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CNS Stimulants

CNS Stimulants. Analeptics Anorexiants Antidepressants Serotonin agonists. CNS Stimulants: Adverse effects. CVS: Palpitation, tachycardia, hypertension, angina, dyshythmia CNS: Nervousness, restlessness, anxiety Endocrine: Hypoglycemia, hyperglycemia GIT: Nausea, vomiting,diarrhea.

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CNS Stimulants

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  1. CNS Stimulants Analeptics Anorexiants Antidepressants Serotonin agonists

  2. CNS Stimulants: Adverse effects • CVS: Palpitation, tachycardia, hypertension, angina, dyshythmia • CNS: Nervousness, restlessness, anxiety • Endocrine: Hypoglycemia, hyperglycemia • GIT: Nausea, vomiting,diarrhea

  3. Analeptic • Used to stimulate respiration when natural reflex is lost • H-cholinomimetic (reflex analeptic) • Central analeptic (Aminophyllin, theophylline,Caffeine, Doxapram)

  4. Did You Know? • Caffeine is a xanthine alkaloid compound that acts as a stimulant in humans. Caffeine is sometimes called guaranine when found in guarana, mateine when found in mate, and theine when found in tea. It is found in the leaves and beans of the coffee plant, in tea, yerba mate, and guarana berries, and in small quantities in cocoa, the kola nut and the Yaupon Holly. Overall, caffeine is found in the beans, leaves, and fruit of over 60 plants, where it acts as a natural pesticide that paralyzes and kills certain insects feeding upon them.

  5. Chemical Properties Molar Mass = 194.19 g mol−1 Density: 1.2 g/cm³ Phase: Solid Melting Point: 237 °C Boiling Point: 178 °C

  6. Uses of Caffeine • Caffeine is a central nervous system (CNS) stimulant, having the effect of temporarily warding off drowsiness and restoring alertness. Beverages containing caffeine, such as coffee, tea, soft drinks and energy drinks enjoy great popularity: caffeine is the world's most widely consumed psychoactive substance. In North America, 90% of adults consume caffeine daily.

  7. Metabolizing Of Caffeine • Caffeine is completely absorbed by the stomach and small intestine within 45 minutes of ingestion. After ingestion it is distributed throughout all tissues of the body and is eliminated by first-order kinetics. The half-life of caffeine varies widely among individuals according to such factors as age, liver function, pregnancy, some concurrent medications, and the level of enzymes in the liver needed for caffeine metabolism. In healthy adults, caffeine's half-life is approximately 3-4 hours. In women taking oral contraceptives this is increased to 5-10 hours, and in pregnant women the half-life is roughly 9-11 hours. Caffeine can accumulate in individuals with severe liver disease when its half-life can increase to 96 hours.

  8. Caffeine • AP • Hate rate • Respiratory stimulation • Adjunctive effect

  9. Doxapram • over dosage of CNS depressant • COPD (chronic obstructive pulmonary disease • Respiratory depression in postoperative recovery period

  10. Doxapram: Contraindication • Newborn • Epilepsy • Hypertension • Stroke

  11. Amphetamines • Produce mood elevation or euphoria, increase mental alertness and capacity for work, decrease fatigue and drowsiness, prolong wakefulness.

  12. Amphetamines usage • Narcolepsy • ADHD (attention-deficit/hyperactivity disorder

  13. Amphetamines • Tolerance • Psychological dependence • High abuse potential (under Control Substance Act

  14. Methylxanthines • COPD (chronic obstructive pulmonary disease • Respiratory depression in postoperative recovery period

  15. Anorexants • Central acting (Benzphetamine, diethylpropion, Sibutramine) • Metabolism acting (orlistat)

  16. Antidepressants • Used to treat depression • Depression, common feelings • Pessimism • Worry • Intense sadness • Loss of concentration • Slowing of mental processes • Problems with eating and sleeping

  17. Serotonin agonist (Sumatriptan) • Treatment of migraine

  18. Loss of interest in usual activities Low self-esteem Self-pity Significant weight loss or gain Insomnia or hypersomnia Extreme restlessness Loss of energy Feelings of worthlessness Diminished ability to think Feelings of guilt Recurrent thoughts of death Suicide attempts AntidepressantsCommon Symptoms of Depression

  19. Antidepressants Depression • Women are affected more often than men • When men are affected, it is usually later in life • Levels of neurotransmitters in the brain may be a causative factor

  20. Mood Disorders • Mania • Bipolar Disorder • Unipolar Disorder

  21. Mood Disorders • Mania Mood of extreme excitement, excessive elation, hyperactivity, agitation, and increased psychomotor activity • Bipolar Disorder • Unipolar Disorder

  22. Mood Disorders • Mania • Bipolar Disorder Mood swings alternate between major depression and mania • Unipolar Disorder

  23. Mood Disorders • Mania • Bipolar Disorder • Unipolar Disorder Major depression with no previous occurrence of mania

  24. Treatment for Depression Electroconvulsive Therapy • Introduction of brief, but convulsive electrical stimulation through the brain • Can induce seizures • Effective for major and delusional depression

  25. Antidepressants • Selective Serotonin Reuptake Inhibitors (SSRIs) • Cyclic Antidepressants • Monoamine Oxidase Inhibitors (MAOIs)

  26. Antidepressants Selective Serotonin Reuptake Inhibitors (SSRIs) • Block the reuptake of serotonin, with little effect on norepinephrine • Fewer side effects than older meds

  27. Treatments Cyclic Antidepressants • Two Types • Tricyclic antidepressants (TCAs) • Tetracyclic antidepressants • Prevent reuptake of norepinephrine and/or serotonin • Agents in this class differ in adverse effects, cost, and response

  28. Treatments Monoamine Oxidase Inhibitors (MAOIs) Allows for buildup of norepinephrine at the synapse

  29. Drug List SSRIs for Depression • citalopram (Celexa) • escitalopram (Lexapro) • fluoxetine (Prozac, Sarafem) • fluvoxamine • paroxetine (Paxil) • sertraline (Zoloft) • venlafaxine (Effexor)

  30. Dispensing Issues Look-Alike Drugs • Prozac and Proscar (urinary drug) • Zoloft and Zocor (high cholesterol) • Celexa and Cerebyx (seizures) and Celebrex (arthritis) Warning!

  31. SSRIDispensing Issues • Do not discontinue abruptly • Alcohol consumption should be avoided while taking these medications Warning!

  32. fluoxetine (Prozac) • Indicated for major depression and obsessive-compulsive disorder (OCD) • Anorexia is a possible adverse effect • Take in the morning to avoid insomnia

  33. paroxetine (Paxil) • Indicated for depression, obsessive-compulsive disorder, and panic disorder

  34. venlafaxine (Effexor) • Blocks reuptake of serotonin and norepinephrine • Indicated for depression • May cause increase in blood pressure and blurred vision

  35. sertraline (Zoloft) • Indicated for depression and obsessive-compulsive disorder • Primary side effect is nausea • May also cause drowsiness

  36. citalopram (Celexa) • Indicated for depression and obsessive-compulsive disorder • Minimal drug interactions

  37. escitalopram (Lexapro) • Similar to Celexa • More potent with fewer side effects

  38. Drug List Cyclic Antidepressants Tricyclic • amitriptyline (Elavil) • clomipramine (Anafranil) • desipramine (Norpramin) • doxepin (Sinequan) • imipramine (Tofranil)

  39. Drug List Cyclic Antidepressants Tricyclic • nortriptyline (Aventyl, Pamelor) • protriptyline (Vivactil) • trimipramine (Surmontil) Tetracyclic • maprotiline

  40. Tricyclic Antidepressants Dispensing Issues • Improvements are usually seen in 10 to 21 days • Can be cardiotoxic in high doses • May cause postural hypotension Warning!

  41. Tricyclic AntidepressantsDispensing Issues Do not discontinue abruptly. Warning!

  42. Cyclic Antidepressants Side Effects • Sedation is common, but tolerance usually occurs • Have many anticholinergic effects

  43. Discussion Why would cyclic antidepressants be prescribed for bed wetting in children?

  44. Discussion Why would TCAs be prescribed for bed wetting in children? Answer They may be prescribed because of their anticholinergic side effects.

  45. Drug List MAOIs • phenelzine (Nardil) • selegiline (Eldepryl) • tranylcypromine (Parnate)

  46. MAOI Dispensing Issues Be cautious of many interactions with foods such as aged cheeses, concentrated yeast extracts, pickled fish, sauerkraut, broad bean pods, chocolate, and alcohol. Warning!

  47. MAOI Dispensing Issues If changing to another class of antidepressant, patient must have a two-week “wash out” period before starting the new medication. Warning!

  48. Drug List Other Antidepressants • bupropion (Wellbutrin, Zyban) • mirtazapine (Remeron) • trazodone (Desyrel)

  49. trazodone (Desyrel) • Prevents reuptake of serotonin and norepinephrine • Has a better side effect profile than TCAs • Caution: possible interaction with Ginkgo

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