Pharm Test 3 Sedative-Hypnotic

Question 1

Clonidine

Answer 1

Modifies autonomic expression of anxiety

Question 2

Propranolol

Answer 2

Performance Anxiety

Question 3

Hydroxyzine

Answer 3

Antihistamine
Antiemetic
anxiolytic

Question 4

Ramelteon

Answer 4

Melatonin receptor agonist
MOA: MT1 and MT2 receptor
Tx of insomnia with difficulty falling asleep

Question 5

Buspirone

Answer 5

5HT1A partial agonist
No hypnotic, anticonvulsant or muscle relaxant properties
Actions/Use: Only has anxiolytic effects and is used in the Tx of anxiety disorders
*Onset in 2-3 weeks, less psychomotor impairment than Benzo’s
*No interaction with EtOH, Benzo’s or other sedatives
*No rebound anxieety or withdrawal when abruptly stopped
*No dependence

Question 6

Zolpidem

Answer 6

Non Benzo Benzo Receptor Agonist
Only act on BZ1
-Short duration of action t.5=1.5-3.5 hours
DOC for difficulty falling asleep insomnia
*minimal muscle relaxing and anticonvulsant effects
Little of no toleraance and low incidence of AE

Question 7

Zaleplon

Answer 7

Non Benzo Benzo Receptor Agonist
Only act on BZ1
Rapid onset and very shorrt duration of action used in short term treatment of insomnia

Question 8

Eszopiclone

Answer 8

Non Benzo Benzo Receptor Agonist
Only act on BZ1

S enantiomer of Zopiclone
*decreases sleep latency and improves sleep maintance in the treatment of insomnia t.5=6hours

Question 9

Phenobarbital
Pentobarbital
Thiopental

Answer 9

Barbituates
Replaced by benzo’s for Tx of anxiety
*Full surgical anesthesia and pronounced central depressant due to multiple sites of action
MOA: Bind GABAa at a different site than Benzos to increase opening duration. Also blocks glutamate and sodium channels
Action/Use: Dose dependent sedation->hypnosis->anesthesia->coma->death
Enzyme induction of CYP450
*Thiopental: ultra short acting used to induce anesthesia
*Phenobarbital: management of tonic clonic seizures, status epilepticus, and eclampsia; hyperbilirubinemia, kernicterus in neonates
AE: Respiratory depression -> decreases hypoxic chemoreceptor response, CNS depression, Paradoxical Excitement (makes pain worse), Hypersensativity, Hangover, Cardiovascular collapse with rapid injection, Addiction (severe withdrawal)
*Induce tolerance, drug metabolizing enzymes, Physical dependence

CI: pt’s with porphyria due to increased porphyria synthesis

Question 10

Flumazenil

Answer 10

DOC for Benzo overdose
Benzo antagonist with a rapid onset and short duration of action
Action/Use: Reverse CNS depression or overdose, hasten recovery after procedures
AE: Precipitate withdrawal, Seizures
*Continuous administration for long acting Benzo’s

Question 11

Oxazepam Short t.5
Triazolam

Alprazolam Med T.5
Lorazepam
Temazepam

Diazepam Long t.5
Flurazepan

Midazolam
Clonazepam

Answer 11

Benzodiazepam
Most widely used and safer than barbituates
*Most undergo phase 1 rxns by CYP3A4, then get conjugated and excreted. Oxa, Lora, and tema directly enter phase 2 rxns.
MOA: Binds CNS GABAa receptors (pentameric Cl- channels) b/w alpha and gamma subunits to increase frequency of opening
Normal GABA binding site is Alpha/Beta.
Actions: Agonist: anxiolytic and anticonvulsant, muscle relaxant, anesthesia. Short term or intermittant Tx of anxiety disorders. Skeletal mm spasm (MS and cerebral palsy), seizures, status epilepticus, Alcohol withdrawal, sleep disorders.
AE: Drowsiness, confusion, ataxia, cognitive impairment. May cause Paradoxical adverse psychological effeects which are dose related and rare. Dependence->abrupt withdrawal can cause withdrawal sxs
**GABA=major inhibitory NT in the CNS–>Cl- influx
*Lipophilic–>rapid and complete oral absorption; high Vd
*Inverse agonists–> anxiety and seizures

Question 12

Diphenhydramine

Doxylamine

Answer 12

OTC antihistamines

Action/use: Mild situational insomnia