Products
Distigmine bromide was commercially available in many countries in tablet form (Ubretide). It had been approved since 1973. Distribution was discontinued in 2020.
Structure and properties
Distigmine bromide (C22H32Br2N4O4, Mr = 576.3 g/mol) is a carbamic acid derivative.
Effects
Distigmine bromide (ATC N07AA03) has indirect parasympathomimetic (cholinergic) properties. The effects are due to reversible inhibition of the enzyme acetylcholinesterase, which is involved in the breakdown of acetylcholine. This enhances the effects of the neurotransmitter:
- Miosis, accommodation disorders, decrease in intraocular pressure.
- Decrease in heart rate and excitation conduction velocity.
- Contraction of the bronchial muscles
- Secretion in the stomach and small intestine
- Increase in tone and peristalsis in the gastrointestinal tract.
- Contraction of the gallbladder, ureter and detrusor of the urinary bladder.
- Increase in the secretion of sweat
- Increase in tone in the skeletal muscles
Distigmine bromide has a low bioavailability of less than 5% and a long mean half-life of 69 hours. It does not cross the blood–brain barrier.
Indications
- Neurogenic bladder voiding disorder with hypotonic detrusor.
- Hypotonic chronic constipation and megacolon.
- Myasthenia gravis.
Dosage
According to the professional information. Tablets are taken fasting, half an hour before breakfast with liquid.
Contraindications
For complete precautions, see the drug label.
Interactions
Drug-drug interactions have been described with anticholinergics, depolarizing muscle relaxants, antiarrhythmics, glucocorticoids, beta-blockers, and some antibiotics such as neomycin, streptomycin, and kanamycin.
Adverse effects
The most common possible adverse effects include nausea, vomiting, diarrhea, increased sweating, and slow heartbeat (bradycardia).
