Saquinavir

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Generic Name: Saquinavir Brand Name(s): Generics only. No brands available.

Uses

What is Saquinavir used for?

Saquinavir used in combination with ritonavir and other HIV medications, is used to help control HIV infection. It helps to decrease the amount of HIV in your body so your immune system can work better. This lowers your chance of getting HIV complications (such as new infections, cancer) and improves your quality of life.

Saquinavir belongs to a class of drugs known as protease inhibitors. It must be given with ritonavir, another protease inhibitor, to increase (“boost”) the levels of saquinavir. This helps saquinavir work better.

Saquinavir is not a cure for HIV infection. To decrease your risk of spreading HIV disease to others, do all of the following: (1) continue to take all HIV medications exactly as prescribed by your doctor, (2) always use an effective barrier method (latex or polyurethane condoms/dental dams) during all sexual activity, and (3) do not share personal items (such as needles/syringes, toothbrushes, and razors) that may have contacted blood or other body fluids. Consult your doctor or pharmacist for more details.

How should I take Saquinavir?

Take your dose of saquinavir and ritonavir by mouth at the same times, as directed by your doctor, with a meal or up to 2 hours after a meal, usually 2 times daily.

To reduce your risk of side effects, your doctor may direct you to start saquinavir at a low dose and gradually increase your dose. Follow your doctor’s instructions carefully.

The dosage is based on your medical condition, response to treatment, and other medications you may be taking. Be sure to tell your doctor and pharmacist about all the products you use (including prescription drugs, nonprescription drugs, and herbal products).

For the best effect, take this medication at evenly spaced times. To help you remember, take this medication at the same times every day.

It is very important to continue taking this medication (and other HIV medications) exactly as prescribed by your doctor. Do not take more or less of this drug than prescribed or stop taking it (or other HIV medicines) even for a short time unless directed to do so by your doctor. Skipping or changing your dose without approval from your doctor may cause the amount of virus to increase, make the infection more difficult to treat, or worsen side effects.

How do I store Saquinavir?

Saquinavir is best stored at room temperature away from direct light and moisture. To prevent drug damage, you should not store Saquinavir in the bathroom or the freezer. There may be different brands of Saquinavir that may have different storage needs. It is important to always check the product package for instructions on storage, or ask your pharmacist. For safety, you should keep all medicines away from children and pets.

You should not flush Saquinavir down the toilet or pour them into a drain unless instructed to do so. It is important to properly discard this product when it is expired or no longer needed. Consult your pharmacist for more details about how to safely discard your product.

Precautions & warnings

What should I know before using Saquinavir?

Before taking saquinavir, tell your doctor or pharmacist if you are allergic to it; or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.

Before using this medication, tell your doctor or pharmacist your medical history, especially of: lipid problems (high cholesterol or triglycerides/fats), diabetes, hemophilia, liver problems.

Saquinavir may cause a condition that affects the heart rhythm (QT prolongation). QT prolongation can rarely cause serious (rarely fatal) fast/irregular heartbeat and other symptoms (such as severe dizziness, fainting) that need medical attention right away.

The risk of QT prolongation may be increased if you have certain medical conditions or are taking other drugs that may cause QT prolongation. Before using saquinavir, tell your doctor or pharmacist of all the drugs you take and if you have any of the following conditions: certain heart problems (heart failure, slow heartbeat, QT prolongation in the EKG), family history of certain heart problems (QT prolongation in the EKG, sudden cardiac death).

Low levels of potassium or magnesium in the blood may also increase your risk of QT prolongation. This risk may increase if you use certain drugs (such as diuretics/”water pills”) or if you have conditions such as severe sweating, diarrhea, or vomiting. Talk to your doctor about using saquinavir safely.

Before having surgery, tell your doctor or dentist about all the products you use (including prescription drugs, nonprescription drugs, and herbal products).

Older adults may be more sensitive to the side effects of this drug, especially QT prolongation.

During pregnancy, this medication should be used only when clearly needed. Treatment can lower the risk of passing HIV infection to your baby, and saquinavir may be part of that treatment. Discuss the risks and benefits with your doctor.

It is unknown if this medication passes into breast milk. Because breast milk can transmit HIV, do not breast-feed.

Is it safe during pregnancy or breast-feeding?

There are no adequate studies in women for determining risk when using this Saquinavir during pregnancy or while breastfeeding. Please always consult with your doctor to weigh the potential benefits and risks before taking Saquinavir. Saquinavir is pregnancy risk category B according to the US Food and Drug Administration (FDA).

FDA pregnancy risk category reference below:

  • A=No risk,
  • B=No risk in some studies,
  • C=There may be some risk,
  • D=Positive evidence of risk,
  • X=Contraindicated,
  • N=Unknown

Side effects

What side effects can occur from Saquinavir?

Diarrhea, nausea, vomiting, stomach pain, or tiredness may occur. If any of these effects persist or worsen, tell your doctor or pharmacist promptly.

Remember that your doctor has prescribed this medication because he or she has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.

As your immune system gets stronger, it can begin to fight off infections you already had, possibly causing disease symptoms to come back. You could also have symptoms if your immune system becomes overactive. This reaction may happen at any time (soon after starting HIV treatment or many months later). Get medical help right away if you have any serious symptoms, including: unexplained weight loss, severe tiredness, muscle aches/weakness that doesn’t go away, headaches that are severe or don’t go away, joint pain, numbness/tingling of the hands/feet/arms/legs, vision changes, signs of infection (such as fever, chills, swollen lymph nodes, trouble breathing, cough, non-healing skin sores), signs of an overactive thyroid (such as irritability, nervousness, heat intolerance, fast/pounding/irregular heartbeat, bulging eyes, unusual growth in the neck/thyroid known as a goiter), signs of a certain nerve problem known as Guillain-Barre syndrome (such as trouble breathing/swallowing/moving your eyes, drooping face, paralysis, trouble speaking).

Get medical help right away if you have any very serious side effects, such as: symptoms of a heart attack (such as chest/jaw/left arm pain, shortness of breath, unusual sweating), fast/slow/irregular heartbeat, severe dizziness, fainting, persistent nausea/vomiting, stomach/abdominal pain, dark urine, yellowing eyes/skin.

This medication may rarely make your blood sugar rise, which can cause or worsen diabetes. Tell your doctor right away if you have symptoms of high blood sugar such as increased thirst/urination. If you already have diabetes, check your blood sugar regularly as directed and share the results with your doctor. Your doctor may need to adjust your diabetes medication, exercise program, or diet.

Changes in body fat may occur while you are taking this medication (such as increased fat in the upper back and stomach areas, decreased fat in the arms and legs). The cause and long-term effects of these changes are unknown. Discuss the risks and benefits of treatment with your doctor, as well as the possible use of exercise to reduce this side effect.

A very serious allergic reaction to this drug is rare. However, seek immediate medical attention if you notice any symptoms of a serious allergic reaction, including: rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing.

Not everyone experiences these side effects. There may be some side effects not listed above. If you have any concerns about a side-effect, please consult your doctor or pharmacist.

Interactions

What drugs may interact with Saquinavir?

Some products that may interact with this drug include: orlistat, trazodone, certain benzodiazepines (midazolam, triazolam), ergot alkaloids (such as dihydroergotamine, ergonovine, ergotamine, methylergonovine), garlic supplements, ranolazine, rifamycins (such as rifampin, rifapentine), certain “statin” cholesterol drugs (simvastatin, lovastatin), St. John’s wort.

Many drugs besides saquinavir may affect the heart rhythm (QT prolongation), including quinidine, pimozide, propafenone, cisapride, amiodarone, dofetilide, flecainide, salmeterol, clarithromycin, erythromycin, pentamidine, tacrolimus, among others.

Other medications can affect the removal of saquinavir from your body, which may affect how saquinavir works. Examples include other HIV protease inhibitors (such as atazanavir, indinavir, nelfinavir, tipranavir), cobicistat, among others.

Saquinavir can slow down the removal of other medications from your body, which may affect how they work. Examples of affected drugs include asunaprevir, dapsone, haloperidol, lurasidone, drugs to treat erectile dysfunction-ED or pulmonary hypertension (such as sildenafil, vardenafil, tadalafil), isavuconazonium, naloxegol, rilpivirine, rivaroxaban, suvorexant, among others.

This medication may decrease the effectiveness of hormonal birth control such as pills, patch, or ring. This could cause pregnancy. Talk to your doctor about additional or alternative reliable forms of birth control, and always use an effective barrier method (latex or polyurethane condoms/dental dams) during all sexual activity to decrease the risk of spreading HIV to others. Tell your doctor if you have any new spotting or breakthrough bleeding, because these may be signs that your hormonal birth control is not working well.

Saquinavir may interact with other drugs that you are currently taking, which can change how your drug works or increase your risk for serious side effects. To avoid any potential drug interactions, you should keep a list of all the drugs you are using (including prescription drugs, nonprescription drugs and herbal products) and share it with your doctor and pharmacist. For your safety, do not start, stop, or change the dosage of any drugs without your doctor’s approval.

Does food or alcohol interact with Saquinavir?

Saquinavir may interact with food or alcohol by altering the way the drug works or increase the risk for serious side effects. Please discuss with your doctor or pharmacist any potential food or alcohol interactions before using this drug.

What health conditions may interact with Saquinavir?

Saquinavir may interact with your health condition. This interaction may worsen your health condition or alter the way the drug works. It is important to always let your doctor and pharmacist know all the health conditions you currently have.

Dosage

The information provided is not a substitute for any medical advice. You should ALWAYS consult with your doctor or pharmacist before using this Saquinavir.

What is the dose of Saquinavir for an adult?

Usual Adult Dose for HIV Infection

Standard dose: Saquinavir 1000 mg plus ritonavir 100 mg orally twice a day

Therapy-naive patients (starting therapy with saquinavir/ritonavir):

-The first 7 days: Saquinavir 500 mg plus ritonavir 100 mg orally twice a day

-After 7 days: Saquinavir 1000 mg plus ritonavir 100 mg orally twice a day

Patients switching immediately (no washout period) from another ritonavir-containing regimen or from a NNRTI-based regimen (excluding delavirdine, rilpivirine): Saquinavir 1000 mg plus ritonavir 100 mg orally twice a day

Patients switching from a regimen containing delavirdine or rilpivirine:

-The first 7 days: Saquinavir 500 mg plus ritonavir 100 mg orally twice a day

-After 7 days: Saquinavir 1000 mg plus ritonavir 100 mg orally twice a day

Use: In combination with ritonavir and other antiretrovirals, for the treatment of HIV-1 infection

Usual Adult Dose for Nonoccupational Exposure

US CDC recommendations: Saquinavir 1000 mg plus ritonavir 100 mg (or saquinavir 400 mg plus ritonavir 400 mg) orally twice a day

Duration of therapy: 28 days

Comments:

-Recommended as part of an alternative regimen for nonoccupational postexposure prophylaxis of HIV infection

-This drug (plus ritonavir) should be used with (lamivudine or emtricitabine) plus (zidovudine or stavudine or abacavir or tenofovir or didanosine).

-Prophylaxis should be started as soon as possible, within 72 hours of exposure.

-Current guidelines should be consulted for additional information.

Usual Adult Dose for Occupational Exposure

US Public Health Service working group recommendations: Saquinavir 1000 mg plus ritonavir 100 mg orally twice a day

Duration of therapy: 28 days, if tolerated

Comments:

-Only with expert consultation, as part of an alternative regimen for use as HIV postexposure prophylaxis

-Prophylaxis should be started as soon as possible, preferably within hours after exposure.

-The optimal duration of prophylaxis is unknown and may differ based on institution protocol.

-Current guidelines should be consulted for additional information.

Renal Dose Adjustments

Mild or moderate renal dysfunction: No adjustment recommended.

Severe renal dysfunction or end-stage renal disease: No adjustment recommended; caution recommended.

Liver Dose Adjustments

Mild or moderate liver dysfunction: No adjustment recommended.

When used with ritonavir:

-Severe liver dysfunction: Contraindicated

Dose Adjustments

If serious or severe toxicity occurs during therapy, this drug should be interrupted until cause is determined or toxicity resolves; at that time, resumption of this drug at the full dose may be considered.

Other Comments

Administration advice:

-Must use in combination with ritonavir and other antiretrovirals.

-Administer this drug at the same time as ritonavir and within 2 hours after a full meal.

-Do not administer additional ritonavir in patients already using ritonavir (100 mg twice a day) as part of their antiretroviral regimen.

-Patients unable to swallow capsules: (1) Open capsules and place contents into empty container; (2) Add 15 mL of either sugar syrup or sorbitol syrup (for patients with type 1 diabetes or glucose intolerance) OR 3 teaspoons of jam to the capsule contents in the container; (3) Stir with spoon for 30 to 60 seconds; (4) Administer the full amount prepared for each dose; suspensions should be at room temperature before use.

Storage requirements:

-Store at 25C (77F); excursion permitted to 15C to 30C (59F to 86F); close bottle tightly.

General:

-The following should be considered when starting this drug: Twice-daily use of this drug (plus ritonavir) is supported by safety and pharmacokinetic data; efficacy of this drug (plus ritonavir) has not been compared against efficacy of antiretroviral regimens currently considered standard of care; the number of baseline primary protease inhibitor mutations affects virologic response to this drug (plus ritonavir).

-Ritonavir significantly inhibits metabolism of this drug, increasing plasma saquinavir levels; the manufacturer product information for ritonavir should be consulted.

-Cobicistat is not interchangeable with ritonavir to increase systemic exposure of this drug.

Monitoring:

-Cardiovascular: ECG (before starting and during therapy); PR interval (if used with other agents that prolong PR interval)

-Metabolic: Potassium and magnesium (periodically during therapy); cholesterol and triglyceride levels (prior to therapy and periodically thereafter)

Patient advice:

-Read the US FDA-approved patient labeling (Medication Guide).

-Consult healthcare provider if dizziness, lightheadedness, or palpitations occur.

What is the dose of Saquinavir for a child?

Usual Pediatric Dose for HIV Infection

16 years or older:

Standard dose: Saquinavir 1000 mg plus ritonavir 100 mg orally twice a day

Therapy-naive patients (starting therapy with saquinavir/ritonavir):

-The first 7 days: Saquinavir 500 mg plus ritonavir 100 mg orally twice a day

-After 7 days: Saquinavir 1000 mg plus ritonavir 100 mg orally twice a day

Patients switching immediately (no washout period) from another ritonavir-containing regimen or from a NNRTI-based regimen (excluding delavirdine, rilpivirine): Saquinavir 1000 mg plus ritonavir 100 mg orally twice a day

Patients switching from a regimen containing delavirdine or rilpivirine:

-The first 7 days: Saquinavir 500 mg plus ritonavir 100 mg orally twice a day

-After 7 days: Saquinavir 1000 mg plus ritonavir 100 mg orally twice a day

Comments:

-Doses that are both reliably effective and safe (i.e., below levels of concern for QT and PR interval prolongation) could not be established for pediatric patients younger than 16 years.

Use: In combination with ritonavir and other antiretrovirals, for the treatment of HIV-1 infection

How is Saquinavir available?

Saquinavir is available in the following dosage forms and strengths:

  • Oral tablet,
  • Oral capsule.

What should I do in case of an emergency or overdose?

In case of an emergency or an overdose, call your local emergency services or go to your nearest emergency room.

What should I do if I miss a dose?

If you miss a dose of Saquinavir, take it as soon as possible. However, if it is almost time for your next dose, skip the missed dose and take your regular dose as scheduled. Do not take a double dose.

Hello Health Group does not provide medical advice, diagnosis or treatment.

Review Date: April 26, 2018 | Last Modified: April 26, 2018

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