Lofepramine is a third Generation tricyclic antidepressant

Tricyclic antidepressant

Tricyclic antidepressants are heterocyclic chemical compounds used primarily as antidepressants. The TCAs were first discovered in the early 1950s and were subsequently introduced later in the decade; they are named after their chemical structure, which contains three rings of atoms...

 which was introduced in 1983 for the treatment of depressive disorders. It is partially converted to its active metabolite

Metabolite

Metabolites are the intermediates and products of metabolism. The term metabolite is usually restricted to small molecules. A primary metabolite is directly involved in normal growth, development, and reproduction. Alcohol is an example of a primary metabolite produced in large-scale by industrial...

 desipramine

Desipramine

Desipramine is a tricyclic antidepressant . It inhibits the reuptake of norepinephrine and to a lesser extent serotonin. It is used to treat depression, but not considered a first line treatment since the introduction of SSRI antidepressants...

 in vivo

In vivo

In vivo is experimentation using a whole, living organism as opposed to a partial or dead organism, or an in vitro controlled environment. Animal testing and clinical trials are two forms of in vivo research...

. However, it is unlikely this property plays a substantial role in its overall effects as lofepramine exhibits lower toxicity

Toxicity

Toxicity is the degree to which a substance can damage a living or non-living organisms. Toxicity can refer to the effect on a whole organism, such as an animal, bacterium, or plant, as well as the effect on a substructure of the organism, such as a cell or an organ , such as the liver...

 and anticholinergic

Anticholinergic

An anticholinergic agent is a substance that blocks the neurotransmitter acetylcholine in the central and the peripheral nervous system. An example of an anticholinergic is dicycloverine, and the classic example is atropine....

 side effect

Side effect

In medicine, a side effect is an effect, whether therapeutic or adverse, that is secondary to the one intended; although the term is predominantly employed to describe adverse effects, it can also apply to beneficial, but unintended, consequences of the use of a drug.Occasionally, drugs are...

s relative to desipramine while retaining equivalent antidepressant efficacy.

Indications

In the United Kingdom

United Kingdom

The United Kingdom of Great Britain and Northern IrelandIn the United Kingdom and Dependencies, other languages have been officially recognised as legitimate autochthonous languages under the European Charter for Regional or Minority Languages...

, 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.

Side effects

Delusions, headache, nightmares, facial oedema, general feeling of being unwell, bleeding from skin, excitement/anxiety, nausea, inflammation 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

Hydrochloride

In chemistry, hydrochlorides are salts resulting, or regarded as resulting, from the reaction of hydrochloric acid with an organic base . This is also known as muriate, derived from hydrochloric acid's other name: muriatic acid....

salt) in the form of 70 mg tablets and 5ml oral suspension as the generic Lomont.