Sodium Picosulfate

Sodium Picosulfate Keith Hillier University of Southampton, Southampton, UK ã 2007 Elsevier Inc. All rights reserved.

Introduction Sodium picosulfate is an orally administered stimulant laxative, used for bowel preparation before surgery, or investigative bowel procedures such as barium enemas Atkin et al (2000), Hamilton et al (1996). It increases colonic peristalsis partly by stimulation of the enteric nervous system. It is also combined in preparations with magnesium oxide and citrate. Stimulant laxatives should have only limited use in the management of constipation.

Nomenclature Name of the Clinical Form Related Names Source: EMTREE

Chemical Names CAS Number

Dulcosan; guttalax; laxoberal; laxoberon; picolax; picosulfate sodium; Sodium picosulphate; Sodium Picosulfate; Phenol, 4,4’-(2-pyridinylmethylene)bis-, bis(hydrogen sulfate) (ester), disodium salt; Laxoberal (trade); dulcosan 10040-45-6

Basic Chemistry Chemical Structure Structure

Chemical Formula Properties Physical Properties Molecular Weight Solubility

C18 H15 N O8 S2

White crystalline solid 437.448 Freely soluble in water, slightly soluble in alcohol; insoluble in most other organic solvents

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Sodium Picosulfate

Human Pharmacokinetics Metabolized to active bis(p-hydroxyphenyl)pyridyl-2-methane by colonic bacteria. Little accessible information available. Is generally orally effective in 10–14 hours, but this could also be as short as 3–6 hours when combined with citrate Jauch et al (1977), Perego et al (1969). Because it is very poorly absorbed, normal pharmacokinetic parameters are not measurable.

Targets-Pharmacodynamics Stimulates the enteric nervous system Target Name(s): Enteric nervous system, myenteric plexus

Therapeutics Sodium picosulfate is a stimulant laxative related to disacodyl and is used for the treatment of constipation. Poor absorption contributes to the low level of nongastrointestinal-related side effects, and it requires metabolism to an active product by colonic bacteria Kim et al (1992). It should be used only for preoperative bowel cleansing. Indications

Value

Units

Prep.and Route of Admin.

Bowel cleansing preparation Dosage 5-10 mg p.o.

Reference

Comments

British National Formulary, 2003

Only fluid by mouth after administration and before procedure. Given at night. Good hydration necessary. 0.25–10 mg for children, depending on age.

Contraindications Obstructive bowel conditions. Severe dehydration. Adverse Effects Stomach cramps; overuse may result in atony, diarrhea, and potassium loss ADRAC (1997).

Pre-Clinical Research It is metabolised to active ingredients in rats Perego et al (1969).

Sodium Picosulfate

Journal Citations Atkin, W.S., Hart, A., Edwards, R., Cook, C.F., Wardle, J., McIntyre, P., Aubrey, R., Sutton, S., Cuzick, J., Senapati, A., Northover, J.M., 2000. Single blind, randomized trial of efficacy and acceptability of oral picolax versus self administered phosphate enema in bowel preparation for flexible sigmoidoscopy screening. Br. Med. J., 320, 1504–1508. Hamilton, D., Mulcahy, D., Walsh, D., Farrelly, C., Tormey, W.P., Watson, G., 1996. Sodium picosulphate compared with polyethylene glycol solution for large bowel lavage: a prospective randomized trial. Br. J. Clin. Pract., 50(2), 73–75. Kim, D.H., Hyun, S.H., Shim, S.B., Kobashi, K., 1992. The role of intestinal bacteria in the transformation of sodium picosulfate. Jpn. J. Pharmacol., 59(1), 1–5. Perego, R., Martinelli, E., Vanoni, P.C., Bonardi, G., Coppi, G., 1969. On the metabolic disposition of sodium picosulfate in rats. Arzneimittelforschung., 19(11), 1889–1890. Sund, R.B., Songedal, K., Harestad, T., Salvesen, B., Kristiansen, S., 1981. Enterohepatic circulation, urinary excretion and laxative action of some bisacodyl derivatives after intragastric administration in the rat. Acta Pharmacol. Toxicol., 48(1), 73–80. ADRAC, 1997. Electrolyte disturbances with oral phosphate bowel preparations. Aust. Adv. Drug React. Bull., 16, 2. Jauch, R., Hammer, R., Busch, U., Kopitar, Z., Ohnuma, N., Niki, T., 1977. Pharmacokinetics and metabolism of sodium picosulfate in the rat. Arzneimittelforschung, 27(5), 1045–1050.

Book Citations British National Formulary 2003 British National Formulary, Edition 42. , British Medical Association, London.

Further Reading S. C. Sweetman, Martindale Extra Pharmacopoeia, Edition 31, Royal Pharmaceutical Society, London, 2000.

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