chapter 12- GABAergic and glutamatergic neurotransmission Flashcards
what is the presumed mechanism of allylglycine
inhibits glutamic acid decarboxylase
what is the presumed mechanism of isoniazid
inhibits pyridoxal kinase (antivitamin B6 effect)
what is the presumed mechanism of tetanus toxin
inhibits GABA and glycine release
what is the presumed mechanism of tiagabine
inhibits GAT-1
what is the presumed mechanism of vigabatrin
inhibits GABA transaminase
what is the presumed mechanism of muscimol
GABAa receptor agonist
what is the presumed mechanism of gaboxadol
GABAa receptor agonist
what is the presumed mechanism of bicuculline
competitive antagonist
what is the presumed mechanism of gabazine
competitive antagonist
what is the presumed mechanism of picrotoxin
noncompetitive antagonist, pore blocker, occludes chloride channel
what is the presumed mechanism of benzodiazepines
potentiate GABA binding
what is the presumed mechanism of barbituates
increase GABA efficacy, weak agonist
what is the presumed mechanism of baclofen
GABAb receptor agonist
what is the main effect of allylglycine
convulsant
what is the main effect of isoniazid
convulsant at high doses
what is the main effect of tetanus toxin
convulsant
what is the main effect of tiagabine
anticonvulsant
what is the main effect of vigabatrin
anticonvulsant
what is the main effect of muscimol
mimics psychosis
what is the main effect of gaoxadol
anticonvulsant
what is the duration of action of clorazepate
short acting
what is the duration of action of midazolam
short acting
what is the duration of action of alprazolam and lorazepam
intermediate action
what is the duration of action of chlordiazepoxide, clonazepam, diazepam
long acting
what is the duration of action of triazolam
shorting acting
what is the duration of action of estrazolam and temazepam
intermediate action
what is the duration of action of flurazepam and quazepam
long acting
what are the short acting barbiturates
amobarbital, pentobarbital, secobarbital, phenobarbital
what are the ultrashort-acting barbiturates
methohexital, thiopental
what are some side effects seen with tiagabine
unexplained sudden death; confusion, sedation, ataxia, amnesia
what is the mechanism of action of tiagabine
enhance GABA activity by blocking gABA reuptake into presynaptic neurons
what are some side effects seen with vigabatrin
retinal atrophy, angioedema, headache, weight gain
what is the mechanism of action of vigabatrin
blocks conversion of GABA to succinct semialdehyde, resulting in high intracellular GABA concentrations and increased synaptic GABA release
what is the mechanism of action of miscimol and gaboxadol
directly activate GABAa receptor
what is the mechanism of action of bicuculline and gabazine
competitive antagonist of GABAa receptor
what is the mechanism of action of picrotoxin
noncompetitive antagonisti of GABAa receptor
what is a therapeutic consideration of bicuculline, gabazine and picrotoxin
produce epileptic convulsions
what short acting benzodiazepine can be used for absence seizures
clonazepam
what are some contraindications of benzodiazepines
acute narrow angle glaucoma and untreated open angle glaucoma
what is the clinical use of flumazenil
reversal of benzodiazepine activity
what barbiturate can be used to treat increased intracranial pressure
thiopental
what are some adverse effects see with barbiturates
SJS, bone marrow suppression, osteopenia, decreased libido
what are some contraindications of barbiturates
porphyria, severe liver dysfunction, respiratory depression
what is the clinical use of etomidate
induction of anesthesia
what are some adverse effects seen with etomidate
CV and respiratory depression, injection-site reaction, myoclonus
what synthesis does etomidate inhibit
cortisol and aldosterone
what is the clinical use of propofol
induction and maintenance of anesthesia; sedation of mechanically ventilated patients
what is the most widely used anesthetic in the USA
propofol
what is the clinical application of baclofen
spasticity
what are some side effects sen with baclofen
coma, seizure, death after abrupt withdrawal, somnolence
how is baclofen primarily cleared
renal
what is clinical application of riluzole
ALS
what is clinical application of memantine
alzheimers disease
what is clinical application of amantadine
parkinson disease; influenza A prophylaxis and infection
what is clinical application of lamotrigine
focal and tonic-clonic seizures; atypical absence seizures; bipolar 1 disorder
what is clinical application of felbamate
refractory epilepsy, especially focal and tonic-clonic seizures
what are some contraindications for felbamate use
blood dyscrasia, liver disease
