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Pharmacology II > Alcohols > Flashcards

Alcohols Flashcards

1
Q

What type of drug is ethanol?

A

Sedative hypnotic

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2
Q

Short term effects of alcohol? (9)

A 
Drunk
Memory loss/blackout
Injury
Violence
Accidents
Spouse abuse
Suicide
Overdose
Death
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3
Q

Long term effects of alcohol? (10)

A 
Dependence
Cancer risk
Learning/memory problems
Mental health
Social problems
Diabetes
Cirrhosis
Pancreatitis
Low birth weight
FASD
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4
Q

What is the Vd of ethanol?

A

equal to total body water

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5
Q

Is ethanol absorbed rapidly or slowly? Partially or completely?

A

Rapidly

Completely

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6
Q

When are peak ethanol levels reached

A

within 30 min

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7
Q

What can delay ethanol absorption?

A

food

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8
Q

Why do women have higher peaks of EtOH than men? (3)

A

Lower body water
More body fat
Lower first-pass metabolism

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9
Q

Where is EtOH oxidized and what percentage? the rest goes where?

A

90% in the liver

Rest excreted by lungs and kidney

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10
Q

Metabolism of ethanol?

What cofactor is needed?

A

Acetaldehyde (Alcohol dehydrogenase)
Acetate (aldehyde dehydrogenase)
NAD+

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11
Q

Where is Alcohol Dehydrogenase (ADH) mainly found?

When is the enzyme active?

A

Cytosol of cells in liver and gut

When NAD+ is available

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12
Q

Can ADH metabolize high doses of ethanol?

A

No

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13
Q

What metabolizes high doses of ethanol

A

microsomal ethanol oxidizing systems (MEOS)

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14
Q

NAD+ is limiting which means what about ethanol metabolism?

A

it is zero-order kinetics

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15
Q

What is zero-order elimination?

A

Constant amount of drug is eliminated per unit of time

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16
Q

What can change the metabolism of ethanol in different people?(2)

A

Tolerance = more enzymes

Genetic polymorphisms

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17
Q

MEOS consists of what? (3)

Uses what as a cofactor?

A

cytochrome p450 2E1, 1A2 and 3A4

NADPH

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18
Q

2 pharmacodynamic effects of ethanol?

A
  1. Dose-dependent CNS effects

2. Rapid onset of sedation, euphoria, impaired attention, impaired motor skills

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19
Q

4 membrane proteins affected by ethanol?

A

GABAA receptors
Inhibits glutamate at NMDA receptors
Inhibits enzymes like ATPases/adenyl cyclases
Ion channels (K channels)

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20
Q

Does alcohol bind orthosteric or allosteric?

A

allosteric

21
Q

3 steps of NMDAR activation?

A
  1. Activation of non-NMDA receptors (cell depolarization)
  2. Activation relieves BMDA receptors of Mg2+ block
  3. Channel opens, cation entry
22
Q

NMDA receptors are important for what? (3)

Blackouts may result from ??

A

Cognitive function
Learning
Memory
Blackouts : NMDA receptor blockade by ethanol

23
Q

4 things that influence blood levels of alcohol?

A
  1. Body size/build - lean muscle = more water
  2. Sex - diff. ratio of lean muscle
  3. General health - liver function
  4. Food - slows absorption
24
Q

Different blood alcohol concentrations and clinical effects? (5)

A 
50-100 mg/dL : sedative
100-200 : impaired motor function, slurred speech, ataxia
200-300 : emesis, stupor
300-400 : coma
>500 : respiratory depression, death
25
Q

Chronic drinkers still seems sober when blood alcohol reaches what conc.?

A

300-400 mg/dL

26
Q

Impaired driver blood level conc.?

27
Q

Standard amount of drinks per day for men and women? per week?

A 
Day
Women : 0-2
Men : 0-3
Week
Women : 10
Men : 15
28
Q

4 reasons why ethanol have negative effects on the body?

A
  1. low potency that is consumed in large quantities
  2. Direct effects of alcohol
  3. Metabolic consequences (oxidative stress, mito damage, inflammation, etc..)
  4. Increased death due to liver disease, cancer, accidents and suicide
29
Q

Myocardial contractions happen at what blood alcohol concentration?

A

> 100 mg/dL

30
Q

Why does vasodilation happen when consuming too much ethanol?

A

depression of vasomotor center in the CNS, direct actions on smooth muscles, leads to hypothermia

31
Q

11 effects of chronic alcohol consumption?

A
  1. Liver function affected
  2. Gluconeogenesis reduced
  3. Hypoglycemia/fat accumulation (NAD+ depletion)
  4. Cirrhosis
  5. induces cyt. p450 enzymes
  6. GI tract affected
  7. Gastritis
  8. Blood and plasma protein loss
  9. Anemia/malnutrition
  10. Malabsorption of vitamins
  11. Pancreatitis
32
Q

3 effects of chronic alcohol on the brain?

A
  1. Loss of gray and white matter
  2. Cognitive deficits
  3. Wernicke-Korsakoff syndrome and peripheral neuropathy are linked to deficiencies in B complex of vitamins
33
Q

2 effects of tolerance and dependence?

A

CNS adaptation

increased metabolism

34
Q

How can a marked abstinence syndrome occur?

A

ethanol-tolerant individual suddenly stops consuming alcohol

35
Q

3 treatments of alcoholism

A
  1. Management of withdrawal
  2. Behavioral modification
  3. Long-term managemenet
36
Q

3 ways to manage acute withdrawal

A
  1. Monitor
  2. Support and stabilize autonomic function
  3. Substitute drug with similar action but extended half-life
37
Q

Example of substitute drug that helps withdrawal? Two reasons why it helps?

A

Diazepam

  1. Lower peak and decrease elimination time, less symptoms
  2. More efficient at GABAA receptors.
38
Q

Disulfiram
acts where?
causes what?

A

inhibits aldehyde dehydrogenase

causes extreme discomfort, flushing, headache, nausea, vomiting, sweating, hypotension, confusion

39
Q

Function of naltrexone?

A

competitive antagonist at opioid receptors and exhibits highest affinity for the u receptor isoform. Reduces cravings

40
Q

Which drug alters activity of NMDA receptors?

Why would we want to alter it?

A

Acamprosate

Ethanol withdrawal can increase glutamate release

41
Q

Drug that could be used for withdrawal in the future?Why?

Preclinical finding?

A

gabapentin
Indirectly modulates gamma-aminobutryic acid (GABA) neurotransmission
Preclinically : gabapentin normalizes stress-induced GABA activation in the amygdala that is associated with alcohol dependence

42
Q

What alcohol can cause alcohol poisoning?

43
Q

Metabolism of methanol?

A

Methanol
Formaldehyde (alcohol dehydrogenase)
Formate

44
Q

Methanol poisoning can cause what?
Toxicity is related to what?
Leads to what? (4)

A

visual disturbances
Toxicity : build up of formaldehyde and formate
Leads to bradycardia, coma, seizures, cessation of respiration

45
Q

Why is ethylene glycol attractive to children and pets?

Toxicity is related to what?

A

sweet taste

Toxicity : build up of oxalate and other metabolites

46
Q

What can be used as inhibitors of ADH? (2)

A

Fomepizole

Ethanol

47
Q

Two large effects of oxalic acid accumulation (deriving from ethylene glycol)?

A

acidosis

nephrotoxicity

48
Q

Two large effects of formaldehyde and formic acid (deriving from methanol)?

A

Severe acidosis

Retinal damage

Pharmacology II (21 decks)

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