NationMaster - Encyclopedia: Stiripentol

Stiripentol (marketed as Diacomit by Laboratoires BIOCODEX) is an anticonvulsant drug used in the treatment of epilepsy. The regulation of therapeutic goods, that is drugs and therapeutic devices, varies by jurisdiction. ... In pharmacology and toxicology, a route of administration is the path by which a drug, fluid, poison or other substance is brought into contact with the body. ... The anticonvulsants, sometimes also called antiepileptics, belong to a diverse group of pharmaceuticals used in prevention of the occurrence of epileptic seizures. ...

It is unrelated to other anticonvulsants and belongs to the group of aromatic allylic alcohols. In chemistry, an aromatic molecule is one in which electrons are free to cycle around circular arrangements of atoms, which are alternately singly and doubly bonded to one another. ... An allyl group is an alkene hydrocarbon group with the formula H2C=CH-CH2-. It is made up of a vinyl group, CH2=CH-, attached to a methylene -CH2. ... In general usage, alcohol (from Arabic al-khwl الكحول, or al-ghawl الغول) refers almost always to ethanol, also known as grain alcohol, and often to any beverage that contains ethanol (see alcoholic beverage). ...

Mechanism of action

As with most anticonvulsants, the precise mechanism is unknown. It has been shown to have anticonvulsant effects on its own. It can prevent the reuptake of GABA and inhibit its metabolism. Gaba may refer to: GabÃ¢ or gabaa (Philippines), the concept of negative karma of the Cebuano people GABA, the gamma-amino-butyric acid neurotransmitter GABA receptor, in biology, receptors with GABA as their endogenous ligand Gaba 1 to 1, an English conversational school in Japan Marianne Gaba, a US model... Structure of the coenzyme adenosine triphosphate, a central intermediate in energy metabolism. ...

It also improves the effectiveness of many other anticonvulsants, possibly due to it inhibiting certain enzymes. This slows the drug's metabolism, increasing blood plasma levels. Blood plasma is the liquid component of blood, in which the blood cells are suspended. ...

Approval history

E.M.E.A approval

Diacomit is indicated for use in conjunction with clobazam and valproate as adjunctive therapy of refractory generalized tonic-clonic seizures in patients with severe myoclonic epilepsy in infancy (SMEI, Dravet's syndrome) whose seizures are not adequately controlled with clobazam and valproate.

Myoclonic seizures are brief twitches or jerks of muscles or groups of muscles. ...

Indications and usage

It is indicated as an adjunctive therapy with sodium valproate and clobazam for treating severe myoclonic epilepsy in infancy (SMEI, also know as Dravet's syndrome). Children with SMEI develop often intractable seizures during their first year of life and mental retardation follows. Small-scale trials have show remarkably high response rates, with a significant minority of those treated becoming seizure free. Sodium valproate (INN) or valproate sodium (USAN) is the sodium salt of valproic acid and is an anticonvulsant used in the treatment of epilepsy. ... Clobazam is triazolobenzodiazepine, also known as a 1,5-benzodiazepine, meaning that its diazepine ring has its nitrogen atoms at the 1 and 5 positions instead of the usual 1 and 4. ... Generalized epilepsy with febrile seizures plus (GEFS+) is a syndromic autosomal dominant disorder where afflicted individuals can exhibit numerous epilepsy phenotypes. ... Generalized epilepsy with febrile seizures plus (GEFS+) is a syndromic autosomal dominant disorder where afflicted individuals can exhibit numerous epilepsy phenotypes. ... Mental retardation is a term for a pattern of persistently slow learning of basic motor and language skills (milestones) during childhood, and a significantly below-normal global intellectual capacity as an adult. ...

In addition, it may be used to treat refractory childhood epilepsy in conjunction with carbamazepine. It appears to be less effective in adolescents and adults.

Dosing

Stiripentol is available as a gelatine capsule (250mg, 500mg) and as a sachet of powder to make a drinkable suspension (250mg, 500mg).

Initial dose is 50 mg/kg per day. This may be increased up to 100 mg/kg per day, with a maximum of 4g. The dose to be divided into two or three with meals. The does of other anticonvulsants may have to be reduced (possibly up to 50%).

Side effects

Side effects are largely due to the increase in plasma concentrations of other anticonvulsants and can be reduced by lowering the does of those drugs. Nausea and vomiting are particularly noted when used in combination with sodium valproate.

Drug interactions

Stiripentol inhibits several cytochrome P450 isoenzymes and so interacts with many anticonvulsants and other medicines. This is both a strength and weakness. It appears to increase the potency of phenobarbital, primidone, phenytoin, carbamazepine, clobazam and diazepam. For example, blood levels of carbamazepine can be maintained whist reducing the dose by 50%. Cytochrome P450 Oxidase (CYP2E1) Cytochrome P450 oxidase (commonly abbreviated CYP) is a generic term for a large number of related, but distinct, oxidative enzymes (EC 1. ... Isozymes, (or isoenzymes) are isoforms (closely related variants) of enzymes. ... Phenobarbital (INN) or phenobarbitone (former BAN) is a barbiturate, first marketed as Luminal by Farbwerke Fr. ... Primidone is an anticonvulsant of the pyrimidinedione[4] class whose active metabolites, phenobarbital (major) and phenylethylmalonamide (PEMA) (minor), are also anticonvulsants. ... Phenytoin sodium (marketed as DilantinÂ® in the USA and as EpanutinÂ® in the UK, by Parke-Davis, now part of Pfizer) is a commonly used antiepileptic. ... Carbamazepine (CBZ) is an anticonvulsant and mood stabilizing drug, used primarily in the treatment of epilepsy and bipolar disorder. ... Clobazam is triazolobenzodiazepine, also known as a 1,5-benzodiazepine, meaning that its diazepine ring has its nitrogen atoms at the 1 and 5 positions instead of the usual 1 and 4. ... Diazepam (IPA: ), first marketed as Valium by Hoffmann-La Roche) is a benzodiazepine derivative drug. ...

References

External links

Categories: Alcohols | Anticonvulsants | Orphan drugs There are several sulphonamide-based groups of drugs. ... Acetazolamide, sold under the trade name DiamoxÂ®, is a carbonic anhydrase inhibitor that is used to treat glaucoma, epileptic seizures, benign intracranial hypertension and altitude sickness. ... Ethoxzolamide (6-ethoxybenzothiazole-2-sulfonamide, alternatively known as Ethoxyzolamide) is a sulfonamide medication that functions as a carbonic anhydrase inhibitor. ... Sultiame (rINN, also known as sulthiame) is a sulfonamide and inhibitor of the enzyme carbonic anhydrase. ... Zonisamide (brand name ZonegranÂ®) is an anticonvulsant used as an adjunctive therapy in adults with partial-onset seizures. ... The propionate (also propanoate) ion is C2H5COOâˆ’ (propionic acid minus one hydrogen ion). ... Beclamide (marketed as Chloracon, Hibicon, Posedrine, Nydrane, Seclar, and other names) is a propionate and was used as a sedative and as an anticonvulsant. ... An aldehyde. ... Paraldehyde is the cyclic form of three acetaldehyde molecules (a trimer). ... A bromide is a phrase, or person who uses phrases, which have been used and repeated so many times as to become either insincere in their meaning, or seem like an attempt at trying to explain the obvious. ... Potassium bromide (KBr) is a salt, used as an anticonvulsant and a sedative in the 1800s. ... Sodium bromide is the chemical compound with the formula NaBr. ...

Contents

Mechanism of action GA_googleFillSlot("encyclopedia_square");