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).
The maximum dose of the chewable tablet is 300 mg twice daily.
Because the formulations have different pharmacokinetic profiles neither the chewable tablets nor the granules for oral suspension should be substituted for the 400 mg tablet or 600 mg tablet (see section 5.2). The chewable tablets and the granules for oral suspension have not been studied in HIV-infected adolescents (12 to 18 years) or adults.
Children at least 11 kg: weight based dose of the chewable tablet to a maximum dose of 300 mg, twice daily as specified in Tables 1 and 2. The chewable tablets are available in 25 mg and scored 100 mg strengths.
See section 5.2 regarding the limited data on which these dose recommendations are based.
Table 1. Recommended Dose* for ISENTRESS Chewable Tablets for Paediatric Patients Weighing at Least 25 kg:
| Body weight (kg) | Dose | Number of chewable tablets |
|---|---|---|
| 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 |
* The weight-based dosing recommendation for the chewable tablet is based on approximately 6 mg/kg/dose twice daily (see section 5.2).
† The 100 mg chewable tablet can be divided into equal 50 mg doses. However, breaking the tablets should be avoided whenever possible.
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 section 5.1).
Table 2. 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.
No data are available in pre-term neonates. The use of ISENTRESS is not recommended in pre-term neonates.
Patients should be instructed to keep scheduled appointments because the ISENTRESS dosage should be adjusted as the child grows.
ISENTRESS is also available in a 400 mg tablet and as granules for oral suspension for use. Refer to the 400 mg tablet and granules for oral suspension SmPCs 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.
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 chewable tablets can be administered with or without food (see section 5.2).
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.
Shelf life: 2 years.
Keep the bottle tightly closed, with the desiccant in order to protect from moisture.
High density polyethylene (HDPE) bottle with a child-resistant polypropylene closure, induction seal and silica gel desiccant: 60 tablets.
No special requirements for disposal.
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