Sedation antiepileptics

Antiepileptics Na+, Ca2+ channels GABA receptors l Na+currents l Ca2+ currents GABA receptor activity l Excitability of peripheral and central neurons l Release of excitatory neurotransmitters Sedation, dizziness, cognitive impairment, ataxia, hepatotoxicity, thrombocytopenia... 

Valproic acid (dipropylacetic acid) is a single branched chain carboxylic acid that is structurally unlike any of the other drugs used in the treatment of bipolar disorder or epilepsy. The amide derivative, valproamide, is available in Europe as a more potent form of valproate. Valproate was first developed in Erance as an antiepileptic agent in 1963. As an antiepileptic agent, it was shown to be active against a variety of epilepsies without causing marked sedation. 

Side effects. Because clobazam has been widely used as an anxiolytic, its side effects are well known and essentially similar to those of the other benzodiazepines. Thus sedation, dizziness, ataxia, blurred vision and diplopia are the most commonly reported in epileptic patients. One of the most problematic features of clobazam is its tendency to produce tolerance, an effect which may occur more frequently with clobazam than with the other widely used benzodiazepine, clonazepam. It has been estimated that at least 50% of patients develop tolerance. Tolerance to the sedative effects of the drug develop more rapidly than those to the antiepileptic effect. Clobazam should be considered as adjunctive therapy whenever treatment with a single first-line drug has proven to be ineffective. 

The leaf essential oil of L. nobilis, which has been used as an antiepileptic remedy in Iranian traditional medicine, was evaluated for anticonvulsant activity against experimental seizures (Sayyah et al., 2002). The essential oil protected mice against tonic seizures induced by maximal electroshock and especially by pentylenetetra-zole. Components responsible for this effect may be methyleugenol, eugenol and pinene present in the essential oil. At anticonvulsant doses, the essential oil produced sedation and motor impairment. This effect seems to be related in part to cineol, eugenol and methyleugenol (Sayyah et al., 2002). 

SODIUM OXYBATE 1. ALCOHOL 2. ANALGESICS - opioids 3. ANTIDEPRESSANTS-TCAs 4. ANTIEPILEPTICS-barbiturates 5. ANTIHISTAMINES 6. ANTIPSYCHOTICS 7. ANXIOLYTICS AND HYPNOTICS-BZDs, buspirone Risk of CNS depression - coma, respiratory depression Additive depression of CNS Avoid co-administration. Caution even with relatively non-sedating antihistamines (cetrizine, desloratidine, fexofenadine, levocetirizine, loratidine, mizolastine) as they can impair the performance of skilled tasks... 

Epilepsy Antiepileptic drugs, surgery Medication serum concentrations, sedation, cognitive abilities, liver function tests, blood dyscrasias, bleeding abnormalities, CNS toxicities, rashes, seizure counts, other drug-specific adverse effects... 

Peripheral neuropathy Tricyclic antidepressants, antiepileptic dmgs, mexilitine, capsacian Sedation, anticholinergic effects, blood dyscrasias, arrhythmias, medication-specific adverse effects, pain relief... 

Chronic pain Surgery, NSAIDs, opiates, tricyclic antidepressants, antiepileptic drugs Sedation, pain relief... 

Tranquilizers are drugs essentially used in the management and, treatment of psychoses and neuroses. They specifically exert their action on the lower brain areas to produce emotional calmness and relaxation without appreciable hypnosis sedation euphoria or motor impairment. In addition many of these drugs also display clinically beneficial actions, for instance skeletal muscle relaxants, antihypertensive, antiemetic and antiepileptic properties. 

Moderate social drinking does not appear to affect the serum levels of carbamazepine, ethosuximide or phenytoin. Some small changes are seen in the serum levels of phenobarbital and sodium valproate, but no changes in the control of epilepsy seem to occur. No pharmacokinetic interaction was detected between tiagabine and alcohol, and tiagabine did not alter the cognitive effect of alcohol. The adverse effects of both alcohol and antiepileptics, such as enhanced sedation, may be additive. 

The pharmacokinetics and pharmacodynamics of a single 15-mg oral dose of midazolam was studied in 6 epileptic patients taking either carbamazepine, phenytoin or both drugs together, and in 7 control subjects not taking either antiepileptic. The AUC of midazolam in the epileptics was reduced to 5.7%, and the peak serum levels to 7.4% of the value in the control subjects. The pharmacodynamic effects of the midazolam (subjective drowsiness, body sway with eyes closed and open, as well as more formal tests) were also reduced. Most of the epileptics did not notice any effects from taking midazolam, while the control subjects were clearly sedated for 2 to 4 hours, and also experienced amnesia after taking the midazolam. ... 

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