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Sedative-Hypnotics Drugs Pharmacology : - Coggle Diagram
Sedative-Hypnotics Drugs
Pharmacology :
1.Benzodiazepines
Clinical Use
Acute anxiety states,panic attacks, GAD,Insomnia,skeletal muscle relaxation,Seizure disorder
Mechanism of Action
Bind GABA A receptor subunits to facilitate chloride channel opening and increase frequency - membrane hyperpolalization
Toxicities
Extension of CNS depressant actions
Drugs
Alprazolam
Chlordiazepoxide
Clorazepate
Clonazepam
Diazepam
Flurazepam
Lorazepam
Midazolam, etc
Pharmacokinetics
Hepatic metabolism ,Half-life : 2-4 hrs.
3.Barbiturates
Clinical Use
Anesthesia (thiopental) ,insomnia and sedation(Secobarbital),Seizure
disorders (phenobarbital)
Pharmacokinetics
Oral activity: Hepatic Metabolism, Half-lives: 4–60 h
Mechanism of Action
Bind to GABA a receptor sites ,Facilitate chloride opening and increase duration
Toxicities
Extension of CNS depressant actions
Drugs
Amobarbital
Butabarbital
Pentobarbital
Phenobarbital
Secobarbital
Thiopental
2.Benzodiazepine antagonist
Drugs
Flumazenil
Mechanism of Action
Antagonist at benzodiazipine sites on GABA a receptor
Clinical Use
Management of benzodiazipine overdose
Pharmacokinetics
IV form,Short half-life
Toxicities
Agitation,Confusion
4.Newer hypnotics
Clinical Use
Sleep disorders
Pharmacokinetics
Oral activity, P450 substrates,Short half-lives
Mechanism of Action
Bind to GABA a receptor sites ,Facilitate chloride opening and increase duration
Toxicities
Extension of CNS depressant effects dependence liability.
Drugs
Eszopiclone
Zaleplon
Zolpidem
6.5-HT agonist
Clinical Use
Generalized anxiety states
Pharmacokinetics
Oral activity , Interaction with CYP3A4 induces and inhibits: Short half-life
Mechanism of Action
Partial agonist at 5-HT receptors and possibly D2 receptors
Toxicities
GI distress, tachycardia,Parathesias
Drugs
Buspirone
5.Melatonin receptor agonist
Clinical Use
Sleep disorders
Pharmacokinetics
Oral activity; forms active metabolite via CYP1A2
Mechanism of Action
Activates MT1 and
MT2 receptors in suprachiasmatic nucleus
Toxicities
Dizziness, fatigue, endocrine changes
Drugs
Ramelteon