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Depressants

Depressants. By Stephanie Rouse Robby Gill.

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Depressants

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  1. Depressants By Stephanie Rouse Robby Gill

  2. Depressants – aka DownersDrugs that calm and relax the central nervous systemby interfering with nerve impulse transmissionslow the function of the brain, heart, and other organs, reduce the rate of breathing, and dull emotional responsesaction strongly based upon dosage of druglow dose – little or no impactmoderate dose – sedationhigh dose – induce sleepextremely high dose – death

  3. GABA is the main inhibitory neurotransmitter in the central nervous system (CNS). GABAergic inhibition is seen at all levels of the CNS, including the hypothalamus, hippocampus, cerebral cortex and cerebellar cortex. As well as the large well-established GABA pathways, GABA interneurones are abundant in the brain, with 50% of the inhibitory synapses in the brain being GABA mediated. Calmness, relaxation, reduction of anxiety, sleepiness, slow breathing, slurred speech, staggering gait, poor judgment, slow, uncertain reflexes If abused result in unconsciousness and death

  4. Tranquilizers • Reduce nervous tension/anxiety without inducing sleep • Examples include: • Alcohol • Denzodiazepines (safer than barbituates) • Valium (diasepam) • Librium

  5. Barbiturates and benzodiazepines are the two major categories of sedative-hypnoticssimilar in chemical structure • Benzodiazepine • Fusion of benzene and diazepine ring systems • Barbiturate • Barbituric Acid • Ultrashort, short, intermediate, and long acting depending upon type used to keep patient from waking before surgery is complete • Short acting are abused • Similar to alcohol • Thiopental ultra-short acting marketed as Sodium Pentothal when dissolved in water in large does becomes one of the3 drugs used in the US to execute prisoners on death row, low dose used as truth serum, decreased inhibitions • Oldest depressant, 35 prescribable 5,5-disubstituted derivatives of barbituric acid (vary by R group from carbon to alkyl, saturation, bromo groups, phenyl group) • Not highly potent • methaquolene

  6. Other depressants Sedatives Hypnotics • Certain barbiturates • Soothing of distress without effects of sleep i • tranquilizers are milder than sedatives • Class of drugs that produce sleep • Ex: Chloral hydrate • Ex: Phenobarbital (barbiturate) behaves as either a sedative or hypnotic dependent upon dose

  7. Continuum of Sedation Behavior Death Coma General Anesthesia Hypnosis Sedation Disinhibition Relief of Anxiety Normal Increasing Dose

  8. Ethanol – a common depressant • Capable of hydrogen bonding, but also • Fat soluble (small size) • Readily penetrates cell and tissue membranes • Easily and completely absorbed from the entire gastrointestinal tract.

  9. Ethanol – a common depressant • 30-50 mg / 100 mL blood • 100 mg / 100 mL blood • 200 mg / 100 mL blood • 400 mg / 100 mL blood • mild intoxication;Silly behavior • slurred speech; staggering; aggression • vision and movement difficult • Coma, death

  10. Ethanol – a common depressant Alcoholism – • a disease • Progressive • Frequently fatal • May run in families • ? genetic component • Other uses • Antiseptic • Tincture of iodine • mouthwashes

  11. Discuss the social and physiological effect of the use and abuse of ethanol. • Include effects on the family, cost to society and the short-and long-term health effects.

  12. Social Effects of the Abuse of Ethanol • Major social costs due to alcohol use and abuse. • In the U.S., Australia, Europe, Japan, and other countries, over 80% of all alcohol-induced costs are borne by society. • Connected to many different degrees of crime. • MADD

  13. Physiological Effects of Ethanol • Short-term effects: • Depressant • Impairs CNS function proportional to intake of alcohol • Impacts Pregnancy - Miscarriage, low birth mass and fetal abnormalities. • Long-term effects: • Cirrhosis and cancer of the liver • coronary heart disease • high blood pressure • Strokes • Digestive issues - gastritis, peptic ulcers. • Poor eating habits.

  14. Other Physical Effects • Driving impairment • Alcoholism is a disease • Includes physical and psychological addiction as well as genetic factors • Enhances the effects of other drugs.

  15. Describe the synergistic effect of ethanol with other drugs.

  16. Reactions with other Drugs • Synergistic Effects - combination of two drugs is more harmful than either drug taken alone • Alcohol + aspiring – increase risk of stomach bleeding • Alcohol + sedatives - increases risk of heavy sedation leading to coma and death • Alcohol + cocaine – cocaethylene forms… extends high… but is very toxic… causes severe constriction of blood vessels (high blood pressure)… and irregular heart beat. • Alcohol + bezodiapenes (mogadon, valium) – suppresses CNS leading to death

  17. Describe and explain the techniques used for the detection of ethanol in the breath and in the blood or urine. Include • potassium dichromate (VI) in the breathalyzer • analysis of blood or urine by chromatography • absorption of infra-red radiation in intoximeter.

  18. Detecting BAC (Question 12) • Breathalyzer test (potassium dichromate [K2Cr2O7] used as oxidizing agent). • Gas Liquid Chromatography • Takes breath sample and detects presence of gases at a quantitative level. • Blood and urine can be used in the machine as well.

  19. Detecting BAC (continued) • Infra-Red Spectroscopy (“intoximeter”) • IR absorption at 2950 cm-1 is used to detect presence of the C-H group. • Very accurate (% C-H absorbed acts as a marker for BAC).

  20. Other Commonly Used Depressants Nitrazepam (mogadon) Hypnotic, induces sleep, control seizures and infantile spasms Prozac (Fluoxetine hydrochloride) Anti-depressant used for mental depression, increases activity of the neurotransmitter serotonin Depressants are often described as anti-depressants because they relieve depression

  21. Valium (diazepam)relief of anxiety and tension Carbon skeleton structures of diazepam and nitrazepam are the same, the two differing in side groups. The structure of Prozac differs from the other two

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