9 - Sedative - Hypnotics Flashcards
MOA of barbiturates
- increase DURATION of opening of chloride channels
- blocks action of glutamic acid
- blocks Na channels
MOA of benzodiazepines
- increase in FREQUENCY in opening of Chloride channels
5 principle pharmacologic effects of benzodiazepine
- Anxiolytic
- Sedative and hypnosis
- Anticonvulsant
- Muscle relaxant
- Anterograde amnesia (take note of this)
Use of benzodiazepines short BEFORE delivery
Floppy baby syndrome
Prenatal BZD exposure
Increase risk of oral cleft
Abnornmal sleep pattern seen in BZD
Decreased REM sleep
Long-acting BZD that is painful on injection
Diazepam
Most effective drug for stopping Status Epilepticus
Diazepam
Date-rape drugs
- Alcohol - most common
- Flunitrazepam (rohypnol) - BZD
- Gamma hydroxybutyrate
Anticonvulsant maintenance
Clonazepam
- intermediate-acting
Status epilepticus
- Lorazepam - intermediate
2. Diazepam- long
Skeletal muscle relaxation (eg cerebral palsy)
Diazepam
Panic disorder, phobia
Alprazolam - intermediate
Clonazepam
Insomnia
- Estazolam - intermediate
- Flurazepam - long
- Triazolam - short
Anesthesia induction
- Midazolam - short
2. Diazepam
Bipolar disorder
Clonazepam
Alcohol withdrawal
- Chlordiazepoxide - long (longest half-life pf 36-200 hours)
- Diazepam
Antidote for BZD overdose
Flumazenil
- BZD antagonist
- competitive
Parent compound of barbiturates
Barbituric acid
Oxygen is found at the 2nd position
Oxybarbiturates
- pentobarbital
- secobarbital
Replacement of oxygen with sulfur which makes it more lipid soluble
Thiobarbiturates
- thiopental
- thiamylal
Phenyl group at 5th position which increases anticonvulsant effect
Phenobarbital
Methyl group of nitrogen increases potency but lowers seizure threshold
Methohexital
For seizure induction for epilepric patients undergoing temporal lobe resection
Methohexital
Contraindication for barbiturate use
Porphyria
- side effect of barbs
Acute intermittent porphyria
- HMB synthase deficiency
High dose BZD and barbs may suppress seizures but at the expense of marked sedation EXCEPT
- clonazepam
- phenobarbital
Considered as DOC for seizures in infants
Phenobarbital
Tx for seizures in pregnancy
Phenobarbital
Intermediate-acting barb
- pentobarbital
- secobarbital
Long-acting barb
- phenobarbital
- mephobarbital
- primidone
BZ1 receptor agonist can will cause sedation ONLY
Zolpidem
BZ2 receptor
- cognition
Used for insomnia and sleep disorders
Zolpidem
Zaleplon
Partial agonist at 5HT1A and D2 agonist For GAD (generalized anxiety disorder)
Buspirone
- safe for pregnant
Anxiolytic:
Melatonin receptor agonist
Ramelteon
Most catastrophic symptom of sedative-hypnotic withdrawal
Rebound suicide
