Plasma levels of lidocaine after intramuscular administration

Cohen, Lawrence S.; Rosenthal, James E.; Horner, Daniel W.; Atkins, James M.; Matthews, Oscar A.; Sarnoff, Stanley J.

doi:10.1016/0002-9149(72)90442-0

Cited by 59 publications

(16 citation statements)

References 11 publications

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“…Since only a small number of patients were saved by the treatment and there was an increase in spurious diagnosis of myocardial infarction in chest-pain victims, warnings were issued about overinterpretation. Taken together with a large study in Israel [31] on the early administration of lidocaine, this study [29] supports the concept that antiarrhythmic drugs may be prophylactic in the early phases of infarction before hospitalization when the likelihood of ventricular fibrillation is increased 10-to 15-fold. With increasing emphasis on early recognition of acute myocardial infarction because of the recommendation to administer thrombolytic therapy, patients are being seen with chest-pain syndromes at earlier times.…”

Section: Is Lidocaine Effective In Preventing Primary Ventricular Fibsupporting

confidence: 74%

Arrhythmia prophylaxis after acute myocardial infraction: A decade of controversy

Harrison

1989

Cardiovasc Drug Ther

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Primary ventricular fibrillation continues to be a major complication of acute myocardial infarction occurring in 5-9% of patients in the coronary care unit and in a higher percentage of pre-hospital admissions. Prophylactic anti-arrhythmic drugs can prevent primary ventricular fibrillation. Lidocaine has been used for this purpose and can be administered safely and effectively in most patients by following well-established programs based on pharmacokinetic and pharmacodynamic data. The in-hospital mortality for patients with primary ventricular fibrillation exceeds that of matched controls not having the arrhythmia, and many studies show a higher 1-, 3-, and 5-year mortality. Other studies have failed to confirm these long-term results and have produced controversy among cardiologists. I continue to recommend prophylactic antiarrhythmic drugs for all patients with acute infarction, especially in those undergoing early interventional therapy.

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Section: Is Lidocaine Effective In Preventing Primary Ventricular Fibsupporting

confidence: 74%

Arrhythmia prophylaxis after acute myocardial infraction: A decade of controversy

Harrison

1989

Cardiovasc Drug Ther

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“…Absorption from Intramuscular Sites Intramuscular administration of lignocaine results in rapid and effective antiarrhythmic action (Bellet et al 1971;Bernstein et al 1972;Cohen et al 1972;Fehmers & Dunning 1972;Ryden et al 1973). After intramuscular injection of lignocaine 200 to 300mg, peak concentrations averaging 2.2 to 3.2 mg/L are observed after 10 to 15 minutes, and plasma concentrations remain in the therapeutic range for 1 to 2 hours (Cohen et al 1972;Oltmanns et al 1982;Singh & Kocot 1976).…”

Section: Absorptionmentioning

confidence: 99%

“…After intramuscular injection of lignocaine 200 to 300mg, peak concentrations averaging 2.2 to 3.2 mg/L are observed after 10 to 15 minutes, and plasma concentrations remain in the therapeutic range for 1 to 2 hours (Cohen et al 1972;Oltmanns et al 1982;Singh & Kocot 1976). The inefficacy of intramuscular lignocaine in preventing ventricular fibrillation during the first 15 minutes after administration t6 patients with acute MI has been attributed to a delay in producing therapeutic plasma concentrations (Koster & Dunning 1985), although pharmacodynamic mechanisms may also have played a role (Nattel et al 1981).…”

Section: Absorptionmentioning

confidence: 99%

“…A larger intramuscular dose of lignocaine (4 to 6 mg/ kg, mean of 450mg) results in therapeutic concentrations within 5 minutes and a longer duration of action, but produces CNS toxicity in the majority of patients (Zener et al 1973). Various sites for intramuscular injection have been studied, and injection into the deltoid muscle results in the most rapid and reliable attainment of therapeutic concentrations (Cohen et al 1972;Schwartz et al 1974).…”

Section: Absorptionmentioning

confidence: 99%

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The Pharmacokinetics of Lignocaine and β-Adrenoceptor Antagonists in Patients with Acute Myocardial Infarction

Nattel

Gagne

Pineau

1987

Clinical Pharmacokinetics

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Lignocaine (lidocaine) and beta-adrenoceptor antagonists are widely used after acute myocardial infarction. The therapeutic value of these agents depends on the achievement and maintenance of safe and effective plasma concentrations. Lignocaine pharmacokinetics after acute myocardial infarction (MI) are controlled by a number of variables. The single most important is left ventricular function, which affects both volume of distribution and plasma clearance. Other major factors include bodyweight, age, hepatic function, the presence of obesity, and concomitant drug therapy. Lignocaine is extensively bound to alpha 1-acid glycoprotein, a plasma protein which is also an acute phase reactant. Increases in alpha 1-acid glycoprotein concentration occur after an acute MI, decreasing the free fraction of lignocaine in the plasma and consequently decreasing total plasma lignocaine clearance without altering the clearance of non-protein-bound lignocaine. Complex changes in lignocaine disposition occur with long term infusions, and therefore early discontinuation of lignocaine infusions (within 24 hours) should be undertaken whenever possible. Because the risk of ventricular tachyarrhythmia declines rapidly after the onset of an acute MI, lignocaine therapy can be rationally discontinued within 24 hours in most patients. Lignocaine has a narrow toxic/therapeutic index, so that pharmacokinetic factors are critical in dose selection. In contrast, beta-adrenoceptor antagonists' adverse effects are more related to the presence of predisposing conditions (such as asthma, heart failure, bradyarrhythmias, etc.) than to plasma concentration. The pharmacokinetics of beta-adrenoceptor antagonists are important to help assure therapeutic efficacy, to provide information about the anticipated time course of drug action, and to predict the possible role of ancillary drug effects (such as direct membrane action) and loss of cardioselectivity. Lipid solubility is the main determinant of the pharmacokinetic properties of a beta-adrenoceptor antagonist. Lipid-soluble agents like propranolol and metoprolol are well absorbed orally, and undergo rapid hepatic metabolism, with important presystemic clearance and a short plasma half-life. Water-soluble drugs like sotalol, atenolol, and nadolol are less well absorbed, and are eliminated more slowly by renal excretion. Clinical assessment of beta-adrenoceptor antagonism is more valuable than plasma concentration determinations in evaluating the adequacy of the dose of a particular beta-adrenoceptor antagonist.(ABSTRACT TRUNCATED AT 400 WORDS)

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“…Response levels to vaccination vary according to intramuscular injection site 2. Different responses depending on site have also been noticed for injections of antibiotics,3 insulin, and lignocaine 4…”

Section: Introductionmentioning

confidence: 99%

Intramuscular gluteal injections in the increasingly obese population: retrospective study

Nisbet¹

2006

BMJ

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As the practices selected were active in research, blood pressure control in these practices may be better than in the UK as a whole. Our analysis was based on the latest blood pressure recorded in the general practice records. This will have reflected several recordings of blood pressure in some cases and a single reading in other instances. This may have resulted in an overestimation of "true" blood pressure in this stroke population compared with measurements in the controlled setting of a study, but these are the readings on which management will be decided.Current national and international guidelines may give appropriate advice for the management of blood pressure of younger patients who have had a recent cerebrovascular event. Unfortunately, these guidelines may act as an impediment to further research. We would urge that further evidence should be collected on the efficacy and adverse effects of intensive blood pressure lowering in representative populations before we implement this guidance in primary care.Contributors: JM conceived and designed the study and analysed the data. RMcM assisted in the design and analysis and supervised the data collection from practices. RH was responsible for data collection. All authors contributed to the drafting of the paper. JM is the guarantor. AbstractAims To examine depth of subcutaneous fat at gluteal intramuscular injection sites. Design Retrospective study. Setting General hospital. Participants 100 consecutive adults who had computed tomography of the pelvis. Main outcome measures Minimum distance between the surface of the skin and the nearest edge of muscle at intramuscular injection sites.Results 12 patients had a ventrogluteal site depth of more than 35 mm, the maximum depth of a green needle, and 26 had a ventrogluteal depth of more than 25 mm, the maximum depth of a blue needle. 43 patients had a dorsogluteal site depth of more than 35 mm, and 72 had a dorsogluteal depth of more than 25 mm. The intramuscular site was likely to be deeper in women. Conclusion Standard green and blue needles do not reach the gluteal muscles in a considerable number of patients.

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Plasma levels of lidocaine after intramuscular administration

Cited by 59 publications

References 11 publications

Arrhythmia prophylaxis after acute myocardial infraction: A decade of controversy

Arrhythmia prophylaxis after acute myocardial infraction: A decade of controversy

The Pharmacokinetics of Lignocaine and β-Adrenoceptor Antagonists in Patients with Acute Myocardial Infarction

Intramuscular gluteal injections in the increasingly obese population: retrospective study

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