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The Eleventh Annual HIV Drug Guide: Agenerase (Amprenavir, APV)

January/February 2007

 

 


Brand Name: Agenerase

Common Name: amprenavir

Class: HIV protease inhibitor (PI)

Standard Dose: 1200 mg twice daily. The 150 mg soft gelatin capsules were taken off the market because of the new formulation (Lexiva), but the 50 mg capsule and liquid remains available. Take missed dose as soon as possible, but do not double up on your next dose.

Approved for children ages 4 and older. Grape, bubblegum, peppermint flavored liquid available. Adults should not use liquid if possible.

AWP: $40.88 for 8 oz. bottle (approximately one day adult dose)

Manufacturer contact: GlaxoSmithKline,
www.treathiv.com, 1 (888) 825–5249

AIDSInfo: 1 (800) HIV–0440 (448–0440), www.aidsinfo.nih.gov

Potential side effects and toxicity:

Most common include: nausea, vomiting, stomach pain, taste disorders, oral or perioral (around the mouth) paresthesia (tingling sensation), parepheral paresthia (tingling sensation in the hands and feet), mood disorders, diarrhea or loose stools, and rash. Rash occurred in about 22% of people on Agenerase, but severe rashes were uncommon. If you experience a rash, notify your doctor. For mild or moderate rashes, your doctor may choose to continue Agenerase, with close follow-up and monitoring. Because Agenerase is a sulfonamide, it should be used with caution in patients with allergies to sulfa drugs. Serious rash (see Viramune), while rare, can be severe; notify your healthcare provider immediately.

As seen with all other protease inhibitors are increased levels of cholesterol and triglycerides, except possibly unboosted Reyataz (atazanavir) and these increased levels may be associated with heart disease. Other possible side effects are lipodystrophy (body fat changes, including thinning of the face, arms and legs, with or without fat accumulation in the stomach, breasts and sometimes the upper back), onset of new cases or worsening of diabetes (see your doctor promptly) and increased bleeding in hemophiliacs.

Potential drug interactions:

See Lexiva. Not recommended to be taken with Kaletra. When taken with Sustiva, boost with Norvir. Do not take with Versed, Halcion, rifampin, ergot derivatives (such as Cafergot, Wigraine and Methergine, D.H.E. 45, in any form -- serious interactions seen with dilation during gynecological exams), garlic supplements, or the herb St. John's wort. Do not take with Tambocor (flecainide) or Rythmol (propafenone) if using Agenerase with Norvir. Do not use Zocor (simvastatin) or Mevacor (lovastatin); lipid-lowering alternatives are Lipitor (atorvastatin), Lescol, and Pravachol (pravastatin), but they should be used with caution due to potential for liver toxicity. Do not take extra vitamin E.

Rescriptor and Viracept greatly increase Agenerase blood levels (and usually stomach discomfort) and prescriber may need to adjust dose accordingly. Sustiva has been shown to significantly reduce blood levels of Agenerase unless also taken with Norvir.

Other drugs that may be involved in interactions with Agenerase include drugs for your heart (antiarrhythmics, anticoagulants, blood pressure medications, cholesterol medications), drugs for seizures, antibiotics and antifungals, sedatives, steroids, immunosuppresants, drugs for heartburn or acid reflux, oral contraceptives, and antidepressants. If you are taking any of these drugs, be sure to let your doctor and pharmacist know so they can monitor your therapy or make adjustments to your medications.

Protease inhibitors increase blood levels of Viagra (sidenafil citrate), Cialis (tadalafil) and Levitra (vardenafil). Use with caution. Initially the Viagra dose should be 12.5 mg (1/2 of 25 mg tablet) and increased as needed and tolerated. It's recommended that people on PIs do not exceed 25 mg of Viagra in a 48-hour period because of potential for serious reaction. Use Cialis at reduced doses of 10 mg every 72 hours and Levitra at reduced doses of no more than 2.5 mg every 72 hours, with increased monitoring for adverse events.

Tips:

On its way to extinction due to new formulation on the market, fos-amprenavir calcium (Lexiva). If you are on Agenerase, you should talk with your doctor about switching to Lexiva. If you are taking the capsules, do not take additional vitamin E; the capsules already have vitamin E in them.

May also penetrate the lymph nodes, where virus can hide out. Label warning: Agenerase Oral Solution should not be given to infants and children below the age of 4 years and should not be used by pregnant women because of the propylene glycol amount.

Doctor
The use of amprenavir has been supplanted by fosamprenavir with superior pharmcokinetic characteristics. The 150 mg capsule is no longer available. The oral solution contains propylene glycol, which is contraindicated in patients with renal or hepatic failure, young children, pregnant women, and patients taking metronidazole or disulfiram. The oral solution and ritonavir should not be co-administered. Numerous difficult to predict drug interactions with other protease inhibitors further complicate use of amprenavir in patients with multi-drug resistance. -- Keith Henry, MD
Activist
See statement for Lexiva. -- Cathy Olufs


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This article was provided by Positively Aware. It is a part of the publication Positively Aware. Visit Positively Aware's website to find out more about the publication.
 
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