Microbiology - Pharmacology Flashcards
How do penicillin drugs work?
Binds to penicillin-binding proteins (transpeptidases) and blocks cross-linking of peptidoglycan
Can be inactivated by penicillinase/β-lactam
Penicillin G
Penicillinase-sensitive penicillin
IV and IM forms
Bactericidal from gram + cocci/rods, gram - cocci, spirochetes
SA: hypersensitivity reactions, hemolytic anemia
Penicillin V
Penicillinase-sensitive penicillin
Oral
Bactericidal from gram + cocci/rods, gram - cocci, spirochetes
SA: hypersensitivity reactions, hemolytic anemia
Ampicillin
Extended-spectrum penicillinase-sensitive aminopenicillin
Can be combined with clavulanic acid (β-lactamase inhibitor)
SA: hypersensitivity reactions, rash, pseudomembranous colitis
Amoxicillin
Extended-spectrum penicillinase-sensitive aminopenicillin
Better oral bioavailability than ampicillin
Can be combined with clavulanic acid (β-lactamase)
SA: hypersensitivity reactions, rash, pseudomembranous colitis
Oxacillin
Narrow-spectrum penicillinase-resistant penicillin
Resistant to penicillinase (bulky R group blocks access to β-lactam ring)
Indicated for MSSA
SA: hypersensitivity reactions, interstitial nephritis
Nafcillin
Narrow-spectrum penicillinase-resistant penicillin
Resistant to penicillinase (bulky R group blocks access to β-lactam ring)
Indicated for MSSA
SA: hypersensitivity reactions, interstitial nephritis
Dicloxacillin
Narrow-spectrum penicillinase-resistant penicillin
Resistant to penicillinase (bulky R group blocks access to β-lactam ring)
Indicated for MSSA, mastitis
SA: hypersensitivity reactions, interstitial nephritis
Ticarcillin
Extended-spectrum antipseudomonal carboxypenicillin
Can be combined with a β-lactamase inhibitor (clavulanic acid, sulbactam, tazobactam)
Indicated for pseudomonas and gram - rods
SA: hypersensitivity reactions
Piperacillin
Extended-spectrum antipseudomonal carboxypenicillin
Can be combined with a β-lactamase inhibitor (clavulanic acid, sulbactam, tazobactam)
Indicated for pseudomonas and gram - rods
SA: hypersensitivity reactions
How do cephalosporins work?
β-lactam drugs that inhibit cell wall synthesis by inhibiting peptidoglycan cross-linking
Less susceptible to penicillinases
Bactericidal
Low cross-reactivity with penicillins
Cefazolin
1st generation cephalosporin
Indicated for gram + cocci, Proteus mirabilis, E. coli, Klebsiella pneumoniae
Used prior to surgery to prevent S. aureus wound infections
SA: hypersensitivity reactions, vitamin K deficiency, ↑ nephrotoxicity of aminoglycosides
Cephalexin
1st generation cephalosporin
Indicated for gram + cocci, Proteus mirabilis, E. coli, Klebsiella pneumoniae
SA: hypersensitivity reactions, vitamin K deficiency, ↑ nephrotoxicity of aminoglycosides
Cefoxitin
2nd generation cephalosporin
Indicated for gram + cocci, Haemophilus pneumoaniae, Enterobacter aerogenes, Neisseria, Proteius mirabilis, E. coli, Klebsiella pneumoniae, Serratia marcescens
SA: hypersensitivity reactions, vitamin K deficiency, ↑ nephrotoxicity of aminoglycosides
Cefaclor
2nd generation cephalosporin
Indicated for gram + cocci, Haemophilus pneumoaniae, Enterobacter aerogenes, Neisseria, Proteius mirabilis, E. coli, Klebsiella pneumoniae, Serratia marcescens
SA: hypersensitivity reactions, vitamin K deficiency, ↑ nephrotoxicity of aminoglycosides
Cefuroxime
2nd generation cephalosporin
Indicated for gram + cocci, Haemophilus pneumoaniae, Enterobacter aerogenes, Neisseria, Proteius mirabilis, E. coli, Klebsiella pneumoniae, Serratia marcescens
SA: hypersensitivity reactions, vitamin K deficiency, ↑ nephrotoxicity of aminoglycosides
Ceftriaxone
3rd generation cephalosporin
Indicated for serious gram - infections resistant to other β-lactams like meningitis and gonorrhea
SA: hypersensitivity reactions, vitamin K deficiency, ↑ nephrotoxicity of aminoglycosides
Cefotaxime
3rd generation cephalosporin
Indicated for serious gram - infections resistant to other β-lactams
SA: hypersensitivity reactions, vitamin K deficiency, ↑ nephrotoxicity of aminoglycosides
Ceftazidime
3rd generation cephalosporin
Indicated for serious gram - infections resistant to other β-lactams like pseudomonas
SA: hypersensitivity reactions, vitamin K deficiency, ↑ nephrotoxicity of aminoglycosides
Cefepime
4th generation cephalosporin
↑ activity against Pseudomonas and gram + organisms
SA: hypersensitivity reactions, vitamin K deficiency, ↑ nephrotoxicity of aminoglycosides
Ceftaroline
5th generation cephalosporin
Broad gram + and gram - coverage including MRSA but not Pseudomonas
SA: hypersensitivity reactions, vitamin K deficiency, ↑ nephrotoxicity of aminoglycosides
How do monobactams (e.g. aztreonam) work?
Monobactams bind to penicillin-binding proteins to prevent peptidoglycan cross-linking of the cell wall
Synergistic with aminoglycosides
No cross-allergenicity with penicillins
Resistant to β-lactamase
Indicated for gram - rods only in patients allergic to penicillins or have renal insufficiency and cannot tolerate aminoglycosides
SA: GI upset
Imipenem
Broad-spectrum β-lactamase-resistent carbapenem
Indicated for gram + cocci, gram - rods, and anaerobes
SA: GI distress, skin rash, CNS toxicity/seizures
Always administer with dilastin (inhibitor of renal dehydropeptidase I) to decreased inactivation of the drug in the renal tubules
Meropenem
Broad-spectrum β-lactamase-resistent carbapenem
Indicated for gram + cocci, gram - rods, and anaerobes
SA: GI distress, skin rash, decreased risk of CNS toxicity/seizures
Ertapenem
Broad-spectrum β-lactamase-resistent carbapenem
Indicated for gram + cocci, gram - rods, anaerobes, limited pseudomonas coverage
SA: GI distress, skin rash, CNS toxicity/seizures
Doripenem
Broad-spectrum β-lactamase-resistent carbapenem
Indicated for gram + cocci, gram - rods, anaerobes, limited pseudomonas coverage
SA: GI distress, skin rash, CNS toxicity/seizures
Vancomycin
Glycopeptide that binds to D-ala D-ala portion of cell wall precursors to inhibit cell wall peptidoglycan formation
Bactericidal
Indicated for gram + only, including MRSA and C. difficile (oral formulation)
SA: nephrotoxicity, ototoxicity, thrombophlebitis, red man syndrome (prevent with slow infusion rate and antihistamines)
Resistance via amino acid modifatio to D-ala D-lac
Mnemonic for antibiotics that inhibit protein synthesis
Buy AT 30, CCEL at 50
30S inhibitors:
A = aminoglycosides (bactericidal)
T = tetrocyclines (bacteriostatic)
50S inhibitors:
C = chloramphenicol, clindamycin (bacteriostatic)
E = erythromycin (macrolides) (bacteriostatic)
L = linezolid (variable)
How do aminoglycosides work?
Aminoglycosides inhibit the formation of the initition complex and cause misreading of mRNA and block translocation
Require O2 for uptake so ineffective against anaerobes
Bactericidal
Resistance when bacterial transferase enzymes inactivate the drug by acetylation, phosphorylation, or adenylation
Gentamicin
Aminoglycoside (inhibits initiation complex and translocation)
Indicated for severe gram - rod infections
Synergistic with β-lactam antibiotics
SA: nephrotoxicity (especially when used with cephalosporins), neuromuscular blockade, ototoxicity (esp. when used with loop diuretics), teratogen
Neomycin
Aminoglycoside (inhibits initiation complex and translocation)
Indicated for severe gram - rod infections, good for bowel surgery
Synergistic with β-lactam antibiotics
SA: nephrotoxicity (especially when used with cephalosporins), neuromuscular blockade, ototoxicity (esp. when used with loop diuretics), teratogen
Amikacin
Aminoglycoside (inhibits initiation complex and translocation)
Indicated for severe gram - rod infections
Synergistic with β-lactam antibiotics
SA: nephrotoxicity (especially when used with cephalosporins), neuromuscular blockade, ototoxicity (esp. when used with loop diuretics), teratogen
Tobramycin
Aminoglycoside (inhibits initiation complex and translocation)
Indicated for severe gram - rod infections
Synergistic with β-lactam antibiotics
SA: nephrotoxicity (especially when used with cephalosporins), neuromuscular blockade, ototoxicity (esp. when used with loop diuretics), teratogen
Streptomycin
Aminoglycoside (inhibits initiation complex and translocation)
Indicated for severe gram - rod infections
Synergistic with β-lactam antibiotics
SA: nephrotoxicity (especially when used with cephalosporins), neuromuscular blockade, ototoxicity (esp. when used with loop diuretics), teratogen
How do tetracyclines work?
Binds to 30S and prevents attachment of tRNA
Limited CNS penetration
Avoid taking with milk (Ca2+), antacids (Ca2+ or Mg2+), or iron-containing preparations because divalent cations inhibit absorption in the gut
Resistance 2/2 plasmid-encoded transport pumps
Tetracycline
Tetracycline (prevents tRNA binding to 30S)
Indicated for rickettsia (Lyme), Mycoplasma pneumoniae, and chlamydia, acne
SA: GI distress, discoloration of teeth and inhibition of bone growth in children → contraindicated in pregnancy, photosensitivity
Avoid milk, antacid, iron 2/2 ↓ uptake in the gut
Doxycycline
Tetracycline (prevents tRNA binding to 30S)
Indicated for rickettsia (Lyme), Mycoplasma pneumoniae, and chlamydia, acne
SA: GI distress, discoloration of teeth and inhibition of bone growth in children → contraindicated in pregnancy, photosensitivity
Avoid milk, antacid, iron 2/2 ↓ uptake in the gut
Minocycline
Tetracycline (prevents tRNA binding to 30S)
Indicated for rickettsia (Lyme), Mycoplasma pneumoniae, and chlamydia, acne
SA: GI distress, discoloration of teeth and inhibition of bone growth in children → contraindicated in pregnancy, photosensitivity
Avoid milk, antacid, iron 2/2 ↓ uptake in the gut
How do macrolides work?
Binds to 50S to block translocation
SA: GI motility, prolonged QT → arrhythmias, acute cholestatic hepatitis, rash, eosinophilia, increases serum concentration of theophyllines and oral anticoagulants
Resistance from methylation of 23S rRNA-binding site preventing binding
Azithromycin
Macrolide (binds to 50S preventing translocation)
Indicated for atypical pneumonias including MAC, chlamydia, gram + cocci
SA: GI motility, prolonged QT → arrhythmias, acute cholestatic hepatitis, rash, eosinophilia, increases serum concentration of theophyllines and oral anticoagulants
Clarithromycin
Macrolide (binds to 50S preventing translocation)
Indicated for atypical pneumonias, chlamydia, gram + cocci
SA: GI motility, prolonged QT → arrhythmias, acute cholestatic hepatitis, rash, eosinophilia, increases serum concentration of theophyllines and oral anticoagulants
Erythromycin
Macrolide (binds to 50S preventing translocation)
Indicated for atypical pneumonias, chlamydia, gram + cocci, prophylaxis for gonococcal or chlamydia conjuctivitis in newborn
SA: GI motility, prolonged QT → arrhythmias, acute cholestatic hepatitis, rash, eosinophilia, increases serum concentration of theophyllines and oral anticoagulants
Cloramphenicol
Blocks peptidyltransferase at 50S
Bacteriostatic
Indicated for bacterial meningitis, Rocky Mountain Spotted Fever
SA: amenia, a plastic anemia, gray baby syndrome (premature infants lack UDP-glucuronyl transferase)
Resistance from plasma-encoded acetyltransferase inactivation
Clindamycin
Blocks translocation at 50S
Bacteriostatic
Indicated for oral and lung anaerobic infections, invasive Group A strep (Treats anaerobes above the diaphragm)
SA: pseudomembranous colitis, fever, diarrhea
Sulfamethoxazole (SMX)
Sulfonamide antibiotic inhibits dihydropteroate synthase blocking conversion of para-aminobenzoic acid (PABA) and pteridine to dihydropteroic acid in the folic acid pathway
Indicated for gram +, gram -, Nocardia, Chlamydia
SA: hypersensitivity reactions, hemolysis if G6PD deficient, nephrotoxicity, photosensitiity, kernicterus in infants, displace other drugs from albumin (e.g. warfarin)
Resistance via altered dihydropteroate synthase, ↓ uptake, ↑ PABA synthesis
Sulfisoxazole
Sulfonamide antibiotic inhibits dihydropteroate synthase blocking conversion of para-aminobenzoic acid (PABA) and pteridine to dihydropteroic acid in the folic acid pathway
Indicated for gram +, gram -, Nocardia, Chlamydia
SA: hypersensitivity reactions, hemolysis if G6PD deficient, nephrotoxicity, photosensitiity, kernicterus in infants, displace other drugs from albumin (e.g. warfarin)
Resistance via altered dihydropteroate synthase, ↓ uptake, ↑ PABA synthesis
Sulfadiazine
Sulfonamide antibiotic inhibits dihydropteroate synthase blocking conversion of para-aminobenzoic acid (PABA) and pteridine to dihydropteroic acid in the folic acid pathway
Indicated for gram +, gram -, Nocardia, Chlamydia
SA: hypersensitivity reactions, hemolysis if G6PD deficient, nephrotoxicity, photosensitiity, kernicterus in infants, displace other drugs from albumin (e.g. warfarin)
Resistance via altered dihydropteroate synthase, ↓ uptake, ↑ PABA synthesis
Trimethoprim (TMP)
Inhibits dihydrofolate reductase preventing conversion of dihydrofolic acid to tetrahydrofolic acid in the folic acid pathway
Used with SMX for UTIs, Shigella, Salmonella, PCP treatment and prophylaxis, toxoplasmosis prophylaxis
SA: megaloblastic anemia, leukopenia, granulocytopenia
How do fluoroquinolones work?
Inhibits DNA gyrase (topoisomerase II) and topoisomerase IV
Bactericidal
Avoid taking with antacids
SA: GI upset, superinfections, skin rashes, headache, dizziness, tendonitis, tendon rupture in patients > 60 taking prednisone, prolonged QT interval, cartilage damage → contraindicated in pregnancy, breastfeeding, children < 18
Resistance from efflux pumps, mutation in DNA gyrase
Ciprofloxacin
Fluoroquinolong (inhibits DNA gyrase/topoisomerase II and topoisomerase IV)
Bactericidal
Avoid taking with antacids
Indicated for gram - rods in urinary and GI tracks, Pseudomonas, Neisseria, meningococcal prophylaxis in adults
SA: GI upset, superinfections, skin rashes, headache, dizziness, tendonitis, tendon rupture in patients > 60 taking prednisone, prolonged QT interval, cartilage damage → contraindicated in pregnancy, breastfeeding, children < 18
Metronidazole
Forms free radical toxic metabolites that damage DNA
Bactericidal, antiprotozoal
Indicated for Giardia, Entamoeba, Gardnerella vaginalis, anaerobes, H. pylori (anaerobic infections below the diaphragm)
SA: disulfiram-like reaction (severe flushing, tachycardia, hypotension) with alcohol, headache, metallic taste
Isoniazid (INH)
↓ synthesis of mycolic acids
Bacterial KatG encodes catalse-peroxidase which converts INH to active metabolite
Indicated for TB treatment and prophylaxis
SA: neurotoxicity → take pyridoxine/vitmain B6, hepatotoxicity, lupus (“INH injures neurons and hepatocytes”)
Rifampin
Inhibits DNA-dependent RNA polymerase
Indicated for TB as part of RIPE, meningococcal prophylaxis in children, Hib prophylaxis, delays resistance to dapsone in leprosy
SA: minor hepatotoxicity, drug interactions (induces P450), red/orange body fluids
Rifabutin
Inhibits DNA-dependent RNA polymerase
Indicated for TB as part of RIPE, MAC, meningococcal prophylaxis, Hib prophylaxis, delays resistance to dapsone in leprosy
SA: minor hepatotoxicity, red/orange body fluids, fewer drug interactions (less induction of P450 compared to rifampin) → better in patients with HIV
Pyrazinamide
Acidifies intracellular environment
Indicated for TB as part of RIPE
SA: hyperuricemia, hepatotoxicity
Ethambutol
Blocks arabinosyltransferase → ↓ carbohydrate polymerase of mycobacterium cell wall
Indicated for TB as part of RIPE
SA: optic neuropathy (red-green colorblindness)
HIV/AIDS prophylaxis
CD4 count < 200 → TMP-SMX for PCP
CD4 count < 100 → TMP-SMX for toxo
CD4 count < 50 → azithromycin for MAC
Antibiotics effective against MRSA
Vancomycin
Daptomycin
Linezolid (can cause serotonin syndrome)
Tigecycline
Ceftaroline
Amphotericin B
Antifungal binds ergosterol and forms membrane pores
Indicated for serious, systemic mycoses
Supplement K+ and Mg2+ 2/2 altered renal tubule permeability
SA: fever/chills, hypotension, nephrotoxicity → prevent with adequate hydration, arrhythmias, anemia, IV phlebitis; liposomal amphortericin decreases toxicity
Nystatin
Topical antifungal binds ergosterol and forms membrane pores
Indicated for oral candidiasis, diaper rash, vaginal candidiasis
Fluconazole
Antifungal inhibits P-450 enzyme that forms sterol (ergosterol)
Indicated for local and less serious systemic mycoses, chronic suppression of cryptococcal meningitis in AIDS and candidal infections of all types
SA: inhibits testosterone synthesis, liver dysfunction
Ketoconazole
Antifungal inhibits P-450 enzyme that forms sterol (ergosterol)
Indicated for local and less serious systemic mycoses
SA: inhibits testosterone synthesis → gynecomastia, liver dysfunction
Itraconazole
Antifungal inhibits P-450 enzyme that forms sterol (ergosterol)
Indicated for local and less serious systemic mycoses, Blastomyces, Coccidioides, Histoplasma
SA: inhibits testosterone synthesis, liver dysfunction
Clotrimazole
Miconazole
Topical antifungal inhibits P-450 enzyme that forms sterol (ergosterol)
Indicated for local and less serious systemic mycoses
SA: inhibits testosterone synthesis, liver dysfunction
Flucytosine
Antifungal is converted into 5-fluorouracil by cytosine deaminase to prevent DNA and RNA biosynthesis
Used with amphotericin B to treat systemic fungal infections, especially Cryptococcus meningitis)
SA: bone marrow suppression
Caspofungin
Micafungin
Anidulafungin
Antifungal echinocandin inhibits synthesis of β-glucan inhibiting cell wall synthesis
Indicated for invasive aspergillosis and candida
SA: GI upset, flushing (via histamine release)
Terbinafine
Inhibits fungal enzyme squaline epoxidase
Indicated for dermatophytoses, especially onychomycosis
SA: GI upset, headaches, hepatotoxicity, taste disturbance
Griseofulvin
Antifungal interferes with microtubule formations thus disrupting mitosis; deposits in keratin-containing tissues
Indicated for oral treatment of superfician infections, inhibits growth of dermatophytes (tinea, ringworm)
SA: teratogenic, carcinogenic, confusion, headache, induce P-450
Treatment of protozoal infections
Toxoplasmosis → pyrimethamine
Trypanosoma brucei → suramin and malarsoprol
Trypanosoma cruzi → nifurtimox
Leishmaniasis → sodium stibogluconate
Chloroquine
Blocks detoxification of heme into hemozoin → build-up of heme is toxic to plasmodia
Indicated for plasmodial species other than P. falciparum (resistant 2/2 efflux pump)
SA: retinopathy, pruritus
Artemether/lumefantrine
Treatment for P. falciparum
Atovaquone/proguanil
Treatment for P. falciparum
Quinidine in U.S.
Qauinine elsewhere
Artesunate
Treatment for life-threatening malaria
Treatmet against flukes?
Praziquantel
Zanamivir
Treats influenza A and B by inhibiting influenza neuraminidase preventing release of progeny virus
Oseltamivir
Treats influenza A and B by inhibiting influenza neuraminidase preventing release of progeny virus
Ribavirin
Inhibits inosine monophosphate dehydrogenase preventing synthesis of guanine nucleotides
Indicated for RSV, chronic hepatitis C
SA: hemolytic anemia, severe teratogen
Acyclovir
Famciclovir (for VZV)
Valacyclovir (prodrug of acyclovir with better oral bioavailability)
Monophosphorylated by viral thymidine kinase forming guanosine analogs which inhibits DNA polymerase by chain termination
Indicated for HSV, VZV, weakly active against EBV
SA: obstructive crystalline nephropathy and acute renal failure if not adequately hydrated
Resistance 2/2 mutated viral thymidine kinase
Ganciclovir
Valganciclovir (prodrug of ganciclovir with better oral bioavailability)
Converted to 5’-monophosphate (guanosine analog) by CMV viral kinase that preferentially inhibits viral DNA polymerase
Indicated for CMV, esp in immunocompromised
SA: leukopenia, neutropenia, thrombocytopenia, renal toxicity
Resistance 2/2 mutated CMV DNA polymerase or lack of viral kinase
Foscarnet
Binds to pyrophosphate-binding site of viral DNA polymerase (does not require activation with viral kinase)
Indicated for CMV retinitis in immunocompromised patients when ganciclovir fails, acyclovir-resistant HSV
Resistance 2/2 mutated DNA polymerase
Cidofovir
Inhibits viral DNA polymerase (doesn’t require activation by viral kinases)
Indicated for CMV retinitis in immunocompromised patients, acyclovir-resistant HSV
SA: nephrotoxicity (coadminister with probenecid and IV saline)
HAART
2 NRTIs + 1 NNRTI OR 1 protease inhibitor OR 1 integrase inhibitor
Which anti-retrovirals have activity against HBV?
Lamivudine (NRTI) Tenofovir (Nucleotide RTI) Emtricitabine (NRTI)
Zidovudine (AZT)
Nucleoside Reverse Transcriptase Inhibitor (NRTI) → drug phosphorylated and competitively inhibits nucleotide binding to reverse transcriptase to terminate DNA (lack 3’ OH group)
SA: lactic acidosis, bone marrow suppression (reversed with G-CSF and EPO), peripheral neuropathy, macrocytic anemia
Used as prophylaxis or treatment of HIV; safe in pregnancy to reduce transmission
Emtricitabine
Nucleoside Reverse Transcriptase Inhibitor (NRTI) → drug phosphorylated and competitively inhibits nucleotide binding to reverse transcriptase to terminate DNA (lack 3’ OH group)
SA: lactic acidosis, bone marrow suppression (reversed with G-CSF and EPO), peripheral neuropathy
Treats HIV and HBV
Abacavir
Nucleoside Reverse Transcriptase Inhibitor (NRTI) → drug phosphorylated and competitively inhibits nucleotide binding to reverse transcriptase to terminate DNA (lack 3’ OH group)
Need to genotype patient to prevent hypersensitivity reaction
SA: lactic acidosis, bone marrow suppression (reversed with G-CSF and EPO), peripheral neuropathy
Lamivudine
Nucleoside Reverse Transcriptase Inhibitor (NRTI) → drug phosphorylated and competitively inhibits nucleotide binding to reverse transcriptase to terminate DNA (lack 3’ OH group)
SA: lactic acidosis, bone marrow suppression (reversed with G-CSF and EPO), peripheral neuropathy
Treats HIV and HBV
Safe during pregnancy
Didanosine
Nucleoside Reverse Transcriptase Inhibitor (NRTI) → drug phosphorylated and competitively inhibits nucleotide binding to reverse transcriptase to terminate DNA (lack 3’ OH group)
SA: lactic acidosis, bone marrow suppression (reversed with G-CSF and EPO), peripheral neuropathy, pancreatitis
Stavudine
Nucleoside Reverse Transcriptase Inhibitor (NRTI) → drug phosphorylated and competitively inhibits nucleotide binding to reverse transcriptase to terminate DNA (lack 3’ OH group)
SA: lactic acidosis, bone marrow suppression (reversed with G-CSF and EPO), peripheral neuropathy
Tenofovir
Nucleotide Reverse Transcriptase Inhibitor (NRTI) → competitively inhibits nucleotide binding to reverse transcriptase to terminate DNA (lack 3’ OH group)
SA: bone marrow suppression (reversed with G-CSF and EPO), peripheral neuropathy, rash
Doesn’t require primary phosphorylation so effective in resting cells
Nephrotoxic (Fanconi’s syndrome –> phosphaturia, glucosuria)
Nevirapine
Non-Nucleoside Reverse Transcriptase Inhibitors (NNRTI) → binds to and inhibits reverse transcriptase at a site different from NRTI (doesn’t require phosphorylation)
Prophylaxis in pregnancy
Side effects include rash, hepatotoxicity, drug-drug interactions (CYP3A4), Stevens Johnson Syndrome
Efavirenz
Non-Nucleoside Reverse Transcriptase Inhibitors (NNRTI) → binds to and inhibits reverse transcriptase at a site different from NRTI (doesn’t require phosphorylation)
Side effects include rash, hepatotoxicity, drug-drug interactions (CYP3A4), vivid dreams, CNS symptoms
Contraindicated in pregnancy
Delavirine
Non-Nucleoside Reverse Transcriptase Inhibitors (NNRTI) → binds to and inhibits reverse transcriptase at a site different from NRTI (doesn’t require phosphorylation)
Side effects include rash, hepatotoxicity, drug-drug interactions (CYP3A4)
Contraindicated in pregnancy
Maraviroc
Inhibits binding of gp120 to CCR5 on T cells/monocytes
Not effective if CXCR4 tropism
SA: skin reaction at injection site
Enfuviritide
Locks gp41 in extended conformation inhibiting viral entry
Injected subcutaneously
SA: skin reaction at injection site
Raltegravir
Reversible integrase inhibitor prevents integration of viral genome into host cell chromosome
SA: hypercholesterolemia
Atazanavir
HIV-1 protease inhibitor → prevents maturation of new virus by inhibiting cleavage of mRNA
SA: lipodystrophy, dyslipidemia, hyperglycemia, insulin resistance, cardiac conduction abnormalities
Lower incidence of lipodystrophy
Darunavir
HIV-1 protease inhibitor → prevents maturation of new virus by inhibiting cleavage of mRNA
SA: lipodystrophy, dyslipidemia, hyperglycemia, insulin resistance, cardiac conduction abnormalities
Given with ritonavir
Fosamprenavir
HIV-1 protease inhibitor → prevents maturation of new virus by inhibiting cleavage of mRNA
SA: lipodystrophy, dyslipidemia, hyperglycemia, insulin resistance, cardiac conduction abnormalities
Indinavir
HIV-1 protease inhibitor → prevents maturation of new virus by inhibiting cleavage of mRNA
SA: lipodystrophy, dyslipidemia, hyperglycemia, insulin resistance, cardiac conduction abnormalities, nephropathy (nephrolithiasis), hematuria
Lopinavir
HIV-1 protease inhibitor → prevents maturation of new virus by inhibiting cleavage of mRNA
SA: lipodystrophy, dyslipidemia, hyperglycemia, insulin resistance, cardiac conduction abnormalities
Given with rito_navir_
Recommended during pregnancy
Ritonavir
HIV-1 protease inhibitor → prevents maturation of new virus by inhibiting cleavage of mRNA
SA: lipodystrophy, dyslipidemia, hyperglycemia, insulin resistance, cardiac conduction abnormalities
Recommended during prenancy
Strongly inhibits CYP3A4 → boosts other drug concentrations
Saquinavir
HIV-1 protease inhibitor → prevents maturation of new virus by inhibiting cleavage of mRNA
SA: lipodystrophy, dyslipidemia, hyperglycemia, insulin resistance, cardiac conduction abnormalities
Sofosbuvir
Inhibits HCV RNA synthesis by inhibiting polymerase
Genotyping to determine if combination therapy needed (IFNα and ribavirin)
Boceprevir
HCV protease inhibitor
Use with IFNα and ribavarin
Telaprevir
HCV protease inhibitor
Use with IFNα and ribavarin
Simeprevir
HCV protease inhibitor
Use with IFNα and ribavarin
Pentamidine
IV form treats PCP
Aerosolized form is PCP prophylaxis (but not protection against disseminated PCP or toxo)
Side effects include nephrotoxicity, hypoglycemia, hepatotoxicity, hypotension, pancreatitis, prolong QT (torsades), low magnesium
Dapsone
Inhibits synthesis of dihydrofolic acid
Treatment or prophylaxis for PCP (also protects against toxo)
Treatment for Hansen’s disease
Comes in liquid form
Check for G6PD deficiency –> hemolytic anemia
Side effect include rash, fever, bone marrow suppression
Contraindicated in patients with a sulfa allergy
Which antibiotics are concentration-dependent?
Aminoglycosides
Daptomycin
Quinolones
Which antibiotics are time-dependent?
β-lactams
Vancomycin
Which antibiotics are AUC?
Chloramphenicol
Clindamycin
Tetracycline
Glycopeptides
Macrolides
Sulfonamides
Which antibiotics are bactericidal?
β-lactams
Aminoglycosides
Vancomycin (variable)
Daptomycin (variable)
Fluoroquinolones
Metronidazole T
ype B streptogramins
Nitrofurantoin
Rifamycins
Which antibiotics are bacteriostatic?
Macrolides
Tetracylines
Sulfonamides
Chloramphenicol (variable)
Clindamycin
Trimethoprim
Linezolid
Interferon-alpha
Indicated for chronic hepatitis B and C, Kaposi sarcoma, hairy cell leukemia, condyloma acuminatum, renal cell carcinoma, malignant melanoma
SA: neutropenia, myopathy
Interferon-beta
Indicated for multiple sclerosis
SA: neutropenia, myopathy
Interferon-gamma
Indicated for chronic granulomatous disease
SA: neutropenia, myopathy
