Antivirals

Question 1

Neuraminidase Inhibitors

Answer 1

Oseltamivir and Zanamivir

Question 2

Nucleotide/Nucleoside Analog used for Respiratory Infections

Answer 2

Ribavirin

Question 3

Ion Channel Blockers

Answer 3

Amantadine

Question 4

Drugs for Respiratory Infections

Answer 4

Neuraminidase Inhibitors, Nucleoside/Nucleotide Analog, Ion Channel Blockers

Question 5

Interferon used for Hepatic infections

Answer 5

Interferon alpha

Question 6

Nucleotide/Nucleoside Analogs used for Hepatic Infections

Answer 6

Lamivudine and Entecavir

Question 7

Protease Inhibitors used for Hepatic Infections

Answer 7

Boceprevir and Telaprevir

Question 8

Purine and Pyrimidine Analogs used for Herpes Infections

Answer 8

Ganciclovir, Acyclovir, Cidofovir, Penciclovir, Trifluridine, Foscarnet

Question 9

MOA of Neuraminidase Inhibitors

Answer 9

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

Question 10

MOA of Ribavirin

Answer 10

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

Question 11

Contraindications of Ribavirin

Answer 11

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

Question 12

Contraindications of Amantadine and Rimantadine

Answer 12

Category X and contraindicated in nursing; crosses BBB

Question 13

MOA of Amantadine and Rimantadine

Answer 13

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

Question 14

Indications of Neuraminidase Inhibitors

Answer 14

Influenza A & B

Question 15

PK/PD of Oseltamivir

Answer 15

Oral prodrug hydrolyzed in the liver

Question 16

PK/PD of Zanamivir

Answer 16

Inhalation

Question 17

Contraindications of Zanamivir

Answer 17

Asthma, COPD

Question 18

AE of Zanamivir

Answer 18

Airway irritation

Question 19

AE of Amantadaine

Answer 19

Hallucinations, ataxia, seizures; monitor in psych patients

Question 20

Synthetic guanosine analog effective against RNA and DNA viruses

Answer 20

Ribavirin

Question 21

Indications of Ribavirin

Answer 21

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

Question 22

Indications for Amantadine and Rimantadine

Answer 22

Influenza A only

Question 23

AE of Ribavirin

Answer 23

Transient anemia, GI, CNS

Question 24

MOA of Interferon alpha

Answer 24

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

Question 25

AE of Interferon alpha

Answer 25

Flu-like symptoms and mental depression

Question 26

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

Answer 26

Lamivudine

Question 27

What does the triphosphate form of Lamivudine do?

Answer 27

Inhibits HBV and HIV Reverse Transcriptase

Question 28

What does the monophosphate form of Lamivudine do?

Answer 28

Incorporated into DNA to cause chain termination

Question 29

Indications of Lamivudine

Answer 29

HBV and HIV

Question 30

Drug Interactions of Interferon alpha

Answer 30

May potentiate myelosuppression by Zidovudine and may cause accumulation of Theophylline

Question 31

Indications of Interferon alpha

Answer 31

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

Question 32

Pegylated to improve PK profile

Answer 32

Interferon alpha

Question 33

Must be phosphorylated to triphosphate (active form)

Answer 33

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

Question 34

Indications of Entecavir

Answer 34

Lamivudine-resistant strains of HBV and HIV

Question 35

AE of Entecavir

Answer 35

Exacerbation of hepatitis upon discontinuation

Question 36

MOA of Entecavir

Answer 36

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

Question 37

MOA of Boceprevir and Telaprevir

Answer 37

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

Question 38

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

Answer 38

Boceprevir, Telaprevir

Question 39

AE of Boceprevir and Telaprevir

Answer 39

Dysgeusia, headache, etc.

Question 40

Prodrug of Acyclovir with greater oral bioavailability

Answer 40

Vancyclovir

Question 41

Acyclovir Indications

Answer 41

Genital Herpes, prophylaxis in immunocompromised and transplant patients

Question 42

Why is CMV resistant to Acyclovir?

Answer 42

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

Question 43

MOA of Acyclovir

Answer 43

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

Question 44

PK/PD of Acyclovir

Answer 44

Partial metabolism causes accumulation in Renal Failure

Question 45

AE of Acyclovir

Answer 45

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

Question 46

Prodrug of Ganciclovir with greater oral bioavailability

Answer 46

Valganciclovir

Question 47

Analog of Acyclovir with activity against CMV

Answer 47

Ganciclovir

Question 48

MOA of Ganciclovir

Answer 48

Phosphorylated by viral (UL97) and cell kinases | DNA chain termination and inhibits DNA Polymerase

Question 49

PK/PD of Valganciclovir

Answer 49

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

Question 50

Contraindications of Ganciclovir

Answer 50

Category C

Question 51

AE of Ganciclovir

Answer 51

Myelosuppression, Neutropenia

Question 52

Resistance mechanisms against Ganciclovir

Answer 52

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

Question 53

MOA of Cidofovir

Answer 53

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

Question 54

Indications of Cidofovir

Answer 54

CMV retinitis, Ganciclovir-resistant HSV

Question 55

Must be co-administered with Probenicid to block renal secretion

Answer 55

Cidofovir

Question 56

AE of Cidofovir

Answer 56

Nephrotoxicity (administered with Probenicid to avoid this)

Question 57

Resistance mechanism against Cidofovir

Answer 57

Mutations in viral DNA polymerase

Question 58

Indication of Penciclovir

Answer 58

HSV-1, HSV-2, and VZV

Question 59

PK/PD of Penciclovir

Answer 59

Topical treatment for cold sores (HSV)

Question 60

MOA of Penciclovir

Answer 60

Monophosphorylated by VIRAL Thymidine Kinase --> activated form is triphosphate Inhibits HSV DNA polymerase --> chain termination

Question 61

AE of Penciclovir

Answer 61

Mild erythema

Question 62

AE of Trifluridine

Answer 62

Palpebral edema and light intolerance

Question 63

MOA of Trifluridine

Answer 63

Triphosphate form incorporated into DNA to cause DNA fragmentation

Question 64

Trifluridine is the DOC for?

Answer 64

HSV Keratoconjunctivitis and recurrent epithelia keratitis

Question 65

Indications of Trifluridine

Answer 65

Vaccina virus, HSV-1, HSV-2

Question 66

PK/PD of Trifluridine

Answer 66

Ophthalmic ointment

Question 67

Organic analog of inorganic pyrophosphate that DOES NOT REQUIRE PHOSPHORYLATION

Answer 67

Foscarnet

Question 68

MOA of Foscarnet

Answer 68

Selectively inhibits pyrophosphate binding site on viral DNA polymerase

Question 69

Indications of Foscarnet

Answer 69

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

Question 70

Resistance to Foscarnet

Answer 70

Point mutations in DNA Polymerase

Question 71

AE of Foscarnet

Answer 71

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