Alcohol 🍸 (Lauren🌭) Flashcards by Shelby SK

Which 2 enzyme systems are used to metabolize alcohol?

ADH (alcohol dehydrogenase)- Primary enzyme

MEOS/CYP2E1- secondary enzyme system

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In nonalcoholics, what enzyme system is used primarily used to metabolize alchohol?

ADH

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In chronic alcoholics, which enzyme system is used to metabolize alcohol and why?

Chronic alcoholics have to start using the MEOS/CYP2E1 enzyme pathway because the ADH system gets saturated

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Alcohol metabilism follows ____ order kinetics

ZERO

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What does Zero order kinetics mean?

Alcohol is metabolized at a constant rate, and it is INDEPENDENT OF CONCENTRATION

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How does alcohol induce its own metabolism?

Alcohol induces CYP2E1 and it is also metabolized by CYP2E1.

This leads to pharmacokinetic tolerance.

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Why do chronic alcoholics have increased alcohol metabolism?

Since alcohol induces CYP2E1, and is also metabolized by 2E1, it leads to pharmacokinetic tolerance.

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Why is acetaminophen more toxic for chronic alcoholics?

Because alcohol induces CYP2E1, and when acetaminophen is metabolized by 2E1, it leads to liver damage.

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What are the Pharmacokinetic vs Pharmacodynamic effects of alcohol tolerance?

Pharmacokinetic: CYP2E1 is induced and alcoholics have increased metabolism

Pharmacodynamic: Down-regulation of GABA receptors. Up-regulation of NMDA receptors.

(Kinetic: what your body does to drugs
Dynamic: what drugs do to your body)

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Alcoholics have a cross-tolerance to what other drugs?

Benzos

Barbiturates

(Due to the down-regulation of GABA)

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Alcohol is a CNS _________

Depressant

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What is the MOA of alcohol?

Binds to GABAa receptor to increase chloride influx and enhance inhibitory GABA effect

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Why is alcohol rewarding?

It increases Dopamine in the mesolimbic pathway

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How come you get SUPER sedated if you take alcohol, benzos, and barbiturates?

They all bind to GABA but at different sites, so they don’t compete

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Why does alcohol give you anterograde amnesia (blackouts)?

Blockade of NMDA receptors

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What are the effects of alcohol On the CNS?

Low concentrations: disinhibition, decreased anxiety, euphoria, increased confidence, memory and concentration are affected, mood swings

Increased dose: motor function and judgment are impaired, slurred speech, ataxia, and the CNS depressant and sedative properties become apparent

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What are the effects of alcohol on smooth muscle?

Vasodilation which causes hypothermia

Can also relax the uterus to prevent labor

Does alcohol warm you up on a cold winter night?

No, it will actually make you colder due to the vasodilation
☃️

What effect does alcohol have on the heart?

Decreased contractility

What effect does alcohol have on the kidneys?

Decreases antidiuretic hormone, producing a DIURETIC effect

YOU PEE A LOT🚽

What are the symptoms of acute alcohol toxicity?

Emesis

Stupor/coma

Respiratory depression

Death

Low BP and Cardiac output

What causes hangovers?

Acetaldehyde buildup

Dehydration

Beginning of withdrawal

If someone is having seizures due to acute alcohol toxicity, what meds can you give them?

Lorazepam (Ativan)- benzo

Phenytoin (Dilantin)- anticonvulsant

What are the effects of chronic alcohol abuse on the liver?

Liver disease is most common complication

Fatty liver—> fibrosis—> cirrhosis

Alcoholic hepatitis

Liver Cancer- occurs 10yrs after you stop drinking due to the livers attempts to heal itself

What are the effects of chronic alcohol abuse on the CNS?

Wernicke-Korsakoff syndrome due to THIAMINE deficiency**

What is Wernicke-Korsakoff syndrome and what causes it?

Paralysis of eye muscles Ataxia Confusion Coma/death Caused by thiamine deficiency

What are the effects of chronic alcohol abuse on the cardiovascular system?

Cardiomyopathy- direct toxic effect of acetaldehyde **Arrhythmias- BINGES can cause both atrial and ventricular arrhytmias Hypertension** Increased risk of stroke and heart disease

What effect does chronic alcohol abuse have on the immune system?

Weakened due to many respiratory infections

What effect does chronic alcohol abuse have on skeleetal muscle?

It ATROPHIES Not so cool now are you

What effect does alcohol have on a fetus?

It crosses the placenta and has teratogenic effects on the baby. May cause Fetal Alcohol Syndrome- small head, mental retardation, flat face, joint problems, heart defects

What 4 drugs can be used to treat alcoholism?

Naltrexone (ReVia) Acamprosate (Campral EC) Disulfiram (Antabuse) Topiramate (Topamax)

Which 3 drugs for the treatment of alcoholism reduce craving?

Naltrexone (ReVia) Acamprosate (Campral EC) Topiramate (Topamax)

How does Naltrexone (ReVia) work to reduce cravings?

It is an opioid receptor antagonist, and since endorphins are endogenous opioids released when you drink, they can’t bind, and no dopamine can be released= reward pathway is blocked

How does Acamprosate (Campral EC) work for the treatment of alcoholism?

It is a GABA analogue that restores the normal balance of GABA and glutamate Decreases craving and the likelihood of relapse

Your patient walks into your clinic and wants some medication to help him quit drinking. You run some tests and find out he has liver failure. Which drug should you NOT use? Which drug should you use instead?

Do NOT use Naltrexone (can cause liver damage) Use Acamprosate instead (excreted by kidneys instead, no liver toxicity)

How does Disulfiram (Antabuse) work?

It inhibits aldehyde dehydrogenase, so acetaldehyde builds up and causes flushing, headache, nausea, confusion, chest pain, hypotension, vertigo, blurred vision and shock It is DANGEROUS and NOT recommended

How does Topiramate (Topamax) work for alcoholism treatment?

Its an anticonvulsant drug that decreases craving. We dont know why it works

How soon do the effects of alcohol withdrawal appear? How long do they last?

Can appear 6-8 hrs after stopping Can last 7-10 days

Alcohol withdrawal can cause deadly seizures. What drugs are used to PREVENT seizures? What drug is used to TREAT seizures that are already happening?

PREVENTION: Diazepam (Valium) or Chlordiazepoxide (Librium) TREAT: Lorazepam (Ativan)

A 43 year old man who has been drinking a liter of vodka/day for 20 years suddenly quits drinking. Three days later, he starts having seizures. Which drug is the best choice to treat the seizures?

Lorazepam (Ativan)

A 43 year old man has been drinking a litter of vodka/day for 20 years and comes to you because he wants to quit drinking. Amazingly, he does not have liver failure. What drug should you give him to reduce his alcohol cravings?

Naltrexone (ReVia)

A 43 year old man has been drinking a litter of vodka/day for 20 years and comes to you because he wants to quit drinking. He has liver failure. What drug should you give him to reduce his alcohol cravings?

Acamprosate (Campral EC)