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Drugs > Antiretrovirals > Flashcards

Antiretrovirals Flashcards

1
Q

NRTIs

A

Abacavir-lamivudine
Tenofovir-emtricitabine

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2
Q

NNRTIs

A

Efavirenz

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3
Q

Protease inhibitors

A

Danrunavir

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4
Q

fusion/attachment inhibitors

A

Enfuviritide
Maraviroc
Fostemsavir

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5
Q

Integrase inhibitors

A

Dolutegravir

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6
Q

Boosting agents

A

Cobicistat
Ritonavir

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7
Q

Antivirals are

A

Virustatic
Nucleuc acid analogs that inhibit replication of viral DNA/RNA

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8
Q

Antiviral agents are ineffective against

A

Latent viruses

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9
Q

HIV treatment

A

3 drug regamin (ART
2 NRTIs plus a third agent (INSTI, PI, NNRTI)

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10
Q

A two drug regamin for treatment of naive patients

A

Lamivudine-dolutegravir

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11
Q

PrEP

A

Tenofovir-emtricitabine (2 NRTIs)
Reduces HIV transmission risk
Used in high-risk HIV negative patients

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12
Q

Probilibilty of HIV resistence is directly proportional to

A

The viral load in the presence of a partially suppressive drug

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13
Q

Consequencers of long term HIV therapy

A

Lipodistrophy
Drug interactions due to inhibition of CYP3A4
Immune reconstitution inflammatory syndrome

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14
Q

Targets of HIV therapy

A

Blockade of viral attachment fusion or entry (GP41/GP120 Spike complex)
Inhibition of reverse transcriptase a viral RNA to DNA (reverse transcriptase)
Inhibition of genomic integration of viral DNA (integrase)
Inhibition of Viron assembly release in maturation (protease) 

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15
Q

Only NRTI prodrug

A

tenofovir

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16
Q

NRTI mechanism of action

A

Converted to active try phosphatases by host cell kinase that inhibit HIV reverse transcriptase and cause retroviral DNA chain termination

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17
Q

Tenofovir, lamivudine, emtricitabine are also active against

A

Hepatitis B virus

18
Q

NRTI resistance

A

Do to monotherapy so drugs must be paired
Tenofoxir-emtricitabine
Abacavir-lamivudine

19
Q

NRTI adverse effects

A

Mitochondrial toxicity-Myelosuppression neuropathy pancreatitis lipoatrophy hepatic stenosis
Black box warning for exacerbation of hepatitis B and cough active patients who discontinue HBV treatment

20
Q

Tenofovir adverse effect

A

Decreased bone mineral density (suppliment calcium-vitamin D)
Renal toxicity (avoid NSAIDs)

21
Q

Abacavir adverse effect

A

Black box warning for fatal hypersensitivity
Contraindicated in HLA-B*5701 allele-positive patients

22
Q

NNRTIs mechanism

A

Allosteric inhibition of HIV-1

23
Q

Efavirenz resistance

A

Due to use as a single agent
Leads to mutations in binding site that reduce affinity

24
Q

NNRTI pharmacokinetics

A

Clearned by CYP3A4

25
Q

NNRTI adverse effects

A

Neurologic and psychiatric (Vivid dreams dizziness headache insomnia)
Rash
Hyperlipidemia
Prolonged QT interval

26
Q

Protease inhibitors mechansim

A

Competitive inhibition of HIV protease
Prevents cleavage of gag and poor poly proteins so virus fails to mature and remains non-infective

27
Q

Resistance to protease inhibitors

A

High barrier to resistance

28
Q

Protease inhibitor metabolism

A

CYP3A4

29
Q

Protease inhibitors are commonly admisitered with

A

Boosting agents:
Ritonair- a PI that inhibits CYP3A4
Cobicistat- inhibits CYP3A4, but has no anti-retroviral activity, used to boost PIs and INSTI elvitegravir

30
Q

Protease inhibitor adverse effects

A

Gi intollerance
Hyperlipidemia
Hyperglycemia
Drug interactions:
CYP inhibitors such as azoles (require dose reduction)
CYP inducers such as rifampin (dose escalation)

31
Q

enfuvirtide is a

A

Meptide mimic of HIV gp41 protein

32
Q

enfuvirtide mechanism

A

Binds gp41 tp prevent HIV envelope from fusing with T cell membrane

33
Q

enfuvirtide must be given

A

Parenternally (only when first-line agents fail)

34
Q

enfuvirtide adverse effects

A

Injection site reactions
Elevated risk of bacterial pneumonia

35
Q

Maraviroc mechanism

A

Blocks CCR5 co-receotir to prevent entry (only antiretroviral that targets host protein)

36
Q

Maraviroc adverse rection

A

Black box warning for hepatotoxicity

37
Q

Fostemsavir mechanism

A

Prodrug that binds to gp120 and prevents attachment (only when first line agents fail)

38
Q

Fostemsavir side effects

A

Hepatotoxicity
prolionged QT interival

39
Q

INSTI (dolutegravir) mechanism

A

Inhibits HIV integrase to prevent insetion of viral DNA (resistance uncomon)

40
Q

NSTI adverse effects

A

Weight gain
Neural tube defects (should be used with birth control)

Drugs (8 decks)

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