What Factors Affect a Sufficient Escitalopram Dose?

Escitalopram oxalate tablets are indicated for the treatment of depressive disorders and panic disorders with or without square phobia.

Escitalopram oxalate tablets are indicated for the treatment of depressive disorders and panic disorders with or without square phobia.

Drug Name

Escitalopram oxalate tablets

Drug type

Prescription drugs, medicines for medical workers' injuries

Use classification

Other antidepressants

Caution on Escitalopram oxalate tablets

Results of short-term clinical trials of suicidal tendency and antidepressants for depression (MDD) and other mental disorders show that antidepressants increase suicide perceptions and commit suicide in children, adolescents and young people ([24 years) compared to placebo Behavioral (Suicidal) Risk. Anyone considering the use of this product or other antidepressants for children, adolescents, or young people ([24 years) must weigh clinical needs and risks. Short-term clinical trials have not shown that the use of antidepressants in adults older than 24 years increases the risk of suicidal tendencies compared to placebo; among adults aged 65 and older, the use of antidepressants increases the risk of suicidal tendencies Decreased. Depression and certain mental disorders are themselves associated with an increased risk of suicide. It is necessary to closely observe and reasonably monitor the deterioration of clinical symptoms, suicidal tendencies, and abnormal changes in behavior of patients of all ages after the start of antidepressant treatment. Families and caregivers should be advised to observe closely and communicate with the doctor. This product has not been approved for use in children (see [Warning], [Cautions], and [Children's Medication]).

Escitalopram oxalate tablets ingredients

Active Ingredient: Escitalopram oxalate.
Chemical name: S (+)-1- (3-dimethylaminopropyl) -1- (4-fluorophenyl) -1,3-dihydroisobenzofuran-5-carbonitrile oxalate.
Chemical Structure:

Molecular formula: C ₂₀ H ₂₁ FN ₂ O · C ₂ H ₂ O ₄
Molecular weight: 414.43

Escitalopram oxalate tablets properties

Tablets 5mg: Round, white film-coated tablets. 10mg: oval, white film-coated tablet.

Escitalopram oxalate tablets indications

Treatment of depressive disorder, panic disorder with or without square phobia.

Specifications of escitalopram oxalate tablets

(1) 5mg (2) 10mg

Escitalopram oxalate tablets dosage

Usage: Oral, can be taken with food.
Dosage:
Depression

1 time daily. The usual dose is 10 mg daily, and the maximum daily dose can be increased to 20 mg based on the individual response of the patient. Antidepressant effects are usually obtained in 2-4 weeks. After the symptoms have resolved, treatment should be continued for at least 6 months to consolidate the effect.
Panic disorder with or without plague horror once a day. The recommended starting dose is 5 mg daily, and it is increased to 10 mg daily after 1 week. According to the individual response of the patient, the dose can continue to increase to the maximum dose of 20 mg daily.
The best results are obtained after about 3 months of treatment. The course of treatment usually lasts several months.
Elderly patients (> 65 years)
It is recommended to start treatment with half of the above-mentioned conventional starting dose (5 mg), and the maximum daily dose should not exceed 10 mg.
Children and adolescents (<18 years)
This product is not suitable for children and adolescents under 18 years of age.
Patients with reduced renal function do not need to adjust the dose for patients with mild to moderate renal function. Patients with severe renal function (CLcr <30 mL / min) should be used with caution.
Those with reduced liver function recommend a starting dose of 5 mg daily for 2 weeks. Depending on the individual response of the patient, the dose can be increased to 10 mg per day. Patients with severely reduced liver function are advised to take special care and increase doses with caution.
Cytochrome P450 2C (CYP2C19) slow metabolizer For patients known to have slow metabolism of CYP 2C19, the recommended starting dose is 5 mg daily for 2 weeks. Depending on the individual response of the patient, the dose can be increased to 10 mg daily.
Withdrawal should be avoided. When it is necessary to stop the treatment of this product, the dose should be gradually reduced within 1-2 weeks to avoid the symptoms of withdrawal.
The safety of doses above 20 mg daily has not been proven.

Adverse reactions of escitalopram oxalate tablets

Adverse reactions occurred in the first 1-2 weeks of treatment, and the severity and incidence of adverse reactions decreased after continuous treatment.
The known adverse reactions reported spontaneously after the placebo-controlled clinical study and market launch of SSRI drugs and escitalopram according to organ system classification and frequency are listed in the table below.
Incidences were derived from clinical trials; listed rates are not adjusted for placebo. The definition of incidence is as follows: very common (1 / 10), common (1 / 100 to <1/10), rare (1 / 1000 to <1/100), and rare (1 / 10,000 to <1 / 1000), very rare (<1/10000), unknown (cannot be estimated from existing data).

1. Suicidal consciousness and suicidal behavior have been reported early in the treatment or discontinuation of this product.
2. Such incidents are reported in the treatment of SSRI drugs.
Cases of QT-interval prolongation reported after marketing are mainly found in patients with existing heart disease, and the reason is unknown. In a double-blind placebo-controlled study of healthy subjects, the QTC (Fridericia-corrected) interval of the electrocardiogram of patients on the 10 mg / day group changed by 4.3 milliseconds from baseline and 10.7 ms on the 30 mg / day group. .
Discontinuation of SSRIs / SNRIs (especially abrupt stops) often results in withdrawal symptoms. Dizziness, paresthesia (including paresthesia and electrical shock sensation), sleep disturbances (including insomnia and nervous dreams), agitation and anxiety, nausea and / or vomiting, tremor, confusion, sweating, headache, diarrhea, palpitations, mood Instability, irritability, and visual impairment were the most commonly reported reactions. These events are generally mild or moderate and self-limiting, but may be severe or prolonged in some patients. Therefore it is recommended that when the treatment of this product is no longer needed, the dose should be gradually reduced to discontinuation. (See Dosage and Precautions)

Escitalopram oxalate tablets contraindications

1. Those who are allergic to the active ingredients of this product or any excipients are prohibited from using it.
2. Do not use in combination with non-selective, irreversible monoamine oxidase inhibitors (MAOI) (see [Warning] and [Drug Interactions]).
3. Prohibition of combined use with linezolid, see [Drug Interactions].
4. It is forbidden to combine medication with pimozide, see [Drug Interactions] for details.
5. In patients with known QT interval prolongation or congenital QT syndrome, the use of this product is prohibited.

Precautions for escitalopram oxalate tablets

Antidepressants are not suitable for children and adolescents under 18. In clinical trials in children and adolescents under 18 years of age, it was found that suicide-related behaviors (suicide attempts and suicidal ideas) and hostility (aggressiveness, confrontational behavior, and irritability) occurred more frequently in the treatment group than in the placebo group. . Even for the clinical needs of clinical trials, patients need to be closely monitored for signs of suicide.
The following special warnings and cautions apply to all types of SSRI drugs.
Paradoxical anxiety < br Some patients with panic disorder may aggravate anxiety symptoms at the beginning of antidepressant treatment. This paradoxical reaction usually decreases gradually within 2 weeks after the start of treatment. It is suggested that reducing the starting dose can reduce this anxiety effect of the drug.
Seizures <br Patients with first seizures or those who have been diagnosed with epilepsy should stop using this product when the frequency of seizures increases. SSRIs should be avoided in patients with unstable seizures, and patients with seizures under control should be monitored during treatment.
Manic SSRIs should be used with caution in patients with a history of manic or hypomanic episodes. Patients who switch to manic episodes should stop using SSRIs.
Diabetes < br For patients with diabetes, treatment with SSRI drugs may affect the regulation of blood glucose. Patients who use insulin and / or oral hypoglycemic drugs need to adjust the dosage of these drugs.
Suicide, suicidal ideation, or worsening of the condition. Depression inherent symptoms may appear suicidal attempt, suicide and suicide (suicide-related events), and will continue until significant improvement due to treatment. Because it may not improve in the first weeks or weeks after treatment, patients using antidepressants should be closely monitored before the disease improves. Clinical experience generally suggests that the risk of suicide may increase during the early stages of recovery. The use of this product in other psychiatric events is also related to the increased risk of suicide-related events. In addition, mental events may be concurrent with depression. Such prevention should also be used when treating other mental disorders associated with depression. Patients who have had suicide-related events or had serious suicidal concepts before treatment with this product are known to have a greater risk of suicidal concepts or suicidal attempts, and should be carefully monitored during treatment. A meta-analysis of antidepressants and placebo-controlled studies in adults with depressive disorder showed that patients under the age of 25 had a higher risk of suicidal behavior than those treated with placebo. Patients should be closely monitored during antidepressant treatment, especially those at high risk, or early in the treatment and dose adjustment period.
The patient (and the patient's caregiver) should closely monitor for any clinical deterioration, suicidal behavior, or changes in mind and abnormal behavior, and seek medical advice immediately if these symptoms appear.
Sedentary Impairment / Psychomotor Disturbance. The use of SSRIs / SNRIs is related to the occurrence of meditation impairment, which is manifested by the subject's unwillingness or distress and anxiety, which requires frequent movement, and cannot sit or stand quietly. Sedation cannot occur mostly during the first few weeks of treatment. If a patient develops these symptoms, further dose increases may be harmful.
Hyponatremia < br Rarely, hyponatremia (possibly due to abnormal secretion of antidiuretic hormone) with SSRIs has been reported, and symptoms usually resolve after stopping medication. Patients at risk, such as the elderly, patients with cirrhosis, or medications known to cause hyponatremia, should be noted.
Bleeding < br There have been reports of subcutaneous bleeding with SSRIs, such as petechiae and purpura. The use of SSRIs in the following populations is advised to be prudent, including: patients who use oral anticoagulants or drugs known to affect platelet function (such as atypical antipsychotics and phenothiazines, Some tricyclic antidepressants, acetylsalicylic acid and non-steroidal anti-inflammatory drugs, ticlopidine and dipyridamole) and patients with a known bleeding tendency.
Electroconvulsive therapy (ECT)
At present, there is only limited clinical experience on the combined use of SSRI drugs and electroconvulsive therapy, so caution is recommended.
Reversible, selective MAO-A inhibitors < br This product is generally not recommended for combination with MAO-A inhibitors, because there may be a risk of serotonin syndrome. (See Drug Interactions)
For combination use with non-selective, irreversible MAO inhibitors, see Drug Interactions.
Serotonin Syndrome < br It is recommended that this product be used in combination with serotoninergic drugs (such as sumatriptan or other triptans, tramadol, and tryptophan). There are rare cases of serotonin syndrome when combined with SSRI drugs and serotonergic drugs. If the following symptoms appear after the combination, such as agitation, tremor, myoclonus, and high fever, suggesting that serotonin syndrome may have occurred. If this problem occurs, SSRI and serotonergic drugs should be stopped immediately and given symptomatic treatment.
St. John's wort < br The combined use of SSRIs and Chinese herbs containing St. John's wort (Hyperitamine) may increase the incidence of adverse reactions.
Discontinuation symptoms < br Discontinuation symptoms are common when treatment is discontinued, especially when abrupt discontinuation (see Adverse Reactions). Of the clinical trial adverse events observed, approximately 25% of patients treated with this product and 15% of patients treated with placebo experienced symptoms of discontinuation. The risk of withdrawal symptoms may depend on several factors, including the duration and dose of treatment, and the rate at which the dose is reduced. The most commonly reported withdrawal reactions are dizziness, paresthesia (including paresthesia and feeling of electrical convulsions), sleep disorders (including insomnia and nervousness), agitation and anxiety, nausea and / or vomiting, tremor, confusion, sweating, Headache, diarrhea, palpitations, emotional instability, irritability, and visual impairment. These symptoms are usually mild to moderate, but some patients may be severe. These symptoms usually occur within the first few days of discontinuation of treatment, and rarely have they been reported in patients who have missed medication due to negligence.
Generally, these symptoms are self-limiting and usually resolve within 2 weeks, although in some individuals it may take longer (2-3 months or more). Therefore, it is recommended to go through a gradual reduction process of several weeks or months according to the needs of the patient when stopping the medicine.
Effects on the ability to drive and operate machines. <br /> Although research has shown that this product does not affect intelligence and psychomotor operations, any psychoactive drug may affect judgment and skills. Patients should be aware of potential hazards that may affect their ability to drive cars and operate machines.
Keep them out of reach of children.

Escitalopram oxalate tablets for pregnant and lactating women

Pregnant women < br There is limited clinical data on the use of this product by pregnant women.
Teratogenic effects were observed in reproductive toxicology studies in rats, but no increase in teratogenicity was found. The clinical data of this product for pregnant women are limited. This product should not be used in pregnant women. If there is a clinical need, use it only after carefully considering its risks / benefits.
If pregnant women use this product, the fetus should be continuously monitored until the third trimester, especially in the third trimester of pregnancy. Avoid sudden withdrawals during pregnancy. Pregnant women continue to use SSRIs until the newborn is born. The reported newborns will experience the following effects: respiratory distress, cyanosis, apnea, seizures, unstable body temperature, vomiting, hypoglycemia, irritability, tremor, hypertension, muscle Increased tension, nervousness, lethargy, persistent crying, lethargy, difficulty sucking or falling asleep. May be serotonergic action or withdrawal syndrome. Pregnant women should not stop taking SSRIs suddenly. In most cases, complications will occur immediately after delivery or [24 hours].
Epidemiological data suggest that the use of SSRIs in pregnant women, particularly in late pregnancy, may increase the risk of persistent pulmonary hypertension (PPHN) in the newborn. About 5 cases were observed in 1000 pregnant women using SSRI. In a group of people, PPHN occurs in 1 to 2 cases per 1,000 pregnant women.
Breastfeeding women <br /> Escitalopram can be secreted in breast milk. Breastfeeding women should not receive treatment with this product or stop breastfeeding during medication.

Escitalopram oxalate tablets for children

Antidepressants are not suitable for children and adolescents under 18. In clinical trials in children and adolescents under 18 years of age, it was found that suicide-related behaviors (suicide attempts and suicidal ideas) and hostility (aggression, confrontational behavior, and irritability) occurred more frequently in this group than in the placebo group. Even for clinical trials, suicide performance needs to be closely monitored.

Escitalopram oxalate tablets for elderly use

See [Dosage and Administration]

Escitalopram oxalate tablets drug interactions

Pharmacodynamic interactions <br /> Contraindications :
Non-selective M, irreversible AOIs
Serious adverse reactions have been reported in patients receiving SSRI drugs who have combined non-selective monoamine oxidase inhibitors (MAOI) with patients who have recently stopped taking SSRI drugs and started MAOI treatment. Some patients have serotonin syndrome .
This product is contraindicated with non-selective MAOIs. This product can be started after stopping irreversible MAOI treatment for at least 14 days and at least 1 day after reversible MAOI (eg, morphobexamide). Non-selective, MAOI treatment can be started at least 7 days after stopping the treatment of this product.
Patients treated with pimozide using this product at 40 mg daily taking a single dose of pimozide at a dose of 2 mg at the same time can lead to an increase in the AUC and maximum plasma concentration of pimozide, even though it was not consistent throughout the study. The combination of pimozide and citalopram resulted in a prolongation of the QTc interval by approximately 10 milliseconds. Because interactions can occur at lower doses of pimozide, the combination of escitalopram and pimozide is prohibited.
Concomitant treatments that require careful attention:
Reversible, selective MAO-A inhibitor (morphlobemide).
Due to the danger of serotonin syndrome, this product is not recommended for combination with MAO-A inhibitors. If concomitant treatment is indeed needed, it should be started with the minimum recommended starting dose, and clinical monitoring should be strengthened.
This product can be started after stopping reversible MAOI treatment for at least 1 day.
Use of selegiline in combination with selegiline, an irreversible MAO-B inhibitor, requires caution because of the risk of serotonin syndrome.
Serotoninergic drugs in combination with serotonergic drugs (such as tramadol, sumatriptan, and other triptans) may cause serotonin syndrome.
Drugs that lower the seizure threshold SSRIs can lower the seizure threshold and caution should be used in combination with other drugs that can lower the seizure threshold. Such as antidepressants (tricyclics, SSRIs), neuroleptics (phenothiazines, thia anthracenes, butyrylbenzenes), mefloquine, amphetamine, and tramadol.
Lithium salts and tryptophan have been reported to have a synergistic effect when combined with SSRI drugs and lithium salts or tryptophan, so caution should be used in combination with SSRI drugs and these drugs.
St. John's wort combined with SSRI drugs and Chinese herbs containing st. John's wort (Hyperitamine) may increase the incidence of adverse reactions.
Bleeding This product may change the anticoagulant effect of such drugs when used in combination with oral anticoagulants. Patients receiving oral anticoagulants should pay special attention to monitoring the anticoagulant effect when starting or stopping treatment with this product.
There is no pharmacokinetic and pharmacodynamic interaction between this product and alcohol. But like other psychoactive drugs, it is not recommended to be used with alcohol.
Pharmacokinetic interactions < br Other drugs that affect the pharmacokinetics of this product <br The metabolism of this product in the body is mainly mediated by CYP 2C19, CYP 3A4 and CYP 2D6 also participate in its metabolism, but the effect is more small. Demethyl escitalopram, the main metabolite of this product, may also be partially catalyzed by CYP 2D6.
The combined use of omeprazole (CYP 2C19 enzyme inhibitor) will cause a moderate increase in plasma concentration of this product (approximately 50%).
The combination of escitalopram and cimetidine (a moderate-intensity inhibitor of multiple enzymes) can moderately increase the plasma concentration of escitalopram (approximately 70%).
Therefore, when this product reaches the upper limit of the therapeutic dose, caution should be taken in combination with CYP 2C19 enzyme inhibitors (such as omeprazole, fluoxetine, fluvoxamine, lansoprazole, ticlopidine) and cimetidine. Ding.
It may be necessary to reduce the dose of this product based on clinical judgment.
The effect of this product on the pharmacokinetics of other drugs < br This product is an inhibitor of CYP 2D6, and should be used with caution in combination with the following drugs, including drugs mainly metabolized by CYP 2D6, drugs with a narrow therapeutic index, such as: Flukanib, propafenone, and metoprolol (when treating heart failure), or some drugs acting on the central nervous system that are primarily metabolized by CYP 2D6 (antidepressants norpromazine, chlorpromazine, and desalination) Metformin, etc., or the antipsychotics risperidone, methiopyrazine, and haloperidol). The dose should be adjusted when combined.
Combination with normipramine or metoprolol may cause plasma concentrations of these two drugs (both CYP 2D6 substrates) to increase more than two-fold.
In vitro studies have shown that this product may also cause mild inhibition of CYP 2C19. Care should be taken when combining it with drugs metabolized by CYP 2C19.

Escitalopram oxalate tablets overdose

Toxicity < br Clinical data on the overdose of this product is very limited, but there have been no reports of any serious adverse reactions when overdose of this product 600 mg. Most of the reported cases are mild or asymptomatic. Cases of death due to this tablet overdose are rarely reported in single use, and most cases are accompanied by overdose of other drugs. This product is used in a single dose of 400-800 mg without any serious symptoms.
Symptoms < br The reported symptoms of escitalopram overdose are mainly related to the following systems: the middle denervation system (from vertigo, tremor and agitation to the rarely reported serotonin syndrome, convulsions and coma), Gastrointestinal system (nausea / vomiting), cardiovascular system (hypotension, tachycardia, prolonged QT-interval, and arrhythmia) and electrolyte / body fluid balance (hypokalemia, hyponatremia).
There are no specific remedies for treatment. Keeping the airways open and ensuring adequate oxygen intake and breathing function are critical. Stomach lavage as soon as possible after oral medication. It is recommended to monitor the heart and vital signs and to give systemic supportive treatment.

Clinical trial of escitalopram oxalate tablets

Of the four double-blind, placebo short-term (8-week) controlled trials of depressive disorder, three trials have shown that escitalopram is effective in depressive disorders. When the dosage of this product is 10 mg and 20 mg, it shows antidepressant effect after 2 weeks of administration. After 8 weeks of treatment, the efficacy of the 20 mg group was better than that of the citalopram 40 mg group. The dose correlation was obvious in patients with major depression, and the efficacy of patients with a dose of 20 mg was better than the usual starting dose of 10 mg.
In a 24-week long-term double-blind trial, the efficacy of the 10 mg escitalopram group was comparable to that of the 20 mg citalopram group, and half of the patients in the escitalopram group dropped out of the trial due to adverse reactions. In a long-term trial to prevent relapse, escitalopram 10 or 20 mg / day was given for 8 weeks of open treatment. In response to treatment, 274 patients were randomly given the same dose of escitalopram or placebo to 36 weeks. In the 36-week study, patients treated with escitalopram experienced significantly later relapses than the placebo group.
Panic disorder < br In a 10-week controlled trial for panic disorder, comparing 5-20 mg / day escitalopram and placebo and 10-40 mg / day citalopram To evaluate the efficacy of escitalopram. By evaluating the frequency, severity, duration, and accompanying symptoms of panic attacks, it was shown that the escitalopram group has a statistically significant advantage over the placebo group. For most treatment-related adverse events (5% of patients), the citalopram group was higher than the escitalopram group.
Three short-term (12-week) studies of social anxiety disorder and a 6-month relapse prevention study showed that escitalopram was effective in patients with social anxiety disorder.
A 24-week long-term placebo-controlled trial demonstrated that escitalopram at doses of 5, 10, and 20 mg was effective.
The efficacy of 20 mg / day escitalopram in the treatment of social anxiety disorders has statistically significant advantages over paroxetine 20 mg / day, escitalopram 5 mg / day, and 10 mg / day. Transient withdrawal symptoms were observed in the treatment group (duration did not exceed 2 weeks in all active treatment groups). Compared with the escitalopram group, the withdrawal symptoms were more pronounced in the paroxetine group (P0.05).
A combined analysis including 670 patients with escitalopram and 341 patients with placebo showed an effective rate of 58.1% and 40.2% (CGI-I score of 1 or 2), and a cure rate of 24.8% and 12.9% (CGI- S-score 1 or 2) (P0.001).
The results of four placebo-controlled trials of generalized anxiety disorder have confirmed the efficacy of escitalopram 10 mg / day and 20 mg / day, but 5 mg / day is not effective.
A combined 8-week clinical trial from three similar regimens showed that in 421 patients treated with escitalopram and 419 patients with placebo, the effective rates were 47.5% and 28.9% (CGI-I score 1 Or 2), the cure rates were 37.1% and 20.8% (CGI-S score of 1 or 2, P 0.001). Sustained effects begin to appear from the first week.
In four 12-week controlled trials with paroxetine, the efficacy of escitalopram 10 mg / day was statistically significantly better than paroxetine 20 mg / day. Transient withdrawal symptoms were observed in both groups, compared to the 5 mg, 10 mg, and 20 mg / day escitalopram group, the withdrawal symptoms were more pronounced in the paroxetine group (P0.01).
A randomized, continuous trial of 24-76 weeks was performed on 373 patients who were effective in the first 12 weeks of open treatment. Patients receiving 20 mg / day of escitalopram had a significantly reduced risk of relapse.

Escitalopram oxalate tablets pharmacology and toxicology

Pharmacological effects:
Escitalopram is the mono-S-enantiomer of the bicyclic hydrogenated phthalic derivative citalopram. The mechanism of antidepressant effect of escitalopram 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 and animal tests have shown that escitalopram is a highly selective 5-HT reuptake inhibitor (SSRI), with less effect on the reuptake of norepinephrine and dopamine. In terms of 5-HT reuptake inhibition, escitalopram is at least 100 times more active than the R-enantiomer. The rat depression model was given no resistance to escitalopram for a long time (up to 5 weeks).
Escitalopram has no affinity for 5-HT1-7 receptor, receptor, receptor, D1-5 receptor, H1-3 receptor, M1-5 receptor, benzodiazepine receptor, or only Has a lower affinity. Escitalopram has no affinity for Na +, K +, Cl-, Ca2 + channels, or has only a low affinity.
Toxicology research:
In the genotoxic citalopram Ames test, in the absence of a metabolic activator, two of the five test strains (TA98 and TA1537) were positive. In the citalopram CHL chromosome aberration test, the results were positive with or without the presence of a metabolic activator. The results of citalopram mouse lymphoma cell forward gene mutation test (HPRT), rat liver cell extraprogrammed DNA synthesis test (UDS), human lymphocyte chromosome aberration test, and mouse micronucleus test were all negative.
Reproductive toxicity < br In the fertility test, rats were orally given citalopram 32, 48, 72 mg / kg / day, and it was seen that the mating rate in each dose group was reduced, and fertility was reduced when the dose was 32 mg / kg / day. The pregnancy time was prolonged at a dose of 48 mg / kg / day. In the rat embryo-fetal developmental toxicity test, rats were orally administered escitalopram 56, 112, 150 mg / kg / day, medium and high doses (calculated based on mg / m2, equivalent to the maximum recommended human dose [MRHD ] 20 mg / day 56 times), the decrease in fetal weight and delayed ossification can be seen. Maternal toxicity (abnormal clinical conditions, decreased weight gain, and decreased food intake) were seen in all dose groups, and no teratogenic effects were seen. The developmentally unaffected dose was 56 mg / kg / day, which was approximately 28 times the MRHD. Pregnancy rats were given escitalopram 6, 12, 24, and 48 mg / kg / day during the perinatal period. The highest dose group (equivalent to about 24 times the MRHD) had a slight increase in mortality and slight retardation of growth. Maternal toxicity (clinical abnormalities, decreased weight gain, reduced food intake). The 24 mg / kg / day dose group showed a slight increase in offspring mortality. The unaffected dose was 12 mg / kg / day, which was equivalent to about 6 times the MRHD.
In animal reproductive toxicity tests, citalopram has shown adverse effects on embryo / fetal development and postnatal development, including teratogenicity that occurs at higher doses than humans. In the rat embryo / fetal toxicity test, rats were given citalopram 32, 56, 112 mg / kg / day orally. At high doses, embryo / fetal growth inhibition, fetal survival, and fetal abnormality increased (including heart rate). Vascular and skeletal defects) and maternal toxicity (normal clinical abnormalities, decreased weight gain), and the unaffected developmental dose was 56 mg / kg / day. Rabbits received citalopram at oral doses of up to 16 mg / kg / day with no abnormalities. In the perinatal toxicity test, rats were orally given citalopram 4.8, 12.8, 32 mg / kg / day. In the high-dose group, the mortality of the young rats increased within 4 days after birth, and the growth of the young rats was arrested. The unaffected dose was 12.8 mg / kg / day.
Carcinogenic NMRI / BOM mice and COBS WI rats were orally given citalopram for 18 and 24 consecutive months, respectively. Mice were not carcinogenic at doses up to 240 mg / kg / day. At a dose of 8 or 24 mg / kg / day, the incidence of small bowel tumors was increased in rats. The relevance of this phenomenon to people is unclear.

Pharmacokinetics of escitalopram oxalate tablets

Absorption < br Complete oral absorption, not affected by food (peak plasma concentration reached 4 hours on average after repeated oral administration). Like citalopram, the absolute bioavailability of this product is about 80%.
Distribution < br The apparent volume of distribution (Vd, / F) after oral administration is about 12-26 L / Kg. The plasma protein binding rate of this product and its metabolites is about 80%.
Metabolism < br This product is mainly metabolized by demethylation and dedimethylation in the liver. Both metabolites are pharmacologically active. In addition, the N group can be oxidized to produce N oxidation metabolites. Prototype drugs and metabolites can be partially excreted by glucuronidation. After multiple administrations, the average plasma concentrations of demethylated and dedimethylated metabolites were 28-31% and [5%] of the original drug concentration, respectively. Demethylation of this product is mainly metabolized by the enzyme cytochrome P450 (CYP) 2C19, and CYP 3A4 and CYP 2D6 may also play a part.
Elimination < br The elimination half-life is about 30 hours after multiple administrations, the plasma clearance (CIoral) of oral drugs is about 0.6 L / min, and the main metabolites of the drugs have a longer half-life. This product and its metabolites are mainly processed by The liver (metabolism) and kidneys are eliminated, mainly excreted from the urine as metabolites.
The pharmacokinetics of this product are linear, reaching steady-state plasma concentration after about 1 week, and the average steady-state plasma concentration of 10 mg daily dose is 50 nmol / L (range: 20-125 nmol / L).
Elderly patients (] 65 years old)
Drug elimination is slower in older patients than in younger patients. Compared with young healthy subjects, the AUC of older people is 50% higher.
Patients with reduced liver function < br In patients with mild and moderate liver damage (Child-Pugh criteria A and B), the half-life of citalopram is about twice that of patients with normal liver function, and the exposure is 60% higher.
Patients with reduced renal function <br In patients with reduced renal function, an increased half-life of citalopram and a slight increase in plasma drug concentration (CLcr10-53 mL / min) were observed. The plasma concentrations of metabolites have not been studied, but their concentrations may increase.
Polymorphisms It has been found that the plasma concentration of slow metabolizers metabolized by CYP 2C19 is twice that of fast metabolizers, while the plasma concentration of slow metabolizers metabolized by CYP 2D6 has not changed significantly.

Storage of escitalopram oxalate tablets

Store below 30 ° C.

Packaging of escitalopram oxalate tablets

Packed in aluminum-plastic board.
5mg: 14 tablets / box; 28 tablets / box.
10mg: 7 tablets / box; 28 tablets / box.

Escitalopram oxalate tablets expiration date

36 months

Standard for Escitalopram oxalate tablets

JX20090196 ^[1]