More neuropharm Flashcards
What does phenobarbital do?
bind to the barbiturate site on the GABA-A receptor and increase GABA activities by increasing length of time that the channel stays open
What does diazepam do?
diazepam is a benzodiazepine. binds as an agonist at the BDZ site (gamma receptor) and increases receptor affinity for GABa
What are uses of benzodiazapines?
anxiety, hypnosis, seizures, muscle relaxation, anmesia. May also be used for alcohol withdrawal.
How are BDZs classified?
duration of action. (diazepam lasts 1-3 days)
alprazolam/Xanax and lorazepam is intermediate duration- 10-12 hr half life.
What is another use of lorazepam?
anti-seizure
What should be used in cases of BDZ overdose?
BDZ antagonists like flumazenil
What should I know about the pharmacokinetics of benzodiazepines?
may be given orally or parenterally
very lipid soluable, so may redistribute into body fat. hepatic metabolism, renal clearance.
Adverse effects of benzodiazepines?
somnolence, consusion, tremor, amnesia, esp. in elderly. respiratory suppression, CNS depression, hypotension, bradycardia. may develop tolerance and/or cross-tolerance (esp. with alcohol).
What is buspirone?
as efficacious as BDZs. Acts at 5-HT receptors. causes litte sedation but may cause tachycardia and GI upset
What is chloral hydrate?
mostly used as a hypnotic
How can propanolol be used for anxiety
block sympathetic symptoms. may be good for social phobia if antidepressants aren’t warranted (stage fright)
What is propofol?
hypnotic sedative, but not an analgesic.
MOA of propofol?
beta subutin of GABA a receptor. stabilizes the activated state (increases length of opening?)
uses of propofol?
anesthetic, status epilepticus
Pharmacokinetics of propofol?
extraheptaic clearance. half-life in body is long, but wake-up is 10-30 mins after sustained sedation. good even in patients with cirrhosis or renal insufficiency.
