efavirenz

REMS

HIV infection (in combination with one or more other antiretroviral agents).

Contraindicated in:

Hypersensitivity
Moderate to severe hepatic impairment.
Concurrent use of elbasvir and grazoprevir
Lactation: Breastfeeding not recommended for women with HIV.

Use Cautiously in:

History of mental illness or substance abuse (↑ risk of psychiatric symptomatology)
Mild hepatic impairment (including coinfection with hepatitis B/C)
History of seizure disorders (↑ risk of seizures)
OB: Use in pregnancy only if other options have been exhausted; birth defects have been reported
Pedi: Children <3 mo (safety and effectiveness not established); ↑ incidence of rash
Geri: Use lower initial dose in older adults due to ↑ incidence of renal or cardiac dysfunction.

CV: QT interval prolongation.

Derm: rash, pruritus, sweating.

Endo: Graves' disease, hypercholesterolemia, hypertriglyceridemia.

GI: nausea, abdominal pain, anorexia, autoimmune hepatitis, diarrhea, dyspepsia, flatulence, HEPATOTOXICITY.

GU: hematuria, renal calculi.

Metab: fat redistribution.

MS: polymyositis.

Neuro: Guillain-Barré syndrome, abnormal dreams, ataxia, catatonia, delusions, depression, dizziness, drowsiness, encephalopathy, fatigue, headache, hypoesthesia, impaired concentration, insomnia, nervousness, psychoses, SUICIDAL THOUGHTS/BEHAVIORS.

Misc: immune reconstitution syndrome.

Drug-Drug:

May lead to loss of virologic response to elbasvir/grazoprevir; concurrent use contraindicated.
Induces (stimulates) the hepatic cytochrome P450 3A4 enzyme system and would be expected to influence the effects of other drugs that are metabolized by this system; efavirenz itself is also metabolized by this system.
↑risk of CNS depression with other CNS depressants, including alcohol, antidepressants, antihistamines, and opioid analgesics.
May ↓ the effectiveness of progestin-containing hormonal contraceptives (e.g., etonogestrel, norelgestromin, levonorgestrel).
Use with voriconazole significantly ↓ voriconazole levels and ↑ efavirenz levels; avoid concurrent use with standard doses of voriconazole; if used together, ↑ dose of voriconazole to 400 mg every 12 hr and ↓ dose of efavirenz to 300 mg daily.
May ↓ posaconazole levels; avoid concurrent use.
May ↓ itraconazole levels; use alternative antifungal agent.
May ↓ ketoconazole levels
May ↓ fosamprenavir levels; ↑ dose of ritonavir when given with fosamprenavir/ritonavir once daily.
May ↓ atazanavir levels; dosage adjustments may be needed in treatment-nave patients; avoid concurrent use in treatment-experienced patients.
May ↓ lopinavir levels; ↑ dose of lopinavir/ritonavir; avoid concurrent use of lopinavir/ritonavir once daily.
May ↑ ritonavir levels; monitor liver function tests.
May ↓ raltegravir levels and effectiveness.
↓maraviroc levels; ↑ maraviroc dose.
May alter the effects of warfarin.
May ↓ levels of cyclosporine, tacrolimus, and sirolimus.
May ↓ levels of bupropion and sertraline.
Rifampin may ↓ levels; ↑ dose of efavirenz
Concurrent use with other NNRTIs including etravirine, nevirapine, and rilpivirine may lead to ↓ effectiveness and should be avoided.
May ↓ levels of raltegravir.
Concurrent use with carbamazepine may ↓ levels of carbamazepine and efavirenz; use alternative anticonvulsant agent
Concurrent use with phenytoin or phenobarbital may ↓ levels of phenytoin, carbamazepine, and efavirenz
May ↓ levels of clarithromycin; consider using azithromycin
May ↓ levels of rifabutin; ↑ daily dose of rifabutin by 50%
May ↓ levels of calcium channel blockers, atorvastatin, pravastatin, simvastatin, methadone, and artemether/lumefantrine.
May ↓ levels of progestin-containing contraceptives and etonogestrel; use reliable method of barrier contraception in addition to hormonal contraceptive agent.
Concurrent use with other QT interval prolonging medications may ↑ risk of QT interval prolongation or torsades de pointes.
May ↓ therapeutic effects of pibrentasvir/glecaprevir, velpatasvir/sofosbuvir, and velpatasivir/sofosbuvir/voxilaprevir; avoid concurrent use.

Drug-Food:

Ingestion following a high-fat meal↑ absorption by 50%.

(Generic available)

Capsules: 50 mg; 200 mg;
Tablets: 600 mg;
In combination with: emtricitabine and tenofovir disoproxil fumarate (Atripla); lamivudine and tenofovir disoproxil fumarate (Symfi, Symfi Lo). (See Appendix [not included in this PDA edition]).

PO (Adults and Children 40 kg): 600 mg once daily; Concurrent rifampin therapy (in patients >50 kg): 800 mg once daily.
PO (Children 3 mo and 32.5–39.9 kg): 400 mg once daily.
PO (Children 3 mo and 25–32.4 kg): 350 mg once daily.
PO (Children 3 mo and 20–24.9 kg): 300 mg once daily.
PO (Children 3 mo and 15–19.9 kg): 250 mg once daily.
PO (Children 3 mo and 7.5–14.9 kg): 200 mg once daily.
PO (Children 3 mo and 5–7.4 kg): 150 mg once daily.
PO (Children 3 mo and 3.5–4.9 kg): 100 mg once daily.

Inhibits HIV reverse transcriptase, which results in disruption of DNA synthesis.

Therapeutic Effects:

Slowed progression of HIV infection and decreased occurrence of sequelae.
Increases CD4 cell counts and decreases viral load.

Therapeutic Classification: antiretrovirals

Pharmacologic Classification: non nucleoside reverse transcriptase inhibitors

Absorption: 50% absorbed when ingested following a high-fat meal.

Distribution: 99.5–99.75% bound to plasma proteins; enters CSF.

Metabolism/Excretion: Mostly metabolized by the liver via the CYP3A4 and CYP2B6 isonezymes. Excreted in urine and feces, primarily as metabolites.

Half-life: Following single dose: 52–76 hr. Following multiple doses: 40–55 hr.

(blood levels)

ROUTE	ONSET	PEAK	DURATION
PO	rapid	3–5 hr	24 hr

Emphasize the importance of taking efavirenz as directed. It must always be used in combination with other antiretroviral drugs. Do not take more than prescribed amount, and do not stop taking without consulting health care professional. Take missed doses as soon as remembered; do not double doses. Advise patient to read Patient Information before starting therapy and with each Rx refill in case of changes.
Instruct patient that efavirenz should not be shared with others.
May cause dizziness, impaired concentration, or drowsiness. Caution patient to avoid driving or other activities requiring alertness until response to medication is known.
Instruct patient to notify health care professional immediately if rash or suicidal thoughts or behaviors occur.
Inform patient that efavirenz does not cure AIDS or prevent associated or opportunistic infections. Efavirenz may reduce the risk of transmission of HIV to others through sexual contact or blood contamination. Caution patient to use a condom and to avoid sharing needles or donating blood to prevent spreading the AIDS virus to others. Advise patient that the long-term effects of efavirenz are unknown at this time.
Inform patient that redistribution and accumulation of body fat may occur, causing central obesity, dorsocervical fat enlargement (buffalo hump), peripheral wasting, breast enlargement, and cushingoid appearance. The cause and long-term effects are not known.
Instruct patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and to consult with health care professional before taking other medications.
Inform patient of risk of developing late-onset neurotoxicity (ataxia, encephalopathy); may occur months to years after starting therapy.
Rep: May cause fetal harm. Advise females of reproductive potential taking oral contraceptives to use a nonhormonal method of birth control during efavirenz therapy and for at least 12 wk following discontinuation and to avoid breastfeeding. Advise patient to notify health care professional if they become pregnant while taking efavirenz. Encourage patients who become pregnant during therapy to join the Antiretroviral Pregnancy Registry that monitors pregnancy outcomes in women exposed to efavirenz during pregnancy. Enroll patient by calling 1-800-258-4263.
Emphasize the importance of regular follow-up exams and blood counts to determine progress and monitor for side effects.

NDC Code^*

0056- Bristol-Myers Squibb Pharma Company
0056-0470- SUSTIVA 0056-0470-30- 30 CAPSULE, GELATIN COATED in 1 BOTTLE (0056-0470-30)

0056- Bristol-Myers Squibb Pharma Company
0056-0474- SUSTIVA 0056-0474-92- 90 CAPSULE, GELATIN COATED in 1 BOTTLE (0056-0474-92)

0056- Bristol-Myers Squibb Pharma Company
0056-0510- SUSTIVA 0056-0510-30- 30 TABLET, FILM COATED in 1 BOTTLE (0056-0510-30)

0378- Mylan Pharmaceuticals Inc.
0378-2233- Efavirenz 0378-2233-93- 30 TABLET, FILM COATED in 1 BOTTLE, PLASTIC (0378-2233-93)

31722- Camber Pharmaceuticals, Inc.
31722-504- Efavirenz 31722-504-25- 250 TABLET, FILM COATED in 1 BOTTLE (31722-504-25)

31722- Camber Pharmaceuticals, Inc.
31722-504- Efavirenz 31722-504-30- 30 TABLET, FILM COATED in 1 BOTTLE (31722-504-30)

64380- Strides Pharma Science Limited
64380-889- Efavirenz 64380-889-04- 30 TABLET in 1 BOTTLE (64380-889-04)

64980- Rising Pharmaceuticals, Inc.
64980-406- Efavirenz 64980-406-03- 30 CAPSULE in 1 BOTTLE (64980-406-03)

64980- Rising Pharmaceuticals, Inc.
64980-407- Efavirenz 64980-407-09- 90 CAPSULE in 1 BOTTLE (64980-407-09)

65862- Aurobindo Pharma Limited
65862-049- Efavirenz 65862-049-10- 3 BLISTER PACK in 1 CARTON (65862-049-10) > 10 TABLET, FILM COATED in 1 BLISTER PACK

65862- Aurobindo Pharma Limited
65862-049- Efavirenz 65862-049-30- 30 TABLET, FILM COATED in 1 BOTTLE (65862-049-30)

65862- Aurobindo Pharma Limited
65862-104- Efavirenz 65862-104-10- 3 BLISTER PACK in 1 CARTON (65862-104-10) > 10 CAPSULE in 1 BLISTER PACK

65862- Aurobindo Pharma Limited
65862-104- Efavirenz 65862-104-30- 30 CAPSULE in 1 BOTTLE (65862-104-30)

65862- Aurobindo Pharma Limited
65862-105- Efavirenz 65862-105-10- 3 BLISTER PACK in 1 CARTON (65862-105-10) > 10 CAPSULE in 1 BLISTER PACK

65862- Aurobindo Pharma Limited
65862-105- Efavirenz 65862-105-30- 30 CAPSULE in 1 BOTTLE (65862-105-30)

65862- Aurobindo Pharma Limited
65862-106- Efavirenz 65862-106-09- 9 BLISTER PACK in 1 CARTON (65862-106-09) > 10 CAPSULE in 1 BLISTER PACK

65862- Aurobindo Pharma Limited
65862-106- Efavirenz 65862-106-10- 3 BLISTER PACK in 1 CARTON (65862-106-10) > 10 CAPSULE in 1 BLISTER PACK

65862- Aurobindo Pharma Limited
65862-106- Efavirenz 65862-106-30- 30 CAPSULE in 1 BOTTLE (65862-106-30)

65862- Aurobindo Pharma Limited
65862-106- Efavirenz 65862-106-90- 90 CAPSULE in 1 BOTTLE (65862-106-90)

65862- Aurobindo Pharma Limited
65862-774- Efavirenz 65862-774-30- 30 TABLET, FILM COATED in 1 BOTTLE (65862-774-30)

69097- Cipla USA Inc.
69097-301- Efavirenz 69097-301-02- 30 TABLET, FILM COATED in 1 BOTTLE (69097-301-02)

70518- REMEDYREPACK INC.
70518-0482- SUSTIVA 70518-0482-0- 30 TABLET, FILM COATED in 1 BLISTER PACK (70518-0482-0)

70518- REMEDYREPACK INC.
70518-1013- Efavirenz 70518-1013-0- 30 TABLET, FILM COATED in 1 BLISTER PACK (70518-1013-0)

70518- REMEDYREPACK INC.
70518-1100- Efavirenz 70518-1100-0- 30 TABLET in 1 BLISTER PACK (70518-1100-0)

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