Efavirenz

DEA Class; Rx

Common Brand Names; Sustiva

  • HIV, NNRTIs

Non-nucleoside reverse transcriptase inhibitor
Used for the treatment of HIV-1 infection in combination with other antiretroviral agents
Advantages include once daily dosing and penetration into cerebrospinal fluid (CSF)

Indicated for the treatment of human immunodeficiency virus (HIV) infection in combination with other antiretroviral agents.

For human immunodeficiency virus (HIV) prophylaxis after occupational exposure.

Previously demonstrated clinically significant hypersensitivity (eg, Stevens-Johnson syndrome, erythema multiforme, or toxic skin eruptions)

Coadministration of efavirenz with elbasvir and grazoprevir

  • Total cholesterol increased (20-40%)
  • Diarrhea (3-14%, children up to 39%)
  • HDL increased (25-35%)
  • Dizziness (28.1%)
  • Rash (5-26%)
  • Fever (children 21%)
  • Depression (19%)
  • Insomnia (16.3%)
  • Cough (children 16%)
  • Vomiting (3-12%)
  • Anxiety (2-13%)
  • Nausea (2-12%)
  • Neutropenia (2-10%)
  • Pruitis (9%)
  • Impaired concentration (8.3%)
  • Transaminases increased (2-8%)
  • Somnolence (7.0%)
  • Abnormal dreams (6.2%)
  • Amylase increased (6%)
  • Hyperglycemia (2-5%)
  • Dyspepsia (4%)
  • Abdominal pain (2-3%)
  • Anorexia (2%)
  • Hallucinations (1.2%)

Hepatic impairment; not recommended for patients with moderate or severe hepatic impairment because there are insufficient data to determine whether dose adjustment is necessary

Monitor liver function tests before and during treatment in patients with underlying hepatic disease, including hepatitis B or C coinfection, marked transaminase elevations, or who are taking medications associated with liver toxicity; among reported cases of hepatic failure, a few occurred in patients with no pre-existing hepatic disease; weigh risk/benefit if AST/ALT >5 xULN; discontinue therapy if elevation of serum transaminases is accompanied by clinical signs or symptoms of hepatitis or hepatic decompensation

Redistribution of fat may occur (cushingoid appearance)

Risk of serious psychiatric events (eg, depression, suicidality, paranoia, manic episodes); immediate medical evaluation recommended for serious psychiatric symptoms such as severe depression or suicidal ideation; there have been occasional postmarketing reports of death by suicide, delusions, psychosis-like behavior and catatonia; a causal relationship to the use of efavirenz cannot be determined from these reports

CNS symptoms reported (eg, dizziness, insomnia, impaired concentration, somnolence, abnormal dreams, and hallucinations); nervous system symptoms (NSS) are frequent and usually begin 1-2 days after initiating therapy and resolve in 2-4 weeks; dosing at bedtime may improve tolerability; NSS are not predictive of onset of psychiatric symptoms

Risk of skin rash – discontinue if severe rash associated wtih blistering, desquamation, mucosal involvement, or fever

Use caution in history of seizures

Pregnancy Category: D

Lactation: Unknown if distributed in human milk; the CDC advises HIV-infected women not to breastfeed to avoid postnatal transmission of HIV

Adults

600 mg/day PO.

Geriatric

600 mg/day PO.

Adolescents

40 kg or more: 600 mg/day PO.
32.5 to 39 kg: 400 mg/day PO.
25 to 32.4 kg: 350 mg/day PO.

Children

40 kg or more: 600 mg/day PO.
32.5 to 39 kg: 400 mg/day PO.
25 to 32.4 kg: 350 mg/day PO.
20 to 24 kg: 300 mg/day PO.
15 to 19 kg: 250 mg/day PO.
7.5 to 14 kg: 200 mg/day PO.
5 to 7.4 kg: 150 mg/day PO.

Infants

3 to 11 months weighing 7.5 to 14 kg: 200 mg/day PO.
3 to 11 months weighing 5 to 7.4 kg: 150 mg/day PO.
3 to 11 months weighing 3.5 to 4 kg: 100 mg/day PO.
1 to 2 months or weighing less than 3.5 kg: Safety and efficacy have not been established.

Neonates

Safety and efficacy have not been established.

Efavirenz 

capsule

  • 50mg
  • 200mg

tablet

  • 600mg

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