MAPROTILINE HYDROCHLORIDE

MAPROTILINE HYDROCHLORIDE
(ma-proe'ti-leen)
Maprotiline HCl
Classifications: psychotherapeutic; tetracyclic antidepressant;
Therapeutic: antidepressant

Prototype: Mirtazapine
Pregnancy Category: B

Availability

25 mg, 50 mg, 75 mg tablets

Action

It selectively inhibits reuptake of norepinephrine at the neuronal membrane. More recent evidence suggests that a better explanation than norepinephrine reuptake may be that the upset of monoamine output (MAO) present in depressed individuals may be regulated by the action of beta-adrenergic receptors following long-term use of these drugs.

Therapeutic Effect

Useful in depression associated with anxiety and sleep disturbances.

Uses

Treatment of depressive neurosis (dysthymic disorder) and manic-depressive illness, depressed type (major depressive disorder).

Unlabeled Uses

Bulimia, pain, panic attack.

Contraindications

Acute MI, AV block, cardiac arrhythmias, QT prolongation; MAOI therapy; tricyclic antidepressant therapy; patients <18 y; history of alcoholism; suicidal ideation; lactation.

Cautious Use

History of seizure activity; psychotic disorders; diabetes mellitus; hepatic disease; GI disease; GERD; BPH; respiratory depression; pregnancy (category B).

Route & Dosage

Mild to Moderate Depression
Adult: PO Start at 75 mg/d and gradually increase q2wk up to 150 mg/d in single or divided doses
Geriatric: PO Start with 25 mg h.s. and gradually increase to 50–75 mg/d

Severe Depression
Adult: PO Start at 100–150 mg/d and gradually increase up to 300 mg/d in single or divided doses if needed

Administration

Oral
  • Give as single dose or in divided doses. Initiate therapy with low dosages to reduce risk of seizures.
  • Store at 15°–30° C (59°–86° F) unless otherwise specified.

Adverse Effects (≥1%)

CNS: Seizures, exacerbation of psychosis, hallucinations, tremors, excitement, confusion, dizziness, drowsiness. CV: Orthostatic hypotension, hypertension, tachycardia. Special Senses: Accommodation disturbances, blurred vision, mydriasis. GI: Nausea, vomiting, epigastric distress, constipation, dry mouth. Urogenital: Urinary retention, frequency. Skin: Hypersensitivity reactions (skin rash, urticaria, photosensitivity).

Interactions

Drug: May decrease some response to antihypertensives; cns depressants, alcohol, hypnotics, barbiturates, sedatives potentiate CNS depression; may increase hypoprothrombinemic effect of oral anticoagulants; transient delirium with ethchlorvynol; with levodopa, sympathomimetics (e.g., epinephrine, norepinephrine) there is possibility of sympathetic hyperactivity with hypertension and hyperpyrexia; with mao inhibitors or linezolid there is possibility of severe reactions, toxic psychosis, cardiovascular instability; methylphenidate increases plasma TCA levels; thyroid drugs increase possibility of arrhythmias; cimetidine may increase plasma TCA levels.

Pharmacokinetics

Absorption: Slowly absorbed from GI tract. Peak: 12 h. Distribution: Distributed chiefly to brain, lungs, liver, and kidneys. Metabolism: In liver. Elimination: 70% in urine, 30% in feces. Half-Life: 51 h.

Nursing Implications

Assessment & Drug Effects

  • Monitor for therapeutic effectiveness; 2–3 wk are usually necessary for full effect.
  • Monitor for increased suicidality, unusual changes in behavior, or suicide attempt. Inform the physician immediately.
  • Assess level of sedative effect. If recovering patient becomes too lethargic to care for personal hygiene or to maintain food intake and interactions with others, report to physician.
  • Monitor bowel elimination pattern and I&O ratio. Severe constipation and urinary retention are potential problems, especially in the older adult. Advise increased fluid intake (at least 1500 mL/d).
  • Observe seizure precautions; risk of seizures appears to be high in heavy drinkers.
  • Bear in mind that if patient uses excessive amounts of alcohol, potentiated effects of maprotiline may increase the danger of overdosage or suicide attempt.

Patient & Family Education

  • Report symptoms of stomatitis and dry mouth when taking high doses. Sore or dry mouth can lead to lack of compliance.
  • Use caution with tasks that require alertness and skill; ability may be impaired during early therapy.
  • Do not change dose or dose schedule without consulting physician.
  • Do not use OTC drugs unless approved by physician.
  • Avoid alcohol; the effects of maprotiline are potentiated when both are used together and for 2 wk after maprotiline is discontinued.

Common adverse effects in italic, life-threatening effects underlined; generic names in bold; classifications in SMALL CAPS; Canadian drug name; Prototype drug

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