DOCSLIB.ORG

(8) No. 1 March 2005 Alexandria Journal of Anaesthesia and Intensive Care 50

Total Page：16

File Type：pdf, Size：1020Kb

Download full-text PDF Read full-text
(8) No. 1 March 2005 Alexandria Journal of Anaesthesia and Intensive Care 50 Alexandria Journal of Anaesthesia and Intensive Care 49 Propacetamol Versus Placebo for Management of Acute Postoperative Pain After Elective Tonsillectomy in Children. Mahmoud A Nassef, MD*. Ashraf M Moustafa, MD**. Ashraf A Moussa, MD***. *Department of Anesthesia, Beni-Suef Faculty of Medicine, Cairo University **Department of Anesthesia, Menoufiya University ***Department of Anesthesia,Menoufiya Liver Institute, Menoufiya University ABSTRACT The analgesic efficacy and safety of propacetamol, an injectable prodrug of acetaminophen, was assessed versus placebo after elective tonsillectomy operation in children. Using a double-blind, randomized parallel group design, 70 children aged 6-12 years were included to evaluate the effect of a single iv infusion of 40 mg/kg propacetamol versus a single infusion of 100 ml normal saline ( placebo ) given at the recovery room. Analgesic efficacy was assessed on pain scores rated on a four-points verbal scale, a five-points visual scale ( faces ) and a four-points pain relief verbal scale; before administration ( T0 ) and 0.25, 0.5, 1, 2, 3, 4, 5 and 6 hours after the infusion. The global efficacy was rated on a five-point scale at the end of the study. Rescue medication was allowed freely and the time for re-medication as well as the occurrence of any side effects was recorded. Propacetamol was statistically superior to placebo on all assessment criteria. The global final efficacy evaluation demonstrated 12 patients in the propacetamol group with good and very good scores compared to only one patient in the placebo group. Rescue medication was used in 40% of patients in the propacetamol group versus 83% in the placebo group. No serious side effects were recorded in both groups and pain at the infusion arm was noticed in 4 patients with propacetamol and 2 patients in the placebo group (P> 0.05). We concluded that, although propacetamol 40 mg/kg infusion may provide greater pain relief than placebo in children after tonsillectomy operation without any significant adverse effects, it is better to be used as a complementary drug to other analgesics in the treatment of moderate to severe postoperative pain. Key words: propacetamol, postoperative pain, acetaminophen, tonsillectomy. Introduction The use of paracetamol in the post- operative period was limited because of the Tonsillectomy is a common procedure temporary contraindication to the oral route (especially in children) in ear-nose-throat and the irregular or slow bioavailability of the (ENT) surgery, causing considerable post- rectal route (5). operative pain. Analgesia with non-opioids is often insufficient while the use of opioids is Propacetamol, N-acetylparaminophenol di- associated with side effects such as nausea, ethyl amino acetic ester, is the first form of sedation and respiratory depression (1, 2). paracetamol that can be injected parentraly. It is a water–soluble prodrug which is rapidly Paracetamol is an effective analgesic in metabolized to acetaminophen ( paracetamol) children (3, 4), it lacks adverse bleeding effects and diethylglycine in a 1: 1 ratio by non- and remains the most commonly used non- specific plasma esterases ; as a result an narcotic analgesic drug. In recent studies, it intravenous administration of one gram has been claimed to be as efficacious as propacetamol yields only 0.5 gram of paracetamol ( 6,7 ). diclofenac in post- tonsillectomy pain relief but it is associated with a lower incidence of The present study was designed to adverse effects like bleeding, adverse renal evaluate the analgesic efficacy as well as the effects and acute bronchospasm. safety of propacetamol versus placebo after elective tonsillectomy operation in children. AJAIC-Vol. (8) No. 1 March 2005 Alexandria Journal of Anaesthesia and Intensive Care 50 METHODS = weak, 2 = moderate, 3 = good and 4 = very good). The occurrence of any side – effects Seventy children aged 6-12 years, ASA was recorded. class 1 and 2 scheduled for elective tonsille- Withdrawal of the children from the study ctomy were included in this study after for insufficient pain relief on evaluation of the obtaining an informed parental written consent. observer was allowed from the beginning of Children with a history of paracetamol allergy the study, but considered valid for the study were excluded. All patients were premedicated only if it occurred at least 30 minutes after the with midazolam 0.3 mg/kg orally one hour beginning of the treatment. The physician was before surgery. Anesthesia was induced with free to choose whether additional medication thiopentone sodium 5mg/kg IV and fentanyl 1.5 should be given and the time for re-medication μg/kg IV, endotracheal intubation was was recorded facilitated with the use of atracurium 0.5 mg/kg IV. Children were mechanically ventilated and For the primary analgesic efficacy data, the anesthesia was maintained with 50% N2O in following variables were derived or computed O2 plus isoflurane 1-2%. Bolus doses of to assess the analgesic efficacy of the study fentanyl and/or atracurium were injected drug: accordingly. At the end of surgery the 1. Pain Intensity Difference (PID): for both neuromuscular block was reversed with visual and verbal scores, PID was calculated neostigmine 0.025 mg/kg and atropine 0.015 as the difference between the base line pain mg/kg IV. ECG, end tidal CO2, pulse oximetery intensity and the pain intensity at each and blood pressure were monitored during evaluation time point. anesthesia. 2. Sum of Pain intensity Difference (SPID): In the recovery room, the children were calculated by adding the PID score over the rated on a five-point visual scale (8) (sequence 6 hours of the study. of faces – Figure 1) as well as a four-point 3. Total Pain Relief (TOTPAR): calculated as verbal scale (0 = none, 1 = mild, 2 = moderate the sum of PID and the pain relief score over and 3 = severe) by an observer who is blind for the 6 hours period. the treatment group. Children with a score of 3- To allow calculation of SPID and TOTPAR, 5 on the visual scale and/or 2-3 on the verbal missing data were replaced by the assessment scale were included in this study (i.e. moderate at the time of withdrawn when patient was to severe pain). Children included in the study withdrawn for insufficient analgesia and by the were randomly allocated into 2 main groups: previous assessment when the patient was Group I {propacetamol group}, received 40 asleep. mg/kg propacetamol (mixed in 100 ml of All data were represented as means ± normal saline) as an IV infusion; and Group II standard deviation, or number of patient {placebo group}, received an IV infusion of 100 Statistical analysis was performed with SPSS ml of normal saline. Infusion was done over 15 version 10.0 Program. For SPID, TOTPAR and minutes in both groups. global efficacy, the tow groups were compared Pain intensity was re-assessed by the using one- sided non- parametric Wilcoxon same observer at 0.25, 0.5, 1, 2, 3, 4, 5 and 6 sign rank tests. Parametric Data and difference hours after the infusion. At the same times, between both groups were analyzed with one- pain relief was measured using a 4 point- way analysis of variance (ANNOVA) and verbal rating scale (0 = complete pain relief, 1 Student’s t-test. The Chi-square test and = good, 2 = slight and 3 = none). At the end of Fisher’s exact test were applied to non- the 6 hours study period, a global rating of the parametric data when appropriate. P value of treatment efficacy was made by both a less than 0.05 was considered statistically physician observer as well as by a nurse significant. observer using the following scale (0 = none, 1 AJAIC-Vol. (8) No. 1 March 2005 Alexandria Journal of Anaesthesia and Intensive Care 51 Figure 1: Visual analogue Scale The final global efficacy evaluation (Sequence of Faces) (8) recorded 10 patients with good result and 2 patients with very good result in the propacetamol group compared to only one patient in the placebo group with good result (Figure 5). Fourteen patients in the propa- cetamol group were withdrawn from the study for insufficient analgesia, versus 29 5 4 3 2 1 patients in the placebo group. Also the mean time for re-medication was significantly RESULTS longer in the propacetamol group ( 163 ± 88 min Vs 116 ± 79 min ) [ p< 0.05] ( Table 3 ). There was no significant difference There were no serious adverse effects between the two groups as regards age, sex, recorded in both groups during the study weight, and duration of surgery as well as hours. Four patients in the propacetamol the amount of intraoperative fentanyl group complained a burning sensation at the requirements (Table 1). infusion arm and 3 patients experienced Pain scores (visual and verbal scales) were postoperative vomiting, while in the placebo almost similar in both groups before starting group burning sensation was recorded only the infusion and during the first 30 min after in 2 patients while 4 patients had post- the infusion, no significant difference was operative vomiting (P > 0.05). detected (P > 0.05). After 30min and till the end of the 6th hour, pain scores were DISCUSSION significantly lower in the propacetamol group than in the placebo group (Figure 2 – 3). A The recommended oral dose of similar significant difference was detected paracetamol for effective analgesia is 15-20 with the pain relief score (Figure 4). For mg/kg every 6 hours (9, 10). In the present derived variables: SPID was significantly study a dose of 40 mg/kg of propacetamol, higher in the propacetamol group than in the which is equivalent to an oral dose of placebo group ( 452.6 ± 68.5 Vs 295.3 ± 20mg/kg was used.
Load more

Recommended publications
  • Pharmaceutical Powder Compressibility – a Science-Based Approach
    Pharmaceutical powder compressibility – a science-based approach Inauguraldissertation zur Erlangung der Würde eines Doktors der Philosophie vorgelegt der Philosophisch-Naturwissenschaftlichen Fakultät der Universität Basel von Nicolaos D.Gentis aus Egrigoros (Chios) Griechenland Oberkulm (AG) Schweiz Basel, 2012 Approval Genehmigt von der Philosophisch-Naturwissenschaftlichen Fakultät auf Antrag von Prof. Dr. Matthias Hamburger und PD Dr. Gabriele Betz und Prof. Dr. Thierry F. Vandamme Basel, den 21. Februar 2012 Prof. Dr. Martin Spiess Dekan 2 Dedicated to my parents with love, appreciation and respect 3 Σωκράτης ―I know one thing, that I know nothing‖ Socrates c. 469 BC – 399 BC 4 Acknowledgements The work for this PhD thesis was carried out in the Industrial Pharmacy Lab, Department of Pharmaceutical Sciences, University of Basel and at the facility of Natoli Engineering Inc. in Saint Louis, Missouri (USA). I would like to express my appreciation and sincere gratefulness to PD Dr. Gabriele Betz for giving me the opportunity to do a PhD under her excellent supervision with essential, continuous support, guidance and brilliant, positive motivation. I would like to thank Prof. Dr. Matthias Hamburger for accepting to be my Faculty Responsible and for the support. My appreciation goes also to Prof. Dr. Thierry F. Vandamme for accepting to assume the co-referencing of this PhD thesis. At this point I would like to thank all former Industrial Pharmacy Research Group members for the unique support and for the great, crazy working atmosphere in the laboratory. Especially I would like to thank Mr. Branko Z. Vranic for his great collaboration and support in the research work of project 2 in this thesis.
    [Show full text]
  • A Comparative Efficacy of Propacetamol and Ketorolac in Postoperative Patient Controlled Analgesia
    Korean J Pain 2015 July; Vol. 28, No. 3: 203-209 pISSN 2005-9159 eISSN 2093-0569 http://dx.doi.org/10.3344/kjp.2015.28.3.203 | Original Article | A Comparative Efficacy of Propacetamol and Ketorolac in Postoperative Patient Controlled Analgesia Department of Anesthesiology and Pain Medicine, Chonnam National University Medical School, Gwangju, Korea Bong Ha Heo, Ji Hun Park, Jung Il Choi, Woong Mo Kim, Hyoung Gon Lee, Soo Young Cho, and Myoung Ha Yoon Background: Ketorolac has been used as a postoperative analgesia in combination with opioids. However, the use of ketorolac may produce serious side effects in vulnerable patients. Propacetamol is known to induce fewer side effects than ketorolac because it mainly affects the central nervous system. We compared the analgesic effects and patient satisfaction levels of each drug when combined with fentanyl patient-controlled analgesia (PCA). Methods: The patients were divided into two groups, each with n = 46. The patients in each group were given 60 mg of ketorolac or 2 g of propacetamol (mixed with fentanyl) for 10 minutes. The patients were then given 180 mg of ketorolac or 8 g of propacetamol (mixed with fentanyl and ramosetron) through PCA. We assessed the visual analogue pain scale (VAS) at the time point immediately before administration (baseline) and at 15, 30, and 60 minutes, and 24 hours after administration. Also, the side effects of each regimen and each patient’s degree of satisfaction were assessed. Results: There was a significant decline in the VAS score in both groups (P ＜ 0.05). However, there were no significant differences in the VAS scores between the groups at each time point.
    [Show full text]
  • Paracetamol Kabi Data Sheet
    NEW ZEALAND DATA SHEET 1 Paracetamol Kabi Solution for Infusion 10mg/mL 2 QUALITATIVE AND QUANTITATIVE COMPOSITION Paracetamol Kabi solution for infusion contains 10 mg/mL of paracetamol (50 mL vial/bag contains 500 mg of paracetamol, 100 mL vial/bag contains 1 g of paracetamol). Paracetamol Kabi solution for infusion contains the excipients mannitol, cysteine hydrochloride, nitrogen (as protective gas), water for injections. 3 PHARMACEUTICAL FORM Paracetamol solution for infusion 10 mg/mL is a clear to slightly yellowish solution. Paracetamol is a white crystalline solid or powder chemically described as 4 – acetamidophenol. It is soluble in water (1 in 70), soluble in alcohol (1 in 7), acetone (1 in 13), glycerol (1 in 40), propylene glycol (1 in 9) and also soluble in solutions of the alkali hydroxides. 4 CLINICAL PARTICULARS 4.1 Therapeutic indications Paracetamol 10 mg/mL solution for infusion is indicated for the relief of mild to moderate pain and the reduction of fever where an intravenous route of administration is considered clinically necessary. 4.2 Dose and method of administration The prescribed dose must be based on the patient’s weight. Unintentional overdose can lead to serious liver damage and death (see section 4.9 OVERDOSE). Healthcare providers are reminded that it is essential to follow both the weight-related dose recommendations and to consider individual patient risk factors for hepatotoxicity including hepatocellular insufficiency, chronic alcoholism, chronic malnutrition (low reserves of hepatic glutathione), and dehydration (see section 4.2 DOSE AND METHOD OF ADMINISTRATION – Hepatic Impairment). It is recommended that suitable oral analgesic treatment be substituted for Paracetamol solution for infusion as soon as the patient can be treated by the oral route (see section 4.3 CONTRAINDICATIONS).
    [Show full text]
  • Treatment for Acute Pain: an Evidence Map Technical Brief Number 33
    Technical Brief Number 33 R Treatment for Acute Pain: An Evidence Map Technical Brief Number 33 Treatment for Acute Pain: An Evidence Map Prepared for: Agency for Healthcare Research and Quality U.S. Department of Health and Human Services 5600 Fishers Lane Rockville, MD 20857 www.ahrq.gov Contract No. 290-2015-0000-81 Prepared by: Minnesota Evidence-based Practice Center Minneapolis, MN Investigators: Michelle Brasure, Ph.D., M.S.P.H., M.L.I.S. Victoria A. Nelson, M.Sc. Shellina Scheiner, PharmD, B.C.G.P. Mary L. Forte, Ph.D., D.C. Mary Butler, Ph.D., M.B.A. Sanket Nagarkar, D.D.S., M.P.H. Jayati Saha, Ph.D. Timothy J. Wilt, M.D., M.P.H. AHRQ Publication No. 19(20)-EHC022-EF October 2019 Key Messages Purpose of review The purpose of this evidence map is to provide a high-level overview of the current guidelines and systematic reviews on pharmacologic and nonpharmacologic treatments for acute pain. We map the evidence for several acute pain conditions including postoperative pain, dental pain, neck pain, back pain, renal colic, acute migraine, and sickle cell crisis. Improved understanding of the interventions studied for each of these acute pain conditions will provide insight on which topics are ready for comprehensive comparative effectiveness review. Key messages • Few systematic reviews provide a comprehensive rigorous assessment of all potential interventions, including nondrug interventions, to treat pain attributable to each acute pain condition. Acute pain conditions that may need a comprehensive systematic review or overview of systematic reviews include postoperative postdischarge pain, acute back pain, acute neck pain, renal colic, and acute migraine.
    [Show full text]
  • 022450Orig1s000
    CENTER FOR DRUG EVALUATION AND RESEARCH APPLICATION NUMBER: 022450Orig1s000 PHARMACOLOGY REVIEW(S) 5 Page(s) of Draft Labeling have been Withheld in Full as b4 (CCI/TS) immediately following this page (b) (4) (b) (4) (b) (4) (b) (4) COPYRIGHT MATERIAL (b) (4) (b) (4) COPYRIGHT MATERIAL (b) (4) (b) (4) COPYRIGHT MATERIAL (b) (4) (b) (4) (b) (4) COPYRIGHT MATERIAL COPYRIGHT MATERIAL COPYRIGHT MATERIAL (b) (4) (b) (4) (b) (4) (b) (4) (b) (4) (b) (4) (b) (4) (b) (4) (b) (4) (b) (4) (b) (4) (b) (4) (b) (4) (b) (4) (b) (4) (b) (4) (b) (4) COPYRIGHT MATERIAL COPYRIGHT MATERIAL COPYRIGHT MATERIAL COPYRIGHT MATERIAL COPYRIGHT MATERIAL COPYRIGHT MATERIAL COPYRIGHT MATERIAL COPYRIGHT MATERIAL (b) (4) (b) (4) (b) (4) (b) (4) COPYRIGHT MATERIAL COPYRIGHT MATERIAL (b) (4) (b) (4) (b) (4) (b) (4) Pharmacology Toxicology Review Addendum Executive Summary I. Recommendations A. Recommendation on approvability From the nonclinical pharmacology perspective, NDA 22-450 is recommended for approval. B. Recommendation for nonclinical studies At this time, there are no nonclinical studies needed that will impact approvability. C. Recommendation on labeling The table below contains the draft labeling submitted by the sponsor, the proposed changes and the rationale for the proposed changes for the nonclinical toxicology section only. Please see the secondary review for final labeling recommendations. (b) (4) 1 Reviewer: Carlic K. Huynh, Ph.D. NDA No. 22-450 (b) (4) II. Summary of nonclinical findings A. Brief overview of nonclinical findings From the previous pharmacology toxicology review of this NDA, acetaminophen is not a mutagen (as demonstrated by negative results in the bacterial Ames test) but is a clastogen (as demonstrated by positive results in the chromosomal aberration assay in cultured human peripheral blood lymphocytes).
    [Show full text]
  • Old Drug, New Route: a Systematic Review of Intravenous Acetaminophen After Adult Cardiac Surgery
    REVIEW ARTICLE Paul G. Barash, MD Giovanni Landoni, MD Section Editors Old Drug, New Route: A Systematic Review of Intravenous Acetaminophen After Adult Cardiac Surgery Daniel J. Douzjian, MD, and Alexander Kulik, MD, MPH HE MANAGEMENT OF postoperative pain after cardiac first discovered in 1877, but it was not until 1950 that it was Tsurgery remains clinically challenging. Well-controlled marketed for clinical use as a pain reliever.18 While it is less pain is critical to maintaining the physical and psychologic potent in its analgesic properties, unlike opiates, acetaminophen well-being of each patient and can help facilitate timely has no respiratory depressant action and does not cause nausea extubation, comfortable breathing, and early postoperative ambu- or vomiting.18,19 It has a minimal hemodynamic effect, and the lation. On the other hand, left poorly managed, postoperative pain only contraindications to its use are severe hepatic impairment, can lead to rising catecholamine levels, ultimately triggering allergy, or hypersensitivity. Given its safety profile, it has myocardial ischemia, stroke, or bleeding complications.1-3 Insuf- become a common household drug and has been available in ficient pain control also can limit patient mobility, increasing the oral form without prescription since 1959.18 To date, the risk of deep vein thrombosis and pneumonia, in addition to the mechanism of action of acetaminophen is not understood harmful psychologic consequences of insomnia and demoraliza- completely, although it is believed to involve
    [Show full text]
  • ASDERA – Overview
    ASDERA – Overview Develop novel drugs for high unmet needs Mission by utilizing a computational biostatistics platform (US 7,664,616), the first to identify genetic risk factors for complex diseases 1800 Gauss-Legendre 1948 Hoeffding Drug 1900 1965 1985 2001 Discovery Ohdner IBM PC GPU Platform 9 Byte 256 kB 16 MB 4 GB ANOVA PCA Bayes u-Stat Validation: Confirmation of known drug targets in epilepsy Proof-of-Concept: L-fucose in Crohn’s disease (in phase 3) Time-Pipeline Current lead: lead: ASD-002 Mefenamic against acid against mutism mutism in autism in autism (phase(phase 3 ready) 3 ready) Next drug: Preventing metastases in breast cancer (pat. pending) Outlook: Delaying Alzheimer ’s and Parkinson ’s (pat. pending) © ASDERA (2017) Confidential Information 1 ASDERA – Overview Develop the first drug to prevent lack-of-language in autism ( unmet need ) Focus by utilizing a computational biostatistics platform (US 7,664,616), the first platform to identify genetic risk factors for complex diseases Disruption of Active Language Development (DALD) Lead Indication: in toddlers developing Autism Spectrum Disorders (ASD) by childhood migraines causing them to Mutism • become non-verbal (primary outcome) and in Autism • develop life-long intellectual disability (ID) Children will still develop autism, but will be verbal (“Asperger’s”). Product ASD-002: Market-exclusive ester-prodrug of mefenamic acid (MFA) Patent filed in US and EU. Orphan Drug Designation for MFA pending Status Preparing CMC / manufacturing for a short 505(b)(2) regulatory
    [Show full text]
  • WO 2013/020527 Al 14 February 2013 (14.02.2013) P O P C T
    (12) INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (10) International Publication Number (43) International Publication Date WO 2013/020527 Al 14 February 2013 (14.02.2013) P O P C T (51) International Patent Classification: (74) Common Representative: UNIVERSITY OF VETER¬ A61K 9/06 (2006.01) A61K 47/32 (2006.01) INARY AND PHARMACEUTICAL SCIENCES A61K 9/14 (2006.01) A61K 47/38 (2006.01) BRNO FACULTY OF PHARMACY; University of A61K 47/10 (2006.01) A61K 9/00 (2006.01) Veterinary and Pharmaceutical Sciences Brno Faculty Of A61K 47/18 (2006.01) Pharmacy, Palackeho 1/3, CZ-61242 Brno (CZ). (21) International Application Number: (81) Designated States (unless otherwise indicated, for every PCT/CZ20 12/000073 kind of national protection available): AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, (22) Date: International Filing BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DK, DM, 2 August 2012 (02.08.2012) DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, (25) Filing Language: English HN, HR, HU, ID, IL, IN, IS, JP, KE, KG, KM, KN, KP, KR, KZ, LA, LC, LK, LR, LS, LT, LU, LY, MA, MD, (26) Publication Language: English ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, (30) Priority Data: NO, NZ, OM, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, 201 1-495 11 August 201 1 ( 11.08.201 1) SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, 2012- 72 1 February 2012 (01.02.2012) TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, 2012-5 11 26 July 2012 (26.07.2012) ZW.
    [Show full text]
  • Propacetamol-Induced Injection Pain Is Associated with Activation of Transient Receptor Potential Vanilloid 1 Channels S
    Supplemental material to this article can be found at: http://jpet.aspetjournals.org/content/suppl/2016/07/25/jpet.116.233452.DC1 1521-0103/359/1/18–25$25.00 http://dx.doi.org/10.1124/jpet.116.233452 THE JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS J Pharmacol Exp Ther 359:18–25, October 2016 Copyright ª 2016 by The American Society for Pharmacology and Experimental Therapeutics Propacetamol-Induced Injection Pain Is Associated with Activation of Transient Receptor Potential Vanilloid 1 Channels s Florian Schillers, Esther Eberhardt, Andreas Leffler, and Mirjam Eberhardt Department of Anaesthesiology and Intensive Care Medicine, Hannover Medical School, Hannover, Germany (F.S., A.L., M.E.); and Department of Anaesthesiology, Friedrich-Alexander University Erlangen-Nuremberg, Erlangen, Germany (E.E.) Received March 8, 2016; accepted July 22, 2016 ABSTRACT Downloaded from Propacetamol (PPCM) is a prodrug of paracetamol (PCM), were expressed in human embryonic kidney 293 cells and which was generated to increase water solubility of PCM for investigated by means of whole-cell patch clamp and ratio- intravenous delivery. PPCM is rapidly hydrolyzed by plasma metric calcium imaging. PPCM (but not PCM) activated esterases to PCM and diethylglycine and shares some struc- TRPV1, sensitized heat-induced currents, and caused an tural and metabolic properties with lidocaine. Although PPCM increase in intracellular calcium. In TRPA1-expressing cells is considered to be comparable to PCM regarding its analgesic however, both PPCM and PCM evoked calcium responses but properties, injection pain is a common side effect described for failed to induce inward currents. Intracutaneous injection of jpet.aspetjournals.org PPCM but not PCM.
    [Show full text]
  • The Antipyretic Efficacy and Safety of Propacetamol Compared With
    Choi et al. BMC Pediatrics (2018) 18:201 https://doi.org/10.1186/s12887-018-1166-z RESEARCHARTICLE Open Access The antipyretic efficacy and safety of propacetamol compared with dexibuprofen in febrile children: a multicenter, randomized, double-blind, comparative, phase 3 clinical trial Seung Jun Choi1,2, Sena Moon3, Ui Yoon Choi3, Yoon Hong Chun3, Jung Hyun Lee3, Jung Woo Rhim3, Jin Lee4, Hwang Min Kim5 and Dae Chul Jeong3,6* Abstract Background: We aimed to compare the antipyretic efficacy, safety, and tolerability between oral dexibuprofen and intravenous propacetamol in children with upper respiratory tract infection (URTI) presenting with fever. Methods: Patients aging from 6 months to 14 years admitted for URTI with axillary body temperature ≥ 38.0 °C were enrolled and randomized into the study or control group. Patients in the study group were intravenously infused with propacetamol and subsequently oral placebo medication was administered. Patients in the control group were intravenously infused with 100 mL of 0.9% sodium chloride solution without propacetamol and then oral dexibuprofen was administered. We checked the body temperature of all patients at 0.5 h (hr), 1 h, 1.5 h, 2 h, 3 h, 4 h, and 6 h after oral placebo or dexibuprofen had been applied. Results: A total of 263 patients (125 in the study group) were finally enrolled. The body temperatures of patients in the study group were significantly lower until 2 h after administration (37.73 ± 0.58 vs 38.36 ± 0.69 °C (p < 0.001), 37. 37 ± 0.53 vs 37.88 ± 0.69 °C (p < 0.001), 37.27 ± 0.60 vs 37.62 ± 0.66 °C (p < 0.001), 37.25 ± 0.62 vs 37.40 ± 0.60 °C (p = 0.0452), at 0.5 h, 1 h, 1.5 h, and 2 h, respectively).
    [Show full text]
  • Australian Product Information- Paracetamol Kabi (Paracetamol)
    AUSTRALIAN PRODUCT INFORMATION- PARACETAMOL KABI (PARACETAMOL) 1. NAME OF MEDICINE Paracetamol 2. QUALITATIVE AND QUANTATIVE COMPOSITION Paracetamol Kabi solution for infusion contains 10 mg/mL of paracetamol (50 mL vial/ bag contains 500 mg of paracetamol, 100 mL vial/bag contains 1 g of paracetamol). Paracetamol Kabi solution for infusion contains the excipients mannitol, cysteine hydrochloride, nitrogen (as protective gas), water for injections. For the full list of excipients, see Section 6.1 List of excipients. 3. PHARMACEUTICAL FORM Paracetamol solution for infusion 10 mg/mL is a clear to slightly yellowish solution. Paracetamol is a white crystalline solid or powder chemically described as 4 – acetamidophenol. It is soluble in water (1 in 70), soluble in alcohol (1 in 7), acetone (1 in 13), glycerol (1 in 40), propylene glycol (1 in 9) and also soluble in solutions of the alkali hydroxides. 4. CLINICAL PARTICULARS 4.1 Therapeutic Indications Paracetamol 10 mg/mL solution for infusion is indicated for the relief of mild to moderate pain and the reduction of fever where an intravenous route of administration is considered clinically necessary. 4.2 Dose and Method of Administration The prescribed dose must be based on the patient’s weight. Unintentional overdose can lead to serious liver damage and death (see section 4.9 Overdose). Healthcare providers are reminded that it is essential to follow both the weight-related dose recommendations and to consider individual patient risk factors for hepatotoxicity including hepatocellular insufficiency, chronic alcoholism, chronic malnutrition (low reserves of hepatic glutathione), and dehydration (see section 4.2 Dose method and Administration – Hepatic Impairment).
    [Show full text]
  • List of Basic Essential Medicines Ministry of Health Seychelles 2010
    LIST OF BASIC ESSENTIAL MEDICINES MINISTRY OF HEALTH SEYCHELLES 2010 Drugs that should never be out of stock Should have minimum of 90-day stock Shortage could create major reactions ANAESTHETICS General Anaesthetics HALOTHANE, 250 ML BOTTLE ISOFLURANE 100ML ETOMIDATE INJECTION 2MG /1ML, 10ML AMPOULE KETAMINE 10MG ML 20ML NITROUS OXIDE OXYGEN, COMPRESSED AIR PROPOFOL INJECTION 1% 10MG/ML THIOPENTONE SODIUM INJECTION, 500MG/VIAL Local Anaesthetics BUPIVACAINE INJECTION 0.5%, 10ML AMPOULE BUPIVACAINE HEAVY INJECTION 5MG & 80MG/ML GLUCOSE, 4ML AMPOULE) LIGNOCAINE HCL INJECTION 2%, 30ML BOTTLE LIGNOCAINE 2% + ADRENALINE 1:200000 20ML LIGNOCAINE 2% + ADRENAINE 1: 80000 1.8ML DENTAL CARTRIDGES LIGNOCAINE METERED HCL SPRAY 10MG /DOSE, 800 DOSES UNIT ETHYL CHLORIDE SPRAY PRILOCAINE 4% DENTAL CARTRIDGE Preoperative Medication and Sedation for short-term Procedures ATROPINE INJECTION 1MG/ML, 1ML AMPOULE FENTANYL INJECTION 50 MCG/ML, 2ML AMPOULE MIDAZOLAM INJECTION 5MG/ML, 3ML AMPOULE MORPHINE SULPHATE INJECTION 10MG/ML, 10ML AMPOULE ANALGESICS, ANTIPYRETICS Non-opioids ASPIRIN TABLET 300MG DICLOFENAC SODIUM TABLET 100MG SR DICLOFENAC SODIUM INECTION 25MG/ML 3ML AMPOULES IBUPROFEN TABLET 400MG INDOMETHACIN CAPSULE 25MG PARACETAMOL TABLET 500MG PARACETAMOL ELIXIR 120MG/5ML, 100ML BOTTLE PARACETAMOL SUPPOSITORIES 125MG ; 250MG ; 1G (C) PROPACETAMOL INJECTION 500MG & 1G/VIAL Page 1 Opioids CODEINE PHOSPHATE TABLET 30MG CODEINE PHOSPHATE SYRUP FENTANYL INJECTION 50MCG /ML, 2ML AMPOULE MORPHINE ORAL SOLUTION 2MG/ML (300ML BOTTLE) MORPHINE SULPHATE
    [Show full text]