Disease relevance of Citanest

• Eutectic lidocaine/prilocaine cream has a very favourable tolerability profile, transient and mild skin blanching and erythema being the most frequent adverse events to occur in association with its application to skin [1].
• Prilocaine-induced methemoglobinemia in a newborn infant [2].
• A comparative study of topical analgesia with a lidocaine/prilocaine cream (EMLA) and infiltration anesthesia for laser surgery of genital warts in men [3].
• In the range of several millimolar concentrations, prilocaine caused a contracture of the single fibers in both polarized and depolarized states [4].
• Although the substitution of prilocaine for lidocaine may reduce the incidence of transient neurologic symptoms, it is unlikely to reduce the risk of actual neural injury [5].

Psychiatry related information on Citanest

• It was concluded that in comparison to lidocaine, bupivacaine, or etidocaine, which have been tested previously and found to impair psychomotor performance, mepivacaine and, especially, prilocaine are the anaesthetic agents to be preferred when effects on central nervous system should be avoided, e.g. in outpatient practice [6].

High impact information on Citanest

• In the FOB group only patients who received local anesthesia by prilocaine bolus injection into the airways via the working channel of the bronchoscope developed fever and increases of IL-6 and IL-beta, whereas patients anaesthetized by inhalation of a prilocaine aerosol remained afebrile and had slight IL-6 increases only [7].
• Prilocaine in arthroscopy: clinical pharmacokinetics and rational use [8].
• 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 [8].
• Resorption of prilocaine by subcutaneous tissues was slow and did not lead to high serum levels [8].
• Four chiral selectors, namely a cationic cyclopeptide, vancomycin, human serum albumin and riboflavin binding protein have been chosen for this study and some analytes such as derivatized amino acids, promethazine and prilocaine have been used as test compounds [9].

Chemical compound and disease context of Citanest

• We investigated in an open pilot study the effect of bilateral block of the greater occipital nerve with 50 mg prilocaine and 4 mg dexamethasone in patients with chronic tension type headache [10].
• Venous irritation and/or urticaria after tourniquet release was observed on 10 occasions in those receiving 2-chloroprocaine and twice in those receiving prilocaine [11].
• The delayed erythema and pallor produced in response to CGRP were not inhibited by oral chlorpheniramine, or by 4% prilocaine injected locally [12].
• Articaine, being a potent local anesthetic with low degree of toxicity and being rapidly metabolized by esterases, could be a useful local anesthetic particularly in IVRA and, perhaps, could challenge prilocaine, the present local anesthetic of choice for this technique [13].
• Contact dermatitis from prilocaine with cross-sensitivity to pramocaine and bupivacaine [14].

Biological context of Citanest

• With increasing prilocaine concentrations above 10 mM, the membrane-bound fluoride-stimulated activity was progressively inhibited, even though bilayer fluidity continued to increase and the activity of the solubilized enzyme remained unaffected [15].
• The concentration of each of eight local anesthetics that produced 50% inhibition of peak chemiluminescence (IC50) had a rank order of dibucaine < tetracaine < bupivacaine < ropivacaine < procaine < mepivacaine < lidocaine = prilocaine [16].
• All the amino alcohols tested had an enantioselective site that overlaps with the catalytically active site of CBH I, whereas the enantioselectivity of prilocaine was not affected by the mutation [17].
• The PCA method showed good results at the same level as the detection limit of baseline-separated prilocaine, outperforming the methods in Chromeleon by a factor of ten [18].
• Prilocaine induces apoptosis in osteoblastic cells [19].

Anatomical context of Citanest

• Prilocaine can increase the fluidity of rat liver plasma membranes, as indicated by a fatty acid spin-probe [15].
• Unlike prilocaine, procaine, also a cation, fluidized both leaflets of these membranes equally [20].
• These results suggest that the mode of action of prilocaine on the sarcoplasmic reticulum could be a depolarization-like action [4].
• Plasma prilocaine concentrations after three techniques of brachial plexus blockade [21].
• Prilocaine 1.5% plain provides adequate sensory and motor blockade for brachial plexus anaesthesia and is a suitable agent for medium duration surgery to the upper limb [22].

Associations of Citanest with other chemical compounds

• Further research in such indications as paediatric lumbar puncture, minor otological surgery, and minor gynaecological, urological and andrological procedures is likely to further broaden the profile of clinical use for eutectic lidocaine/prilocaine cream [1].
• We have in a recent study demonstrated that pethidine could be an interesting alternative to prilocaine in arthroscopy with local anaesthetic technique [23].
• Glucagon-stimulated adenylate cyclase detects a selective perturbation of the inner half of the liver plasma-membrane bilayer achieved by the local anaesthetic prilocaine [15].
• Prilocaine increased the release of Ca++ with increasing concentration, but, unlike caffeine, prilocaine could not enhance the Ca++-induced Ca++ release mechanism of the sarcoplasmic reticulum [4].
• In Group A, surgery was performed under supraclavicular brachial plexus block only; a mixture of equal parts of prilocaine 1% and bupivacaine 0.5% without adrenaline was used [24].

Gene context of Citanest

• Ten patients in each group received 50 mg (P50), 100 mg (P100), 200 mg (P200) of pethidine or prilocaine (5 mg/ml) + adrenaline (4 mg/ml) (PC), injected intra-articularly (i.a.) before surgery [23].
• METHODS: Men, scheduled for removal of genital warts by cryotherapy, were randomly selected to receive one of three treatments: (1) lidocaine/prilocaine cream application, (2) 1% lidocaine infiltration, and (3) lidocaine/prilocaine cream application followed by infiltration of 1% lidocaine [25].
• A marked increase in intracellular response for prilocaine 1000 micrograms.ml-1 (3894 mumol.l-1) accompanied by a reduction in extracellular response, using FMLP +/- HRP as a stimuli, was noted [26].
• A thoracic epidural block from T1 to T12 was performed with plain prilocaine in four patients with coronary artery disease who were scheduled for abdominal aortic aneurysm surgery [27].
• No association could be detected in water or 0.1 mol dm-3 electrolyte for butacaine hemisulphate and the hydrochlorides of procaine, proparacaine, mepivacaine, lignocaine, bupivacaine and prilocaine at drug concentrations of less than 0.2 mol dm-3 [28].

Analytical, diagnostic and therapeutic context of Citanest

• 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 [8].
• 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 [8].
• Eutectic lidocaine/prilocaine cream 5% is a eutectic mixture of the local anaesthetics lidocaine (lignocaine) 25 mg/g and prilocaine 25 mg/g that provides dermal anaesthesia/analgesia following topical application [1].
• Comparison of lidocaine and prilocaine for intravenous regional anesthesia [29].
• The emulsion of lidocaine and prilocaine (EMLA) is effective in preventing the pain of venipuncture in children [30].

References