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CHAPTER 12

CHAPTER 12. Sedative-Hypnotic Drugs and Alcohol. Sedatives and Hypnotics. Sedatives are drugs used to induce a mild state of CNS depression characterized by both mental and physical calmness Hypnotics are drugs used to induce and maintain sleep

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CHAPTER 12

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  1. CHAPTER 12 Sedative-Hypnotic Drugs and Alcohol

  2. Sedatives and Hypnotics • Sedatives are drugs used to induce a mild state of CNS depression characterized by both mental and physical calmness • Hypnotics are drugs used to induce and maintain sleep • The same drugs are used to induce both sedation and hypnosis; however, the dosage for inducing sedation is lower

  3. Classification of Sedative- Hypnotic Drugs • Barbiturates – a drug family of chemically similar drugs with similar actions and features • Benzodiazepines – a drug family of chemically similar drugs with similar actions and features • Miscellaneous nonbarbiturates – a group of drugs with dissimilar chemical structures and pharmacologic features

  4. Pharmacology of Barbiturates • Drugs classified as short, intermediate, and long-acting sedative-hypnotics • At low doses they increase the inhibitory effects of GABA • At high doses they act like general anesthetics, and can cause profound CNS depression and death in overdosage • Barbiturates are also anticonvulsants

  5. Barbiturates to Know • Phenobarbital (Luminal) – long acting (6-12 hr) “hangover” – often used for epilepsy • Pentobarbital (Nembutal) – intermediate (4-6 hr) • Secobarbital (Seconal) – short (2-4 hr) help falling asleep

  6. Effects of Barbiturates on the Sleep Cycle • Decrease stage 1, falling asleep • Increase stage 2, a lighter stage of sleep • Decrease stages 3 and 4 referred to as deep sleep or slow-wave sleep • Decrease REM sleep, and may cause REM rebound

  7. Adverse Features of Barbiturates • Cause drug tolerance with chronic use and drug dependency with abuse • Can cause a severe type of physical drug addiction when chronically abused • The withdrawal reaction from barbiturates can be serious, resulting in convulsions and death • Drug interactions, induce microsomal enzymes to increase the rate of drug metabolism of all drugs metabolized by the microsomal enzymes

  8. Reasons for decreasing use • Enzyme induction tolerance,  DMMS • Confusion in elderly • Automatism • REM rebound effect – nightmares • Dangerous with alcohol

  9. Pharmacology of Benzodiazepines • Drugs classified as short, intermediate, and long-acting sedative-hypnotics • Drugs also produce antianxiety, skeletal muscle relaxing, and anticonvulsant effects • Act by increasing the inhibitory effects of GABA • Drugs do not induce the drug metabolizing microsomal enzymes

  10. Effect of Benzodiazepines on the Sleep Cycle • Decrease stage 1, falling asleep • Increase stage 2 • Decrease stages 3 and 4 • Do not significantly decrease REM sleep • Benzodiazepines are considered safer drugs than the barbiturates, especially in overdosage

  11. Benzodiazopines to Know • Most frequent sleeping pill in hospital • Flurazepam (Dalmane) – long acting (1-2 days) • Temazepam (Restoril) – intermediate (8-10 hr) • Triazolam (Halcion) short • Decrease restfull sleep (stage3-4) not REM – Does not induce DMMS

  12. Miscellaneous Nonbarbiturates • Zolpidem and zaleplon are short-acting hypnotics that do not disrupt the sleep cycle • These drugs increase the inhibitory effects of GABA but differently than other drugs • Both drugs are considered to be safer than other hypnotics and are at low risk for abuse • Side effects include dizziness, headache, GI disturbances, and mental confusion

  13. To Know • Zolpidem (Ambien) short acting (2-3 hr) doesn’t alter stage 3-4 or REM • Zaleplon (Sonata) similar to Ambien

  14. Alcohol • Classified as a CNS depressant drug • Unlike other drugs, alcohol provides nutritional calories • Like other drugs of abuse, alcohol causes development of drug tolerance, dependency, and withdrawal reactions • Most of the pharmacology of alcohol centers around its chronic use, abuse, and toxicology

  15. Alcohol • Metabolized at a constant rate • 10-15 cc alcohol = oz vodka = beer = glass wine • Toxic effect: • Low dose = carbohydrate • High dose or with Tylenol = Toxic

  16. Disulfiram (Antibuse) • Used to treat alcoholism and deter drinking • Disulfiram inhibits metabolism of alcohol, allowing acetaldehyde to accumulate • Increased acetaldehyde produces severe nausea, vomiting, headache, and hypotension • Alcoholics take the drug on a daily basis, knowing that if they drink any alcohol they will become violently ill

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