Calcium Dobesilate

Calcium Dobesilate is a Capillary-protective agent belonging to the pharmacological class of Venotonics or Vasculoprotectives

Calcium Dobesilate has been approved to relieve symptoms and also for the treatment and maintenance of Chronic Venous Insufficiency (CVI), Diabetic Retinopathy, Microangiopathy.

After 24 hours of administration of Calcium Dobesilate, the blood level decreases to about 3μg/ml. The protein-binding rate is approximately 20 - 25%. In animals, calcium dobesilate does not cross the hematoencephalic or placental barriers, but it is uncertain if this applies to humans as well. However, only small quantities of calcium dobesilate enter maternal milk (around 0.4 μg/ml after a 1500 mg intake, as observed in one study). The drug does not undergo entero-hepatic recirculation and is primarily excreted unchanged, with only 10% being metabolized. Approximately 50% of the orally administered dose is eliminated in the first 24-hour urine, while the remaining 50% is excreted in the feces. The plasma half-life of calcium dobesilate is approximately 5 hours.

The common side effects of Calcium Dobesilate include Nausea, Diarrhea, Vomiting, Pruritus, Rash, Fever, Chills, Arthralgia, Tachycardia, Blood and lymphatic system disorders.

Calcium Dobesilate is available in the form of Tablets..

Calcium Dobesilate is approved in Germany, Japan, Malaysia, India, the U.K., the U.S., and China.

Calcium Dobesilate, belonging to the pharmacological class of Venotonics or Vasculoprotectives, acts as an Capillary-protective agent.

Calcium dobesilate is known to exert its therapeutic effects in conditions related to capillary dysfunction, the specific mechanism by which it achieves these effects was not clearly understood. Calcium dobesilate is believed to act on the capillary walls by regulating their impaired physiological functions, including reducing increased permeability and enhancing resistance. It is also thought to have antioxidant properties, which may help protect blood vessels from oxidative damage. Furthermore, the drug is reported to inhibit platelet hyper aggregation, potentially reducing the formation of blood clots within the capillaries. Additionally, calcium dobesilate is suggested to decrease plasma and blood hyper viscosity, leading to improved blood flow and rheological properties.

Calcium Dobesilate has been approved to relieve symptoms and also for the treatment and maintenance of Chronic Venous Insufficiency (CVI), Diabetic Retinopathy, Microangiopathy.

After oral administration of 500 mg of calcium dobesilate, its blood concentration reaches a peak (Cmax) of 8μg/ml approximately 6 hours later (tmax).

Calcium Dobesilate is found to be available in the form of Tablets.

Calcium Dobesilate can be used in the following treatment:

• Chronic Venous Insufficiency (CVI)
• Diabetic Retinopathy
• Microangiopathy

Calcium Dobesilate can help to relieve symptoms and also for the treatment and maintenance of Chronic Venous Insufficiency (CVI), Diabetic Retinopathy, and Microangiopathy.

Calcium Dobesilate is approved for use in the following clinical indications:

• Chronic Venous Insufficiency (CVI)
• Diabetic Retinopathy
• Microangiopathy

Chronic Venous Insufficiency (CVI):

Dosage: The usual recommended dosage for adults is 500 mg of Calcium Dobesilate taken orally two to three times daily.

Diabetic Retinopathy:

Dosage: The usual recommended dosage for adults is 500 mg of Calcium Dobesilate taken orally two to three times daily.

Microangiopathy:

Dosage: The usual recommended dosage for adults is 500 mg of Calcium Dobesilate taken orally two to three times daily.

Calcium Dobesilate is available in the following dosage forms and strengths:

• Tablets: 500mg

Tablets.

• Dosage Adjustments in Kidney Patients:

Caution should be exercised when using Calcium Dobesilate in patients with a history of kidney disease or active kidney disease, as this may elevate the risk of severe adverse effects. Any unusual symptoms should be promptly reported to the doctor. Depending on the patient's clinical condition, appropriate dose adjustments or switching to a suitable alternative may be necessary.

• Dosage Adjustments in Hepatic Impairment Patients:

There are found to be no dosage adjustments in the manufacturer's labeling.

• Dosage Adjustments in Pediatric Patients:

The use of Calcium Dobesilate in pediatric patients and its specific pediatric dosage strengths may not have been extensively studied or approved in all regions. Therefore, there may not be well-established pediatric dosages or indications for this drug.

No specific Dietary requirements have been found to be reported.

The dietary restriction should be individualized as per patient requirements.

Calcium Dobesilate may be contraindicated under the following conditions:

• Calcium Dobesilate should not be used in patients who have shown or are known to have hypersensitivity to the medication or any other components of Calcium Dobesilate .

In extremely rare cases (estimated incidence of 0.32/million patients based on spontaneous reports), the intake of calcium dobesilate may lead to agranulocytosis, likely due to a hypersensitivity reaction. This condition can manifest with symptoms such as high fever, oral cavity infections (tonsillitis), sore throat, anogenital inflammation, and accompanying symptoms, which are often indicative of an infection. Patients should be informed that if they experience any signs of infection, they must promptly notify their physician. In such instances, it is crucial to immediately monitor the blood formula and leucogram and discontinue the treatment.

While there is no direct interaction between Calcium Dobesilate and alcohol, patients should avoid excessive alcohol consumption during treatment. Alcohol can strain the liver and kidneys, which may already be affected by the medication.

Calcium dobesilate is found in minimal amounts in maternal milk (approximately 0.4 μg/ml after taking 3x500 mg). As a precautionary measure, either the treatment or breastfeeding should be discontinued.

Pregnancy:

Pregnancy category C:

There are no available studies in pregnant women or animals regarding calcium dobesilate. Since it is uncertain whether the drug crosses the placental barrier in humans, its administration should be considered only if the potential benefits outweigh the potential risks to the fetus.

There were no specific food warnings related to the use of calcium dobesilate.

The adverse reactions related to Calcium Dobesilate can be categorized as follows:

• Nausea
• Diarrhea
• Vomiting
• Pruritus
• Rash
• Fever
• Chills
• Arthralgia
• Tachycardia
• Blood and lymphatic system disorders

The clinically relevant drug interactions of Calcium Dobesilate is briefly summarized here:

No sufficient evidence of traceable drug interactions has been found.

The following are the side effects involving Calcium Dobesilate:

• Nausea
• Diarrhea
• Vomiting
• Pruritus
• Rash
• Fever
• Chills
• Arthralgia
• Tachycardia
• Blood and lymphatic system disorders

The use of Calcium Dobesilate should be prudent in the following group of special populations:

Pregnancy:

Pregnancy category C:

There are no available studies in pregnant women or animals regarding calcium dobesilate. Since it is uncertain whether the drug crosses the placental barrier in humans, its administration should be considered only if the potential benefits outweigh the potential risks to the fetus.

Lactation:

Calcium dobesilate is found in minimal amounts in maternal milk (approximately 0.4 μg/ml after taking 3x500 mg). As a precautionary measure, either the treatment or breastfeeding should be discontinued.

Pediatric:

No Sufficient evidence regarding the use of Calcium Dobesilate in Pediatric Population has been found.

Geriatric Use:

No Sufficient evidence regarding the use of Calcium Dobesilate in Geriatric Population has been found.

The physician should be vigilant about the knowledge pertaining to the identification and treatment of overdosage of Calcium Dobesilate.

No Sufficient evidence regarding the overdose of Calcium Dobesilate has been found.

Pharmacodynamics:

Calcium dobesilate functions as a regulator of capillary functions. It acts on the capillary walls, addressing their impaired physiological functions, which involve increased permeability and decreased resistance. The compound brings about various beneficial effects, including the enhancement of erythrocyte flexibility, the inhibition of platelet hyperaggregation, and the reduction of plasma and blood hyperviscosity in cases of diabetic retinopathy. This leads to improved blood rheological properties and tissue irrigation. These actions effectively correct capillary dysfunctions arising from functional issues or resulting from underlying metabolic disorders, be they constitutional or acquired. Moreover, calcium dobesilate also contributes to the reduction of edema.

Pharmacokinetics:

After taking 500 mg of calcium dobesilate orally, its blood concentration exceeds 6μg/ml between the 3rd and 10th hour, reaching a peak (Cmax) of 8μg/ml approximately 6 hours after intake (tmax). Twenty-four hours later, the blood level drops to around 3μg/ml. The protein-binding rate is approximately 20 - 25%.

In animals, calcium dobesilate does not pass through the haematoencephalic or placental barriers, but it is unclear if the same applies to humans. However, only minimal amounts of calcium dobesilate enter maternal milk (around 0.4 μg/ml after a 1500 mg intake, as reported in one study).

Calcium dobesilate does not undergo entero-hepatic recirculation and is primarily excreted unchanged, with only 10% being metabolized. Roughly 50% of the orally administered dose is eliminated in the first 24-hour urine, while the other 50% is excreted in the feces.

The plasma half-life of calcium dobesilate is approximately 5 hours.

1. https://go.drugbank.com/salts/DBSALT002519
2. https://www.drugs.com/international/calcium-dobesilate.html
3. https://www.e-lactancia.org/media/papers/Dobesilate-DS-OMPharma2018.pdf
4. https://www.clinicalkey.com/#!/content/book/3-s2.0-B9780444537171004388