Sustiva, Stocrin (efavirenz) - HIV Drug Information

Photograph courtesy Bristol-Myers Squibb

Classification:

Sustiva (efavirenz) is an antiretroviral drug used in the treatment of HIV in both adults and children.

Sustiva is classified as a non-nucleoside reverse transcriptase inhibitor (NNRTI) and is also a component of the fixed dose combination drug Atripla (tenofovir + emtricitabine + efavirenz) commonly used as in first-line therapy in the U.S.

Sustiva was approved for use by the U.S. Food and Drug Administration (FDA) on September 21, 1998.

In Europe and many other parts of the world, the drug is marketed under a different trade name, Stocrin.

Drug Formulations:

Sustiva is available in a 600mg tablet. The yellow, oblong tablet is film coated and printed wit number "SUSTIVA" on both sides.

Sustiva is also available in 200mg and 50mg capsule form. The 200mg capsules are gold in color, printed with "SUSTIVA" on the body of the capsule and "200 mg" on the cap. The 50mg capsules have a gold cap printed with "SUSTIVA" and a white body printed with "t0 mg."

Sustiva must never be used as monotherapy but rather in combination with other appropriate antiretroviral drugs.

Dosages:

For adults, take one 600mg tablet once daily, ideally before bedtime and on an empty stomach. Addtionally:

  • If coadministered with rifampin (used frequently in the treatment of tuberculosis coinfection), increase the dosage to 800mg once daily for patients weighing over 110 lbs (50kg).
     

For children of at least three years of age and over 7.7 lbs (35kg), prescribe as follows:

  • 7.7 lbs (3.5kg) to less than 11 lbs (5kg): 100mg
  • 11 lbs (5kg) to less than 16.5 lbs (7.5kg): 150mg
  • 16.5 lbs (7.5kg) to less than 33 lbs (15kg): 200mg
  • 33 lbs (15kg) to less than 44 lbs (20kg): 250mg
  • 44 lbs (20kg) to less than 55 lbs (25kg): 300mg
  • 55 lbs (25kg) to less than 71.6 lbs (32.5kg): 350mg
  • 71.6 lbs (32.5kg) to less than 88lbs (40kg): 400mg
  • 88 lbs (40kg) and over: 600mg

Sustiva capsules can be swallowed whole or as sprinkles. Sustiva in tablet form, on the other hand, should never be crushed as this can caused inadequate dosing (or potential overdosing) in children.

Common Side Effects:

The most common side effects associated with Sustiva use (in 10% of cases or less) are:

  • Rash
  • Nausea
  • Dizziness
  • Headache
  • Fatigue
  • Insomnia
  • Vomiting
  • Impaired concentration
  • Upset stomach
  • Abnormal, vivid dreams
  • Diarrhea
  • Depression
  • Nervousness/anxiety

Most of the symptoms are generally short-lasting, often resolving themselves within several weeks to a month. Some the central nervous systems effects (dizziness, impaired concentration) can be mitigated by taking Sustiva just before bedtime.

Sustiva-Associated Skin Rashes

In controlled clinical studies, 26% of patients newly exposed to Sustiva experienced some degree of skin rash, although most were mild to moderate in severity and usually appeared within the first two weeks of initiation.

If you develop a rash soon after starting Sustiva, contact your doctor or healthcare provider. In a rare instances (less than 1% of cases), the rash may be severe, presenting with fever and blisters, indicative of a potentially deadly all-body inflammation called Stevens-Johnson syndrome, which requires not only termination of therapy but immediate medical attention.

In all other cases, the rash will most often resolve itself without having to stop treatment.  

Contraindications:

Sustiva should never be used with other non-nucleoside reverse transcriptase inhibitors: Edurant (rilpivirine), Intelence (etravirine), Rescriptor (delavirdine), or Viramune (nevirapine).

Patient with a previous hypersensitivity reaction to Sustiva—including Stevens-Johnson syndrome (see above) or toxic skin eruptions—should not rechallenged with this drug or prescribed Atripla, a fixed dose combination drug formulation which includes Sustiva.

Sustiva is also not recommended when coadministered with the hepatitis C (HCV) drugs Victrelis (boceprevir) and Olysio (simeprevir) because of loss of therapeutic effect for these two HCV antivirals.

Treatment Considerations:

Sustiva has been associated with fetal abnormalities in a number of animal studies. While there is still contention as to whether Sustiva poses any real risk in human, it is recommended that Sustiva be avoided during pregnancy, particularly in the first trimester. Mothers are also advised not to breastfeed while taking Sustiva.

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Sources:

U.S. Food and Drug Administration (FDA).  "Drug Approval  Package - Sustiva (efavirenz) 50mg, 100mg, 200mg capsules." Silver Spring, Maryland; issued September 21, 1998.

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