Sedatives, Anxiolytics, Anticonvulsant Flashcards
Drugs that produce drowsiness and encourage the onset and maintenance of a state of sleep. Involve more pronounced CNS depression than sedation
Hypnotics
Drugs that reduce anxiety and exert calming effect
Sedatives (anxiolytics)
Major inhibitory neurotransmitter?
GABA - Glycine in the spinal cord
Major excitatory neurotransmitters?
Glutamate, aspartate (dicarboxylate)
Short acting benzodiazepine, for acute anxiety, anesthesia induction, preoperative sedation. May cause anterograde amnesia. And has additive CNS depression with ethanol
Midazolam
Intermediate acting benzodiazepine, for anxiety disorders, insomnia, tranquilizer. With additive CNS depression with ethanol
Lorazepam
What abnormal sleep pattern results from use of benzodiazepines?
Decreased REM sleep
Long acting benzodiazepine, for anxiety disorder, skeletal muscle relaxation, alcohol withdrawal. May cause anterograde amnesia.
Diazepam - binds GABA A receptor subunits to increase frequency of chloride channel opening. Membrane hyperpolarization
Benzodiazepine drug used as a date-rape drug.
Flunitrazepam together with Alcohol (most common) and Gamma hydroxybutyrate
Which benzodiazepine has the longest half life?
Chlordiazepoxide
Preferred benzodiazepine: anticonvulsant maintenance
Clonazepam - intermediate
Preferred benzodiazepine: status epilepticus
Lorazepam and diazepam
Preferred benzodiazepine: skeletal muscle relaxation
Diazepam - eg. Cerebral palsy
Preferred benzodiazepine: panic disorders and phobias
Alprazolam, Clonazepam
Preferred benzodiazepine: insomnia
Estrazolam, Flurazepam and Triazolam
Preferred benzodiazepine: anesthesia induction
Midazolam and Diazepam
Preferred benzodiazepine: bipolar disorder
Clonazepam
Preferred benzodiazepine: alcohol withdrawal
Chlordiazepoxide and Diazepam
Antidote for Benzodiazepine toxicity
Flumazenil - a competitive BZ receptor antagonist
Ultrashort acting barbiturate, for anesthesia induction and increased ICP. May cause acute intermittent porphyria
Thiopental-potent inducer of CYP450 enzymes
Short to intermediate acting barbiturate for insomnia, preoperative sedation
Pentobarbital
Long acting barbiturates, for insomnia. Gilbert disease, seizure disorder in children
Phenobarbital - bind to GABA A receptor sites. Increases duration of chloride channel opening
Imidazopyridine drug, for insomnia only. Lacks anti-convulsant, anti-anxiety and muscle relaxant
Zolpidem - SIMD: Zaleplon and Eszopiclone
Anxiolytic drug for generalized anxiety disorder by partial agonist at 5-HT receptors and possibly D2 receptors
Buspirone - no anticonvulsant, no muscle relaxant properties with minimal CNS depressant effects
Effects of Zolpide. Can be reversed with?
Flumazenil
Cytosolic, NAD+ dependent enzyme, mainly in liver and gut, for metabolism of low to moderate doses of ethanol
Alcohol dehydrogenase
Fixed metabolism of ethanol:7-10g/h
Responsible for ethanol metabolism at blood levels higher than 100mg/dL
Microsomal Ethanol Oxidizing System (MEOS)
Blood alcohol concentration that causes impairment of driving ability
60-80mg/dL
Blood alcohol concentration that causes coma
300 to 400mg/dL
Blood alcohol concentration that causes respiratory depression and death
> 500mg/dL
Most common neurologic abnormality in chronic alcoholics
Peripheral neuropathy
Syndrome associated with alcohol use presenting with ataxia, confusion, paralysis of the extra-ocular muscles
Wernicke-Korsakoff syndrome
Changes in the brain seen in Wernicke-Korsakoff syndrome.
Hemorrhagic necrosis of the mamillary bodies
Most common mental retardation syndrome, presents with microcephaly, underdevelopment of midface region associated with heavy consumption of alcohol during the first trimester of pregnancy
Fetal alcohol syndrome
Drug of choice for alcohol withdrawal syndrome
Long acting benzodiazepines
Inhibits aldehyde dehydrogenase leading to acetaldehyde accumulation then nausea, headache, flushing and hypotension
Disulfiram
What Drugs can causes Disulfiram reaction?
Chlorpropamide Cefoperazone Cefomandole Cefotetan Procarbazine Metronidazole
Treatment for methanol poisoning
Ethanol - retards formation of formaldehyde
Fomepizole - inhibitor of alcohol dehydrogenase
Refers to finite episode of brain dysfunction resulting from abnormal discharge of cerebral neurons
Seizures
Type of seizure wherein the consciousness is preserved
Simple partial seizures
Type of seizure: impaired consciousness
Complex partial seizure
Type of seizure: involves abrupt loss of consciousness, muscle rigidity and respiratory arrest for less than 1min then followed with jerking of the body muscles, lip and tongue biting, and fecal and urinary incontinence for 2-3mins
Generalized tonic-clonic seizure (Grand Mal)
Type of seizure: with impaired consciousness (often abrupt onset and brief) begin in childhood and usually cease by age of 20years
Absence seizure (Petit Mal)
Type of seizure: sudden, brief, shocklike contractions of musculature (myoclonic jerks)
Myoclonic seizures
Series of seizures (usually tonic-clonic) without recovery of consciousness between attacks. Life-threatening emergency
Status epilepticus
Anticonvulsant drug for generalized tonic-clonic seizure, partial seizures. Status epilepticus. May cause ataxic diplopia, gingival hyperplasia. Follows zero order kinetic, potent inducer of CYP450
Phenytoin - blocks voltage-gated Na channels
Drug of choice for Trigeminal neuralgia
Carbamazepine
Anticonvulsant drug for generalized tonic-clonic seizures, partial seizures, bipolar disorder and trigeminal neuralgia
Carbamazepine - blocks voltage gated Na channels and decreases glutamate release
Anticonvulsant drug for myoclonic seizure, generalized tonic-clonic seizures and acute mania. May cause Spina bifida. Inhibitor of CYP450
Valproic acid - blocks high-frequency firing of neurons modifies amino acid metabolism
Anticonvulsant drug for absence seizures. May cause GI distress, lethargy, headache and behavioral changes
Ethosuximide - decreases Ca2+ currents in thalamus
Anticonvulsant drug for partial seizure, neuropathic pain and migraine. May cause dizziness, sedation, nystagmus, tremor and ataxia
Gabapentin - SIMD: Pregabalin, blocks Ca2+ channels, increases GABA release. Inhibits neuronal discharge from seizure foci
Anticonvulsant drug for generalized tonic-clonic seizure, partial seizures and juvenile myoclonic epilepsy
Levetiracetam - selectively binds synaptic vesicular protein SV2A. Modify synaptic release of glutamate and GABA
Anticonvulsant drug for generalized tonic-clonic seizures, absence seizures, partial seizures, Lennox-Gastaut syndrome, West syndrome and migraine. Noted to be the anti-seizure drug with most number of mechanisms of action
Topiramate - multiple actions on synaptic function via actions on phosphorylation
Drugs of choice: generalized tonic-clonic seizures
Valproic acid
Phenytoin
Carbamazepine
Drugs of choice: partial seizure
Carbamazepine
Lamotrigine
Phenytoin
Drugs of choice: absence mal
Ethosuximide
Valproic acid
Drugs of choice: myoclonic and atypical absence syndromes
Valproic acid
Drugs of choice: status epilepticus
Lorazepam
Diazepam
Phenytoin
Phenobarbital
First line for patients with mania, bipolar affective disorder
Valproic acid
Drug of choice for Trigeminal neuralgia
Carbamazepine