SEDATIVES and HYPNOTICS.

sedative hyptonics

1. SEDATIVES and HYPNOTICS 1 Prepared by, Ms. KOTE R. B. Lecturer PRES’s Institute of Pharmacy Loni .

2. Sedative-Hypnotics CNS Depressant drugs Qualitatively same effect But Quantitatively differs Effects are Dose dependent Same drug in small doses acts as Sedative and in higher doses acts as Hypnotics It means their effects are dose dependent 2

3. Sedatives depress CNS, reduce excitement, calm mind and impart tranquility Sedatives induce drowsiness and alleviate anxiety So they also act as Antinxiety or Anxiolytics . Hypnotics are CNS depressants that induce sleep resembling to natural sleep 3 Sedative

4. Sleep is absence of wake full ness Essential in life Person spends about one third of life in sleep Normal Sleep has Two phases These phases cyclically repeat over an interval of about 1 hour NREM (Non Rapid Eye movement Sleep) phase occurs 80 minutes is followed by REM (Rapid eye movement Sleep) phase (occurs for about 20 minutes) 4 Sleep

5. 5 During REM phase eye movements increase in pulse ,respiration, blood pressure Persons get dream in this phase after end of this phase person goes in NREM phase of next cycle and after repeatation of six to seven cycles more or less person wakes up and gets refreshed and relieved from mental fatigueness Although REM phase is disturbing it is essential refreshing brain

6. Classification of Barbiturates according to Duration of action Clas s SUB class Examples Barbiturate Long acting (8 Hours or More) Phenobarbitone ( gardinal Luminal) Mephobarbitone,methobarbitone , Intermedtate acting (4 to 8 Hours) Amobarbitone,Butabarbitonr,pentobarbitone Short acting (Less than 4 Hours) Hexobarbitone and Secobarbitone Ultra short acting (1/2 to 1 Hour Thiopentone sodium ( Intraval ) Metho hexitone 6

7. Classification of Sedative Hypnotic drugs Based on Chemical nature (Continued ) Clas s SUB class Examples Benzodiazepine Diazepam , Oxezapam,Nitrazepam,Lorazapam Chlordiazepoxide ,Clonazepam Flurazepam Midazolam, Alprazolam ( Alprax / Restyl ) Alcohol Ethanol Bromides Sodium bromide , Potassium bromide,Ammonium Bromide Aldehydes Chloraldehyde , Paradehyde Urieds Glutethimide Miscellaneous Antihistaminics Promethazine( Avomine ),Diphenhydramine ( Benadryl 7

8. Barbiturates Pharmacology ADME Absorption from stomach as these are weak acids (more absorbed from acidic medium Metabolised in liver Excreted through kidney P H of urine plays important role excretion increases in alkaline urine .In barbiturate poisoning I.V Sodium bicarbonate is given 8

9. Pharmacological Actions ON CNS – CNS depressant effect . Sedation - Small dose of barbiturates effective in reducing restlessness irritability & nervousness Hypnotics- Depresses CNS induce sleep resembling natural sleep. It is characterized by hangover. Anti-Epileptics- Barbiturates effectively control convulsions of epilepsy & tetanus. 9

10. Respiration - Barbiturates produce respiratory depression CVS- Barbiturates produce fall in Blood pressure& decreases heart rate Kidney - Urine output is decreased due to low Blood Pressure and Increase in ADH and Reduced GFR. Causing oliguria 10

11. Adverse effects Megaloblastic anaemia Tolerance Oliguria Dependence Acute Barbiturate Poisoning 11

12. Therapeutic uses Sr.No . Use Examples 1 Sedation Phenobarbitone,Amylobarbitone,Butobarbitone 2 Hypnosis Phenobarbitone,Pentobaritone,Secobarbitone, 3 Anticonvulsants Antiepileptics ) Phenobarbitone 4 IV General Anaesthetic for Minor surgery Thiopentone sodium, Metho hexitone 5 Preanaesthetic medication Phenobarbitone , Thiopentone sodium 12

13. Preparation- Phenobarbitone - Gardenal , luminal- 30mg, 60mg tab, oral Butobarbitone - Soneryl – 100 mg tab, oral Amylobarbitone – Amytal - 60 mg tab, oral 13

14. Barbturate Poisoning Overdose of Barbiturates causes intoxication Causes - 1) Accidental over doses by drug addicts. 2) Drug automization 3) Suicidal Intention 14

15. 15 Symptoms include Weak but rapid pulse Shallow breathing Chyen stokes breathing Paralytic dilatation of Pupil Renal complication Respiratory depression Coma Death

16. Treatment of Barbiturate poisoning Prompt Hospitalization- within 4 hrs after ingestion patient is hospitalized Gastric lavage or Stomach wash – If patient conscious vomiting can be induced by syrup of ipecac or conc. Salt solution If patient unconscious, simple stomach wash & remove gastric contents Forced diuresis - IV Mannitol or Frusemide Alkalinisation of Urine- Produce significant increase in excretion of barbiturates. Sodium bicarbonate 3.5gm/50ml added in 1 litre fluid administred IV. 16

17. Artificial Respiration Administration of IV Fluids- During treatment forced diuretics advised results in dehydration. To rehydrate to patient IV fluid adviced Peritonial dialysis – for promoting excretion of barbiturates General Nursing care 17

18. Benzodiazepines- Hypnotic action , produce natural sleep without hangover All benzodiazepines relieve anxiety Anticonvulsants These agents are relatively less toxic. Preparations- Diazepam- Valium, calmpose- 5-10 mg Flurazepam- 15-30 mg Nitrazepam- 15-30 mg 18