amoxapine
(a-mox-a-peen)
Asendin

Classification
Therapeutic: antidepressants

Pregnancy Category C


Copyright © 2007 by F.A. Davis Company

Indications
Treatment of depression accompanied by anxiety, often used in conjunction with psychotherapy.

Action
Potentiates the effects of serotonin and norepinephrine in the CNS. Has significant anticholinergic properties. Also has antianxiety effect related to sedative properties. Therapeutic Effects: Antidepressant and antianxiety action.

Pharmacokinetics
Absorption: Well absorbed following oral administration
Distribution: Widely distributed; enters breast milk
Protein Binding: 92% bound to plasma proteins
Metabolism and Excretion: Extensively metabolized by the liver
Half-life: 8 hr

TIME/ACTION PROFILE (antidepressant effect)

ROUTEONSETPEAKDURATION
POwithin 1–2 wk2–6 wkdays–wks


Contraindications/Precautions
Contraindicated in: Narrow-angle glaucoma.
Use Cautiously in: Geri: Geriatric patients (dosage reduction required). Pre-existing cardiovascular disease. Prostatic hypertrophy (increased susceptibility to urinary retention). History of seizures (threshold may be lowered). May ↑ risk of suicide attempt/ideation especially during dose early treatment or dose adjustment; risk may be greater in children or adolescents. OB: Pregnancy; use only if clearly needed and maternal benefits outweigh risk to fetus. Lactation (may result in sedation in infant). Children <16 yr (safety not established).

Adverse Reactions/Side Effects*
*CAPITALS indicate life threatening; underlines indicate most frequent.

CNS: NEUROLEPTIC MALIGNANT SYNDROME, fatigue, sedation, extrapyramidal reactions, tardive dyskinesia. EENT: blurred vision, dry eyes, dry mouth. CV: ARRHYTHMIAS, hypotension, ECG changes. GI: constipation, increased appetite, paralytic ileus. GU: testicular swelling, urinary retention. Derm: photosensitivity, rash. Endo: gynecomastia, sexual dysfunction. Hemat: blood dyscrasias. Misc: fever, weight gain.

Interactions
Drug–Drug: Amoxapine is metabolized in the liver by the cytochrome P450 2D6 enzyme, and its action may be affected by drugs that compete for metabolism by this enzyme, including other antidepressants, phenothiazines, carbamazepine, and class 1C antiarrhythmics including propafenone, and flecainide; when these drugs are used concurrently with amoxapine, dosage reduction of one or the other or both may be necessary. Concurrent use of other drugs that inhibit the activity of the enzyme, including cimetidine, quinidine, amiodarone, and ritonavir may result in ↑ effects of amoxapine. May cause hypotension, tachycardia, and potentially fatal reactions when used with MAO inhibitors (avoid concurrent use—discontinue 2 wk before starting amoxapine). Concurrent use with SSRI antidepressants may result in ↑ toxicity and should be avoided ( fluoxetine should be stopped 5 wk before starting amoxapine). Concurrent use with clonidine may result in hypertensive crisis and should be avoided. Concurrent use with levodopa may result in delayed/decreased absorption of levodopa or hypertension. Blood levels and effects may be ↓ by rifamycins ( rifapentine, rifampin, rifabutin). Cimetidine, fluoxetine, phenothiazines, or oral contraceptives ↑ levels and may cause toxicity. Increased risk of extrapyramidal reactions with other drugs causing extrapyramidal reactions ( phenothiazines).

Route/Dosage

PO (Adults): 50 mg 2–3 times daily, increase to 100 mg 2–3 times daily by end of 1 week (not to exceed 300 mg daily in outpatients, 600 mg daily in divided doses in hospitalized patients). Once optimal dose is achieved, may be given as a single bedtime dose; no single dose to exceed 300 mg.
PO (Geriatric Patients): 25 mg 2–3 times daily, may be increased to 50 mg 2–3 times daily (not >300 mg/day).

Availability
Tablets: 25 mg, 50 mg, 100 mg, 150 mg.

NURSING IMPLICATIONS


Assessment
Monitor mental status and affect. Assess for suicidal tendencies, especially during early therapy. Restrict amount of drug available to patient.
Monitor blood pressure and pulse before and during initial therapy. Notify physician or other health care professional of decreases in blood pressure (10–20 mmHg) or sudden increase in pulse rate. Patients taking high doses or with a history of cardiovascular disease should have ECG monitored before and periodically during therapy.
Observe for onset of extrapyramidal side effects (akathisia—restlessness; dystonia—muscle spasms and twisting motions; pseudoparkinsonism—mask facies, rigidity, tremors, drooling, shuffling gait, dysphagia, pill-rolling motions). Dose reduction or discontinuation may be necessary. Trihexyphenidyl or diphenhydramine may be used to control these symptoms.
Monitor for tardive dyskinesia (lip smacking or puckering, puffing of cheeks, rhythmic chewing or worm-like movement of tongue and mouth, uncontrolled movements of extremities). Notify physician or other health care professional immediately if these symptoms occur; they may be irreversible.
Monitor for development of neuroleptic malignant syndrome (fever, respiratory distress, tachycardia, convulsions, diaphoresis, hypertension or hypotension, pallor, tiredness, severe muscle stiffness, loss of bladder control). Notify physician or other health care professional immediately if these symptoms occur.
Lab Test Considerations: May cause ↑ serum prolactin levels Monitor CBC and differential during chronic therapy. May rarely cause bone marrow suppression.
In chronic therapy, periodically monitor hepatic and renal function. Serum glucose may be ↑ or ↓.
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Potential Nursing Diagnoses
Ineffective coping (Indications).
Risk for injury (Side Effects).


Implementation
Dose increases should be made at bedtime because of sedation. Dosage titration is a slow process; may take weeks to months. May give entire dose (if <300 mg) at bedtime, when dose is stabilized.
PO: Administer medication with or immediately after a meal to minimize gastric irritation.


Patient/Family Teaching
Instruct patient to take medication as directed. Abrupt discontinuation may cause nausea, headache, and malaise.
Inform patient of the possibility of extrapyramidal symptoms and tardive dyskinesia. Instruct patient to report these symptoms immediately.
May cause drowsiness and blurred vision. Caution patient to avoid driving and other activities requiring alertness until response to drug is known.
Orthostatic hypotension, sedation, and confusion are common during early therapy, especially in geriatric patients. Protect patient from falls and advise patient to make position changes slowly.
Advise patient to avoid alcohol or other CNS depressant drugs during and for 3–7 days after therapy.
Instruct patient to notify health care professional if dry mouth or constipation persists or if urinary retention, uncontrolled movements, or rigidity occur. Sugarless candy or gum may diminish dry mouth, and an increase in fluid intake or bulk may prevent constipation. If these symptoms persist, dosage reduction or discontinuation may be necessary. Consult health care professional if dry mouth persists for more than 2 wk.
Advise patient to inform health care professional if breast enlargement or sexual dysfunction occurs.
Caution patient to use sunscreen and protective clothing to prevent photosensitivity reactions.
Inform patient to monitor dietary intake. Increased appetite may lead to undesired weight gain.
Advise female patient to notify health care professional if pregnancy is planned or suspected or if breastfeeding.
Advise patient to notify health care professional of medication regimen before treatment or surgery.
Therapy for depression is usually prolonged. Emphasize the importance of follow-up exams to monitor effectiveness and side effects.


Evaluation/Desired Outcomes
Increased sense of well-being Renewed interest in surroundings.
Increased appetite.
Improved energy level.
Improved sleep.
Decreased anxiety. Initial response may be noted in 4–7 days in some patients. Most patients respond within 2 wk.
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Copyright © 2007 by F.A. Davis Company