3. Sedation : A state of calm, decrease in
alertness and responsiveness. Sleep can
produced by a sedative drug (Tranquillizer).
Hypnosis : A trance-like state, subjects are
passive and highly suggestible – used in
psychiatry.
Anxiety : Adaptive response of the subject
3
14. Kinetics:
• Triazolam > diazepam, alprazolam > oxazepam, lorazepam
• Absorption from IM irregular
• Diazepam, oxazepam, chlordiazepoxide- high protein
bound
• Undergo dealkylation, aliphatic hydroxylation and
Glucuronidation
• Cumulation on repeated administration
14
15. Anti anxiety effect
Hypnosis
Anesthetic effect
Anticonvulsant properties
Muscle relaxant properties
Effects on respiratory and CVS functions
Effects on GI systems
15
16. Anxiety disorders – Alprazolam (with anti
depressants)
Insomnia – Triazolam being the most preferred drug
Lorazepam – compulsive obsessive neuroses
Pre anesthetic medication
Epileptic disorders – Status epilepticus
Myoclonic jerks
Absence seizures
Skeletal muscle relaxation in muscle rigidity due to
cerebral palsy
Alcohol withdrawal
Phencyclidine induced hyper excitability
Atropine poisoning (with diazepam)
16
21. Novel benzodiazepine receptor agonists
BZD1 - anxiolysis, hypnotic
BZD2 – muscle relaxant, amnesia
Zolpidem, zaleplon
Mainly used for insomnia
Minimal effects on REM sleep, muscle relaxant and
Anticonvulsant actions
Safer in pregnancy
21
22. Non benzodiazepine antianxiety, sedative –
hyptonic drugs
Buspirone:
Anxiolytic without sedative or euphoric effects
No anticonvulsant or muscle relaxant effects
No GABA mediated action
Its actions are mediated by 5-HT1A receptor (agonist)
It does not relieve panic disorder
Does not impair driving skills unlike diazepam or
barbiturates
Dose : 5-10mg twice a day
22
23. Classification of barbiturates:
1. Long acting :
With a duration of action of 6 to 8 hrs or more –
Phenobarbitone, Mephobarbitone
2. Intermediate acting:
With a duration of action of 4 to 6 hrs – Amylobarbitone
3. Short acting:
With a duration of action of 2 to 4 hrs- Pentobarbitone,
Secobarbitone
4. Ultra short acting:
With a duration of action of 15 to 30mts – Thiopental,
Thiamylol
23
24. Mechanism of action:
Enhance GABA action --- Cl- influx --- hyperpolarization
Increase duration of opening
Decrease activation of AMPA receptors
24
26. 1. Sedative hypnotic action
2. Anticonvulsant action
3. Action on peripheral nervous system
4. Action of skeletal muscle
5. Respiratory system effects
6. Cardiovascular system effects
7. Effects on gastrointestinal system
8. Hyperalgesia
26
27. Clinical uses of barbiturates:
For initial and short term management of
insomnia
Pre-anesthetic medication
Induction of general anesthesia
For countering the convulsions associated with
chemical substances (tetanus toxin) and clinical
condition like eclampsia, status epilepticus
Long term management of grandmal epilepsy
Hyper bilirubinemia and kernicterus in neonates
27
28. Side effects of Barbiturates:
Potentiating effects with drugs having similar action
CNS, CVS and Respiratory depression,
Tolerance, dependence, Hyperalgesia
Drug automatism
Acute in toxication – forced alkaline diuresis
Drug interactions – steroids, oral contraceptives
Porphyria – contraindicated in acute intermittent
porphyria
Treatment of barbiturate poisoning
28
Sleep is a naturally recurring state of mind and body, characterized by altered consciousness, relatively inhibited sensory activity, inhibition of nearly all voluntary muscles, and reduced interactions with surroundings.
*Sadetives: Drugs that subdue excitement/reduce anxiety (overcome, quieten, or bring under control (a feeling or person)) and clams the patient without inducing normal sleep.
*Hypnotics: drugs which induces and/or maintains sleep, similar to normal sleep.
*Phencyclidine (PCP) is a mind-altering drug that may lead to hallucinations (a profound distortion in a person's perception of reality). It is considered a dissociative drug, leading to a distortion of sights, colors, sounds, self, and one's environment.
