Open Up

Uses

Open Up is used in the treatment of chronic and habitual constipation, treatment of acute and the prevention and treatment of chronic Portal-systemic encephalopathy including the stages of hepatic pre-coma and coma.

Open Up is a hyperosmolar laxative which is used as an effective treatment approach for constipation. It is a non-absorbable disaccharide which draws water into the bowel; causes distention through fluid accumulation, thus promotes soft stool and accelerates bowel motion.

Open Up is also used to associated treatment for these conditions: Constipation, Hepatic Encephalopathy (HE)

How Open Up works

Open Up is a synthetic disaccharide derivative of lactose that consists of one molecule of galactose and one molecule of fructose. Saccharolytic bacteria present in the large intestine subsequently break the substance down into organic acids like lactic acid and small amounts of formic and acetic acids. Such resultant volatile fatty acid metabolites, in combination with hydrogen and methane that is also generated consequently enhance intraluminal gas formation, peristaltic gut motility, and elicit an osmotic effect that facilitates an increase in the water content of stool as well as associated stool softening. All of these actions ultimately assist in facilitating and increasing the frequency of bowel movements in patients experiencing constipation, although it may take 24 to 48 hours after using the medication for this laxative effect to become evident.

At the same time, the formation of such acids via the metabolism of lactulose by colonic bacteria also acidifies the contents of the colon, thereby contributing to the treatment of portal-systemic encephalopathy (PSE). As one of the principal features of PSE involves the accumulation of nitrogenous waste products like ammonia in the systemic circulation, a state in which the colonic contents become more acidic than blood allows ammonia in the circulation to diffuse into the colon.. Furthermore, ammonia that diffuses into the acidic colon is ionized to ammonium ions that are incapable of being absorbed back into the blood. These effects, combined with the laxative action of lactulose facilitates the excretion of excess ammonia. And finally, it is also believed that an acidic colonic environment results in the elimination of urease-producing bacteria that contribute to the formation of ammonia while surviving colonic bacteria use up any trapped ammonia in the colon as a source of nitrogen for protein synthesis.

Dosage

Open Up dosage

Adults (including elderly): 3 tea spoonful or 15 ml twice daily

Children 5 to 10 years: 2 tea spoonful or 10 ml twice daily

Children under 5 years: 1 tea spoonful or 5 ml twice daily

Babies under 1 year: ½ tea spoonful or 2.5 ml twice daily (paediatric dose should be given after breakfast)

Each dose of Open Upmay, if necessary, be taken with water or fruit juices, usually once a day, preferably in the morning. If a dose is forgotten it should be taken as soon as one remembers up to 8 hours before bedtime. If later, wait for next scheduled dose (don’t double this dose). Don’t take at bedtime. Usual time lapse before drug works is 30 minutes to 3 hours.

Side Effects

Life threatening: None expected

Common: Increased thirst, cramps, nausea, diarrhoea, flatulence

Infrequent: Irregular heart beat, muscle cramps

Rare: Dizziness, confusion, fatigue, weakness.

Toxicity

It has been documented that the oral LD50 of lactulose is 48.8 mL/kg in mice and more than 30 mL/ kg in rats.

It is expected that overdosage with lactulose would result in abdominal cramps and diarrhea, both of which should be treated with fluid and electrolyte replacement as required.

Considering the use of lactulose during pregnancy in humans has not been formally investigated, the agent should only be used during pregnancy only when clearly needed. Similarly, it is unknown whether lactulose is distributed into human breastmilk. Use of the medication in nursing women should subsequently be undertaken with caution.

Reproduction studies in rats, mice, and rabbits have not revealed any evidence of impaired fertility as a result of administering lactulose.

Data regarding the safety and efficacy of using lactulose in children for the treatment of chronic constipation or portal-systemic encephalopathy (PSE) is either very limited or yet to be established.

Information regarding the long-term mutagenic potential of lactulose solution in animals or humans and about the long-term carcinogenic potential in humans are not available.

Precaution

It should be avoided if one is allergic to any hyperosmotic laxative, have symptoms of appendicitis, inflammatory bowel diseases or intestinal blockage, have missed a bowel movement for only 1 or 2 days. Adverse reactions over age 60 year may be more frequent and severe than in younger persons.

Interaction

Reduced effect with non-absorbable antacids, neomycin and other oral anti-infectives. Concomitant use with other laxatives may falsely suggest that adequate lactulose dosage has been achieved.

Food Interaction

• Drink plenty of fluids. This drug may cause fluid loss.
• Take with or without food.

Open Up Drug Interaction

Moderate: docusate, docusate, furosemide, furosemide, polyethylene glycol 3350, polyethylene glycol 3350, ondansetron, ondansetronUnknown: acetaminophen, acetaminophen, acetaminophen, acetaminophen, cyanocobalamin, cyanocobalamin, ascorbic acid, ascorbic acid, cholecalciferol, cholecalciferol, rifaximin, rifaximin

Open Up Disease Interaction

Major: galactosemia, inflammatory bowel disease, intestinal obstruction disordersModerate: diabetes

Volume of Distribution

Negligible amounts of lactulose - metabolized or non-metabolized - are absorbed into the body.. Most lactulose that is administered subsequently remains predominantly around the gastrointestinal tract area.

Elimination Route

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.

Half Life

The data regarding the half-life of lactulose is not readily available or accessible.

Clearance

Negligible amounts of lactulose - metabolized or non-metabolized - are absorbed into the body.. Regardless, data regarding the clearance of lactulose is not readily available or accessible.

Elimination Route

The renal excretion of any lactulose that manages to be absorbed into the circulation has been determined to be 3% or less and is generally complete within 24 hours. Any unabsorbed lactulose is largely excreted with stool.

Pregnancy & Breastfeeding use

In pregnancy no proven problems were detected. Avoid the drug if possible. Consultation with physician is required. It has no side effect during breast feeding. Open Up oral solution could be used in infants and children only under medical supervision. It should not be used to ‘flush out’ the system or as a ‘tonic'.

Contraindication

Open Up is contraindicated in patients with galactosaemia and intestinal obstruction.

Acute Overdose

There have been no reports of accidental overdosage. In the event of acute overdosage it is expected that diarrhoea and abdominal cramps would be the major symptoms.

Storage Condition

Store between 15-30° C.

Innovators Monograph

You find simplified version here Open Up