Antilepsin - General Information
An anticonvulsant used for several types of seizures, including myotonic or atonic seizures, photosensitive epilepsy, and absence seizures, although tolerance may develop. It is seldom effective in generalized tonic-clonic or partial seizures. The mechanism of action appears to involve the enhancement of gamma-aminobutyric acid receptor responses.
Pharmacology of Antilepsin
Antilepsin, a benzodiazepine, is used primarily as an anticonvulsant in the treatment of absence seizures, petit mal variant seizures (Lennox-Gastaut syndrome), akinetic and myoclonic seizures, and nocturnal myoclonus.
Antilepsin for patients
Clonazepam is used for the treatment of seizures. Notify your physician if you
are pregnant or nursing. This medication may cause dizziness, drowsiness, or
blurred vision; use caution while driving or operating hazardous machinery.
Do not take any other sedating drugs or drink alcohol while taking clonazepam.
Do not change the dose or stop taking clonazepam without talking with your physician.
This medication may be habit forming. Seizures or withdrawal symptoms may occur after
you stop taking it. This medication should be taken with meals to avoid stomach upset.
Effect of Clonazepam on the Pharmacokinetics of Other Drugs: Clonazepam does not appear to alter the pharmacokinetics of phenytoin, carbamazepine, or phenobarbital. The effect of clonazepam on the metabolism of other drugs has not been investigated.
Effect of Other Drugs on the Pharmacokinetics of Clonazepam: Literature reports suggest that ranitidine, an agent that decreases stomach acidity, does not greatly alter clonazepam pharmacokinetics.
In a study in which the 2 mg clonazepam orally disintegrating tablet was administered with and without propantheline (an anticholinergic agent with multiple effects on the GI tract) to healthy volunteers, the AUC of clonazepam was 10% lower and the Cmax of clonazepam was 20% lower when the orally disintegrating tablet was given with propantheline compared to when it was given alone.
Fluoxetine does not affect the pharmacokinetics of clonazepam. Cytochrome P-450 inducers, such as phenytoin, carbamazepine and phenobarbital, induce clonazepam metabolism, causing an approximately 30% decrease in plasma clonazepam levels. Although clinical studies have not been performed, based on the involvement of the cytochrome P-450 3A family in clonazepam metabolism, inhibitors of this enzyme system, notably oral antifungal agents, should be used cautiously in patients receiving clonazepam.
Pharmacodynamic Interactions: The CNS-depressant action of the benzodiazepine class of drugs may be potentiated by alcohol, narcotics, barbiturates, nonbarbiturate hypnotics, antianxiety agents, the phenothiazines, thioxanthene and butyrophenone classes of antipsychotic agents, monoamine oxidase inhibitors and the tricyclic antidepressants, and by other anticonvulsant drugs.
Clonazepam is not indicated in patients with epilepsy who have been treated with benzodiazepines. Antagonism of the benzodiazepine effect in such patients may provoke seizures. Serious sequelae are rare unless other drugs or alcohol have been taken concomitantly.
Additional information about Antilepsin
Antilepsin Indication: Used as an anticonvulsant in the treatment of the Lennox-Gastaut syndrome (petit mal variant), akinetic and myoclonic seizures.
Mechanism Of Action: Allosteric interactions between central benzodiazepine receptors and gamma-aminobutyric acid (GABA) receptors potentiate the effects of GABA. As GABA is an inhibitory neurotransmitter, this results in increased inhibition of the ascending reticular activating system. Benzodiazepines, in this way, block the cortical and limbic arousal that occurs following stimulation of the reticular pathways.
Drug Interactions: Cimetidine Cimetidine increases the effect of the benzodiazepine
Clozapine Increased risk of toxicity
Fluconazole Fluconazole increases the effect of the benzodiazepine
Indinavir The protease inhibitor increases the effect of the benzodiazepine
Itraconazole The imidazole increases the effect of the benzodiazepine
Kava Kava increases the effect of the benzodiazepine
Ketoconazole The imidazole increases the effect of the benzodiazepine
Nelfinavir The protease inhibitor increases the effect of the benzodiazepine
Omeprazole Omeprazole increases the effect of benzodiazepine
Ritonavir The protease inhibitor increases the effect of the benzodiazepine
Saquinavir The protease inhibitor increases the effect of the benzodiazepine
St. John's Wort St. John's Wort could reduce the benzodiazepine effect
Voriconazole The imidazole increases the effect of the benzodiazepine
Food Interactions: Avoid alcohol.
Take without regard to meals.
Avoid excessive quantities of coffee or tea (Caffeine).
Generic Name: Clonazepam
Synonyms: Clonazepamum; Chlonazepam
Drug Category: Anticonvulsants; Benzodiazepines
Drug Type: Small Molecule; Illicit; Approved
Other Brand Names containing Clonazepam: Antelepsin; Antilepsin; Cloazepam; Clonopin; Iktorivil; Klonopin; Klonopin Rapidly Disintegrating; Landsen; Rivotril;
Absorption: Clonazepam is rapidly and completely absorbed after oral administration. The absolute bioavailability of clonazepam is about 90%.
Toxicity (Overdose): Somnolence, confusion, coma, and diminished reflexes
Protein Binding: 85%
Biotransformation: Hepatic (cytochrome P450, including CYP3A). Biotransformation occurs mainly by reduction of the 7-nitro group to the 4-amino derivative. This derivative can be acetylated, hydroxylated, and glucuronidated.
Half Life: 30-40 hours
Dosage Forms of Antilepsin: Tablet Oral
Chemical IUPAC Name: 5-(2-chlorophenyl)-7-nitro-1,3-dihydro-1,4-benzodiazepin-2-one
Chemical Formula: C15H10ClN3O3
Clonazepam on Wikipedia: http://en.wikipedia.org/wiki/Clonazepam
Organisms Affected: Humans and other mammals