC underproduction anemia -irreversible aplastic anemia due to BM suppression -grey baby syndrome (infants have ineffective glucoronidase, cannot detox/degrade Chlor): flaccidity, hypothermia, shock |
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Linezolid |
Mechanism -binds 50S ribosome, inhibits formation of initiation complex -STATIC Indications (GP) -COMPLICATED HAP, skin/soft tissue infections -Staph (MRSA) -Strep -Enterococcus UTI & Endocarditis (especially Vanco-resistant) Adverse -thrombocytopenia -anemia, neutropenia -optic and glove/stock peripheral neuropathy -serotonin syndrome (inhibitor of MAO) with MAOI, SSRI, SNRI, bupropion |
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Gentamycin/Tobramycin Neomycin Paromomycin Streptomycin Amikacin Kanamycin (broad spec) |
Mechanism -aminoglycoside -irreversible binding of 30S ribosome, inhibits formation of initiation complex -CIDAL -coupled with BETA-LACTAMS or VANCOMYCIN to enter GNR -transport into bacteria via oxygen-dependent process (aerobic bacteria only) -IV delivery Indications -Aerobic GN bacilli -especially for MDR or suspicion of sepsis -PO neomycin for bowel prep before colorectal surgery (does not exit GI tract) -PO paromomycin for GI parasites (Entamoeba histolytica) -Streptomycin for Francisella tulleremia (ticks) and Yersinia pestis (fleas) -Gentamycin for MDR GNRs (Enterobacter, Klebsiella, Serratia) causing septicemia, HAP, complicated UTI, intra-abdominal infection, osteomyelitis -PSEUDOMONAS -Enterococcus UTI/Endocarditis when coupled with a cell wall-active agent (PCN or Vanco) Adverse -ototoxicity (vestibular or cochlear) -ATN nephrotoxicity (especially with loop diuretics or other nephrotoxic agents) -not AIN nephrotox!! -neuromuscular blockade (MG contraind) -PREGNANCY CONTRAINDICATION (newborn deafness) Resistance -Enterococcus acetylation enzyme confers resistance to low levels of aminoglycosides |
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Rifampin |
Mechanism -inhibits bacterial DNA-dependent RNA Pol Clinical Indication -mycobacteria -Gram Neg -single agent for meningitis PROPHYLAXIS -can be used for MAC but RIFABUTIN is preferable in AIDS pts due to less potent P450 induction which quickly metabolizes ARVs -Mycobacterium Leprae Resistance -RNA Pol mutations Adverse -potent inducer of Cyto P450 -rapid resistance when used as SINGLE agent -hepatitis only with predisposing factors: full RIPE Tx -orange discoloration of body fluids (benign) -hepatitis |
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Isoniazid (INH) |
Mechanism -inhibition of mycolic acid synthesis -delivered as PRODRUG and activated by CAT-G of mycobacteria -metabolized by hepatic N-Acetyltransferase -inhibits Cyto P450 Clinical Indications -part of RIPE and RI therapy for TB -can be used alone for LATENT TB (prevent reactivation) Adverse of INH -INH=Injury to Nerves and Hepatocytes! -worsened by SLOW N-ACETYLTRANSFERASE -peripheral neuropathy (excretion of B6); prevented by pyridoxine (B6) administration -ataxia -paresthesia -seizures, altered mental status -asymptomatic rise in LFT (AST and ALT) -hepatitis -Drug-induced SLE (with anti-histone Ab) -high AG metabolic acidosis -inhibition of Cytochrome P450 Resistance -downregulation of Cat-G (need to activate Isoniazid prodrug) |
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Pyrazinamide |
Mechanism Indications -RIPE TB Tx Adverse -hyperuricemia (may precipitate gout) -hepatotoxic wit possible liver necrosis |
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Ethambutol |
Mechanism -inhibition of arabinosyl transferase -inhibit carbohydrate formation for cell wall -STATIC Indications -RIPE TB Tx -Ethambutol/Azithromycin/Rifabutin for Mycobacterium Avium (HIV CD4<50) Adverse -optic neuritis (red-green colorblindness) -hepatitis |
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TB Therapy |
RIPE for 2 months (rifampin, isoniazide, pyrazinamide, ethambutol) Then RI for 4 months Adverse -all RIPE drugs associated with hepatotoxicity |
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MAC Therapy |
Ethambutol/Azithromycin/Rifampin or for HIV with CD4<50: Ethambutol/Azithromycin/Rifabutin (less potent induction of P450 which decreases ARV half-life) |
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Dapsone |
Clinical Indications -Myco Leprae -Dapsone/Clofazimine for Lepromatous leprosy Adverse -agranulocytosis -hemolytic anemia in G6PD deficiency (see bite cells and Heinz bodies) |
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Trimethoprim-Sulfamethoxazole (Bactrim) |
Mechanism -anti-folate (inhibit bacterial conversion of PABA>DHF>THF) -SMX is a PABA analog (blocks dihydropteroate synthase: PABA>DHF) TMP block dihydrofolate reductase (DHF>THF) -CIDAL Clinical Indications -first line for UTI and GI (GNR) -prostatitis -MRSA (not first line though) -Nocardia (branching, acid-fast GP) -PCP tx and prophylaxis (HIV w/ CD4<200) -Toxoplasmosis prophylaxis (HIV w/ CD4<100) -Toxo is TREATED with pyrimethamine/sulfadiazine (similar) Adverse -pancytopenia -megaloblastic anemia -teratogenic in 1st trimester (neural tube) -drug-induced SLE (anti-histone) Sulfa-specific Adverse -allergic drug reaction (fever, urticaria, rash) -hemolytic anemia in G6PD deficiency w/ bite cells and Heinz bodies -Stevens-Johnson (and Toxic Epidermal Necrolysis) -T4 RTA (with hyperkalemia) -interstitial nephritis -photosensitivity -neonatal kernicterus (jaundice) if used in last month of pregnancy (displace bilirubin bound to serum albumin, increase indirect bilirubin) -displace warfarin from albumin, result in overanticoagulation, bleeding -Inhibit P450, increase drug availability |
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Ciprofloxacin Levofloxacin Moxifloxacin |
Mechanism -Fluoroquinolone -inhibit bacterial topo (DNA gyrase) -CIDAL Clinical Indication -COMPLICATED UTI GNR (E coli, Proteus) such as in DB or UT obstruction -GI GNR -PSEUDOMONAS -Pyelonephritis -acute prostatitis -GNR osteomyelitis (especially in Sickle Cell with Salmonella) -Bacillus anthracis -Respiratory FQ (Levo or Moxi) for Strep Pneumo and atypicals (CAP) Adverse -absorption impaired by divalent cations (Ca2+, Mg2+, Fe2+), ingest hours before or after milk, antacids, iron supplements -long QT, torsade -N/V/D -tendon/cartilage damage arthropathy in the elderly, those using steroids, and fetuses (teratogen) and children <10 |
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Metronidazole |
Mechanism -generation of free radicals which disrupt DNA -CIDAL Clinical Indication -polymicrobial intraabdominal infection -Entamoeba histolytica (dysentery and liver abscess) -Giardia lamblia (acute watery diarrhea) -Trichomonas strawberry vaginitis/cervicitis (given to both patient and partner) -Gardnerella vaginosis (NOT INFLAMMATORY) -H. pylori triple therapy ampicillin substitute (clarithromycin/metro/PPI) for allergic pts -Anaerobic Bacteroides, Prevotella, Fusobacterium, Clostridium Adverse -DISULFRAM reaction with alcohol: flushing, tachycardia, palpitations, N/V, metal taste |
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Amphotericin B |
Mechanism -binds ergosterol (component of fungal cell wall) -forms pores in cell wall, causes electrolyte and macromolecule leakage -CIDAL (lysis) -always begin saline infusion before AmB to mitigate the GFR decrease Clinical Indications (BRAOD SPEC) -IV use for any SERIOUS/SYSTEMIC fungal infection (PNA, Meningitis, disseminated) -intrathecal deliver for CNS fungal infection -AmB/Flucytosine for Crypto meningitis Adverse -LESS TOXIC when delivered on LIPOSOMES -result from AmB non-selective binding of cholesterol -INFUSION rxns are universal: fever, chills, muscle spasm, vomiting, hypotension, thrombophlebitis -seizures for intrathecal delivery -CUMULATIVE tox: renal damage in 100% (pre-renal azotemia or tubular damage with T1RTA which is hypokalemic and renal magnesium wasting) with anemia due to decreased EPO Resistance -changing components of cell membrane |
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Flucytosine |
Mechanism -converted to 5FU by cytosine deaminase -halts fungal DNA/RNA synthesis Clinical Indications -AmB/Flucytosine for Crypto meningitis |
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Nystatin |
Mechanism -binds ergosterol (component of fungal cell wall) -forms pores in cell wall, causes electrolyte and macromolecule leakage -CIDAL (lysis) Clinical Indications -mucocutaneous and OP Candida (not esophageal or sytemic!!) |
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Azole antifungals |
Mechanism -inhibition of ergosterol SYNTHESIS (from lanosterol by Fungal Cyto P450) -STATIC Clinical Indications -Voraconazole for invasive Aspergillosis and for Candida esophagitis -Fluconazole for mucocutaneous Candida and given IV for Candida esophagitis -Fluconazole for Cryptococcal meningitis -Itraconazole for DIMORPHIC fungi (histo, blasto, coccidio, sporothrix) -Clotrimazole, Miconazole, Itraconazole for tinea/onycho/dermato and vaginal candida Adverse -drug interactions due to inhibition of mammalian Cyto P450 especially with VORACONAZOLE (which requires dose reduction of other drugs like cyclosporine, tacrolimus, statins) -Voraconazole vision disturbances -Ketoconazole not used systemically due to adrenal inhibition of 17,20-desmolase which is necessary for production of cholesterol (low cortisol, androgen, estrogen) |
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Griseofulvin |
Mechanism -binds fungal microtubules, halts mitosis -accumulates in keratin containing tissues (skin) Clinical Indication -PO for dermatophytoses (scalp/skin) Adverse -CYTO P450 INDUCTION -GI distress -HA -rash -hepatotoxicity -granulocytopenia |
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Terbinafine |
Mechanism -interferes with ergosterol synthesis by inhibiting SQUALENE EPOXIDASE -leads to toxic accumulation of SQUALENE inside fungal cells -CIDAL Indication -topical for dermatophytoses -PO first line for tinea capitis and ONYCHOMYCOSIS Adverse -Diarrhea -hepatotoxicity |
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Echinocandins: Caspofungin Micafungin Anidulafungin |
Mechanism -inhibit beta-1,3-glucan -disrupt fungal cell wall synthesis Indications -IV for SYSTEMIC CANDIDA, including ESOPHAGEAL candidiasis -Prophylaxis in transplant patients -invasive aspergillosis Adverse -very WELL TOLERATED -rarely flushing and GI adverse -anidulafungin may trigger histamine release during IV infusion |
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Interferon a |
Indications -HBV/HCV (PEG-IFNa plus Ribavirin) -PEG-IFNa for longer half life -hairy (B) cell leukemia -malignant melanoma -HHV8/KSV -HPV condyloma accuminata -RCC Adverse 6 hours after dosing, resolves after 1 week: -flu-like sxs Chronic toxicity: -profound fatigue -tinnitus -retinopathy -confusion -myelosupression -drug-induced SLE (anti-Histone, anti-dsDNA) |
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Interferon b |
Indications -relapsing MS |
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Interferon y |
Indications -Chronic Granulomatous Disease macrophage activation (NADPH Oxidase deficiency) |
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Ribavirin |
Mechanism -guanosine nucleoside analog Indications -Ribavirin plus PEG-IFNa -RSV historically (now more palivizumab) Adverse -dose-dependent HEMOLYTIC ANEMIA (occurs in 10-20%) -teratogenic |
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Sofosbuvir |
Mechanism -nucleoside analog (NS5B RNA-dependent RNA Polymerase inhibitor) Indication -HCV genotypes 1-4 -can be combined with RIBAVIRIN without the need for IFN (and its associated toxicities!) Adverse -fatigue -nausea |
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Simeprevir |
Mechanism -Protease (NS3/4A) inhibitor Indication -HCV genotype 1 Adverse -photosensitivity -rash -inhibits Cyto P450 |
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Acyclovir |
Mechanism -guanosine nucleoside analog -must be phosphorylated by VIRAL THYMIDINE KINASE (TK) allowing for viral specificity -inhibits viral DNA-dependent DNA Pol (termination of viral DNA synthesis) Indications -HSV 1, 2, VZV -NO ACTION against CMV/EBV! (lack TK) -IV for HSV1 encephalitis, neonatal HSV, serious VZV -prophylaxis for HIV, transplant, pregnant (week 36) Adverse -interstitial nephritis & crystalline nephropathy (prevent with hydration and slow infusion) -delirium confusion vertigo hallucinations Resistance -mutation of thymidine kinase (TK) |
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Valacyclovir |
Mechanism -Acyclovir prodrug with better PO AVAILABILITY Indications -daily suppressive therapy for recurrent HSV -preferable for VZV (less frequent dosing) -effective in active shingles if given withing 3 days of sxs onset Adverse -delirium confusion vertigo hallucinations |
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Famcyclovir |
Indications -preferable for VZV (less frequent dosing) -effective in active shingles if given withing 3 days of sxs onset Adverse -delirium confusion vertigo hallucinations |
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Cidofovir |
Mechanism -direct inhibition of viral DNA-dependent DNA Pol -does NOT require TK phosphorylation, only cellular phosphorylation Indications -Acyclovir/Ganciclovir-resistant HSV, VZV, CMV -especially found in AIDS pts -IV administration always with PROBENECID (blocks tubular Cidofovir secretion) for RENAL PROPHYLAXIS Adverse -delirium confusion vertigo hallucinations -nephrotoxicity (proteinuria azotemia acidosis) |
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Foscarnet |
Mechanism -PYROPHOSPHATE analog -direct inhibition of viral DNA-dependent DNA Pol -already in active form, does not require ANY CELLULAR PHOSPHORYLATION Indications -Acyclovir/Ganciclovir-resistant HSV/VZV/CMV Adverse -delirium confusion vertigo hallucinations seizures -reversible renal insufficiency -hypocalcemia/hypomagnesemia (chelator) and subsequent HYPOKALEMIA |
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Ganciclovir |
Mechanism -guanosine analog -first phosphorylation step by UL97 (CMV kinase) Indications -hemorrhagic/infiltrative CMV retinitis (AIDS CD4<50) -CMV prophylaxis in transplant and ImDef Adverse -MYELOSUPPRESSION Resistance -UL97 CMV kinase mutations |
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Valganciclovir |
Mechanism -ganciclovir prodrug w/ better PO AVAILABILITY -guanosine analog phosphorylated by UL97 (CMV kinase) Indications -CMV retinitis -CMV prophylaxis in transplant and ImDef Adverse -MYELOSUPPRESSION |
