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Overview on
pharmacological
management of
depression
By: ph. Abeer abd elrahman
What is depression?
•Depression is a state of low mood that
can affect a person's thoughts,
behavior, feelings, and sense of well-
being.
•It's caused mainly by deficiency in
some neurotransmitters in the brain or
more specifically in the synaptic cleft
like nor-epinephrine and serotonin.
Types of depression:
• A) major depression
• B) bipolar depression
mood episodes that range from extremes of high energy
with an "up" mood to low "depressive" periods.
Traditional antidepressants are not always recommended
as first-line treatments for bipolar depression
At the beginning we should know how
a nervous signal is transmitted
through nervous cells:
• Nervous action potential is transmitted from the
axon of one nerve cell to the dendrimers of the
next nerve cell via chemical signals mediated by
neurotransmitters such as nor-epinephrine,
serotonin and dopamine
• after doing their action by docking to receptors
of the next nerve cell they undergo two
processes:
a) Broken down by mono amine oxidase enzyme
b) Are reuptaken back into nerve cells
• So the idea of treating the deficiency of nor-
epinephrine and serotonin (depression) is by
acting on these two mechanisms
Major lines od pharmacological ttt
1) mono-amine-oxidase inhibitors
MAOI
• Monoamine oxidase inhibitors are drugs inhibiting the
action of mono-amine-oxidase enzyme (MAO) which is
responsible for the breakdown of nor-epinephrine and
serotonin so increase their amount and action in the
synaptic cleft
There are two forms of monoamine
oxidase enzyme
(MAO-A)
•tyramine
•norepinephrine
•serotonin
•dopamine
(MAO-B)
•dopamine
Examples for available MOAI in the
markets:
non-selective
MAOI
• Phenelzine
• Tranylcypromine
(Parnetil)
Selective MAO-A I
•No longer
commercially
available
Selective MAO-
B I
•Rasagiline
(parkintreat)
•Selegiline
(parkineast)
Atypical MAOIs:
• Linezolid (averzolid) is an antibiotic drug with weak
MAO-inhibiting activity.
• Methylene blue (provay blue), the antidote indicated
for drug-induced methemoglobinemia (hemoglobin that
contains the ferric [Fe3+] form of iron) is a highly
potent, reversible MAO inhibitor.
side effects of MOAI:
• it increases the level of many neurotransmiiters
1) Increase
sympathetic tone
(HTN,TACHYCARDI
A)
2) Atropine like
action
Hypertensive crisis
• The intake of non-selective MAOI Increases NE, EPI and
tyramine which are excitatory NT Alone not a big deal
• The problem happens with the intake of tyramine containing
food as aged cheese, smoked or proccessed meat
2) Tricyclic antidepressants (TCAs):
• They act by inhibiting reuptake of nor-epinephrine and
serotonin by blocking the transporters responsible for
reuptake of these neurotransmitters.
•This inhibition elevates the concentration
of neurotransmitters in the synapses and
triggers further neurotransmission.
• Tricyclic antidepressants are used to treat
depression, bipolar disorder, anxiety,
obsessive-compulsive disorder and other
mood disorders.
•They are also effective as analgesics so are
used to treat chronic pain and used for
migraine prophylaxis.
Examples for available TCAs :
• Anafranil generic name: clomipramine
• tryptizol generic name: amitriptyline
• Tofranil generic name: imipramine
• Main side effects: Urinary retention so it has off lable
use in treatment of nocturnal enuresis.
•
3) Selective serotonin reuptake
inhibitors(SSRI):
• Unlike TCA, SSRIs are believed to increase the
extracellular level of the serotonin specifically by
limiting its reabsorption into the presynaptic cell
Examples for SSRIs:
• Citalopram citalo, depram
• Escitalopram cipralex, citapronex
• Fluoxetine prozac, depreban
• Fluvoxamine faverin
• Paroxetine seroxat, cetralin
• Sertraline lustral, moodapex, deprestat
Cautions:
•Not recommended for bipolar depression.
•Not used less than 6 months
•Should be withdrawn gradually to avoid
withdrawal symptoms (rebound
depression).
•Withdrawal regimen is to decrease doses
each dose reduction for 2 weeks at least.
SSRIs
• Longest t1/2 (1week).
• For patients with problems with dose remembering.
• One of the safer SSRi for pregnant and breast feeding.
• Taken after meals due to gastric upsets
• The most rapidly absorbed SSRI so used in acute
depression.
• Highly tolerable and less interacting SSRI.
• Not for below 18 YO
• The active form of citalopram
• The most tolerable the most safe the least interacting.
• used for 12 YO and older
• FDA approved for obsessive compulsive disorder (OCD)
•
References:
• https://www.webmd.com/depression/guide/depression-
types#2-4
• https://www.researchgate.net/figure/Physiological-
functions-of-MAO-and-types-of-MAO-inhibitors-with-their-
drawbacks-and_fig2_279306450
• https://www.youtube.com/watch?v=pGEQILM7C7Y
• https://www.drugs.com/drug-class/tricyclic-
antidepressants.html
• http://www.mayoclinic.org/diseases-
conditions/depression/in-depth/maois/art-20043992
• https://www.youtube.com/watch?v=l8pObJTzRzY

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Overview on pharmacological management of depression

  • 2. What is depression? •Depression is a state of low mood that can affect a person's thoughts, behavior, feelings, and sense of well- being. •It's caused mainly by deficiency in some neurotransmitters in the brain or more specifically in the synaptic cleft like nor-epinephrine and serotonin.
  • 3. Types of depression: • A) major depression • B) bipolar depression mood episodes that range from extremes of high energy with an "up" mood to low "depressive" periods. Traditional antidepressants are not always recommended as first-line treatments for bipolar depression
  • 4. At the beginning we should know how a nervous signal is transmitted through nervous cells: • Nervous action potential is transmitted from the axon of one nerve cell to the dendrimers of the next nerve cell via chemical signals mediated by neurotransmitters such as nor-epinephrine, serotonin and dopamine
  • 5. • after doing their action by docking to receptors of the next nerve cell they undergo two processes: a) Broken down by mono amine oxidase enzyme b) Are reuptaken back into nerve cells • So the idea of treating the deficiency of nor- epinephrine and serotonin (depression) is by acting on these two mechanisms
  • 6. Major lines od pharmacological ttt
  • 7. 1) mono-amine-oxidase inhibitors MAOI • Monoamine oxidase inhibitors are drugs inhibiting the action of mono-amine-oxidase enzyme (MAO) which is responsible for the breakdown of nor-epinephrine and serotonin so increase their amount and action in the synaptic cleft
  • 8. There are two forms of monoamine oxidase enzyme (MAO-A) •tyramine •norepinephrine •serotonin •dopamine (MAO-B) •dopamine
  • 9. Examples for available MOAI in the markets: non-selective MAOI • Phenelzine • Tranylcypromine (Parnetil) Selective MAO-A I •No longer commercially available Selective MAO- B I •Rasagiline (parkintreat) •Selegiline (parkineast)
  • 10. Atypical MAOIs: • Linezolid (averzolid) is an antibiotic drug with weak MAO-inhibiting activity. • Methylene blue (provay blue), the antidote indicated for drug-induced methemoglobinemia (hemoglobin that contains the ferric [Fe3+] form of iron) is a highly potent, reversible MAO inhibitor.
  • 11. side effects of MOAI: • it increases the level of many neurotransmiiters 1) Increase sympathetic tone (HTN,TACHYCARDI A) 2) Atropine like action
  • 12. Hypertensive crisis • The intake of non-selective MAOI Increases NE, EPI and tyramine which are excitatory NT Alone not a big deal • The problem happens with the intake of tyramine containing food as aged cheese, smoked or proccessed meat
  • 13. 2) Tricyclic antidepressants (TCAs): • They act by inhibiting reuptake of nor-epinephrine and serotonin by blocking the transporters responsible for reuptake of these neurotransmitters.
  • 14. •This inhibition elevates the concentration of neurotransmitters in the synapses and triggers further neurotransmission. • Tricyclic antidepressants are used to treat depression, bipolar disorder, anxiety, obsessive-compulsive disorder and other mood disorders. •They are also effective as analgesics so are used to treat chronic pain and used for migraine prophylaxis.
  • 15. Examples for available TCAs : • Anafranil generic name: clomipramine • tryptizol generic name: amitriptyline • Tofranil generic name: imipramine • Main side effects: Urinary retention so it has off lable use in treatment of nocturnal enuresis. •
  • 16. 3) Selective serotonin reuptake inhibitors(SSRI): • Unlike TCA, SSRIs are believed to increase the extracellular level of the serotonin specifically by limiting its reabsorption into the presynaptic cell
  • 17. Examples for SSRIs: • Citalopram citalo, depram • Escitalopram cipralex, citapronex • Fluoxetine prozac, depreban • Fluvoxamine faverin • Paroxetine seroxat, cetralin • Sertraline lustral, moodapex, deprestat
  • 18. Cautions: •Not recommended for bipolar depression. •Not used less than 6 months •Should be withdrawn gradually to avoid withdrawal symptoms (rebound depression). •Withdrawal regimen is to decrease doses each dose reduction for 2 weeks at least.
  • 19. SSRIs • Longest t1/2 (1week). • For patients with problems with dose remembering.
  • 20. • One of the safer SSRi for pregnant and breast feeding. • Taken after meals due to gastric upsets
  • 21. • The most rapidly absorbed SSRI so used in acute depression.
  • 22. • Highly tolerable and less interacting SSRI. • Not for below 18 YO
  • 23. • The active form of citalopram • The most tolerable the most safe the least interacting. • used for 12 YO and older
  • 24. • FDA approved for obsessive compulsive disorder (OCD) •
  • 25.
  • 26. References: • https://www.webmd.com/depression/guide/depression- types#2-4 • https://www.researchgate.net/figure/Physiological- functions-of-MAO-and-types-of-MAO-inhibitors-with-their- drawbacks-and_fig2_279306450 • https://www.youtube.com/watch?v=pGEQILM7C7Y • https://www.drugs.com/drug-class/tricyclic- antidepressants.html • http://www.mayoclinic.org/diseases- conditions/depression/in-depth/maois/art-20043992 • https://www.youtube.com/watch?v=l8pObJTzRzY