Lofepramine

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IUPAC_name = N-methyl-N- [4-Chlorobenzoyl-methyl-3-(10.11-dihydro-5H-dibenz (b, t) azepin-5-yl] -propylamine

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width = 140
CAS_number = 23047-25-8
ATC_prefix = N06
ATC_suffix = AA07
PubChem = 3947
DrugBank =
C=26 | H=27 | Cl=1 | N=2 | O=1
molecular_weight = 418.958 g/mol
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routes_of_administration = Oral

Lofepramine (trademarked Gamanil, Tymelyt, generic Lomont) is a third generation tricyclic antidepressant used in the treatment of depressive disorders. It has both antidepressant and anxiolytic properties. Lofepramine is metabolized "in vivo" into desipramine; hence its pharmacological profile is extremely similar.

Indications

In the United Kingdom, lofepramine is licensed for the treatment of depression.Description: An antidepressant administered orally (as tablets). It has fewer sedative properties than many of the products used to treat depressive illnesses and is suited to patients whose symptoms tend towards withdrawal and apathy, rather than restlessness and agitation.

It is commonly prescribed for major depressive disorder, anxiety, insomnia, neuropathic/chronic pain, and treatment resistant depression. [Essential Psychopharmacology: The Prescriber's Guide, ISBN 0521683505, http://books.google.com/books?id=-ppHkXw5zwMC, p.263]

ide effects

Drowsiness, dry mouth, heartbeat irregularities, sweating, low blood pressure, constipation, blurred vision palpatations, dizziness and urinary retention. Can cause confusion in elderly patients or behavioural disturbance in the young. May produce weight gain or cause changes in the levels of blood sugar. Some patients report muscular discomfort, particularly in the shoulders. However, lofepramine is less sedating than, for instance, amitriptyline, and is safer in overdose than older tricyclics.

Warnings

To be used with caution for epileptic patients or those with glaucoma or psychosis. Lofepramine should not be given to people who have suffered liver failure or heart disease. Not advisable for use in pregnant women.

Availability

In the United Kingdom, lofepramine is marketed (as the hydrochloride salt) in the form of 70mg tablets and 5ml oral suspension as the generic Lomont. [ [http://emc.medicines.org.uk/emc/assets/c/html/DisplayDoc.asp?DocumentID=10656 Lomont , SPC from the eMC ] ]

Dosage

140-210mg daily in divided doses.

Before dispensing medication on a set course, the first prescribed dosage to a patient must be 70mg (one tablet) to be taken at NIGHT only. If no adverse side effects have been reported then the next course would be 140mg (2 tablets to be taken at NIGHT) for a period of 2-3 weeks.

Then again, if no adverse side effects have been reported, the patient must undergo the full dosage of 210mg per DAY for a period of 3 WEEKS.

If the patient is using the maximum daily dosage of 210mg, then the dosage must be divided into THREE SEPARATE time slots, preferably one in the morning, one in the afternoon and one at night; or alternatively one in the morning and two at night (it is safe to take two 70mg tablets at the same time).

Development history

G.B. patent 1,177,525 filed on 1967-04-13 by the Swedish Leo corporation (Leo Aktiebolaget) covers Lofepramine as a member of a family of heterocyclic aminoketones, touting as a primary object low toxicity of oral dosage in mice relative to imipramine, amitriptyline, and desipramine for comparable effectiveness. [ [http://v3.espacenet.com/textdoc?DB=EPODOC&IDX=GB1177525&F=1&QPN=GB1177525 esp@cenet document view ] ]

U.S. patent 3,637,660 granted on 1972-01-25 covers Lofepramine as a member of a family of dibenzazepine derivatives, with similar description and claims. [ [http://www.freepatentsonline.com/result.html?query_txt=PN/3637660 Patents: PN/3637660 ] ]

References