Delving into the Latest Updates on Lornoxicam with Synapse

Berberine hydrochloride (BER), a promising candidate in treating tumors, diabetes and pain management, has relatively low oral absorption and bioavailability due to its low intestinal permeability. To address these challenges, we developed a BER and lornoxicam cocrystal (BLCC) by a solvent evaporation method and characterized it using X-ray diffraction, differential scanning calorimetry and thermogravimetric analysis. Compared with BER, BLCC exhibited an instant release in pH 1.0 HCl and a sustained release up to 24 h in pH 6.8 buffer solutions and water. The Caco-2 permeability of BLCC has shown a remarkable increase compared to that of BER (i.e., P_app(a→b): 50.30 × 10^-7vs 8.82 × 10^-7 cm/s), which is attributed to the improved lipophilicity of BER (i.e., log P: 1.29 vs -1.83) and the reduced efflux amount of BER (i.e., ER: 1.71 vs 12.11). Furthermore, BLCC demonstrated a relative bioavailability of 410 % in comparison to the original BER, due to notably enhanced intestinal permeability of BLCC and its continuous dissolution in simulated intestinal fluid. BLCC has the potential to tailor the dissolution behavior, improve intestinal permeability, and boost the bioavailability of BER. This indicates that the cocrystal strategy holds promise as an effective approach to improving the oral absorption and bioavailability of active pharmaceutical molecules with low permeability during drug development.

31 Oct 2024·Cureus Journal of Medical Science

Enhancing Postoperative Analgesia After Cesarean Section: Insights Into Transversus Abdominis Plane Block, Intrathecal Opioids, and Other Analgesic Techniques

Article

Author: Al-Kayyal, Yusra S ; Awaleh, Fouad I ; Ahmed, Rania S ; Shaheen, Issam S ; Alsubaie, Abdullah T ; El-Tallawy, Salah N ; Amlih, Haneen F ; Pergolizzi, Joseph V ; Ali, Wegdan A ; Fairaq, Moaaz M

BACKGROUND:

Cesarean section (CS) is associated with moderate to severe pain that may delay recovery and interfere with the mother's ability to take care of the newborn. This clinical study aimed to evaluate different analgesic protocols for postoperative pain management after CS.

METHODS:

The study included 300 parturients scheduled for CS and classified into five equal groups as follows: general anesthesia (GA group), GA plus transversus abdominis plane (TAP) block (GA+TAP group), spinal anesthesia (SA) plus intrathecal fentanyl (ITF group), SA plus fentanyl + TAP block (ITF+TAP group), and SA plus intrathecal morphine (ITM group). Multimodal analgesia was added to all groups in the form of paracetamol 1 g/6 hours intravenously (IV), lornoxicam (8 mg/8 hours/IV), in addition to rescue opioid analgesia (morphine or oxycodone 4 mg/IV) upon the patient's request. Primary outcomes included pain assessments by numerical rating scale (NRS), worst and least pain scores, and time in maximum pain. Secondary outcomes included time to first request of analgesia, total opioid consumption, patient request for additional analgesia, function, and satisfaction scores. Possible side effects and neonatal Apgar scores were recorded at five and 10 minutes.

RESULTS:

The results showed a significant difference between the study groups regarding pain relief. The best pain relief, lowest worst pain, least pain, and total opioid consumption were reported by the ITM group, followed by ITF+TAP, GA+TAP, then SA, and GA groups (p < 0.05). The lower percentage of time in the worst pain and the longest time to the first request of analgesia were reported with ITM and ITF+TAP groups followed by the ITF group and GA+TAP group. In contrast, the longest time spent in the worst pain and the shortest duration until the first request of analgesia was observed in the GA group (p < 0.05). The best function scores were observed with ITF+TAP and then ITM, while the highest satisfaction scores were reported with ITM, ITF+TAP followed by SA and GA+TAP, and the lowest scores were observed in the GA group (p < 0.001 and p < 0.005, respectively). Side effects such as itching, nausea, and vomiting were significantly higher in the ITM group when compared to the other groups (p < 0.05). There were no significant differences between the study groups regarding the Apgar scores at five and 10 minutes (p = 0.271 and 0.760).

CONCLUSIONS:

Bilateral TAP block has the potential to effectively enhance postoperative analgesia and reduce the need for systemic opioids after both GA and SA. Compared to ITF, ITM provides a higher quality and longer duration of analgesia with minimal analgesic-related side effects. Further studies to find an optimal analgesic protocol with few to no side effects are warranted.

01 Oct 2024·INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES

Identifying alkaline phosphatase inhibitory potential of cyclooxygenase-2 inhibitors: Insights from molecular docking, MD simulations, molecular expression analysis in MCF-7 breast cancer cell line and in vitro investigations

Article

Author: Hussain, Safdar ; Putra, Purnawan Pontana ; Ashraf, Muhammad ; Hamid, Sujhla ; Iqbal, Ambar

Alkaline phosphatases (APs, EC 3.1.3.1) belong to a superfamily of biological macromolecules that dephosphorylate many phosphometabolites and phosphoproteins and their overexpression is intricated in the spread of cancer to liver and bones, neuronal disorders including Alzheimer's disease (AD), inflammation and others. It was hypothesized that cyclooxygenase-2 (COX-2) selective inhibitors may possess anti-APs potential and may be involved in anticancer proceedings. Three COX-2 inhibitors including nimesulide, piroxicam and lornoxicam were evaluated for the inhibition of APs using in silico and in vitro methods. Molecular docking studies against tissue nonspecific alkaline phosphatase (TNAP) offered the best binding affinities for nimesulide (-11.14 kcal/mol) supported with conventional hydrogen bonding and hydrophobic interactions. MD simulations against TNAP for 200 ns and principal component analysis (PCA) reiterated the stability of ligand-receptor complexes. Molecular expression analysis of TNAP enzyme in the breast cancer cell line MCF-7 exhibited 0.24-fold downregulation with 5 μM nimesulide as compared with 0.26-fold standard 10 μM levamisole. In vitro assays against human placental AP (hPAP) displayed potent inhibitions of these drugs with IC₅₀ values of 0.52 ± 0.02 μM to 3.46 ± 0.13 μM and similar results were obtained for bovine intestinal AP (bIAP). The data when generalized collectively emphasizes that the inhibition of APs by COX-2 inhibitors provides another target to work on the development of anticancer drugs.

1

News (Medical) associated with Lornoxicam

01 Mar 2020

·acino.swiss

Acino completes acquisition with Takeda for primary care portfolio in key emerging markets

Acino and Takeda Pharmaceuticals announced today the completion of the acquisition for parts of Takeda’s primary care portfolio in selected countries in the Middle East, Africa, and Ukraine. Acino has received anti-trust approvals in Turkey, South Africa, and Ukraine and can now proceed with the integration as planned. As part of the transaction, Acino acquired the rights to selected pain management, gastroenterology, cardiovascular and respiratory products from Takeda’s prescription pharmaceutical and OTC portfolio. Around 270 employees, primarily sales and marketing professionals supporting the portfolio, are also transitioning to Acino. ‘We are excited to welcome our new colleagues to Acino and to expand our offering in our key therapeutic areas and markets’, says Steffen Saltofte, CEO of Acino. ‘The portfolio we have acquired fits very well with our strategy to make high-quality medicines accessible to patients and healthcare professionals in emerging markets.’ The transfer comprises approximately 30 selected prescription pharmaceutical and OTC medicines including Pantoprazole, Dexlansoprazole, Cardiomagnyl, Xefo and Montelukast. The acquisition enables Acino to further reinforce its position in the key markets of the United Arab Emirates, Egypt, Saudi Arabia, Ukraine and South Africa. Additionally, Acino has opened a company in Istanbul, Turkey, to expand its footprint in this country. As previously announced in October 2019, Acino agreed to acquire the assets from Takeda for a total value in excess of $200 million. Additionally, both parties have entered into a multi-year manufacturing and supply agreement, under which Takeda will continue to manufacture the products on behalf of Acino.

Acquisition

100 Deals associated with Lornoxicam

Login to view more data

External Link

KEGG	Wiki	ATC	Drug Bank
D01866	Lornoxicam	M01AC05	DB06725

R&D Status

Approved

10 top approved records.

Login

to view more data

Indication	Country/Location	Organization	Date
Bursitis	JP	Taisho Pharmaceutical Co., Ltd.	02 Feb 2001
Cervicobrachial syndrome	DK	-	01 Jan 1997
Low Back Pain	DK	-	01 Jan 1997
Neuralgia	DK	-	01 Jan 1997
Osteoarthritis	DK	-	01 Jan 1997
Pain	DK	-	01 Jan 1997
Pain, Postoperative	DK	-	01 Jan 1997
Periarthritis	DK	-	01 Jan 1997
Rheumatic Diseases	DK	-	01 Jan 1997
Rheumatoid Arthritis	DK	-	01 Jan 1997

Developing

10 top R&D records.

Login

to view more data

Indication	Highest Phase	Country/Location	Organization	Date
Headache	Phase 2	US	POZEN, Inc.	01 Dec 2005
Migraine Disorders	Phase 2	US	POZEN, Inc.	01 Dec 2005

Login to view more data

Clinical Result

Indication

Phase

Evaluation

View All Results

Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT01117948 (CTgov)	Phase 2	Alzheimer Disease	219	Lornoxicam (Lornoxicam)	cufllfoulj(cjnmkcqfxl) = jczmsbwprz efmlutjkwh (tglunrlchh, rqrrfflpqi - hzycsfulli) View more	-	29 Nov 2012
				Placebo (Placebo)	cufllfoulj(cjnmkcqfxl) = drauaeqyub efmlutjkwh (tglunrlchh, ibdnpheeqw - ghtkuaybhi) View more