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Raltegravir

Isentress_pilules.png

Raltegravir is an antiretrovial drug from the relatively new integrase inhibitor class. It is the only integrase inhibitor currently approved for use in Australia and is only available to people who have limited treament options open to them.

Integrase inhibitors target an enzyme called integrase which HIV uses to integrate its genetic code into human cells. Because this is a different point of action to that targeted by other drug classesA group of anti-HIV drugs with the same target of action. Anti-HIV drug classes include nucleoside analogue reverse transcriptase inhibitors, protease inhibitors and non-nucleoside analogue reverse transcriptase inhibitors, as well as several others. Combining drugs from three or more classes is the basis of Highly Active Antiretroviral Therapy (HAART)., there is a good chance that people who have failed several prior treatment regimens will benefit from this drug, especially if it is combined with an optimised background regimen.

Generic name: raltegravir (RAL)
Pronunciation:ral-TEGG-ra-veer
Brand name:Isentress
Also known as:MK-0518 (former code name)
Drug class:integrase inhibitor
Availability in Australia:
  • Available on a restricted authority basis the Pharmaceutical Benefits Scheme (PBS) through S100 prescribers since 2008.
  • This drug may be available through clinical trials in Australia.
  • You may be able to import this drug from overseas for your personal use.

Raltegravir is available on the PBS[Pharmaceutical Benefits Scheme] The federal government program which subsidises medication costs in Australia. Anti-HIV drugs are part of a special part of the PBS called Section 100 (S100) which is used for expensive, highly specialised drugs. only to people who have failed treatment with, or have documented resistanceHIV which has mutated and is less susceptible to the effects of one or more anti-HIV drugs is said to be resistant. to, at least three other antiretroviralA medication or other substance which is active against retroviruses such as HIV. regimens. Your doctor will be able to advise if this restriction applies to you.

Presentation:400mg tablet
What the treatment guidelines say:

Most of the clinical trial evidence for raltegravir comes from trials in people who had taken several other treatment regimens in the past, and so the Australian guidelines do not recommend raltegravir as first-line therapy (in people who have not taken treatments before).

Raltegravir is a recommended option for people who experience antiretroviral treatment failure, especially for people who may have failed several prior regimens or who have few new treatment options remaining.

Links:

Like all anti-HIV drugs, raltegravir must be taken in combination with other drugs to be completely effective. Your doctor will advise you on the right combination of drugs to suit your circumstances.

Dosage

The usual adult dose is one 400mg tablet, taken twice a day.

Regardless of what you read on this website or elsewhere, you should always take your medications according to your doctor's instructions. If you're unsure, speak to your doctor or pharmacist.

With or without food?

Raltegravir may be taken with or without food.

Side effects

All drugs can produce side effects in some people. These may be mild, moderate or severe, so you should be aware of potential side effects before starting any drug, and speak to your doctor if you experience side effects that concern you.

  • Common side effects may include nausea (upset stomach, feeling sick to the stomach), diarrhoea, headache..
  • Less common side effects may include fever, CPK elevation.
  • Rare side effects may include depression, abnormal liver function.
  • It's unlikely you will experience all of these side effects, and you may not experience any side effects at all. Before starting any new drug, ask your doctor about side effects you might experience and discuss strategies for dealing with side effects if they do occur. If you experience any significant side effect you should continue taking your medicine and see your doctor as soon as possible.

Interactions with other drugs

Raltegravir is broken down via a different method than most drugs, and so there are very few serious interactions with other anti-HIV drugs. Some evidence does exist that, when taken with tenofovir and ritonavir, levels of raltegravir in the blood may be reduced. When combined with atazanavir and ritonavir, blood levels of raltegravir may be increased.
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The table below shows all the clinical trials in the database with the keyword raltegravir.

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This Treatments database entry was first published on 3 June 2009.

While the content of this treatments database entry was checked for accuracy at the time of publication, NAPWA recommends checking to determine whether the information is the most up-to-date available, especially when making decisions which may affect your health.

This article may contain medical information. NAPWA makes every reasonable effort to ensure the information on this website is accurate, reliable and up-to-date, including obtaining technical reviews by medically-qualified reviewers, however the authors of information on this website are not qualified to give medical advice, except where explicitly stated.

The content of this website is intended to support, not replace, the relationship between people living with HIV/AIDS and their medical advisers, and is not intended as a substitute for medical advice.

HIV Clinical Trials update