saquinavir


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Related to saquinavir: ritonavir, nelfinavir, Saquinavir mesylate

inhibitor

 [in-hib´ĭ-tor]
1. any substance that interferes with a chemical reaction, growth, or other biologic activity.
2. a chemical substance that inhibits or checks the action of a tissue organizer or the growth of microorganisms.
3. an effector that reduces the catalytic activity of an enzyme.
ACE i's (angiotensin-converting enzyme i's) see angiotensin-converting enzyme inhibitors.
angiogenesis inhibitor a group of drugs that prevent growth of new blood vessels into a solid tumor.
aromatase i's a class of drugs that inhibit aromatase activity and thus block production of estrogens; used to treat breast cancer and endometriosis.
C1 inhibitor (C1 INH) a member of the serpin group, an inhibitor of C1, the initial component activated in the classical complement pathway. Deficiency of or defect in the protein causes hereditary angioedema.
carbonic anhydrase inhibitor an agent that inhibits the enzyme carbonic anhydrase; used in treatment of glaucoma and sometimes for epilepsy, familial periodic paralysis, acute mountain sickness, and kidney stones of uric acid.
cholinesterase inhibitor anticholinesterase.
COX-2 i's (cyclooxygenase-2 i's) a group of nonsteroidal antiinflammatory drugs that act by inhibiting cyclooxygenase-2 activity; they have fewer gastrointestinal side effects than other NSAIDs. Two members of the group are celecoxib and rofecoxib.
gastric acid pump inhibitor an agent that inhibits gastric acid secretion by blocking the action of H+,K+-ATPase at the secretory surface of gastric parietal cells; called also proton pump i.
HIV protease inhibitor any of a group of antiretroviral drugs active against the human immunodeficiency virus; they prevent protease-mediated cleavage of viral polyproteins, causing production of immature viral particles that are noninfective. Examples include indinavir sulfate, nelfinavir mesylate, ritonavir, and saquinavir.
HMG-CoA reductase i's a group of drugs that competitively inhibit the enzyme that catalyzes the rate-limiting step in cholesterol biosynthesis, and are used to lower plasma lipoprotein levels in the treatment of hyperlipoproteinemia. Called also statins.
membrane inhibitor of reactive lysis (MIRL) protectin.
monoamine oxidase inhibitor any of a group of drugs that inhibit the action of monoamine oxidase, the enzyme that breaks down norepinephrine and serotonin, prescribed for their antidepressant action; the most widely used ones are isocarboxazid, phenelzine, and tranylcypromine. They are also used in the prevention of migraine.
α2-plasmin inhibitor α2-antiplasmin.
plasminogen activator inhibitor (PAI) any of several regulators of the fibrinolytic system that act by binding to and inhibiting free plasminogen activator. Their concentration in plasma is normally low, but is altered in some disturbances of bodily hemostasis. PAI-1 is an important fast-reacting inhibitor of t-plasminogen activator and u-plasminogen activator. Its synthesis, activity, and release are highly regulated; elevated levels of it have been described in a number of disease states. PAI-2 is a normally minor inhibitor that greatly increases in concentration during pregnancy and in certain disorders. PAI-3 is protein C inhibitor.
platelet inhibitor any of a group of agents that inhibit the clotting activity of platelets; the most common ones are aspirin and dipyridamole. See also antiplatelet therapy.
protease inhibitor
1. a substance that blocks activity of endopeptidase (protease), such as in a virus.
protein C inhibitor the primary inhibitor of activated anticoagulant protein C; it is a glycoprotein of the serpin family of proteinase inhibitors and also inhibits several other proteins involved in coagulation (thrombin, kallikrein, and coagulation factors X and XI) and urokinase. Called also plasminogen activator inhibitor 3.
proton pump inhibitor gastric acid pump i.
reverse transcriptase inhibitor a substance that blocks activity of the reverse transcriptase of a retrovirus and is used as an antiretroviral agent. Some are nucleosides or nucleoside analogues, and those that are not are therefore often called non-nucleoside reverse transcriptase inhibitors.
selective serotonin reuptake inhibitor (SSRI) any of a group of drugs that inhibit the inactivation of serotonin by blocking its absorption in the central nervous system; used as antidepressants and in the treatment of obsessive-compulsive disorder and panic disorder.
serine protease inhibitor (serine proteinase inhibitor) serpin.
topoisomerase i's a class of antineoplastic agents that interfere with the arrangement of DNA in cells.

saquinavir

(sə-kwĭn′ə-vîr)
n.
A protease-inhibiting drug given in the form of its mesylate, used usually in combination with other drugs to suppress the replication of HIV.

saquinavir

A PROTEASE INHIBITOR drug used in conjunction with other anti-HIV drugs to treat AIDS. Saquinavir acts by blocking the enzyme aspartic protease, so preventing the cleavage of gag and gag-pol polyproteins into functional proteins. The result is the production of immature and non-infectious viral particles. The drug is on the WHO official list. A brand name is Invirase.
References in periodicals archive ?
CurrWt MutScor 0 Mut 1 Mut A5 SAQUINAVIR NELFINAVIR D4T: 0.1 0.1 0.0 0.0 If stop NELFINAVIR: 0.6 0.0 0.0 If stop SAQUINAVIR: 1.1 0.0 0.0 If stop D4T: 2.1 0.0 0.1 2 Mut 3 Mut A5 SAQUINAVIR NELFINAVIR D4T: 0.0 0.1 If stop NELFINAVIR: 0.0 0.6 If stop SAQUINAVIR: 0.1 1.0 If stop D4T: 0.6 1.1 Limitations
If you take saquinavir (Invirase) you will also need to take one or two other antiviral medications, called reverse transcriptase inhibitors.
By the time of the 11th International Conference on AIDS, held July 8-11, 1996 in Vancouver, British Columbia, researchers from a variety of groups--the ADARC, Boehringer Ingelheim, Merck, and Abbott--showed that various 3-drug antiretroviral combinations--AZT and 3TC plus ritonavir or nelfinavir (Viracept), AZT and ddI plus nevirapine, or even ritonavir plus saquinavir without any reverse transcriptase inhibitors--could reduce HIV levels in the bloodstream by over 99% to below limits of detection (ranging from less than 500 to less than 25 HIV copies per milliliter of blood)--in a substantial majority (70% to 100%) of those treated.
The only exception: Invirase (saquinavir), a protease inhibitor taken by some people with HIV, is so poorly absorbed that using grapefruit juice to boost its effect can only help.
And before that the agency cleared saquinavir, which Hoffmann-La Roche Inc.
Antiretroviral drugs saquinavir and ritonavir reduce inhibitory concentration values of itraconazole against Histoplasma capsulatum strains in vitro.
Atazanavir is a once-daily drug and, while both fosamprenavir and saquinavir boosted by ritonavir have been shown to work in once-daily studies, they are not licensed for this indication.
Level 1 interactions were between: (i) indinavir and lanzoprazole (N=3; 17.65%), omeprazole (N=2; 11.76%) and simvastatin (N=1; 5.88%); (ii) ritonavir and simvastatin (N=4; 23.53%), digoxin (N=5; 29.41%) and fentanyl (N=1; 5.88%); and (iii) saquinavir and fentanyl (N=1; 5.88%).
Saquinavir did not cause many side effects, mainly because the drug was poorly absorbed and in comparison to the other 2 protease inhibitors, did not produce as large a viral load reduction.
Rifampin should not be given along with ritonavir-boosted saquinavir as part of combination antiretroviral therapy for HIV infection, according to the Food and Drug Administration and the drug's maker, Roche Laboratories Inc.