DOBESIL -H CREAM

Indications

• Diabetic retinopathy
• Chronic venous insufficiency
• Microangiopathies

Dosage

Children: Paediatric dosing information is not provided, refer to the BNF for Children for appropriate guidance.

Adults: The typical adult dosage is 500 mg taken orally, three times daily. The duration of treatment and specific indications should be guided by clinical judgment and individual patient response.

Mechanism of action

Dobesilate is believed to exert its effects by stabilizing capillary membranes and reducing their permeability to plasma proteins. It also inhibits the release of inflammatory mediators from activated endothelial cells, leading to a reduction in edema and inflammation. This action contributes to its therapeutic effects in microangiopathies and vascular disorders.

Pharmacodynamics

Dobesilate exhibits vasoprotective properties, which involve actions on the vascular endothelium, providing protection against damage and reducing leakage of plasma proteins. Its anti-inflammatory effects may also contribute to reducing the progression of diseases associated with microcirculation disturbances. The drug has also shown to have positive effects on blood flow in microcirculation by improving the rheological properties of blood.

Pharmacokinetics

Dobesilate is absorbed after oral administration, though the specifics of its bioavailability are not well established. It undergoes hepatic metabolism, and its elimination half-life is approximately 3-4 hours. The drug is primarily excreted via the kidneys, and dose adjustments may be necessary in patients with renal impairment to avoid accumulation.

Contra-indications

• Hypersensitivity to dobesilate or any of its components
• Severe renal impairment

Adverse effects

• Gastrointestinal disturbances
• Skin rashes
• Headache
• Dizziness
• Fatigue
• Nausea

Precautions

• Use with caution in patients with renal impairment
• Monitor for signs of hypersensitivity

Pregnancy

There are no adequate and well-controlled studies in pregnant women. Dobesilate should only be used during pregnancy if the potential benefit justifies the potential risk to the fetus.

Breast-feeding

It is not known whether dobesilate is excreted in human milk. Caution should be exercised when administering to nursing mothers.

Storage

Store below 25 degrees Celsius, in a dry place, protected from light.

Formulations

• Capsules
• Tablets
• Oral suspension

Indications

• Local pain relief
• Inflammatory skin conditions
• Dermatitis
• Eczema
• Psoriasis
• Post-surgical pain management

Dosage

Children: Refer to specific formulations for dosing information, as it varies based on the condition being treated and the formulation used.

Adults: Refer to specific formulations for dosing information, as it varies based on the condition being treated and the formulation used.

Mechanism of action

Lidocaine functions as a sodium channel blocker, inhibiting the influx of sodium ions during action potentials in nerve cells, which results in decreased neuronal excitability and conduction. Hydrocortisone, a corticosteroid, exerts its effects by binding to glucocorticoid receptors, leading to alterations in gene expression that promote anti-inflammatory activity and immune system suppression.

Pharmacodynamics

Lidocaine provides rapid onset of local anesthesia, typically within minutes of application, and its effects can last for a few hours depending on the formulation. Hydrocortisone's anti-inflammatory effects can take hours to days to manifest, as it works on a cellular level to reduce the activity of inflammatory mediators and modulate the immune response. When used together, these drugs can effectively manage pain and inflammation in various conditions.

Pharmacokinetics

Lidocaine is well-absorbed when applied topically, with peak plasma concentrations occurring within 30 minutes to 2 hours post-application. It undergoes extensive hepatic metabolism, with a half-life of approximately 1.5 to 2 hours. Hydrocortisone is also absorbed through the skin, with the systemic bioavailability influenced by the formulation. It is metabolized primarily in the liver, with a half-life of about 1 to 2 hours. Both medications can be excreted in urine as metabolites.

Contra-indications

• Hypersensitivity to lidocaine or hydrocortisone
• Severe heart block
• Adrenal insufficiency

Adverse effects

• Local irritation or burning at the site of application
• Allergic reactions including rash, itching, or swelling
• Systemic effects such as cardiovascular disturbances
• Nausea or vomiting
• Dizziness or headache
• Blurred vision

Interactions

• May enhance the effects of other local anesthetics
• Caution when used with anticoagulants due to increased bleeding risk
• Potential interaction with corticosteroid medications leading to additive effects

Precautions

• Use with caution in patients with liver dysfunction
• Monitor for signs of systemic absorption, especially in large areas of application
• Avoid use in patients with a history of significant allergic reactions
• Use with caution in pregnant women and those with renal impairment

Pregnancy

Lidocaine and hydrocortisone should only be used during pregnancy if clearly needed, as safety in pregnancy has not been established.

Breast-feeding

Lidocaine and hydrocortisone may be excreted in breast milk, caution is advised when administering to nursing mothers.

Storage

Store at room temperature, away from light and moisture. Keep out of reach of children.

Formulations

• Topical cream
• Ointment
• Gel