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Intelence - etravirine

General Information This drug is almost always used as one component of a multidrug combination to suppress the human immunodeficiency (HIV) viral load.  It is also potentially useful to prevent mothers from transmitting HIV to their babies at or around the time of birth.
Specifics Etravirine has been used for several years to treat HIV.  According to many experts, etravirine may be as potent as a protease inhibitor.  It acts by preventing the formation of HIV genetic material.  It is classified as a nonnucleoside reverse transcriptase inhibitor (NNRTI) or "non-nuke."
Dosing Generally etravirine is taken as 200 mg twice a day with food.  The tablets may also be dispersed in water to produce a tasteless solution.
(this refers to your willingness, ability, and actual performance in taking your medications)

For further information and tips on adherence, go to the Adherence section of this site.

As with any antiviral drug or antibiotic, try not to ever miss a dose.  If you miss a dose and notice that you have done so within a few hours of its scheduled time, you may take the dose as usual and take the next dose at its regular time. 

It is very important that you NOT stop this medicine suddenly without substituting other medications first.  If you you do no substitute other medications for a couple of weeks, your virus might develop resistance to etravirine and the entire class of non-nukes.  Your provider can help you with this process.

If you miss more than one dose, look at the reasons why you missed them and come up with a plan to avoid it in the future.  For example, if you fell asleep too early, take the medicine earlier in the evening, with your later meal, set an alarm, or have someone appointed to wake you up for your medicine.  

It is strongly recommended that you consider using weekly pill boxes and arrange all of your doses a week in advance.  Buy a small pill box so that you can carry a dose or two of your medicines with you in case you are away from home.

Possible Side Effects
The package insert for most drugs including etravirineis often overwhelming and scary with perhaps an overemphasis on side effects.  We have summarized the important and more common problems here.

Most people take etravirine without many side effects. 

Possible side effects include rash (roughly 1 of 20 people that take the drug), nausea, headache, muscle aches, or liver problems.  Usually you will have blood tests done in the first month to look for the beneficial effects of etravirine and any side effects. 

Many minor side effects will either stay constant or get better with time.  It is mainly the side effects that are severe or get worse that may cause significant health risks for you.

The rash that develops in some people that take etravirine may be anything from mild to very severe like a burn on the entire body.  Most mild rashes will stay mild or even go away.  The rashes of major concern are the ones that get worse and worse, the ones associated with fever, or the ones that are severe.  Notify your provider promptly for any rash.  Do not stop the medication unless instructed to do so by a healthcare provider familiar with etravirine usage.

Etravirine can also cause inflammation of the liver which is called hepatitis.  Mild hepatitis does not cause symptoms but it can be seen on liver blood tests.  Worse hepatitis causes loss of appetite, nausea and vomiting, possibly turning the skin and eyes yellow (jaundice), dark (cola-colored) urine, and light colored stools.  You should notify your healthcare provider promptly if you have any of these symptoms so that you can get liver tests done.

All drugs of this type can cause or contribute to abnormal fat redistribution characterized by thinning of the face, arms, or legs.  In most cases this would be also accompanied by elevated cholesterol levels, elevated triglyceride levels, and perhaps a tendency to develop diabetes.  Etravirine has less of a tendency to cause these problems than perhaps the nukes (NRTIs) or protease inhibitors.

This refers to the way that etravirine affects other medications and how other drugs affect etravirine in the bloodstream.
Certain drugs should not be used with etravirine:

Antibiotics: clarithromycin (Biaxin)
Oral contraceptive pills
Antifungal drug: ketoconazole (Nizoral)
Antimycobacterial drug: rifampin
Herbal drug: St John's wort
Protease inhibitors other than darunavir (Intelence)

Certain drugs should be used with caution:

Antifungal drug: fluconazole (Diflucan)
Antimycobacterial drug: rifabutin (Mycobutin)
Drugs for heart rhythm disturbances (antiarrhythmics): amiodarone, disopyramide, lidocaine
Drugs for seizure or epilepsy or convulsions: carbemazepine (Tegretol), clonazepam (Klonipin), ethosuximide
Cancer chemotherapy: cyclophosphamide
Drugs for migraine headaches or ergot alkaloids: ergotamine
Immunosuppressing drugs or drugs used for organ transplants: cyclosporin, tacrolimus, sirolimus
Drugs to increase activity of the stomach: cisapride
Opiate pain meds: fentanyl
Anticlotting drugs: warfarin

etravirine increases the metabolism of certain drugs so that dose adjustments or substitutions may be necessary:

Protease inhibitors: indinavir (Crixivan), lopinavir/ritonavir (Kaletra), nelfinavir (Viracept), saquinavir (Invirase or Fortovase), fosamprenavir (Lexiva)
Narcotic pain reliever: methadone

Report to you healthcare provider or go to an Emergency Room if you have rash, severe side effects, increasing side effects, shortness of breath, uncontrollable diarrhea, fever, weakness, jaundice (eyes and skin turn yellow,) muscle pain, nausea and vomiting so that you cannot hold down your food and liquids.
You can download this handout in PDF format for offline viewing or printing by clicking HERE.