L5 Hypnotic - Sedatives

Question 1

Sedatives Examples.

Answer 1

1.Diazepam
2.Chlordiazepoxide
3.Nitrazepam
4.Lorazepam
5.Clonazepam
6.Alprazolam
7.chlordiazepoxide
8.Bromazepam

Question 2

Hypnotics Examples

Answer 2

A. Barbiturates:
Phenobarbital
Zolpidem
Zoleplam
Buspiron
Diazepam

Question 3

Actions of sedatives & hypnotics?

Answer 3

1.Sedation Reduce anxiety in low doses, cause amnesia
2. Hypnosis If used in high doses
3. Anesthesia If used in very high doses.
4. Anticonvulsant effect. (Diazepam & clonazepam)
5. Muscles relaxation( Diazepam).
6. Respiratory depression & death. In high doses.
7. Tolerance Develops to all.

Question 4

Mechanism of action of Benzodiazepines

Answer 4

-enhance the GABAergic action of GABA , GABA acts as inhibitory neurotransmitter.
-Facilitates the activity of nGABA A1 to open Chloride channels. Not direct

Question 5

MOA of hypnotic as barbiturate ?

Answer 5

direct effect on GABA receptors. Prolong opening of the channel associated with GABA binding,
increase conductance.

Question 6

Sedative Hypnotics can cause?

Answer 6

Acute Intoxication

Question 7

Therapeutic uses of sedatives ?

Answer 7

1- Anxiety disorder (diazepam & Bromazepam )

2- Muscular disorders Multiple sclerosis & cerebral palsy (diazepam )

3- Amnesia Before anesthesia (Medazolam) injectable.

4- Seizures (Diazepam)

5- Alcohol withdrawal syndrome (Diazepam)

6- Grand-mal epilepsy, status epilepticus, febrile convulsion (Diazepam)

5- Sleep disoreers (Triazolam)

(Not used in alcohol intoxication )

Question 8

Benzodiazepines (Adverse effects):

Answer 8

cause weakness, hypotonia
Tolerance & apnea

Question 9

competitive drug antagonist used for reversal of central effects of benzodiazepines (Antidote)?

Answer 9

Flumazenil
But it Can cause:
Agitation, confusion & dizziness.

Question 10

Drug interaction with BDZs?

Answer 10

antihistaminics and anticholinergic
narcotics, alcohol

Question 11

SSRI’s and oral contraceptives decrease metabolism of?

Answer 11

BDZs

Question 12

Phenobarbitone, Secobarbitone,Thiopental Mechanism of action:

Answer 12

­inc. GABA,A action, open Cl- channel for longer time, cause dose related overall depression of CNS

Question 13

Uses of barbiturate:

Answer 13

-Anxiety & insomnia:
Secobarbitone (short-acting & is enzyme inducer for its own self)

• Induction of anesthesia: Thiopental (ultrashort acting)

• Epilepsy: Phenobarbitone (long acting)

Question 14

Therapeutic uses of barbiturates?

Answer 14

1- Anaesthesia : thiopental
2- Anticonvulsant: Phenobarbitol
3-Anxiety

Question 15

AEs of barbiturate?

Answer 15

tolerance
porphyria
respiratory depression

Question 16

Miscellaneous sedatives-hynotics :

Answer 16

(H 1 - antihistamines) : Promethazine
β-blockers: Propranolol
Buspiron
Zoleplam

Question 17

Z drugs ( Zolpedem-Zoleplam):

Answer 17

-GABA mimetic action كلهم
-Hypnotic used for insomnia/dysomnia كلهم
-Oral , rapid onset كلهم
-Rebound anxiety الاول
-Less abuse potential كلهم
-potentiates the CNS depressant مع الثاني
-1/2 t only 1h

minimal muscles relaxant & anticonvulsant actions الاول
Rifampicin & Cimetidine induce them

Question 18

Buspiron?

Answer 18

-partial Agonist of 5-HT1A receptors; presynaptic
and dec. release of serotonin x
-has affinity to D2 in brain
-Oral
-Used in generalized chronic anxiety Slow acting
- no marked sedation
-Not suitable for acute panic attacks
-No withdrawal effects or dependence or rebound anxiety
-no muscle relaxant or anticonvulsant

Question 19

(H 1- antihistamines):

Answer 19

• Diphenhydramine & Promethazine
• Mechanism: Block H1 histamine & M3 receptors.
• Possess anti-emetic and anti-allergic properties.
• Depressant effect on RAS related to sedation.
• Use:
Anxiety, insomnia, vomiting & allergic reactions
• Adverse effects:
• May cause drowsiness the next day
• Dry mouth, constipation & blurred vision
• No withdrawal effects. No dependence & abuse

Question 20

• β-blockers: • Propranolol (Block β 1 & β2 receptors)

Answer 20

Propranolol
• Relieve mainly autonomic symptoms of anxiety: tachycardia, palpitation & tremors
• Do not reduce psychological & non-autonomic symptoms like fear, worry & muscle tension

Question 21

Sedative-hypnotic Toxicity related to dose

Answer 21

Drowsiness, amnesia
Renal failure dec. bowl sounds, dilated pupil
Decreased learning , Decreased motor skills
Dec. resp, dec. BP, shock

Question 22

acute intoxication of sedative hypnotics signs

Answer 22

a. Pupils are normal
b. BP is decreased
c. Respiration is depressed
d. Nystagmus on lateral gaze
e. Confusion

F. Tendon reflexes decreased
G. Slurred speech
H. Coma & shock
I. Risk of Death