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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)
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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)

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3
Q

Abacavir- Elimination

A

Half life 1-10h

Renal excretion

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4
Q

Abacavir- Clinical Use

A

Combination therapy in HIV-1

Experienced patients

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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

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6
Q

Abacavir- Adverse Effects/Contraindications

A

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

CI IN PATIENTS WITH HLA-B5701

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7
Q

Emtricitabine- Cllinical Use

A

1st Choice for combination therapy for HIV-1

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8
Q

Tenofovir- Clinical Use

A

1st Choice for combination therapy for HIV-1

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9
Q

Zidovudine / Azidothymidine (AZT)- Clinical Use

A

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

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10
Q

Zidovudine / Azidothymidine (AZT)- Adverse Effects/Contraindications

A

May cause anemia or neutropenia

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11
Q

Zidovudine / Azidothymidine (AZT)- Drug Rxns

A

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

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12
Q

Nonnucleoside Reverse Transcriptase Inhibitors (NNRTIs)- Available Drugs

A 
Delaviridine
Efavirenz
Etravirine
Nevirapine
Rilpivirine
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13
Q

NNRTIs- Mech of Action

A

NON-COMPETITIVE INHIBITORS

BIND REVERSE TRANSCRIPTASE & INDUCE CONFORMATIONAL CHANGE TO REDUCE ENZYME ACTIVITY

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14
Q

Efavirenz- Clinical Use

A

Preferred component of therapy for HIV-1

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15
Q

Efavirenz- Adverse Effects/Contraindications

A

CAN CAUSE BIRTH DEFECTS

CONTRINDICATED IN PREGNANCY

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16
Q

Efavirenz- Drug Rxns

A

CYP3A4 INDUCER

= LOWERS LEVELS OF SOME PROTEASE INHIBITORS AND METHADONE

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17
Q

NNRTIS- Absorption, Distribution

A

Rapidly absorbed

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18
Q

NNRTIs- Elimination

A

Rapidly metabolized by hepatic Cyps

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

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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
Q

Protease Inhibitors- Mech of Action

A

INHIBIT HIV PROTEASE

= BLOCK PROCESSING OF VIRAL PROTEINS REQUIRED TO MAKE MATURE VIRUS

26
Q

Protease Inhibitors- Absorption, Distribution

A

Poor bioavailability
Enhanced by high fat meals
High protein binding

27
Q

Protease Inhibitors- Elimination

A

All metabolized by hepatic CYP enzymes

28
Q

Protease Inhibitors- Adverse Effects/Contraindications

A

METABOLIC SYNDROME (hyperlipidemia, hypertriglyceridemia, decreased HDL, increased LDL)
PARESTHESIAS
chronic use associated with lipodystrophy

29
Q

Protease Inhibitors- Drug Rxns

A

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
Q

Protease Inhibitors- Available Drugs

A 
Ritonavir
Fosamprenavir
Atazanavir
Indinavir
Lopinavir
Nelfinavir
Saquinavir
Tipranavir
Darunavir
31
Q

Ritonavir- Clinical Use

A

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
Q

Ritonavir- Adverse Effects/Contraindications

A

NOT WELL TOLERATED AT LEVELS REQUIRED FOR ARV THERAPY = PARESTHESIAS

Contraindicated in Rifampin use

33
Q

Raltegravir- Mech of Action

A

BLOCK INTEGRASE ENZYME

= BLOCK INSERTION OF VIRAL cDNA INTO HOST GENOME

34
Q

Raltegravir- Clinical Use

A

Combination therapy in experienced patients with suppression failure or excess toxicity with other drugs

35
Q

Raltegravir- Adverse Effects/Contraindications

A

Diarrhea, headache, nausea

36
Q

Enfuvirtide- Mech of Action

A

BLOCK FUSION OF VIRAL GP41 TO CELL MEMBRANE

37
Q

Enfuvirtide- Absorption, Distribution

A

THE ONLY INJECTABLE HIV DRUG

38
Q

Enfuvirtide- Clinical Use

A

Only effective for HIV-1 as component of combination therapy in experienced patients

39
Q

Enfuvirtide- Adverse Effects/Contraindications

A

Injection site reaction

Contraindicated in patients with known hypersensitivity to drug or any of its components

40
Q

Maraviroc- Mech of Action

A

BLOCK CCR5 BINDING TO VIRAL GP120

41
Q

Maraviroc- Clinical Use

A

Combination therapy component for experienced patients with viral suppression failure

Some HIV uses CxCr4 instead of CCr5, thus need tropism test

42
Q

Maraviroc- Adverse Effects/Contraindications

A

caution in patients with liver dysfunction

43
Q

Maraviroc- Drug Rxns

A

Concentrations can be altered by Rifampin or Ritonavir

44
Q

PREFERRED COMBINATION THERAPY FOR NAIVE PATIENT

A

1 NNRTI + 2 NRTI OR

PI (BOOSTED W/ RTV) + 2 NRTI

45
Q

PREFERRED DUAL NRTI

A

TENOFOVIR + EMTRICITABINE

46
Q

PREFERRED NNRTI

A

EFAVIRENZ

ALTERNATIVE= NEVIRAPINE

47
Q

PREFERRED PROTEASE INHIBITOR

A 
ATAZANAVIR
DARUNAVIR
FOSAMPRENAVIR
LOPINAVIR
(ALL BOOSTED WITH RITANOVIR)

Pharm II Test 2 (8 decks)

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