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B&B Pharm > Anxiolytics, Sedatives and Hypnotics > Flashcards

Anxiolytics, Sedatives and Hypnotics Flashcards

1
Q

Why is it harder to overdose on benzos than barbituates?

A

Barbituates have increasing effects with increasing dose

Benzos max out with increasing dosage (safer)

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2
Q

At minimal concentrations what effect do benzos and barbs have?

A

Anti-anxiety

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3
Q

What happens with severe toxicity in sedative-hypnotics?

A

respiratory and cardiovascular depression

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4
Q

What ion does GABA-A pump?

A

Cl-

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5
Q

What are more selective, benzo, barbituates or newer hyponotics?

A

Newer hyponotics are the most seletive, then benzos and barbituates bind to multiple isoforms and sites (AMPA receptors)

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6
Q

What role does a1 subunit binding have?

A

Sedation
Amnesia
Ataxia

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7
Q

What role does a1 and a3 subunit binding have?

A

Anxiolytic

Muscle relaxing

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8
Q

What role does a5 subunit binding have?

A

Memory impairment?

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9
Q

Does cross tolerance in sedative-hypnotics occur?

A

Yes

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10
Q

How do you alleviate withdrawal symptoms of short-acting sedative-hypnotics?

A

Longer acting sedative hypnotics

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11
Q

What happens if you stop a sedative-hypnotic suddenly?

A

Death

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12
Q

What happens causes withdrawal symptoms of sed-hypn?

A

The long term effects have caused downregulation of GABA-A and upregulation of GluTR receptors

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13
Q

How quick is the absorption and distribution of barbituates and why?

A

Its rapid because they are lipophilic

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14
Q

What sed-hypn do you use for headaches?

A

Butalbital

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15
Q

What did they use for truth interviews?

A

Amobarbital

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16
Q

What exam findings might you get from barbituate toxicity?

A

Small to midpoint pupils

Diminished reflexes

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17
Q

What are severe toxic effects of barbituates?

A

coma
hypothermia
resp failure
decreased myocardial contractility

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18
Q

What is the major contraindication of barbituates?

A

patients with porphyria

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19
Q

What are some reasons for the decline in barbituate use?

A

Ease of suicide/low margin of safety
No antidote
Addiction/physiological dependence
Cardiovascular/autonomic effects

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20
Q

Where in the brainstem can you find the cardiovascular and respiratory centers that hypnotics depress?

A

Medulla

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21
Q

What effect do benzos have on gabaergic neurons?

A

allosteric agonists increase freq of opening events

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22
Q

What effect do barbituates have on gabaergic neurons?

A

Increase the duration of opening events in GABA
Gabamimetic - directly activate chloride channels
ALSO!!! Depress actions of glutamate

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23
Q

What three benzodiazepines can be given to liver failure patients? Why?

A

Lorazepam
Temazepam
Oxazepam
(No active metabolites)

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24
Q

What are short acting benzos usually used for?

A

Anesthesia

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25
Q

What are long acting benzos usually used for?

A

Anxiety, keeping a patient asleep

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26
Q

What benzo can be used for anesthesia? Why?

A

Midazolam

Fast onset

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27
Q

What are intermediate duration benzos used for compared with long duration?

A

Intermediate - falling asleep

Long - staying asleep

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28
Q

Advantages of benzodiazepines?

A

Rel high therapeutic index
Rapid onset of action
Antidote (flumazenil)
Minimal CV and autonomic effects

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29
Q

What patients will have adverse reactions to benzos?

A

Cardio or pulm patients can more easily resp depression

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30
Q

What are newer hypnotics used for?

A

Sleep aids

31
Q

What are the 3 Zs?

A

Zolpidem
Zalepon
Eszopiclone

32
Q

What effects do benzos and barbs have on sleep?

A

Increase stage 2 sleep

Decrease REM and stage 4

33
Q

What does zolipdem do to sleep patterns?

A

decreases REM

34
Q

Zalepon has what effect on sleep patterns?

A

decreases latency of sleep but little effect on total sleep time

35
Q

Eszopiclone effects

A

increases total sleep time

Increases stage 2 NREM

36
Q

When is tolerance induced to newer hypnotics?

A

> 1-2 wks

37
Q

What are adverse effects of zolpidem?

A

Parasomnias

38
Q

What drugs does flumazenil block and how?

A

Benzos and newer hypnotics acts as a competitive antagonist at GABA-A

39
Q

What limits its use?

A

Adverse effects - seizures, cardiac arrythmias

40
Q

Why is ramelteon useful?

A

Helps falling asleep without effecting sleep architecture

41
Q

What does ramelteon do?

A

Turn you into a woman!!!

Reduces testosterone and increase prolactin

42
Q

How and where does buspirone act?

A

Partial agonist at 5HT1A recepetors

43
Q

What is buspirone used for?

A

GAD

44
Q

Buspirone disadvantage

A

More than a week to have an effect

45
Q

Buspirone advantage

A

Low abuse liability

46
Q

When is dexmedetomidine used most?

A

Intubation

47
Q

What receptor and how does dexmedetomidine act?

A

Alpha2 adrenergic receptor agonist

48
Q

How does dexmedetomidine induce sedation?

A

Lowers sympathetic activity

49
Q

Advantages of dexmedetomidine

A

NO respiratory depression

50
Q

Disadvantages dexmedetomidine

A

$$$$

contrindicated in CV patients (heart block or severe ventricular dysfunction)

51
Q

What are concerns for sed-hynos with pregnant patients?

A

All cross placental barrier

Can get withdrawal symptoms in newborns

52
Q

What drug has the same effect as a common alcohol related genetic deficiency?

A

Disulfiram is used in alcohol-use disorders because it causes the build up of acetaldehyde. Asians commonly lack the acetaldehyde dehydrogenase gene

53
Q

What antagonist effects does alcohol have in the CNS?

A

It blocks glutamates ability to open the NMDA channel

54
Q

Acute effects of ethanol

A

Heart: Depression of contractility
Smooth muscle: Vasodilator, uterine relaxation
GI: Nausea, vomiting

55
Q

Why might an alcoholic suffer from malnutrition symptoms?

A

1) Chronic pancreatitis
2) Injury to small intestine - malabsorption of vitamins
3) Dietary deficiency
4) Gastritis

56
Q

What is the progression of an alcoholic liver?

A

Fatty liver -> alcoholic hepatitis -> cirrhosis

57
Q

Why is heart failure possible in alcohols?

A

Dilated L cardiomyopathy

58
Q

Withdrawal symptoms of alcohol and why?

A

Delirium tremens, hyperexcitability, seizures

Upregulation of NMDA receptors and Ca2+ channels underlie seizures

59
Q

Does alcohol have neurotoxic effects?

A

Dementia
Generalized symmetric peripheral neuropathy
Cerebellar - ataxia
Optic nerve degeneration

60
Q

Can alcohol lead to cancer?

A

Acetaldehyde can damage DNA -> mouth, larynx, pharynx, esophageal, liver cancer (anything the alcohol touches)

61
Q

Why might an alcoholic present as an anemic?

A

Inhibits proliferation of cellular elements in bone marrow

Impairs hematopoiesis

62
Q

Why might an alcoholic come in with pneumonia?

A

Immune system is impaired in lungs

NOTE: It is enhanced or even redirected to pancreas and liver

63
Q

How much alcohol can get into the placenta and why is this dangerous?

A

Teratogenic.

Alcohol can reach levels equal to that of the mother in the fetus and cannot be metabolized because of the lack of alcohol dehydrogenase.

64
Q

Why should an alcoholic avoid tylenol?

A

Alcohol has inductive effects which would convert acetaminophen to to reactive hepatotoxic metabolites

65
Q

Why should someone taking a sleep aid or anti-anxiety avoid alcohol?

A

Alcohol inhibits metabolism of other drugs which creates additive CNS depression

66
Q

What three key vitamins and nutrients are important to give an acute alcoholic intoxication?

A

Thiamine
Glucose
Long acting benzodiazepine

67
Q

When is alcohol withdrawal a medical emergency?

A

Delirium tremens

68
Q

Who do you give naltrexone to?

A

a reformed alcoholic without liver issues or opioid history who has severe craving

69
Q

What can you use to treat alcohol dependence?

A

Naltrexone
Acamprosate
Disulfiram

70
Q

What patients cannot handle acamprosate?

A

Renal failure/disease

71
Q

What type of learning behavior does disulfiram exhibit?

A

Punishment - causes extreme discomfort for those who drink because of acetaldehyde build up

72
Q

Who should not be given disulfiram?

A

Patients with poor compliance

73
Q

How do you treat someone with metabolic acidosis and visual disturbances?

A

Methanol poisoning
Support respiration - sudden cessation = death
Fomepizole (alcohol dehydrogenase inhibitor) or alcohol (competitively inhibits)
Bicarb - counteract metabolic acidosis
Hemodialysis

74
Q

Patient presents with oxolate crystals in urine, anion gap acidosis, and osmolar gap but NO visual symptoms. What do you give?

A

Fomepizole and hemodialysis

B&B Pharm (6 decks)

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