nortriptyline (Aventyl, Pamelor)
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Introduction
Tradenames: Aventyl, Pamelor.
Indications
- treatment of depression
- enuresis in children
- analgesic for chronic pain
- management of anxiety/panic attacks
- smoking cessation[7]
- attention-deficit hyperactivity disorder[7]
Contraindications
- patients with narrow-angle glaucoma
- concurrent administration of MAO inhibitor
Dosage
Tabs: 10, 25, 50, 75 mg.
Solution: 10 mg/5 mL.
Pharmacokinetics
- peak effect may take more than 2 weeks
- metabolized in liver by cyt P450 2D6 to active metabolite 10-OH-nortriptyline
- metabolites are eliminated in the urine
- 1/2life of 28-31 hours
- nortriptyline is the active metabolite of amitriptyline
- therapeutic range: 50-175 ng/mL.
elimination via liver
1/2life = 18-90 hours
protein binding = 93-95 %
elimination by hemodialysis = -
elimination by hemodialysis = -
Adverse effects
- common (> 10%)
- dizziness, drowsiness, dry mouth, constipation, headache, increased appetite, nausea, weakness, unpleasant taste, weight gain
- less common (1-10%)
- blurred vision, confusion, delirium, hallucinations, difficult urination, eye pain, arrhythmias, fine muscle tremors, hypotension, nervousness, restlessness, parkinsonism, sexual dysfunction, diarrhea, excessive sweating, heartburn, insomnia
- uncommon (< 1%)
- agranulocytosis, alopecia, anxiety, breast enlargement, galactorrhea, cholestatic jaundice, seizures, SIADH, tinnitus, testicular swelling, gum disorder, decreased lower esophageal sphincter tone, GERD, leukopenia, eosinophilia, abnormal liver function tests, increased intraocular pressure, allergic reactions, photosensitivity
- cardiovascular: hypotension, hypertension, tachycardia, arrhythmias, heart block, myocardial infarction, stroke
- psychiatric: confusional states especially in the elderly, hallucinations, disorientation, delusion, anxiety, restlessness, agitation, insomnia, panic, nightmares, hypomania, exacerbation of psychosis
- neurologic: paresthesias, numbness, ataxia, peripheral neuropathy, extrapyramidal symptoms, seizures, tinnitus
- allergic: skin rash, petechiae, urticaria, photosensitivity, edema, drug fever
- hematologic: bone marrow depression
- gastrointestinal: nausea/vomiting, diarrhea, stomatitis
- endocrine: gynecomastia, impotence, testicular swelling, SIADH
- moderate anticholinergic effects
- other: jaundice, alopecia, urinary frequency
- low sedation
- low incidence of orthostatic hypotension compared with amitriptyline
- drug adverse effects of tricyclic antidepressants
- drug adverse effects of antidepressants
- drug adverse effects of psychotropic agents
Drug interactions
- coadministration enhances metabolism of nortriptyline
- coadministration decreases protein binding of nortriptyline
- coadministration inhibits metabolism of nortriptyline
- monoamine oxidase (MAO) inhibitors: hyperpyrexia, seizures
- alcohol may potentiate effects
- nortriptyline may reduce hypotensive effects of clonidine & guanethidine
- nortriptyline may potentiate CNS effects of CNS depressants & sympathomimetics
- additive side effects in combination with anti-cholinergic agents
- nortriptyline may enhance anticoagulant effects of warfarin
- astemizole & terfenadine should be avoided
- any pharmaceutical agent that inhibits cyt P450 2D6 may increase levels of nortriptyline
- drug interaction(s) of tricyclic antidepressants with physostigmine
- drug interaction(s) of antidepressant in combination with GLP1-agonist
- drug interaction(s) of benzodiazepines with antidepressants
- drug interaction(s) of antidepressants with benzodiazepines
- drug interaction(s) of NSAIDs with antidepressants
- drug interaction(s) of antidepressant with opiates
Laboratory
- nortriptyline in serum
- serum, plasma (EDTA)
- collect at steady state trough; > 12 hours after dose
- methods: HPLC, GLC, GC-MS, RIA
- interferences:
- nortriptyline may be displaced from protein-binding sites by plasticizers in collecting devices
- other laboratory measurements with Loincs
Mechanism of action
- increases serotonin & norepinephrine in at synapses by inhibiting re-uptake
- tricyclic antidepressant activity
More general terms
Additional terms
- amitriptyline (Elavil, Endep)
- cytochrome P450 2D6 (cytochrome P450 2D, cytochrome P450 DB1, debrisoquine-4-hydroxylase, CYP2D6)
- depression
- enuresis
References
- ↑ The Pharmacological Basis of Therapeutics, 9th ed. Gilman et al, eds. Permagon Press/McGraw Hill, 1996
- ↑ 1997 PDR
- ↑ Drug Information & Medication Formulary, Veterans Affairs, Central California Health Care System, 1st ed., Ravnan et al eds, 1998
- ↑ Kaiser Permanente Northern California Regional Drug Formulary, 1998
- ↑ Clinical Guide to Laboratory Tests, 3rd ed. Teitz ed., W.B. Saunders, 1995
- ↑ Harrison's Principles of Internal Medicine, 14th ed. Fauci et al (eds), McGraw-Hill Inc. NY, 1998, pg 56
- ↑ 7.0 7.1 7.2 Deprecated Reference