Sedative Hynotics

Sedative Hypnotics
• Sedative : dose that reduces excitement,

physical activity and calms the person.
• Hypnotic : dose that produces sleep that

resembling with normal sleep.
• Sleep - Phases
Non Rapid Eye Movement (NREM )
Rapid Eye Movement (REM )
Sedative Hypnotics
1.Benzodizepines 2.Barbiturates
Long acting:
Long acting: Phenobarbitone
Diazepam, Flurazepam
Nitrazepam Short acting:
Pentobarbitone
Short acting: Butobarbitone
Alprazolam, Triazolam, Ultra short acting:
Temazepam Thiopentone
Methohexitone
3. Non benzodizepines: Zolpidem,Zopiclone,Zaleplon

Benzodizepines: Commonly used
Wide safety / High therapeutic index
Mech. of action /(M.O.A) BZDs
Bind to GABAA receptor Cl Channel
Increase frequency of opening of Cl Channels
Increase Cl ion conductance
Membrane hyperpolarization and CNS depression

Pharmacological actions:
CNS: Sedation– Hypnotic– Anaesthesia- Coma

Reduce anxiety, Skeletal muscle relaxation
Anticonvulsant and Amnesia.
CVS: decrease B.P & H.R (higher dose)
Resp. System: depress respiration
Gastric gland: decrease nocturnal acid secretion

prevent stress induced ulcers.
PK: Given orally, intravenously (IV) and rectal (Children)
IM rarely used.
undergoes enterohepatic circulation (Diazepam)
cross placental barrier
(R.S depression & Hypotonia- Floppy Baby syndrome)
secreted in milk
A/E: Drowsiness, confusion, blurred vision, amnesia

Vertigo, Weakness, urine retention, dry mouth
sometimes paradoxical effects – anxiety
convulsions
irritability
Tolerance & Dependence: less with BZDs (Short term )
Uses:
1.Insomnia : i) Transient (1-3 days) Environmental or
situational change
ii) Short term(3-21days) Emotional problem
Physical illness
iii) Chronic insomnia( >21 days) COPD
severe pain, GERD, CHF, Psychosis.
2. Antianxiety /anxiolytic effect :Act on limbic system and

relieve anxiety (at low dose)
3. Skeletal muscle relaxant : inhibit polysynaptic
reflexes at spinal and supra spinal level.
Useful in spinal injury, tetanus, cerebral palsy, and
sprain.
4. Preanaesthetic medication : Sedation, Hypnotic,

Anaesthesia, Reduce anxiety, Skeletal muscle
relaxation, Amnesia (Pt cant recall preoperative event)
5. Anticonvulsant : Diazepam used in status epileptics,

tetanus, febrile convulsions (IV)
Clonazepam used in the absence seizure
6. Gen. anaesthesia : Midazolam / Diazepam used to
maintained.
7. Diagnostic & minor operative procedures:

Endoscopies, before ECT, in Obstetrics
8. To control alcohol withdrawal symptoms : anxiety,

nausea, vomiting, palpitation etc.
9.Conscious sedation : pt is able to communicate &

co-operate during procedure.
10. Along with analgesics and antiulcer agents.

Barbiturates : derivatives of barbituric acid
low therapeutic index
M.O.A : Barbiturates
Prolong the duration of opening of Cl Channels
Increase Cl ion conductance
Membrane hyperpolarization and CNS depression
High dose : GABA mimetic effect, decrease Ca++ and

glutamate activity
Pharmacological actions:
CNS: Sedation– Hypnotic– Anaesthesia- Coma- death

Skeletal muscle relaxation, Anticonvulsant
CVS: decrease B.P & H.R (higher dose)
Resp. System: depress respiration (medullary paralysis)
GIT: decrease tone & motility
GUT : increase release of ADH (decrease urine output)

PK: Given orally, intravenously (IV)
hepatic microsomal enzyme inducers
cross placental barrier, secreted in milk.
A/E: Headache, Drowsiness, confusion, nausea,

Vomiting, vertigo, ataxia, hypotension.
Megaloblastic anaemia (on prolong use)
Precipitation of porphyria (Induce ALA synthase)
Hypersensivity reaction.
Physical & psychological dependence develops on
repeated use
Uses:
1.Insomnia :not recommended (low therapeutic index)
2. Preanaesthetic medication : were used for sedation,

Hypnotic effect.
3. Gen. anaesthesia : Thiopentone or Methohexitone

used for induction of GA
4. Anticonvulsant : Phenobarbitone used in GTCS,

Status epileptics, eclampsia,
Febrile convulsions (IV)
5.Neonatal jaundice of non haemolytic type &
Kernicterus : Phenobarbitone accelerate metabolism
of bilirubin (enzyme induction- glucuronyl transferase)
6. Diagnostic aid in psychiatry : low dose of thiopentone

facilitate verbal communication. (mainly in hysteria)
Acute barbiturate poisoning: rare

mostly accidental or suicidal
Symptoms: Resp. depression, HypoTN, CVS collapse,
Renal failure, and skin eruptions.
Treatment : maintain airway, breathing, circulation

Gastric lavage – after stomach wash
activated charcoal prevent absorption
Alkaline diuresis: IV Sod. Bicarbonate

(facilitate elimination of acidic drugs)
Haemodialysis & haemoperfusion

(through column of activated charcoal / other adsorbant )
Non BZDs
Facilitate GABA mediated neuronal inhibition
CNS depression
 Used for short term treatment

 Rapid & Short acting agents
 Minimal A/E
 Don’t produced dependence/withdrawal effects
Ramelteon: agonist of melatonin receptor
(MT1 & MT2)
reduces sleep latency period
no - rebound insomnia
withdrawal symptoms.
undergoes first pass metabolism.
half life: 2-5 hrs.
S/E : dizziness, drowsiness, ↓testosterone,
↑ prolactin level.
Buspirone: partial agonist of 5 HT1a receptors.
inhibit further release of serotonin.
Benzodizepines Barbiturates
• High therapeutic index • Low therapeutic index

• Commonly use • Restricted use
• Increase frequency of • Prolong duration of opening
opening Cl Channel Cl channel
• No GABA mimetic effect • GABA mimetic effect
• Don’t affect RS & CVS • Can affect
functions
• Low abuse liability • High abuse liability
• No enzyme induction • Enzyme inducers
property
• Antidote – Flumazenil • No antidote available in
Used in overdosage poisoning

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Sedative Hypnotics

• Sedative : dose that reduces excitement,

• Hypnotic : dose that produces sleep that

3. Non benzodizepines: Zolpidem,Zopiclone,Zaleplon

Mech. of action /(M.O.A) BZDs

Bind to GABAA receptor Cl Channel

Increase frequency of opening of Cl Channels

Increase Cl ion conductance

Membrane hyperpolarization and CNS depression

CNS: Sedation– Hypnotic– Anaesthesia- Coma

CVS: decrease B.P & H.R (higher dose)

Resp. System: depress respiration

Gastric gland: decrease nocturnal acid secretion

A/E: Drowsiness, confusion, blurred vision, amnesia

2. Antianxiety /anxiolytic effect :Act on limbic system and

4. Preanaesthetic medication : Sedation, Hypnotic,

5. Anticonvulsant : Diazepam used in status epileptics,

7. Diagnostic & minor operative procedures:

8. To control alcohol withdrawal symptoms : anxiety,

9.Conscious sedation : pt is able to communicate &

10. Along with analgesics and antiulcer agents.

Bind to GABAA receptor Cl Channel

Prolong the duration of opening of Cl Channels

Increase Cl ion conductance

Membrane hyperpolarization and CNS depression

High dose : GABA mimetic effect, decrease Ca++ and

CNS: Sedation– Hypnotic– Anaesthesia- Coma- death

CVS: decrease B.P & H.R (higher dose)

Resp. System: depress respiration (medullary paralysis)

GIT: decrease tone & motility

GUT : increase release of ADH (decrease urine output)

A/E: Headache, Drowsiness, confusion, nausea,

2. Preanaesthetic medication : were used for sedation,

3. Gen. anaesthesia : Thiopentone or Methohexitone

4. Anticonvulsant : Phenobarbitone used in GTCS,

6. Diagnostic aid in psychiatry : low dose of thiopentone

Acute barbiturate poisoning: rare

Treatment : maintain airway, breathing, circulation

Alkaline diuresis: IV Sod. Bicarbonate

Haemodialysis & haemoperfusion

Bind to GABAA receptor Cl Channel

Facilitate GABA mediated neuronal inhibition

 Used for short term treatment

• High therapeutic index • Low therapeutic index

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