Anxiolytics and hypnotic drugs 2 Flashcards
Drug if it Excreted in the breast milk leading to sedation in fetus?
BZDs
Mechanism of action of BZDs?
- BDZs potentiate the inhibitory effect of GABA:
1) BDZs bind to specific BDZs receptors causing conformational changes in GABA .A receptor.
2) increase affinity of GABA.A receptor to bind with the inhibitory neurotransmitter GABA.
3) increase in the frequency of opening of CL channels linked to GABA.A receptors.
4) increase in chloride influx across the membrane.
5) neuronal hyperpolarization which cause sedative, hypnotic effect.
BZDs bind to both BDZI, BDZ II receptors and activate them which lead to ?
1) Activation of BDZI receptor => anxiolytic, hypnotic& sedative effect.
2) Activation of BDZII receptor => anticonvulsant effect &skeletal muscle relaxant effect.
T OR F / Longer acting BDZs that have anxiolytic effect on CNS actions obtained at small doses.
T
T OR F / Short acting BDZS that have Hypnotic effect on CNS action obtained by high doses while the Intermediate acting BDZS that have the same effect on CNS actions obtained at small doses.
F , both short and Intermediate acting BDZS
obtained by high doses
Drugs used in panic attack (Anxiety disorders)?
Longer acting BDZs : C.O.L.D
Chlorazepate
oxazepam
lorazepam
diazepam
Anxiolytic effect obtained by small doses
Drug used for Initial
insomnia ( difficulty to fall into sleep)?
triazolam ( Hypnotic effect ,Short acting
BDZS ) obtained by high doses
Drug used for latent Insomnia (Interrupting sleep)?
1) Intermediate acting BDZs : Temazepam
2) long acting BDZs: Flurazepam
Hypnotic effect obtained by high doses
Precautions for use of BDZs as Hypnotics on CNS action?
1) preferred for the shortest period (Not more
than 3 weeks)
2) Interrupted use is better to avoid tolerance
3) Start by the minimal dose and then dose can be increased if needed
4) Gradual withdrawal is essential to avoid
withdrawal symptoms.
Hypnotic effect characters?
1) reduce sleep latency (time taken to go to sleep) stage 0
2) Shortening of stage I of NREM
3) Prolong stage II of NREM (total sleep time)
4) Shortening the duration of stage III, IV of NREM (↓ nightmares, ↓ terrors)
5) Shortening the duration of REM (Rapid eye movement sleep).
Drug used to cause anterograde amnesia and sedation at preanesthetic medication?
1) Diazepam, lorazepam
2) Midazolam
Drug used in IV anesthesia for endoscopy, cardiac catheterization and in ICU to cause anterograde amnesia?
1) Diazepam, lorazepam
2) Midazolam
Drugs used in Anti-Convulsant (anti-seizure)?
Anti-epileptics:
1) Clonazepam for absence seizure.
2) Diazepam &lorazepam (Iv) for status epilepticus
Therapeutic uses of Clonazepam ?
1) Anti-epileptics for absence seizure.
2) Spastic conditions of the skeletal muscles as spinal cord lesions, cerebral palsy => skeletal muscle relaxant
3) Control withdrawal symptoms of Alcohol.
Effect of BDZs on respiratory system?
1) High doses depress ventilation, induce acidosis
2) may cause apnea if given with opioids, alcohol & patient with COPD { chronic obstructive pulmonary disease } .
