-
International Journal of Pharmaceutics Jun 2021Lipid nanocapsules (LNC) are special drug delivery system (DDS) carriers obtained by the phase-inversion temperature method (PIT). This study describes the encapsulation...
Lipid nanocapsules (LNC) are special drug delivery system (DDS) carriers obtained by the phase-inversion temperature method (PIT). This study describes the encapsulation of the local anesthetics (LA) prilocaine (PLC) and lidocaine (LDC) in lipid nanocapsules (LNC) optimized by 2 factorial design, characterized through DLS, NTA, CRYO-EM and release kinetics and incorporated in carbopol gel (Gel) prior to in vivo anesthetic effect (in mice) evaluation. A very homogeneous population of small (50 nm; polydispersity index = 0.05) spherical nanocapsules with negative zeta potentials (-21 mV) and ca. 2.3 × 10 particles/mL was obtained. The encapsulation efficiency was high (81% and 89% for prilocaine and lidocaine, respectively). The release rate profile was free PLC = free LDC > LNC > Gel. The hybrid system increased (4x) the anesthesia time in comparison to an equipotent gel formulation prepared without LNC. No tissue damage was detected on the tail skin of mice that received the formulations. This study shows that lipid nanocapsules are suitable carriers for PLC and LDC, promoting longer and safer topical anesthesia. Gel is mucoadhesive and suitable for application in the mouth, where it could be used as a pre-anesthetic, to reduce pain of needle stick (infiltrative anesthesia).
Topics: Anesthetics, Local; Animals; Lidocaine; Lipids; Mice; Nanocapsules; Prilocaine
PubMed: 33961954
DOI: 10.1016/j.ijpharm.2021.120675 -
Journal of Dental Anesthesia and Pain... Apr 2020Dental local anesthesia is performed daily on a global scale. Adverse effects are rare, but the topic of neurotoxicity of local anesthetics deserves to be explored, as... (Review)
Review
Dental local anesthesia is performed daily on a global scale. Adverse effects are rare, but the topic of neurotoxicity of local anesthetics deserves to be explored, as publications can be controversial and confusing. Therefore, a need was felt to address and question the evidence for potential neurotoxicity of dental local anesthetics. This review aimed to assess the studies published on the neurotoxicity of dental local anesthetics. A Pubmed® search was conducted between January 2019 and August 2019. This revealed 2802 hits on the topic of neurotoxicity or cytotoxicity of the following anesthetics: lidocaine, prilocaine, mepivacaine, articaine, ropivacaine, and bupivacaine. Only 23 papers were deemed eligible for this review: 17 studies, 3 reviews and 3 audits of national inquiries. The heterogeneous literature on this topic showed that all dental local anesthetics are potentially neurotoxic in a concentration and/or exposure time fashion. There seems no consensus about what cell lines are to be used to investigate the neurotoxicity of local anesthetics, which makes the comparison between studies difficult and ambiguous. However, the bottom line is that all dental local anesthetics have a neurotoxic potential, but that there is no unanimity in the publications about which local anesthetic is the least or the most neurotoxic.
PubMed: 32395611
DOI: 10.17245/jdapm.2020.20.2.63 -
Swiss Dental Journal Sep 2022When choosing local anesthetics, risk factors such as underlying diseases, use of other medications and allergies have to be taken into consideration. Systematic...
When choosing local anesthetics, risk factors such as underlying diseases, use of other medications and allergies have to be taken into consideration. Systematic complications might occur if a specific limit in the plasma concentration is exceeded. Articaine and prilocaine are metabolized extrahepatically. In case of an absolute contraindication for vasoconstrictors, the use of mepivacaine, bupivacaine or articaine is recommended.
Topics: Aged; Anesthetics, Local; Bupivacaine; Carticaine; Humans; Mepivacaine; Prilocaine
PubMed: 36052970
DOI: 10.61872/sdj-2022-09-03 -
BMC Pediatrics Jun 2023To characterize clinical profile of pediatric local anesthetic (LA) systemic toxicity (LAST) and to identify determinants of life-threatening outcomes.
PURPOSE
To characterize clinical profile of pediatric local anesthetic (LA) systemic toxicity (LAST) and to identify determinants of life-threatening outcomes.
METHODS
Spontaneous reports notified to the French Pharmacovigilance Network were retrieved and followed by a case-by-case review, according to the following criteria: LA as suspected drug, age < 18 years, adverse drug reactions related to nervous system, cardiac, respiratory, psychiatric or general disorders. Multivariate logistic regression analysis was performed to identify factors leading to life-threatening reaction (i.e. continuous seizures or cardiorespiratory arrest).
RESULTS
Among 512 cases retrieved, 64 LAST cases were included (neonates 11%, infants 30%, children 36%, adolescents 23%) mainly involving lidocaine (47%), lidocaine + prilocaine (22%) and ropivacaine (14%). Toxicity profiles were neurological (58%), cardiac (11%) or mixed (20%) and 7 patients (11%) developed methemoglobinemia. LAST was life-threatening for 23 patients (36%) and 2 patients died. Doses were above recommendations in 26 patients (41%) and were not different between life-threatening and non-life-threatening cases. The context of use (general and orthopedic surgery, p = 0.006) and the type of LA agent (lidocaine, p = 0.016) were independently associated with a life-threatening outcome.
CONCLUSION
In this national retrospective analysis, LAST in children appear to be a rare event. Neurological and cardiac signs were the most frequently reported reactions. LAST in children can be life-threatening, even at therapeutic doses. Although a fatal outcome may anecdotally occur, the vast majority of patients recovered after appropriate medical care.
Topics: Infant; Infant, Newborn; Adolescent; Humans; Child; Anesthetics, Local; Pharmacovigilance; Retrospective Studies; Lidocaine; Ropivacaine; Lidocaine, Prilocaine Drug Combination
PubMed: 37355586
DOI: 10.1186/s12887-023-04126-7 -
Current Pharmaceutical Design May 2023Local anesthetic (LA) compounds decrease the permeability of the ion channels to sodium, which in turn, diminishes the rate of depolarization. These agents (a.k.a....
Local anesthetic (LA) compounds decrease the permeability of the ion channels to sodium, which in turn, diminishes the rate of depolarization. These agents (a.k.a. -caines) are also used to depress mucosal sensations, e.g., gag reflex in the form of topical anesthetics. Overdose of LA can lead to local anesthetic systemic toxicity (LAST), which is the precursor of potentially lethal consequences on clinical grounds. There is a wide array of possible presentations of LAST, from mild findings, such as temporary hypertensive events, to serious conditions, including refractory cardiac dysfunction, dysrhythmias and prearrest situations. Lidocaine, prilocaine, mepivacaine, ropivacaine, and bupivacaine are among the most commonly used members of the family. The agents' dosages should be adjusted in children, elderly and fragile individuals and those with organ failures, as the metabolism of the compounds will be impaired. The ideal body weight, along with hepatic and renal functional reserves, will have an impact on elimination kinetics. Systemic absorption is an untoward consequence of LA administration which deserves every means of prevention. Intravenous lipid emulsion is an important life-saving treatment in severe, life-threatening cases. This narrative review article is designed to cover the clinical uses of LA in children, recognition, and management of untoward effects of the agents, with special emphasis on the LAST.
PubMed: 37231720
DOI: 10.2174/1381612829666230525122040 -
Journal of Anesthesia History Jul 2019Intravenous regional anesthesia (IVRA) is an established, safe and simple technique, being applicable for various surgeries on the upper and lower limbs. In 1908, IVRA... (Review)
Review
Intravenous regional anesthesia (IVRA) is an established, safe and simple technique, being applicable for various surgeries on the upper and lower limbs. In 1908, IVRA was first described by the Berlin surgeon August Bier, hence the name "Bier's Block". Although his technique was effective, it was cumbersome and fell into disuse when neuroaxial and percutaneous plexus blockades gained widespread popularity in the early 20 century. In the 1960s, it became widespread, when the New Zealand anesthesiologist Charles McKinnon Holmes praised its use by means of new available local anesthetics. Today, IVRA is still popular in many countries being used in the emergency room, for outpatients and for high-risk patients with contraindications for general anesthesia. IVRA offers a favorable risk-benefit ratio, cost-effectiveness, sufficient muscle relaxation and a fast on- and offset. New upcoming methods for monitoring, specialized personnel and improved emergency equipment made IVRA even safer. Moreover, IVRA may be applied to treat complex regional pain syndromes. Prilocaine and lidocaine are considered as first-choice local anesthetics for IVRA. Also, various adjuvant drugs have been tested to augment the effect of IVRA, and to reduce post-deflation tourniquet pain. Since major adverse events are rare in IVRA, it is regarded as a very safe technique. Nevertheless, systemic neuro- and cardiotoxic side effects may be linked to an uncontrolled systemic flush-in of local anesthetics and must be avoided. This review gives a historical overview of more than 100 years of experience with IVRA and provides a current view of IVRA with relevant key facts for the daily clinical routine.
Topics: Anesthesia, Conduction; Anesthesia, Intravenous; Anesthetics, Local; Cocaine; Contraindications, Procedure; History, 19th Century; History, 20th Century; History, 21st Century; Humans
PubMed: 31570204
DOI: 10.1016/j.janh.2018.10.007 -
BMC Veterinary Research May 2022In dogs undergoing routine elective orthopaedic surgeries carried out as same-day surgeries regional anaesthetic techniques (RATs) should aim to produce analgesia but...
BACKGROUND
In dogs undergoing routine elective orthopaedic surgeries carried out as same-day surgeries regional anaesthetic techniques (RATs) should aim to produce analgesia but minimising the postoperative motor dysfunction. Our objective was to compare the perioperative analgesic effects and the time to motor recovery between spinal anaesthesia (SA) with hyperbaric solution of prilocaine 2% (mg = 4 x [0.3 × BW (kg) + 0.05 × SCL (cm)]) and morphine (0.03 mg/kg) and combined ultrasound (US) and electro stimulator-guided psoas compartment and ischiatic nerve block (PB) with ropivacaine 0.375% (0.45 mL/kg). Dogs undergoing tibial plateau levelling osteotomy (TPLO) were randomly assigned to receive either SA or PB. Procedural failure, perioperative rescue analgesia, motor block recovery and complications were recorded.
RESULTS
Procedural failure rate (PFR) was 19% (7 out of 36) for SA and 9% (3 out of 32) for PB (p = 0.31). Intraoperative rescue analgesia was administered to 6/29 (21%) SA group dogs and in 15/29 (52%) PB group dogs, respectively (p = 0.03). At 3 h after RAT, percentage of dogs with complete block recovery was 25/29 (86%) and 25/29 (86%) in group SA and PB, respectively (p = 1). Two cases of pruritus and one case of urinary retention were recorded in the SA group. Residual ischiatic nerve block was noted at 12 h after RAT in 2/15 (13%) of dogs in group PB; it completely resolved 24 h after RAT.
CONCLUSIONS
SA with prilocaine 2% and PB with ropivacaine 0.37% were found suitable for dogs undergoing same-day TPLO surgery. Pruritus and urinary retention in SA and residual block in both groups might occasionally delay the time of discharge.
Topics: Anesthesia, Spinal; Anesthetics, Local; Animals; Dog Diseases; Dogs; Female; Male; Osteotomy; Pain, Postoperative; Prilocaine; Pruritus; Ropivacaine; Urinary Retention
PubMed: 35549713
DOI: 10.1186/s12917-022-03277-6 -
Journal of Cutaneous Pathology Oct 2021Case series have described disruptive histopathologic changes following lidocaine/prilocaine cream anesthetic for biopsies. (Randomized Controlled Trial)
Randomized Controlled Trial
BACKGROUND
Case series have described disruptive histopathologic changes following lidocaine/prilocaine cream anesthetic for biopsies.
METHODS
A study of histopathologic changes was performed following a randomized trial comparing topical lidocaine/prilocaine cream to 1% lidocaine injection anesthesia for vulvar biopsy. Histopathology was reviewed by two independent dermatopathologists blinded to the type of anesthetic. Specimens were scored on six histopathologic criteria described in the literature. Individual scores for each histopathologic feature and the total score across features were compared between the two groups using marginal models with generalized estimating equations.
RESULTS
Of 37 specimens reviewed, 19 were randomized to lidocaine/prilocaine cream and 18 to 1% lidocaine. Subjects exposed to lidocaine/prilocaine had the following odds of histopathologic changes, relative to lidocaine-exposed subjects: acantholysis (odds ratio 2.48; 95% confidence intervals [CI] 0.51, 12.06), clefting (2.42; 0.64, 9.14), pallor/necrosis (1.13; 0.28, 4.50), spongiosis (0.71; 0.18, 2.85), and papillary dermal edema (1.17; 0.41, 3.29). Total scores were not significantly different between treatment arms (risk ratio 0.98; 0.71, 1.35).
CONCLUSION
This histopathologic analysis of a randomized trial between lidocaine/prilocaine cream and injected lidocaine as anesthesia for vulvar biopsy shows the absence of significant disruptive histopathologic features secondary to the type of anesthetic. Additional studies in different clinical contexts are warranted.
Topics: Administration, Topical; Adult; Aged; Aged, 80 and over; Anesthetics, Local; Biopsy; Female; Humans; Lidocaine, Prilocaine Drug Combination; Middle Aged; Vulva; Vulvar Diseases
PubMed: 33846983
DOI: 10.1111/cup.14018 -
European Journal of Clinical... Jun 2022Catheter-related bladder discomfort (CRBD) is a common complication of intraoperative urinary catheterization. Various studies have evaluated the efficacy of different... (Meta-Analysis)
Meta-Analysis Review
OBJECTIVE
Catheter-related bladder discomfort (CRBD) is a common complication of intraoperative urinary catheterization. Various studies have evaluated the efficacy of different interventions in postoperative CRBD. The present review was performed to assess the efficacy of these interventions.
METHODS
PubMed, Embase, and CENTRAL (Cochrane Central Register of Controlled Trials) databases were systematically searched to identify randomized controlled trials (RCTs) investigating the efficacy of different drugs for the prevention of postoperative CRBD. This review evaluated the incidence and severity of CRBD after different interventions at 0, 1, 2, and 6 h postoperatively.
RESULTS
Forty-five studies including 31 different drugs were analyzed. Eleven drugs were investigated in more than two RCTs, of which dexmedetomidine, gabapentin, tolterodine, tramadol, ketamine, nefopam, oxybutynin, pregabalin, and pudendal nerve block (PNB) generally showed significantly higher efficacy than controls postoperatively. Solifenacin only showed significant efficacy compared with the control at 0 h, and intravenous lidocaine only showed significant efficacy compared with the control at 6 h. There were insufficient trials to draw conclusions regarding atropine, butylscopolamine, chlorpheniramine, clonidine, darifenacin, diphenhydramine, glycopyrrolate, intravesical bupivacaine, ketamine-haloperidol, pethidine-haloperidol, ketorolac, lidocaine-prilocaine cream, magnesium, hyoscine n-butyl bromide, oxycodone, paracetamol, parecoxib, trospium, resiniferatoxin, or amikacin. However, all but pethidine-haloperidol and chlorpheniramine showed some efficacy at various time points compared with controls.
CONCLUSION
This review suggests that dexmedetomidine, gabapentin, tolterodine, tramadol, ketamine, nefopam, oxybutynin, pregabalin, and PNB are effective in preventing postoperative CRBD. Considering the efficacy and adverse effects of all drugs, dexmedetomidine and gabapentin were ranked best.
Topics: Chlorpheniramine; Dexmedetomidine; Gabapentin; Haloperidol; Humans; Ketamine; Lidocaine; Meperidine; Nefopam; Pain, Postoperative; Pregabalin; Tolterodine Tartrate; Tramadol; Urinary Bladder; Urinary Catheters
PubMed: 35218404
DOI: 10.1007/s00228-021-03251-5 -
AORN Journal Jul 2020Ensuring patient safety under time pressure Key words: on-time starts, turnover time, briefing, team communication, delays. Holes in the outer layer of sterilization...
Ensuring patient safety under time pressure Key words: on-time starts, turnover time, briefing, team communication, delays. Holes in the outer layer of sterilization wraps Key words: package integrity, defects, sterilization wrap, contaminated item, sterile field. Changing surgical attire after smoking outside Key words: surgical attire, cigarette smoke, tobacco smoke, third-hand smoke, wound healing. Methemoglobinemia after local anesthesia Key words: methemoglobinemia, methemoglobin (MetHb), lidocaine-prilocaine, methylene blue, cyanosis.
PubMed: 32598070
DOI: 10.1002/aorn.13090