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Lofepramine
Systematic (IUPAC) name
N-(4-chlorophenethyl)-3-(10,11-dihydro-5H-dibenzo[b,f]azepin-5-yl)-N-methylpropan-1-amine
Identifiers
CAS number 23047-25-8
ATC code N06AA07
PubChem 3947
Chemical data
Formula C26H27ClN2O 
Mol. mass 418.958 g/mol
Pharmacokinetic data
Half life 4-6 hours (lofepramine - prodrug); 21-23 hours (desipramine - active metabolite)
Therapeutic considerations
Pregnancy cat.  ?
Legal status Prescription only
Routes Oral

Lofepramine (Gamanil, Tymelyt, Lomont) is a tricyclic antidepressant which was introduced in 1983 for the treatment of depressive disorders.[1] It is partially converted to its active metabolite desipramine in vivo.[1] However, it is unlikely this property plays a substantial role in its overall effects as lofepramine exhibits lower toxicity and anticholinergic side effects relative to desipramine while retaining equivalent antidepressant efficacy.[1]

Contents

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.[2]

Side effects

Delusions, headache, nightmares, facial oedema, general feeling of being unwell, bleeding from skin, excitement/anxiety, nausea, inflamation of mucous membranes, loss of taste, parasthesia, skin rash, psychiatric problems such as self harm, drowsiness, dry mouth, pins and needles, 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 70 mg tablets and 5ml oral suspension as the generic Lomont.[3]

See also

References

  1. ^ a b c Leonard BE (October 1987). "A comparison of the pharmacological properties of the novel tricyclic antidepressant lofepramine with its major metabolite, desipramine: a review". International Clinical Psychopharmacology 2 (4): 281–97. PMID 2891742. 
  2. ^ Essential Psychopharmacology: The Prescriber's Guide, ISBN 0521683505, http://books.google.com/books?id=-ppHkXw5zwMC, p.263
  3. ^ Lomont , SPC from the eMC







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