| ATC Code | N07AA03 |
| CAS number | 17299-00-2 |
| PUB number | 3116 |
| Drugbank ID | DB13694 |
| Empirical formula | C22H32N4O4 |
| Molar mass (g·mol−1) | 416,513 |
| Physical state | solid |
| Melting point (°C) | 185,37 |
| Boiling point (°C) | 476,76 |
| PKS value | 19,23 |
| Solubility | 0.000462 mg/mL |
Distigmine is an active substance for the treatment of neurogenic bladder emptying disorders, chronic constipation and myasthenia gravis. It is an indirect parasympathomimetic agent and belongs to the group of cholinesterase inhibitors. It is a carbamic acid derivative and is usually present as distigmine bromide.
Distigmine works by inhibiting the enzyme acetylcholinesterase. This enzyme is responsible for the breakdown of acetylcholine to acetate and choline. Distigmine prevents this cleavage. This increases the concentration of acetylcholine in the synaptic cleft and the probability of muscle contraction increases. This has a particularly positive effect on the sphincter muscles of the bladder and anus, which explains the therapeutic effects on urinary incontinence and chronic constipation. In myasthenia gravis, the probability of muscle contraction is also increased.
The bioavailability, i.e. the percentage of the active ingredient available in the blood, is less than 5%. The half-life, i.e. the time the body needs to excrete half of the active substance, is approx. 69 hours. Distigmine does not cross the blood-brain barrier.
Always take Distigmin exactly as described in the package leaflet or as advised by your doctor.
The usual recommended dose for adults is 5 mg per day .
However, as Distigmin is very individualized, this is only a guide.
The following side effects may occur:
Very common:
Frequent:
Occasional:
Rarely:
Very rare:
No known interactions.
Distigmin must NOT be taken in the following cases:
Distigmine should only be taken during pregnancy after consulting your doctor, as no systematic studies have been carried out and the amount of experience is very limited. Pyridostigmine can be used as an alternative for myasthenia gravis.
Distigmine should also only be used during breastfeeding after consulting your doctor, as here too no systematic studies have been carried out and the amount of experience is also limited. Pyridostigmine is also an alternative for the treatment of myasthenia gravis during breastfeeding.
Thomas Hofko
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