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Drug Action > Ethanol > Flashcards

Ethanol Flashcards

the drug action of ethanol

1
Q

How does Ethanol affect the CNS?

A

It is a depressant of the CNS

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2
Q

What happens as the dose of ethanol increases?

A

As increase dose:
o Relief from anxiety
o Disinhibition
o Sedation
o Hypnosis (sleep)
o General anesthesia
o Coma
o Death

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3
Q

CNS depressants have additives effects, meaning?

A

Their effects add up
a. Sedatives, antidepressants, anticoagulants, antianxiety, opioids
b. Take sleeping pill after a lot of drinks, additive effects, never wake up

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4
Q

Can the effects of ethanol be reversed by a CNS stimulant?

A

No, coffee will not fix the problem

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5
Q

CNS Depressants will have a rebound excitation when stop taking it?

A

Take alcohol every day, stop drinking, rebound excitation that can be very serious

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6
Q

What are the consequences of cross tolerance of CNS depressants?

A

a. Need to keep taking more of them to get the same effect
b. Frequent drinkers go to the hospital and are given another drug at higher dose because of cross tolerance

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7
Q

Alcohol effects your? (3 things)

A

Emotions
Judgement
Voluntary motor skills

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8
Q

What are two types of amnesia possible when drinking alcohol?

A

Partial amnesia, blackouts

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9
Q

What is partial amnesia?

A

Partial amnesia: fragmental loss of memory, person later unaware of memory gaps, universal, dose related

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10
Q

What are blackouts?

A

Blackouts: total loss of memory for specific time, person later aware of 0 memory, susceptibility varies, not everybody has this, don’t have to be at a high level

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11
Q

What pathways does ethanol act on?

A

Acts on:
- Vision
- Sensation
- Movement
- Coordination
- Memory
- Judgement
- Reward (addiction) increase dopamine

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12
Q

What type of ion channel is the GABA A receptor?

A

A ligand gated ion channel for chlorine.

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13
Q

How does ethanol act to depress the CNS?

A

Ethanol acts presynaptically on GABA receptors that release GABA to activate the postsynaptic GABA receptors allowing Chlorine (Cl) to flow in causing inhibition of the CNS. (ethanol increases GABA inhibition)
Ethanol also releases Glycine, another inhibitory pathway

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14
Q

Ethanol effects the inhibitory pathway and the excitatory pathways?

A

Ethanol blocks glutamate transmission:
Impair intellectual function

Increased inhibition (GABA)
Decreased excitation (NMDA receptor for glutamate)
Inhibits excitation: glutamate receptors
Potentiates inhibition: GABA and Glycine receptors

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15
Q

How does alcohol withdrawal cause excitation?

A

When you chronically block glutamate receptors, they are upregulated, alcohol withdrawal risk of convulsions

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16
Q

What neurotransmitter concentrations does ethanol effect?

A

Lowers release of Acetylcholine, serotonin
Facilitates release of dopamine, opiate neuropeptides

Blocks voltage gated Ca channels
aggression serotonin neurotransmission
Decrease: impulsiveness

Ethanol blocks Ach release: amnesia, cognitive impairment
In reward pathway lowers GABA inhibition, more dopamine release

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17
Q

Is ethanol well absorbed?

A

Yes, its highly lipid soluble

18
Q

How fast does ethanol onset? When is the peak effect?

A

Rapid, detect in 5 minutes in blood, peak at 30-90 minutes
- Rate of absorption increased by carbonation goes into small intestine faster absorbs very well in intestine, decreased by food, fat

19
Q

Where is ethanol absorbed?

A

stomach, small intestine
- About 20% absorbed in stomach, high level of ADH in gastric mucosa, side effect gastritis
- Rate of absorption is much greater on an empty stomach because it will get to the small intestine faster

20
Q

Apparent volume of distribution ethanol =?

A

total body water
- Males have more total body water, so women will have a higher percentage of alcohol since their total body water is less

21
Q

Is ethanol well distributed?

A

Yes, ethanol is a small molecule, it can pass through cell membranes easily

22
Q

Apparent volume of distribution (AVD)

A

Amount of drug in the body / concentration of drug in circulation
Ethanol has a high AVD
therefore, most is bound to tissues

23
Q

Does ethanol get to the brain fast?

A

yes, High blood flow to the brain, ethanol enters rapidly, ethanol can just dissolve in the membranes to get to the brain

24
Q

Does Ethanol stimulate the CTZ?

A

yes, it makes you vomit as a protection mechanism

25
Q

What is the biotransformation of ethanol from first to zero order?

A

At low doses metabolism is first order
At high doses drug metabolism is zero order, since all enzymes that break it down are saturated
Result:
Drink rapidly, greater blood levels
Greater rate of absorption
Lower rate of metabolism

26
Q

Will peak alcohol levels be higher in males or females?

A

Females

27
Q

What are the 2 stages of Ethanol metabolism?

A
  1. Ethanol to acetaldehyde using alcohol dehydrogenase
  2. Acetaldehyde to acetate (acetic acid) using acetaldehyde dehydrogenase
28
Q

Is acetaldehyde toxic to humans?

A

Yes, alcohol dehydrogenase breaks down alcohol to form acetaldehyde

29
Q

What is genetically less active for 50% of Asians?

A

Acetaldehyde dehydrogenase, causes them to take longer to get rid of acetaldehyde

30
Q

What symptoms can acetaldehyde cause?

A

flushing, headache, vomiting, hypotension, sweating

31
Q

What can you treat alcoholics with to make their acetaldehyde dehydrogenase less active, making it uncomfortable to drink?

A

Disulfiram block aldehyde dehydrogenase, treat alcoholics make it uncomfortable to drink

32
Q

What cytochrome P450 can be induced by alcohol use?

A

CYP2E1 10-20% increased with chronic use

33
Q

Why do you pee more when drinking alcohol?

A

Ethanol decreases the reabsorption of water in the kidneys

34
Q

What is the therapeutic index of ethanol?

A

It has a very low therapeutic index. Ethanol toxicity
0.4-0.5 – coma
0.7 respiratory centers affected, death
Lethal level/” recreational level” only 4
Ethanol has a very low therapeutic index

35
Q

What can fetal alcohol syndrome cause?

A
  • Facial changes
  • Mental retardation
  • Greatest risk in early pregnancy
36
Q

Is there any benefit from low dose alcohol?

A

No, Alcohol is a carcinogen causing 7 types of cancer
Regular use increases heart attacks and stroke

37
Q

Cardiovascular consequences of ethanol?

A

Arrythmias even following social drinking
Hypertension
Stroke
Cardiomyopathy

38
Q

What can aldehyde toxicity cause?

A

Esophageal cancer, smoking and drinking

39
Q

What are ascites?

A

Ascites: accumulation of fluid in the abdominal cavity

40
Q

Acute ethanol tolerance?

A

Effect at the same blood level is lower during the decline than the rise

Drug Action (18 decks)

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