Pharmacodynamics and Pharmacokinetics
Dipiroximum (active ingredient — trimedoxime bromide) is a classic cholinesterase reactivator.
Chemically, it is a quaternary ammonium compound. This structural feature is critical for its pharmacokinetics: the drug exhibits low lipophilicity and poorly crosses the blood-brain barrier (BBB). Consequently, its action is limited to the peripheral nervous system, effectively reversing peripheral signs of toxicity while having virtually no effect on the central nervous system (CNS).
In contrast, tertiary amine reactivators (such as isonitrosin) readily cross the BBB and alleviate both peripheral and central symptoms.
Indications and Clinical Use
The drug is an emergency agent used exclusively in hospital settings. Its primary goal is enzyme reactivation in severe intoxications. It is administered parenterally (intramuscularly).
Contraindications
An absolute contraindication is poisoning by reversible anticholinesterase agents (specifically carbamates). Dipiroximum is clinically ineffective in these types of intoxication.
Formulations and Administration
The drug is available in two main formulations:
- Powder;
- 15% solution in 1 mL ampoules.
Regimen: Administered intramuscularly as 1 mL of a 15% solution. If symptoms persist and continued therapy is needed, injections are repeated every 1–2 hours. The total maximum cumulative dose is strictly limited to 4 mL.
Prescription Example: Rp.: Sol. Dipiroximi 15% - 1 ml D.t.d. N. 10 in ampull. S. Intramuscularly, 1 mL. Repeat every 1–2 hours if necessary (maximum total dose — 4 mL).