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pharma C.DAM > 6. Antiretroviral agents. > Flashcards

6. Antiretroviral agents. Flashcards

1
Q

Antiretroviral agents

A

Nucleoside Reverse Transcriptase Inhibitors (NRTI)
Non-Nucleoside Reverse Transcriptase Inhibitors (NNRTIs)
Protease inhibitors
Entry inhibitors
Integrase inhibitors

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2
Q

NRTIs can be divide to …

A

Thymidine analogs
Purine analogs
Cytidine analogs

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3
Q

Cytidine analogs

A

Lamivudine (3TC)

Emtricitabine (FTC)

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4
Q

Thymidine analogs

A

ZIdovudine (AZT)

Stavudine (d4T)

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5
Q

Purine analogs

A

Didanosine (ddI)
Tenofovir (TDF)
Abacavir (ABC)

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6
Q

NNRTIs can be divide to …

A

2 generations

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7
Q

Nevirapine
Efavirenz
Etravirine
Rilpivirine

A

NNRTI
MOA: noncompetitive inhibition of reverse transcriptase
binds to an hydrophobic allosteric site
only effective against HIV-1 (highly selective inhibitors of HIV-1 RT)

Pharmacokinetics: catabolized in the liver by CYP enzymes

Administration: oral
General adverse effects:
Liver and GI disorder
Skin reactions – up to Stevens-Johnson syndrome

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8
Q

1st generation NNRTI

A

Resistance to the drug is A single point-mutation causes total cross-resistance for all 1st generation agents

drugs …
Nevirapine
Efavirenz

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9
Q

2nd generation NNRTI

A

Etravirine

Rilpivirine

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10
Q

Nevirapine

A

NNRTI

penetrates well in the CNS
urine excretion

AE: Liver and GI disorder
Skin reactions & CNS problem !!!

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11
Q

Rilpivirine

A

NNRTI
pH dependant absorption (given with PPIs)
feces excretion

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12
Q

Efavirenz adverse effects

A

Liver and GI disorder
Skin reactions
and can cause CNS problems and it is highly teratogenic, nightmares

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13
Q

Thymidine analogs

A

ZIdovudine (AZT)

Stavudine (d4T)

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14
Q

Purine analogs

A

Didanosine (ddI)
Tenofovir (TDF)
Abacavir (ABC)

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15
Q

Cytidine analogs

A

Lamivudine (3TC)

Emtricitabine (FTC)

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16
Q 
ZIdovudine (AZT) 
Stavudine (d4T)
Didanosine (ddI) 
Tenofovir (TDF) 
Abacavir (ABC)
Lamivudine (3TC) 
Emtricitabine (FTC)
A

MOA: terminate DNA chain elongation

Kinetics: 
Primarily renally excreted 
abacavir metabolized in the liver
All except tenofovir penetrate the CNS
Administration: oral

Adverse effects: Lactate acidosis (damage of mitochondria), liver toxicity

17
Q

Protease inhibitors

A

suffix -navir

Ritonavir
Lopinavir
Atazanavir
Darunavir
Tipranavir
18
Q 
Ritonavir
Lopinavir
Atazanavir
Darunavir
Tipranavir
A

MOA: HIV protease cleaves Gag and Gag-Pol polyproteins of HIV

Pharmacokinetics:
The bioavailability is different can be increased by P-glycoproteins
They do not penetrate CNS
They are metabolized in the liver primary through CYP3A4
!!!In low dose Ritonavir block CYP2C19 and P-glycoprotein
There is no general cross-resistance between PIs

Adverse effects:
Insulin-resistance (after 5 years 5% new diabetic patients)
Hyperlipidemia (LDL, total cholesterol and triglyceride elevation)
GI disorders

19
Q

Entry inhibitors

A

Maraviroc

Enfuvirtide

20
Q

Integrase inhibitors

A

inhibits integration of proviral DNA to host chromosome

Administration: oral

Adverse effects: GI intolerance, headache

Resistance: A single point-mutation (of integrase gene)

drugs ..
Raltegravir
Elvitegravir
Dolutegravir

21
Q

Raltegravir
Elvitegravir
Dolutegravir

A

Integrase inhibitors

22
Q

Raltegravir

A

Kinetics: conjugated to glucuronic acid (CYP450) | forms complex with bivalent cations (reduces bioavailability

Well tolerated (GI problems, CK elevation due to myopathy, rhabdomyolysis)

Relative fast resistance development

23
Q

Elvitegravir

A

Cross-resistance with raltegravir

Combined tablet:
elvitegravir (+cobicistat = “booster”) + emtricitabine + tenofovir
!!!Administered once a day with “booster” (CYP3A inhibitor: ritonavir or cobicistat) increases duration of action from 3 to 9 hours

24
Q

Dolutegravir

A

Extensive hepatic metabolism (glucuronidation)

Low cross-resistance, high genetic barrier

25
Q

Maraviroc

A 
Entry inhibitors
(CCR5 coreceptor antagonist) - CCR5 viruses are mainly present in earlier stage of the disease

Prior to use a test to determine viral tropism is required to distinguish if the drug will have any effect (CCR5 / CXCR4/dual)

Orally administered,
metabolized in the liver (CYP3A4, note drug interactions)

Adverse effects: Generally well tolerated (Headache, dizziness, orthostatic hypotension)

26
Q

Enfuvirtide

A

Polypeptide
Entry inhibitors
Binds to gp41 HIV and inhibits the binding to the cells (a fusion inhibitor)

Administration: subcutaneous administered

Mainly well tolerated (local reactions on injection site, headache, nausea)

pharma C.DAM (17 decks)

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