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Invirase

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Invirase

Invirase Side Effects Center

Medical Editor: John P. Cunha, DO, FACOEP

Invirase (saquinavir mesylate) is used to treat HIV, which causes acquired immunodeficiency syndrome (AIDS). It is not a cure for HIV or AIDS. It is a type of antiviral medication called a protease inhibitor. Common side effects include diarrhea, nausea, vomiting, stomach pain, or tiredness.

The recommended dose of Invirase for adults over the age of 16 years is 1000-mg twice daily (5 x 200-mg capsules or 2 x 500-mg tablets) in combination with ritonavir 100-mg twice daily. Ritonavir should be taken at the same time as Invirase, and both should be taken within 2 hours after a meal. Invirase may interact with digoxin, fluticasone, garlic, St. John's wort, antibiotics, antidepressants, blood thinners, calcium channel blockers, cholesterol-lowering medicines, drugs that weaken the immune system, other HIV /AIDS medicines, insulin or oral diabetes medications, medicines to treat erectile dysfunction, or seizure medications. Other medicines may interact with Invirase. Tell your doctor all medications and supplements you use. Tell your doctor if you are pregnant before using Invirase. It is unknown if this drug passes into breast milk. Because breast milk can transmit HIV, do not breastfeed.

Our Invirase (saquinavir mesylate) Side Effects Drug Center provides a comprehensive view of available drug information on the potential side effects when taking this medication.

This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

What is Patient Information in Detail?

Easy-to-read and understand detailed drug information and pill images for the patient or caregiver from Cerner Multum.

Invirase in Detail - Patient Information: Side Effects

Get emergency medical help if you have any of these signs of an allergic reaction: hives; difficulty breathing; swelling of your face, lips, tongue, or throat.

Stop taking saquinavir and call your doctor at once if you have a serious side effect such as:

  • increased thirst or urination, excessive hunger, fruity breath odor;
  • cough with yellow or green mucus, stabbing chest pain, wheezing, feeling short of breath;
  • fever, chills, body aches, flu symptoms, mouth and throat ulcers;
  • any type of infection, skin infection, or open sores;
  • rapid heart rate, increased sweating, tremors in your hands, anxiety, feeling irritable, sleep problems (insomnia);
  • diarrhea, unexplained weight loss, menstrual changes, impotence, loss of interest in sex;
  • swelling in your neck or throat (enlarged thyroid);
  • muscle weakness, tired feeling, trouble speaking or swallowing, joint or muscle pain, feeling short of breath;
  • weakness or prickly feeling in your fingers or toes;
  • problems with walking, breathing, speech, swallowing, or eye movement; or
  • severe lower back pain, loss of bladder or bowel control.

Less serious side effects may include:

  • mild nausea, vomiting, stomach pain;
  • tired feeling; or
  • changes in the shape or location of body fat (especially in your arms, legs, face, neck, breasts, and waist).

This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

Read the entire detailed patient monograph for Invirase (Saquinavir Mesylate) »

What is Patient Information Overview?

A concise overview of the drug for the patient or caregiver from First DataBank.

Invirase Overview - Patient Information: Side Effects

SIDE EFFECTS: 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.

Some people may experience worsening of a previous medical condition (such as an old infection) as their immune systems improve, or develop new conditions because their immune systems have become overactive. This reaction may occur at any time (soon after starting HIV treatment or many months later). Tell your doctor right away if you have any serious side effects, including: unexplained weight loss, persistent muscle aches/weakness, joint pain, numbness/tingling of the hands/feet/arms/legs, severe tiredness, vision changes, severe/persistent headaches, signs of infection (such as fever, chills, 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 difficulty breathing/swallowing/moving your eyes, drooping face, paralysis, slurred speech).

Seek immediate medical attention if any of these rare but serious side effects occur: 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 infrequently make your blood sugar level rise, which can cause or worsen diabetes. Tell your doctor immediately if you develop symptoms of high blood sugar such as increased thirst and urination. If you already have diabetes, check your blood sugar levels regularly. 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.

This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.

In the US -

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

In Canada - Call your doctor for medical advice about side effects. You may report side effects to Health Canada at 1-866-234-2345.

Read the entire patient information overview for Invirase (Saquinavir Mesylate)»

What is Prescribing information?

The FDA package insert formatted in easy-to-find categories for health professionals and clinicians.

Invirase FDA Prescribing Information: Side Effects
(Adverse Reactions)

SIDE EFFECTS

The following adverse reactions are discussed in greater detail in other sections of the labeling:

  • PR Interval Prolongation [see WARNINGS AND PRECAUTIONS]
  • QT Interval Prolongation [see WARNINGS AND PRECAUTIONS ]

Clinical Trial Experience in Adult Subjects

Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in clinical practice.

The original INVIRASE safety database consisted of a total of 574 adult subjects who received saquinavir 600 mg alone or in combination with ZDV or ddC. Combination dosing with ritonavir is based on 352 HIV-1 infected subjects and 166 healthy subjects who received various combinations of either saquinavir (hard gel or soft-gel capsules) with ritonavir.

The recommended dose of INVIRASE is 1000 mg twice daily co-administered with ritonavir 100 mg twice daily, in combination with other antiretroviral agents. Table 2 lists grade 2, 3 and 4 adverse events that occurred in ≥ 2% of subjects receiving saquinavir soft gel capsules with ritonavir (1000/100 mg bid).

Table 2 : Grade 2, 3 and 4 Adverse Events (All Causalitya) Reported in ≥ 2% of Adult Subjects in the MaxCmin 1 Study of Saquinavir Soft Gel Capsules in Combination with Ritonavir 1000/100 mg twice a day

Adverse Events Saquinavir soft gel capsules 1000 mg plus Ritonavir 100 mg bid (48 weeks)
N=148
n (%=n/N)
Endocrine Disorders
  Diabetes mellitus/hyperglycemia 4 (3)
  Lipodystrophy 8 (5)
Gastrointestinal Disorders
  Nausea 16 (11)
  Vomiting 11 (7)
  Diarrhea 12 (8)
  Abdominal Pain 9 (6)
  Constipation 3 (2)
General Disorders and Administration Site Conditions
  Fatigue 9 (6)
  Fever 5 (3)
Musculoskeletal Disorders
  Back Pain 3 (2)
Respiratory Disorders
  Pneumonia 8 (5)
  Bronchitis 4 (3)
  Influenza 4 (3)
  Sinusitis 4 (3)
Dermatological Disorders
  Rash 5 (3)
  Pruritus 5 (3)
  Dry lips/skin 3 (2)
  Eczema 3 (2)
aIncludes events with unknown relationship to study drug

Limited experience is available from three trials investigating the pharmacokinetics of the INVIRASE 500 mg film-coated tablet compared to the INVIRASE 200 mg capsule in healthy volunteers (n=140). In two of these trials saquinavir was boosted with ritonavir; in the other trial, saquinavir was administered as single drug. The INVIRASE tablet and the capsule formulations were similarly tolerated. The most common adverse events were gastrointestinal disorders (such as nausea, vomiting, and diarrhea). Similar bioavailability was demonstrated and no clinically significant differences in saquinavir exposures were seen. Thus, similar safety profiles are expected between the two INVIRASE formulations.

A study investigating the drug-drug interaction of rifampin 600 mg/day daily and INVIRASE 1000 mg/ritonavir 100 mg twice daily enrolled 28 healthy volunteers. Eleven of 17 healthy volunteers (65%) exposed concomitantly to rifampin and ritonavir-boosted INVIRASE developed severe hepatocellular toxicity which presented as increased hepatic transaminases. In some subjects, transaminases increased up to > 20-fold the upper limit of normal and were associated with gastrointestinal symptoms, including abdominal pain, gastritis, nausea, and vomiting. Following discontinuation of all three drugs, clinical symptoms abated and the increased hepatic transaminases normalized [see CONTRAINDICATIONS].

Additional Adverse Reactions Reported During Clinical Trials with Saquinavir

Blood and lymphatic system disorders: anemia, hemolytic anemia, leukopenia, lymphadenopathy, neutropenia, pancytopenia, thrombocytopenia

Cardiac disorders: heart murmur, syncope

Ear and labyrinth disorders: tinnitus

Eye disorders: visual impairment

Gastrointestinal disorders: abdominal discomfort, ascites, dyspepsia, dysphagia, eructation, flatulence, gastritis, gastrointestinal hemorrhage, intestinal obstruction, mouth dry, mucosal ulceration, pancreatitis

General disorders and administration site conditions: anorexia, asthenia, chest pain, edema, lethargy, wasting syndrome, weight increased

Hepatobiliary disorders: chronic active hepatitis, hepatitis, hepatomegaly, hyperbilirubinemia, jaundice, portal hypertension

Immune system disorders: allergic reaction

Investigations: ALT increase, AST increase, blood creatine phosphokinase increased, increased alkaline phosphatase, GGT increase, raised amylase, raised LDH

Metabolism and nutrition disorders: increased or decreased appetite, dehydration, hypertriglyceridemia

Musculoskeletal and connective tissue disorders: arthralgia, muscle spasms, myalgia, polyarthritis

Neoplasms benign, malignant and unspecified (incl cysts and polyps): acute myeloid leukemia, papillomatosis

Nervous system disorders: confusion, convulsions, coordination abnormal, dizziness, dysgeusia, headache, hypoaesthesia, intracranial hemorrhage leading to death, loss of consciousness, paresthesia, peripheral neuropathy, somnolence, tremor

Psychiatric disorders: anxiety, depression, insomnia, libido disorder, psychotic disorder, sleep disorder, suicide attempt

Renal and urinary disorders: nephrolithiasis

Respiratory, thoracic and mediastinal disorders: cough, dyspnea

Skin and subcutaneous tissue disorders: acne, alopecia, dermatitis bullous, drug eruption, erythema, severe cutaneous reaction associated with increased liver function tests, Stevens-Johnson syndrome, sweating increased, urticaria

Vascular disorders: hypertension, hypotension, thrombophlebitis, peripheral vasoconstriction

Clinical Trial Experience in Pediatric Subjects

Limited safety data are available from two pediatric clinical trials of saquinavir hard gel capsules (approximately 50 mg per kg twice daily) used in combination with either low dose ritonavir or lopinavir/ritonavir. These trials enrolled pediatric subjects aged 4 months to 16 years old. In the HIVNAT 017 study (INVIRASE + lopinavir/ritonavir), adverse events were reported in 90% of the 50 subjects enrolled. The most commonly reported adverse events considered related to study treatment were diarrhea (18%) and vomiting (10%). In the NV20911 study (INVIRASE + ritonavir), 4 subjects (22% of 18 enrolled) experienced adverse events that were considered related to INVIRASE + ritonavir. These events (n) were vomiting (3), abdominal pain (1) and diarrhea (1). All reported adverse events were mild or moderate in intensity. The adverse reaction profile of INVIRASE in the pediatric trials is similar to that observed in adult trials.

Postmarketing Experience

Additional adverse events identified during postmarketing use are similar to those observed in clinical trials with INVIRASE and saquinavir soft gel capsules alone or in combination with ritonavir. Because these events are reported voluntarily from a population of uncertain size, it is not always possible to reliably estimate their frequency or establish a causal relationship to INVIRASE exposure. In addition, torsades de pointes has been reported rarely [see WARNINGS AND PRECAUTIONS].

Read the entire FDA prescribing information for Invirase (Saquinavir Mesylate) »

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Report Problems to the Food and Drug Administration

 

You are encouraged to report negative side effects of prescription drugs to the FDA. Visit the FDA MedWatch website or call 1-800-FDA-1088.


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