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MOHD IV > Exam 2 > Flashcards

Exam 2 Flashcards

1
Q

Maraviroc

A

HIV antiviral. Targets host cell CCR5. Blocks entry. Viral resistance arises by changing HIV gp120. Used as salvage therapy. CYP3A4 metabolism.

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2
Q

Enfuvirtide

A

HIV antiviral. Blocks membrane fusion event. Mimics N peptide sequence on gp41 (fusion). Injected subcu. Resistance due to gp41 N peptide changes.

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3
Q

AZT

A

HIV antiviral. RT inhibitor. Nucleoside RT inhib. Only used for vertical transmission. Prodrug, needs phosphorylation. Effective b/c cellular polymerase excludes analog nucleosides (our drug). Viral RT does not.

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4
Q

Tenofovir

A

HIV antiviral. NtRTI. Similar mech as NRTIs but have one phosphate group on prodrug. Combination pill w/ emitricitabine available. Also used for HBV (retrovirus).

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5
Q

Abacavir

A

NRTIs. Guanosine analog.

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6
Q

Emtricitabine

A

NRTI. Cytosine analog. Combination pill w/ tenofovir.

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7
Q

Lamivudine

A

NRTI. Cytosine analog

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8
Q

Reverse Transcriptase Inhibitor

A

HIV antiviral. NNRTIs. Binds to allosteric site on RT, reducing polymerase activity. Not used as frontline medication. Mutation in RT confer resistance.

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9
Q

Dolutegravir

A

HIV antiviral. Integrase inhibitor. Blocks integration of viral DNA (3’ end). Resistance arises through AA change in enzyme.

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10
Q

Darunavir and Ritonavir

A

Protease Inhibitors. Normally cleave gag and gag-pol into functional proteins. Darunavir favored. Ritonavir blocks CYP3A4 and boosts protease inhibitors (pharmacokinetic enhancer). Sx: Lipodystrophy (centrally). Resistance from changes in protease.

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11
Q

Combination therapy

A

Cart therapy: 2 NRTIs + any third inhibitor + Ritonavir (enhancer)

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12
Q

Acyclovir, Valacyclovir

A

Alpha herpes antiviral. Administered as prodrug. Selectively activated by viral nucleoside kinase, incorporates into viral DNA chain terminating production. Tx: HSV in normal or compromised patients. Varicella Zoster. Sx: HSV inhibs elevate some HIV NRTIs.

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13
Q

Famcicolvir

A

Alpha herpes antiviral. Similarly mech to other cicolvir. Oral.

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14
Q

Foscarnet

A

Alpha herpesvirus Inhib. Analogue of pyrophosphate. Bind directly to pyrophosphate binding sites of HSV DNA polymerase. Noncompetitve inhib. 100x more selective for viral DNA polymerase.

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15
Q

Docosanol

A

Alpha herpesvirus Inhib. Saturated fatty alcohol approved as topical cream. Mixed efficacy.

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16
Q

Ganciclovir

A

Beta and Gamma Herpesvirus. Derivative of acyclovir. IV used to treat life threatening CMV infections. Sx: granulocytopenia, thrombocytopenia. CMV has protein kinase that phos. Ganciclovir.

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17
Q

Valganciclovir

A

Beta and gamma herpesviruses antiviral. Oral prodrug of ganciclovir.

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18
Q

Fomivirsen

A

Antisense RNA antiviral against CMV. Useable against CMV retinitis in immunocompromised.

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19
Q

Amantadine

A

Influenza antiviral. Viral uncoating inhibitor. Alters pH of endosome to prevent uncoating.

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20
Q

Zanamivir, Oseltamivir

A

Influenza antiviral. Neuraminidase inhibitors. Blocks release of visions from infected cells. Effective against influenza A and B.

21
Q

Palivizumab

A

RSV antiviral. Used for high risk young children. Prophylactically administered for RSV. Targets fusion glycoprotein. Monoclonal antibody.

22
Q

Ribavirin

A

RSV antiviral. Hospitalized, acutely ill may take this. Nucleoside analog (guanine). Leads to GTP depletion due to enzyme inhib. Also blocks 5 prime capping of RNA. Can base pair with cytosine or uridine and produce mutations leading to defective viral genome. Best broad spectrum antiviral. Shifts CD4+ T cells to Th.2 to Th.1 phenotype. Very toxic.Bronchodilator and antibiotics if needed.

23
Q

Entecavir

A

Hepatitis B antiviral. Nucleoside (guanine) analog. NRTI. IFN a-2a also administered to generate antiviral state.

24
Q

Simeprevir

A

Hep C antiviral. Protease inhibs. Blocks viral protein processing.

25
Q

Ladispavir

A

Hep C antiviral. Phosphoprotein inhibitor. Require to bind to polymerase for it function properly.

26
Q

Sofosbuvir

A

Hep C antiviral. Polymerase inhibitor. Works well.

27
Q

Chronic Hepatits C Treatment

A

Combination treatment of protease, polymerase, and phosphoprotein treatments. In past only Ribavirin and IFN was given.

28
Q

Rifampin

A

Inhibits mRNA synthesis. TB antibiotic

29
Q

Isoniazid

A

Inhibits cell wall synthesis. TB antibiotic.

30
Q

Ethambutol

A

Inhibits cell wall synthesis. TB antibiotic.

31
Q

Pyrazinamide

A

Disrupts membranes and energy metabolism. TB antibiotic.

32
Q

Polyene Antibiotics

A

Binds to sterol (ergosterol) compromise fungal cell membrane.

33
Q

Antimetabolites

A

Pyramiding analog; inhibits fungal DNA and RNA synthesis.

34
Q

Azoles

A

Block ergosterol synthesis, by blocking CP450 enzyme (lanosterol 14a-demethylase). Relatively non toxic. Fungistatic drugs. Oral and parenterally for local and systemic infect. Resistance via efflux/affinity/upregulation. Imidazoles less specific for fungal CYPs. Numerous drug interactions.

35
Q

Allylamines

A

Block ergosterol synthesis at a step other than that inhibited by azoles. (Squalene epoxidase).

36
Q

Glucan synthesis inhibitors

A

Inhibits synthesis of glucan, a key component of fungal cell walls.

37
Q

Amphotericin B

A

Broadest spectrum antifungal. Polyene. Oral (poor absorp, GI) topical and parenteral. Binds to ergosterol and forms pores in membrane. Drug of choice for most life threatening system infects. Including (Candida, Aspergillus, Cryptococcus). Usually fungicidal (pH dependant). Resistance: ergosterol syn inhibs (azoles) or ergosterol’s affinity for drug is reduced (mutation). Sx: irritation, infusion reactions (fever, chills, muscle spasms, vomit, headache, hypotension) allergic anaphylaxis and thrombophlebitis. NEPHROtoxicity. Drug Interactions: Digitalis (hypokalemia) Azoles (^%resistance) aminoglycosides + cyclosporine (also nephrotoxic)

38
Q

Nystatin

A

Polyene. Not well absorbed. Too toxic parenterally. Topical / oral. Mech similar to amphotericin B. Candidal infect of mucosa, skin, oral cavity, intestinal tract, and vagina. Bitter and very unpleasant taste.

39
Q

Griseofulvin

A

Fungistatic. Interacts with polymerized microtubules. Oral admin for systemic treatment of dermatophytosis. Induces CYP isoforms (affects other drugs).

40
Q

Flucytosine

A

Analogue of cytosine. Orally effective for systemic fungal infections. Taken up and metabolized by fungi, metabolites inhibit fungal DNA synthesis, and reduces RNA protein synthesis. Low toxicity. Poor TI if used alone (resistance) combined with amphotericin B. (Synergistic). Good CNS penetration. Renal excretion.

41
Q

Miconazole

A

Imidazole. Effective topically against cutaneous candidiasis. Tx: jock itch, ring worms, athletes foot, vaginal infections, oral thrush.

42
Q

Clotrimazole

A

Imidazole. Oral/topical admin for local distribution. Uses: oropharyngeal candidiasis in AIDs patients. Topically as a troche.

43
Q

Itraconazole

A

Triazoles. Broader spectrum than fluconazole. Uses: systemic Aspergillus, fluconzaole-resistant candida (esophageal candidiasis).

44
Q

Fluconazole

A

Triazole. Better CNS penetration. Good Oral availability, also IV. Used to treat crptococcal meningitis. Not active against aspergillus. 1st live agent against invasion candida.

45
Q

Voriconazole

A

Same spectrum as Itraconazole, more potent vs in vitro yeasts/molds. Oral, IV. Toxicity dose related. Transient visual side eff. Best for invasive mold infect. Used: aspergillosis (standard for care).

46
Q

Posaconazole

A

IV triazole. Similar spec as voriconazole. Only azole with activity against zygomycoses. Oral. FDA approved for prophylaxis of invasive fungal infections in hematologic malignancy and neutropenia.

47
Q

Efinaconazole

A

Triazole. Topical treatment of onychomycosis. Uses: safe mono therapy for fungal toe nail infect.

48
Q

Terbinafine

A

Allylamines. Primarily effective against dermatophytes. Fungicidal. Topical or Oral admin. Accumulates in skin, nail, and fatty tissue (sites of infection). Uses: skin/nail infection, unusual / refractory mold infections.

49
Q

Caspofungin, Micofungin

A

Inhibit glucan synthesis. Given IV. Uses: invasive candidiasis resistant to other antifungals. Invasive aspergillosis / mold infects.

MOHD IV (2 decks)

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