Antidepressant Drugs

Major depressive
disorder ,
or
endogenous depression ,
is a

depression of mood without

any
obvious medical / situational
causes
.
manifested by an
inability to
cope
with
ordinary
events or
experience pleasure .

Major depression ui characterized

by symptoms like :

iii Sad mood * is

change
in Appetite
Liii loss
of Interest & Pleasure *in
change in
sleep
iii , low viii, Melancholia
energy (

in worthlessness in suicidal thoughts .

( v1 Guilt etc .

serotonin
"

Depression results due to decreased Monoamine (

rgic
°

5 HT - &

N A)
activity in Brain .

Norad
1

renaline

activity
-

So their called
•

Drugs increasing are

Typical Anti-depressants .

other mechanism
•

Drugs acting by Atypical Anti -

depressa
-
nts .

A- mine Hypothesis :

Drugs like Reserpine depletes ME ,

547 , DA and cause

depression
severe .

•
Acute mechanism of Antidepressants : 9 ME .
I 5Mt

takes
•
However , antidepressant effect several weeks to occur .
 A. Typical Antidepressants

Drugs may increase monoamine

rgic
transmission
by
•

inhibiting the
reuptake or metabolism
of 5- me or NA -

(1)
Tricyclic Antidepressants ( TCAs )

Drugs Amitriptyline imipramine and

clomipramine
•
-

, ,

blockade Reuptake
•
Mechanism :
Nonspecific of
5Mt & ME

↳ This results increased concentration these

in
of
transmitters in
synaptic cleft .
 Uses

(a)
Major depressions
states
(b) Phobic and
panic anxiety
(c)
Obsessive-compulsive disorders ( o CDs )

(d) Neuropathic pain

(e) Enuresis

Toxicity
3C 's Convulsions and cardio
( ) coma
toxicity
-

.
.

Drug interactions :

Hypertensive crisis with MAO Inhibitors .

-
Serotonin
syndrome with SSRIs
,
MAO Inhibitors and

meperidine
Prevent
antihypertensive action
of ✗
Agonists
-
.

a
(2) Selective Serotonin
Reuptake Inhibitors ( SSRIs)
Fluoxetine
Drugs -

.
paroxetine .
sertraline ,
citalopram ,

flu v0 ✗ amine

Mechanism Selective Blockade of Reuptake

•

:
5 HT .

•
Uses

(a) Major Depression

(b) OCD

(c) Bulimia

(d) disorder
Anxiety
(e) Premenstrual dysphoric
disorder ( PMDD )
side Effects :

Anxiety
•

Agitation
• Bruxism

•
Sexual
dysfunction
• lnlt Loss .

Toxicity Serotonin Syndrome

-
A 5 HT : serotonin
syndrome
-

Symptoms -

Sweating Rigidity
. ,
Myoclonus .
Seizures .

AMS instability . Hyperthermia .

 (3) MAO Inhibitors :

oxidase
Two
types of Monoamine
enzymes ( B)
•

MAO -

A &

involved metabolism
are
in
of monoamine .

A
predominantly
MAO
metabolizes and DA and
-

MA ,
5- HT

in
present in Intestine ,
peripheral Nerve
endings &

Leiser .

preferentially metabolism
MAO -
B
Dopamine and in
present
in brain , platelets and liver .

[ A)
Non selective MAO Inhibitors
Tranydypromine
-

Isocarboxazid .

Inhibits both
isoform Phenelzine
•

of MAO
irreversibly .

These anti -

depressants effect takes 3-4 weeks to develop .

•
These
drugs exhibit a
large
number
of drug and
food
interactions .

Important ones :
' a ' cheese
Reaction .

(b) Seno tonic

syndrome .
[ B) Reversible Inhibitors (
of MAO -
A RIMA )

Moclebemide inhibits MAO A

selectively and
Reversibly
-

• As it is Reversible & Short

Action .
it does not

exhibit cheese reaction with foods .

be used alternative treatment

•
It can as an to TCAs for
of depression .

[ c] Selective MAO -
B Inhibitors :

inhibits and
•

Selegi line MAO -

B in
useful in

Parkinsonism .

☐ It in available as Transdermal patch for treatment

of depression .
 Atypical Antidepressants
in Trazodone : Prominent ✗ blocker and weaker 5- HE

antagonist .

Associated with Cardiac

•

Arrhythmias
and
priapism
.

121
Venlafaxine :
Nonselective Reuptake blocker devoid of
ANS side
effects
(3)
Bupropion : Inhibits uptake of NA &
DA -

Fewer side
effects
Used cessation
in
smoking
.

(4) Mirtazapine : ✗
a
Antagonist ,
associated with wt -

gain
-

T important Drugs
-
:
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. .

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