Agenerase

Name: Agenerase

What brand names are available for amprenavir?

Agenerase (Discontinued Brand)

Do I need a prescription for amprenavir?

Yes

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Reviewed on 8/7/2017 References Medically reviewed by John Cunha, DO

Reference: FDA Prescribing Information

Agenerase Interactions

Agenerase can cause dangerous and life-threatening interactions if taken with certain other medicines. Tell your healthcare provider about all the medicines you take, including prescription and nonprescription medicines, vitamins, and herbal supplements. The following medications should not be taken with Agenerase. Especially tell your doctor if you take:

  • Halcion (triazolam; used for insomnia)
  • Ergot medicines: dihydroergotamine, ergonovine, ergotamine, and methylergonovine such as Cafergot, Migranal, D.H.E. 45, ergotrate maleate, Methergine, and others (used for migraine headaches)
  • Propulsid (cisapride), used for certain stomach problems
  • Rifampin
  • St. John's Wort
  • Ritonavir
  • Lovastatin and Simvastatin
  • Versed (midazolam), used for sedation
  • Orap (pimozide), used for Tourette’s disorder
  • Revatio (sildenafil), used for treatment of pulmonary arterial hypertension
  • Uroxatral (alfuzosin), used for benign prostatic hyperplasia (BPH)
  • Birth control pills. Women who use birth control pills should choose a different kind of contraception. The use of Agenerase may decrease the effectiveness of birth control pills. Talk to your healthcare provider about choosing an effective contraceptive.

Patients taking antacids (or the buffered formulation of didanosine) should take Agenerase at least 1 hour before or after antacid (or the buffered formulation of didanosine) use.

You should not take Agenerase (amprenavir) and fosamprenavir at the same time.

This is not a complete list of Agenerase drug interactions. Ask your doctor or pharmacist for more information.

Tell your healthcare provider about all medicines you are taking before you begin taking Agenerase. 

Agenerase Precautions

Agenerase may cause the following side effects:

  • skin rash. Skin rashes, some with itching, have happened in patients taking Agenerase. Swelling of the face, lips, and tongue (angioedema) has also been reported. Tell your healthcare provider if you get a rash or develop facial swelling after starting Agenerase.
  • diabetes and high blood sugar (hyperglycemia). Some patients had diabetes before taking Agenerase while others did not. Some patients may need changes in their diabetes medicine. Others may need a new diabetes medicine.
  • increased bleeding problems in some patients with hemophilia.
  • worse liver disease. Patients with liver problems, including hepatitis B or C, are more likely to get worse liver disease when they take anti-HIV medicines like Agenerase.
  • changes in blood tests. Some people have changes in blood tests while taking Agenerase. These include increases seen in liver function tests and decreases in white blood cells. Your healthcare provider may do regular blood tests to see if Agenerase is affecting your body.
  • changes in body fat. These changes have happened in patients taking antiretroviral medicines like Agenerase. The changes may include an increased amount of fat in the upper back and neck ("buffalo hump"), breast, 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.
  • increase in lipids. Cholesterol and triglycerides can become elevated after taking Agenerase. Your doctor will order lab tests before treatment and during treatment. 
  • bleeding in patients with hemophilia A and B. Additional factor VIII may be required.
  • kidney stones have been reported in some patients taking Agenerase. If you develop signs or symptoms of kidney stones (pain in your side, blood in your urine, pain when you urinate) tell your healthcare provider right away.

Do not take supplemental vitamin E since Agenerase includes high amount of vitamin E already. 

Do not drink alcohol while taking Agenerase. 

Do not take Agenerase if you:

  • are allergic to fosamprenavir or any of its ingredients. 
  • are allergic to Agenerase (amprenavir) or any of its ingredients
  • are pregnant
  • have liver or kidney failure
  • taking metronidazole, disulfiram, Dihydroergotamine, ergonovine, ergotamine, methylergonovine, cisapride, pimozide, Midazolam, triazolam

Avoid doing things that can spread HIV infection since Agenerase doesn't stop you from passing the HIV infection to others.

  • Do not share needles or other injection equipment.
  • Do not share personal items that can have blood or body fluids on them, like toothbrushes or razor blades.
  • Do not have any kind of sex without protection. Always practice safer sex by using a latex or polyurethane condom to lower the chance of sexual contact with semen, vaginal secretions, or blood.

Agenerase Usage

Take Agenerase exactly as your healthcare provider prescribed.

  • Do not take more or less than your prescribed dose of Agenerase at any one time. Do not change your dose or stop taking Agenerase without talking with your healthcare provider.
  • This medication comes in capsule and oral solution forms and is usually taken two to three times a day, with or without food. 
  • You can take Agenerase with or without food.
  • Do not take Agenerase with high-fat meals. High-fat meals may decrease the way the body absorbs Agenerase and reduces how it works. 
  • Do not take vitamin E while taking Agenerase. It contains large amounts of vitamin E.
  • When your supply of Agenerase or other anti-HIV medicine starts to run low, get more from your healthcare provider or pharmacy. The amount of HIV virus in your blood may increase if one or more of the medicines are stopped, even for a short time.
  • Stay under the care of a healthcare provider while using Agenerase.
  • It is important that you do not miss any doses. If you miss a dose of Agenerase by more than 4 hours, wait and take the next dose at the regular time. However, if you miss a dose by fewer than 4 hours, take your missed dose right away. Then take your next dose at the regular time.

Agenerase Description

Agenerase (amprenavir) is an inhibitor of the human immunodeficiency virus (HIV) protease. The chemical name of amprenavir is (3S)-tetrahydro-3-furyl N-[(1S,2R)-3-(4-amino-N-isobutylbenzenesulfonamido)-1-benzyl-2-hydroxypropyl]carbamate. Amprenavir is a single stereoisomer with the (3S)(1S,2R) configuration. It has a molecular formula of C25H35N3O6S and a molecular weight of 505.64. It has the following structural formula:

Amprenavir is a white to cream-colored solid with a solubility of approximately 0.04 mg/mL in water at 25°C.

Agenerase Capsules are available for oral administration. Each 50-mg capsule contains the inactive ingredients d-alpha tocopheryl polyethylene glycol 1000 succinate (TPGS), polyethylene glycol 400 (PEG 400) 246.7 mg, and propylene glycol 19 mg. The capsule shell contains the inactive ingredients d-sorbitol and sorbitans solution, gelatin, glycerin, and titanium dioxide. The soft gelatin capsules are printed with edible red ink. Each 50-mg Agenerase Capsule contains 36.3 IU vitamin E in the form of TPGS. The total amount of vitamin E in the recommended daily adult dose of Agenerase is 1,744 IU.

Precautions

General

Agenerase Capsules and Agenerase Oral Solution are not interchangeable on a milligram-per-milligram basis(see CLINICAL PHARMACOLOGY: Pediatric Patients).

Amprenavir is a sulfonamide. The potential for cross-sensitivity between drugs in the sulfonamide class and amprenavir is unknown. Agenerase should be used with caution in patients with a known sulfonamide allergy.

Agenerase is principally metabolized by the liver. Agenerase, when used alone and in combination with low-dose ritonavir, has been associated with elevations of SGOT (AST) and SGPT (ALT) in some patients. Caution should be exercised when administering Agenerase to patients with hepatic impairment (see DOSAGE AND ADMINISTRATION). Appropriate laboratory testing should be conducted prior to initiating therapy with Agenerase and at periodic intervals during treatment.

Formulations of Agenerase provide high daily doses of vitamin E (see Information for Patients, DESCRIPTION, and DOSAGE AND ADMINISTRATION). The effects of long-term, high-dose vitamin E administration in humans is not well characterized and has not been specifically studied in HIV-infected individuals. High vitamin E doses may exacerbate the blood coagulation defect of vitamin K deficiency caused by anticoagulant therapy or malabsorption.

Patients with Hemophilia

There have been reports of spontaneous bleeding in patients with hemophilia A and B treated with protease inhibitors. In some patients, additional factor VIII was required. In many of the reported cases, treatment with protease inhibitors was continued or restarted. A causal relationship between protease inhibitor therapy and these episodes has not been established.

Immune Reconstitution Syndrome: Immune reconstitution syndrome has been reported in patients treated with combination antiretroviral therapy, including Agenerase. During the initial phase of combination antiretroviral treatment, patients whose immune system responds may develop an inflammatory response to indolent or residual opportunistic infections (such as Mycobacterium avium infection, cytomegalovirus, Pneumocystis jirovecii pneumonia [PCP], or tuberculosis), which may necessitate further evaluation and treatment.

Fat Redistribution

Redistribution/accumulation of body fat, including central obesity, dorsocervical fat enlargement (buffalo hump), peripheral wasting, facial wasting, breast enlargement, and “cushingoid appearance,” have been observed in patients receiving antiretroviral therapy. The mechanism and long-term consequences of these events are currently unknown. A causal relationship has not been established.

Lipid Elevations

Treatment with Agenerase alone or in combination with ritonavir has resulted in increases in the concentration of total cholesterol and triglycerides. Triglyceride and cholesterol testing should be performed prior to initiation of therapy with Agenerase and at periodic intervals during treatment. Lipid disorders should be managed as clinically appropriate. See PRECAUTIONS Table 8: Established and Other Potentially Significant Drug Interactions for additional information on potential drug interactions with Agenerase and HMG-CoA reductase inhibitors.

Resistance/Cross-Resistance

Because the potential for HIV cross-resistance among protease inhibitors has not been fully explored, it is unknown what effect amprenavir therapy will have on the activity of subsequently administered protease inhibitors. It is also unknown what effect previous treatment with other protease inhibitors will have on the activity of amprenavir (see MICROBIOLOGY).

Information for Patients

A statement to patients and healthcare providers is included on the product’s bottle label: ALERT: Find out about medicines that should NOT be taken with Agenerase. A Patient Package Insert (PPI) for Agenerase Capsules is available for patient information.

Patients treated with Agenerase Capsules should be cautioned against switching to Agenerase Oral Solution because of the increased risk of adverse events from the large amount of propylene glycol in Agenerase Oral Solution. Please see the complete prescribing information for Agenerase Oral Solution for full information.

Patients should be informed that Agenerase is not a cure for HIV infection and that they may continue to develop opportunistic infections and other complications associated with HIV disease. The long-term effects of Agenerase (amprenavir) are unknown at this time. Patients should be told that there are currently no data demonstrating that therapy with Agenerase can reduce the risk of transmitting HIV to others through sexual contact.

Patients should remain under the care of a physician while using Agenerase. Patients should be advised to take Agenerase every day as prescribed. Agenerase must always be used in combination with other antiretroviral drugs. Patients should not alter the dose or discontinue therapy without consulting their physician. If a dose is missed, patients should take the dose as soon as possible and then return to their normal schedule. However, if a dose is skipped, the patient should not double the next dose.

Patients should inform their doctor if they have a sulfa allergy. The potential for cross-sensitivity between drugs in the sulfonamide class and amprenavir is unknown.

Agenerase may interact with many drugs; therefore, patients should be advised to report to their doctor the use of any other prescription or nonprescription medication or herbal products, particularly St. John’s wort.

Patients taking antacids (or the buffered formulation of didanosine) should take Agenerase at least 1 hour before or after antacid (or the buffered formulation of didanosine) use.

Patients receiving sildenafil should be advised that they may be at an increased risk of sildenafil-associated adverse events, including hypotension, visual changes, and priapism, and should promptly report any symptoms to their doctor.

Patients taking Agenerase should be instructed not to use hormonal contraceptives because some birth control pills (those containing ethinyl estradiol/norethindrone) have been found to decrease the concentration of amprenavir. Therefore, patients receiving hormonal contraceptives should be instructed to use alternate contraceptive measures during therapy with Agenerase.

High-fat meals may decrease the absorption of Agenerase and should be avoided. Agenerase may be taken with meals of normal fat content.

Patients should be informed that redistributionor accumulation of body fat may occur in patients receiving antiretroviral therapy and that the cause and long-term health effects of these conditions are not known at this time.

Adult and pediatric patients should be advised not to take supplemental vitamin E since the vitamin E content of Agenerase Capsules and Oral Solution exceeds the Reference Daily Intake (adults 30 IU, pediatrics approximately 10 IU).

Laboratory Tests

The combination of Agenerase and low-dose ritonavir has been associated with elevations of cholesterol and triglycerides, SGOT (AST), and SGPT (ALT) in some patients. Appropriate laboratory testing should be considered prior to initiating combination therapy with Agenerase and ritonavir and at periodic intervals or if any clinical signs or symptoms of hyperlipidemia or elevated liver function tests occur during therapy. For comprehensive information concerning laboratory test alterations associated with ritonavir, physicians should refer to the complete prescribing information for NORVIR® (ritonavir).

Drug Interactions

See also CONTRAINDICATIONS, WARNINGS, and CLINICAL PHARMACOLOGY: Drug Interactions.

Agenerase is an inhibitor of cytochrome P450 3A4 metabolism and therefore should not be administered concurrently with medications with narrow therapeutic windows that are substrates of CYP3A4. There are other agents that may result in serious and/or life-threatening drug interactions (see CONTRAINDICATIONS and WARNINGS).

Table 7. Drugs That Should Not Be Coadministered With Agenerase

Drug Class/Drug Name

Clinical Comment

Antimycobacterials:

Rifampin*

May lead to loss of virologic response and possible resistance to Agenerase or to the class of protease inhibitors.

Ergot derivatives: Dihydroergotamine, ergonovine, ergotamine, methylergonovine

CONTRAINDICATED due to potential for serious and/or life-threatening reactions such as acute ergot toxicity characterized by peripheral vasospasm and ischemia of the extremities and other tissues.

GI motility agents:

Cisapride

CONTRAINDICATED due topotential for serious and/or life-threatening reactions such as cardiac arrhythmias.

Herbal products:

St. John’s wort (hypericum perforatum)

May lead to loss of virologic response and possible resistance to Agenerase or to the class of protease inhibitors.

HMG Co-reductase inhibitors:

Lovastatin, simvastatin

Potential for serious reactions such as risk of myopathy including rhabdomyolysis.

Neuroleptic:

Pimozide

CONTRAINDICATED due to potential for serious and/or life-threatening reactions such as cardiac arrhythmias.

Non-nucleoside reverse transcriptase inhibitor:

Delavirdine*

May lead to loss of virologic response and possible resistance to delavirdine.

Oral contraceptives:

Ethinyl estradiol/norethindrone

May lead to loss of virologic response and possible resistance to Agenerase. Alternative methods of non-hormonal contraception are recommended.

Sedative/hypnotics:

Midazolam, triazolam

CONTRAINDICATED due to potential for serious and/or life-threatening reactions such as prolonged or increased sedation or respiratory depression.

*See CLINICAL PHARMACOLOGY for magnitude of interaction, Tables 3 and 4.

Table 8. Established and Other Potentially Significant Drug Interactions: Alteration in Dose or Regimen May Be Recommended Based on Drug Interaction Studies or Predicted Interaction

Concomitant Drug Class: Drug Name

Effect on Concentration of Amprenavir or Concomitant Drug

Clinical Comment

HIV-Antiviral Agents

Non-nucleoside reverse transcriptase inhibitors:

Efavirenz, nevirapine

↓Amprenavir

Appropriate doses of the combinations with respect to safety and efficacy have not been established.

Nucleoside reverse transcriptase inhibitor: Didanosine (buffered formulation only)

↓Amprenavir

Take Agenerase at least 1 hour before or after the buffered formulation of didanosine.

HIV protease inhibitors:

Indinavir*, lopinavir/ritonavir, nelfinavir*

↑Amprenavir

Amprenavir’s effect on other protease inhibitors is not well established.

Appropriate doses of the combinations with respect to safety and efficacy have not been established.

HIV protease inhibitor:

Ritonavir*

↑Amprenavir

The dose of amprenavir should be reduced when used in combination with ritonavir (see Dosage and Administration). Also, see the full prescribing information for NORVIR for additional drug interaction information.

HIV protease inhibitor:

Saquinavir*

↓Amprenavir

Amprenavir’s effect on saquinavir is not well established.

Appropriate doses of the combination with respect to safety and efficacy have not been established.

Other Agents

Antacids

↓Amprenavir

Take Agenerase at least 1 hour before or after antacids.

Antiarrhythmics:

Amiodarone, lidocaine (systemic), and quinidine

↑Antiarrhythmics

Caution is warranted and therapeutic concentration monitoring is recommended for antiarrhythmics when coadministered with Agenerase, if available.

Antiarrhythmic:

Bepridil

↑Bepridil

Use with caution. Increased bepridil exposure may be associated with life-threatening reactions such as cardiac arrhythmias.

Anticoagulant:

Warfarin

Concentrations of warfarin may be affected. It is recommended that INR (international normalized ratio) be monitored.

Anticonvulsants:

Carbamazepine, phenobarbital, phenytoin

↓Amprenavir

Use with caution. Agenerase may be less effective due to decreased amprenavir plasma concentrations in patients taking these agents concomitantly.

Antidepressant:

Trazodone

↑Trazodone

Concomitant use of trazodone and Agenerase with or without ritonavir may increase plasma concentrations of trazodone. Adverse events of nausea, dizziness, hypotension, and syncope have been observed following coadministration of trazodone and ritonavir. If trazodone is used with a CYP3A4 inhibitor such as Agenerase, the combination should be used with caution and a lower dose of trazodone should be considered.

Antifungals: Ketoconazole, itraconazole

↑Ketoconazole

↑Itraconazole

Increase monitoring for adverse events due to ketoconazole or itraconazole. Dose reduction of ketoconazole or itraconazole may be needed for patients receiving more than 400 mg ketoconazole or itraconazole per day.

Antimycobacterial:

Rifabutin*

↑Rifabutin and rifabutin metabolite

A dosage reduction of rifabutin to at least half the recommended dose is required when Agenerase and rifabutin are coadministered.* A complete blood count should be performed weekly and as clinically indicated in order to monitor for neutropenia in patients receiving amprenavir and rifabutin.

Benzodiazepines: Alprazolam, clorazepate, diazepam, flurazepam

↑Benzodiazepines

Clinical significance is unknown; however, a decrease in benzodiazepine dose may be needed.

Calcium channel blockers:

Diltiazem, felodipine, nifedipine, nicardipine, nimodipine, verapamil, amlodipine, nisoldipine, isradipine

↑Calcium channel blockers

Caution is warranted and clinical monitoring of patients is recommended.

Corticosteroid: Dexamethasone

↓Amprenavir

Use with caution. Agenerase may be less effective due to decreased amprenavir plasma concentrations in patients taking these agents concomitantly.

Erectile dysfunction agent:

Sildenafil

↑Sildenafil

Use with caution at reduced doses of 25 mg every 48 hours with increased monitoring for adverse events.

HMG-CoA reductase inhibitors:

Atorvastatin

↑Atorvastatin

Use lowest possible dose of atorvastatin with careful monitoring or consider other HMG-CoA reductase inhibitors such as pravastatin or fluvastatin in combination with Agenerase.

Immunosuppressants:

Cyclosporine, tacrolimus, rapamycin

↑Immunosup-pressants

Therapeutic concentration monitoring is recommended for immunosuppressant agents when coadministered with Agenerase.

Inhaled/nasal steroid:

Fluticasone

Agenerase

↑Fluticasone

Agenerase/

Ritonavir

↑Fluticasone

Concomitant use of fluticasone propionate and Agenerase (without ritonavir) may increase plasma concentrations of fluticasone propionate. Use with caution. Consider alternatives to fluticasone propionate, particularly for long-term use.

Concomitant use of fluticasone propionate and Agenerase/ritonavir may increase plasma concentrations of fluticasone propionate, resulting in significantly reduced serum cortisol concentrations. Coadministration of fluticasone propionate and Agenerase/ritonavir is not recommended unless the potential benefit to the patient outweighs the risk of systemic corticosteroid side effects (see WARNINGS).

Narcotic analgesics:

Methadone*

↓Amprenavir

↓Methadone

Agenerase may be less effective due to decreased amprenavir plasma concentrations in patients taking these agents concomitantly. Alternative antiretroviral therapy should be considered.

Dosage of methadone may need to be increased when coadministered with Agenerase.

Tricyclic antidepressants:

Amitriptyline, imipramine

↑Tricyclics

Therapeutic concentration monitoring is recommended for tricyclic antidepressants when coadministered with Agenerase.

*See CLINICAL PHARMACOLOGY for magnitude of interaction, Tables 3 and 4.

Carcinogenesis and Mutagenesis

Amprenavir was evaluated for carcinogenic potential by oral gavage administration to mice and rats for up to 104 weeks. Daily doses of 50, 275 to 300, and 500 to 600 mg/kg/day were administered to mice and doses of 50, 190, and 750 mg/kg/day were administered to rats. Results showed an increase in the incidence of benign hepatocellular adenomas and an increase in the combined incidence of hepatocellular adenomas plus carcinoma in males of both species at the highest doses tested. Female mice and rats were not affected. These observations were made at systemic exposures equivalent to approximately 2 times (mice) and 4 times (rats) the human exposure (based on AUC0-24 hr measurement) at the recommended dose of 1,200 mg twice daily. Administration of amprenavir did not cause a statistically significant increase in the incidence of any other benign or malignant neoplasm in mice or rats. It is not known how predictive the results of rodent carcinogenicity studies may be for humans. However, amprenavir was not mutagenic or genotoxic in a battery of in vitro and in vivo assays including bacterial reverse mutation (Ames), mouse lymphoma, rat micronucleus, and chromosome aberrations in human lymphocytes.

Fertility

: The effects of amprenavir on fertility and general reproductive performance were investigated in male rats (treated for 28 days before mating at doses producing up to twice the expected clinical exposure based on AUC comparisons) and female rats (treated for 15 days before mating through day 17 of gestation at doses producing up to 2 times the expected clinical exposure). Amprenavir did not impair mating or fertility of male or female rats and did not affect the development and maturation of sperm from treated rats. The reproductive performance of the F1 generation born to female rats given amprenavir was not different from control animals.

Pregnancy and Reproduction

Pregnancy Category C. Embryo/fetal development studies were conducted in rats (dosed from 15 days before pairing to day 17 of gestation) and rabbits (dosed from day 8 to day 20 of gestation). In pregnant rabbits, amprenavir administration was associated with abortions and an increased incidence of 3 minor skeletal variations resulting from deficient ossification of the femur, humerus trochlea, and humerus. Systemic exposure at the highest tested dose was approximately one twentieth of the exposure seen at the recommended human dose. In rat fetuses, thymic elongation and incomplete ossification of bones were attributed to amprenavir. Both findings were seen at systemic exposures that were one half of that associated with the recommended human dose.

Pre- and post-natal developmental studies were performed in rats dosed from day 7 of gestation to day 22 of lactation. Reduced body weights (10% to 20%) were observed in the offspring. The systemic exposure associated with this finding was approximately twice the exposure in humans following administration of the recommended human dose. The subsequent development of these offspring, including fertility and reproductive performance, was not affected by the maternal administration of amprenavir.

There are no adequate and well-controlled studies in pregnant women. Agenerase should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.

Agenerase Oral Solution is contraindicated during pregnancy due to the potential risk of toxicity to the fetus from the high propylene glycol content.

Antiretroviral Pregnancy Registry

To monitor maternal-fetal outcomes of pregnant women exposed to Agenerase, an Antiretroviral Pregnancy Registry has been established. Physicians are encouraged to register patients by calling 1-800-258-4263.

Nursing Mothers

The Centers for Disease Control and Prevention recommend that HIV-infected mothers not breastfeed their infants to avoid risking postnatal transmission of HIV. Although it is not known if amprenavir is excreted in human milk, amprenavir is secreted into the milk of lactating rats. Because of both the potential for HIV transmission and the potential for serious adverse reactions in nursing infants, mothers should be instructed not to breastfeed if they are receiving Agenerase.

Pediatric Use

Two hundred fifty-one patients aged 4 and above have received amprenavir as single or multiple doses in studies. An adverse event profile similar to that seen in adults was seen in pediatric patients.

Agenerase Capsules have not been evaluated in pediatric patients below the age of 4 years (see CLINICAL PHARMACOLOGY and DOSAGE AND ADMINISTRATION).

Agenerase Oral Solution is contraindicated in infants and children below the age of 4 years due to the potential risk of toxicity from the large amount of the excipient, propylene glycol. Please see the complete prescribing informationfor Agenerase Oral Solution for full information.

Geriatric Use

Clinical studies of Agenerase did not include sufficient numbers of patients aged 65 and over to determine whether they respond differently from younger adults. In general, dose selection for an elderly patient should be cautious, reflecting the greater frequency of decreased hepatic, renal, or cardiac function, and of concomitant disease or other drug therapy.

Patient information

Agenerase® (amprenavir) Capsules

ALERT: Find out about medicines that should not be taken with Agenerase. Read the section:“What important information should I know about taking Agenerase with other medicines?”

Read this information carefully before you start taking Agenerase (ah-GEN-er-ase). Read the information each time you get more medicine. There may be new information. This information does not take the place of talks with your healthcare provider when you start this medicine and at checkups.

What is the most important information I should know about Agenerase?

Agenerase can cause serious and life-threatening side effects if you take it with certain other medicines. For information about these medicines, see the section “What important information should I know about taking Agenerase with other medicines?”

What is Agenerase?

Agenerase is a medicine you take by mouth to treat HIV infection. HIV is the virus that causes AIDS (acquired immune deficiency syndrome.) Agenerase belongs to a class of anti-HIV medicines called protease inhibitors.

Agenerase is used only in combination with other anti-HIV medicines. When used in combination therapy, Agenerase may help lower the amount of HIV found in your blood, raise CD4 (T) cell counts, and keep your immune system as healthy as possible, so it can help fight infection. However, Agenerase does not have these effects in all patients.

Agenerase does not cure HIV infection or AIDS. We do not know if Agenerase will help you live longer or have fewer of the medical problems (opportunistic infections) that people get with HIV or AIDS. Therefore, be sure to see your healthcare provider regularly. The long-term effects of Agenerase are not known.

Agenerase has not been shown to reduce the risk of passing HIV to others through sexual contact or blood. Continue to practice safe sex and do not use or share dirty needles.

Children from 4 to 12 years of age can take Agenerase. Your healthcare provider will tell you if the oral solution (liquid) or capsule is best for your child. Your child’s healthcare provider will decide the right dose based on your child’s weight and age.

Agenerase has not been studied in people who have taken anti-HIV medicine combinations before that included a protease inhibitor.

Who should not take Agenerase?

Do not take Agenerase Capsules if

  • you are taking certain medicines. Read the section entitled“What important information
  • should I know about taking Agenerase with other medicines?”
  • you have had an allergic reaction to Agenerase or any of its ingredients.

Children younger than age 4 should not take Agenerase Capsules or Agenerase Oral Solution.

Tell your healthcare provider if

  • you are pregnant, Agenerase Capsules may not be right for you.
  • you are breastfeeding. Your baby can get HIV from your milk. Also, Agenerase can pass through your milk and harm the baby.

Tell your healthcare provider about all your medical conditions. Agenerase may not be right for you, or you may need a dosage change in Agenerase. Be sure to tell your healthcare provider if you

  • have liver or kidney problems.
  • have hemophilia.
  • are allergic to sulfa medicines. Agenerase may cause problems for you.

What important information should I know about taking Agenerase with other medicines?

Tell your healthcare provider about all the medicines you take, including prescription and non-prescription medicines, vitamins, and supplements. Some of them may cause dangerous and life-threatening side effects if you take them during treatment with Agenerase. For other medicines, you may need to change your dose to avoid problems.

  • If you are on methadone therapy, talk to your doctor about possible interactions.

Do NOT take the following medicines* with Agenerase. You could develop serious or life-threatening problems.

  • HALCION® (triazolam; used for insomnia)
  • CAFERGOT® and other ergot medicines (used for migraine headaches)
  • PROPULSID® (cisapride, used for certain stomach problems)
  • VERSED® (midazolam; used for sedation)
  • ORAP® (pimozide; used for Tourette’s disorder)

You will need to be monitored with regular blood tests if you take the following medicines* with Agenerase.

  • CORDARONE® (amiodarone; used for certain abnormal heart rhythms)
  • Quinidine (used for certain abnormal heart rhythms)
  • COUMADIN® (warfarin; used for blood thinning)
  • Lidocaine (used for certain abnormal heart rhythms)
  • ELAVIL® (amitriptyline), TOFRANIL® (imipramine) (tricyclic antidepressants)
  • SANDIMMUNE® or NEORAL® (cyclosporine), PROGRAF® (tacrolimus), RAPAMUNE® (rapamycin or sirolimus) (immunosuppressants)

You will need to have your dose adjusted if you take the following medicines* with Agenerase.

  • MYCOBUTIN® (rifabutin; used to prevent Mycobacterium avium complex [MAC])
  • NORVIR® (ritonavir; used to treat HIV infection)
  • VIAGRA® (sildenafil; used for impotence). You may get increased side effects such as low blood pressure, changes in vision, or erections that last more than 4 hours. If an erection lasts more than 4 hours, get medical help right away.

The following medicines* may cause serious problems if you take them with Agenerase. Tell your healthcare provider if you are taking any of these medicines.

  • RESCRIPTOR® (delavirdine; used for HIV) and certain other anti-HIV medicines
  • St. John’s wort (hypericum perforatum) or products containing St. John’s wort
  • VASCOR® (bepridil; used for chronic stable angina)
  • RIFADIN®, RIFAMATE®, RIFATER®, or RIMACTANE® (rifampin, used for tuberculosis)
  • MEVACOR® (lovastatin), ZOCOR® (simvastatin), and LIPITOR® (atorvastatin)
  • (cholesterol-lowering medicines)
  • Phenobarbital (used for seizures)
  • TEGRETOL®, CARBATROL® (carbamazepine; used for seizures and trigeminal neuralgia)
  • DILANTIN® (phenytoin; used for seizures)
  • DECADRON®(dexamethasone, used to reduce inflammation)
  • Hormonal contraceptives (e.g., birth control pills) because the effectiveness of one or both
  • drugs may be decreased. Talk to your doctor about choosing a different type of contraceptive.
  • Vitamin E. Agenerase contains high daily doses of vitamin E that could interfere with
  • medicines that help you stop bleeding.

This list is not complete. Be sure to tell your healthcare provider about all the medicines you take.

How should I take Agenerase?

  • Take Agenerase Capsules every day exactly as your healthcare provider has prescribed it, so it will be as effective as possible. Your healthcare provider will decide the right dose for you.
  • If you miss a dose by more than 4 hours, wait and take the next dose at the regular time.
  • However, if you miss a dose by fewer than 4 hours, take your missed dose right away. Then take your next dose at the regular time.
  • Do not take more or less than your prescribed dose of Agenerase Capsules at any one time. Do not change your dose or stop taking Agenerase without talking with your healthcareprovider.
  • You can take Agenerase Capsules with or without food. However, do not take Agenerase with a high-fat meal. This could reduce the effectiveness of the medicine.
  • If you take Agenerase with the buffered form of VIDEX® (didanosine, ddI), take them at least 1 hour apart.
  • If you take Agenerase Capsules with antacids, take them at least 1 hour apart.
  • When your supply of Agenerase or other anti-HIV medicine starts to run low, arrange to get more from your healthcare provider or pharmacy. The amount of virus in your blood may increase if one or more of the drugs are stopped, even for a short time.
  • Stay under the care of a healthcare provider while using Agenerase.

What should I avoid while taking Agenerase?

Do not

  • switch from Agenerase Capsules to Agenerase Oral Solution without talking toyour healthcare provider. You may get increased side effects if you switch.
  • take vitamin E while taking Agenerase. It contains large amounts of vitamin E.
  • take Agenerase with a high-fat meal. It could reduce the effectiveness of the medicine.

What are the possible side effects of Agenerase?

Agenerase can cause a severe or life-threatening rash. Call your healthcare provider right away if you have a rash. Your healthcare provider will advise you whether your symptoms can be managed on therapy or whether Agenerase should be stopped.

Common side effects of Agenerase are nausea, vomiting, diarrhea, rash, and a tingling feeling, especially around the mouth, and change in taste. These are usually mild to moderate. Depression and mood problems have also been reported in patients taking Agenerase.

Changes in body fat have been seen in some patients taking antiretroviral therapy. These changes may include increased amount of fat in the upper back and neck (“buffalo hump”), breast, 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.

Other side effects include high blood sugar or diabetes, diabetes complications, high cholesterol, or high triglycerides.

This list of side effects is not complete. Your healthcare provider or pharmacist can give you a more complete list of possible side effects. Talk with your healthcare provider about any concerns about the way you are feeling while you are taking Agenerase.

How should I store Agenerase Capsules?

Agenerase Capsules should be stored at room temperature and should not be refrigerated.

General advice about prescription medicines

Medicines are sometimes prescribed for conditions that are not mentioned in patient information leaflets. Do not use Agenerase for a condition for which it was not prescribed. Do not give Agenerase to other people, even if they have the same symptoms you have. It may harm them.

This leaflet summarizes the most important information about Agenerase. If you would like more information, talk with your doctor. You can ask your pharmacist or doctor for information about Agenerase that is written for health professionals.

Agenerase is a registered trademark of GlaxoSmithKline.

*The brands listed are trademarks of their respective owners and are not trademarks of GlaxoSmithKline. The makers of these brands are not affiliated with and do not endorse GlaxoSmithKline or its products.

Licensed from

GlaxoSmithKline Vertex Pharmaceuticals Incorporated

Research Triangle Park, NC 27709 Cambridge, MA 02139

©2005, GlaxoSmithKline. All rights reserved.

May 2005 RL-2194

Agenerase 
amprenavir capsule
Product Information
Product Type HUMAN PRESCRIPTION DRUG LABEL Item Code (Source) NDC:0173-0679
Route of Administration ORAL DEA Schedule     
Active Ingredient/Active Moiety
Ingredient Name Basis of Strength Strength
amprenavir (amprenavir) amprenavir 50 mg
Inactive Ingredients
Ingredient Name Strength
d-alpha tocopheryl polyethylene glycol 1000 succinate (TPGS)  
polyethylene glycol 400 246.7 mg  in 1 
propylene glycol 19 mg  in 1 
gelatin  
glycerin  
titanium dioxide  
edible red ink  
d-sorbitol and sorbitans solution  
vitamin E in form of TPGS 36.3   in 1 
Product Characteristics
Color WHITE (opaque, off-white to cream-colored) Score no score
Shape CAPSULE (oblong) Size 19mm
Flavor Imprint Code GX;CC1
Contains     
Coating false Symbol false
Packaging
# Item Code Package Description
1 NDC:0173-0679-00 480 CAPSULE (480 CAPSULE) in 1 BOTTLE
Labeler - GlaxoSmithKline
Revised: 06/2006   GlaxoSmithKline
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