Flashcards

Structures of drugs affecting the CNS and their SAR

Ayman Barghout Inglês 21 flashcards

Flashcards do conjunto (21)

1—Barbituric acid
2General structure of barbiturates
3Uses of barbituratesThey 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
4Mechanism 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)
5—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
6—Methohexital
ltra short acting barbiturate for the induction of anesthesia
Outpatient oral surgical procedures cuz:
Quick onset
Rapid recovery
7—Secobarbital
Short acting barbiturate
relatively potent with rapid onset of action 10-15 mins
Short duration 3-4 hours
8—Amobarbital
Intermediate acting barbiturate
slow onset (30 - 60 mins)
intermediate duration (6 - 8 hours)
9—Phenobarbital
Long acting barbiturate
slow onset ( 45 - 60 minutes )
Long duration ( 10 - 16 hours )
Typical anti-convulsant
10General structures of benzodiazepines
11—Diazepam
Long acting anxiolytic, short term management of insomnia associated with daytime anxiety
Rapid control of status epilepticus
12—Flurazepam
Higher lipid soluble and more potent than diazepam.
Metabolised by N-dealkylation and hydroxylation gives active metabolites
13—Oxazepam
Short acting anxiolytics for short term management of insomnia
preferred with patients with hepatic impairment, but with withdrawal symptoms.
14—Lorazepam
Same as Oxazepam but more potent due to the 2-Cl..
Effective when given IV for rapid control of status epilepticus
15—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.
16—Clonazepam
Mainly metabolized through nitro reduction.
Approved by FDA for treatment of epilepsy and panic disorder.
17—Midazolam
Imidazobenzodiazepine derivative
Fast onset and short duration ( 3 - 4 hours)
Preoperative secation and induction of general anesthesia.
18—Alprazolam
Triazolobenzodiazepine derivative.
Short acting anxiolytic ( 10 - 15 hours)
Approved for management of anxiety disorder
19—Quazepam
Increased selectivity due to sulfur substitution.
Long acting due to N1 Substitutions, Cl & F.
20—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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