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Selective CNS depressants that bind to the BZ binding site on the GABAa receptor on the alpha subunit
these are inverse agonists at the BZ receptor that negatively modulate GABA function and oppose BZ action
Melatonin receptor agonist with hypnotic actions and lower abuse liablity.
Used for delayed sleep phase syndrome
Actions mediated by MT1 andMT2 receptors in the suprachiasmatic nucleus where the circadian pacemaker is located
-fluvoxamine (antidepressant) increase half life 190fold
-rifampin decrease serum levals via CYP1A2 activation
Affect hormone levels and is contraindicated in pubescent/ prepubescent patients and pregnancy
5ht partial agonist structurally unrelated to BZs used for general anxiety disorder due to gradual onset.
No anticonvulsant or hypnotic actions and minimal sedation or psychomotor impairment
Takes 1-3 weeks to take action and is rapidly absoprbed and undergoes extensive first pass metabolism
Can cause pupillary constriction, anti-cholinergic symptoms, and hypertension(when used with MAOI)
5 functions of Benzodiazepines
2. Hypnotic- idiopathic or behavioral (not in sleep apnea)
3. Anticonvulsant- status epilepticus, absence seizures
5. Muscle relaxant- suppreses reticular system (doesn't work at nmj)
Sedative and anticonvulsant actions*
Tolerance develops most for these two actions of BZs (*more slowly, clonazepam resistant)
Difference from Non-selective CNS depressants
BZ structure determines their actions at the GABAa receptor
(as opposed to lipophillic nature
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