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1、奥思平(盐酸度洛西汀肠溶片)药品说明书（Ausi Ping (Duloxetine Hydrochloride Enteric-coated Tablets) drug instructions）Drug instructionsDrug nameDuloxetine Hydrochloride Enteric-coated TabletsItem name: Duloxetine Hydrochloride Enteric CapsuleChinese Pinyin: YanSuanDuLuoXiDingChangRongJiaoNangDosage form, Chinese Pharma
2、copoeia, dosage form, capsuleThe content of this product is white or small white like pellets.The main ingredients of duloxetine hydrochloride chemical name: (+) - (S) -N- methyl gamma (1- naphthyl oxygen) -2- thiophene propanol amine hydrochloride molecular formula: C18H19NOS molecular weight: 333.
3、88 HCL.Indications for the treatment of depression.Specifications 20mg*20 granuleThe adverse reaction of MDD in the treatment of acute phase of the placebo-controlled study, receiving duloxetine treated patients, the adverse reaction rate was higher than 2% and higher than in the placebo group. One
4、of the most common adverse reactions (incidence of less than 5%, which is at least two times higher than the placebo group the incidence of) including nausea, dry mouth and constipation, loss of appetite, fatigue, lethargy, increased sweating (please consult a specialist) - the urgency of duloxetine
5、 is known to influence the drug resistance of urethra. If the use of duloxetine in the course of the treatment of urinary urgency, should consider the possibility of drug-induced. Laboratory changes - 9 weeks MDD or 13 weeks DPNP placebo-controlled study, compared with baseline, after duloxetine tre
6、atment, ALT, AST, CPK and alkaline phosphatase (vinegar) enzyme increased slightly. Compared with the placebo group, these abnormalities occurred in patients treated with duloxetine as episodic, intermediate, and transient abnormalities (see note). Changes of vital signs in 9 weeks MDD placebo-contr
7、olled study, duloxetine dose of 40-120mg/ day, leads to increased blood pressure, compared with placebo, the average systolic blood pressure increased diastolic blood pressure increased by an average of 2mrnHg, 0.5mmHg, systolic blood pressure increased incidence of more than 140mmHg. In the 9 week
8、MDD and 13 week DPN cadaveric placebo-controlled study, duloxetine resulted in a mild increase in heart rate, with an increase of about 2 / minute compared with placebo.Dosage 1. initial treatment. The starting dose of this product is 40mg/ days (20mg two times a day) to 60mg/ days (once a day or 30
9、mg two times a day) without regard to food intake. The available clinical data do not confirm that the dose over 60mg/ will increase the efficacy. It is generally believed that the acute attack of depression takes months or longer, but there is not enough experimental data to determine how long the
10、patient should continue to take duloxetine. For such patients, the need for acceptance, maintenance, and the appropriate dose should be assessed periodically. 2. special population. Impaired kidney function in patients with end-stage renal disease (a dosage for dialysis patients), or severe renal im
11、pairment (estimated creatinine clearance 30 mL/min) patients, do not recommend this product (see pharmacology and toxicology). The amount of patients with hepatic dysfunction. It is recommended that patients with any hepatic dysfunction avoid taking this product (see pharmacology, toxicology, and pr
12、ecautions). For elderly patients, it is recommended that dose not be adjusted according to age. Like any drug, care should be taken for the treatment of elderly patients. In elderly patients, additional doses should be taken with extra caution when adjusted individually.For pregnancy after treatment
13、 of female patients with three months of a pregnancy within three months after exposure to SSRIs or SNRls (five serotonin and norepinephrine reuptake inhibitor) of the newborn, the complications can lead to prolonged hospitalization, respiratory support and feeding pipeline (see note). When women ar
14、e treated with duloxetine during the pregnancy, doctors should evaluate the potential risks and benefits of treatment three months after pregnancy. Doctors should consider increasing the amount of duloxetine late in pregnancy. 3. degrees duloxetine withdrawal. The discontinuation of this product and
15、 other SSRI and SNRIs drugs has been reported (see note). These symptoms should be monitored at the time of withdrawal. It is recommended to gradually reduce the drug as soon as possible instead of the drug. The use of past prescription doses may be considered when reducing the dose or withdrawal of
16、 drugs resulting in intolerable symptoms. The drug is then slowed down at a slower rate. 4. change of administration with monoamine oxidase inhibitor (MOA, I). MOAT can start the treatment at least 14 days after the withdrawal. At least 5 days after the drug is discontinued, you can begin the treatm
17、ent of MOAT (see contraindications and warnings).Contraindicated 1. degrees duloxetine enteric coated capsules are contraindicated in patients who are allergic to duloxetine, enteric coated capsules, or any inactive ingredient in the product.2. prohibit the use of monoamine oxidase inhibitors (MAOIs
18、). (see warning)3. untreated narrow angle glaucoma4. clinical trials show that duloxetine increases the risk of mydriasis, and untreated patients with narrow angle glaucoma should avoid the use of duloxetineNote hepatotoxicity - duloxetine has an increased risk of serum aminotransferase levels. Elev
19、ated liver transaminase resulted in discontinuation of treatment for patients treated with duloxetine at 0.4% (31/8454). The median duration of aminotransferase elevation in these patients was 2 months. In a controlled trial in patients with depression, 09% (8/930) costs rose by more than 3 times th
20、e normal limit in patients treated with duloxetine (ALT), compared with 0.3% in the placebo group (2/652). In all placebo-controlled studies, 1% of patients in the duloxetine group (39/3732) had elevated ALT by more than 3 times the normal limit, compared with 0.2% in the placebo group (6/2568). In
21、a fixed dose placebo-controlled study, there was evidence that ALT increased by more than 3 times the normal limit and AST increased by more than 5 times the normal limit and had a dose effect relationship with the drug dose.Duloxetine is not usually used in patients with habitual alcohol consumptio
22、n or chronic liver disease.Blood pressure should be measured before treatment begins and regular measurements should be taken after treatment.Duloxetine should be used with caution in patients who have been prescribed alcohol or who have had a history of liver disease.Patients who had had a history
23、of seizures were careful with duloxetine.Patients who had had a history of mania were careful with duloxetineWithdrawal - a systematic study of the discontinuation of duloxetine has been conducted. In patients with depression in the 9 week placebo-controlled trial, arrest drug, the observed rate of
24、2% was significantly higher than that of placebo or arrest symptoms including the occurrence of duloxetine in the treatment of patients with dizziness, nausea, headache, feelingPregnancy in pregnant women and lactating women: classification of pregnancy C-; in animal reproductive studies, duloxetine
25、 was found to have an adverse effect on embryonic / fetal and postnatal development.The rats and rabbits during oral administration of duloxetine in the embryonic organ, dose of 45mg/kg/ day (rats at a dose of 7 times MRHD, 60mg/kg/, 4 times in accordance with the calculation of the index weight / b
26、ody surface area body dose 120mg/; rabbits at a dose of 15 times MRHD, 7 times in accordance with the weight / body mass index calculated body dose 120mg/ days), found no teratogenic effect. At this dose, the fetus loses weight. No effect dose was 10mg/kg/ days (in rats was 2 times at MRHD, about 1
27、times in accordance with the calculation of the index weight / body surface area body dose 120mg/; rabbits at a dose of 3 times at MRHD, about 2 times in accordance with the calculation of the index weight / body surface area body dose 120mg/). Throughout pregnancy and lactation treated with duloxet
28、ine in pregnant rats, at the dose of 30 mg/kg/ day (5 times MRHD, 2 times according to the weight / body surface area index calculation of mg/m2 human dose 120mg/), after the birth of children survived for 1 days, birth and lactation weight loss; no effect the dose is 10 mg/kg/. Moreover, the dose o
29、f duloxetine was 30 mg/kg/, and the childrens behavior was consistent with the increase of reactivity, such as the surprised reaction to the noise and the habitual decrease of voluntary activities. However, maternal use of duloxetine did not negatively affect offspring growth and reproductive behavi
30、or after weaning. Due to the lack of adequate, well-designed, women controlled studies during pregnancy, the use of duloxetine in pregnancy is considered only when weighing the potential benefit of the fetus over risk. Recent mothers of duloxetine, whose newborn babies may suffer from the following
31、symptoms of withdrawal, include dystonia, tremors, nervousness, feeding difficulties, respiratory distress and seizures. Non teratogenic effect of newborn in the second trimester of pregnancy three months of exposure to SSRIs or SNRIs (five serotonin and norepinephrine reuptake inhibitor), the compl
32、ications can lead to prolonged hospitalization, respiratory support and feed pipe. These complications occur immediately after birth. The clinical findings include respiratory distress, cyanosis, apnea, seizures and temperature instability, feeding difficulty, vomiting, hypoglycemia, dystonia, hyper
33、tonia, hyperreflexia, tremor, overreaction, irritability, crying. These conditions may be caused by the direct toxicity of SSRIs and SNRIs, or may be a withdrawal reaction of drugs. It should be noted that in some cases, the clinical presentation is consistent with the five serotonin syndrome (see w
34、arnings, monoamine oxidase inhibitors). When pregnant women are treated with duloxetine for three months at the end of pregnancy, the doctor should carefully evaluate the potential risks and benefits of the treatment (see usage and dosage). Labor: the effect of duloxetine on human labor is not clear
35、. Therefore, it is only considered that the potential benefit of duloxetine over fetal risk exceeds the risk of being considered during delivery. Lactation: duloxetine can be secreted by lactating women. The estimated daily dose of the baby is about 0.14% (mg/kg) of the mothers dose. Because duloxet
36、ine does not have an effect on infants, patients with duloxetine are not recommended for breast feeding.The efficacy and safety of pediatric medication in pediatric patients is unclear (see warning).If considering the use of duloxetine in children and adolescents, the potential risks and clinical ne
37、eds must be weighed.There is limited data on the use of excessive doses of duloxetine in humans, and 3000mg is rapidly swallowed up in clinical data. Alone or in combination with other drugs, no fatal events have been reported. However, there were reports of acute drug overdose deaths after the list
38、ing, mainly mixed drug overdose, and a single dose of duloxetine about 1000mg. Excessive withdrawal and symptoms (mostly mixed drug overdoses) include serotonin syndrome, lethargy, vomiting, and seizures.Drug interactions may affect other drug duloxetine metabolism of duloxetine with CYP1A2 and CYP2
39、D6 inhibitors of CYP1A2 - duloxetine and Hide Saki (CYP1A2 inhibitor) combined application in male subjects (n=14), duloxetine AUC increased more than 5 times, Cmax increased by about 2.5 times T1/2, an increase of about 3 times. Other drugs inhibit the metabolism of CYP1A2 include: cimetidine, quin
40、olone antibiotics such as ciprofloxacin and enoxacin. CYP2D6 inhibitors as CYP2D6 in duloxetine metabolism, so the combined use of duloxetine and strong CYP2D6 inhibitors, duloxetine hydrochloride concentration will increase, (see note under drug interactions). Other drugs that duloxetine may affect
41、 other drugs through CYP1A2 metabolism - drug interactions in vitro showed that Lositin did not induce CYP1A2 activity. Therefore, although no clinical studies on enzyme induction have been performed, it is expected that the metabolism of CYP1A2 substrates (e.g. theophylline and caffeine) will not i
42、ncrease because of enzymatic induction. Although in vitro studies showed that duloxetine was a CYP1A2 inhibitor, the pharmacokinetics of theophylline did not change significantly when combined with the use of theophylline as a substrate of CYP1A2 (60 mg two times daily). Therefore, the metabolic eff
43、ects of duloxetine on CYP1A2 substrates are unlikely to produce clinically significant effects. Duloxetine, a drug that is metabolized through CYP2D6, is a moderate CYP2D6 inhibitor that increases the AUC and Cmax levels of drugs that are metabolized by CYP2D6. (see notice). Therefore, caution shoul
44、d be taken when combined with duloxetine and other major drugs that are metabolizing the enzyme and treating a narrow dose range (see drug interactions under notice). An in vitro study of CYP2C9 metabolism showed that duloxetine did not inhibit the activity of CYP2C9 enzymes. Thus, although clinical
45、 studies were not performed, it was estimated that duloxetine did not inhibit the metabolism of CYP2C9 substrate. The results of in vitro studies on the CYP3A metabolism showed that duloxetine did not inhibit or induce the activity of CYP3A. Thus, although clinical studies have not been carried out,
46、 it is expected that CYP3A substrate (e.g., oral contraceptives and other steroid drugs) will not cause metabolic enhancement or inhibition because of enzyme induction or inhibition. The results of in vitro studies of CYP2C19 metabolism showed that the concentration of duloxetine did not inhibit the
47、 activity of CYP2C19. Thus, although clinical studies were not performed, it was estimated that duloxetine did not inhibit the metabolism of CYP2C19 substrate.Study on the combined use of benzene two nitrogen drugs, Laura Si - steady-state concentration of duloxetine (60mg, Q, 12, HRS) and Laura Si
48、(2mg Q 12hrs) when combined, Laura Si pharmacokinetics is not affected by combined treatment. Temazepam steady-state concentration of duloxetine (20mg QHS) and temazepam (30mg QHS) when combined effects of temazepam pharmacokinetics by combination therapy. Drug - high plasma protein binding for dulo
49、xetine and high plasma protein binding, undergoing other high plasma protein binding drug treated patients, taking duloxetine, may increase the concentration of free of other drugs, which may lead to the occurrence of adverse drug reactions. Central nervous system drugs - when duloxetine is used in combination with other centrally acting drugs, especially in combination with drugs with similar mechanisms of action (including alcohol), should be used wi