Block 3 Bolded Drugs Part 2 Flashcards

Question

Fidamoxicin

Answer 1

Inhibitor of RNA polymerase and inhibits RNA synthesis 1st line therapy for C. diff Oral admin with poor absorption (this is good for treatment of C. diff).

Answer 2

Blocks N-acetylmuramic acid from being made (needed for PG synthesis) Treats uncomplicated UTI's caused by E. coli or enterococcus.

Answer 3

Aminoglycoside Binds 30S ribosome to stop initiation of protein synthesis

Answer 4

Carbapenem with broad spectrum, resistant to many B-lactamases including extended spectrum beta lactamases

Answer 5

AUC/MIC is most important for effectiveness Generally want >125 hours for effectiveness Quinolones

Answer 6

Inhibits protein synthesis by binding to the 50S subunit and preventing formation of the 70S initiation complex

Answer 7

Anaerobes reduce nitro group to make product that damages DNA (cidal)

Answer 8

Tetracycline For penG sensitive syphilis and uncomplicated gonorrhea. Ca2+ binding < tetracycline and >doxycycline

Answer 9

Fluoroquinolone - Inhibits DNA gyrase Better at killing gram + than ciprofloxacin. Also treats respiratory infections.

Answer 10

Nitroreductase enzyme converts drug to reactive compound that damages DNA Used for lower UTIs from e. coli, enterococcus, and staphylococcus

Answer 11

Fluoroquinolone inhibits DNA gyrase Prototype for UTIs but NO LONGER used as 1st line for UTIs

Answer 12

Methicillin-type drug used to treat B-lactamase + staphylococci IV/IM

Answer 13

Anaerobes (esp gram +), gram positives that don't make B lactamase like staph, a few gram negatives: neisseria meningitidis and spirochetes (syphilis). V is oral G is IV/IM

Answer 14

Gram - spectrum like ticarcillin but also some pseudomonas and klebsiella, including those that are ticarcillin resistant.

Answer 15

Cationic detergent binds LPB in the OM of gram negatives Topical use only

Answer 16

Binds/inhibits RNA pol B to inhibit RNA synthesis Bactericidal Treats TB and prophylaxis for meningitis from neisseria and haemophilus

Answer 17

Sulfonamide antibiotic Competitive analog of p-aminobenzoic acid, a precursor in folate synthesis Used topically for infection prevention in burn pts

Answer 18

Sulfonamide antibiotic Competitive analog of p-aminobenzoic acid, a precursor in folate synthesis Often used with trimethoprim

Answer 19

B-lactamase inhibitor B-lactamase analog that binds irreversibly to B-lactamse Works with ampicillin, amoxicillin, ticarcillin, and pipercillin.

Answer 20

Antibiotic with some gram + coverage, some anaerobes, and extended gram negative including pseudomonas aeruginosa. Susceptible to B-lactamases

Answer 21

Like tetracyclines, but also binds to additional unique sites of the ribosome and doesn't have cross-resistance. Last line drug due to increased risk of death.

Answer 22

Amount (%) of time above the minimal inhibitory concentration is what's important for effectiveness Works best at 4x above the MIC for 50% of the time

Answer 23

Aminoglycoside antibiotic Binds 30S ribosome to stop initiation of protein synthesis

Answer 24

Inhibits folate synthesis. It's a dihydrofolate analog that competitively inhibits dihydrofolate reductase. Often used in combo with sulfamethoxazole (TMP/SMX)

Answer 25

Bactericidal antibiotic Binds free D-ala-D-ala of pentapeptide to inhibit cross-linking and elongation of PG chains. Works on gramp positives only. First line for C. diff.

Answer 26

Effective broad spectrum antifungal for most serious systemic mycoses. Gold standard for effectiveness. Binds ergosterol to cause membrane instability. Can be used topically.

Answer 27

Inhibits fungal cell wall synthesis by non-competitively blocking synthesis of B(1,3)-D-glucan Treats invasive aspergillus and esophageal and systemic candida.

Answer 28

Used to treat fungal nail infections topically

Answer 29

Antimycobacterial used in multi-drug treatment of M. avium intracellulare in AIDs pts

Answer 30

Binds DNA and interferes with reproduction and growth; can cause red-brown skin/sclera Antimycobacterial used in combination therapy

Answer 31

Mechanism similar to fluconazole (inhibits 14a-sterol demethylase, a fungal p450 that converts lanosterol to ergosterol) Can be given as oral troches, in creams for vaginal infections, or topically for dermatophyte s

Answer 32

Antimycobacterial Analog of para-aminobenzoic acid (PABA) that inhibits folic acid synthesis Static drug used in combination with other drugs for prophylaxis and treatment of pneumocystis jiroveci in AIDs pts.

Answer 33

1st line TB (tuberculostatic) Interferes with arabinosyl transferase, thereby blocking cell wall synthesis.

Answer 34

Inhibits 14a-sterol demethylase, a fungal p450 that converts lanosterol to ergosterol Treats cryptococcus, candida infections in the CNS and urinary tract, most C. albicans, some C. glabrata, but NOT C. krusei.

Answer 35

Fungi have cytosine deaminase that converts 5-FC to 5-FU and metabolites of 5-FU block nucleic acid synthesis. Treats candida and cryptococcus infections. Used with amphotericin B.

Answer 36

Oral antifungal that interferes with microtubule function, mitotic spindles, and mitosis. Treats stubborn dermatophytic infections of the hair, skin, and nails, including tinea capitis.

Answer 37

1st line TB Cidal drug for actively growing cells. Activated by KatG protein and inhibits mycolic acid synthesis by targeting enoyl-acyl carrier protein reductase (InhA protein).

Answer 38

inhibits 14a-sterol demethylase, a fungal p450 that converts lanosterol to ergosterol. Treats blastomyces, histoplasma, and candida: more C. albicans than glabrata, but not CNS or urinary. Do not give to pts taking drugs with CYP3A4 metabolism.

Answer 39

Same mechanism as fluconazole Topical cream or suppositories for vaginal candida.

Answer 40

Similar mechanism to amphotericin B Used for ophthalmic fungal infections, especially fusarium, cephalosporium, and aspergillus.

Answer 41

Mechanism like amphotericin B Works on azole resistant strains Topically for candida or oral for GI candida (but causes GI distress)

Answer 42

Cidal drug, 1st line for TB Blocks mycolic acid synthesis by inhibiting fatty acid synthase 1 Good for CNS involvement

Answer 43

Prophylaxis for M. avium celllulare (MAC) in AIDs pts Alternate to rifampin for multi-drug treatment of MAC

Answer 44

1st line drug for TB

Answer 45

1st line for TB Binds several ribosome sites to stop initiation and cause misreading Reserved for most severe TB

Answer 46

Topical antifungal for dermatophytes or oral for 12 wk therapy for nail infections Causes squalene to accumulate, causing lipid droplets that disrupt fungal cell membranes

Answer 47

Topical treatment for dermatophyte fungal infection

Answer 48

Inhibits 14a-sterol demethylase, a fungal p450 that converts lanosterol to ergosterol Treats aspergillus, candida glabrata and krusei but NOT urinary.

Answer 49

Treats echinococcos, cutaneous larval migrans, and neurocysticercosis. Well distributed, Causes increased hepatic enzymes, headache, nausea, vomiting, and abdominal pain.

Answer 50

Selectively inhibits malarial mitochondrial electron transport (cytochrome bc1) and thereby disrupts pyrimidine synthesis. Treats toxoplasma gondii

Answer 51

Proguanil is a prodrug that inhibits malarial dihydrofolate reductase to block folate synthesis. Atovaquone selectively inhibits malarial mitochondrial electron transport (cytochrome bc1). Both drugs disrupt pyrimidine synthesis.

Answer 52

Blood schizonticide Parasitized RBCs concentrate drug >25 fold by a pH dependent mechanism into acidic vacuoles. It inhibits heme polymerization, causing heme to accumulate at toxic levels.

Answer 53

Treats multi-drug resistant P. falciparum and can be used for prophylaxis for chloroquine resistant P. falciparum

Answer 54

Luminal amebicide Used alone for asymptomatic infection or with a tissue amebicide for symptomatic infections. Contraindication in those hypersensitive to iodine.

Answer 55

Treats many intestinal roundworms and some ova. Poorly absorbed, which means there low systemic toxicity.

Answer 56

Similar MOA to chloroquine; Blood schizonticide Can be used for prophylaxis in chloroquine-resistant areas; treats chloroquine-resistant P. falciparum and P. vivax. Black box warning for psych effects.

Answer 57

Cidal tissue amebicide for symptomatic entamoeba infections.

Answer 58

Inhibits pyruvate: ferredoxin oxidoreductase and disrupts anaerobic energy metabolism. Treats giardia lamblia and cryptosporidium parvum

Answer 59

3rd choice for tapeworm infections, for those that don't tolerate praziquantel or albendazole Luminal amebicide used alone for asymptomatic infection or with tissue amebicide for symptomatic infection.

Answer 60

Treats trematodes (flukes) Drug of choice for schistosoma; some activity on other flukes; treats many cestodes including taenia solium (And its eggs). Causes abdominal discomfort and nausea.

Answer 61

Kills liver hypnozoites Cure/terminal prophylaxis of P. vivax and ovale (in combo with blood schizonticide). Used with clindamycin for pneumocystic jiroveci in AIDs pts.

Answer 62

Treats hookworm, pinworm, and roundworm but NOT whipworm (trichuris). Poorly absorbed; mild GI symptoms

Answer 63

MOA like chloroquine Blood schizonticide for all four malarial parasites; for acute attacks Treats chloroquine resistant P. falciparum

Answer 64

Treats strongyloides and cutaneous larval migrans from disseminated dog or cat hookworm. Rapidly absorbed; causes nausea, vomiting, and dizziness.

Answer 65

Nucleoside analog, triphosphate form inhibits reverse transcriptase and causes DNA chain termination. Treats HIV Hypersensitivity rxn can occur with HLA-B* 5701 allele

Answer 66

Phosphorylated form is made 40-100x faster in infected cells by herpes thymidine kinase. Inhibits herpes DNA Pol 10-30x better than host DNA Pol Competes with deoxy-GTP for DNA polymerase.

Answer 67

IV: severe genital herpes, systemic HSV, HSV encephalitis, and disseminated neonatal HSV Oral: Genital herpes, herpetic gingivostomatitis Topical: Genital herpes

Answer 68

Prophylaxis and treatment for influenza A (NOT B); Blocks viral uncoating by interfering with influenza A M2 protein (an ion channel) Best when given within 48 hrs of symptom onset Can cause CNS effects

Answer 69

Non-nucleoside inhibitor of reverse transcriptase that binds different sites than NRTI's and disrupts RT active site. #1 anti-HIV drug in 2005 Can cause rash and psych effects

Answer 70

Analog of lamivudine with same MOA. Treats HIV and some HepB

Answer 71

Binds gp41 subunit of HIV glycoprotein to block membrane fusion to CD4+ cells Treats HIV-1 only, and only used for pts who failed other regimens. Bad side effects: severe injection site rxn, diarrhea, nausea, fatigue

Answer 72

Prodrug activated to penciclovir-triP Inhibits viral DNA pol Treats acute herpes zoster(shingles), and recurrent genital herpes

Answer 73

Inhibits cytomegalovirus DNA pol by binding to its pyrophosphate binding site. Does not need to be converted to a triphosphate form to be active Treats CMV retinitis and acyclovir-resistant herpes simplex

Answer 74

Cytomegalovirus prophylaxis and treatment Same MOA as acyclovir except the mono-phosphorylated by CMV protein kinase. Treats CMV retinitis and is used in transplant prophylaxis

Answer 75

Treats condyloma accuminata (genital warts), HepB, and HepB (in combo with other drugs). Pegylation decreases clearance which is beneficial for treatment. Not used long term due to side effects: flu-like, BM suppression, neurotoxicity, and myalgia.

Answer 76

Nucleoside analog activated to tri-P form Competitively inhibits RT of hepatitis B virus polymerase, causing chain termination Treats HepB, HIV, and AZT-resistant HIV strains Synergistic with AZT (zidovudine) for HIV.

Answer 77

Inhibits NS5A phosphorylation Given with sofosbuvir for HSV types 1, 4, 5, and 6 Avoid use with p-glycoprotein inducers

Answer 78

Prevents viral aspartic protease from cleaving Gag-pol polypeptide into functional viral proteins, resulting in non-infectious viral particles. Protease inhibitor; Treats HIV Causes redistribution of fat, diabetes, and is a potent CYP3A inhibitor

Answer 79

Antagonist of chemokine co-receptor CCR5 (only HIV drug that targets human protein) Treats CCR5-tropic HIV strains and strains that are resistant to other drugs CCRV-tropic infections typically predominate early in the infection.

Answer 80

Prodrug, competitively inhibits influenza neuraminidases and interferes with viral release and penetration. Prophylaxis and treatment of influenza A and B Give within 48 hours of symptom onset

Answer 81

Humanized monoclonal Ab that binds to fusion protein of RSV to prevent fusion to host cells. Prevents severe RSV in high risk peds patients.

Answer 82

MOA like acyclovir Treats recurrent herpes of lips and faec (topical)

Answer 83

Inhibits HIV-1 integrase, preventing integration of HIV-1 FNA into host genome. Common 1st line drug Treats HIV-1 and strains that are resistant to other drugs.

Answer 84

Monophosphate form inhibits inosine-5'-phosphate dehydrogenase and thus GMP/GTP synthesis Triphosphate form inhibits GTP-dependent capping of viral mRNA Both forms interfere with viral mRNA syntehsis Aerosol used for severe RSV, oral for HepC (in combo with PEG-IFN-alpha)

Answer 85

Used to BOOST levels of other protease inhibitors by blocking their metabolism by CYP3A Avoid using with other drugs that are metabolized by CYP3A

Answer 86

Reversibly inhibits hepC NS3/NS4A protease and blocks cleavage of polyprotein and thus formation of infectious virus. Treats HepC genotype 1 Metabolized by CYP3A

Answer 87

Prodrug nucleoside analog; in triphosphate form it inhibits HIV NS5B RNA pol causing chain termination. Treats all Hep C genotypes Avoid taking P-glycoprotein inducers with this

Answer 88

Monophosphate prodrug converted to Tri-P form and competitively inhibits RT domain of hepatitis B virus polymerase, causing chain termination Treats HepB and HIV

Answer 89

Thymidine analog that interferes with DNA synthesis Ophthalmic use; treats HSV 1 and HSV2

Answer 90

Nucleoside reverse transcriptase inhibitor Triphosphate form competitively inhibits reverse transcriptase and acts as a chain terminator Anti-HIV drug that can treat 3TC resistant strains. Avoid use with glucuronyltransferase inhibitors (as they can increase the hematologic toxicity)