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Anti depressant Drugs

Anti depressant Drugs. Rezaei M. MD Psychiatrist. Tricyclics. Tertiary amines: Imipiramine Amitriptyline Clomipramine Trimipiramine Doxepin Secondary amines Desipiramine Nortriptyline protriptyline. Tetracyclics. Amoxapine Maprotiline Minaserin. Pharmacological actions.

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Anti depressant Drugs

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  1. Anti depressant Drugs Rezaei M. MD Psychiatrist

  2. Tricyclics • Tertiary amines: • Imipiramine • Amitriptyline • Clomipramine • Trimipiramine • Doxepin • Secondary amines • Desipiramine • Nortriptyline • protriptyline

  3. Tetracyclics • Amoxapine • Maprotiline • Minaserin

  4. Pharmacological actions • Absorbed from oral administration • Peak plasma concentration 2-8 hrs • Half life vary from 10 to 70 hrs ( nortriptyline, maprotiline and protriptyline may have longer half lives ) • 5-7 days are needed to reach steady state plasma concentration • Metabolized in liver by cytochrome p-450 enzyme • Drug interaction with quinidine, cimetidine , fluxetine, serteraline, paroxetine , phenothiazine, carbamazepine • Genetic variability between persons are responsible for up to 40-fold differences in plasma concentrations of TCA`s

  5. Mechanism of action: • Block the reuptake of NEP and serotonin • Competitive antagonists at the muscarinic acetylcholine, histamine H1, @1 and @2-adrenergic receptors.( Amoxapine, nortriptyline, desipramine, maprotiline have the least anticholinergic activity. Doxepine has the most antihistaminergic activity, clomipramine is the most sertonin-selective of the TCAs)

  6. Adverse effects • Psychiatric effects • A major adverse effect is the possibility of inducing a manic episode in patients +/- history of BMD I disorder • Anticholinergic effects • Patient may develop a tolerance for these effects with continued treatment. • Amitriptyline • Imipramine • Doxepin • Trimipramine • Dry mouth, constipation, blurred vision , urinary retention, • Treatment • Beware of narrow angle glaucoma • Severe reactions may induce CNS anticholinergic syndrome with confusion and delirium

  7. Sedation • Amitriptyline • Trimipramine • Doxepin • The least sedative effects are in desipiramine and protriptyline • Autonomic effects • Orthostatic HOTN ,Partly because of @1-adrenergic blockade • Nortriptyline least likely cause the problem • Fludrocortisone may be helpful • Other effects include sweating , palpitation, HTN

  8. Cardiac effects • In the usual therapeutics doses: tachycardia, flattened T wave, prolonged QT interval, and depressed ST segment • Because the drug prolong conduction time, their use in patients with preexisting conduction defects is contraindicated. • The drug should be discontinued several days before elective surgery because of occurrence of hypertensive episodes during surgery in patients receiving TCAs.

  9. Neurlogical effects • Desipramine and protriptyline are associated with psychomotor stimulation: • Myoclonic jerks and tremors of tongue and upper extremities • Speech block • Paresthesia • Peroneal palsy • Ataxia • Amoxapineis unique in causing • Parkinsonian symptoms • Akathisia • Dyskinesia • rarely; neuroleptic malignant syndrome

  10. Maprotiline may cause seizures if • Dose increase too quickly • Dose keep at high level for too long • Overall TCAs have relatively low risk for inducing seizures, except in patients who are at risk for seizures.

  11. Allergic and hematological effects • Rash in 4-5 % in maprotiline • Jaundice is rare • Agranulocytosis, leukopenia and leukocytosis are rare. • However , a patient with fever or sore throat during the first few months of TCA treatment, should have a CBC immediately.

  12. Other adverse effects : • Weight gain • Impotence • Gynecomastia • Amenorrhea • Nausea • Hepatitis • Vomiting • SIADH

  13. SSRI • Major differences between them is different pharmacokinetics profiles • Fluoxetine has the longest half life of 2-3 days, others of about 2o hrs. • All well absorbed orally and metabolized in the liver • Paroxetine and fluoxetine are metabolized by CYP 2D6, be careful in coadministration of drugs with the same enzyme metabolizer • Fluvoxamine inhibits the CYP 3A4, so interfere with terfenadine and astemizole. • If taken with food, it reduce nausea and diarrhea.

  14. Therapeutic indications of SSRI • Depression ; they are first line in the general population ( mild and moderate Dep. ), the elderly, the medically ill and those who are pregnant. • Serteraline may be more effective for treatment of severe depression with melancholia • Over 50% of persons who respond poorly to one SSRI will respond favorably to another.

  15. Augmentation strategies • In depressed persons with partial response : • Bupropion • Lithium • Levothyroxine • Sympathomimetics • Pindolol • Clonazepam

  16. Suicide • Markedly reduce the risk of suicide • Depression during pregnancy • No documented adverse reaction • SSRI may produce a self limited neonatal withdrawal syndrome that consist of jitterness and mild tachypnea, it begins several hrs after birth and may persist for days to a few weeks. It is rare and does not interfere with feeding.

  17. Postpartum depression(+/- psychotic feature) • Depression in the Elderly and Medically ill • Precise diagnostic evaluation to rule out dementia and delirium. • They are less well tolerated by persons with preexisting GI symptoms. • Chronic depression • They have to continue taking SSRI`s for at least 1 year.

  18. Depression in children • Children of depressed adults are at increased risk of depression. • Adverse effects in children includes GI symptoms, insomnia, motor restlessness, social disinhibition, and hypomania or mania; so SSRI use with small doses. • OCD • Fluvoxamine and Serteraline are approved for treatment of pediatric OCD • Effective dose for OCD is higher than those required for depression.

  19. Panic Disorders • SSRI`s are far superior to benzodiazepines for treatment of panic disorder with depression. • Are effective for childhood panic symptoms • Social Phobia • Posttraumatic Stress Disorder • SSRI`s are more effective than TCAD and MAO`s inhibitor • Marked improvement of both intrusive and avoidant symptoms. • Specific phobias, GAD, separation anxiety

  20. Bulimia Nervosa and other Eating Disorder • Fluoxetine • Obesity ; fluoxetine in combination with behavioral program • PremensturalDysphoric Disorder • Fluoxetine and Serteraline

  21. Adverse Reactions of SSRI`s • Sexual dysfunction: inhibited orgasm and decreased libido. • Gastrointestinal : nausea, diarrhea, vomiting, dyspepsia, anorexia. • Weight Gain • Headaches; 18-20 % • Anxiety • Insomnia and Sedation • Vivid dreams and Nightmares • Seizures • Extrapyramidal Symptoms • Galactorrhea • Hypoglycemia , rarely hyponatremia and SIADH

  22. Serotonin Syndrome • Concurrent administration of an SSRI with MAOI, l-tryptophan, or lithium can rise plasma serotonin concentration • Diarrhea • Restlessness • Agitation , hyperreflexia, autonomic instability, rapid fluctuations of vital signs • Myoclonus , seizures, hyperthermia, rigidity, • Delirium , coma, cardiovascular collapse and death.

  23. SSRI`s Withdrawal • Dizziness • Weakness • Nausea • Headaches • Rebound depression • Anxiety • Insomnia • Poor concentration • Upper respiratory symptoms • Paresthesia • Migranelike symptoms

  24. BUPROPION • More effective against symptoms of depression than those of anxiety. • Half life 12 hrs. • Blockade of dopamine reuptake • Therapeutic indications: • Depression • Bipolar Disorders • ADHD • Cocaine Detoxification • Smoking cesation

  25. BUPROPION • Adverse reaction • Headache • Insomnia • Upper respiratory symptoms • Nausea • Restlessness • Agitation • Irritability • Weight loss 25% • Dry mouth • constipation

  26. Trazodone • Half life is 6-11 hrs • Specific inhibitor of serotonin reuptake • Depressive Disorder • Insomnia

  27. Venlafaxine • May have faster onset of action than other antidepressant • Most effective drugs for treatment of severe depression with melancholic features & GAD • Half life 3.5 hrs( SR-form 9 hrs ) • Inhibitor of serotonin & norepinephrine reuptake and weak inhibitor of dopamine reuptake • Therapeutic indications • Depression • GAD • OCD • Panic • Agarophobia , social phobia, ADHD

  28. Adverse reactions: • Nausea • Somnolence • Dry mouth • Dizziness • Constipation • Asthenia • Anxiety • Anorexia • Blurred vision • Abnormal ejaculation and orgasm • Errectile disturbance and impotence

  29. Duloxetine • Inhibitor of serotonin and norepinephrine

  30. MAIO Drugs • Used less frequently than others • Increase biogenic amine neurotransmitter level • There are two type of MAO : A & B • MAOA metabolize NEP, SER, EPI • MAOB metabolize DOP, TYR • Therapeutic indications: • Depression, Atypical depression • Panic • Agarophobia • PTSD • Eating Disorder • Social phobia • Pain Disorder

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