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Brain and behavior > Sedatives, Hypnotics, Anxiolytics, and Alcohol > Flashcards

Sedatives, Hypnotics, Anxiolytics, and Alcohol Flashcards

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1
Q

General effects of sedative hypnotics

A

Anti-anxiety/calming effect, sedation, anterograde amnesia, sleep, anesthesia, anticonvulsant, muscle relaxation, effects on respiratory and cardiac function.

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2
Q

Why are benzodiazepines safer than barbiturates?

A

Because they have a flatter dose response curve, and they increase frequency of GABA a channel opening, but don’t keep the channel open themselves.

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3
Q

What happens when benzo/barbs administered with other CNS depressants?

A

Additive effects.

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4
Q

Order of effects for benzos/barbs

A

Anti-anxiety, sedation, hypnosis, anesthesia, coma

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5
Q

Most common GABA a receptor structure

A

2 alpha 1s
2 beta 2s
1 gamma 1

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6
Q

Where do GABA, Benzos, Barbiturates bind on GABA a receptor?

A

GABA: Between A and B subunits
Benzos: Between A and G subunits
Barbiturates: many sites

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7
Q

Do sedative hypnotics have a high affinity for the GABA B receptor?

A

No

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8
Q

Role of A1, A2/3, and A5 subunits in the GABA receptor?

A

A1- sedation, amnesia, ataxia
A2/3 - anxiolysis, muscle relaxing properties
A5- Memory impairment?

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9
Q

Sedative-hypnotic withdrawal symptoms?

A

Anxiety/agitation, restlessness, tremor, seizures, hyperactive reflexes

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10
Q

Worst consequence of sudden withdrawal from benzos, barbs, alcohol?

A

Death

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11
Q

Ultra short acting barbiturate?

A

Thiopental, no longer available in the US

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12
Q

Immediate acting barbiturates?

A

Secobarbital, butalbital.

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13
Q

Long acting barbiturate?

A

Phenobarbital

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14
Q

Pharmocokinetics

A

AD: rapid
M: Oxidation to form alcohols, acids, and ketones.
E: Renal.

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15
Q

Use of Barbiturates in clinical practice?

A

Epilepsy, induction of anesthesia, PAS, capital punishment, combination headache remedies.

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16
Q

Barbiturate Toxicit

A

Small/midpoint pupils, coma, hypertension, decreased myocardial contractivity.

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17
Q

Key group in benzodiazepines?

A

Carboxamide group

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18
Q

Do barbiturates work anywhere else?

A

Yes they also depress some of the actions of the AMPA receptor.

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19
Q

Role for benzodiazepines in clinical practice?

A

Panic, anxiety, phobia disorders. Insomnia, epilepsy, alcohol withdrawal. Etc.

20
Q

How are benzodiazepines metabolized?

A

They are all phase I oxidation in the liver except for LORAZEPAM, OXAZEPAM, TEMAZEPAM. Renal excretion.

21
Q

Which benzos are safest in liver patients?

A

Lorazepam, Oxazepam, Temazepam

22
Q

Short acting Benzodiazepines

A

Midazolam, triazolam, oxazepam

23
Q

Intermediate Acting Benzos

A

Temazepam, Alprazolam, Lorazepam, Estazolam

24
Q

Long acting Benzos

A

Clonazepam, Diazepam, Chlordiazepoxide

25
Q

Non-Benzo Hypnotics

A

Zolpidem, Zaleplon, Eszopiclone

26
Q

Which non-benzo hypnotics are fast acting, which are slow?

A

Zolpidem and zaleplon are fast. Eszopiclone is slow.

27
Q

Effect of Benzodiazepines on Sleep

A

Decreases REM, increases Stage 2

28
Q

Effect of new hypnotics on sleep

A

Zolpidem decreases rem, but doesnt effect other things. Zaleplon doesn’t affect REM.

29
Q

Flumazenil

A

Competitive antagonist at benzodiazepine binding site on GABAa receptor, does not block effect of barbs/etoh. Has horrible side effects. R

30
Q

Ramelteon

A

Melatonin receptor agonist, doesn’t do much.

31
Q

Buspirone

A

Some anxiolytic effects, partial agonist at brain 5-HT1A receptors. Some therapeutic latency (1 week)

32
Q

Dexmedetomidine

A

Given IV in ICUs frequently. A2 receptor agonist, sedation by reducing sympathetic activity. Given to respirator patients for sedation. Costs lots. Caution with heart problems.

33
Q

Sedative hypnotics and pregnancy

A

All cross blood brain barrier, some risk of terratogenicity, but is disputed.

34
Q

EtOH metabolism

A

Zero-order: Rate of oxidation is independent of time and concentration of drug.

35
Q

Primary metabolism of EtOH

A

Alcohol dehydrogenase with NAD to turn into acetaldehyde, which is then turned into acetate by aldehyde dehydrogenase. This last step is blocked by disulfiram.

36
Q

Disulfiram

A

Blocks oxidation of Acetaldehyde, causes horrible symptoms when drinking.

37
Q

Ethanol mechanism of action

A

Enhances action of GABA at GABA A receptors, antagonizes glutamate at NMDA.

38
Q

Effect of acute alcohol on heart?

A

Depression of myocardial activity, tachycardia.

39
Q

Ethanol effect on vessels?

A

Vasodilator

40
Q

Effect of chronic alcohol on heart

A

Dilated cardiomyopathy, CAD, hypertension.

41
Q

Wernicke-Korsakoff syndrome

A

Paralysis of external eye muscles, ataxia, confusion, thimine deficiency, chronic disabling memory disorder.

42
Q

Why is taking tylenol bad on alcohol

A

Chronic alcohol use leads to the induction of Cyp450 enzymes, which convert acetaminophen to hepatotoxic metabolites

43
Q

Delirium Tremens

A

Onset due to alcohol withdrawal, roughly 3 days after. Tachycardia, hypertension, low-grade fever, tremor, delirium,

44
Q

How to combat alcohol withdrawal?

A

Benzodiazepine treatment (chlordiazepoxide, diazepam if good hepatic function, lorazepam, oxazepam if poor).

45
Q

Other drugs to treat alcohol abuse?

A

Naltrexone, acamprosate (GABA a activator, nmda receptor antagonist), disulfiram

46
Q

Methanol

A

Broken down into formaldehyde. Late symptoms of poisoning are really severe. Anion gap metabolic acidosis

47
Q

Methanol vs ethylene glycol poisoning?

A

Methanol has visual disturbances, both have anion gap metabolic acidosis.

Brain and behavior (55 decks)

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