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Antidepressants
Antidepressants
Antidepressants
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Antidepressant Drugs
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Mania
Mania is characterized by the opposite behavior
that is
1. enthusiasm
2. rapid thought and speech patterns
3. extreme self confidence
4. and impaired judgment.
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grief, grandiosity,
flight of ideas,
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Mechanism of action
Although antidepressant drugs may cause
changes in brain amine activity within hours,
weeks may be required for them to achieve
clinical effects!!!!
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Drug categories
Class drugs
TCA Imipramine, Amitriptyline, Cloimpramine,
Doxepin, Trimpramine
Heterocyclic Desipramine, Nortriptyline, Amoxapine,
Maprotiline, Portriptyline
5-HT/NE RIs Venlafaxine, Duloxetine
Atypical Bupropion, Mirtazapine Nefazodone,
Trazodone
SSRIs Fluoxetine, Citalopram, Escitalopram,
Fluvoxamine, Paroxetine, Sertraline
MAOIs Phenelzine, Moclobemide, Isocarboxazid,
Tranylcypromine
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Classification:
*SSRI:
1. fluoxetine
2. citalopram
3. paroxetine
4. sertraline
5. Fluvoxamine
*5-HT/NE RI:
1. venlafaxine
2. duloxetine
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Classification:
*atypical antidepressants :
1. bupropion
2. mirtazapine
3. nefazodone
4. trazodon
*monoamine oxidase inhibitors (MAOIs):
1. phenelzine
2. Moclobemide
3. isocarboxazide
4. tranylcypromine
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Chemical Classification:
*cyclic antidepressants:
Tricyclic (TCA)
1. Imipramine
2. Amitryptiline
3. Clomipramine
4. Doxepin
5. trimipramine
Heterocyclic
1. Desipramine
2. Nortriptylinr
3. Amoxapine
4. Maproltiline
5. protriptylline
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Actions
They typically take 2 to 12 weeks to
produce improvement in mood
SSRI have little ability to block the
dopamine transporter.
SSRI have little blocking activity at
muscarinic, α-adrenergic, and
histaminic H1 receptors (fewer side
effects).
They are well tolerated by
patients with heart disease
the elderly, who are especially sensitive
to the anticholinergic and orthostatic
effects of the TCA.
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1. Depression.
2. Obsessive compulsive disorder (the only indication
for fluvoxamine ).
3. Panic disorder .
4. Generalized anxiety .
5. Premenstrual dysphoric disorder .
6. Bulimia nervosa .
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Pharmacokinetics
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Adverse affects :
With initiation of therapy with an SSRI, some
patients describe anxiety or agitation.
Insomnia
Paroxetine and fluvoxamine are sedating,
and may be useful in patients who have
difficulty sleeping.
Conversely, patients who are fatigued may
benefit from one of the more activating
antidepressants, such as fluoxetine.
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Adverse effects
Sexual dysfunction: loss of libido, delayed
ejaculation, and anorgasmia.
replace the offending antidepressant with a drug
having fewer sexual side effects, such as Bupropion
or mirtazapine.
The SSRIs tend to be weight neutral with the
exception of paroxetine (Paxil), which is associated
with weight gain.
Use in children and teenagers: 1/50 children
become more suicidal as a result of SSRIs
treatment.
Serotonin syndrome
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Serotonin syndrome
muscle rigidity,
myoclonus
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Venlafaxine
1. Venlafaxine: Is a potent inhibitor of serotonin
reuptake and, at higher doses, is an inhibitor of NE
reuptake. It is also a mild inhibitor of dopamine
reuptake.
It has minimal inhibition of the CYP P450
isoenzymes. The t1/2 of the parent compounds plus
its active metabolite is approximately 11 hours.
SE: nausea, dizziness, insomnia, sedation, and
constipation. At high doses, there may be an
increase in blood pressure..
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Duloxetine
2. duloxetine :inhibits serotonin and NE
reuptake at all doses.
3. It is extensively metabolized in the liver to
numerous metabolites, should not be
administered to patients with hepatic
insufficiency. Metabolites are excreted in
the urine.
4. Food delays the absorption of the drug. t1/2
is ~12 hours.
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nausea,
dry mouth,
and constipation are common.
Insomnia,
dizziness,
somnolence,
sweating.
Sexual dysfunction also occurs.
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Atypical antidepressants
They are a mixed group of agents that have actions at
several different sites.
1. Bupropion:
Acts at unidentified site. It has minimal effects on NE
or 5-HT systems, but blocks DA reuptake.
Its short half-life may require more than once-a-day
dosing or the administration of an extended release
formulation, it decreases the craving of nicotine in
tobacco abusers.
Side effects include: dry mouth ,sweating ,tremor and
seizures at high doses.
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2. Mirtazapine:
block 5-HT2 and α2 receptors.
It is a sedative because of its potent
antihistaminic activity, which may be used to
advantage in depressed patients having
difficulty sleeping,
but it does not cause the antimuscarinic SEs
of TCAs,
Does not interfere with sexual functioning, as
do the SSRIs.
Increased appetite and weight gain frequently
occur.
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Mechanism of action:
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Therapeutic uses
Sever major depression,
phobic and panic anxiety disorders,
Neuropathic pain,
obsessive compulsive disorder (OCD),
nocturnal enuresis; Imipramine has been
used to control bed-wetting in children (older
than six years) by causing contraction of the
internal sphincter of the bladder.
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Adverse effects:
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Adverse effects
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Therapeutic uses
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Adverse effects
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Mechanism of action:
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Adverse effects
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