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Pharmacology Exam IV > Anti-Retrovirals > Flashcards

Anti-Retrovirals Flashcards

1
Q

NRTI’s (5)

A 
Zidovudine
Lamivudine
Abacavir
Tenofovir disoproxil
Emtricitabine
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2
Q

NNRTI’s (2)

A

Nevirapine

Efavirenz

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3
Q

Fusion Inhibitor

A

Enfuvirtide

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4
Q

Protease Inhibitors (3)

A

Ritonavir
Atazanavir
Darunavir

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5
Q

Co-Receptor Antagonist

A

Maraviroc

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6
Q

Integrase Inhibitors (3)

A

Raltegravir
Elvitegravir
Dolutegravir

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7
Q

Abacavir MOA

A

GUANOSINE ANALOGUE - incorporated into DNA and INHIBIT REVERSE TRANSCRIPTASE FUNCTION - leads to chain termination

activated by cellular kinases

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8
Q

Abacavir adverse reactions

A

ALLERGIC REACTION WITH HLA-B5707

Cardiac events

Lowers methadone effectiveness

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9
Q

Lamivudine MOA

Important characteristics (3)

A

CYTOSINE ANALOGUE - incorporated into DNA and INHIBIT REVERSE TRANSCRIPTASE FUNCTION - leads to chain termination

short half life
GI/CNS adverse effects with higher doses
single base change can cause high level resistance

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10
Q

Emtricitabine MOA

Important characteristics (2)

A

FLUORINATED ANALOGUE OF LAMIVUDINE - incorporated into DNA and INHIBIT REVERSE TRANSCRIPTASE FUNCTION - leads to chain termination

Longer half life than lamivudine
Single mutation can cause resistance

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11
Q

Tenofovir MOA

Given as?

A

ADENOSINE ANALOGUE - incorporated into DNA and INHIBIT REVERSE TRANSCRIPTASE FUNCTION - leads to chain termination

tenofovir disoproxil - better absorption

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12
Q

Tenofovir adverse effects

A 
GI
headache
asthenia
Renal and bone toxicity
CROSSES PLACENTA
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13
Q

Zidovudine MOA

Two significant adverse effects

A

DEOXYTHYMIDINE ANALOGUE - incorporated into DNA and INHIBIT REVERSE TRANSCRIPTASE FUNCTION - leads to chain termination

Myelosuppression
Nail hyperpigmentation

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14
Q

Non-nucleoside reverse transcriptase inhibitors MOA

A

BIND AND INHIBIT REVERSE TRANSCRIPTASE ENZYME

DO NOT REQUIRE ACTIVATION/PHOSPHORYLATION

Bind site separate from active site

NOT ACTIVE AGAINST HIV 2

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15
Q

Common adverse effects of NNRTI’s

A

rash, steven johnson syndrome, hepatotoxicity

DRUG-DRUG INTERACTIONS WITH P450 ENZYMES

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16
Q

Efavirenz Important characteristics

A

TERATOGENIC (in primate models)

Cross resistance with nevirapine

Contraindicated in pregnancy

17
Q

Nevirapine Important Characteristics

A

Lipophilic - high oral bioavailability

PREVENTION OF VERTICAL TRANSMISSION - CAN BE USED IN PREGNANCY

18
Q

Protease Inhibitors MOA

A

MIMIC PEPTIDE TARGETS OF PROTEASES

block maturation of virion particles after budding

19
Q

Protease Inhibitors common adverse effects

A

hyperlipidemia, lipodystrophy, hepatotoxic, GI interolance, increased bleeding risk

DRUG-DRUG INTERACTIONS with P450 activity

20
Q

Atazanavir Important characteristics

A

REQUIRES ACID FOR ABSORPTION - don’t use with PPI’s

Peripheral neuropathy, hyperbilirubinemia potentially

21
Q

Ritonavir Important Characteristics

A

peptidomimetic PI

POTENT INHIBITOR OF P450 ENZYME

USED IN LOW DOSES AS A BOOSTER - INCREASES HALF LIFE OF CO-ADMINISTERED ARV’s

22
Q

Darunavir Important Characteristics

A

CO-ADMIN WITH P450 INHIBITOR

increase liver enzymes and serum amylase

90% of HIV-1 with resistance to others are STILL SUSCEPTIBLE TO DARUNAVIR

23
Q

Co-receptor Antagonist MOA

A

BINDS CCR5 CO-RECEPTOR TO PREVENT VIRAL ATTACHMENT TO HOST CELLS

24
Q

Maraviroc important characteristics

A

Allergic reaction, cardiac events in susceptible patients

resistance through CHANGE IN TROPISM (CCR5 predominant to CXCR4) or MUTATIONS IN gp120

25
Q

Fusion inhibitor MOA

A

prevents fusion of viral membrane with host cell membrane

PREVENTS CONFORMATIONAL CHANGE OF GP120 THAT WOULD NORMALLY BRING MEMBRANES TOGETHER

26
Q

Enfuvirtide important characteristics

A

PAINFUL ERYTHEMATOUS NODULE AT INJECTION SITE

ONLY PARENTERALLY DELIVERED ARV

RESERVED FOR TREATMENT EXPERIENCED PATIENTS WITH INCREASING VIRAL LOAD in the face of consistent ARV treatment

27
Q

Integrase Inhibitor MOA

A

PREVENTS VIRAL GENETIC MATERIAL FROM BEING INCORPORATED INTO HOST CELL GENOME

28
Q

Raltegravir important characteristics

A

MYOPATHY, RHABDOMYOLYSIS

single mutation can confer resistance

29
Q

Elvitegravir important characteristics

A

REQUIRES CO ADMIN WITH “BOOSTERS” (cobicistat or ritonavir)

30
Q

Dolutegravir Important Characteristics

A

Hypersensitivity reactions, elevation of aminotransferases, fat redistribution syndrome

RETAINS ACTIVITY AGAINST SOME VIRUSES THAT ARE RESISTANT TO BOTH RALTEGRAVIR AND ELVITEGRAVIR

Pharmacology Exam IV (12 decks)

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