The pharmacokinetics and pharmacodynamics of regular u500 insulin in health nonobese subjects regular u500 insulin is being regular u500 insulin is being used with increasing frequency in. Pharmacokinetic and pharmacodynamic properties of insulin. Another pk study in nine severely insulin resistant obese patients with type 2 diabetes total daily dose, 333 units demonstrated a brisk rise in serum insulin by 30 min and peak mean insulin levels at 5 h with persistent elevation of insulin levels at 7 h after a subcutaneous 100unit morning dose of u500r. Type of insulin lispro aspart glulisine intermediate. Insulin glargine lixisenatide soliqua 10033 high insulin. Because the names of the different drugs are often very similar novolin vs novalog it can difficult for emergency providers to keep all of the agents straight. Insulin aspart is a novel rapidacting insulin analogue with improved subcutaneous absorption properties when compared with soluble human insulin. In one study of the effect of albumin concentration on total and free phenytoin concentrations, free. Pharmacokinetics and pharmacodynamics of subcutaneous. The glp1 receptor agonist helps release insulin when blood glucose is high and lower the amount of glucose produced by the liver.
Some drugs, notably insulin, are routinely administered sc. The two basal insulin analogs, insulin glargine and insulin detemir, were developed to ameliorate the wellknown limitations of nph insulin. Pharmacokinetics and pharmacodynamics of therapeutic doses. Novolog mix 7030 70% insulin aspart protamine suspension and 30% insulin aspart injection, rdna origin is a human insulin analog suspension containing 70% insulin aspart protamine crystals and 30% soluble insulin aspart.
Use of insulin therapy in managing type 2 diabetes mellitus. Pharmacokinetics and pharmacodynamics of basal insulins. Diabetes medication pharmacology bja education oxford. The pharmacokinetics of insulin aspart have been studied in healthy caucasian and asianjapanese volunteers, in patients with type 1 and 2 diabetes mellitus, and in children with diabetes, with both pre and postprandial administration and during continuous subcutaneous insulin infusion. The pharmacokinetics and pharmacodynamics of regular u500. Pharmacokinetics pk and pharmacodynamics pd of oral. Rapid pharmacokinetics of intradermal insulin administered using microneedles in type 1 diabetes subjects. The pharmacokinetics of insulin comprise the absorption process, the distribution including binding to circulating insulin antibodies, if present, and to insulin receptors, and its ultimate. Insulin, which first became available for patients with diabetes mellitus in 1922 3,4, was originally extracted from porcine and bovine pancreases and differed in structure from human insulin by. The development of procedures for purifying and modifying insulin.
A study investigating the pharmacokinetic properties of. Insulin history, biochemistry, physiology and pharmacology shashank r. Pharmacokinetics pk and pharmacodynamics pd of oral insulin in healthy subjects objective. Pharmacokinetics of insulin fundamental pharmacology concepts in pharmacology. Following injection into subq tissue, neutralization of insulin glargine solution results in formation of microprecipitates from which the drug is slowly released. To evaluate the safety, pharmacokinetics and pharmacodynamics of oral insulin. Pharmacokinetics and pharmacodynamics of subcutaneous injection of longacting human insulin analog glargine, nph insulin, and ultralente human insulin and continuous subcutaneous infusion of insulin lispro mauro lepore, simone pampanelli, carmine fanelli, francesca porcellati, linda bartocci. Use of insulin therapy in managing type 2 diabetes mellitus continuing pharmacy education this continuing pharmacy education discussion guide is part of the educational initiative, individualization of insulin. Patients were free of any detectable microangiopathic complication and tested negative at the screening for autonomic neuropathy, as determined by a standard battery of cardiovascular tests 11. The distribution and metabolism of absorbed insulin follow that of endogenous insulin. Very few studies have investigated the pharmacokinetics and pharmacodynamics of nph insulin in type 2 diabetes 1,2. Insulin, a polypeptide hormone dissected from the pancreas, is substantially responsible for the uptake of glucose into the cells for its metabolization.
The pharmacokinetics of insulin comprise the absorption process, the distribution including binding to circulating insulin antibodies, if present, and to insulin receptors, and its ultimate degradation and excretion. The pharmacodynamic characteristics of the basal insulin analogues insulin detemir idet and insulin glargine iglar have been examined extensively via euglycaemic clamp studies. Pharmacokinetics and pharmacodynamics of subcutaneous injection of longacting human insulin analog glargine, nph insulin, and ultralente human insulin and continuous subcutaneous infusion of insulin. Since then, numerous formulations with various similar names have been produced and marketed. Insulin glargine pharmacokinetics absorption bioavailability. B 28 is replaced by aspartic acid mimics physiological insulin insulin. Comparison of pharmacokinetics and dynamics of the long. Basal insulin requirements are covered by injection of long acting insulin.
To make things even more fun the pharmacodynamics of insulin would change over time in a given person because of the formation of insulin antibodies that appeared over time. Another pk study in nine severely insulinresistant obese patients with type 2 diabetes total daily dose, 333 units demonstrated a brisk rise in serum insulin by 30 min and peak mean. Novolog mix 7030 is a blood glucoselowering agent with a rapid onset and an intermediate duration of action. To compare the pharmacokinetics dynamics of the longacting insulin analog glargine with nph, ultralente, and continuous subcutaneous sc infusion of insulin lispro continuous subcutaneous insulin. A comparison of pharmacodynamics and pharmacokinetics of. Pdf p9 pharmacokinetics of a rapidacting human insulin. P9 pharmacokinetics of a rapidacting human insulin analogue, insulin aspart, in children and adolescents with type 1 diabetes. The insulin helps glucose enter the cells to be used as fuel. This article evaluates and summarizes the pharmacokinetics and pharmacodynamics of insulin. Pharmacokinetics, pharmacodynamics, and pharmacogenomics. Pharmacokinetics of the rapidacting insulin analog. The objective of this study was to compare the pharmacokinetics and pharmacodynamics of insulin aspart ia, a rapidly acting insulin analog, with those of human soluble regular insulin hi.
Combines longacting insulin with a glp1 receptor agonist. Total insulin measures the sum of the antibodybound and the free insulin. Pharmacokinetics of insulin detemir in subjects with type 1 diabetes the safety and scientific validity of this study is the responsibility of the study sponsor and investigators. In this case, the presence of insulin binding antibodies can alter the pharmacokinetics of insulin and lead to an abnormal period of hyperglycemia in response to a delayed increase in the free fraction. For many drugs, the gastrointestinal absorption rate, but not the extent of. Recombinant human insulin analog preparations are currently the most effective therapy available for patients with diabetes who require insulin. Delayed insulin absorption would likely hinder the performance of closedloop systems. Pharmacokinetics of insulin aspart and glucagon in type 1. Modifications of the insulin molecule have resulted in two longacting insulin analogs glargine and detemir and three rapidacting insulin analogs aspart, lispro, and glulisine with improved pkpd profiles table 1. A comparison of pharmacodynamics and pharmacokinetics of insulin aspart, biasp70, biasp50 and fastacting human insulin the safety and scientific validity of this study is the.
Pharmacokinetics of insulin detemir in subjects with type. The study included 10 patients with type 2 diabetes who were treated with insulin. Pharmacology and disease management michael king, md assistant professor residency program director university of kentucky dept. Pharmacokinetics and pharmacodynamics of highdose human. The pharmacokinetics and pharmacodynamics of rapid. In the last 30 years, insulin pharmacology has been revolutionized by the introduction of recombinant dna technology and genetically engineered human insulin, which has replaced the animalderived insulin. These studies have provided valuable information that is limited, however, by a short period of observation 1216 h and by the comparison of nph with only one longacting insulin. The goal of prandial insulin therapy is to mimic the physiolog ical metabolic effect induced by endogenously secreted insu lin to limit postprandial glycemic excursions after a meal. Although the pharmacodynamics varied based on time, the pharmacokinetics of insulin glargine was not affected by administration time, reported francesca porcellati, md, of the university of perugia medical school in perugia, italy, and colleagues. Comparison of pharmacokinetics and dynamics of the longacting insulin analogs glargine and detemir at steady state in type 1 diabetes a doubleblind, randomized, crossover study francesca. In contrast to rapidacting analogs, which differ exclusively in terms of primary structure while sharing similar pharmacokinetics pk and pharmacodynamics pd, the two longacting insulin. Titration of insulin glargine u300 would result in less volume and a lower risk of hypoglycemia, compared with insulin glargine u100.
Reversing proline and lysine at b 28 and b 29 position quick acting, just before meals insulin aspart. Pharmacokinetic and pharmacodynamic properties of insulin aspart and human insulin 225 where it pmol l is the total serum insulin concentration, i b pmol l is the basal endogenous insulin concentration assumed to be constant, and v i l is the distribution volume for insulin. Insulin analogues recombinant dna technology, modified pharmacokinetic greater stability and consistency insulin lispro. Pharmacokinetics and pharmacodynamics of insulin analogs. Clinical pharmacokinetics and pharmacodynamics of insulin.
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