Psychotropic Agents 103SELECTIVE SEROTONIN
REUPTAKE INHIBITORSSelective serotonin reuptake inhibitors
(SSRI) are currently used group of drug in
treatment of depression. These have a faster
onset of action and are better tolerated.
SERTRALINE
Sertraline is a potent and selective inhibi-
tor of neuronal serotonin (5-HT) reuptake.
It has only a weak effect on neuronal up-
take of norepinephrine and dopamine.
Sertraline’s inhibition of serotonin reuptake
enhances serotonergic transmission.
It has a wide therapeutic index and can
be administered in elderly patients and
those with underlying cardiovascular dis-
orders.
Adverse effects include nausea, head-
ache, diarrhoea, insomnia, dry mouth,
tremor and fatigue.
It is indicated for the treatment of symp-
toms of depressive illness including accom-
panying symptoms of anxiety. It is also in-
dicated in preventing relapse of the initial
episode of depression or recurrence of fur-
ther depressive episodes including accom-
panying symptoms of anxiety.
It is indicated in the treatment of obses-
sions and compulsions in patients with ob-
sessive compulsive disorder.
It is also indicated for the treatment
of panic disorder with or without agorapho-
bia.
CITALOPRAM
It is orally active SSRI. The mechanism
of action is due to potentiation of serotoner-
gic activity in the CNS resulting from its in-
hibition of CNS neuronal reuptake of sero-
tonin (5-HT).
Following a single oral dose of
citalopram, peak blood levels occur at about
four hours.
Adverse effects include activation of
mania/hypomania, dizziness, insomnia,
agitation, nausea and vomiting, dry mouth,
diarrhoea, tachycardia, postural hypoten-
sion, cardiac failure, MI, arthralgia, myal-
gia, arthritis, purpura, anaemia, leukocyto-
sis, decreased or increased weight, thirst,
ejaculation disorder, impotence, dysmenor-
rhoea, decreased or increased libido, cough-
ing, epistaxis, bronchitis, rash, pruritus, pho-
tosensitivity reaction, urticaria, acne, abnor-
mal accommodation, conjunctivitis, eye
pain, fatigue and fever.
It is indicated in the treatment of depres-
sion.PAROXETINE
It is an orally administered SSRI.
Paroxetine is readily absorbed from the
GIT with peak plasma concentration occur-
ring within about five hours. It is widely
distributed throughout body tissues and is
about 95% bound to plasma proteins. Excre-
tion is via the urine and the faeces, mainly
as metabolites.
Adverse effects include asthenia, sweat-
ing, nausea, decreased appetite, somno-
lence, dizziness, insomnia, tremor, nervous-
ness, constipation, ejaculatory disturbance
and impotence.
It is indicated in the treatment of depres-
sion, obsessive compulsive disorder and
panic disorder.