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Propiverine: Mechanism of Action, Side Effects, Contraindications, and Dosage

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

Mechanism of Action

Propiverine is a lipophilic tertiary amine with anticholinergic effects on muscarinic receptors. Propiverine also has a relaxing effect on smooth muscle by inhibiting voltage-dependent calcium channels.

The inhibition of M₃ receptors with propiverine reduces smooth muscle detrusor contraction, increases functional bladder capacity, and alleviates urinary urgency. Propiverine is used to treat enuresis, overactive bladder, urge incontinence, neurogenic lower urinary tract dysfunction and catheter-related bladder discomfort (CRBD).

Pharmacokinetics of Propiverine:

Good absorption after oral administration, high first-pass metabolism in the liver. Metabolites are excreted in urine (60%) and feces. Half-life 14–20 hours.

Side Effects of Propiverine

Muscarinic receptors are present in numerous organs. M₃ receptors are mainly found in smooth muscle and glands. Propiverine lacks organ specificity for the bladder, causing 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:

• Dizziness, loss of concentration, drowsiness
• Aggravation of dementia
• Headache
• Fear, anxiety, and confusion are possible 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. Propiverine mitigates the effects of gastrointestinal prokinetics. Ketakonazole increases the plasma concentration of propiverine.

Contraindications of Propiverine

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

Dosage of Propiverine:

• For adults, the standard dosage is 15 mg 1-0-1 p.o., which can be increased to 1-1-1. Extended-release preparations are available for once-daily dosing (30–45 mg).
• Children receive 0.8 mg/kgBW/day divided into 2–3 doses.
• Propiverine is approved in the EU, UK, and Asia.

References

Ouslander 2004 OUSLANDER, J. G.: Management of overactive bladder.
In: N Engl J Med
350 (2004), Nr. 8, S. 786–99

Yoshimura und Chancellor 2002 YOSHIMURA, N. ; CHANCELLOR, M. B.: Current and future pharmacological treatment for overactive bladder.
In: J Urol
168 (2002), Nr. 5, S. 1897–913

  Deutsche Version: Nebenwirkungen und Dosierung von Propiverin

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