Doxepin

Table of contents

  • Brand Names
  • Chemistry
  • Pharmacologic Category
  • Mechanism of Action
  • Therapeutic Use
  • Unlabeled Use
  • Pregnancy and Lactation Implications
  • Contraindications
  • Warnings and Precautions
  • Adverse Reactions
  • Caution and personalized dose adjustment in patients with the following genotypes
  • Other genes that may be involved
  • Substrate of
  • Inhibits
  • Drug Interactions
  • Nutrition/Nutraceutical Interactions
  • Dosage
  • Pharmacokinetics and Pharmacodynamics
  • Special Considerations

Brand Names

Europe

Austria: Sinequan; Belgium: Sinequan; Denmark: Sinquan; Finland: Doxal; France: Quitaxon; Germany: Aponal, Doneurin, Doxe, Doxepia, Doxepin, Espadox, Mareen, Sinquan; Greece: Sinequan; Ireland: Xepin; Lithuania: Doxepin; Netherlands: Sinequan; Poland: Doxepin, Poldoxin, Sinequan; Romania: Doxepin; Slovenia: Sinequan; Spain: Sinequan.

North America

Canada: Doxepin, Doxepine, Sinequan, Zonalon; USA: Doxepin, Silenor, Zonalon.

Latin America

Mexico: Sinequan.

Drug combinations

Chemistry

Doxepin Hydrochloride: C~19~H~21~NO HCl. Mw: 315.84. (1) 1-Propanamine, 3-dibenz[b,e]oxepin-11(6H)ylidene-N,N-dimethyl-, hydrochloride; (2) N,N-Dimethyldibenz[b,e]oxepin-Δ^11(6H)^,γ-propylamine hydrochloride. CAS-1229-29-4; CAS-1668-19-5 (doxepin); CAS-4698-39-9 (E-isomer); CAS-25127-31-5 (Z-isomer)(1964).

Pharmacologic Category

Antidepressants; Tricyclics and Other Norepinephrine-reuptake Inhibitors, Tertiary Amine. Skin and Mucous Membrane Agents; Antipruritics and Local Anesthetics. (ATC-Code: N06AA12).

Mechanism of action

Doxepin is a dibenzoxepin-derivative tricyclic antidepressant. It increases the synaptic concentration of serotonin and norepinephrine in the CNS by inhibition of their reuptake by the presynaptic neuronal membrane.

Therapeutic use

Used orally for the treatment of depression and/or anxiety in psychoneurotic patients, depression and/or anxiety associated with alcoholism or organic disease, and psychotic depressive disorders with associated anxiety, including involutional depression and manic-depressive disorders. Also used topically as short-term (<8 days) management of moderate pruritus in adults with atopic dermatitis or lichen simplex chronicus.

Pregnancy and lactiation implications

There are no adequate, well-controlled studies in pregnant women. Use during pregnancy only if clearly needed. Generally, it is not recommended to breast-feed if taking antidepressants.

Unlabeled use

Analgesic for certain chronic and neuropathic pain.

Contraindications

Hypersensitivity to doxepin, drugs from a similar chemical class, or any component of the formulation. Narrow-angle glaucoma. Urinary retention. Use of MAO inhibitors within 14 days. Use during acute recovery phase of MI.

Warnings and precautions

Antidepressants increase the risk of suicidal thinking and behavior (suicidality) in children, adolescents, and young adults (18-24 years of age) with major depressive disorder and other psychiatric disorders. Doxepin is approved for treatment of depression in adolescents. May unmask bipolar disorder. Doxepin is not approved for use in treating bipolar depression. Possible activation of mania and hypomania, particularly in bipolar disorder. Possible exacerbation of psychosis in schizophrenia. May cause anticholinergic effects (use with caution in decreased GI motility, paralytic ileus, urinary retention, benign prostatic hyperplasia, xerostomia, or visual problems). May cause orthostatic hypotension (use with caution in patients at risk of this effect or in those who would not tolerate transient hypotensive episodes, e.g. cerebrovascular disease, cardiovascular disease, hypovolemia, or concurrent medication use which may predispose to hypotension/bradycardia). May cause sedation (degree of sedation is very high relative to other antidepressants). Use with caution in history of cardiovascular disease (including previous MI, stroke, tachycardia, or conduction abnormalities). Use with caution in hepatic or renal impairment. Use with caution in patients at risk of seizures, including those with history of seizures, head trauma, brain damage, alcoholism, or concurrent therapy with medications which may lower seizure threshold. Use with caution in patients with hyperthyroidism or those receiving thyroid supplementation. Effects may be potentiated when used with other sedative drugs or ethanol. Use with caution in the elderly. Used topically for >8 days, may increase risk of contact sensitization. Therapy should not be abruptly discontinued in patients receiving high doses for prolonged periods. May increase the risks associated with electroconvulsive therapy.

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