10 - B) CLASSIFICATION OF HYPNOTICS Flashcards
CLASSIFICATION OF HYPNOTICS
1st generation; Barbiturates, they are nowadays obsolete.
2nd generation: BENZODIAZEPINES (most used)
TRIAZOLAM ?
MIDAZOLAM Dormicum
FLURAZEPAM Dormodor
3rd generation: non-BZD non-barbiturate hypnotics (SAFEST & most effective) ZOLPIDEM ZOPICLONE – OF CHOICE - ZALEPLON (CLOMETIAZOL) CHLORAL HYDRATE Other: ANTIHISTAMINIC
BENZODIAZEPINES THAT CAN BE USED AS HYPNOTICS
Flurazepam Lormetazapam Brotilozam Midazolam Triazolam
Long acting BZP
Chronic anxiety
Hypnotic with anxiolytic effect
+ risk of accumulation and interactions
Flurazapam
Short acting BZD
Hypnotic wihout residual effects
Lormetazepam
Ultrashort- acting BZD
Acute panic attack
Fast sleep induction
+ risk of abstinence and dependance
Brotilozam
Mizalozam
Trialozam
Trialozam
Ultrashor- acting BZD
Midazolam
Ultrashort-acting BZD
Flurazapam
Long acting BZD
Lormetazepam
Short acting BZD
Zolpidem
3rd generation
Zopiclone
3rd generation
chatacteristics of the 3rd eneration drugs
Selective ligands of the BZD site in the α1 subunit of the GABAA receptor
- Less disturbance of the sleep structure than BZD
- Reduce latency periods of sleep
- Short half-life: fast absorption and elimination
- Minimal rebound effect
- Low dependence
- Certain tolerance with continued use
- Not authorized for long-term treatments
Clomethiazole
It’s structurally related to thiamine (Vit B1), I’ts hypnotic, sedative and anticonvulsant. It has limited use due to its great addictive potential.
Antihistaminics
Difenhidramine
Hydroxyzine
Doxylamine
They block H-1 receptors, in the CNS, crossing BBB. They produce sedating effetcs, mainly in children. A subjetctie short- term improvement was shown, but it was not demonstrated for long- term. They may cause tolerance and anticholinergic effects. They are 2nd choice and over- the- counter drugs.
