Butylscopolamine

Butylscopolamine is a synthetically produced drug from the group of muscarinic receptor antagonists (parasympatholytics) with a quaternary nitrogen group. The substance has the molecular formula C21H30NO4 and a molar mass of 440.37 g/mol. Butylscopolamine is a derivative of scopolamine and, in contrast to scopolamine, has only a peripheral effect due to its tertiary nitrogen group (this results in a high polarity, which ensures that no central nervous effects occur - Tytgat GN 2008) (Graefe KH 2016).

Butylscopolamine is a muscarinic receptor antagonist, i.e. the substance blocks the muscarinic acetylcholine receptor. Thus the substance has an antispasmodic effect on smooth muscles. In pharmacotherapy it is used in the form of its bromide salt N-butylscopolaminium bromide both orally and parenterally as an antispasmodic. In addition, butylscopolamine has an antimotility effect on the peristalsis of the stomach and intestines.

Butylscopolamine can be applied orally or rectally for mild cramps despite very low absorption (1-6%). For severe cramp-like pain, the drug can be applied intramuscularly, subcutaneously or intravenously.

Orally applied butylscopolamine is used for the treatment of intestinal cramps or for cramp-induced abdominal pain. Its efficacy has been demonstrated in phase III studies with irritable bowel syndrome patients over four weeks as well as in recurrent crampy abdominal pain over three weeks (Tytgat GN 2008).

Butylscopolamine is commonly used parenterally in combination with metamizole for severe biliary or ureteral colic, although its efficacy in ureteral colic is in doubt (Papadopoulos G et al).

Single dose for oral administration: 10 to 20 mg butylscopolaminium bromide; maximum daily dose: 60 mg butylscopolaminium bromide.

Single dose for parenteral administration: Adults with acute spastic pain receive 1 - 2 ampoules of Buscopan (single dose: 20 - 40 mg butylscopolaminium bromide; maximum daily dose: up to 100 mg butylscopolaminium bromide). The injection can be administered i. m., s. c. or slowly i. v.

Overdose symptoms are rare and are treated with the cholinesterase inhibitor physostigmine.

Due to the antagonistic effect of butylscopolamine on acetylcholine receptors and the resulting parasympathicolytic effect, the following side effects occur. They are usually minor, dose-dependent and reversible:

Constipation, dry mouth, accommodation disorders, tachycardia, micturition difficulties, hypohidrosis, nausea. Sudden deaths after intramuscular application have been described in isolated cases (Ikegaya H et al. 2006).

glaucoma, cardiac arrhythmia, heart failure, pregnancy, breastfeeding, prostate hyperplasia, thyrotoxicosis, hereditary fructose intolerance, megacolon

Buscopan®

1. DGU: S2k Guideline for the Diagnosis, Therapy and Metaphylaxis of Urolithiasis (AWMF Registry Number 043 - 025), updated 2018
2. Graefe KH et al muscarinic receptor antagonists. In: Graefe KH et al (Eds) Pharmacology and Toxicology. Georg Thieme Publisher Stuttgart S.114-115
3. Ikegaya H et al (2006) A case of sudden death after intramuscular injection of butylscopolamine bromides. Leg Med (Tokyo)8:194-197.
4. Knoll T et al (2016) S2k guidelines on diagnostics, therapy and metaphylaxis of urolithiasis (AWMF 043/025): Abstract [S2k guidelines on diagnostics, therapy and metaphylaxis of urolithiasis (AWMF 043/025): Compendium]. Urologist A 55:904-922.
5. Papadopoulos G et al (2014) Hyoscine N-butylbromide (Buscopan®) in the treatment of acute ureteral colic: what is the evidence? Urol Int 92:253-257.
6. Tytgat GN (2008) Hyoscine butylbromide - a review on its parenteral use in acute abdominal spasm and as an aid in abdominal diagnostic and therapeutic procedures. Curr Med Res Opin 24):3159-3173.