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Dr.Khaled Radaideh
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Classification :The molecule of the clinically useful LA agents consists of 1. A tertiary amine attached to an 2. Aromatic ring by an 3. Intermediate chain.
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Classification of LA Agents
There are 2 classes of local anaesthetic drugs defined by the nature of the intermediate chain.
1.
The ester LA agents include cocaine, procaine, and chloroprocaine The amide LA agents include lidocaine, prilocaine, bupivacaine, etidocaine,
2.
mepivacaine
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Mode of action
After injection, the tertiary amine base is liberated by the relatively alkaline pH of tissue fluids: These effects are due to blockade of sodium channels, thereby impairing sodium ion flux, across the membrane. B.HCl + HCO3 <--> B + H2CO3 + ClIn clinical practice, local anaesthesia may be influenced by the local availability of free base (B), as only the unionised portion can diffuse through the neuronal membrane. Thus, local anaesthetics are relatively inactive when injected into tissues with an acid pH (e.g. pyogenic abscess), which is presumably due to reduced release of free base.
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Preparations of LA
1.
2.
LA agents are usually acid (pH range 4.0-5.5) and contain reducing agent (e.g. sodium metabisulphite) to enhance the stability of added vasoconstrictors preservative and a fungicide
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1g substance in each
100mls
1 g in 100 ml = 1000mg in 100 ml
10 mg in 1 ml
multiplying the percentage strength by 10. Therefore a 0.25% solution of lidocaine contains
2.5mg/ml of solution (10 * 0.25=2.5 mg /ml)
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vasoconstrictors
Most LA produce some degree of vasodilation, and they may be rapidly absorbed after local injection. vasoconstrictors decrease the systemic toxicity and increase the safety margin of local anaesthetics by reducing their rate of absorption vasoconstrictors are frequently added to LA to enhance their potency and prolong their duration of action Adrenaline is the most commonly used vasoconstrictorin concentrations ranging from 1 in 80,000 to 1 in 300,000
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Adrenaline dilution 1:200000 means 1 g in 200000 ml = 1000 mg in 200000 ml 1 mg in 200 ml = 0.1 mg in 20 ml 1:80000..= 0.1 mg in 8 ml
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1: Topical Anaesthesia
LA may be applied to the skin, the eye, the ear, the nose and the mouth as well as other mucous membranes. most useful and effective: Lidocaine (i.e.gel 2%) and prilocaine(i.e.EMLA)
2: Infiltration Anaesthesia
provide anaesthesia for minor surgical procedures. commonly used Amide LA are (Lidocaine prilocaine,mepivacaine and Bupivacaine)., The site of action is at unmyelinated nerve endings and onset is almost immediate
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IVRA (BIER s Block) analgesia for minor surgical procedures. The local anaesthetic agent is injected into a vein of a limb that has been previously exsanguinated and occluded by a tourniquet. The site of action is probably the unmyelinated nerve fibres, Prilocaine and Ldocaine are commonly used. Bupivacaine and etidocaine should never be used for IVRA! They are significantly protein bound and once the tourniquet is released there is a risk of cardiotoxicity. Several deaths have been reported during IVRA with bupivacaine.
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prilocaine,
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Lig.Flavum.
usually used mainly isobaric Bupivacaine 0.5% or lidocaine (2.0%)
6.: Spinal Anaesthesia injction directly into the cerebrospinal fluid (subarachnoid space) produces spinal anaesthesia.
commonly used : mainly hyperbaric Bupivacaine 0.5% or lidocaine (5%)
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with I.V fluids and vasopressors: Ephedrin : If not available or not effective in correcting the hypotension .Adrenaline Treat arrhythmias. Start chest compressions if cardiac arrest occurs. Treat Convulsions with anticonvulsant drugs (Diazepam 0.2-0.4mg/kg , Thiopentone 1-4 mg/kg)
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