Brainscape's Knowledge GenomeTM


Top Flashcards (Certified)
All Flashcards

Pharm II Test 2 > HIV Drugs > Flashcards

HIV Drugs Flashcards

1
Q

Nucleoside/Nucleotide Reverse Transcriptase Inhibitors (NRTIs)- Available Drugs

A 
Abacavir
Didanosine
Emtricitabine
Lamivudine
Stavudine
Tenofovir
Zidovudine/Azidothymidine (AZT)
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

NRTIs- Mech of Action

A

NUCLEOSIDE OR NUCLEOTIDE ANALOGS THAT LACK A 3’-OH GROUP

PREVENT ELONGATION OF PROVIRAL DNA WHEN INCORPORATED INTO CHAIN

DOES NOT EFFECT MAJOR DNA POLYMERASE (ALPHA)

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

Abacavir- Elimination

A

Half life 1-10h

Renal excretion

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

Abacavir- Clinical Use

A

Combination therapy in HIV-1

Experienced patients

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

NRTIs- Adverse Effects/Contraindications

A

LACTIC ACIDOSIS-HEPATIC STEATOSIS SYNDROME (BLOCK DNA POL. GAMMA, BLOCKING mtDNA AND INHIBITING OXYDATIVE PHOSPHORYLATION COMPLEXES–> FAVOR PRODUCTION OF LACTATE. DEPLETE NAD WHICH IS NECESSARY FOR LIPID BREAKDOWN)

DIDANOSINE>STAVUDINE> ZIDOVUDINE

HBV FLARE WHEN DISCONTINUING AN NRTI THAT HAD ANTI-HBV EFFECTS (EMTRICITABINE, LAMIVUDINE, TENOFOVIR)

Generally safe and tolerable
Resistance develops slowly
Anemia, myopathy, pancreatitis

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

Abacavir- Adverse Effects/Contraindications

A

HYPERSENSITIVITY IN PATIENTS WITH SPECIAL HLA SUBTYPE- RECHALLENGE CAN BE FATAL

CI IN PATIENTS WITH HLA-B5701

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

Emtricitabine- Cllinical Use

A

1st Choice for combination therapy for HIV-1

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

Tenofovir- Clinical Use

A

1st Choice for combination therapy for HIV-1

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

Zidovudine / Azidothymidine (AZT)- Clinical Use

A

Exposure prophylaxis, component of combination therapy for HIV-1 and HIV-2

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

Zidovudine / Azidothymidine (AZT)- Adverse Effects/Contraindications

A

May cause anemia or neutropenia

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

Zidovudine / Azidothymidine (AZT)- Drug Rxns

A

STAVUDINE IS ANTAGONISTIC
Ribavirin is antagonistic
Cotrimoxazole and Ganciclovir can cause bone marrow toxicity

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

Nonnucleoside Reverse Transcriptase Inhibitors (NNRTIs)- Available Drugs

A 
Delaviridine
Efavirenz
Etravirine
Nevirapine
Rilpivirine
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

NNRTIs- Mech of Action

A

NON-COMPETITIVE INHIBITORS

BIND REVERSE TRANSCRIPTASE & INDUCE CONFORMATIONAL CHANGE TO REDUCE ENZYME ACTIVITY

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

Efavirenz- Clinical Use

A

Preferred component of therapy for HIV-1

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

Efavirenz- Adverse Effects/Contraindications

A

CAN CAUSE BIRTH DEFECTS

CONTRINDICATED IN PREGNANCY

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

Efavirenz- Drug Rxns

A

CYP3A4 INDUCER

= LOWERS LEVELS OF SOME PROTEASE INHIBITORS AND METHADONE

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

NNRTIS- Absorption, Distribution

A

Rapidly absorbed

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

NNRTIs- Elimination

A

Rapidly metabolized by hepatic Cyps

Large range of half lives 2-11 (Delaviridine) to 40-55 (Efavirenz)

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

NNRTIs- Notes

A

Resistance is common
Works on HIV-1 but not HIV-2
Can use early to put off use of protease inhibitors

20
Q

Nevirapine- Clinical Use

A

Combination therapy for HIV-1

Recommended alternative to Efavirenz in naive patients with pretreatment CD4 <400 (men)

21
Q

Nevirapine- Adverse Effects/Contraindications

A

MAY CAUSE SEVERE HEPATOTOXICITY

CONTRAINDICATED IN CD4 >250 (WOMEN) or CD4 >400 (MEN)

22
Q

Nevirapine- Drug Rxns

A

CYP3A4 INDUCER= LOWER LEVELS OF SOME PROTEASE INHIBITORS AND METHADONE

23
Q

Rilpivirine- Clinical Use

A

New approved combination component for HIV-1

24
Q

Rilpivirine- Drug Rxns

A

CYP3A INDUCERS AND INHIBITORS

ANTACIDS

25
Protease Inhibitors- Mech of Action
INHIBIT HIV PROTEASE | = BLOCK PROCESSING OF VIRAL PROTEINS REQUIRED TO MAKE MATURE VIRUS
26
Protease Inhibitors- Absorption, Distribution
Poor bioavailability Enhanced by high fat meals High protein binding
27
Protease Inhibitors- Elimination
All metabolized by hepatic CYP enzymes
28
Protease Inhibitors- Adverse Effects/Contraindications
METABOLIC SYNDROME (hyperlipidemia, hypertriglyceridemia, decreased HDL, increased LDL) PARESTHESIAS chronic use associated with lipodystrophy
29
Protease Inhibitors- Drug Rxns
Cyp Interactions: RIFAMPIN (strong cyp inducer) Midazolam, Phenobarbitol, Warfarin, St. John's Wart CAREFUL WHEN TREATING METABOLIC SYNDROME WITH STATINS (SOME HAVE CYP INTERACTIONS= SIMVASTATIN, ATORVASTATIN, LOVASTATIN)
30
Protease Inhibitors- Available Drugs
``` Ritonavir Fosamprenavir Atazanavir Indinavir Lopinavir Nelfinavir Saquinavir Tipranavir Darunavir ```
31
Ritonavir- Clinical Use
GIVE AT LOW DOSES TO INHIBIT CYP3A4 TO BOOST LEVELS OF OTHER PROTEASE INHIBITORS (REDUCE DOSE OF OTHER PROTEASE INHIBITORS TO REDUCE SIDE EFFECTS)
32
Ritonavir- Adverse Effects/Contraindications
NOT WELL TOLERATED AT LEVELS REQUIRED FOR ARV THERAPY = PARESTHESIAS Contraindicated in Rifampin use
33
Raltegravir- Mech of Action
BLOCK INTEGRASE ENZYME | = BLOCK INSERTION OF VIRAL cDNA INTO HOST GENOME
34
Raltegravir- Clinical Use
Combination therapy in experienced patients with suppression failure or excess toxicity with other drugs
35
Raltegravir- Adverse Effects/Contraindications
Diarrhea, headache, nausea
36
Enfuvirtide- Mech of Action
BLOCK FUSION OF VIRAL GP41 TO CELL MEMBRANE
37
Enfuvirtide- Absorption, Distribution
THE ONLY INJECTABLE HIV DRUG
38
Enfuvirtide- Clinical Use
Only effective for HIV-1 as component of combination therapy in experienced patients
39
Enfuvirtide- Adverse Effects/Contraindications
Injection site reaction | Contraindicated in patients with known hypersensitivity to drug or any of its components
40
Maraviroc- Mech of Action
BLOCK CCR5 BINDING TO VIRAL GP120
41
Maraviroc- Clinical Use
Combination therapy component for experienced patients with viral suppression failure Some HIV uses CxCr4 instead of CCr5, thus need tropism test
42
Maraviroc- Adverse Effects/Contraindications
caution in patients with liver dysfunction
43
Maraviroc- Drug Rxns
Concentrations can be altered by Rifampin or Ritonavir
44
PREFERRED COMBINATION THERAPY FOR NAIVE PATIENT
1 NNRTI + 2 NRTI OR PI (BOOSTED W/ RTV) + 2 NRTI
45
PREFERRED DUAL NRTI
TENOFOVIR + EMTRICITABINE
46
PREFERRED NNRTI
EFAVIRENZ ALTERNATIVE= NEVIRAPINE
47
PREFERRED PROTEASE INHIBITOR
``` ATAZANAVIR DARUNAVIR FOSAMPRENAVIR LOPINAVIR (ALL BOOSTED WITH RITANOVIR) ```

Pharm II Test 2 (8 decks)

Brainscape helps you reach your goals faster, through stronger study habits.
© 2025 Bold Learning Solutions. Terms and Conditions