Delving into the Latest Updates on Drotaverine Hydrochloride with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Drotaverin, Drotaverine, Deolin

+ [1]

Target

PDE4

Action

inhibitors

Mechanism

PDE4 inhibitors(Phosphodieterase 4 inhibitors)

Therapeutic Areas

Nervous System DiseasesSkin and Musculoskeletal Diseases

Active Indication

Muscle Spasticity

Inactive Indication-

Originator Organization

CHINOIN Pharmaceutical Co.

Active Organization

CHINOIN Pharmaceutical Co.

Inactive Organization-

License Organization-

Drug Highest PhaseApproved

First Approval Date-

Regulation-

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Structure/Sequence

Molecular FormulaC24H32ClNO4

InChIKeyJBFLYOLJRKJYNV-UHFFFAOYSA-N

CAS Registry985-12-6

View All Structures (2)

主要研究目的：按有关生物等效性试验的规定，选择Opella Healthcare为持证商的盐酸屈他维林片（商品名：NO-SPA；规格：40mg）为参比制剂，对石家庄四药有限公司生产并提供的受试制剂盐酸屈他维林片（规格：40mg）进行空腹和餐后给药人体生物等效性试验，比较受试制剂中药物的吸收速度和吸收程度与参比制剂的差异是否在可接受的范围内，评价两种制剂在空腹和餐后给药条件下的生物等效性。次要研究目的：观察健康志愿受试者口服受试制剂盐酸屈他维林片（规格：40mg）和参比制剂盐酸屈他维林片（商品名：NO-SPA；规格：40mg）的安全性。

[Translation]

The main purpose of the study: According to the relevant provisions of the bioequivalence test, Opella Healthcare was selected as the reference preparation for the drotaverine hydrochloride tablets (trade name: NO-SPA; specification: 40 mg), and the test preparation drotaverine hydrochloride tablets (specification: 40 mg) produced and provided by Shijiazhuang Siyao Co., Ltd. was used for the human bioequivalence test of fasting and postprandial administration. The absorption rate and degree of the drug in the test preparation were compared with the reference preparation to see whether they were within the acceptable range, and to evaluate the bioequivalence of the two preparations under fasting and postprandial administration conditions. The secondary purpose of the study: To observe the safety of oral administration of the test preparation drotaverine hydrochloride tablets (specification: 40 mg) and the reference preparation drotaverine hydrochloride tablets (trade name: NO-SPA; specification: 40 mg) to healthy volunteers.

Start Date03 Dec 2023

Sponsor / Collaborator

Shijiazhuang No. 4 Pharmaceutical Co., Ltd.

CTR20232627

/ CompletedNot Applicable

盐酸屈他维林片生物等效性试验

[Translation] Bioequivalence study of drotaverine hydrochloride tablets

主要研究目的评价中国健康成年受试者空腹及餐后条件下单次单剂量口服江西亿友药业有限公司生产的盐酸屈他维林片（受试制剂，规格：40mg）和Opella Healthcare France SAS持证的盐酸屈他维林片（参比制剂，商品名：NO-SPA®，规格：40mg）后的药代动力学特点和生物等效性。次要研究目的研究盐酸屈他维林片的受试制剂（规格：40mg）和参比制剂（NO-SPA®，规格：40mg）在中国健康成年受试者中的安全性。

[Translation]

Main study objectives To evaluate the pharmacokinetic characteristics and bioequivalence of single oral doses of drotaverine hydrochloride tablets (test preparation, specification: 40 mg) produced by Jiangxi Yiyou Pharmaceutical Co., Ltd. and drotaverine hydrochloride tablets (reference preparation, trade name: NO-SPA®, specification: 40 mg) certified by Opella Healthcare France SAS in healthy Chinese adult subjects under fasting and postprandial conditions. Secondary study objectives To study the safety of the test preparation (specification: 40 mg) and reference preparation (NO-SPA®, specification: 40 mg) of drotaverine hydrochloride tablets in healthy Chinese adult subjects.

Start Date28 Aug 2023

Sponsor / Collaborator

Jiangxi Yiyou Pharmaceutical Co., Ltd.

100 Clinical Results associated with Drotaverine Hydrochloride

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100 Translational Medicine associated with Drotaverine Hydrochloride

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100 Patents (Medical) associated with Drotaverine Hydrochloride

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589

Literatures (Medical) associated with Drotaverine Hydrochloride

01 Apr 2025·Journal of Pharmaceutical Sciences

Optimization of HPLC method for determination of Abraham solvation parameters of pharmaceuticals

Article

Author: Knašienė, Birutė ; Sadaunykas, Audrius ; Sazonovas, Andrius ; Balčiūnas, Simonas ; Naujalis, Evaldas ; Lanevskij, Kiril

Abraham solvation equation (Absolv) is a popular and well-established approach for modeling solute partitioning between phases of different polarity, which finds its applications in both organic chemistry and biomedical fields. Parameters constituting this equation are good quantitative descriptors of solute hydrogen bonding potential that are useful for QSAR modeling of more complex chemical and biological phenomena. Numerous studies dealing with fast determination of Abraham descriptors using HPLC can be found in the literature, but these mostly focus on small un-ionizable industrial and environmental chemicals, whereas experimental data for pharmaceutical molecules are clearly lacking. In the current study we build upon a previously published chromatographic approach, aiming to adapt the method to ionizable drug-like compounds, and optimize it by reducing the number of required HPLC columns. The analysis involves determination of the overall H-bond acidity (A), H-bond basicity (B) and polarity/polarizability (S) descriptors for 62 pharmaceutical molecules with previously unpublished parameter values.

24 Mar 2025·Journal of Biomolecular Structure and Dynamics

Bioprospecting of Meliaceae family phytomolecules for the treatment of monkeypox virus infection: a QSAR modeling and MD simulation approach

Article

Author: AlShehail, Bashayer M. ; Al Kaabi, Nawal A. ; Alotaibi, Nouf ; Alissa, Mohammed ; Alsomali, Ghaneema ; Alqahtani, Ali S. ; Al-Subaie, Maha F. ; Rabaan, Ali A. ; Almansour, Zainab H. ; Alshehri, Ahmad A. ; Halwani, Muhammad A. ; Khamis, Faryal

Recent monkeypox virus (MPXV) infections show the risk of MPXV transmission that persists today and the significance of surveillance and quick response methods to stop the virus's spread. Currently, the monkeypox virus infection is not specifically treated. In this study, QSAR models were designed using known inhibitors of cysteine proteinase from the vaccinia virus, where the Random Forest model and Ridge model had showed the best correlation between predicted and observed EC₅₀. These models were used to screen Maliaceae family phytochemicals against MPXV cysteine proteinase. The compound, IMPHY010637 was detected in top 5 from both the QSAR screening models and showed best docked score (-8.6 kcal/mol) and thus selected for further investigation. Further, the IMPHY010637 showed interaction with the catalytic residue His²⁴¹ of the protein as reported in earlier studies. The ADMET analysis of the compound showed the acceptable drug-like properties of IMPHY010637. However, these properties could be improved after experimental validation of protein-ligand binding. Both docked complex and poses created in 100 ns MD simulation of the protein-ligand complex showed the presence of multiple hydrogen bonds. RMSD and conformation analysis showed stable binding of IMPHY010637 with the cysteine proteinase of MPXV at its active site. Compared to the known inhibitor, IMPHY010637 showed better binding with the protein as observed by the PCA and MM/GBSA analysis. This study concluded IMPHY010637 as a potential inhibitor for the cysteine proteinase of MPXV using computational methods that could be tested in in-vitro experiments.

01 Mar 2025·Biological Trace Element Research

Mercury Levels in Selected Medicines and Dietary Supplements in Poland

Article

Author: Ahnert, Bożena ; Brodziak-Dopierała, Barbara ; Fischer, Agnieszka

AbstractCurrent trends are promoting youth, beauty, health, and fitness. Individuals often seek out remedies, such as medicines or dietary supplements (DS), to achieve these goals. However, highly processed foods, chronic stress, and environmental pollution contribute to the development of civilization diseases. The aim of this study was to evaluate the mercury (Hg) content in medicines and DS that are available in Poland. A total of 139 preparations were tested (75 drugs, 64 DS). The medicines contained preparations belonging to antibacterial, antiviral, antifungal; analgesic, antipyretic, and anti-inflammatory; heart and blood vessel disease preventatives; respiratory tract infections treatment; diuretics; aiding digestion; supplements; antidiarrhoeals; anti-allergics; anti-rheumatics; antibiotics; and others. The tested dietary supplements had an effect on the following: improve the condition of skin, hair, and nails; vitamins; minerals; probiotics; weight loss; special for women; and others. The Hg content of the samples was determined using atomic absorption spectrometry (AAS). The Hg content of all the preparations varied widely (0.1–57.4 µg/kg), with a median Hg concentration of 1.2 µg/kg. The median Hg concentration for medicines was 0.8 µg/kg, prescription medicines having higher Hg concentrations (0.9 µg/kg) than over-the-counter (OTC) drugs (0.5 µg/kg). For DS, the Hg content was found to be higher than for drugs, at 2.0 µg/kg. The herbal preparations showed the highest Hg content among the individual DS groups (3.4 µg/kg). The Hg concentrations in the tested drug and DS samples did not exceed acceptable standards. However, if multiple pharmaceutical preparations are taken simultaneously over a long period of time, and there is existing environmental exposure, there is a possibility of Hg concentration accumulation and adverse health effects.

100 Deals associated with Drotaverine Hydrochloride

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External Link

KEGG	Wiki	ATC	Drug Bank
-	Drotaverine Hydrochloride	A03AD02	DB06751

R&D Status

10 top approved records.

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Indication	Country/Location	Organization	Date
Muscle Spasticity	China	CHINOIN Pharmaceutical Co.	-

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


WCLC2013	Not Applicable	Advanced Lung Adenocarcinoma	558	Gefitinib treatment	(sbucpotxoa) = cxgmhttihn orqudnjthm (ytxxqjcrfq )	Positive	30 Oct 2013
				No Gefitinib treatment	(sbucpotxoa) = qgaoxjwjal orqudnjthm (ytxxqjcrfq )
NCT00731198 (CTgov)	Phase 3	Pancreatic Diseases \| Bile Duct Diseases	650	Drotaverine hydrochloride (Experimental)	mnjkjqcodi(okimttraxu) = azfkpcvkon umhajsntww (tismookfrf, wrwvvfojgh - lbytebqwpk) View more	-	23 Dec 2009
				Hyoscine-N-butylbromide (Active Comparator)	mnjkjqcodi(okimttraxu) = ruuzsminse umhajsntww (tismookfrf, frpqnvhakh - ifvxrvbmme) View more
IAS2003	Not Applicable	-	1,290	ZDV -> D4T switch	hsykbhejhm(hrcexhkhzc) = vntchfxpit wavsyrjrxn (ocxdpqtabe )	-	01 Jan 2003
				DDI <-> 3TC switch	hsykbhejhm(hrcexhkhzc) = ldfqmvyfzr wavsyrjrxn (ocxdpqtabe )