A-Z Drug Facts > Nevirapine

Nevirapine

Pronouncation: (nuh-VEER-uh-peen)
Class: Non-nucleoside reverse transcriptase inhibitor

Trade Names:
Viramune
- Tablets 200 mg
- Oral solution 50 mg/mL (as hemihydrate)

Pharmacology

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Inhibits replication of retroviruses, including HIV.

Pharmacokinetics

Absorption

Nevirapine oral absorption is more than 90%, bioavailability is 93% (tablets) and 91% (oral solution), T _max is 4 h, and C _max is approximately 2 mcg/mL.

Distribution

Nevirapine crosses the placenta and is found in breast milk. Protein binding is approximately 60% and is highly lipophilic and widely distributed. Nevirapine Vd is 1.21 L/kg (IV), and cerebrospinal fluid approximates 45% of concentration in plasma.

Metabolism

Nevirapine is eliminated in urine (81.3%) and feces (10.1%). Less than 3% of the parent compound is excreted in urine. Autoinduction results in a decrease of the t _{1/ 2} from 45 h (single dose) to approximately 25 to 30 h (multiple dose).

Indications and Usage

In combination with other antiretroviral agents for treatment of HIV-1 infection.

Contraindications

Standard considerations.

Dosage and Administration

Adults Initial therapy

PO 200 mg daily for 14 days. Total daily dose not to exceed 400 mg.

Maintenance therapy

PO 200 mg twice daily in combination with other antiretroviral agents.

Children (2 mo to 8 yr of age)

PO 4 mg/kg daily for 14 days followed by 7 mg/kg twice daily. Total daily dose not to exceed 400 mg.

Children (at least 8 yr of age)

PO 4 mg/kg daily for 14 days followed by 4 mg/kg twice daily. Total daily dose not to exceed 400 mg.

General Advice

• Tablets and oral suspension are interchangeable on a mg-to-mg basis at doses up to 200 mg.
• Administer without regard to meals. Administer with food if GI upset occurs.
• Shake suspension before measuring dose. Administer dose using oral dosing syringe or dosing cup. If using dosing cup, thoroughly rinse dosing cup with water and administer rinse water to patient.

Storage/Stability

Store tablets and oral suspension at controlled room temperature (59° to 86°F).

Drug Interactions

Clarithromycin

Clarithromycin concentrations may be reduced, while concentrations of the active metabolite of clarithromycin may be increased.

Contraceptives, oral

Lower hormone levels and potential contraceptive failure.

Efavirenz, methadone

Concentrations of these agents may be decreased by nevirapine.

Fluconazole

Nevirapine concentrations may be increased.

Ketoconazole

Coadministration resulted in significant reduction in ketoconazole plasma concentrations. Do not coadminister ketoconazole and nevirapine.

Protease inhibitors

Lower protease inhibitor plasma levels.

Rifabutin

Rifabutin concentrations may be increased.

Rifampin, rifabutin

Lower nevirapine plasma levels.

St. John's wort

May reduce nevirapine concentrations, resulting in loss of virologic response and possible resistance to nevirapine and the class of non-nucleoside reverse transcriptase inhibitors.

Warfarin

Plasma concentrations of warfarin may be altered, resulting in potential increases in coagulation time.

Laboratory Test Interactions

None well documented.

Adverse Reactions

CNS

Fatigue (5%); headache (4%); somnolence, paresthesia, malaise (postmarketing).

Dermatologic

Rash (all grades 24% [life-threatening 2%]); Stevens-Johnson syndrome; toxic epidermal necrolysis; angioedema, bullous eruptions, urticaria, blistering (postmarketing); facial edema.

EENT

Conjunctivitis (postmarketing).

GI

Nausea (9%); abdominal pain, diarrhea (2%); vomiting, ulcerative stomatitis, oral lesions (postmarketing).

Hepatic

Hepatitis (including fatal fulminant hepatitis); hepatic failure; jaundice, cholestatic hepatitis, hepatic necrosis (postmarketing).

Hematologic-Lymphatic

Eosinophilia; granulocytopenia; lymphadenopathy; anemia, neutropenia (postmarketing).

Hypersensitivity

Hypersensitivity, including severe rash or rash accompanied by fever, general malaise, fatigue, muscle or joint aches, blisters, oral lesions, conjunctivitis, facial edema; anaphylaxis (postmarketing).

Lab Tests

Abnormal LFTs (7%).

Metabolic

Redistribution and accumulation of body fat (postmarketing).

Musculoskeletal

Arthralgia, muscle and joint pain (postmarketing).

Renal

Renal function impairment.

Miscellaneous

Fever (postmarketing).

Precautions

Warnings Dermal reactions Severe, life-threatening skin reactions (sometimes fatal) occurred during therapy. Cases include Stevens-Johnson syndrome, toxic epidermal necrolysis, and hypersensitivity reactions. Dosing A 14-day initiation period (200 mg/day) must be strictly followed. Hepatotoxicity Severe, life-threatening, and in some cases fatal, including fulminant and cholestatic hepatitis, necrosis, and failure. Patient monitoring Closely monitor for first 18 wk to detect signs and symptoms of skin/hepatic reactions.

Monitor Perform clinical chemistry tests, including LFTs, prior to initiating therapy and at regular intervals during therapy.

Pregnancy

Category C .

Lactation

Excreted in breast milk. HIV-infected mothers should not breast-feed their infants.

Children

For use in children at least 2 mo of age. Nevirapine Cl at least 2-fold greater in children younger than 8 yr of age.

Renal Function

Use with caution in patients with renal function impairment.

Hepatic Function

Use with caution in patients with moderate hepatic function impairment. Do not administer to patients with severe hepatic function impairment.

Fat redistribution

Redistribution or accumulation of body fat, including central obesity, dorsocervical fat enlargement, peripheral wasting, facial wasting, breast enlargement, and cushingoid appearance may occur.

Hepatotoxicity

Permanently discontinue therapy if hepatotoxicity occurs.

Missed doses

Patients who interrupt maintenance dosing for more than 7 days should restart the recommended dosing (1 daily for 14 days followed by 1 twice daily).

Resistance

When used as monotherapy, resistant virus emerges rapidly and uniformly.

Skin reactions

Discontinue drug if skin rash accompanied by constitutional symptoms (eg, fever, blistering, oral lesions, conjunctivitis, swelling, muscle or joint aches, general malaise) occurs. If rash is mild to moderate in severity and not accompanied by constitutional symptoms, the drug can be continued with close monitoring. If rash develops during first 14 days of therapy, do not increase dose beyond 200 mg daily until rash resolves.

Overdosage

Symptoms

Edema, erythema nodosum, fatigue, fever, headache, insomnia, nausea, pulmonary infiltrates, rash, vertigo, vomiting, weight decrease.

Patient Information

• Warn patient that this drug is not to be used by itself but is combined with other antiretroviral agents and not to change the dose or stop taking any of the antiretroviral agents unless advised by health care provider.
• Advise patient to review patient information leaflet before starting therapy and with each refill of the medication.
• Advise patient to take prescribed dose without regard to meals but to take with food if stomach upset occurs.
• Advise patient or caregiver using suspension to shake suspension before measuring dose and to administer prescribed dose using oral dosing syringe or dosing cup. If using dosing cup, advise patient or caregiver to thoroughly rinse the dosing cup with water and administer rinse water to patient.
• Advise patient that a 14-day lead-in period (lower dose) is used to reduce frequency of rash and not to exceed the prescribed dose during this period.
• Advise patient that if a dose is missed, to take the dose as soon as possible and then return to the normal schedule. However, if it is almost time for the next dose, advise patient to skip the dose and take the next dose at the regular time. Caution patient not to double the dose to catch up.
• Instruct patient that if therapy is stopped for longer than 7 days for any reason, not to restart therapy without discussing how to restart nevirapine with health care provider. Advise patient that therapy may have to be restarted using the 14-day lead-in dose again.
• Instruct patient to discontinue use and notify health care provider immediately if any of the following are noted: severe skin rash or rash accompanied by fever, general body discomfort, nausea, appetite loss, fatigue, muscle or joint aches, blisters, mouth sores, red or inflamed eyelids, facial swelling, swollen lymph nodes, decreased urination, dark urine, pale stools, tenderness on right side below ribs, or yellowing of skin or eyes.
• Advise patient that changes in body fat (increased fat in upper back and neck, breast, or around the trunk and loss of fat from legs, arms, or face) may occur but that the cause and long-term health effects of these changes are not known at this time. Advise patient to discuss with health care provider if noted and significant.
• Inform patient that drug does not completely eliminate HIV virus and, therefore, does not reduce risk of transmitting HIV. Appropriate precautions must still be followed.
• Advise patient that drug is not a cure for HIV infection and that illnesses associated with HIV infection, including opportunistic infections, may still be acquired. Patient should remain under a health care provider's care.
• Advise women using combination oral contraceptives to use an additional nonhormonal form of contraception because nevirapine can reduce the effectiveness of combination oral contraceptives.
• Caution HIV-infected mother that breast-feeding a baby could cause HIV infection in the baby.

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