stiripentol

Absorption: 30% absorbed; undergoes extensive first-pass metabolism.

Distribution: Unknown.

Protein Binding: 99%.

Metabolism/Excretion: Primarily metabolized in liver via CYP1A2, CYP2C19, and CYP3A4 isoenzymes. Primarily excreted by the kidneys (73%, primarily as metabolites); 18% excreted in feces as unchanged drug.

Half-Life: 4.5–13 hr.

Time/Action Profile ⬆ ⬇

(plasma concentrations)

ROUTE	ONSET	PEAK	DURATION
PO	unknown	2–3 hr	8–12 hr

Contraind./Precautions ⬆ ⬇

Contraindicated in:

Moderate or severe renal impairment;
Moderate or severe hepatic impairment.

Use Cautiously in:

All patients (may ↑ risk of suicidal thoughts/behaviors);
Phenylketonuria (powder contains phenylalanine);
OB: Use during pregnancy only if potential maternal benefits outweigh potential fetal risks;
Lactation: Use while breastfeeding only if potential maternal benefits outweigh potential risks to infant;
Pedi: Children <6 mo (safety and effectiveness not established); may hinder growth in children;
Geri: Older adults may have ↑ sensitivity to effects due to age-related decline in hepatic and/or renal function.

Adv. Reactions/Side Effects ⬆ ⬇

CNS: SUICIDAL THOUGHTS/BEHAVIORS, agitation, dysarthria, insomnia, sedation, aggression

EENT: nasopharyngitis

GI: nausea, ↑salivation, vomiting

Hemat: neutropenia, thrombocytopenia

Metab: ↓appetite, weight loss, ↓growth (in children), ↑weight

MS: hypotonia

Neuro: ataxia, tremor

Resp: bronchitis

Misc: fatigue, fever

Interactions ⬆ ⬇

Drug-drug:

May ↑ concentrations of clobazam and its active metabolite; if excessive sedation, consider ↓ clobazam dose by 25%.
May ↑ or ↓ levels of CYP1A2 substrates, including theophylline and caffeine.
May ↑ or ↓ levels of CYP2B6 substrates, including sertraline and thiotepa.
May ↑ or ↓ levels of CYP3A4 substrates, including midazolam, triazolam, and quinidine.
May ↑ levels and risk of toxicity of CYP2C19 substrates, including diazepam and clopidogrel; consider ↓ dose of CYP2C19 substrate.
May ↑ levels and risk of toxicity of P-glycoprotein (P-gp) substrates, including carbamazepine; consider ↓ dose of P-gp substrate.
May ↑ levels and risk of toxicity of breast cancer resistance protein (BCRP) substrates, including methotrexate, prazosin, and glyburide; consider ↓ dose of BCRP substrate.
CYP1A2 inducers, CYP2C19 inducers, and CYP3A4 inducers, including carbamazepine, rifampin, phenobarbital, and phenytoin, may ↓ levels and effectiveness; avoid concurrent use.
Additive CNS depression with other CNS depressants, including alcohol, antihistamines, antidepressants, opioids, and sedative/hypnotics.

Route/Dosage ⬆ ⬇

PO (Adults and Children ≥1 yr and ≥10 kg): 16.67 mg/kg 3 times daily (max dose = 3000 mg/day) or 25 mg/kg twice daily (max dose = 3000 mg/day).
PO (Children ≥1 yr and 7–<10 kg): 25 mg/kg twice daily.
PO (Children 6 mo–<1 yr and ≥7 kg): 25 mg/kg twice daily.

Availability ⬆ ⬇

Capsules: 250 mg; 500 mg
Powder for oral suspension fruit flavor: 250 mg/pkt (contains 1.4 mg phenylalanine); 500 mg/pkt (contains 2.8 mg phenylalanine)

Assessment ⬆ ⬇

Monitor frequency of seizure activity. Institute seizure precautions.
Pedi: Carefully monitor the growth, appetite, and weight of pediatric patients.
Monitor for somnolence; dose adjustments may be necessary. Consider ↓ the initial dose of coadministered clobazam by 25%, with an additional 25% ↓ if somnolence persists. Also, adjust the doses of other concurrent anticonvulsant drugs with sedating properties.
Monitor for the emergence or worsening of depression, suicidal thoughts or behavior, and any unusual changes in mood or behavior. Assess mental status (orientation, mood, behavior) before and periodically during therapy. Assess for suicidal tendencies. Restrict amount of drug available to patient.

Lab Test Considerations:

Obtain CBC with differential prior to initiation and every 6 mo thereafter; may cause neutropenia and thrombocytopenia.

Implementation ⬆ ⬇

PO: Administer during a meal. Give capsules whole with a glass of water. DNC: Do not open or crush capsules. Mix suspension with a glass of water (100 mL) and consume immediately after mixing. Add a small amount of water (25 mL) to the drinking cup and have patient drink all the remaining mixture to ensure no medicine is left in the glass.
Discontinue gradually to minimize the risk of seizures and status epilepticus; monitor closely if abrupt withdrawal is necessary.

Patient/Family Teaching ⬆ ⬇

Explain purpose and side effects of stiripentol to patient. Advise patient to take whole capsules or suspension as directed with water during a meal. Take missed dose as soon as possible; if it is almost time for the next dose, the missed dose should not be taken, and the next scheduled dose should be taken as usual. Do not double dose. Do not stop receiving drug without consulting health care professional. Advise patient to read Patient Information before starting therapy.
Emphasize the importance of routine follow-up exams and lab studies as indicated.
Medication may cause drowsiness and dizziness. Caution patient to avoid driving or other activities requiring alertness until response to medication is known.
Advise patient and caregiver against sudden discontinuation of drug due to potential for seizure recurrence.
May cause depression or suicide. Instruct patients and caregivers to monitor for emergence of suicidal thoughts and behaviors. Notify health care professional immediately if suicidal thoughts; new or worsening depression; anxiety; changes in behavior or mood; thoughts of suicide, dying, or hurting self; or acting on dangerous impulses occur. Instruct patient to carry wallet card and to call the National Suicide Prevention Lifeline at 1-800-273-8255 or visit www.988lifeline.org if they experience suicidal thoughts.
Advise patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and to consult health care professional before taking other medications.
Advise patients with phenylketonuria to consider combined daily amount of phenylalanine from all sources while taking stiripentol.
Advise patient to avoid alcohol during treatment.
Rep: May cause fetal harm. Advise patient to notify health care professional if pregnancy is planned or suspected or if breastfeeding. Encourage women who become pregnant while taking stiripentol to enroll in the North American Antiepileptic Drug (NAAED) Pregnancy Registry at 1-888-233-2334 or visit http://www.aedpregnancyregistry.org.

Evaluation/Desired Outcomes ⬆ ⬇

Reduction in generalized clonic or tonic-clonic seizures.

US Brand Names ⬆ ⬇

Code ⬆

NDC Code

42765- Metrochem API Private Limited
- 42765-058-
  - 42765-058-15- 15 kg in 1 DRUM (42765-058-15)

58159- NURAY CHEMICALS PRIVATE LIMITED
- 58159-069-
  - 58159-069-01- 35 kg in 1 DRUM (58159-069-01)

58159- NURAY CHEMICALS PRIVATE LIMITED
- 58159-069-
  - 58159-069-02- 20 kg in 1 DRUM (58159-069-02)

58159- NURAY CHEMICALS PRIVATE LIMITED
- 58159-069-
  58159-069-03- 15 kg in 1 DRUM (58159-069-03)

58159- NURAY CHEMICALS PRIVATE LIMITED
- 58159-069-
  58159-069-04- 10 kg in 1 DRUM (58159-069-04)

58159- NURAY CHEMICALS PRIVATE LIMITED
- 58159-069-
  58159-069-05- 5 kg in 1 DRUM (58159-069-05)

68418- BIOCODEX, INC.
- 68418-7939- Diacomit
  68418-7939-6- 1 BOTTLE in 1 CARTON (68418-7939-6) / 60 CAPSULE in 1 BOTTLE

68418- BIOCODEX, INC.
- 68418-7940- Diacomit
  - 68418-7940-6- 1 BOTTLE in 1 CARTON (68418-7940-6) / 60 CAPSULE in 1 BOTTLE

68418- BIOCODEX, INC.
- 68418-7941- Diacomit
  - 68418-7941-6- 60 PACKET in 1 CARTON (68418-7941-6) / 1 POWDER, FOR SUSPENSION in 1 PACKET

68418- BIOCODEX, INC.
- 68418-7942- Diacomit
  - 68418-7942-6- 60 PACKET in 1 CARTON (68418-7942-6) / 1 POWDER, FOR SUSPENSION in 1 PACKET

69766- MSN Life Sciences Private Limited
- 69766-075-
  - 69766-075-01- 50 kg in 1 DRUM (69766-075-01)

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Pronunciation ⬇

Classifications ⬆ ⬇

Indications ⬆ ⬇

Action ⬆ ⬇

Pharmacokinetics ⬆ ⬇