Sodium Picosulfate

Products

Sodium picosulfate is commercially available in the form of tablets, soft capsules (pearls), and drops (e.g., Laxoberon, Dulcolax Picosulfate). It has been approved in many countries since 1973.

Structure and properties

Sodium picosulfate (C18H13NNa2O8S2, Mr= 481.41 g/mol) is structurally closely related to bisacodyl. The difference is that it is esterified with sulfuric acid instead of acetic acid. It exists as a white crystalline powder that dissolves readily in water. Sodium picosulfate is a diphenylmethane and triarylmethane derivative. It is a prodrug and is converted by intestinal bacteria to the free diphenol BHPM. This is the same active metabolite responsible for the effects of bisacodyl. Sodium picosulfate is not absorbed and therefore, unlike bisacodyl, does not need to be administered in the form of enteric-coated tablets.

Effects

Sodium picosulfate (ATC A06AB08) has laxative properties. The active metabolite stimulates intestinal motility and secretion of water and electrolytes into the intestine.

Indication

Sodium picosulfate is used for short-term use in constipation and in conditions requiring facilitated bowel evacuation. Under medical supervision, it may also be used on a longer-term basis to treat constipation that occurs as a result of treatment with opioids (see also Opioids and Constipation).

Dosage

As directed in the package insert. Sodium picosulfate, unlike bisacodyl, is not absorbed in the small intestine and is therefore undrugged and more finely dosed, for example, in the form of drops. The effect usually occurs after 6-12 hours.

Contraindications

  • Hypersensitivity
  • Intestinal obstruction
  • Acute disease of the digestive tract
  • Severe abdominal pain associated with nausea or vomiting.
  • Severe dehydration
  • Hypokalemia

It should not be taken during pregnancy and lactation. Full precautions can be found in the drug label.

Interactions

Sodium picosulfate may increase potassium loss from other drugs, such as diuretics and glucocorticoids. The resulting hypokalemia may increase sensitivity to cardiac glycosides. Antibiotics may lead to loss of the laxative effect of sodium picosulfate when administered concomitantly.

Adverse effects

The most common possible adverse effects include digestive symptoms such as cramps, abdominal pain, nausea, and diarrhea. Improper use may cause electrolyte imbalance and hypokalemia and dependence.