导升明 胶囊 Doxium
制造商 依比威
性状
每胶囊含500 mg羟苯磺酸钙，即2,5-二羟基苯磺酸钙。
药理作用
本药可减低微血管壁的通透性，促进淋巴循环。降低血液及血浆粘稠度，纠正白蛋白/球蛋白比值，降低血小板的高聚集性，从而防止血栓形成，并提高红细胞柔韧性。还可抑制血管活性物质(组织胺、5-羟色胺、缓激肽、透明质酸酶、前列腺素等)对微血管引起的高通透作用，减少内皮损伤，改善基底膜胶原的生物合成，从而起到保护血管的作用。
适应症
糖尿病性视网膜病及肾小球硬化症(基-威二氏综合征)，非糖尿病性微血管病变 ：如突发性或长期使用香豆素衍生物、细胞抑制剂、口服避孕药或其它药物促发的微血管病变 ；与慢性器质性疾病(如高血压、动脉硬化和肝硬变)相关的微循环障碍。原发性静脉曲张引起疼痛、腿痛、肌肉痛性痉挛，感觉异常，手足发绀，紫癜性皮炎。静脉曲张状态，出现慢性静脉功能不全，静脉炎及表浅性血栓性静脉炎，血栓后综合征，静脉曲张性溃疡，妊娠性静脉曲张。痔疮综合征，还可作为静脉剥离和静脉硬化法的辅助治疗，术后综合征，水肿及组织浸润的治疗。
用法用量
静脉曲张综合征及静脉功能不全 1 g/日，疗程1-3周，糖尿病性视网膜病变 1-1.5 g/日，疗程4-6月，各种微血管病 1-1.5 g/日，疗程1-2月。进餐时吞服，勿嚼。
不良反应
极少病例，尤在大剂量时可有胃部不适、恶心、胃灼热及厌食，罕见变态反应。
禁忌症
对本药任何成分过敏。
孕妇及哺乳期妇女用药
在实验研究中并无致畸作用，也不能通过胎盘。为谨慎起见，不要使用于妊娠头3个月及哺乳期。
贮藏/有效期
阴凉、干燥处放置，避免光照。
Doxium ®500
Product Monograph
Doxium ®500 contains calcium dobesilate as active principle. It acts by normalizing the resistance and permeability of the vascular wall of capillaries and improves venous blood flow.
Doxium ®500 improves blood flow disorders in retinal vessels in case of diabetic retinopathy, as well as in skin diseases linked to chronic venous diseases and haemorrhoids.
Properties/Effects
Calcium dobesilate acts on the capillary walls by regulating their impaired physiological functions - increased permeability and decreased resistance.
It increases erythrocyte flexibility, inhibits platelet hyperaggregation and, in diabetic retinopathy, it reduces plasma and blood hyperviscosity, thus improving blood rheological properties and tissue irrigation.
These effects allow to correct capillary dysfunctions either of functional origin or caused by constitutional or acquired metabolic disorders.
Calcium dobesilate contributes to reduce oedema.
Composition
Active principle: calcium dobesilate
Capsule: calcium dobesilate 500 mg. Colour. (E 132), excipients for capsule.
Pharmacokinetics
After oral administration of 500 mg of calcium dobesilate, its blood level is above 6 μg/ml between the 3rd and 10th hour, with a maximum (Cmax) of 8 μg/ml on the average after 6 hours (tmax). Twenty four hours after intake blood level is about 3 μg/ml. The rate of protein-binding is 20 - 25 %. In animals, calcium dobesilate does not cross the haematoencephalic or the placental barrier, but it is not known whether this is also the case in humans. Calcium dobesilate enters the maternal milk in very low quantities (0,4 μg/ml after intake of 1500 mg as observed in one study).
Calcium dobesilate does not enter the enterohepatic cycle and is excreted mainly unchanged with only 10 % being excreted as metabolites.
About 50 % of the orally administered dose are eliminated in the first 24-hour urine and about 50 % in the faeces.
Plasma half-life is around 5 hours.
Kinetics in particular clinical situations
It is not known to what extent renal function disorders influence the pharmacokinetic properties of calcium dobesilate (see "Precautions").
Indications
•
Microangiopathies, in particular diabetic retinopathy.
•
Clinical signs of chronic venous insufficiency in the lower limbs (pain, cramps, paresthesia, oedema, stasis dermatosis), as adjuvant in superficial thrombophlebitis.
•
Haemorrhoidal syndrome, microcirculation disorders of arteriovenous origin.
Dosage and administration
Generally 1000 mg - 2 Capsules 500 mg Per Day- to be taken with the main meals.
Treatment duration, which is generally between a few weeks and several months, depends on the disease and its evolution.
Dosage should be adapted individually according to the severity of the case.
Limitations for use
Contraindications
Hypersensitivity towards calcium dobesilate and/or sulfites.
Precautions
Dosage should be reduced in case of severe renal insufficiency requiring dialysis.
In very rare cases (0.32/million patients), incidence estimated on the basis of spontaneous reports, the intake of calcium dobesilate may induce agranulocytosis, probably linked to a hypersensitivity reaction. This condition may be expressed by symptoms such as high fever, oral cavity infections (tonsillitis), sore throat, anogenital inflammation and accompanying symptoms, that are often signs of an infection. The patient should be told that by any sign of infection he/she must immediately inform his/her physician. In that case, it is essential to control without delay the blood formula and leucogram and to discontinue the treatment.
Pregnancy and lactation
Pregnancy category C: studies in pregnant women or animals are not available. As it is not known whether calcium dobesilate crosses the placental barrier in humans, the drug should only be administered if the potential benefit justifies the potential risk to the foetus. Calcium dobesilate enters the maternal milk in very low quantities (0,4 μg/ml after intake of 1500 mg). As a precaution, either the treatment or the breast-feeding should be stopped.
Adverse effects
Rarely gastrointestinal disorders including nausea and diarrhoea, skin reactions and fever have been reported.
In case of gastrointestinal disorders, the dosage should be reduced or the treatment temporarily withdrawn.
In case of skin reactions and fever, the treatment must be stopped and the treating physician informed as this may constitute an allergic reaction.
Doxium tablets contain sodium bisulfite as antioxidant which may cause allergic reactions, nausea and diarrhea in predisposed patients. These allergic reactions may lead to anaphylactic shock and life-threatening asthma attacks. The prevalence in the general population is not known, but is probably low.
However, sulfite hypersensitivity is observed more frequently in asthmatics than in non-asthmatics (see "Contraindications").
In case of hypersensitity reactions, the intake of Doxium tablets must be stopped immediately.
Interactions
No interaction is known up to now.
Particular remarks
Incompatibilities
No incompatibility is known up to now.
Information
At therapeutic doses, calcium dobesilate may interfere with the assay of creatinine (too low values).
Presentation
Capsules (500 mg): packs of 30 capsules