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