ANTIDEPRESSANTS

INTRODUCTION:
Major depression is characterised by symptoms like sad mood, loss of interest and pleasure, low energy,
worthlessness, guilt, psychomotor retardation or agitation, change in appetite and /or sleep, melancholia,
suicidal thoughts etc. On the other hand pathological anxiety may lead to depression.

DEFINITION :
These are drugs which can elevate mood in depressive illnesses.

BASIC FUNCTION AND CLASSIFICATION :

Practically all antidepressants affect monoaminergic transmission in the brain in one way or the other. These
substances acts upon reuptake/metabolism of biogenic amines and on pre/post junctional aminergic/
cholinergic receptors , on the basis of which we can classify them as given below :
ANTIDEPRESSANTS

Reversible inhibitors of Tricyclic antidepressants Selective serotonin Atypical

MAO-A (RIMAs) (TCAs) Reuptake Inhibitor (SSRI) Antidepressants

MAO INHIBITORS :
MAO is an enzyme involved in the oxidative deamination of biogenic amines. These drugs functions by
inhibiting these enzymes.

INTERACTIONS :
The MAO inhibitors elevate the mood and in some cases it may progress into hypomania and mania.
These drugs may inhibit a no. of other enzymes also, and interacts with many other foods and drugs.
For eg. Cheese reactions(hypertensive crisis), cold and cough remedies, reserpine, TCA ,levodopa,
antiparkinsons, anticholinergics, barbiturates, alcohol, opioids, antihistamines, pethidine.

Due to these substances several reactions like HTN crisis, CVA, hallucinations, excitation, delirium
respiratory depression may occur in MAO inhibited patients.
ADVERSE EFFECTS :

Nausea, dizziness, headache, insomnia, rarely excitement and liver damage.

INTERACTIONS:

Caution is advised while prescribing SSRIs, TCAs, alcohol.

Can be given in mild to moderate depression, social phobia, and an tolerated alternative for TCAs.

TRICYCLIC AGENTS (TCAs):

It inhibited NA and 5-HT reuptake into neurons which is associated with antidepressant action. TCAs
inhibits monoamine reuptake and interact with a variety of receptors viz. 5-HT, and occasionally with
dopamine D2 that add to mood elevating action.
These have more limited spectrum of action.

E.g. of TCA is imipramine.

TCAs may cause dry mouth ,blurring vision, constipation, and urinary hesitancy. Effects on CVS may
be seen in therapeutic and overdoses. Tachycardia, postural hypotension, ECG changes and cardiac
arrhythmias.

TOLERENCE and DEPENDANCE:

– malaise, chills, muscle pain may occur on discontinuation.

PHARMACOKINETICS :

Oral absorption is good though often slow. they are extensively metabolised in liver. The half life of
these drugs ranges between 16-24 hours. These are mainly given at once daily at be time for daily
dose.50-200ng/ml act as therapeutic dose for antidepressants.

ADVERSE EFFECTS :

 Epigastric distress, urinary retention, blurred vision, palpitation, arrhythmias),

 sedation, mental confusion,
 increased appetite and weight gain, dysphoric agitated state or mania, sweating and fine tremors.
 Seizure, postural hypotension,
 Rashes and jaundice.
INTERACTIONS :

Dangerous when given with MAO inhibitors. Hypertensive crisis may occur.
TCAs delays gastric emptying and retard absorption of other drugs as well as of their own too.

TETRACYCLICS e.g. Amoxapine,

this compound blocks dopamine D2 receptors. Overdose may cause seizures, risk for EPS is also there.

REBOXETINE : This is selective NA reuptake blocker. It has fewer side effects and safer in overdose.

SELECTIVE SEROTONIN REUPTAKE INHIBITORS (SSRI):

Also used in anxiety ,phobias, OCD and related disorders like social phobias, PTSD. Other uses of
SSRIs are in body dysmorphic disorders. these substances selectively inhibit membrane associated
SERT. These have more tolerability both in therapeutic and overdose. Acts faster than others. Do not
interfere with cognitive and psychomotor function. Suitable for elderly. So, These are relatively safer
and better acceptable.

Prominent side effects are gastrointestinal ; nausea, but tolerance level develops after a time, can
interfere with orgasm and ejaculation. Restlessnes ,insomnia, anorexia, dyskinesia, headache, diarrhoea
is associated with mild side effects. Epistaxis and echhymosis may be reported.

SSRIs are preffered for prophylaxis of recurrent depression.

FLUOXETINE :
Bicyclic compound, with t1/2 of 2 days, slower onset of antidepressant effect. More appropriate for
poorly compliant patients. Can be given in children for depression and OCD.

Causes agitation and dermatological reactions.

FLUVOXAMINE :

Short acting SSRI with no active metabolite. relatively more nausea ,agitation, and discontinuation
reactions.
Most commonly used in hospitalized patients.

PAROXETINE :

Short acting SSRI does not produce active metabolites. G.I. side effects are observed after
discontinuation.
ATYPICAL ANTIDEPRESSANTS :

These drugs blocks 5-HT uptake and has prominent alpha blocking and weak 5-HT2 antagonist action.
Bradycardia, nausea, sedation, penile erection problems, may occur . it’s is safer in overdose.

MIANSERIN :

It blocks presynaptic alpha2 receptors and increase release of NA in brain which may be responsible for
antidepressant effect, have antagonistic action on 5-HT2,5-HT1C as well as on H1.

Use :
 sedative,
 relieves associated anxiety
 supresses panic attacks.

liver dysfunction are reported-which made its use restricted.

TIANEPTINE :
It increase 5-HT uptake, neither sedative nor stimulant.

AMINEPTINE:
It also increase serotonin uptake but has antidepressant property too. It produces anticholinergic side
effects too.

MIRTAZAPINE :
It blocks alpha2 auto-and hetero receptors enhancing both NA and 5-HT release.

BUPROPION : the inhibitor of DA and NA uptake.

USES OF ANTIDEPRESSANTS :

 Endogenous (major) depression

 Obsessive compulsive and phobic states
 Anxiety disorders
 Neuropathic pain
 ADHD
 Enuresis
 Migraine
 Pruritus
ROLE OF NURSE :
 Patient assessment
 Coordination of treatment modalities
 Psychopharmacological drug administration
 Monitoring drug effects
 medication education
 Drug maintainance programs
 Clinical research drug trials
 Prescriptive authority
 Documentation
 Promoting patient adherence