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Citalopram | apollo +9191 46 950 950
Citalopram | apollo +9191 46 950 950
Citalopram
CAS Number : 59729-33-8
Molecular Weight : 324.39 g/mol
Molecular Formula : C20H21FN2O
Systematic (IUPAC) : 1-[3-(dimethylamino)propyl]-1
-(4-fluorophenyl)-1,3-dihydro-2-benzofuran-5-carbonitrile
Type : small molecule
Description
Citalopram hydrobromide belongs to a class of antidepressant agents known as selective serotonin-
reuptake inhibitors (SSRIs). Despite distinct structural differences between compounds in this class, SSRIs
possess similar pharmacological activity. As with other antidepressant agents, several weeks of therapy may be required before a clinical effect is seen. SSRIs are potent
inhibitors of neuronal serotonin reuptake. They have little to no effect on norepinephrine or dopamine
reuptake and do not antagonize α- or β-adrenergic, dopamine D2 or histamine H1 receptors. During acute
use, SSRIs block serotonin reuptake and increase serotonin stimulation of somatodendritic 5-HT1A and
terminal autoreceptors. Chronic use leads to desensitization of somatodendritic 5-HT1A and terminal
autoreceptors. The overall clinical effect of increased mood and decreased anxiety is thought to be due to adaptive changes in neuronal function that leads to
enhanced serotonergic neurotransmission. Side effects include dry mouth, nausea, dizziness, drowsiness, sexual
dysfunction and headache. Side effects generally occur within the first two weeks of therapy and are usually less
severe and frequent than those observed with tricyclic antidepressants. Citalopram is approved for treatment
of depression. Unlabeled indications include mild dementia-associated agitation in nonpsychotic patients, smoking cessation, ethanol abuse, obsessive-compulsive
disorder (OCD) in children, and diabetic neuropathy. Citalopram has the fewest drug-drug interactions of the
SSRIs.
Categories
Antidepressants
Selective Serotonin Reuptake Inhibitors (SSRIs)
Serotonin Uptake Inhibitors
Taxonomy
Kingdom : Organic
Classes
Benzofurans
Benzyl Alcohols and Derivatives
Nitriles and Derivatives
Substructures
Benzofurans
Benzyl Alcohols and Derivatives
Nitriles and Derivatives
Ethers
Benzene and Derivatives
Cyanides
Aliphatic and Aryl Amines
Halobenzenes
Heterocyclic compounds
Aromatic compounds
Aryl Halides
Pharmacology
Indication : For the treatment of depression.
Unlabeled indications include: treatment of mild dementia-associated agitation in nonpsychotic patients, smoking cessation, ethanol abuse, obsessive-compulsive
disorder (OCD) in children, and diabetic neuropathy.
Pharmacodynamics : Citalopram is one of a class of antidepressants known as selective serotonin reuptake
inhibitors (SSRIs). It is used to treat the depression associated with mood disorders. It is also used on
occassion in the treatment of body dysmorphic disorder and anxiety. The antidepressant, antiobsessive-
compulsive, and antibulimic actions of citalopram are presumed to be linked to its inhibition of CNS neuronal
uptake of serotonin. In vitro studies show that citalopram is a potent and selective inhibitor of neuronal
serotonin reuptake and has only very weak effects on norepinephrine and dopamine neuronal reuptake.
Citalopram has no significant affinity for adrenergic (α1, α2, β), cholinergic, GABA, dopaminergic, histaminergic, serotonergic (5HT1A, 5HT1B, 5HT2), or benzodiazepine
receptors; antagonism of such receptors has been hypothesized to be associated with various
anticholinergic, sedative, and cardiovascular effects for other psychotropic drugs. The chronic administration of
citalopram was found to downregulate brain norepinephrine receptors, as has been observed with
other drugs effective in the treatment of major depressive disorder. Citalopram does not inhibit
monoamine oxidase.
Mechanism of action : The antidepressant,
antiobsessive-compulsive, and antibulimic actions of citalopram are presumed to be linked to its inhibition of
CNS neuronal uptake of serotonin. Citalopram blocks the reuptake of serotonin at the serotonin reuptake
pump of the neuronal membrane, enhancing the actions of serotonin on 5HT1A autoreceptors. SSRIs bind with
significantly less affinity to histamine, acetylcholine, and
norepinephrine receptors than tricyclic antidepressant drugs.
Absorption : Rapidly and well absorbed from the GI
tract. Peak plasma concentrations occur within 4 hours of a single orally administered dose. Bioavailability is
80% following oral administration. Food does not affect absorption.
Volume of distribution : 12 L/kg
Citalopram is highly lipophilic and likely widely distributed throughout the body.
Protein binding : 80% based on in vitro studies.
Metabolism : Citalopram is metabolized mainly in the
liver via N-demethylation to its principle metabolite, demethylcitalopram. Other metabolites include
didemethylcitalopram, citalopram N-oxide, and a deaminated propionic acid derivative. Cytochrome P450 (CYP) 3A4 and 2C19 isozymes appear to be principally
involved in producing demethylcitalopram. Demethylcitalopram appears to be further N-
demethylated by CYP2D6 to didemethylcitalopram. Citalopram metabolites possess little pharmacologic
activity in comparison to their parent compound and do not likely contribute to the clinical effect of the drug.
Route of elimination : The systemic clearance of
citalopram was 330 mL/min, with approximately 20% of that due to renal clearance. Citalopram is metabolized to
demethylcitalopram (DCT), didemethylcitalopram
(DDCT), citalopram-N-oxide, and a deaminated propionic acid derivative.
Half life : 35 hours
Toxicity : Symptoms most often accompanying
citalopram overdose, alone or in combination with other drugs and/or alcohol, included dizziness, sweating, nausea, vomiting, tremor, somnolence, and sinus
tachycardia. In more rare cases, observed symptoms included amnesia, confusion, coma, convulsions,
hyperventilation, cyanosis, rhabdomyolysis, and ECG changes (including QTc prolongation, nodal rhythm,
ventricular arrhythmia, and very rare cases of torsade de pointes). Acute renal failure has been very rarely
reported accompanying overdose. Withdrawal symptoms include flu-like symptoms, insomnia, nausea,
imbalance, sensory changes and hyperactivity.
Affected organisms : Humans and other mammals
What is citalopram?
Citalopram is an antidepressant in a group of drugs called selective serotonin reuptake inhibitors (SSRIs). It
affects chemicals in the brain that may become unbalanced and cause depression.
Citalopram is used to treat depression.
Citalopram may also be used for purposes not listed in this medication guide.
Drug Class And Mechanisms
Citalopram is an antidepressant medication that affects neurotransmitters, the chemicals that nerves within the
brain use to communicate with each other. Neurotransmitters are manufactured and released by nerves and then travel and attach to nearby nerves.
Thus, neurotransmitters can be thought of as the communication system of the brain. Many experts
believe that an imbalance among neurotransmitters is the cause of depression. Citalopram works by preventing the uptake of one neurotransmitter, serotonin, by nerve
cells after it has been released. Since uptake is an important mechanism for removing released
neurotransmitters and terminating their actions on adjacent nerves, the reduced uptake caused by
citalopram results in more free serotonin in the brain to stimulate nerve cells. Citalopram is in the class of drugs called selective serotonin reuptake inhibitors (SSRIs), a class that also contains fluoxetine (Prozac), paroxetine
(Paxil) and sertraline (Zoloft). Citalopram was approved by the FDA in July 1998.
Dosing
The usual starting dose is 20 mg in the morning or evening. The dose may be increased to 40 mg daily after
one week. A dose of 60 mg has not been shown to be more effective than 40 mg. As with all antidepressants, it
may take several weeks of treatment before maximum effects are seen. Doses are often slowly adjusted
upwards to find the most effective dose.
Drug interactions
All SSRIs, including citalopram, should not be taken with any of the mono-amine oxidase (MAO) inhibitor-
class of antidepressants, for example, isocarboxazid (Marplan), phenelzine (Nardil), tranylcypromine (Parnate), selegiline (Eldepryl), and procarbazine
(Matulane). Such combinations may lead to confusion, high blood pressure, tremor, and hyperactivity. If
treatment is to be changed from citalopram to an MAOI or vice-versa, there should be a 14 day period without
either drug before the alternative drug is started. Tryptophan, a common dietary supplement, can cause headaches, nausea, sweating, and dizziness when taken
with any SSRI.
Side Effects
The most common side effects associated with citalopram are nausea, dry mouth, vomiting, excessive
sweating, headache, tremor, drowsiness, and inability to sleep. Overall, between 1 in 6 and 1 in 5 persons
experience a side effect. Citalopram is also associated with sexual dysfunction. Some patients may experience
withdrawal reactions upon stopping citalopram. Symptoms of withdrawal include dizziness, tingling
sensations, tiredness, vivid dreams, and irritability or poor mood.
Antidepressants increased the risk of suicidal thinking and behavior (suicidality) in short-term studies in
children and adolescents with depression and other psychiatric disorders. Anyone considering the use of citalopram or any other antidepressant in a child or
adolescent must balance this risk with the clinical need. Patients who are started on therapy should be closely
observed for clinical worsening, suicidality, or unusual changes in behavior.
Warning
Antidepressant medications are used to treat a variety of conditions, including depression and other
mental/mood disorders. These medications can help prevent suicidal thoughts/attempts and provide other
important benefits. However, studies have shown that a small number of people (especially people younger than
25) who take antidepressants for any condition may experience worsening depression, other mental/mood symptoms, or suicidal thoughts/attempts. Therefore, it is very important to talk with the doctor about the risks
and benefits of antidepressant medication (especially for people younger than 25), even if treatment is not for a
mental/mood condition.
Tell the doctor immediately if you notice worsening depression/other psychiatric conditions, unusual
behavior changes (including possible suicidal thoughts/attempts), or other mental/mood changes
(including new/worsening anxiety, panic attacks, trouble sleeping, irritability, hostile/angry feelings,
impulsive actions, severe restlessness, very rapid speech). Be especially watchful for these symptoms
when a new antidepressant is started or when the dose is changed.
Uses
Citalopram is an antidepressant (selective serotonin reuptake inhibitor-SSRI) used to treat depression. It
works by restoring the balance of certain natural substances (neurotransmitters such as serotonin) in the
brain. Citalopram may improve your feelings of well-being and energy level.OTHER This section contains uses of this drug that are not listed in the approved
professional labeling for the drug but that may be prescribed by your health care professional. Use this
drug for a condition that is listed in this section only if it has been so prescribed by your health care
professional.This drug is also used to treat other mental conditions (obsessive-compulsive disorder, panic
disorder).
How To Use?
Read the Medication Guide provided by your pharmacist before you start using citalopram and each time you get a refill. If you have any questions, consult your doctor or
pharmacist.Take this medication once daily in the morning or evening, with or without food or as directed
by your doctor. The dosage is based on your medical condition and response to treatment. If you are using the
liquid form of this medication, measure the dose carefully using a special measuring device/spoon. Do not
use a household spoon because you may not get the correct dose.To reduce your risk of side effects, your
doctor may direct you to start taking this drug at a low dose and gradually increase your dose. Follow your
doctor's instructions carefully. Do not take more or less medication or take it more frequently than prescribed.
Your condition will not improve any faster, and your risk of side effects will increase. Use this medication
regularly in order to get the most benefit from it. To help you remember, use it at the same time each day.It is
important to continue taking this medication even if you feel well. Do not stop taking this medication without
consulting your doctor. Some conditions may become worse when the drug is suddenly stopped. Your dose may need to be gradually decreased.This medication
may cause withdrawal reactions, especially if it has been used regularly for a long time or in high doses. In such
cases, withdrawal symptoms (such as nervousness, headache, numbness, tingling, trouble sleeping,
nightmares) may occur if you suddenly stop using this medication. To prevent withdrawal reactions, your
doctor may reduce your dose gradually. Consult your doctor or pharmacist for more details, and report any withdrawal reactions immediately.It may take 1 to 2
weeks to feel a benefit from this drug and 4 weeks to feel the full benefit of this medication. Tell your doctor if
your condition persists or worsens.
Important information about citalopram
Do not take citalopram together with pimozide (Orap), linezolid (Zyvox), or a monoamine oxidase inhibitor
(MAOI) such as furazolidone (Furoxone), isocarboxazid (Marplan), phenelzine (Nardil), rasagiline (Azilect),
selegiline (Eldepryl, Emsam, Zelapar), or tranylcypromine (Parnate).
Before you take citalopram, tell your doctor if you have seizures or epilepsy, a bleeding disorder, liver or kidney disease, bipolar disorder, heart disease, a heart rhythm disorder, recent history of heart attack, or a history of
drug abuse or suicidal thoughts.
Treatments for depression are getting better everyday and there are things you can start doing right away.
You may have thoughts about suicide when you first start taking an antidepressant such as citalopram,
especially if you are younger than 24 years old. Your doctor will need to check you at regular visits for at least
the first 12 weeks of treatment.
Report any new or worsening symptoms to your doctor, such as: mood or behavior changes, anxiety, panic attacks, trouble sleeping, or if you feel impulsive,
irritable, agitated, hostile, aggressive, restless, hyperactive (mentally or physically), more depressed, or
have thoughts about suicide or hurting yourself.
Tell your doctor right away if you become pregnant while taking this medication. Citalopram may cause
heart defects or serious lung problems in a newborn if you take the medication during pregnancy. However,
you may have a relapse of depression if you stop taking your antidepressant. Do not start or stop taking
citalopram during pregnancy without your doctor's advice.
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