(Moclobemide)
The chemical name of moclobemide is p-chloro-N-
(2-morpholinoethyl) benzamide. Its empirical formula is C13H17O2N2Cl with a
molecular weight of 268.74.
Pharmacology:
Pharmacodynamics: Moclobemide is an antidepressant that affects the
monoaminergic cerebral neurotransmitter system by means of a reversible
inhibition of monoamine oxidase. Pharmacokinetics:
Distribution: Due to its lipophilic nature, moclobemide is extensively
distributed in the body with an apparent volume of distribution (Vss) of about
1.2L/kg. Binding of the drug to plasma proteins, mainly albumin, is relatively
low (50%).
Metabolism: Moclobemide is almost entirely metabolised before its
elimination from the body. Metabolism occurs largely via oxidative reactions on
the morpholine moiety of the molecule. Moclobemide is metabolised in part by
the polymorphic isoenzymes CYP2C9 and CYP2D6.
Blood clearance is approximately 20-50L/hr; the average
elimination half-life is two hours with a slight increase at increased doses.
Indications:
Treatment
of major depression.
Contra-indications:
Known
hypersensitivity to the drug.
Acute confusional states.
Co-administration of selegiline (L-deprenyl) is
contraindicated.
Co-administration of moclobemide with clomipramine should be
avoided in clinical practice due to the risks of increased incidence of adverse
reactions.
Serotonin Syndrome - See Interactions with other Drugs in
the original package insert.
Precautions:
Please read the original package insert for details.
Use in Pregnancy and Lactation:
Please read the original package insert for details.
Aurorix should not be used in children, as there is no
clinical experience in this age group as yet.
Interactions with other Drugs:
Please read the original package insert for details.
Adverse Reactions:
Aurorix is
usually well tolerated. No adverse event occurred with an increased frequency
of more than 5% compared to placebo. The following transient effects have been
observed: sleep disturbances, dizziness, nausea, and headache. In very rare
cases confusional states have been observed, but these rapidly disappeared on
discontinuation of therapy.
Please read the original package insert for details.
Dosage and Administration:
Adults: Aurorix therapy should be initiated in two divided daily doses. The
recommended initial daily dose is 300 or 450\mg. The recommended dose range is
300 - 600\mg/day. Aurorix should be taken after meals.
Dosage in the elderly: No dosage adjustments are necessary in elderly
patients.
Dosage in patients with impaired renal function: Single dose pharmacokinetic data
suggest that no dosage adjustment may be required in patients with reduced
renal function. However, multiple dose studies with moclobemide have not been
performed in patients with renal dysfunction, therefore Aurorix should be used
with caution in this patient population. In normal volunteers, the absolute
bioavailability almost doubles following multiple dosing as compared to a
single dose.
Dosage in patients with impaired hepatic function: In patients with severely impaired
hepatic metabolism, the daily dose of Aurorix should be reduced to half or one
third of the dose to reach the usual plasma level.
Overdosage:
Please read the original package insert for details.
Pack:
Tablets 150mg, oval, cylindrical, pale yellow, film-coated,
scored: 10s, 60s. Tablets 300\mg, oval, cylindrical, white to yellowish white,
film-coated, scored marked ROCHE 300: 10s, 60s
Storage:
Aurorix
tablets should be stored below 30&C. The tablets should not be used after
the expiry date imprinted on the blister pack and carton.
Please read the original package
insert for details!