SAQUINAVIR (Systemic)

Some commonly used brand names are:

In the U.S.?

• Fortovase
• Invirase

In Canada?

• Fortovase
• Invirase

Category

• Antiviral, systemic

Description

Saquinavir (sa-KWIN-a-veer) is used, usually in combination with otherHIV medicines including ritonavir (e.g., Norvir), in the treatment of theinfection caused by the human immunodeficiency virus (HIV). HIV is the virusthat causes acquired immune deficiency syndrome (AIDS).

Saquinavir will not cure or prevent HIV infection or AIDS; however, ithelps keep HIV from reproducing and appears to slow down the destruction ofthe immune system. This may help delay the development of problems usuallyrelated to AIDS or HIV disease. Saquinavir will not keep you from spreadingHIV to other people. People who receive this medicine may continue to haveother problems usually related to AIDS or HIV disease.

This medicine is available only with your doctor's prescription, in thefollowing dosage forms:

Oral
• Capsules (U.S., Canada)
• Tablets (U.S.)
• Soft gelatin capsules (U.S., Canada)

Before Using This Medicine

In deciding to use a medicine,the risks of taking the medicine must be weighed against the good it willdo. This is a decision you and your doctor will make. For saquinavir, thefollowing should be considered:

Allergies?Tell your doctor if you have ever had any unusual orallergic reaction to saquinavir. Also tell your health care professional ifyou are allergic to any other substances, such as foods, preservatives, ordyes.

Pregnancy?Studies have not been done in humans. However, saquinavirhas not been reported to cause birth defects or other problems in animal studies.

Breast-feeding?It is not known whether saquinavir passes intohuman breast milk. However, breast-feeding is usually not recommended in AIDSpatients because of the risk of passing the AIDS virus on to the infant.

Children?There is no specific information comparing use ofsaquinavir in children with use in other age groups.

Older adults?Many medicines have not been studied specificallyin older people. Therefore, it may not be known whether they work exactlythe same way they do in younger adults. There is no specific information comparinguse of saquinavir in the elderly with use in other age groups.

Other medicines?Although certain medicines should not be usedtogether at all, in other cases two different medicines may be used togethereven if an interaction might occur. In these cases, your doctor may want tochange the dose, or other precautions may be necessary. When you are takingsaquinavir, it is especially important that your health care professionalknow if you are taking any of the following:

• Amiodarone (e.g., Cordarone) or
• Bepridil (e.g., Vascor) or
• Flecainide (e.g., Tambocor) or
• Propafenone (e.g., Rythmol) or
• Quinidine (e.g., Quinidex)?Do not take any of these medicineswith saquinavir.

• Astemizole (e.g., Hismanal) or
• Cisapride (e.g., Propulsid) or
• Ergot medicines (dihydroergotamine [e.g., D.H.E. 45], ergoloid mesylates[e.g., Hydergine], ergotamine [e.g., Ergotrate], methylergonovine [e.g., Methergine],methysergide [e.g., Sansert]) or
• Midazolam (e.g., Versed) or
• Pimozide (e.g., Orap) or
• Rifampin (e.g., Rifadin) or
• Terfenadine (e.g., Seldane) or
• Triazolam (e.g., Halcion)?Do not take any of these medicineswith saquinavir.

• Calcium channel blocking agents (bepridil [e.g., Vascor], diltiazem[e.g., Cardizem], felodipine [e.g., Plendil], isradipine [e.g., DynaCirc],nicardipine [e.g., Cardene], nifedipine [e.g., Procardia], nimodipine [e.g.,Nimotop], verapamil [e.g., Calan])?There is a possibility that saquinavirmay interfere with the removal of these medicines from the body, which couldlead to increased side effects

• Carbamazepine (e.g., Tegretol) or
• Dexamethasone (e.g., Decadron) or
• Nevirapine (e.g., Viramune) or
• Phenobarbital (e.g., Luminal) or
• Phenytoin (e.g., Dilantin) or
• Rifabutin (e.g., Mycobutin)?These medicines may decrease theamount of saquinavir in the body

• Delavirdine (e.g., Rescriptor) or
• Nevirapine (e.g., Viramune) or
• Ritonavir (e.g., Norvir)?This medicine may increase the amountof saquinavir in the body, which could lead to increased side effects

• Efavirenz (e.g., Sustiva)?Can cause both medicines to not workas well.

• Erectile dysfunction drugs (sildenafil [e.g., Viagra], tadalafil[e.g., Cialis], vardenafil [e.g., Levitra])?Dose adjustments will needto be made when taken together with saquinavir

• Ethinyl estradiol-containing birth control pills except progestin only or ?mini pills? (e.g., Nor-QD, Micronor,Ovrette)?May need to use a different kind of birth control pill whentaking saquinavir

• Garlic capsules?Do not take garlic capsules while you are takingthis medicine

• Methadone (e.g., Dolophine)?Methadone dose may need to be increasedwhile you are taking saquinavir

Other medical problems?The presence of other medicalproblems may affect the use of saquinavir. Make sure you tell your doctorif you have any other medical problems, especially:

• Alcoholism or
• Cirrhosis of the liver or
• Hepatitis B or
• Hepatitis C?May cause liver problems to become worse

• Diabetes mellitus (sugar diabetes) or
• High blood sugar?May make these conditions worse.

• Hemophilia?Possible increased risk of bleeding

• Kidney disease, severe?Caution should be used

• Liver disease?Effects of saquinavir may be increased becauseof slower removal of the medicine from the body; also saquinavir has beenreported to cause unwanted effects on the liver. If liver disease is severe,do not take saquinavir.

Proper Use of This Medicine

It is importantthat this medicine be taken with food in order to work properly. Take saquinavir within 2 hours after a meal.

Take this medicine exactly as directed by your doctor. Do not take it more often, and do not take it for a longer time thanyour doctor ordered. Also, do not stop taking this medicine without checkingwith your doctor first.

Keep taking saquinavir for the full time of treatment, even if you begin to feel better.

This medicine works best when there is a constant amount in the blood. To help keep the amount constant, do not miss any doses.Also, it is best to take the doses at evenly spaced times, day and night.For example, if you are to take three doses a day, the doses should be spacedabout 8 hours apart. If you need help in planning the best times to take yourmedicine, check with your health care professional.

Take only the brand name of this medicine that the doctor has prescribedfor you. Do not switch from one brand name to another unless your doctor tellsyou to. Different brands may not contain the same amount of medicine.

Only take medicine that your doctor has prescribed specially for you. Donot share your medicine with others.

Dosing?The dose of saquinavir will be different fordifferent patients. Follow your doctor's orders or thedirections on the label. The following information includes only theaverage doses of saquinavir. If your dose is different,do not change it unless your doctor tells you to do so.

• For oral dosage form (capsules and tablets[brand name Invirase]):
  • For treatment of HIV infection:
    • Adults?1000 milligrams (mg) two times a day, in combinationwith ritonavir (e.g., Norvir).
    • Children up to 16 years of age?Use and dose must be determinedby your doctor.

  Note:

  Invirase must be used in combination withritonavir (e.g., Norvir). Your doctor will tell you the dose of ritonavirthat you should take.

• For oral dosage form (soft gelatin capsules[brand name Fortovase]):
  • For treatment of HIV infection:
    • Adults?1200 mg three times a day, alone or in combination withother medicines for HIV infection.
    • Children up to 16 years of age?Use and dose must be determinedby your doctor.

Missed dose?If you miss a dose of this medicine, take it assoon as you remember. However, if it is almost time for your next dose, skipthe missed dose and go back to your regular dosing schedule. Do not doubledoses.

Storage?To store this medicine:

• Keep out of the reach of children.
• Store away from heat and direct light.
• Store the soft gelatin capsule form ( Fortovase) in the refrigerator. The Invirase capsulesdo not need to be refrigerated.
• Do not store in the bathroom, near the kitchen sink, or in otherdamp places. Heat or moisture may cause the medicine to break down.
• Do not keep outdated medicine or medicine no longer needed. Be surethat any discarded medicine is out of the reach of children.

Precautions While Using This Medicine

Do not take any other medicines without checking with your doctorfirst. To do so may increase the chance of side effects from saquinaviror other medicines.

It is very important that your doctor check your progressat regular visits to make sure this medicine is working properly andto check for unwanted effects, especially increases in blood sugar.

This medicine may decrease the effects of some oral contraceptives (birthcontrol pills). To avoid unwanted pregnancy, it is agood idea to use some additional contraceptive measures while being treatedwith saquinavir..

Saquinavir does not decrease the risk of transmittingthe HIV infection to others through sexual contact or by contamination throughblood. HIV may be acquired from or spread to others through infectedbody fluids, including blood, vaginal fluid, or semen. If you are infected, it is best to avoid any sexual activity involving anexchange of body fluids with other people. If you do have sex, always wear(or have your partner wear) a condom (?rubber?). Only usecondoms made of latex, and use them every time you havevaginal, anal, or oral sex. The use of a spermicide (such as nonoxynol-9)may also help prevent the spread of HIV if it is not irritating to the vagina,rectum, or mouth. Spermicides have been shown to kill HIV in lab tests. Donot use oil-based jelly, cold cream, baby oil, or shortening as a lubricant?theseproducts can cause the condom to break. Lubricants without oil, such as K-Y Jelly, are recommended. Women may wish to carry theirown condoms. Birth control pills and diaphragms will help protect againstpregnancy, but they will not prevent someone from giving or getting the AIDSvirus. If you inject drugs, get help to stop. Do not share needles or equipment with anyone.In some cities, more than half of the drug users are infected, and sharingeven 1 needle or syringe can spread the virus. If you have any questions aboutthis, check with your health care professional.

Side Effects of This Medicine

Along with its needed effects, a medicine maycause some unwanted effects. Although not all of these side effects may occur,if they do occur they may need medical attention.

Check with your doctor as soon as possibleif any of the following side effects occur:

Less common

Chest pain

Rare

Burning or prickling sensation; confusion; dehydration; dry or itchyskin; fruity mouth odor; increased hunger; increased thirst; increased urination; nausea; skin rash; unusual tiredness; vomiting; weight loss

Other side effects may occur that usually do not need medical attention.These side effects may go away during treatment as your body adjusts to themedicine. However, check with your doctor if any of the following side effectscontinue or are bothersome:

Less common or rare

Abdominal pain; acid or sour stomach; belching; bloated fullfeeling; change in taste; decreased interest in sexual intercourse; diarrhea; difficulty having a bowel movement (stool); discouragement; excess air or gas instomach or intestines; fear; feeling sad or empty; headache; heartburn; inability to have or keep an erection; indigestion; irritability; lack of appetite; lossin sexual ability, desire, drive, or performance; loss of interest or pleasure; mouth ulcers; nervousness; passing gas; skin rash encrusted, scaly, and oozing; skin warts; sleeplessness; stomach upset, discomfort or pain; tiredness; trouble concentrating; trouble sleeping; unable to sleep; unusualtiredness or weakness; weakness

Other side effects not listed above may also occur insome patients. If you notice any other effects, check with your doctor.