Lidocaine + Epinephrine


Thông tin thuốc gốc
Chỉ định và Liều dùng
Epidural
Caudal block, Lumbar epidural block
Adult: Available preparation for epidural test dose:
Lidocaine 1.5% (15 mg) and epinephrine 1:200,000 (5 mcg) per mL solution for inj

Administer test dose (2-3 mL) at least 5 minutes prior to injecting the total volume required for a lumbar or caudal block.

Available preparations for epidural anaesthesia:
Lidocaine 1% (10 mg) and epinephrine 1:200,000 (5 mcg) per mL solution for inj
Lidocaine 1.5% (15 mg) and epinephrine 1:200,000 (5 mcg) per mL solution for inj
Lidocaine 2% (20 mg) and epinephrine 1:200,000 (5 mcg) per mL solution for inj

Dosage varies with the number of dermatomes to be anaesthetised (generally 2-3 mL/dermatome). Max: Lidocaine 7 mg/kg (not to exceed 500 mg). For continuous epidural or caudal anaesthesia, Max dose should not be administered at intervals of <90 minutes. Dosage recommendations may vary among countries and individual products (refer to specific product guidelines).

Parenteral
Dental infiltration and dental nerve block
Adult: Available preparations:
Lidocaine 2% (20 mg) and epinephrine 1:100,000 (10 mcg) per mL solution for inj
Lidocaine 2% (20 mg) and epinephrine 1:80,000 (22.7 mcg) per mL solution for inj

Dose is individualised based on the physical status of the patient, the vascularity of the oral tissues, the area of the oral cavity to be anaesthetised, and the technique of anaesthesia used. For oral infiltration or mandibular block: 1-5 mL. Max: Lidocaine 7 mg/kg (not to exceed 200-500 mg, depending on the procedure and product used). Dosage recommendations may vary among countries and individual products (refer to specific product guidelines).
Child: Dose is individualised based on the physical status of the patient, the vascularity of the oral tissues, the area of the oral cavity to be anaesthetised, and the technique of anaesthesia used. For oral infiltration or mandibular block: <10 years 0.9-1 mL; ≥10 years Same as adult dose. Max: Lidocaine 7 mg/kg. Dosage recommendations may vary among countries and individual products (refer to specific product guidelines).

Parenteral
Infiltration anaesthesia
Adult: Available preparations:
Lidocaine 1% (10 mg) and epinephrine 1:200,000 (5 mcg) per mL solution for inj
Lidocaine 1.5% (15 mg) and epinephrine 1:200,000 (5 mcg) per mL solution for inj
Lidocaine 2% (20 mg) and epinephrine 1:200,000 (5 mcg) per mL solution for inj

Dose is individualised based on the procedure, degree and duration of anaesthesia required, vascularity of tissue and physical status of the patient. Max: Lidocaine 7 mg/kg. Dosage recommendations may vary among countries and individual products (refer to specific product guidelines).
Child: Infants, children and adolescents Dose is individualised based on the age and weight, procedure, degree and duration of anaesthesia required, vascularity of tissue and physical status of the patient. Max: Lidocaine 7 mg/kg. Dosage recommendations may vary among countries and individual products (refer to specific product guidelines).
Hướng dẫn pha thuốc
Available concentrations may be diluted with 0.9% NaCl inj to obtain the required final concentration.
Chống chỉ định
Hypersensitivity to lidocaine or other anaesthetics of the amide type, para-amino benzoic acid (PABA) and epinephrine.
Thận trọng
Patient with hypovolaemia; G6PD deficiency, congenital or idiopathic methaemoglobinaemia, exposure to oxidizing agents or their metabolites, bradycardia, severe shock, heart block, impaired CV or respiratory function, diabetes, poorly controlled hyperthyroidism; neurological disease, spinal deformities, septicaemia, and severe hypertension (if used as epidural anaesthesia). Debilitated and acutely ill patients. Hepatic or severe renal impairment. Children. Pregnancy and lactation. Not intended for intravascular inj. Use with caution in areas of the body supplied by end arteries or having otherwise compromised blood supply and when there is inflammation and/or sepsis in the region of the proposed inj.
Tác dụng không mong muốn
Significant: Cardiac depression (e.g. hypotension, bradycardia); CNS toxicity (e.g. dizziness, blurred vision, tinnitus, tremors, drowsiness, restlessness, anxiety, or depression).
Cardiac disorders: Rarely, arrhythmia.
Gastrointestinal disorders: Nausea, vomiting.
Nervous system disorders: Paraesthesia.
Vascular disorders: Hypertension.
Potentially Fatal: Methaemoglobinaemia. Rarely, cardiac or respiratory arrest, anaphylaxis.
Thông tin tư vấn bệnh nhân
This drug may temporarily impair mental alertness or locomotion; if affected, do not drive or operate machinery.
Chỉ số theo dõi
Monitor CV and respiratory vital signs and state of patient's consciousness constantly. Perform ECG during administration of test dose. Monitor for signs and symptoms of methaemoglobinaemia (e.g. cyanosis, headache, rapid pulse, shortness of breath, light-headedness, fatigue) and CNS toxicity.
Quá liều
Symptoms: Apnoea, convulsions, circulatory depression which if not treated immediately can result in hypoxia, acidosis, bradycardia, arrhythmia and cardiac arrest. Management: Maintain patent airway. If ventilation is inadequate, provide assisted or controlled ventilation with oxygen and a delivery system capable of permitting immediate positive airway pressure by mask. Evaluate adequacy of circulation. Should convulsions persist despite adequate respiratory support, and if the status of the circulation permits, an ultra-short acting barbiturate (e.g. thiopental, thiamylal) or a benzodiazepine (e.g. diazepam) may be administered in small increments intravenously. Supportive treatment for circulatory depression (e.g. administration of fluids and/or vasopressor [e.g. ephedrine]). If cardiac arrest should occur, perform standard CPR. If prolonged ventilatory support is needed or if there is difficulty in the maintenance of a patent airway, endotracheal intubation may be indicated.
Tương tác
Epinephrine: Enhanced vasopressor effect with MAOIs, TCAs, non-selective β-blockers (e.g. propranolol). Diminished vasoconstricting effect with butyrophenones (e.g. haloperidol) and phenothiazines (e.g. promethazine). Concomitant use with ergot-type oxytocic agents may result in severe, persistent hypertension and possibly cerebrovascular and cardiac accidents. Increased risk of serious cardiac arrythmias with inhalational anaesthetics (e.g. halothane, enflurane).
Lidocaine: Enhanced adverse effect with other local anaesthetics. Increased serum concentration with amiodarone. Reduced clearance with cimetidine and β-blockers.
Tác dụng
Description: Lidocaine is an amide-type local anaesthetic. It stabilises the neuronal membrane by blocking the ionic fluxes required for the initiation and conduction of impulses thereby effecting local anaesthetic action.
Epinephrine is a sympathomimetic agent. It increases the duration of lidocaine by causing vasoconstriction which slows the vascular absorption of lidocaine.
Synonym: lignocaine + adrenaline.
Onset: Dental: ≤2-4 minutes.
Duration: Dental: Approx 2.5 hours (infiltration); 3-3.5 hours (nerve block); dose and anaesthetic procedure dependent.
Pharmacokinetics:
Absorption: Lidocaine: Readily absorbed from inj site.
Distribution: Lidocaine: Rapidly and widely distributed into highly perfused tissues and further redistributed into skeletal muscle and adipose tissue. Crosses the blood-brain and placental barrier; enters breast milk. Plasma protein binding: Concentration-dependent (1-4 mcg/mL: 60-80%, mainly to α1-acid glycoprotein).
Epinephrine: Crosses the placenta.
Metabolism: Lidocaine: Rapidly metabolised in the liver mainly by CYP1A2 and CYP3A4 into active metabolites, monoethylglycinexylidide and glycinexylidide. Undergoes extensive first-pass metabolism.
Epinephrine: Metabolised by MAO and COMT in the adrenergic neuron. Circulating drugs are metabolised in the liver.
Excretion: Lidocaine: Via urine (90% as metabolites, <10% as unchanged drug). Elimination half-life: 1.5-2 hours.
Epinephrine: Via urine (mainly as inactive metabolites [e.g. metanephrine, and sulfate and hydroxy derivatives of mandelic acid]; small amounts as unchanged drug).
Đặc tính

Chemical Structure Image
Lidocaine

Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 3676, Lidocaine. https://pubchem.ncbi.nlm.nih.gov/compound/Lidocaine. Accessed Sept. 29, 2020.


Chemical Structure Image
Epinephrine

Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 5816, Epinephrine. https://pubchem.ncbi.nlm.nih.gov/compound/Epinephrine. Accessed Sept. 24, 2021.

Bảo quản
Store between 20-25°C or 2-8°C, depending on the product used. Storage recommendations may vary among countries or individual products. Protect from light. Refer to specific product guidelines.
Phân loại MIMS
Thuốc gây mê-gây tê
Phân loại ATC
N01BB52 - lidocaine, combinations ; Belongs to the class of amides. Used as local anesthetics.
S01EA51 - epinephrine, combinations ; Belongs to the class of sympathomimetics used in the treatment of glaucoma.
Tài liệu tham khảo
Anon. Adrenaline [Epinephrine] (Systemic). Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 20/08/2021.

Anon. Lidocaine (Systemic). Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 20/08/2021.

Anon. Lidocaine and Adrenaline (Epinephrine). Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 20/08/2021.

Buckingham R (ed). Adrenaline. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 20/08/2021.

Buckingham R (ed). Lidocaine. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 20/08/2021.

Dentsply Sirona (N.Z.) Limited. 2% Xylocaine Dental with Adrenaline (Epinephrine) 1:80,000 Injection data sheet 11 December 2018. Medsafe. http://www.medsafe.govt.nz. Accessed 20/08/2021.

Henry Schein Regional Limited. Henry Schein Lidocaine HCl 2% and Epinephrine 1:100,000 Solution for Injection data sheet 4 June 2019. Medsafe. http://www.medsafe.govt.nz. Accessed 20/08/2021.

Lidocaine Hydrochloride and Epinephrine (Hospira, Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 20/08/2021.

Xylocaine 2% with Adrenaline 1:200,000 (Aspen Pharma Trading Limited). MHRA. https://products.mhra.gov.uk. Accessed 20/08/2021.

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