Use LEFT and RIGHT arrow keys to navigate between flashcards;
Use UP and DOWN arrow keys to flip the card;
H to show hint;
A reads text to speech;
42 Cards in this Set
- Front
- Back
What is the GABAa receptor?
|
a chloride channel
|
|
What happens when the GABAa receptor is stimulated?
|
the chloride channel opens, chloride enters the cell, and it becomes hyperpolarized
|
|
Where do benzodiazepines (BDZs) bind?
|
to an allosteric site on the GABAa receptor
|
|
What is the effect of BDZ binding to the GABAa receptor?
|
they increase the frequency of opening of the chloride channels, increasing the amplitude of the IPSP
|
|
Which is safer: BDZs or barbiturates? Why?
|
BDZs, they have fewer side effects (esp. respiratory depression)
|
|
How are BDZs administered and where are they metabolized?
|
orally; in the liver
|
|
BDZs are dangerous when taken in combination with what?
|
alcohol or other CNS depressants
|
|
Sudden withdrawal of BDZs after prolonged use may cause what?
|
SEIZURES and psychosis
|
|
Which drugs decrease the metabolism of BDZs, thereby increasing their levels?
|
cimetidine, disulfiram, ethanol, isoniazid, and valproic acid (also displaces BDZs from binding sites)
|
|
Which drug decreases diazepam excretion?
|
acetaminophen
|
|
Which drugs decrease the absorption of BDZs, thereby decreasing their levels?
|
antacids
|
|
Which drugs increase the metabolism of BDZs?
|
oral contraceptives
|
|
Which BDZs are used to treat insomnia?
|
triazolam (halcion), temazepam (restoril), and flurazepam
|
|
Which BDZ is used to treat only anxiety?
|
oxazepam
|
|
Which BDZ is used to treat only panic disorders?
|
alprazolam (xanax)
|
|
Which BDZ is used for the treatment of anxiety, preanesthetic medication, and status epilepticus?
|
lorazepam (ativan)
|
|
Which BDZ is used for anesthesia and medical procedures?
|
midazolam (versed)
|
|
Which BDZ is used for the treatment of epilepsy and anxiety?
|
clorazepate
|
|
Which BDZ is used for the treatment of anxiety, skeletal muscle relaxation, preanesthetic medication, and status epilepticus?
|
diazepam (valium)
|
|
Which BDZ is used for ethanol withdrawal symptoms, anxiety, and preanesthetic medication?
|
chlordiazepoxide
|
|
On what does the CNS depressant action of barbiturates depend?
|
their lipid solubility
|
|
If a barbiturate has high lipid solubility, how does this affect its pharmacokinetics?
|
it works faster, has decreased duration of action, increased metabolic degradation, and greater hypnotic effect
|
|
How is the action of barbiturates terminated?
|
physical redistribution to fat tissue, hepatic metabolism, and urinary excretion
|
|
Which enzymes do barbiturates induce?
|
hepatic microsomal enzymes
|
|
How do barbiturates work?
|
they bind to GABAa receptors, increasing the duration of the opening of the chloride channel
|
|
What is the longest-acting barbiturate and what is its use?
|
phenobarbital; it's an anticonvulsant
|
|
What are the two ultra-short-acting barbiturates and what is their use?
|
thiopental and methohexital; induction of anesthesia
|
|
Sudden withdrawal of barbiturates after prolonged use may cause what dangerous side effects?
|
SEIZURES, orthostatic hypotension, cardiovascular collapse
|
|
What are the symptoms of barbiturate overdose?
|
mild OD is like ethanol intoxication; severe OD can cause coma, shock, and hypothermia
|
|
What are some side effects of barbiturates? (hint: there are a LOT; no one should take these!!)
|
sedation, ataxia, respiratory depression, rash, angioedema, folate-responsive megaloblastic anemia, osteomalacia, acute intermittent porphyria
|
|
When barbiturates induce microsomal enzymes, they increase the metabolism of what other drugs?
|
phenytoin, steroid hormones, tricyclic antidepressants, oral anticoagulants, digoxin, quinidine, theophylline, and beta-blockers
|
|
How does buspirone work?
|
it's a partial agonist at 5HT1a receptors; it decreases serotonin
|
|
What is different about the effects buspirone when compared to BDZs?
|
buspirone has no muscle relaxant or anticonvulsant activity and doesn't increase the CNS depressant effect of ethanol
|
|
How does zolpidem tartrate work?
|
It is a GABAa agonist (?)
it's BZ1 selective as opposed to BDZs, which interact with BZ1 and BZ2 |
|
What is buspirone used for? Zolpidem tartrate?
|
anxiety; short-term treatment of insomnia
|
|
What is meprobamate used for?
|
anxiety and sedation
|
|
What is chloral hydrate used for?
|
sleep inducer
|
|
What are the side effects of chloral hydrate?
|
irritation of mucous membranes and inhibition of ethanol metabolism
|
|
What is glutethimide used for?
|
sedation/hypnotic
|
|
What are the side effects of glutethimide?
|
anticholinergic effects
|
|
Which drugs induce hepatic microsomal enzymes?
|
barbiturates, meprobamate, glutethimide
|
|
Phenobarbital has been used to treat what neonatal illness? Why?
|
kernicterus and hyperbilirubinemia; it increases the elimination of bilirubin
|