nevirapine

nevirapine /ne·vir·a·pine/ (nĕ-vir´ah-pēn) a nonnucleoside inhibitor of HIV-1reverse transcriptase, used in combination with other antiretroviral agents in the treatment of HIV infection.

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ne·vir·a·pine (n-vîr-pn, -pn)

n.

A non-nucleoside analog that is used as an antiviral drug in treating HIV infection.

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nevirapine,

an antiretroviral nonnucleoside reverse transcriptase inhibitor.

indication It is prescribed in combination for the treatment of human immunodeficiency virus infection.

contraindications It should not be given to patients with an allergy or sensitivity to the medication or to patients taking ketoconazole or oral contraceptives. When used alone, there is rapid and uniform appearance of viral resistance.

adverse effects The side effects most often reported include headache, rash, drug fever, and diarrhea.

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nevirapine

Viramune

Pharmacologic class: Nonnucleoside reverse transcriptase inhibitor

Therapeutic class: Antiretroviral

Pregnancy risk category C

FDA Boxed Warning

• Drug has caused severe, life-threatening, and in some cases fatal hepatotoxicity, particularly in first 18 weeks. In some cases, patients had nonspecific, prodromal signs or symptoms of hepatitis and progressed to hepatic failure. These events are commonly associated with rash. Hepatotoxicity can occur at any time during therapy. Patients should discontinue drug and seek immediate medical help if they develop hepatitis signs or symptoms or have increased transaminase levels along with rash or other systemic symptoms.
• Severe, life-threatening skin reactions (including fatal cases) have occurred; these have included Stevens-Johnson syndrome, toxic epidermal necrolysis, and hypersensitivity reactions. Patients who develop signs or symptoms of severe skin reactions or hypersensitivity reactions should discontinue drug and seek immediate medical help.
• Monitor patients intensively during first 18 weeks of therapy. Be especially vigilant during first 6 weeks. Don't restart drug in patient who has had severe hepatic, skin, or hypersensitivity reaction.

Action

Inhibits human immunodeficiency virus (HIV) nonnucleoside reverse transcriptase by binding directly to reverse transcriptase and blocking RNA-dependent and DNA-dependent polymerase activity

Availability

Oral suspension: 50 mg/5 ml

Tablets: 200 mg

⊘Indications and dosages

➣ Adjunctive treatment of HIV-1 infection in patients showing deterioration

Adults: 200 mg P.O. daily for 14 days, then 200 mg P.O. b.i.d., given with a nucleoside analogue. Total daily dosage is 400 mg.

Children ages 8 and older: 4 mg/kg P.O. daily for 14 days, followed by 4 mg/kg b.i.d. Total daily dosage is 400 mg.

Children ages 2 months to 8 years: 4 mg/kg P.O. daily for 14 days, followed by 7 mg/kg b.i.d. Total daily dosage is 400 mg.

Dosage adjustment

• Hepatic impairment
• Chronic hemodialysis

Off-label uses

• Prophylaxis of maternal-fetal HIV transmission

Contraindications

• Hypersensitivity to drug or its components

Precautions

Use cautiously in:
• impaired renal or hepatic function
• pregnant or breastfeeding patients
• children.

Administration

• Give with or without food.

Route	Onset	Peak	Duration
P.O.	Unknown	4 hr	Unknown

Adverse reactions

CNS: paresthesia, headache, malaise, fatigue

GI: nausea, diarrhea, abdominal pain

Hematologic: agranulocytosis

Hepatic: hepatitis, hepatotoxicity , hepatic failure

Musculoskeletal: myalgia, pain

Skin: rash, blistering, toxic epidermal necrolysis, Stevens-Johnson syndrome

Other: fever

Interactions

Drug-drug. Drugs extensively metabolized by CYP3A-P450, hormonal contraceptives, protease inhibitors: decreased blood levels of these drugs

Prednisone: increased risk of rash

Rifabutin, rifamycin: decreased nevirapine blood level

Drug-diagnostic tests. Alanine aminotransferase, aspartate aminotransferase, bilirubin, gamma-glutamyltransferase: increased levels

Hemoglobin, neutrophils: decreased levels

Drug-herbs. St. John's wort: decreased nevirapine blood level

Patient monitoring

☞ Check closely for rash (which may be first sign of Stevens-Johnson syndrome), especially during first 6 months of therapy.
• Monitor patient's weight, temperature, and chest X-ray periodically.
• Assess patient's appetite and energy and physical activity levels.
• Monitor liver function tests and CBC with white cell differential.

Patient teaching

• Tell patient he may take with or without food.
• Instruct patient to take missed dose as soon as he remembers. But if it's almost time for next dose, tell him to skip missed dose. Caution him not to double the dose.
• Inform female patient that hormonal contraceptives, implants, or shots may be ineffective during nevirapine therapy. Urge her to use alternative birth-control method.
☞ Teach patient to recognize and immediately report rash, easy bruising or bleeding, and signs and symptoms of hepatotoxicity.
• Inform patient that nevirapine won't cure HIV or prevent its transmission.
• Caution female not to breastfeed, because breast milk may transfer HIV to infant.
• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs, tests, and herbs mentioned above.

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nevirapine

Viramune^® AIDS An antiretroviral non-nucleoside reverse transcriptase inhibitor, combined with nucleoside RTIs to manage HIV infection Adverse effects Rash. See Nonnucleoside reverse transcriptase inhibitor, TIBO. Cf Antiretroviral agent, Delavirdine.