|
|
| Line 1: |
Line 1: |
| {{Drugbox|
| |
| | IUPAC_name = 3-(10,11-dihydro-5H-dibenzo[a,d] cyclohepten-5-ylidene)- N-methyl-1-propanamine
| |
| | image=Nortriptyline.png
| |
| | width =120
| |
| | CAS_number = 72-69-5
| |
| | CAS_supplemental = 894-71-3 (hydrochloride)
| |
| | ATC_prefix=N06
| |
| | ATC_suffix=AA10
| |
| | PubChem=4543
| |
| | DrugBank=APRD00602
| |
| | C=19 | H=21 | N=1
| |
| | molecular_weight = 263.377 g/mol
| |
| | bioavailability = well absorbed
| |
| | metabolism = [[Hepatic]]
| |
| | elimination_half-life = 16 and 90 hours
| |
| | excretion = [[Renal]]
| |
| | pregnancy_AU =
| |
| | pregnancy_US =
| |
| | pregnancy_category = C
| |
| | legal_status = Rx-only
| |
| | routes_of_administration = oral
| |
| }}
| |
| '''Nortriptyline''' is a second generation [[tricyclic antidepressant]] marketed as the [[hydrochloride]] under the trade names '''Aventyl'''®, '''Pamelor'''® and '''Nortrilen'''®. It is used in the treatment of [[clinical depression|depression]] and childhood [[nocturnal enuresis]] (bedwetting). In addition it is sometimes used for [[chronic pain]] modification, [[Migraine]], and [[labile affect]] in some neurological conditions.
| |
|
| |
|
| ==Clinical pharmacology==
| |
| Nortriptyline inhibits the reuptake of [[serotonin]], and, to a lesser extent, [[norepinephrine]] (noradrenalin) (''Basic & Clinical Pharmacology, 10th Edition'', Bertram G. Katzung, MD, PhD). Operant conditioning techniques in rats and pigeons suggest that nortriptyline has a combination of stimulant and depressant properties.
| |
|
| |
| ==Indications==
| |
| FDA-approved for treatment of depressive disorders. In the [[United Kingdom]] also may be used for treating nocturnal enuresis with courses of treatment lasting no more than three months. Also used [[off-label use|off-label]] for the treatment of [[panic disorder]], [[irritable bowel syndrome|irritable bowel disease]], prevention of [[migraine]] headaches and chronic pain or [[neuralgia]] modification (particularly [[Temporomandibular joint disorder]]).<ref name="Martindale2002-Sweetman">{{cite book | editor = Sweetman SC | title =Martindale. The complete drug reference | edition = 33 | year = 2002 | publisher = Pharmaceutical Press | id = ISBN 0-85369-499-0}}</ref> It can also aid in quitting smoking with one study showing a six-month abstinence rate of 14% for subjects receiving nortriptyline compared to 3% for subjects not undergoing pharmacological treatment.<ref name="Arch Intern Med1998-prochazka">{{cite journal | author = Prochazka A, Weaver M, Keller R, Fryer G, Licari P, Lofaso D | title = A randomized trial of nortriptyline for smoking cessation. | journal = Arch Intern Med | volume = 158 | issue = 18 | pages = 2035-9 | year = 1998 | id = PMID 9778204}}</ref>
| |
|
| |
| ==Metabolism==
| |
| Nortriptyline is metabolised in the liver by [[hepatic enzyme]] [[CYP2D6]]. Approximately 7 to 10 percent of [[Caucasian race|Caucasians]] are poor metabolisers and might experience more adverse effects, so a lower dosage is often necessary in these individuals.{{Fact|date=February 2007}} Blood levels of nortriptyline should be obtained during long term treatment to avoid toxicity and optimise response.
| |
|
| |
| ==Dosage==
| |
| For depression: low starting doses are used, increasing as necessary to 75–100mg (0–50mg for adolescents and the elderly). Maximum daily dosage is 150mg.<ref name="BNF">[[British National Formulary]] '''45''' March 2003</ref>
| |
|
| |
| For the management of noctiral enuresis: lower dosages are used with the maximum period of treatment, including gradual withdrawal, being three months and a full examination including [[electrocardiogram]] (ECG or EKG) required before further courses.<ref name="BNF"/>
| |
|
| |
| For its off-label use for migraine and headache prophylaxis and treating chronic pain: treatment is started at very low 10mg once at night to minimise side-effects. The dose is then increased every two weeks if required to a maximum of 150mg.
| |
|
| |
| ==Side effects==
| |
| Dry mouth, drowsiness, [[orthostatic hypotension]], [[urinary retention]], [[constipation]], and rapid or [[irregular heartbeat]]. Some sexual side effects may be a problem as well. Less commonly, [[seizures]] and ECG/EKG changes have been reported, especially in [[overdose]].
| |
|
| |
| Alcohol may exacerbate some of its side effects and should be avoided.
| |
|
| |
| However, the incidence of side effects with nortriptyline is somewhat lower than with the first generation tricyclics (e.g. [[imipramine]] (Tofranil®), [[amitriptyline]] (Elavil®)).
| |
|
| |
| ==Warnings==
| |
| Closer monitoring is required for those with a history of cardiovascular disease, [[stroke]], [[glaucoma]] and/or [[seizures]] as well as those who have [[hyperthyroidism]] or are receiving thyroid medication.
| |
|
| |
| ==Contraindications==
| |
| In the acute recovery phase after [[myocardial infarction]] (e.g. heart attack). As for all tricyclic antidepressants concurrent use, or failure to allow a two week gap, with [[monoamine oxidase inhibitor]]s (MAO inhibitors, e.g. phenelzine, tranylcypromine, etc.) may precipitate [[hyperthermia|hyperpyretic]] crises and/or severe [[convulsions]]; fatalities have occurred.
| |
|
| |
| ==Overdose==
| |
| {{main|Tricyclic antidepressant}}
| |
| The symptoms and the treatment of an overdose are largely the same as for the other tricyclic antidepressants.
| |
|
| |
| ==Footnotes==
| |
| <div class="references-small">
| |
| {{reflist|2}}
| |
| </div>
| |
|
| |
|
| |
| {{Antidepressants}}
| |
|
| |
| [[Category:Tricyclic antidepressants]]
| |
|
| |
| [[nl:Nortriptyline]]
| |