Lofepramine is a tricyclic antidepressant (TCA) used primarily in the treatment of depressive disorders. It is a tertiary-amine tricyclic compound and is structurally related to imipramine. Lofepramine is converted in the body to active metabolites, including desipramine, which contributes significantly to its antidepressant activity.
Lofepramine primarily enhances noradrenergic and serotonergic neurotransmission by inhibiting the reuptake of norepinephrine and serotonin at presynaptic nerve terminals. This increases the availability of these neurotransmitters in the synaptic cleft.
Lofepramine is a synthetic small-molecule pharmaceutical compound with the molecular formula C26H29ClN2O and a molecular weight of approximately 404.98 g/mol. Its CAS Number is 23047-25-8.
Lofepramine is commonly encountered as lofepramine hydrochloride, the pharmaceutical salt form used in medicinal products. The free-base compound is lipophilic and the hydrochloride salt provides improved pharmaceutical handling characteristics.
Lofepramine inhibits the reuptake of norepinephrine (noradrenaline) and, to a lesser extent, serotonin in the central nervous system.
By reducing neurotransmitter reuptake, it increases the concentration of these monoamines within the synaptic cleft and enhances neurotransmission. Its active metabolite, desipramine, has a predominantly noradrenergic mechanism and contributes to the overall antidepressant effect.
Lofepramine is used as an antidepressant for the treatment of depressive illness. It belongs to the tricyclic antidepressant class and has historically been used for depressive disorders, including depression associated with anxiety symptoms.
Its use and availability vary between countries and according to local regulatory approvals.
Lofepramine API can be evaluated using validated analytical procedures for identification, assay, related substances, water content, residual solvents, elemental impurities and other applicable quality attributes.
Chromatographic and spectroscopic techniques may be used for identity, assay and purity determination. Where the hydrochloride salt is manufactured, appropriate control of salt formation and related physicochemical characteristics should be included in the applicable specification.
Acceptance criteria should be based on the applicable manufacturer's drug-substance specification, Certificate of Analysis and relevant pharmacopoeial and regulatory requirements.
Lofepramine should be stored in a tightly closed pharmaceutical-grade container under controlled conditions. It should be protected from excessive heat, moisture and direct light.
Specific storage and transportation conditions should follow the applicable manufacturer's approved specification.
Lofepramine API may be supplied for qualified pharmaceutical manufacturing, formulation development, analytical and research applications, subject to applicable quality and regulatory requirements.
Lofepramine API is available for qualified pharmaceutical development and manufacturing requirements subject to applicable quality and regulatory standards. Customers can request product specifications, Certificate of Analysis, analytical documentation, packaging information and commercial details according to their requirements.
| Parameter | Specification |
|---|---|
| Appearance | White to off-white crystalline powder |
| Identification | IR & HPLC compliant |
| Assay (HPLC) | 98.0% – 102.0% |
| Loss on Drying | NMT 2.0% |
| Residue on Ignition | NMT 0.5% |
| Individual Impurity | NMT 0.5% |
| Total Impurities | ≤ 1.5% |
| Water Content | NMT 1.0% |