AGENTS, CONTROLLING THE FUNCTIONS OF THE CENTRAL NERVOUS SYSTEM - Antiseizure drugs Flashcards
The mechanism of action of antiseizure drugs is
- Enhancement of GABAergic (inhibitory) transmission
- Diminution of excitatory (usually glutamatergic) transmission
- Modification of ionic conductance
Which antiseizure drugs produces enhancement of GABA-mediated inhibition?
Phenobarbital
Indicate an antiseizure drug, which has an impotent effect on the T-type calcium channels in thalamic neurons?
Ethosuximide
Which antiseizure drugs produces a voltage-dependent inactivation of sodium channels?
- Lamotrigine
- Carbamazepin
- Phenytoin
Indicate an antiseizure drug, inhibiting central effects of excitatory amino acids
Lamotrigine
The drug for partial and generalized tonic-clonic seizures is
- Carbamazepine
- Valproate
- Phenytoin
Indicate an anti-absence drug
Valproate
The drug against myoclonic seizures is
Clonazepam
The most effective drug for stopping generalized tonic-clonic status epilepticus in adults is
Diazepam
Phenytoin
It blocks sodium channels
Phenytoin is used in the treatment of
Grand mal epilepsy
Dose-related adverse effect caused by phenytoin is
Gingival hyperplasia
Granulocytopenia, gastrointestinal irritation, gingival hyperplasia, and facial hirsutism are possible adverse effects of
Phenytoin
The antiseizure drug, which induces hepatic microsomal enzymes, is
Phenytoin
The drug of choice for partial seizures is
Carbamazepin
The mechanism of action of carbamazepine appears to be similar to that of
Phenytoin
Which antiseizure drugs is also effective in treating trigeminal neuralgia?
Carbamazepine
The most common dose-related adverse effects of carbamazepine are
Diplopia, ataxia, and nausea
Indicate the drug of choice for status epilepticus in infants and children
Phenobarbital sodium
Barbiturates are used in the emergency treatment of status epilepticus in infants and children because of
They significantly decrease of oxygen utilization by the brain, protecting cerebral edema and ischemia
Which antiseizure drugs binds to an allosteric regulatory site on the GABA-BZ receptor, increases the duration of the Cl-channels openings
Phenobarbital
Adverse effect caused by phenobarbital is
- Physical and phychological dependence
- Exacerbated petit mal epilepsy
- Sedation
Which antiseizure drugs is a prodrug, metabolized to phenobarbital?
Primidone
Indicate the antiseizure drug, which is a phenyltriazine derivative
Lamotrigine
Lamotrigine can be used in the treatment of
- Partial seizures
- Absence
- Myoclonic seizures
The mechanism of vigabatrin′s action is
Inhibition of GABA aminotransferase
Indicate an irreversible inhibitor of GABA aminotransferase (GABA-T)
Vigabatrin
Tiagabine
Blocks neuronal and glial reuptake of GABA from synapses
The mechanism of both topiramate and felbamate action is
- Reduction of excitatory glutamatergic neurotransmission
- Inhibition of voltage sensitive Na+ channels
- Potentiation of GABAergic neuronal transmission
The drug of choice in the treatment of petit mal (absence seizures) is
Ethosuximide
The dose-related adverse effect of ethosuximide is
- Gastrointestinal reactions, such as anorexia, pain, nausea and vomiting
- Exacerbated grand mal epilepsy
- Transient lethargy or fatigue
Valproate is very effective against
- Absence seizures
- Myoclonic seizures
- Generalized tonic-clonic seizures
The drug of choice in the treatment of myoclonic seizures is
Valproate
The reason for preferring ethosuximide to valproate for uncomplicated absence seizures is
Valproate′s idiosyncratic hepatotoxicity
The mechanism of valproate action is
- Facilitation glutamic acid decarboxylase, the enzyme responsible for GABA synthesis and inhibition of GABAaminotransferase, the enzyme responsible for the breakdown of GABA (enhance GABA accumulation)
- Inhibition of voltage sensitive Na+ channels
- Inhibition of low threshold (T-type) Ca2+ channels
Indicate the antiseizure drug, which is a sulfonamide derivative, blocking Na+ channels and having additional ability to inhibit T-type Ca2+ channels
Zonisamide
Indicate the antiseizure drug – a benzodiazepine receptor agonist
Lorazepam
Which antiseizure drugs acts directly on the GABA receptor-chloride channel complex?
Diazepam
Benzodiazepine΄s uselfulness is limited by
Tolerance
A long-acting drug against both absence and myoclonic seizures is
Clonazepam
Which antiseizure drugs may produce teratogenicity?
- Phenytoin
- Valproate
- Topiramate
The most dangerous effect of antiseizure drugs after large overdoses is
Respiratory depression
