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Non-Nucleoside Reverse Transcriptase Inhibitors

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delavirdine (Rescriptor ®) efavirenz (Sustiva ® )
etravirine - INTELENCE® nevirapine (Viramune ®)
rilpivirine hydrochloride - EDURANT™  
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delavirdine (Rescriptor ®)  top of page

INDICATIONS AND USAGE
RESCRIPTOR Tablets are indicated for the treatment of HIV-1 infection in combination with at least 2 other active antiretroviral agents when therapy is warranted.

The following should be considered before initiating therapy with RESCRIPTOR in treatment-naive patients. There are insufficient data directly comparing RESCRIPTOR-containing antiretroviral regimens with currently preferred 3-drug regimens for initial treatment of HIV. In studies comparing regimens consisting of 2 NRTIs (currently considered suboptimal) to RESCRIPTOR plus 2 NRTIs, the proportion of patients receiving the RESCRIPTOR regimen who achieved and sustained an HIV-1 RNA level <400 copies/mL over one year of therapy was relatively low.

Resistant virus emerges rapidly when RESCRIPTOR is administered as monotherapy. Therefore, RESCRIPTOR should always be administered in combination with other antiretroviral agents.

Mechanism of Action
Delavirdine is a non-nucleoside reverse transcriptase inhibitor (NNRTI) of HIV-1. Delavirdine binds directly to reverse transcriptase (RT) and blocks RNA-dependent and DNA-dependent DNA polymerase activities. Delavirdine does not compete with template: primer or deoxynucleoside triphosphates. HIV-2 RT and human cellular DNA polymerases alpha, gamma, or delta are not inhibited by delavirdine. In addition, HIV-1 group O, a group of highly divergent strains that are uncommon in North America, may not be inhibited by delavirdine


Dosing (Adult): Oral: 400 mg 3 times/day

Administration
Patients with achlorhydria should take the drug with an acidic beverage; antacids and delavirdine should be separated by 1 hour

Supplied: 100, 200mg tablets. Warn of rash.

efavirenz (Sustiva ® ) top of page

Mechanism of Action
Efavirenz (EFV) is an NNRTI of HIV-1. EFV activity is mediated predominantly by noncompetitive inhibition of HIV-1 reverse transcriptase (RT). HIV-2 RT and human cellular DNA polymerases alpha,beta, gamma, and delta are not inhibited by EFV

Warn of CNS toxicity that is usually self-limited to the first three weeks of treatment. May need to avoid driving or work during this period.

DOSAGE AND ADMINISTRATION

Adults
The recommended dosage of SUSTIVA (efavirenz) is 600 mg orally, once daily, in combination with a protease inhibitor and/or nucleoside analogue reverse transcriptase inhibitors (NRTIs). It is recommended that SUSTIVA be taken on an empty stomach, preferably at bedtime. The increased efavirenz concentrations observed following administration of SUSTIVA with food may lead to an increase in frequency of adverse reactions [see package insert Clinical Pharmacology (12.3)]. Dosing at bedtime may improve the tolerability of nervous system symptoms [see package insert Warnings and Precautions (5.5), Adverse Reactions (6.1), and Patient Counseling Information (17.4)].

Concomitant Antiretroviral Therapy
SUSTIVA must be given in combination with other antiretroviral medications [see see package insert Indications and Usage (1), Warnings and Precautions (5.2), Drug Interactions (7.1), and Clinical Pharmacology (12.3)].

Dosage Adjustment
If SUSTIVA is coadministered with voriconazole, the voriconazole maintenance dose should be increased to 400 mg every 12 hours and the SUSTIVA dose should be decreased to 300 mg once daily using the capsule formulation (one 200-mg and two 50-mg capsules or six 50-mg capsules). SUSTIVA tablets should not be broken.

If SUSTIVA is coadministered with rifampin to patients weighing 50 kg or more, an increase in the dose of SUSTIVA to 800 mg once daily is recommended

DOSAGE FORMS AND STRENGTHS
Capsules
200-mg capsules are gold color, reverse printed with “SUSTIVA” on the body and imprinted “200 mg” on the cap.

50-mg capsules are gold color and white, printed with “SUSTIVA” on the gold color cap and reverse printed “50 mg” on the white body.

Tablets
600-mg tablets are yellow, capsular-shaped, film-coated tablets, with “SUSTIVA” printed on both sides.

etravirine - INTELENCE® top of page

INDICATIONS AND USAGE
INTELENCE® is a human immunodeficiency virus type 1 (HIV-1) specific, non-nucleoside reverse transcriptase inhibitor (NNRTI) indicated:

In combination with other antiretroviral agents for the treatment of HIV-1 infection in treatment-experienced adult patients, who have evidence of viral replication and HIV-1 strains resistant to an NNRTI and other antiretroviral agents.

In patients who have experienced virologic failure on an NNRTI-containing regimen, do not use INTELENCE® in combination with onlyN[t]RTIs.

The safety and efficacy of INTELENCE® have not been established in pediatric patients or treatment-naïve adult patients.

DOSAGE AND ADMINISTRATION
The recommended oral dose of INTELENCE® tablets is 200 mg (one 200 mg tablet or two 100 mg tablets) taken twice daily following a meal. The type of food does not affect the exposure to etravirine. Patients who are unable to swallow INTELENCE® tablet(s) whole may disperse the tablet(s) in a glass of water. Once dispersed, patients should stir the dispersion well and drink it immediately. The glass should be rinsed with water several times and each rinse completely swallowed to ensure the entire dose is consumed.

HOW SUPPLIED
INTELENCE® 100 mg Tablets
INTELENCE® 100 mg tablets are supplied as white to off-white oval tablets debossed with "TMC125" on one side and "100" on the other side.


INTELENCE® 200 mg Tablets
INTELENCE® 200 mg tablets are supplied as white to off-white, biconvex, oblong tablets debossed with "T200" on one side

nevirapine (Viramune ®)  top of page

DOSAGE AND ADMINISTRATION

Adults
The recommended dose for nevirapine 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 administered antiretroviral therapy, the manufacturer's recommended dosage and monitoring should be followed.

Nevirapine extended release tablets (400 mg once daily) is also available for use after the lead-in period. Patients must never take more than one form of nevirapine at the same time.

Pediatric: see package insert.

Monitoring of Patients
Intensive clinical and laboratory monitoring, including liver enzyme tests, is essential at baseline and during the first 18 weeks of treatment with nevirapine. The optimal frequency of monitoring during this period has not been established. Some experts recommend clinical and laboratory monitoring more often than once per month, and in particular, would include monitoring of liver enzyme tests at baseline, prior to dose escalation, and at two weeks post-dose escalation. After the initial 18-week period, frequent clinical and laboratory monitoring should continue throughout nevirapine treatment [see Warnings and Precautions (5)]. In some cases, hepatic injury has progressed despite discontinuation of treatment.

Dosage Adjustment
Patients with Rash
Discontinue nevirapine if a patient experiences severe rash or any rash accompanied by constitutional findings [see package insert - Boxed Warning, Warnings and Precautions (5.2), and Patient Counseling Information (17.1)]. Do not increase nevirapine dose if a patient experiences mild to moderate rash without constitutional symptoms during the 14-day lead-in period of 200 mg/day (150 mg/m2/day in pediatric patients) until the rash has resolved [see package insert Warnings and Precautions (5.2) and Patient Counseling Information (17.1)]. The total duration of the once daily lead-in dosing period should not exceed 28 days at which point an alternative regimen should be sought.

Patients with Hepatic Events
If a clinical (symptomatic) hepatic event occurs, permanently discontinue nevirapine. Do not restart nevirapine after recovery [see package insert Warnings and Precautions (5.1)].

Patients with Dose Interruption
For patients who interrupt nevirapine dosing for more than 7 days, restart the recommended dosing, using one 200 mg tablet daily (150 mg/m2/day in pediatric patients) for the first 14 days (lead-in) followed by one 200 mg tablet twice daily (150 mg/m2 twice daily for pediatric patients).

Patients with Renal Impairment
Patients with CrCL greater than or equal to 20 mL/min do not require an adjustment in nevirapine dosing. An additional 200 mg dose of nevirapine following each dialysis treatment is indicated in patients requiring dialysis. Nevirapine metabolites may accumulate in patients receiving dialysis; however, the clinical significance of this accumulation is not known.

DOSAGE FORMS AND STRENGTHS
Tablets: 200 mg, white, oval, biconvex, tablets embossed with 54 193 on one side
Oral suspension: 50 mg per 5 mL, white to off-white oral suspension

rilpivirine hydrochloride - EDURANT™ top of page

INDICATIONS AND USAGE
EDURANT is a human immunodeficiency virus type 1 (HIV-1) specific, non-nucleoside reverse transcriptase inhibitor (NNRTI) indicated:

In combination with other antiretroviral agents for the treatment of HIV-1 infection in treatment-naïve adult patients.

The following points should be considered when initiating therapy with EDURANT:

More EDURANT treated subjects with HIV-1 RNA greater than 100,000 copies/mL at the start of therapy experienced virologic failure compared to subjects with HIV-1 RNA less than 100,000 copies/mL at the start of therapy.

The observed virologic failure rate in EDURANT treated subjects conferred a higher rate of overall treatment resistance and cross-resistance to the NNRTI class compared to efavirenz.

More subjects treated with EDURANT developed lamivudine/emtricitabine associated resistance compared to efavirenz.

DOSAGE AND ADMINISTRATION
The recommended dose of EDURANT is one 25 mg tablet once daily taken orally with a meal.

Rifabutin Co-administration: For patients concomitantly receiving rifabutin, the EDURANT dose should be increased to 50 mg (two tablets of 25 mg each) once daily, taken with a meal. When rifabutin co-administration is stopped, the EDURANT dose should be decreased to 25 mg once daily, taken with a meal.

HOW SUPPLIED
25 mg tablets

Reference(s)

National Institutes of Health, U.S. National Library of Medicine, DailyMed Database.
Provides access to the latest drug monographs submitted to the Food and Drug Administration (FDA). Please review the latest applicable package insert for additional information and possible updates.  A local search option of this data can be found here.

Disclaimer

Listed dosages are for - Adult patients ONLY. PLEASE READ THE DISCLAIMER CAREFULLY BEFORE ACCESSING OR USING THIS SITE. BY ACCESSING OR USING THIS SITE, YOU AGREE TO BE BOUND BY THE TERMS AND CONDITIONS SET FORTH IN THE DISCLAIMER. GlobalRPH does not directly or indirectly practice medicine or provide medical services and therefore assumes no liability whatsoever of any kind for the information and data accessed through the Service or for any diagnosis or treatment made in reliance thereon.

David F. McAuley, Pharm.D., R.Ph.  GlobalRPh Inc.
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