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Stiripentol

Medically reviewed by Drugs.com. Last updated on Oct 2, 2020.

Pronunciation

(stir i PEN tol)

Index Terms

  • BCX 2600
  • Estiripentol

Dosage Forms

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Capsule, Oral:

Diacomit: 250 mg [contains fd&c blue #2 (indigotine)]

Diacomit: 500 mg

Packet, Oral:

Diacomit: 250 mg (60 ea); 500 mg (60 ea) [contains aspartame]

Brand Names: U.S.

  • Diacomit

Pharmacologic Category

  • Anticonvulsant, Miscellaneous

Pharmacology

Precise mechanism behind anticonvulsant effects is unknown. May enhance GABAergic inhibitory neurotransmission by weak partial agonism and/or positive allosteric modulation of gamma-aminobutyric acid (GABA)-A receptors (Fisher 2009). Also inhibits multiple cytochrome P450 isoenzymes involved in the metabolism of other anticonvulsants; concurrent use may increase their systemic exposure and efficacy.

Absorption

Well absorbed; extensive first-pass metabolism (Walker 1995). Maximum concentration obtained with powder for suspension is slightly higher than that observed with capsules (Diacomit prescribing information [Canada 2012]).

Metabolism

Hepatic through demethylenation, primarily by CYP1A2, 2C19, 3A4, and glucuronidation (Moreland 1986)

Excretion

Urine (73%, primarily metabolites); feces (18% as unchanged drug) (Moreland 1986)

Time to Peak

Median: 2 to 3 hours

Half-Life Elimination

Adults: 4.5 to 13 hours (dose-dependent)

Protein Binding

~99% to plasma proteins

Special Populations: Children

In a pharmacokinetic study of children (n=35; median age: 7.3 years) with Dravet syndrome, clearance and volume of distribution were related to body weight and elimination half-life increased from 8.5 hours (10 kg) to 23.5 hours (60 kg). Adolescents may require lower dosing than younger children (May 2012).

Use: Labeled Indications

Dravet syndrome: Adjunctive treatment of refractory generalized tonic-clonic seizures in conjunction with clobazam and valproic acid (off-label) in patients ≥2 years with Dravet syndrome (previously known as severe myoclonic epilepsy in infancy) (Chiron 2000; Wirrell 2016).

Contraindications

There are no contraindications listed in the manufacturer's labeling.

Canadian labeling: Additional contraindications (not in US labeling): Hypersensitivity to stiripentol or any component of the formulation

Dosing: Adult

Note: Not appropriate for monotherapy. The dosage of concomitant clobazam and valproate may need to be adjusted. Systemic exposure is slightly higher with the powder for suspension than that observed with capsules; patient monitoring is recommended when switching between dosage forms (Canadian labeling).

Dravet syndrome (adjunctive therapy): Oral: Usual: 50 mg/kg/day given in 2 or 3 divided doses. Maximum dose: 3 g/day (manufacturer's labeling). Some experts recommend initiating with 25 mg/kg/day and increasing by 10 mg/kg/day every 1 to 2 weeks up to 3 g/day (Andrade 2020).

Dosing: Geriatric

Refer to adult dosing.

Dosing: Pediatric

Note: FDA approved in combination with clobazam; international labeling (European Medicines Agency, Health Canada) recommends combination with clobazam and valproic acid. Other concomitant antiepileptic agents have also been studied (eg, topiramate) and efficacy data are evolving; although, experts suggest avoiding sodium channel blockers (eg, carbamazepine) which may exacerbate seizures (Wirrell 2016). The concomitant dosage of clobazam and/or valproate may need to be adjusted with initiation of stiripentol. Systemic exposure is slightly higher with the powder for suspension than that observed with capsules; patient monitoring is recommended when switching between dosage forms (Diacomit prescribing information [Canada 2012]). Two strengths of powder packets are available (250 mg and 500 mg); may combine the two strengths to achieve the appropriate dosage; ensure appropriate product selection.

Dravet syndrome (adjunctive therapy): Children and Adolescents: Limited data available in children <2 years of age: Oral: 50 mg/kg/day in 2 or 3 divided doses; round dose to nearest available dosage form; maximum daily dose: 3,000 mg/day. Some experts recommend initiating at a lower dosage of 10 to 15 mg/kg/day in divided doses and titrating to initial target dose of 50 mg/kg/day over a 2- to 4-week period (Wirrell 2016). Higher doses were reported in one open-label, multicenter trial of patients with Dravet syndrome (n=23; ages: 1 to 22 years); the initial dose was 50 mg/kg/day in divided doses in patients <20 kg and a fixed dose of 1,000 mg/day in divided doses in patients ≥20 kg; after 4 weeks, dosage was adjusted based on clinical response up to a maximum of 100 mg/kg/day (or 4,000 mg/day) in divided doses. In patients 1 to 8 years (n=15), mean daily dose was 59 mg/kg/day (range: 30 to 100 mg/kg/day) and in patients 13 to 22 years (n=8), mean daily dose was 1,469 mg/day (range: 500 to 3,000 mg/day) (Inoue 2009). Pharmacokinetic modeling studies indicate adolescents may require lower doses of 20 to 30 mg/kg/day (May 2012; Wirrell 2016).

Reconstitution

Mix powder for suspension with a glass of water.

Administration

Oral: Administer in 2 or 3 divided doses daily with a meal. Capsule should be swallowed whole with a glass of water. Do not crush, chew, or open capsule. Powder for suspension should be mixed with a glass of water and consumed immediately. After administering suspension, add a small amount of water (eg, 25 mL) to the dosing cup and drink the entire mixture to be sure there is no medication left in the cup.

Dietary Considerations

Some products may contain phenylalanine; use with caution in patient with phenylketonuria.

Storage

Store at 20°C to 25°C (68°F to 77°F); excursions permitted between 15°C and 30°C (59°F and 86°F). Store in original package. Protect from light. Powder for suspension should be consumed immediately after reconstitution and not stored.

Drug Interactions

Abametapir: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Avoid combination

Agomelatine: CYP1A2 Inhibitors (Moderate) may increase the serum concentration of Agomelatine. Monitor therapy

Alcohol (Ethyl): Stiripentol may enhance the sedative effect of Alcohol (Ethyl). Avoid combination

Alizapride: May enhance the CNS depressant effect of CNS Depressants. Monitor therapy

Alosetron: CYP1A2 Inhibitors (Moderate) may increase the serum concentration of Alosetron. Management: Avoid concomitant use of alosetron and moderate CYP1A2 inhibitors whenever possible. If combined use is necessary, monitor for increased alosetron effects/toxicities. Consider therapy modification

Azelastine (Nasal): CNS Depressants may enhance the CNS depressant effect of Azelastine (Nasal). Avoid combination

Bendamustine: CYP1A2 Inhibitors (Moderate) may increase the serum concentration of Bendamustine. Management: Consider alternatives to moderate CYP1A2 inhibitors during therapy with bendamustine due to the potential for increased bendamustine plasma concentrations and increased bendamustine toxicity. Consider therapy modification

Blonanserin: CNS Depressants may enhance the CNS depressant effect of Blonanserin. Management: Use caution if coadministering blonanserin and CNS depressants; dose reduction of the other CNS depressant may be required. Strong CNS depressants should not be coadministered with blonanserin. Consider therapy modification

Brexanolone: CNS Depressants may enhance the CNS depressant effect of Brexanolone. Monitor therapy

Brimonidine (Topical): May enhance the CNS depressant effect of CNS Depressants. Monitor therapy

Brivaracetam: CYP2C19 Inhibitors (Moderate) may increase the serum concentration of Brivaracetam. Monitor therapy

Bromazepam: CYP1A2 Inhibitors (Moderate) may increase the serum concentration of Bromazepam. Monitor therapy

Bromopride: May enhance the CNS depressant effect of CNS Depressants. Monitor therapy

Bromperidol: May enhance the CNS depressant effect of CNS Depressants. Avoid combination

Buprenorphine: CNS Depressants may enhance the CNS depressant effect of Buprenorphine. Management: Consider reduced doses of other CNS depressants, and avoiding such drugs in patients at high risk of buprenorphine overuse/self-injection. Initiate buprenorphine at lower doses in patients already receiving CNS depressants. Consider therapy modification

Caffeine and Caffeine Containing Products: Stiripentol may increase the serum concentration of Caffeine and Caffeine Containing Products. Avoid combination

Cannabidiol: Stiripentol may increase the serum concentration of Cannabidiol. Cannabidiol may increase the serum concentration of Stiripentol. Monitor therapy

Cannabis: May enhance the CNS depressant effect of CNS Depressants. Monitor therapy

CarBAMazepine: Stiripentol may increase the serum concentration of CarBAMazepine. Avoid combination

Carisoprodol: CYP2C19 Inhibitors (Moderate) may decrease serum concentrations of the active metabolite(s) of Carisoprodol. CYP2C19 Inhibitors (Moderate) may increase the serum concentration of Carisoprodol. Monitor therapy

Chlormethiazole: May enhance the CNS depressant effect of CNS Depressants. Management: Monitor closely for evidence of excessive CNS depression. The chlormethiazole labeling states that an appropriately reduced dose should be used if such a combination must be used. Consider therapy modification

Chlorphenesin Carbamate: May enhance the adverse/toxic effect of CNS Depressants. Monitor therapy

Cilostazol: CYP2C19 Inhibitors (Moderate) may increase serum concentrations of the active metabolite(s) of Cilostazol. CYP2C19 Inhibitors (Moderate) may increase the serum concentration of Cilostazol. Management: Reduce the cilostazol dose to 50 mg twice daily in patients who are also receiving moderate inhibitors of CYP2C19. Monitor clinical response to cilostazol closely. Consider therapy modification

Citalopram: CYP2C19 Inhibitors (Moderate) may increase the serum concentration of Citalopram. Management: Limit citalopram dose to a maximum of 20 mg/day if used with a moderate CYP2C19 inhibitor. Patients using this combination should be monitored closely for evidence of citalopram toxicity (eg, serotonin syndrome, QT prolongation). Consider therapy modification

CloBAZam: CYP2C19 Inhibitors (Moderate) may increase serum concentrations of the active metabolite(s) of CloBAZam. CYP2C19 Inhibitors (Moderate) may increase the serum concentration of CloBAZam. Monitor therapy

Clofazimine: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Monitor therapy

ClomiPRAMINE: CYP1A2 Inhibitors (Moderate) may increase the serum concentration of ClomiPRAMINE. Monitor therapy

Clopidogrel: CYP2C19 Inhibitors (Moderate) may decrease serum concentrations of the active metabolite(s) of Clopidogrel. Monitor therapy

CloZAPine: CYP1A2 Inhibitors (Moderate) may increase the serum concentration of CloZAPine. Monitor therapy

CNS Depressants: May enhance the adverse/toxic effect of other CNS Depressants. Monitor therapy

Conivaptan: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Avoid combination

CYP3A4 Inducers (Moderate): May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Monitor therapy

CYP3A4 Inducers (Strong): May increase the metabolism of CYP3A4 Substrates (High risk with Inducers). Management: Consider an alternative for one of the interacting drugs. Some combinations may be specifically contraindicated. Consult appropriate manufacturer labeling. Consider therapy modification

CYP3A4 Inhibitors (Moderate): May decrease the metabolism of CYP3A4 Substrates (High risk with Inhibitors). Monitor therapy

CYP3A4 Inhibitors (Strong): May decrease the metabolism of CYP3A4 Substrates (High risk with Inhibitors). Management: Consider avoiding this combination. Some combinations are specifically contraindicated by manufacturers; others may have recommended dose adjustments. If combined, monitor for increased substrate effects. Consider therapy modification

CYP3A4 Substrates (High risk with Inhibitors): Stiripentol may increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Management: Use of stiripentol with CYP3A4 substrates that are considered to have a narrow therapeutic index should be avoided due to the increased risk for adverse effects and toxicity. Any CYP3A4 substrate used with stiripentol requires closer monitoring. Consider therapy modification

Dabrafenib: May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Management: Seek alternatives to the CYP3A4 substrate when possible. If concomitant therapy cannot be avoided, monitor clinical effects of the substrate closely (particularly therapeutic effects). Consider therapy modification

Deferasirox: May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Monitor therapy

Dexlansoprazole: CYP2C19 Inhibitors (Moderate) may increase the serum concentration of Dexlansoprazole. Monitor therapy

Dimethindene (Topical): May enhance the CNS depressant effect of CNS Depressants. Monitor therapy

Doxylamine: May enhance the CNS depressant effect of CNS Depressants. Management: The manufacturer of Diclegis (doxylamine/pyridoxine), intended for use in pregnancy, specifically states that use with other CNS depressants is not recommended. Monitor therapy

Dronabinol: May enhance the CNS depressant effect of CNS Depressants. Monitor therapy

Droperidol: May enhance the CNS depressant effect of CNS Depressants. Management: Consider dose reductions of droperidol or of other CNS agents (eg, opioids, barbiturates) with concomitant use. Exceptions to this monograph are discussed in further detail in separate drug interaction monographs. Consider therapy modification

DULoxetine: CYP1A2 Inhibitors (Moderate) may increase the serum concentration of DULoxetine. Monitor therapy

Enzalutamide: May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Management: Concurrent use of enzalutamide with CYP3A4 substrates that have a narrow therapeutic index should be avoided. Use of enzalutamide and any other CYP3A4 substrate should be performed with caution and close monitoring. Consider therapy modification

Escitalopram: CYP2C19 Inhibitors (Moderate) may increase the serum concentration of Escitalopram. Monitor therapy

Esketamine: May enhance the CNS depressant effect of CNS Depressants. Monitor therapy

Etravirine: CYP2C19 Inhibitors (Moderate) may increase the serum concentration of Etravirine. Monitor therapy

Fenfluramine: Stiripentol may increase the serum concentration of Fenfluramine. Management: Limit the fenfluramine dose to a maximum daily dosage of 0.2 mg/kg twice daily (17 mg/day) when used in combination with stiripentol and clobazam. Consider therapy modification

Flunitrazepam: CNS Depressants may enhance the CNS depressant effect of Flunitrazepam. Management: Reduce the dose of CNS depressants when combined with flunitrazepam and monitor patients for evidence of CNS depression (eg, sedation, respiratory depression). Use non-CNS depressant alternatives when available. Consider therapy modification

Fosnetupitant: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Monitor therapy

Fosphenytoin-Phenytoin: May decrease the serum concentration of Stiripentol. Stiripentol may increase the serum concentration of Fosphenytoin-Phenytoin. Management: Avoid this combination when possible. If combined, monitor for decreased stiripentol concentrations and effects and monitor for increased phenytoin concentrations and effects. Dose adjustments of either medication may be needed. Consider therapy modification

Fusidic Acid (Systemic): May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Avoid combination

HydrOXYzine: May enhance the CNS depressant effect of CNS Depressants. Monitor therapy

Idelalisib: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Avoid combination

Kava Kava: May enhance the adverse/toxic effect of CNS Depressants. Monitor therapy

Lansoprazole: CYP2C19 Inhibitors (Moderate) may increase the serum concentration of Lansoprazole. Monitor therapy

Lemborexant: May enhance the CNS depressant effect of CNS Depressants. Management: Dosage adjustments of lemborexant and of concomitant CNS depressants may be necessary when administered together because of potentially additive CNS depressant effects. Close monitoring for CNS depressant effects is necessary. Consider therapy modification

Lisuride: May enhance the CNS depressant effect of CNS Depressants. Monitor therapy

Lofexidine: May enhance the CNS depressant effect of CNS Depressants. Management: Drugs listed as exceptions to this monograph are discussed in further detail in separate drug interaction monographs. Monitor therapy

Magnesium Sulfate: May enhance the CNS depressant effect of CNS Depressants. Monitor therapy

Mefloquine: May diminish the therapeutic effect of Anticonvulsants. Mefloquine may decrease the serum concentration of Anticonvulsants. Management: Mefloquine is contraindicated for malaria prophylaxis in persons with a history of convulsions. If anticonvulsants are being used for another indication, monitor anticonvulsant concentrations and treatment response closely with concurrent use. Consider therapy modification

Melatonin: CYP1A2 Inhibitors (Moderate) may increase the serum concentration of Melatonin. Monitor therapy

Methotrimeprazine: May enhance the CNS depressant effect of CNS Depressants. CNS Depressants may enhance the CNS depressant effect of Methotrimeprazine. Management: Reduce the usual dose of CNS depressants by 50% if starting methotrimeprazine until the dose of methotrimeprazine is stable. Monitor patient closely for evidence of CNS depression. Consider therapy modification

Metoclopramide: May enhance the CNS depressant effect of CNS Depressants. Monitor therapy

MetyroSINE: CNS Depressants may enhance the sedative effect of MetyroSINE. Monitor therapy

Mianserin: May diminish the therapeutic effect of Anticonvulsants. Monitor therapy

MiFEPRIStone: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Management: Minimize doses of CYP3A4 substrates, and monitor for increased concentrations/toxicity, during and 2 weeks following treatment with mifepristone. Avoid cyclosporine, dihydroergotamine, ergotamine, fentanyl, pimozide, quinidine, sirolimus, and tacrolimus. Consider therapy modification

Minocycline (Systemic): May enhance the CNS depressant effect of CNS Depressants. Monitor therapy

Mitotane: May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Management: Doses of CYP3A4 substrates may need to be adjusted substantially when used in patients being treated with mitotane. Consider therapy modification

Moclobemide: CYP2C19 Inhibitors (Moderate) may increase the serum concentration of Moclobemide. Monitor therapy

Nabilone: May enhance the CNS depressant effect of CNS Depressants. Monitor therapy

Netupitant: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Monitor therapy

OLANZapine: CYP1A2 Inhibitors (Moderate) may increase the serum concentration of OLANZapine. Monitor therapy

Omeprazole: CYP2C19 Inhibitors (Moderate) may increase the serum concentration of Omeprazole. Monitor therapy

Opioid Agonists: CNS Depressants may enhance the CNS depressant effect of Opioid Agonists. Management: Avoid concomitant use of opioid agonists and benzodiazepines or other CNS depressants when possible. These agents should only be combined if alternative treatment options are inadequate. If combined, limit the dosages and duration of each drug. Consider therapy modification

Orlistat: May decrease the serum concentration of Anticonvulsants. Monitor therapy

Orphenadrine: CNS Depressants may enhance the CNS depressant effect of Orphenadrine. Avoid combination

Oxomemazine: May enhance the CNS depressant effect of CNS Depressants. Avoid combination

Oxybate Salt Products: CNS Depressants may enhance the CNS depressant effect of Oxybate Salt Products. Management: Consider alternatives to this combination when possible. If combined, dose reduction or discontinuation of one or more CNS depressants (including the oxybate salt product) should be considered. Interupt oxybate salt treatment during short-term opioid use. Consider therapy modification

OxyCODONE: CNS Depressants may enhance the CNS depressant effect of OxyCODONE. Management: Avoid concomitant use of oxycodone and benzodiazepines or other CNS depressants when possible. These agents should only be combined if alternative treatment options are inadequate. If combined, limit the dosages and duration of each drug. Consider therapy modification

Paraldehyde: CNS Depressants may enhance the CNS depressant effect of Paraldehyde. Avoid combination

Pentoxifylline: CYP1A2 Inhibitors (Moderate) may increase the serum concentration of Pentoxifylline. Monitor therapy

Perampanel: May enhance the CNS depressant effect of CNS Depressants. Management: Patients taking perampanel with any other drug that has CNS depressant activities should avoid complex and high-risk activities, particularly those such as driving that require alertness and coordination, until they have experience using the combination. Consider therapy modification

PHENobarbital: May decrease the serum concentration of Stiripentol. Avoid combination

Pirfenidone: CYP1A2 Inhibitors (Moderate) may increase the serum concentration of Pirfenidone. Management: Avoid concomitant use of pirfenidone and moderate CYP1A2 inhibitors whenever possible. If combined, decrease the pirfenidone dose to 1,602 mg per day (534 mg three times daily) and monitor for increased pirfenidone toxicities. Consider therapy modification

Piribedil: CNS Depressants may enhance the CNS depressant effect of Piribedil. Monitor therapy

Pomalidomide: CYP1A2 Inhibitors (Moderate) may increase the serum concentration of Pomalidomide. Monitor therapy

Pramipexole: CNS Depressants may enhance the sedative effect of Pramipexole. Monitor therapy

Proguanil: CYP2C19 Inhibitors (Moderate) may decrease serum concentrations of the active metabolite(s) of Proguanil. CYP2C19 Inhibitors (Moderate) may increase the serum concentration of Proguanil. Monitor therapy

Propranolol: CYP1A2 Inhibitors (Moderate) may increase the serum concentration of Propranolol. Monitor therapy

Ramelteon: CYP1A2 Inhibitors (Moderate) may increase the serum concentration of Ramelteon. Monitor therapy

Ramosetron: CYP1A2 Inhibitors (Moderate) may increase the serum concentration of Ramosetron. Monitor therapy

Rasagiline: CYP1A2 Inhibitors (Moderate) may increase the serum concentration of Rasagiline. Management: Limit rasagiline dose to 0.5 mg once daily in patients taking moderate CYP1A2 inhibitors. Consider therapy modification

ROPINIRole: CNS Depressants may enhance the sedative effect of ROPINIRole. Monitor therapy

ROPINIRole: CYP1A2 Inhibitors (Moderate) may increase the serum concentration of ROPINIRole. Monitor therapy

Ropivacaine: CYP1A2 Inhibitors (Moderate) may increase the serum concentration of Ropivacaine. Monitor therapy

Rotigotine: CNS Depressants may enhance the sedative effect of Rotigotine. Monitor therapy

Rufinamide: May enhance the adverse/toxic effect of CNS Depressants. Specifically, sleepiness and dizziness may be enhanced. Monitor therapy

Sarilumab: May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Monitor therapy

Siltuximab: May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Monitor therapy

Suvorexant: CNS Depressants may enhance the CNS depressant effect of Suvorexant. Management: Dose reduction of suvorexant and/or any other CNS depressant may be necessary. Use of suvorexant with alcohol is not recommended, and the use of suvorexant with any other drug to treat insomnia is not recommended. Consider therapy modification

Tasimelteon: CYP1A2 Inhibitors (Moderate) may increase the serum concentration of Tasimelteon. Monitor therapy

Tetrahydrocannabinol: May enhance the CNS depressant effect of CNS Depressants. Monitor therapy

Tetrahydrocannabinol and Cannabidiol: May enhance the CNS depressant effect of CNS Depressants. Monitor therapy

Thalidomide: CNS Depressants may enhance the CNS depressant effect of Thalidomide. Avoid combination

Theophylline Derivatives: CYP1A2 Inhibitors (Moderate) may increase the serum concentration of Theophylline Derivatives. Management: Consider avoidance of this combination. If coadministration is necessary, monitor for increased theophylline serum concentrations and toxicities when combined. Theophylline dose reductions will likely be required. Exceptions: Dyphylline. Consider therapy modification

TiZANidine: CYP1A2 Inhibitors (Moderate) may increase the serum concentration of TiZANidine. Management: If combined use cannot be avoided, initiate tizanidine in adults at 2 mg and increase in 2 to 4 mg increments based on patient response. Monitor for increased effects of tizanidine, including adverse reactions. Consider therapy modification

Tocilizumab: May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Monitor therapy

Trimeprazine: May enhance the CNS depressant effect of CNS Depressants. Monitor therapy

Zolpidem: CNS Depressants may enhance the CNS depressant effect of Zolpidem. Management: Reduce the Intermezzo brand sublingual zolpidem adult dose to 1.75 mg for men who are also receiving other CNS depressants. No such dose change is recommended for women. Avoid use with other CNS depressants at bedtime; avoid use with alcohol. Consider therapy modification

Adverse Reactions

Note: Adverse reactions reported with combination (clobazam) therapy.

>10%:

Central nervous system: Drowsiness (67%), agitation (27%), ataxia (27%), hypotonia (18% to 24%), dysarthria (12%), insomnia (12%)

Endocrine & metabolic: Weight loss (27%)

Gastrointestinal: Decreased appetite (45% to 46%), nausea (15%)

Hematologic & oncologic: Decreased platelet count (13%), neutropenia (13%)

Neuromuscular & skeletal: Tremor (15%)

1% to 10%:

Central nervous system: Aggressive behavior (9%), fatigue (9%)

Endocrine & metabolic: Weight gain (6%)

Gastrointestinal: Vomiting (9%), sialorrhea (6%)

Respiratory: Bronchitis (6%), nasopharyngitis (6%)

Miscellaneous: Fever (6%)

Warnings/Precautions

Concerns related to adverse effects:

• Appetite/weight loss: Loss of appetite and weight loss have been observed in 46% and 27% of patients (mean age: 9.2 years), respectively, during clinical trials; monitor the growth rate of pediatric patients closely. Valproate dose reduction by 30% may help minimize appetite and weight loss.

• Blood dyscrasias: Neutropenia and thrombocytopenia have been observed in clinical trials; monitor CBC during therapy.

• CNS depression: May cause CNS depression (eg, drowsiness, sleepiness) and impair physical or mental abilities; patients must be cautioned about performing tasks that require mental alertness (eg, operating machinery or driving). If CNS depression occurs during co-administration with clobazam, consider dosage adjustment of clobazam and/or other concomitant antiseizure drugs.

• Suicidal ideation: Pooled analysis of trials involving various antiepileptics (regardless of indication) showed an increased risk of suicidal thoughts/behavior (incidence rate: 0.43% treated patients compared to 0.24% of patients receiving placebo); risk observed as early as 1 week after initiation and continued through duration of trials (most trials ≤24 weeks). Monitor all patients for notable changes in behavior that might indicate suicidal thoughts or depression; notify health care provider immediately if symptoms occur.

Disease-related concerns:

• Hepatic impairment: Use with caution in patients with mild impairment; primarily undergoes hepatic metabolism. Avoid use in patients with moderate to severe hepatic impairment.

• Renal impairment: Use with caution in patients with mild impairment; elimination of metabolites is primarily renal. Avoid use in patients with moderate to severe renal impairment.

Concurrent drug therapy issues:

• Drug-drug interactions: Potentially significant interactions may exist, requiring dose or frequency adjustment, additional monitoring, and/or selection of alternative therapy. Consult drug interactions database for more detailed information.

Dosage form specific issues:

• Powder for suspension: Systemic exposure is slightly higher with the powder for suspension than that observed with capsules; may consider patient monitoring when switching between dosage forms. Powder for suspension contains phenylalanine; use caution in patients with phenylketonuria.

Other warnings:

• Appropriate use: Must be used in conjunction with clobazam (labeled use) and valproate (off-label use) (Chiron 2000; Wirrell 2016); not approved for use as monotherapy.

• Withdrawal: Anticonvulsants should not be discontinued abruptly because of the possibility of increasing seizure frequency; therapy should be withdrawn gradually (over at least 1 month) to minimize the potential of increased seizure frequency, unless safety concerns require a more rapid withdrawal.

Monitoring Parameters

CBC (prior to initiation and every 6 months or as clinically indicated thereafter); weight; growth rate in children.

Pregnancy Considerations

Adverse events have been observed in animal reproduction studies. Information related to the use of stiripentol in pregnancy has not been located (de Jong 2016).

Stiripentol is used in combination with clobazam or valproic acid (off-label); refer to individual monographs for additional information.

Data collection to monitor pregnancy and infant outcomes following exposure to stiripentol is ongoing. Patients may enroll themselves in the North American Antiepileptic Drug (NAAED) Pregnancy Registry (1-888-233-2334 or http://www.aedpregnancyregistry.org).

Patient Education

What is this drug used for?

• It is used to help control certain kinds of seizures.

All drugs may cause side effects. However, many people have no side effects or only have minor side effects. Call your doctor or get medical help if any of these side effects or any other side effects bother you or do not go away:

• Dizziness

• Fatigue

• Lack of appetite

• Weight gain

• Weight loss

• Nausea

• Vomiting

• Trouble sleeping

• Increased saliva

• Stuffy nose

• Sore throat

WARNING/CAUTION: Even though it may be rare, some people may have very bad and sometimes deadly side effects when taking a drug. Tell your doctor or get medical help right away if you have any of the following signs or symptoms that may be related to a very bad side effect:

• Agitation

• Sensing things that seem real but are not

• Tremors

• Decreased muscle tone

• Trouble controlling movements

• Twitching

• Change in balance

• Trouble swallowing

• Trouble speaking

• Severe loss of strength and energy

• Bruising

• Bleeding

• Irritability

• Panic attacks

• Mood changes

• Depression like thoughts of suicide, anxiety, emotional instability, or confusion

• Infection

• Signs of an allergic reaction, like rash; hives; itching; red, swollen, blistered, or peeling skin with or without fever; wheezing; tightness in the chest or throat; trouble breathing, swallowing, or talking; unusual hoarseness; or swelling of the mouth, face, lips, tongue, or throat.

Note: This is not a comprehensive list of all side effects. Talk to your doctor if you have questions.

Consumer Information Use and Disclaimer: This information should not be used to decide whether or not to take this medicine or any other medicine. Only the healthcare provider has the knowledge and training to decide which medicines are right for a specific patient. This information does not endorse any medicine as safe, effective, or approved for treating any patient or health condition. This is only a limited summary of general information about the medicine's uses from the patient education leaflet and is not intended to be comprehensive. This limited summary does NOT include all information available about the possible uses, directions, warnings, precautions, interactions, adverse effects, or risks that may apply to this medicine. This information is not intended to provide medical advice, diagnosis or treatment and does not replace information you receive from the healthcare provider. For a more detailed summary of information about the risks and benefits of using this medicine, please speak with your healthcare provider and review the entire patient education leaflet.

Further information

Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.

Related questions