-
Injury Sep 1988Recent evidence has shown that there may be leakage of anaesthetic drugs into the systemic circulation during the tourniquet inflation phase of intravenous regional...
Recent evidence has shown that there may be leakage of anaesthetic drugs into the systemic circulation during the tourniquet inflation phase of intravenous regional anaesthesia. This, together with increased pressure in forearm vessels during manipulation of fractures, prompted the measurement of arterial levels of local anaesthetic to assess potential toxicity. Prilocaine levels were measured in nine patients undergoing manipulation of Colles' fractures and six patients undergoing other upper limb procedures. Eleven patients had measurable concentrations of prilocaine in the arterial circulation during the time the tourniquet was inflated, the maximum levels being measured in those patients having fractures manipulated. Considerable vigilance should be ensured during the time of tourniquet inflation in intravenous regional anaesthesia, particularly for fracture manipulation.
Topics: Anesthesia, Conduction; Equipment Failure; Fracture Fixation; Humans; Injections, Intravenous; Prilocaine; Tourniquets
PubMed: 3255712
DOI: 10.1016/0020-1383(88)90106-4 -
British Journal of Anaesthesia Jun 1979The tolerance and pharmacokinetic properties of mepivacaine and prilocaine were compared following i.v. infusion of 250 mg (0.88 and 0.97 mmol respectively) of each drug... (Clinical Trial)
Clinical Trial Comparative Study Randomized Controlled Trial
The tolerance and pharmacokinetic properties of mepivacaine and prilocaine were compared following i.v. infusion of 250 mg (0.88 and 0.97 mmol respectively) of each drug in five healthy volunteers. Side-effects were minor and occurred in only two subjects during the infusion of mepivacaine. Plasma concentrations of mepivacaine were greater in each subject than the corresponding values for prilocaine. The elimination half-life of mepivacaine was generally longer than that for prilocaine, whereas the total body clearance of prilocaine was consistently greater than the corresponding value for mepivacaine. For each subject the clearance of prilocaine substantially exceeded normal heptic blood flow and therefore an extra-hepatic site of metabolism of prilocaine has been postulated.
Topics: Adult; Clinical Trials as Topic; Double-Blind Method; Drug Tolerance; Humans; Infusions, Parenteral; Kinetics; Male; Mepivacaine; Prilocaine; Random Allocation
PubMed: 380609
DOI: 10.1093/bja/51.6.481 -
Clinical Pediatrics Apr 1997
Topics: Anesthetics, Local; Circumcision, Male; Drug Combinations; Humans; Infant, Newborn; Lidocaine; Lidocaine, Prilocaine Drug Combination; Male; Methemoglobinemia; Ointments; Prilocaine
PubMed: 9114997
DOI: 10.1177/000992289703600410 -
Dental Traumatology : Official... Dec 2016Soft tissue injuries have been reported as being sutured using only topical anesthesia applied in the laceration wound. The objective of this study was to assess the...
BACKGROUND/AIM
Soft tissue injuries have been reported as being sutured using only topical anesthesia applied in the laceration wound. The objective of this study was to assess the pharmacokinetic profile of components of Oraqix (2.5% prilocaine and 2.5% lidocaine) when applied in a laceration as compared to intact skin application in the mouse.
MATERIALS AND METHODS
A total of 200 BALB/c male mice were used in this study. The mice were divided into three groups: group A: shaved and laceration group (80 mice); B: shaved and intact skin group (80 mice); and C: control group (shaved, no treatment; 40 mice) which underwent the same procedures but without application of Oraqix . Blood samples were collected over 90 min. Plasma sample analysis employing liquid chromatography coupled with the tandem mass spectrometric (LC-MS/MS) method was used to determine plasma concentrations of lidocaine and prilocaine. Pharmacokinetic analysis of mouse plasma concentrations was carried out by standard non-compartmental methods.
RESULTS
Absorption of both lidocaine and prilocaine was rapid. C and AUC values of lidocaine were significantly increased by fourfold and twofold, respectively, in lacerated mouse skin compared to intact skin. Similarly, prilocaine's C and AUC values were also increased by 2.5-fold and fourfold, respectively, in lacerated skin compared to intact skin.
CONCLUSION
When Oraqix was applied directly into the skin laceration, the plasma concentration of lidocaine and prilocaine was significantly increased as compared to when applied on intact skin. The present study, albeit in mice, indicates that the plasma levels of lidocaine and prilocaine can reach very high levels when the thermosetting gel Oraqix is placed directly in wounds.
Topics: Anesthesia; Anesthetics, Local; Animals; Lacerations; Lidocaine; Lidocaine, Prilocaine Drug Combination; Male; Mice; Mice, Inbred BALB C; Prilocaine
PubMed: 27397548
DOI: 10.1111/edt.12294 -
BMJ (Clinical Research Ed.) Jul 1990
Topics: Anesthetics, Local; Child; Child, Preschool; Drug Combinations; Humans; Infant; Lidocaine; Lidocaine, Prilocaine Drug Combination; Methemoglobinemia; Prilocaine; Time Factors
PubMed: 2390601
DOI: 10.1136/bmj.301.6744.153 -
Journal of the Royal Society of Medicine Nov 1995
Topics: Analgesia; Anesthetics, Local; Drug Combinations; Humans; Lidocaine; Lidocaine, Prilocaine Drug Combination; Ointments; Phlebotomy; Prilocaine
PubMed: 8544157
DOI: No ID Found -
Journal of Physiology and Pharmacology... Jun 2019Prilocaine is widely used for spinal anesthesia. Its intermediate effect makes it a valuable choice for one-day surgery. The duration of the motor blockade (DMB) may... (Clinical Trial)
Clinical Trial Observational Study
Prilocaine is widely used for spinal anesthesia. Its intermediate effect makes it a valuable choice for one-day surgery. The duration of the motor blockade (DMB) may have an impact on the length of stay. The goal of this study was to establish a correlation between the DMB and different parameters (hyperbaric prilocaine dose, puncture level, surgical position, age, patient weight, and patient height). We prospectively enrolled adult patients scheduled for ambulatory surgery (n = 384). Univariate and multivariate regressions (backward stepwise) were applied. A P value lower than 0.05 was considered significant. We performed first analyzes on the entire population. We achieved same on a subgroup only composed of patients who received 60 mg of hyperbaric prilocaine between L4 and L5 and staying on dorsal position during surgery. The univariate analyses of the entire population demonstrate a significant correlation between DMB and 1) the prilocaine dose (P < 0.001), and 2) the BMI (P = 0.011). On the same population, the multivariate analyses confirm these two independent parameters correlated to the DMB: the patient height (P = 0.03) and the hyperbaric prilocaine dose (P < 0.001). The second analyses performed on the subgroup (n = 65), demonstrate a wide variability in the DBM (mean ± SD): 90.12 ± 30.36 minutes. For this concern, univariate analyses illustrate that only the patient height was significantly correlated to the DMB (P = 0.005). The multivariate analyses confirm that patient height could be considered as an independent parameter of DBM (P = 0.005). Within our entire population, there exists a considerable variation in the duration of the motor block after a unique injection of hyperbaric prilocaine. The prilocaine dose and the patient height were the only independent factors of the extension of the DMB. However, this relation is extremely weak and only allows explaining the variability of the DMB in a minority of the patients. This unknown pharmacological property of hyperbaric prilocaine could restrict its use for day-care surgery.
Topics: Ambulatory Surgical Procedures; Anesthesia, Spinal; Female; Humans; Injections; Injections, Spinal; Male; Middle Aged; Prilocaine; Prospective Studies
PubMed: 31539887
DOI: 10.26402/jpp.2019.3.08 -
Advances in Dermatology 1990Eutectic Mixture of Local Anesthetics (EMLA) containing 5% lidocaine and prilocaine in a cream was found to give effective topical analgesia in normal and diseased skin,... (Review)
Review
Eutectic Mixture of Local Anesthetics (EMLA) containing 5% lidocaine and prilocaine in a cream was found to give effective topical analgesia in normal and diseased skin, making it useful for superficial surgery and various other clinical procedures. To be effective, an adequate amount must be applied under occlusion and at the right time before the intervention.
Topics: Administration, Topical; Anesthetics, Local; Dermatology; Dose-Response Relationship, Drug; Drug Combinations; Humans; Lidocaine; Lidocaine, Prilocaine Drug Combination; Prilocaine
PubMed: 2204380
DOI: No ID Found -
Physical Chemistry Chemical Physics :... Jul 2019In glass-forming substances, the addition of water tends to produce the effect of lowering the glass transition temperature, Tg. In a previous work by some of us (Ruiz...
In glass-forming substances, the addition of water tends to produce the effect of lowering the glass transition temperature, Tg. In a previous work by some of us (Ruiz et al., Sci. Rep., 2017, 7, 7470) we reported on a rare anti-plasticizing effect of water on the molecular dynamics of a simple molecular system, the pharmaceutically active prilocaine molecule, for which the addition of water leads to an increase of Tg. In the present work, we study pure and hydrated prilocaine confined in 0.5 nm and 1 nm pore size molecular sieves, and carry out a comparison with the bulk compounds in order to gain a better understanding of the microscopic mechanisms that result in this rare effect. We find that the Tg of the drug under nanometric confinement can be lower than the bulk value by as much as 17 K. Through the concurrent use of differential scanning calorimetry and broadband dielectric spectroscopy we are able to observe the antiplasticizing effect of water in prilocaine also under nanometric confinement, finding an increase of Tg of up to almost 6 K upon hydration. The extension of our analysis to nanoconfined systems provides a plausible explanation for the very uncommon antiplasticizing effect, based on the formation of water-prilocaine molecular complexes. Moreover, this study deepens the understanding of the behavior of drugs under confinement, which is of relevance not only from a fundamental point of view, but also for practical applications such as drug delivery.
Topics: Molecular Dynamics Simulation; Nanostructures; Prilocaine; Water
PubMed: 31267115
DOI: 10.1039/c9cp01771b -
Prescrire International Jun 2000(1) The lidocaine + prilocaine combination, as a cream or adhesive dressings, is now approved for anaesthesia of healthy skin in children of 0 to 3 months, an age range...
(1) The lidocaine + prilocaine combination, as a cream or adhesive dressings, is now approved for anaesthesia of healthy skin in children of 0 to 3 months, an age range in which it used to be contraindicated. (2) The clinical file on the lidocaine + prilocaine combination in this age range is of acceptable methodological quality. (3) For circumcision, two trials showed that the lidocaine + prilocaine cream was more effective than a placebo cream in preventing pain. Two other trials showed that the lidocaine + prilocaine cream was less effective than penile block or local anaesthetic injection in newborns. (4) During heel blood sampling in newborns, the two available comparative trials showed no analgesic efficacy of the lidocaine + prilocaine combination. However, heel blood sampling is an unnecessary procedure. (5) The two comparative trials involving venepuncture in newborns showed, at best, a moderate analgesic effect of the lidocaine + prilocaine combination. (6) Cases of symptomatic methaemoglobinaemia have occurred when recommended conditions of use are not observed.
Topics: Administration, Cutaneous; Age Factors; Blood Specimen Collection; Circumcision, Male; Drug Therapy, Combination; France; Humans; Infant, Newborn; Lidocaine; Methemoglobinemia; Pain; Prilocaine; Punctures; Treatment Outcome
PubMed: 11010744
DOI: No ID Found