Calcium dobesilate: Difference between revisions
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== Chemistry == |
== Chemistry == |
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The compound appears as a white [[hygroscopic]] powder . Very soluble in water and easily soluble in [[ethanol|alcohol]], it is practically insoluble in [[dichloromethane]] and poorly soluble in [[2-propanol|isopropyl alcohol]]. At the concentration of 10% the aqueous solution has a [[pH]] of between 4.5 and 6.0. |
The compound appears as a white [[hygroscopic]] powder . Very soluble in water and easily soluble in [[ethanol|alcohol]], it is practically insoluble in [[dichloromethane]] and poorly soluble in [[2-propanol|isopropyl alcohol]]. At the concentration of 10% the aqueous solution has a [[pH]] of between 4.5 and 6.0.{{Citation needed|date=March 2020}} |
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== Pharmacodynamics == |
== Pharmacodynamics == |
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The molecule has the property of optimizing the microcirculatory function. In fact, it reduces capillary permeability both by stabilizing the basement membrane for an action on the collagen chains that constitute it, and by interacting with different biochemical mediators that favor endothelial permeability itself. In this way it favors a reduction in blood hyperviscosity and also performs an anti- platelet aggregation action |
The molecule has the property of optimizing the microcirculatory function. In fact, it reduces capillary permeability both by stabilizing the basement membrane for an action on the collagen chains that constitute it, and by interacting with different biochemical mediators that favor endothelial permeability itself. In this way it favors a reduction in blood hyperviscosity and also performs an anti- platelet aggregation action.{{Citation needed|date=March 2020}} |
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== Pharmacokinetics == |
== Pharmacokinetics == |
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Calcium dobesilate after oral administration is well absorbed from the gastrointestinal tract . Maximum plasma concentrations (C max ) of 6-8 µg / ml are reached approximately six hours after oral administration of 500 mg, which are generally maintained for over 12 hours. In the body the drug is poorly metabolized (less than 10%) and its binding with plasma proteins is rather low. Elimination occurs mainly through excretion from the renal excretion |
Calcium dobesilate after oral administration is well absorbed from the gastrointestinal tract . Maximum plasma concentrations (C max ) of 6-8 µg / ml are reached approximately six hours after oral administration of 500 mg, which are generally maintained for over 12 hours. In the body the drug is poorly metabolized (less than 10%) and its binding with plasma proteins is rather low. Elimination occurs mainly through excretion from the renal excretion.{{Citation needed|date=March 2020}} |
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== Clinical uses == |
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Calcium dobesilate is indicated in states of fragility and altered capillary permeability and in diabetic retinopathy.<ref name="pmid15230646">{{cite |
Calcium dobesilate is indicated in states of fragility and altered capillary permeability and in diabetic retinopathy.<ref name="pmid15230646">{{cite journal | last = Allain | first= H. | author2= AA. Ramelet; E. Polard; D. Bentué-Ferrer|url=https://pubmed.ncbi.nlm.nih.gov/15230646/ | title = Safety of calcium dobesilate in chronic venous disease, diabetic retinopathy and haemorrhoids. | journal= Drug Saf | volume = 27 | number = 9 | page = 649-60 | year = 2004 | pmid = 15230646 }}</ref> In combination with lidocaine or with lidocaine and dexamethasone, the drug enters the composition of preparations for the therapy of hemorrhoidal disease. In association with potassium hydrodex-sulfate enters the composition of adjuvant gels in the treatment of varicose veins. The efficacy of calcium dobesilate has been described e.g. in patients with diabetic retinopathy.<ref>{{cite journal |last1=Zhang |first1=XinYuan |last2=Liu |first2=Wei |last3=Wu |first3=ShanShan |last4=Jin |first4=JingLong |last5=Li |first5=WeiHong |last6=Wang |first6=NingLi |title=Calcium dobesilate for diabetic retinopathy: a systematic review and meta-analysis |journal=Science China Life Sciences |date=1 January 2015 |volume=58 |issue=1 |pages=101–107 |doi=10.1007/s11427-014-4792-1 |url=https://link.springer.com/article/10.1007%2Fs11427-014-4792-1 |language=en |issn=1869-1889}}</ref><ref>{{cite journal |last1=Haller |first1=Hermann |last2=Ji |first2=Linong |last3=Stahl |first3=Klaus |last4=Bertram |first4=Anna |last5=Menne |first5=Jan |title=Molecular Mechanisms and Treatment Strategies in Diabetic Nephropathy: New Avenues for Calcium Dobesilate—Free Radical Scavenger and Growth Factor Inhibition |journal=BioMed Research International |date=2017 |doi=10.1155/2017/1909258 |url=https://www.hindawi.com/journals/bmri/2017/1909258/}}</ref> |
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In combination with lidocaine or with lidocaine and dexamethasone, the drug enters the composition of preparations for the therapy of hemorrhoidal disease . [1] [8] [9] |
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In association with potassium hydrodex-sulfate enters the composition of adjuvant gels in the treatment of varicose veins . [10] [11] [12] [13] [14] |
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Calcium dobesilate is also indicated for the specific treatment of microangiopathy. The efficacy of calcium dobesilate has been described e.g. in patients with [https://link.springer.com/article/10.1007%2Fs11427-014-4792-1 diabetic retinopathy]<ref>Zhang, XinYuan; Liu, Wei; Wu, ShanShan; Jin, JingLong; Li, WeiHong; Wang, NingLi (2014-12-20). "Calcium dobesilate for diabetic retinopathy: a systematic review and meta-analysis". Science China Life Sciences. 58 (1): 101–107. doi:10.1007/s11427-014-4792-1. ISSN 1674-7305. {{PMID|25528255}}.</ref> or [https://www.hindawi.com/journals/bmri/2017/1909258/ diabetic nephropathy].<ref>Haller, Hermann; Ji, Linong; Stahl, Klaus; Bertram, Anna; Menne, Jan (2017). "Molecular Mechanisms and Treatment Strategies in Diabetic Nephropathy: New Avenues for Calcium Dobesilate—Free Radical Scavenger and Growth Factor Inhibition". BioMed Research International. 2017: 1909258. doi:10.1155/2017/1909258. ISSN 2314-6133. PMC 5634607. {{PMID|29082239}}. </ref> |
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== Side effects == |
== Side effects == |
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During treatment, gastrointestinal disorders can be observed: dyspepsia, nausea, vomiting, diarrhea . These disorders generally regress with the simple decrease in the dose taken, or with the temporary suspension of the treatment. Other adverse events related to hypersensitivity reactions have also been reported : among these skin rashes, skin rash, fever, arthralgia (joint pain). Rare cases of agranulocytosis have also been reported in medical literature |
During treatment, gastrointestinal disorders can be observed: dyspepsia, nausea, vomiting, diarrhea . These disorders generally regress with the simple decrease in the dose taken, or with the temporary suspension of the treatment. Other adverse events related to hypersensitivity reactions have also been reported : among these skin rashes, skin rash, fever, arthralgia (joint pain). Rare cases of agranulocytosis have also been reported in medical literature. The rarity of the latter adverse effect led several authors to conclude that perhaps there could have been methodological errors in risk assessments.{{Citation needed|date=March 2020}} |
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The rarity of the latter adverse effect led several authors to conclude that perhaps there could have been methodological errors in risk assessments. [20] |
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== Contraindications == |
== Contraindications == |
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The drug is contraindicated in subjects with known hypersensitivity to the active ingredient or to any of the inactive ingredients contained in the pharmaceutical formulation. |
The drug is contraindicated in subjects with known hypersensitivity to the active ingredient or to any of the inactive ingredients contained in the pharmaceutical formulation. |
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It is also contraindicated in women who are pregnant and breastfeeding |
It is also contraindicated in women who are pregnant and breastfeeding.{{Citation needed|date=March 2020}} |
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== Therapeutic doses == |
== Therapeutic doses == |
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Calcium dobesilate is administered orally at a daily dose of 1-1.5 g (equivalent to 2-3 tablets). It can also be administered rectally in the case of hemorrhoidal disease |
Calcium dobesilate is administered orally at a daily dose of 1-1.5 g (equivalent to 2-3 tablets). It can also be administered rectally in the case of hemorrhoidal disease.{{Citation needed|date=March 2020}} |
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==References== |
==References== |
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Revision as of 17:55, 24 March 2020
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| Clinical data | |
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| AHFS/Drugs.com | International Drug Names |
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| CompTox Dashboard (EPA) | |
| ECHA InfoCard | 100.039.559 |
| Chemical and physical data | |
| Formula | Ca(C6H5O5S)2 |
| Molar mass | 418.4098 g/mol |
| 3D model (JSmol) | |
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Calcium dobesilate is a vasoprotective. It is the calcium salt of dobesilic acid. It is a synthetic molecule with the ability to reduce capillary permeability in the body. In Italy the drug is sold by the pharmaceutical company OM Pharma under the trade name of Doxium in capsules containing 500 mg of active ingredient.
Chemistry
The compound appears as a white hygroscopic powder . Very soluble in water and easily soluble in alcohol, it is practically insoluble in dichloromethane and poorly soluble in isopropyl alcohol. At the concentration of 10% the aqueous solution has a pH of between 4.5 and 6.0.[citation needed]
Pharmacodynamics
The molecule has the property of optimizing the microcirculatory function. In fact, it reduces capillary permeability both by stabilizing the basement membrane for an action on the collagen chains that constitute it, and by interacting with different biochemical mediators that favor endothelial permeability itself. In this way it favors a reduction in blood hyperviscosity and also performs an anti- platelet aggregation action.[citation needed]
Pharmacokinetics
Calcium dobesilate after oral administration is well absorbed from the gastrointestinal tract . Maximum plasma concentrations (C max ) of 6-8 µg / ml are reached approximately six hours after oral administration of 500 mg, which are generally maintained for over 12 hours. In the body the drug is poorly metabolized (less than 10%) and its binding with plasma proteins is rather low. Elimination occurs mainly through excretion from the renal excretion.[citation needed]
Clinical uses
Calcium dobesilate is indicated in states of fragility and altered capillary permeability and in diabetic retinopathy.[1] In combination with lidocaine or with lidocaine and dexamethasone, the drug enters the composition of preparations for the therapy of hemorrhoidal disease. In association with potassium hydrodex-sulfate enters the composition of adjuvant gels in the treatment of varicose veins. The efficacy of calcium dobesilate has been described e.g. in patients with diabetic retinopathy.[2][3]
Side effects
During treatment, gastrointestinal disorders can be observed: dyspepsia, nausea, vomiting, diarrhea . These disorders generally regress with the simple decrease in the dose taken, or with the temporary suspension of the treatment. Other adverse events related to hypersensitivity reactions have also been reported : among these skin rashes, skin rash, fever, arthralgia (joint pain). Rare cases of agranulocytosis have also been reported in medical literature. The rarity of the latter adverse effect led several authors to conclude that perhaps there could have been methodological errors in risk assessments.[citation needed]
Contraindications
The drug is contraindicated in subjects with known hypersensitivity to the active ingredient or to any of the inactive ingredients contained in the pharmaceutical formulation. It is also contraindicated in women who are pregnant and breastfeeding.[citation needed]
Therapeutic doses
Calcium dobesilate is administered orally at a daily dose of 1-1.5 g (equivalent to 2-3 tablets). It can also be administered rectally in the case of hemorrhoidal disease.[citation needed]
References
- ^ Allain, H.; AA. Ramelet; E. Polard; D. Bentué-Ferrer (2004). "Safety of calcium dobesilate in chronic venous disease, diabetic retinopathy and haemorrhoids". Drug Saf. 27 (9): 649-60. PMID 15230646.
{{cite journal}}: CS1 maint: multiple names: authors list (link) - ^ Zhang, XinYuan; Liu, Wei; Wu, ShanShan; Jin, JingLong; Li, WeiHong; Wang, NingLi (1 January 2015). "Calcium dobesilate for diabetic retinopathy: a systematic review and meta-analysis". Science China Life Sciences. 58 (1): 101–107. doi:10.1007/s11427-014-4792-1. ISSN 1869-1889.
- ^ Haller, Hermann; Ji, Linong; Stahl, Klaus; Bertram, Anna; Menne, Jan (2017). "Molecular Mechanisms and Treatment Strategies in Diabetic Nephropathy: New Avenues for Calcium Dobesilate—Free Radical Scavenger and Growth Factor Inhibition". BioMed Research International. doi:10.1155/2017/1909258.
{{cite journal}}: CS1 maint: unflagged free DOI (link)
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