Chapter 15: Drugs treating anxiety/promoting sleep Flashcards
GABA
gamma-aminobutyric acid. An inhibitory neurotransmitter that opposes the excitatory NT glutamate. GABA causes hyperpolarizition of post-synaptic neurons which increases the threshold for excitation.
Selective Serotonin Reuptake Inhibitors (SSRIs)
A class of antidepressant drugs that indirectly increase the amt of serotonin available in synapses. This action treats the low serotonin levels present in ps with mood/anxiety disorders. SSRIs are considered first-line therapy for anxiety disorders bc they do not cause ataxia or drowsiness. SSRIs can cause sex dysfunction and the effects can take several weeks.
Tricyclic Antidepressants (TCAs)
Class of antidepressant drugs that affect the regulation of serotonin and NE in the brain. TCAs are not used as frequently as SSRIs bc of their high AE profile, but are just as effective in treating anxiety disorders. TCAs can take weeks of therapy before full effect is evident.
Monoamine Oxidase Inhibitors (MAOIs)
The oldest class of antidepressants which work by inhibiting monoamine oxidase, the enzyme that degrades serotonin. This action allows more serotonin to remain in the synapses which makes it effective at treating panic disorder and social phobia. MAOIs have serious life-threatening drug-drug/food interactions (tyramine foods), thus, they are less commonly prescribed compared to SSRIs and TCAs.
Benzodiazepines
Class of drugs used for a variety of conditions including anxiety, sleep disorders, muscle disorders, epilepsy, and pre-op sedation/anesthesia. Benzodiazepines work by enhancing the effects of GABA, thus, causing CNS depression. They have a wide therapeutic index. Common ending: -azepam/-azolam.
Lorazepam (Ativan)
A benzodiazepine used for anxiety disorders, insomnia, and pre-op sedation. Lorazepam works by enhancing the effects of GABA, causing CNS depression. Side effects of Lorazepam include drowsiness, ataxia, confusion, respiratory changes, brady-c, and hypotension. Doses shouldn’t exceed 3mg/day and should be lowered for asians, elderly, and children.
Buspirone (BuSpar)
A nonbenzodiazepine used for short-term tx of anxiety. The pharmacodynamics (actions) are unknown; it has no effects on the NT GABA. Optimum relief of anxiety usually takes 3-4 weeks.
Hydroxyzine (vistaril)
a miscellaneous-nonbenzodiazepine/anti-anxiety drug that rapidly yields a calm feeling and relieves anxiety w/out impairing mental alertness. Hydroxyzine is commonly coadministered with a narcotic to relieve the nausea caused by the narcotic. Hydroxyzine also has bronchodilation, antihistamine, analgesic, and antiemetic effects.
Eszopiclone (Lunesta)
nonbenzodiazepine hypnotic drug that induces sleep and prevents waking during the night by interacting with GABA receptor-benzodiazepine receptor complexes. In fact, Lunesta is the the only drug approved for long-term use for insomnia (up to 6 mths). Side effects= headache, drowsiness, unpleasant taste. Lunesta has a rapid onset-taken before bedtime.
Zaleplon (Sonata)
a nonbenzodiazepine sedative prescribed for short-term tx for difficulty falling asleep. Works by interacting with GABA-benzodiazepine complexes, decreasing the amt of time needed to fall asleep. Side effects include D/D, light-h, difficulty with coordination, rebound insomnia. Sonata can lead to dependency.
Zolpidem (Ambien)
“City never sleeps, better slip you an ambien.” Drug used for short-term tx of insomnia (7-10 days), that works by interacting with GABA-BZ receptor complexes, inducing sleep rapidly. It should be taken before bedtime and generally preserves all sleep stages. Side effects include headache, drowsiness, dizziness.
RaMELteon (RoZerem)
melatonin receptor agonist used to tx insomnia (difficulty falling asleep) and works by binding to melatonin receptors. Melatonin the hormone that helps regulate circadian rhythms. Side effects include headache, dizziness, sleepiness, nausea, and even worsening insomnia.
TraZodone (Desyrel)
an atypical antidepressant used to promote sleep, prescribed especially for patients who receive another antidepressant that causes insomnia. TraZodone can cause significant sedation.
Chloral Hydrate
(think chloroform) a nonbarbiturate hypnotic used to induce sleep, cause pre-op sedation, or used as an adjunct to opiates/analgesics. The exact pharmacodynamics are unknown. Chloral hydrate has numerous CNS SEs, but little effect on respirations, BP, or reflexes in therapeutic doses.
Barbiturates
a class of CNS depressants that stimulate GABA receptors (like the benzo’s), causing drowsiness, hypnosis, sedation, and less motor activity. They were used to tx insomnia before benzo’s, however, they are highly habit forming and tolerance can dvlp.
