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maprotiline (Ludiomil)
Tradename: Ludiomil.
Indications:
- treatment of depression
Dosage: Start 25-75 mg PO QHS, max 225 mg/day.
Tabs: 25, 50, 75 mg.
Pharmacokinetics:
1) metabolized in the liver by cyt P450 2D6
-> active metabolite desmethylmaprotiline
2) secreted into breast milk at approximately same concentration as in maternal blood
Adverse effects: (increased at > 300 ng/mL)
1) tinnitus
2) skin rash
3) constipation
4) nausea/vomiting
5) trembling
6) weight loss
7) unusual excitement
8) higher incidence of seizures than other antidepressants
9) overdose results in prolongation of the QT interval
Drug interactions:
1) coadmistration may decrease maprotiline levels
a) barbiturates
b) chloral hydrate
c) glutethimide
d) phenytoin
e) primidone
f) carbamazepine
g) smoking
h) chronic alcohol
2) coadmistration may increase maprotiline levels
a) antipsychotics
b) methylphenidate
c) fenfluramine
d) norethindrone
e) estrogens
f) isoniazid
g) disulfiram
h) alprazolam
i) cimetidine
j) erythromycin
k) chloramphenicol
3) coadministration of anticonvulsants
a) decreased seizure threshold
b) decreased effects of anticonvulsants
4) any pharmaceutical agent that inhibits cyt P450 2D6 may increase levels of maprotiline [2]
Laboratory:
1) specimen: serum
2) methods: GC, GC-MS, HPLC
3) interferences: protriptyline may interfere with HPLC assay
Notes: Maprotiline is a secondary amine.
Interactions
drug interactions
drug adverse effects (more general classes)
Related
cytochrome P450 2D6 (cytochrome P450 2D, cytochrome P450 DB1, debrisoquine-4-hydroxylase, CYP2D6)
General
tricyclic antidepressant (TCA)
Properties
MISC-INFO: elimination route LIVER
1/2life 28 HOURS
therapeutic-range 200-600 NG/ML
protein-binding 88%
elimination by hemodialysis -
peritoneal dialysis -
pregnancy-category B
safety in lactation ?
Database Correlations
PUBCHEM correlations
References
- The Pharmacological Basis of Therapeutics, 9th ed.
Gilman et al, eds. Permagon Press/McGraw Hill, 1996
- Clinical Guide to Laboratory Tests, 3rd ed. Teitz ed.,
W.B. Saunders, 1995
- Prescriber's Letter 13(3): 2006
Cytochrome P450 drug interactions
Detail-Document#: 220233
(subscription needed) http://www.prescribersletter.com