Peringatan Keamanan

The oral LD50 of nortriptyline in the rat is 405 mg/kg.L11920Symptoms of overdose with nortriptyline include cardiac arrhythmias, severe hypotension, shock, congestive heart failure, pulmonary edema, convulsions, coma, and CNS depression.L11878,L11899 Changes in the electrocardiogram, particularly in QRS segment, may be indicative of tricyclic antidepressant toxicity.A191170

Nortriptyline

DB00540

small molecule approved

Deskripsi

Nortriptyline hydrochloride, the active metabolite of amitriptyline, is a tricyclic antidepressant (TCA).L11878 It is used in the treatment of major depression and is also used off-label for chronic pain and other conditions.L11881

Struktur Molekul 2D

Berat 263.3767
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) The average plasma half-life of nortriptyline in healthy volunteers is about 26 hours, but is said to range from 16 to 38 hours.[A191098,L11878,L11911] One study mentions a mean half-life of about 39 hours.[A191101]
Volume Distribusi The apparent volume of distribution (Vd)?, estimated after intravenous administration is 1633 ± 268 L within the range of 1460 to 2030 (21 ± 4 L/kg).[L11911] Nortriptyline crosses the placenta and is found in the breast milk. It distributes to the heart, lungs, brain, and the liver.[L11899]
Klirens (Clearance) The average plasma clearance of nortriptyline in a study of healthy volunteers was 54 L/h.[A191098] The average systemic clearance of nortriptyline is 30.6 ± 6.9 L / h, within the range of 18.6 to 39.6 L/hour.[L11911]

Absorpsi

Nortriptyline is readily absorbed in the gastrointestinal tract with extensive variation in plasma levels, depending on the patient. This drug undergoes first-pass metabolism and its plasma concentrations are attained within 7 to 8.5 hours after oral administration.L11899 The bioavailability of nortriptyline varies considerably and ranges from 45 to 85%.A191167,L11911

Metabolisme

Nortriptyline is metabolized via demethylation and hydroxylation in the liver followed by glucuronic acid conjugation. CYP2D6 plays a large role in nortriptyline metabolism, with contributions from CYP1A2, CYP2C19 and CYP3A4.A15182,L11878,A14832 The main active metabolite is 10-hydroxynortriptyline exists in both cis and a trans form, with the trans form is higher in potency. 10-hydroxynortriptyline is the most frequently found in the plasma. Most of the other metabolites are conjugated, and are less potent.L11911

Rute Eliminasi

Nortriptyline and its metabolites are mainly excreted in the urine, where only small amounts (2%) of the total drug is recovered as unchanged parent compound.L11911 Approximately one-third of a single orally administered dose is excreted in urine within 24 hours.L11899 Small amounts are excreted in feces via biliary elimination.L11911

Farmakogenomik

7 Varian
CYP2D6 (rs3892097)

Patients with this genotype have reduced metabolism of nortriptyline.

CYP2D6 (rs35742686)

The presence of this polymorphism in CYP2D6 is associated with reduced or poor metabolism of nortriptyline.

CYP2D6 (rs3892097)

The presence of this polymorphism in CYP2D6 is associated with reduced or poor metabolism of nortriptyline.

CYP2D6 (None)

The presence of this polymorphism in CYP2D6 is associated with reduced or poor metabolism of nortriptyline.

CYP2D6 (rs5030655)

The presence of this polymorphism in CYP2D6 is associated with reduced or poor metabolism of nortriptyline.

CYP2D6 (rs1135824)

The presence of this polymorphism in CYP2D6 is associated with reduced or poor metabolism of nortriptyline.

CYP2D6 (rs28371733)

The presence of this polymorphism in CYP2D6 is associated with reduced or poor metabolism of nortriptyline.

Interaksi Makanan

2 Data
  • 1. Avoid alcohol.
  • 2. Take with or without food. Food decreases gastrointestinal irritation.

Interaksi Obat

2099 Data
Modafinil The metabolism of Nortriptyline can be increased when combined with Modafinil.
Armodafinil The metabolism of Nortriptyline can be increased when combined with Armodafinil.
Valsartan Nortriptyline may decrease the antihypertensive activities of Valsartan.
Remikiren Nortriptyline may decrease the antihypertensive activities of Remikiren.
Torasemide Nortriptyline may decrease the antihypertensive activities of Torasemide.
Guanadrel Nortriptyline may decrease the antihypertensive activities of Guanadrel.
Olmesartan Nortriptyline may decrease the antihypertensive activities of Olmesartan.
Nitroprusside Nortriptyline may decrease the antihypertensive activities of Nitroprusside.
Minoxidil Nortriptyline may decrease the antihypertensive activities of Minoxidil.
Fosinopril Nortriptyline may decrease the antihypertensive activities of Fosinopril.
Trandolapril Nortriptyline may decrease the antihypertensive activities of Trandolapril.
Benazepril Nortriptyline may decrease the antihypertensive activities of Benazepril.
Cyclothiazide Nortriptyline may decrease the antihypertensive activities of Cyclothiazide.
Candoxatril Nortriptyline may decrease the antihypertensive activities of Candoxatril.
Lisinopril Nortriptyline may decrease the antihypertensive activities of Lisinopril.
Nitroglycerin Nortriptyline may decrease the antihypertensive activities of Nitroglycerin.
Cryptenamine Nortriptyline may decrease the antihypertensive activities of Cryptenamine.
Candesartan cilexetil Nortriptyline may decrease the antihypertensive activities of Candesartan cilexetil.
Fenoldopam Nortriptyline may decrease the antihypertensive activities of Fenoldopam.
Eprosartan Nortriptyline may decrease the antihypertensive activities of Eprosartan.
Quinapril Nortriptyline may decrease the antihypertensive activities of Quinapril.
Telmisartan Nortriptyline may decrease the antihypertensive activities of Telmisartan.
Deserpidine Nortriptyline may decrease the antihypertensive activities of Deserpidine.
Diazoxide Nortriptyline may decrease the antihypertensive activities of Diazoxide.
Epoprostenol Nortriptyline may decrease the antihypertensive activities of Epoprostenol.
Cilazapril Nortriptyline may decrease the antihypertensive activities of Cilazapril.
Saprisartan Nortriptyline may decrease the antihypertensive activities of Saprisartan.
Spirapril Nortriptyline may decrease the antihypertensive activities of Spirapril.
Tienilic acid Nortriptyline may decrease the antihypertensive activities of Tienilic acid.
Diethylnorspermine Nortriptyline may decrease the antihypertensive activities of Diethylnorspermine.
Temocapril Nortriptyline may decrease the antihypertensive activities of Temocapril.
Rauwolfia serpentina root Nortriptyline may decrease the antihypertensive activities of Rauwolfia serpentina root.
Enalaprilat Nortriptyline may decrease the antihypertensive activities of Enalaprilat.
Angiotensin 1-7 Nortriptyline may decrease the antihypertensive activities of Angiotensin 1-7.
Imidapril Nortriptyline may decrease the antihypertensive activities of Imidapril.
BQ-123 Nortriptyline may decrease the antihypertensive activities of BQ-123.
Zofenopril Nortriptyline may decrease the antihypertensive activities of Zofenopril.
Guanoxan Nortriptyline may decrease the antihypertensive activities of Guanoxan.
Delapril Nortriptyline may decrease the antihypertensive activities of Delapril.
Vincamine Nortriptyline may decrease the antihypertensive activities of Vincamine.
Linsidomine Nortriptyline may decrease the antihypertensive activities of Linsidomine.
Guanoxabenz Nortriptyline may decrease the antihypertensive activities of Guanoxabenz.
Tolonidine Nortriptyline may decrease the antihypertensive activities of Tolonidine.
Endralazine Nortriptyline may decrease the antihypertensive activities of Endralazine.
Cadralazine Nortriptyline may decrease the antihypertensive activities of Cadralazine.
Bietaserpine Nortriptyline may decrease the antihypertensive activities of Bietaserpine.
Guanazodine Nortriptyline may decrease the antihypertensive activities of Guanazodine.
Methoserpidine Nortriptyline may decrease the antihypertensive activities of Methoserpidine.
Guanoclor Nortriptyline may decrease the antihypertensive activities of Guanoclor.
Muzolimine Nortriptyline may decrease the antihypertensive activities of Muzolimine.
Xipamide Nortriptyline may decrease the antihypertensive activities of Xipamide.
Candesartan Nortriptyline may decrease the antihypertensive activities of Candesartan.
Tocopherylquinone Nortriptyline may decrease the antihypertensive activities of Tocopherylquinone.
Benazeprilat Nortriptyline may decrease the antihypertensive activities of Benazeprilat.
Fosinoprilat Nortriptyline may decrease the antihypertensive activities of Fosinoprilat.
Ramiprilat Nortriptyline may decrease the antihypertensive activities of Ramiprilat.
Perindoprilat Nortriptyline may decrease the antihypertensive activities of Perindoprilat.
Quinaprilat Nortriptyline may decrease the antihypertensive activities of Quinaprilat.
Furosemide Nortriptyline may decrease the antihypertensive activities of Furosemide.
Enalapril Nortriptyline may decrease the antihypertensive activities of Enalapril.
Captopril Nortriptyline may decrease the antihypertensive activities of Captopril.
Guanethidine Nortriptyline may decrease the antihypertensive activities of Guanethidine.
Pinacidil Nortriptyline may decrease the antihypertensive activities of Pinacidil.
Riociguat The serum concentration of Nortriptyline can be increased when it is combined with Riociguat.
Macitentan Nortriptyline may decrease the antihypertensive activities of Macitentan.
Aliskiren Nortriptyline may decrease the antihypertensive activities of Aliskiren.
Eplerenone Nortriptyline may decrease the antihypertensive activities of Eplerenone.
Ramipril Nortriptyline may decrease the antihypertensive activities of Ramipril.
Perindopril Nortriptyline may decrease the antihypertensive activities of Perindopril.
Dihydralazine Nortriptyline may decrease the antihypertensive activities of Dihydralazine.
Levamlodipine Nortriptyline may decrease the antihypertensive activities of Levamlodipine.
Buthiazide Nortriptyline may decrease the antihypertensive activities of Buthiazide.
Azilsartan medoxomil Nortriptyline may decrease the antihypertensive activities of Azilsartan medoxomil.
Buprenorphine Nortriptyline may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
Doxylamine Doxylamine may increase the central nervous system depressant (CNS depressant) activities of Nortriptyline.
Dronabinol Dronabinol may increase the central nervous system depressant (CNS depressant) activities of Nortriptyline.
Droperidol Droperidol may increase the central nervous system depressant (CNS depressant) activities of Nortriptyline.
Hydrocodone Nortriptyline may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Magnesium sulfate The therapeutic efficacy of Nortriptyline can be increased when used in combination with Magnesium sulfate.
Methotrimeprazine Nortriptyline may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
Metyrosine Nortriptyline may increase the sedative activities of Metyrosine.
Minocycline Minocycline may increase the central nervous system depressant (CNS depressant) activities of Nortriptyline.
Nabilone Nabilone may increase the central nervous system depressant (CNS depressant) activities of Nortriptyline.
Orphenadrine Nortriptyline may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
Paraldehyde Nortriptyline may increase the central nervous system depressant (CNS depressant) activities of Paraldehyde.
Perampanel Perampanel may increase the central nervous system depressant (CNS depressant) activities of Nortriptyline.
Pramipexole Nortriptyline may increase the sedative activities of Pramipexole.
Ropinirole Nortriptyline may increase the sedative activities of Ropinirole.
Rotigotine Nortriptyline may increase the sedative activities of Rotigotine.
Rufinamide The risk or severity of adverse effects can be increased when Rufinamide is combined with Nortriptyline.
Sodium oxybate Nortriptyline may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Suvorexant Nortriptyline may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
Tapentadol Tapentadol may increase the central nervous system depressant (CNS depressant) activities of Nortriptyline.
Thalidomide Nortriptyline may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
Zolpidem Nortriptyline may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
Aclidinium The risk or severity of adverse effects can be increased when Nortriptyline is combined with Aclidinium.
Mianserin Mianserin may increase the anticholinergic activities of Nortriptyline.
Mirabegron The risk or severity of urinary retention can be increased when Nortriptyline is combined with Mirabegron.
Potassium chloride The risk or severity of gastrointestinal ulceration can be increased when Nortriptyline is combined with Potassium chloride.
Pramlintide The risk or severity of reduced gastrointestinal motility can be increased when Pramlintide is combined with Nortriptyline.

Target Protein

Sodium-dependent noradrenaline transporter SLC6A2
Sodium-dependent serotonin transporter SLC6A4
5-hydroxytryptamine receptor 2A HTR2A
5-hydroxytryptamine receptor 1A HTR1A
Histamine H1 receptor HRH1
Alpha-1A adrenergic receptor ADRA1A
Alpha-1D adrenergic receptor ADRA1D
5-hydroxytryptamine receptor 2C HTR2C
Alpha-1B adrenergic receptor ADRA1B
Alpha-2 adrenergic receptors ADRA2A
Beta adrenergic receptor ADRB1
D(2) dopamine receptor DRD2
Sigma receptor PGRMC1
5-hydroxytryptamine receptor 2C Htr2c
Muscarinic acetylcholine receptor CHRM1

Referensi & Sumber

Synthesis reference: Abraham Nudelman, "ACID ADDITION SALT OF A NORTRIPTYLINE-GABA CONJUGATE AND A PROCESS OF PREPARING SAME." U.S. Patent US20130184347, issued July 18, 2013.
Artikel (PubMed)
  • PMID: 9778204
    Prochazka AV, Weaver MJ, Keller RT, Fryer GE, Licari PA, Lofaso D: A randomized trial of nortriptyline for smoking cessation. Arch Intern Med. 1998 Oct 12;158(18):2035-9.
  • PMID: 10401446
    Nelson JC, Kennedy JS, Pollock BG, Laghrissi-Thode F, Narayan M, Nobler MS, Robin DW, Gergel I, McCafferty J, Roose S: Treatment of major depression with nortriptyline and paroxetine in patients with ischemic heart disease. Am J Psychiatry. 1999 Jul;156(7):1024-8. doi: 10.1176/ajp.156.7.1024.
  • PMID: 2050651
    Fabre LF, Scharf MB, Itil TM: Comparative efficacy and safety of nortriptyline and fluoxetine in the treatment of major depression: a clinical study. J Clin Psychiatry. 1991 Jun;52 Suppl:62-7.
  • PMID: 11791642
    Heymann RE, Helfenstein M, Feldman D: A double-blind, randomized, controlled study of amitriptyline, nortriptyline and placebo in patients with fibromyalgia. An analysis of outcome measures. Clin Exp Rheumatol. 2001 Nov-Dec;19(6):697-702.
  • PMID: 9178335
    Lustman PJ, Griffith LS, Clouse RE, Freedland KE, Eisen SA, Rubin EH, Carney RM, McGill JB: Effects of nortriptyline on depression and glycemic control in diabetes: results of a double-blind, placebo-controlled trial. Psychosom Med. 1997 May-Jun;59(3):241-50.
  • PMID: 17471183
    Gillman PK: Tricyclic antidepressant pharmacology and therapeutic drug interactions updated. Br J Pharmacol. 2007 Jul;151(6):737-48. Epub 2007 Apr 30.
  • PMID: 12631677
    Clouse RE: Antidepressants for irritable bowel syndrome. Gut. 2003 Apr;52(4):598-9. doi: 10.1136/gut.52.4.598.
  • PMID: 6994983
    Dawling S, Crome P, Braithwaite R: Pharmacokinetics of single oral doses of nortriptyline in depressed elderly hospital patients and young healthy volunteers. Clin Pharmacokinet. 1980 Jul-Aug;5(4):394-401. doi: 10.2165/00003088-198005040-00007.
Menampilkan 8 dari 15 artikel.
Textbook
  • ISBN: 978-0-7020-3471-8
    46. (2012). In Rang and Dale's Pharmacology (7th ed., pp. 574-575). Edinburgh: Elsevier/Churchill Livingstone.

Contoh Produk & Brand

Produk: 243 • International brands: 9
Produk
  • Apo-nortriptyline
    Capsule • 10 mg • Oral • Canada • Generic • Approved
  • Apo-nortriptyline
    Capsule • 25 mg • Oral • Canada • Generic • Approved
  • Ava-nortriptyline
    Capsule • 10 mg • Oral • Canada • Generic • Approved
  • Ava-nortriptyline
    Capsule • 25 mg • Oral • Canada • Generic • Approved
  • Aventyl
    Capsule • 10 mg • Oral • Canada • Approved
  • Aventyl
    Capsule • 25 mg • Oral • Canada • Approved
  • Dom-nortriptyline 10mg Capsules
    Capsule • 10 mg • Oral • Canada • Generic • Approved
  • Dom-nortriptyline 25mg Capsules
    Capsule • 25 mg • Oral • Canada • Generic • Approved
Menampilkan 8 dari 243 produk.
International Brands
  • Allegron
  • Ateben
  • Avantyl
  • Noritren
  • Norpress
  • Nortrilen
  • Psychostyl
  • Sensaval
  • Sensoval

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