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Presented by:
Zafreen chaudary
Definition of Depression
 “An affective disorder
characterized by loss of
interest or pleasure in
almost all a person’s
usual activities or
pastimes.”
Symptoms Associated With
Depression
 Sadness, Despair, Guilt,
Pessimism
 Decrease in energy
 Decrease in sex drive
 Insomnia and fatigue
 Thoughts of death and
suicide
 Mental slowing, lack of
concentration
Treatment of Depression
 Antidepressant Pharmacology
 First introduced 40 years ago
 Also used for treatment of other disorders
including:
Anxiety disorders, dysthymia, chronic pain and
behavioral problems
Treatment
 Evolution of drug therapy
 Antidepressants discovered accidentally while investigating
antipsychotic efficacy of modifications of phenothiazines
 Imipramine - first antidepressant discovered
 Around the same time, monoamine oxidase inhibitors were
identified
 Late 1980’s- SSRI’s were developed
 Now working on other antidepressant treatments
Serotonin - Specific
Reuptake Inhibitors
(SSRI’s) Available for the past 15 years
 Allows for more serotonin to be available to
stimulate postsynaptic receptors
 Available to treat depression, anxiety
disorders, ADHD, obesity, alcohol abuse,
childhood anxiety, etc.
Citalopram
 Citalopram (Celexa) – well
absorbed orally, few drug
interactions, treats major
depression, social phobia,
panic disorder and OCD its
side effects are as follow:
 drowsiness, tired feeling;
 sleep problems (insomnia);
 mild nausea, diarrhea,
upset stomach, dry mouth;
 cold symptoms such as
stuffy nose, sneezing,
sore throat, cough;
 increased sweating or
urination, weight
changes; or.
 decreased sex drive,
impotence, or difficulty
having an orgasm.
Escitalopram
 It prevents the reuptake of one
neurotransmitter, serotonin, an action which
results in more serotonin in the brain to attach
to receptors.The FDA approved escitalopram
in August 2002. But it has some side effects
drowsiness, dizziness; sleep problems
(insomnia);mild nausea, gas, heartburn, upset
stomach, constipation; weight changes;
decreased sex drive, impotence, or difficulty
having an orgasm; or. dry mouth, yawning,
ringing in your ears
Fluoxetine
 Fluoxetine (Prozac) – first
SSRI available, long half
life, slow onset of action,
can cause sexual
dysfunction, anxiety,
insomnia and agitation
 Fluvoxamine (Luvox) –
structural derivative of
Prozac, became available
for OCD, also treats PTSD,
dysphoria, panic disorder,
and social phobia
SSRI’s
 Paroxetine (Paxil) – third SSRI available, more selective
than Prozac, highly effective in reducing anxiety and
posttraumatic stress disorder (PTSD) as well as OCD,
panic disorder, social phobia, premenstrual dysphoric
disorder, and chronic headache
 Sertraline (Zoloft) – second SSRI approved, low risk of
toxicity, few interactions, more selective and potent than
Prozac
SSRI’s
 Serotonin syndrome
 At high doses or combined with other drugs an exaggerated
response can occur
 This is due to increased amounts of serotonin
 Alters cognitive function, autonomic function and
neuromuscular function
 Potentially fatal
 Serotonin withdrawal syndrome
 With discontinuation of any SSRI onset of withdrawal symptoms
occur within a few days and can persist 3-4 weeks
 Symptoms: disequilibrium, gastrointestinal problems, flu-like
symptoms, sensory disturbances, sleep disturbances
SEROTONIN/NOREPINEPHRINE REUPTAKTE
INHIBITORS SNRIs
 SNRIs may be effective in
treating depression in patient
in whom SSRIs are ineffective
 Depression is often
accompanied by chronic
painful symptoms such as,
backache, and muscle ache.
Both SNRIs andTCAs with
their dual inhibition of both
serotonin and norepinephrine
reuptake are effective in
relieving such pains.
VENLAFAXINE
 Venlafaxine (VEN-la-fax-
een) is potent inhibitor of
serotonin reuptake.
 The most common side
effects of venlafaxine are
nausea, headache, sexual
dysfunction, dizziness,
insomnia, sedation and
constipation.
 High doses may be
increase blood pressure
and heart rate.
DULOXETINE
 Duloxetine (doo-LOX-
e-teen) inhibit
serotonin and
norepinephrine
reuptake at all doses.
 G1 side effects are
common with
duloxetine.
 Overdose may increase
blood pressure and
heart rate.
LEVONMILNAXCIPRAN
 Levonmilnacipran (leevo-mil-NA-si-pran)
use for treatment of depression and its
side effects are same as the other SNRIs.
Second Generation
(Atypical) Antidepressants
 Developed in the late 1970’s and 1980’s
 Bupropion – selectively inhibits Dopamine reuptake,
used for ADHD, side effects include: anxiety, restlessness,
tremors, and insomnia
 Mirtazapine- it enhances serotonin and norepinephrine
neurotransmitter. Mirtazapine is used to treat Major
depressive disorder, side effect includes: Dizziness,
Drowsiness ,Dry Mouth, Feeling Weak, High Cholesterol,
Incomplete or Infrequent Bowel Movements, Increased
hunger, Weight Gain.
Trazodone
 Trazodone probably improves symptoms of depression
by inhibiting the uptake of serotonin by nerves in the
brain. This results in more serotonin to stimulate other
nerves. Trazodone also may increase directly the action
of serotonin.
 Side effects including: Headache, Muscle ache, Nausea,
vomiting, loss of appetite, or stomachache.Constipation
or diarrhea, Loss of interest in sex (erectile dysfunction in
men) Dizziness or loss of balance, Dry mouth or dry eyes,
Numbness, burning, or tingling sensations.
 It will not cause of weight gain.
Tricyclic Antidepressants
 Effectively relieve depression with anxiolytic (used to
reduce anxiety) and analgesic action
(a remedy that relieves pain)
 First choice for treatment of depression
 Pharmacological properties
 Block presynaptic norepinephrine reuptake transporter
 Block presynaptic serotonine reuptake transporter
 Block postsynaptic histamine receptors
 Block postsynaptic acytalcholine receptors
Imipramine and
Amitriptyline
 Prototypical Tricyclic Antidepressants
 Desipramine (Norpramin) –
pharmacologically active intermediate
metabolite of imipramine (tofranil)
 Nortriptyline (Pamelor) – an active
intermediate metabolite of amitriptyline
(elavil)
Clinical Limitations of
Tricyclic Antidepressants
 Slow onset of action
 Wide variety of effects on CNS (adverse side effects):
 Can directly impair attention, motor speed, dexterity
(learning skills), and memory
 Cardiotoxic and potentially fatal in overdoses
Pharmacological Effects of
Tricyclic Antidepressants
 In CNS: blocks presynaptic serotonin, norepinephrine
receptors
 Blocking of Acetylcholine receptors leads to dry mouth,
confusion, blurry vision and mental confusion
 Blocking of histamine receptors leads to drowsiness and
sedation
 Effects on the Peripheral nervous system include: cardiac
depression, increased electrical irritability, can be life
threatening with over dosages
THANK
YOU

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anti depressant drugs

  • 2. Definition of Depression  “An affective disorder characterized by loss of interest or pleasure in almost all a person’s usual activities or pastimes.”
  • 3. Symptoms Associated With Depression  Sadness, Despair, Guilt, Pessimism  Decrease in energy  Decrease in sex drive  Insomnia and fatigue  Thoughts of death and suicide  Mental slowing, lack of concentration
  • 4. Treatment of Depression  Antidepressant Pharmacology  First introduced 40 years ago  Also used for treatment of other disorders including: Anxiety disorders, dysthymia, chronic pain and behavioral problems
  • 5. Treatment  Evolution of drug therapy  Antidepressants discovered accidentally while investigating antipsychotic efficacy of modifications of phenothiazines  Imipramine - first antidepressant discovered  Around the same time, monoamine oxidase inhibitors were identified  Late 1980’s- SSRI’s were developed  Now working on other antidepressant treatments
  • 6. Serotonin - Specific Reuptake Inhibitors (SSRI’s) Available for the past 15 years  Allows for more serotonin to be available to stimulate postsynaptic receptors  Available to treat depression, anxiety disorders, ADHD, obesity, alcohol abuse, childhood anxiety, etc.
  • 7. Citalopram  Citalopram (Celexa) – well absorbed orally, few drug interactions, treats major depression, social phobia, panic disorder and OCD its side effects are as follow:  drowsiness, tired feeling;  sleep problems (insomnia);  mild nausea, diarrhea, upset stomach, dry mouth;
  • 8.  cold symptoms such as stuffy nose, sneezing, sore throat, cough;  increased sweating or urination, weight changes; or.  decreased sex drive, impotence, or difficulty having an orgasm.
  • 9. Escitalopram  It prevents the reuptake of one neurotransmitter, serotonin, an action which results in more serotonin in the brain to attach to receptors.The FDA approved escitalopram in August 2002. But it has some side effects drowsiness, dizziness; sleep problems (insomnia);mild nausea, gas, heartburn, upset stomach, constipation; weight changes; decreased sex drive, impotence, or difficulty having an orgasm; or. dry mouth, yawning, ringing in your ears
  • 10. Fluoxetine  Fluoxetine (Prozac) – first SSRI available, long half life, slow onset of action, can cause sexual dysfunction, anxiety, insomnia and agitation  Fluvoxamine (Luvox) – structural derivative of Prozac, became available for OCD, also treats PTSD, dysphoria, panic disorder, and social phobia
  • 11. SSRI’s  Paroxetine (Paxil) – third SSRI available, more selective than Prozac, highly effective in reducing anxiety and posttraumatic stress disorder (PTSD) as well as OCD, panic disorder, social phobia, premenstrual dysphoric disorder, and chronic headache  Sertraline (Zoloft) – second SSRI approved, low risk of toxicity, few interactions, more selective and potent than Prozac
  • 12. SSRI’s  Serotonin syndrome  At high doses or combined with other drugs an exaggerated response can occur  This is due to increased amounts of serotonin  Alters cognitive function, autonomic function and neuromuscular function  Potentially fatal  Serotonin withdrawal syndrome  With discontinuation of any SSRI onset of withdrawal symptoms occur within a few days and can persist 3-4 weeks  Symptoms: disequilibrium, gastrointestinal problems, flu-like symptoms, sensory disturbances, sleep disturbances
  • 13. SEROTONIN/NOREPINEPHRINE REUPTAKTE INHIBITORS SNRIs  SNRIs may be effective in treating depression in patient in whom SSRIs are ineffective  Depression is often accompanied by chronic painful symptoms such as, backache, and muscle ache. Both SNRIs andTCAs with their dual inhibition of both serotonin and norepinephrine reuptake are effective in relieving such pains.
  • 14. VENLAFAXINE  Venlafaxine (VEN-la-fax- een) is potent inhibitor of serotonin reuptake.  The most common side effects of venlafaxine are nausea, headache, sexual dysfunction, dizziness, insomnia, sedation and constipation.  High doses may be increase blood pressure and heart rate.
  • 15. DULOXETINE  Duloxetine (doo-LOX- e-teen) inhibit serotonin and norepinephrine reuptake at all doses.  G1 side effects are common with duloxetine.  Overdose may increase blood pressure and heart rate.
  • 16. LEVONMILNAXCIPRAN  Levonmilnacipran (leevo-mil-NA-si-pran) use for treatment of depression and its side effects are same as the other SNRIs.
  • 17. Second Generation (Atypical) Antidepressants  Developed in the late 1970’s and 1980’s  Bupropion – selectively inhibits Dopamine reuptake, used for ADHD, side effects include: anxiety, restlessness, tremors, and insomnia  Mirtazapine- it enhances serotonin and norepinephrine neurotransmitter. Mirtazapine is used to treat Major depressive disorder, side effect includes: Dizziness, Drowsiness ,Dry Mouth, Feeling Weak, High Cholesterol, Incomplete or Infrequent Bowel Movements, Increased hunger, Weight Gain.
  • 18. Trazodone  Trazodone probably improves symptoms of depression by inhibiting the uptake of serotonin by nerves in the brain. This results in more serotonin to stimulate other nerves. Trazodone also may increase directly the action of serotonin.  Side effects including: Headache, Muscle ache, Nausea, vomiting, loss of appetite, or stomachache.Constipation or diarrhea, Loss of interest in sex (erectile dysfunction in men) Dizziness or loss of balance, Dry mouth or dry eyes, Numbness, burning, or tingling sensations.  It will not cause of weight gain.
  • 19. Tricyclic Antidepressants  Effectively relieve depression with anxiolytic (used to reduce anxiety) and analgesic action (a remedy that relieves pain)  First choice for treatment of depression  Pharmacological properties  Block presynaptic norepinephrine reuptake transporter  Block presynaptic serotonine reuptake transporter  Block postsynaptic histamine receptors  Block postsynaptic acytalcholine receptors
  • 20.
  • 21. Imipramine and Amitriptyline  Prototypical Tricyclic Antidepressants  Desipramine (Norpramin) – pharmacologically active intermediate metabolite of imipramine (tofranil)  Nortriptyline (Pamelor) – an active intermediate metabolite of amitriptyline (elavil)
  • 22. Clinical Limitations of Tricyclic Antidepressants  Slow onset of action  Wide variety of effects on CNS (adverse side effects):  Can directly impair attention, motor speed, dexterity (learning skills), and memory  Cardiotoxic and potentially fatal in overdoses
  • 23. Pharmacological Effects of Tricyclic Antidepressants  In CNS: blocks presynaptic serotonin, norepinephrine receptors  Blocking of Acetylcholine receptors leads to dry mouth, confusion, blurry vision and mental confusion  Blocking of histamine receptors leads to drowsiness and sedation  Effects on the Peripheral nervous system include: cardiac depression, increased electrical irritability, can be life threatening with over dosages