Aceclofenac Sustained Release Tablets
This product is a non-steroidal anti-inflammatory drug with anti-inflammatory and analgesic effects. Its mechanism of action is mainly through the inhibition of cyclooxygenase activity, thereby reducing prostaglandin synthesis.
Key words:
Aceclofenac Sustained Release Tablets
Classification:
Hotline:
Graphic Details
Approval date: January 4, 2009
First revision date: March 10, 2009
Second revision date: May 05, 2015
Third revision date: October 19, 2020
[Name of Drug]
Common Name: Aceclofenac Sustained Release Tablets
English name:Aceclofenac Sustained-release Tablets
Chinese pinyin:Culvfensuan Huanshi Pian
[Ingredients]:The main ingredients of this product are: Aceclofenac
Chemical Name: 2-[(2), 6-Dichlorophenyl) amino]-phenylacetoxyacetic acid
ChemistryStructural formula:
Molecular formula: C16H13Cl2NO4
Molecular weight: 354.19
[Traits]This product is white or almost white film
[Pharmacology and Toxicology]
1. Pharmacological action
This product is a non-steroidal anti-inflammatory drug with anti-inflammatory and analgesic effects. Its mechanism of action is mainly through the inhibition of cyclooxygenase activity, thereby reducing prostaglandin synthesis.
2. Toxicological Studies
Repeated dose toxicity: Continuous oral administration in rats 1months, the dose was 1550 and 100 mg/kg/day. As a result, only the 100 mg/kg/day group died with fecal occult blood. Histopathological examination showed that the animals in this group had gastric or intestinal mucosal irritation. Similar to other non-steroidal anti-inflammatory drugs, the test animals were poorly tolerated. In addition, the difference in pharmacokinetics between animals and humans makes it difficult to judge its potential toxicity. However, the toxicological test results of rats (which can metabolize aceclofenac to diclofenac) and monkeys (some unmetabolized prototype drugs) administered at the maximum tolerated dose show that this product has no toxic effects other than the common toxicity of non-steroidal anti-inflammatory drugs.
Genotoxicity: The result of genotoxicity test was negative.
Reproductive toxicity: It has been reported that the inhibition of prostaglandin synthesis by anti-inflammatory drugs may lead to severe embryotoxicity. Can inhibit uterine contractions, resulting in delayed labor. It can cause stenosis or closure of fetal ductus arteriosus in utero, resulting in neonatal pulmonary hypertension and respiratory insufficiency. Anti-inflammatory drugs can also inhibit fetal platelet function and affect its renal function, resulting in oligohydramnios and neonatal anuria. Therefore, the use of anti-inflammatory drugs is prohibited in the last trimester of pregnancy. However, it has been reported in the literature that this product will also affect fetal hair in the middle and early stages of pregnancy. It is not known whether this product is excreted in human milk, so women who are breastfeeding should not use this product unless the doctor deems it necessary.
Carcinogenicity: Carcinogenicity studies in mice and rats did not show any carcinogenic effect.
[pharmacokinetics]
(I)BeaglePharmacokinetics in dogs
Single dose gavage 200mgAfter this sustained-release tablet Tmax,T1/2,MRT,CmaxRespectively: 5.0±2.7h,6.03±1.95h,9.79±1.71h,61.36±20.75mg/Ml. The corresponding value of Aceclofenac ordinary tablets is: 2.3±0.6h,4.97±1.95h,7.41±1.90h,81.35±15.63mg/Ml. This product has a sustained release effect. and the AUC of both preparations24and AUCBioequivalent with a relative bioavailability of 91.42±11.17%.
Multiple doses of gavage (200mg/Day, 5.days), there was no significant difference between the peak concentration, plateau concentration, valley concentration and fluctuation coefficient of the slow-release tablet and the ordinary tablet of aceclofenac, and the relative bioavailability in the steady state was 93.4.
(II)human pharmacokinetics
A single dose of oral aceclofenac sustained-release tablets, the blood concentration changes over time, in line with the first-order absorption of a compartment model. The main pharmacokinetic parameters were: T1/2Ka(h)=1.30±0.39,T1/2Ke(h)=4.66±0.29,Tmax(h)=4.00±0.46,Cmax(μg·mL-1)=10.87±1.04, MRI (h)= 7.52 ± 0.40,AUC0~24(μg·h-1·mL-1)=73.23± 10.35,AUC0~ ∞(μg·h-1·mL-1)=81.81± 11.00. Multiple doses of oral aceclofenac sustained-release tablets, for 9 consecutive days to achieve steady-state blood concentration, over the course of blood concentration changes, in line with the first-order absorption of a compartment model. The main pharmacokinetic parameters on day 9 were: T1/2Ka(h)=1.33±0.27,T1/2Ke= 4.64 ± medium 0.29,Tmax(h) =3.40±0.50,Cmax(μg·mL-1)=14.41±1.34,Cmin (μg·mL-1)=0.97±0.19, MRI (h)= 7.15 ± 0.31,AUCSS(μg·h-1·mL-1)=100.60±14.81,CHunting(μg·mL-1)=4.19±0.62,DF(%)=323.98±31.86。
[Indications]
Treatment of symptoms of pain and inflammation caused by osteoarthritis, rheumatoid arthritis and ankylosing spondylitis.
[Specifications]:0.2g
[Usage Dosage]
Oral: must be swallowed whole, do not chew. Each 0.2g (one piece)Once daily, or as directed by a doctor.
[Adverse Reaction]
According to the results of clinical trials and related literature reports, the adverse reactions of this product are:
1Common adverse reactions
Gastrointestinal system disorders: dyspepsia, abdominal pain, nausea and diarrhea.
Liver and gallbladder: elevated liver enzymes
2Occurrence of adverse reactions (incidence rate 1%-0.1%)
Usually for dizziness. Gastrointestinal system: flatulence, gastritis, constipation, vomiting, ulcerative oral mucositis. Skin: itching, rash, dermatitis, eczema. Metabolism and nutrition: increased urea nitrogen and creatinine.
3, rare adverse reactions (incidence less than 0.1%)
Headache, fatigue, facial swelling, allergic symptoms, weight gain. Blood: anemia, granulocytopenia, thrombocytopenia, neutropenia. Cardiovascular: edema, palpitations, gastrocnemius spasm, flushing, purpura. Urinary system: interstitial nephritis. Central and peripheral nervous system: sensory disturbance, tremor. Disorders of the gastrointestinal systemGastrointestinal bleeding and ulcers, hemorrhagic diarrhea, hepatitis or pancreatitis, tarry stool, oral mucosal inflammation. Skin: Eczema. Metabolism and nutrition: increased alkaline phosphatase, hyperkalemia.
Psychiatry: depression, dreaminess, lethargy, insomnia. Eyes: visual abnormalities.
Other: wrong taste, vasculitis.
As with other NSAIDs, severe mucocutaneous hypersensitivity reactions may occur.
[Taboo]
Prohibited in the following patients:
1.Known allergic to this product;
2.Patients taking non-steroidal anti-inflammatory drugs with similar mechanism of action such as aspirin, diclofenac, etc. cause asthma, bronchospasm, acute rhinitis;
3.Patients with or suspected of having gastric or duodenal ulcers, or patients with a history of recurrence of gastric or duodenal ulcers, gastrointestinal bleeding or other bleeding or coagulation disorders;
4.Suffering from severe heart failure, liver and kidney dysfunction;
5.Pregnancy last 3Prohibited during the month of pregnant women.
[Notes]
1.Oral must be swallowed whole, do not chew. Chewing will affect the sustained release effect and increase the possibility of side effects.
2.Patients with gastrointestinal diseases or peptic ulcer, cerebrovascular hemorrhage, ulcerative colitis, Crobn’sSystemic lupus erythematosus (SLE)Use with caution or under close monitoring in patients with a history of porphyria and hematopoiesis and coagulation disorders;
3.Mild, moderate liver, kidney, heart dysfunction and fluid retention, diuretic treatment or other patients with the same risk of hypovolemia should be used with caution;
4.Patients with dizziness and other disorders of the central nervous system after taking non-steroidal anti-inflammatory drugs should avoid driving or engaging in mechanical operations;
5.Patients taking nonsteroidal anti-inflammatory analgesics for a long time should be checked frequently to prevent adverse effects on liver and kidney function and blood cell count.
[Medication for pregnant and lactating women]
Anti-inflammatory drugs may block uterine contractions and delay labor. They may cause constriction and atresia of intrauterine arterial ducts, leading to neonatal pulmonary hypertension and respiratory insufficiency. Anti-inflammatory drugs may also reduce fetal platelet function and inhibit fetal renal function, causing oligohydramnios and neonatal anuria. Therefore, pregnant women in the last three months of pregnancy to disable this product. It is not clear whether this product is secreted into breast milk, so women should not use this product during breastfeeding unless the doctor deems it necessary.
[Children's Medication]
The safety and effectiveness of the drug in children have not been established, so it is not recommend to children.
[medication in elderly patients]
There is generally no need to lower the dose. However, elderly patients are more likely to have side effects and are more likely to cause kidney, cardiovascular and liver damage. During treatment, many times patients have no previous symptoms or obvious history, resulting in severe gastrointestinal bleeding and/or/Or perforated, should be used with caution.
[drug interaction]
1.Avoid use with the following drugs:
Non-steroidal anti-inflammatory drugs can inhibit the secretion of methotrexate in the renal tubules, which may have a slight metabolic interaction, resulting in a decrease in methotrexate clearance. Therefore, non-steroidal anti-inflammatory drugs should always be avoided during high-dose methotrexate treatment.
Some non-steroidal anti-inflammatory drugs can inhibit the elimination process of lithium salt in the kidney and increase the concentration of lithium in the blood. It should be avoided in combination with lithium salt. If necessary, it should be ensured that the level of lithium in serum can be measured frequently.
Non-steroidal anti-inflammatory drugs can inhibit platelet aggregation and damage the gastrointestinal mucosa, can increase the activity of anticoagulant drugs, resulting in the tendency of gastrointestinal bleeding in patients with anticoagulant drugs. The combination of coumarin with oral anticoagulants, ticlopidine, thrombolytic agents and heparin should be avoided.
2.This product and the following drugs need to adjust the dose or double the attention:
In the use of this product, even if the use of low-dose methotrexate, should also pay attention to their possible drug interactions, especially in patients with renal insufficiency, if 24The use of these two drugs within hours should be more vigilant, because the blood concentration of methotrexate may increase and lead to increased toxicity.
Non-steroidal anti-inflammatory drugs are used together with cyclosporine or tacolium, because the former will reduce the synthesis of renal prostaglandins and increase the risk of nephrotoxicity, so the renal function should be closely monitored when combined with drugs.
Taking this product and aspirin or other non-steroidal anti-inflammatory drugs at the same time will increase the risk of side effects and should be vigilant.
Non-steroidal anti-inflammatory drugs can weaken the diuretic effect of some diuretics such as furan aniline acid and butyric acid, and also reduce the antihypertensive effect of thiazide diuretics. Simultaneous use with potassium-preserving diuretics can increase potassium level, so potassium should be monitored. Non-steroidal anti-inflammatory drugs and ACE (angiotensin converting enzyme)Simultaneous use of inhibitors increases the risk of acute renal failure in patients with water loss.
This product and benzfluorothiazide (diuretic antihypertensive drugs)The effect of blood pressure control was found at the end of the combination. However, it cannot be ruled out that this product and other antihypertensive drugs suchβ-Interaction with the combined use of receptor antagonists.
It has been reported that this product may cause hypoglycemia, and the dosage of hypoglycemic drugs should be adjusted when used.
3.This product is mainly P4502C9 by cytochromeMetabolism, and therefore possible risk of drug interactions with phenytoin, digoxin, cimetidine, tolbutamide, phenylbutazone, amiodarone, miconazole, and sulfaphenopyrazole.
Since this product is almost completely combined with plasma protein, those drugs with high protein binding rate may be replaced by this product, so it should be noted and monitored.
[Overdose]
There are no study data on human overdose use of this product. Symptoms that may occur after overdose are nausea, vomiting, stomach pain, dizziness, drowsiness and headache. At this time, if necessary, gastric lavage, administration of activated charcoal, if necessary, the use of antacids or other symptomatic treatment.
[Storage] Seal and store in a dry place.
[Packaging]Aluminum plastic packaging, 6Pieces/Plate, 1 plate/box; 6 pieces/plate. 2 plates/box; 12 pieces/plate, 1 plate/box.
[Validity]24Months
[Executive Standards]YBH00212009
[Approval No.]Chinese medicine quasi-word H20090011
[Drug Marketing Authorization Holder]
Name: Zhejiang Jianfeng Pharmaceutical Co., Ltd.
Registered Address: 2nd Floor, Office Quality Inspection Building, X02, No.58 Gaofan Section, Baisha Downline, Wucheng District, Jinhua City, Zhejiang Province
[production enterprises]
Company: Zhejiang Jianfeng Pharmaceutical Co., Ltd.
Production address: No.58, Gaofan Section, Baitang Lower Line, Wucheng District, Jinhua City, Zhejiang Province
Postal Code: 321075
Related Products
Welcome your message consultation