Dental Alcohol

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Which of the following best describes the pharmacologic properties of alcohol?

It is a sedative that depresses the central nervous system.

What is the effect of alcohol on blood vessels?

It dilates blood vessels.

At what blood alcohol concentration would an individual experience lethal respiratory depression?

0.5-0.6%

What is the effect of alcohol on nerve conduction?

It blocks nerve conduction.

What happens to the cell cytoplasm when exposed to alcohol?

It becomes toxic.

What effect does alcohol have on the mucosa and skin surfaces?

It causes irritation of the mucosa.

How does the presence of food in the stomach affect alcohol absorption?

It decreases the rate of absorption

Which body compartments are very permeable to alcohol?

Placenta and brain

When is the rate of alcohol absorption the fastest?

30-90 minutes after ingestion

Which barriers in the body are highly permeable to alcohol?

Placenta and blood brain barrier

Which body system receives a high proportion of the alcohol present in the body?

Nervous system

Which organ is primarily responsible for the metabolism of alcohol?

Liver

What happens to the remaining percent of alcohol that is not metabolized?

It is eliminated through the lungs, skin, and urine

What type of kinetics does alcohol metabolism follow?

Zero Order Kinetics

Which enzyme systems in the liver are responsible for breaking down alcohol?

Alcohol dehydrogenase and Aldehyde dehydrogenase

Which of the following factors affects the rate at which a person metabolizes alcohol?

Body weight

How much alcohol can an individual metabolize per hour on average?

6-8 gm

Which enzyme system in the liver is responsible for metabolizing alcohol?

Alcohol dehydrogenase

What is the additional metabolic system that becomes active in chronic alcoholics or when large quantities of alcohol are ingested?

Microsomal Ethanol Oxidizing System (MEOS)

Which coenzyme does the Microsomal Ethanol Oxidizing System (MEOS) use for alcohol metabolism?

NADPH

What can induce the Microsomal Ethanol Oxidizing System (MEOS) apart from chronic alcohol consumption?

Barbiturates

How does the rate of alcohol metabolism change with increased alcohol consumption?

Increases

What does alcohol inhibit in the central nervous system?

Glutamate system

Which neurotransmitter systems does alcohol enhance in the central nervous system?

GABAergic and serotonergic

Which of the following is a cardiovascular effect of alcohol consumption?

Vasodilatation

What effect does alcohol have on voltage gated calcium channels in the central nervous system?

Inhibits Ca++ entry

What is the effect of alcohol on platelet aggregation?

Inhibits platelet aggregation

What is the overall effect of alcohol on body temperature?

Decreases body temperature, overall heat loss

Which of the following is a gastrointestinal effect of alcohol consumption?

Increased G.I. bleeding

What is the effect of alcohol on the liver?

Leads to inflammation and liver failure

How does alcohol affect cardiovascular system?

Increases levels of high-density lipoprotein (HDL)

What is the metabolic effect of alcohol on the body?

Increases fat production

Which hormone is inhibited by alcohol, leading to an increase in diuresis (increased urine production)?

Antidiuretic hormone (ADH)

Which hormone stimulates the anterior pituitary gland and is increased by alcohol?

Adrenocorticotropic hormone (ACTH)

Which hormone, when inactivated by the liver enzyme MEOS, can lead to feminization of males with chronic alcohol consumption?

Testosterone

Which situation leads to an increase in drug metabolism in the liver?

Chronic alcoholism

Which type of drugs interact considerably with alcohol?

Sedatives/hypnotics

What effect does alcohol have on platelet aggregation?

Inhibits platelet aggregation

How does alcohol affect the metabolism of oral hypoglycemics?

Alcohol decreases metabolism of oral hypoglycemics

What is the primary action of tolbutamide on blood glucose levels?

Decreases blood glucose levels

What effect does alcohol have on blood glucose levels?

Decreases blood glucose levels

Which BAC level is considered illegal for drivers under the age of 21 in all US states?

0.01%

What is the blood-alcohol limit for commercial drivers in the US?

0.04%

What is the legal BAC limit for driving in the US?

0.08%

What is the BAC limit for pilots of aircraft in the US?

0.04%

Which BAC level was the legal limit for driving in the US before 2002?

0.1%

What has been criticized regarding the testing equipment for alcohol measurement?

Validity of both breath and blood testing

Which nutrient deficiencies are commonly associated with chronic alcoholism?

Vitamin deficiencies

What is the effect of chronic alcohol consumption on weight?

Weight loss

Which condition is characterized by disorientation, confabulation, peripheral neuritis, and amnesia?

Korsakoff's psychosis

How does chronic alcohol consumption affect the central nervous system?

It causes CNS degeneration

Which enzyme does Disulfiram (Antabuse) inhibit?

Aldehyde dehydrogenase

What effect does Disulfiram (Antabuse) have when combined with alcohol?

Increases acetaldehyde levels

What is Disulfiram (Antabuse) used for in the treatment of chronic alcoholism?

Negative reinforcement

Which drug is used in the treatment of poisoning by ethylene glycol?

Fomepizole (Antizole)

What is the primary use of Naltrexone (ReVia)?

Treatment of alcoholism

Which drug should never be used in combination with Disulfiram?

Naltrexone (ReVia)

What was the main purpose of developing Ro15-4513?

To treat alcohol addiction

How does Ro15-4513 compare to flumazenil in blocking the effects of benzodiazepines?

Ro15-4513 is less effective

What is the main disadvantage of Ro15-4513 in terms of its half-life?

It has a short half-life

What is the main disadvantage of Ro15-4513 in terms of blocking the effects of ethanol?

It only masks the effects of ethanol temporarily

What class of drugs is Ro15-4513 a weak partial inverse agonist of?

Benzodiazepines

What is Ro15-4513 structurally related to?

Flumazenil

Which drug effectively blocks the effects of benzodiazepine agonists but is ineffective in blocking alcohol actions?

Flumazenil

What is one disadvantage of using Ro15-4513 for blocking the effects of ethanol?

It has a short half-life

What is the primary use of flumazenil?

Treating overdoses of benzodiazepine agonists

Which drug selectively blocks the effects of ethanol but is less effective at blocking the effects of benzodiazepines compared to flumazenil?

Ro15-4513

What would happen if only one dose of Ro15-4513 were used to block the effects of alcohol?

It would wear off before the alcohol had been metabolized

Study Notes

Pharmacologic Properties of Alcohol

  • Pharmacologic properties of alcohol include sedation, anesthesia, and death due to respiratory depression
  • Alcohol is a central nervous system depressant, causing decreased activity and depressing nerve conduction
  • It is a vasodilator, causing increased blood flow to the skin, and is a diuretic due to inhibition of vasopressin

Effects on Blood Vessels

  • Alcohol causes vasodilation, leading to increased blood flow to the skin and decreased blood pressure

Lethal Respiratory Depression

  • Lethal respiratory depression occurs at a blood alcohol concentration of 0.35-0.40%

Nerve Conduction

  • Alcohol slows down nerve conduction velocity and increases the refractory period

Effects on Cell Cytoplasm

  • Alcohol causes disruption of cell membranes, leading to increased permeability and altered cell function

Effects on Mucosa and Skin

  • Alcohol causes irritation and inflammation of mucosa and skin surfaces, leading to increased permeability and susceptibility to infection

Food and Absorption

  • Presence of food in the stomach slows down alcohol absorption, but does not affect the overall amount absorbed

Permeable Body Compartments

  • Body compartments very permeable to alcohol include the brain, liver, and kidneys

Rate of Absorption

  • Rate of alcohol absorption is the fastest when the stomach is empty

Barriers to Absorption

  • Barriers highly permeable to alcohol include the blood-brain barrier and the placenta

Body System and Metabolism

  • The liver is the primary organ responsible for the metabolism of alcohol, and the body system receiving the highest proportion of alcohol is the circulatory system

Metabolism and Elimination

  • 90-95% of alcohol is metabolized, and the remaining 5-10% is excreted unchanged through the kidneys, lungs, and sweat

Metabolic Kinetics

  • Alcohol metabolism follows zero-order kinetics, meaning that the rate of metabolism is constant and independent of concentration

Enzyme Systems

  • The enzyme systems responsible for breaking down alcohol in the liver are the alcohol dehydrogenase (ADH) and the microsomal ethanol oxidizing system (MEOS)

Factors Affecting Metabolism

  • Factors affecting the rate of alcohol metabolism include gender, body weight, and food intake

Average Metabolism Rate

  • The average person can metabolize 0.01-0.02% of blood alcohol concentration per hour

Microsomal Ethanol Oxidizing System (MEOS)

  • MEOS is an additional metabolic system that becomes active in chronic alcoholics or when large quantities of alcohol are ingested
  • MEOS uses the coenzyme NADPH and can be induced by chronic alcohol consumption, resulting in increased tolerance

Induction of MEOS

  • MEOS can be induced by chronic alcohol consumption, resulting in increased tolerance

Rate of Metabolism and Consumption

  • The rate of alcohol metabolism increases with increased alcohol consumption

Central Nervous System

  • Alcohol inhibits the GABA-inhibitory neurotransmitter system and enhances the GABA-stimulatory system
  • It also inhibits the voltage-gated calcium channels in the central nervous system

Cardiovascular Effects

  • Cardiovascular effects of alcohol consumption include decreased blood pressure, increased heart rate, and vasodilation

Gastrointestinal Effects

  • Gastrointestinal effects of alcohol consumption include increased acid production, inflammation, and damage to the liver

Metabolic Effects

  • Metabolic effects of alcohol on the body include increased glucose production, decreased fat metabolism, and increased lipogenesis

Hormonal Effects

  • Hormonal effects of alcohol include inhibition of vasopressin, leading to increased diuresis, and stimulation of the anterior pituitary gland

Hormone Regulation

  • Chronic alcohol consumption can lead to feminization of males due to inhibition of the hormone dihydrotestosterone

Drug Interactions

  • Alcohol interacts with certain drugs, such as oral hypoglycemics, and can affect their metabolism and efficacy
  • The legal blood-alcohol limit for driving in the US is 0.08%, and the limit for commercial drivers is 0.04%
  • The legal limit for pilots of aircraft in the US is 0.04%
  • The BAC level considered illegal for drivers under the age of 21 in all US states is 0.02%

Testing Equipment

  • Criticisms of the testing equipment for alcohol measurement include concerns about accuracy and reliability

Chronic Alcoholism

  • Nutrient deficiencies commonly associated with chronic alcoholism include thiamine deficiency and Wernicke-Korsakoff syndrome
  • Chronic alcohol consumption can lead to weight loss and decreased muscle mass
  • It can also lead to disorientation, confabulation, peripheral neuritis, and amnesia

Disulfiram (Antabuse)

  • Disulfiram (Antabuse) inhibits the enzyme aldehyde dehydrogenase and causes the accumulation of acetaldehyde, leading to unpleasant symptoms when combined with alcohol
  • It is used in the treatment of chronic alcoholism to deter alcohol consumption

Naltrexone (ReVia)

  • Naltrexone (ReVia) is used in the treatment of opioid and alcohol dependence

Ro15-4513

  • Ro15-4513 is a benzodiazepine receptor antagonist that can block the effects of ethanol
  • It is structurally related to benzodiazepines and can induce anxiety and withdrawal symptoms
  • Limitations of Ro15-4513 include its short half-life and inability to block the effects of ethanol at high concentrations

Test your knowledge on the pharmacologic properties and effects of alcohol with this quiz. Explore its role as a CNS depressant, its impact on cell toxicity and dehydration, and its ability to cause inflammation and irritation. Learn about alcohol's vasodilation effects and more.

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