Lidocaine + Adrenaline Pharmacology
Lidocaine + Adrenaline
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%
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.
2.Muscle twitching
3.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)
4.Transient effect on auditory system of neonate
5.Erythema
6.Pigmentation
7.Pain
8.Headache
9.Palpitations
10.Local necrosis
11.Pulmonary oedema
12.Hyperglycaemia
13.Bradycardia
14.Reduced cardiac output
15.Anxiety
16.Epidural may cause hypotension, bradycardia, nausea and vomiting
17.Intraoral inj may cause stress reactions such as diaphoresis, palpitation, hyperventilation, generalised pallor and faintness
18.Topically: papules, burns, rash, skin irritation, burning sensation and blanching.
19.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.
20.Allergic reactions including anaphylactic symptoms and possibly life threatening asthmatic episodes in susceptible patients may occur due to sodium metabisulphate constituent.
21.Central nerve blocks may cause CV depression (especially in hypovolaemia).
22.Retrobulbar inj may reach subarachnoid space causing CV collapse, apnoea, convulsions, temporary blindness.
23.Paracervical block may cause foetal bradycardia/tachycardia (careful monitoring of foetal heart rate is necessary).
2.Hypertension
3.Cerebral arteriosclerosis
4.Ischaemic heart disease
5.IV admin
6.Anaesthetise digits or appendages
7.Myasthenia gravis
2.Impaired cardiac conduction
3.CHF
4.DM
5.Closed angle glaucoma
6.Impaired liver function (if site of admin is likely to result in high blood levels)
7.Severe renal dysfunction
8.Local anaesthetic effect may be reduced if injected into an inflamed or infected area.
9.Cerebrovascular insufficiency
10.Hyperthyroidism
11.Neonates
12.Patients in poor general condition (optimise patient's condition before major block),
2.Nerve blocks, epidural and caudal anaesthesia
2.Benzodiazepines & barbiturates raise the convulsive threshold to lidocaine
3.Vasopressors potentiate pressor effects of adrenaline
4.Bp may increase with non-selective ?-blockers
5.Tcas, halogenated inhalational anaesthetics and ?-blockers; general anaesthetics may increase sensitivity of myocardium to dysrhythmic effects of epinephrine
6.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
7.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
8.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.
9.Potentially fatal: possible additive cardiac effects with amiodarone (ecg monitoring should be considered).
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.
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.
Lidocaine
Adrenaline
Subcutaneous: 5 to 15minutes
Inhalation: Within 5 minutes
I.V.: Short
Subcutaneous: 1 to 4 hours
Inhalation: 1 to 3 hours
2.Hypertension
3.Tachycardia
4.Ventricular fibrillation
5.Shock
6.Anginal pain
7.ECG changes
8.Arrhythmias
9. Tremor
10.Nervousness
11.Headache
12.Vertigo
13.Disorientation
14.Agitation
15.Dizziness
16.Drowsiness
17.Fear
18.Weakness
19.Lightheadedness
20.Nervousness
21.Excitation
22.Dyspnoea
23.Nausea
24.Vomiting.
2.Shock other than anaphylactic shock,
3.Angle closure glaucoma,
4.Anaesthesia of extreamities,
5.During labour,
6.Cardiac dilatation,
7.Coronary insufficiency,
8.Organic brain damage,
9.Cerebral arteriosclerosis,
10.Arrhythmias,
11.Along general anaesthesia with halogenated hydrocarbons or cyclopropane.
2.Emphysema
3.Hyperthyroidism
4.Cardiovascular disease
5.Psychoneurosis
6.Diabetes
7.Parkinson`s disease(ophthalmic preparation)
2.Bronchodilator
3.Hypersensitivity reactions
4.Anaphylactic shock
5.To restore cardiac rhythm in cardiac arrest
6.Haemostasis
7.Prolong duration of anaesthesia
8.Nasal congestion
9.Open angle glaucoma.
Cardiac glycosides: May make cardiac arrhythmias more likely.
Ergot alkaloids and phenothiazines: May reverse the pressor effects of adrenaline.
Antihistamines: Pressor effect may be potentiated.
Halogenated hydrocarbon anaesthetics: Sensitise the myocardium to the effects of catecholamines leading to serious arrhythmias.
Oxytocic drugs: May cause severe persistent hypertension.
Sympathomimetic drugs: Additive effects and increased toxicity. May induce serious cardiac arrhythmias.
Tricyclic antidepressants: Pressor response may be potentiated.
Adults: Starts with 0.1 to 0.5mg (0.1 to 0.5ml of a 1: 1,000 solution) S.C. or I.M. Repeat as required at 10 to 15minute intervals. Alternatively 0.1 to 0.25mg (1 to 2.5ml of a 1: 10,000 solution) I.V.; slowly over 5 to 10 minutes. Repeated if required at every 5 to 15minutes or followed by 1 to 4mcg/minute I.V. infusion.
Children: 0.01mg/kg (0.01ml/kg of a 1: 1000 solution) S.C. Dose not to exceed 0.5mg. Repeated as required; at every 20 minutes to 4hour intervals. Alternatively 0.02 to 0.025 mg/kg (0.004 to0.005 mi/kg) of a 1:200 solution. Repeat if required but not to exceed than four times daily. Alternatively
To restore cardiac rhythm in cardiac arrest:
Starts with 0.5 to 1mg (5 to 10ml of 1: 10,000 solutions) diluted to 10ml and administered I.V. or intra cardiac. During resuscitation 0.5 to 1mg I.V. every 5minutes or injected through endotracheal tube. Administer 10ml containing 1ml adrenaline (0.1mg/ml) by 5 rapid insufflations directly in to the tube and followed by 5 rapid insufflations.
Adults: I.V.: 100mcg to 250mcg injected slowly.
Neonates: 0.01mg/kg
Infants: 50mcg initial dose repeated at 20 to 30 minutes intervals in asthma attacks.
Resuscitation for children and neonates: 0.iml/kg of 1: 10000solution I.V.
As a haemostatic agent:
Adults: 1: 50,000 to 1: 1000 applied topically.
To prolong local anaesthetic effect: 1:500000 to 1: 50000 mixed with local anaesthetic agent.
Intra spinal use: 0.2 to 0.4ml of 1: 2000 solutions added to anaesthetic fluid to prolong anaesthetic action.
Nasal congestion, local superficial bleeding: Instill 1 to 2 drops of solution.
Open angle glaucoma: 1 to 2 drops instill daily or twice daily.
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