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Clomipramine

Pharmacology

Antidepressant - Antiobsessional

Clomipramine is a tricyclic agent with both antidepressant and antiobsessional properties. Like other tricyclics, clomipramine inhibits norepinephrine and serotonin uptake into central nerve terminals, possibly by blocking the membrane-pump of neurons, thereby increasing the concentration of transmitter monoamines at receptor sites. Clomipramine is presumed to influence depression and obsessive and compulsive behaviour through its effects on serotonergic neurotransmission. The actual neurochemical mechanism is unknown, but clomipramine's capacity to inhibit serotonin reuptake is thought to be important. Clomipramine appears to have a mild sedative effect which may be helpful in alleviating the anxiety component often accompanying depression.

Absorption is rapid and complete after oral administration in man. The plasma half-life after a single oral dose is approximately 21 hours. 

Binding to serum proteins at 96 to 97% is very high. 

Clomipramine is extensively metabolized in the body with hydroxylation, demethylation and N-oxidation being the quantitatively more important routes of metabolism.

Owing to the lower clearance of clomipramine in plasma, elderly patients require lower doses of clomipramine than patients in younger age groups.

 


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