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Citalopram Pharmacodynamics and Mechanism of action

Introduction
A furancarbonitrile that is one of the serotonin uptake inhibitors used as an antidepressant. The drug is also effective in reducing ethanol uptake in alcoholics and is used in depressed patients who also suffer from tardive dyskinesia in preference to tricyclic antidepressants, which aggravate this condition

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 (alpha1, alpha2, beta), 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.

Side Effect of Citalopram
Call your doctor at once if you have any of these serious side effects:
    very stiff (rigid) muscles, high fever, sweating, fast or uneven heartbeats, tremors, overactive reflexes;
    nausea, vomiting, diarrhea, loss of appetite, feeling unsteady, loss of coordination; or
    headache, trouble concentrating, memory problems, weakness, confusion, hallucinations, fainting, seizure, shallow breathing or breathing that stops.

Less serious citalopram side effects may include:
  •     Drowsiness;
  •     Sleep problems (insomnia);
  •     Mild nausea, gas, upset stomach;
  •     Weight changes;
  •     Urinating more than usual;
  •     Decreased sex drive, impotence, or difficulty having an orgasm;
  •     Dry or watery mouth, yawning; or
  •     Cold symptoms such as stuffy nose, sneezing, sore throat.

Interaction of Citalopram
Citalopram (HBr) is known to interact with other drugs like Alcohol, Cimetidine (HCl), Iproniazid Phosphate, Methotrimeprazine (Maleate), Methylamphetamine, Naratriptan, Paregoric, Phenelzine, Sumatriptan, Trimeprazine (Tartrate).These interactions are sometimes beneficial and sometimes may pose threats to life. Always consult your physician for the change of dose regimen or an alternative drug of choice that may strictly be required.

Half Life of Citalopram
35 hours

Dosge of Citalopram 
 Adults: Depression:
Initial: 20 mg/day, generally with an increase to 40 mg/day; doses of more than 40 mg are not usually necessary. Should a dose increase be necessary, it should occur in 20 mg increments at intervals of no less than 1 week. Maximum dose: 60 mg/day; reduce dosage in elderly or those with hepatic impairment.
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Ditulis oleh: Unknown - Sunday, 24 April 2011