Anxiolytics and hypnotic drugs 3 Flashcards
Mention the adverse effects of BDZs?
1) Residual effect : Sedation, drowsiness, increase in reaction time, impaired mental functions, confusion.
2) Paradoxical effect : anxiety, restlessness, Irritability, night mares, sweating, tachycardia and suicidal tendency {during first weeks of therapy}
3) Cardiovascular and respiratory depression with overdoses.
4) Tolerance (mainly dynamic), physical dependence
5) Withdrawal symptoms upon sudden withdrawal { anxiety, restlessness, Irritability, night mares sweating, tachycardia}
6) Fatal drug interaction with alcohol which enhance the associated CNs depression (Pharmacodynamics drug
interaction)
7) may induce hepatic encephalopathy in patients with chronic liver disease
Precautions and contraindications of BDZs?
1- Alcohol users.
2- Driving and machinery users
3- Respiratory insufficiency as COPD.
4- Pregnancy and lactation.
Act only on BDZ receptor type I ?
Zaleplon, Zolpidem & Eszopiclone
Drugs used only as hypnotics ?
Zaleplon, Zolpidem & Eszopiclone
Drugs use only when the patients has difficulty falling asleep due to their short duration?
Zaleplon, Zolpidem & Eszopiclone
- Zaleplon (T1/2=1hr) used to reduce sleep latency { stage 0 of NREM }
- Zolpidem (T1/2=2hr) used to prolong total sleep time { stage II of NREM }
T OR F / Z-Compounds act on BDZ receptor type I & II
F, Act only on BDZ receptor type I
give reason Z-Compounds replaced BDZs as hypnotics?
1) Less or even no RISK OF tolerance, physical dependence
2) No rebound insomnia on abrupt withdrawal
3) Minimal shortening of REM stage of sleep
BDZs antagonists?
Flumazenil
Flumazenil is ?
A) Selective competitive antagonist
B) Non- Selective agonist
C) Non-competitive antagonist
D) Selective antagonist
A) Selective Competitive antagonist
Give reason Flumazenil should be given IV ?
1) Extensive 1st pass metabolism
2) Short duration of action (30-60) minutes
can precipitate withdrawal syndrome in BDZs addict patients?
Flumazenil
Enumerate the therapeutic uses of Flumazenil?
1) Diagnosis and treatment of benzodiazepines toxicity
2) Reverse benzodiazepines sedation after their use for endoscopy, dentistry & ICU
3) Hepatic encephalopathy due to BDZs in patients with chronic liver diseases.