Local Anaesthetics
Local Anaesthetics
Local Anaesthetics
Amides Lidocaine (Xylocaine) Bupivacaine (Marcaine) Mepivacaine (Carbocaine) Prilocaine (Citanest) Etidocaine (Duranest) Esters Procaine (Novocain) Chloroprocaine (Nesacaine) Tetracaine (Pontocaine)
The local adverse effects of anesthetic agents include neurovascular manifestations such as prolonged anesthesia (numbness) and paresthesia (tingling, feeling of "pins and needles", or strange sensations). These are symptoms of localized nerve impairment or nerve damage.
Depending on local tissue concentrations of local anesthetics there may be excitatory or depressant effects At lower concentrations, a relatively selective depression of inhibitory neurons results in cerebral excitation, which may lead to generalized convulsions.
A profound depression of brain functions occurs at higher concentrations which may lead to coma, respiratory arrest and death. Due to 1.very high plasma levels after intravenous injection of a large dose. 2. direct exposure of the central nervous system through the CSF, i.e. overdose in spinal anesthesia or accidental injection into the subarachnoid space in epidural anesthesia.
The signs and symptoms of CNS toxicity induced by local anesthetics resemble vasovagal responses. Early symptoms, such as a metallic taste, tinnitus, lightheadedness, and confusion, are followed by tremors and shivering.
The conductive system of the heart is quite sensitive to the action of local anesthetics. Lidocaine is often used as an antiarrhythmic drug and has been studied extensively, but the effects of other local anesthetics are probably similar to those of Lidocaine. Lidocaine acts by blocking sodium channels, leading to slowed conduction of impulses. This may obviously result in bradycardia, but tachyarrhythmia can also occur. With high plasma levels of lidocaine there may be higher-degree atrioventricular block and severe bradycardia, leading to coma and possibly death.
Recent case reports have been published of the successful use of lipid emulsion in this way (Rosenblatt 2006, Litz 2006, Foxall 2007) to save patients who were unresponsive to the usual resuscitation methods. All patients recovered completely shortly after intravenous injections of lipid.
20% Intralipid: 1.5 mL/kg as an initial bolus, followed by 0.25 mL/kg/min for 30-60 minutes Bolus could be repeated 1-2 times for persistent asystole Infusion rate could be increased if the BP declines.
Adverse reactions to local anesthetics (especially the esters) are not uncommon, but true allergy is very rare. Allergic reactions to the esters is usually due to a sensitivity to their metabolite, paraaminobenzoic acid (PABA), and does not result in cross-allergy to amides. There are also cases of allergy to paraben derivatives, which are often added as preservatives to local anesthetic solutions.
The pain of injection is caused by insertion of the needle and infiltration of the anesthetic into the skin. Ideally, the smallest gauge needle, usually 25 to 30, should be used to inject all anesthetics. Adjunctive techniques using topical anesthetics, cryotherapy, or distraction may complement the routine use of lidocaine. Pinching the skin stimulates local sensory nerves, partially blocking the transmission of other painful stimuli. Injecting slowly and steadily can minimize the pain of the anesthetic itself. If clinically indicated, injecting into the subcutaneous tissues is less painful than infiltrating directly into the dermis to raise a wheal. Physicians should remember that ethyl chloride is flammable and should not be used with electrocautery.
The addition of epinephrine at 1:100,000 to 200,000 (5 to 10 g per mL) is useful to prolong the duration of anesthesia and provide some degree of hemostasis. When working on highly vascular tissues such as the scalp, the physician may need to wait between injection and surgery. The onset of optimal vasoconstrictive effect from epinephrine is approximately five minutes. With the vasoconstriction and resultant delay in absorption afforded by epinephrine, the maximum recommended dose of lidocaine increases from 4 to 7 mg per kg1 (Table 23-5).
Adrenaline 1:1000 contains 1 gram of adrenaline per 1000mls solution i.e. 1mg/ml. To prepare a 1 in 200,000 solution the 1:1000 must be diluted 200 times. This is achieved by taking 0.1ml (= 0.1mg) and adding 19.9 mls of local anaesthetic solution.
With mg/kg 9 7 2
Adrenaline containing solutions should never be used for infiltration around end-arteries i.e. penis, ring block of fingers or other areas with a terminal vascular supply as the intense vasoconstriction may lead to severe ischaemia and necrosis.
[edit] Hypersensitivity/Allergy Adverse reactions to local anesthetics (especially the esters) are not uncommon, but true allergy is very rare. Allergic reactions to the esters is usually due to a sensitivity to their metabolite, para-aminobenzoic acid (PABA), and does not result in cross-allergy to amides. Therefore, amides can be used as alternatives in those patients. Non-allergic reactions may resemble allergy in their manifestations. In some cases, skin tests and provocative challenge may be necessary to establish a diagnosis of allergy. There are also cases of allergy to paraben derivatives, which are often added as preservatives to local anesthetic solutions
Methemoglobinemia The systemic toxicity of prilocaine is comparatively low, however its metabolite, otoluidine, is known to cause methemoglobinemia. As methemoglobinemia reduces the amount of hemoglobin that is available for oxygen transport, this side effect is potentially life-threatening. Therefore dose limits for prilocaine should be strictly observed. Prilocaine is not recommended for use in infants.
There are few absolute contraindications for local injection anesthetics. Allergy to amide anesthetics such as lidocaine is rare, and when it does occur, it is usually caused by the preservative methylparaben.1 One way to circumvent a potential allergic reaction is to use preservative-free lidocaine, which is available in single-dose vials. History of an allergy to an ester anesthetic such as procaine (Novocain) is not a contraindication to the use of lidocaine,1 because they are chemically different, and cross-reaction is rare (Table 1). Another approach includes using 1 percent diphenhydramine (Benadryl), which has proved effective in randomized studies.2 The addition of epinephrine, a potent vasoconstrictor, is contraindicated when it may compromise blood flow in a confined space. Epinephrine should never be used in digital and penile blocks or in skin flaps with marginal viability. The use of epinephrine in the nasal tip and ear is relatively contraindicated for the same reasons, but it has been used in studies in which the treated areas are kept warm to prevent additional vasoconstriction.3 The clinician should exercise caution when contemplating the use of vasoconstrictors in dirty wounds because of the increased risk of infection. In addition, certain patients with diabetes, hypertension, heart block, or cerebrovascular disease may be particularly sensitive to epinephrine
Local anaesthetics applied to the skin, the eye, the ear, the nose and the mouth as well as other mucous membranes. In general, cocaine, amethocaine, lignocaine and prilocaine are the most useful and effective local anaesthetics for this purpose. When used to produce topical anaesthesia, they usually have a rapid onset of action (5-10mins) and a moderate duration of action (30-60 mins). Cocaine is a potent vasoconstrictor and is useful in the reduction of bleeding as well as topical anaesthesia. Absorption of local anaesthetics through intact skin is usually slow and unreliable and high concentrations (e.g. 20% benzocaine or 40% lignocaine) are required
Amide anaesthetics with a moderate duration of action are commonly used (lignocaine, prilocaine and mepivacaine). The site of action is at unmyelinated nerve endings and onset is almost immediate. The duration of local anaesthesia is variable. Procaine has a short duration of action (15-30 min), while lignocaine, mepivacaine and prilocaine have a moderate duration of action (70-140 min). Bupivacaine has the longest duration of action (approximately 200 min). The addition of adrenaline (1 in 200,000) will increase the quality and prolong the duration of anaesthesia.
Most pure anesthetic agents exist as solids. Eutectic mixtures are liquids and melt at lower temperatures than any of their components, permitting higher concentrations of anesthetics. Eutectic mixture of local anesthetics (EMLA) represents the first major breakthrough for dermal anesthesia on intact skin. It consists of 25 mg per mL of lidocaine, 25 mg per mL of prilocaine, a thickener, an emulsifier, and distilled water adjusted to a pH level of 9.4.3
EMLA is applied in a thick layer (1 to 2 g per 10 cm2, up to a maximal dose of 10 g) to intact skin.8After application, the area is covered with a patch of Tegaderm or clear plastic wrap to facilitate penetration through the stratum corneum (Figure 1). Depth of anesthesia depends on contact time with EMLA. Anesthetic effect has been shown to reach a maximal depth of 3 mm after a 60-minute application, and 5 mm after a 120-minute application.9 It was also found that dermal analgesia continues and may even increase for 30 to 60 minutes after the cream is removed.9 EMLA should not be applied to the palms and soles because of variable penetration.
EMLA has been associated with occasional adverse reactions, including blanching and redness at the application site.8,12 Perhaps the most serious complication is methemoglobinemia. Cases of methemoglobinemia have occurred in infants younger than three months of age who were exposed to high doses of EMLA for prolonged periods.8 Since then, other studies have demonstrated that 1 g of EMLA applied to the penis for one hour is safe to use in healthy, full-term neonates before circumcision.13,14 Although using EMLA is better than using no anesthesia at all, the dorsal penile nerve block still offers superior analgesia before circumcision, and the methods may be combined.13