Date of approval.
Date of revision.
Calcium Hydroxybenzene Sulfonate Tablets Instructions
Please read the instructions carefully and use under the guidance of a physician
Drug Name]
Generic Name: Calcium Hydroxybenzenesulfonate Tablets
Trade Name: Calcium Dobesilate Tablets
English name: Calcium Dobesilate Tablets
Hanyu Pinyin: Qiangbenhuangsuangai Pian
Ingredients
The main ingredient of this product is calcium hydroxybenzenesulfonate.
Chemical name: Calcium 2,5-dihydroxybenzenesulfonate monohydrate
Chemical structure formula.
Molecular formula: C12H10CaO10S2-H2O
Molecular weight: 436.42
Properties
This product is white or off-white tablet.
【Indications】.
1. Treatment of microangiopathy.
Diabetic microangiopathy — retinopathy and glomerulosclerosis (Ki- wi syndrome).
Microvascular injury — with increased capillary fragility and permeability, capillary disease, hand and foot cyanosis.
2. for the adjuvant treatment of chronic venous insufficiency (varicose vein syndrome) and its sequelae (post-embolism syndrome, leg ulcers, purpura dermatitis and other depressive skin diseases, peripheral vascular depressive edema, etc.).
Specification
0.5g (based on C12H10CaO10S2-H2O).
Dosage]
Diabetic retinopathy: 1 tablet once, 3 times a day (once in the morning, once in the afternoon and once in the evening).
Other indications: 1 tablet once, 2 times a day (once in the morning and once in the evening). If the clinical symptoms improve, omit taking the drug once in the evening (after about one month of taking the drug).
[Adverse reactions].
Regarding the frequency of occurrence defined as follows.
Very common (≥1/10); common (≥1/100, <1/10); rare (≥1/1000, <1/100); rare (≥1/10,000, <1/1000); very rare (<1/10,000); unclear (cannot be assessed based on available data).
Immune system disorders: rare: hypersensitivity reactions (including rash, atopic dermatitis, pruritus, urticaria, facial edema); very rare: allergic reactions.
Neurological disorders: common: headache.
Gastrointestinal disorders: common: abdominal pain, diarrhea, nausea, vomiting.
Bone and connective tissue disorders: common: arthralgia, myalgia.
Systemic diseases and administration site conditions: rare: fever, chills, malaise, fatigue.
Abnormal test results: common: elevated alanine aminotransferase. These reactions are reversible once the drug is discontinued.
Post-marketing spontaneous reports: blood and lymphatic system disorders: granulocyte deficiency, neutropenia, leukopenia.
[Contraindications].
Hypersensitivity to any of the ingredients of this product.
Precautions】
Dosage should be reduced in patients with severe renal insufficiency requiring dialysis.
In very rare cases, calcium hydroxybenzenesulfonate may cause granulocyte deficiency. In such cases, symptoms including high fever, oral infections (tonsillitis), sore throat, anal and genital inflammation and other common infections may occur and should be discontinued as soon as these symptoms develop during treatment and blood composition and leukocyte picture should be evaluated immediately.
Calcium hydroxybenzenesulfonate may induce severe hypersensitivity reactions (allergic reactions or shock) and should be discontinued immediately if this condition occurs.
Calcium hydroxybenzenesulfonate does not affect driving or use of machinery.
For Pregnant and Lactating Women]
Since it is not clear whether calcium hydroxybenzenesulfonate crosses the human placental barrier, the advantages and disadvantages of using this drug should be weighed. Calcium hydroxybenzenesulfonate may be present in trace amounts in breast milk (0.4μg/ml in breast milk after administration of 1500mg). It is prudent to discontinue the drug or discontinue breastfeeding.
Pediatric Use]
Safety data for children have not been established.
Geriatric use]
This product is indicated for elderly patients. No data on dose adjustment due to advanced age have been established.
Drug Interactions]
No interactions with other drugs have been identified. The use of therapeutic doses of calcium hydroxybenzoate may interfere with the determination of creatinine (at very low values) (PAP method).
Drug overdose]
Not yet known.
Pharmacology and Toxicology
Pharmacological effects: As a vasoprotective agent, it acts mainly in the following three aspects.
1) microvascular wall —- increasing resistance and reducing its pathological hyperpermeability.
2) In blood flow —- reduces blood and plasma viscosity, decreases platelet hypercoagulability and prevents thrombosis.
3) In microvascular lesions, the product eliminates or alleviates their clinical signs (edema, capillary oozing, heaviness and pressure sensation in the lower extremities).
Toxicology: The LD50 value of intravenous administration in mice is about 715mg/kg, and the LD50 value of oral administration in mice and rats< 4000mg/kg. embryotoxicity and mutagenicity experiments show no toxicity.
Pharmacokinetics]
After oral administration of 500 mg of calcium hydroxybenzenesulfonate, the blood concentration level was above 6 μg/ml during the 3rd and 10th hours, and the maximum blood concentration (Cmax) was reached after 6 hours (tmax) with a mean of 8 μg/ml. 24 hours after administration, the blood concentration was about 3 μg/ml. the protein binding rate was 20-25%. Animal studies have shown that calcium hydroxybenzenesulfonate does not cross the blood-brain or placental barriers, but it is unclear whether the same is true in humans. Trace amounts may be present in breast milk (0.4 μg/ml in breast milk after administration of 1500 mg was observed in one study). Calcium hydroxybenzenesulfonate does not enter the enterohepatic circulation and is excreted mainly in its original form, with only 10% excreted as metabolites. Approximately 50% of the oral dose is excreted in the urine and approximately 50% is excreted in the feces within 24 hours of dosing.
The plasma half-life is around 5 hours.
Kinetics in Special Clinical Situations: It is not clear what degree of renal dysfunction affects the pharmacokinetic properties of calcium hydroxybenzenesulfonate.
Storage】 Keep sealed.
Package】 Aluminum-plastic package, 10 tablets/plate/box; 10 tablets/plate×2 plates/box; 10 tablets/plate×3 plates/box.
Expiration date】 24 months.
Execution Standard
【Approval number】 State Drug Certificate H20030087
[Drug Marketing Licensee
Name: Nanjing Chang’ao Pharmaceutical Co.
Registered Address: No. 63, Kexin Road, Jiangbei New District, Nanjing
Postal Code: 211505
Telephone number: 025-68161999
Fax number: 025-68161009
Web address: www.changao.com
Manufacturer
Company name: Nanjing Chang’ao Pharmaceutical Co.
Address: No. 63, Kexin Road, Jiangbei New District, Nanjing
Postal Code: 211505
Telephone number: 025-68161999
Fax number: 025-68161009
Web address: www.changao.com