Dr. Liu: Antianxiety Medications Flashcards
Sedatives
- Drugs which decrease activity
- Produce sedation with OUT sleep
Hypnotics
- Drugs which produce drowsiness
- Facilitate the onset and maintenance of sleep
Chloral Hydrate
- First sedative hypnotic drug
- Active form = trichloroethanol
- Both of these have a nasty taste (so this drug is often given as a prodrug)
Barbiturates
1) Must be a weak acid
2) Must possess a lipid-water partition coefficient within certain limits
Adverse aspects of barbiturate treatment
- Enzyme induction: leading to many drug interactions
- Low therapeutic index: easy to over dose
- Tolerance and dependence
Barbiturate SAR Summary
1) Carbons off of C5 should be between 6-10
2) Two groups must be present on C5
3) Sulfur on C2 makes for a quick onset
- But two sulfurs decrease activity
4) Substitution on both N1 and N3 destroys activity (Salt cannot be formed)
Benzodiazepines
1) Speed of onset
2) Duration of action
Which Benzodiazepines are safe in the elderly/ hepatically impaired
- Oxazepam
- Temazepam
Triazolams duration of action
- Short
- Decreases hang over effect
Side effects of Benzodiazepines
- Driving impairment
- Light headedness
- Confusion
- Dry mouth
Advantages of benzodiazepines as sedative hypnotics
-Less severe:
Tolerance
Dependence
Sleep issues
Zolpidem (Ambien)
- Imidazopyridine hypnotics
- Interacts on GABA(a) receptor
- Very selective for GABA benzodiazepine receptor subtypes!
Antihistamines
- Cause significant degrees of CNS depression
ex. Diphenhydramine, doxylamine, pyrilamine, and promethazine
Phenothiazines
- Drowsiness is a well known side effect
- Can be used as a sedative preoperatively or during labor
ex. Propiomazine (Largon)
Major classes of antianxiety drugs
- Propanediol Carbamates
- Benzodiazepines
- 5HT1A receptor related anxiolytics
