Protease inhibitors (PIs)


Protease inhibitors (PIs) are synthetic drugs that interrupt the action of the HIV enzyme protease PIs bind the active site on the HIV enzyme known as protease. Protease cleaves the long inactive protein strands produced during viral protein synthesis into active viral component proteins. Protease inhibitors bind to the active site of the protease enzyme and prevent the maturation of the newly produced virions so that they remain non-infectious.

Drugs in this class are associated with metabolic abnormalities including dyslipidemia, hyperglycemia, insulin resistance, lipodystrophy, etc.

Generic name Adverse Events
Atazanavir Jaundice, elevated liver function tests (LFT), PR interval elongation
Darunavir Rash, LFTs,
Indinavir Nephrolithiasis, jaundice, LFTs, alopecia, insomnia, taste alteration
Nelfinavir Diarrhea, nausea, vomiting (DNV), LFTs, fatigue
Ritonavir/Lopinavir DNV, dyslipidemai, LFTs, taste alteration
Saquinavir DNV, LFTs, headache, oral ulceration
Tipranavir >DNV, LFTs, rash, intracranial hemorrhage

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Click on the interactive diagram HIV Virus: Anatomy and Physiology and review the Maturation phase.
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Protease inhibitors interfere with maturation of HIV by cutting p55 and p160.

True
False

Reference

List of Protease inhibitors. Drugs.com. (n.d.). https://www.drugs.com/drug-class/protease-inhibitors.html.

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