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

/sa·quin·a·vir/ (sah-kwin´ah-vir) an HIV protease inhibitor that causes formation of immature, noninfectious viral particles; used as the base or the mesylate salt in treatment of HIV infection and AIDS.

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

an antiviral.
indications It is used to treat HIV in combination with zidovudine and zalcitabine.
contraindication Known hypersensitivity to this drug prohibits its use.
adverse effects Adverse effects of this drug include buccal mucosa ulceration, headache, musculoskeletal pain, asthenia, and hyperglycemia. Common side effects are diarrhea, abdominal pain, nausea, paresthesia, and rash.

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 ?
Ritonavir and saquinavir combinations therapy for the treatment of HIV infection', AIDS 13, 213-224.
In a randomised open-label two-arm non-inferiority Phase IIIb study ritonavir-boosted saquinavir dosed 1000/100mg was compared against ritonavir-boosted lopinavir both dosed twice daily (the GEMINI study) together with fixed-dose emtricitabine and tenofovir [8].
A patient taking ritonavir 600 mg twice daily and saquinavir 400 mg twice daily is reported to have developed symptoms of PI toxicity 1 week after itraconozole was increased from 100 mg to 200 mg twice daily, (15) and 2 of 4 patients receiving indinavir developed hyperbilirubinaemia and slightly elevated transaminase levels while on itraconazole.
With the introduction of saquinavir in December 1995 and two other drugs the following spring, patients were now seeing HIV viral loads drop to undetectable levels--and they were reengaging with the future.
The FDA approved Roche's saquinavir in December 1995.
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.
Ritonavir acts in a similar (and beneficial) way with other protease inhibitors like indinavir (Crixivan) and saquinavir (Fortovase), causing the levels of these drugs to increase in the blood.
In addition, the HIV protease inhibitors also act as inhibitors of CYP3A4 to varying degrees (ritonavir > indinavir > nelfinavir > saquinavir in terms of inhibitory potency) (8, 9).
Although the drugs apparently stopped replication of the virus, it remained in the body after treatment with the drugs, ritonavir and saquinavir, which are protease inhibitors.
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.
Both people who had the virologic failure were on Kaletra and saquinavir (either Invirase or Fortovase).
FDA Pregnancy Categories of Antiretroviral Drugs Nucleoside Nonnucleoside Reverse Reverse Transcriptase Transcriptase Protease Category Inhibitors Inhibitors Inhibitors B didanosine (ddl) atazanavir emtricitabine nelfinavir tenofovir ritonavir saquinavir C abacavir efavirenz amprenavir lamivudine (3TC) nevirapine indinavir stavudine (d4T) lopinavir/ritonavir zalcitabine (ddC) zidovudine (AZT) D Fusion Miscellaneous Category Inhibitors Agents B enfuvirtide C D hydroxyurea Note: No antiretroviral agents in pregnancy category A or X.