Anti-Hiv Agents

Front 1

Know the NRTIs:

Back 1

- nucleoside phosphorylated to 5'triphosphate by cellular enzymes.
- Inhibit the activity of RT by competing with dNTP and by incorporated with nascent viral DNA, RESULTING IN Dna termination.

Front 2

Resistance to NRTIs AND a.e.?

Back 2

- from RT mutations.
A.E.: LACTIC ACIDOSIS, HEPATIC STEATOSIS.

Front 3

What are some A.E.:
- Zidovudine:
- Abacavir
- Didanosin, Stavudine, Zalcitabine
- Didanosine, Stavudine
- Didanosine:

Back 3

Zidovudine: anemia, neutropenia.
Abacavir: Fatal hypersensitivity reactions
Didanosine, Stavudine, Zalcitabine: Peripheal Neuropathy.
Didanosine, Stavudine: pancretitis
Didanosine: Fat redistribution and retinal changes and optic neuritis
Zalcitabine Ulceration: buccal mucosa, soft palate, tongue, pharnyx.

Front 4

Drug-Drug Interactions:

Back 4

- Stavudine + Zidovudine = intracellular activation.
- Lamivudine + Zalcitabine = interfering with its phosphorylation.
- Ethanol + abacvir = increase conc.
- Didanosin + zalcitabine = increase peripheal neuropathy.

Front 5

NNRTIs MOA:

Back 5

- Block RT activity by binding adjacent to the enzyme's binding site -> induces conformational changes.
- metabolized by CYP 450

Front 6

NNRTIs drug names:

Back 6

- Nevirapine (Viramune)
- Delavirdine (Rescriptor)
- Efavirenz (Sustiva)

Front 7

Most common A.E. for all NNRTIS?

Back 7

RASH.

Nevirapine: Stevens-Johnsons Syndrome and hepatitis.

Efavirenz: HA, dizziness, abnormal dreams, impaired conc., PSYCHIATRIC DISTURBANCES.
- tetrogenic
- increased liver enzymes

Delavirdine: increased liver enzymes.

Front 8

Protease Inhibitors: (avir)

Back 8

HIV proteases is essential for viral polyproteins (gag and gag-pol) into active viral enzymes (RT, integrase, protease) and structural proteins.

- Binds REVERSIBLY to active site of protease.

Front 9

PI:

Back 9

- poor oral bioavailability
- all under go metabolism by CYP3A4 and p-glycoprotein
- extensivily binds to plasma protein.

Front 10

PI Adverse Effects:

Back 10

Hyperglycemia
Hyperlipidemia
Fat Redistribution
Increased Liver Enzymes
GI nausea, vomiting, Diarrhea.

Front 11

Atazanavir A.E.:

Back 11

- PR interval prolongation of ECG.

Front 12

Ritonavir and Tipranivir combo:

Back 12

1. fatal and non-fatal intracranial hemorrhage

Front 13

Ritonavir and tipranivir:

Back 13

- hepatitis and hepatic decompensation

Front 14

ritonavir can cause;

Back 14

- crsytalluria, renal colic, nephrlithiasis.

Front 15

Fusion inhibitors:

Back 15

- Enfuviritide (Fuzeon)
binds to gp41
- given in combo with other drugs
- protein binding is high.
-

Front 16

A.E. of Enfuviritide:

Back 16

- Local injection site reactions:
- Pneumonia
- Allergic Reaction