Sertraline is an antidepressant in a group of drugs called selective serotonin reuptake inhibitors (SSRIs). Sertraline affects chemicals in the brain that may become unbalanced and cause depression, panic, anxiety, or obsessive-compulsive symptoms. Until 2002, sertraline was only approved for use in adults ages 18 and over; that year, it was approved by the FDA for use in treating children aged 6 or older with severe obsessive-compulsive disorder (OCD).
Abstract
Sertraline is an antidepressant in a group of drugs called selective serotonin reuptake inhibitors (SSRIs). Sertraline affects chemicals in the brain that may become unbalanced and cause depression, panic, anxiety, or obsessive-compulsive symptoms.
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Brand Names
Zoloft,
Lustral
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Manufacturers
APOTEX CORP
ACTAVIS ELIZABE
WATSON LABS
NNOVIANT PHARMA
PLIVA, INC
CORE PHARMA
SOUTHWOOD PHARMA
NORTHSTAR RX LL
STAT RX USA
CARACO PHARMA
REENSTONE LLC
RANBAXY PHARMA
AUROBINDO PHARMA
PRESCRIPT PHARM
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History
The history of sertraline dates back to the early 1970s, when Pfizer chemist Reinhard Sarges invented a novel series of psychoactive compounds based on the structures of neuroleptics chlorprothixene and thiothixene. Further work on these compounds led to tametraline, a norepinephrine and weaker dopamine reuptake inhibitor. Development of tametraline was soon stopped because of undesired stimulant effects observed in animals. A few years later, in 1977, pharmacologist Kenneth Koe, after comparing the structural features of a variety of reuptake inhibitors, became interested in the tametraline series.
Until 2002, sertraline was only approved for use in adults ages 18 and over; that year, it was approved by the FDA for use in treating children aged 6 or older with severe obsessive-compulsive disorder (OCD). In 2003, the UK Medicines and Healthcare products Regulatory Agency issued a guidance that, apart from fluoxetine (Prozac), SSRIs are not suitable for the treatment of depression in patients under 18. However, sertraline can still be used in the UK for the treatment of OCD in children and adolescents. In 2005, the FDA added a black box warning concerning pediatric suicidal behavior to all antidepressants, including sertraline. In 2007, labeling was again changed to add a warning regarding suicidal behavior in young adults ages 18 to 24.
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Uses
Sertraline is used to treat depression, obsessive-compulsive disorder, panic disorder, anxiety disorders, post-traumatic stress disorder (PTSD), and premenstrual dysphoric disorder (PMDD).
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Pharmacology
Sertraline is absorbed slowly when taken orally, achieving its maximal concentration in the plasma 4–6 hours after ingestion. In the blood, it is 98.5% bound to plasma proteins. Its half-life in the body is 13–45 hours and, on average, is about 1.5 times longer in women (32 hours) than in men (22 hours), leading to a 1.5-times-higher exposure in women. According to in vitro studies, sertraline is metabolized by multiple cytochrome 450 isoforms: CYP2D6, CYP2C9, CYP2B6, CYP2C19 and CYP3A4. It appeared unlikely that inhibition of any single isoform could cause clinically significant changes in sertraline pharmacokinetics.No differences in sertraline pharmacokinetics were observed between people with high and low activity of CYP2D6;however, poor CYP2C19 metabolizers had a 1.5-times-higher level of sertraline than normal metabolizers.
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Schedule
It is not a controlled substance in the US.
Dosage
The dosage depends on the reason why it is prescribed for an individual. In general,
50 mg PO qDay
May increase by 25 mg at 1 week intervals to not more than 200 mg qDay.
6-12 years: 25 mg PO qDay initially
13-17 years: 50 mg PO qDay initially
The elderly are prone to SSRI/SNRI-induced hyponatremia, monitor closely.
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Drug Interactions
Contraindicated interactions with:
furazolidone
isocarboxazid
moclobemide
pargyline
phenelzine
pimozide
procarbazine
thioridazine
tranylcypromine
Serious interactions with:
amitriptyline
amoxapine
axitinib
buspirone
doxepin
duloxetine
escitalopram
fluoxetine
fluvoxamine
milnacipran
nefazodone
nortriptyline
ondansetron
paroxetine
venlafaxine
vilazodone
warfarin
Significant interactions with:
abiraterone
aceclofenac
acemetacin
carvedilol
celecoxib
diclofenac
diflunisal
dihydroergotamine
hydrocodone
hydromorphone
ibuprofen
methamphetamine
metoprolol
mibefradil
mifepristone
tolmetin
tramadol
valdecoxib
zolmitriptan
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Adverse Effects
Nausea (20-25%)
Headache (20-25%)
Insomnia (20-25%)
Ejaculation disorder (10-15%)
Dizziness (10-15%)
Dry mouth (10-15%)
Fatigue (10-15%)
Somnolence (10-15%)
Agitation (5-10%)
Anorexia (5-10%)
Constipation (5-10%)
Dyspepsia (5-10%)
Decreased libido (5-10%)
Sweating (5-10%)
Tremor (5-10%)
Vomiting (4%)
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Contraindications
Hypersensitivity
Concomitant MAOIs & other strong serotonergic drugs: risk of serotonin syndrome
Allow at least 14 d after stopping before starting one or the other
Do not use disulfiram concomitantly with oral soln due to EtOH in preparation
Concomitant pimozide: Risk of long QT Syndrome.
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Cautions
Risks of: hyponatremia; abnormal bleeding; impairment of cognitive/motor functions
Pregnancy: Conflicting evidence regarding use of SSRIs during pregnancy and increased risk of persistent pulmonary hypertension of the newborn (see Pregnancy)
In neonates exposed to SNRIs/SSRIs late in third trimester: risk of complications such as feeding difficulties, irritability, and respiratory problems
Avoid abrupt withdrawal
Coadministration with other drugs which enhance the effects of serotonergic neurotransmission (eg, tryptophan, fenfluramine, fentanyl, 5-HT agonists, St. John’s Wort) should be undertaken with caution and avoided whenever possible due to the potential for pharmacodynamic interaction
May cause false-positive urine immunoassay screening tests for benzodiazepines.
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Pricing
The pricing varies depending on what form one would like to buy, and the brand.
The 25mg tablet is priced in between $0.50 to $7.12. The price for 50mg tablet vary from
$0.50 to $9.39. The 100mg tablet would cost in the range of $4.34 to $15.96. The prices of other
dosage may vary from $0.50 to $11.19.
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Referenecs
[1] http://reference.medscape.com/drug/zoloft-sertraline-342962#90
[2] http://www.drugs.com/sertraline.html
[3] http://pubs.acs.org/doi/abs/10.1021/jm00267a010
[4] http://dmd.aspetjournals.org/content/33/2/262
[5] http://reference.medscape.com/drug/zoloft-sertraline-342962#13
[6] http://reference.medscape.com/drug/zoloft-sertraline-342962#3
[7] http://reference.medscape.com/drug/zoloft-sertraline-342962#4
[8] http://reference.medscape.com/drug/paxil-paxil-cr-paroxetine-342959#5
