n.
A protease-inhibiting drug usually used in combination with other drugs to suppress the replication of HIV.
[saquin- (perhaps alteration of (i)soquin(oline) : ISO- + QUINOLINE) + A(NTI)VIR(AL).]
saquinavir
Dictionary:
sa·quin·a·vir (sə-kwĭn'ə-vîr) 
|
n.
A protease-inhibiting drug usually used in combination with other drugs to suppress the replication of HIV.
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| Drug Info: Saquinavir |
Brand names: Fortovase®Invirase®
Chemical formula:
- Drug Forms:
- Saquinavir capsules (below)
- Saquinavir Mesylate Oral tablet
- Saquinavir Mesylate Oral capsule
- Español:
- Cápsulas de saquinavir
- Mesilato de saquinavir, Tableta oral
- Mesilato de saquinavir, Cápsula oral
Saquinavir capsules
What are saquinavir capsules?
SAQUINAVIR (Invirase®, Fortovase®) is an antiviral drug called a protease inhibitor. Saquinavir is used to treat human immunodeficiency virus (HIV) infection. Saquinavir may reduce the amount of HIV in the blood and increase the number of CD4 cells (T-cells) in the blood. Saquinavir is used in combination with other drugs to treat the HIV virus. You may still develop other infections or conditions associated with HIV. Saquinavir will not cure or prevent HIV infection or AIDS. Generic saquinavir capsules are not yet available.
NOTE: In the U.S., the Fortovase® brand of saquinavir will not be available after February 2006. Talk to your health care professional about what other treatment options are available for you.
What should I tell my health care provider before I take this medicine?
They need to know if you have any of these conditions:
• diabetes mellitus or high blood sugar
• hemophilia
• high cholesterol levels
• high triglyceride levels
• liver disease, including hepatitis
• an unusual or allergic reaction to saquinavir, other medicines, foods, dyes, or preservatives
• pregnant or trying to get pregnant
• breast-feeding
How should I take this medicine?
Take saquinavir capsules by mouth. Follow the directions on the prescription label. Swallow capsules with a drink of water. Take saquinavir within two hours after a full meal. Take your doses at regular intervals. Do not take your medicine more often than directed.
To help to make sure that your anti-HIV therapy works as well as possible, be very careful to take all of your medicine exactly as prescribed. Do not stop taking except on your prescriber's advice.
Contact your pediatrician or health care professional regarding the use of this medicine in children. Special care may be needed.
What if I miss a dose?
If you miss a dose, take it as soon as you can. If it is almost time for your next dose, take only that dose. Do not take double or extra doses.What drug(s) may interact with saquinavir?
Do not take saquinavir with the following medicines:
• astemizole (Hismanal®)
• cisapride (Propulsid®)
• dofetilide (Tykosin®)
• ergot alkaloids (e.g., dihydroergotamine, ergotamine, methysergide)
• garlic supplements
• lovastatin (Mevacor®)
• midazolam (Versed®)
• red yeast rice
• simvastatin (Zocor®)
• St. John's wort or any herbal products containing St. John's wort
• terfenadine (Seldane®)
• triazolam (Halcion®)
Other medicines that may interact with saquinavir include:
• bosentan
• certain medicines for anxiety or difficulty sleeping
• carbamazepine
• clarithromycin
• dexamethasone
• doxercalciferol
• grapefruit juice
• ketoconazole
• medicines for diabetes
• medicines for high cholesterol
• paricalcitol
• phenobarbital
• phenytoin
• pimozide
• ranitidine
• rifabutin
• rifampin
• sildenafil
Tell your prescriber or health care professional about all other medicines you are taking, including nonprescription medicines, nutritional supplements, or herbal products. Also tell your prescriber or health care professional if you are a frequent user of drinks with caffeine or alcohol, if you smoke, or if you use illegal drugs. These may affect the way your medicine works. Check with your health care professional before stopping or starting any of your medicines.
What should I watch for while taking saquinavir?
Visit your prescriber or health care professional for regular checks on your progress. Discuss any new symptoms with your prescriber or health care professional.
Saquinavir will not cure HIV and you can still get other illnesses or complications associated with your disease. Taking saquinavir does not reduce the risk of passing HIV infection to others through sexual or blood contact. It is best to avoid sexual contact so that you do not spread the disease to others. For any sexual contact, use a condom. Be careful about cuts, abrasions and other possible sources of blood contact. Never share a needle or syringe with anyone.
What side effects may I notice from taking saquinavir?
Side effects that you should report to your prescriber or health care professional as soon as possible:
• severe dizziness
• unusual tiredness or weakness
• yellow color of skin or eyes
Side effects that usually do not require medical attention (report to your prescriber or health care professional if they continue or are bothersome):
• depression
• diarrhea
• stomach or intestinal gas
• headache
• nausea, vomiting
• stomach pain
• tiredness
Where can I keep my medicine?
Keep out of the reach of children in a container that small children cannot open.
Store at Invirase® at room temperature between 15—30 degrees C (59—86 degrees F). Keep container tightly closed. Throw away any unused medicine after the expiration date.
Store Fortovase® in the refrigerator at 2—8 degrees C (36—42 degrees F); discard after the expiration date on the label. If Fortovase® is kept at room temperature (15—30 degrees C or 59—86 degrees F), discard after 3 months. (NOTE: The Fortovase® brand of saquinavir will not be available after February 2006. Talk to your health care professional about what other treatment options are available for you.)
Last updated: 10/13/2005 2:50:00 PM
Important Disclaimer: The drug information provided here is for educational purposes only. It is intended to supplement, not substitute for, the diagnosis, treatment and advice of a medical professional. This drug information does not cover all possible uses, precautions, side effects and interactions. It should not be construed to indicate that this or any drug is safe for you. Consult your medical professional for guidance before using any prescription or over the counter drugs.
| Wikipedia: Saquinavir |
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| Systematic (IUPAC) name | |
|---|---|
| (2S)-N-[(2S,3R)-4-[(3S)-3-(tert-butylcarbamoyl)-decahydroisoquinolin-2-yl]-3-hydroxy-1-phenylbutan-2-yl]-2-(quinolin-2-ylformamido)butanediamide | |
| Identifiers | |
| CAS number | 127779-20-8 |
| ATC code | J05AE01 |
| PubChem | 60787 |
| DrugBank | APRD00623 |
| Chemical data | |
| Formula | C38H50N6O5 |
| Mol. mass | 670.841 g/mol |
| Pharmacokinetic data | |
| Bioavailability | ? |
| Protein binding | 98% |
| Metabolism | ? |
| Half life | 9 - 15 houres |
| Excretion | ? |
| Therapeutic considerations | |
| Pregnancy cat. |
B1 (Australia) |
| Legal status | |
| Routes | ? |
 (what is this?) (verify) |
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Saquinavir is an antiretroviral drug used in HIV therapy. It falls in the protease inhibitor class. Two formulations have been marketed:
- a hard-gel capsule formulation of the mesylate, with trade name Invirase, which requires combination with ritonavir to increase the saquinavir bioavailability;
- a soft-gel capsule formulation of saquinavir, with trade name Fortovase.
Both formulations are generally used as a component of highly active antiretroviral therapy (HAART).
Contents |
History
Saquinavir was the first protease inhibitor (and sixth antiretroviral) approved by the Food and Drug Administration (FDA). It was approved on December 6, 1995, as Invirase, a poorly-absorbed hard gel capsule which quickly led to viral resistance in many of the pioneer patients. The manufacturer, Roche, is alleged to have rushed Invirase to market, but the conditions that prevailed at the time were very bad and there was a lot of pressure to produce products quickly.
It was approved again on Nov 7, 1997 as Fortovase, a soft gel capsule reformulated for improved bioavailability. Roche announced in May 2005 that, owing to reduction in demand, Fortovase would cease being marketed early in 2006 in favour of Invirase boosted with ritonavir. [1]
Mode of action
Saquinavir is a protease inhibitor. Proteases are enzymes that cleave protein molecules into smaller fragments. HIV protease is vital for both viral replication within the cell and release of mature viral particles from an infected cell. Saquinavir inhibits both HIV-1 and HIV-2 proteases.
Adverse reactions
The most frequent adverse events with saquinavir in either formulation are mild gastrointestinal symptoms, including diarrhea, nausea, loose stools & abdominal discomfort. Invirase is better tolerated than Fortovase.
Bioavailability and drug interactions
Saquinavir, in the Invirase formulation, has a low and variable oral bioavailability, when given alone. The Fortovase formulation at the standard dosage delivers approximately eightfold more active drug than Invirase, also at the standard dosage.[2]
In the clinic, it was found that the oral bioavailability of saquinavir in both formulations significantly increases when patients also receive the PI ritonavir. For patients, this has the major benefit that they can take less saquinavir, while maintaining sufficient saquinavir blood plasma levels to efficiently suppress the replication of HIV.
The mechanism behind this welcome observation was not directly known, but later it was determined that ritonavir inhibits the cytochrome P450 3A4 isozyme. Normally, this enzyme metabolizes saquinavir to an inactive form, but with the ritonavir inhibiting this enzyme, the saquinavir blood plasma levels increased considerably. Additionally, ritonavir also inhibits multidrug transporters, although to a much lower extent.
Unlike other protease inhibitors, the absorption of saquinavir seems to be improved by omeprazole.[3]
References
- ^ Withdrawal of Fortovase (PDF)
- ^ FortovaseTM (saquinavir) soft gelatin capsules. Product information (November 1997)
- ^ Winston A, Back D, Fletcher C, et al. (2006). "Effect of omeprazole on the pharmacokinetics of saquinavir-500 mg formulation with ritonavir in healthy male and female volunteers". AIDS 20 (10): 1401–6. doi:.
Further reading
- Cohen Stuart JW, Schuurman R, Burger DM, et al. (1999) Randomized trial comparing saquinavir soft gelatin capsules versus indinavir as part of triple therapy (CHEESE study). AIDS 13:F53-58
- Dragsted UB, Gerstoft J, Pedersen C, et al. (2003) Randomized trial to evaluate indinavir/ritonavir versus saquinavir/ritonavir in human immunodeficiency virus type 1-infected patients: the MaxCmin 1 Trial. J Infect Dis 188:635-642
- Actual photo of saquinavir and more saquinavir information.
This entry is from Wikipedia, the leading user-contributed encyclopedia. It may not have been reviewed by professional editors (see full disclaimer)
Learn More
 | Antiretroviral Drugs: Interactions |
| indinavir |
| ritonavir |
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 | Dictionary. The American Heritage® Dictionary of the English Language, Fourth Edition Copyright © 2007, 2000 by Houghton Mifflin Company. Updated in 2009. Published by Houghton Mifflin Company. All rights reserved. Read more |
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| Drug Info. Gold Standard. Copyright © 2008 by Gold Standard. All rights reserved. Read more |
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| Wikipedia. This article is licensed under the Creative Commons Attribution/Share-Alike License. It uses material from the Wikipedia article "Saquinavir". Read more |
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Mentioned in
- Cápsulas de saquinavir
- protease inhibitor (drug)
- Saquinavir Mesylate Oral tablet
- Saquinavir Mesylate Oral capsule
- Antiretroviral Drugs
- AIDS: Treatment
- Mesilato de saquinavir, Tableta oral
- Mesilato de saquinavir, Cápsula oral
- Loperamide Hydrochloride Oral tablet
- Omeprazole Oral capsule, gastro-resistant sprinkles
