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Butylscopolamine: Adverse Effects, Contraindications, and Dosage

• Anticholinergics: general pharmacology
• Trospium chloride
• Oxybutynin
• Propiverine
• Tolterodine
• Fesoterodine
• Darifenacin
• Solifenacin
• Butylscopolamine

Mechanism of Action

Butylscopolamine is a quaternary amine with anticholinergic properties due to competitive antagonism at muscarinic receptors.

The inhibition of M₃ receptors with butylscopolamine reduces smooth muscle detrusor contraction, increases functional bladder capacity, and alleviates urinary urgency. Butylscopolamine is used to treat acute spasms and pain caused by diseases of the bile ducts, stomach, bowel, lower urinary tract, and catheter-related bladder discomfort (CRBD). Butylscopolamine has no relevant efficacy in renal colic (Weltings et al., 2021). It is not recommended for pain from the upper urinary tract.

Approval: Widely available in Europe, Asia–Pacific, Africa, South America, Mexico, and Canada. Butylscopolamine is not approved for human use in the USA.

Pharmacokinetics of Butylscopolamine

Quaternary amine, low oral bioavailability (less than 10%). Parenteral administration is more effective in cases of acute colic. Hydrolytic cleavage and excretion of metabolites via the kidneys. Half-life 5 hours.

Adverse Effects of Butylscopolamine

Muscarinic receptors are present in numerous organs. M₃ receptors are mainly found in smooth muscle and glands. Butylscopolamine lacks organ specificity for the bladder and leads to a high rate of unwanted side effects.

Eye:

• Mydriases
• Disturbed accommodation
• Dry eyes due to an inhibited lacrimal gland
• Risk of increased intraocular pressure in patients with glaucoma

Gastrointestinal tract:

• Dry mouth due to inhibited salivary glands
• Inhibition of intestinal motility (constipation)

Heart:

• Tachycardia

CNS:

Low penetration of the blood-brain barrier and thus reduced cerebral side effects compared to other anticholinergics: dizziness, headaches, and rare psychiatric side effects.

Skin:

• Dry skin due to inhibited sweat glands.
• Impaired temperature regulation in fever.

Drug Interactions

Increased anticholinergic effect with antiparkinson drugs, antihistamines, antipsychotics, and tricyclic antidepressants. Amplification of the tachycardic effect of sympathomimetic medications. Butylscopolamine mitigates the effects of gastrointestinal prokinetics.

Contraindications of Butylscopolamine

• Risk of urinary retention
• Narrow-angle glaucoma
• Ileus, gastrointestinal stenosis
• Myasthenia gravis
• Tachyarrhythmias

Dosage of Butylscopolamine

• For spasms of the urinary tract, 10–20 mg s.c. or IV up to 3–5 times daily.
• Children receive 0.3–0.6 mg/kg body weight; the maximum daily dose is 1.5 mg/kg body weight.
• Oral administration is also appropriate for gastrointestinal spasms and pain: 10–20 mg 1-1-1 p.o.

References

Holdgate A, Oh CM. Is there a role for antimuscarinics in renal colic? A randomized controlled trial. J Urol. 2005 Aug;174(2):572-5; discussion 575. doi: 10.1097/01.ju.0000165337.37317.4c.

P. Kallidonis, D. Liourdi, and E. Liatsikos, “Medical treatment for renal colic and stone expulsion,” Eur Urol Suppl, vol. 10, pp. 415–422, 2011.

Weltings S, Buddingh KT, van Diepen DC, Pelger RCM, Putter H, Rad M, Schout BMA, Roshani H. The BUSCOPAN study: a randomized-controlled non-inferiority trial of a continuous butylscopolamine infusion versus placebo in patients with a renal colic not responding to oral non-steroidal anti-inflammatory drugs. World J Urol. 2021 Jul;39(7):2747-2752. doi: 10.1007/s00345-020-03460-0. Epub 2020 Sep 19.

  Deutsche Version: Buthylscopolamin

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