Cns stimulants

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Cns stimulants

  1. 1. CNS STIMULANTS DRUG OF ABUSE
  2. 2. <ul><li>Tolerance </li></ul><ul><li>Dependence </li></ul><ul><li>withdrawal </li></ul>
  3. 3. CNS STIMULANTS <ul><li>PSYCHOMOTOR STIMULANTS </li></ul><ul><li>-METHYLXANTHINES </li></ul><ul><li>-NICOTINE </li></ul><ul><li>-COCAINE </li></ul><ul><li>-AMPHETAMINE </li></ul><ul><li>PSYCHOTOMIMETIC DRUGS </li></ul><ul><li>-LSD </li></ul><ul><li>-PCP </li></ul><ul><li>-THC </li></ul>
  4. 4. METHYLXANTHINES <ul><li>Act translocation of extracellular calcium </li></ul><ul><li>Increase in cAMP& cGMPcaused by inhibition of phosphodiesterase </li></ul><ul><li>Blockade of adenosine receptors </li></ul>
  5. 5. Actions <ul><li>CNS: decrease in fatigue & increased mental alertness, anxiety & tremors, spinal cord stimulated </li></ul><ul><li>CVS: positive inotropic & chronotropic effects </li></ul><ul><li>Renal: mild diuretic action </li></ul><ul><li>Gastric mucosa: stimulate secretion of HCl </li></ul>
  6. 6. <ul><li>Therapeutically it relax the smooth muscle of the bronchioles </li></ul><ul><li>Adverse effects: -insomnia, anxiety, </li></ul><ul><li>agitation </li></ul><ul><li>-emesis, convulsions </li></ul><ul><li>-cardiac arrhythmias </li></ul><ul><li>-lethargy, irritability, </li></ul><ul><li>headache </li></ul>
  7. 7. NICOTINE <ul><li>In low doses, Ganglionic stimulation by depolarization </li></ul><ul><li>In high doses, ganglionic blockade </li></ul>
  8. 8. Actions <ul><li>CNS : euphoria, arousal </li></ul><ul><li>central respiratory paralysis </li></ul><ul><li>severe hypotension </li></ul><ul><li>Peripheral effects : </li></ul><ul><li>-stimulation of sympathetic ganglia , adrenal medulla increases blood pressure & heart rate. </li></ul><ul><li>-stimulation of parasympathetic ganglia, increases motor activity of the bowel </li></ul>
  9. 9. Adverse Effects <ul><li>CNS: irritability & tremors </li></ul><ul><li>CVS: increased heart rate & blood pressure </li></ul><ul><li>Others: intestinal cramps & diarrhea </li></ul>
  10. 10. Withdrawal Syndrome <ul><li>Nicotine- addictive substance </li></ul><ul><li>Physical dependence- rapidly & severe </li></ul><ul><li>Characteristics- irritability anxiety restlessness difficulty in concentrating headache insomnia appetite GI pain </li></ul>Smoking cessation Transdermal patch & chewing gum containg nicotine
  11. 11. COCAINE <ul><li>Highly addictive drug </li></ul><ul><li>It blocks the central & peripheral effects of NE, serotonin & dopamine re-uptake into the presynaptic terminals </li></ul><ul><li>Prolongation of dopaminergic effects in limbic system , produces intense euphoria –cocaine initially causes </li></ul><ul><li>Chronic intake of cocaine depletes dopamine </li></ul>
  12. 12. Actions <ul><li>CNS: behavioral effects, increases mental awareness & produces feeling of well-being, hallucinations delusions & paranoia, increases motor activity, high doses-tremors & convulsions, followed by respiratory & vasomotor depression </li></ul>
  13. 13. <ul><li>Sympathetic nervous system: produces the fight or flight syndrome </li></ul><ul><li>Tachycardia, hypertension, pupillary dilation , peripheral vasoconstriction </li></ul>
  14. 14. Therapeutic Uses <ul><li>Applied topically as a local anesthetic during eye, ear, nose , throat surgery </li></ul><ul><li>Cardiac arrhythmias </li></ul>
  15. 15. Adverse Effects <ul><li>Anxiety : acute ingestion anxiety reaction includes hypertension, tachycardia sweating, paranoia </li></ul><ul><li>Depression: shows physical & emotional depression-tx with Benzodiazepines or Phenothiazines </li></ul><ul><li>Heart disease : seizures, fatal cardiac </li></ul><ul><li>arrhythmias-tx IV diazepam </li></ul><ul><li>& propranolol </li></ul><ul><li>incidence of MI </li></ul>
  16. 16. AMPHETAMINE <ul><li>It similar like cocaine </li></ul><ul><li>Elevation of catecholamine transmitters in synaptic spaces- releases intracellular stores of catecholamines </li></ul><ul><li>Blocks MAO, high level of catecholamines are readily released into synaptic spaces </li></ul>
  17. 17. Actions <ul><li>CNS : incresed alertness, decreased fatigue, depressed appetite, insomnia, convulsions. These CNS stimulant effects of amphetamine & its derivatives have led to their use in the therapy of depression, hyperactivity in children , narcolepsy, appetite control </li></ul><ul><li>SNS : indirectly stimulating receptors through NE release </li></ul>
  18. 18. Therapeutic Uses <ul><li>Attention deficit syndrome- tx Methylphenidate </li></ul><ul><li>narcolepsy </li></ul>
  19. 19. Adverse Effects <ul><li>Central effects : irritability, hyperactive reflexes, delirium, panic states, sucidal tendencies, amphetamine psychosis, overdose can be treated with Chlorpromazine </li></ul><ul><li>CVS : palpitations, cardiac arrhythmias, hypertension, anginal pain , circulatory collapse, headache, chills. Excessive sweating </li></ul><ul><li>GIT : nausea, vomiting, diarrhea, anorexia, abdominal cramps </li></ul>
  20. 20. HALLUCINOGENS <ul><li>Lysergic acid diethylamide (LSD) </li></ul><ul><li>Tetrahydrocannabinol </li></ul><ul><li>Phencyclidine (PCP) </li></ul>
  21. 21. LSD <ul><li>Serotonin agonist activity at presynaptic receptors in midbrain </li></ul><ul><li>Activation of SNS- pupillary dilation, increased Bp, piloerection, increased body temperature </li></ul><ul><li>Orally taken </li></ul><ul><li>Hallucinations with brilliant colors & mood alteration occurs </li></ul><ul><li>Tolerance & physical dependence </li></ul><ul><li>Adverse effects: hyperreflexia nausea muscular weakness </li></ul>
  22. 22. THC <ul><li>Marijuana- dronabinol produces euphoria </li></ul><ul><li>THC impairs short term memory & mental activity </li></ul><ul><li>Decreases muscle strength & impairs highly skilled motor activity </li></ul><ul><li>Increases appetite, xerostomia visual hallucinations, delusions enhancement of sensory activity </li></ul><ul><li>Adverse effects: HR Bp redding of conjunctiva, psychosis </li></ul>
  23. 23. PCP <ul><li>Inhibits re-uptake of dopamine, 5-HT, NE </li></ul><ul><li>Also has anticholinergic activity but produces Hypersalivation </li></ul><ul><li>Ketamine –anesthesia and analgesia </li></ul><ul><li>produces numbness of extremities, staggered gait slurred speech muscular rigidity </li></ul><ul><li>Tolerance often develops </li></ul>
  24. 24. Cont’d CNS STIMULANTS AND DRUG OF ABUSE
  25. 25. <ul><li>Sedative-hypnotics eg, ethanol, phenobarbital, diazepam </li></ul><ul><li>repetitive use and development of psychological dependence </li></ul><ul><li>acute overdoses leads to depress medullary and cardiovascular centres- death </li></ul><ul><li>Inhalants eg, nitrous oxide, benzene, chloroform </li></ul><ul><li>anesthetics, industrial solvents, organic nitrites </li></ul>
  26. 26. <ul><li>Opioids eg, heroin , fentanyl, meperidine </li></ul><ul><li>I/V administration with rapid development of tolerance, psychological and physical dependence. </li></ul><ul><li>oral administration milder effects. </li></ul><ul><li>overdoses leads to respiratory depression </li></ul><ul><li>Steroids </li></ul><ul><li>potential for abuse, increased muscle mass & strength rather than euphoria. Excessive use behavioral, cvs and musculoskeletal effects, acne, antiandrogenic effects produced. Hepatic dysfunction and increased risk of MI. withdrawal symptoms associated with fatigue and depression of mood </li></ul>

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