Venlafaxine HCl

Синонимы: (±)-1-[2-(Dimethylamino)-1-(4-methoxyphenyl)ethyl]cyclohexanol hydrochloride, Wy-45030, Venlafaxine hydrochloride, Effexor, Trevilor, Dobupal

Venlafaxine HCl is the hydrochloride salt of venlafaxine, a bicyclic phenylethylamine derivative that acts as a serotonin-norepinephrine reuptake inhibitor (SNRI). First approved in the 1990s, it has become a mainstay in the treatment of major depressive disorder, generalized anxiety disorder, and panic disorder. Its distinct pharmacological profile—weak dopamine reuptake inhibition at higher doses—sets it apart from selective serotonin reuptake inhibitors (SSRIs).

Chemically, venlafaxine HCl is a racemic mixture of two enantiomers, with the (R)-enantiomer primarily responsible for norepinephrine reuptake inhibition and the (S)-enantiomer for serotonin reuptake inhibition. This dual action contributes to its broad efficacy across mood and anxiety disorders. The hydrochloride salt form offers improved aqueous solubility and stability, making it suitable for a range of immediate-release and extended-release oral dosage forms.

Manufacturers and CDMOs rely on venlafaxine HCl as a key API for generic formulations, particularly extended-release capsules and tablets. The compound is also a frequent subject in bioequivalence studies and analytical method development, given its well-characterized pharmacokinetics and established therapeutic window. Its patent-expired status has made it a high-volume item in the global generic market.

Функция

• Serotonin reuptake inhibition: Blocks serotonin transporter (SERT), increasing synaptic serotonin levels.
• Norepinephrine reuptake inhibition: Inhibits norepinephrine transporter (NET), enhancing noradrenergic neurotransmission.
• Dopamine reuptake inhibition: Mild inhibition at higher doses, contributing to broader mood effects.
• Antidepressant activity: Alleviates symptoms of major depressive disorder.
• Anxiolytic activity: Reduces anxiety in generalized anxiety disorder and panic disorder.

Source & Standardization

• Source: Synthetic chemical process starting from cyclohexanone and 4-methoxyphenylacetic acid derivatives.
• Manufacturing: Multi-step organic synthesis followed by salt formation and recrystallization.
• Standardization: Complying with EP, USP, and IP monographs; typical assay 98.0%–102.0% (HPLC).
• Forms: White to off-white crystalline powder.
• Приложения: Generic antidepressants, extended-release formulations, clinical research.

Технические характеристики

Documentation & Supply

• Monthly capacity: 5 metric tons
• Срок выполнения заказа: 3–5 рабочих дней (товары, имеющиеся в наличии)
• Documentation: COA, MSDS, TDS, DMF available upon request
• Packaging: 25 kg fiber drum with double polyethylene liners, or as per customer requirements

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