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Trospium Chloride: Side Effects, Contraindications and Dosage
- Anticholinergics: general pharmacology
- Trospium chloride
- Oxybutynin
- Propiverine
- Tolterodine
- Fesoterodine
- Darifenacin
- Solifenacin
- Butylscopolamine
Mechanism of Action
Trospium chloride is a quaternary amine with anticholinergic properties, there is a high affinity for M1 and M3 muscarinic receptors. Due to the low penetration of the blood-brain barrier, there are fewer neurological side effects, which is advantageous for older patients or in cases of neurological side effects from other anticholinergic drugs.
The inhibition of M3 receptors with trospium chloride reduces smooth muscle detrusor contraction, increases functional bladder capacity, and alleviates urinary urgency. Trospium chloride is used to treat enuresis, overactive bladder, urge incontinence and neurogenic lower urinary tract dysfunction.
Pharmacokinetics of Trospium Chloride:
Poor bioavailability of 10% when taken orally; trospium chloride should be taken on an empty stomach. Low plasma protein binding, low penetration of the blood-brain barrier. Half-life 10–20 hours depending on galenics. Low hepatic metabolism, mainly unchanged renal excretion.
Side Effects of Trospium Chloride
Muscarinic receptors are present in numerous organs, M3 receptors are mainly found in smooth muscle and glands. Trospium lacks organ specificity for the bladder and leads to a high rate of unwanted side effects.
Eye:
- Mydriases
- Disturbed accommodation
- Dry eyes due to 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 antocholinergics: dizziness, headaches, 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. Trospium chloride mitigates the effects of gastrointestinal prokinetics.
Contraindications of Trospium Chloride
- Risk of urinary retention
- Narrow-angle glaucoma
- Ileus, gastrointestinal stenosis
- Myasthenia gravis
- Tachyarrhythmias
Dosage of Trospium Chloride:
Immediate-release formulation: 15 mg single dose 1–3 times daily up to a maximum daily dose of 45 mg. Children over 12 years receive 0.2–0.4 mg/kg body weight as a single dose. In renal insufficiency with a GFR below 30 ml/min, the maximum daily dose is 20 mg.
Trospium is also available in a extended-release formulation, with a dosage of 60 mg once daily. The extended-release formulation is not suitable for children or patients with hepatic or renal insufficiency.
Anticholinergics | Index | Oxybutynin |
Index: 1–9 A B C D E F G H I J K L M N O P Q R S T U V W X Y Z
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: Trospium Chlorid
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