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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 -
Daru : Journal of Faculty of Pharmacy,... Jun 2021This study investigated whether thymoquinone (TQ) could alleviate central nervous system (CNS) and cardiovascular toxicity of prilocaine, a commonly used local...
PURPOSE
This study investigated whether thymoquinone (TQ) could alleviate central nervous system (CNS) and cardiovascular toxicity of prilocaine, a commonly used local anesthetic.
METHODS
Rats were randomized to the following groups: control, prilocaine treated, TQ treated and prilocaine + TQ treated. Electroencephalography and electrocardiography electrodes were placed and trachea was intubated. Mechanical ventilation was initiated, right femoral artery was cannulated for continuous blood pressure measurements and blood-gas sampling while the left femoral vein was cannulated for prilocaine infusion. Markers of myocardial injury, reactive oxygen/nitrogen species (ROS/RNS) generation and total antioxidant capacity (TAC) were assayed by standard kits. Aquaporin-4 (AQP4), nuclear factor(NF)κB-p65 and -p50 subunit in brain tissue were evaluated by histological scoring.
RESULTS
Blood pH and partial oxygen pressure, was significantly decreased after prilocaine infusion. The decrease in blood pH was alleviated in the prilocaine + TQ treated group. Prilocaine produced seizure activity, cardiac arrhythmia and asystole at significantly lower doses compared to prilocaine + TQ treated rats. Thymoquinone administration attenuated levels of myocardial injury induced by prilocaine. Prilocaine treatment caused increased ROS/RNS formation and decreased TAC in heart and brain tissue. Thymoquinone increased heart and brain TAC and decreased ROS/RNS formation in prilocaine treated rats. AQP4, NFκB-p65 and NFκB-p50 expressions were increased in cerebellum, cerebral cortex, choroid plexus and thalamic nucleus in prilocaine treated rats. Thymoquinone, decreased the expression of AQP4, NFκB-p65 and NFκB-p50 in brain tissue in prilocaine + TQ treated rats.
CONCLUSION
Results indicate that TQ could ameliorate prilocaine-induced CNS and cardiovascular toxicity.
Topics: Animals; Anticonvulsants; Aquaporin 4; Benzoquinones; Blood Pressure; Brain; Cardiotonic Agents; Cardiotoxicity; Epilepsy; Heart; Heart Rate; Male; Myocardium; NF-kappa B p50 Subunit; Neuroprotective Agents; Prilocaine; Rats, Wistar; Reactive Nitrogen Species; Reactive Oxygen Species; Transcription Factor RelA; Rats
PubMed: 33469802
DOI: 10.1007/s40199-020-00385-2 -
Canadian Family Physician Medecin de... Oct 1998To consider topical anesthetic options available to primary care physicians, indications for their use, and efficacy and safety of these agents as supported by the... (Review)
Review
OBJECTIVE
To consider topical anesthetic options available to primary care physicians, indications for their use, and efficacy and safety of these agents as supported by the literature.
QUALITY OF EVIDENCE
Five randomized controlled trials were retrieved that compared various topical anesthetics as well as topical anesthetics versus infiltrative anesthesia.
MAIN FINDINGS
A combination of lidocaine, epinephrine, and tetracaine (LET) is currently the topical anesthetic of choice for repair of simple lacerations involving the faces and scalps of children. A promising new topical preparation is bupivacaine and epinephrine, but its efficacy must be studied in larger populations before widespread use can be advocated. Using EMLA (eutectic mixture of local anesthetics) for repair of extremity lacerations requires further study and cannot yet be recommended. Continued use of topical tetracaine, adrenaline, and cocaine (TAC) is not supported in the literature, because of its greater expense, its status as a restricted narcotic, its potential for toxicity, and better availability of an equally efficacious alternative, LET.
CONCLUSIONS
Children's simple facial and scalp lacerations can be safely repaired using topical LET gel. Physicians must adhere to recommendations to avoid mucous membrane contact and ensure appropriate dosing with these agents. Bupivacaine-epinephrine topical preparation is a promising analgesic agent that warrants further study.
Topics: Adult; Anesthetics, Combined; Anesthetics, Local; Child; Cocaine; Drug Combinations; Epinephrine; Humans; Lidocaine; Lidocaine, Prilocaine Drug Combination; Pain; Patient Selection; Prilocaine; Research Design; Suture Techniques; Tetracaine; Wounds and Injuries
PubMed: 9805170
DOI: No ID Found -
International Wound Journal Oct 2019This study aimed to demonstrate the antibacterial effects of bupivacaine and prilocaine on Escherichia coli, Staphylococcus aureus, and Pseudomonas aeruginosa. In our... (Comparative Study)
Comparative Study
This study aimed to demonstrate the antibacterial effects of bupivacaine and prilocaine on Escherichia coli, Staphylococcus aureus, and Pseudomonas aeruginosa. In our study, the in vitro antimicrobial effects of 20 mg/mL prilocaine and 5 mg/mL bupivacaine were tested against a S. aureus American-type culture collection (ATCC) 29213, P. aeruginosa ATCC 27853, and E. coli ATCC 25922, divided into Group P (Prilocaine) and Group B (Bupivacaine), respectively. S. aureus ATCC 29213, P. aeruginosa ATCC 27853, and E. coli ATCC 25922 were cultured on Mueller Hinton agar (Oxoid, Basingstoke, UK) plates for 18 to 24 hours at 37°C. In terms of inhibition zone diameters, inhibition of S. aureus ATCC 29213 was observed in both groups at the 12th and 24th hours. The 12th- and 24th-hour S. aureus ATCC 29213 value was significantly higher in Group P compared with Group B (P = .008). At the 12th and 24th hours, inhibition of E. coli ATCC 25922 was observed in both groups. The 12th- and 24th-hour E. coli ATCC 25922 value was significantly higher in Group P compared with Group B (P = .008). In our study, it was seen that prilocaine and bupivacaine had an antimicrobial effect on S. aureus and E. coli. In the comparison between these two local anesthetics (LAs), this effect was found to be significantly higher in prilocaine than bupivacaine. Therefore, we are of the opinion that antimicrobial effect potentials should also be taken into account in the selection of an LA agent in order to prevent the complications of an infection that might develop during LA infiltration and might lead to serious morbidity.
Topics: Bupivacaine; Escherichia coli; Humans; In Vitro Techniques; Microbial Sensitivity Tests; Prilocaine; Pseudomonas aeruginosa; Sensitivity and Specificity; Staphylococcus aureus; Statistics, Nonparametric
PubMed: 31407480
DOI: 10.1111/iwj.13180 -
Urologia Dec 2017Premature ejaculation (PE) is a common complaint of male sexual dysfunction affecting men and their partners and consequently causing significant personal and... (Review)
Review
Premature ejaculation (PE) is a common complaint of male sexual dysfunction affecting men and their partners and consequently causing significant personal and interpersonal distress. Increased sensitivity of the glans penis and abnormalities of the afferent-efferent reflex pathway within the ejaculatory process are involved in the occurrence of PE. Drugs that either selectively reduce penile sensitization or modify the afferent-efferent reflex are well established therapeutic options for PE. Fortacin™ is the first topical treatment to be officially approved for the treatment of primary PE in adult men, and is mentioned as an experimental aerosol (as TEMPE) in the current European Association of Urology guidelines. It was approved for use in the European Union and launched in the United Kingdom in November 2016. Fortacin™ is a eutectic-like mixture of lidocaine 150 mg/mL and prilocaine 50 mg/mL that meets the requirements of an ideal treatment for PE because it is fast acting (within 5 minutes), has durable effects, can be easily used "on-demand", and shows minimal side-effects. The metered-dose spray delivery system allows the desensitizing agents to be deposited in a dose-controlled, concentrated film onto the glans penis consequently reducing its sensitivity. This is translated into a delaying of the ejaculatory latency time without adversely affecting the sensation of ejaculation and orgasmic pleasure. The efficacy and safety of Fortacin™ have been proven by means of increased ejaculatory latency, control, and sexual satisfaction in large scale studies demonstrating the significant benefits for both patients and their partners.
Topics: Anesthetics, Local; Humans; Lidocaine, Prilocaine Drug Combination; Premature Ejaculation; Treatment Outcome
PubMed: 30047847
DOI: 10.5301/uj.5000275 -
Local and Regional Anesthesia 2017Prilocaine is a local anesthetic characterized by intermediate potency and duration and fast onset of action. As hyperbaric formulation of 5% solution, it was introduced... (Review)
Review
Prilocaine is a local anesthetic characterized by intermediate potency and duration and fast onset of action. As hyperbaric formulation of 5% solution, it was introduced and has been successfully used for spinal anesthesia since 1960. A new formulation of 2% plain and hyperbaric solution is currently available in Europe. Because of its lower incidence of transient neurological symptoms, prilocaine is suggested as substitute to lidocaine and mepivacaine in spinal anesthesia for ambulatory surgery, as well as a suitable alternative to low doses of long-acting local anesthetics. The National Library of Medicine database, the Excerpta Medica database, the Cochrane Database of Systematic Reviews, and the Cochrane Central Register of Controlled Trials database, were searched for the period 1970 to September 2016, with the aim to identify studies evaluating the intrathecal use of 2% prilocaine. A total of 13 randomized clinical trials (RCTs), 1 observational study, 2 dose finding, and 4 systematic reviews has been used for this review. The studies evaluated showed that 2% hyperbaric prilocaine due to a favorable anesthetic and safety profile is an alternative drug to lidocaine and mepivacaine for spinal anesthesia of intermediate or short duration. In comparison with plain solutions, hyperbaricity remarkably accelerates the onset and offset times of intrathecal 2% prilocaine. Literature suggests a dose ranging between 40 and 60 mg of prilocaine for lower extremities and lower abdominal procedures lasting up to 90 min, whereas a dose ranging from 10 to 30 mg is appropriate for perineal surgery. Readiness for discharge occurs in ~4 h from spinal administration.
PubMed: 28408851
DOI: 10.2147/LRA.S112756 -
British Journal of Anaesthesia Jul 1986The most important clinical properties of local anaesthetic agents are potency, onset, duration of action and relative blockade of sensory and motor fibres. These... (Review)
Review
The most important clinical properties of local anaesthetic agents are potency, onset, duration of action and relative blockade of sensory and motor fibres. These qualities are related primarily to the physicochemical properties of the various compounds. In general, lipid solubility determines the relative intrinsic potency of the various agents, while protein binding influences the duration of anaesthesia and pKa is correlated with the onset of action. In general, the local anaesthetics for infiltration, peripheral nerve blockade, and extradural anaesthesia can be classified into three groups: agents of low potency and short duration, for example procaine and chloroprocaine; agents of moderate potency and duration, for example lignocaine, mepivacaine and prilocaine; and agents of high potency and long duration, for example amethocaine, bupivacaine and etidocaine. These local anaesthetics also vary in terms of onset: chloroprocaine, lignocaine, mepivacaine, prilocaine and etidocaine have a rapid onset, while procaine, amethocaine and bupivacaine are characterized by a longer latency period.
Topics: Anesthesia, Local; Anesthetics, Local; Bupivacaine; Carbon Dioxide; Dextrans; Humans; Nerve Block; Structure-Activity Relationship; Time Factors; Vasoconstrictor Agents
PubMed: 2425835
DOI: 10.1093/bja/58.7.701 -
The Western Journal of Medicine Sep 2001
Review
Topics: Adolescent; Anesthetics, Local; Child; Child, Preschool; Evidence-Based Medicine; Glucosephosphate Dehydrogenase; Humans; Infant; Infant, Newborn; Male; Methemoglobinemia; Methylene Blue; Oxidants; Prilocaine
PubMed: 11527852
DOI: 10.1136/ewjm.175.3.193