Saquinavir

Saquinavir is a prescription medication used in combination with other medications to treat human immunodeficiency virus (HIV) infection. Saquinavir belongs to a group of drugs called protease inhibitors. This medication works by preventing HIV cells from multiplying.

This medication comes in capsule form and tablet forms. It is usually taken twice daily.

Some of the common side effects of saquinavir include nausea, vomiting, diarrhea, stomach pain, and tiredness. 

Saquinavir is a prescription medication used in combination with other medications to treat human immunodeficiency virus (HIV) infection in people 16 years and older. 

This medication may be prescribed for other uses. Ask your doctor or pharmacist for more information.

• Take saquinavir exactly as your healthcare provider tells you.
• Saquinavir must be taken in combination with Norvir (ritonavir).
• Adults (over the age of 16 years ): Saquinavir 1000 mg twice daily (5 × 200 mg capsules or 2 × 500 mg tablets) in combination with ritonavir 100 mg twice daily.
• For patients already taking ritonavir 100 mg twice daily as part of their treatment, no additional ritonavir is needed.
• Saquinavir and ritonavir should be taken within 2 hours after a meal.

Saquinavir may cause serious side effects including:

• Interactions with other medicines. It is important to know the medicines that should not be taken with saquinavir. See "Saquinavir Interactions".
• Changes in your heart rhythm and the electrical activity of your heart. These changes may be seen on an EKG (electrocardiogram) and can lead to serious heart problems. Your risk for these problems may be higher if you:
  • already have a history of abnormal heart rhythm, including Congenital Long QT Syndrome, or other types of heart disease.
  • take other medicines that can affect your heart rhythm while you take saquinavir.

Tell your healthcare provider right away if you have any of these symptoms while taking saquinavir:

• dizziness
• lightheadedness
• fainting
• sensation of abnormal heartbeats

Do not take saquinavir if:

• you are taking certain medicines. See "Saquinavir Interactions".
• your healthcare provider has told you that you have a condition called Congenital Long QT Syndrome.
• your healthcare provider has told you that you have complete AV (atrioventricular) block and you do not have a pacemaker or you are at risk for complete AV block.
• your healthcare provider has told you that you have low potassium or low magnesium in your blood.
• you have severe liver problems.
• you have had a severe allergic reaction to saquinavir or any of the ingredients in saquinavir.

• See "Drug Precautions".

Diabetes and high blood sugar. Some people who take protease inhibitors get new or more serious diabetes, or high blood sugar. Tell your healthcare provider if you notice an increase in thirst or urinate more often than normal while taking saquinavir.

• Liver problems. People with liver problems such as Hepatitis B or C, cirrhosis or have a history of alcoholism may have worsening liver problems. 
  Tell your healthcare provider right away if you have any of these signs and symptoms of liver problems:
  • loss of appetite
  • yellowing of your skin or whites of your eyes (jaundice)
  • dark-colored urine
  • pale colored stools
  • itchy skin
  • stomach area (abdominal) pain
• Increased bleeding in people with hemophilia. Some people with hemophilia have increased bleeding with protease inhibitors including saquinavir.
• Increase in certain fat (cholesterol and triglycerides) levels in your blood. Your healthcare provider will check your blood for high levels of cholesterol and triglycerides before you start saquinavir and during treatment with saquinavir.
• Changes in body fat. Changes in body fat have been seen in some people who take anti-HIV medications. These changes may include increased amount of fat in the upper back and neck ("buffalo hump"), breasts, and around the trunk. Loss of fat from the legs, arms and face may also happen. The cause and long-term health effects of these conditions are not known at this time.
• Immune System Changes (Immune Reconstitution Syndrome). Your immune system may get stronger and begin to fight infections that have been hidden in your body for a long time. Tell your healthcare provider if you start having new or worse symptoms of infection after you start taking saquinavir.

The most common side effects of saquinavir include:

• nausea
• vomiting
• diarrhea
• stomach area (abdominal) pain
• tiredness
• pneumonia

Tell your healthcare provider if you have any side effect that bothers you or that does not go away.

These are not all of the possible side effects of saquinavir. For more information, ask your healthcare provider or pharmacist.

Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

You may also report side effects to Genentech at 1-800-835-2555.

Tell your healthcare provider about all the medicines you take, including prescriptions and non-prescriptions medicines, vitamins and herbal supplements. Saquinavir and other medicines may affect each other causing side effects. Do not start taking a new medicine without talking with your healthcare provider or pharmacist. Your healthcare provider can tell you if it is safe to take saquinavir with other medicines.

Taking saquinavir with certain other medicines can cause serious problems or life threatening reactions.

Medicines you should not take with saquinavir and Norvir include:

• alfuzosin (Uroxatral)
• anti-infectives: clarithromycin (Biaxin), erythromycin, halofantrine, pentamidine (Pentam)
• atazanavir (Reyataz)
• tacrolimus (Prograf)
• chlorpromazine
• clozapine (Clozaril)
• haloperidol (Haldol)
• mesoridazine
• phenothiazines
• thioridazine
• ziprasidone (Geodon)
• CYP3A4 substrates: dapsone, disopyramide (Norpace), quinine
• cobicistat (Tybost)
• amiodarone (Cordarone, Pacerone)
• dofetilide (Tikosyn)
• flecainide (Tambocor)
• lidocaine
• propafenone (Rhythmol)
• quinidine
• trazodone (Oleptro)
• rifampin (Rifadin, Rifamate, Rifater, Rimactane)
• Ergot containing medicines, including:
  • dihydroergotamine mesylate (DHE 45, Embolex, Migranal)
  • ergonovine, ergonovine and methylergonovine (Ergotrate, Methergine), ergotamine and methylergonovine
  • ergotamine tartrate (Cafergot, Migergot, Ergomar, Ergostate, Medihaler Ergotamine, Wigraine, Wigrettes)
• lovastatin (Mevacor)
• simvastatin (Zocor)
• pimozide (Orap)
• sildenafil (Revatio)
• triazolam (Halcion)
• midazolam hydrochloride oral syrup

The following medicines may increase blood levels and side effects of saquinavir when taken with saquinavir and Norvir:

• delavirdine (Rescriptor)
• omeprazole (Prilosec)
• indinavir (Crixivan)

Saquinavir and Norvir may not work as well when taken together with the following medicines, herbal products, or dietary supplements:

• efavirenz (Sustiva)
• nevirapine (Viramune)
• tipranavir (Aptivus)
• ritonavir (Norvir)
• Anticonvulsants such as carbamazepine (Carbatrol, Tegretol), phenobarbital, and phenytoin (Dilantin)
• dexamethasone
• garlic capsules, an herbal product sold as a dietary supplement
• the herbal supplement St. John's wort (Hypericum perforatum) or products containing St. John's wort

Your healthcare provider may need to monitor your therapy more closely if you take saquinavir and Norvir with the following medicines:

• medicines for erectile problems, such as tadalafil (Cialis), vardenafil (Levitra), or sildenafil citrate (Viagra)
• a blood thinner medicine such as warfarin (Coumadin, Jantoven)
• Antidepressants such as trazodone (Desyrel), amitriptyline (Elavil), or imipramine (Tofranil)
• Benzodiazepines used as sedatives or sleeping pills such as alprazolam (Xanax), clorazepate (Tranxene), diazepam (Valium), and flurazepam (Dalmane)
• atorvastatin (Lipitor) used for lowering cholesterol
• Calcium channel blockers used for treatment of high blood pressure or heart disease, such as diltiazem (Cardizem, Cartia XT, Dilacor XR, Diltzac, Taztia XT, Tiazac), felodipine (Plendil), nifedipine (Procardia), nicardipine (Cardene), nimodipine (Nimotop), verapamil-containing medications (such as Calan, Verelan), amlodipine-containing medications (such as Caduet, Norvasc), nisoldipine (Sular), and isradipine (Dynacirc)
• ketoconazole (Nizoral) and itraconazole (Sporanox) used to treat fungal infections
• Medicines to prevent organ transplant rejection: cyclosporine (Sandimmune), cyclosporine (Neoral), sirolimus (Rapamune)
• fluticasone propionate (Flonase, Flovent, Advair), given by nose or inhaled to treat allergic symptoms or asthma
• digoxin (Lanoxin) used to treat heart rhythm problems or other heart conditions
• bosentan (Tracleer) and tadalafil (Adcirca) used to treat pulmonary arterial hypertension
• medicines for gout, such as colchicine (Colcrys)
• Oral contraceptives containing ethinyl estradiol used for preventing pregnancy
• Methadone
• rifabutin (Mycobutin)

If you are not sure if you take a medicine above, ask your healthcare provider or pharmacist.

Know the medicines you take. Keep a list of them to show your healthcare provider and pharmacist when you get a new medicine.

Tell your doctor if you are pregnant or plan to become pregnant.

The FDA categorizes medications based on safety for use during pregnancy. Five categories - A, B, C, D, and X, are used to classify the possible risks to an unborn baby when a medication is taken during pregnancy.

This medication falls into category B. Experience in pregnant women is limited. Saquinavir should be used during pregnancy only if the potential benefit justifies the potential risk to the unborn baby.

If you take saquinavir during pregnancy, talk with your healthcare provider about how you can take part in an antiretroviral pregnancy registry. The purpose of the pregnancy registry is to collect information about the health of you and your baby.

Tell your healthcare provider if you are breastfeeding or plan to breastfeed. Do not breastfeed. We do not know if saquinavir can be passed to your baby in your breast milk and whether it could harm your baby. Also, mothers with HIV-1 should not breastfeed because HIV-1 can be passed to the baby in the breast milk.

Saquinavir can cause changes in body fat. Changes in body fat have been seen in some people who take anti-HIV medications. These changes may include increased amount of fat in the upper back and neck ("buffalo hump"), breasts, and around the trunk. Loss of fat from the legs, arms and face may also happen.

Saquinavir must be used along with ritonavir (Norvir).

Take saquinavir with meals or up to 2 hours after a meal.

Grapefruit and grapefruit juice may interact with saquinavir and lead to potentially dangerous effects. Discuss the use of grapefruit products with your doctor.

When your saquinavir supply starts to run low, get more from your doctor or pharmacy. This is very important because the amount of virus in your blood may increase if the medicine is stopped for even a short time. The virus may develop resistance to ritonavir and become harder to treat.