Drotaverin

In the clinical treatment of diseases related to smooth muscle spasm, the selection of antispasmodic drugs directly affects the efficiency of discomfort relief and prognostic experience of patients. Drotaverine is an isoquinoline class of smooth muscle antispasmodic. It specifically inhibits the activity of phosphodiesterase 4 (PDE4) to increase the level of cyclic adenosine monophosphate in smooth muscle cells, and at the same time intervenes in the calcium ion binding process of calmodulin, so as to achieve a direct relaxation effect on the smooth muscles of the gastrointestinal tract, biliary tract, urinary tract and reproductive system without affecting the function of the autonomic nervous system. It is clinically mostly used to relieve gastrointestinal spasm, biliary colic and renal colic, and can also be used for the symptomatic treatment of dysmenorrhea and uterine spasm. Compared with traditional anticholinergic antispasmodics, it has no anticholinergic side effects such as dry mouth and palpitations, and the applicable population covers adults and children over 6 years old, especially suitable for people with contraindications to anticholinergic drugs such as glaucoma and prostatic hyperplasia.

The global drotaverine market size has maintained steady growth in recent years. In 2023, the overall market size was approximately USD 1.28 billion, with a compound annual growth rate maintained at around 4.2%. In terms of the domestic market, with the improvement of the awareness of rational use of antispasmodic drugs in primary medical institutions, the sales of drotaverine at terminals of domestic public medical institutions exceeded RMB 1.8 billion in 2023, among which oral preparations accounted for approximately 62% and injections accounted for 38%. At present, there are more than 20 domestic generic drug manufacturers. After the coverage of centralized procurement, the price of oral preparations has dropped by 59%, and the accessibility for patients has been significantly improved. The supply of upstream APIs has basically achieved domestic substitution, and only a small number of high-end preparations still use imported APIs.

The original research enterprise of drotaverine is Chinoin Pharmaceutical Works of Hungary, and the original research brand name is "No-spa". Its core compound patent expired globally in 1999. The dosage forms of the original research drug approved in China include 40mg tablets and 2ml:40mg injections, both of which have been included in the China Listed Drug Catalogue as reference preparations. In terms of domestic API registration, there are currently 13 drotaverine API registration numbers including that of the original research drug, among which 8 have been activated in A status and can be associated with domestic preparation applications. More than 30 related generic preparations have been approved for marketing in China, covering oral and injection dosage forms. (Data as of October 2024, please refer to the official website of CDE for the latest information)

CATO can provide a full set of drotaverine impurity reference standards. Most products are available from stock. Orders for in-stock products placed before 16:00 can be shipped on the same day. All products meet the compliance requirements of multiple regulatory systems such as the Chinese Pharmacopoeia and FDA, and can fully meet the reference standard requirements for the whole process of API R&D, quality research and declaration.