anti-psychotic drugs

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anti-psychotic drugs

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anti-psychotic drugs

  1. 1. ANTI-PSYCHOTIC DRUGS http://crisbertcualteros.page.tl
  2. 2. ANTI – PSYCHOTIC DRUGS • NEUROLEPTIC DRUGS • ANTI-SCHIZOPHRENIC DRUGS • MAJOR TRANQUILIZERS • DOPAMINE RECEPTOR ANTAGONISTS
  3. 3. TYPES OF PSYCHOSIS • SCHIZOPHRENIA • AFFECTIVE DISORDERS (DEPRESSION/MANIA) • ORGANIC PSYCHOSES (CAUSED BY HEAD INJURY, ALCOHOLISM, OTHERS)
  4. 4. THE NATURE OF SCHIZOPHRENIA • Begins at an early age • Strong hereditary factor POSITIVE SYMPTOMS  Delusions / Hallucinations Thought disorder NEGATIVE SYMPTOMS Withdrawal from social contacts Flattening of emotional responses
  5. 5. THE DOPAMINE HYPOTHESIS • SCHIZOPRENIA: WITH EXCESSIVE DOPAMINIERGIC ACTIVITY 1. ANTIPSYCHOTIC DRUGS BLOCK POSTSYNAPTIC D2 RECEPTORS IN CNS 2. DRUGS THAT INCREASE DOPA AGGRAVATE SCHIZOPHRENIA
  6. 6. THE DOPAMINE HYPOTHESIS 3. DOPAMINE RECEPTOR DENSITY ↑ in schizophrenia 4. POSITRON EMISSION TOMOGRAPHY (PETS) ↑ DRD 5. HOMAVANILLIC ACID (HAV) change in amount
  7. 7. CLASSIFICATION OF ANTIPSYCHOTIC DRUGS 1. TYPICAL ANTIPSYCHOTICS a. Phenothiazine derivatives • Aliphatic Derivative: CHLORPROMAZINE • Piperidine Derivative: THIORIDAZINE • Piperazine Derivative: FLUPENAZINE, PERPHENAZINE, TRIFLUOPERAZINE b. Thioxanthene Derivative: THIOTHIXENE c. Butyrophenone: HALOPERIDOL
  8. 8. CLASSIFICATION OF ANTIPSYCHOTIC DRUGS 2. ATYPICAL ANTIPSYCHOTICS • CLOZAPINE LOXAPINE • OLANZAPINE QUETIAPINE • RISPERIDONE MOLINDONE • ZIPRASIDONE • SERTINDOLE ARIPIPRAZOLE
  9. 9. PHARMACOKINETICS • READILY BUT INCOMPLETELY ABSORBED • FIRST PASS METABOLISM • HIGHLY LIPID SOLUBLE • LARGE V d > 7 L / kg • PROTIEN BOUND • COMPLETELY METABOLIZED • LITTLE EXCRETED UNCHANGED • T ½ is 10 -24 hours
  10. 10. MECHANISM OF ACTION • DOPAMINE RECEPTOR-BLOCKING ACTIVITY IN THE BRAIN • SEROTONIN RECEPTOR-BLOCKING ACTIVITY IN THE BRAIN • BLOCK CHOLINERGIC, ADRENERGIC & HISTAMINERGIC RECEPTORS
  11. 11. DOPAMINERGIC SYSTEM • MESOLIMBIC-MESOCORTICAL : substancia nigra………>limbic system BEHAVIOR 2. NIGROSTRIATAL : substancia nigra,,,……...>caudate & putamen VOLUNTARY MOVEMENTS 3.TUBEROINFUNDIBULAR: arcuate nuclei & periventricular neurons,,,> hypothalamus & post pituitary; INHIBITS PROLACTIN SECRETION
  12. 12. DOPAMINERGIC SYSTEM 4.MEDULLARY-PERIVENTRICULAR : motor nuclei of the vagus EATING BEHAVIOR 5. INCERTOHYPOTHALAMUS : from the medial zona incerta to the hypothalamus and the amygdala REGULATE THE ANTICIPATORY MOTIVATIONAL PHASE OF COPULATORY BEHAVIOR IN RATS
  13. 13. DOPAMINE RECEPTORS • D1: CHROMOSOME 5; ↑ cAMP…> activation of adenyl cyclase • D5 : CHROMOSOME 4; ↑ cAMP • D2: CHROMOSOMES 11: ↓ cAMP…> blocks Ca ++ channels…> opens K + channels • D3: CHROMOSOME 11: ↓ cAMP • D4: ↓ cAMP
  14. 14. DIFFERENCES AMONG ANTIPSYCHOTIC DRUGS CHLORPROMAZINE: a1=5HT2 >D2 >D1 HALOPERIDOL: D2>D1=D4>a1>5HT2 CLOZAPINE : D4=a1>5HT>D2=D1
  15. 15. DIFFERENCES AMONG ANTIPSYCHOTIC DRUGS OLANZAPINE: 5HT2A >D4 >D2 >a1 >D1 ARIPIPRAZOLE: D2 = 5HT 2A > D4 > a1 =H1 > > D1 QUETIAPINE: H1 >a1 > M1,3 > D2 > 5 HT2a
  16. 16. ANTIPSYCHOTIC AGENTS • PSYCHOLOGICAL EFFECTS > sleepiness, restlessness, impaired performance & judgment • NEUROPHYSIOLOGIC EFFECTS > hypersyncrony focal /unilateral • ENDOCRINE EFFECTS > amenorrhea, galactorrhea, increase libido, false( +) pregnancy tests • ↓ libido in males, gynecomastia
  17. 17. ANTIPSYCHOTIC AGENTS • CARDIOVASCULAR EFFECTS orthostatic hypotension  high resting pulse rate ↑ PR, ↓ stroke volume, ↓ mean arterial pressure, ↓ peripheral resistance NAUSEA & VOMITING Block the chemoreceptor trigger zone
  18. 18. CLINICAL INDICATIONS A. PSYCHIATRY INDICATIONS • SCHIZOPHREMIA • SCHIZOAFFECTIVE DISORDERS • MANIC EPISODES IN BIPOLAR DISORDERS • GILLES DE TOURETTE SYNDROME • SENILE DEMENTIA B. NONPSYCHIATRIC INDICATIONS >ANTI-EMETIC EFFECT (prochlorperazine) >ANTI-PRURITIC EFFECTIphenothiazines) >PREOPERATIVE ANESTHESIA.promethazine >NEUROLEPTIC ANESTHESIA..droperidol
  19. 19. SIDE EFFECTTS OF NEUROLEPTIC DRUGS A. NEUROLOGIC EFFECTS 1. ACUTE DYSTONIA : Spasm of muscles tongue, face, neck, back, may mimic seizures • During the first 1 -5 days of Rx • Mechanism unknown • Rx: antiparkinson’s agents 2. AKATHISIA : Motor restlessness • 5 -60 days • Mechanism unknown; Rx with diphenhydramine
  20. 20. 3. PARKINSONISM  bradykinesia, rigidity, tremor, mask facies, shuffling gait seen in 5-30 days Mechanism is antagonism of Dopamine Rx: Antiparkinson’s Agents 4. NEUROLEPTIC MALIGNANT SYNDROME: catatonia, stupor, fever, unstable BP, myoglobulinemia after weeks of treatment Mechanism: Antagonism of Dopamine Rx: Stop neuroleptic immediately; Dandrolene; Bromocriptine, Antiparks not effective
  21. 21. 5. PERIODIC TREMOR (RABBIT SYNDROME) Perioral tremors  after months or years of treatment Mechanism : unknown Rx Antiparkinson’s Drugs 6. TARDIVE DYSKINESIA oral-facial dyskinesia, choreoathetosis, dystonia After months or years of Rx Worse on withdrawal Mechanism: excess function of dopamine Rx: prevention crucial Rx unsatisfactory
  22. 22. ADVERSE EFFECTS II. BEHAVIORAL EFFECTS: • Pseudo-depression; toxic confusional state III. AUTONOMIC NERVOUS SUSTEM EFFECTS : • urinary retention,dry mouth, loss of accommodation, constipation (MUSCARINIC CHOLINERGIC BLOCKADE) • orthostatic hypotension, impotence, failure to ejaculate ( ALPHA ADRENORECEPTOR BLOCKADE)
  23. 23. ADVERSE EFFECTS IV. METABOLIC & ENDOCRINE EFFECTS Weight gain, hyperglycemia, hyper - prolactenemia, amenorrhea-galactorrhea syndrome, infertility, impotence in males V. TOXIC OR ALLERGIC REACTIONS Agranulocytosis (clozapine) , cholestatic jaundice, skin eruptions VI. CARDIAC TOXICITY Ventricular arrythmias (thioridazine) VII. OCULAR COMPLICATIONS: “ browning of vision”
  24. 24. ANTIMANIC AGENTS • MOOD STABILIZING AGENT • BIPOLAR DISORDERS (MANIC- DEPRESSIVE) • DISORDER WITH PREPONDERANCE OF CATHECHOLAMINE RELATED ACTIVITY • LITHIUM CARBONATE • CARBAMAZEPINE, VALPROIC ACID
  25. 25. LITHIUM P’KINETICS ABSORPTION : virtually complete within 6 -8 hrs; peak plasma levels in 30 min to 2 hrs DISTRIBUTION: in total body water; slow entry into intracellular compartment. No protein binding METABOLISM: None EXCRETION: virtually entirely in urine; plasma half life is about 20 hours
  26. 26. LITHIUM ‘ DYNAMICS • EFFECTS ON ELECTROLYTES & IONS TRANSPORT: Substitute for sodium • EFFECTS ON NEUROTRANSMITTER  enhance effects of serotonin? Decrease norepinephrine & dopamine turnover Block dopamine receptor supersensitivity Augment synthesis of acetylcholine?
  27. 27. LITHIUM PHARMACODYNAMICS • EFFECTS ON SECOND MESSENGER effect on IP3/ DAG EFFECTS ON PHOSPHOINOSITOL TURNOVER…..> EARLY RELATIVE REDUCTION OF MYOINOSITOL IN HUMAN BRAIN
  28. 28. LITHIUM ADVERSE EFFECTS 1. CNS EFFECTS; dizziness, mild ataxia 2. NEUROMUSCULAR EFECTS: fine tremors 3. CV EFFECTS: ventricular arrythmias 4. GIT EFFECTS: nausea, vomiting, diarrhea 5. GUT EFFECTS: polyuria 6. ENDOCRINE EFFECTS: hypothyroidism 7. ALLERGIC REACTION: pruritus, rash 8. OVERDOSE TOXICITY: vomiting, drowsiness, decrease consciousness seizures Rx: dialysis
  29. 29. LITHIUM CONTRAINDICATION A. MARKED DEHYDRATION OR SODIUM DEPLETION B.SIGNIFICANT RENAL OR CARDIAC DISEASES C. PREGNANCY(W) D. RENAL CONCENTRATION ABILITY(W) • Nephrogenic diabetes insipidus with polyuria
  30. 30. DRUG INTERACTIONS A. THIAZIDE DIURETICS: ↓ RENAL CLEARANCE OF LITHIUM B. NSAID: ↓ LITHIUM CLEARANCE C. ANTIPYSCHOTIC AGENTS: ↑ NEUROTOXICITY
  31. 31. DEPRESSION I.REACTIVE OR SECONDARY DEPRESSION Core Depression Syndrome: depression, anxiety, tension, bodily complaints, guilt (> 60%) II.ENDOGENOUS DEPRESSION Core Depression Syndrome plus ABNORMAL VS rhythm of sleep, motor activity, livido, decrease appetite ( 25%) III. DEPRESSION ASSOCIATED WITH BIPOLAR AFFECTIVE DISORDER (10-15%)
  32. 32. ANTIDEPRESSANTS I.TRICYCLIC ANTIDEPRESSANTS IMIPRAMINE. AMITRYPTYLINE, DOXAPIN, NORTRIPTYLLINE ,DESIPRAMINE. CLOMIPRAMINE , PROTIPTYLINE, TRIMIPRAMINE B. HETEROCYCLIC, SECOND & THIRD DEGENERATIONS 1. SECOND GENERATIONS AMOXAPINE, MAPROTILINE TRAZODON, BUPROPION 2. THIRD GENERATIONS MIRTAZAPINE, VENLAFAZINE NEFAXODONE
  33. 33. ANTIDEPRESSANTS C. SELECTIVE SEROTONIN REUPTAKE INHIBITORS (SSRI) • FLUOXETINE FLUVOXAMINE • PAROXETINE ESCITALOPRAM • SERTRALINE CITALOPRAM D. MONOAMINE OXIDASE INHIBITORS (MAOI) • PHENELZINE, TRANYLCYPROMINE • MOCLOBEMIDE
  34. 34. ANTIDEPRESSANTS PHARMADYNAMICS A. ACTION OF ANTIDEPRESSANTS ON BIOGENIC AMINE NEUROTRANSMITTERS  TRICYCLICS: BLOCK AMINE REUPTAKE PUMPS  MAOI: BLOCK DEGRADATIVE PATHWAY FOR THE AMINE NEUROTRANSMITTERS  TRAZODON, NEFAZODONE & MIRTAZAPINE: SERETONIN RECEPTORS ANTAGONIST
  35. 35. B.RECEPTOR & POSTRECEPTOR EFFECTS • SSRI: ↓ in norepinephrine cAMP & in beta -adrenoreceptor binding • MAOI: mixed action with norepinephrine & serotonin • ↑ serotonergic transmission mediated through diverse mechanisms
  36. 36. Drug Sedati Muscar NE 5HT reuptake ve inicrBl reuptake block ock Block Amitryptyline +++ +++ ++ +++ Imipramine ++ + + ++ Amoxapine ++ + ++ + Bupropion - - - - Trazodone +++ - - ++ Mirtazepine +++ - - - Venlafaxine - - +++ ++ Fluoxetine - + - +++
  37. 37. PHARMACOKINETICS • A. TRICYCLICS Incompletely reabsorbed First pass metabolism Large Vd Metabolized HETEROCYCLICS Variable bioavailabilitiy High protein binding Variable and large Vd Active metabolites
  38. 38. PHARMACOKINETICS • SSRI : FLUOXETINE • Well absorbed • PPC: 4 – 8 hrs • Inhibits drug metabolizing enzymes • MAOI • Readily absorbed
  39. 39. CLINICAL INDICATIONS A. DEPRESSION B. PANIC DISORDER C. OBSESSIVE COMPULISVE D. ENURESIS E. CHRONIC PAIN F. OTHERS: Eating Disorder(Bulemia) Cataplexy asstd with Narcolepsy, School Phobia, Attention Deficit Syndrome
  40. 40. ADVERSE EFFECTS • TRICYCLICS Sedation: Sleepiness Synpathomimetic; tremors, insomnia Antimuscarinic; blurred vision. constipation confusion, urinary incontinence
  41. 41. TRICYCLICS Psychiatric: psychoses aggravated CVS: orthostatic hypotension Neurologic: Seizures Metabolic-Endocrine: weight gain, sexual disturbance
  42. 42. ADVERSE EFFECTS MAO INHIBITORS headache, drowsiness, dry mouth, weight gain, postural hypotension, sexual distn AMOXAPIN  Tricyclic & antipsychotic effects MAPROTILINE Tricyclic Effects
  43. 43. ADVERSE EFFECTS TRAZODONE & NEFAZODONE: drowsiness, dizziness, insomnia, nausea, agitation BUPROPION dizziness, dry mouth, tremor FLUOXETINE Anxiety, insomnia, tremors, decr libido, GIT effects
  44. 44. Foods that interact with MAOI • High in tyramine content: BEER. BROAD BEANS, LAVA BEANS CHEESE. CHICKEN LIVER  SAUSAGES  SNAILS WINE, RED WINE YEAST
  45. 45. Drugs that Interact with MAOI A.INDIRECTLY ACTING SYMPATHOMIMETICS: amphetamines, ephedrine, metaraminol, phenylpropanolamine B. OTHER ADRENORECEPTOR AGENTS & RELATED AGENTS: levodopa, methyldopa, guanethidine, reserpine C. OPIOID ANALGESICS & DERIVATIVES: morphine, codeine, meperidine, dextromethorpham D.MISCELLANEOUS DRUGS: buspirone, fluoxetine, LSD

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