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ANTIDEPRESSANTS
Dr Thekiso
Classification
● 1. Tricyclic and tetracyclic antidepressants (TCA)
● 2. Selective serotonin reuptake inhibitors (SSRI)
● 3. Monoamine oxidase inhibitors (MAO inhibitors)
● 4. Selective serotonin -norepinephrine reuptake
inhibitors (SSNRI)
● 5. Dopamine norepinephrine reuptake inhibitors
(DNRI)
1. Tricyclic Antidepressants
● Drug
● Amitriptyline
● Clomipramine
● Desipramine
● Doxepin
● Imipramine
● Nortriptyline
● Dose Ranges
● 50-300mg/day
● 50-300mg/day
● 50-300mg/day
● 50-300mg/day
● 50-300mg/day
● 20-150mg/day
1. Tricyclic and tetracyclic
antidepressants
● Mechanism of action
● Block the reuptake of serotonin and norepinephrine
at presynaptic nerve ending
● Also block muscarinic, histaminic and alpha
adrenergic receptors
● Metabolized by liver and excreted through kidneys
● Drug levels are increased by drugs that inhibit the
cytochrome p450
1. Tricyclic and tetracyclic
antidepressants
● Indications
● Major depressive disorder
● Panic disorder
● Generalized anxiety disorder
● Post traumatic stress disorder
● Obsessive compulsive disorder
● Panic syndromes
1. Tricyclic and tetracyclic
antidepressants
Adverse Effects
● Peripheral:
● Anticholinergic effects: constipation, urinary
hesitancy, dry mouth and blurred vision
● Antihistaminic effects: sedation, weight gain
● Alpha adrenergic effects: orthostatic hypotension
and reflex tachycardia
● Cardiac effects:most worrisome : prolong QT
interval, flatten T waves, ST segment depression
may also increase premature ventricular contractions
1. TCA Continue
● Allergic and hematologic: Rashes,agranulocytosis,
leukopaenia and eosinophilia
● Central Effects:
● Tremors and lowering of seizure threshold
2. Monoamine oxidase inhibitors
● Drug
● Isocarboxazid
● Phenelzine
● tranylpromine
● Dose Ranges mg/day
● 10-50
● 15-90
● 20-90
2. Monoamine oxidase inhibitors
● Mechanism of action
● Monoamine oxidase is an enzyme which degrades
serotonin, dopamine, tyramine and norepinephrine
● Block this enzyme
● Two types of mono amine oxidase A and B
● MAO-A brain, liver , gut and sympathetic nerves
● MAO-B brain , liver and platelets
2. MAO inhibitors continued
● Indications
● Depression with anxiety symptoms
● Panic disorders
● Agoraphobia
● Social phobia PTSD
● Bulimia nervosa
● Atypical depression
2. MAO inhibitors continued
● Adverse effects
● Anticholinergic
● Antihistaminic
● Alpha adrenergic blockage
● Most worrisome is the ingestion of tyramine
containing food concomitantly which may
precipitate severe hypertensive crises
● Patients encouraged to avoid such foods
● Patients advised to seek immediate medical attention
when symptoms of crisis appear I.e headache,
2. MAO Inhibitors continue
● Can be treated with nefidipine 10mg tablet or
intravenous phentolamine
● The following foods should be avoided:
● Cheese, fish, meat, caviar, salami, sausages,
overripe or canned fruits,yeast extracts or fermented
products, chocolate, colas, tea, coffee, soya sauce,
beer, wine
● Drugs: OTC pain medication,cold and allergy med,
cough preparations, decongestants, inhalers,
stimulants, diet pills and SSRI
3. Selective serotonin reuptake
inhibitors
● Drug
● Citalopram
● Escitalopram
● Fluoxetine
● Fluvoxamine
● Paroxetine
● Sertraline
● Dose Ranges mg/day
● 10-60
● 10-30
● 20-80
● 100-300
● 20-50
● 50-200
3. Selective serotonin reuptake
inhibitors
● Mechanism of action
● Selectively inhibit the the reuptake of 5HT at
presynaptic neuron
● They lack the side effects of TCA caused by
blockage of muscarinic, alpha adrenergic and
histaminic
● Therefore they are the most widely prescribed
and better tolerated
3. SSRI Continued
● Indications
● Major depressive disorder
● Obsessive compulsive disorder
● Social anxiety disorder
● Panic disorder
● Generalized anxiety disorder
● Post traumatic stress disorder
3. SSRI Continued
● Premenstrual phosphoric syndrome
● Bulimia nervosa
3. SSRI Continued
● Adverse Effects
● Largely dose related
● Central
● Restlessness, anxiety, muscle tension, insomnia and
headache
● Sedation, vivid dreams
3. SSRI continued
● Peripherally
● GIT: loose bowel movements
● GUT: decrease libido, delay ejaculation and
anorgasmia
● Rare cases of serotonin syndrome reported when
patients take two or more drugs boosting serotonin
levels
● Presents with restlessness, lethargy, mental
confusion, flushing, sweating, tremors and
myoclonic jerks. Later develop hyperthermia,
hypertonicity, rhabdomyolysis, renal failure and
3. SSRI continued
● Inhibit cytochrome p450 isoenzyme therefore can
lead to increase in drugs metabolized by this system
● Safe to use in pregnancy but should be avoided in
breastfeeding
● May not be used concurrently with MAO inhibitors
4. Selective serotonin-nor epinephrine
reuptake inhibitors
● Drugs
● Venlafaxine
● Duloxetine
● Desvenlafaxine
● Dose Ranges mg/day
● 75-350
● 40-60
4. SNRI Continued
● Indications:
● Major depressive disorder
● Generalized anxiety disorder
● Social anxiety
● Panic disorders
● ADHD
● Dual diagnosis of cocaine dependence
4. SNRI continued
● Mechanism of action
● Potent inhibitors of serotonin and norepinephrine
reuptake
● No activity on other receptors
Adverse Effects
● Similar to SSRI
5. Dopamine norepinephrine reuptake
inhibitors
● Drug
● Bupropion
● Dose range mg/day
● 150-450
5. DNRI Continued
● Mechanism of action
● Inhibits the reuptake of dopamine and
norepinephrine
● Indications
● Major depressive disorder
● Smoke cessation
● ADHD
5. DNRI Continued
● Well tolerated
● Has minimal effects on weight gain, cardiac
conduction or sexual dysfunction
● Adverse Effects
● Central
● Headaches, anxiety, tremors, insomnia, sweating,
seizures at higher doses.
THANK YOU

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12. antidepressants

  • 2. Classification ● 1. Tricyclic and tetracyclic antidepressants (TCA) ● 2. Selective serotonin reuptake inhibitors (SSRI) ● 3. Monoamine oxidase inhibitors (MAO inhibitors) ● 4. Selective serotonin -norepinephrine reuptake inhibitors (SSNRI) ● 5. Dopamine norepinephrine reuptake inhibitors (DNRI)
  • 3. 1. Tricyclic Antidepressants ● Drug ● Amitriptyline ● Clomipramine ● Desipramine ● Doxepin ● Imipramine ● Nortriptyline ● Dose Ranges ● 50-300mg/day ● 50-300mg/day ● 50-300mg/day ● 50-300mg/day ● 50-300mg/day ● 20-150mg/day
  • 4. 1. Tricyclic and tetracyclic antidepressants ● Mechanism of action ● Block the reuptake of serotonin and norepinephrine at presynaptic nerve ending ● Also block muscarinic, histaminic and alpha adrenergic receptors ● Metabolized by liver and excreted through kidneys ● Drug levels are increased by drugs that inhibit the cytochrome p450
  • 5. 1. Tricyclic and tetracyclic antidepressants ● Indications ● Major depressive disorder ● Panic disorder ● Generalized anxiety disorder ● Post traumatic stress disorder ● Obsessive compulsive disorder ● Panic syndromes
  • 6. 1. Tricyclic and tetracyclic antidepressants Adverse Effects ● Peripheral: ● Anticholinergic effects: constipation, urinary hesitancy, dry mouth and blurred vision ● Antihistaminic effects: sedation, weight gain ● Alpha adrenergic effects: orthostatic hypotension and reflex tachycardia ● Cardiac effects:most worrisome : prolong QT interval, flatten T waves, ST segment depression may also increase premature ventricular contractions
  • 7. 1. TCA Continue ● Allergic and hematologic: Rashes,agranulocytosis, leukopaenia and eosinophilia ● Central Effects: ● Tremors and lowering of seizure threshold
  • 8. 2. Monoamine oxidase inhibitors ● Drug ● Isocarboxazid ● Phenelzine ● tranylpromine ● Dose Ranges mg/day ● 10-50 ● 15-90 ● 20-90
  • 9. 2. Monoamine oxidase inhibitors ● Mechanism of action ● Monoamine oxidase is an enzyme which degrades serotonin, dopamine, tyramine and norepinephrine ● Block this enzyme ● Two types of mono amine oxidase A and B ● MAO-A brain, liver , gut and sympathetic nerves ● MAO-B brain , liver and platelets
  • 10. 2. MAO inhibitors continued ● Indications ● Depression with anxiety symptoms ● Panic disorders ● Agoraphobia ● Social phobia PTSD ● Bulimia nervosa ● Atypical depression
  • 11. 2. MAO inhibitors continued ● Adverse effects ● Anticholinergic ● Antihistaminic ● Alpha adrenergic blockage ● Most worrisome is the ingestion of tyramine containing food concomitantly which may precipitate severe hypertensive crises ● Patients encouraged to avoid such foods ● Patients advised to seek immediate medical attention when symptoms of crisis appear I.e headache,
  • 12. 2. MAO Inhibitors continue ● Can be treated with nefidipine 10mg tablet or intravenous phentolamine ● The following foods should be avoided: ● Cheese, fish, meat, caviar, salami, sausages, overripe or canned fruits,yeast extracts or fermented products, chocolate, colas, tea, coffee, soya sauce, beer, wine ● Drugs: OTC pain medication,cold and allergy med, cough preparations, decongestants, inhalers, stimulants, diet pills and SSRI
  • 13. 3. Selective serotonin reuptake inhibitors ● Drug ● Citalopram ● Escitalopram ● Fluoxetine ● Fluvoxamine ● Paroxetine ● Sertraline ● Dose Ranges mg/day ● 10-60 ● 10-30 ● 20-80 ● 100-300 ● 20-50 ● 50-200
  • 14. 3. Selective serotonin reuptake inhibitors ● Mechanism of action ● Selectively inhibit the the reuptake of 5HT at presynaptic neuron ● They lack the side effects of TCA caused by blockage of muscarinic, alpha adrenergic and histaminic ● Therefore they are the most widely prescribed and better tolerated
  • 15. 3. SSRI Continued ● Indications ● Major depressive disorder ● Obsessive compulsive disorder ● Social anxiety disorder ● Panic disorder ● Generalized anxiety disorder ● Post traumatic stress disorder
  • 16. 3. SSRI Continued ● Premenstrual phosphoric syndrome ● Bulimia nervosa
  • 17. 3. SSRI Continued ● Adverse Effects ● Largely dose related ● Central ● Restlessness, anxiety, muscle tension, insomnia and headache ● Sedation, vivid dreams
  • 18. 3. SSRI continued ● Peripherally ● GIT: loose bowel movements ● GUT: decrease libido, delay ejaculation and anorgasmia ● Rare cases of serotonin syndrome reported when patients take two or more drugs boosting serotonin levels ● Presents with restlessness, lethargy, mental confusion, flushing, sweating, tremors and myoclonic jerks. Later develop hyperthermia, hypertonicity, rhabdomyolysis, renal failure and
  • 19. 3. SSRI continued ● Inhibit cytochrome p450 isoenzyme therefore can lead to increase in drugs metabolized by this system ● Safe to use in pregnancy but should be avoided in breastfeeding ● May not be used concurrently with MAO inhibitors
  • 20. 4. Selective serotonin-nor epinephrine reuptake inhibitors ● Drugs ● Venlafaxine ● Duloxetine ● Desvenlafaxine ● Dose Ranges mg/day ● 75-350 ● 40-60
  • 21. 4. SNRI Continued ● Indications: ● Major depressive disorder ● Generalized anxiety disorder ● Social anxiety ● Panic disorders ● ADHD ● Dual diagnosis of cocaine dependence
  • 22. 4. SNRI continued ● Mechanism of action ● Potent inhibitors of serotonin and norepinephrine reuptake ● No activity on other receptors Adverse Effects ● Similar to SSRI
  • 23. 5. Dopamine norepinephrine reuptake inhibitors ● Drug ● Bupropion ● Dose range mg/day ● 150-450
  • 24. 5. DNRI Continued ● Mechanism of action ● Inhibits the reuptake of dopamine and norepinephrine ● Indications ● Major depressive disorder ● Smoke cessation ● ADHD
  • 25. 5. DNRI Continued ● Well tolerated ● Has minimal effects on weight gain, cardiac conduction or sexual dysfunction ● Adverse Effects ● Central ● Headaches, anxiety, tremors, insomnia, sweating, seizures at higher doses.