Lidocaine + Epinephrine


Thông tin thuốc gốc
Chỉ định và Liều dùng
Injection
Local or regional anaesthesia, nerve blocks, epidural and caudal anaesthesia
Adult: Per ml prep contains lidocaine HCl 20 mg and epinephrine 5 mcg. Dosage depends on several factors such as route, type and extent of surgical procedure, duration of anaesthesia and patient's condition and age. Max dose of lidocaine given with epinephrine: 7 mg/kg and not >500 mg.
Child: 3 mth-12 yr: Per ml prep contains lidocaine HCl 20 mg and epinephrine 5 mcg. Dosage depends on several factors such as route, type and extent of surgical procedure, duration of anaesthesia and patient's condition and age. Max dose 3 mg/kg. Ideal body weight should be used in children with high body weight.
Hướng dẫn pha thuốc
Can be diluted if necessary in glucose 5%, sodium chloride 0.9% and lactated Ringer's solution.
Tương kỵ
Y-site administration: ampicillin, thiopental, ampthotericin B cholesteryl sulphate complex; in syringe: cefazolin, sodium bicarbonate; when admixed: aminophylline, hyaluronidase, mephentemine, amphotericin B, decarbazine, methohexital and thiopental.
Chống chỉ định
Tachycardia, hypertension, cerebral arteriosclerosis, ischaemic heart disease, IV admin, anaesthetise digits or appendages, myasthenia gravis.
Thận trọng
Epilepsy, impaired cardiac conduction, CHF, DM, closed angle glaucoma, impaired liver function (if site of admin is likely to result in high blood levels), severe renal dysfunction. Local anaesthetic effect may be reduced if injected into an inflamed or infected area. Cerebrovascular insufficiency, hyperthyroidism. Neonates, elderly, patients in poor general condition (optimise patient's condition before major block), pregnancy.
Phản ứng phụ
Severity of adverse effects in CNS and CVS are directly related to blood levels of lidocaine; the effects are more likely to occur after systemic administration rather than infiltration; dizziness; muscle twitching; local anaesthetic of mouth/throat impairs swallowing and increases the risk of aspiration (patients cautioned against eating or drinking for 3-4 hr after anaesthesia); transient effect on auditory system of neonate; erythema; pigmentation; pain; headache; palpitations; local necrosis; pulmonary oedema; hyperglycaemia; bradycardia; reduced cardiac output; anxiety. Epidural may cause hypotension, bradycardia, nausea and vomiting. Intraoral inj may cause stress reactions such as diaphoresis, palpitation, hyperventilation, generalised pallor and faintness. Topically: papules, burns, rash, skin irritation, burning sensation and blanching.
Potentially Fatal: Severity of adverse effects in CNS and CVS related to blood levels of lidocaine; effects more likely to occur after systemic administration rather than infiltration. CNS toxicity (due to inadvertent IV admin), medullary depression with tonic & clonic convulsions; ventricular fibrillation; severe hypertension with cerebral haemorrhage and pulmonary oedema; unconsciousness; possibly respiratory arrest. Allergic reactions including anaphylactic symptoms and possibly life threatening asthmatic episodes in susceptible patients may occur due to sodium metabisulphate constituent. Central nerve blocks may cause CV depression (especially in hypovolaemia). Retrobulbar inj may reach subarachnoid space causing CV collapse, apnoea, convulsions, temporary blindness. Paracervical block may cause foetal bradycardia/tachycardia (careful monitoring of foetal heart rate is necessary).
Quá liều
Lidocaine has a narrow therapeutic index. Symptoms: dizziness, paresthesia, sedation, confusion, coma, seizures, ataxia; respiratory arrest, pulmonary oedema; arrhythmias, cardiac toxicity (sinus arrest, AV block, asystole, and hypotension); QRS and QT intervals are usually normal, although they may be prolonged after massive overdose; renal failure; metabolic acidosis and hypertension which may result in subarachnoid haemorrhage and hemiplegia. Treatment: supportive and symptom specific. Lidocaine not removed by haemofiltration.
Tương tác
Significance of interaction depends on route of delivery and systemic exposure; lidocaine prolongs duration of action of suxamethonium; benzodiazepines & barbiturates raise the convulsive threshold to lidocaine; vasopressors potentiate pressor effects of adrenaline; BP may increase with non-selective β-blockers, TCAs, halogenated inhalational anaesthetics and α-blockers; general anaesthetics may increase sensitivity of myocardium to dysrhythmic effects of epinephrine; lidocaine may increase levels and effects of benzodiazepines, calcium channel blockers, ciclosporine, aminophylline, fluvoxamine, mexiletine, mirtazapine, ropinirole, theophylline, trifluoperazine, dextromethorphan, fluoxetine, nefazodone, paroxetine, risperidone, TCAs and venlafaxine. Levels and effects of lidocaine may be increased by propranolol, chlorpromazine, delavirdine, fluoxetine, miconazole, pergolide, quinidine, quinine, ritonavir, ropinirole, cimetidine, azole antifungals, clarithromycin, diclofenac, doxycycline, erythromycin, isoniazid, nicardipine and verapamil. Lidocaine may decrease levels and effects of codeine, hydrocodone, oxycodone, tramadol, carbamazepine, nafcillin, nevirapine, phenobarbital, phenytoin and rifamycins. Midazolam, cisapride, ergot alkaloids, lovastatin and simvastatin are not recommended in combination with lidocaine.
Potentially Fatal: Possible additive cardiac effects with amiodarone (ECG monitoring should be considered).
Food Interaction
St John's Wort may reduce lidocaine level, avoid; ephedra and yohimbe may cause CNS stimulation, avoid.
Lab Interference
Lidocaine may increase creatinine phosphokinase which may interfere with diagnosis of MI.
Tác dụng
Description: Lidocaine is a local anaesthetic which decreases permeability of sodium ions, blocking induction and conduction of nerve impulses. Combination with epinephrine restricts systemic spread of lidocaine, vascular absorption and its duration of local anaesthetic effect.
Onset: Peak effect: approx 5 min.
Duration: Approx 2 hr; dose and anaesthetic procedure dependant.
Pharmacokinetics:
Absorption: Topical: lidocaine: minimal; epinephrine: minimal; readily absorbed from GI tract, mucous membranes, damaged skin, inj sites including muscle.
Distribution: Crosses placenta and blood-brain barrier. Volume of distribution: lidocaine: 1.1-2.1 L/kg, altered by many patient factors eg CHF, liver disease. Protein binding: lidocaine: 60-80% to α1 acid glycoprotein.
Metabolism: Lidocaine: 90% via hepatic 1st pass metabolism to active metabolites which can cause CNS toxicity. Epinephrine: metabolised by monoamine oxidase and catechol-o-methyltransferase taken up in the adrenergic neuron; circulating ephedrine is hepatically metabolised.
Excretion: Lidocaine: elimination half life: 2 hr; excreted via urine (<10% unchanged). Ephedrine: excreted via urine as inactive metabolites and small amounts of unchanged drug.
Bảo quản
Protect from light. Transdermal systems: 20-25 °C. Inj: store at 2-8 °C and discard within 3 days of opening.
Phân loại MIMS
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