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Pharmacology II > Alcohols > Flashcards

Alcohols Flashcards

(48 cards)

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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?

21
Q

3 steps of NMDAR activation?

Study These Flashcards
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 ??

Study These Flashcards
A

Cognitive function
Learning
Memory
Blackouts : NMDA receptor blockade by ethanol

23
Q

4 things that influence blood levels of alcohol?

Study These Flashcards
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)

Study These Flashcards
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
Chronic drinkers still seems sober when blood alcohol reaches what conc.?
300-400 mg/dL
26
Impaired driver blood level conc.?
80 mg/dL
27
Standard amount of drinks per day for men and women? per week?
``` Day Women : 0-2 Men : 0-3 Week Women : 10 Men : 15 ```
28
4 reasons why ethanol have negative effects on the body?
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
Myocardial contractions happen at what blood alcohol concentration?
>100 mg/dL
30
Why does vasodilation happen when consuming too much ethanol?
depression of vasomotor center in the CNS, direct actions on smooth muscles, leads to hypothermia
31
11 effects of chronic alcohol consumption?
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
3 effects of chronic alcohol on the brain?
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
2 effects of tolerance and dependence?
CNS adaptation | increased metabolism
34
How can a marked abstinence syndrome occur?
ethanol-tolerant individual suddenly stops consuming alcohol
35
3 treatments of alcoholism
1. Management of withdrawal 2. Behavioral modification 3. Long-term managemenet
36
3 ways to manage acute withdrawal
1. Monitor 2. Support and stabilize autonomic function 3. Substitute drug with similar action but extended half-life
37
Example of substitute drug that helps withdrawal? Two reasons why it helps?
Diazepam 1. Lower peak and decrease elimination time, less symptoms 2. More efficient at GABAA receptors.
38
Disulfiram acts where? causes what?
inhibits aldehyde dehydrogenase | causes extreme discomfort, flushing, headache, nausea, vomiting, sweating, hypotension, confusion
39
Function of naltrexone?
competitive antagonist at opioid receptors and exhibits highest affinity for the u receptor isoform. Reduces cravings
40
Which drug alters activity of NMDA receptors? | Why would we want to alter it?
Acamprosate | Ethanol withdrawal can increase glutamate release
41
Drug that could be used for withdrawal in the future?Why? | Preclinical finding?
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
What alcohol can cause alcohol poisoning?
methanol
43
Metabolism of methanol?
Methanol Formaldehyde (alcohol dehydrogenase) Formate
44
Methanol poisoning can cause what? Toxicity is related to what? Leads to what? (4)
visual disturbances Toxicity : build up of formaldehyde and formate Leads to bradycardia, coma, seizures, cessation of respiration
45
Why is ethylene glycol attractive to children and pets? | Toxicity is related to what?
sweet taste | Toxicity : build up of oxalate and other metabolites
46
What can be used as inhibitors of ADH? (2)
Fomepizole | Ethanol
47
Two large effects of oxalic acid accumulation (deriving from ethylene glycol)?
acidosis | nephrotoxicity
48
Two large effects of formaldehyde and formic acid (deriving from methanol)?
Severe acidosis | Retinal damage

Pharmacology II (21 decks)

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