Toplep - Pharmacology: Precise mechanism is unknown, but Toplep may block repetitively elicited action potentials, affect ability of chloride ion to move into neurons, and antagonize an excitatory amino acid receptor.
Indication: Initial monotherapy for partial onset or primary generalized tonic-clonic seizures; adjunctive therapy for partial onset seizures, primary generalized tonic-clonic seizures, seizures associated with Lennox-Gastaut syndrome, prophylaxis of migraine headache.
Unlabeled Uses
Adjunctive therapy for bipolar disorder, alcohol and cocaine dependence, binge eating disorder, bulimia nervosa, cluster headaches, infantile spasms, weight loss or obesity, and smoking.
Toplep is an anticonvulsant indicated in the treatment of epilepsy and migraine. Toplep enhances GABA-activated chloride channels. In addition, Toplep inhibits excitatory neurotransmission, through actions on kainate and AMPA receptors. There is evidence that Toplep has a specific effect on GluR5 kainate receptors. It is also an inhibitor of carbonic anhydrase, particular subtypes II and IV, but this action is weak and unlikely to be related to its anticonvulsant actions, but may account for the bad taste and the development of renal stones seen during treatment. Its possible effect as a mood stabilizer seems to occur before anticonvulsant qualities at lower dosages. Toplep inhibits maximal electroshock and pentylenetetrazol-induced seizures as well as partial and secundarily generalized tonic-clonic seizures in the kindling model, findings predective of a broad spectrum of antiseizure activities clinically.
Toplep is used to treat epilepsy (also known as fits or seizures). It may be used on its own or together with other epilepsy medicines. Toplep is also used to prevent migraine headaches.
Oral Adjunct for seizures associated with the Lennox-gastaut syndrome
Adult: Initially, 25 mg at night for 1 wk, thereafter increase in steps of 25-50 mg at intervals of 1-2 wk until effective dose is achieved. Doses >25 mg/day should be taken in 2 divided doses. Usual dose: 200-400 mg daily. Max: 800 mg daily.
Child: 2-16 yr: Initially, 25 mg nightly for the 1st wk increased at intervals of 1-2 wk by increments of 1-3 mg/kg daily according to response. Daily doses of >25 mg should be taken in 2 divided doses. Usual dose: 5-9 mg/kg daily. Max: 30 mg/kg/day. Renal impairment: Moderate to severe: Doses should be halved. Haemodialysis: Supplemental dose equal to about ½ of the daily dose should be given in divided doses (at the start and finish of haemodialysis). Hepatic impairment: Dosage adjustment may be needed. Oral Epilepsy
Adult: Monotherapy: Initially, 25 mg at night for 1 wk, thereafter increase in steps of 25-50 mg at intervals of 1-2 wk. Doses >25 mg/day should be taken in 2 divided doses. Usual dose: 100-400 mg daily. Max: 400 mg daily. Adjunctive treatment: Initially, 25 mg at night for 1 wk, thereafter increase in steps of 25-50 mg at intervals of 1-2 wk until effective dose is achieved. Doses >25 mg/day should be taken in 2 divided doses. Usual dose: 200-400 mg daily. Max: 800 mg daily.
Child: 10-16 yr: Initially, 0.5-1 mg/kg at night for the 1st wk, increased at intervals of 1-2 wk by increments of 0.5 to 1 mg/kg daily. Usual dose: 3-6 mg/kg daily. Daily doses >25 mg should be taken in 2 divided doses. Max: 16 mg/kg/day. Renal impairment: Moderate to severe: Doses should be halved. Haemodialysis: Supplemental dose equal to about ½ of the daily dose should be given in divided doses (at the start and finish of haemodialysis). Hepatic impairment: Dosage adjustment may be needed. Oral Prophylaxis of migraine
Adult: >16 yr: Initially 25 mg daily at night for 1 wk, increased in steps of 25-mg at wkly intervals. Usual dose: 50-100 mg daily in 2 divided doses. Daily doses >25 mg should be taken in 2 divided doses. Renal impairment: Moderate to severe: Doses should be halved. Haemodialysis: supplemental dose equal to about ½ of the daily dose should be given in divided doses (at the start and finish of haemodialysis). Hepatic impairment: Dosage adjustment may be needed.
Oral Adjunctive treatment of seizures associated with the Lennox-gastaut syndrome
Adult: Initially, 25 mg at night for 1 wk, thereafter increase in steps of 25–50 mg at intervals of 1–2 wk until effective dose is achieved. Doses >25 mg/day should be taken in 2 divided doses. Usual dose: 200–400 mg daily. Max: 800 mg daily.
Child: 2-16 yr: Initially, 25 mg nightly for the 1st wk increased at intervals of 1-2 wk by increments of 1-3 mg/kg daily according to response. Daily doses of >25 mg should be taken in 2 divided doses. Usual dose: 5-9 mg/kg daily. Max: 30 mg/kg/day. Renal impairment: Moderate to severe: Doses should be halved. Haemodialysis: Supplemental dose equal to about ½ of the daily dose should be given in divided doses (at the start and finish of haemodialysis). Hepatic impairment: Dosage adjustment may be needed. Oral Monotherapy and adjunctive treatment of generalised tonic-clonic seizures or partial seizures with or without secondary generalisation
Adult: Monotherapy: Initially, 25 mg at night for 1 wk, thereafter increase in steps of 25–50 mg at intervals of 1–2 wk. Doses >25 mg/day should be taken in 2 divided doses. Usual dose: 100-400 mg daily. Max: 400 mg daily. Adjunctive treatment: Initially, 25 mg at night for 1 wk, thereafter increase in steps of 25–50 mg at intervals of 1–2 wk until effective dose is achieved. Doses >25 mg/day should be taken in 2 divided doses. Usual dose: 200–400 mg daily. Max: 800 mg daily.
Child: 10-16 yr: Initially, 0.5-1 mg/kg at night for the 1st wk, increased at intervals of 1-2 wk by increments of 0.5 to 1 mg/kg daily. Usual dose: 3-6 mg/kg daily. Daily doses >25 mg should be taken in 2 divided doses. Max: 16 mg/kg/day. Renal impairment: Moderate to severe: Doses should be halved. Haemodialysis: Supplemental dose equal to about ½ of the daily dose should be given in divided doses (at the start and finish of haemodialysis). Hepatic impairment: Dosage adjustment may be needed. Oral Migraine prophylaxis
Adult: >16 yr: Initially 25 mg daily at night for 1 wk, increased in steps of 25-mg at wkly intervals. Usual dose: 50-100 mg daily in 2 divided doses. Daily doses >25 mg should be taken in 2 divided doses. Renal impairment: Moderate to severe: Doses should be halved. Haemodialysis: supplemental dose equal to about ½ of the daily dose should be given in divided doses (at the start and finish of haemodialysis). Hepatic impairment: Dosage adjustment may be needed.
Indications:
Adult: PO Adjunct in seizures associated w/ Lennox-gastaut syndrome Initial: 25 mg at night for 1 wk, then increase slowly. Usual: 200-400 mg/day. Max: 800 mg/day. Epilepsy Monotherapy: Initial: 25 mg at night for 1 wk, then increase slowly. Usual: 100-400 mg/day. Max: 400 mg/day. Adjunct: Initial: 25 mg at night for 1 wk, then increase slowly. Usual: 200-400 mg/day. Max: 800 mg/day. Migraine prophylaxis >16 yr: Initial: 25 mg at night for 1 wk, then increase slowly. Usual: 50-100 mg/day in 2 divided doses.
Epilepsy ( treatment adjunct ) – Toplep is indicated for use in the adjunctive treatment of partial onset seizures in adults and pediatric patients ages 2 to 16 years. Toplep is also indicated for use in the treatment of primary generalized tonic – clonic seizures in adults and in pediatric patients ages 2 to 16 years. |
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