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Investigation of Vasoconstrictor Properties of Local Anaesthetic

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Investigation of Vasoconstrictor Properties of Local Anaesthetic ,t4 tn INVTSTIGATION OF VASOCONSTRI CTOR PROPERTIES OF LOCAL ANAESTHITIC SOLUTIONS DALE COURTNEY GERÍ<E, B.D.S., B.Sc.Denf. (Hons.) DEPARTMENT OF HUMAN PHYSIOLOGY AND PHARMACOLOGY, THE UNIVERSITY OF ADELAIDE, SOUTH AUSTRALI A. oCToBER 1977 Lr'' lÌ'"r' ft¡.io, 4, ,,/ fVovx" tl CONTENTS Page CONTENTS tt SUMMARY vi i DECLARAT I ON x ACKNOI/V LEDGEMENTS xi PUBLI CATI OlS xi ii I . GENERAL INTRODUCTION I ntroduct i on 1 1 The vascu I ar mode I system 1 3 The scope of the study 1 6 Factors i nf I uenci ng the sensi ti vity of sma I I 1 I smooth muscle arteries to exogenous catecholamines (i) Neuronal uptake 1.9 ( ¡ ¡ ) Exlraneurona I upfake 1.13 ( ¡ ¡ i ) Monoami ne oxi dase (MAO) 1 .17 ( iv) Catechol-O-methyl transferase (COMT) 1.19 (v) Sensítivily of the rabbit ear to 1,20 catecholamines Abbrevialions 1.25 Concentrati ons 1.25 I I. GENERAL METHODS lsolation and perfusion of lhe central artery 2.1 of the rabbif ear Modification of apparatus for isolated rabbit 2.4 whole ear or rat tai I segment perfusion Surgical sympathetic denervalion of the rabbil 2.9 ear artery Measurement of arteri a I responses and ca I cu I ation 2.12 of potenti ation or depression Tests of signi ficance 2.15 iîi Page lll. THE EFFECTS OF LOCAL ANAESTHETI CS ON THE VASOCONSTRICTOR RESPONSE OF THE ISOLATED PERFUSED AFITERY TO ADRENALINE AND NORADRENALINE I nlroduct i on 3.1 Ivlethods 3.3 Resu I fs 3.6 3.6 'ExtraluminalComparison of responses lo catecholamine isomers drug appl ication causing 3.6 potentiation Extraluminal drug appl ication causing 3. 10 depress i on Denervated arleries 3 4 Exlraluminal drug appl ication in the presence 3 4 of propranolol I nlra I umi na I drug app I i cation 3 6 lndivi dual local anaeslhetic administration 3 B Change in arferial sensitivity wifh time 3 B Di scuss i on 3 22 lv. A HISTOG.IEMICAL STUDY ON THE EFFECT OF LOCAL ANAESTHETICS ON THE NEURONAL UPTAKE OF CATECHOLAMINES IN ISOLATED ARTERIES I ntroduct i on 4.1 Methods 4.2 Replelion of catecholamines 4.2 Blockade of neuronal uptake 4.3 H i stochemi stry 4.3 Grading of f luorescence 4.3 Resu I ts 4.5 NA and Ad uPtake 4.5 The effect of I ignocaine and pri locaÌne after 4.5 60 min incubation in catecholamÎne The effecl of I ignocaine and pri locaîne after 4.13 eifher 30 or '15 min incubaf ion in catecholamine Cocaine blockade 4.17 Di scuss î on 4.14 V THE COMPARATIVE EFFECTS 0F PRILOCAINE, L-IGNOCAINE AND COCAINE ON THE UPTAKE OF LABELLED CATECHOLAMINES INTO SYMPATHETIC NERVE ENDINGS OF THE RABBIT EAR ARTERY I ntroduct i on 5,1 Methods 5.2 lncubation with label led catecholamine 5.2 Measurement of radioactivitY 5.3 Resu I ts 5.4 Catechol ami ne uPtake 5. 10 Blockade of uptake of catecholamines by local anae CS Di scu ss i on 5.12 tv. Page vl. THE EFFECT OF NEURONAL AND EXTRANEURONAL UPTAKE ON THE RESPONSE OF THE RABBIT EAR ARTERY TO ADRENALINE ANID NORADRENAL I NE I nfroduct i on 6.1 Methods 6.2 Resu I ts 6.3 Di scuss i on 6,7 vil. THE EFFECTS OF 2-PHENYLALANINE-B-LYSI NE VASOPRESS IN ON BLOOD VESSELS IN THE RAT TAI L I ntroducti on 7.1 Methods 7.5 Resu I ts 7.8 Tachyphy laxi s to octapressi n 7,8 Potenf i at i ng effecf on cafecho I ami nes 7.8 The effect of a-receptor blockade 7 .14 Di scuss i on 7 .17 .THE VI I I. INFLUENCE OF ADRENERGIC NERVES ON THE RESPONSE OF BLOOD VESSELS IN THE RABBIT EAR TO 2-PHENYLALANINE-B- LYS I NE VASOPRESS I N I nt rod uct i on 8. 1 luelhods 8.2 Resu I fs 8.4 Differences in responses between preparafions 8.4 Response Ìo octapressin affer blockade of 8.7 di fferent recepfors Neuronal component in the overal I vasoconstricfor 8.9 response to octapressin Di scuss i on B. 13 IX. THE SYNERGISTIC VASOCONSRICTOR EFFECT OF OCTAPRESSIN@ AND CATECIIOLAMINES ON THE ISOLATED RABBIT EAR ARTERY I nf rod uct i on 9.1 Methods 9.2 Resu lls 9,4 Di scuss i on 9.8 Page X THE EFFECTS OF COMMERCIAL LOCAL ANAESTHETIC SOLUTIONS ON THE ISOLATED RABBIT EAR ARTERY PART A - THE VASOCONSTRICTOR EFFECTS OF COMMERCIALLY MANUFACTURED LOCAL ANAESTHETi C SOLUT IONS I ntroduct i on 10.3 Methods 10.4 Drugs 10. 4 Experimental protocol 10.4 pH of solutions 10.5 Batch number 10.5 Resu I ts 10.6 rCitanest 50f 10.6 rXylocaine wîth Adr 10.6 fXylotox with NAr 10.6 Batch number 10. i3 Di scuss i on 10.14 PART B - THE EFFECT OF STORAGE ON THE ACTI VITY OF ADRENALINE IN LOCAL ANAESTHETIC SOLUTIONS: AN EVALUATION USING BIOASSAY AND FLUOROMETRIC TECIìN IQUES I ntroduct i on 10.16 Methods 10. 17 Resu I ts 10.20 t t I Bi oassay of Xy I oca i ne and Ci tanestr 10.20 Contro I so I ut i ons used for f I uorometri c 10.26 assay Fluorometric assay of tXylocainer and 10.26 I Ci tanestl Two month trial 10.29 Di scuss i on 10.33 PART C - THE USE OF MIKIURES OF OCTAPRTSSIU@ NUO ADRENALINE IN LOCAL ANAESTHETIC SOLUTIONS TO OBTAIN MORE EFFECTIVE VASOCONSTRICTION I ntroducl i on 10,37 Methods 10. 38 Resu lts 10. 40 Laboratory sol utions 10. 40 Commercial solutions 10. 40 Decreased adrena I i ne concentration 10. 46 Cumu lative addition of octapress in 10.46 Di scuss i on 10.52 vt. Page XI . GENERAL DISCUSS IOf{ APPENDI CES APPENDIX ONE - Krebts bi carbonate solution Appendix page A. 1 Perfusion pump A. 1 pH measurements A.2 Liquid scinfi I lation spectrometry A.2 Drugs A.2 Preparalion of drugs A.3 Concentrat i ons A.4 APPENDI X Tl^lO - ADRENERGIC INNERVATION OF HUMAN MESENTERIC BLOOD VESSELS I ntroduct i on A.6 Methods A.7 Resu I ts A.B Di scuss i on A. 10 BIBLIOGRAPHY Bibl iography pages 1-25 vtt. SUMMARY The aim of this study was to examine the effect on blood vessels of solutions vlhich had various vasoconstrictor and local anaesthetic agents incorporated into them. Special attention has been paid to lhe interactions that occurred between the componenls used in these solutions and the consequent effecl of these interactions on the vascular response. 2 The vascular model used vtas, in most inslances, the central arfery of the rabbit ear. However, during some parts of the investigation, the responses of the vessels of the isolaled whole rabbit ear and of the isolated rat tail segment were also studied. 3 Pharmacological studies showed thaf pri locaine, I ignocaine and cocaine potentiated the response of the arfery to extraluminal ly administered adrenal ine. This potentiation was not seen in sympatheli ca I I y denervated arteries or when adrena I i ne was administered intraluminal ly. 0f the three local anaesthetics listed above, only cocaine potentiated the response to erlra- I umi na I ly admi n i slered noradrena I i ne. vttt. 4 It was shown histochemical ly that pri locaine and I ignocaine were less effective than cocaine in causing blockade of neuronal uptake of catecholamines. lt was further shown fhat neuronal uptake of adrena I i ne was more effecti ve ly b locked by prÎ loca i ne and I ignocaine than was the uptake of noradrenal ine. 5 Uptake of tritiated adrenal ine and noradrenal ine into the arteries was also sludied. ln the presence of pri locaine, lignocaine or cocaine the amounl of uptake of label led adrenal ine into the artery was less than lhat observed with label led noradrenal ine. lt was further shown that lhe percentage inhibition of uptake of label led catecholamine into the tissues caused by these local anaesfhelic agents was greater for adrenal ine than it was for noradrenal ine. lt was therefore concluded that pri locaîne, I ignocaine and cocaine blocked the neuronal uptake of adrenal ine more effectively than that of noradrenal ine. 6 Cocaine was found to polenfiate the resPonses to extraluminal noradrenal ine to a greater extent than extraluminal adrenal ine. However, when uptake2 was inhibited by deoxycorticosterone acetate lhe response to extra I umi na I adrena I i ne was potenti aled more by cocaine than was the response to noradrenal ine appl ied by this route. lt has therefore been suggested that uplake2 plays an importanl role in determining the response of the artery to extraluminal ly administered catecholamines in the presence ix. 7 The constrictor response to Octapressin@ *u, ulro investigated on several vascular beds. Marked tachyphylaxis to this agenl was noted in al I of these studies. The results obtained also suggested that the action of Octapr"rrin@ on the vasculature may involve two componenls i.e. (a) it may act direcÌly on the smooth muscle via its own receptor and (b) it may also act indi rectly on the neuronal storage sites, releasing noradrena- I ine which in turn would activate a-receptors in vascular smooth muscle. B It was found that Octapressin@ potentiated the vasoconstrictor response to cafecholamines. A proposal has therefore been oullined for utilising this potentiating effect in relation lo clinical local anaesthetic solutions.
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