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23 Cards in this Set
- Front
- Back
Pharmacokinetics: Absorption of Alcohol
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Absorbed readily in Duodenum.
Blood Alcohol Concentrationo (BAC) depends on: -amount, rate, food, gastric metabolism, hepatic first pass. |
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Distribution of Alcohol
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Volume of distribution = total body water.
Higher Fat = less water content and smaller volume for distribution of alcohol. Women are affected more by alcohol in general. |
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Metabolism of Alcohol
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1. Alcohol is convert by Alcohol Dehydrogenase (ADH) to Acetaldehyde. RATE LIMITING STEP.
2. Acetaldehyde is converted by Aldehyde Dehydrogenase (ALDH) to Acetate. Not rate limiting step unles ADH activity is high. |
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Alcohol Elimination Rate
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7.0g/hr metabolism or 0.015% disappearance per hour.
Females eliminate faster than males. |
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Alcohol Dehydrongenase Isoenzymes
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There are three ADH isoenzymes:
ADH1A, ADH1B, ADH1C. |
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Aldehyde Dehydrogenase Isoenzymes
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There are two ALDH isoenzymes:
ALDH1, ALDH2 |
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Polymorphisms of ADHB and ADHC
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Mutations in ADH1B*2,ADH1B*3 and ADHC*1 result in rapid metabolism of alcohol and decreased risk in alcoholism.
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Acetaldehyde Toxicity
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Accumulation of Acetaldehyde associated with intense reactin to alcohol.
Headache, gastritis, nausea, dizzines (hangover). ALDH2*2: decreased elimination gene. Less susceptibility to alcoholism. |
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Why is alcohol tolerance important?
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Cross-tolerance to other depressant drugs can occur. Ex) BZ and Barb - will not work at normal doses during surgery in a secret alcoholic.
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Alcohol effect on GABA
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Interacts with GABA-A receptor and facilitates GABA transmission.
Binds to Serine270 of Receptor and increases Cl influx = hyperpolarization. |
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CNS effects of Alcohol
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Sedative, Anxiolytic, Withdrawal.
Activates mesolimbic and mesocortical dopamine neurons (reward/pleasure center.) |
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Chronic Alcohol effect on GABA
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Chronic use leads to less Cl influx and decreased GABA function.
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Effect of Alcohol on Opioid peptide System
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Activation of the opioid peptide system.
Reward: Mu Aversion: Kappa Craving. |
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Alcohol as a Reinforcer
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Positive Reinforcment: pleasure, alter coonsciousness, conform to behavior of peers.
Negative Reinforcing: relieve stress and negative emotions, avoid withdrawal symptoms. |
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Alcohol Effect on NMDA (Glutamate) System
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Blocks NMDA Glutamate System which contributes to sedative/hypnotic effects. Participates in withdrawal syndrome.
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Alcohol Toxicity
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General Cell Toxicant.
Inflammation and cancer of throat, esophagus, stomach, pancreas, small intestine, colon. Pancreatitis, diabetes. |
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Alcohol Liver Toxicity
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Supress vitamin function and appetite leading to malnutrition.
Inflammation and FAT deposits leading to alcoholic hepatitis and liver cancer. Cell death and scar tissue leading to cirrhosis. |
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Cardiovascular Toxicity
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High BP and atherosclerosis from liver FAT production.
Cariomyopathy. Impairment of blood cell production (anemia and immune weakness). Vasodilation and heat loss. RBC clumping, poor circulation and capillary rupture/stroke. |
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CNS Toxicity
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Impairs Judgement, VISION, coordination leading to accidnets.
Brain cell death leading to dementia. Acute overdose leading to brain stem failure and coma/death. |
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Disulfiram
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Alcohol drug.
Inhibits Aldehyde Dehydrogenase so acetaldehyde builds up in the body. Person has huge hangover. |
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Naltrexone
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Newer Alcohol drug.
Opioid antagonist that reduces alcohol craving. Reduces relapse in recover alcoholics. |
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Acamprosate
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Glutamate antagonist, GABA agonist.
Decreases drinking behavior. |
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Benzodiazepines
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Usefull in treating withdrawal symptoms.
Facilitates GABAergic function. Compensates for reduced function in chronic alcoholics |