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Clinical Pharmacology and Therapeutics Nov 1985Prilocaine pharmacokinetics were determined in 60 patients receiving the drug by two different routes of administration (intra-articular and subcutaneous) during...
Prilocaine pharmacokinetics were determined in 60 patients receiving the drug by two different routes of administration (intra-articular and subcutaneous) during arthroscopy under local anesthesia with controlled pressure irrigation. Resorption of prilocaine by subcutaneous tissues was slow and did not lead to high serum levels. On the contrary, prilocaine resorption by the synovium was fast and induced a sharp serum peak (265.8 +/- 163.5 ng/ml) in the hour after the end of the examination. The drug was completely eliminated from the blood after 24 hours, as the prilocaine t1/2 is about 5 hours. The first procedure was perfected to reduce the risk of methemoglobinemia, which occurred in four of 105 patients. Applied pressure was lowered to 100 mm Hg to prevent the escape of anesthetic solution into the soft tissue of the leg, the prilocaine concentration was reduced to 1 gm/L, and the arthroscope was only set up after a delay to allow the intra-articular anesthetic effect of prilocaine to become established. So far, 200 arthroscopies have been performed with this improved protocol without any problem.
Topics: Adolescent; Adult; Anesthesia; Arthroscopy; Female; Humans; Kinetics; Male; Prilocaine
PubMed: 4053490
DOI: 10.1038/clpt.1985.222 -
International Journal of Impotence... Apr 2022Topical anaesthetics are considered a first-line therapy option in men with premature ejaculation (PE). A cross-sectional retrospective analysis was performed to...
Topical anaesthetics are considered a first-line therapy option in men with premature ejaculation (PE). A cross-sectional retrospective analysis was performed to evaluate the real-life use of the eutectic mixture of prilocaine/lidocaine spray (FORTACIN™) in a cohort of 198 white-European men who had been consecutively and prospectively seen at a single tertiary-referral andrology centre for self-reported PE and naive for previous PE treatments. Descriptive statistics was used to describe the whole cohort and the paired t-test was applied to investigate potential differences throughout a 12-month follow-up (baseline, 1, 3, 6 and 12 months). Overall, mean (SD) age was 37 (6.5) years. Of all, lifelong, acquired and subjective PE were reported in 101 (51%), 59 (29.8%) and 38 (19.2%) patients at baseline, respectively. FORTACIN™ use increased up to 6 months, with 184 (92.9%) and 128 (66.4%) men who had tried and regularly used the compound, respectively. At 12-month follow-up, 53 (26.8%) men reported a regular use of the compound. Mean Premature Ejaculation Diagnostic Tool score significantly decreased at 6 and 12 months compared to baseline (all p < 0.05). Conversely, mean IELT significantly improved at 6-month follow-up compared to baseline (all p ≤ 0.04). Overall, FORTACIN™ emerged to be a safe and effective treatment option in PE patients of various types, with almost one fourth of patients still under treatment after 12 months. Timing and dosing of the drug can deserve to be adjusted according to patient's needs and their sexual ecology.
Topics: Adult; Cross-Sectional Studies; Ejaculation; Female; Humans; Lidocaine; Lidocaine, Prilocaine Drug Combination; Male; Premature Ejaculation; Prilocaine; Retrospective Studies
PubMed: 33828264
DOI: 10.1038/s41443-021-00424-9 -
Upsala Journal of Medical Sciences 1985A new, topical anaesthetic formulation, EMLA 5% cream (Eutectic Mixture of Local Anaesthetics), and placebo have been compared in a randomized double-blind study of 51... (Clinical Trial)
Clinical Trial Randomized Controlled Trial
A new, topical anaesthetic formulation, EMLA 5% cream (Eutectic Mixture of Local Anaesthetics), and placebo have been compared in a randomized double-blind study of 51 children. The objectives were to test if EMLA diminishes pain from venipuncture, to evaluate possible adverse reactions, and to determine if there is any influence upon the ease with which the insertion procedure is carried out. Pain was evaluated using a three-graded verbal rating scale. EMLA relieved pain significantly better than placebo (p less than 0.001), and the procedure was considered to be easier after EMLA treatment. No oedema occurred, but a few cases of local redness and paleness were observed after EMLA treatment. However, these reactions were clinically insignificant. It is concluded that EMLA significantly reduces pain from venipuncture, and side effects are mild and transient.
Topics: Anesthetics, Local; Child; Clinical Trials as Topic; Double-Blind Method; Drug Combinations; Humans; Lidocaine; Lidocaine, Prilocaine Drug Combination; Pain; Prilocaine; Punctures
PubMed: 3913095
DOI: 10.3109/03009738509178485 -
Pediatric Nursing 1993EMLA cream is a topical emulsion composed of prilocaine and lidocaine, produced complete anesthesia of intact skin following application. For the optimum effect, EMLA...
EMLA cream is a topical emulsion composed of prilocaine and lidocaine, produced complete anesthesia of intact skin following application. For the optimum effect, EMLA cream must be applied and covered with an occlusive dressing for 60 minutes prior to the procedure. This limits its use in emergency situations. However, in most situations where procedures are anticipated, EMLA can be applied in advance, including outpatient surgery. Furthermore, if the procedure is a venipuncture, multiple sites should be prepared in case one's initial attempt is unsuccessful. EMLA has been used in children of all ages and provides significant pain relief for venipunctures and lumbar punctures; it is being investigated in children for intramuscular injections and circumcision.
Topics: Absorption; Adolescent; Anesthetics, Local; Body Weight; Child; Drug Combinations; Humans; Lidocaine; Lidocaine, Prilocaine Drug Combination; Methemoglobinemia; Prilocaine; Racial Groups
PubMed: 8233672
DOI: No ID Found -
Aesthetic Plastic Surgery 2004As a reaction to reported adverse outcomes after lidocaine infiltration in tumescent liposuction, prilocaine has gained increasing popularity. Previous studies...
BACKGROUND
As a reaction to reported adverse outcomes after lidocaine infiltration in tumescent liposuction, prilocaine has gained increasing popularity. Previous studies investigating large-volume liposuction procedures found maximum prilocaine levels and methemoglobinemia up to 12 h postoperatively, suggesting that liposuction should be performed as a hospital procedure only. The aim of this study was to determine prilocaine plasma levels and methemoglobinemia in patients after low- to average-volume liposuction for the purpose of defining the required postoperative surveillance period.
METHODS
In 25 patients undergoing liposuction involving less than 2,000 ml prilocaine levels and methemoglobinemia were measured over 4 h postoperatively. Liposuction was conducted after the tumescent technique using a 0.05% hypotonic prilocaine solution with epinephrine.
RESULTS
The average prilocaine dose was 6.8 + 0.8 mg/kg, with a maximum dose of 15 mg/kg. The peak prilocaine plasma level of 0.34 mug/ml occurred 3 h after the infiltration. The mean methemoglobinemia at this time point was 0.65%. Only one patient demonstrated a slightly elevated methemoglobin level of 1.4%, but lacked any clinical signs of methemoglobinemia. The prilocaine recovery in the aspirate averaged 36 +/- 4%, indicating that a large amount is removed by suctioning.
CONCLUSIONS
The patients did not experience high plasma levels of prilocaine or methemoglobinemia undergoing liposuction involving less than 2,000 ml using a 0.05% hypotonic prilocaine solution. The authors therefore conclude that this procedure can be performed safely with a monitoring period of 12 h.
Topics: Adult; Anesthetics, Local; Drug Administration Schedule; Female; Humans; Lipectomy; Male; Methemoglobinemia; Middle Aged; Postoperative Care; Preoperative Care; Prilocaine
PubMed: 15870963
DOI: 10.1007/s00266-004-0009-5 -
Anaesthesia Feb 1984Six volunteers underwent intravenous regional anaesthesia of the non-dominant arm on four occasions using two equipotent doses of bupivacaine and prilocaine,... (Clinical Trial)
Clinical Trial Comparative Study Randomized Controlled Trial
Six volunteers underwent intravenous regional anaesthesia of the non-dominant arm on four occasions using two equipotent doses of bupivacaine and prilocaine, administered in a randomised double-blind sequence. Equipotent doses produced similar degrees of motor and sensory blockade. Bupivacaine produced more rapid motor power loss and delayed motor recovery (p less than 0.01). Prilocaine produced more prolonged objective blockade following tourniquet release (p less than 0.01), although this was not clinically useful, and bupivacaine led to a marked prolongation of subjective blockade (p less than 0.01). Increase of dose with both drugs gave more rapid and complete sensory and motor blockade and delayed recovery (p less than 0.05). This was, however, associated with more marked toxicity. It is suggested that in intravenous regional anaesthesia there are no clinical differences between the drugs in equipotent solutions, and that the lower concentrations are the appropriate ones for standard use.
Topics: Adult; Anesthesia, Conduction; Anesthesia, Intravenous; Bupivacaine; Forearm; Humans; Male; Nerve Block; Prilocaine; Therapeutic Equivalency; Time Factors; Tourniquets
PubMed: 6703268
DOI: 10.1111/j.1365-2044.1984.tb09504.x -
Archives of Pharmacal Research Jul 2012Prilocaine, one of local anesthetics, has been used for regional pain relief. When applied as an ointments or creams, it is hard to expect their effects to last for long...
Prilocaine, one of local anesthetics, has been used for regional pain relief. When applied as an ointments or creams, it is hard to expect their effects to last for long time, because they are easily removed by wetting, movement and contacting. For more comfortable and better application, we developed a prilocaine gel system using a bioadhesive polymer, carboxymethyl cellulose (CMC). For suitable bioadhesion, the bioadhesive force of various polymers was tested using an auto-peeling tester. The bioadhesive force of various types of CMC such as 100MC, 150MC and 300MC, was 0.0264, 0.0461 and 0.0824 N, at 1.5% concentration, respectively. The CMC-300MC gels showed the most suitable bioadhesive forces. The effect of drug concentration on drug release was studied from the prepared 1.5% CMC gels using a synthetic cellulose membrane at 37 ± 0.5°C. As the concentration of drug increased, the drug release increased. The effects of temperature on drug release from the 1.0% prilocaine gels were evaluated at 27, 32, 37 and 42°C. As the temperature of the drug gels increased, drug release increased. The enhancing effects of penetration enhancers such as pyrrolidones, non-ionic surfactants, fatty acids and propylene glycol derivatives were studied. Among the enhancers used, polyoxyethylene 2-oleyl ether was superior. The anesthetic effects were studied by a tail flick analgesic meter. In the rat tailflick test, 1.0% prilocaine gels containing polyoxyethylene 2-oleyl ether showed the most prolonged local analgesic effects. The results support the view that prilocaine gels with enhanced local anesthetic action could be developed using CMC bioadhesive polymer.
Topics: Adhesiveness; Administration, Cutaneous; Administration, Topical; Anesthetics, Local; Animals; Carboxymethylcellulose Sodium; Chemistry, Pharmaceutical; Drug Carriers; Excipients; Gels; Imidazoles; Kinetics; Male; Pain Threshold; Polyethylene Glycols; Prilocaine; Rats; Rats, Sprague-Dawley; Skin; Skin Absorption; Solubility; Technology, Pharmaceutical; Temperature; Viscosity
PubMed: 22864742
DOI: 10.1007/s12272-012-0710-x -
Anaesthesia Aug 1984
Topics: Anesthesia, Conduction; Anesthesia, Intravenous; Bupivacaine; Humans; Prilocaine
PubMed: 6476332
DOI: 10.1111/j.1365-2044.1984.tb06562.x -
BMJ (Clinical Research Ed.) Nov 1988
Review
Topics: Administration, Cutaneous; Drug Combinations; Humans; Lidocaine; Prilocaine
PubMed: 3145057
DOI: 10.1136/bmj.297.6658.1215 -
Anesthesia Progress 1993The development of new local anesthetics has not been an area of particularly active research for a number of years. However, as the use of regional anesthesia has... (Review)
Review
The development of new local anesthetics has not been an area of particularly active research for a number of years. However, as the use of regional anesthesia has expanded, additional anesthetic requirements and techniques have stimulated the search for newer drugs and ways of modifying existing ones. This article reviews some of the more recent developments in this field.
Topics: Anesthesia, Dental; Anesthesia, Local; Anesthetics, Local; Animals; Carticaine; Dose-Response Relationship, Drug; Drug Combinations; Humans; Lidocaine; Lidocaine, Prilocaine Drug Combination; Prilocaine
PubMed: 8185087
DOI: No ID Found