Overview
11 DESCRIPTION Table 4. Description Proprietary Name DIACOMIT Established Name Stiripentol Route of Administration Oral Chemical Name 4,4-dimethyl-1-[3,4-(methylendioxyphenyl)-1-pentene-3-ol Structural Formula Stiripentol is a white to pale yellow crystalline powder with a bitter taste; it is practically insoluble in water (at 25°C), sparingly soluble in chloroform, and soluble in acetone,...
Mechanism of Action
12 CLINICAL PHARMACOLOGY 12.1 Mechanism of Action The mechanism by which DIACOMIT exerts its anticonvulsant effect in humans is unknown. Possible mechanisms of action include direct effects mediated through the gamma-aminobutyric acid (GABA) A receptor and indirect effects involving inhibition of cytochrome P450 activity with resulting increase in blood levels of clobazam and its active metabolite. 12.2 Pharmacodynamics There are no relevant data on the pharmacodynamic effects of DIACOMIT. 12.3 Pharmacokinetics The following pharmacokinetic properties of stiripentol have been found in studies in adult healthy volunteers and adult patients. Systemic exposure of stiripentol increases in a greater than dose proportional manner from 500 mg to 2000 mg.
Indications
- 1 INDICATIONS AND USAGE DIACOMIT is indicated for the treatment of seizures associated with Dravet syndrome (DS) in patients taking clobazam who are 6 months of age and older and weighing 7 kg or more. There are no clinical data to support the use of DIACOMIT as monotherapy in Dravet syndrome. DIACOMIT is indicated for the treatment of seizures associated with Dravet syndrome in patients taking clobazam who are 6 months of age and older and weighing 7 kg or more . There are no clinical data to support the use of DIACOMIT as monotherapy in Dravet syndrome. ( 1 )
Common Doses
- 50 mg
- 16.67 mg
- 25 mg
- 150 mg
Dosage
2 DOSAGE AND ADMINISTRATION The dosage of DIACOMIT is 50 mg/kg/day, administered by mouth in 2 or 3 divided doses, depending on age and weight. ( 2.2 ) Capsules must be swallowed whole with a glass of water during a meal. Capsules should not be broken or opened. ( 2.3 ) Powder for suspension should be mixed in a glass of water and should be taken immediately after mixing during a meal. ( 2.3 ) Reduce dose or discontinue dose gradually. ( 2.5 ) 2.
Contraindications
- 4 CONTRAINDICATIONS None. None ( 4 )
Side Effects
- 6 ADVERSE REACTIONS The following serious or otherwise clinically significant adverse reactions are described elsewhere in the labeling: Somnolence [see Warnings and Precautions (5.1) ] Decreased Appetite and Decreased Weight [see Warnings and Precautions (5.2) ] Neutropenia and Thrombocytopenia [see Warnings and Precautions (5.3) ] Withdrawal Symptoms [see Warnings and Precautions (5.4) ] Risks in Patients with Phenylketonuria [see Warnings and Precautions (5.5) ] Suicidal Behavior and Ideation [see Warnings and Precautions (5.
Interactions
- 7 DRUG INTERACTIONS DIACOMIT increases the plasma concentration of clobazam and its metabolite through metabolic inhibition of CYP3A4 and CYP2C19. Consider dose reduction of clobazam in case of adverse reactions. ( 7.1 ) Substrates of CYP2C8, CYP2C19, P-gp and BCRP may require a dose reduction. (7.1) Substrates of CYP1A2, CYP2B6 and CYP3A4 may require a dose adjustment. ( 7.1 ) Strong inducers of CYP1A2, CYP3A4 or CYP2C19: Consider dose increase of DIACOMIT. ( 7.2 ) 7.