Barbiturates

Presented By

Rasel mahbub
&
Ananta sutradhar
CNS depressants
 CNS depressants are substances that can slow brain activity by
selectively depressing neuronal activity in posterior
hypothalamus.
 Barbiturates are derivatives which is synthesized by urea &
malonic acid.
Malonic acid

Barbituric acid

Barbiturates
 It was first prepare by a german scientist Adlof Von Baeyer in
1864,combining urea from animal & malonic acid from apples.
 It was used as sleeping aid(hypnotic only) from 1903-
1950.Since 1950 they have been popular drug in the
UK,these were previously popular drug of abuse.
 It was estimated that 27000 peoples died from
barbiturates overdose in the UK between 1959-1974.
Synthesis
Progressive grade of CNS
depressant
Sedation

Hypnosis

Narcosis

General anaesthesia

Coma

Death
Classification
according to duration of action

.Ultra-short acting Properties

1.Theopental act within second
2.Hexo-barbitone D/A:30 min
Main use:
as I/V anaesthesia
Short acting Properties

1.Pento-barbitone D/A:2 hours

2.Quino-barbitone Main use:
as sedative
 Intermediate acting Properties
 1.Amilo-barbitone D/A:3-6 hour
 2.Allo-barbitone Main use
 3.Buto-barbitone Hypnotic
 4.Vin-barbitone
 A)Long acting Properties

1.Barbitone D/O:>6 hour

2.Pheno-barbitone Main use:
3.Mepho-barbitone Anticonvulsant
4.Apo-barbitone
According to chemical structure
 1.Oxybarbiturate
 (If oxygen is present)
 2.Thiobarbiturate
 (If oxygen is replaced by sulpher)
Mechanism Of Action
 Barbiturates are general depressants of all cell of the
body,acting as a cellular histotoxic agent.But the cell of the
CNS are more sensitive to barbiturate action.
 1.Barbiturate induce sleep by selectively depressing RAS in
the brain stem.
 2.Barbiturate selectively depress neuronal activity in
posterior hypothalamus,amygdaloid nucleus& limbic
structure (CNS depression)
 3.Barbiturates depress monosynptic pathway of spinal
cord(anticanvulsion)
 4.Barbiturates have also GABA like activity or enhance
GABA activity.
Mechanism of action
Barbiturate+GABA

Activation of GABA receptor

Opening of chloride channel

Increase the duration of GABA gated channel opening

Hyperpolarisation of cells

Depression of CNS
Pharmacological action of
Barbiturates
 A.On CNS
 1.Mild degree of sedation to general anaesthesia.
 2.Anticonvulsant effect.
 3.Respiratory centre depression

 B.On CVS
 1.Hypotension
 2.Decrease heart rate
 3.Circulatory collapse
 C.On liver
 1.Enzyme induction,so increase metabolism of itself &
other drugs.
 2.Stimulate glucoronyl transferase.

 D.On kidney
 1.Antidiuretic effect (increase ADH)
 2.Decrease urinary output by depressing GFR
 E.On eye
 1.No effect (normal dose)
 2.Miosis ( toxic effect)

 F.On GIT
 1.Constipation (on prolong use)
Structure
Indication
1.As anticonvulsant
tetanus
eclampasia,
epilesy
cerebral haemorrhage
convulsant drug poisoning
during surgical anaesthesia
2.As sedative & hypnotic
3.Intravenous anaesthesia
4.Hyperbilurobinaemia & kernicterous
 5.Haemolytic jaundice
 6.Cholestasis
 7.In narco analysis &narcopathy
 8.Identifying the dominant cerebral haemisphere for
speech prior to neuro surgery
 9.Kernicterus in children
Contraindication
 1.Pulmonary insufficiency,pulmonary emphysema
 2.In idiosyncratic patient
 3.Acute intermittent pophyria
 4.In impaired renal function
 5.In hepatic failure
 6.Ptient with suicidal tendency
 7.CCF & hypovolmic shock
Adverse effect of Barbiturates
 1.Pain;Localized or diffuse myalgic,neuralgic or
arthritic pain especially in psychoneurotic patient.
 2.Allergic skin lessions
 3.After effects
 drowsiness
 Hangover effect
 Over excitement
 Night mares & night terrors
 weakness & lethargy
 4.Drug automatism
 5.Enzyme induction (so tolerance develops rapidly)
 6.Idiosyncratic reaction:barbiturates precipitate
attacks of acute porphyria in sussceptible individual.
Doses of barbiturates
 The typical dose of phenobarbital use as
anticonvulsant,,
 For adult:50-100 mg,2/3 times per day
 For newborn:2-4 mg per kilogram of body weight per
day
 For infant:5-8 mg per kilogram pf body weight
 For sedation before surgery 100-200 mg,one hour
before surgery
Commercial brand name available
in BD
 Brand Name Manufacturer
 Barbit Incepta pharma
 Genesia DS Square
 Nelepsin Beximco
 Parotin ACI pharma
 Sedative:Drugs that reduce anxiety,excitement & exert
calming effect without effecting mental function.It is
usually lower or normal dose,not higher dose.
 Hypnotic:Drugs those cause of sleep are called
hypnotic. Usually higher dose not normal or lower
dose
 Sedative given day time hour,they makes patient
drowsy not sleep
 Hypnotics are given at night of sleep