Inostral ®
Sertraline (as
Hydrochloride)
Category:
Antidepressant,Antianxiety agent
Chemistry:
(1S-cis)-4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-N-methyl-1-naphthalenamine
hydrochloride. The empirical formula C17H17NCl2•HCl is represented by the
following structural formula:
Mechanism
of action / Pharmacokinetics:
Sertraline
is a potent and specific inhibitor of neuronal serotonin (5 HT) uptake in
vitro, which results in the potentiation of the effects of 5-HT in animals. It
has only very weak effects on norepinephrine and dopamine neuronal reuptake. In
accord with its selective inhibition of 5-HT uptake, sertraline does not
enhance catecholaminergic activity. Sertraline has no affinity for muscarinic
(cholinergic), serotonergic, dopaminergic, adrenergic, histaminergic, GABA or
benzodiazepine receptors.
Pharmacokinetics properties:
|
Absorption
|
Slow and consistent
|
|
Effect of food on absorption
|
Absorption rate is
increased with food
|
|
Distribution
|
20 L/Kg
|
|
Protein binding
|
Very high (98%)
|
|
Biotransformation
|
Undergoes extensive
first-pass metabolism in the liver.
|
|
Elimination Half life
|
Sertraline:24-26 hours
N-desmethylsertraline: 62-104
hours
|
|
Onset of action
|
2-4 weeks for antidepressant
and antipanic properties
|
|
Time to peak concentration
|
4.5 to 8.4 hours following administration of 50 to 200
mg of sertraline once daily for 14 days
|
|
Dialysis
|
Not effective
|
|
Elimination
|
Renal:
40 - 45% and 0.2 % as unchanged
Fecal:
40 – 45% including 12-14% as unchanged
|
Indications:
Sertraline
is indicated for the treatment of Major depressive episodes, Panic disorders,
with or without agoraphobia,Obsessive compulsive disorder (OCD) in adults and
paediatric patients aged 6-17 years.Also is indicated for treatment of Social anxiety disorder and Post traumatic stress disorder (PTSD)
Contraindications:
Sertraline is contraindicated in patients with:
-
Hypersensitivity to the
active substance or to any of the excipients
-
Concomitant treatment with
irreversible monoamine oxidase inhibitors (MAOIs) is contraindicated due to the
risk of serotonin syndrome with symptoms such as agitation, tremor and
hyperthermia.
-
Sertraline must not be
initiated for at least 14 days after discontinuation of treatment with an
irreversible MAOI. Sertraline must be discontinued for at least 7 days before
starting treatment with an irreversible MAOI .
-
Concomitant intake of
pimozide is contraindicated.
-
Do not use this medicine with
Grapefruit juice.
Warnings and precautions:
Use sertraline with caution in
below conditions:
-
Serotonin Syndrome (SS) or
Neuroleptic Malignant Syndrome (NMS)
-
QTc Prolongation/Torsade de
Pointes (TdP)
-
Activation of hypomania or
mania
-
Schizophrenia
-
Seizures
-
Suicide/suicidal
thoughts/suicide attempts or clinical worsening
-
Paediatric population
-
Abnormal
bleeding / Haemorrhage
-
Hyponatraemia
-
Akathisia/psychomotor restlessness
-
Hepatic impairment
-
Renal impairment
-
Use in elderly
-
Diabetes
-
Angle-Closure glaucoma
(Medicines.uk)
Pregnancy:
There
are no well controlled studies in pregnant women. If you think you might be
pregnant, or are planning to get pregnant, you must tell your doctor before you
take Sertraline Tablets.
Medicines.uk
Breast – Feeding:
Published
data concerning Sertraline levels in breast milk show that small quantities of
sertraline and its metabolite N-desmethylsertraline are excreted in milk.. If
you are breast-feeding or about to start breast-feeding you must tell your
doctor before taking Sertraline Tablets.
Medicines.uk
Drug Interactions
Sertraline may affect or be affected by other medicines
such as :
-
Drugs that Prolong the QT Interval
-
Lithium, Phenytoin, phenobarbital,
carbamazepine, St John´s Wort, rifampicin
, sumatriptan,Warfarin, digoxin, atenolol, cimetidine, ketoconazole,
itraconazole, voriconazole, clarithromycin, erythromycin, fluconazole,
verapamil and diltiazem, omeprazole, lansoprazole, pantoprazole, Drugs
affecting platelet, rabeprazole, fluoxetine, fluvoxamine
-
function (e.g. NSAIDs,
acetylsalicylic acid and ticlopidine)
-
Neuromuscular Blockers
-
Drugs metabolized by
Cytochrome P450
Medicine. uk
Adverse reactions:
Common adverse reactions may
include:
drowsiness,
tiredness, feeling anxious or agitated,indigestion, nausea,
diarrhea, loss of
appetite,sweating ,tremors or shaking, sleep
problems (insomnia),decreased sex drive, impotence,
or difficulty having an orgasm.
Call
your doctor at once if you have seizure (convulsions),blurred
vision,severe weakness,
feeling unsteady or manic episodes,
unusual risk-taking behavior, extreme happiness, being irritable or talkative.
Get emergency medical help if you
have signs of an allergic reaction(skin rash or hives), difficulty
breathing, swelling of your face, lips, tongue, or throat.
Overdosage:
Symptoms of overdose include
serotonin-mediated side-effects such as somnolence, gastrointestinal
disturbances (e.g. nausea and vomiting), tachycardia, tremor, agitation and
dizziness. Coma has been reported although less frequently.
Medicine .uk
Dosage and Administration:
Adults:
Depression
and Obsessive Compulsive Disorder: Initial dose is 50 mg/day. The daily dose
may be increased in 50 mg increments and at intervals of at least one week over
a period of weeks.
The
maximum recommended dose is 200 mg/day.
Panic disorder, Social anxiety disorder and
Post Traumatic Stress Disorder: Treatment should be started at 25 mg/day, and
increased to 50 mg/day after one week. The daily dose then may be increased in
50 mg increments over a period of weeks.
The
maximum recommended dose is 200 mg/day.
children
and adolescents: Sertraline must only be used to treat children and
adolescents suffering from OCD aged 6-17 years old.
Obsessive Compulsive Disorder (aged 6 to 12) :
The recommended starting dose is 25 mg daily. After one week, your doctor may
increase this to 50 mg daily.
The
maximum dose is 200 mg daily.
Adolescents
aged 13 to 17:The recommended starting dose is 50 mg daily.
The maximum dose is 200 mg daily.
Medicine
.uk
Storage:
Store below 30 and away from heat
& direct light.
How Supplied
Inostral
® (Sertraline) tablets
are available as 50 and 100 mg Sertraline (as Hydrochloride). There are
blisters of 10's in a box of 50.
Reference:
1- PDR 2016 2- USPDI 2007 3- Martindale 2017
4- Drug facts 2015