Dose-dependent analgesic activity of mexiletine on thermally induced pain in rats

Background: Pain is an unpleasant sensory and emotional experience associated with actual or potential tissue damage or described in terms of such damage. In spite of many advances in pain research, we are unable to deal in an effective way. The cost for new drug development is increasing day by day. Drug repurposing is an approach to look for new use in drugs that are already approved for other indications. Mexiletine is a sodium channel blockers that is being approved for treatment of arrhythmias. It is being tried in treatment of various painful conditions. The present study is to evaluate the dose-dependent analgesic activity of mexiletine with ibuprofen.Methods: The analgesic activity of mexiletine was compared at doses of 15mg/kg, 30mg/kg and 45mg/kg with the standard dose of ibuprofen at 10mg/kg in male Wistar rats in thermal model of tail flick analgesiometer.Results: At lower doses (15mg/kg) of mexiletine, analgesic activity of ibuprofen was significantly higher. At higher doses (30 mg/kg and 45 mg/kg) of mexiletine, it was observed that there is no significant difference between the analgesic activities of both drugs.Conclusions: Mexiletine demonstrated a dose-dependent analgesic activity. There was no statistically significant difference between the analgesic activities of higher doses of mexiletine when compared to ibuprofen

A prospective, randomized, double blind, comparative study of intramuscular nalbuphine hydrochloride, butorphanol tartrate and pentazocine lactate for post-operative pain relief following abdominal hysterectomy

Background: This study aimed to compare the efficacy and safety of intramuscularly administered nalbuphine, butorphanol and pentazocine for post-operative pain relief after abdominal hysterectomy.Methods: Seventy-five adult female patients, aged between 20-50 years, belonging to American Society of Anaesthesiologists (ASA) class 1 and 2, posted for abdominal hysterectomy under spinal anesthesia were included in the study. The subjects were randomly divided into 3 groups (n=25 each) and given – Group A: pentazocine lactate (30 mg, 1mL), Group B: butorphanol tartarate (2 mg, 1 ml) and Group C: nalbuphine hydrochloride (10 mg, 1 mL) when post-operative pain intensity reached ≥4 mm on the Visual analogue scale (VAS). The onset, duration, time to peak effect and adverse events were recorded at regular intervals for 24 hours, postoperatively.Results: The mean time to onset of anesthesia was significantly faster (P<0.05 each) in the nalbuphine (10.2±2.2 minutes) and butorphanol (11.3±2 minutes) groups when compared to the pentazocine group (14±2.7 minutes). Duration of analgesic action was significantly longer (P<0.05 each) in the nalbuphine (236.4±75.1 minutes) and butorphanol (202±59.2 minutes) groups when compared to the pentazocine group (177.4±55.3 minutes). No significant differences in respiratory and cardiovascular parameters were noted between the groups. Nausea and vomiting was seen significantly higher in the pentazocine group (36%) when compared to butorphanol (20%) and nalbuphine (8%) groups (p<0.05 each).Conclusions: Intramuscular nalbuphine and butorphanol provided effective analgesia with rapid onset and longer duration of action, with lower incidence of nausea and vomiting when compared to pentazocine. In particular, nalbuphine can be a suitable agent to provide post-operative pain relief in gynecologic lower abdominal surgery

Second year medical students’ feedback on teaching-learning methodologies and evaluation methods in Pharmacology: a questionnaire based study

Background: Pharmacology enables medical students with the art of rational prescriptions of drugs. It is one of the rapidly evolving subjects in medical sciences. The purpose of the study was to assess whether teaching-learning methodologies and evaluation methods are supporting the curriculum goals and what modifications can be made for the benefit of medical students.Methods: After approval by the Institutional Ethics Committee the study was carried out in January-February 2017. A total of 128 students of 2nd MBBS were administered a pre-validated questionnaire after explaining the purpose of the study. Descriptive statistics were used for analysis of data. Frequency was expressed as percentage.Results: A total response rate of 93.75% was observed. Most of the students mentioned cardiovascular system (20.8%) as the most interesting topic. 78.3% preferred teaching by use of combination of both audio-visual aids and chalk and board. Majority of the students rated practical classes as similar to theory (34.2%). 91.7% students mentioned that seminars are useful to them. 95% of students are interested in continuation of the integrated classes conducted at the end of each chapter. 98.3% of students for written tests and 90% for viva voce responded positively for the need of such periodic evaluation in addition to university prescribed evaluations. 95% students mentioned that field visits helps them in better understanding of pharmacology.Conclusions: The present study helped us to elicit student preferences regarding teaching and evaluation methods in pharmacology. Implementation of the same would be helpful for better outcome of students

Analysis of spontaneously reported cutaneous adverse drug reactions in a tertiary care teaching hospital in South India

Background: Skin is the most common organ involved in adverse reactions due to drugs. With newer drugs released into market every year, there is changing pattern of the reported cutaneous adverse drug reactions (ADRs). In order to ensure safer use of medicines in patients, there is need for continuous monitoring of ADRs. This is a retrospective study to analyse spontaneously reported cutaneous ADRs.Methods: All the cutaneous ADRs reported between January 2017 and September 2018 were analysed for clinical patterns, suspected medications, causality, severity and preventability.Results: Of the 1035 reports received during the study period, 232 (22.41%) included cutaneous reactions. 113 (48.7%) were male and 119 (51.29%) were female. Maculopapular rash 70 (30.17%), pruritus 31 (13.36%), palmar plantar erythrodysesthesia 30 (12.93%), acne 19 (8.19%), urticaria 16 (6.89%) and fixed drug eruptions (FDE) 13 (5.6%) were the common clinical patterns. Antimicrobial agents followed by anticancer drugs, nonsteroidal anti-inflammatory drugs (NSAIDs), hormones and related drugs, and antiepileptic drugs were the common suspected group of drugs. Causality assessment as done by WHO-UMC scale showed that 3 (1.29%) were certainly related, 174 (75%) were probably related and 55 (23.7%) were possibly related to the suspected medication.Conclusions: Cutaneous ADRs are most frequently reported ADRs in the present study. With newer drugs released into market, there is a need for continuous monitoring of use of drugs to promote safer use of medicines in patients

Analgesic activity of Alpinia galanga extract in mice models and TNF-alpha receptor computational docking analysis on its leads with pharmacokinetics prediction

Background: Alpinia galanga is an ayurvedic herb recognized and used across many traditional medicine systems for its analgesic and anti-inflammatory activity. The present study scientifically validates the potential anti nociceptive action of ethanolic extract of Alpinia galanga by chemical, neurogenic and inflammatory nociception model in mice followed by identification of potential lead compound by computational analysis.Methods: The assessment of anti nociceptive action is evaluated by Acetic acid induced abdominal constrictions and Formalin assay on ethonolic extract of Alpinia galanga, followed by 20 compounds with known chemical structure of Alpinia galanga is subjected to computational analysis to predict possible lead compound with desirable pharmacokinetic and drug like features.Results: The percentage inhibition rate of Aspirin (100mg/kg) was 82.15% compared to Alpinia galanga (100mg/kg) 19.63%, (200mg/kg) 33.02% and (400mg/kg) 57.13% by acetic acid induced abdominal constrictions antinociceptive mice model. Alpinia galanga 400mg/kg (71.70%) had comparable percentage inhibition of nociception to standard group indomethacin (88.71%) in formalin induced nociceptive mice model. Among 20 compounds screened for pharmacokinetic and drug like features, Galanal B had the binding free energy -56.664 when compared to control compound 2AZ5-56.000.Conclusions: The Alpinia galanga extract had significant anti nociceptive activity and followed by computational analysis of 20 compounds with known chemical structure predicted Galanal B as lead compound with best insilico pharmacokinetic and drug like features