Monograph
C02AC05 - Moxonidine |
Not porphyrinogenic |
NP |
Rationale
Low dose substance; probably insignificant hepatic exposure. Structural similarity to clonidine where there are conflicting references, several of which warn strictly.
Chemical description
Clonidine-like imidazole derivative.
Therapeutic characteristics
Antihypertensive imidazoline derivative, given in a dose of 200-400 ug/d.
Hepatic exposure
Daily dose is below 1 mg and therapeutic plasmaconcentrations seem normally well below 100nM. This exposure would not be enough to give rise to clinical porphyrinogenic effects.
Metabolism and pharmacokinetics
About 50 to 75% of an oral dose is excreted as unchanged drug. No significant first passage metabolism. Oxidative liver metabolism occurs, but it has not been described which enzymes are involved. Approximately 10% to 20% of a dose is metabolised to 4,5-dehydroxymoxonidine and to a guanidine derivative by ring opening. No clinical observations of CYP interaction. Mainly eliminated by tubular excretion.
Preclinical data
None.
Personal communication
None.
Published experience
None.
IPNet drug reports
Uneventful use reported in 1 patient with acute porphyria.
Similar drugs
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