Lofepramine
Chemical compound / From Wikipedia, the free encyclopedia
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Lofepramine, sold under the brand names Gamanil, Lomont, and Tymelyt among others, is a tricyclic antidepressant (TCA) which is used to treat depression.[7][3][8] The TCAs are so named as they share the common property of having three rings in their chemical structure. Like most TCAs lofepramine is believed to work in relieving depression by increasing concentrations of the neurotransmitters norepinephrine and serotonin in the synapse, by inhibiting their reuptake.[7] It is usually considered a third-generation TCA, as unlike the first- and second-generation TCAs it is relatively safe in overdose and has milder and less frequent side effects.[9]
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Trade names | Gamanil, Lomont, Tymelyt, others |
Other names | Lopramine; DB-2182; Leo-460; WHR-2908A[1][2][3][4] |
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Routes of administration | Oral |
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Bioavailability | 7%[5] |
Protein binding | 99%[6] |
Metabolism | Hepatic (via cytochrome P450, including CYP2D6)[7] |
Metabolites | Desipramine (major) |
Elimination half-life | Up to 5 hours;[1] 12–24 hours (active metabolites) |
Excretion | Urine, feces (mostly as metabolites) |
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ECHA InfoCard | 100.041.254 |
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Formula | C26H27ClN2O |
Molar mass | 418.97 g·mol−1 |
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Lofepramine is not available in the United States, Canada, Australia or New Zealand, although it is available in Ireland, Japan, South Africa and the United Kingdom, among other countries.[1]