関: propitocaine

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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2017/07/03 20:17:34」(JST)

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Prilocaine (/ˈpraɪləˌkeɪn/^[1]) is a local anesthetic of the amino amide type first prepared by Claes Tegner and Nils Löfgren. In its injectable form (trade name Citanest), it is often used in dentistry. It is also often combined with lidocaine as a topical preparation for dermal anesthesia (lidocaine/prilocaine or EMLA), for treatment of conditions like paresthesia. As it has low cardiac toxicity, it is commonly used for intravenous regional anaesthesia (IVRA).

Contraindications

In some patients, ortho-toluidine, a metabolite of prilocaine, may cause methemoglobinemia, which may be treated with methylene blue. Prilocaine may also be contraindicated in people with sickle cell anemia, anemia, or symptomatic hypoxia.^[2]

People with pseudocholinesterase deficiency may have difficulty metabolizing this anesthetic.

Combinations

It is given as a combination with the vasoconstrictor epinephrine under the trade name Citanest Forte.

Compendial status

United States Pharmacopeia 31 ^[3]

Notes

^ "Prilocaine". Merriam-Webster Dictionary. Retrieved 2016-01-21.
^ Patel, Vinod; Morrissey, John (2011-09-15). Practical and Professional Clinical Skills. Oxford University Press. p. 267. ISBN 9780199585618.
^ The United States Pharmacopeial Convention. "Revision Bulletin: Lidocaine and Prilocaine Cream–Revision to Related Compounds Test". Retrieved 10 July 2009.

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English Journal

Diagnosis of Brugada's syndrome after subarachnoid injection of prilocaine.

Oliván B1, Arbeláez A2, de Miguel M2, Pelavski A2.
Revista española de anestesiología y reanimación.Rev Esp Anestesiol Reanim.2016 Oct;63(8):483-6. doi: 10.1016/j.redar.2015.11.010. Epub 2016 Jan 9.
Brugada syndrome is an autosomal dominant genetic disease affecting sodium ion channels. It is characterised by right bundle branch block and ST elevation in the right precordial leads, and with no structural cardiac abnormalities. It is associated with sudden death. This disease may be unmasked by
PMID 26778671

A Novel Pain Alternative for Patients with Anorectal Pathologies: The Comparison of Transperineal Prostatic Blockage Technique with Periprostatic Nerve Blockage and Rectal Gel Technique in Initial Transrectal Ultrasound-Guided Prostate Biopsy - A Prospective, Randomized Trial.

Bolat D1, Degirmenci T, Gunlusoy B, Aydin E, Aydogdu O, Ceylan Y.
Urologia internationalis.Urol Int.2016 Sep 6. [Epub ahead of print]
INTRODUCTION: The study aimed to compare the efficiency of periprostatic nerve blockage (PPNB) and intrarectal lidocaine gel (PPNB + gel) with a transperineal prostatic block (TPPB) technique during transrectal ultrasound-guided prostate biopsy (TRUS-PBx) in patients with anorectal pathologies.MATER
PMID 27595402

Local Anesthetics Affect Gramicidin A Channels via Membrane Electrostatic Potentials.

Efimova SS1, Zakharova AA2, Schagina LV2, Ostroumova OS2.
The Journal of membrane biology.J Membr Biol.2016 Sep 3. [Epub ahead of print]
The effects of local anesthetics (LAs), including aminoamides and aminoesters, on the characteristics of single gramicidin A (GA) channels in 1,2-dioleoyl-sn-glycero-3-phosphocholine (DOPC) bilayers were studied. Aminoamides, namely lidocaine (LDC), prilocaine (PLC), mepivacaine (MPV), and bupivacai
PMID 27592116

Japanese Journal

Local Anesthetic Cream Prepared from Lidocaine-Tetracaine Eutectic Mixture

大関圭一,北原雅樹,鈴木憲子,田口恭次,山崎勇樹,秋山真二,高橋健太郎,神崎〓
藥學雜誌 128(4), 611-616, 2008-04-01
… The LT formulation was compared with a lidocaine-prilocaine (LP cream) eutectic mixture formulated using the same base as EMLA. …
NAID 110006656198

Percutaneous Penetration Kinetics of Lidocaine and Prilocaine in Two Local Anesthetic Formulations Assessed by in Vivo Microdialysis in Pigs(Biopharmacy)

WEI Huilin,CHEN Yun,XU Lanfang,ZHENG Jiarun
Biological & pharmaceutical bulletin 30(4), 830-834, 2007-04-01
… The aim of this study was to characterize and compare the percutaneous penetration kinetics of lidocaine (L) and prilocaine (P) in two local anesthetic formulations by in vivo microdialysis coupled with HPLC. … The microdialysis system for studying lidocaine and prilocaine was calibrated by a no-net-flux method in vitro and retrodialysis method in vivo, respectively. …
NAID 110006271235

「propitocaine」

Prilocaine
Clinical data
AHFS/Drugs.com	Monograph
MedlinePlus	a603026
Pregnancy; category	B (U.S.);
ATC code	N01BB04 (WHO);
Pharmacokinetic data
Protein binding	55%
Metabolism	Hepatic and renal
Biological half-life	10-150 minutes, longer with impaired hepatic or renal function
Identifiers
	IUPAC name (RS)-N-(2-methylphenyl)-N2-propylalaninamide;
CAS Number	721-50-6 ;
PubChem CID	4906;
IUPHAR/BPS	7276;
DrugBank	DB00750 ;
ChemSpider	4737 ;
UNII	046O35D44R;
KEGG	D00553 ;
ChEBI	CHEBI:8404 ;
ChEMBL	CHEMBL1194 ;
ECHA InfoCard	100.010.871
Chemical and physical data
Formula	C13H20N2O
Molar mass	220.311 g/mol
3D model (Jmol)	Interactive image;
Chirality	Racemic mixture
Melting point	37 to 38 °C (99 to 100 °F)
	SMILES O=C(Nc1ccccc1C)C(NCCC)C ;
	InChI InChI=1S/C13H20N2O/c1-4-9-14-11(3)13(16)15-12-8-6-5-7-10(12)2/h5-8,11,14H,4,9H2,1-3H3,(H,15,16) ; Key:MVFGUOIZUNYYSO-UHFFFAOYSA-N ;
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