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Pharmacology of GABA
Some cards based on GABAnergic pharmacology
38
Pharmacology
Professional
02/21/2011

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Cards

Term
Which type of GABA receptors are most common in the CNS?
Definition
GABA-A
Term
What type of ion do GABA receptors let in?
Definition
Chloride
Term
Which GABA receptors are ionotropic?
Definition
GABA-A and GABA-C
Term
which GABA receptors are metabotropic
Definition
GABA-B
Term
Which GABA receptors are found in the retina?
Definition
GABA-C
Term
Which subunits do barbiturates work on?
Definition
they work on a and B, but NOT gamma
Term
Which subunits to zolpidem, zaleplon, and eszopiclonen work on?
Definition
a1
Term
True or false: Benzos work on all alpha subunits
Definition
true
Term
What does tiagabine work on?
Definition
GAT-1
Term
what does vigabatrin work on?
Definition
It blocks GABA-T, increasing concentration of GABA in synapses
Term
What drug is associated with retinal atrophy?
Definition
vigabatrin
Term
What drug is an antagonist to benzodiazepines?
Definition
Flumazenil
Term
What benzos are intermediate acting?
Definition
Lorazepam, Alprazolam, Temazepam, Estazolam (remember LATE)
Term
Which benzos are short acting?
Definition
Triazolam, midozolam, clorazepate, zolpidem (NON benzo)
Term
Which benzos are long acting?
Definition
Chlorodiazepoxide, clonazepam, diazepam, flurazepam, quazepam (mostly PAMS)
Term
True or false: benzos stimulate gaba receptors directly
Definition
false: they bind allosterically and modulate the frequency of Cl- ion channel opening
Term
True or false: benzo overdose is frequently fatal
Definition
false: due to the indirect nature of benzos, they do not usually cause severe CNS depression
Term
True or false: benzos do NOT cause a true general anestesia
Definition
true
Term
Which benzo is associated with fatal respiratory depression?
Definition
Midozalam given via IV
Term
What is the drug of choice for pre-procedure anxiety?
Definition
Midozalam. It's rapid onsdet and sedative/amnesstic abilities are preferred here.
Term
True or false: benzos increase the length of REM sleep
Definition
false: they alter sleep architecture and DECREASE REM sleep
Term
Which benzo has the most antiepilleptic effects?
Definition
Clonazepam
Term
What are the mechanisms for benzo tolerance?
Definition
decreased expression of GABA-A receptors and uncoupling of the binding site from the GABA receptor
Term
Which benzo has the least rebound insomnia?
Definition
Flurazepam. It's long half-life means it does not cause rebound insomnia, but it DOES sometimes cause daytime sedation.
Term
True or false: barbiturates directly stimulate GABA receptors
Definition
true
Term
What is the effect of barbiturates on Cl- channels?
Definition
They increase opening time, allowing for greater Cl- influx
Term
Which drugs are used for partial tonic-clonic seizures?
Definition
phenobarbital
Term
Which drugs are used for status epileptics?
Definition
pentobarbital and amobarbital
Term
Which barbiturates are used for anesthesia?
Definition
thiopental, pentobarbatial, and methohexital
Term
True or false, barbiturates undergo signifcant first-pass metabolism
Definition
true
Term
True or false, barbiturates are CYP inhibitors
Definition
False: they are CYP inducers
Term
What things do barbiturates have drug interactions with?
Definition
benzodiazepines, phenytoin, digoxin, oral contraceptives, steroid hormones, bile salts, cholesterol, and vitamins D and K
Term
True or false: barbiturates can cause fatal CNS depression
Definition
true
Term
True or false: barbiturates are contraindicated in pulminary insufficiency
Definition
true
Term
True or false: rapid administration of barbiturates via IV is not associated with cardiovascular problems
Definition
False: it can cause cardiovascular collapse.
Term
What is baclofen used for?
Definition
multiple sclerosis
Term
What is baclofen's mechanism of action?
Definition
it stimulates GABA receptors in the spinal cord to increase Ca+ and K+ second messengers downstream
Term
True or false: chronic oral baclofen is associated with tolerance
Definition
False: there is no tolerance to oral baclofen
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