dox·e·pin hydrochloride (d k s -p n )n. A tricyclic antidepressant drug. |
doxepin hydrochloride
doxepin hydrochloride
Apo-Doxepin (CA), Novo-Doxepin (CA), Prudoxin, Zonalon
Pharmacologic class: Tricyclic antidepressant
Therapeutic class: Antidepressant, anxiolytic, antipruritic
Pregnancy risk category C
FDA Boxed Warning
• Drug may increase risk of suicidal thinking and behavior in children and adolescents with major depressive disorder and other psychiatric disorders. Risk must be balanced with clinical need, as depression itself increases suicide risk. With patient of any age, observe closely for clinical worsening, suicidality, and unusual behavior changes when therapy begins. Advise family and caregivers to observe patient closely and communicate with prescriber as needed.
• Drug isn't approved for use in pediatric patients.
Action
Unknown. May prevent reuptake of norepinephrine, serotonin, or both at presynaptic neurons, increasing levels of these neurotransmitters in CNS. Exact mechanism in pruritus also unknown, but drug is a potent histamine1- and histamine2-blocker.
Availability
Capsules: 10 mg, 25 mg, 50 mg, 75 mg, 100 mg, 150 mg
Cream (topical): 5% in 30-g tube
Oral concentrate: 10 mg/ml
⊘Indications and dosages
➣ Endogenous depression; anxiety
Adults: Initially, 25 mg P.O. t.i.d., increased as needed up to 150 mg daily in outpatients and 300 mg daily in hospitalized patients.
Elderly adults: Initially, 25 to 50 mg P.O. daily; may be increased as needed
➣ Short-term relief of histamine-mediated pruritus of moderate severity accompanying such conditions as eczematous dermatitis
Adults: Apply a thin film of cream to skin q.i.d., with 3 to 4 hours between applications, for a maximum of 8 days.
Off-label uses
• Adjunct in peptic ulcer disease
Contraindications
• Hypersensitivity to drug or other dibenzoxepins
• Glaucoma
• Predisposition to urinary retention
• MAO inhibitor use within past 14 days
Precautions
Use cautiously in:
• cardiovascular disease, prostatic enlargement, seizures
• elderly patients
• pregnant or breastfeeding patients.
Administration
• If desired, mix contents of capsule with food.
• Dilute oral concentrate with 120 ml of water, milk, or juice. Be aware that drug is incompatible with carbonated beverages.
• Know that drug may be given at bedtime to prevent daytime sleepiness.
☞ Don't give within 14 days of MAO inhibitor, because drug interaction may cause cardiovascular instability.
☞ Avoid concurrent use of other CNS depressants, because inadvertent overdose may occur.
• With topical cream, don't apply to broken skin or use occlusive dressings, because doing so increases dermal absorption.
• Be aware that drug is usually given in conjunction with psychotherapy when used for depression.
| Route | Onset | Peak | Duration |
| P.O. | Unknown | 2 hr | Unknown |
| Topical | Unknown | Unknown | Unknown |
Adverse reactions
CNS: fatigue, sedation, agitation, confusion, hallucinations, drowsiness, dizziness, extrapyramidal reactions, poor concentration, syncope, seizures, cerebrovascular accident, increased risk of suicide or suicidal ideation (especially in child or adolescent)
CV: hypotension, orthostatic hypotension, hypertension, vasculitis, ECG changes, tachycardia, palpitations, arrhythmias, myocardial infarction, heart block
EENT: blurred vision, increased intraocular pressure, lacrimation, tinnitus, nasal congestion
GI: nausea, constipation, dry mouth, paralytic ileus
GU: urinary retention, delayed voiding, urinary tract dilation, gynecomastia, galactorrhea, menstrual irregularities, testicular swelling, libido changes
Hematologic: purpura, bone marrow depression, eosinophilia, agranulocytosis, thrombocytopenia, leukopenia
Metabolic: hyperglycemia, hypoglycemia
Skin: photosensitivity; rash; urticaria; pruritus; diaphoresis; flushing; petechiae; alopecia; local burning, stinging, tingling, irritation, or rash (with topical use)
Other: increased appetite, weight gain or loss, hyperthermia, chills, edema, drug-induced fever, hypersensitivity reactions
Interactions
Drug-drug. Barbiturates, CNS depressants (including antihistamines, clonidine, opioids, sedative-hypnotics): additive CNS depression
Carbamazepine, class IC antiarrhythmics (flecainide, propafenone), other antidepressants, other CYP450-2D6 inhibitors (amiodarone, cimetidine, quinidine, ritonavir), phenothiazines: increased doxepin blood level and effects
Clonidine: hypertensive crisis
Guanethidine: antagonism of antihypertensive effects
Levodopa: delayed or decreased levodopa absorption, hypertension
MAO inhibitors: tachycardia, seizures, potentially fatal reactions
Rifamycin: decreased doxepin effects
Selective serotonin reuptake inhibitors: increased risk of toxicity
Sparfloxacin: increased risk of adverse cardiovascular effects
Drug-diagnostic tests. Bilirubin, hepatic enzymes: increased levels
Glucose: increased or decreased level
Liver function tests: altered results
Drug-herbs. Angel's trumpet, jimsonweed, scopolia: increased anticholinergic effects
Chamomile, hops, kava, skullcap, valerian: increased CNS depression
Evening primrose oil: additive or synergistic effects
S-adenosylmethionine (SAM-e), St. John's wort, yohimbe: serotonin syndrome
Drug-behaviors. Alcohol use: increased CNS depression
Smoking: increased drug metabolism and altered effects
Sun exposure: increased risk of photosensitivity reactions
Patient monitoring
☞ Record mood changes and watch for suicidal tendencies, especially in child or adolescent.
• Assess bowel elimination pattern. Increase fluids and administer stool softeners as ordered to ease constipation.
• Monitor fluid intake and output. Report changes in voiding pattern.
• Monitor liver function test results, CBC with white cell differential, and glucose level.
Patient teaching
• Advise patient on long-term therapy not to stop taking drug abruptly because this may lead to nausea, headache, and malaise.
☞ Instruct patient and significant other, as appropriate, to monitor mental status carefully and to immediately report increased depression or suicidal thoughts or behavior (especially when used in child or adolescent).
☞ Tell patient to promptly report easy bruising or bleeding.
• Caution patient to avoid driving and other hazardous activities until he knows how drug affects concentration and alertness.
• Instruct patient to move slowly when sitting up or standing, to avoid dizziness or light-headedness from sudden blood pressure decrease.
• Explain that drowsiness and dizziness usually subside after several weeks.
• Tell patient that using topical cream on more than 10% of body surface area may cause drowsiness.
• Caution patient using topical cream not to apply it to broken skin and not to use occlusive dressings. Also tell him to avoid contact with eyes and to rinse eyes thoroughly with warm water if contact occurs.
• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs, tests, herbs, and behaviors mentioned above.
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