喜普妙Celexa（西酞普兰）

Celexa(Citalopram)

 

Citalopram, sold under the brand name Celexa among others, is an antidepressant of the selective serotonin reuptake inhibitor (SSRI) class.[1]It is used to treat major depressive disorder, obsessive compulsive disorder, panic disorder, and social phobia.[1] Benefits may take one to four weeks to occur.[1] It is taken by mouth.[1]

 

Common side effects include nausea, trouble sleeping, sexual problems, shakiness, feeling tired, and sweating.[1] Serious side effects include an increased risk of suicide in those under the age of 25, serotonin syndrome, glaucoma, and QT prolongation.[1] It should not be used in someone on a MAO inhibitor.[1] Antidepressant discontinuation syndrome may occur when stopped.[1] There are concerns that use during pregnancy may harm the baby.[3]

 

Citalopram was approved for medical use in the United States in 1998.[1] It is available as a generic medication.[4] In the United Kingdom, a typical dose costs less than 20 GBP per month.[4] In the United States, it costs 50 to 100 USD per month as of 2016.[5] In 2016, it was the 21st most prescribed medication in the United States, with more than 26 million prescriptions.[6]

 

Medical uses

Depression

In the National Institute for Health and Clinical Excellence ranking of 10 antidepressants for efficacy and cost-effectiveness[7] citalopram is fifth in effectiveness (after mirtazapine, escitalopram, venlafaxine, and sertraline) and fourth in cost-effectiveness. The ranking results were based on the meta-analysis by Andrea Cipriani.[8] In another analysis by Cipriani, citalopram was found to be more efficacious than paroxetine and reboxetine, and more acceptable than tricyclics, reboxetine, and venlafaxine, but less efficacious than escitalopram.[9]

 

Evidence for effectiveness of citalopram for treating depression in children is uncertain.[10][11]

Panic disorder

Citalopram is licensed in the UK and other European countries[12] for panic disorder, with or without agoraphobia. The dose is 10 mg/d for a week, increasing to 20–30 mg/d, with a maximum of 40 mg/d.[13]

Other

Citalopram is frequently used off-label to treat anxiety, panic disorder, dysthymia,[14]premenstrual dysphoric disorder, body dysmorphic disorder, and obsessive–compulsive disorder.[15]

 

It has been shown to be effective in 85% of patients with generalized anxiety disorder, including some who had failed with other SSRIs.[16] It also appears to be as effective as fluvoxamine and paroxetine in obsessive–compulsive disorder.[17] Some data suggest the effectiveness of intravenous infusion of citalopram in resistant OCD.[18] Citalopram is well tolerated and as effective as moclobemide in social anxiety disorder.[19] There are studies suggesting that citalopram can be useful in reducing aggressive and impulsive behavior.[20][21] It appears to be superior to placebo for behavioural disturbances associated with dementia.[22] It has also been used successfully for hypersexuality in early Alzheimer’s disease.[23]

 

A meta-analysis, including studies with fluoxetine, paroxetine, sertraline, escitalopram, and citalopram versus placebo, showed SSRIs to be effective in reducing symptoms of premenstrual syndrome, whether taken continuously or just in the luteal phase.[24] Citalopram has produced a modest reduction in alcoholic drink intake and increase in drink-free days in studies of alcoholics, possibly by decreasing desire or reducing the reward.[25]

 

Citalopram has been found to reduce the symptoms of diabetic neuropathy.[26]

While on its own citalopram is less effective than amitriptyline in the prevention of migraines, in refractory cases, combination therapy may be more effective.[27]

 

Citalopram and other SSRIs can be used to treat hot flashes.[28]:107

A 2009 multisite randomized controlled study found no benefit and some adverse effects in autistic children from citalopram, raising doubts whether SSRIs are effective for treating repetitive behavior in children with autism.[29]

 

Some research suggests citalopram interacts with cannabinoid protein-couplings in the rat brain, and this is put forward as a potential cause of some of the drug's antidepressant effect.[30]

 

Administration

Citalopram is typically taken in one dose, either in the morning or evening. It can be taken with or without food. Its absorption does not increase when taken with food,[31] but doing so can help prevent nausea. Nausea is often caused when the 5HT3 receptors actively absorb free serotonin, as this receptor is present within the digestive tract.[32] The 5HT3 receptorsstimulate vomiting. This side effect, if present, should subside as the body adjusts to the medication.

 

Citalopram is considered safe and well tolerated in the therapeutic dose range. Distinct from some other agents in its class, it exhibits linear pharmacokinetics and minimal drug interaction potential, making it a better choice for the elderly or comorbid patients.[33]

 

Adverse effects

 

Sexual dysfunction is often a side effect with SSRIs. Specifically, common side effects include difficulty becoming aroused, lack of interest in sex, and anorgasmia (trouble achieving orgasm). One study showed, however, when remission of major depressive disorder is achieved, quality of life and sexual satisfaction is reported to be higher in spite of sexual side effects.[34]

 

Citalopram theoretically causes side effects by increasing the concentration of serotonin in other parts of the body (e.g., the intestines). Other side effects, such as increased apathy and emotional flattening, may be caused by the decrease in dopamine release associated with increased serotonin. Citalopram is also a mild antihistamine, which may be responsible for some of its sedating properties.[28]:104

 

Common side effects of citalopram include drowsiness, insomnia, nausea, weight changes (usually weight gain), increase in appetite, vivid dreaming, frequent urination, decreased sex drive, anorgasmia, dry mouth,[31] increased sweating, trembling, diarrhea, excessive yawning, severe tinnitus, and fatigue. Less common side effects include bruxism, vomiting, cardiac arrhythmia, blood pressure changes, dilated pupils, anxiety, mood swings, headache, and dizziness. Rare side effects include convulsions, hallucinations, severe allergic reactions and photosensitivity.[31] If sedation occurs, the dose may be taken at bedtime rather than in the morning. Some data suggest citalopram may cause nightmares.[35] Citalopram is associated with a higher risk of arrhythmia compared to other SSRIs.[36][37]

 

Withdrawal symptoms can occur when this medicine is suddenly stopped, such as paraesthesiae, sleeping problems (difficulty sleeping and intense dreams), feeling dizzy, agitated or anxious, nausea, vomiting, tremors, confusion, sweating, headache, diarrhea, palpitations, changes in emotions, irritability, and eye or eyesight problems. Treatment with citalopram should be reduced gradually when treatment is finished.

 

Citalopram and other SSRIs can induce a mixed state, especially in those with undiagnosed bipolar disorder.[28]:105

 

Overdose

 

Overdosage may result in vomiting, sedation, disturbances in heart rhythm, dizziness, sweating, nausea, tremor, and rarely amnesia, confusion, coma, or convulsions.[28]:105 Overdose deaths have occurred, sometimes involving other drugs, but also with citalopram as the sole agent. Citalopram and N-desmethylcitalopram may be quantified in blood or plasma to confirm a diagnosis of poisoning in hospitalized patients or to assist in a medicolegal death investigation. Blood or plasma citalopram concentrations are usually in a range of 50-400 μg/l in persons receiving the drug therapeutically, 1000–3000 μg/l in patients who survive acute overdosage and 3–30 mg/l in those who do not survive.[56][57][58] It is the most dangerous of SSRIs in overdose.[59]