Roche issues warning about use of boosted saquinavir with rifampicin

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Boosted saquinavir should not be taken with the anti-tuberculosis drug rifampicin because of the risks of drug-induced hepatitis, according to a warning issued by saquinavir’s manufacturer, Roche. The drug company is advising anybody taking this protease inhibitor and rifampicin to contact their doctor immediately.

The advice was issued after Roche conducted a study involving 28 HIV-negative volunteers who were provided with 1000mg of saquinavir boosted by 100mg of ritonavir twice daily with the standard 60mg daily dose of rifampicin.

In total 39% of the volunteers developed significant drug-induced hepatitis, and one individual was admitted to hospital with mild liver failure. The study was immediately discontinued, and liver function returned to normal in all the affected individuals.

Glossary

boosting agent

Booster drugs are used to ‘boost’ the effects of protease inhibitors and some other antiretrovirals. Adding a small dose of a booster drug to an antiretroviral makes the liver break down the primary drug more slowly, which means that it stays in the body for longer times or at higher levels. Without the boosting agent, the prescribed dose of the primary drug would be ineffective.

metabolism

The physical and chemical reactions that produce energy for the body. Metabolism also refers to the breakdown of drugs or other substances within the body, which may occur during digestion or elimination.

contraindication

A specific situation or circumstance which means that a drug or medical procedure should not be used because it may be harmful. For example, it may be contraindicated to provide drug A to someone who is already taking drug B.

Roche is advising all patients who are currently taking boosted saquinavir with rifampicin to contact their HIV doctor for immediate advice. However, they do not anticipate that a large number of patients in the UK will be affected.

Unboosted saquinavir and rifampicin are also contraindicated. Rifampicin accelerates the metabolism of unboosted saquinavir leading to sub-therapeutic blood levels of the protease inhibitor.