Analgesic Effect Study of Young Coconut Water (Cocos nucifera L.) on Mice (Mus musculus) Induced with Pain using Acetic Acid

Introduction: Pain signals tissue damage that is capable of reducing thequality of life. Non-Steroidal Anti-inflammatory Drugs (NSAIDs) are known as effective analgesic drugs which have various side effects, therefore natural minerals are used as an alternative medicine for pain and inflammation, one of which is known to be coconut water. Hence this research was conducted to find out the differences of the analgesic effect between young coconut water (Cocos nucifera L.) with non-selective and COX-2 selective NSAID on mice induced with pain from acetic acid 0.6% 1 ml/100gBW of mice.Methods: True experimental, conducted at the Pharmacology Laboratory in Faculty of Medicine of Airlangga University involving the sample of 48 mice (6 groups). The recorded data was tested using the oneway ANOVA methodology before then continued with the posthoc test of LSD.Results: The addition of young coconut water (Cocos nucifera L.) with the dosage of 3 ml/100gBW, 4 ml/100gBW, and 4.5 ml/100gBW of mice doesn't give any significant analgesic effect even though the analgesic protection percentage increases accordingly to its dosage (12.32%, 18.72%, 26.88%), but non-selective and COX-2 selective NSAID give significant analgesic effect (p<0.05) on mice induced with pain from acetic acid 0.6% 1 ml/100gBW of mice.Conclusion: There are differences in the analgesic effect of young coconut water (C. nucifera L.) with non-selective and COX-2 selective NSAID on mice induced with pain from acetic acid 0.6% 1 ml/100gBW of mice.

Comparison of Nociceptive Effects of Buprenorphine, Firocoxib, and Meloxicam in a Plantar Incision Model in Sprague–Dawley Rats

Due to their reduced frequency of dosing and ease of availability, NSAIDs are generally preferred over opioids for rodent analgesia. We evaluated the efficacy of the highly COX2-selective NSAID firocoxib as compared with meloxicam and buprenorphine for reducing allodynia and hyperalgesia in rats in a plantar incision model of surgical pain. After a preliminary pharmacokinetic study using firocoxib, Sprague–Dawley rats (n = 12 per group, 6 of each sex) were divided into 6 groups: no surgery (anesthesia only), saline (surgery but no analgesia), buprenorphine (0.05 mg/kg SC every 8 h), meloxicam (2 mg/kg SC every 24 h), and 2 dosages of firocoxib (10 and 20 mg/kg SC every 24 h). The nociception assays were performed by using von Frey and Hargreaves methodology to test mechanical allodynia and thermal hyperalgesia. These assays were performed at 24 h before and at 20, 28, 44, and 52 h after start of surgery. None of the analgesics used in this study produced significantly different responses in allodynia or hyperalgesia from those of saline-treated rats. In the Hargreaves assay, female saline-treated rats experienced significantly greater hyperalgesia than did males. These findings add to a growing body of literature suggestingthat commonly used dosages of analgesics may not provide sufficient analgesia in rats experiencing incisional pain.

Perioperative anesthesia. Features of anesthesia for patients with different surgeries and traumas

Background. Chronic postoperative and post-traumatic pain is included in the new edition of the International Classification of Diseases, which should become valid on 01.01.2022. Routine adherence to specialized differentiated evidence-based protocols for perioperative management of patients is the best way to optimize perioperative analgesia. The patient and his relatives should be informed about the possibility of postoperative pain (POP) and treatment options. It is advisable to use multimodal analgesia (MMA) with non-pharmacological methods to eliminate POP. Objective. To describe modern points of view on perioperative analgesia. Materials and methods. Analysis of literature data on this topic. Results and discussion. Analgesics are divided into antinociceptive drugs (hyperalgetics (morphine and μ-agonists) and antihyperalgetics – paracetamol, nonsteroidal anti-inflammatory drugs (NSAID), glucocorticoids, nefopam, tramadol) and non-antinociceptive antihyperalgetics (ketamine, gabapentine, topical anesthetics, clonidine, adenosine, neostigmine). Whenever possible, every anesthesiologist should take a multimodal approach. In the absence of contraindications, all patients should receive NSAID around the clock, including cyclooxygenase-2 inhibitors or acetaminophen (paracetamol). Intravenous paracetamol has a number of advantages over oral one. With the infusion of paracetamol (Infulgan, “Yuria-Pharm”), the time to achieve clinically significant analgesia is only 8 minutes, and to achieve maximum anesthesia – 15 minutes. Preoperative intravenous paracetamol has convincingly demonstrated an opioid-sparing effect in various surgical interventions (joint replacement, bariatric surgery, surgery for head and neck tumors) and delivery. The financial and economic feasibility of treatment with intravenous paracetamol has been proven. Additionally, the administration of regional blockades with topical anesthetics should be considered. It is also advisable to use pregabalin or gabapentin. The choice of drug, dose, route of administration and duration of therapy should be individualized. Intramuscular administration of analgesics should be avoided. In neuropathic POP, first-line drugs include tricyclic antidepressants, norepinephrine and serotonin reuptake inhibitors, antiepileptics, topical anesthetics (bupivacaine – Longocaine, “Yuria-Pharm”), second-line – opioids, tramadol, and third-line – mexiletine, NMDA-receptor antagonists, capsaicin. It should be noted that bupivacaine is 2-3 times more effective than lidocaine and 6-12 times more effective than novocaine. Local anesthetics can be used for infiltration anesthesia, blockade, intraperitoneal injection and direct infusion into the wound. Dexmedetomidine, which also provides sedation and additional analgesia, can be used to prolong sensory and motor anesthesia with bupivacaine. Analgesia in different interventions is slightly different. Thus, in total joint arthroplasty, a single blockade of the adductor canal is effective. When restoring the rotator cuff, it is advisable to use an arthroscopic approach, paracetamol (Infulgan), NSAID, dexamethasone and regional anesthesia. In spinal surgery, postoperative MMA involves the use of cold compresses, pregabalin, cyclobenzaprine, tramadol, if necessary – oxycodone. In total mastectomy, gabapentin and paracetamol should be prescribed before surgery, and opioids, ondansetron, and/or lorazepam on demand – after surgery. After abdominal hysterectomy, in severe pain opioids are used in combination with cyclooxygenase-2 inhibitors or non-selective NSAID, in mild pain – cyclooxygenase-2 inhibitors or non-selective NSAID in combination with paracetamol and, if necessary, weak opioids. Postoperative management of women after caesarean section involves the use of oral NSAID and paracetamol, opioids (rescue analgesia) and long-term infusions of local anesthetics into the wound. Conclusions. 1. Anesthesia plays a leading role in accelerated postoperative rehabilitation programs. 2. When choosing an approach to analgesia one should take into account the area of intervention. 3. Rational reduction in the opioids amount is achieved through balanced MMA. 4. The most basic components of MMA include NSAID, paracetamol and regional techniques.

The estimation of competitive positions of non-steroid anti-inflammatory drugs on pharmaceutical market of Ukraine

The aim of our analysis is the estimation of non-steroid anti-inflammatory drugs (NSAID) competitiveness level, calculation of capacity, share and saturation of studied segment of market that allow to improve the competitive strategies of pharmaceutical manufacturing enterprises. MATERIALS AND METHODS: According to the results of content-analysis of foreign and native economic literature, we elaborated the methodology of estimation of NSAID competitive positions that consists of six main stages. The offered model of estimation of competitiveness of the studied group of medicines is based on the construction of competition map of medicines on the example of non-selective NSAID as the largest group by the number of presented trade names (TN) using the calculation of market share of medicines for 2015-2016 and dynamics of its growth. RESULTS: The results of NSAID TN distribution in groups according to the market share volume testify that only 8 TN of medicines among 74 are the leaders of market and 10 TN are characterized with strong competitive position. At the same time 51 NSAID TN are outsiders and 5 TN have weak competitive position. The results of NSAID TN distribution in groups according to the change of their competitive position allow state that 16 TN among 74 have fast worsening competitive position, 43 TN belong to the group with worsening competitive position and only 5 TN has competitive position, characterized by fast improvement. CONCLUSION: The analysis of position, occupied by NSAID TN in matrix, demonstrated that 8 TM of medicines are the leaders of the market. At the same time 51 medicines TN are outsiders. The results of research demonstrated that 59 NSAID TN are characterized with worsening and fast worsening competitive positions.

Evaluation of community pharmacists’ roles in screening and communication of risks about non-steroidal anti-inflammatory drugs in Thailand

AimThis study aimed to explore community pharmacists’ roles on screening for risk factors, providing safety information-related non-steroidal anti-inflammatory drugs (NSAIDs) to patients.BackgroundNSAIDs are widely dispensed without a prescription from pharmacies in Thailand, while they are frequently reported as causing adverse events.MethodsSelf-administered questionnaires were distributed to all accredited pharmacies in Thailand, inviting the main pharmacist in each pharmacy to participate in this study.FindingsOut of 406 questionnaires distributed, 159 were returned (39.2%). Almost all pharmacists claimed to engage in NSAID dispensing practice, but not all of them provided relevant good practice, such as, screening for risk factors (56.3–95.5%), communication on adverse drug reactions (ADRs) (36.9–63.2%) and ADR management (58.9–79.7%), history of gastrointestinal (GI) problems was frequently mentioned for screening, but many pharmacists did not screen for history of NSAID use (24.7–35.5%), older age (45.2–48.9%), concomitant drug (63.7%), and problems of cardiovascular (24.1%), renal (34.9–43.3%), and liver systems (60.3–61.0%). Male pharmacists were significantly less likely to inform users of non-selective NSAIDs about ADRs [odds ratio (OR) 0.44], while provision of information about selective NSAID ADRs was higher among pharmacy owners (OR 2.28), pharmacies with more pharmacists (OR 3.18), and lower in pharmacies with assistants (OR 0.41). Screening for risk factors, and risk communication about NSAIDs were not generally conducted in Thai accredited community pharmacists, nor were NSAID complications fully communicated. Promoting of community pharmacists’ roles in NSAID dispensing should give priority to improving, especially in high-risk patients for taking NSAIDs.

CHRONIC GASTRITIS CLINICAL FEATURES AND STOMACH FUNCTIONAL STATE DURING NONSTEROIDAL ANTI-INFLAMMATORY DRUGS ADMINISTRATION IN PATIENTS WITH OSTEOARTHRITIS

Aim. Determination of chronic gastritis clinical features and stomach functional state during nonsteroidal anti-inflammatory drugs (NSAID) administration in patients with osteoarthritis (OA). Materials and methods. 122 patients with OA and verified chronic gastritis (CG) (50 males and 72 females) aged 42 to 64 years (mean age – 49.65±3.51) were observed. Depending on gastritis morphological form, patients were divided into 2 groups: 54 patients with OA in combination with non-atrophic gastritis (NAG) were included into the group I, 68 patients with OA in combination with atrophic gastritis (AG) – into group II. 40 patients with OA without concomitant gastroduodenal pathology in anamnesis were included into the group III. All patients obtained selective NSAID for OA treatment: Meloxicam 15 mg daily or Nimesulide 200 mg daily. The control group was formed by 20 persons, which were found to be healthy after a complex examination. Stomach acid-forming function was investigated using esophageal pH monitoring. In the gastric contents, which obtained by aspiration, concentration of sialic acids glycoproteins, fucose, and hexosamines was determined. Results. Clinical picture of NSAID gastropathy at NAG characterized by abdominal pain of varying intensity and not associated with eating, but in patients with AG severity and discomfort symptoms dominated over weakly expressed pain syndrome. As a result of NSAID, in the group I dyspepsia developed in 31 (57.4 %), and erosive gastropathy developed in 9 (16.7 %) patients. In the group II, erosive gastropathy and dyspepsia were observed in 15 (22.1%) and in 35 (51.5 %) patients, respectively. In the group III, erosive gastropathy was observed 3.3 times (c2=84.33; р=0.009) and 4.4 times (c2=36.78; р=0.002) less than in groups I and II, respectively. In 25% patients of the group I after NSAID therapy intragastric pH increased from normacid to hyperacid status. In the group II, NSAID administration led to stomach mucosal (SM) protective factors depletion, which was observed in 73.3 % and in 28.6 % of patients with erosive gastropathy and NSAID-associated dyspepsia, respectively. At AG with erosive gastropathy, unlike NAG, several protective factors simultaneous reduction was observed. Coonclusion. In anamnesis, CG factor at selective NSAID administration (Meloxicam and Nimesulide) in relation to OA significantly increases the risk of erosive gastropathy, compared with patients without CG in anamnesis. At OA NSAID administration in patients with NAG led to gastric contents acidification and in patients with AG – to SM protective factors depletion (glycoprotein, fucose, and hexosamine).