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Sedatives hypnotic

4th year med student!!psychiatry....

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Sedatives hypnotic

  2. 2. • Sedative-refers to a substance that moderates activity and excitement while inducing calming effect. • Hypnotic-refers to a substance that causes drowsiness and facilitates the onset and maintenance of natural sleep.
  3. 3. SEDATIVE- HYPNOTICS Benzodiapines Barbiturates Miscellaneou s
  4. 4. BENZODIAPINES • All the benzodiapines have the same general chemical structure • They are mostly classified into 3 groups: a) short-acting b) Intermediate acting c) Long acting
  5. 5. BENZODIAPINE CLASSIFICATION HALF-LIFE Midazolam Short-acting 2-6 Triazolam Short-acting 2-3 Alprazolam Intermediate-acting 12-15 Estazolam Intermediate-acting 10-24 Lorazepam Intermediate-acting 10-20 Temazepam Intermediate-acting 10-40 Clonazepam Long-acting 18-50 Clorazepate Long-acting 40-50 Diazepam Long-acting 20-80 Flurazepam Long-acting 40-100
  6. 6. MOA • They act on GABA receptors, either increasing or decreasing the concentrations and activities of the neurotransmitters, like GABA, serotonin, noradrenaline, thus inducing sleep. • Indications • benzodiazepine can be used in a variety of treatments. They are used to treat nervousness and anxiety; therefore they are very effective to treat insomnia associated with anxiety and mood instability.
  7. 7. • The use of benzodiazepines can lead to abuse, whether they are taken properly or for the wrong reasons • Prescribing benzodiapines guidelines 1. Be very cautious about initiating a prescription for benzodiapines. 2. Prescribe the lowest dose possible. 3. Limit the prescription to 2-3 weeks. 4. Do not have prescriptions available for routine repeat refills 5. Never re-prescribe if the patient reports losing or forgetting their tablets 6. Do not prescribe benzodiapines for another doctor’s patients; tell them to go to their usual prescriber.
  8. 8. Short term effects(low doses) • Euphoria • “Being in a happy world” • Fatigue • Feeling drowsy • Shallow breathing • Not being able to take full, deep, normal breaths (2) • Trouble coordinating your movements Short term effects(high doses) • Paranoia • Aggression • Easily agitated • Difficulty remembering • Irritability • l
  9. 9. Long term effects • “Rebound effects” • Over use of these drugs can cause a reversal effect • Seizures can occur; calm and relaxed feelings dissipate • Tolerance develops, resulting in dependence • Must have more and more of the drug to feel an even minor effects • Higher risk of overdose • Withdrawal • This leads to dependence as well • No one wants to feel the unpleasant withdrawal effects, so continues use (2) COGNITVE EFFECTS • Memory impairment/Amnesia • Confusion • Sleepiness
  10. 10. BARBITURATES • Barbiturates are actually known as CNS depressants or central nervous system depressants and are in this class of drug along with benzodiazepines • Basically, the barbiturates have had their day in medicine and largely been replaced by much safer benzodiapines and other CNS drugs. • The molecular site of action for the barbiturates is nearly the same as for the benzodiapines
  11. 11. • However, there is a significant difference in the effect of barbiturates at these receptors that is dependent on dose administered: I. At lower doses, barbiturates act like benzodiapines and simply increase the effect of GABA at GABAα receptor I. At higher doses ,barbiturates may act as direct agonists at GABAα receptors in place of GABA ,producing profound CNS depression.
  12. 12. EXAMPLES OF BARBITURATES Barbiturate Reference Table (list of barbiturates) Chemical Name Brand Name Half Life Allobarbital n/a n/a Alphenal n/a n/a Amobarbital Amytal Short Aprobarbital Alurate Short Brallobarbital Vesparax (mixed) No Reference Butobarbital Soneryl, Butisol Short Butalbital Fiorinal, Fioricet Medium Cyclobarbital Phanodorm Medium Methylphenobarbital Prominal Long Mephobarbital Mebaral Long Methohexital Brevital Very Short Pentobarbital Nembutal Short Phenobarbital Luminal Long Secobarbital Seconal Short Talbutal Lotusate Medium Thiamylal Surital Very Short Thiopental Pentothal Very Short
  13. 13. USES • A barbiturate may be prescribed for a variety of reasons, the list is extensive, but the most common use today is as an anesthesia for surgery. This form is hardly ever abused because they cause almost immediate unconsciousness. However, other forms like Phenobarbital are used in treating various seizure disorders as an anticonvulsant. Other uses of this form of barbiturate along with mephobarbital include treating anxiety, insomnia, epilepsy and delirium tremens
  14. 14. SIDE EFFECTS • The symptoms of barbiturate intoxication resemble those of alcohol: slurred speech,incoherence,drowsiness and low mood. • Tolerance develops to barbiturates, although less quickly than to opioids. • Withdrawal -The abrupt withdrawal of barbiturates from dependent person can be followed by a withdrawal syndrome resembling that occurring with alcohol, with a high risk of seizures.
  15. 15. OTHER SEDATIVE/MISCELLANEOUS • Zalopan,Zolpidem and Zoplicone • All of the bind to the benzodiapine receptor at the GABAα receptor and increase the effect of GABA. • However ,none of these drugs produce effects that are identical to the benzodiapines ,and all of these drugs have chemical structure that are unrelated to the benzodiapines.
  16. 16. • For the treatment of insomnia, they act quickly but short duration of action. Hence, making them more suitable for patients who have trouble falling asleep and have a preference for less residual effects the next day.
  17. 17. THANK YOU  