Microbiology - Pharmacology Flashcards
(117 cards)
1
Q
How do penicillin drugs work?
A
Binds to penicillin-binding proteins (transpeptidases) and blocks cross-linking of peptidoglycan
Can be inactivated by penicillinase/β-lactam
2
Q
Penicillin G
A
Penicillinase-sensitive penicillin
IV and IM forms
Bactericidal from gram + cocci/rods, gram - cocci, spirochetes
SA: hypersensitivity reactions, hemolytic anemia
3
Q
Penicillin V
A
Penicillinase-sensitive penicillin
Oral
Bactericidal from gram + cocci/rods, gram - cocci, spirochetes
SA: hypersensitivity reactions, hemolytic anemia
4
Q
Ampicillin
A
Extended-spectrum penicillinase-sensitive aminopenicillin
Can be combined with clavulanic acid (β-lactamase inhibitor)
SA: hypersensitivity reactions, rash, pseudomembranous colitis
5
Q
Amoxicillin
A
Extended-spectrum penicillinase-sensitive aminopenicillin
Better oral bioavailability than ampicillin
Can be combined with clavulanic acid (β-lactamase)
SA: hypersensitivity reactions, rash, pseudomembranous colitis
6
Q
Oxacillin
A
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
7
Q
Nafcillin
A
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
8
Q
Dicloxacillin
A
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
9
Q
Ticarcillin
A
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
10
Q
Piperacillin
A
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
11
Q
How do cephalosporins work?
A
β-lactam drugs that inhibit cell wall synthesis by inhibiting peptidoglycan cross-linking
Less susceptible to penicillinases
Bactericidal
Low cross-reactivity with penicillins
12
Q
Cefazolin
A
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
13
Q
Cephalexin
A
1st generation cephalosporin
Indicated for gram + cocci, Proteus mirabilis, E. coli, Klebsiella pneumoniae
SA: hypersensitivity reactions, vitamin K deficiency, ↑ nephrotoxicity of aminoglycosides
14
Q
Cefoxitin
A
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
15
Q
Cefaclor
A
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
16
Q
Cefuroxime
A
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
17
Q
Ceftriaxone
A
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
18
Q
Cefotaxime
A
3rd generation cephalosporin
Indicated for serious gram - infections resistant to other β-lactams
SA: hypersensitivity reactions, vitamin K deficiency, ↑ nephrotoxicity of aminoglycosides
19
Q
Ceftazidime
A
3rd generation cephalosporin
Indicated for serious gram - infections resistant to other β-lactams like pseudomonas
SA: hypersensitivity reactions, vitamin K deficiency, ↑ nephrotoxicity of aminoglycosides
20
Q
Cefepime
A
4th generation cephalosporin
↑ activity against Pseudomonas and gram + organisms
SA: hypersensitivity reactions, vitamin K deficiency, ↑ nephrotoxicity of aminoglycosides
21
Q
Ceftaroline
A
5th generation cephalosporin
Broad gram + and gram - coverage including MRSA but not Pseudomonas
SA: hypersensitivity reactions, vitamin K deficiency, ↑ nephrotoxicity of aminoglycosides
22
Q
How do monobactams (e.g. aztreonam) work?
A
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
23
Q
Imipenem
A
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
24
Q
Meropenem
A
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
25
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
26
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
27
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
28
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)
29
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
30
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
31
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
32
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
33
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
34
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
35
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
36
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
37
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
38
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
39
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
40
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
41
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
42
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
43
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
44
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
45
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
46
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
47
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
48
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
49
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
50
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
51
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
52
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_ **_i_**njures **_n_**eurons and **_h_**epatocytes")
53
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_
54
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
55
Pyrazinamide
Acidifies intracellular environment
Indicated for TB as part of RIPE
SA: hyperuricemia, hepatotoxicity
56
Ethambutol
Blocks arabinosyltransferase → ↓ carbohydrate polymerase of mycobacterium cell wall
Indicated for TB as part of RIPE
SA: _optic neuropathy (red-green colorblindness)_
57
HIV/AIDS prophylaxis
CD4 count \< 200 → TMP-SMX for PCP
CD4 count \< 100 → TMP-SMX for toxo
CD4 count \< 50 → azithromycin for MAC
58
Antibiotics effective against MRSA
Vancomycin
Daptomycin
Linezolid (can cause serotonin syndrome)
Tigecycline
Ceftaroline
59
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
60
Nystatin
Topical antifungal binds ergosterol and forms membrane pores
Indicated for oral candidiasis, diaper rash, vaginal candidiasis
61
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
62
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
63
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
64
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
65
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
66
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)
67
Terbinafine
Inhibits fungal enzyme squaline epoxidase
Indicated for dermatophytoses, especially onychomycosis
SA: GI upset, headaches, hepatotoxicity, taste disturbance
68
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
69
Treatment of protozoal infections
Toxoplasmosis → pyrimethamine
Trypanosoma brucei → suramin and malarsoprol
Trypanosoma cruzi → nifurtimox
Leishmaniasis → sodium stibogluconate
70
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
71
Artemether/lumefantrine
Treatment for P. falciparum
72
Atovaquone/proguanil
Treatment for P. falciparum
73
Quinidine in U.S.
Qauinine elsewhere
Artesunate
Treatment for life-threatening malaria
74
Treatmet against flukes?
Praziquantel
75
Zanamivir
Treats influenza A and B by inhibiting influenza neuraminidase preventing release of progeny virus
76
Oseltamivir
Treats influenza A and B by inhibiting influenza neuraminidase preventing release of progeny virus
77
Ribavirin
Inhibits inosine monophosphate dehydrogenase preventing synthesis of guanine nucleotides
Indicated for RSV, chronic hepatitis C
SA: hemolytic anemia, severe teratogen
78
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
79
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
80
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
81
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)
82
HAART
2 NRTIs + 1 NNRTI OR 1 protease inhibitor OR 1 integrase inhibitor
83
Which anti-retrovirals have activity against HBV?
Lamivudine (NRTI) Tenofovir (Nucleotide RTI) Emtricitabine (NRTI)
84
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
85
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
86
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
87
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
88
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_
89
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
90
**_T_**enofovir
Nucleo**_t_**ide 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)
91
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
92
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
93
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
94
Maraviroc
Inhibits binding of gp120 to CCR5 on T cells/monocytes
Not effective if CXCR4 tropism
SA: skin reaction at injection site
95
Enfuviritide
Locks gp41 in extended conformation inhibiting viral entry
Injected subcutaneously
SA: skin reaction at injection site
96
Raltegravir
Reversible integrase inhibitor prevents integration of viral genome into host cell chromosome
SA: hypercholesterolemia
97
Ataza**_navir_**
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
98
Daru**_navir_**
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_**
99
Fosampre**_navir_**
HIV-1 protease inhibitor → prevents maturation of new virus by inhibiting cleavage of mRNA
SA: lipodystrophy, dyslipidemia, hyperglycemia, insulin resistance, cardiac conduction abnormalities
100
Indi**_navir_**
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_
101
Lopi**_navir_**
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
102
Rito**_navir_**
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_
103
Saqui**_navir_**
HIV-1 protease inhibitor → prevents maturation of new virus by inhibiting cleavage of mRNA
SA: lipodystrophy, dyslipidemia, hyperglycemia, insulin resistance, cardiac conduction abnormalities
104
Sofosbuvir
Inhibits HCV RNA synthesis by inhibiting polymerase
Genotyping to determine if combination therapy needed (IFNα and ribavirin)
105
Boceprevir
HCV protease inhibitor
Use with IFNα and ribavarin
106
Telaprevir
HCV protease inhibitor
Use with IFNα and ribavarin
107
Simeprevir
HCV protease inhibitor
Use with IFNα and ribavarin
108
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
109
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
110
Which antibiotics are concentration-dependent?
Aminoglycosides
Daptomycin
Quinolones
111
Which antibiotics are time-dependent?
β-lactams
Vancomycin
112
Which antibiotics are AUC?
Chloramphenicol
Clindamycin
Tetracycline
Glycopeptides
Macrolides
Sulfonamides
113
Which antibiotics are bactericidal?
β-lactams
Aminoglycosides
Vancomycin (variable)
Daptomycin (variable)
Fluoroquinolones
Metronidazole T
ype B streptogramins
Nitrofurantoin
Rifamycins
114
Which antibiotics are bacteriostatic?
Macrolides
Tetracylines
Sulfonamides
Chloramphenicol (variable)
Clindamycin
Trimethoprim
Linezolid
115
Interferon-alpha
Indicated for chronic hepatitis B and C, Kaposi sarcoma, hairy cell leukemia, condyloma acuminatum, renal cell carcinoma, malignant melanoma
SA: neutropenia, myopathy
116
Interferon-beta
Indicated for multiple sclerosis
SA: neutropenia, myopathy
117
Interferon-gamma
Indicated for chronic granulomatous disease
SA: neutropenia, myopathy
