5384209
Description
Flashcards by Ayman Barghout, updated more than 1 year ago
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Created by Ayman Barghout
almost 8 years ago
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| Question | Answer |
| Barbituric acid | |
| General structure of barbiturates | |
| Uses of barbiturates | They were popular in treating insomnia, now they are not usually used due to their higher toxicity, tolerance, and dependance. They have sedative, hypnotic and anxiolytic action |
| Mechanism of action of barbiturates and BZs | (Potentiating the action of GABA) Enhancing the ability of GABA to bind to the GABA-A receptor which alters its conformation and as a result GABA can bind more easily (allosteric regulation) |
| Thiopental Ultra-short acting barbiturate Available as Sodium salt for IV Induction of anesthesia immediate onset (~ 35 secs), very short duration of action (~ 7.5 mins) Rapid redistribution and metabolism | |
| Methohexital ltra short acting barbiturate for the induction of anesthesia Outpatient oral surgical procedures cuz: Quick onset Rapid recovery | |
| Secobarbital Short acting barbiturate relatively potent with rapid onset of action 10-15 mins Short duration 3-4 hours | |
| Amobarbital Intermediate acting barbiturate slow onset (30 - 60 mins) intermediate duration (6 - 8 hours) | |
| Phenobarbital Long acting barbiturate slow onset ( 45 - 60 minutes ) Long duration ( 10 - 16 hours ) Typical anti-convulsant | |
| General structures of benzodiazepines | |
| Diazepam Long acting anxiolytic, short term management of insomnia associated with daytime anxiety Rapid control of status epilepticus | |
| Flurazepam Higher lipid soluble and more potent than diazepam. Metabolised by N-dealkylation and hydroxylation gives active metabolites | |
| Oxazepam Short acting anxiolytics for short term management of insomnia preferred with patients with hepatic impairment, but with withdrawal symptoms. | |
| Lorazepam Same as Oxazepam but more potent due to the 2-Cl.. Effective when given IV for rapid control of status epilepticus | |
| Clorazepic acid Clorazepate is an intermediate acting anxiolytic prodrug, (Oral) decarboxylated to Nordiazepam then hydroxylated to Oxazepam. Treatment of epilepsy and to relief anxiety associated with alcohol withdrawal. | |
| Clonazepam Mainly metabolized through nitro reduction. Approved by FDA for treatment of epilepsy and panic disorder. | |
| Midazolam Imidazobenzodiazepine derivative Fast onset and short duration ( 3 - 4 hours) Preoperative secation and induction of general anesthesia. | |
| Alprazolam Triazolobenzodiazepine derivative. Short acting anxiolytic ( 10 - 15 hours) Approved for management of anxiety disorder | |
| Quazepam Increased selectivity due to sulfur substitution. Long acting due to N1 Substitutions, Cl & F. | |
| Phenytoin Hydantoin derivative ring contracted analogue of phenobarbital All kind of seizure except for absence seizure. Inhibits the excessive neuronal firing by binding to a site neigboring to VGSC. | |
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