Invirase (Capsule)

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ALERT: Find out about medicines that should NOT be taken with INVIRASE. Please also read the section MEDICINES YOU SHOULD NOT TAKE WITH INVIRASE. Please read this product information carefully before you start taking INVIRASE and each time you renew your prescription. There may be new information. Reading this information can help you take this medicine correctly. However, it is not a substitute for your doctor's advice about the safety and benefits of INVIRASE. You should talk to your doctor about INVIRASE as part of your long-term treatment plan for HIV before you start taking your medication and ask any questions you may have at regular checkups. Remember, you should remain under a doctor's care when using INVIRASE and should not change or stop your therapy without talking to your doctor first. What is INVIRASE? How does INVIRASE work? INVIRASE fights HIV as it grows inside cells by blocking an enzyme (protease) that HIV needs to reproduce. Who should not take INVIRASE? Anyone who has had a severe allergic reaction to INVIRASE or any of the ingredients in the capsule or tablet should not take it. The use of INVIRASE in patients under 16 years of age, over 65 years of age, or patients with severe liver problems has not been fully investigated. How should INVIRASE/Norvir' (ritonavir) be taken? What results have been seen with INVIRASE? INVIRASE with ritonavir has been shown to reduce the amount of virus in the blood ("viral load") and increase CD(T) cells when taken with other HIV therapy. What are the side effects of INVIRASE? People treated with INVIRASE in combination with Norvir may have side effects. The majority of these have been described as mild. In clinical studies of patients who received saquinavir in combination with Norvir and other HIV drugs the side effects seen most often were: body fat change (5.4%), nausea (10.8%), vomiting (7.4%), diarrhea (8.1%), stomach pain (6.1%), tiredness (6.1%), and pneumonia (5.4%). Diabetes (new onset or worsening) and increased blood sugar levels have been reported with the use of protease inhibitors. In addition, increased bleeding in patients with hemophilia has also been associated with these drugs. When saquinavir is taken with ritonavir, some patients may experience large increases in triglyceride and lipid levels. The long-term chance of getting complications such as heart attack and stroke due to increases in triglyceride and cholesterol levels caused by protease inhibitors is not known at this time. Changes in body fat have been seen in some patients taking 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 and arms may also happen. The cause and long-term health effects of these conditions are not known at this time. These are not the only side effects that can occur with INVIRASE. Your doctor can discuss with you a more complete list of side effects and laboratory abnormalities that may accompany this medication. If any side effects or unusual symptoms do occur, contact your doctor immediately. Do not stop or decrease your dose on your own. Lowering the dose may make INVIRASE less effective in fighting HIV. Are there other medications that I should not take with INVIRASE/Norvir (ritonavir)? There are some drugs that should not be taken with INVIRASE. Before starting therapy with INVIRASE; be sure to tell your doctor all of the medicines���prescription medications, as well as over-the- counter drugs and nutritional supplements���that you are now taking or plan to take. INVIRASE causes increased blood levels of these compounds. This can lead to serious or life-threatening reactions such as irregular heartbeat or prolonged sedation. Taking INVIRASE with St. John's wort (hypericum perforatum), an herbal product sold as a dietary supplement, or products containing St. John's wort is not recommended. Talk with your doctor if you are taking or are planning to take St. John's wort. Taking St. John's wort may decrease INVIRASE levels and lead to increased viral load and possible resistance to INVIRASE or cross-resistance to other antiretroviral drugs. No data are available for the coadministration of INVIRASE and Norvir with garlic capsules. Garlic capsules should not be used while taking saquinavir due to the potential for garlic capsules to decrease the amount of saquinavir in the blood. Your doctor may want to change your medicine if you are taking rifampin (known as Rifadin', Rifamate, Rifater or Rimactane) or Mycobutin (rifabutin); these drugs substantially reduce the level of INVIRASE in the blood. Rifampin, in combination with INVIRASE and ritonavir, may also cause severe liver problems. Caution should be exercised when taking INVIRASE with digoxin. Your doctor may want to decrease the dose of digoxin and monitor the levels of digoxin in your blood. The following drugs increase blood levels of INVIRASE: Norvir (ritonavir), Viracept (nelfinavir), Rescriptor (delavirdine), Nizoral (ketoconazole), Crixivan (indinavir), Biaxin(clarithromycin) and omeprazole. Talk to your doctor if you are taking lipid (cholesterol) lowering drugs and Viagra (sildenafil citrate), Levitra (vardenafil), and Cialis (tadalafil). Does INVIRASE cure HIV/AIDS? INVIRASE does not cure AIDS, and it does not prevent you from getting other illnesses that result from advanced HIV infection. In addition, INVIRASE has not been shown to reduce the risk that you may transmit HIV to others through sexual contact or infected blood. You must continue to follow all of your doctor's recommendations for managing your illness. What else should I discuss with my doctor? Inform your doctor: How is INVIRASE supplied? INVIRASE is available as light brown and green capsules in a 200-mg strength. INVIRASE comes in bottles of 270 capsules. INVIRASE is also available as light orange to greyish- or brownish-orange tablets in a 500-mg strength. INVIRASE comes in bottles of 120 tablets. How should I store INVIRASE? INVIRASE capsules and tablets should be stored at room temperature. The bottles should be kept tightly closed. INVIRASE has been prescribed specifically for you, and only for a particular condition. Do not use it for anything else. Do not give it to anyone else. If you think you have taken more than your prescribed dose, seek medical attention. Keep this medication and all other medications out of the reach of children. Do not keep medicine that is out of date or that you no longer need. Be sure that if you throw any medicine away, it is out of the reach of children. This provides only a brief summary of product information about INVIRASE. If you have any questions about INVIRASE or HIV, talk to your doctor. FORTOVASE and Versed are registered trademarks of Hoffmann-La Roche Inc. Norvir, Rhythmol, and Biaxin are registered trademarks of Abbott Laboratories. Halcion, Mycobutin and Rescriptor are registered trademarks of Pharmacia&Upjohn Co. Hismanal, Propulsid and Nizoral are registered trademarks of Janssen Pharmaceutica Inc. Seldane, Rifadin, Rifamate and Rifater are registered trademarks of Hoechst Marion Roussel. Rimactane and Cafergot are registered trademarks of Novartis Pharmaceuticals Corporation. Viracept is a registered trademark of Agouron Pharmaceuticals Inc. Crixivan is a registered trademark of Merck&Co., Inc. Viagra is a registered trademark of Pfizer, Inc. Levitra is a registered trademark of Bayer Pharmaceuticals Corp. Cialis is a registered trademark of Eli Lilly and Company. Tambocor is a registered trademark of 3M. Pacerone is a registered trademark of Upsher-Smith. If you have any questions about INVIRASE, call toll free at 1-800-910-4687. 27899381 10085697 Revised: July 2007 Copyright��1999-2007 by Roche Laboratories Inc. All rights reserved.

INVIRASE brand of saquinavir mesylate is an inhibitor of the human immunodeficiency virus (HIV) protease. INVIRASE is available as light brown and green, opaque hard gelatin capsules for oral administration in a 200-mg strength (as saquinavir free base). Each capsule also contains the inactive ingredients lactose, microcrystalline cellulose, povidone K30, sodium starch glycolate, talc, and magnesium stearate. Each capsule shell contains gelatin and water with the following dye systems: red iron oxide, yellow iron oxide, black iron oxide, FD&C Blue #2, and titanium dioxide. INVIRASE is also available as a light orange to greyish- or brownish-orange, oval cylindrical, biconvex film-coated tablet for oral administration in a 500-mg strength (as saquinavir free base). Each tablet also contains the inactive ingredients lactose, microcrystalline cellulose, povidone K30, croscarmellose sodium, and magnesium stearate. Each film coat contains hypromellose, titanium dioxide, talc, iron oxide yellow, iron oxide red, and triacetin. The chemical name for saquinavir mesylate is N-tert-butyl-decahydro-2-[2(R)-hydroxy-4-phenyl-3(S)-[[N-(2-quinolylcarbonyl)-L-asparaginyl]amino]butyl]-(4aS,8aS)-isoquinoline-3(S)-carboxamide methanesulfonate with a molecular formula CHNO���CHOS and a molecular weight of 766.96. The molecular weight of the free base is 670.86. Saquinavir mesylate has the following structural formula: Saquinavir mesylate is a white to off-white, very fine powder with an aqueous solubility of 2.22 mg/mL at 25��C.

dailymed-ingredient:saquinavir_mesylate

INVIRASE 200-mg capsules are light brown and green opaque capsules with ROCHE and 0245 imprinted on the capsule shell���bottles of 270 (NDC 0004-0245-15). INVIRASE 500-mg film-coated tablets are light orange to greyish- or brownish-orange, oval cylindrical, biconvex tablets with ROCHE and SQV 500 imprinted on the tablet face���bottles of 120 (NDC 0004-0244-51). The capsules and tablets should be stored at 25��C (77��F); excursions permitted to 15��to 30��C (59��to 86��F) [see USP Controlled Room Temperature] in tightly closed bottles.

dailymed-ingredient:FD&C_Blue_#2, dailymed-ingredient:black_iron_oxide, dailymed-ingredient:gelatin, dailymed-ingredient:lactose, dailymed-ingredient:magnesium_stearate, dailymed-ingredient:microcrystalline_cellulose, dailymed-ingredient:povidone_K30, dailymed-ingredient:red_iron_oxide, dailymed-ingredient:sodium_starch_glycolate, dailymed-ingredient:talc, dailymed-ingredient:titanium_dioxide, dailymed-ingredient:water, dailymed-ingredient:yellow_iron_oxide

saquinavir mesylate

INVIRASE must be used in combination with ritonavir, which significantly inhibits saquinavir's metabolism to provide increased plasma saquinavir levels.<br/>Concomitant Therapy with Ritonavir Adverse Reactions: In combination with ritonavir the recommended dose of INVIRASE is 1000 mg two times daily with ritonavir 100 mg two times daily in combination with other antiretroviral agents. Table 7 lists grade 2, 3 and 4 related adverse events that occurred in���2% of patients receiving saquinavir soft gel capsules with ritonavir (1000/100 mg bid). Limited experience is available from three studies 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 studies saquinavir was boosted with ritonavir; in the other study, 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 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. In a study investigating the drug-drug interaction of rifampin 600 mg/day daily and INVIRASE 1000 mg/ritonavir 100 mg twice daily (ritonavir-boosted INVIRASE) involving 28 healthy volunteers, 11 of 17 healthy volunteers (65%) exposed concomitantly to rifampin and ritonavir-boosted INVIRASE developed severe hepatocellular toxicity 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 .<br/>Additional Adverse Reactions Reported with Saquinavir: Additionally, adverse experiences of any intensity, at least remotely related to saquinavir, that were reported from clinical trials using INVIRASE or saquinavir soft gel capsules with or without ritonavir, are listed below by body system: Body as a Whole: allergic reaction, anorexia, asthenia, chest pain, drug fever, edema, fatigue, fever, intoxication, mucosa damage, parasites external, retrosternal pain, shivering, wasting syndrome, weakness generalized, weight decrease, redistribution/accumulation of body fat (see PRECAUTIONS: Fat Redistribution ) Cardiovascular: cyanosis, heart murmur, heart valve disorder, hypertension, hypotension, peripheral vasoconstriction, syncope, thrombophlebitis, vein distended Endocrine/Metabolic: appetite decrease, appetite disturbance, dehydration, diabetes mellitus, dry eye syndrome, hypercalcemia, hyperglycemia, hyperkalemia, hypernatremia, hyperphosphatemia, hypertriglyceridemia, hypocalcemia, hypokalemia, hyponatremia, hypophosphatemia, weight increase, xerophthalmia Gastrointestinal: ascites, abdominal discomfort, buccal mucosa ulceration, cheilitis, colic abdominal, constipation, dyspepsia, dysphagia, esophagitis, eructation, exacerbation of chronic liver disease with grade 4 LFT, feces bloodstained, feces discolored, flatulence, gastralgia, gastritis, gastrointestinal inflammation, intestinal obstruction, gingivitis, glossitis, hemorrhage rectum, hemorrhoids, hepatitis, hepatomegaly, hepatosplenomegaly, hyperbilirubinemia, infectious diarrhea, jaundice, liver enzyme disorder, melena, pain pelvic, painful defecation, pancreatitis, parotid disorder, portal hypertension, right and left upper quadrant abdominal pain, salivary glands disorder, stomach upset, stomatitis, toothache, tooth disorder, vomiting Hematologic: anemia, bleeding dermal, hemolytic anemia, leucopenia, microhemorrhages, neutropenia, pancytopenia, splenomegaly, thrombocytopenia, thrombocytopenia leading to death Investigations: ALT increase, AST increase, GGT increase, increased alkaline phosphatase, increased creatine phosphokinase, increased gamma GT, isolated increase in transaminase, raised amylase, raised LDH, TSH increase Musculoskeletal: arthralgia, arthritis, back pain, cramps leg, cramps muscle, creatine phosphokinase increased, musculoskeletal disorders, musculoskeletal pain, myalgia, stiffness, tissue changes, trauma Neoplasms benign, malignant and unspecified: acute myeloblastic leukemia Neurological: ataxia, bowel movements frequent, confusion, convulsions, dizziness, dysarthria, dysesthesia, extremity numbness, headache, heart rate disorder, hyperesthesia, hyperreflexia, hyporeflexia, light-headed feeling, mouth dry, myelopolyradiculoneuritis, numbness face, pain facial, paresis, paresthesia, peripheral neuropathy, poliomyelitis, prickly sensation, progressive multifocal leukoencephalopathy, seizures, spasms, tremor, unconsciousness Psychological: agitation, amnesia, anxiety, anxiety attack, depression, dreaming excessive, euphoria, hallucination, insomnia, intellectual ability reduced, irritability, lethargy, libido disorder, overdose effect, psychic disorder, psychosis, somnolence, speech disorder, suicide attempt Reproductive System: impotence, prostate enlarged, vaginal discharge Resistance Mechanism: abscess, angina tonsillaris, candidiasis, cellulitis, herpes simplex, herpes zoster, infection bacterial, infection mycotic, infection staphylococcal, influenza, lymphadenopathy, moniliasis, tumor Respiratory: bronchitis, cough, dyspnea, epistaxis, hemoptysis, laryngitis, pharyngitis, pneumonia, pulmonary disease, respiratory disorder, rhinitis, sinusitis, upper respiratory tract infection Skin and Appendages: acne, alopecia, bullous skin eruption and polyarthritis, chalazion, dermatitis, dermatitis seborrheic, eczema, erythema, folliculitis, furunculosis, hair changes, hot flushes, nail disorder, night sweats, papillomatosis, photosensitivity reaction, pigment changes skin, rash maculopapular, severe cutaneous reaction associated with increased liver function tests, skin disorder, skin nodule, skin ulceration, Stevens-Johnson syndrome, sweating increased, urticaria, verruca, xeroderma Special Senses: blepharitis, earache, ear pressure, eye irritation, hearing decreased, otitis, taste alteration, tinnitus, visual disturbance Urinary System: micturition disorder, nephrolithiasis, renal calculus, urinary tract bleeding, urinary tract infection<br/>Postmarketing Experience with INVIRASE: Additional adverse events that have been observed during the postmarketing period are similar to those seen in clinical trials with INVIRASE and saquinavir soft gel capsules alone or in combination with ritonavir.

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Invirase