etravirine

ETRAVIRINE

Complete information including dosage, side effects, interactions and pregnancy & breast feeding warnings for patient and professional use

Overview and uses

Etravirine is a medicine used for HIV treatment. It is available only as a prescription medicine. Etravirine is prescribed by a doctor in combination with other medicines for HIV treatment. This is done to increase the therapeutic efficacy of the medicines used in the treatment of HIV. Also, combination therapy reduces the risk of virus getting resistant to any one particular medicine.

Etravirine does not cure HIV, but it slows down the progression of HIV within the body. HIV destroys CD4+ T Lymphocytes – a type of white blood cells (WBC) that gives immunity to the body. In other words, these cells protect the body against the infections or illness caused by various organisms like bacteria, viruses and other germs. Thus, one may conclude that HIV infection, if left untreated, may make the body susceptible to this infections/illness.

Brand names: Intelence.

Pharmacological classification: Nonnuucleoside reverse transcriptase inhibitor anti-retroviral drug

Mechanism of action: Etravirine directly inhibits the HIV reverse transcriptase and terminates the elongation of proviral DNA.

Indication (used for):

  • For the treatment of HIV-1 infections in adults and children with age of 6 years or older, particularly for those patients infected with HIV-1 strains resistant to a nonnucleoside reverse transcriptase inhibitor and other anti-retroviral medicines.

Dosage

Etravirine should be taken after meals as food increases the AUC by 50%.

  • Adult dose:
    • 200 mg twice a day after meals.
  • Pediatric dose (based on body weight) for children with 6 years or more of age:
    • 16 kg or more but less than 20 kg: 100 mg twice a day.
    • 20 kg or more but less than 25 kg: 125 mg twice a day.
    • 25 kg or more but less than 30 kg: 150 mg twice a day.
    • 30 kg or more: 200 mg twice a day.

Dosage form: Etravirine is available as tablets in strength of 25 mg, 50 mg and 100 mg.

Over dosage:

  • No known antidote for Emtricitabine overdose.
  • Overdose of Efavirenz may lead to increased nervous system symptoms.
  • Standard supportive treatment should be applied as and when necessary.
  • Activated charcoal may be used to remove any unabsorbed drug.
  • Efavirenz is highly unlikely to remove by dialysis as it is highly protein bound.
  • Avoid meals that are high in fat.

Unwanted or side effects:

  • Severe skin and hypersensitivity reactions have been reported.
    • Consult your doctor as soon as possible if a rash occurs.
  • Occurrence of life threatening Stevens-Johnson syndrome is rare.
    • Seek medical attention as soon as possible by contacting emergency department of local hospital as this condition is life threatening.
  • Fat redistribution or accumulation of body fat including central obesity, dorsocervical fat enlargement (buffalo hump), peripheral wasting, facial wasting, breast enlargement and “cushingoid appearance” have been observed in patients receiving anti HIV therapy.
  • Immune reconstitution syndrome: during the initial phase of the treatment, patients whose immune systems respond may develop an inflammatory response to opportunistic infections, which may necessitate further evaluation and treatment. Auto immune disorders have also been reported to occur in some people at any time after the initiation of the treatment.

Contraindications of Etravirine:

Pregnancy

Category B, which means that Animal reproduction studies have failed to demonstrate a risk to the fetus and there are no adequate and well-controlled studies in pregnant women.

Nursing mothers:

  • Mothers are advised not to breast feed if they are receiving
  • In general, it is advisable that mothers don’t breast feed their children to avoid post-natal transmission of HIV.

Interactions

Drug – drug interactions:

  • Etravirine can be combined with Darunavir/Ritonavir, Lopinavir/Ritonavir and Saquinavir/Ritonavir without the need of dose adjustments.
  • Etravirine significantly reduces the plasma concentrations of Dolutegravir.
  • Etravirine when co-administered with Nevirapine or Efavirenz significantly reduces the plasma concentrations of Etravirine. Hence, these medicines should not be administered concomitantly.
  • Delavirdine, Nevirapine and Rilpivirine should not be co-administered with Etravirine as these combinations have no beneficial effects.
  • Etravirine should not be co-administered with atazanavir without low-dose ritonavir.
  • Concomitant use of Etravirine with fosamprenavir without low-dose ritonavir may cause a significant alteration in the plasma concentration of amprenavir.
  • Concomitant use of Etravirine with Indinavir without low-dose ritonavir may cause a significant alteration in the plasma concentration of Indinavir.
  • Nelfinavir and Etravirine should not be co-administered without low dose Ritonavir.
  • Etravirine and Ritonavir 600 mg twice daily should not be co-administered.
  • Tipranavir/ Ritonavir should not be co-administered with Etravirine.
  • Dose of Maraviroc should be doubled to 600 mg twice a day when co-administered with Etravirine.
  • Etravirine may increase the concentrations of Digoxin and Warfarin.
  • Etravirine may decrease the concentrations of amiodarone, bepridil, disopyramide, flecainide, lidocaine (systemic), mexiletine, propafenone and quinidine.
  • Voriconazole, Ketoconazole, Posaconazole, Itraconazole and Fluconazole significantly increase the exposure of Etravirine.
  • Etravirine reduces the AUC of larithromycin, Artemether and Lumefantrine and hence should not be co-administered with these medicines.
  • Concomitant use of Etravirine with dexamethasone (systemic) and /or st. john’s wort reduces the activity of Etravirine.
  • Etravirine increases the activity of Diazepam.
  • Etravirine and boceprevir can be used together without any dose adjustments. However, such use is not recommended in presence of any other drug which may further decrease the AUC of Etravirine.
  • Etravirine reduces the concentrations of fluvastatin and pitavastatin whereas decreases the concentrations of atorvastatin, lovastatin and simvastatin.
  • Etravirine may decrease the concentrations of cyclosporine, sirolimus and tacrolimus.
  • Etravirine can be co-administered with buprenorphine, naloxone and methadone without any dose adjustments. However, dose of maintenance therapy may require adjustments in some patients.
  • Alternative to clopidogrel should be considered.
  • The dose of sildenafil may need to be altered based on clinical effect.

Drug – food interactions of Etravirine:

  • Food increases the AUC of Etravirine by 50%.

Important information on anti HIV and anti AIDS medicines

Benefits of taking your anti HIV medicines regularly

  • Sustained viral suppression.
  • Reduced risk of resistance.
  • Reduced risk of treatment failure.
  • Improved quality of life and overall health.
  • Reduced risk of HIV transmission.

Getting the most from your treatment

  • Precisely follow every advice given to you by your doctor and pharmacist regarding your medications. Take your dose regularly without missing out a single one.
  • Make all the necessary changes in your lifestyle and eating/food habits as advised by your doctor and pharmacist. This may include quitting smoking, alcohol, other substances of abuse, taking up exercise and some/many others that your doctor finds it best in your interest.
  • Do not make any changes in your dose unless suggested/recommended by your doctor.
  • Keep your regular appointments with your doctor so that the progress can be monitored. This may involve blood tests and other test that a doctor finds necessary.
  • Consult your doctor if you develop an infection or an allergy after you start the treatment.
  • Consult your doctor if you feel low or even depressed. This is common especially after diagnosis and during the early stages of treatment.
  • Some people who have taken anti HIV medicines for a long period of time may develop Osteonecrosis – a condition where bone tissue dies due to reduced blood supply. This causes joint pain, stiffness and difficulty in movement. Consult your doctor if you if you notice any of this symptoms.
  • If you are going to take any operation/surgery or a dental treatment, tell doctor who is going to carry out operation/surgery or dental procedure about all the medicines that you are taking. If possible, carry your containers with you to the doctor even if it is empty.
  • If you buy any medicines, supplements including your vitamin supplements, herbal medicines or even the medicines that do not require a prescription, check with your pharmacist whether they can be taken along with your anti HIV medicines or not.
  • Treatment of HIV is life-long. Continue taking your anti HIV medicines even if you feel well. This should be done to keep your immune system healthy.

Forgot to take your medicine?

  • Forgetting a dose/frequent missed out doses may lead to viral resistance or treatment failure.
  • If you forget to take a dose, take it immediately as soon as you remember unless it’s almost the time for your next dose.
  • Do not take two doses at the same time to make up for the missed out dose.
  • If you are forgetting/missing your dose frequently or very often, try using pill boxes that are available as weekly or monthly dose boxes. Alternatively, you can also try posting reminder notes on places like doors of refrigerator, wardrobe, bathroom, side tables of your bed, above or below switch boards etc. You can also set a reminder on your cell phone.
  • If possible, ask your family members and friends to remind you of your dose.

Click here to go to Etravirine forums

Etravirine wikipedia page

Note: The sole purpose of every information shared on this article is to bring awareness. Do not use this information as a medical advice or prescription advice or as a tool for the treatment, diagnosis or prevention of the disease.

By |2018-12-29T07:09:03+00:00May 2nd, 2017|medicines|Comments Off on etravirine

About the Author:

B. Pharm (K.L.E. society's S.V.V. Patil College of Pharmacy, Bengaluru) M. Pharm (Maharishi Arvind Institute of Pharmacy, Jaipur)

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