Anticholinergic effects and passage through the intestinal wall of N-butylhyoscine bromide

Abstract

The effects of N‐butylhyoscine bromide (Buscopan) were examined on responses of guinea‐pig isolated intestine to transmural stimulation and to peristalsis induced by raising the intraluminal pressure. The drug acted rapidly and in low concentration to abolish peristaltic activity and responses to transmural stimulation when applied to the serosal surface of the ileum, but from 100 to 1000 times the concentration was required when it was applied to the mucosal surface. The effects were more persistent after mucosal than after serosal application. N‐Butylhyoscine bromide was bound to mucus and mucosal material, the ratio of free to bound drug being 2:1. The drug passed through portions of the intestinal wall containing Peyer's patches more rapidly than through portions containing no macroscopically visible lymphoid tissue. The rate of passage through Peyer's patches, but not through other portions, increased with increasing hydrostatic pressure. These findings help to explain why enterally administered N‐butylhyoscine bromide exerts anti‐cholinergic effects on the gut without producing systemic actions.

Effect of hyoscine butylbromide (Buscopan®) on cholinergic pathways in the human intestine

“…Therefore, there was only limited inhibition of the EFS response by HBB. The weak antisecretory effect of mucosally applied HBB is likely due to the expression of muscarinic receptors on the basolateral membrane of epithelial cells together with the very slow absorption of HBB . Moreover, our experimental conditions may not favor absorption through the mucosa as on‐going mucus secretion and lack of vascular perfusion will impair absorption through the mucosa and distribution of drugs in the tissue.…”

“…Moreover, our experimental conditions may not favor absorption through the mucosa as on‐going mucus secretion and lack of vascular perfusion will impair absorption through the mucosa and distribution of drugs in the tissue. It has been shown in preclinical in vitro (isolated guinea pig intestine) and in vivo (canine ileal and colonic motility) studies that mucosal, compared with serosal, administration of HBB required much higher concentrations to evoke spasmolytic actions. The clinical data clearly show that HBB must be absorbed in relevant concentrations as its antispasmodic effect has been shown in many studies .…”

Symptoms and Their Interpretation in Patients Self-Treating Abdominal Cramping and Pain with a Spasmolytic (Butylscopolamine Bromide)—A Pharmacy-Based Survey

“…However, orally administered butylscopolamine is only minimally absorbed [21] and hence can hardly act on the uterine muscle. For treating intestinal cramps this does not pose a problem since butylscopolamine enters the gut wall from the lumen and inhibits intestinal muscle contractions [22,23]. Its clinical efficacy is independent of the galenic formulation as tablets or capsules [24].…”

On-demand hyoscine butylbromide for the treatment of self-reported functional cramping abdominal pain

“…Hyoscine butylbromide (HBB) is a quaternary ammonium derivative that reduces the tone of smooth muscle in vitro [1]. Over the past six decades, HBB (Buscopan Ò ) has found widespread use as a spasmolytic and smooth muscle relaxant in the treatment of abdominal pain.…”