Exam 7 Flashcards by Conor Young

GABA Related CNS Depressants

Alprazolam
Lorazepam
Midazolam
Zolpidem
Flumazenil

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Non GABA CNS Depressants

Buspirone
Suvorexant
Ramelteon

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Sedation

A state of decreased state of responsiveness to external stimuli

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Hypnosis

Sleep like state from which the individual can still be aroused

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Unconsciousness

Unresponsive to external stimuli but still responsive to pain and showing involuntary movement

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Anesthesia

Deeper state of unconsciousness where individual is unresponsive to external stimuli and pain and is paralyzed an amnestic

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Hypnotic Sedative Site of Action

Pons and Brainstem

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Benzodiazepine General Mechanism

Allosteric GABA A receptor agonist
Binds to the alpha and gamma subunit interface
Enhances effect of GABA on the receptor

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GABA A Receptor Function

Lets Cl- into the cell which leads to hyperpolarization

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GABA A Alpha 1 Receptor Activation Effect

Sedation
Anterograde amnesia
Ataxia

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GABA A Alpha 2 and 3 Receptor Activation Effect

Anxiolytic
Skeletal muscle relaxation

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Alprazolam Use

Anxiolysis

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Alprazolam Half Life

12 hrs

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Lorazepam Use

Anxiolysis
Status Epilepticus
Procedural Sedation
Alcohol Withdrawal

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Lorazepam Half Life

10 to 12 hrs

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Midazolam Use

Procedural Sedation
Anxiolysis

Midazolam Half Life

Anxiety Before Surgical Procedures
Procedural Sedation

Benzodiazepine Onset Time

Same regardless of duration

Benzodiazepines as a Treatment for Epilepsy

Not advised
Tolerance develops

Benzodiazepine Tolerance

Develops quickly to hypnosis and seizure treatment
DOES NOT DEVELOP TO ANXIOLYSIS

Difference Between Benzodiazepines and Barbiturates

Barbiturates can activate the GABA A receptor without GABA present

Flumazenil Mechanism

Competitive antagonist at the benzodiazepine receptor

Flumazenil Pharmacokinetics

Give IV
1 to 2 min onset
1 hr half life

Flumazenil Usage

Rapid reversal of benzodiazepine sedation
Antidote to benzodiazepine overdose
DOES NOT REVERSE AMNESIA

Flumazenil Adverse Effects

Benzodiazepine withdrawal seizures More apparent in seizure prone patients

Z Drug Non Benzodiazepine Benzodiazepine Receptor Agonists

Zolpidem

Z Drugs Specific Mechanism

Same as Benzodiazepines but Selective for GABA A Alpha 1 Subunits Only gives hypnosis and amnesia NO ANXIOLYSIS OR MUSCLE RELAXATION

Z Drug Pharmacokinetics

Oral Short 1.5 to 7 hr half life

Z Drug Adverse Effects

Daytime Sedation Cognitive Impairment Ataxia Complex Sleep Behavior Additive Effects With Other Depressants

Dual Orexin Receptor Antagonist DORAs

Suvorexant

Orexin A and B Neuropeptide Function

Regulate arousal, wakefulness, and appetite Lack of this receptor causes Type 1 Narcolepsy Cataplexy

DORA General Mechanism

Inhibits Orexin A B Receptors Induces sleep by inhibiting these wakefulness receptors

DORA Uses

Insomnia in adults and Alzheimer’s patients Short acting hypnotic half life 12 hrs

DORA Adverse Effects

Residual daytime sedation Ataxia Complex sleep behaviors and REM disorders Mild potential for dependence and abuse

Melatonin Receptor Agonists

Ramelteon

Melatonin Receptor Agonist Mechanism

Agonist at MT1 MT2 hypothalamic melatonin receptor

Melatonin Receptor Agonist Use

Mild insomnia Regulation of sleep wake cycles Jet lag

Buspirone Mechanism

Presynaptic 5 HT1A Autoreceptor Partial Agonist Dopamine D2 and Adrenergic Alpha 2 Receptor Antagonist DOES NOT INTERACT WITH GABA

Buspirone Use

Anxiolysis WITHOUT SEDATION Only good for GAD No Dependence or Withdrawal Not additive with other CNS depressants 3 to 4 week onset