Pharmacological investigation of Thespesea populnea bark extract for analgesic activity

Background: Pain is an unpleasant and distressing common problem with profound impact on individuals and society. Existing treatment modalities used for pain management are either less effective or exhibits several side effects. The aim of current study is to investigate the analgesic activity of stem bark extract of Thespesea populnea for pain management.Methods: Thirty Swiss albino were divided into five groups including control, standard and three tests groups (different doses of Thespesea populnea bark extract). Groups were investigated for analgesic activity using hot plate induced paw withdrawal, acetic acid induced writhing and formalin induced paw licking models.Results: Findings of hot plate model revealed that, percent increase in reflex latency of paw licking response in mice for test drug (10 mg/kg), attained peak effect of 136% at 180 minutes, whereas for standard pentazocine peak effect of 125% was attained at 180 minutes. In acetic acid model, the maximum percent inhibition in number of writhings for the test drug (30 mg/kg) was 68% and for standard diclofenac, it was 80%. In formalin model, percent inhibition in licking response in early and late phases for test drug (30 mg/kg) were 81% and 91% and for standard diclofenac it was 56% and 94% respectively. It was thus depicted that analgesic activity of test drug was significantly more than the standard in early phase and equivalent to standard in late phase.Conclusions: It was concluded that Thespesea populnea bark extract at a dose of 10 mg/kg showed potential peripheral and central analgesic activity

Screening of a novel-substituted furan compound for analgesic activity in mice

Background: Pain is an unpleasant sensation and is the most primitive of all senses. It is a major symptom in many medical conditions and can significantly interfere with a person's quality of life and general functioning. Analgesics like opioids and NSAIDS are used to treat pain but due to their side effects on long term use it is necessary to develop a compound with reduced side effects. Hence the present study was focused on screening of novel compound of novel compound 2-(4-nitrophenylimino)-N-cyclohexyl-4,5 diphenylfuran-3- carboxamide (AMSM-2(a-k) for analgesic activity in mice.Methods: The analgesic activity of test compound AMSM-2(a-k) at different doses (5 mg/kg, 10 mg/kg and 20 mg/kg) was evaluated by using Eddy’s hot plate for determining central analgesic activity using morphine (5 mg/kg) as standard drug, acetic acid induced writhing test for peripheral analgesic activity and formalin induced writhing test to evaluate both central and peripheral analgesic activity using aspirin as standard drug (300 mg/kg). The percentages of inhibition of writhing’s were calculated for acetic acid and formalin induced pain model. The statistical analysis was done using one way ANOVA followed by Dunnett’s test. All values with P <0.05 were considered statistically significant.Results: In hot plate method, the percentage increase in the latency of licking for test compound AMSM-2(a-k) at 20 mg/kg was significantly comparable to standard drug. Morphine (10 mg/kg) and AMSM-2(a-k) (20 mg/kg) gave the peak effect at 90 minutes. In acetic acid induced writhing method the percentage inhibition for AMSM-2(a-k) (20 mg/kg) was 73.93% for up to 20 min and for aspirin was 57.12%. In formalin induced paw licking method, the percentage inhibition in licking response in the early phase for AMSM-2(a-k) with 20 mg/kg was 63.23% which was more significant than the standard drug aspirin (100 mg/kg) which gave a percentage inhibition of 42.17%. In the late phase the percentage inhibition in licking response for AMSM-2(a-k) (20 mg/kg) was 74.33% and aspirin (100 mg/kg) gave a percentage inhibition of 60.82%.Conclusions: The test drug AMSM-2(a-k) at a dose of 20 mg/kg showed promising results in hot plate method, equally comparable to the standard drug morphine and in acetic acid induced writhing test and formalin induced paw licking (early and late phase) methods they are more significant than the standard drug aspirin. This suggests AMSM-2(a-k) had potential central and peripheral analgesic activity

Effect of oral clonidine premedication on attenuating haemodynamic response to laryngoscopy and intubation during general anaesthesia

Background: Laryngoscopy with or without tracheal intubation evokes a defense mechanism that in turn alters patients’ haemodynamic responses in terms of increased heart rate (HR) and arterial blood pressure (ABP). Aim of current investigation was to study the efficacy of orally administered clonidine in a dose of 3-3.5 µg/kg given 90 minutes prior to scheduled time of the surgery, in attenuating the adverse haemodynamic responses to laryngoscopy and intubation of the trachea. Methods: Eighty normotensive patients between 20-60 years of age and having ASA grade I/II physical status were subdivided in two groups with 40 patients in each; test group received clonidine in a dose of 3-3.5 mcg/kg of body weight orally, 90 min before surgery and control group did not receive clonidine premedication. Induction was done with Thiopentone intravenous injection (5 mg/kg), followed by succinylcholine (1-1.5 mg/kg). Results: Haemodynamic responses in terms of parameters like HR, systolic blood pressure (SBP), diastolic blood pressure (DBP), mean arterial pressure (MAP) were recorded at pre induction and at 1, 2, 3, 5 minutes following laryngoscopy. The 1-minute post induction values of SBP, DBP, MAP were significantly less in clonidine group (p&lt;0.001) and the significance in listed parameters between two groups persisted until 5 minutes. Increase in HR was less in clonidine group than in control group. Conclusions: Premedication with oral clonidine 3-3.5 mcg/kg of body weight, 90 minutes before laryngoscopy and intubation is an efficient, simple and inexpensive method in attenuating the haemodynamic response generated due to laryngoscopy and intubation

Pharmacological evaluation of substituted 4, 5-diphenyl furan-3-carboxamide compound for antidepressant activity in mice

Background: Depressive disorder is a prevalent psychiatric disorder, which affects 21% of the world population. Many drugs are available as effective antidepressants. But still there is necessity of developing novel compounds with minimized side effects. Hence this study was aimed to investigate the antidepressant activity of novel furan compound in albino mice.Methods: Antidepressant activity of novel furan compound was investigated by using forced swimming test (FST) and tail suspension test (TST) models. Fluoxetine was used as standard drug in this study.Results: It has been observed from our study that medium dose of test compound (10 mg/kg) reduced duration of immobility time to 35 seconds when compared to control group (147 seconds) in FST model. In TST model, the test compound of medium dose (10 mg/kg) had produced 83% protection against passive behaviour which is almost similar to standard drug fluoxetine (100%).Conclusions: The results of the specifies that compared to other two doses of test compound (5 mg/kg and 20 mg/kg), medium dose of test compound found as an effective dose for treating depression produced due to stress. However, further expansion of the study is needed for this compound to prove as a novel effective antidepressant compared to other drugs available for treating depression

A prospective comparative study of efficacy of lenalidomide plus dexamethasone combination therapy versus VAD (vincristine, doxorubicin and dexamethasone) regimen in the treatment of multiple myeloma

Background: Lenalidomide plus Dexamethasone (Len-Dex) and VAD (Vincristine, Doxorubicin and Dexamethasone) regimen are the two common drug therapies employed in the treatment of Multiple myeloma.Objectives: To compare the efficacy of Len-Dex versus VAD regimen based on complete remission achieved with treatment in newly diagnosed cases of multiple myeloma in a tertiary care hospital in Kerala.Methods: Eighty patients (forty in each group) of newly diagnosed cases of multiple myeloma, who were willing to give the informed consent, were included in the study. Patients were allocated by the treating physician to two groups; one group was given Len-Dex (lenalidomide + dexamethasone) regimen and the other VAD (Vincristine, Adriamycin, Dexamethasone) regimen. A total of six cycles were given for both groups. Their baseline investigations and follow up investigations were collected at regular intervals, based on these values, the outcome was classified as partial remission and complete remission and the results were compared and analyzed.Results: Among the forty patients in each group, 17 (38%) on VAD regimen and 28 (62%) on Len-Dex regimen achieved complete remission. The statistical analysis was done using chi square test (χ2= 6.13, df= 1, p= 0.01) which showed statistically significant difference.Conclusions: The study showed that the efficacy of Lenalidomide-Dexamethasone (Len-Dex) combination therapy is clearly higher than that of VAD regimen among the study population. The overall efficacy of Len-Dex combination is 70% and that of VAD regimen is only 42.5%

Synthesis and Characterisation of Bis-(chloromethyl) Oxetane, its Homopolymer and Copolymer with Tetrahydrofuran

Bis-(chloromethyl) oxetane (BCMO) was synthesised from pentaerythritol by chlorination,followed by ring closure. It was polymerised using BF3-etherate and butanediol system, similarlythe BCMO–THF (tetrahydrofuran) copolymer was also synthesised. The monomers and thepolymers were characterised by IR, 1H-NMR and molecular weight. Flame retardant propertiesof the poly-BCMO were also investigated

Sizing of cracks embedded in sub-cladding using the ultrasonic synthetic aperture focusing technique (SAFT)

This paper deals with the experimental work carried out to demonstrate the feasibility of the ultrasonic Synthetic Aperture Focusing Technique (SAFT) to obtain improved detection and sizing of vertical/inclined (10° and 15° simulated cracks underneath different claddings. Crack heights ranging from 1.68 mm to 19.04 mm underneath stainless steel, Inconel and ferritic steel cladding were sized with an accuracy of ±0.1 to ±0.3 mm. The problems encountered in TOFD with regard to sizing of near-surface cracks was successfully overcome by SAFT. Mis-oriented (inclined) defects embedded below the cladding suffer added disadvantage for ultrasonic detection due to loss of reflected energy due to mis-orientation. Using SAFT even these defects could be sized accurately