Lactulose

Lactulose is a Drug for Constipation belonging to Osmotic Laxative.

Lactulose is a disaccharide derivative of lactose used to treat constipation and portal systemic encephalopathy.

After administration by the oral route, less than 3% of the given dose of lactulose solution is absorbed by the small intestine. The remaining unabsorbed lactulose reaches the large intestine where it is metabolized - but even then, negligible quantities of unchanged lactulose or its metabolites are absorbed across the colon.Lactulose metabolized by colonic bacterial flora into low molecular organic acids (mainly lactic acid and small amounts of formic and acetic acids). The Excretion of Lactulose take placemainly via faeces; urine (≤3% as unchanged drug).

Lactulose shows side effects like Diarrhea, gas, nausea.

Lactulose is available in the form of Oral syrup, Oral and rectal liquid, Powder for reconstitution.

Lactulose is available in India, US, Canada, Italy, Spain, Singapore, Malaysia, China, Russia, France, Japan, and Switzerland.

Lactulose belongs to the Osmotic Laxative acts as a Drug for Constipation.

The bacterial degradation of lactulose resulting in an acidic pH inhibits the diffusion of NH₃ into the blood by causing the conversion of NH₃ to NH₄+; also enhances the diffusion of NH₃ from the blood into the gut where conversion to NH₄+ occurs; produces an osmotic effect in the colon with resultant distention promoting peristalsis; reduces blood ammonia concentration to reduce the degree of portal systemic encephalopathy.

The Onset of action of Lactulose is approximately up to 24 to 48 hours to produce a normal bowel movement.

The Data of Duration of action and Tmax is not clinically established.

Lactulose is available in the form of Oral syrup, Oral and rectal liquid, Powder for reconstitution.

Lactulose is a laxative used to treat constipation. It makes it easy for you to pass your stool by softening it. It is also used to treat or prevent hepatic encephalopathy, which is a type of brain damage caused due to the inability of the liver to remove toxins from the blood.

Lactulose is a Drug for Constipation belonging to Osmotic Laxative.

The bacterial degradation of lactulose resulting in an acidic pH inhibits the diffusion of NH₃ into the blood by causing the conversion of NH₃ to NH₄+; also enhances the diffusion of NH₃ from the blood into the gut where conversion to NH₄+ occurs; produces an osmotic effect in the colon with resultant distention promoting peristalsis; reduces blood ammonia concentration to reduce the degree of portal systemic encephalopathy.

Lactulose is approved for use in the following clinical indications

Adult indication:

• Constipation
• Hepatic encephalopathy, treatment, or prevention

Pediatric indication:

• Constipation, palliative care
• Portal systemic encephalopathy, prevention

Adult Dose:

• Constipation

Oral: 10 to 20 g (15 to 30 mL or 1 to 2 packets) daily; may increase to 40 g (60 mL or 2 to 4 packets) daily if necessary.

• Hepatic encephalopathy, treatment, or prevention

Hepatic encephalopathy, treatment, or prevention:

Prevention:

Oral: 20 to 30 g (30 to 45 mL) 2 to 4 times daily; may adjust dose every 1 to 2 days to achieve 2 to 3 soft stools/day.

Treatment:

Oral: Initial: 20 to 30 g (30 to 45 mL) every 1 to 2 hours to induce ~2 soft stools/day, then reduce to 20 to 30 g (30 to 45 mL) 2 to 4 times daily; may adjust dose every 1 to 2 days to achieve 2 to 3 soft stools/day.

Rectal (alternative route): Retention enema: 200 g (300 mL) in 700 mL NS or water, retain for 30 to 60 minutes; may repeat every 4 to 8 hours based on responsiveness to therapy.

Pediatric Dose:

• Constipation, palliative care

Constipation: Infants, Children, and Adolescents: Oral solution (10 g per 15 mL): Oral: 0.667 to 2 g/kg/day (1 to 3 mL/kg/day) divided once or twice daily; maximum daily dose: 60 g/day (90 mL/day).

Palliative care: Limited data available: Children and Adolescents: Oral solution (10 g per 15 mL): Oral: 2 to 30 mL every 6 to 24 hours; others have suggested 5 to 10 mL every 2 hours until bowel movement.

• Portal systemic encephalopathy, prevention

Infants: Oral: 1.7 to 6.7 g/day (2.5 to 10 mL/day) in divided doses; adjust dosage to produce 2 to 3 stools/day.

Children and Adolescents: Oral: 26.7 to 60 g/day (40 to 90 mL/day) in divided doses; adjust dosage to produce 2 to 3 stools/day.

Lactulose is available in various strengths as 10 g/15 mL; 10 g; 20 g.

Lactulose is available in the form ofOral syrup, Oral and rectal liquid, Powder for reconstitution.

Drink plenty of fluids, Lactulose may cause fluid loss.

Lactulose is contraindicated in patients with

• Irritable bowel syndrome

Irritable bowel syndrome (IBS) is a common disorder that affects the large intestine. Signs and symptoms include cramping, stomach pain, bloating, gas, and diarrhoea or constipation, or both. Lactulose is not recommended for use in patients with have inflammatory bowel disease as it might causecolonic perforation (holes in your colon).

• Intestinal obstruction disorders

It is a condition of digestive system in which digested material is prevented from passing normally through the bowel. Lactulose is not recommended for use in patients having intestinal obstruction disorders as it may further reduce the movement of digestive material, therefore worsening your condition.

• Electrolyte imbalance

Monitor periodically for electrolyte imbalance when lactulose is used >6 months or in patients predisposed to electrolyte abnormalities (eg, elderly, debilitated patients). Hepatic disease may predispose patients to electrolyte imbalance. Infants receiving lactulose may develop hyponatremia and dehydration.

• Diabetes

Use with caution in patients with diabetes mellitus; solution contains galactose and lactose.

• Electrocautery procedures

During proctoscopy or colonoscopy procedures involving electrocautery, a theoretical risk of reaction between H₂ gas accumulation and electrical spark may exist; thorough bowel cleansing with a nonfermentable solution is recommended.

Lactulose is not recommended to be taken while breastfeeding as it is not known if this medicine is present in breast milk or not. All the risks and benefits should be considered before taking this medicine.

Animal studies failed to reveal evidence of fetal harm. There are no controlled data in human pregnancy. Lactulose should only be given during pregnancy when need has been clearly established.

Drink plenty of fluids, Lactulose may cause fluid loss.

• Common

Abdominal cramps, abdominal distention, abdominal distress, abdominal pain, anorexia, bloating, diarrhea, eructation, flatulence, nausea, vomiting.

• Dichlorphenamide

Laxatives may enhance the hypokalemic effect of Dichlorphenamide.

• Glutamine

May diminish the therapeutic effect of Lactulose. Specifically, glutamine may diminish the ammonia-lowering effects of lactulose.

• Vitamin K Antagonists (eg, warfarin)

Lactulose may enhance the anticoagulant effect of Vitamin K Antagonists.

The common side effects of Lactulose include the following

• Common side effects

Diarrhea, gas, nausea.

• Rare side effects

Stomach pain or cramps, vomiting.

• Pregnancy

Pregnancy Category B

Animal studies failed to reveal evidence of fetal harm. There are no controlled data in human pregnancy. Lactulose should only be given during pregnancy when need has been clearly established.

• Nursing Mothers

Lactulose is not recommended to be taken while breastfeeding as it is not known if this medicine is present in breast milk or not. All the risks and benefits should be considered before taking this medicine.

Symptoms: Diarrhoea, loss of electrolyte, abdominal pain.

Management: Symptomatic treatment. Administer fluid and electrolyte replacement as necessary for extensive fluid loss caused by diarrhoea or vomiting.

Pharmacodynamic

Lactulose formulations are most administered via the oral route or the rectal route. Consequently, because the substance experiences minimal absorption by the gut it typically remains localized in the gastrointestinal tract environment and ultimately demonstrates almost all of its pharmacologic effects within the gut. In particular, as lactulose elicits its laxative effects in enhancing stool amounts and softening stool, such biochemical and physiologic activities can cause increased bowel sounds (borborygmi), a feeling of bloatedness, belching, frequent flatus, and diarrhea.

Pharmacokinetics

• Absorption

After administration by the oral route, less than 3% of the given dose of lactulose solution is absorbed by the small intestine. The remaining unabsorbed lactulose reaches the large intestine where it is metabolized - but even then, negligible quantities of unchanged lactulose or its metabolites are absorbed across the colon.

• Distribution

Information is not available.

• Metabolism and Excretion

Lactulose metabolized by colonic bacterial flora into low molecular organic acids (mainly lactic acid and small amounts of formic and acetic acids). The Excretion of Lactulose take placemainly via faeces; urine (≤3% as unchanged drug).

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