Anxiolytics Flashcards

1
Q

Describe the mechanism of action of barbiturates.

A

They bind to sites on the GABA-A receptor which enhances the duration of GABA-mediated Cl- flux. At high doses it can directly open the Cl- channels. This causes hyperpolarization resulting in neuronal inhibition.

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2
Q

Name the barbiturates.

A

Phenobarbital

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3
Q

Describe the adverse effects associated with barbiturates.

A

They have a low therapeutic index putting patients at risk for overdose and also have a high rate of dependence/addiction.

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4
Q

What anxiolytics are CYP inducers?

A

Barbiturates

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5
Q

What are some clinical indications for barbiturates?

A

Anesthesia and seizure disorders, rarely as a sedative or hypnotic

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6
Q

Describe the mechanism of action of benzodiazepines.

A

They bind to sites on the GABA-A receptor facilitating GABA-mediated Cl- influx, causing hyperpolarization and thus neuronal inhibition.

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7
Q

Describe the adverse effects associated with benzodiazepines.

A

Higher doses can cause anterograde amnesia (though this is beneficial for anesthesia purposes), resp depression, decreased BP, increased HR, some tolerance (but less than barbiturates)

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8
Q

Describe the drug interactions of benzodiazepines.

A

There aren’t any.

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9
Q

Name the clinical indications for benzodiazepines.

A

Epilepsy tx, anesthesia (e.g. midazolam- Versed), muscle relaxation for neuro disorders

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10
Q

What is a contraindication for benzodiazepines?

A

Sleep apnea (b/c of resp depression)

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11
Q

Describe the pharmacokinetic properties of benzodiazepines.

A

They have slower absorption (2-4 hours, but rapid CNS entry), convert to active metabolizes, and are excreted in the urine.

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12
Q

How do benzodiazepines differ from barbiturates?

A

Benzos can’t directly open the Cl- channel so they have no effect without the presence of GABA, which helps to limit toxicity and have a higher therapeutic index than barbiturates.

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13
Q

Describe the mechanism of action of benzodiazepine receptor agonists.

A

They are chemically distinct from benzodiazepines but bind to the same benzodiazepine binding site on a subset of the GABA-A receptors

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14
Q

Name the drugs that act at the GABA receptor.

A

Barbiturates, benzodiazepines, benzodiazepine receptor agonists, and benzodiazepine receptor antagonists

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15
Q

What are the adverse effects associated with benzodiazepine receptor agonists?

A

Decreased clearance in elderly/hepatic dysfunction, resp depression at high doses, anterograde amnesia, sleep-walking

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16
Q

What are the clinical indications for benzodiazepine receptor agonists?

A

Middle of the night waking. Has less REM suppression and less tolerance/psychological dependance/abuse than benzos

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17
Q

Describe the pharmacokinetic properties of benzodiazepine receptor agonists.

A

They are rapid-acting, short duration drugs.

18
Q

Describe the mechanism of action of benzodiazepine receptor antagonists.

A

They reverse the effects of benzos and hypnotics like zoipidem

19
Q

What are the adverse effects associated with benzodiazepine receptor antagonists?

A

They can precipitate severe withdrawal in patients with psychological dependence (as severe as seizures)

20
Q

Describe the clinical indications for benzodiazepine receptor antagonists.

A

Benzo overdose and to hasten recovery post-op

21
Q

Describe the pharmacokinetic properties of benzodiazepine receptor antagonists.

A

They are rapid-active and short duration (30-60 min) so in cases of overdose you have to give repeated doses.

22
Q

Do benzodiazepine receptor antagonists reverse alcohol or bartiturates?

A

No mothafucka

23
Q

Name the benzodiazepines.

A

Diazepam (Valium), triazolam, alprazolam (Xanax), clonazepam (Klonopin), midazolam (Versed)

24
Q

Name the benzodiazepine receptor agonists.

A

Zolpidem (Ambien), eszopiclone (Lunesta)

25
Q

Name the benzodiazepine receptor antagonists.

A

Flumazenil

26
Q

Describe the mechanism of action of melatonin congener (ramelteon).

A

It is a synthetic agonist acting at the MT1 and MT2 melatonin receptors.

27
Q

Describe the adverse effects associated with melatonin congener.

A

Dizziness, hyperprolactinemia (elevated prolactin- a pituitary hormone that induces breast milk production)

28
Q

Describe the clinical indications for melatonin congener (ramelteon).

A

Insomnia (approved for longterm use), best against delayed onset sleep and circadian rhythm problems.

29
Q

Describe the mechanism of action of non-sedative anxiolytics.

A

Partial agonists at CNS 5-HT receptors.

30
Q

Describe the adverse effects associated with non-sedative anxiolytics.

A

They are slow to act, poor efficacy with panic disorders. Can cause chest pain, tachycardia, palpitations, dizziness, nervousness, tinnitus, GI problems

31
Q

What are the contraindications associated with non-sedative anxiolytics.

A

DO NOT USE WITH MAOIs.

32
Q

Describe the pharmacokinetic properties of non-sedative anxiolytics.

A

They are rapidly absorbed.

33
Q

Name the non-sedative anxiolytics.

A

Buspirone

34
Q

What is the definition of a sedative?

A

A drug causing a calming effect; tranquilizer

35
Q

What is the definition of hypnotic?

A

A sleep-inducing or promoting drug

36
Q

What is the definition of an anxiolytic?

A

To cut anxiety

37
Q

How are panic disorders best treated?

A

With antidepressants, particularly SSRIs. Alprazolam is effective but can cause rebound anxiety when discontinued.

38
Q

What medication is useful for the treatment of agoraphobia?

A

Alprazolam

39
Q

What are effective treatments for social phobia?

A

Behavioral therapy, SSRIs, other ADDs, and clonazepam

40
Q

What treatment is effective for generalized anxiety disorder (GAD)?

A

Benzodiazepines, buspirone, some ADDs.