ISENTRESS

ISENTRESS- raltegravir potassium tablet, film coated
RedPharm Drug, Inc.


These highlights do not include all the information needed to use ISENTRESS safely and effectively. See full prescribing information for ISENTRESS.
ISENTRESS ® (raltegravir) film-coated tablets, for oral use
ISENTRESS ® (raltegravir) chewable tablets, for oral use
ISENTRESS ® (raltegravir) for oral suspension
Initial U.S. Approval: 2007

INDICATIONS AND USAGE

ISENTRESS is a human immunodeficiency virus integrase strand transfer inhibitor (HIV-1 INSTI) indicated:

In combination with other antiretroviral agents for the treatment of HIV-1 infection in patients 4 weeks of age and older (1).

The use of other active agents with ISENTRESS is associated with a greater likelihood of treatment response (14).

DOSAGE AND ADMINISTRATION

ISENTRESS can be administered with or without food (2.1).

Do not substitute ISENTRESS chewable tablets or ISENTRESS for oral suspension for the ISENTRESS 400 mg film-coated tablet.

See specific dosing guidance for chewable tablets and the formulation for oral suspension (2.1).

Adults

400 mg film-coated tablet orally, twice daily (2.2).
During coadministration with rifampin in adults, 800 mg twice daily (2.1).

Children and Adolescents

If at least 25 kg: One 400 mg film-coated tablet orally, twice daily. If unable to swallow a tablet, consider the chewable tablet, as specified in Table 1 (2.3).
If at least 3 kg to less than 25 kg: Weight based dosing, as specified in Table 2. For patients weighing between 11 and 20 kg, either the chewable tablet or the formulation for oral suspension can be used, as specified in Table 2 (2.3).

DOSAGE FORMS AND STRENGTHS

Film-Coated Tablets: 400 mg (3).
Chewable Tablets: 100 mg scored and 25 mg (3).
For Oral Suspension: Single-use packet of 100 mg (3).

CONTRAINDICATIONS

None (4).

WARNINGS AND PRECAUTIONS

Severe, potentially life-threatening and fatal skin reactions have been reported. This includes cases of Stevens-Johnson syndrome, hypersensitivity reaction and toxic epidermal necrolysis. Immediately discontinue treatment with ISENTRESS and other suspect agents if severe hypersensitivity, severe rash, or rash with systemic symptoms or liver aminotransferase elevations develops and monitor clinical status, including liver aminotransferases closely (5.1).
Monitor for Immune Reconstitution Syndrome (5.2).
Inform patients with phenylketonuria that the 100 mg and 25 mg chewable tablets contain phenylalanine (5.3).

ADVERSE REACTIONS

The most common adverse reactions of moderate to severe intensity (≥2%) are insomnia, headache, dizziness, nausea and fatigue (6.1).
Creatine kinase elevations were observed in subjects who received ISENTRESS. Myopathy and rhabdomyolysis have been reported. Use with caution in patients at increased risk of myopathy or rhabdomyolysis, such as patients receiving concomitant medications known to cause these conditions and patients with a history of rhabdomyolysis, myopathy or increased serum creatine kinase (6.2).

To report SUSPECTED ADVERSE REACTIONS, contact Merck Sharp & Dohme Corp., a subsidiary of Merck & Co., Inc., at 1-877-888-4231 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch.

DRUG INTERACTIONS

Coadministration of ISENTRESS and other drugs may alter the plasma concentration of raltegravir. The potential for drug-drug interactions must be considered prior to and during therapy (7).
Coadministration of ISENTRESS with drugs that are strong inducers of UGT1A1, such as rifampin, may result in reduced plasma concentrations of raltegravir (2.1, 7.2).

USE IN SPECIFIC POPULATIONS

Pregnancy:

ISENTRESS should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus (8.1).

Nursing Mothers:

Breastfeeding is not recommended while taking ISENTRESS (8.3).

See 17 for PATIENT COUNSELING INFORMATION and FDA-approved patient labeling.

Revised: 2/2015

FULL PRESCRIBING INFORMATION: CONTENTS*

1 INDICATIONS AND USAGE
2 DOSAGE AND ADMINISTRATION
2.1 General Dosing Recommendations
2.2 Adults
2.3 Pediatrics
2.4 Method of Administration
3 DOSAGE FORMS AND STRENGTHS
4 CONTRAINDICATIONS
5 WARNINGS AND PRECAUTIONS
5.1 Severe Skin and Hypersensitivity Reactions
5.2 Immune Reconstitution Syndrome
5.3 Phenylketonurics
6 ADVERSE REACTIONS
6.1 Clinical Trials Experience
6.2 Postmarketing Experience
7 DRUG INTERACTIONS
7.1 Effect of Raltegravir on the Pharmacokinetics of Other Agents
7.2 Effect of Other Agents on the Pharmacokinetics of Raltegravir
7.3 Drugs without Clinically Significant Interactions with ISENTRESS
8 USE IN SPECIFIC POPULATIONS
8.1 Pregnancy
8.3 Nursing Mothers
8.4 Pediatric Use
8.5 Geriatric Use
8.6 Use in Patients with Hepatic Impairment
8.7 Use in Patients with Renal Impairment
10 OVERDOSAGE
11 DESCRIPTION
12 CLINICAL PHARMACOLOGY
12.1 Mechanism of Action
12.2 Pharmacodynamics
12.3 Pharmacokinetics
12.4 Microbiology
13 NONCLINICAL TOXICOLOGY
13.1 Carcinogenesis, Mutagenesis, Impairment of Fertility
14 CLINICAL STUDIES
14.1 Treatment-Naïve Adult Subjects
14.2 Treatment-Experienced Adult Subjects
14.3 Pediatric Subjects
16 HOW SUPPLIED/STORAGE AND HANDLING
17 PATIENT COUNSELING INFORMATION

*
Sections or subsections omitted from the full prescribing information are not listed.

1 INDICATIONS AND USAGE

ISENTRESS® is indicated in combination with other antiretroviral agents for the treatment of human immunodeficiency virus (HIV-1) infection in patients 4 weeks of age and older.

The use of other active agents with ISENTRESS is associated with a greater likelihood of treatment response [see CLINICAL STUDIES (14)].

2 DOSAGE AND ADMINISTRATION

2.1 General Dosing Recommendations

ISENTRESS Film-Coated Tablets, Chewable Tablets and For Oral Suspension can be administered with or without food [see CLINICAL PHARMACOLOGY (12.3)].
Because the formulations are not bioequivalent, do not substitute ISENTRESS chewable tablets or ISENTRESS for oral suspension for the ISENTRESS 400 mg film-coated tablet. See specific dosing guidance for chewable tablets and the formulation for oral suspension.
During coadministration of ISENTRESS 400 mg film-coated tablets with rifampin, the recommended dosage of ISENTRESS is 800 mg twice daily in adults. There are no data to guide co-administration of ISENTRESS with rifampin in patients below 18 years of age [see DRUG INTERACTIONS (7.2)].
Maximum dose of chewable tablets is 300 mg twice daily.
Maximum dose of oral suspension is 100 mg twice daily.
Each single-use packet for oral suspension contains 100 mg of raltegravir which is suspended in 5 mL of water giving a final concentration of 20 mg/mL.

2.2 Adults

For the treatment of adult patients with HIV-1 infection, the dosage of ISENTRESS is one 400 mg film-coated tablet administered orally, twice daily.

2.3 Pediatrics

If at least 25 kg: One 400 mg film-coated tablet orally, twice daily.
If unable to swallow a tablet, consider the chewable tablet, as specified in Table 1.

Table 1: Alternative Dose* with ISENTRESS Chewable Tablets for Pediatric Patients Weighing at Least 25 kg
Body Weight
(kg) Dose Number of Chewable Tablets

*
The weight-based dosing recommendation for the chewable tablet is based on approximately 6 mg/kg/dose twice daily [see CLINICAL PHARMACOLOGY (12.3)].

The 100 mg chewable tablet can be divided into equal halves.

25 to less than 28 150 mg twice daily 1.5 × 100 mg† twice daily
28 to less than 40 200 mg twice daily 2 × 100 mg twice daily
At least 40 300 mg twice daily 3 × 100 mg twice daily

If at least 4 weeks of age and weighing at least 3 kg to less than 25 kg: Weight based dosing, as specified in Table 2.
For patients weighing between 11 and 20 kg, either the chewable tablet or oral suspension can be used, as specified in Table 2. Patients can remain on the oral suspension as long as their weight is below 20 kg. Refer to Table 2 for appropriate dosing [see CLINICAL STUDIES (14.3)].

Table 2: Recommended Dose* for ISENTRESS For Oral Suspension and Chewable Tablets in Pediatric Patients Weighing Less than 25 kg
Body Weight
(kg) Volume (Dose) of Suspension to be Administered Number of Chewable Tablets

*
The weight-based dosing recommendation for the chewable tablet and oral suspension is based on approximately 6 mg/kg/dose twice daily[see CLINICAL PHARMACOLOGY (12.3)].

For weight between 11 and 20 kg either formulation can be used.
Note: The chewable tablets are available as 25 mg and 100 mg tablets.

The 100 mg chewable tablet can be divided into equal halves.

3 to less than 4 1 mL (20 mg) twice daily
4 to less than 6 1.5 mL (30 mg) twice daily
6 to less than 8 2 mL (40 mg) twice daily
8 to less than 11 3 mL (60 mg) twice daily
11 to less than 14† 4 mL (80 mg) twice daily 3 × 25 mg twice daily
14 to less than 20† 5 mL (100 mg) twice daily 1 × 100 mg twice daily
20 to less than 25 1.5 × 100 mg‡ twice daily

2.4 Method of Administration

ISENTRESS Film-Coated Tablets

Film-Coated Tablets must be swallowed whole

ISENTRESS Chewable Tablets

Chewable Tablets may be chewed or swallowed whole

ISENTRESS For Oral Suspension

Each single-use ISENTRESS packet for oral suspension contains 100 mg of raltegravir which is to be suspended in 5 mL of water giving a final concentration of 20 mg/mL.

Pour packet contents of ISENTRESS for oral suspension into 5 mL of water and mix
Once mixed, measure the recommended volume (dose) of suspension with a syringe and administer the dose orally
The volume (dose) of suspension should be administered orally within 30 minutes of mixing
Discard any remaining suspension
For more details on preparation and administration of the suspension, see INSTRUCTIONS FOR USE.

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