Central Nervous System Depressants

zsh43378's version from 2015-04-14 03:07


Question Answer
What do they do?Receptor sites for drugs binding GABA Cl- ion channel (nerve hyper polarization). Also has ethanol binding site and barbiturate binding site
Acamprosatealcohol abstinence enhancer. It is a neurotransmitter analog of GABA. Interacts with GABA and glutamate receptors and restores balance between excitatory and inhibitory neurotransmission. Reduces alcohol intake in animal studies. Treatment of alcohol dependence.
BuspironeAntianxiety agent. It is a serotonin 5HT1A partial agonist. Activates presynaptic 5HT1A receptors in dorsal raphe nucleus, decreased firing of serotonergic neurons. Treatment for generalized anxiety disorder. Metabolized by CYP450.
CarbamazepineAnticonvulsant drug. It is a neuronal Na+ channel blocker. Decreasing firing of ectopic foci and decreasing spread of seizures. Used for partial seizures, tonic clonic seizures, neuropathic pain. Induces own metabolism along with steroids, warfarin, valproate, lamotrigine, haloperidol. BONE MARROW SUPPRESSION
DiazepamVALIUM. Antianxiety. Benzodiazepine. GABAa Cl- channel activator. Levels increased by oral contraceptives, fluoxetine, valproate. Reversed by flumazenil. Alprazolam, chlordizepoxide, lorazepam, oazepam, temazepam are similar.
DisulfiramAlcohol abuse deterrent. Acetaldehyde hydrogenase inhibitor. Causes blurred vision, chest pain, palpitations, nausea, vomiting. Reinforcement of alcohol abstinence. Similar drugs are acamprosate and naltrexone
EthosuximideAnticonvulsant drug. Blocks T-type calcium channels in thalamic neurons that generate 3-Hz spike waves during absence seizures. Drug of choice for children with generalized absence seizures. Valproate is usually more effective for adults
FlumazenilAntidote to benzodiazepines. Competitively blocks benzodiazepine receptor sites in GABA Cl- channels
GabapentinAnticonvulsant. GABA analogue. Increases GABA release from central neurons. Inhibits neuronal discharges from seizure foci. Inhibits pain neurotransmission. Treatment of ALL forms of partial seizures, chronic pain, migraine prophylaxis.
LamotrigineAnticonvulsant. Neuronal Na+ channel blocker. Blocks voltage-sensitive Na+ channel, neuronal membrane conduction, and release of glutamate. Prevents spread of seizure foci discharges. Steven-Johnson's Syndrome!!! Adverse increased and metabolism decreased by valproate.
LorazepamBenzodiazepine. GABA Cl- channel activator. Binds to GABAa ion channels and causes hyper polarization of neurons.
PhenobarbitalBarbiturate that binds GABA Cl- channel, increasing duration of channel opening and directly increasing influx of Cl-. Treatment of febrile seizures in children; preoperative sedation. Second-line drug for tonic-clonic seizures. May increase folate requirement during long term therapy. Induces more cytochrome P450 enzymes. Similar drugs are Carbamazepine and phenytoin.
PhenytoinAnticonvulsant drug. Neuronal Na+ channel blocker. Blocks voltage-sensitie sodium channels, neuronal membrane conduction, release of glutamate. Prevents spread of seizure foci discharges. First-line drug for partial seizures, tonic clonic seizures. Drug of choice for status epilepticus.
RamelteonHypnotic drug. Melatonin receptor agonist. Activates melatonin receptors and reduces sleep latency (time to go to sleep). Treatment of sleep-onset insomnia. The only noncontrolled drug for treatment of insomnia. Does not produce dependence.
TopiramateAnticonvulsant drug. Monosaccharide derivative with multiple actions. Blocks neuronal Na+ channels, augments GABA activation of receptors, blocks glutamate receptors (kainate and AMPA). Monotherapy for generalized tonic clonic seizures. Prophylaxis of migraine headaches in adults. Decrease dose in person with renal impairment. Effects decreased by phenytoin, carbamazepine, valproate.
ValproateAnticonvulsant drug. increases GABA levels by increasing release or decreasing metabolism of uptake. Treatment of simple and complex absence seizures, complex partial seizures, tonic-clonic, and myoclonic. Prevention of migraine, treatment of manic phase of bipolar disorder. HEPATOTOXICITY. Increases levels of lamotrigine, phenobarbital, and primidone. Levels decreased by carbamazepine and phenytoin.
ZolpidemHypnotic drug. NONBENZODIAZEPINE gaba cl- channel activator. Treatment of insomnia. Shorter half-life, less effect on sleep architecture, causes less tolerance and dependence.