Product introduction of rosiglitazone hydrochloride tablets Generic name: rosiglitazone hydrochloride tablets
Manufacturer: Zhejiang Wanma Pharmaceutical Co., Ltd.
Approval number: National Medicine Zhunzi H2004 1408
Drug specification: 2mg* 14 tablets.
Drug price: 25 yuan
Instructions for Rosiglitazone Hydrochloride Tablets General Name Rosiglitazone Hydrochloride Tablets
Product name: rosiglitazone hydrochloride tablets (Ilicis)
English name rosiglitazone hydrochloride tables
Pinyin Full Code Eye Calculation Rosiglitazone Tablets (Italian)
Main ingredients: rosiglitazone hydrochloride.
Chemical name: (? ) 5-[4-[2-(5- ethyl -2- pyridine) ethoxy] benzyl]-2,4- thiazolidinedione hydrochloride
Molecular formula: C 19H20N2O3S? Highcostofliving
Molecular weight: 392.89
Characteristics Rosiglitazone hydrochloride tablets (Ilicis) are film-coated tablets, and the film-coated tablets are white or white-like.
Indications/Functions: Rosiglitazone hydrochloride tablets (Ilicis) are suitable for the treatment of type 2 diabetes.
Specification model 2mg* 14s
Usage and dosage are all taken orally, and taking medicine has nothing to do with eating. Diabetes treatment should be individualized. Monotherapy: the initial dose can be 4mg per day, 1 time or twice per day. If the initial dose is not good, it can be gradually increased to 8mg per day. Combined medication with sulfonylureas: the initial dose can be 4mg per day, 1-2 times per day, and the dose of sulfonylureas should be reduced when hypoglycemia occurs. Combined medication with metformin: the initial dose can be 4mg per day, 1-2 times per day. 12 weeks later, if the fasting blood glucose control is not ideal, the dose is increased to 8mg per day. The recommended dose is 8 mg per day, once or twice a day.
The adverse reaction was 1. Mild to moderate edema, the literature reported that the incidence of edema was 4.8% when single drug was used. 2. Anemia, the incidence rate is about 1%. Rosiglitazone hydrochloride tablets (Ilicis) can reduce hemoglobin and hematocrit, which may be related to the increase of plasma volume caused by rosiglitazone hydrochloride. 3. Hypoglycemia reaction, there is a risk of hypoglycemia when combined with other hypoglycemic drugs. 4. Abnormal liver function, all of which are mild to moderate transaminase increase, reversible. 5. Elevated blood lipids.
Pioglitazone hydrochloride is contraindicated in patients who are allergic to rosiglitazone hydrochloride tablets (Ilicis) or any ingredients in rosiglitazone hydrochloride tablets.
Precautions 1. Rosiglitazone hydrochloride tablets (Ilicis) are not suitable for 1 diabetic patients and diabetic ketoacidosis patients. 2. Rosiglitazone hydrochloride tablets (Ilicis) may lead to menopause and stop ovulation in women who ovulate again, so attention should be paid to contraception during medication. 3. During taking rosiglitazone hydrochloride tablets (Ilicis), patients should adhere to diet control and exercise. 4. If the patient has some unexplained symptoms such as nausea, vomiting, abdominal pain, fatigue, loss of appetite and dark urine during taking the medicine, he should immediately inform the doctor. When you have serious side effects (such as heart attack and congestive heart failure) when using rosiglitazone or rosiglitazone combined with insulin, you should contact your doctor. 6. People who are allergic to such drugs, as well as patients with severe liver injury and acute heart failure, are prohibited from taking such drugs.
The safety of children's medication has not been determined.
There is no need to adjust the dose of rosiglitazone hydrochloride tablets (Ilicis) for elderly patients because of their age.
The safety of medication for pregnant and lactating women has not been determined, and pregnant women and women who may be pregnant should weigh the advantages and disadvantages. Animal (rat) experiments show that rosiglitazone hydrochloride tablets (Ilicis) can migrate into milk, and breastfeeding should be avoided during taking rosiglitazone hydrochloride tablets (Ilicis).
Drug interaction 1. Drugs metabolized by cytochrome P450: In vitro drug metabolism test showed that rosiglitazone did not inhibit the main P450 enzyme at clinical dose. In vitro experimental data confirmed that rosiglitazone was mainly metabolized by CYP2C8, and a small amount was metabolized by CYP2C9. 2. Nimodipine and oral contraceptives (ethinylestradiol and norethindrone) are mainly metabolized through CYP3A4 pathway, so the combination of nimodipine and rosiglitazone hydrochloride tablets (4 mg, twice a day) has no clinical significance for the pharmacokinetics of the two drugs. 3. Glibenclamide: For diabetic patients whose condition is stable after taking glibenclamide, the combined application of rosiglitazone hydrochloride tablets (Yixixi) (2mg/ time, twice a day) and glibenclamide (3.75mg/ day to 10mg/ day) for 7 days will not change their 24-hour average steady-state blood glucose level. 4. Metformin: For healthy subjects, the combination of rosiglitazone hydrochloride tablets (irinotecan) (2mg/ time, twice a day) and metformin (500mg/ time, twice a day) for 4 days will not change the steady-state pharmacokinetic parameters of rosiglitazone hydrochloride tablets (irinotecan) and metformin. 5. Acarbose: Acarbose (65,438+000 mg/time, 3 times a day) was taken orally by healthy subjects for 7 days, which had no effect on the pharmacokinetic parameters of rosiglitazone hydrochloride tablets (Ilicis). 6. Digoxin: In healthy volunteers, continuous administration of rosiglitazone hydrochloride tablets (Ilicis) (8mg/ time, 1 time/day) 14 days has no effect on the steady-state pharmacokinetic parameters of digoxin (0.375mg/ time, 1 time/day). 7. Warfarin: Continuous administration of rosiglitazone hydrochloride tablets (Ilicis) has no effect on the steady-state pharmacokinetic parameters of warfarin enantiomers. 8. Ethanol: Patients with type 2 diabetes who take rosiglitazone hydrochloride tablets (Ilicis) will not increase the risk of acute hypoglycemia if they drink a proper amount of ethanol once. 9. Ranitidine: Ranitidine (150mg/ time, twice a day) is taken by healthy subjects for 4 days, and the pharmacokinetic parameters of rosiglitazone will not be changed after a single oral or intravenous injection. The results showed that the increase of gastrointestinal pH did not affect the oral absorption of rosiglitazone hydrochloride tablets (Ilicis).
Drug overdose According to the clinical study of volunteers, a single oral dose of rosiglitazone hydrochloride tablets (Ilicis) is less than 20mg, which is well tolerated. In the event of drug overdose, appropriate symptomatic support treatment can be given according to the patient's clinical complaint, which can generally be alleviated.
Pharmacology and Toxicology Rosiglitazone Hydrochloride Tablets (Ilicis) belong to thiazolidinedione hypoglycemic drugs, which can effectively control blood sugar by improving insulin sensitivity. Is rosiglitazone hydrochloride tablet (Ilicis) a peroxisome proliferator-activated receptor? (PPAR-？ ) is a highly selective and powerful agonist. Human PPAR receptor exists in the main target tissues of insulin, such as liver, fat and muscle. Rosiglitazone hydrochloride tablets (Ilicis) activate PPAR-? Nuclear receptors can regulate the transcription of insulin-responsive genes involved in glucose production, transport and utilization. In addition, PPAR response genes are also involved in the regulation of fatty acid metabolism. In the clinical study of rosiglitazone hydrochloride tablets (Ilicis), the results of fasting blood glucose (FPG) and HbA 1c showed that rosiglitazone hydrochloride tablets (Ilicis) could improve blood glucose control, accompanied by the decrease of blood insulin and C-peptide levels, as well as the decrease of postprandial blood glucose and insulin levels. Rosiglitazone hydrochloride tablets (Ilicis) can improve blood sugar control for 52 weeks. The main pathophysiological feature of type 2 diabetes is insulin resistance. The antidiabetic effect of rosiglitazone hydrochloride tablets (Ilixicam) has been shown in animal models of type 2 diabetes (hyperglycemia and/or abnormal glucose tolerance due to insulin resistance of target tissues). It can effectively reduce the blood sugar of Ob/0b obese mice, db/db diabetic mice and fa/faZucker obese rats, relieve their hyperinsulinemia, and delay the development of diabetes in db/db mice and Zucker obese rats. Animal studies suggest that the antidiabetic effect of rosiglitazone hydrochloride tablets (Ilicis) is achieved by improving the sensitivity of liver, muscle and adipose tissue to insulin and increasing the gene expression of insulin-regulated glucose transporter GLUT-4 in adipose tissue. In model animals with type 2 diabetes and/or abnormal glucose tolerance, rosiglitazone hydrochloride tablets (Ilicis) alone will not cause hypoglycemia. Animal toxicity: When the dosage of rosiglitazone hydrochloride tablet (Yixixi) was 3mg/kg/ day for mice, 4mg/kg/ day for rats and 2mg/kg/ day for dogs (equivalent to 5, 22 and 2 times of the recommended daily dosage AUC), the heart weight increased, and the ventricular hypertrophy was observed by morphological examination, which may be related to the increase of heart load caused by the increase of blood volume. Genotoxicity: the results of bacterial gene mutation test in vitro, chromosome aberration test of human lymphocytes in vitro, micronucleus test of mice in vivo and unscheduled DNA synthesis test of rats in vitro and in vivo were all negative. In vitro test of mouse lymphoma, the mutation rate increased slightly (about 2 times) under the condition of metabolic activation. Reproductive toxicity: the dose of rosiglitazone hydrochloride tablets (Yixixi) reached 40mg/kg/ day (equivalent to 1 16 times of AUC at the recommended daily dose), and it had no effect on the mating and fertility of male rats. Rosiglitazone hydrochloride tablets (Ilicis) can change the estrous cycle of female rats (2mg/kg/ day, equivalent to 20 times of AUC at the recommended daily dose), and reduce the fertility of female rats (40mg/kg/ day, equivalent to 200 times of AUC at the recommended daily dose), accompanied by the decrease of progesterone and estrogen in blood. At a dose of 0.2mg/kg/ day (equivalent to 3 times the AUC of the recommended daily dose), the above changes were not observed. The dosage of rosiglitazone hydrochloride tablets (Ilicis) is 0.6 mg/kg/day and 4.6mg/kg/ day (equivalent to 3 times of AUC and 15 times of the recommended daily dosage), which can reduce the serum estradiol level in follicular phase, further reduce the luteinizing hormone level and progesterone level in luteal phase, and lead to amenorrhea, which may be related to the direct inhibition of ovarian steroid hormone production by rosiglitazone hydrochloride tablets (Ilicis). Rats taking rosiglitazone hydrochloride tablets in early pregnancy have no effect on implantation and embryo. However, taking rosiglitazone hydrochloride tablets (Ilicis) in the second and third trimester of pregnancy can lead to embryo death and growth retardation in rats and rabbits. When the doses of rats and rabbits reached 3mg/kg/ day and 100mg/kg/ day respectively (20 times and 75 times of AUC at the recommended daily dose), no teratogenic effect was observed. When rats receive a dose of 3 mg/kg/day, the placenta will have pathological changes. Continuous administration during pregnancy and lactation can reduce the litter size, reduce the vitality of newborn rats and delay the growth after birth, but the growth delay can be restored after puberty. The ineffective doses of rosiglitazone hydrochloride tablets (Ilicis) to placenta, embryo/fetus and offspring of rats and rabbits were 0.2 mg/kg and 65,438 0.5 mg/kg/day, respectively, which was about four times of the recommended daily dose AUC of human body. There is no completely strictly controlled clinical research data of pregnant women. Only when the potential benefits to the fetus outweigh the potential risks can pregnant women take rosiglitazone hydrochloride tablets (Ilicis). The related substances of rosiglitazone hydrochloride tablets (Ilicis) were detected in rat milk, but it is not clear whether rosiglitazone hydrochloride tablets (Ilicis) are secreted by human milk. Because many drugs can be secreted by human milk, rosiglitazone hydrochloride tablets (Ilicis) are not suitable for lactating women. The existing data clearly suggest that abnormal blood glucose level during pregnancy can increase the incidence, morbidity and mortality of neonatal congenital malformation. Therefore, most experts recommend using insulin alone during pregnancy to maintain normal blood sugar levels as much as possible. Carcinogenicity: Rosiglitazone hydrochloride tablets (Ilicis) were given to mice for 2 years at the doses of 0.4, 1.5 and 6mg/kg/ day respectively (the high dose is equivalent to 12 times of AUC at the recommended daily dose), and no carcinogenic effect was found, but it was at 1.5mg/kg/ day. Rosiglitazone hydrochloride tablets (Ilicis) were given orally to rats for 2 years at doses of 0.05, 0.3 and 2mg/kg/ day [the high dose is equivalent to 10 times (male) and 20 times (female) of the recommended daily dose], and the incidence of benign adipose tissue tumors in rats can be significantly increased at doses of 0.3mg/kg/ day and higher. The proliferation reaction found in the above two animals is related to the excessive and lasting pharmacological effect of rosiglitazone hydrochloride tablets (Ilicis) on adipose tissue.
The absolute bioavailability of rosiglitazone is 99%. The plasma concentration of rosiglitazone tablets in healthy adults reached a high level after 1 hour, and the Cmax was about 3 19ng/ml (rosiglitazone tablets were 2mg at a time, and the Cmax was 156 ng/ml) T 1/23-.
Storage and shading, sealed preservation.
Packaging 2mg* 14 tablets/box.
Valid for 24 months.
The approval number is National Medicine Zhunzi H2004 1408.
Zhejiang wanma pharmaceutical co., ltd.
The efficacy and function of rosiglitazone hydrochloride tablets (Ilicis) are suitable for the treatment of type 2 diabetes.
Frequently asked questions about rosiglitazone hydrochloride tablets: What are the indications of rosiglitazone hydrochloride tablets (Ilicis)?