Details
Date of approval: November 27, 2006
Modified date: November 30, 2015
Sertraline hydrochloride tablets instructions
Please read the instructions carefully and use them under the guidance of a physician.
【Drug Name】
Generic name: Sertraline hydrochloride tablets
Product Name: Bi Mele
English name: Sertraline Hydrochloride Tablets
Chinese Pinyin: Yansuan Shequlin Pian
[Ingredients] The main component of this product is sertraline hydrochloride. Its chemical name is: (1S, 4S)-4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-N- Methyl-1-naphthylamine hydrochloride.
Molecular formula: C17H17Cl2N·HCl
Molecular weight: 342.70
【Properties】 This product is a film-coated tablet, which is white or off-white after removal of the coating.
[indications]
Sertraline is used to treat symptoms associated with depression, including depression with or without history of mania. After satisfactory results, continued use of sertraline can effectively prevent recurrence and recurrence of depression.
Sertraline is also used to treat obsessive-compulsive disorder. After initial treatment, sertraline maintains its effectiveness, safety and tolerability during the two years of treatment of obsessive-compulsive disorder.
[Specification] 50mg (according to C17H17Cl2N)
【Dosage】
Adults take the drug once a day, either early or late, with or without food. The effective dose for the treatment of depression and obsessive-compulsive disorder is usually 50 mg/day.
When a small number of patients have poor efficacy and are well tolerated by drugs, they can gradually increase the dose according to the effect within a few weeks, increasing by 50 mg each time, up to 200 mg/day, once a day. Since the elimination half-life of sertraline is 24 hours, the interval between dose adjustments should not be shorter than one week.
The effect can be seen in about 7 days, and the complete effect will appear in the second to fourth weeks of taking the drug. The appearance of obsessive-compulsive symptoms may take longer.
Long-term medication should be adjusted according to the efficacy and maintained at the lowest effective therapeutic dose.
【Adverse reactions】
1. According to the literature, common adverse reactions in a controlled clinical study of sertraline and placebo in the treatment of depression are as follows:
Autonomic nervous system: dry mouth and sweating.
Central and peripheral nervous system: dizziness and tremors.
Gastrointestinal tract: diarrhea / loose stools, indigestion and nausea.
Spirit: anorexia, insomnia and lethargy.
Reproductive system: sexual dysfunction (mainly male ejaculation delay).
2. Sertraline tablets have been on the market for many years. According to the literature, the adverse events spontaneously reported during the patient's administration of sertraline are as follows:
Autonomic nervous system: enlarged pupils and abnormal erection of the penis.
Whole body: allergic reactions, allergies, allergic reactions, asthma, fatigue, fever, flushing, discomfort, weight loss, weight gain.
Cardiovascular system: chest pain, peripheral edema, hypertension, palpitations, periocular edema, syncope, and tachycardia.
Central and peripheral nervous system: coma, convulsions, headache, migraine, dyskinesia (including extrapyramidal side effects such as hyperactivity, increased muscle tone, molars and gait abnormalities), muscle involuntary contractions, paresthesia, and dysesthesia . There are also symptoms and signs associated with serotonin syndrome, such as anxiety, confusion, sweating, diarrhea, fever, high blood pressure, myotonia and tachycardia caused by the simultaneous use of serotoninergic drugs.
Endocrine system: galactorrhea, excessive mammary gland development, hyperprolactinemia and hypothyroidism, ADH secretion disorders syndrome.
Gastrointestinal system: abdominal pain, increased appetite, constipation, pancreatitis and vomiting.
Hearing/vestibular function: tinnitus.
Blood system: changes in platelet function, abnormal bleeding (such as nosebleeds, gastrointestinal bleeding or hematuria), neutropenia, purpura and thrombocytopenia.
Laboratory examination changes: abnormal clinical test results.
Hepatobiliary system: severe liver disease (including hepatitis, jaundice, and liver failure) and asymptomatic serum transaminase elevation (SGOT and SGPT).
Metabolic/nutrition system: hyponatremia and elevated cholesterol.
Musculoskeletal system: joint pain.
Spirit: anxiety, aggression, anxiety, depressive symptoms, euphoria, hallucinations, loss of female sexual desire, male libido, nightmares, mental illness and yawning.
Reproductive system: irregular menstruation.
Respiratory system: bronchospasm.
Skin system: alopecia, angioedema, skin photoreaction, itching, rash (rare skin dermatitis, such as erythema multiforme: Stevens-Johnson syndrome, epidermal necrolysis) and urticaria.
Urinary system: facial edema, urinary incontinence and urinary retention.
Vision: visual anomalies.
Other: There are reports of symptoms after discontinuation of sertraline: anxiety, anxiety, dizziness, headache, nausea, and paresthesia.
[Contraindications] Disabled for those who are allergic to sertraline; prohibited from combination with monoamine oxidase inhibitors.
【Precautions】
1. Sertraline should be carefully considered when combined with drugs that increase serotonin neurotransmission, such as tryptophan or fenfluramine, to avoid possible pharmacodynamic interactions.
2. There is no experience in the optimal timing of conversion from other serotonin reuptake inhibitors, antidepressants or antiobsessive drugs to sertraline. Care should be taken when switching treatments, especially long-acting drugs such as fluoxetine, and should be carefully evaluated and monitored. The washout period for conversion from a selective serotonin reuptake inhibitor to another drug has not been determined.
Mania/manic activation: About 0.4% of patients receiving sertraline experienced hypoconvuls or mania during the pre-marketing trial. When other anti-depressant drugs or anti-obsessive-compulsive drugs have been used to treat affective disorders, a few patients have reported mania or mild mania.
3. Antidepressants and anti-obsessive-compulsive drugs have the potential to induce seizures. In all trials with sertraline for depression, approximately 0.08% of seizures occurred; no seizures were reported in the trial of sertraline for panic disorder. Of the approximately 1,800 patients with obsessive-compulsive disorder who received sertraline, 4 (about 0.2%) developed seizures, 3 of whom were adolescents, 2 had epilepsy, and 1 had a family history of epilepsy, all of which None of the 4 patients received anti-epileptic drugs. All seizures have not been determined to be directly related to sertraline treatment. Sertraline has not been evaluated in patients with epilepsy, so it should be avoided in patients with unstable epilepsy. Patients with epilepsy whose condition has been controlled should be closely monitored, and any patients who have seizures during sertraline should stop taking the drug.
4. Because of the possibility of suicide attempts in patients with depression, and may persist until clinically significant relief, patients with suicidal risk should be closely monitored early in the treatment.
Since obsessive-compulsive disorder and depression are often common, it is also necessary to monitor suicidal tendencies when treating obsessive-compulsive patients.
5. Women who of childbearing age use sertraline should take adequate safety measures.
6. Although clinical pharmacology studies have shown that sertraline has no effect on psychomotor activity. However, antidepressant or anti-obsessive-compulsive drugs can affect the energy and physical energy necessary for driving a potentially dangerous job such as driving or operating a machine. Therefore, such patients should be careful when taking sertraline.
7. Patients with hepatic insufficiency: Sertraline should be used with caution in patients with liver disease. Patients with liver damage should reduce the dose or frequency of administration.
8. Patients with renal insufficiency: There is no need to adjust the dose of sertraline according to the degree of renal impairment.
[Pregnant women and lactating women]
Reproductive toxicity studies have been conducted in rats and rabbits, and there is no teratogenic evidence at dose levels of 20 times and 10 times (in mg/kg/day) of human maximum dose. However, at dose levels equivalent to 2.5 to 10 times the maximum dose of humans (in mg/kg/day), sertraline is associated with delayed ossification of the embryo and may have secondary effects on the embryonic barrier.
At a dose level of approximately 5 times the maximum dose in humans (in mg/kg/day), the survival rate of newborn young children decreased after administration of the parental sertraline. For other antidepressants, there has been a description of the reduction in the survival rate of newborn babies, and the clinical significance of these effects is still unclear.
There have not been enough good controlled studies for pregnant women. Pregnant women can only take medicine if the benefits outweigh the disadvantages.
The available data on the concentration of sertraline in milk is limited. A sporadic study of small sample sizes of lactating mothers and infants suggests that although the concentration of sertraline in milk is higher than the serum concentration, the concentration of sertraline in infant serum is extremely low or undetectable. Breastfeeding women can only use if the benefits outweigh the disadvantages.
When taking sertraline during pregnancy and / or lactation, the doctor should pay attention to the symptoms of withdrawal. Mothers taking serotonin-based antidepressants including sertraline have been reported in newborns with similar withdrawal symptoms.
[Children's medication] Although children's metabolism of sertraline is slightly faster, in order to avoid excessive blood concentration, it is recommended to use lower doses for children, especially those with a light weight of 6-12 years old.
[Geriatric Use] The range of doses for elderly patients is the same as for younger patients. A total of more than 700 elderly patients (>65 years old) participated in clinical trials confirming the efficacy of sertraline in this population. The form and incidence of adverse reactions in elderly patients are similar to those in younger patients.
【medicine interactions】
Monoamine oxidase inhibitors (MAOIs): Sertraline combined with monoamine oxidase inhibitors, including the selective monoamine oxidase inhibitor selegiline and the reversible monoamine oxidase inhibitor moclobemide treatment has experienced severe side effects, sometimes fatal. Some cases are similar to serotonin syndrome, including: fever, rigidity, muscle spasm, autonomic dysfunction with rapid fluctuations in vital signs; changes in mental status including mental disorders, irritability and extreme agitation until development into sputum and coma. Therefore, sertraline should not be taken within 14 days of taking a monoamine oxidase inhibitor or stopping the monoamine oxidase inhibitor; similarly, it takes more than 14 days for sertraline to stop treatment of the monoamine oxidase inhibitor.
Central nervous system inhibitors and alcohol: taking 200 mg of sertraline daily does not increase the effects of ethanol, carbamazepine, haloperidol or phenytoin on cognitive function and psychomotor activity in healthy subjects, but not Advocate the combination of sertraline and alcohol.
Lithium: In a placebo-controlled trial of normal volunteers, the combination of sertraline and lithium did not significantly alter the pharmacokinetic parameters of the lithium agent, but the tremor increased compared with placebo, indicating the presence of a drug between the two drugs. The possibility of ergonomic interaction. When sertraline is combined with other drugs that act on the serotoninergic mechanism, such as lithium, the patient should be monitored.
Phenytoin: In a placebo-controlled study of healthy volunteers, long-term administration of 200 mg of sertraline daily did not significantly inhibit phenytoin metabolism. However, if combined with sertraline, the plasma concentration of phenytoin should be monitored at the beginning of the addition of sertraline, and the dose of phenytoin should be adjusted appropriately.
Sumatriptan: After the listing of sertraline, there were individual reports of the combination of sertraline and sumatriptan, which showed frailty, hyperreflexia, ataxia, confusion, anxiety and agitation. If sertraline is clinically required to be combined with the drug, the patient should be closely observed.
Protein-bound drugs: Due to the binding of sertraline to plasma proteins, attention should be paid to the possibility of interaction between sertraline and other plasma protein-binding drugs. However, in three formal studies in which sertraline interacted with diazepam, tolbutamide, and warfarin, sertraline did not significantly affect the protein binding rate of these drugs.
Warfarin: The combination of sertraline 200mg/day and warfarin increased the prothrombin time to some extent, but the clinical significance was not clear. Therefore, prothrombin time should be closely monitored when sertraline is combined or discontinued with warfarin.
Interaction with other drugs: Studies have been conducted on the interaction between sertraline and other drugs. Daily combination of 200 mg of sertraline with diazepam or tolbutamide resulted in minor, but statistically significant, changes in some pharmacokinetic parameters. Combined with cimetidine can significantly reduce the clearance of sertraline. The clinical significance of these changes is unclear. Sertraline had no effect on the beta-adrenergic blockade of atenolol. There is no interaction between 200 mg of sertraline daily and glibenclamide or digoxin.
Electroconvulsive therapy (ECT): There have been no clinical trials examining the advantages or risks of combination of sertraline and electroconvulsive therapy.
Cytochrome P450 (CYP) 2D6 Metabolism Drugs: The degree of inhibition of the drug metabolism isoenzyme CYP 2D6 by antidepressants is not the same. Its clinical significance depends on the degree of inhibition and the therapeutic index of the combined drug. The CYP 2D6 substrate with a narrow therapeutic index includes tricyclic antidepressants such as propafenone, flecainide, and class 1C antiarrhythmic drugs. Existing drug interaction studies have shown that long-term administration of 50 mg of sertraline per day can slightly increase the steady-state plasma concentration of desipramine (a marker of CYP 2D6 isoenzyme activity) (average 30- 40%).
Other cytochrome (CYP) enzyme metabolism drugs (CYP 3A3/4, CYP 2C9, CYP 2C19, CYP 1A2):
CYP 3A3/4: In vivo drug interaction assays show that long-term administration of sertraline 200 mg/day does not inhibit CYP 3A3/4 mediated hydroxylation of endogenous cortisol or metabolism of carbamazepine and terfenadine . In addition, long-term administration of 50 mg of sertraline per day did not inhibit CYP 3A3/4 mediated drug metabolism of alprazolam. This indicates that sertraline is not an inhibitor of CYP 3A3/4.
CYP 2C9: Long-term administration of sertraline 200 mg/day had no significant effect on the plasma concentrations of tolbutamide, phenytoin and warfarin. This suggests that sertraline is not a clinically relevant inhibitor of CYP 2C9.
CYP 2C19: Long-term use of sertraline 200mg/day had no significant effect on the plasma concentration of diazepam, indicating that sertraline is also not an inhibitor of CYP 2C19.
CYP 1A2: In vitro studies have shown that sertraline has no significant inhibitory effect on CYP 1A2.
Other serotonergic drugs: Sertraline should be carefully considered when combined with drugs that enhance serotonin neurotransmission, such as tryptophan or fenfluramine, to avoid possible pharmacodynamic interactions.
【Drug overdose】
There is evidence that sertraline still has a large safety margin when overdosed. There have been reports of sertraline alone taking up to 13.5 grams. There have been reports of excessive use of sertraline leading to death, but most have appeared with other drugs and/or
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