2

2 5 R A Z O N , R A Y M U N D G E R A R D D.
3K–PHARMACY
What are Tricyclic
Antidepressants?
 4

TRICYCLIC
ANTIDEPRESSANTS
ave a fused three-ring system of molecules
H of secondary and tertiary amine derivatives
ase depression by impacting chemical
messengers (neurotransmitters) used to
E communicate between brain cells
eplaced by antidepressant which cause few
side effects because this causes blurred vision,
R constipation, drowsiness, and urine retention
ther uses of TCAs are for the treatment of
O mood disorders, to reduce bed-wetting, to
manage OCDs and to prevent migraines
 The principal tricyclic antidepressants are derivatives of
diabenzazepine (Imipramine, Desipramine, Clomipramine,
Trimipramine) and dibenzocycloheptadiene (Amitryptyline,
Nortriptyline, Protriptyline)

Other closely related tricyclic antidepressants

include dopexin, a dibenzoxepine, and
amoxapine, a dibenzoxapine

A closely related tetracyclic agent is

TRICYCLIC maprotiline (Ludiomil)
ANTIDEPRESSANTS
 6

A. PRINCIPAL TRICYCLIC ANTIDEPRESSANTS

DERIVATIVES OF DIBENZAZEPINE AND DIBENZOCYCLOHEPTADIENE
as Imipramine (Tofranil)

CH2CH2CH2N(CH3)2
3-(10,11-dihydro-5H-dibenzo[bf]azepin-5-yl)-
N,N-dimethylpropan-1-amine
 Imipramine
Tofranil
A medication to treat depression may N
improve your mood, sleep, appetite, and
energy level and may help restore your CH2CH2CH2N(CH3)2
interest in daily living. Imipramine can help
your child control nighttime bed-wetting.
as Desipramine (Norpramine)

CH2CH2CH2NCH3
 Desipramine
Norpramin
This medication is used to treat depression. N
This medication may improve your mood,
sleep, appetite, and energy level and may CH2CH2CH2NHCH3
help restore your interest in daily living.
 DDIBENZAZEPINE DERIVATIVES

Imipramine (Tofranil) Desipramine (Norpramine)

N N

CH2CH2CH2N(CH3)2 CH2CH2CH2NHCH3
as Amitriptyline (Elavil)

CHCH2CH2N(CH3)2
3-(10,11-dihydro-5H-dibenzo[a,d]cycloheptene-
5-ylidene)-N,N-dimethylpropan-1-amine
 Amitriptyline
Elavil
This medication is used to treat mental/mood N
problems such as depression. It may help
improve mood and feelings of well-being, CHCH2CH2N(CH3)2
relieve anxiety and tension, help you sleep
better, and increase your energy level.
as Nortriptyline (Aventyl)

CHCH2CH2NHCH3
 Nortriptyline
Aventyl N
It affects chemicals in the brain that may
be unbalanced in people with CH2CH2CH2NHCH3
depression. Nortriptyline is used to treat
symptoms of depression.
 DDIBENZOCYCLOHEPTADIENE DERIVATIVES

Amitriptyline (Elavil) Nortriptyline (Aventyl)

N N

CHCH2CH2N(CH3)2 CHCH2CH2NHCH3
 19

B. CLOSELY RELATED TRICYCLIC ANTIDEPRESSANT

DIBENZOXIPINE AND DIBENZOXAPINE
 DOXEPIN 20

DIBENZOXEPINE

Doxepin affects chemicals in the brain that may

become unbalanced. It is used to treat symptoms of
depression and or anxiety associated
with alcoholism, psychiatric conditions, or manic-
depressive conditions.
 21

AMOXAPINE
DIBENZOXAPINE
Amoxapine affects chemicals in the brain that
may become unbalanced. Amoxapine is used to
treat symptoms of depression, anxiety,
or agitation.
 22

C. CLOSELY RELATED TETRACYCLIC AGENT

 23

MAPROTILINE
LUDIOMIL
Maprotiline affects chemicals in the brain that
may become unbalanced and cause depression.
Maprotiline is used to treat major
depressive disorder, depressive neurosis, and
manic-depression illness.
ATYPICAL
ANTIDEPRESSANTS
What are Atypical
Antidepressants?
ATYPICAL ANTIDEPRESSANT
• Have varied structures ranging from the
aminopropiophenone bupropion to the
complex heterocyclics trazodone and
nefazodone
• The chemically unrelated serotonin re-uptake
inhibitors fluoxetine, paroxetine, sertraline,
fluvoxamine, and venlafaxine
CONTENT TITLE
ATYPICAL
CONTENT TITLE ANTIDEPRESSANTS

TRAZODONE
Desyrel FLUOXETINE
Prozac

2-{3-[4-(3-chlorophenyl)piperazin-1- N-methyl-3-phenyl-[4-(trifluoromethyl)
yl]propyl}[1,2,4]triazolo[4,3-a]pyridine-3(2H)-one phenoxy]propan-1-amine
CONTENT TITLE
ATYPICAL
CONTENT TITLE ANTIDEPRESSANTS

TRAZODONE
Desyrel FLUOXETINE
Prozac

An antidepressant that increases serotonin activity

in the brain. Trazodone is used for depression, It is mainly used to treat major depression,
anxiety, sleep and pain. obsessive-compulsive disorder, and panic disorder.
 29

ANTIMANIC
ANTIDEPRESSANTS
 30

ANTIMANIC ANTIDEPRESSANTS

MOOD STABILIZERS
Lithium is an element that is used in the
form of the carbonate salt in the
treatment of manic depression or bipolar
disease. Other agents in the therapeutic
category include the organic compounds
valproic acid and carbamazepine.
 31

VALPROIC ACID
► This medication is used to treat certain
types of seizures (epilepsy).
► This medicine is an anticonvulsant that
works in the brain tissue to stop seizures.
► Valproic acid is also used to treat the
manic phase of bipolar disorder (manic-
depressive illness), and helps prevent
migraine headaches.
 32

CARBAMAZEPINE
► Carbamazepine is an anticonvulsant. It
works by decreasing nerve impulses that
cause seizures and pain.
► Carbamazepine is used to treat seizures
and nerve pain such as trigeminal
neuralgia and diabetic neuropathy.
► Carbamazepine is also used to treat
bipolar disorder.
 33

THERAPEUTIC INDICATIONS
Mechanismo of Action Inhibitors, Tricyclic and Atypical,
Lithium and Valproic Acid
Mechanism of Action
Inhibitors

 Are indicated to treat

depression, phobic anxiety, and
narcolepsy that have not
responded to other treatments
 However, their use is limited by
their adverse effects
Agents of choice for endogenous depression

Imipramine is used to treat enuresis

Clomipramine, Fluoxetine and

Fluvoxamine are used in obsessive
compulsive disorder;

Doxepin for anxiety

TRICYCLIC AND ATYPICAL

ANTIDEPRESSANTS
LITHIUM AND VALPROIC ACID

Treatment for manic

depression or bipolar disease

These also includes

Carbamazepine, an antiepileptic drug

has been used but is not approved as a
mood stabilizer in bipolar illness