Depression Symptoms Treatment

Drug Approvals

(British Approved Name, rINN)

Citalopram Hydrobromide

(British Approved Name Modified, rINNM)

Drug Nomenclature

Pharmacopoeias. In US.

The United States Pharmacopeia 31, 2008 (Citalopram Hydrobromide). A white to almost white, crystalline powder. Freely soluble in water, in alcohol, and in chloroform. A 0.5% solution in water has apH of 5.5 to 6.5.

Citalopram Hydrochloride

Drug Approvals

(British Approved Name Modified, rINNM)

Adverse Effects, Treatment, and Precautions

As for SSRIs in general (see Fluoxetine) although increased appetite and weight gain have also been reported with citalopram. Citalopram may be more cardiotoxic in overdosage than other SSRIs for further details.

Breast feeding. For comments on the use of SSRIs in breast feeding patients, see under Precautions for Fluoxetine.

Children. SSRIs are associated with an increased risk of potentially suicidal behaviour when used for the treatment of depression in children and adolescents under 18 years old for further details, see under Effects on Mental State in Fluoxetine.

Interactions

For interactions associated with SSRIs, see Fluoxetine.

Pharmacokinetics

Citalopram is readily absorbed from the gastrointestinal tract and maximum plasma concentrations are reached 2 to 4 hours after oral doses. Citalopram is widely distributed throughout the body protein binding is less than 80%. Citalopram is metabolised by demethylation, deamination, and oxidation to active and inactive metabolites. The demethylation of citalopram to one of its active metabolites, demethylcitalopram, involves the cytochrome P450 isoenzymes CYP3A4 and CYP2C19 the metabolism of citalopram is also partly dependent on CYP2D6. Didemeth-ylcitalopram has also been identified as a metabolite of citalopram. The elimination half-life of citalopram is reported to be about 36 hours. It is excreted mainly via the liver (85%) with the remainder via the kidneys. About 12% of the daily dose is excreted in the urine as unchanged drug. Citalopram is distributed into breast milk in very low concentrations (see Breast Feeding under Precautions in Fluoxetine).

Uses and Administration

Citalopram, a phthalane derivative, is an SSRI with actions and uses similar to those of fluoxetine. Citalopram is given orally as the hydrobromide or hydrochloride, usually as a single daily dose. Doses are expressed in terms of citalopram citalopram hydrobromide 25.0 mg and citalopram hydrochloride 22.3 mg are each equivalent to about 20.0 mg of citalopram.

In the treatment of depression, the initial dose (given as tablets or a liquid) is the equivalent of 20 mg daily by mouth. After at least one week, the dose may be increased to 40 mg daily a dose of 60 mg daily may be necessary in some patients. In the UK citalopram is also given as the hydrochloride in the form of concentrated oral drops containing the equivalent of 40 mg/mL of citalopram. The bioavailability of the drops is about 25% greater than that of the tablets and consequently daily doses appear to be lower: a 20-mg tablet dose is equivalent to a 16-mg (8 drops) dose of the concentrate. In some countries, citalopram hydrochloride has also been given by intravenous infusion in doses of 20 to 40 mg when the oral route is impracticable.

In the treatment of panic disorder with or without agoraphobia, the initial oral dose is 10 mg (or the equivalent as the concentrate) daily increasing to 20 mg daily after one week. The dose may be increased thereafter as required up to a maximum of 60 mg daily. In some countries citalopram is also used in the treatment of obsessive-compulsive disorder in doses similar to those used in depression (see above). A dose of 20 mg daily, up to a maximum of 40 mg (or their equivalents as the concentrate), should be used in elderly patients. For dosage in hepatic and renal impairment see below.

Citalopram should be withdrawn gradually to reduce the risk of withdrawal symptoms.

The S-enantiomer of citalopram, escitalopram is given for the treatment of depression and some anxiety disorders.

Administration in hepatic or renal impairment. Licensed drug information suggests that dosage of citalopram should be restricted to the lower end of the dose range in patients with hepatic impairment. A usual oral dose for depression in this group would be 20 mg daily although the dose may be increased up to 40 mg daily, if necessary.

There is no need for dose adjustment in mild to moderate renal impairment although information is lacking on appropriate dosage in severe impairment.

Anxiety disorders. Citalopram has been given in anxiety disorders including panic disorder, obsessive-compulsive disorder, post-traumatic stress disorder, and social anxiety disorder (see under Phobic Disorders.

Depression. As discussed, there is very little difference in efficacy between the different groups of antidepressant drugs. SSRIs such as citalopram are widely used as an alternative to the older tricyclics as they have fewer adverse effects and are safer in overdosage.

Pathological crying or laughing. Inappropriate or uncontrolled crying or laughing can occur in patients with lesions in certain areas of the brain. Attempts at treatment have mostly been with antidepressant drugs, including SSRIs. Favourable results with citalopram have been reported in a double-blind placebo-controlled study and in case reports.

Schizophrenia. The treatment of schizophrenia consists mainly of a combination of social therapy and antipsychotic drugs. Like other antidepressants, citalopram has been examined for its potential value as an adjuvant in schizophrenia. In a preliminary placebo-controlled study in 15 patients with chronic schizophrenia who exhibited signs of impulsive aggression, adding citalopram to existing antipsychotic therapy significantly reduced the frequency, but not the average severity, of aggressive incidents. In a subsequent study involving 90 patients, citalopram appeared to improve subjective well-being but had no clear effect onpsychopathological symptoms.

Sexual dysfunction. SSRIs have been tried in the treatment of premature ejaculation, but results with citalopram have been conflicting, see under Fluoxetine.

Preparations

The United States Pharmacopeia 31, 2008: Citalopram Tablets.

Proprietary Preparations

Argentina: Humorap Psiconor Seropram Zentius

Australia: Celapram Ciazil Cipramil Talam Talohexal

Austria: Apertiaf Cipram † Cital hexal † Citalon † Citalostad Citarcana Citor Eostar Pram Sepramf Seropram

Belgium: Cipramil

Brazil: Alcytam Cipramil Citta Denyl Prodmax

Canada: Celexa

Chile: Actipram Cimal Cipramil Cortran Finap Pramcil Prisma Semax Setronil Temperax Zebrak Zentius

Czech Republic: Apertiaf Apo-Cital Cerotor Cipram Cita Citalec Citalon Citaratio Dalsan Pram Sepramf Seropram Zyloram

Denmark: Akarin Cipramil Citadur Citaham

Finland: Cipramil Emocalf Sepram

France: Seropram

Germany: Cilex Cipramil Citadura CitaLich Citalo-Q Citalon Sepramf Serital

Hong Kong: Cipram Cital

Hungary: Citagen Citalodep Citalon Citalowin Citapram Dalsan Oropram Seropram Serotor Zyloram

India: Citadep Citopam

Indonesia: Cipram

Ireland: Ciprager Cipramil Ciprapine Ciprotan Citrol

Israel: Cipramil Recital

Italy: Elopram Felipram Feliximir Frimaind Kaidor Lampopram Marpram Percital Pramexyl Reap Seropram Verisan

Malaysia: Cipram

Mexico: Citox Seropram Xylorane

The Netherlands: Cipramil Ciprapine Lontax

Norway: Cipramil Desital

New Zealand: Celapram Cipramil

South Africa: Adco-Talomil Cilift Cipramil CitaloHexal Depramil Talomil

Singapore: Cipram

Spain: Citalvir Genprol Presar Prisdal Relapaz Seropram Somac

Sweden: Cipramil Citavie

Switzerland: Alutan Claropram Rudopram Seropram

Thailand: Cipram

Turkey: Cipram Citara Citol Citolap

UK: Cipramil

USA: Celexa

Venezuela: Seropram