PRESENTED  BY- PATEL KUNWAR VIKAS PRESENTED TO – M.PHARM 1 St  YEAR Mr.- TALHA JAWAID HOD  PHARMACOLOGY HIPER LKW.
DEFINITION
<ul><li>Cause of depression </li></ul><ul><li>Depression is caused by- </li></ul><ul><li>Deficiency of amines, </li></ul><...
<ul><li>Unipolar </li></ul><ul><li>Where   patient/ subject feel depression symptom (Mind swing in some direction.)   </li...
What is mania? <ul><li>It is also refers to a pathological change in mood state. But in Mania amine level is increased.  <...
Causes of Mania   <ul><li>may be caused by drug. </li></ul><ul><li>may be caused by disease. </li></ul><ul><li>may be caus...
Classification of Antidepressant drugs <ul><li>Tricyclic anti-depressants (TCAs): </li></ul><ul><li>NA and 5 HT reuptake i...
<ul><li>D.   Serotonin nor epinephrine reuptake inhibitor: </li></ul><ul><li>  Venlafaxine, Duloxetine. </li></ul><ul><li>...
 
A . Tricyclic Antidepressants (TCAs) <ul><li>Depression is associated with reduced levels of the monoamines in the brain, ...
. <ul><li>This re-uptake blockade leads to the accumulation of 5-HT in the synaptic cleft and the concentration of 5-HT re...
 
<ul><ul><li>5HT and NA neurotransmission is similarly affected but the effect on  the  dopamine system is much less import...
<ul><li>Pharmacological action: </li></ul><ul><li>CNS-mood elevation in depress patient,can cause ataxia,epilepsy,seizures...
 
<ul><li>Side Effects: </li></ul><ul><li>Atropine-like side effects: dry mouth, paradoxical excessive perspiration, constip...
3 . Less commonly, tricyclics may interfere with the anti-hypertensive actions of methyl nor epinephrine( the active metab...
Adverse Effects Pharmacological Action Adverse Effect Muscarinic receptor Blockage/ Anticholinergic <ul><li>Dry mouth, tac...
Toxic Effects <ul><li>CVS : Ventricular fibrillation, Conduction disturbances, Low BP, --- ecg shows prolong PR and QT int...
B.  Selective Serotonin Re-uptake Inhibito r s (SSRI) <ul><li>SSRIs (selective serotonin reuptake inhibitors) are the most...
<ul><li>SSRIs block the reabsorption (reuptake) of the neurotransmitter serotonin in the brain.  </li></ul><ul><li>SSRIs a...
Adverse effects <ul><li>Relative improvement to other antidepressants  (mostly mild) </li></ul><ul><li>Less Cardiotoxic co...
  Safety concerns with selective serotonin reuptake inhibitors SSRIs are relatively safe. However, there are some things y...
MAO INHIBITORS <ul><li>Mechanism of action: </li></ul><ul><li>Inhibit MAO enzymes (non-selective):  </li></ul><ul><li>1) I...
<ul><li>The mechanism of action of monoamine oxidase A inhibitors </li></ul><ul><li>Monoamine oxidase A (MAOA) is an enzym...
<ul><li>The mechanism of action of monoamine oxidase B inhibitors  </li></ul><ul><li>Monoamine oxidase B (MAOB) is an enzy...
<ul><li>Interactions with Food/Tobacco/Alcohol </li></ul><ul><li>Caffeine </li></ul><ul><li>Dopamine Containing Food </li>...
<ul><li>Serotonin and norepinephrine reuptake inhibitors  </li></ul><ul><li>Serotonin and nor epinephrine reuptake inhibit...
<ul><li>Side effects and cautions </li></ul><ul><li>All SNRIs work in a similar way and generally cause similar side effec...
<ul><li>Safety concerns: </li></ul><ul><li>Antidepressants and pregnancy. </li></ul><ul><li>Drug interactions.  </li></ul>...
<ul><li>Atypical antidepressants </li></ul><ul><li>Atypical antidepressants ease depression by affecting chemical messenge...
Side effects. S.N. DRUGS Side effects 1 Bupropion   Anxiety, restlessness or agitation, Confusion, Constipation, Dry mouth...
THANK    You    ALL
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Antidepressant

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Antidepressant

  1. 1. PRESENTED BY- PATEL KUNWAR VIKAS PRESENTED TO – M.PHARM 1 St YEAR Mr.- TALHA JAWAID HOD PHARMACOLOGY HIPER LKW.
  2. 2. DEFINITION
  3. 3. <ul><li>Cause of depression </li></ul><ul><li>Depression is caused by- </li></ul><ul><li>Deficiency of amines, </li></ul><ul><li>Functional deficiency of amines (dopamine, adrenaline, nor-adrenaline, etc.) </li></ul><ul><li>in any part of brain. </li></ul><ul><li>Types of Depression </li></ul><ul><li>Unipolar </li></ul><ul><li>Bipolar </li></ul><ul><li>Endogenous depression </li></ul>
  4. 4. <ul><li>Unipolar </li></ul><ul><li>Where patient/ subject feel depression symptom (Mind swing in some direction.) </li></ul><ul><ul><ul><li>Depression – pathologically depressed mood (life time prevalence up to 17%) </li></ul></ul></ul><ul><ul><ul><li>Bipolar </li></ul></ul></ul><ul><ul><ul><li>Depression associated with mania. </li></ul></ul></ul><ul><ul><ul><li>sometimes called by, manic depression. </li></ul></ul></ul><ul><ul><ul><li>Endogenous depression </li></ul></ul></ul><ul><ul><ul><li>Due to shock (It is for short period of time.) </li></ul></ul></ul>
  5. 5. What is mania? <ul><li>It is also refers to a pathological change in mood state. But in Mania amine level is increased. </li></ul><ul><li>Mania alone is rare (10%) and most frequently cycles with Major/endogenous depression (Manic-Depressive Disease, Bipolar Disorder). </li></ul><ul><li>SYMPTOMS </li></ul><ul><li>Irritable mood, </li></ul><ul><li>Racing thought, </li></ul><ul><li>Reduced sleep, </li></ul><ul><li>Violent behaviour, </li></ul><ul><li>Loss of contact with reality, </li></ul><ul><li>Accelerated speech. </li></ul>
  6. 6. Causes of Mania <ul><li>may be caused by drug. </li></ul><ul><li>may be caused by disease. </li></ul><ul><li>may be caused by different vitamins. </li></ul><ul><li>Antidepressant drug </li></ul><ul><li>These are drugs which can elevate mood in depressive illness. </li></ul>
  7. 7. Classification of Antidepressant drugs <ul><li>Tricyclic anti-depressants (TCAs): </li></ul><ul><li>NA and 5 HT reuptake inhibitors – </li></ul><ul><li>Imipramine, Amitryptiline, Doxepin, Dothiepin and Clomipramine, Nortriptyline, Triimipramine. </li></ul><ul><ul><ul><li>b) NA reuptake inhibitors – </li></ul></ul></ul><ul><ul><ul><li>Desimipramine, Nortriptyline, Amoxapine, </li></ul></ul></ul><ul><li>B . Selective Serotonin reuptake inhibitors: </li></ul><ul><ul><li>Fluoxetine, Fluvoxamine, Sertraline, Paroxetine, Escitalopram and Citalopram. </li></ul></ul><ul><li>C. Atypical antidepressants: </li></ul><ul><ul><li>Trazodone, Mianserin, Mirtazapine, Bupropion </li></ul></ul><ul><ul><li>and Tianeptine. </li></ul></ul>
  8. 8. <ul><li>D. Serotonin nor epinephrine reuptake inhibitor: </li></ul><ul><li> Venlafaxine, Duloxetine. </li></ul><ul><li>E. MAO inhibitors: </li></ul><ul><ul><li>Irreversible: Isocarboxazid, Iproniazid, Phenelzine and Tranylcypromine. </li></ul></ul><ul><ul><li>Reversible: Moclobemide and Clorgyline. </li></ul></ul>
  9. 10. A . Tricyclic Antidepressants (TCAs) <ul><li>Depression is associated with reduced levels of the monoamines in the brain, such as 5-HT (serotonin) & noradrenaline(NA). </li></ul><ul><li>The selective 5-HT re-uptake inhibitors (SSRIs) are thought to restore the levels of 5-HT in the synaptic cleft by binding at the 5-HT re-uptake transporter preventing the re-uptake and subsequent degradation of 5-HT. </li></ul>
  10. 11. . <ul><li>This re-uptake blockade leads to the accumulation of 5-HT in the synaptic cleft and the concentration of 5-HT returns to within the normal range. </li></ul><ul><li>This action of SSRIs is though to contribute to the alleviation of the symptoms of depression. </li></ul><ul><li>In the presence of the SSRI, small amounts of 5-HT continue to be degraded in the synaptic cleft. </li></ul>
  11. 13. <ul><ul><li>5HT and NA neurotransmission is similarly affected but the effect on the dopamine system is much less important (compare with cocaine). </li></ul></ul><ul><ul><li>In most TCA , other receptors (incl. those outside the CNS) are also affected: blockade of H1-receptor,  -receptors, M-receptors </li></ul></ul>
  12. 14. <ul><li>Pharmacological action: </li></ul><ul><li>CNS-mood elevation in depress patient,can cause ataxia,epilepsy,seizures and coma. </li></ul><ul><li>CVS-orthostatic hypotension. </li></ul><ul><li>ANS-anticholinergic effects.Most potent anticholinergic action. </li></ul>
  13. 16. <ul><li>Side Effects: </li></ul><ul><li>Atropine-like side effects: dry mouth, paradoxical excessive perspiration, constipation, blurred vision, mydriasis, metallic taste, urine retention => muscarinic blockade. </li></ul><ul><li>Drowsiness, sedation and weight gain => Histamine-Receptor blockade. </li></ul><ul><li>Drug interaction: </li></ul><ul><li>Tricyclic interaction includes additive depression of the CNS with other antidepressants include ethanol, barbiturates, benzodiazepines, and opioids. </li></ul><ul><li>Tricyclic may also cause reversal of the anti-hypertensive action of guanethidine by blocking its transport into sympathetic nerve endings. </li></ul>
  14. 17. 3 . Less commonly, tricyclics may interfere with the anti-hypertensive actions of methyl nor epinephrine( the active metabolite of methyldopa) and clonidine. 4. Tricyclics also share metabolic pathways with phenytoin, hence it may increase concentrations of phenytoin. 5. Tricyclics also potentiate the pressor effects of adrenaline and noradrenaline, so that there is a potential hazard when a local anesthetic is used with a pressor amine.
  15. 18. Adverse Effects Pharmacological Action Adverse Effect Muscarinic receptor Blockage/ Anticholinergic <ul><li>Dry mouth, tachycardia, blurred vision, glaucoma </li></ul><ul><li>Constipation, Urinary retention, Sexual dysfunction </li></ul><ul><li>Cognitive impairement </li></ul>ᾴ1 Adrenoceptor blockade <ul><li>Drowsiness, Postural Hypotension, Sexual dysfunction (loss of libido, impaired erection) </li></ul><ul><li>Cognitive Impairement </li></ul>Histamine H1 receptor Blockade Drowsiness, Weight Gain Membrane stabilizing properties Cardiac conduction defects, Cardiac arrythmia, Seizures Others Rash, Oedema, Leukopenia, Elevated liver enzymes
  16. 19. Toxic Effects <ul><li>CVS : Ventricular fibrillation, Conduction disturbances, Low BP, --- ecg shows prolong PR and QT intervals, depressed ST, flattened T waves. Heartblock occasionally </li></ul><ul><li>RS : Respiratory depression -> Hypoxia, Aspiration pneumonia </li></ul><ul><li>CNS : Agitation, twitching, convulsions, hallucinations, delerium, coma. Parasympathetic dry mouth, dilated pupil, blurred vision, urine retention, pyrexia </li></ul>
  17. 20. B. Selective Serotonin Re-uptake Inhibito r s (SSRI) <ul><li>SSRIs (selective serotonin reuptake inhibitors) are the most commonly prescribed antidepressants. They are relatively safe and generally cause fewer side effects than other types of antidepressants. </li></ul><ul><li>More modern (1 st drug fluoxetine available in 1988) and safe antidepressants </li></ul><ul><li>Principal mechanism of action: </li></ul><ul><ul><li>selective inhibition of 5-HT (sero to nin) reuptake  more extracellular seratonin -> More action on seratonin receptors on post synaptic -> more stimulation </li></ul></ul><ul><ul><li>SSRIs ease depression by affecting chemical messengers (neurotransmitters) used to communicate between brain cells. </li></ul></ul>
  18. 21. <ul><li>SSRIs block the reabsorption (reuptake) of the neurotransmitter serotonin in the brain. </li></ul><ul><li>SSRIs are called selective because they seem to primarily affect serotonin, not other neurotransmitters. </li></ul><ul><li>Pharmacokinetics : </li></ul><ul><li>Good absorption after oral administration </li></ul><ul><li>Important biotransformation in the liver </li></ul><ul><li>Long half-lives of elimination(s) </li></ul><ul><ul><li>fluoxetine (T 1/2 =50h) + active metabolite (T 1/2 =240h) </li></ul></ul><ul><li>Drug interaction: based on plasma protein binding and CYP blockade </li></ul><ul><ul><li>increased effect of co-administered TCA but also  -blockers, benzodiazepines etc. </li></ul></ul>
  19. 22. Adverse effects <ul><li>Relative improvement to other antidepressants (mostly mild) </li></ul><ul><li>Less Cardiotoxic compared to TCA </li></ul><ul><li>Generally, much safer in overdose </li></ul><ul><li>Lack anticholinergic effects and are not Sedating </li></ul><ul><li>GIT – nausea, vomiting, diarrhea </li></ul><ul><li>Neuropsychiatry – Headache, Irritability, Restless (Akathisia)-EPS more common in SSRI than TCA, Agitation, Tremor, Insomnia and daytime somnolence, Seizures Mania </li></ul><ul><li>Sexual dysfunctions – Ejaculatory delay, anorgasmia </li></ul><ul><li>Suicidal Behavior </li></ul><ul><li>Serotonin syndrome upon intoxication or drug interactions </li></ul>
  20. 23. Safety concerns with selective serotonin reuptake inhibitors SSRIs are relatively safe. However, there are some things you should think about before you take one of these antidepressants: <ul><li>Antidepressants and pregnancy. </li></ul><ul><li>Drug interactions. </li></ul><ul><li>Blood-thinning medications and SSRIs.  </li></ul><ul><li>Serotonin syndrome.  </li></ul>
  21. 24. MAO INHIBITORS <ul><li>Mechanism of action: </li></ul><ul><li>Inhibit MAO enzymes (non-selective): </li></ul><ul><li>1) Irreversible MAO inhibitors Phenelzine and isocarboxazid => hydrazides. </li></ul><ul><li>2) Reversible MAO Inhibitors. Tranylcypromine => non-hydrazide,prolonged blockade, but reversible within 4hr. </li></ul><ul><ul><li>Decrease metabolism of most biogenic amines (NE, 5HT, DA, </li></ul></ul><ul><ul><li>tyramine, octopamine). </li></ul></ul>
  22. 25. <ul><li>The mechanism of action of monoamine oxidase A inhibitors </li></ul><ul><li>Monoamine oxidase A (MAOA) is an enzyme involved in the metabolism of the monoamines, eg 5-HT and noradrenaline. </li></ul><ul><li>It converts the monoamines into their corresponding carboxylic acid via an aldehyde intermediate. </li></ul><ul><li>MAOA regulates both the free intraneuronal concentration and the releasable stores of 5-HT and noradrenaline. </li></ul><ul><li>MAOA inhibitors, such as phenelzine, bind to and inhibit MAOA, preventing monoamine degradation. </li></ul><ul><li>MAOA inhibitors are used in the treatment of depression. </li></ul><ul><li>People with depression have lower than normal levels of the monoamines and MAOA inhibitors restore the levels to within the normal range. </li></ul>
  23. 26. <ul><li>The mechanism of action of monoamine oxidase B inhibitors </li></ul><ul><li>Monoamine oxidase B (MAOB) is an enzyme involved in the metabolism of dopamine. </li></ul><ul><li>It converts dopamine to its corresponding carboxylic acid via an aldehyde intermediate. </li></ul><ul><li>MAOB regulates both the free intraneuronal concentration of dopamine and the releasable stores. </li></ul><ul><li>MAOB inhibitors, such as selegiline, bind to and inhibit MAOB, preventing dopamine degradation. </li></ul><ul><li>This results in greater stores of dopamine available for release. MAOB inhibitors are used in the treatment of depression. </li></ul><ul><li>People with depression have lower than normal levels of dopamine and MAOB inhibitors restore the levels to within the normal range.  </li></ul>
  24. 27. <ul><li>Interactions with Food/Tobacco/Alcohol </li></ul><ul><li>Caffeine </li></ul><ul><li>Dopamine Containing Food </li></ul><ul><li>Tyramine Containing Food </li></ul><ul><li>Side Effects </li></ul><ul><li>Chest pain (severe) </li></ul><ul><li>enlarged pupils </li></ul><ul><li>fast or slow heartbeat </li></ul><ul><li>headache (severe) </li></ul><ul><li>increased sensitivity of eyes to light </li></ul><ul><li>increased sweating (possibly with fever or cold, clammy skin) </li></ul><ul><li>nausea and vomiting </li></ul><ul><li>Dizziness or lightheadedness (severe), especially when getting up from a lying or sitting position. </li></ul><ul><li>More common(side effects) </li></ul><ul><li>Burred vision </li></ul><ul><li>decreased amount of urine </li></ul><ul><li>decreased sexual ability </li></ul><ul><li>dizziness or lightheadedness (mild), especially when getting up from a lying or sitting position </li></ul><ul><li>headache (mild) </li></ul><ul><li>increased appetite (especially for sweets) or weight gain </li></ul><ul><li>increased sweating </li></ul><ul><li>muscle twitching during sleep </li></ul><ul><li>tiredness and weakness </li></ul><ul><li>trouble in sleeping </li></ul>
  25. 28. <ul><li>Serotonin and norepinephrine reuptake inhibitors </li></ul><ul><li>Serotonin and nor epinephrine reuptake inhibitors (SNRIs) ease depression by affecting chemical messengers (neurotransmitters) used to communicate between brain cells. </li></ul><ul><li>Most antidepressants work by changing the levels of one or more of these naturally occurring brain chemicals. </li></ul><ul><li>SNRIs block the absorption (reuptake) of the neurotransmitters serotonin and nor epinephrine in the brain. </li></ul><ul><li>They also affect certain other neurotransmitters. </li></ul><ul><li>Changing the balance of these chemicals seems to help brain cells send and receive messages, which in turn boosts mood. </li></ul><ul><li>Medications in this group of antidepressants are sometimes called dual reuptake inhibitors. </li></ul>
  26. 29. <ul><li>Side effects and cautions </li></ul><ul><li>All SNRIs work in a similar way and generally cause similar side effects. </li></ul><ul><li>Side effects of SNRIs can include: </li></ul><ul><li>Nausea (particularly with duloxetine) </li></ul><ul><li>Dry mouth </li></ul><ul><li>Dizziness </li></ul><ul><li>Insomnia </li></ul><ul><li>Sleepiness </li></ul><ul><li>Constipation </li></ul><ul><li>Increased blood pressure (with venlafaxine) </li></ul><ul><li>Excessive sweating </li></ul><ul><li>Reduced sexual desire or difficulty reaching orgasm </li></ul><ul><li>Inability to maintain an erection (erectile dysfunction) </li></ul><ul><li>Increased heart rate </li></ul><ul><li>Heart palpitation </li></ul><ul><li>Difficulty urinating </li></ul><ul><li>Tremor </li></ul><ul><li>Headache </li></ul><ul><li>Agitation or anxiety </li></ul><ul><li>Changes in appetite </li></ul><ul><li>Abnormal vision, such as blurred vision or double vision </li></ul><ul><li>Muscle weakness </li></ul>
  27. 30. <ul><li>Safety concerns: </li></ul><ul><li>Antidepressants and pregnancy. </li></ul><ul><li>Drug interactions.  </li></ul><ul><li>Venlafaxine and blood pressure.  </li></ul><ul><li>Blood thinning medications and SNRIs. </li></ul><ul><li>Duloxetine and liver problems.  </li></ul><ul><li>Serotonin syndrome. </li></ul>
  28. 31. <ul><li>Atypical antidepressants </li></ul><ul><li>Atypical antidepressants ease depression by affecting chemical messengers (neurotransmitters) used to communicate between brain cells. </li></ul><ul><li>Most antidepressants work by changing the levels of one or more of these naturally occurring brain chemicals. </li></ul><ul><li>Like other types of antidepressants, atypical antidepressants affect neurotransmitters including dopamine, serotonin and norepinephrine. </li></ul><ul><li>Changing the balance of these chemicals seems to help brain cells send and receive messages, which in turn boosts mood. </li></ul>
  29. 32. Side effects. S.N. DRUGS Side effects 1 Bupropion Anxiety, restlessness or agitation, Confusion, Constipation, Dry mouth, Headache, Increased, irregular heartbeat, Insomnia, Nausea, Sore throat, Tremor. 2 Mirtazapine Constipation, Dizziness or lightheadedness, Dry mouth, Increased appetite, Increased cholesterol, Increased or decreased blood pressure, Low white blood cell count, Sleepiness, Weakness, Weight gain. 3 Nefazodone Blurred vision, Confusion, Constipation, Dizziness or lightheadedness, Dry mouth, Headache, Low blood pressure, Nausea, Sleepiness, Weakness. 4 Trazodone Sleepiness, Headache, Dry mouth, Dizziness or lightheadedness, Nausea, Fatigue, Diarrhea, Constipation, Insomnia, Low BP, Confusion, Blurred vision, Irregular heartbeat.
  30. 33. THANK You ALL

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