Antivirals/HIV drugs Flashcards

(60 cards)

1
Q

Mechanism of oseltamivir/zanamivir

A

inhibits influenza neuraminidase –> decreased release of progeny virions

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

Use of oseltamivir/zanamivir

A

treat and prevent both influenza A and B within 72 hrs

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

Mechanism of acyclovir, famciclovir, valacyclovir

A

guanosine analogs
monophosphorylated by HSV/VZV thymidine kinase and not phosphorylated in uninfected cells –> few adverse effects
triphosphate formed by cellular enzymes
preferentially inhibit viral DNA polymerase by chain termination

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

Use of acyclovir, famciclovir, valacyclovir

A

HSV - against mucocutaneous and genital lesions and encephalitis
VZV
weak against EBV

prophylaxis in immunocompromised patients
no effect on latent HSV or VZV

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

What do use for herpes zoster?

A

famciclovir

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

What is special about valacyclovir

A

prodrug of acyclovir and has better bioavailability

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

Toxicity of acyclovir, famciclovir, valacyclovir

A

obstructive crystalline nephropathy and acute renal failure if not adequately hydrated

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

Mechanism of resistance of acyclovir, famciclovir, valacyclovir

A

mutated viral thymidine kinase

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

Mechanism of ganciclovir

A

5’-monophosphate formed by a CMV viral kinase
guanosine analog
triphosphate formed by cellular kinase
preferentially inhibits viral DNA polymerase by chain termination

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

Use of ganciclovir

A

CMV, especially in immunocompromised pts

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

What is valganciclovir?

A

prodrug of ganciclovir with better oral bioavailability

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

Toxicity of ganciclovir

A

leukopenia, neutropenia, thrombocytopenia, renal toxicity

more toxic to host enzymes than acyclovir

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

Mechanism of resistance of ganciclovir

A

mutated viral kinase

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

Mechanism of foscarnet

A

viral DNA/RNA polymerase inhibitor and HIV reverse transcriptase inhibitor
binds to pyrophosphate-binding site on enzyme
NO activation required by viral kinase

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

Use of foscarnet

A

CMV retinitis in immunocompromised pts when ganciclovir fails
acyclovir-resistant HSV

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

Toxicity of foscarnet

A

nephrotoxicity, electrolyte abnormalities (hypo- or hypercalcemia, hypo- or hyperphosphatemia, hypokalemia, hypomagnesemia) can lead to seizures

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
17
Q

Mechanism of resistance of foscarnet

A

mutated DNA polymerase

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
18
Q

Mechanism of cidofovir

A

preferentially inhibits viral DNA polymerase

dose not require phosphorylation by viral kinase

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
19
Q

Use of cidofovir

A

CMV retinitis in immunocompromised patients
acyclovir-resistant HSV
long half-life

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
20
Q

Toxicity of cidofovir

A

nephrotoxicity (coadminister with probenecid and IV saline to decrease toxicity)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
21
Q

What is the standard HART regimen?

A

2 NRTIs + 1 NNRTI or 1 protease inhibitor or 1 integrase inhibitor

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
22
Q

Name the protease inhibitors

A

“-navir”

atazanavir
darunavir
fosamprenavir
indinavir
lopinavir
ritonavir
saquinavir
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
23
Q

Mechanism of protease inhibitors

A

assembly of virions depends on HIV-1 protease (pol genes), which cleaves the polypeptide produces of HIV mRNA into their functional parts
thus, protease inhibitors prevent maturation of new viruses

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
24
Q

Ritonavir and p450

A

INHIBITS cyt p450

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
25
Toxicity of protease inhibitors
hyperglycemia GI intolerance (nausea, diarrhea) lipodystrophy neuropathy, hematuria (indinavir)
26
Rifampin and protease inhibitors
rifampin AMPs up the cyt p450 enzymes and thus can lower protease inhibitor concentrations
27
Name the NRTIs
``` abacavir didanosine emtricitabine lamivudine stavudine tenofovir zidovudine ```
28
Mechanism of NRTIs
competitively inhibit nucleotide binding to reverse transcriptase and terminates the DNA chain (lack a 3'OH group)
29
Which of the NRTIs is nucleotides?
Tenofovir
30
What do need to do to NRTIs that are nucleosides?
need to be phosphorylated to be active
31
Use of zidovudine
general prophylaxis | PREGNANCY
32
Toxicity of NRITs
``` bone marrow suppression (give G-CSF and Epo) peripheral neuropathy lactic acidosis (nucleoside) anemia (ZDV) pancreatitis (didanosine) ```
33
Name the NNRTIs
Delavirdine Efavirenz Nevirapine
34
Mechanism of NNRTIs
bind to reverse transcriptase at site different from NRTIs | do NOT require phosphorylation to be active or compete with nucleotides
35
Toxicity of NNRTIs
rash and hepatotoxicity are common to all
36
Toxicity of efavirenz
rash and hepatotoxicty | vivid dreams and CNS symptoms
37
Contraindication of efavirenz and delavirdine
do NOT use in pregnancy
38
Name the integrase inhibitor
raltegravir
39
Mechanism of integrase inhibitor
inhibits HIV genome integration into host cell chromosome by irreversibly inhibiting HIV integrase
40
Toxicity of integrase inhibitor
increased creatine kinase
41
Mechanism of enfuvirtide
binds gp41, inhibiting viral entry
42
Toxicity of enfuvirtide
skin reaction at injection site
43
Mechanism of maraviroc
binds CCR5 on surface of T cells/monocytes inhibiting interaction with gp120
44
Mechanism of interferons
glycoprotein normally synthesized by virus-infect cells | exhibits antiviral and antihumoral properties
45
Use of interferon-alpha
chronic hepatitis B and C, Kaposi sarcoma, hairy cell leukemia, condyloma acuminatum, renal cell carcinoma, malignant melanoma
46
Use of interferon-beta
multiple sclerosis
47
Use of interferon-gamma
chronic granulomatous disease
48
Toxicity of interferons
neutropenia, myopathy
49
Drugs to treat hepatitis C
ribavirin, simeprevir, sofosbuvir
50
Mechanism of ribavirin
inhibits synthesis of guanine nucleotides by competitely inhibiting inosine monophosphate dehydrogenase
51
Use of ribavirin
chronic HCV, also RSV (palivizumab preferred in children)
52
Toxicity of ribavirin
hemolytic anemia | severe teratogen
53
Mechanism of simeprevir
HCV protease inhibitor | prevents viral replication
54
Use of simeprevir
chronic HCV in combo with ribavirin and peginterferon alfa
55
Can use simeprevir as monotherapy?
NO
56
Toxicity of simeprevir
photosensitivity reactions, rash
57
Mechanism of sofosbuvir
inhibits HCV RNA-dependent RNA polymerase acting as a chain terminator
58
Use of sofosbuvir
chronic HCV in combo with ribavirin +/- peginterferon alfa
59
Can you use sofosbuvir as monotherapy?
NO
60
Toxicity of sofosbuvir
fatigue, headache, nausea