CALDOBERG

Indications

• Constipation
• Softening of impacted feces
• Bowel cleansing prior to medical procedures

Dosage

Children: For children aged 2-11 years: 12.5 to 25 mg 3 times a day, adjusted according to response. For children aged 12-17 years: 120 mg for 1 dose.

Adults: For oral use: 50 to 500 mg daily in divided doses, adjusted according to response. For rectal use: 120 mg as a single dose.

Mechanism of action

Docusate sodium acts as a stool softener by increasing the wetting efficiency of the intestinal fluid, facilitating the mixing of aqueous and fatty substances, which leads to a reduction in stool hardness. It also promotes the secretion of intestinal fluids, which aids in the overall ease of bowel movements.

Pharmacodynamics

Docusate sodium works by altering the surface tension of the stool, making it easier for water to mix with the stool, thus softening it. Its effects are generally observed within 1 to 3 days of oral administration, while rectal administration can lead to a quicker response, typically within 20 minutes.

Pharmacokinetics

Docusate sodium is absorbed in the gastrointestinal tract, with a peak plasma concentration occurring approximately 1 to 2 hours after administration. The elimination half-life is not well-characterized, but the drug is excreted mainly in the urine. The onset of action varies depending on the route of administration; oral doses typically take 1-3 days to have an effect, whereas rectal doses have a faster onset.

Contra-indications

• Inflammatory bowel disease (except under medical supervision)
• Intestinal obstruction
• Hypersensitivity to soya
• History of hypersensitivity to arachis oil or peanuts

Adverse effects

• Anal irritation
• Contact dermatitis
• Granuloma pneumonia
• Lipoid pneumonia
• Rectal discharge

Interactions

• Avoid concurrent use with liquid paraffin
• Excessive use of stimulant laxatives may cause diarrhea and related effects such as hypokalemia

Precautions

• Prolonged use should be avoided
• Administered at night for optimal effect
• Rectal preparations not indicated if hemorrhoids or anal fissure are present

Pregnancy

Manufacturer advises caution; consult a healthcare professional before use during pregnancy.

Breast-feeding

Manufacturer advises caution; present in small amounts in milk following oral administration.

Storage

Store in a cool, dry place away from direct sunlight. Keep out of reach of children.

Formulations

• Docusate sodium 2.5 mg per 1 ml oral solution
• Docusate sodium 10 mg per 1 ml oral solution
• Docusate sodium 12.5 mg/5 ml oral solution
• Docusate sodium 100 mg capsules
• Docusate sodium 120 mg enema

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

• Constipation
• Prevention of straining during bowel movements
• Management of conditions such as hemorrhoids or anal fissures

Dosage

Children: Refer to the BNF for Children for appropriate dosing in children.

Adults: The usual oral dosage is 50 to 500 mg daily in divided doses, or 100 to 250 mg taken once daily. Rectal administration can involve 283 to 566 mg as a single dose.

Mechanism of action

Docusate exerts its effects primarily through its surfactant properties in the intestines. It allows for the incorporation of fat and water into the feces, which softens the stool. Studies have shown that docusate increases the secretion of water, sodium, chloride, and potassium while decreasing the absorption of glucose and bicarbonate. This mechanism may involve an increase in intracellular cyclic AMP, either directly by docusate or through E series prostaglandins.

Pharmacodynamics

As an anionic detergent and laxative, docusate promotes stool softening by reducing surface tension. Its onset of action varies, with oral administration taking 6 to 72 hours and rectal administration acting within 2 to 15 minutes. The effects are localized in the jejunum, aiding in the passage of feces.

Pharmacokinetics

Docusate is absorbed in the gastrointestinal tract, but its specific absorption and elimination characteristics are not well-documented. It is primarily metabolized in the intestines, and the active metabolites facilitate the stool softening effect. The pharmacokinetic profile indicates that its action can vary based on the route of administration and individual patient factors.

Adverse effects

• Abdominal cramping
• Diarrhea
• Nausea
• Throat irritation

Precautions

• Use with caution in patients with intestinal obstruction or abdominal pain of unknown origin
• Not recommended for long-term use

Pregnancy

Docusate is generally considered safe to use during pregnancy, but it is advisable to consult a healthcare provider before use.

Breast-feeding

Docusate is excreted in breast milk; however, it is considered safe to use while breastfeeding.

Storage

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

Formulations

• Oral capsules
• Oral liquid
• Rectal suppositories

Mechanism of action

Recent studies suggest that docusate's mechanism of action is due largely to it's surfactant effect in the intestines, which allow fat and water into the feces to soften the stool. Docusate’s mechanism of action was investigated in 1985 on healthy patients. Docusate was added directly to the jejunum based on calculated concentrations of docusate in the jejunum. At this concentration, there was an increase in secretion of water, sodium, chloride, and potassium as well as a decrease in absorption of glucose and bicarbonate. Based on in vitro data, the authors suggested this effect was due to an increase in intracellular cyclic AMP either directly through docusate or E series prostaglandins.

Pharmacodynamics

Docusate sodium is a laxative and an anionic detergent that supposedly promotes incorporation of water and fats into stool through a reduction in surface tension, resulting in softer fecal mass. Docusate's onset of action is 6-72 hours orally and 2-15 minutes rectally. The effects of docusate are thought to be exerted locally in the jejunum.