Hepalac

Lactulose.

Each 100 ml contains lactulose 66.7 g.

Pharmacodynamics: Mechanism of Action: Lactulose, a synthetic disaccharide analog of lactose containing galactose and fructose, decreases blood ammonia concentrations and reduces the degree of portal - systemic encephalopathy.
The human GI tissue does not have an enzyme capable of hydrolysis of this disaccharide; as a result, oral doses pass to the colon virtually unchanged. After reaching the colon, lactulose is metabolized by bacteria resulting in the formation of lactic acid, formic acid, acetic acid and carbon dioxide. These products produce an increased osmotic pressure and slightly acidify the colonic contents, resulting in an increase in stool water content and stool softening. Because the colonic contents are more acidic than the blood, ammonia can migrate from the blood into the colon. The acid colonic contents convert NH₂ to the ammonium ion [NH₄]⁺, trapping it and preventing its absorption. The laxative action of the lactulose metabolites then expels the trapped ammonium ion from the colon.
Pharmacokinetics: Lactulose is poorly absorbed. When given orally, only small amounts reach the blood. Urinary excretion is ≤ 3% and is essentially complete within 24 hours. Lactulose does not exert its effect until it reaches the colon. Transit time through the colon may be slow; therefore, 24 to 48 hours may be required to produce a normal bowel movement.
Onset: Constipation: up to 24 - 48 hours to produce a normal bowel movement.
Encephalopathy: at least 24 - 48 hours.
Absorption: not appreciable.
Metabolism: Via colonic flora to lactic acid and acetic acid requires colonic flora for drug activation.
Excretion: Primarily feces, urine (≤ 3%).

Constipation: For the treatment of constipation. In patients with a history of chronic constipation, lactulose therapy increases the number of bowel movements per day and the number of days on which bowel movements occur.
Portal-systemic encephalopathy: For the prevention and treatment of portal - systemic encephalopathy, including the stages of hepatic precoma and coma.

Recommended Doses: Constipation: Adults: 10-20 g (15-30 mL) daily; may increase to 40 g (60 mL) daily if necessary.
Portal systemic encephalopathy, acute treatment: Adults: 20-30 g (30-45 mL) every 1 hour to induce rapid laxation; reduce to 20-30 g (30-45 mL) 3-4 times daily after laxation is achieved titrate to produce 2-3 soft stools/day.
Portal systemic encephalopathy, prevention: Infants: 1.7-6.7 g/day (2.5-10 mL/day) in divided doses; adjust dosage to produce 2-3 stools/day.
Children: 26.7-60 g/day (40-90 mL/day) in divided doses; adjust dosage to produce 2-3 stools/day.
Adults: 20-30 g (30-45 mL) 3-4 times daily; adjust dose every 1-2 days to produce 2-3 soft stools/day.
Mode of Administration: Oral solution: May mix with fruit juice, water or milk.

Overdose: There have been no reports of accidental lactulose overdose. It is expected that diarrhea and abdominal cramps would be the major symptoms, discontinue the drug.

Hypersensitivity to any ingredient; nausea, vomiting or other symptoms of appendicitis; fecal impaction; intestinal obstruction; undiagnosed abdominal pain; patients who require a low galactose diet.

Prior to using laxatives, consider living habit affecting bowel function, including disease state and drug history. Treatment and prevention of constipation include the following: adequate fluid intake (4 to 6 glasses (8 oz) of water daily), proper dietary habits including increasing fiber intake, responding to the urge to defecate and daily exercise. Restrict self-medication to short-term therapy of constipation; chronic use of laxative may lead to dependence. (See table.)

Click on icon to see table/diagram/image

Fluid and electrolyte balance: Excessive laxative use may lead to significant fluid and electrolyte imbalance. Monitor patients periodically.
Geriatric, debilitated patients who receive lactulose for more than 6 months should have serum electrolytes (e.g., potassium, chloride, carbon dioxide) measured periodically during therapy.
Abuse-dependency: Chronic use of laxatives may result in fluid and electrolyte imbalances, steatorrhea, osteomalacia, diarrhea, cathartic colon and liver disease. Also known as laxative abuse syndrome (LAS), it is difficult to diagnose. It is often seen in women with depression, personality disorders or anorexia nervosa. Many agents can be detected in urine or stool samples; however, it is important to follow up negative test results if LAS is suspected, because patients may be intermittent abusers or change laxative products frequently.
Cathartic colon: Cathartic colon, a poorly functioning colon, results from the chronic abuse of stimulant cathartics.
Electrocautery procedures: A theoretical hazard may exist from patients being treated with lactulose who may undergo electrocautery procedures during proctoscopy or colonoscopy. Accumulation of H₂ gas in significant concentration in the presence of an electrical spark may result in an explosion. Although this complication has not been reported with lactulose, patients should have a thorough bowel cleansing with a nonfermentable solution.
Diabetic patients: Lactulose syrup contains galactose (less than 1.6 g/15 mL) and lactose (less than 1.2 g/15 mL). Use with caution in these individuals.
Concomitant laxative use: Do not use other laxatives, especially during the initial phase of therapy for portal-systemic encephalopathy; the resulting loose stools may falsely suggest adequate lactulose dosage.
Rectal bleeding or failure to respond: Rectal bleeding or failure to respond to therapy may indicate a serious condition, which may require further medical attention.
Use in Children: Limited information on the use of lactulose for prevention and treatment of portal-systemic encephalopathy in young children and adolescents is available. Safety and efficacy of the drug for the treatment of chronic constipation in children have not been established.

Pregnancy category B.
Adverse events have not been observed in animal reproduction studies.
Lactation: Excretion in breast milk unknown/use caution.

Endocrine & metabolic: Dehydration, hypernatremia, hypokalemia.
Gastrointestinal: Abdominal discomfort, abdominal distention, belching, cramping, diarrhea (excessive dose), flatulence, nausea, vomiting.

Laxatives: Additional laxatives should not be administered with lactulose solution, especially when lactulose therapy is initiated, because the loose stools produced may be falsely interpreted as an indication that adequate dosage of lactulose has been achieved.
Anti-infective agents: Theoretically, orally administered neomycin and possibly other anti-infective agents, when administered concurrently with lactulose could eliminate colonic bacteria that are necessary to metabolize lactulose and thereby prevent acidification of the contents of the colon. Limited data obtained from experiments in healthy individuals tend to support the theoretical incompatibility of these agents. There is, however, evidence that lactulose remains active when administered with neomycin to patients with portal-systemic encephalopathy. In addition, there have been reports that concomitant therapy with lactulose and neomycin may be more effective than either drug alone in the treatment of portal-systemic encephalopathy. Therefore, until there is conclusive evidence that concurrent administration of lactulose and neomycin or other oral anti-infective agents is efficacious, patients receiving lactulose and an oral anti-infective agents should be closely monitored for possible inadequate response to lactulose.
Antacids: Results of limited studies in rats and humans suggest that nonabsorbable antacid administered concomitantly with lactulose may inhibit the desired decrease in fecal pH in the colon. The potential lack of desired effect of lactulose should be considered before a nonabsorbable antacid is administered concomitantly with lactulose.

Store below 30°C.

Laxatives, Purgatives / Cholagogues, Cholelitholytics & Hepatic Protectors

A06AD11 - lactulose ; Belongs to the class of osmotically acting laxatives.

NDD