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55 Cards in this Set
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Acyclovir
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antiviral
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-Used in high dose IV formulation in neonatal infection, CNS infection in adults
-Used in lower dose for mucocutaneous disease treatment and prophylaxis -Frequent oral dosing necessary -Poor oral bioavailability -Toxicities more likely with high dose -Nausea, headache, Crystal formation in renal tubules with impaired renal function |
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Valacyclovir, Famciclovir
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antiviral
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-Excellent oral bioavailability
-Valacyclovir is valine ester of acyclovir -Actively transported by the small bowel -Both approved for suppressive therapy of frequent genital herpes outbreaks (once or twice daily) -Both useful for treatment of shingles (reactivation of latent varicella-zoster) |
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Ganciclovir, Valganciclovir
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antiviral
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-Approved for treatment, prevention of CMV disease
-Ganciclovir used IV mostly, poor oral bioavailability Intravitreal injections or implants for CMV retinitis -Improved oral bioavailability of Valganciclovir Valine ester actively transported by small bowel -Toxicities mostly related to bone marrow suppression Anemia Neutropenia Thrombocytopenia |
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Ribavirin
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antiviral
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-Synthetic guanosine analogue with an incomplete purine ring
-Once phosphorylated, interferes with transcription of viral RNA and the synthesis of viral ribonucleoprotein complexes -Available as aerosol for treatment of respiratory syncitial virus (RSV) -Used orally for Hepatitis C virus. -Toxicity Bronchospasm may occur during aerosol therapy Teratogenic in a variety of mammalian species Hemolytic anemia common when given orally |
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Oseltamivir
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antiviral
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- neuraminidase inhibitors, structural analogues of sialic acid, used as a receptor by influenza viruses
-Influenza A and B - Oseltamivir has good oral bioavailability due to the presence of an ethyl ester moiety - Major side Effect - Mild GI side effects (nausea and vomiting, ameliorated by taking with food), Rare neuropsychiatric effects |
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Zanamivir
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antiviral
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- neuraminidase inhibitors, structural analogues of sialic acid, used as a receptor by influenza viruses
-Influenza A and B - Major side effect: Bronchospasm; use with caution if underlying airway disease. |
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Trimethoprim/Sulfamethoxazole
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anti-metabolite
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= Sulfonamides
- Bacterial folate synthesis inhibitor (tetrahydroptroic acid synthetase) - highly protein bound, hepatic metabolism and urinary excretion that can form crystals, can cause severe allergic reaction (SJS), hematopoeitic production issues, kernicterus (like Reye's) - can interact with sulfonylurea (hypoglycemic) and phenytoin (displace from albumin) - resistance through PABA overproduction or enzyme mutation =Trimethoprim - DHFR inhibitor -Can cause nausea, vomiting, hematopoetic, or hyperkalemia =TM/SMX -Widely active against Gram positives and Gram negatives -Increasing resistance in E. coli limits current use in UTIs -Now commonly used to treat skin infections with community associated methicillin-resistant Staphylococcus aureus (CA-MRSA) -Pneumocystis jiroveci pneumonia prophylaxis (and similar drugs for treatment) -Caveats: Limited activity vs. Group A streptococcus Enterococci are intrinsically resistant |
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Penicillin G, Penicillin V
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B-lactam inhibitor - Penicillins
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- Pen G is IV/IM, Pen V is PO
-Drug of choice for Streptococcal infection, syphilis, spirochetes - Full list: Enterococcus, pneumococcus, clostridium tetnas, perfringens actinomyces - Benzathine-pen used for sensitizaiton of patients how have just rash allergies slow release - If patient has had a rash in history, may still use; do not use if there is h of anaphylaxis, urticaria -Highly susceptible to beta lactamases - |
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Ampicillin (+/-) Sulbactam
Amoxicillin (+/-) Clavulanate |
B-lactam inhibitor - Aminopenicillins
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-Enhanced Gram negative activity (due to amination)
-Remain highly susceptible to beta lactamases and are often combined with beta lactamas inhibitors (sulbactam, clavulanate) - G+ (Streptococcus sp, Staphylococcus sp, Listeria), G- (Klebsiella sp, E. coli, H. influenzae, P. mirabilis, Shigella sp, Salmonella sp) - amoxicillin + omeprazole + clarithromycin = triple therapy for h. pylori - SE: GI symptoms, others of B-lactams |
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Cefazolin, Cephalexin
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B-lactamase - Cephalosporins (1st gen)
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Cefazolin (IV), Cephalexin (PO)
- Good gram positive, limited gram negative activity (GN resistance common) - designed to be more B-lactamase resistant than aminopenicillins - Good coverage gram(+) bacilli & cocci, (Strep, Staph (except Enterococcus); some gram(–) (PEK - E. coli, Proteus, Klebsiella) |
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Cefuroxime, Cefoxitin
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B-lactam - Cephalosporins (2nd gen)
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Cefuroxime (PO), Cefoxitin (IV)
- Cefoxitin and cefotetan have good anaerobic activity - Respiratory tract infections: S. pneumo, H. influenzee, Moraxella catarrhalis - Intra-abdomial infections: anaerobic bacteria: bacteroides fragilis, pre-op bowel surgery |
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Ceftriaxone
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B-lactam - Cephalosporins (3rd gen)
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- IV/IM
-gonorrhea - Only 3rd gen with usable activity against S. aureus -not for children, inteferes with bilirubin = Common for 3rd gens - All have very good activity against gram negatives - Pneumonia, meningitis, pyelonephritis + metronidazole, S. pneumonae, intraabdomin infections - : interferes with vit K depend clotting factors – poor coagulation, dec etOH metabolism, rash, leukopenia, Inc trasaminases |
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Ceftazidime
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B-lactam - Cephalosporins (3rd gen)
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- IV
- Pseudomonas aeruginosas = Common for 3rd gens - All have very good activity against gram negatives - Pneumonia, meningitis, pyelonephritis + metronidazole, S. pneumonae, intraabdomin infections - : interferes with vit K depend clotting factors – poor coagulation, dec etOH metabolism, rash, leukopenia, Inc transaminases |
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Cefixime
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B-lactam - Cephalosporins (3rd gen)
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- Cefixime- PO, STD clinics but no longer recommended
= Common for 3rd gens - All have very good activity against gram negatives - Pneumonia, meningitis, pyelonephritis + metronidazole, S. pneumonae, intraabdomin infections - : interferes with vit K depend clotting factors – poor coagulation, dec etOH metabolism, rash, leukopenia, Inc trasaminases |
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Cefdinir
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B-lactam - Cephalosporins (3rd gen)
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- PO (good tasting liquid for pediatric use)
= Common for 3rd gens - All have very good activity against gram negatives - Pneumonia, meningitis, pyelonephritis + metronidazole, S. pneumonae, intraabdomin infections - : interferes with vit K depend clotting factors – poor coagulation, dec etOH metabolism, rash, leukopenia, Inc trasaminases |
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Cefepime
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B-lactam - Cephalosporins (4th gen)
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- Psuedonomas aeruginosa,
- G+ and G- Strep, Staph (MSSA only), K. pneumonia, E. coli, enterobacter UTI, febrile neutropenia, skin/soft tissue infections SE: rash, fever, hemolysis (coombs test), seizures |
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Vancomycin
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non-B-lactam cell wall inhibitor
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- Hospital acquired MRSA
- All G+, serious MRSA, enterococcus (faecalis and faecium), S epidermidis, endocarditis by staph/strep - IV for systemic treatment (not absobed PO) - PO for C. diff - Used if penecillin allergy if cephalosporins are resistant -Synergy with aminoglycosides - Vancomycin resistant enterococcus (VRE) common in hospital: terminal D-Ala D-Ala changed to D-Ala D-Lac -SE: red man syndrome- fast IV infusion, treat with anti-histamine, ototoxic, nephrotoxic, neutropenia |
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Tetracyclines, Doxycycline
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Protein synthesis inhibitors, 30s subunit
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- CA-MRSA
- Atypical pneumonia: klebsiella, chlamydia, mycoplasma - Malaria prophylaxis - Rickettsia, C. trachomatis, borrelia, leptospira, tick-born brucella, acne, myco, pneumonia (2nd line erythro) - Bind to 30S subunit of ribosome, preventing access of aminoacyl tRNA to acceptor (A) site on the mRNA-ribosome complex - don't give with dairy or other divalent cations - Distribute to bones and teeth - DONT GIVE TO KIDS/PREGGERS: Cross the placenta where they can stain developing teeth - Elimination: glucuronidation, with urinary excretion (most) and minor biliary excretion, EXCEPTION: Doxycycline is almost entirely excreted in bile safe in renal failure - GI upset, chance for sueperinfectoin, phototox, vestibular upset...can cause liver failure at very high doses - Resistance mech: Drug efflux, target site mod, porin mutation |
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Daptomycin
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Cell membrane electron transport
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- Bacterialcidal
- creates a K+ channel - G+ only, like vancomycin - MRSA, VRE, S. pyogenes, s. agalactiae, doesn’t work for pneumonia (inactivated by surfactant)! - Use this and clin and protein synth inhibitors for toxin producing bugs - SE: myopathy with elevated CK, eosinophillic pneumonia |
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Rifampin
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Rifamycin class
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- Inhibits DNA-dependent RNA polymerase in bacterial cells, preventing transcription
- Active against gram positives (S. aureus), mycobacteria - SE: Hepatotoxicity (cholestatic), nausea, vomiting -Extensive drug interactions (enhances clearance of coumadin, digoxin, azole antifungals, antiretrovirals) -Stains excretions red-orange |
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Metronidazole
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Electron acceptor
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- Acts as an electron acceptor; once activated by reduction, it damages DNA and other macromolecules
- Available IV and PO - Penetrates well into all tissues - Highly bactericidal for anaerobic bacteria, no activity against other Gram positives or Gram negatives - Also used to treat wide array of protozoans, Trichomoniasis, Giardiasis, Amebiasis, Gardonella - SE: Disulfiram-like reactions with alcohol. Sensory neuropathy with prolonged use. "anaerobic bacterial and protozoal infections in the following conditions: Amebiasis, symptomatic and asymptomatic trichomoniasis; skin and skin structure infections, bone and joint infections, CNS infections, endocarditis, gynecologic infections, intra-abdominal infections (as part of combination regimen), respiratory tract infections (lower), systemic anaerobic infections; treatment of antibiotic-associated pseudomembranous colitis (AAPC); as part of a multidrug regimen for H. pylori eradication to reduce the risk of duodenal ulcer recurrence; surgical prophylaxis (colorectal); " |
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Treatment: Anaerobic strep
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Penicillin
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Treatment: GI infection - Oropharyngeal (eg. abscess)
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Clindamycin
Penicillin Penicillin class + beta lactamase inhibitor |
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Treatment: GI infection - Intestinal (eg ruptured appendix)
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Metronidazole
Cefoxitin/Cefotetan Carbapenem Penicillin class + beta lactamase inhibitor Clindamycin |
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Treatment: Abcesses
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Metronidazole
Chloramphenicol (not in US) |
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Treatment: VRE
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Daptomycin, Linezolid
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Treatment: CA-MRSA
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Clindamycin
TMP/SMX Tetracylcines Linezolid Daptomycin Vanc |
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Levofloxacin
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Fluoroquinalones
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- Better S. pneumoniae
- Target DNA gyrase in G- and TopoIV in G+ - Orally bio available, but don't give with milk or divalent cations - GI, hepatic tox, tendinopathy, cartilage concerns - UTI, GI infections, pneumonia, osteomyelitis, Chlamydia (resistance in Gonorrhea) - Prophylxis against anthrax and n. meninigitidis |
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Ciprofloxacin
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Fluoroquinalones
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- Better Pseudomonas
- Target DNA gyrase in G- and TopoIV in G+ - Orally bio available, but don't give with milk or divalent cations - GI, hepatic tox, tendinopathy, cartilage concerns - UTI, GI infections, pneumonia, osteomyelitis, Chlamydia (resistance in Gonorrhea) - Prophylxis against anthrax and n. meninigitidis |
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Treatment: pseudomonas
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-Fluoroquinalones (cipro- preferred)
- Penicillins: Carbenicillin, Ticarcillin, Piperacillin (+ tazobactam) - imipenem - cefepime, ceftazidine |
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Isoniazid
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Unknown, mycolic acid synthesis
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- Part of initial treatment (RIPE) and continuation phase with rifampin
SE: -Hepatotoxicity - Risk increases with age, alcohol use - Peripheral neuropathy - Vitamin B6 (pyridoxine) helps prevent |
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Ethambutol
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Cell wall inhibitor
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- inhibits arabinosyl transferase resulting in impaired mycobacterial cell wall synthesis
SE: Optic neuritis...also hepatotoxic |
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Pyrazinamide
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Unknown mechanism
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Part of first-line TB treatment
SE: Hepatotox, malaise, GI upset, arthralgia, myalgia, gout, photosensitivity |
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Amphotericin B
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Polyene anti-fungal
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- Molecules form channel allowing loss of intracellular cations
- IV for systemic use: Infusion–related reactions (~75%) of fever, chills, myalgias, nausea, vomiting, headache...these can be minimized by slow infusion or newer fromulations - Works against most fungi, but some candida and aspergillus are resistant - SE:Concern with nephrotox |
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Nystatin
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Polyene anti-fungal
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Generally a topical treatment
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Caspofungin
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Echinocandin
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- beta glucan (cell wall) synthetase inhibitor
- Well tolerated but alters tacrolimus metabolism - IV - Useful for treatment of aspergillus and candida |
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Terbinafine
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squalene epoxidase inhibitor
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- inhibits ergosterol synthesis
- Oral and topical formulations - Indicated for onychomycosis, tinea - GI upset, hepatotoxicity |
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Imipenem, Ertapenem
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Carbapenems
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-Not active against MRSA
- Inhibits cell wall synthesis - Metabolized in kidneys can cause nephrotoxicity, do not use if allergic to penicillin, seizures - Imipenem IV [includes pseudomonas] - Ertapenem IV [no activity against pseudomonas, longer half life, diabetic foot inf] |
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Piperacillin +/- Tazobactam
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Anti-pseudomonas penicillins
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- pseudomonas, Enhanced Gram negative coverage (due to extensive side chain addition)
- Highly susceptible to beta lactamases - may alter sodium load |
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Methicillin, oxacillin, dicloxacillin
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Anti-staph penicillins
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- Use for MSSA
- Methicillin IV - Oxacillin IV - Dicloxacillin PO - More stable to beta lactamases, due to modifications near beta lactam ring - Poor entry into gram negative bacteria, active against gram positives only - SE: normal B lactam things, methicillin - interstitial nephritis |
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Fluconazole
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Azole
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- Active against most Cryptococcus, Candida species (C. krusei resistant)
Aspergillus species are resistant =Azoles - inhibition of ergosterol synthesis by interfering with lanosterol 14a demethylase, a fungal CYP450 molecule - CSF penetration by fluconazole and voriconazole - Interfere with our CYP450 metabolism of many other drugs: must watch drug-srug interaction |
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Voriconazole
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Azole
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- the treatment of choice for most forms of invasive aspergillosis
- Active against most Candida species |
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Posaconazole
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Azole
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- Active against most Candida species
- Active against most Aspergillus species - Active against many molds (e.g. the agents of zygomycosis) - PO only |
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Chloroquine
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Quinacrine
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- Inhibits polymerization of hemozoin in Plasmodium food vacuole
- oral, cheap, weekly dosing - widespread resistance in p. falciprum - causes itching in africans |
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Mefloquine (Lariam)
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Later generation quinacrine
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- Weekly dosing
- Active against chloroquine resistant malaria - Toxicities: vertigo, lightheadedness, neuropsychiatric (nightmares, psychosis, suicide risk) |
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Atovaquone proguanil (Malarone)
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Combination anti-malarial
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-Atovaqone inhibits mitochondrial electron transport
- Proguanil acts as a DHFR inhibitor - Expensive, daily dose - Toxicities: GI upset, rash, but overall well tolerated |
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Artemesinins
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herbal derivatives—qinghaosu
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- Unknown mechanism
? Interference with plasmodial sarcoplasmic/endoplasmic calcium ATPase (SERCA) - Used in combination - Not licensed for use in US, but a mojor drug worldwide |
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Praziquantel
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Anti-hemlinth
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- Unknown mechanism of action?membrane permeability
- Schistosomiasis, Chlonorchiasis, other flukes, but not Fasciola hepatica - Toxicities: GI upset, abdominal pain, rash |
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Chloroquine
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Quinacrine
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- Inhibits polymerization of hemozoin in Plasmodium food vacuole
- oral, cheap, weekly dosing - widespread resistance in p. falciprum - causes itching in africans |
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Albendazole, Mebendazole
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tubilin inhibitors
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- Inhibit tubulin polymerization, microtubule formation in worms
- Pinworm, whipworm, hookworm, ascariasis, Echinoccocus, cysticercosis, trichinosis, Strongyloidiasis, toxocariasis, cutaneous larva migrans, Filaria |
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Mefloquine (Lariam)
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Later generation quinacrine
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- Weekly dosing
- Active against chloroquine resistant malaria - Toxicities: vertigo, lightheadedness, neuropsychiatric (nightmares, psychosis, suicide risk) |
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Atovaquone proguanil (Malarone)
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Combination anti-malarial
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-Atovaqone inhibits mitochondrial electron transport
- Proguanil acts as a DHFR inhibitor - Expensive, daily dose - Toxicities: GI upset, rash, but overall well tolerated |
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Artemesinins
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herbal derivatives—qinghaosu
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- Unknown mechanism
? Interference with plasmodial sarcoplasmic/endoplasmic calcium ATPase (SERCA) - Used in combination - Not licensed for use in US, but a mojor drug worldwide |
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Praziquantel
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Anti-hemlinth
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- Unknown mechanism of action?membrane permeability
- Schistosomiasis, Chlonorchiasis, other flukes, but not Fasciola hepatica - Toxicities: GI upset, abdominal pain, rash |
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Albendazole, Mebendazole
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tubilin inhibitors
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- Inhibit tubulin polymerization, microtubule formation in worms
- Pinworm, whipworm, hookworm, ascariasis, Echinoccocus, cysticercosis, trichinosis, Strongyloidiasis, toxocariasis, cutaneous larva migrans, Filaria |
