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29 Cards in this Set
- Front
- Back
Drugs for treatment of alcoholism
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1) Disulfram
2) Diazepam 3) Chlordiazepoxide 4) Naltrexone 5) Acamprosate 6) Fomepizole |
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Ethanol
Mechanism |
Agonist GABAa
Inhibits NMDA Long term ETOH use causes down regulation of GABAa and up regulation of NMDA |
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Ethanol
Effects |
1) Low dose- inhibits inhibitory pathways: disinhibition
2) High dose-inhibits excitatory pathways:General CNS depressant 3) Impairment of intellectual and motor function 4) Anterograde amnesia |
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Ethanol
Pharmacokinetics |
1) Absorbtion: Stomach, Small intestines, faster on empty stomach
2)Gastric metabolism of ETOH slower in women 3)Distributed in body water: crosses Blood brain barrier and placenta |
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Ethanol
Metabolism |
1)Alcohol dehydrogenase-> acetaldehyde
2) Aldehyde dehydrogenase-> acetic acid 3)Zero Order kinetics 4)Induces CYP 2E1 |
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Ethanol
CNS Effects Low concentration |
1) Disinhibition
2) Decreased anxiety 3) Mild euphoria 4) Sedation |
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Ethanol
CNS Effects high concentration |
1) Motor and Judgment impaired
2) Speech slurs 3) Ataxia |
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Ethanol
Smooth Muscle effects |
1) Vasodialation (hypothermia)
2)Relax uterus (stop preterm labor) |
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Ethanol
Kidney effect |
1) Reduce ADH = Diuresis
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Ethanol
Toxicity |
1) Emesis 6) Metabolic and
2) Stupor Electrolyte disturbance 3) Coma 7) Hypothermia 4) Respiratory depression 5)Death |
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Ethanol Chronic Consumption
Malnutrition |
1) Alcohol has calories may displace food
2) Folate and thiamine |
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Ethanol Chronic Consumption
Gastritis and Pancreatitis |
1) Direct Damage of pancreas
2) Erosive gastritis and malabsorption 3) Lesions of duodenum and esophagus |
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Ethanol Chronic Consumption
Hepatotoxicity |
1) Heavy drinkers develop liver disease
2) Reduces glutathione =Oxidative stress 3) Acetaldehyde accumulates = mitochondrial membrane damage 4)Fatty liver, Fibrosis, Cirhosis 5) Combined with Hep B or C increased risk of liver cancer |
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Ethanol Chronic Consumption
Cardiovascular effects |
1) Cardiomyopathy
2) Hypertention 3) Stroke |
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Ethanol Chronic Consumption
Teratogenicity |
1) Mental retardation
2) Congenital malformations 3) Fetal alcohol syndrome |
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Ethanol Chronic Consumption
Other effects |
1)Increased carcinogenicity: tobacco
2) Mild anemia 3) Sexual dysfunction 4) Decreased immune function 5) Wericke-Korsakoff 6) Peripheral Neuropathy 7) Skeletal muscle atrophy 8) Hypothermia |
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Ethanol
Tolerance and Dependence |
1) Tolerance develops to effects because of increased metabolism.
2) Severe withdrawal syndrome 3) Cross tolerance with Barbituates, Benzodiazepines and general anesthetics 4) Lethal Dose not changed |
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Ethanol
Withdrawal |
1) Anxiety,
2) Irritability, 3) Nightmares, 4) Nausea, 5) Tachycardia, 6) Palpitations |
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Ethanol
Severe withdrawal |
1) Anxiety,
2) Fear, 3) Hallucinations, 4) Delirium, 5) Tremors, 6) Tonic-clonic seizures, 7) Arrythmias, 8) Increased blood pressure |
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Ethanol
Withdrawal Treatment |
1) Prevent seizures, Delirium tremens, and arrythmias
2) Long acting benzodiazepine to taper withdrawal 3) Haloperidol to treat hallucinations |
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Ethanol
Naltrexone |
1) Opioid Receptor antagonist
2) Blocks ability of alcohol to stimulate reward pathway. 3) Reduces craving |
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Ethanol
Naltrexone Side effects |
1) Nausea
2) Liver damage 3) Contraindicated in Liver disease, hepatitis, or liver failure |
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Ethanol
Acamprosate |
1) GABA analogue
2) Restores normal balance of GABA/ Glutamate transmission 3) No Liver Toxicity |
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Ethanol
Disulfiram |
1) Blocks aldehyde dehydrogenase and inhibits P450
2) If person drinks EtOH: Flushing intense throbbing headache nausea and confusion 3) Has a long duration of action (3-4 days) 4) Dangerous not recommended |
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Ethanol
Disulfiram like drugs |
1) Metronidazole
2) Some Cephalosporins 3)Oral Hypoglycemic agents |
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Methanol toxicity
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Converted to formate by alcohol dehydrogenase
Visual disturbances |
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Ethylene glycol toxicity
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Converted to Aldehydes and oxalate by alcohol dehydrogenase
Severe metabolic acidosis |
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Treatment of Methanol and ethylene glycol toxicity
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Administer ethanol to compete with alcohol dehydrogenase
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Fomepizole
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Alcohol dehydrogenase inhibitor
Few side effects |