Viracept

Common Name: nelfinavir

Brand Name: Viracept

Class: HIV protease inhibitor (PI)

Standard dose: 1,250 mg taken as either two 625 mg tablets or five 250 mg tablets twice daily with food. Take missed dose as soon as possible, unless it is almost time for your next dose. Do not double up on your next dose. Viracept Oral Powder also available for children and individuals unable to swallow tablets.

AWP: $796.99 / month for 250 and 625 mg tablets

Manufacturer contact: ViiV Healthcare, 1 (877) 844-8872

Potential side effects and toxicity: Most common include diarrhea (15-20% of patients), stomach discomfort, nausea, gas, weakness, and rash. People with phenylketonuria should be aware that the powder contains phenylalanine. As seen with other protease inhibitors (except unboosted Reyataz), there can be increased levels of cholesterol and triglycerides which may be associated with an increased risk of heart disease. Other possible side effects seen with protease inhibitors are lipodystrophy (body fat changes, including thinning of the face, arms and legs, with or without fat accumulation in the stomach, breasts, and upper back), onset of new cases or worsening of diabetes (see your doctor promptly), and increased bleeding in hemophiliacs. Immune Reconstitution Inflammatory Syndrome (IRIS) may occur as the immune system regains strength; signs and symptoms of inflammation from previous infections may occur soon after anti-HIV treatment is initiated. Report symptoms of illness, such as shingles and TB, to a health care provider.

Potential drug interactions: Viracept increases levels of Invirase and Crixivan (see Crixivan for potential drug interactions), so dose adjustments may be needed. Do not take with Versed (midazolam), Cordarone (amiodarone), Halcion (triazolam), Rifadin (rifampin), Prilosec-OTC (omeprazole), ergot derivatives (such as Cafergot, D.H.E. 45, Methergine, Wigraine), garlic supplements, or the herb St. John's wort. Do not use Advicor, Altoprev, Mevacor (lovastatin), Simcor, Vytorin, or Zocor (simvastatin) for the treatment of high lipids. Lipid-lowering alternatives are Crestor, Lescol, Lipitor, and Pravacol (pravastatin), but should be used with caution. Viracept may decrease methadone levels but withdrawal rarely occurs; methadone doses may need to be increased. Use calcium channel blockers with caution.

Blood levels of Viracept are reduced by rifampin and may be reduced by phenobarbital, phenytoin, and carbamazepine (Tegretol and others), so it is important to inform your doctor if you are taking any of these medications. Mycobutin (rifabutin) dose must be decreased when used with Viracept. Prescriber may need to adjust doses of any of these drugs accordingly.

Cialis, Levitra, and Viagra levels are increased; doses should not exceed 10 mg Cialis or 2.5 mg Levitra per 72 hours, or 25 mg Viagra per 48 hours.

Increased levels of the inhaled and nasal sprays with fluticasone, a steroid for asthma or allergies (found in Advair, Flonase, and Flovent), can occur and therefore should be used with caution. The effectiveness of birth control pills may be decreased; alternative or additional methods of contraception with barrier should be used. Also, increased levels of trazodone can occur and this combination should be used with caution. A lower dose of trazodone is recommended.

Tips: This is the only protease inhibitor that is never used with Norvir. Do not leave the pharmacy without anti-diarrhea meds such as Immodium, or Tums or other calcium products. Taking a 500 mg calcium supplement with doses hugely decreases diarrhea. Also try Solgar oat bran tablets, psyllium husk fiber bars, and pancreatic enzymes (all with meals). As an extra precaution, take a change of clothes with you everyday for the first several weeks -- stick it out, most often, symptoms improve after two or three weeks. The oral powder tastes horrible and requires a large amount for mixing into food.

People using Viracept can crush adult tablets or dissolve tablets in a small amount of water. Mixing Viracept with acidic food or juice (e.g. orange/apple juice or apple sauce) is not recommended, due to resulting bitter taste. To get the full benefit of Viracept by increasing its level in the body, it must be taken with a meal. Please see package insert for more complete potential side effects and interactions.

Doctor

Viracept (nelfinavir) was approved for use in combination with other antiretroviral drugs in the treatment of HIV infection in 1997. In 2003, the dosage formulation of nelfinavir was simplified to two tablets twice daily. The level of drug in the bloodstream was adequate only when it was taken with food and this was one factor leading to the results of studies showing lower rates of virologic suppression versus other choices that were not as reliant on food to be adequately absorbed. It was initially a very popular drug when first released, as it was better tolerated than the other choices that were available at that time. However, when the boosted PI Kaletra demonstrated a better rate of achieving virologic suppression, there was less enthusiasm in relying on this unboosted PI. Diarrhea is its most prominent problem occurring in many, though not all, who take it. With the availability of other protease inhibitors that have both more reliable efficacy in virologic suppression, plus better tolerability and fewer pills to take, nelfinavir use has signifcantly decreased. -- Cal Cohen, M.D.

Activist

The best thing you can say about Viracept is that it's a good protease inhibitor to fail, as you can still be rescued by another boosted PI. Other than that, given the explosive blue diarrhea, there's little left to recommend this drug anymore. The one exception is for women trying to conceive, as it's one alternative PI recommended to prevent mother-to-child HIV transmission. (Although the aforementioned diarrhea might prove a disincentive to conception, let alone nine months of pregnancy.) -- Jeff Taylor