Maprotiline

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Maprotiline
Black Box Warning
Adult Indications & Dosage
Pediatric Indications & Dosage
Contraindications
Warnings & Precautions
Adverse Reactions
Drug Interactions
Use in Specific Populations
Administration & Monitoring
Overdosage
Pharmacology
Clinical Studies
How Supplied
Images
Patient Counseling Information
Precautions with Alcohol
Brand Names
Look-Alike Names

Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]; Associate Editor(s)-in-Chief: Pratik Bahekar, MBBS [2]

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Black Box Warning

Suicidality and Antidepressant Drugs
See full prescribing information for complete Boxed Warning.
Condition Name: Antidepressants increased the risk compared to placebo of suicidal thinking and behavior (suicidality) in children, adolescents and young adults in short-term studies of major depressive disorder (MDD) and other psychiatric disorders. Anyone considering the use of maprotiline or any other antidepressant in a child, adolescent, or young adult must balance this risk with the clinical need. Short-term studies did not show an increase in the risk of suicidality with antidepressants compared to placebo in adults beyond age 24; there was a reduction in risk with antidepressants compared to placebo in adults aged 65 and older. Depression and certain other psychiatric disorders are themselves associated with increases in the risk of suicide. Patients of all ages who are started on antidepressant therapy should be monitored appropriately and observed closely for clinical worsening, suicidality, or unusual changes in behavior. Families and caregivers should be advised of the need for close observation and communication with the prescriber. Maprotiline is not approved for use in pediatric patients. (See warning: Clinical Worsening and Suicide Risk, precautions: Information for Patients and precautions: Pediatric Use.)

Overview

Maprotiline is a tetracyclic antidepressant that is FDA approved for the {{{indicationType}}} of bipolar disorder, depressed phase, depression, dysthymia, mixed anxiety and depressive disorder. There is a Black Box Warning for this drug as shown here. Common adverse reactions include constipation, xerostomia, dizziness , feeling nervous , myoclonus, somnolence, blurred vision, visual disturbance.

Adult Indications and Dosage

FDA-Labeled Indications and Dosage (Adult)

  • Bipolar disorder, depressed phase
  • Outpatients: 75 mg/day PO (2-3 divided doses) for 2 weeks; may increase in 25 mg increments up to a max of 225 mg/day in single or divided doses
  • Inpatients: 100-150 mg/day PO (2-3 divided doses) for 2 weeks; may increase in 25 mg increments up to a max of 225 mg/day in single or divided doses
  • Maintenance: 75-150 mg/day PO in single or divided doses
  • Depression
  • 75 mg/day PO (2-3 divided doses) for 2 weeks; increase in 25 mg increments up to a max of 225 mg/day in single or divided doses
  • Inpatients: 100-150 mg/day PO (2-3 divided doses) for 2 weeks, increase in 25 mg increments up to a max of 225 mg/day in single or divided doses
  • Maintenance: 75-150 mg/day ORALLY in single or divided doses
  • Dysthymia
  • 75 mg/day PO (2-3 divided doses) for 2 weeks, increase in 25 mg increments up to a max of 225 mg/day in single or divided doses
  • Inpatients: 100-150 mg/day PO (2-3 divided doses) for 2 weeks; may increase in 25 mg increments up to a MAX of 225 mg/day in single or divided doses
  • Maintenance: 75-150 mg/day ORALLY in single or divided doses
  • Mixed anxiety and depressive disorder
  • Outpatients 75 mg/day PO (2-3 divided doses) for 2 weeks, increase in 25 mg increments up to a max of 225 mg/day in single or divided doses
  • Inpatients: 100-150 mg/day PO (2-3 divided doses) for 2 weeks, increase in 25 mg increments up to a max of 225 mg/day in single or divided doses
  • Maintenance: 75-150 mg/day ORALLY in single or divided doses

Off-Label Use and Dosage (Adult)

Guideline-Supported Use

There is limited information about Off-Label Guideline-Supported Use of Maprotiline in adult patients.

Non–Guideline-Supported Use

  • Pain
  • There is limited information about Off-Label Non–Guideline-Supported Use of Maprotiline in adult patients.

Pediatric Indications and Dosage

FDA-Labeled Indications and Dosage (Pediatric)

Safety has not been established below 18 years of age.

Off-Label Use and Dosage (Pediatric)

Guideline-Supported Use

There is limited information about Off-Label Guideline-Supported Use of Maprotiline in pediatric patients.

Non–Guideline-Supported Use

  • There is limited information about Off-Label Non–Guideline-Supported Use of Maprotiline in pediatric patients.

Contraindications

  • Contraindicated in patients hypersensitive to maprotiline and in patients with known or suspected seizure disorders.
  • It should not be given concomitantly with monoamine oxidase (MAO) inhibitors.
  • A minimum of 14 days should be allowed to elapse after discontinuation of MAO inhibitors before treatment with maprotiline is initiated.
  • Effects should be monitored with gradual increase in dosage until optimum response is achieved.
  • Not recommended for use during the acute phase of myocardial infarction.

Warnings

Suicidality and Antidepressant Drugs
See full prescribing information for complete Boxed Warning.
Condition Name: Antidepressants increased the risk compared to placebo of suicidal thinking and behavior (suicidality) in children, adolescents and young adults in short-term studies of major depressive disorder (MDD) and other psychiatric disorders. Anyone considering the use of maprotiline or any other antidepressant in a child, adolescent, or young adult must balance this risk with the clinical need. Short-term studies did not show an increase in the risk of suicidality with antidepressants compared to placebo in adults beyond age 24; there was a reduction in risk with antidepressants compared to placebo in adults aged 65 and older. Depression and certain other psychiatric disorders are themselves associated with increases in the risk of suicide. Patients of all ages who are started on antidepressant therapy should be monitored appropriately and observed closely for clinical worsening, suicidality, or unusual changes in behavior. Families and caregivers should be advised of the need for close observation and communication with the prescriber. Maprotiline is not approved for use in pediatric patients. (See warning: Clinical Worsening and Suicide Risk, precautions: Information for Patients and precautions: Pediatric Use.)

Clinical Worsening and Suicide Risk

  • Patients with major depressive disorder (MDD), both adult and pediatric, may experience worsening of their depression and/or the emergence of suicidal ideation and behavior (suicidality) or unusual changes in behavior, whether or not they are taking antidepressant medications, and this risk may persist until significant remission occurs. Suicide is a known risk of depression and certain other psychiatric disorders, and these disorders themselves are the strongest predictors of suicide. There has been a long-standing concern, however, that antidepressants may have a role in inducing worsening of depression and the emergence of suicidality in certain patients during the early phases of treatment. Pooled analyses of short-term placebo-controlled trials of antidepressant drugs (SSRIs and others) showed that these drugs increase the risk of suicidal thinking and behavior (suicidality) in children, adolescents, and young adults (ages 18 to 24) with major depressive disorder (MDD) and other psychiatric disorders. Short-term studies did not show an increase in the risk of suicidality with antidepressants compared to placebo in adults beyond age 24; there was a reduction with antidepressants compared to placebo in adults aged 65 and older.
  • The pooled analyses of placebo-controlled trials in children and adolescents with MDD, obsessive compulsive disorder (OCD), or other psychiatric disorders included a total of 24 short-term trials of 9 antidepressant drugs in over 4,400 patients. The pooled analyses of placebo-controlled trials in adults with MDD or other psychiatric disorders included a total of 295 short-term trials (median duration of 2 months) of 11 antidepressant drugs in over 77,000 patients. There was considerable variation in risk of suicidality among drugs, but a tendency toward an increase in the younger patients for almost all drugs studied. There were differences in absolute risk of suicidality across the different indications, with the highest incidence in MDD. The risk differences (drug vs. placebo), however, were relatively stable within age strata and across indications.
  • No suicides occurred in any of the pediatric trials. There were suicides in the adult trials, but the number was not sufficient to reach any conclusion about drug effect on suicide.
  • It is unknown whether the suicidality risk extends to longer-term use, i.e., beyond several months. However, there is substantial evidence from placebo-controlled maintenance trials in adults with depression that the use of antidepressants can delay the recurrence of depression.
  • All patients being treated with antidepressants for any indication should be monitored appropriately and observed closely for clinical worsening, suicidality and unusual changes in behavior, especially during the initial few months of a course of drug therapy, or at times of dose changes, either increases or decreases.
  • The following symptoms, anxiety, agitation, panic attacks, insomnia, irritability, hostility, aggressiveness, impulsivity, akathisia (psychomotor restlessness), hypomania, and mania, have been reported in adult and pediatric patients being treated with antidepressants for major depressive disorder as well as for other indications, both psychiatric and nonpsychiatric. Although a causal link between the emergence of such symptoms and either the worsening of depression and/or the emergence of suicidal impulses has not been established, there is concern that such symptoms may represent precursors to emerging suicidality.
  • Consideration should be given to changing the therapeutic regimen, including possibly discontinuing the medication, in patients whose depression is persistently worse, or who are experiencing emergent suicidality or symptoms that might be precursors to worsening depression or suicidality, especially if these symptoms are severe, abrupt in onset, or were not part of the patient's presenting symptoms.
  • Families and caregivers of patients being treated with antidepressants for major depressive disorder or other indications, both psychiatric and nonpsychiatric, should be alerted about the need to monitor patients for the emergence of agitation, irritability, unusual changes in behavior, and the other symptoms described above, as well as the emergence of suicidality, and to report such symptoms immediately to healthcare providers. Such monitoring should include daily observation by families and caregivers. Prescriptions for maprotiline should be written for the smallest quantity of tablets consistent with good patient management, in order to reduce the risk of overdose.

Screening Patients for Bipolar Disorder

  • A major depressive episode may be the initial presentation of bipolar disorder. It is generally believed (though not established in controlled trials) that treating such an episode with an antidepressant alone may increase the likelihood of precipitation of a mixed/manic episode in patients at risk for bipolar disorder. Whether any of the symptoms described above represent such a conversion is unknown. However, prior to initiating treatment with an antidepressant, patients with depressive symptoms should be adequately screened to determine if they are at risk for bipolar disorder; such screening should include a detailed psychiatric history, including a family history of suicide, bipolar disorder, and depression. It should be noted that maprotiline is not approved for use in treating bipolar depression.

Seizures have been associated with the use of maprotiline

  • Most of the seizures have occurred in patients without a known history of seizures. However, in some of these cases, other confounding factors were present, including concomitant medications known to lower the seizure threshold, rapid escalation of the dosage of maprotiline, and dosage that exceeded the recommended therapeutic range. The incidence of direct reports is less than 1/10 of 1%. The risk of seizures may be increased when maprotiline is taken concomitantly with phenothiazines, when the dosage of benzodiazepines is rapidly tapered in patients receiving maprotiline or when the recommended dosage of maprotiline hydrochloride is exceeded. While a cause and effect relationship has not been established, the risk of seizures in patients treated with maprotiline may be reduced by
  1. Initiating therapy at a low dosage,
  2. Maintaining the initial dosage for 2 weeks before raising it gradually in small increments as necessitated by the long half-life of maprotiline (average 51 hours), and
  3. Keeping the dosage at the minimally effective level during maintenance therapy. (See dosage and administration.)
  • Extreme caution should be used when this drug is given to:
  • Patients with a history of myocardial infarction;
  • Patients with a history or presence of cardiovascular disease because of the possibility of conduction defects, arrhythmias, myocardial infarction, strokes and tachycardia.

General precautions

  • The possibility of suicide in seriously depressed patients is inherent in their illness and may persist until significant remission occurs. Therefore, patients must be carefully supervised during all phases of treatment with maprotiline, and prescriptions should be written for the smallest number of tablets consistent with good patient management.
  • Hypomanic or manic episodes have been known to occur in some patients taking tricyclic antidepressant drugs, particularly in patients with cyclic disorders. Such occurrences have also been noted, rarely, with maprotiline.
  • Prior to elective surgery, maprotiline should be discontinued for as long as clinically feasible, since little is known about the interaction between maprotiline and general anesthetics.
  • Maprotiline should be administered with caution in patients with increased intraocular pressure, history of urinary retention, or history of narrow angle glaucoma because of the drug's anticholinergic properties.

Adverse Reactions

Clinical Trials Experience

Central Nervous System

Drowsiness (16%), dizziness (8%), tremor (3%), and, rarely, numbness, tingling, motor hyperactivity, akathisia, seizures, EEG alterations, tinnitus, extrapyramidal symptoms, ataxia, and dysarthria.

Cardiovascular

Rare occurrences of hypotension, hypertension, tachycardia, palpitation, arrhythmia, heart block, and syncope have been reported with maprotiline.

psychiatric

Nervousness (6%), anxiety (3%), insomnia (2%), and agitation (2%); rarely, confusional states (especially in the elderly), hallucinations, disorientation, delusions, restlessness, nightmares, hypomania, mania, exacerbation of psychosis, decrease in memory, and feelings of unreality.

Gastrointestinal

Nausea (2%) and, rarely, vomiting, epigastric distress, diarrhea, bitter taste, abdominal cramps and dysphagia.

Hypersensitive Reactions

Rare instances of skin rash, petechiae, itching, photosensitization, edema, and drug fever.

Anticholinergic

Dry mouth (22%), constipation (6%), and blurred vision (4%); rarely, accommodation disturbances, mydriasis, urinary retention, and delayed micturition.

Miscellaneous

Weakness and fatigue (4%) and headache (4%); rarely, altered liver function, jaundice, weight loss or gain, excessive perspiration, flushing, urinary frequency, increased salivation, nasal congestion and alopecia.

Postmarketing Experience

There is limited information regarding Maprotiline Postmarketing Experience in the drug label.

Drug Interactions

  • Anticholinergic or sympathomimetic drugs
  • Close supervision and careful adjustment of dosage are required when administering maprotiline concomitantly with anticholinergic or sympathomimetic drugs because of the possibility of additive atropine like effects.
  • Electroshock therapy
  • Concurrent administration of maprotiline with electroshock therapy should be avoided because of the lack of experience in this area.
  • Thyroid medication
  • Caution should be exercised when administering maprotiline to hyperthyroid patients or those on thyroid medication because of the possibility of enhanced potential for cardiovascular toxicity of maprotiline.
  • Guanethidine
  • Maprotiline should be used with caution in patients receiving guanethidine or similar agents since it may block the pharmacologic effects of these drugs.
  • Phenothiazines or benzodiazepines
  • The risk of seizures may be increased when maprotiline is taken concomitantly with phenothiazines or when the dosage of benzodiazepines is rapidly tapered in patients receiving maprotiline.
  • Hepatic enzyme inhibitors
  • Because of the pharmacologic similarity of maprotiline hydrochloride to the tricyclic antidepressants, the plasma concentration of maprotiline may be increased when the drug is given concomitantly with hepatic enzyme inhibitors (e.g., cimetidine, fluoxetine) and decreased by concomitant administration with hepatic enzyme inducers (e.g., barbiturates, phenytoin), as has occurred with tricyclic antidepressants. Adjustment of the dosage of maprotiline hydrochloride may therefore be necessary in such cases.

Use in Specific Populations

Pregnancy

Pregnancy Category (FDA): B Reproduction studies have been performed in female laboratory rabbits, mice, and rats at doses up to 1.3, 7, and 9 times the maximum daily human dose respectively and have revealed no evidence of impaired fertility or harm to the fetus due to maprotiline. There are, however, no adequate and well controlled studies in pregnant women. Because animal reproduction studies are not always predictive of human response, this drug should be used during pregnancy only if clearly needed.
Pregnancy Category (AUS): There is no Australian Drug Evaluation Committee (ADEC) guidance on usage of Maprotiline in women who are pregnant.

Labor and Delivery

Although the effect of maprotiline on labor and delivery is unknown, caution should be exercised as with any drug with CNS depressant action.

Nursing Mothers

Maprotiline is excreted in breast milk. At steady-state, the concentrations in milk correspond closely to the concentrations in whole blood. Caution should be exercised when maprotiline hydrochloride is administered to a nursing woman.

Pediatric Use

Safety and effectiveness in the pediatric population have not been established. Anyone considering the use of maprotiline in a child or adolescent must balance the potential risks with the clinical need.

Geriatic Use

There is no FDA guidance on the use of Maprotiline in geriatric settings.

Gender

There is no FDA guidance on the use of Maprotiline with respect to specific gender populations.

Race

There is no FDA guidance on the use of Maprotiline with respect to specific racial populations.

Renal Impairment

There is no FDA guidance on the use of Maprotiline in patients with renal impairment.

Hepatic Impairment

There is no FDA guidance on the use of Maprotiline in patients with hepatic impairment.

Females of Reproductive Potential and Males

There is no FDA guidance on the use of Maprotiline in women of reproductive potentials and males.

Immunocompromised Patients

There is no FDA guidance one the use of Maprotiline in patients who are immunocompromised.

Administration and Monitoring

Administration

  • A single daily dose is an alternative to divided daily doses. Therapeutic effects are sometimes seen within 3 to 7 days, although as long as 2 to 3 weeks are usually necessary.
  • Initial Adult Dosage
  • An initial dosage of 75 mg daily is suggested for outpatients with mild to moderate depression. However, in some patients, particularly the elderly, an initial dosage of 25 mg daily may be used. Because of the long half-life of maprotiline, the initial dosage should be maintained for 2 weeks. The dosage may then be increased gradually in 25 mg increments as required and tolerated. In most outpatients a maximum dose of 150 mg daily will result in therapeutic efficacy. It is recommended that this dose not be exceeded except in the most severely depressed patients. In such patients, dosage may be gradually increased to a maximum of 225 mg.
  • More severely depressed, hospitalized patients should be given an initial daily dose of 100 mg to 150 mg which may be gradually increased as required and tolerated. Most hospitalized patients with moderate to severe depression respond to a daily dose of 150 mg although dosages as high as 225 mg may be required in some cases. Daily dosage of 225 mg should not be exceeded.
  • Elderly Patients
  • In general, lower dosages are recommended for patients over 60 years of age. Dosages of 50 mg to 75 mg daily are usually satisfactory as maintenance therapy for elderly patients who do not tolerate higher amounts.

Monitoring

  • Maintenance
  • Dosage during prolonged maintenance therapy should be kept at the lowest effective level. Dosage may be reduced to levels of 75 mg to 150 mg daily during such periods, with subsequent adjustment depending on therapeutic response.

IV Compatibility

There is limited information regarding the compatibility of Maprotiline and IV administrations.

Overdosage

  • Deaths may occur from overdosage with this class of drugs. Multiple drug ingestion (including alcohol) is common in deliberate overdose. As the management is complex and changing, it is recommended that the physician contact a poison control center for current information on treatment. Signs and symptoms of toxicity develop rapidly after overdose. Therefore, hospital monitoring is required as soon as possible.
  • Animal Oral LD50
  • The oral LD50 of maprotiline hydrochloride is 600 to 750 mg/kg in mice, 760 to 900 mg/kg in rats, > 1000 mg/kg in rabbits, > 300 mg/kg in cats, and > 30 mg/kg in dogs.
  • Manifestations
  • Data dealing with overdosage in humans are limited with only a few cases on record. Signs and symptoms of maprotiline hydrochloride overdose are similar to those seen with tricyclic overdose. Critical manifestations of overdose include cardiac dysrhythmias, severe hypotension, convulsions and CNS depression including coma. Changes in the electrocardiogram, particularly in QRS axis or width are clinically significant indicators of toxicity. Other clinical manifestations include drowsiness, tachycardia, ataxia, vomiting, cyanosis, shock, restlessness, agitation, hyperpyrexia, muscle rigidity, athetoid movements, and mydriasis. Since congestive heart failure has been seen with overdosages of tricyclic antidepressants, it should be considered with maprotiline hydrochloride overdosage.
  • Management
  • Obtain an ECG and immediately initiate cardiac monitoring. Protect the patient's airway, establish an intravenous line and initiate gastric decontamination. A minimum of 6 hours of observation with cardiac monitoring and observation for signs of CNS or respiratory depression, hypotension, cardiac dysrhythmias and/or conduction blocks, and seizures is necessary. If signs of toxicity occur at any time during this period, extended monitoring is required. There are case reports of patients succumbing to fatal dysrhythmias late after tricyclic overdose; these patients had clinical evidence of significant poisoning prior to death and most received inadequate gastrointestinal decontamination. Monitoring of plasma drug levels should not guide management of the patient.
  • Gastrointestinal Decontamination
  • All patients suspected of overdose should receive gastrointestinal decontamination. This should include large volume gastric lavage followed by activated charcoal. If consciousness is impaired, the airway should be secured prior to lavage. Emesis is contraindicated.
  • Cardiovascular
  • A maximal limb lead QRS duration of ≥ 0.10 seconds may be the best indication of the severity of the overdose. Intravenous sodium bicarbonate should be used to maintain the serum pH in the range of 7.45 to 7.55. If the pH response is inadequate, hyperventilation may also be used. :*Concomitant use of hyperventilation and sodium bicarbonate should be done with extreme caution, with frequent pH monitoring. A pH > 7.60 or a Pco2 < 20 mmHg is undesirable. Dysrhythmias unresponsive to sodium bicarbonate therapy/hyperventilation may respond to lidocaine, bretylium, or phenytoin. Type 1A and 1C antiarrhythmics are generally contraindicated (e.g., quinidine, disopyramide, and procainamide).
  • In rare instances, hemoperfusion may be beneficial in acute refractory cardiovascular instability in patients with acute toxicity. However, hemodialysis, peritoneal dialysis, exchange transfusions, and forced diuresis generally have been reported as ineffective.
  • CNS
  • In patients with CNS depression, early intubation is advised because of the potential for abrupt deterioration. Seizures should be controlled with benzodiazepines, or if these are ineffective, other anticonvulsants (e.g., phenobarbital, phenytoin). Physostigmine is not recommended except to treat life threatening symptoms that have been unresponsive to other therapies, and then only in consultation with a poison control center.
  • Psychiatric Follow-up
  • Since overdosage is often deliberate, patients may attempt suicide by other means during the recovery phase. Psychiatric referral may be appropriate.
  • Pediatric Management
  • The principles of management of child and adult overdosages are similar. It is strongly recommended that the physician contact the local poison control center for specific pediatric treatment.

Pharmacology

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Maprotiline
Systematic (IUPAC) name
N-Methyl-9,10-ethanoanthracene-9(10H)-propanamine
Identifiers
CAS number 10262-69-8
ATC code N06AA21
PubChem 4011
DrugBank DB00934
Chemical data
Formula C20H23N 
Mol. mass 277.403 g/mol
SMILES eMolecules & PubChem
Pharmacokinetic data
Bioavailability 66 to 70%
Protein binding 88%
Metabolism hepatic
Half life 27-58 hours
Excretion biliar (30%) and urine (57%) as gluconurides, 3 to 4% as unchanged drug
Therapeutic considerations
Pregnancy cat.

?(US)

Legal status

Prescription Only (S4)(AU) -only(US)

Routes oral, intramuscular, intravenous (infusion)

Mechanism of Action

The mechanism of action of maprotiline is not precisely known. It does not act primarily by stimulation of the central nervous system and is not a monoamine oxidase inhibitor. The postulated mechanism of maprotiline is that it acts primarily by potentiation of central adrenergic synapses by blocking reuptake of norepinephrine at nerve endings. This pharmacologic action is thought to be responsible for the drug's antidepressant and anxiolytic effects. The mean time to peak is 12 hours. The half-life of elimination averages 51 hours. It exerts blocking effects at the following postsynaptic receptors:

  • Strong : alpha1
  • Moderate : 5-HT2, muscarinic, H1, D2
  • Weak : alpha2
  • Extremely weak : 5-HT1

The pharmacologic profile of Maprotiline explains its antidepressant, sedative, anxiolytic, sympatholytic, and anticholinergic activities. Additionally, it shows a strong antagonism against Reserpine-induced effects in animal studies, as do the other 'classical' antidepressants. Although Maprotiline behaves in most regards as a 'first generation antidepressant' it is commonly referred to as 'second generation antidepressant'.

Sedation has a fast onset (the same day), while remission of the depression itself is noted usually after a latent period of one to four weeks.

Maprotiline does not brighten up the mood in nondepressed persons.

Structure

Maprotiline hydrochloride, USP is a tetracyclic antidepressant, available as 25 mg, 50 mg and 75 mg tablets for oral administration. Its chemical name is N-methyl-9,10-ethanoanthracene-9(10H)-propylamine hydrochloride, and its structural formula is:

This image is provided by the National Library of Medicine.

Maprotiline hydrochloride is a fine, white to off-white, practically odorless crystalline powder. It is freely soluble in methanol and in chloroform, slightly soluble in water, and practically insoluble in isooctane. Its molecular weight is 313.87. The tablets contain the following inactive ingredients: colloidal silicon dioxide, croscarmellose sodium, hypromellose, magnesium stearate, microcrystalline cellulose, polydextrose, polyethylene glycol, pregelatinized starch, sodium lauryl sulfate, titanium dioxide and triacetin. Additionally, the 50 mg tablet contains FD&C Blue No. 1 Aluminum Lake.

Pharmacodynamics

There is limited information regarding Maprotiline Pharmacodynamics in the drug label.

Pharmacokinetics

There is limited information regarding Maprotiline Pharmacokinetics in the drug label.

Nonclinical Toxicology

There is limited information regarding Maprotiline Nonclinical Toxicology in the drug label.

Clinical Studies

There is limited information regarding Maprotiline Clinical Studies in the drug label.

How Supplied

Maprotiline Hydrochloride, USP is available as tablets containing 25 mg, 50 mg, or 75 mg of maprotiline hydrochloride. The 25 mg tablets are white film-coated, round, scored tablets debossed with 6 to the left of the score and 0 to the right of the score on one side of the tablet and M on the other side. They are available as follows: NDC 0378-0060-01 bottles of 100 tablets The 50 mg tablets are light blue film-coated, round, scored, tablets debossed with 8 to the left of the score and 7 to the right of the score on one side and M on the other side. They are available as follows: NDC 0378-0087-01 bottles of 100 tablets The 75 mg tablets are white film-coated, round, scored tablets debossed with 9 to the left of the score and 2 to the right of the score on one side and M on the other side. They are available as follows: NDC 0378-0092-01 bottles of 100 tablets

Storage

Store at 20° to 25°C (68° to 77°F). [See USP for Controlled Room Temperature.]

Images

Drug Images

003780060.jpg

Drug Name: Maprotiline Hydrochloride 25 MG Oral Tablet
Ingredient(s): silicon dioxide, croscarmellose sodium, hypromelloses, magnesium stearate, cellulose, microcrystalline, polydextrose, polyethylene glycols, starch, corn, sodium lauryl sulfate, titanium dioxide, triacetin
Imprint: 6;0;M
Dosage: 25 mg
Color(s): White
Shape: Round
Size (mm): 6
Score: 2
NDC:0378-0060-01

Drug Label Author: Mylan Pharmaceuticals Inc.

This pill image is provided by the National Library of Medicine's PillBox.
003780087.jpg

Drug Name: Maprotiline Hydrochloride 50 MG Oral Tablet
Ingredient(s): silicon dioxide, croscarmellose sodium, fd&c blue no. 1, hypromelloses, magnesium stearate, cellulose, microcrystalline, polydextrose, polyethylene glycols, starch, corn, sodium lauryl sulfate, titanium dioxide, triacetin
Imprint: 8;7;M
Dosage: 50 mg
Color(s): Blue
Shape: Round
Size (mm): 7
Score: 2
NDC:0378-0087-01

Drug Label Author: Mylan Pharmaceuticals Inc.

This pill image is provided by the National Library of Medicine's PillBox.
003780092.jpg

Drug Name: Maprotiline Hydrochloride 75 MG Oral Tablet
Ingredient(s): silicon dioxide, croscarmellose sodium, hypromelloses, magnesium stearate, cellulose, microcrystalline, polydextrose, polyethylene glycols, starch, corn, sodium lauryl sulfate, titanium dioxide, triacetin
Imprint: 9;2;M
Dosage: 75 mg
Color(s): White
Shape: Round
Size (mm): 8
Score: 2
NDC:0378-0092-01

Drug Label Author: Mylan Pharmaceuticals Inc.

This pill image is provided by the National Library of Medicine's PillBox.

Package and Label Display Panel

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This image of the FDA label is provided by the National Library of Medicine.
MAPRO3.jpg
This image of the FDA label is provided by the National Library of Medicine.
MAPRO4.jpg
This image of the FDA label is provided by the National Library of Medicine.
Mapro5.jpg
This image of the FDA label is provided by the National Library of Medicine.

Patient Counseling Information

Prescribers or other health professionals should inform patients, their families, and their caregivers about the benefits and risks associated with treatment with maprotiline and should counsel them in its appropriate use. A patient Medication Guide about "Antidepressant Medicines, Depression and other Serious Mental Illness and Suicidal Thoughts or Actions" is available for maprotiline. The prescriber or health professional should instruct patients, their families, and their caregivers to read the Medication Guide and should assist them in understanding its contents. Patients should be given the opportunity to discuss the contents of the Medication Guide and to obtain answers to any questions they may have. The complete text of the Medication Guide is reprinted at the end of this document. Patients should be advised of the following issues and asked to alert their prescriber if these occur while taking maprotiline.

Clinical Worsening and Suicide Risk

Patients, their families and their caregivers should be encouraged to be alert to the emergence of anxiety, agitation, panic attacks, insomnia, irritability, hostility, aggressiveness, impulsivity, akathisia (psychomotor restlessness), hypomania, mania, other unusual changes in behavior, worsening of depression, and suicidal ideation, especially early during antidepressant treatment and when the dose is adjusted up or down. Families and caregivers of patients should be advised to look for the emergence of such symptoms on a day to day basis, since changes may be abrupt. Such symptoms should be reported to the patient's prescriber or health professional, especially if they are severe, abrupt in onset, or were not part of the patient's presenting symptoms. Symptoms such as these may be associated with an increased risk for suicidal thinking and behavior and indicate a need for very close monitoring and possibly changes in the medication.

  • Medication Guide
  • Antidepressant Medicines, Depression and other Serious Mental Illnesses, and Suicidal Thoughts or Actions

Read the Medication Guide that comes with you or your family member's antidepressant medicine. This Medication Guide is only about the risk of suicidal thoughts and actions with antidepressant medicines. Talk to your, or your family member's, healthcare provider about:

  • All risks and benefits of treatment with antidepressant medicines
  • All treatment choices for depression or other serious mental illness
  • What is the most important information I should know about antidepressant medicines, depression and other serious mental illnesses, and suicidal thoughts or actions?
  • Antidepressant medicines may increase suicidal thoughts or actions in some children, teenagers, and young adults within the first few months of treatment.
  • Depression and other serious mental illnesses are the most important causes of suicidal thoughts and actions. Some people may have a particularly high risk of having suicidal thoughts or actions. These include people who have (or have a family history of) bipolar illness also called manic-depressive illness) or suicidal thoughts or actions.
  • How can I watch for and try to prevent suicidal thoughts and actions in myself or a family member?
  • Pay close attention to any changes, especially sudden changes, in mood, behaviors, thoughts, or feelings. This is very important when an antidepressant medicine is started or when the dose is changed.
  • Call the healthcare provider right away to report new or sudden changes in mood, behavior, thoughts, or feelings.
  • Keep all follow-up visits with the healthcare provider as scheduled. Call the healthcare provider between visits as needed, especially if you have concerns about symptoms.
  • Call a healthcare provider right away if you or your family member has any of the following symptoms, especially if they are new, worse, or worry you:
  • Thoughts about suicide or dying
  • Attempts to commit suicide
  • New or worse depression
  • New or worse anxiety
  • Feeling very agitated or restless
  • Panic attacks
  • Trouble sleeping (insomnia)
  • New or worse irritability
  • Acting aggressive, being angry, or violent
  • Acting on dangerous impulses
  • An extreme increase in activity and talking (mania)
  • Other unusual changes in behavior or mood
  • What else do I need to know about antidepressant medicines?
  • Never stop an antidepressant medicine without first talking to a healthcare provider. Stopping an antidepressant medicine suddenly can cause other symptoms.
  • Antidepressants are medicines used to treat depression and other illnesses. It is important to discuss all the risks of treating depression and also the risks of not treating it. Patients and their families or other caregivers should discuss all treatment choices with the healthcare provider, not just the use of antidepressants.
  • Antidepressant medicines have other side effects. Talk to the healthcare provider about the side effects of the medicine prescribed for you or your family member.
  • Antidepressant medicines can interact with other medicines. Know all of the medicines that you or your family member takes. Keep a list of all medicines to show the healthcare provider. Do not start new medicines without first checking with your healthcare provider.
  • Not all antidepressant medicines prescribed for children are FDA approved for use in children. Talk to your child's healthcare provider for more information.
  • Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.
  • This Medication Guide has been approved by the U.S. Food and Drug Administration for all antidepressants.

Precautions with Alcohol

Alcohol-Maprotiline interaction has not been established. Talk to your doctor about the effects of taking alcohol with this medication.

Brand Names

There is limited information regarding Maprotiline Brand Names in the drug label.

Look-Alike Drug Names

There is limited information regarding Maprotiline Look-Alike Drug Names in the drug label.

Drug Shortage Status

Price

References

The contents of this FDA label are provided by the National Library of Medicine.









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