Sedative-Hypnotic Drugs Flashcards
Alprazolam
Benzodiazepine
Benzodiazepines
Alprazolam Chlordiazepoxide Clonazepam Diazepam Lorazepam Triazolam
Chlordiazepoxide
Benzodiazepine
Clonazepam
Benzodiazepine
Diazepam
Benzodiazepine
Lorazepam
Benzodiazepine
Lorazepam
Benzodiazepine
Diazepam
Lorazepam
Mechanism of action
Bind to specific GABA(A) receptor subunits at central nervous system (CNS) neuronal synapses facilitating frequency of GABA-mediated chloride ion channel opening- enhance membrane hyperpolarization
Bind to specific GABA(A) receptor subunits at central nervous system (CNS) neuronal synapses facilitating frequency of GABA-mediated chloride ion channel opening- enhance membrane hyperpolarization
Diazepam
Lorazepam
Mechanism of action
Diazepam
Lorazepam
Effects
Dose-dependent depressant effect on the CNS including sedation and relief of anxiety, Amnesia, Hypnosis, Anesthesia, Coma and Respiratory depression
Dose-dependent depressant effect on the CNS including sedation and relief of anxiety, Amnesia, Hypnosis, Anesthesia, Coma and Respiratory depression
Diazepam
Lorazepam
Effects
Diazepam
Lorazepam
Clinical applications
Acute anxiety states, Panic attacks, Generalized anxiety disorder, Insomnia and other sleep disorders, Relaxation of skeletal muscle, Anesthesia (adjunctive) Seizure disorders
Acute anxiety states, Panic attacks, Generalized anxiety disorder, Insomnia and other sleep disorders, Relaxation of skeletal muscle, Anesthesia (adjunctive) Seizure disorders
Diazepam
Lorazepam
Clinical applications
Diazepam
Lorazepam
(Benzodiazepines in general)
Pharmacokinetics, Toxicities, Interactions
Half-lives from 2-40 h, Oral activity, Hepatic metabolism-some active metabolites, TOXICITY: extensions of CNS depressant effects, dependence liability, INTERACTIONS: Additive CNS depression with ethanol and many other drugs
Half-lives from 2-40 h, Oral activity, Hepatic metabolism-some active metabolites, TOXICITY: extensions of CNS depressant effects, dependence liability, INTERACTIONS: Additive CNS depression with ethanol and many other drugs
Diazepam
Lorazepam
(Benzodiazepines in general)
Pharmacokinetics, Toxicities, Interactions
Benzodiazepine antagonist
Flumazenil
Flumazenil
Benzodiazepine antagonist
Flumazenil
Mechanism of action
Antagonist at benzodiazepine binding sites on the GABA(A) receptor
Antagonist at benzodiazepine binding sites on the GABA(A) receptor
Flumazenil
Mechanism of action
Flumazenil
Effects
Blocks actions of benzodiazepines and zolpidem but not other sedative-hypnotic drugs
Blocks actions of benzodiazepines and zolpidem but not other sedative-hypnotic drugs
Flumazenil
Effects
Flumazenil
Clinical applications
Management of benzodiazepine overdose
Management of benzodiazepine overdose
Flumazenil
Clinical applications
Flumazenil
Pharmacokinetics, Toxicities, Interactions
IV, short half-life, TOXICITY: Agitation, Confusion, Possible withdrawal symptoms in benzodiazepine dependence
IV, short half-life, TOXICITY: Agitation, Confusion, Possible withdrawal symptoms in benzodiazepine dependence
Flumazenil
Pharmacokinetics, Toxicities, Interactions
Barbiturates
Amobarbital Butabarbital Mephobarbital Pentobarbital Phenobarbital Secobarbital
Amobarbital
Barbiturate
Butabarbital
Barbiturate
Barbiturate
Barbiturate
Mephobarbital
Barbiturate
Pentobarbital
Barbiturate
Phenobarbital
Barbiturate
Secobarbital
Barbiturate
Secobarbital
Pentobarbital
Phenobarbital
Mechanism of action
Bind to specific GABA(A) receptor subunits at CNS neuronal synapses increasing duration of GABA-mediated chloride ion channel opening, enhance membrane hyperpolarization
Bind to specific GABA(A) receptor subunits at CNS neuronal synapses increasing duration of GABA-mediated chloride ion channel opening, enhance membrane hyperpolarization
Secobarbital
Pentobarbital
Phenobarbital
Mechanism of action
Secobarbital
Pentobarbital
Phenobarbital
Effects
Dose-dependent depressant effect on the CNS including sedation and relief of anxiety, Amnesia, Hypnosis, Anesthesia, Coma and Respiratory depression.
Steeper dose-response relationship then Benzodiazepines
Dose-dependent depressant effect on the CNS including sedation and relief of anxiety, Amnesia, Hypnosis, Anesthesia, Coma and Respiratory depression.
Steeper dose-response relationship then Benzodiazepines
Secobarbital
Pentobarbital
Phenobarbital
Effects
Barbiturates
Clinical applications
Anesthesia (thiopental)
Insomnia (secobarbital)
Seizure disorders (phenobarbital)
Anesthesia (thiopental)
Insomnia (secobarbital)
Seizure disorders (phenobarbital)
Barbiturates
Clinical applications
Secobarbital
Pentobarbital
Phenobarbital
(Barbiturates in general)
Pharmacokinetics, Toxicities, Interactions
Half-lives from 4-60 h, Oral activity, Hepatic metabolism-phenobarbital 20% renal elimination. TOXICITY: extensions of CNS depressant effects, dependence liability > benzodiazepines. INTERACTIONS: Additive CNS depression with ethanol and many other drugs, induction of hepatic drug-metabolizing enzymes
Half-lives from 4-60 h, Oral activity, Hepatic metabolism-phenobarbital 20% renal elimination. TOXICITY: extensions of CNS depressant effects, dependence liability > benzodiazepines. INTERACTIONS: Additive CNS depression with ethanol and many other drugs, induction of hepatic drug-metabolizing enzymes
Secobarbital
Pentobarbital
Phenobarbital
(Barbiturates in general)
Pharmacokinetics, Toxicities, Interactions
Newer hypnotics
Eszopiclone
Zaleplon
Zolpidem
Eszopiclone
Newer hypnotic
Zaleplon
Newer hypnotic
Zolpidem
Newer hypnotic
Eszopiclone
Zaleplon
Zolpidem
Mechanism of action
Bind selectively to a subgroup of GABA(A) receptors, acting like benzodiazepines to enhance membrane hyperpolarization
Bind selectively to a subgroup of GABA(A) receptors, acting like benzodiazepines to enhance membrane hyperpolarization
Eszopiclone
Zaleplon
Zolpidem
Mechanism of action
Eszopiclone
Zaleplon
Zolpidem
Effects
Rapid onset of hypnosis with few amnestic effects or day-after psychomotor depression or somnolence
Rapid onset of hypnosis with few amnestic effects or day-after psychomotor depression or somnolence
Eszopiclone
Zaleplon
Zolpidem
Effects
Eszopiclone
Zaleplon
Zolpidem
Clinical applications
Sleep disorders, especially those categorized by difficulty in falling asleep
Sleep disorders, especially those categorized by difficulty in falling asleep
Eszopiclone
Zaleplon
Zolpidem
Clinical applications
Eszopiclone
Zaleplon
Zolpidem
Pharmacokinetics, Toxicities, Interactions
Oral activity, short half-lives, CYP substrates. TOXICITY: extensions of CNS depressant effects, dependence liability, INTERACTIONS: Additive CNS depression with ethanol and many other drugs
Oral activity, short half-lives, CYP substrates. TOXICITY: extensions of CNS depressant effects, dependence liability, INTERACTIONS: Additive CNS depression with ethanol and many other drugs
Eszopiclone
Zaleplon
Zolpidem
Pharmacokinetics, Toxicities, Interactions