Lofepramine
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| Trade names | Lomont, Emdalen, Gamanil |
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Oral |
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| Pharmacokinetic data | |
| Bioavailability | 7% |
| Protein binding | 99% |
| Metabolism | Hepatic (via P450 cytochromes) |
| Biological half-life | 1.7-2.5 hours (dose-dependent; parent drug); 12-24 hours (active metabolites) |
| Excretion | Urine (mostly as metabolites) |
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| ECHA InfoCard | 100.041.254 |
| Chemical and physical data | |
| Formula | C26H27ClN2O |
| Molar mass | 418.958 g/mol |
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Lofepramine (brand name: Lomont (UK) Emdalen (ZA), Gamanil (IE, UK (discontinued)) & Tymelyt (discontinued)) is a third generationtricyclic antidepressant which was introduced in 1983 for the treatment of depressive disorders. Lofepramine is less sedating than, for instance, amitriptyline, and is safer in overdose than older tricyclics.
In the United Kingdom, Lofepramine is licensed for the treatment of depression which is its primary use in medicine.
Delusions, nightmares, facial oedema, general feeling of being unwell, bleeding from skin, inflammation of mucous membranes, loss of taste, psychiatric problems such as self-harm, pins and needles, sweating, dizziness. Can cause 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.
Lofepramine is known to interact with
Lofepramine is a strong inhibitor of norepinephrine reuptake (Ki=5.4 nM) and a moderate inhibitor of serotonin reuptake (Ki=70 nM). It is a weak-intermediate level antagonist of the muscarinic acetylcholine receptors (Ki values of 67 nM, 330 nM, 130 nM, 340 nM, 460 nM for M1, M2, M3, M4 & M5 respectively).
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