Sedative Hypnotic, Anti-anxiety, and central acting Muscle Relaxing drugs Flashcards
What is the general progression of the CNS-depressing effects of these drugs?
anxiolysis sedation hypnosis anesthesia respiratory failure
What is a muscle spasm?
when the excitatory input overwhelms the inhibitory input
the result of faulty coordination of the spinal cord mediated reflex arc mediating control of movement.
What are the two main classes of drugs of the sedative-hypnotic and anti-anxiety drugs?
barbiturates and benzodiazapines
Both barbiturates and benzodiazepines increase ___ conductance via the action at ___-_ receptors.
Cl-; GABA-A
What type of receptor is GABA-A? GABA-B?
A: ligand gated ion channel
B: G protein coupled receptor
GABA-___ receptors hyperpolarize by activating ___ channels via ___. They also diminish ___ entry into cells.
B: K: GbetaGgamma; Ca2+
Barbiturates and benzodiazepines are ___ regulators of GABA-___ receptors.
allosteric; A
T/F. Benzodiazepines increase the duration of GABA-mediated channel opening.
False, BARBITURATES increase the duration of GABA-mediated channel opening. Benzos increase the FREQUENCY of these channels opening.
T/F. Both barbiturates and benzodiazepines produce hyperpolarization and decrease excitability.
True.
Like ACh receptors, GABA-A receptors are ___.
heterogeneous
T/F. Benzodiazepines are more toxic than barbiturates.
False, barbituates are more toxic than Benzodiazepines.
___ ___ by benzodiazepines is not a problem by itself but it is if used with opioids.
Respiratory depression
What benzodiazepine antagonist is used to treat overdose?
Flumazenil
IV administration can reverse in 1-2 minutes
Why did benzodiazepines largely replace tranquilizers?
less potential for abuse (less likely to produce dependence)
better therapeutic index
___ is a non-benzodiazepine sedative-hypnotic that is structurally unrelated but binds to the same site.
Zolpidem (ambien)
