2. SEDATIVE – HYPNOTICS
• Sedative : Produce drowsiness without inducing sleep.
They decrease activity and calms the patient. Site of
Action on limbic system of brain
• Hypnotics : Induce sleep resembling like natural sleep.
They produce drowsiness results in onset of sleep, also
maintain sleep. Site of Action on mid brain & RAS of
brain
Mainly drugs used to produce sleep are called
Hypnotics.
4. SEDATIVE – HYPNOTICS
• Lower dose of sedative hypnotics have
calming effect or Anxiolytic effect.
• Higher dose of sedative hypnotics produce
sleep & Therapeutic Coma.
5. CLINICAL USES
• They are used as (Clinical triad)
• Antianxiety
• Anticonvulsant
• Muscle relaxant
• Treatment of Insomnia
• To produce therapeutic coma in case of head injury
• Used for anesthesia eg :- Theopentone
• Treatment of seizure activity.
• Kernicterus (hyper billirubinemia in neonates)
• Treatment of Anxiety disorders.
• Treatment of alcohol withdrawl symptoms.
8. BARBITURATES
• Barbiturates are class of drugs that used to relax the
body and help to produce sleep.
• EXAMPLES :-
– Phenobarbitone & barbital (Long Acting- 6-8 hrs)
– Butobarbitone & Pentobarbitone (Intermediate acting 3-6 hrs)
– Theopentone & Propofol (Short acting 10 – 30 min.)
• Barbiturates depress respiratory center and induce
therapeutic coma.(head injury first line treatment)
• Sudden withdrawal of barbiturate may cause Status
epilepticus
9. Barbiturates Actions
1. These are powerful cerebral depressants.
(a) In smaller doses they produce sedative and in higher doses hypnotic
action. REM sleep is depressed, this produces hangover and increases
dreaming and nightmares on withdrawal
(b) Specific anticonvulsant effect is exerted by Phenobarbitone.
2. In hypnotic doses the blood pressure is reduced marginally but in larger
doses fall in BP is appreciable.
3. In hypnotic doses barbiturates do not exert much effect on kidneys, heart,
liver and intestine.
4. Chronic use of barbiturates results in induction of liver enzymes (P450)
responsible for drug metabolism. This action is responsible for number
of drug interactions.
10. Uses
• 1. For sedating the patient. These drugs have been used to relieve
anxiety and tension during treatment of hypertension, peptic ulcer
and hyperthyroidism.
• 2. Short acting barbiturates are employed to induce sleep.
Intermediate acting barbiturates are used in patients who have
tendency to wake up in middle of the night.
• 3. Phenobarbitone may be used in grandmal epilepsy. It also
controls severe types of convulsions such as status epilepticus and
eclamptic fits.
• 4. It was used as preanesthetic medication.
• 5. It is given in premature children to treat kernicterus.
11. Nursing care
• Ideally barbiturates should not be given to the patient who complains of
insomnia (sleeplessness) without investigating the cause
• Elderly patients should not be given barbiturates. These drugs occasionally
induce confusion and disorientation and during phase of forgetfulness,
these individuals consume many tablets leading to toxicity.
• These drugs are metabolised in the liver and excreted in urine-these
agents should be given cautiously in patients with renal and hepatic
disorders.
• Barbiturates should not be combined with other drugs-especially CNS
depressants.
• Patients must be warned against taking alcoholic drink along with
barbiturates.
12. BENZODIAZEPINES
• Benzodiazepines are class of drugs that works on C.N.S
and used to treat insomnia and anxiety.
• EXAMPLES :-
• Diazepam & Clonazepam (Long Acting)-1-3 days
• Alprazolam, Lorazepam, Nitrazepam (intermediate) -10-20 hrs
• Midazolam, oxazepam (Short)-3-8 hrs
• Benzodiazepines are most commonly used Anxiolytics
• Benzodiazepines MIMICS of GABA
• GABA is main inhibitory neurotransmitter of brain
• Benzodiazepine antagonist/ Antidote – flumazenil.
13. Benzodiazepines
Diazepam, flurazepam and nitrazepam are used as hypnotics. These drugs produce
following actions:
• (a) Sedation or calming: Aggressiveness is reduced. Because of this effect these
agents are used in anxious neurotic patients.
• (b) Hypnosis: Sleep resembling normal sleep is produced. Unlike barbiturates
benzodiazepines do not interfere with REM sleep.
• (c) Anticonvulsant activity: They possess strong anticonvulsant activity. These
agents are used in status epilepticus.
• (d) They relax skeletal muscles and are used in treatment of spastic disorders.
• (e) Benzodiazepines lower blood pressure and are usually prescribed for
hypertension.
• (f) Exert antígrade amnesia.
15. CONTRAINDICATIONS
• Allergy to benzodiazepines
• Pregnancy –cleft lip, cleft palate, pyloric stenosis
• Lactation – neonatal sedation
• Psychosis- (loss of touch and reality, patient might see,
hear and believe are not reality-may have
hallucination or delusion) can increase effect of
psychosis.
• Renal & Hepatic diseases.