laxatrol

laxatrol Uses, Dosage, Side Effects, Food Interaction and all others data.

Docusate acts primarily by increasing the penetration of fluid into the faeces. It may also have effects on intestinal fluid secretion, and probably act both as stimulant and faecal softening agent. It also softens ear wax through penetration into the dry matrix of the ceruminous mass, reducing it into semi-solid debris.

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.

Senna glycoside, also known as sennoside or senna, is a medication used to treat constipation and empty the large intestine before surgery. The medication is taken by mouth or via the rectum. It typically begins working in minutes when given by rectum and within twelve hours when given by mouth. It is a weaker laxative than bisacodyl or castor oil.

Sennosides A and B increase intestinal motility through release of active anthraquinones into the colon by colonic bacteria. Purified sennosides (sennosides A and B) are used similarly to senna.

Senna stimulates peristalsis and increases fecal water content to increase motility of feces through the large intestine.

laxatrol
Uses
Dosage
Side Effect
Precautions
Interactions
Uses during Pregnancy
Uses during Breastfeeding
Accute Overdose
Food Interaction
Half Life
Volume of Distribution
Clearance
Interaction With other Medicine
Contradiction
Storage

Trade Name	laxatrol
Generic	Docusate + Sennosides
Weight	50, 8mg
Type	Tablet, Film Coated
Therapeutic Class
Manufacturer	Jamjoom Pharmaceuticals Company
Available Country	Saudi Arabia
Last Updated:	September 19, 2023 at 7:00 am

Uses

Docusate is used for Constipation, Bowel evacuation, Softening of ear wax, Constipation

It is used to treat hard stools (constipation).

laxatrol is also used to associated treatment for these conditions: Constipation, Occasional Constipation, Bowel preparation therapyConstipation, Hemorrhoids, Auto-intoxication, Meteorism

How laxatrol works

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.

Sennoside A and B, the components of senna, are metabolized by gut bacteria into the active metabolite rheinanthrone Rheinanthrone. Rheinanthrone Rheinanthrone appears to increase cyclooxegenase 2 (COX2) expression in macrophage cells leading to an increase in prostaglandin E2 (PGE2). This increase in PGE2 is associated with a decrease in aquaporin 3 expression in mucosal epithelial cells of the large intestine. A decrease in aquaporin 3 expression likely produces the laxative effect by restricting water reabsorption by the large intestine thereby increasing fecal water content. The exact mechanism by which rheinanthrone increases COX2 expression is unknown. Rheinanthrone Rheinanthrone also stimulates peristalsis in the large intestine although the mechanism behind this effect is unknown. Rhein Rhein, another active metabolite is thought to excite submucosal acetylcholinergic neurons resulting in increased chloride and prostaglandin secretion. The movement of chloride ions into the large intestine would also help to draw water into the lumen.

Dosage

laxatrol dosage

Constipation:

Adult: 50-300 mg daily in divided doses. Max: 500 mg daily.
Child: ≥12 yr Same as adult dose.

Bowel evacuation:

Adult: As adjunct to abdominal radiological procedures: 400 mg given with barium meal.
Child: ≥12 yr Same as adult dose.

Constipation

Adult: 15-30 mg (as total sennosides) 1-2 times daily.
Child: 2-6 yr: 3.75-7.5 mg once daily in the morning; 6-12 yr: 7.5-15 mg once daily at night or in the morning; ≥12 yr: 15-30 mg at bedtime.

Bowel evacuation

Adult: 105-157.5 mg of sennosides on the day before the procedure. May be given as a liquid preparation.

Side Effects

Anorectal pain or bleeding (rectal). Rarely, diarrhoea, abdominal cramps, nausea, skin rash.

Mild abdominal discomfort e.g. colic and cramps; diarrhoea, hypokalaemia and atonic non-functioning colon (prolonged use); reversible melanosis coli (chronic use). May colour the urine yellowish-brown at acidic pH or red at alkaline pH.

Toxicity

Docusate is not known to be carcinogenic or cause reproductive toxicity. It was not mutagenic in the Ames assay . Acute oral LD50 in rat is 1900 mg/kg .

Senna causes increased amounts of apoptosis in the large intestine shortly after use due to upregulated p53 activity. This is normally reversed after 18 hours however chronic use has been shown to be associated with p53 resistance and potential carcinogenicity leading to colon cancer. The LD50 value in rats was 5000mg/kg. Subacute studies in rats receiving 20mg/kg and dogs receiving 500mg/kg did not produce signs of toxicity. Tests for mutagenicity and reproductive toxicity do not indicate toxic effects.

Sennosides are not recommended for use in pregnancy due to genotoxic risks associated with chemically similar compounds. The active metabolite of sennosides is excreted in breast milk, though there are no reports of the laxitive effect in breast fed babies. There is no data on the effects of sennosides on fertility.

Precaution

Rectal admin in patient with haemorrhoids or anal fissures. Children. Pregnancy and lactation.

Inflammatory bowel disease. Avoid prolonged use.

Interaction

May enhance GI uptake of other drugs (e.g. liquid paraffin). May increase effects of anthraquinone laxatives. Increased incidence of adverse effects in GI mucosa with aspirin.

Volume of Distribution

The volume of distribution of radiolabelled intravenous sennoside B in rats was 0.802±0.124L/kg.

Elimination Route

Docusate is not absorbed systemically. As the actions of docusate are local and it is not absorbed, the pharmacokinetic parameters are not available.

12.

Half Life

The half life of radiolabelled intravenous sennoside B in rats was 8.568±0.651h.

Clearance

The clearance of radiolabelled intravenous sennoside B in rats was 0.065±0.007L/h/kg.

Elimination Route

If docusate is systemically absorbed, it undergoes biliary excretion .

3-6% of metabolites are excreted in urine with some in bile. >90% of sennosides are excreted in the feces as polymers with 2-6% of the parent compounds excreted unchanged.

Pregnancy & Breastfeeding use

Pregnancy Category C. Either studies in animals have revealed adverse effects on the foetus (teratogenic or embryocidal or other) and there are no controlled studies in women or studies in women and animals are not available. Drugs should be given only if the potential benefit justifies the potential risk to the foetus.

Sennosides has been assigned to pregnancy category C by the FDA. Animal studies have failed to reveal evidence of teratogenicity. There are no controlled data in human pregnancy. Sennosides should only be given during pregnancy when benefits outweigh risks.

Sennosides is not excreted into human milk. However, Sennosides is a prodrug which is metabolized in vivo to the active sennosides (glucosides of rhein). Rhein is excreted into human milk in very small amounts. No adverse effects have been observed in nursing infants. The American Academy of Pediatrics considers Sennosides to be compatible with breast-feeding.