Nevirapine Roxane

Uses

Nevirapine Roxane is used for combination antiretroviral treatment of HIV-1 infection in adults and in pediatric patients 15 days and older.

Additional important information regarding the use of Nevirapine Roxane for the treatment of HIV-1 infection:

• Based on serious and life-threatening hepatotoxicity observed in controlled and uncontrolled trials, Nevirapine Roxane should not be initiated in adult females with CD4+ cell counts greater than 250 cells/mm³ or in adult males with CD4+ cell counts greater than 400 cells/mm³ unless the benefit outweighs the risk.
• The 14-day lead-in period with Nevirapine Roxane 200 mg daily dosing must be strictly followed; it has been demonstrated to reduce the frequency of rash.
• If rash persists beyond the 14-day lead-in period, do not dose escalate to 200 mg twice daily. The 200 mg once-daily dosing regimen should not be continued beyond 28 days, at which point an alternative regimen should be sought.

Nevirapine Roxane is also used to associated treatment for these conditions: Human Immunodeficiency Virus (HIV) Infections

How Nevirapine Roxane works

Nevirapine Roxane binds directly to reverse transcriptase (RT) and blocks the RNA-dependent and DNA-dependent DNA polymerase activities by causing a disruption of the enzyme's catalytic site. The activity of nevirapine does not compete with template or nucleoside triphosphates.

Dosage

Nevirapine Roxane dosage

Adult Patients: The recommended dose for Nevirapine Roxane is one 200 mg tablet daily for the first 14 days, followed by one 200 mg tablet twice daily, in combination with other antiretroviral agents. The lead-in period has been observed to decrease the incidence of rash. For concomitantly administeredantiretroviral therapy, the manufacturer's recommended dosage and monitoring should be followed.

Pediatric Patients: The recommended oral dose for pediatric patients 15 days and older is 150 mg/m² once daily for 14 days followed by 150 mg/m² twice daily thereafter. The total daily dose should not exceed 400 mg for any patient.

Side Effects

Skin rash, nausea, vomiting, headache, abnormal LFT, fatigue, diarrhoea, abdominal pain.

Toxicity

Symptoms of overdose include edema, erythema nodosum, fatigue, fever, headache, insomnia, nausea, pulmonaryinfiltrates, rash, vertigo, vomiting, and weight decrease. The most common adverse reaction is rash.

Precaution

Caution should be taken during pregnancy. Interrupt treatment if severe hepatotoxicity or life-threatening skin reactions develop. Renal or hepatic insufficiency. Monitor liver function periodically.

Interaction

Mutually increased levels effects when used with drugs extensively metabolised by CYP3A. Reduced levels/effects of methadone.

Food Interaction

• Avoid alcohol.
• Take with or without food. The absorption is unaffected by food.

Nevirapine Roxane Drug Interaction

Moderate: testosterone, phenytoin, alprazolamUnknown: aspirin, aspirin, aspirin, emtricitabine / tenofovir alafenamide, metoprolol, acetaminophen, emtricitabine / tenofovir, valproic acid, multivitamin, thiamine, cyanocobalamin, riboflavin, pyridoxine, ascorbic acid, cholecalciferol, phytonadione, zinc sulfate

Nevirapine Roxane Disease Interaction

Major: hepatotoxicity, rashModerate: hemodialysis, renal dysfunction

Volume of Distribution

• 1.21 ± 0.09 L/kg [apparent volume of distribution, healthy adults, IV] Nevirapine Roxane is capable of crossing the placenta and is found in breast milk.

Elimination Route

Nevirapine Roxane is readily absorbed (greater than 90%) after oral administration in healthy subjects and adults with HIV-1 infection. The absolute bioavailability in healthy adults following a single dose administration is 93 ± 9% (mean ± SD) for a 50 mg tablet and 91 ± 8% for an oral solution. Peak plasma nevirapine concentrations of 2 ± 0.4 mcg/mL (7.5 micromolar) were attained by 4 hours following a single 200 mg dose. Nevirapine Roxane tablets and suspension have been shown to be comparably bioavailable and interchangeable at doses up to 200 mg. When the oral tablet is given with a high-fat meal, the extent of absorption is compared to that of the fasted-state.

Half Life

45 hours

Elimination Route

Thus cytochrome P450 metabolism, glucuronide conjugation, and urinary excretion of glucuronidated metabolites represent the primary route of nevirapine biotransformation and elimination in humans. Only a small fraction (<5%) of the radioactivity in urine (representing <3% of the total dose) was made up of parent compound; therefore, renal excretion plays a minor role in elimination of the parent compound.

Pregnancy & Breastfeeding use

Nursing Mothers: The Centers for Disease Control and Prevention recommend that HIV-1 infected mothers not breastfeed their infants to avoid risking postnatal transmission of HIV-1. Nevirapine Roxane is excreted in breast milk. Because of both the potential for HIV-1 transmission and the potential for serious adverse reactions in nursing infants, mothers should be instructed not to breastfeed if they are receiving Nevirapine Roxane.

Contraindication

Hypersensitivity. Lactation. Severe hepatic impairment.

Special Warning

Pediatric Use: The safety, pharmacokinetic profile, and virologic and immunologic responses of Nevirapine Roxane have been evaluated in HIV-1 infected pediatric subjects age 3 months to 18 years. The safety and pharmacokinetic profile of Nevirapine Roxane has been evaluated in HIV-1 infected pediatric subjects age 15 days to less than 3 months.

The most frequently reported adverse events related to Nevirapine Roxane in pediatric subjects were similar to those observed in adults, with the exception of granulocytopenia, which was more commonly observed in children receiving both zidovudine and Nevirapine Roxane.

Geriatric Use: Clinical trials of Nevirapine Roxane did not include sufficient numbers of subjects aged 65 and older to determine whether elderly subjects respond differently from younger subjects. In general, dose selection for an elderly patient should be cautious, reflecting the greater frequency of decreased hepatic, renal or cardiac function, and of concomitant disease or other drug therapy.

Renal Impairment: In subjects with renal impairment (mild, moderate or severe), there were no significant changes in the pharmacokinetics of nevirapine. Nevirapine Roxane is extensively metabolized by the liver and nevirapine metabolites are extensively eliminated by the kidney. Nevirapine Roxane metabolites may accumulate in patients receiving dialysis; however, the clinical significance of this accumulation is not known. No adjustment in nevirapine dosing is required in patients with CrCL greater than or equal to 20 mL per min. The pharmacokinetics of nevirapine have not been evaluated in patients with CrCl less than 20 mL per min. In patients undergoing chronic hemodialysis, an additional 200 mg dose following each dialysis treatment is indicated.

Hepatic Impairment: Because increased nevirapine levels and nevirapine accumulation may be observed in patients with serious liver disease, do not administer Nevirapine Roxane to patients with moderate or severe (Child-Pugh Class B or C, respectively) hepatic impairment.

Acute Overdose

There is no known antidote for Nevirapine Roxane overdosage. Cases of Nevirapine Roxane overdose at doses ranging from 800 to 1800 mg per day for up to 15 days have been reported. Patients have experienced events including edema, erythema nodosum, fatigue, fever, headache, insomnia, nausea, pulmonary infiltrates, rash, vertigo, vomiting, and weight decrease. All events subsided following discontinuation of Nevirapine Roxane.

Storage Condition

Store at 15-30° C

Innovators Monograph

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