Source: European Medicines Agency (EU) Revision Year: 2019 Publisher: Merck Sharp & Dohme B.V., Waarderweg 39, 2031 BN Haarlem, The Netherlands
ISENTRESS is indicated in combination with other anti-retroviral medicinal products for the treatment of human immunodeficiency virus (HIV-1) infection (see sections 4.2, 4.4, 5.1 and 5.2).
Therapy should be initiated by a physician experienced in the management of HIV infection.
ISENTRESS should be used in combination with other active anti-retroviral therapies (ARTs) (see sections 4.4 and 5.1).
Because the formulations have different pharmacokinetic profiles neither the granules for oral suspension nor the chewable tablets should be substituted for the 400 mg tablet or 600 mg tablet (see section 5.2). The granules for oral suspension and the chewable tablets have not been studied in HIV-infected adolescents (12 to 18 years) or adults.
Dosing is weight based from birth as specified in Table 1 and Table 2. Patients can remain on the granules for oral suspension as long as their weight is below 20 kg. For patients weighing between 11 and 20 kg, either the granules for oral suspension or the chewable tablet can be used as specified in Table 1 (see section 5.2). Refer to the chewable tablet SmPC for additional dosing information.
The safety and efficacy of raltegravir in preterm (<37 weeks of gestation) and low birth weight (<2000 g) newborns have not been established. No data are available in this population and no dosing recommendations can be made.
Table 1. Recommended Dose* for ISENTRESS Granules For Oral Suspension and Chewable Tablets in Paediatric Patients at least 4 weeks of age and weighing 3 to 25 kg
| Body Weight (kg) | Volume (Dose) of Suspension to be Administered | Number of Chewable Tablets |
|---|---|---|
| 3 to less than 4 | 2,5 ml (25 mg) twice daily | |
| 4 to less than 6 | 3 ml (30 mg) twice daily | |
| 6 to less than 8 | 4 ml (40 mg) twice daily | |
| 8 to less than 11 | 6 ml (60 mg) twice daily | |
| 11 to less than 14† | 8 ml (80 mg) twice daily | 3 × 25 mg twice daily |
| 14 to less than 20† | 10 ml (100 mg) twice daily | 1 × 100 mg twice daily |
| 20 to less than 25 | 1,5 × 100 mg‡ twice daily |
* The weight-based dosing recommendation for the chewable tablet, and oral suspension in 10mL of water is based on approximately 6 mg/kg/dose twice daily (see section 5.2).
† 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.
Table 2. Recommended Dose for ISENTRESS For Oral Suspension in Full-Term Neonates (Birth to 4 weeks [28 days] of age*:
Note: If the mother has taken ISENTRESS 2-24 hours before delivery, the infant’s first dose should be given between 24-48 hours after birth.
| Body Weight (kg) | Volume (Dose) of Suspension to be Administered |
|---|---|
| Birth to 1 Week – Once daily dosing† | |
| 2 to less than 3 | 0,4 ml (4 mg) once daily |
| 3 to less than 4 | 0,5 ml (5 mg) once daily |
| 4 to less than 5 | 0,7 ml (7 mg) once daily |
| 1 to 4 Weeks – Twice daily dosing‡ | |
| 2 to less than 3 | 0,8 ml (8 mg) twice daily |
| 3 to less than 4 | 1 ml (10 mg) twice daily |
| 4 to less than 5 | 1,5 ml (15 mg) twice daily |
Maximum dose of oral suspension is 100 mg twice daily.
Each single-use sachet contains 100 mg of raltegravir which is to be suspended in 10 mL of water giving a final concentration of 10 mg per mL (see section 6.6).
Scheduled appointments for the patient should be kept because the ISENTRESS dosage should be adjusted as the child grows.
ISENTRESS is also available in a 400 mg tablet for use in adults, adolescents and children weighing at least 25 kg and able to swallow a tablet. For patients weighing at least 25 kg but are unable to swallow a tablet, consider the chewable tablet. Refer to the 400 mg and chewable tablet SmPCs for additional dosing information.
ISENTRESS is also available for adults and paediatric patients (weighing at least 40 kg), as a 600 mg tablet to be administered as 1,200 mg once daily (two 600 mg tablets) for treatment-naïve patients or patients who are virologically suppressed on an initial regimen of ISENTRESS 400 mg twice daily. Refer to the 600 mg tablet SmPCs for additional dosing information.
There is limited information regarding the use of raltegravir in the elderly (see section 5.2). Therefore ISENTRESS should be used with caution in this population.
No dosage adjustment is required for patients with renal impairment (see section 5.2).
No dosage adjustment is required for patients with mild to moderate hepatic impairment. The safety and efficacy of raltegravir have not been established in patients with severe underlying liver disorders. Therefore, ISENTRESS should be used with caution in patients with severe hepatic impairment (see sections 4.4 and 5.2).
Oral use.
ISENTRESS granules for oral suspension can be administered with or without food (see section 5.2).
For details on preparation and administration of the suspension, see section 6.6.
No specific information is available on the treatment of overdose with raltegravir.
In the event of an overdose, it is reasonable to employ the standard supportive measures, e.g., remove unabsorbed material from the gastrointestinal tract, employ clinical monitoring (including obtaining an electrocardiogram), and institute supportive therapy if required. It should be taken into account that raltegravir is presented for clinical use as the potassium salt. The extent to which raltegravir may be dialysable is unknown.
2 years for unopened sachet.
After reconstitution: 30 minutes when stored at or below 30°C.
This medicinal product does not require any special temperature storage conditions. Store in the original package in order to protect from moisture.
For storage conditions after reconstitution of the medicinal product, see section 6.3.
PET/aluminium/LLDPE sachets.
One carton contains 60 sachets, two 1 mL, two 3 mL and two 10 mL oral dosing syringes and 2 mixing cups.
Any unused medicinal product or waste material should be disposed of in accordance with local requirements.
Each single-use sachet contains 100 mg of raltegravir which is to be suspended in 10 mL of water giving a final concentration of 10 mg per mL.
After administration of the required volume, the remaining suspension in the mixing cup cannot be reused and must be discarded.
Parents and/or caregivers should be instructed to read the instructions for use booklet before preparing and administering ISENTRESS granules for oral suspension to paediatric patients.
The dose should be administered orally within 30 minutes of mixing.
Complete details on preparation and administration of the suspension can be found in the instructions for use booklet that is included in the carton.
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