Pentazocine versus tramadol-paracetamol combination as analgesia in labor: A randomized controlled trial

Objectives: Labor should be a satisfactory experience and effective pain management should be employed as recommended by the American Congress of Obstetricians and Gynaecologists. In developing countries, pain management in labor is still a big challenge and the search for the ultimate labor analgesia is still ongoing. The objectives of the study were to determine whether the synergistic analgesic effect of the combination of tramadol and paracetamol will produce analgesia comparable to pentazocine with a better side effect profile. Material and Methods: This was a randomized controlled, double-blinded trial of tramadol-paracetamol combination versus pentazocine as labor analgesia and was carried out at the University of Abuja Teaching Hospital, Abuja, between June 2018 and March 2019. A total of 218 eligible parturients recruited at term, were counseled on labor analgesia, its benefits, and the options made available to them and educated on the pain scoring system. Parturients were allocated into two groups using computer-generated numbers with the WINPEPI software. Group A was given tramadol-paracetamol combination, while Group B received pentazocine, both at standard doses. Hourly pain scores, APGAR scores, labor duration, patients' satisfaction, and side effects were collated. The level of significance was set at <0.05. Results: Tramadol-paracetamol was administered to 109 (50.9%) while pentazocine was administered to105 (49.1%) of the study participants. The mean age in the tramadol-paracetamol group was 29.6 ± 4.8 years, and in the pentazocine group, it was 28.8 ± 4.5 years. The difference in pain scores on the visual analog scale was statistically significant at the 3rd and 4th h (P = 0.02 and 0.004), but not significant in the 1st and 2nd h (P = 0.05 and 0.22) in the two groups. Overall, the average pain score in the tramadol-paracetamol group was significantly higher compared to the pentazocine group (5.27 ± 1.86 vs. 4.72 ± 1.54; P = 0.02). The 1st and 5th min APGAR scores (P = 0.44 and 0.67, respectively) of neonates in the tramadol-paracetamol and pentazocine groups were comparable. Nausea and drowsiness occurred more frequently in the pentazocine group at P-values of 0.047 and 0.0015, respectively. There was no statistically significant difference in the duration of labor between the tramadol-paracetamol and pentazocine groups. not statistically significant, a higher proportion of parturients in the pentazocine group was satisfied compared with the tramadol-paracetamol group (71.4% vs. 63.3%; P = 0.13).Conclusion: This study showed that intravenous pentazocine provides better pain relief in labor, but the tramadol-paracetamol combination has fewer side effects

Investigating The Role Of Nf-Κb, Cox-1, Cox-2, Comt, Il-10, Il-6 And Tnf-Α In Modulating Anti-Nociceptive Activity Of Methanolic Extract Of Entada Phaseoloides

Objective: To investigate the analgesic activity of methanolic extract of Entada phaseoloides (MEEP) along with its molecular mechanistic pathway. Methods: Swiss albino female mice and Wistar rats of either sex were administered orally with MEEP extracts (100, 200 and 400 mg/kg) and pentazocine, tramadol and diclofenac sodium, as standard drugs. Following administration, anti-nociceptive activity was evaluated using an acetic acid-induced writhing test, Eddy’s hot plate, and hot water immersion test. Serum was collected for molecular expression of various proteins and genes using Reverse Transcriptase PCR and Western Blotting. Results: Acetic acid writhing test, a frequently used method to assess peripheral analgesic activity, revealed that MEEP reduced peripherally induced pain in a dose-dependent manner. Likewise, Eddy’s hot plate and hot water immersion methods, often implicated for testing central analgesic activities, showed that MEEP is bestowed with the capability to counteract analgesia in a dose and time-dependent manner. Pro-inflammatory cytokines and factors like COX-2, IL-6, TNF-α, and NF-κB that cause inflammatory responses and pain were significantly reduced, suggesting its analgesic and anti-inflammatory potential. This analgesic and the anti-inflammatory role played by MEEP is also supported by the up-regulation of anti-inflammatory cytokine IL-10 and COMT and COX-1 enzyme demonstrated no significant difference between the groups. Conclusion: The study revealed the weak peripheral and potent central analgesic property MEEP by modulating pro-inflammatory and anti-inflammatory pathways.

Comparative Effects of Single Agent Rectal Diclofenac versus a Combination of Rectal Diclofenac and Intramuscular Pentazocine, on Post Caesarean Section Pain Relief in a Tertiary Institution in Southern Nigeria

Background: Caesarean section commonly causes moderate to severe pain in the first 24 hours after surgery with associated discomfort, delayed ambulation, difficulty initiating breastfeeding and prolonged hospital stay. Receiving adequate analgesia after caesarean section is very important for the patient’s comfort, overall wellbeing and recovery.Objective:To compare the efficacy, time to rescue-analgesia and side effects of single agent rectal diclofenac versus its combination with intramuscular pentazocine for pain management after caesarean section in Rivers State University Teaching Hospital (RSUTH). Methodology:A randomized double-blind clinical trial was carried out at the RSUTH. A total of 120 patients scheduled for either elective or emergency caesarean section were recruited. Group ‘A’ received rectal diclofenac 100mg and intramuscular placebo (unimodal group) while group ‘B’ received rectal diclofenac 100mg and intramuscular pentazocine 30mg (multimodal group). Socio-demographic information was collected via structured proforma, while Visual Analog Scale (VAS) was used to assess the level of pain. Data were analyzed using SPSS version 20 and statistical significance was set at p< 0.05.Results:The mean ages of respondents in unimodal and multimodal groups were 31.7 ± 4.3 years and 31.3 ± 5.2 years respectively. The difference in the median pain score and range was significant only at 8 hours between the groups, there was no significant difference before and after 8 hours. Although the mean time (in minutes) to first rescue-analgesia was shorter in the unimodal (147.5 ± 60.1) as compared to the multimodal group (170.0), this difference was not statistically significant. There was no side effect noticed in either of the two groups.Conclusion: The combined agents (diclofenac and pentazocine) had a superior analgesic effect to the single agent (diclofenac alone) when given as used in the study.

A study to evaluate the analgesic activity of Origanum vulgare in mice using tail flick method

Background: Pain is a complex experience consisting of physiological and psychological response to a noxious stimulus. Analgesics like opiates and non-steroidal anti-inflammatory drugs are commonly used for relieving pain but are associated with various unwanted side effects; therefore this study was conducted by using Origanum vulgare for their analgesic efficacy.Methods: In vivo model used was tail flick method. Origanum vulgare (84 mg/kg p.o) was administered in mice. The analgesic activity was studied by recording the reaction time after administration of the drug at frequent intervals up to 3 hours. The results were analysed by ANOVA and Tukey’s test. P-value <0.05 was considered as significant. Pentazocine showed statistically prolongation in the reaction time after 30 min as compared to Origanum vulgare.Results: In tail flick method, pentazocine showed statistically significant increase in the reaction time after 30 min of administration as compared to control group. However, Origanum vulgare in a dose of 84 mg/kg showed significant increase in the reaction time after 30 min of administration as compared to control group. On comparing pentazocine and Origanum vulgare, pentazocine showed highly significant increase in the reaction time after 30 min as compared to Origanum vulgare at 84 mg/kg dose.Conclusions: From the present study, it was concluded that extract of Origanum vulgare exerted analgesic activity in both the models. However, it was less potent than pentazocine. Thus, Origanum vulgare can be used in mild to moderate painful conditions.

Combined anticonvulsant effect of nifedipine and pentazocine in experimentally induced seizures in rats

Background: Epilepsy is one of the common disorders of human with a prevalence of approximately 1% of the total population. Majority of seizures can be controlled with available antiepileptic drugs, about 20% of them still remain resistant to treatment. Recognizing this, there is a need to develop newer antiepileptic drugs with therapeutic potential. Present work is based upon the production of convulsions by maximal electroshock in rats. Evaluation of combined anticonvulsant effect of nifedipine and pentazocine on the duration of convulsion and duration of tonic hind limb extension and recovery in rats.Methods: The study was commenced after obtaining approval from IAEC, Department of Pharmacology, Osmania Medical College, Koti, Hyderabad. All the wistar rats were induced convulsions by Maximal Electro-Shock (MES) method and rats showing tonic hind limb extension response were randomised into four groups (six animals in each group). Group 1 received distilled water, group 2 treated with nifedipine 10mg/kg BW, group 3 treated with pentazocine 30mg/kg BW and group 4 treated with both nifedipine 10mg/kg BW and pentazocine 30mg/kg BW. Drug administered by intraperitoneal route. The data analysed using ANOVA and group means with LSD Post Hoc Test. p?values <0.05 were considered as significant.Results: When nifedipine and pentazocine were combined, the mean duration of convulsions, tonic hind limb extension and recovery were significantly decreased compared to control, nifedipine and pentazocine.Conclusions: The results obtained in this study provide supporting pharmacological evidence of efficacy, possible potential benefit of combining nifedipine with pentazocine in epilepsy.

A study to evaluate the analgesic activity of Origanum vulgare in mice using hot plate method

Background: The International Association for Study of pain, has defined pain as actual or potential tissue damage or described in terms of such damage. But the burden of unwanted side effects with current regimens are high. To explore the potential of Ayurveda drugs, this study is done by using Origanum vulgare.Methods: In vivo model used-Hot plate method. Origanum vulgare (84 mg/kg p.o) was administered in mice. The analgesic activity was studied by recording the reaction time after administration of the drug at frequent intervals up to 3 hrs. The results were analysed by ANOVA and Tukey’s test. P value <0.05 was considered as significant. Pentazocine showed statistically prolongation in the reaction time after 30 min as compared to Origanum vulgare.Results: In hot plate method, pentazocine showed statistically significant increase in the reaction time after 30 min of administration as compared to control group. However, Origanum vulgare in a dose of 84 mg/kg showed significantly increase in the reaction time after 30 min of administration as compared to control group. On comparing pentazocine and Origanum vulgare, pentazocine showed highly significant increase in the reaction time after 30 min as compared to Origanum vulgare at 84 mg/kg dose.Conclusions: From the present study, it was concluded that extract of Origanum vulgare exerted analgesic activity in both the models. However, it was less potent than pentazocine. Thus, Origanum vulgare can be used in mild to moderate painful conditions.

Comparison of Ketamine and Pentazocine with Fentanyl and Propofol combination for anaesthesia during laparoscopic tubal ligation

Background: Laparoscopic tubal ligation have advantages of minimally invasive surgical technique, without risk of major haemorrhage, early postoperative ambulation and alimentation, making it suitable for ambulatory surgery. The choice of aneasthesia for laparoscopic ligation hence should consider the anaesthetic agents with a rapid onset of action and fast recovery time, with minimal problems for intraoperative control of haemodynamic, airway and pain relief as well as take consideration of the safety, quality, efficacy, and utilization of resources available to the given situation.Methods: A total of 100 patients aged from 18 to 45 years who were scheduled to undergo laparoscopic tubal ligation  were divided into Group I-  Ketamine plus pentazocine group (n=50), Group II- Propofol plus fentanyl group (n=50) and studied  for the intraoperative parameters (hemodynamic and respiratory profile), recovery time, postoperative side effects and discharge time.Results: Intraoperatively MAP and HR were consistently higher in group I as compared to group II. Incidence of apnea and need for bag and mask ventilation was significantly more in Group II than in Group I as was the incidence of Bradycardia. Postoperative nausea and vomiting, psychomimetic effects were significantly more in Group I than in Group II. The time to reach modified PADSS ≥9 (discharge time) was significantly longer in group I (140.3±12.82 min than in group II 102.2±9.2 min), P<0.01.Conclusions: Combination of ketamine and pentazocine gives good anaesthetic conditions during procedure with less incidence of airway and haemodynamic complications intraoperatively but more incidence of postoperative side effects like nausea, vomiting, psycomimetic effects, and time to meet discharge criteria, compared to propofol plus fentanyl.

Effect of dexmedetomidine combined with pentazocine intravenous anesthesia on percutaneous kyphoplasty for osteoporotic vertebral compression fractures / 中华创伤杂志

Objective To investigate the clinical efficacy of dexmedetomidine (DEX) combined with pentazocine intravenous anesthesia in percutaneous kyphoplasty (PKP) for osteoporotic vertebral compression fracture (OVCF) in the elderly.Methods A retrospective case-control study was performed to analyze 63 elderly OVCF patients treated with PKP and admitted to Tianjin Hospital from June 2018 to December 2018.There were 20 males and 43 females,aged 65-86 years [(74.7 ± 1.1)years].There were 15 patients with thoracic compression fractures and 48 with lumbar compression fractures,in whom the vertebral height loss was ＜ 30％ without posterior ligament complex damage.Nineteen patients received local anesthesia with lidocaine (Group A),21 patients received intravenous anesthesia with pentazocin and propofol (1 mg/kg) (Group B),and 23 patients received intravenous anesthesia with pentazocin and DEX (0.5 μg/kg) (Group C).Heart rate,systolic blood pressure,respiratory rate and blood oxygen saturation (SPO2) were recorded at 5 time points:at rest in the operating room (T0),after intravenous injection of pentazocine (T1),when the balloon dilated (T2),after the injection of cement (T3),and blinking after being called or at the end of the operation (T4).The levels of plasma cortisol were recorded before and at T3 in three groups.Visual analogue score (VAS) at T4 was recorded.The operation time,patient satisfaction and incidence of adverse reactions were recorded.The wake-up time and orientation recovery time of groups B and C were recorded.Results The heart rate,mean systolic blood pressure,respiratory rate in Group A at T2,T3 and T4 were higher than those in Groups B and C (P ＜ 0.05),but there was no significant difference between Groups B and C (P ＞ 0.05).There was no significant difference in SPO2 at only time among the groups (P ＞ 0.05).No significant differences were found in cortisol between the three groups before surgery.The cortisol level of Group A at T3 was higher than those of Groups B and C with significant difference (P ＜ 0.05),but no significant difference was found between Groups B and C (P ＞0.05).The VAS in Group A was significantly higher than those in groups B and C (P ＜ 0.01).The operative time in Group A was longer than those in Groups B and C (P ＜ 0.05),but no significant difference was found between Groups B and C (P ＞ 0.05).There was no significant difference in patient satisfaction between Groups B and C,and both of them were higher than Group A (P ＜0.01).There was no significant difference in the incidence of adverse reactions between the three groups (P ＞ 0.05).The wake-up time and orientation recovery time of Group C were shorter than those of Group B (P ＜ 0.01).Conclusion For elderly OVCF patients,pentazocin combined with propofol or DEX can be applied in PKP,which has satisfactory analgesic effect,slight effect on respiratory and circulatory,less adverse reactions,and good patient feedback.DEX has more advantages of awakening and orientation recovery and is worthy of clinical application.

Improved synthesis of analgesic pentazocine / 中国药科大学学报

@#A new synthetic process of pentazocine has been developed. Starting from 3, 4-dimethylpyridin and benzyl chloride, via quaternarization, Grignard reaction addition/reduction/salt, cyclization, hydrogenation, alkylation and recrystallization, pentazocine were obtained in a total yield of 8. 4%(with a molar mass of 3, 4-dimethylpyridin), with purity greater than 99. 97%. The improved synthetic route is suitable for industrial production.

Effects of Pentazocine on Emergence Agitation of Patients after Upper Limb Operation with General Anesthesia / 中国药师

Objective: To observe the effects of pentazocine on emergence agitation.Methods: Totally 60 patients with scheduled upper limb operation with general anesthesia were randomly divided into two groups (n =30).Group Ⅰ was given pentazocine 0.25 mg·kg-1 (diluted to 10ml) and group Ⅱ was treated with 0.9% sodium chloride (10 ml) and both were with slow intravenous injection above 3 min before the surgical stitching.BP and HR were recorded and compared before the induction (T 0), before the extubation (T 1) ,at the extubation (T 2), and 5, 10 and in 15 minutes after the extubation (T 3 , T 4 and T 5).The time of recovery, time of extubation and agitation scores in 15 min after the extubation were recorded and compared, and nausea and vomiting were observed as well in both groups.Results: Compared with those in group Ⅰ, HR and BP in group Ⅱ were significantly higher (P＜0.05) at T 3 , T 4 and T 5.There were no significant differences in the breathing recovery time and awakening time between the groups (P＞0.05).The restlessness score in group Ⅰ was significantly lower than that in groupⅡ (P＜0.05).The incidence and degree of postoperative nausea and vomiting in groupⅠ were significantly higher than those in group Ⅱ (P＜0.05).Conclusion: Pentazocine (0.25 mg·kg-1) given before stitching can maintain stable circulation, reduce emergence agitation and protect the safety of patients.

Profile of female patients seeking in-patient treatment for prescription opioid abuse from a tertiary care drug dependence treatment centre from India.

Background & objectives: There has been a limited focus on prescription drug abuse among women in the country. Choice of psychoactive substance, reasons for initiation and co-occurring disorders have been found to be different among men and women. The current study was aimed at studying the profile of female patients seeking in-patient treatment for prescription drug use over a period of five years at a tertiary care drug dependence treatment centre in India. Methods: Case records of all female patients admitted with substance use disorder at a national level drug dependence treatment centre in north India across five years (between January 2008 and December 2012) were reviewed retrospectively to study their socio-demographic and clinical profile. The information was gathered using a semi-structured proforma and detailed case records. Abstinence, relapse and retention rates were calculated. Results: Over the five years, 31 female patients were admitted with prescription drug abuse. Of them, 12 (39%) used prescription opioids and 11 (36%) used prescription opioid along with benzodiazepines. Commonest prescription opioid was pentazocine used by 87 per cent of the women. Twenty two (71%) women were introduced to opioid by medical practitioners and commonest reason for introduction was pain (among 48%). Common co-occurring psychiatric diagnoses were depressive disorder (26%), cluster B traits/disorder (19%) and somatoform disorder (13%). Eight women did not complete treatment and left against medical advice. Thirteen women were advised maintenance treatment, and 70 per cent of them were retained for at least six months. Interpretation & conclusions: Our fi ndings revealed a link between mental illness, pain and non-medical use of prescription opioids among women. Majority of these women received opioids as a legitimate prescription form physician. Therefore, these legitimate prescribers should be trained for pain management to facilitate proper treatment of pain and to prevent the subsequent misuse of these medicines. Female patients with frequent pain complaints should be assessed for psychopathology while prescribing opioids.

Anesthesia Effect of Dezocine and Pentazocine in Painless Artificial Abortion / 医药导报

Objective To observe the anesthesia effect of dezocine and pentazocine in painless artificial abortion, in order to provide a basis for safe use of anesthesia drug in clinical practice. Methods Totally,300 patients undergoing painless artificial abortion were included in this study.The patients were randomly divided into four groups: group A (simple propofo), group B ( propofol combined with fentanyl) ,group C ( propofol combined with dezocine) and group D ( propofol combined with pentazocine)(n=75 each).Four groups of patients were intravenously injected with propofol (1-1.5 mg?kg-1) according to the situation in operation when necessary to maintain anesthesia effect.Heart rate (HR),mean arterial pressure (MAP),arterial oxygen saturation ( SpO2 ) and respiratory frequency were observed and recorded before induction,after induction,at the beginning of the operation,during operation and anesthesia recovery. The onset time of anesthesia, the recovery time, the recovery time of orientation,the postoperative pain score and the incidence of adverse reaction of the four groups were recorded. Results All of the patients achieved good effects of anesthesia in operations. There was no significant difference in the onset time of anesthesia (P>0.05).Awakening time and time of orientation recovery in groups B,C and D were significantly shorter than those in group A (P0.05),but the changes were relatively stable as compared with group A (P<0.05).The rates of adverse reactions in group B,C and D were significantly lower than that in group A (P<0.05).The incidence rates of respiratory depression,nausea and vomiting in group C and D were significantly lower than those in group A and B (P<0.05).The postoperative pain scores of VAS in group B,C and D were significantly lower than that of group A (P<0.05). Conclusion The analgesia effects of dezocine and pentazocine are similar.Application of them can reduce the dosage of propofol and shorten the anesthesia awakening time in painless artificial abortion,at the same time they have less adverse reactions,and they are safe and effective to be used in clinical anesthesia.

Analgesic and antioxidant activities of the methanolic extract of Operculina turpethum leaves in mice.

Background: Operculina turpethum Linn. (Convolvulaceae) is commonly called “Trivrit” or “India jalap” in English. It is a perennial herbaceous plant with purplish stem and milky-white exudates. This study was aimed at evaluation of the analgesic and antioxidant effects of the methanolic extract of O. turpethum leaves in mice. Methods: The acute oral toxicity of the extract was evaluated using up and down method. The analgesic effects were assessed using acetic acid-induced abdominal writhing reflex and tail flick methods, while the antioxidant activity (AA) was assayed using photometric 2, 2-diphenyl-1-picrylhydrazyl free radical scavenging assay method. Results: The extract produced a concentration-dependent increase in the AA with inhibitory concentration 50% >400 μg/ml. The extract (100, 200 and 400 mg/kg) and aspirin (100 mg/kg) produced a significant (p<0.05) dose-dependent reduction in the number of abdominal constriction induced by intraperitoneal injection of acetic acid in treated mice when compared to the distilled water treated mice. The extract (100, 200, and 400 mg/kg) and pentazocine (3 mg/kg) caused a significant (p<0.05) dose-dependent increase in the pain reaction time in the treated mice groups, when compared to the distilled water treated groups. Conclusion: The study showed that O. turpethum possesses analgesic and antioxidant properties and confirmed the folkloric use of O. turpethum leaves in the traditional pain management.

Pentazocine abuse in Sickle Cell Disease Patients Seen at a Tertiary Hospital in Nigeria: A Chronic Menace.

Background: Pentazocine abuse in patients with Sickle cell disease (SCD) has not received adequate attention in Nigeria. Many of these SCD patients have had their conditions unduly worsened and quality of life severely breached by complications of pentazocine abuse. Despite the growing incidence observed in clinical practice and palpable tendency to degenerate further, given the current ease of access to the drug in our environment, it has remained underreported. This study evaluated the myriad physical complications and socioeconomic burden of pentazocine abuse on patients with SCD. Method: This study was carried out on SCD patients (attending the adult hematology clinic) who abused parenteral pentazocine. Data were obtained mainly from detailed history and physical examination. The findings were analysed accordingly. Results: Eleven SCD patients who abused pentazocine were recruited and comprised of 8 males (72.7%) and 3 females (27.3%). Their mean age was 34±6 years, 81.8% were not married, 81.8% had some kind of job and 22.2% of these suffered loss of job. The mean duration of pentazocine abuse was 7.4±3.7 years while mean dose of pentazocine injected by the study participants on daily basis was 279±228 mg; 63.6% needed no prescription papers to purchase the drug and 36.4% used forged prescription papers. The mean monthly expenditure on pentazocine was NGN 27,000±22,000 (Nigerian Naira). It was also noted that 18.2% (2) of the study participants abused other drugs alongside pentazocine. As high as 90.9% (10) had scars and/or ulcers; 63.6% (7) developed lymphedema while 90.9% (10) had some degree of fibrous myopathy. Majority (63.6%) of the participants had fixed contractures and/or deformities of their limbs (and digits) with varying degrees of loss of joint movement and/or gait abnormalities observed in 72.7% (8) of participants. Conclusion: We advocate vigorous sensitization of both healthcare givers and SCD patients on the risk and complications (consequences) of pentazocine abuse. This is to underscore the need for more caution with pentazocine prescription and use. As much as possible oral formulations, when necessary, should be recommended since most of the observed physical complications were apparently due to the parenteral route of administration of the drug. Finally, any SCD patient presenting with the highlighted physical complications must be considered as a case of pentazocine abuse until proven otherwise.

Effects of pentazocine on intubation stress response during slow induction of anesthesia / 实用医学杂志

Objective To investigate the effect of pentazocine combined with midazolam on intubation stress response in slow induction of anesthesia. Mtheods Forty ASAⅠ~Ⅱpatients were divided into two groups. Anesthesia was induced with midazolam 0.03 mg/kg in both groups,and pentazocine 0.8 mg/kg (i.v.) was given in pentazocine group or fentanyl 2 μg/kg (i.v.) in fentanyl group. Five minutes later, 2 mL of 1% decicaine was administered by cricothyroid membrane puncture to facilitate the intubation.The SpO2, circulatory indexes (HR, SBP, DBP, BIS) and sedation level were measured at T0, T1, T2, T3, T4, T5, T6. Results Both pentazocine and fentanyl can inhibit stress responses to tracheal intubation effectively,but pentazocine group is better than fentanyl group on the cardiovascular stability during slow induction of anesthesia. Conclusion Pentazocine 0.8 mg/kg can inhibit stress responses to tracheal intubation effectively with a low incidence of adverse reactions in the slow induction of anesthesia.

Optimum dose of pentazocine when combined with propofol for gastroscopy in elderly patients / 中华麻醉学杂志

Objective To determine the optimum dose of pentazocine when combined with propofol for gastroscopy in elderly patients.Methods One hundred and forty ASA physical status Ⅰ or Ⅱ patients,aged 6575 yr,scheduled for elective gastroscopy under general anesthesia,were randomly assigned into Ⅰ-Ⅳ groups (n =35 each) using a random number table.Before insertion of the gastroscope,pentazocine 0.2,0.4 and 0.8 mg/kg were injected intravenously in Ⅱ-Ⅳ groups,respectively,while the equal volume of normal saline was given in Ⅰ group.Propofol was then administered by target-controlled infusion (TCI).The half-effective concentration (EC50 of propofol was determined by up-and-down sequential trial.The target plasma concentration (Cp) was set at 3.5 μg/ml in the first patient.Gastroscopy was performed at 5 min after the target effect-site and plasma concentrations were balanced.The response to gastroscopy was defined as positive when body movement and/or bucking occurred during gastroscopy.Each time the Cp increased/decreased by 0.3 μg/ml in the next patient depending on whether or not the response to gastroscopy was positive.EC50 and 95 ％ confidence interval of propofol TCI inhibiting the response to gastroscopy were calculated using Probit analysis.The development of respiratory depression and hypotension was observed.Results EC50 (95 ％ confidence interval) of propofol TCI inhibiting the response to gastroscopy was 2.82 (2.63-3.02) μg/ml,2.78 (2.58-2.97) μg/ml,2.16 (2.00-2.32) μg/ml and 2.03 (1.88-2.19) μg/ml in Ⅰ-Ⅳ groups,respectively.Compared with group Ⅰ,EC50 was significantly decreased in Ⅲ and Ⅳ groups,and the incidence of respiratory depression was increased in Ⅳ group (P ＜ 0.05).Conclusion The optimum dose of pentazocine when combined with propofol is 0.4 mg/kg for gastroscopy in elderly patients.

Clinical comparison of propofol combined with pentazocine or fentanyl on analgesic artificial abortion / 中国医师进修杂志

ObjectiveTo investigate the effects of propofol combined with pentazocine or fentanyl on analgesic artificial abortion.MethodsOne hundred and thirty cases of early pregnancy were divided into fentanyl-propofol group (group A) and pentazocine -propofol group (group B) with 65 cases each by random digits table.The change of systolic pressure,diastolic pressure,heart rate,breathing rate,pulse oxygen saturation (SpO2) was compared,anesthetic induce time,operation time,awaking time,adverse effect was recorded.ResultsSystofic pressure,breathing rate and SpO2 intraoperative in two groups was significantly lower than that before anesthesia(P＜ 0.05 ),breathing rate,SpO2 intraoperative in group A was significantly lower than that in group B (P ＜ 0.05 ).The incidence of respiratory depression in group A was significantly higher than that in group B [20.0％(13/65) vs.6.2％(4/65)](P＜0.05).ConclusionPentazocine combined with propofol anesthesia used in analgesic artificial abortion lead to less incidence of adverse reactions,which is a more effective and safe method.

Endoscopic hemorrhoidal sclerotherapy using 50% dextrose water: A preliminary report.

Injection sclerotherapy has a prominent role in the treatment of bleeding hemorrhoids. The commonly used sclerosants are not available or very expensive in Nigeria. We prospectively evaluated 50% dextrose water, used as a nonallergenic sclerosant, in the treatment of bleeding internal hemorrhoids. Forty consenting adult patients (median age 50 years [range 35–67]; 22 women) with bleeding hemorrhoids, seen over a 2-year period, were offered injection sclerotherapy with 50% dextrose water. They were assessed for response, tolerance and complications. The duration of symptoms before presentation was 3 months to 15 years. The bleeding stopped after the injection in all patients. No patient needed a repeat procedure. No complication was recorded during follow up which ranged from 2 months to 12 months. We conclude that endoscopic hemorrhoidal sclerotherapy using 50% dextrose water offers a simple, safe and effective modality of treatment if properly utilized.

Effect of Opioid Agonists , Diazepam and Ketamine on the Estrous and Pregnant Rat Uteri , in Vitro / 대한마취과학회지

Opiates have been used as analgesics in obstetrics since the Babylonian Sinee that time, a wide variety of opiates have been employed in an attempt to provide analgesia for childbirh. The effect of opioids on uterine contractility is of considerable interest. Morphine caused a concentration dependent decrease in the frequency of contraction of the estrous uterus, In contrast, both pethidine and pentazocine enhanced the contraction rate. The pregnant uterus showed little response to morphine, but exhibited an enhanced response to the stimulant activity of both pethidine and pentazocine.It has long been recognized that the tension development of uterine muscle is largely dependent on intracellular Ca2+ pools. Smooth muscle contraction is initiated by depolarization induced calcium entry into the myoplasm through voltage dependent calcium channels, The spontaneous or KC1-induced tension development in isolated uterine smooth musele is reduced by lowering the calium ion (Ca2+) concentration of the bathing medium. In our study, the effect of morphine, pethidine and pentazocine on estrous and pregnant uterine activity, and the effect of extracellular calcium on opiate induced uterine motility have been examined in rats in vitro The following results were obtained: 1) The frequency of contraction of the estrous and pregnant rat uteri in the control group decreased gradually with time. 2) Morphine caused a concentration- dependent decrease in the frequency of contraction of the estrous and pregnant rat uteri, but it was not significant 3) Pethidine and pentazocine caused a concentration dependent incrase in the frequency of contraction of the estrous and pregnant rat uteri.but it was not significant.4) Diazepam caused a concentration-dependent decrease in the frequency of contraction of the estrous and pregnant rat uteri. 5) Ketamine casued a concentration- dependent decrease in the frequency of contraction of the estrous and pregnant rat uteri, but it was not significant. 6) Addition of CaCI, to the Krebs Henseleit solution did not make any significant change in the result. 7) According to the condition of the estrous and pregnant rat uteri the change of contraction frequency was statistically significant in the control, morphine, pethidine and pentazocine groups.

Neurophysiologic - Histological Changes Following Injection of Morphine , Meperidine , Pentazocine on Sciatic Nerve of Dogs / 대한마취과학회지

The authors have already reported good local anesthetic effects of meperidine and pentazocine clinically in patients scheduled for various surgeries, followed by experimental evaluation of toxic effects of two drugs on the sciatic nerve of rats. Intraspinal (spinal, epidural) morphine as well as other narcotics administration has been widely used and well established for pain control. The action mechanism of intraspinal narcotics has been well defined, and meperidine and Pentazocine have been reported to be used as a sole agent for spinal anesthesia. We assurned that the action mechanism of subarachoid meperidine or pentazocine might be different to some extent from that of morphine. This investigation was primarily undertaken to examine the difference in action between meperidine and morphine and also to evaluate neurotoxic effects on sciatic nerve of dogs. Adult Korean dogs were chosen as exoerunebtak abunaks because it is easy to observe physiologic activity with responses and to avoid of manipulating trauma. The dogs were intubated and anesthetised with halothane and nitrous oxide. The sciatic nerve of the dogs was exposed and stimulated by a nerve stimulator to observe myoneural response and then injectied with 1% morphine 0.5 mg (Group 1), 5% meperidine 25 mg (Group 2) and 3% pentazocine 15 mg (Group 3). The dog was carefully observed in recovery room to see the myoneural activity After 1 week, 1 month or 2 months of careful observation, a specimen was taken under reanesthesia at 1 week, 1 month and 2 months after the careful obaervation, When the sciatic nerve was stimulated by a nerve stimulator, the normal muscle twitch was observed clearly in Group 1 with themorphine injection but was not observed in Group 2 with meperidine and Group 3 with pentazocine injection. Complete motor paralysis was noticed in Group 2 and 3 during the recovery period which lasted about 90 minutes, almost the same as the duration of drugs for spinal anesthesia, No complications were noticed in the 3 group during the periods of one week one month and two months. All specimens were examined and no abnormal findings were observed in the 3 groups. All specimens of the 3 groups were investigated under electrom microscopic examination and they revealed mild vacuolizations scattered in axon and ummyelinated nerves on the only some of the specimens and these were not significant. Severe nerve damage which was seen in the meperidine group of a preliminary experiment was not observed in this study. As a result of this investigation, we have not observed significant toxic effects microscopically or fuctioually.