protease inhibitors

Protease Inhibitors



A protease inhibitor is a type of drug that cripples the enzyme protease. An enzyme is a substance that triggers chemical reactions in the body. The human immunodeficiency virus (HIV) uses protease in the final stages of its reproduction (replication) process.


The drug is used to treat selected patients with HIV infection. Blocking protease interferes with HIV reproduction, causing it to make copies of itself that cannot infect new cells. The drug may improve symptoms and suppress the infection but does not cure it.


Patients should not discontinue this drug even if symptoms improve without consulting a doctor.
These drugs do not necessarily reduce the risk of transmitting HIV to others through sexual contact, so patients should avoid sexual activities or use condoms.


Protease inhibitors are considered one of the most potent medications for HIV developed so far.
This class of drugs includes indinavir (Crixivan), ritonavir (Norvir), nelfinavir (Viracept), amprenavir (Agenerase), lopinavir plus ritonavir (Kaletra), saquinavir (Fortovase), and a new drug called atazanavir (Reyataz). Reyataz received approval from the U.S. Food and Drug Administration (FDA) in mid-2003 and was the first protease inhibitor approved for once-daily dosing. Several weeks or months of drug therapy may be required before the full benefits are apparent.
The drug should be taken at the same time each day. Some types should be taken with a meal to help the body absorb them. Each of the types of protease inhibitor may have to be taken in a different way. In most cases, protease inhibitors are part of a combination therapy, used in conjunction with other classes of HIV drugs.


Common side effects include diarrhea, stomach discomfort, nausea, and mouth sores. Less often, patients may experience rash, muscle pain, headache, or weakness. Rarely, there may be confusion, severe skin reaction, or seizures. Some of these drugs can have interactions with other medication, and indinavir can be associated with kidney stones. Diabetes or high blood pressure may become worse when these drugs are taken. Reyatraz has been shown to have fewer side effects than some protease inhibitors, though it can interact with other medications, including certain heart medications and antidepressants.
Experts do not know whether the drugs pass into breast milk, so breastfeeding mothers should avoid them or should stop nursing until the treatment is completed.



"HIV Drugs Approved as of August 2003." AIDS Treatment News July 25, 2003: 4.
LoBuono, Charlotte. "FDA Gives Bod to First Once-daily Protease Inhibitor." Drug Topics July 21, 2003: 16.
Wilson, Billie Ann. "Understanding Strategies for Treating HIV." Medical Surgical Nursing 6 (April 1, 1997): 109-111.


National AIDS Treatment Advocacy Project. 580 Broadway, Ste. 403, New York, NY 10012. (888) 266-2827.

Key terms

Human immunodeficiency virus (HIV) — The virus that causes AIDS.
Gale Encyclopedia of Medicine. Copyright 2008 The Gale Group, Inc. All rights reserved.

protease inhibitors

A range of drugs that interfere with the action of the enzyme protease used by HIV to activate the synthesis of its capsid by processing the viral GAG protein. These drugs slow the progression of the infection and lengthen life. An undesirable direct or indirect effect is the abnormal laying-down of body fat and high levels of lipids in the blood, which may lead to coronary artery disease and strokes. Brand names are indinavir, ritonavir and saquinavir.
Collins Dictionary of Medicine © Robert M. Youngson 2004, 2005
References in periodicals archive ?
There are six main types of antiretroviral drugs that currently exist based on the stage in the viral life cycle where they are targeted: (i) nucleoside reverse transcriptase inhibitors (NRTIs) and nucleotide reverse transcriptase inhibitors (NtRTIs), that work by blocking the reverse transcriptase enzyme so that HIV cannot make new virus copies of itself; (ii) non-nucleoside reverse transcriptase inhibitors (NNRTIs), which work by blocking the enzyme reverse transcriptase and prevent reverse transcription, thus stopping HIV replication; (iii) protease inhibitors (PIs), that work by blocking the activity of protease enzymes.
Enanta has discovered novel protease inhibitors for use against the hepatitis C virus.
San Diego, CA, February 19, 2016 --( Jared Cumming, Director, Global Chemistry at Merck, will give a distinguished speaker presentation on, "Discovery of Verubecestat (MK-8931): A beta-Secretase Inhibitor in Phase 3 Clinical Development for Alzheimer's Disease" at GTCbio's 2nd Protease Inhibitors in Drug Discovery Conference to be held on March 1-2, 2016 in San Diego, CA.
Also, research suggests that protease inhibitors may have direct anticancer effects.
Protease inhibitors were extracted from the seeds of Lavatera cashmeriana Camb by ammonium sulphate precipitation and purified by chromatography on DEAE-cellulose and Sephadex G-100 column.
Rifampicin, a key component of TB treatment, is a potent inducer of drug metabolism and decreases plasma concentrations of many co-administered drugs, including non-nucleoside reverse transcriptase inhibitors, protease inhibitors and integrase inhibitors.
Avila has used its proprietary Avilomics platform to design covalent irreversible protease inhibitors that are highly selective, potent and with superior duration of action as compared to conventional protease inhibitors.
A dimeric 70-kDa chymotrypsin inhibitor with substantial N-terminal sequence homology to serine protease inhibitors was isolated from Acacia confusa seeds.
They recorded the incidence of myocardial infarction during the follow-up period and looked at the associations between myocardial infarction and exposure to protease inhibitors or non-nucleoside reverse transcriptase inhibitors.
Eight protease inhibitors currently are on the market and have greatly improved the quality of life for those suffering from HIV, Ghosh notes.
These protective proteins belong to a class of molecules called protease inhibitors. People have many types of protease inhibitors in their blood, but not the ones that break down certain venoms.