ANTIDEPRESSANT DRUGS

TRULY SITORUSDepart.Of Pharmacology & Therapy

Faculty Of Medicine – Padjadjaran University

ANTIDEPRESSANT DRUGSDEPRESSANTIs due to a deficiency of monoamine such as:

NOR EPINEPHRINESEROTONINEDOPAMINE

THE SYMPTOM OF DEPRESSANT:– Intense feelings of sadness– Hopelessness– Despair– Inability ti experience pleasure in usual activities

MANIACaused by an overproduction of MONOAMINE NEUROTRANSMITTERS

CLASIFICATIONI. TRICYCLIC/ POLYCYCLIC ANTIDEPRESSANT

1ST generation: AMITRIPTYLINE 2ND generation: AMOXAPINE

II. SELECTIVE SEROTONIN REUPTAKE INHIBITORS (SSRI) Fluoxetine

III. MONOAMINE OXIDASE INHIBITORS (MAO INHIBITORS)

Isocarboxazid

Drugs used to treat mania: LITHIUM SALTS

TCAIncrease the function of monoamine synapses by inhibiting reuptake of the neurotransmitter substances.

Pharmacokinetics

Relative receptor specificity of antidepressant drugs

Drug

UPTAKE INHIBITION RECEPTOR AFINITIESNorepinephrine Serotonin Muscarinic Histaminergic Adrenergic

Tricyclic antidepressant imipramide

++ +++ ++ - +

Selective serotonin reuptake inhibitor Fluoxetine

0 ++++ 0 0 0

INDICATION1. SEVERE MAJOR DEPRESSION2. PANIC DISORDERS3. CONTROL BED-WETTING IN CHILDREN (older

than 6 years)

ADVERSE EFFECTS• Antimuscarinic effects• Cardiovascular effects• Orthostatic hypotension• Sedation

DRUGS INTERACTIONPotentiate effects of biogenic amines drugs by preventing

Their removal from synaptic cleft

Direct actingAdrenergic

drugs

Tricyclicantidepressants

Indirect-actingAdrenergic

drugs

Block effects of Indirect-acting sympathomimetic drugs byPreventing the drugs from reaching their intraceluller sites of action

EthanolOther CNS depressants

Toxicsedation

MAOInhibitors

Mutual enhancement:Hypertension,hyperpyrexia,

convulsions, and coma

SSRISelectively inhibit serotonin reuptake by nerveEndings

– Antimuscarinic effects– Cardiotoxicity

DRUGS INTERACTION

INDICATION1. Depression2. Bulimia nervosa3. Obsessive – compulsive4. Anorexia nervosa5. Panic disorder6. PAIN associated with DIABETIC

NEUROPATHY7. Premenstrual syndrome

MAO INHIBITOR

Inactive the enzyme monoamine neurotransmitter

ISOCARBOXAZID

INDICATION1. Depressed patient – Unresponsive to TCA2. Allergic to TCA3. Strong anxiety4. Atypical depression CONTRAINDICATION1. Food: aged cheeses, chicken liver, beer, and

red wines (contain TYRAMINE)2. SRRI