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Pharmacology - Midterm 2 > Antivirals > Flashcards

Antivirals Flashcards

1
Q

Neuraminidase Inhibitors

A

Oseltamivir and Zanamivir

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2
Q

Nucleotide/Nucleoside Analog used for Respiratory Infections

A

Ribavirin

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3
Q

Ion Channel Blockers

A

Amantadine

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4
Q

Drugs for Respiratory Infections

A

Neuraminidase Inhibitors, Nucleoside/Nucleotide Analog, Ion Channel Blockers

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5
Q

Interferon used for Hepatic infections

A

Interferon alpha

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6
Q

Nucleotide/Nucleoside Analogs used for Hepatic Infections

A

Lamivudine and Entecavir

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7
Q

Protease Inhibitors used for Hepatic Infections

A

Boceprevir and Telaprevir

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8
Q

Purine and Pyrimidine Analogs used for Herpes Infections

A

Ganciclovir, Acyclovir, Cidofovir, Penciclovir, Trifluridine, Foscarnet

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9
Q

MOA of Neuraminidase Inhibitors

A

Inhibit release of virus by inhibiting sialic acid (substrate for Neuraminidase)

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10
Q

MOA of Ribavirin

A

Inhibits GTP formation and prevents viral mRNA capping; Inhibits RNA-dependent RNA polymerase –> inhibiting viral protein synthesis

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11
Q

Contraindications of Ribavirin

A

Category X; must have -ve pregnancy test before and during treatment

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12
Q

Contraindications of Amantadine and Rimantadine

A

Category X and contraindicated in nursing; crosses BBB

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13
Q

MOA of Amantadine and Rimantadine

A

Uncoating Inhibitors; block viral M2 protein (H+ channel) needed for viral uncoating

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14
Q

Indications of Neuraminidase Inhibitors

A

Influenza A & B

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15
Q

PK/PD of Oseltamivir

A

Oral prodrug hydrolyzed in the liver

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16
Q

PK/PD of Zanamivir

A

Inhalation

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17
Q

Contraindications of Zanamivir

A

Asthma, COPD

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18
Q

AE of Zanamivir

A

Airway irritation

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19
Q

AE of Amantadaine

A

Hallucinations, ataxia, seizures; monitor in psych patients

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20
Q

Synthetic guanosine analog effective against RNA and DNA viruses

A

Ribavirin

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21
Q

Indications of Ribavirin

A

RSV, HCV (combined with IFN alpha), and Lassa Fever

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22
Q

Indications for Amantadine and Rimantadine

A

Influenza A only

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23
Q

AE of Ribavirin

A

Transient anemia, GI, CNS

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24
Q

MOA of Interferon alpha

A

Induces expression of proteins that inhibit RNA and DNA synthesis and viral infection

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25
Q

AE of Interferon alpha

A

Flu-like symptoms and mental depression

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26
Q

Nucleoside/Nucleotide Analog for Hepatic Infections that is found in monophosphate and triphosphate forms

A

Lamivudine

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27
Q

What does the triphosphate form of Lamivudine do?

A

Inhibits HBV and HIV Reverse Transcriptase

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28
Q

What does the monophosphate form of Lamivudine do?

A

Incorporated into DNA to cause chain termination

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29
Q

Indications of Lamivudine

A

HBV and HIV

30
Q

Drug Interactions of Interferon alpha

A

May potentiate myelosuppression by Zidovudine and may cause accumulation of Theophylline

31
Q

Indications of Interferon alpha

A

HBV, HCV, condyloma acuminata, Hairy Cell Leukemia, Kaposi Sarcoma

32
Q

Pegylated to improve PK profile

A

Interferon alpha

33
Q

Must be phosphorylated to triphosphate (active form)

A

Lamivudine and Entecavir (Nucleoside/Nucleotide Analogs for Hepatic Infections)

34
Q

Indications of Entecavir

A

Lamivudine-resistant strains of HBV and HIV

35
Q

AE of Entecavir

A

Exacerbation of hepatitis upon discontinuation

36
Q

MOA of Entecavir

A

Phosphorylated form competes with natural substrates for viral polymerase –> inhibition of polymerase blocs RT activity

37
Q

MOA of Boceprevir and Telaprevir

A

Reversible binding to non-structural protein 3 (NS3) serine protease to decrease replication

38
Q

Used to treat HCV in adults who failed treatment with IFN alpha and Ribavirin, or treatment-naive

A

Boceprevir, Telaprevir

39
Q

AE of Boceprevir and Telaprevir

A

Dysgeusia, headache, etc.

40
Q

Prodrug of Acyclovir with greater oral bioavailability

A

Vancyclovir

41
Q

Acyclovir Indications

A

Genital Herpes, prophylaxis in immunocompromised and transplant patients

42
Q

Why is CMV resistant to Acyclovir?

A

It does not encode Thymidine Kinase, which is needed for monophosphorylation of Acyclovir

43
Q

MOA of Acyclovir

A

3 phosphorylation steps for activation; viral THYMIDINE KINASE does monophosphorylation while host enzymes complete phosphorylation to di- and triphosphate forms –> competes with dGTP for incorporation into DNA –> chain termination and inhibition of viral DNA polymerase

44
Q

PK/PD of Acyclovir

A

Partial metabolism causes accumulation in Renal Failure

45
Q

AE of Acyclovir

A

Local irritation (topical administration), Acute Renal Failure (IV administration)

46
Q

Prodrug of Ganciclovir with greater oral bioavailability

A

Valganciclovir

47
Q

Analog of Acyclovir with activity against CMV

A

Ganciclovir

48
Q

MOA of Ganciclovir

A

Phosphorylated by viral (UL97) and cell kinases

DNA chain termination and inhibits DNA Polymerase

49
Q

PK/PD of Valganciclovir

A

Rapid hydrolysis to Ganciclovir in liver and intestine; excreted in urine

50
Q

Contraindications of Ganciclovir

A

Category C

51
Q

AE of Ganciclovir

A

Myelosuppression, Neutropenia

52
Q

Resistance mechanisms against Ganciclovir

A

Decreased intracellular phosphorylation or mutations in viral kinase (UL97) or viral DNA polymerase

53
Q

MOA of Cidofovir

A

Activated by HOST cell kinases –> DNA chain termination and DNA polymerase inhibitor

54
Q

Indications of Cidofovir

A

CMV retinitis, Ganciclovir-resistant HSV

55
Q

Must be co-administered with Probenicid to block renal secretion

A

Cidofovir

56
Q

AE of Cidofovir

A

Nephrotoxicity (administered with Probenicid to avoid this)

57
Q

Resistance mechanism against Cidofovir

A

Mutations in viral DNA polymerase

58
Q

Indication of Penciclovir

A

HSV-1, HSV-2, and VZV

59
Q

PK/PD of Penciclovir

A

Topical treatment for cold sores (HSV)

60
Q

MOA of Penciclovir

A

Monophosphorylated by VIRAL Thymidine Kinase –> activated form is triphosphate

Inhibits HSV DNA polymerase –> chain termination

61
Q

AE of Penciclovir

A

Mild erythema

62
Q

AE of Trifluridine

A

Palpebral edema and light intolerance

63
Q

MOA of Trifluridine

A

Triphosphate form incorporated into DNA to cause DNA fragmentation

64
Q

Trifluridine is the DOC for?

A

HSV Keratoconjunctivitis and recurrent epithelia keratitis

65
Q

Indications of Trifluridine

A

Vaccina virus, HSV-1, HSV-2

66
Q

PK/PD of Trifluridine

A

Ophthalmic ointment

67
Q

Organic analog of inorganic pyrophosphate that DOES NOT REQUIRE PHOSPHORYLATION

A

Foscarnet

68
Q

MOA of Foscarnet

A

Selectively inhibits pyrophosphate binding site on viral DNA polymerase

69
Q

Indications of Foscarnet

A

CMV retinitis in immunocompromised, Acyclovir-resistant HSV and CMV retintis, and Ganciclovir-resistant VZV and CMV

70
Q

Resistance to Foscarnet

A

Point mutations in DNA Polymerase

71
Q

AE of Foscarnet

A

Nephrotoxicity and electrolyte disturbances (Ca, Mg, K, PO4), genital ulceration in men, hallucinations

Pharmacology - Midterm 2 (16 decks)

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