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Pharm Block 3 > Block 3 Bolded Drugs Part 2 > Flashcards

Block 3 Bolded Drugs Part 2 Flashcards

1
Q

Amikacin

A

Aminoglycoside: binds to 30S ribosome to stop initiation of protein synthesis.

Used for tobramycin and gentamicin ressistant strain.

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2
Q

Amoxicillin

A

1 choice for pediatric otitis media and an alternate choice for lyme disease

B-lactam that treats gram + and gram - that don’t make B lactamases: listeria, strep, enterococcus.

Oral only

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3
Q

Ampicillin

A

B lactam that treats gram + and - that don’t make B lactamases such as listeria, strep, and enterococcus.

Oral or IV

Treats meningitis and GI infections (amox doesnt)

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4
Q

Azithromycin

A

Macrolide: binds to 50S ribosome to block translocation

Common for outpatient respiratory tract infections and genital infections.

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5
Q

Aztreonam

A

Used against gram - aerobic rods; no cross allergic reactions with B-lactams

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6
Q

Bacitracin

A

Topical use only

Interferes with carrier that moves early cell wall components through the cell membrane

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7
Q

Bacteriocidal

A

Inhibits bacterial growth

Effective at the minimal inhibitory concentration (MIC)

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8
Q

Bacteriostatic

A

Kills the bacteria

Effective at minimal bacteriocidal concentration (MBC)

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9
Q

Cefazolin

A

1st generation cephalosporin

Best gram + activity of the 1st gens

Longer half life: 1-2 hrs

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10
Q

Cefepime

A

4th generation cephalosporin

Spectrum like ceftazidime except more B-lactamase resistant

Used to treat severe inpatient infections

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11
Q

Cefoxitin

A

2nd generation cephalosporin with good tolerance to many gram - B-lactamases

Good for anaerobes and some strains of bacteroides fragilis

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12
Q

Ceftazidime

A

3rd generation cephalosporin

Most active 3rd gen against pseudomonas aeruginosa, poorest for gram +

Short half life: ~90 min

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13
Q

Ceftriaxone

A

3rd gen cephalosporin good for types of meningitis and drug of choice for gonorrhea.

Half life: 6-9 hrs

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14
Q

Cefuroxime

A

2nd generation cephalosporin; only second generation to penetrate the CSF

Best against haemophilus

Good tolerance to many gram - B-lactamases

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15
Q

Cephalexin

A

1st generation cephalosporin

Oral, half life of 50 minutes

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16
Q

Chloramphenicol

A

Interferes with binding of aminoacyl tRNA to 50S subunit and inhibits peptide pond formation.

Very restricted use due to serious side effects

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17
Q

Ciprofloxacin

A

Fluoroquinolone - inhibits DNA gyrase

Good for UTIs, infectious diarrhea, bone/joint/skin infections.

Not good for gram + or respiratory infections

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18
Q

Clarithromycin

A

Macrolide - binds 50S to block translocation

Less freq dosing and less effects on GI motility than erythromycin

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19
Q

Clavulanic acid

A

B-lactamase inhibitor

B-lactamase analog that binds irreversibly to B-lactamase

Works with ampicillin, amoxicillin, ticarcillin, and pipercillin

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20
Q

Clindamycin

A

Binds 50S ribosomal subunit to block translocation

Significant cause of enterocolitis

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21
Q

Concentration-dependent killin

A

Peak concentration (Cmax) must be met

Aminoglycosides use this killing - as long as they hit a peak concentration, they can still have their effects below the MIC

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22
Q

Daptomycin

A

Binds bacterial cytoplasmic membrane causing rapid depolarization

Gram + spectrum

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23
Q

Doxycycline

A

Tetracycline used for PenG sensitive syphilis and uncomplicated N. gonorrhoeae

Least affinity for Ca2+

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24
Q

Erythromycin

A

Macrolide - binds to 50S to block translocation

Treats unusual bugs such as chlamydia, mycoplasma, legionella, campylobacter, and bordetella.

Mostly treats gram +

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25
Q

Fidamoxicin

A

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).

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26
Q

Fosfomycin

A

Blocks N-acetylmuramic acid from being made (needed for PG synthesis)

Treats uncomplicated UTI’s caused by E. coli or enterococcus.

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27
Q

Gentamicin

A

Aminoglycoside

Binds 30S ribosome to stop initiation of protein synthesis

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28
Q

Imipenem

A

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

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29
Q

Killing dependent on concentration x time

A

AUC/MIC is most important for effectiveness

Generally want >125 hours for effectiveness

Quinolones

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30
Q

Linezolid

A

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

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31
Q

Metronidazole

A

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

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32
Q

Minocycline

A

Tetracycline

For penG sensitive syphilis and uncomplicated gonorrhea.

Ca2+ binding < tetracycline and >doxycycline

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33
Q

Moxifloxacin

A

Fluoroquinolone - Inhibits DNA gyrase

Better at killing gram + than ciprofloxacin. Also treats respiratory infections.

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34
Q

Nitrofurantoin

A

Nitroreductase enzyme converts drug to reactive compound that damages DNA

Used for lower UTIs from e. coli, enterococcus, and staphylococcus

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35
Q

Norfloxacin

A

Fluoroquinolone inhibits DNA gyrase

Prototype for UTIs but NO LONGER used as 1st line for UTIs

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36
Q

Oxacillin

A

Methicillin-type drug used to treat B-lactamase + staphylococci

IV/IM

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37
Q

penicillin G and V

A

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

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38
Q

Piperacillin

A

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

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39
Q

Polymyxin B

A

Cationic detergent binds LPB in the OM of gram negatives

Topical use only

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40
Q

Rifampin

A

Binds/inhibits RNA pol B to inhibit RNA synthesis

Bactericidal

Treats TB and prophylaxis for meningitis from neisseria and haemophilus

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41
Q

Silver Sulfadiazine

A

Sulfonamide antibiotic

Competitive analog of p-aminobenzoic acid, a precursor in folate synthesis

Used topically for infection prevention in burn pts

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42
Q

Sulfamethoxazole

A

Sulfonamide antibiotic

Competitive analog of p-aminobenzoic acid, a precursor in folate synthesis

Often used with trimethoprim

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43
Q

Tazobactam

A

B-lactamase inhibitor

B-lactamase analog that binds irreversibly to B-lactamse

Works with ampicillin, amoxicillin, ticarcillin, and pipercillin.

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44
Q

Ticarcillin

A

Antibiotic with some gram + coverage, some anaerobes, and extended gram negative including pseudomonas aeruginosa.

Susceptible to B-lactamases

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45
Q

Tigecycline

A

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.

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46
Q

Time dependent killing

A

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

47
Q

Tobramycin

A

Aminoglycoside antibiotic

Binds 30S ribosome to stop initiation of protein synthesis

48
Q

Trimethoprim

A

Inhibits folate synthesis.

It’s a dihydrofolate analog that competitively inhibits dihydrofolate reductase.

Often used in combo with sulfamethoxazole (TMP/SMX)

49
Q

Vancomycin

A

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.

50
Q

Amphotericin B

A

Effective broad spectrum antifungal for most serious systemic mycoses.

Gold standard for effectiveness.

Binds ergosterol to cause membrane instability. Can be used topically.

51
Q

Caspofungin

A

Inhibits fungal cell wall synthesis by non-competitively blocking synthesis of B(1,3)-D-glucan

Treats invasive aspergillus and esophageal and systemic candida.

52
Q

Ciclopirox

A

Used to treat fungal nail infections topically

53
Q

Clarithromycin (what can it treat in AIDs pts)?

A

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

54
Q

Clofazimine

A

Binds DNA and interferes with reproduction and growth; can cause red-brown skin/sclera

Antimycobacterial used in combination therapy

55
Q

Clotrimazole

A

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

56
Q

Dapsone

A

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.

57
Q

Ethambutol

A

1st line TB (tuberculostatic)

Interferes with arabinosyl transferase, thereby blocking cell wall synthesis.

58
Q

Fluconazole

A

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.

59
Q

Flucytosine (5-FC)

A

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.

60
Q

Griseofulvin

A

Oral antifungal that interferes with microtubule function, mitotic spindles, and mitosis.

Treats stubborn dermatophytic infections of the hair, skin, and nails, including tinea capitis.

61
Q

Isoniazid

A

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).

62
Q

Itraconazole

A

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.

63
Q

Miconazole

A

Same mechanism as fluconazole

Topical cream or suppositories for vaginal candida.

64
Q

Natamycin

A

Similar mechanism to amphotericin B

Used for ophthalmic fungal infections, especially fusarium, cephalosporium, and aspergillus.

65
Q

Nystatin

A

Mechanism like amphotericin B

Works on azole resistant strains

Topically for candida or oral for GI candida (but causes GI distress)

66
Q

Pyrazinamide

A

Cidal drug, 1st line for TB

Blocks mycolic acid synthesis by inhibiting fatty acid synthase 1

Good for CNS involvement

67
Q

Rifabutin

A

Prophylaxis for M. avium celllulare (MAC) in AIDs pts

Alternate to rifampin for multi-drug treatment of MAC

68
Q

Rifampin (what severe infection does this treat)?

A

1st line drug for TB

69
Q

Streptomycin

A

1st line for TB

Binds several ribosome sites to stop initiation and cause misreading

Reserved for most severe TB

70
Q

Terbinafine

A

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

71
Q

Tolnaftate

A

Topical treatment for dermatophyte fungal infection

72
Q

Voriconazole

A

Inhibits 14a-sterol demethylase, a fungal p450 that converts lanosterol to ergosterol

Treats aspergillus, candida glabrata and krusei but NOT urinary.

73
Q

Albendazole

A

Treats echinococcos, cutaneous larval migrans, and neurocysticercosis.

Well distributed,

Causes increased hepatic enzymes, headache, nausea, vomiting, and abdominal pain.

74
Q

Atovaquone

A

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

Treats toxoplasma gondii

75
Q

Atovaquone + proguanil

A

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.

76
Q

Chloroquine

A

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.

77
Q

Doxycycline (antimalarial)

A

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

78
Q

Idodoquinol

A

Luminal amebicide

Used alone for asymptomatic infection or with a tissue amebicide for symptomatic infections.

Contraindication in those hypersensitive to iodine.

79
Q

Mebendazole

A

Treats many intestinal roundworms and some ova.

Poorly absorbed, which means there low systemic toxicity.

80
Q

Mefloquine

A

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.

81
Q

Metronidazole (amebicide)

A

Cidal tissue amebicide for symptomatic entamoeba infections.

82
Q

Nitazoxanide

A

Inhibits pyruvate: ferredoxin oxidoreductase and disrupts anaerobic energy metabolism.

Treats giardia lamblia and cryptosporidium parvum

83
Q

Paromomycin sulfate

A

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.

84
Q

Praziquantel

A

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.

85
Q

Primaquine

A

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.

86
Q

Pyrantel pamoate

A

Treats hookworm, pinworm, and roundworm but NOT whipworm (trichuris).

Poorly absorbed; mild GI symptoms

87
Q

Quinine

A

MOA like chloroquine

Blood schizonticide for all four malarial parasites; for acute attacks

Treats chloroquine resistant P. falciparum

88
Q

Thiabendazole

A

Treats strongyloides and cutaneous larval migrans from disseminated dog or cat hookworm.

Rapidly absorbed; causes nausea, vomiting, and dizziness.

89
Q

Abacavir

A

Nucleoside analog, triphosphate form inhibits reverse transcriptase and causes DNA chain termination.

Treats HIV

Hypersensitivity rxn can occur with HLA-B* 5701 allele

90
Q

Acyclovir

A

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.

91
Q

What are the three ways that acyclovir can be given and what does each treat?

A

IV: severe genital herpes, systemic HSV, HSV encephalitis, and disseminated neonatal HSV

Oral: Genital herpes, herpetic gingivostomatitis

Topical: Genital herpes

92
Q

Amantadine

A

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

93
Q

Efavirenz

A

1 anti-HIV drug in 2005

Non-nucleoside inhibitor of reverse transcriptase that binds different sites than NRTI’s and disrupts RT active site.

Can cause rash and psych effects

94
Q

Emtricitabine

A

Analog of lamivudine with same MOA.

Treats HIV and some HepB

95
Q

Enfuvirtide

A

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

96
Q

Famciclovir

A

Prodrug activated to penciclovir-triP

Inhibits viral DNA pol

Treats acute herpes zoster(shingles), and recurrent genital herpes

97
Q

Foscarnet

A

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

98
Q

Ganciclovir

A

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

99
Q

Interferon-alpha

A

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.

100
Q

Lamivudine (3TC)

A

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.

101
Q

Ledipasvir

A

Inhibits NS5A phosphorylation

Given with sofosbuvir for HSV types 1, 4, 5, and 6

Avoid use with p-glycoprotein inducers

102
Q

Lopinavir

A

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

103
Q

Maraviroc

A

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.

104
Q

Oseltamivir

A

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

105
Q

Palivizumab

A

Humanized monoclonal Ab that binds to fusion protein of RSV to prevent fusion to host cells.

Prevents severe RSV in high risk peds patients.

106
Q

Penciclovir

A

MOA like acyclovir

Treats recurrent herpes of lips and faec (topical)

107
Q

Raltegravir

A

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.

108
Q

Ribavirin

A

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)

109
Q

Ritonavir

A

Used to BOOST levels of other protease inhibitors by blocking their metabolism by CYP3A

Avoid using with other drugs that are metabolized by CYP3A

110
Q

Simeprevir

A

Reversibly inhibits hepC NS3/NS4A protease and blocks cleavage of polyprotein and thus formation of infectious virus.

Treats HepC genotype 1

Metabolized by CYP3A

111
Q

Sofosbuvir

A

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

112
Q

Tenofovir

A

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

Treats HepB and HIV

113
Q

Trifluridine

A

Thymidine analog that interferes with DNA synthesis

Ophthalmic use; treats HSV 1 and HSV2

114
Q

Zidovudine (AZT)

A

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)

Pharm Block 3 (15 decks)

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