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 23,468 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Citalopram is an antidepressant belonging to a new class of drugs which enhance serotoninergic neurotransmission through potent and selective inhibition of serotonin reuptake. Preliminary trials suggest that its short term therapeutic efficacy is significantly greater than that of placebo and mianserin, and comparable to that of amitriptyline, maprotiline and imipramine. It appears to be a weaker antidepressant agent than clomipramine, but better tolerated. Its elimination half-life of 33 hours permits once daily oral administration. Symptomatic improvement obtained with short term treatment has been maintained when therapy has been extended for up to 1 year; in the few patients studied for this extended period, the relapse rate was lower than with fluvoxamine, fluoxetine or imipramine. Compared to standard antidepressant agents, citalopram is well tolerated. It does not appear to be cardiotoxic, has not been associated with seizures in humans, and is relatively nonsedating. Unlike the tricyclic antidepressants, citalopram has minimal anticholinergic effects. Mild and transient nausea, with or without vomiting, is the most frequent adverse effect--occurring in 20% of patients--and increased perspiration, headache, dry mouth, tremor and insomnia are experienced by 15 to 18% of patients. Citalopram thus offers similar therapeutic efficacy and a more favourable tolerability profile than the tricyclic antidepressants. Preliminary data suggest that it may be particularly useful in patients who cannot tolerate the anticholinergic or cardiovascular side effects of tricyclic antidepressants and in those for whom sedation is not indicated.
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PMID:Citalopram. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic potential in depressive illness. 171 47

Citalopram, a selective 5-HT uptake inhibitor with antidepressant properties, was assessed in three studies in 12 healthy subjects using a battery of EEG, psychological, subjective and symptomatic measures. Study A involved the administration of citalopram, 20 mg and 40 mg, amitriptyline 50 mg and placebo in single dose using a balanced cross-over design. The test battery was applied before, and 1 and 3 h after each drug. Citalopram decreased slow-wave EEG activity whereas amitriptyline increased power in most EEG wavebands. Citalopram increased tapping rate and symbol copying whereas amitriptyline impaired these and other psychomotor tasks. Subjectively, amitriptyline was much more sedative than citalopram and produced more complaints of dry mouth. Study B comprised the administration of citalopram in the usual clinical dose of 40 mg, amitriptyline in the low clinical dose of 75 mg and placebo, each given for 9 nights using a balanced cross-over design. The test battery was applied on the first morning (pre-drug) and on the morning after the last nightly dose. None of the physiological tests showed any drug effects. Subjectively, citalopram was associated with feelings of shaking, nausea, loss of appetite and physical tiredness; amitriptyline produced feelings of shaking, nausea, loss of appetite, dryness of mouth, irritability, dizziness and indigestion; in general, amitriptyline effects were more marked than those of citalopram. Plasma samples were taken on the last day and plasma concentrations of both drugs and their metabolites were found to be in the expected range for the regimens used.(ABSTRACT TRUNCATED AT 250 WORDS)
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PMID:The effects of citalopram in single and repeated doses and with alcohol on physiological and psychological measures in healthy subjects. 346 75

Inhibitors of serotonin (5HT) re-uptake have generally been successful in inducing modest but statistically significant weight reductions in clinical trials. Citalopram is a new, highly selective inhibitor of 5HT re-uptake. It is effective and safe in relieving major depression at doses up to 60 mg daily. In our study, 72 severely obese subjects (BMI > 44 kg/m2) were instructed in a 4500 kJ carbohydrate-rich (50%) diet. The initial two week run-in diet+placebo period was followed by a 12 week double-blind period of diet+citalopram or placebo. There were seven withdrawals during the initial two weeks. Of the remaining 65 patients, 45 were randomized to 60 mg citalopram daily and 20 received placebo. A trend towards a higher frequency of nausea at week 6 was noted in the citalopram group. Weight loss during the initial two weeks was 2.01 kg. In the following 12 weeks, mean weight loss was 3.78 kg in the citalopram group vs. 2.64 kg in the placebo group (P = 0.29), reductions occurring almost entirely during the initial four weeks of the treatment period. We conclude that citalopram is of no clinical value in the treatment of obesity when added to a 4500 kJ diet.
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PMID:Treatment of severe obesity with a highly selective serotonin re-uptake inhibitor as a supplement to a low calorie diet. 811 71

Since citalopram was first approved in 1989, it has been prescribed to an estimated > 600 000 patients. An integrated safety database has been prepared, including data from 3107 patients from 24 clinical trials. In placebo-controlled trials, nausea, dry mouth, somnolence, increased sweating, tremor, diarrhoea, and ejaculation failure, mostly of mild to moderate severity, occurred significantly (p < 0.05) more frequently with citalopram. The excess incidence of these events over placebo was always less than 10%. In pooled comparative studies, citalopram's tolerability profile was similar to that of other selective serotonin reuptake inhibitors (SSRIs) and superior to that of tricyclic antidepressants (TCAs). Spontaneous adverse event reports arising from clinical use have confirmed the safety profile defined during the trials programme. Specific monitoring of all serious adverse events from around 10 000 patients receiving citalopram in clinical trials (including small open studies) has indicated a low potential for convulsions and extrapyramidal effects. There is no evidence of withdrawal phenomena on abrupt discontinuation, no clinically relevant effects on cardiac or laboratory parameters, and little or no effect on psychomotor function. When taken in overdose alone, citalopram appears to have a relatively wide margin of safety. Citalopram has been well tolerated in both short- and long-term use, and the profile seen in trials has been confirmed in the clinic.
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PMID:The safety and tolerability of citalopram. 873 43

The effect of comedication with fluvoxamine on the plasma concentrations of the enantiomers of citalopram and its metabolites in dextromethorphan/mephenytoin phenotyped patients pretreated with citalopram (CIT) was studied: seven female patients (45.1 +/- 13.9 years) suffering from a major depressive episode [ICD-10: F32.2 (n = 3 patients), F33.2 (n = 2), F32.10 (n = 1) or F32.11 (n = 1)], who were non-responders to a 3-week treatment with 40 mg/day CIT (From day-21 to day 0) (day 0: MADRS score > or = 12), were co-medicated for another 3 weeks with fluvoxamine (50 mg/day from day 1-7, 100 mg/day from day 14-21). All patients were extensive metabolizers of mephenytoin (CYP2C19) and dextromethorphan (CYP2D6), except one patient, who had a genetic deficiency of CYP2D6. There was a significant increase of the plasma concentrations of S- and R-citalopram from day 0 (27 +/- 14 micrograms/l and 55 +/- 23 micrograms/l, respectively) to day 21 (83 +/- 38 micrograms/l and 98 +/- 44 micrograms/l, respectively), after addition of fluvoxamine (P < 0.02, for each comparison), and the mean ratio S/R-citalopram increased from 0.48 to 0.84. S-Citalopram inhibits more potently 5-HT uptake than R-citalopram: therefore, fluvoxamine increases the pharmacologically more active S-citalopram with some stereoselectivity. According to a previous in vitro study, this pharmacokinetic interaction occurs on the level of CYP2C19, but also of CYP2D6 and CYP3A4 which, in contrast to CYP1A2, contribute to the N-demethylation of citalopram and which are stereoselectively inhibited by fluvoxamine. All but one patient showed clinical improvement by a decrease of the MADRS score by at least 50% and a final score < or = 13 (mean +/- SD: day 0:30.6 +/- 9.2; day 21:11.0 +/- 6.5). Some patients showed minor symptoms, such as nausea and tremor, but the combined treatment was generally well tolerated.
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PMID:Non-response to citalopram in depressive patients: pharmacokinetic and clinical consequences of a fluvoxamine augmentation. 898 13

A meta-analysis of 20 short term comparative studies of 5 selective serotonin reuptake inhibitors (SSRIs; citalopram, fluoxetine, fluvoxamine, paroxetine and sertraline) has shown no difference in efficacy between individual compounds but a slower onset of action of fluoxetine. There were suggestions that fluoxetine caused more agitation, weight loss and dermatological reactions than the other SSRIs. More patients discontinued fluvoxamine and fewer patients stopped sertraline because of adverse effects than their comparator SSRIs. The most common adverse reactions to the SSRIs were gastrointestinal (especially nausea) and neuropsychiatric (particularly headache and tremor). Data from the Committee on Safety of Medicines showed more reports of suspected reactions (including discontinuation reactions) to paroxetine, and of gastrointestinal reactions to fluvoxamine and paroxetine, than the other SSRIs during their first 2 years of marketing. Prescription-event monitoring revealed a higher incidence of adverse events related to fluvoxamine than its comparators. There were higher incidences of gastrointestinal symptoms, malaise, sedation and tremor during treatment with fluvoxamine and of sedation, tremor, sweating, sexual dysfunction and discontinuation reactions with paroxetine. Fluoxetine was not associated with a higher incidence of suicidal, aggressive and related events than the other SSRIs. Patients have survived large overdoses of each of the compounds, but concern has been expressed over 6 fatalities following overdoses of citalopram. Drug interactions mediated by cytochrome P450 enzymes are theoretically less likely to occur during treatment with citalopram and sertraline, but there is a sparsity of clinical data to support this. Methodological difficulties and price changes do not allow choice for recommendations on the choice of SSRI based on pharmacoeconomic data. Taking into account the strengths and weaknesses of the methods used to compare drugs, guidelines to the selection of individual SSRIs in clinical practice are proposed. Citalopram should be avoided in patients likely to take overdoses. Fluoxetine may not be the drug of first choice for patients in whom a rapid antidepressant effect is important or for those who are agitated, but it may have advantages over other SSRIs in patients who are poorly compliant with treatment and those who have previously had troublesome discontinuation symptoms. Fluvoxamine, and possibly paroxetine, should not be used as first choice in patients especially prone to SSRI-related adverse reactions, while paroxetine should be avoided if previous discontinuation of treatment was troublesome. When in doubt about the risks of drug interactions, citalopram or sertraline should be considered given the lower theoretical risk of interactions.
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PMID:Systematic review and guide to selection of selective serotonin reuptake inhibitors. 1065 95

Selective serotonin reuptake inhibitors (SSRIs) are the treatment of choice for pathological crying after brain injury, independent of accompanying depression. In a series of 26 consecutive patients with acquired brain damage and episodes of involuntary crying, the efficacy and tolerability of paroxetine and citalopram were compared. The severity of pathological crying or laughing was rated based on clinical interviews with symptom provocation. The first 13 patients were treated with paroxetine and another 13 patients received citalopram in single daily doses of 10 to 40 mg. Rapid onset (within 1-3 days) and highly significant (p < 0.001) improvements of emotionalism were observed after both paroxetine and citalopram. There were no efficacy differences, despite the longer symptom duration in the citalopram group. The only adverse effect after paroxetine was nausea, which was reversible, in two patients, and nausea with vomiting in another two patients, who were switched to citalopram. Citalopram was tolerated without adverse effects.
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PMID:Paroxetine versus citalopram treatment of pathological crying after brain injury. 1057 64

Citalopram at a dose of 20 mg was used as monotherapy in the treatment of 91 outpatients with depression mostly of moderate intensity. The duration of treatment was 2 months. Patients were assessed by Clinical Global Impression Scale (CGI) before, after 1st and 2nd months of therapy. Twenty three patients were additionally rated after 2 weeks. Observed and spontaneously adverse events were also recorded. A large proportion of treated patients (75%) showed full or almost full remission (1 or 2 on CGI) at the end of study. There were only few mainly mild adverse events during treatment. Nausea (7.7%) and headache (3.3%) occurred most often. The author conclude that citalopram is a well-tolerated and efficacious antidepressant drug for outpatients.
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PMID:[Citalopram (Cipramil) in monotherapy of depressed outpatients]. 1105 87

Citalopram is a chiral antidepressant drug. Its eutomer, S-citalopram (escitalopram), has recently been introduced as an antidepressant. In an open pilot study, four outpatients and two inpatients with a major depressive episode (ICD-10), and who were nonresponders to a 4-week pretreatment with 40-60 mg/day citalopram, were comedicated for another 4-week period with carbamazepine (200-400 mg/day). Some of the patients suffered also from comorbidities: Phobic anxiety disorder with panic attacks (n=2), generalised anxiety disorder, alcohol abuse, dependent personality disorder, hypertension (n=1). After a 4-week augmentation therapy with carbamazepine, a significant (P<0.03) decrease of the plasma concentrations of S-citalopram and R-citalopram, by 27 and 31%, respectively, was observed. Apparently, the probable induction of CYP3A4 by carbamazepine results in a nonstereoselective increase in N-demethylation of citalopram. Moreover, there was a significant (P<0.03) decrease of the ratio S/R-citalopram propionic acid derivative, the formation of it being partly regulated by MAO-A and MAO-B. Already, within 1 week after addition of carbamazepine, there was a slight but significant (P<0.03) decrease of the MADRS depression scores, from 27.0+/-7.7 (mean+/-S.D.) to 23.3+/-6.6, and the final score on day 56 was 18.8+/-10.9. The treatment was generally well tolerated. There was no evidence of occurrence of a serotonin syndrome. After augmentation with carbamazepine, treatment related adverse events were: Nausea in one case, diarrhea in one case, and rash in two cases. In conclusion, the results of this pilot study suggest that carbamazepine augmentation of a citalopram treatment in previous nonresponders to citalopram may be clinically useful, but that in addition carbamazepine can lead to a decrease of the plasma concentrations of the active enantiomer escitalopram.
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PMID:Carbamazepine augmentation in depressive patients non-responding to citalopram: a pharmacokinetic and clinical pilot study. 1200 77

We obtained information on the efficacy and safety of citalopram in settings that resemble actual clinical practice. A total of 1,783 patients participated in this open, uncontrolled, naturalistic Phase IV evaluation of citalopram at 447 U.S. investigative sites. Participants were selected by guidelines in the citalopram package insert using minimal exclusion criteria. Citalopram dosing began at 20 mg/day and could be titrated to 60 mg/day. Outcomes included the Clinical Global Impressions-Improvement scale (CGI-I) and a Patient Global Evaluation. Separate analyses were performed on patients with a primary diagnosis of major depressive disorder (MDD) (76%) who reported intolerance or nonresponse to previous selective serotonin reuptake inhibitors (SSRIs). Patients included tended to have treatment-resistant or intolerant, chronic or recurrent, comorbid depression with a mean duration of illness of 10 years. At study completion, more than 68% of treatment completers were classified as responders (CGI-I score of 1 or 2). Endpoint analyses showed response rates of 54% in all patients, 56% in patients with MDD, 49% in SSRI nonresponsive patients, and 53% in patients with a history of SSRI intolerance. Nausea (9.8%) and headache (7.3%) were the most often reported adverse events. Patients with a history of SSRI intolerance had a discontinuation rate of 21.8%, whereas those without such a history had a discontinuation rate of 13.3%. Citalopram administered at an average dose of 23.6 mg/day was associated with favorable outcomes and was generally well tolerated.
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PMID:Naturalistic study of the early psychiatric use of citalopram in the United States. 1241 37


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