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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 2. The amide LA agents include lidocaine, prilocaine, bupivacaine, etidocaine,
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 + Cl In 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
LA agents are usually acid (pH range 4.0-5.5) and contain 1. reducing agent (e.g. sodium metabisulphite) to enhance the stability of added vasoconstrictors 2. 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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agents Absolute contraindication (should never be used) for: 1.infiltration around end-arteries i.e. ring block of fingers, penis or other areas with a terminal vascular supply as the intense vasoconstriction may lead to severe ischaemia and necrosis. 2. Intravenous regional anaesthesia (IVRA) Relative contraindication: 1.Patient with severe hypertension 2.General anaesthesia with halothane
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7.
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Tumescent Anesthesia
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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
2: Infiltration Anaesthesia
provide anaesthesia for minor surgical procedures. commonly used Amide LA are (Lidocaine
prilocaine(i.e.EMLA)
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
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Minor nerve blocks involve the blocking of single nerve entities such as the inferior alveolar nerve, mental nerve, ulnar or radial nerve. Major nerve blocks involve the blocking of deeper nerves or trunks with a wide dermatomal distribution (e.g. brachial plexus blockade).
usually used 0.5% Bupivacaine (mainly) or lidocaine (2.0%) 6.: Spinal Anaesthesia injction directly into the cerebrospinal fluid (subarachnoid space) produces spinal anaesthesia.
commonly used : Bupivacaine 0.5% (mainly hyperbaric), lidocaine (5%)
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Essential Precautions and Treatment Precautions: Secure intravenous access before injection
of any dose that . Always have adequate resuscitation equipment and drugs available before starting to inject.
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