Delving into the Latest Updates on Tolfenamic Acid with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Tolfenamic acid (JAN/INN), NSC-757873, NTX 010

+ [4]

Target

COX

Mechanism

COX inhibitors(Cyclooxygenases inhibitors)

Therapeutic Areas

Nervous System DiseasesSkin and Musculoskeletal DiseasesEndocrinology and Metabolic Disease+ [1]

Active Indication

ArthritisDysmenorrheaMigraine Disorders+ [3]

Inactive Indication

Supranuclear Palsy, Progressive

Originator Organization

Hangzhou Minsheng Pharmaceutical Co., Ltd.

Active Organization

Hangzhou Minsheng Pharmaceutical Co., Ltd.

NeuroTau, Inc.StartupSandoz A/S

Inactive Organization-

Drug Highest PhaseApproved

First Approval Date

DK (06 Jun 2000),

Acute migraine

Regulation-

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Structure

Molecular FormulaC14H12ClNO2

InChIKeyYEZNLOUZAIOMLT-UHFFFAOYSA-N

CAS Registry13710-19-5

The purposes of this study are to:
Evaluate the safety and toxicity of tolfenamic acid when used with gemcitabine and radiation therapy in patients with locally advanced or metastatic pancreatic cancer.
Determine the maximum-tolerated dose (MTD) of tolfenamic acid when used with gemcitabine and radiation in pancreatic cancer.
Characterize the pharmacokinetic profile of tolfenamic acid when used with gemcitabine and radiation.
Assess the anti-tumor response to tolfenamic acid when used with gemcitabine and radiation in patients with advanced pancreatic malignancies.

Start Date01 Mar 2014

Sponsor / Collaborator

Orlando Health, Inc.

100 Clinical Results associated with Tolfenamic Acid

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100 Translational Medicine associated with Tolfenamic Acid

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100 Patents (Medical) associated with Tolfenamic Acid

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410

Literatures (Medical) associated with Tolfenamic Acid

01 Nov 2024·VETERINARY ANAESTHESIA AND ANALGESIA

Perioperative pain management in dogs and cats: Attitudes and practices among Thai veterinarians

Article

Author: Mama, Khursheed ; Niyom, Sirirat ; Thunpattranon, Teerapat ; Lekchareonsuk, Chalermpon ; Kasemsuwan, Suwicha

OBJECTIVE:

To assess attitudes of Thai veterinarians towards perioperative pain management in dogs and cats, and explore associations between demographic characteristics and use of analgesics and pain assessment.

STUDY DESIGN:

Paper-based survey distributed in person during various small animal practitioner conferences in 2022.

METHODS:

The questionnaire encompassed six sections: demographic information, use of analgesic techniques, postoperative pain evaluation, pain indicators, general opinions and confidence in managing postoperative pain in dogs and cats. Chi-square test, logistic regression model and Mann-Whitney U or Kruskal-Wallis tests were used for data analysis; p < 0.05 was considered significant.

RESULTS:

A total of 390 completed questionnaires were collected, with one discarded owing to potential erroneous responses. The most widely used analgesics were alpha-2 adrenergic receptor agonists (84%), postoperative non-steroidal anti-inflammatory drugs (NSAIDs; 83.5%) and preoperative opioids (74.3%). Carprofen (87.3%) and tolfenamic acid (80.9%) were the most frequently administered NSAIDs, while tramadol (86%) and morphine (71%) were the most widely used opioids. Preoperative and postoperative opioid administration were less common among males than females, with odds ratios (ORs) of 0.53 and 0.56, respectively (both p = 0.009). Veterinarians who graduated after 2014 were less likely to prescribe preoperative NSAIDs than those who graduated before 2009 (OR = 0.25; p < 0.001). Epidural anesthesia, nerve blocks and pre- and postincisional blocks were more frequently used by referral center veterinarians than those working in non-referral clinics (ORs = 30.5, 14.7, 4.29 and 8.85, respectively; all p < 0.001) and by veterinarians holding advanced degrees beyond the Doctor of Veterinary Medicine (DVM) compared with those with a DVM degree (OR = 6.25, 4.83, 2.25 and 5.75, respectively; all p < 0.001).

CONCLUSIONS AND CLINICAL RELEVANCE:

This study reveals variations in perioperative pain management practices in dogs and cats among veterinarians, influenced by sex, graduation year, education and workplace.

01 Nov 2024·Veterinary Medicine and Science

Plasma and Milk Pharmacokinetics and Estimated Milk Withdrawal Time of Tolfenamic Acid in Lactating Sheep

Article

Author: Durna Corum, Duygu ; Elmas, Muammer ; Uney, Kamil ; Cetin, Gul ; Coskun, Devran ; Corum, Orhan

ABSTRACT:

Objective:

This study aimed to investigate the plasma and milk pharmacokinetics, as well as the withdrawal time (WT) from milk of tolfenamic acid (2 and 4 mg/kg) following intravenous (IV) administration to eight healthy lactating Akkaraman sheep.

Methods:

The trial was conducted in two periods in accordance with a crossover pharmacokinetic design. The concentrations of tolfenamic acid in the plasma and milk were determined using high‐pressure liquid chromatography and evaluated using non‐compartmental analysis. The WT of tolfenamic acid in milk was calculated using the WT 1.4 software.

Results:

Compared to the 2 mg/kg dose, plasma volume of distribution at steady state (from 0.43 to 0.50 L/kg), terminal elimination half‐life (from 2.41 to 4.14 h) and dose‐normalized area under the plasma concentration–time curve (AUC0−∞, from 9.46 to 30.11 h µg/mL) increased, whereas total body clearance (from 0.21 to 0.13 L/h/kg) decreased at the 4 mg/kg dose. The peak milk concentration (Cmax) and AUC0−∞ values in milk were 0.26 µg/mL and 0.28 h µg/mL, respectively, for 2 mg/kg, and 0.43 µg/mL and 0.55 h µg/mL, respectively, for 4 mg/kg. Although the dose‐normalized Cmax of milk decreased depending on the dose, no difference was observed in dose‐normalized AUC0−∞. The AUC0−∞ milk/AUC0−∞ plasma ratio was 0.03 for 2 mg/kg and 0.02 for 4 mg/kg. The WT values calculated for milk at dosages of 2 and 4 mg/kg were 3 and 4 h, respectively.

Conclusions:

A decrease in plasma elimination and an increase in plasma concentration of tolfenamic acid were observed depending on the dose. Tolfenamic acid lowly passed into sheep's milk at 2 and 4 mg/kg doses. This study may provide valuable information for clinicians’ decision‐making processes.

01 Jul 2024·Veterinary Medicine and Science

Pharmacokinetics, bioavailability and plasma protein binding of tolfenamic acid in rainbow trout (Oncorhynchus mykiss)

Article

Author: Acar, Omer Faruk ; Durna Corum, Duygu ; Aksoy, Mert ; Marin, Pedro ; Uney, Kamil ; Corum, Orhan

Abstract:

Background:

Although research on the mechanism and control of pain and inflammation in fish has increased in recent years, the use of analgesic drugs is limited due to the lack of pharmacological information about analgesic drugs. Tolfenamic acid is a non‐steroidal anti‐inflammatory drug and can be used in fish due to its low side effect profile and superior pharmacokinetic properties.

Objectives:

The pharmacokinetics, bioavailability and plasma protein binding of tolfenamic acid were investigated following single intravascular (IV), intramuscular (IM) and oral administration of 2 mg/kg in rainbow trout at 13 ± 0.5°C.

Methods:

The experiment was carried out on a total of 234 rainbow trout (Oncorhynchus mykiss). Tolfenamic acid was administered to fish via IV, IM and oral route at a dose of 2 mg/kg. Blood samples were taken at 13 different sampling times until the 72 h after drug administration. The plasma concentrations of tolfenamic acid were quantified using high pressure liquid chromatography–ultraviolet (UV) and pharmacokinetic parameters were assessed using non‐compartmental analysis.

Results:

The elimination half‐life (t1/2ʎz) of tolfenamic acid for IV, IM and oral routes was 3.47, 6.75 and 9.19 h, respectively. For the IV route, the volume of distribution at a steady state and total body clearance of tolfenamic acid were 0.09 L/kg and 0.03 L/h/kg, respectively. The peak plasma concentration and bioavailability for IM and oral administration were 8.82 and 1.24 µg/mL, and 78.45% and 21.48%, respectively. The mean plasma protein binding ratio of tolfenamic acid in rainbow trout was 99.48% and was not concentration dependent.

Conclusions:

While IM route, which exhibits both the high plasma concentration and bioavailability, can be used in rainbow trout, oral route is not recommended due to low plasma concentration and bioavailability. However, there is a need to demonstrate the pharmacodynamic activity of tolfenamic acid in rainbow trout.

100 Deals associated with Tolfenamic Acid

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External Link

KEGG	Wiki	ATC	Drug Bank
D01183	Tolfenamic Acid	M01AG02	DB09216

R&D Status

Approved

10 top approved records.

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Indication	Country/Location	Organization	Date
Arthritis	CN	Hangzhou Minsheng Pharmaceutical Co., Ltd.	13 Jul 2005
Dysmenorrhea	CN	Hangzhou Minsheng Pharmaceutical Co., Ltd.	13 Jul 2005
Migraine Disorders	CN	Hangzhou Minsheng Pharmaceutical Co., Ltd.	13 Jul 2005
Pain	CN	Hangzhou Minsheng Pharmaceutical Co., Ltd.	13 Jul 2005
Acute migraine	DK	Sandoz A/S	06 Jun 2000