CNS Sedative & Hypnotics

Question 1

Defn =
Insomnia somnolence narcolepsy sleep apnea somnambulism nocturnal enuresis

Answer 1

Insomnia = Inability to sleep
Somnolence = A state of drowsiness or strong desire to sleep
Narcolepsy = A condition characterised by extreme tendency to fall asleep during the day
Sleep apnea = Sleep related breathing disorder in which repetitive pauses in breathing , periods of shallow breathing or collapse of upper airway during sleep
Somnambulism = walking or habit of walk while asleep
Nocturnal enuresis = Accidental / involuntary peeing during sleep

Question 2

Definition sedation , hypnosis , anxiety , sedative , hypnotic , anxiolytic

Answer 2

Sedation = state of CNS depression characterised by state of calmness.

Hypnosis = It is the state CNS depression characterised by prolongation of sleep

Anxiety = feeling of nervousness , fear , apprehension and worrying.

Sedative = the drug which reduces anxiety and produce calming effect.

Hypnotic = the drug which initiate and maintainence of sleep

Anxiolytic = the drug which relieve anxiety

Question 3

Sedative/ Hypnotic drugs are

Answer 3

A] Benzodiazepines

1)Short acting = Midazolam Triazolam
2) Intermediate acting = Bromazepam, Lorazepam , Oxazepam, Alprazolam
3)Long acting = Diazepam Nitrazepam , Clonazepam

B]Barbiturate
1)Short acting = Pentobarbitone, Secobarbitone, Hexobarbitone
2)Intermediate acting = Amobarbitone , Butabarbitone
3)Long acting = Phenobarbitone
4)Ultra short acting = Thiopental sodium

C] Non- benzodiazepine
Zopiclone
Eszopiclone
Zolpidem
Zalepon

Question 4

M/A of diazepam

Answer 4

Diazepam/ Clonazepam ==~> Bind with GABAreceptor ==> Enhancement of GABAergic action ==> Increase frequency of Cl- channel ==> Hyperpolarization ==>CNS depression ==> hypnotic / sedative action

Question 5

Pharmacological action of diazepam

Answer 5

CNS EFFECTS
Sedation
Hypnotic / anxiolytic
Muscle relaxant
Anticonvulsant
Anaesthetic action

CVS EFFECTS
Hypotension
Tachycardia
Heart failure

RESPIRATORY EFFECTS
Respiratory failure
Medullary depression
Sensitivity to CO2

GIT EFFECT
Decrease nocturnal HCL secretion

Question 6

Clinical use of diazepam

Answer 6

Insomnia
Anxiety disorder
Muscle relaxant
Pre anaesthetic medication
Anti convulsant ( febrile convulsion in children )
Anti epileptic

Question 7

A/e of diazepam

Answer 7

Drowsiness
Hangover effects
Lethargy
Somnolence
Amnesia
Tolerance
Dependence
Impaired judgement
Diminished motor skills = driving ability , job performance

Question 8

Contraindications of diazepam

Answer 8

Bronchial asthma
COPD
Sleep apnoea
H/O diarrhoea
Myasthenia gravis

Question 9

Clinical uses of Phenobarbitone

Answer 9

Anticonvulsant
Antiepileptic
Neonatal jaundice
Sedative and hypnotics

Question 10

How does diazepam relax skeletal muscle

Answer 10

Diazepam ==> inhibit polysynaptic reflexes ==> intranuclear transmission ==> skeletal muscle relaxation

Question 11

Criteria of ideal hypnotic drug

Answer 11

Potency and efficacy should be good
Should not alter normal REM sleep pattern
Should not hamper normal daily activity or reduce strength or motor skills
Should not hamper learning or memory
Should not produce = dependence , hangover effects, tolerance , cardio respiratory depression
Should devoid of extra pyramidial symptoms

Question 12

Adv of benzodiazepine over barbiturates

Answer 12

Dose difference between hypnosis and medullary paralysis in case of BNZ is greater than that of barbiturate .

BNZ has antidote = FLUMAZENIL

BNZ doesn’t induce drug metabolising enzymes.

BNZ has minimal effects on CVS and autonomic functions

Question 13

Adv of non benzodiazepine

Answer 13

No = hangover effect
Somnolence
Lethargy
Drowsiness
Diminished motor skills
Chance of amnesia
Chance of cardio respiratory depression
No or less chance of developing addiction
No down regulation and development of tolerance

Question 14

M/A of barbiturate

Answer 14

Bind with GABA receptor ==> Enhancement of GABAergic action ==> increase duration of Cl- channel ==> Hyperpolarization ==> CNS depression ==> sedative hypnotic action

Question 15

How will you manage a case of benzodiazepine poisoning

Answer 15

1) urgent hospitalisation
2) Maintainence of ABC
3)Incase of cardio - respiratory depression = Artifical respiration , Transfer to ICU
4) incase of early hospitalization and conscious patient = induce Vomitting
5) Gastric lavage = by activated charcoal 50gm in 400ml of distilled water
6) I/V fluid = 5% da 2000cc 5%DNS 10000cc I/V @30 drops/ min
7) Acidosis = sodium bicarbonate (I/V)
8) Antidote = FLUMAZENIL

Question 16

Explain the role of Phenobarbitone in treatment of neonatal jaundice

Answer 16

Phenobarbitone ==> induce hepatic metabolizing enzyme ==> increase concentration of GLUCORONYL TRANSFERASE enzyme==> increase conjugation of bilirubin ==> increase metabolism of bilirubin ==> decrease serum bilirubin level ==> correction of neonatal jaundice