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Pronunciation |
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(ma
PROE ti
leen) |
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U.S. Brand
Names |
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Ludiomil® |
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Generic
Available |
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Yes |
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Synonyms |
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Maprotiline Hydrochloride |
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Pharmacological Index |
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Antidepressant, Tetracyclic |
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Use |
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Treatment of depression and anxiety associated with depression
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Pregnancy Risk
Factor |
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B |
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Contraindications |
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Hypersensitivity to maprotiline; use of monoamine oxidase inhibitors within
14 days; use in a patient during the acute recovery phase of
MI |
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Adverse
Reactions |
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>10%:
Central nervous system: Drowsiness
Gastrointestinal: Xerostomia
1% to 10%:
Central nervous system: Insomnia, nervousness, anxiety, agitation, dizziness,
fatigue, headache
Gastrointestinal: Constipation, nausea
Neuromuscular & skeletal: Tremor, weakness
Ocular: Blurred vision
<1%: Hypotension, hypertension, tachycardia, palpitations, arrhythmias,
heart block, syncope, confusion, hallucinations, disorientation, delusions,
restlessness, nightmares, hypomania, mania, exacerbation of psychosis,
hyperglycemia, breast enlargement, rash, petechiae, photosensitivity,
diaphoresis (excessive), vomiting, diarrhea, bitter taste, epigastric distress,
abdominal cramps, dysphagia, weight gain or loss, edema of testicles, urinary
retention, decreased libido, impotence, numbness, tingling, motor hyperactivity,
akathisia, seizures, EPS, ataxia, dysarthria, accommodation disturbances,
mydriasis, tinnitus |
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Drug
Interactions |
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CYP1A2 and 2D6 enzyme substrate
Maprotiline inhibits the antihypertensive response to bethanidine, clonidine,
debrisoquin, guanadrel, guanethidine, guanabenz, guanfacine; monitor BP;
consider alternate antihypertensive agent
Abrupt discontinuation of clonidine may cause hypertensive crisis,
maprotiline may enhance the response
Use with altretamine may cause orthostatic hypertension
Maprotiline may be additive with or may potentiate the action of other CNS
depressants (sedatives, hypnotics, or ethanol); with MAO inhibitors,
hyperpyrexia, hypertension, tachycardia, confusion, seizures, and deaths
have been reported (serotonin syndrome), this combination should be avoided
Maprotiline may increase the prothrombin time in patients stabilized on
warfarin
Cimetidine and methylphenidate may decrease the metabolism of maprotiline
Additive anticholinergic effects seen with other anticholinergic agents
The SSRIs, to varying degrees, inhibit the metabolism of TCAs and clinical
toxicity may result
Use of lithium with a TCA may increase the risk for neurotoxicity
Phenothiazines may increase concentration of some TCAs and TCAs may increase
concentration of phenothiazines; monitor for altered clinical response
TCAs may enhance the hypoglycemic effects of tolazamide, chlorpropamide, or
insulin; monitor for changes in blood glucose levels
Cholestyramine and colestipol may bind TCAs and reduce their absorption;
monitor for altered response
TCAs may enhance the effect of amphetamines; monitor for adverse CV effects
Verapamil and diltiazem appear to decrease the metabolism of imipramine and
potentially other TCAs; monitor for increased TCA concentrations. The pressor
response to I.V. epinephrine, norepinephrine, and phenylephrine may be enhanced
in patients receiving TCAs; this combination is best avoided.
Grapefruit juice, indinavir, ritonavir may inhibit the metabolism of
clomipramine and potentially other TCAs; monitor for altered effects; a decrease
in TCA dosage may be required
Quinidine may inhibit the metabolism of TCAs; monitor for altered effect
Combined use of anticholinergics with TCAs may produce additive
anticholinergic effects; combined use of beta-agonists with TCAs may predispose
patients to cardiac arrhythmias |
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Mechanism of
Action |
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Traditionally believed to increase the synaptic concentration of
norepinephrine in the central nervous system by inhibition of their reuptake by
the presynaptic neuronal membrane. However, additional receptor effects have
been found including desensitization of adenyl cyclase, down regulation of
beta-adrenergic receptors, and down regulation of serotonin
receptors. |
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Pharmacodynamics/Kinetics |
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Absorption: Slow
Serum half-life: 27-58 hours (mean, 43 hours)
Time to peak serum concentration: Within 12 hours |
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Usual Dosage |
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Oral:
Adults: 75 mg/day to start, increase by 25 mg every 2 weeks up to 150-225
mg/day; given in 3 divided doses or in a single daily dose
Elderly: Initial: 25 mg at bedtime, increase by 25 mg every 3 days for
inpatients and weekly for outpatients if tolerated; usual maintenance dose:
50-75 mg/day, higher doses may be necessary in nonresponders
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Dietary
Considerations |
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May be administered with food to decrease GI distress |
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Dental Health: Local
Anesthetic/Vasoconstrictor
Precautions |
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Use with caution; epinephrine, norepinephrine and levonordefrin have been
shown to have an increased pressor response in combination with
TCAs |
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Dental Health:
Effects on Dental Treatment |
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>10% of patients experience dry mouth; long-term treatment with TCAs such
as amoxapine increases the risk of caries by reducing salivation and salivary
buffer capacity |
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Patient
Information |
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Avoid alcohol ingestion; do not discontinue medication abruptly; may cause
drowsiness; full effect may not occur for 3-6 weeks; dry mouth may be helped by
sips of water, sugarless gum, or hard candy; rise slowly to avoid
dizziness |
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Nursing
Implications |
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Offer patient sugarless hard candy for dry mouth
Monitor blood pressure and pulse rate prior to and during initial therapy;
evaluate mental status; monitor weight and appetite |
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Dosage Forms |
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Tablet, as hydrochloride: 25 mg, 50 mg, 75 mg |
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References |
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Bergman RN and Watson WA,
"Cardiac Toxicity Associated With Acute Maprotiline Self Poisoning," Am J
Emerg Med, 1983, 2(2):144-6.
Boakes AJ, Laurence DR, Teoh PC, et al,
"Interactions Between Sympathomimetic Amines and Antidepressant Agents in Man,"
Br Med J, 1973, 1(849):311-5.
Hrdina PD, Rovei V, Henry JF, et al,
"Comparison of Single-Dose Pharmacokinetics of Imipramine and Maprotiline in the Elderly,"
Psychopharmacology, 1980, 70(1):29-34.
Jastak JT and Yagiela JA,
"Vasoconstrictors and Local Anesthesia: A Review and Rationale for Use," J Am
Dent Assoc, 1983, 107(4):623-30.
Larochelle P, Hamet P, and Enjalbert M,
"Responses to Tyramine and Norepinephrine After Imipramine and Trazodone,"
Clin Pharmacol Ther, 1979, 26(1):24-30.
Mitchell JR,
"Guanethidine and Related Agents. III Antagonism by Drugs Which Inhibit the Norepinephrine Pump in Man,"
J Clin Invest, 1970, 49(8):1596-604.
Rundegren J, van Dijken J, Mörnstad H, et al,
"Oral Conditions in Patients Receiving Long-Term Treatment With Cyclic Antidepressant Drugs,"
Swed Dent J, 1985, 9(2):55-64.
Svedmyr N,
"The Influence of a Tricyclic Antidepressive Agent (Protriptyline) on Some of the Circulatory Effects of Noradrenaline and Adrenalin in Man,"
Life Sci, 1968, 7(1):77-84.
Wynn RL, "New Antidepressant Medications," Gen Dent, 1997, 45(1):24-8.
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