Amitriptyline

Table of contents

  • Brand Names
  • Drug Combinations
  • 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: Tryptizol; Belgium: Redomex; Bulgaria: Amitriptylin; Cyprus: Amirol, Ormal, Saroten Retard; Czech Republic: Amitriptylin; Denmark: Amitriptylin, Saroten; Estonia: Amitriptylin, Amitriptyline, Saroten; Finland: Triptyl; France: Elavil, Laroxyl; Germany: Amineurin, Amitriptylin, Psypharm, Saroten, Syneudon; Greece: Maxivalet, Saroten, Stelminal, Thymontil; Hungary: Teperin; Ireland: Amitriptyline; Italy: Adepril, Amitr, Laroxyl, Triptizol; Latvia: Amitriptyline, Amitriptylinum, Saroten Retard; Lithuania: Amitriptyline; Luxembourg: Equilibrin; Malta: Amirol, Tryptizol; Netherlands: Amitriptyline, Sarotex, Tryptizol; Poland: Amitriptylinum; Portugal: Adt, Tryptizol; Romania: Amitriptilin, Amitriptilina; Slovakia: Amitriptylin; Slovenia: Amyzol; Spain: Deprelio, Tryptizol; Sweden: Saroten, Tryptizol; UK: Amitriptyline.

North America

Canada: Amitriptyline, Elavil, Levate, Novo-Triptyn; USA: Amitriptyline.

Latin America

Argentina: Amitriptilina, Fiorda, Tryptalgin, Tryptanol, Uxen Retard; Brazil: Amitriptilina, Amytril, Neo Amitriptilin, Neurotrypt, Protanol, Trisomatol, Tryptanol; Mexico: Anapsique, Tryptanol.

Asia

Japan: Amiplin, Normaln, Tryptanol.

Drug combinations

Amitriptyline and Chlordiazepoxide

Amitriptyline and Medazepam

Amitriptyline and Perphenazine

Amitriptyline, Diazepam, and Perphenazine

Chemistry

Amitriptyline Hydrochloride: C~20~H~23~N HCl. Mw: 313.86. (1) 1-Propanamine, 3-(10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5-ylidene)-N,N-dimethyl-, hydrochloride; (2) 10,11-Dihydro-N,N-dimethyl-5H-dibenzo[a,d]cycloheptene-Δ^5^,^γ^-propylamine hydrochloride. CAS-549-18-8; CAS-50-48-6 (amitriptyline).

Pharmacologic Category

Antidepressants; Tricyclics and Other Norepinephrine-reuptake Inhibitors. (ATC-Code: N06AA09).

Mechanism of action

Increases synaptic concentration of serotonin and/or norepinephrine in the central nervous system by inhibiting their reuptake in the presynaptic neuronal membrane.

Therapeutic use

Relief of symptoms of depression.

Pregnancy and lactiation implications

Teratogenic effects have been observed in animal studies. Amitriptyline crosses the human placenta and CNS effects, limb deformities and developmental delay have been noted in case reports. Administration is not recommended during lactation.

Unlabeled use

Analgesic for certain chronic and neuropathic pain. Prophylaxis against migraine headaches. Treatment of depressive disorders in children.

Contraindications

Hypersensitivity to amitriptyline or any component of the formulation (cross-sensitivity with other tricyclics). Use of MAO inhibitors.

Warnings and precautions

Risk of suicidal thinking and behavior. May worsen psychosis or precipitate a shift to mania or hypomania in bipolar disorder. Not for treatment of bipolar depression. Anticholinergic effects (constipation, xerostomia, blurred vision, urinary retention) may occur. Bone marrow suppression (rarely). May cause orthostatic hypotension. Sedation. Caution in cardiovascular disease (previous myocardial infarction, stroke, tachycardia, or conduction abnormalities), diabetes mellitus, hepatic and renal impairment, hyperthyroidism/thyroid supplementation or seizures. Hyperpyrexia (in combination with anticholinergics and/or neuroleptics) has been observed. Effects may be potentiated with other sedative drugs or ethanol. Therapy should not be abruptly discontinued. May increase risks associated with electroconvulsive therapy.

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