Abixa

Memantine is indicated for the treatment of all froms of dementia of the Alzheimer’s type. Memantine may also be indicated in other types of dementia.

Persistent activation of N-methyl-D-aspartate (NMDA) receptors in Central Nervous System by the excitatory amino acid glutamate has been hypothesized to contribute to the symptomatology of Alzheimer’s disease. Memantine is postulated to exert its therapeutic effect through its action as a low to moderate affinity as an uncompetitive (open-channel) NMDA receptor antagonist which binds preferentially to the NMDA receptor-operated cation channels.

Memantine is well absorbed after oral administration and has linear pharmacokinetics over the therapeutic dose range. It is excreted predominantly unchanged in the urine and has a terminal elimination half-life of about 60-80 hours. Following oral administration, Memantine is highly absorbed with peak concentrtions reached in about 3-7 hours. Food has no effect on the absorption of Memantine. The mean volume of distribution of Memantine is 9-11 L/kg and the plasma protein binding is low (45%). emantine undergoes partial hepatic metabolism. About 48% of administered drug is excreted unchanged in urine; the remainder is converted primarily to three polar metabolites which possess minimal NMDA receptor antagonistic activity: the N-glucuronide conjugate, 6-hydroxy Memantine and 1-nitroso-deaminated Memantine. A total of 74% of the administered dose is excreted as the sum of the parent drug and the N-glucuronide conjugate. The hepatic microsomal CYP-450 enzyme system does not play a significant role in the metabolism of Memantine.

Due to the pharmacological effects and mechanism of action of memantine suggests that the effects of L-dopa, dopaminergic agonists, and anticholinergics may be enhanced by concomitant treatment with NMDA-antagonists such as memantine. The effects of barbiturates and neuroleptics may be reduced. Concomitant administration of mematine with the antispasmodic agents, dantrolene or baclofen, can modify their effects and a dosage adjustment may be necessary. Memantine should not be used with amantadine, ketamine, dextromethorphan, phenytoin, cimetidine, ranitidine, procainamide, quinidine, quinidine, quinine & nicotine.

Most frequent side effects (frequency of 2% or less) include hallucination, confusion, dizziness, headache and fatigue. Occasional side effects include anxiety, hypertonus (heightened muscle tension), vomiting, bladder infections and increased sexual drive. If there is a history of epileptic seizures, there is a slight chance that Memantine may increase the probability of an attack.

Pregnancy Category B. Yet there are no adequate and well controlled studies of Memantine in pregnant women. Memantine should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. It is not known whether Memantine is excreted in human breast milk. Because many drugs are excreted in human milk, caution should be exercised when Memantine is administered to a nursing mother.

Caregivers should be instructed in the recommended administration (twice per day for doses above 5 mg) and dose escalation (minimum interval of one week between dose increases). If the patients suffer from kidney dysfunction, the kidney function should be monitored at regular basis.

Seizures: Memantine has not been systematically evaluated in patients with a seizure disorder. One clinical trial shows that seizures occurred in 0.2% of patients treated with Memantine and 0.5% of patients treated with placebo.

Carcinogenesis, Mutagenesis and Impairment of Fertility: Study shows that no risk of carcinogenesis, mutagenesis and impairment of fertility are caused after Memantine use.

Operating Vehicles or Machinery: Taking Memantine may alter the reaction time significantly; therefore safe driving and safe operation of machinery may no longer be possible.

Store in a cool and dry place, protected from light. Keep this medication out of reach of children.