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.
SEDATIVE – HYPNOTICS Sedative : Hypnotics :
SEDATIVE – HYPNOTICS Lower dose of sedative hypnotics have calming effect or Anxiolytic effect . Higher dose of sedative hypnotics produce sleep & Therapeutic Coma.
CLINICAL USES They are used as (Clinical triad) A ntianxiety A nticonvulsant M uscle 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.
DOSE DEPENDENT ACTION SEDATIVE EFFECT HYPNOTIC EFFECT ANESTHESIA COMA
TYPES OF SEDATIVE HYPNOTICS BARBITURATES Benzodiazepines (Anti Anxiety drugs) New Benzodiazepine Long Acting ( 6-8 hrs ) Phenobarbitone Barbital Intermediate Acting ( 3-6 hrs ) Butobarbitone Pentobarbitone Short acting (10-30 min) Theopentone Propofol Long Acting (1-3 days) Diazepam Clonazepam Intermediate Acting (10-20 hrs) Alprazolam Lorazepam Nitrazepam Short acting (3-8 hrs) Midazolam Oxazepam Zolpidem Zolpiclone (only hypnotic)
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
Barbiturates Actions 1. These are powerful cerebral depressants. 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 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.
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.
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.
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 .
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.
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.