What Is Serotonin Withdrawal Syndrome?

The main ingredient of this product is citalopram hydrobromide ^[1] . Its chemical name is: (±) -1- [3- (dimethylamino) propyl] -1- (4-fluorophenyl) -1,3-dihydro-5-cyanoisobenzofuranhydrobromide Acid salt.

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The main ingredient of this product is citalopram hydrobromide ^[1]

Common name: Citalopram hydrobromide tablets ^[2]

Those who are highly sensitive to this product are prohibited. This product cannot be used at the same time as MAOI'S (see note).

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Animal reproductive studies have proven that the drug has toxic side effects on the fetus, but pregnant women have not yet undergone a sufficiently rigorous controlled study, and the benefits of using the drug for pregnant women may outweigh its potential harm; or the drug has not been tested in animals and has not Fully rigorous controlled studies in pregnant women.

The safety of citalopram during pregnancy has not been determined. Therefore, it should not be taken during pregnancy and lactation unless the benefits to the patient far outweigh the theoretical risks to the fetus or infant.

The safety and effectiveness of children's medications have not been determined.

Medication for Elderly Patients-Elderly patients over 65 years of age should be reduced as appropriate, see [Usage and Administration].

This product should not be taken with monoamine oxidase inhibitors (such as isocarbozide and morphlobemide for the treatment of depression, and propynylamphetamine hydrochloride for the treatment of Parkinson's disease), otherwise it will cause serious adverse reactions. The interval between this product and the monoamine oxidase inhibitor should be more than 14 days. However, if a reversible monoamine oxidase inhibitor with a short half-life, such as morphobexamide (with a half-life of 1 to 2 hours), can be used after 1 day of discontinuation.

Central Nervous System Drugs-Because citalopram works primarily in the central nervous system, it should be used with caution in combination with other drugs that act on the central nervous system. Alcohol-Although citalopram does not enhance the effects of alcohol on sensory and motor nerves in clinical trials, like other psychiatric drugs, it is recommended that patients with depression who take citalopram not take alcoholic products.

Cimipramine--Subjects took citalopram at a dose of 40mg / day for 21 days, then combined with cimipramine (400mg / day) and citalopram for 8 days, and found that the AUC and Cmax of citalopram increased respectively. 43% and 39%. The clinical significance of this finding is unknown.

Digoxin-After taking citalopram at a dose of 40mg / day for 21 days, the combination of digoxin (1mg) and citalopram will not significantly affect the pharmacokinetics of citalopram and digoxin .

Lithium-combined citalopram (40 mg / day, 10 days) and lithium (30 mmol / day, 5 days) were not found to have a significant effect on the pharmacokinetics of citalopram and lithium. Because lithium enhances the activity of citalopram's serum activin, plasma lithium levels should be monitored and appropriate adjustments made to the lithium dose to meet clinical trial standards. Caution should be used in combination with citalopram and lithium.

Theophylline-combined use of citalopram (40 mg / day, 21 days) and the CYP1A2 substrate theophylline (300 mg single dose) has no effect on the pharmacokinetics of theophylline. The effect of theophylline on the pharmacokinetics of citalopram has not been evaluated.

Sumatriptan-Post-marketing reports of patients using serotonin inhibitors and sumatriptan found to be weak, hyperreflexive, and uncooperative. If it is clinically necessary to use sumatriptan in combination with SSRI (eg fluoxetine, fluvoxamine, paroxetine, sertraline, citalopram), the patient should be appropriately observed.

Warfarin-Continuous use of citalopram 40mg / day for 21 days has no effect on the pharmacokinetics of warfarin, a substrate of CYP3A4. The prothrombin time increased by 5%, and its clinical significance is unknown.

Amide imidazine-combined citalopram (40 mg / day, 14 days) and amide imidazine (dose gradually increased to 400 mg / day, 35 days), did not significantly affect amidazine (a CYP3A4 enzyme substrate) Pharmacokinetics. Although the plasma trough concentration of citalopram is not affected, amidazine has an enzyme induction effect, so the possibility of increased citalopram clearance should be considered when the two are combined.

Triazolam-citalopram (dose gradually increased to 40 mg / day, 28 days) in combination with the CYP3A4 enzyme substrate triazolam (single dose 0.25 mg) had no significant effect on the pharmacokinetics of the two.

Ketoconazole-citalopram (40 mg) combined with ketoconazole (200 mg) reduced Cmax and AUC of ketoconazole by 21% and 10%, respectively, and the pharmacokinetics of citalopram were not significantly affected.

CYP3A4, CYP2C19 inhibitors-In vitro studies have shown that CYP3A4 and CYP2C19 are the main enzymes involved in the metabolism of citalopram. However, the combination of citalopram (40 mg) and ketoconazole (200 mg), an effective inhibitor of CYP3A4, had no significant effect on the pharmacokinetics of citalopram. Because citalopram is metabolized by multiple enzyme systems, inhibition of only one enzyme may not slightly reduce the clearance of citalopram.

Metoprolol-Citalopram 40 mg / day, 22-day treatment results increased the beta-adrenergic inhibitor metoprolol plasma levels by a factor of two. Increased metoprolol plasma levels are associated with reduced selectivity to the heart. The effect of combined use of citalopram and metoprolol on blood pressure and heart rate was not clinically significant. Imipramine (an antidepressant) and other tricyclic antidepressants (TCAs)-in vitro studies have shown that citalopram is a relatively weak inhibitor of CYP2D6. The combination of citalopram (40 mg / day, ten days) and the enzyme substrate of the tricyclic antidepressant imipramine-CYP2D6 (a single dose of 100 mg) did not significantly affect the plasma concentrations of both. However, the concentration of imipramine, desipramine, increased by 50%. The clinical significance of the change in desipramine concentration is unknown. Use caution when using imipramine with citalopram.

Excessive use alone or in combination with other drugs can cause the following symptoms

Dizziness, sweating, nausea, vomiting, tremor, drowsiness, sinus tachycardia, and rare amnesia, doubt, coma, convulsions, hyperventilation, cyanosis, rhabdomyolysis, and ECG changes (prolonged QT interval, nodular Heart rhythm, ventricular arrhythmias, apical torsional ventricular tachycardia). If you overdo it, take this product package to the hospital emergency room as soon as possible, regardless of whether you feel unwell.

Overdose

Take symptomatic and supportive therapies. Stomach washes as soon as possible after oral overdose. Keep the airway open and oxygen supply. Because citalopram is widely distributed in the body, strong diuresis, dialysis, and blood exchange have no significant effect on improving symptoms. Citalopram has no special antidote.

Citalopram is an antidepressant and is a bicyclic hydrogenated phthalate derivative. The antidepressant mechanism of citalopram may be related to the inhibition of 5-HT reuptake by central nervous system neurons, thereby enhancing the function of central serotoninergic nerves. In vitro tests and animal tests suggest that citalopram is a highly selective 5-HT reuptake inhibitor, which has less effect on the reuptake of norepinephrine and dopamine. Rats were given citalopram for 14 days, and the effect of inhibiting 5-HT uptake was not tolerated. Citalopram is a racemate, and its effect of inhibiting 5-HT reuptake is mainly exerted by its (S) -enantiomer.

Citalopram has 5-HT1A, 5-HT2A, D1 receptor, D2 receptor, 1 receptor, 2 receptor, receptor, H1 receptor, GABA receptor, M receptor, benzodiazepine? Receptor No affinity, or only low affinity.

Single and multiple doses of citalopram hydrobromide in the range of 10-60mg / day, its pharmacokinetics are linear and dose-dependent, mainly through liver conversion, with an average terminal half-life of 35h. Once a day, the plasma concentration of citalopram hydrobromide reached a steady state level in about one week. The steady state plasma accumulation of citalopram is determined by its half-life, and its plasma concentration is 2.5 times the plasma concentration after a single administration.

A single dose of 40 mg citalopram, the blood concentration reached a peak in about 4 hours. Compared to intravenous administration, citalopram has a bioavailability of 80% and absorption is not affected by food. The distribution volume of citalopram is 12 L / kg, and 80% of citalopram, norcitalopram, and dimethylcitalopram combined with plasma proteins.

Citalopram is metabolized to norcitalopram (DCT), nordimethylcitalopram (DDCT), N-oxidized citalopram, and deaminopropionic acid derivatives. In the human body, citalopram is mainly present in the plasma in its original form. At steady state, the concentrations of the metabolites DCT and DDCT of citalopram are 1/2 and 1/10 of the original drug, respectively, and are excreted through urine and feces.

Special population

Age-The pharmacokinetics of healthy volunteers aged 60 or older were compared with young healthy volunteers. In a single dose, the area under the drug curve (AUC) and the half-life of the drug in the elderly population increased by 30% and 50%, respectively, compared with those in the young population, and increased by 23% and 30% respectively in multiple administrations. The recommended dosage for most elderly patients is 20 mg (see Dosage and Administration).

Hepatic Impairment-Citalopram clearance is reduced by 37% and the half-life is doubled compared to healthy subjects The recommended dosage for patients with liver impairment is 20 mg (see Dosage and Administration).

Renal Impairment-Citalopram clearance is reduced by 17% in patients with mild to moderate renal impairment. Dosage adjustment is not recommended for patients with impaired renal function. The pharmacokinetics of patients with severe renal insufficiency (creatinine clearance <20 mL / min) has not been studied.

Character

This product is a film-coated tablet that appears white after removal of the coating.

Store

Keep sealed. Store out of children's reach.

package

Medicinal PTP aluminum foil packaging, 14 capsules / box

Expiration date

Tentative 24 months

manufacturer

Sichuan Pearl Pharmaceutical Co., Ltd.

Drug classification

Antidepressants