Long-acting Insulin Analogs
These pages are best viewed with Netscape version 3.0 or higher or Internet Explorer version 3.0 or higher. When viewed with other browsers, some characters or attributes may not be rendered correctly. ORIGINAL ARTICLE Ralf H. Rosskamp, MD Glen Park, PHARMD, FCCP Once daily injection of existing intermediate/long-acting insulin preparations does not provide a 24-h basal insulinemia in most patients. High variability, pronounced insulin peaks, and (as a result) a high risk of nocturnal hypoglycemia only poorly simulate normal physiology. One principle to prolong insulin action is the shift of the isoelectric point of insulin towards neutral. One example is HOE 901, which shows in healthy volunteers a constant peakless profile over the entire 24-h clamp period. In 4-week trials in comparison to NPH insulin, significant lower fasting plasma glucose levels were achieved with lower rates of nocturnal hypoglycemia. Another principle to prolong insulin action is the use of soluble fatty acid acylated insulins that are bound to albumin after absorption. The combination of long- and short-acting insulins might provide the tools towards the final goal of achieving sustained normoglycemia in diabetic patients. Diabetes Care 22 (Suppl. 2):B109–B113, 1999 Initially, treatment with insulin consisted of subcutaneous injections shortly before meals (1). However, to avoid multiple injections, a number of attempts were made early on to prolong the duration of action by using substances to retard absorption, e.g., gum arabic (1923), lecithin (1923) or oil suspensions (1925) (2). These attempts failed mainly because of poor stability or side effects at the local injection site. The first successful insulin preparation with a prolonged action was protamine insulin (3). The principle of pr Continue reading >>
Types Of Insulin
Insulin analogs are now replacing human insulin in the US. Insulins are categorized by differences in onset, peak, duration, concentration, and route of delivery. Human Insulin and Insulin Analogs are available for insulin replacement therapy. Insulins also are classified by the timing of their action in your body – specifically, how quickly they start to act, when they have a maximal effect and how long they act.Insulin analogs have been developed because human insulins have limitations when injected under the skin. In high concentrations, such as in a vial or cartridge, human (and also animal insulin) clumps together. This clumping causes slow and unpredictable absorption from the subcutaneous tissue and a dose-dependent duration of action (i.e. the larger dose, the longer the effect or duration). In contrast, insulin analogs have a more predictable duration of action. The rapid acting insulin analogs work more quickly, and the long acting insulin analogs last longer and have a more even, “peakless” effect. Background Insulin has been available since 1925. It was initially extracted from beef and pork pancreases. In the early 1980’s, technology became available to produce human insulin synthetically. Synthetic human insulin has replaced beef and pork insulin in the US. And now, insulin analogs are replacing human insulin. Characteristics of Insulin Insulins are categorized by differences in: Onset (how quickly they act) Peak (how long it takes to achieve maximum impact) Duration (how long they last before they wear off) Concentration (Insulins sold in the U.S. have a concentration of 100 units per ml or U100. In other countries, additional concentrations are available. Note: If you purchase insulin abroad, be sure it is U100.) Route of delivery (whether they a Continue reading >>
How To Use Long-acting Insulin: Types, Frequency, Peak Times, And Duration
Long-acting insulin can help to stabilize blood sugar levels throughout the day, with only one or two shots. Fast-acting insulin replaces the surge of insulin that a healthy pancreas would release at mealtime. In contrast, long-acting insulin mimics the low-level flow of insulin normally released between meals and overnight. In this way, long-acting insulin works to establish a healthy baseline blood sugar level for the body to work around. Contents of this article: Using long-acting insulin Long-acting insulin cannot be delivered in pill form because it would be broken down in the stomach. Instead, it must be injected into the fatty tissue under the skin. From here, it can be gradually released into the bloodstream. Delivery methods According to the National Institute of Diabetes and Digestive and Kidney Diseases, there are a few ways to deliver long-acting insulin. These include: Needle and syringe: a dose of insulin is drawn from a vial into a syringe. Different types of insulin must not be mixed in the same syringe. Pen: this can be loaded with a cartridge containing a premeasured dose, or prefilled with insulin and discarded after use. Injection port: a short tube is inserted into the tissue beneath the skin. Insulin can be delivered using either a syringe or a pen. This only requires the skin to be punctured when the tube needs to be replaced. Injection sites Long-acting insulin can be injected into the abdomen, upper arms, or thighs. Abdomen injections deliver insulin into the blood most quickly. The process takes a little more time from the upper arms, and it is even slower from the thighs. It is important to stay consistent with the general injection area, but the exact injection site should be rotated frequently. Repeat injections at the same spot on the skin Continue reading >>
Long-acting Insulin: How It Works
When you eat, your pancreas releases a hormone called insulin. Insulin moves sugar (glucose) from your blood to your cells for energy or storage. If you take insulin, you may need some at mealtime to help lower your blood sugar after you eat. But even between meals, you need insulin in small amounts to help keep blood sugar stable. This is where long-acting insulin comes in. If you have diabetes, either your pancreas can’t produce enough (or any) insulin, or your cells can’t use it efficiently. To control your blood sugar, you need to replace or supplement the normal function of your pancreas with regular insulin injections. Insulin comes in many types. Each type differs in three ways: onset: how quickly it starts working to lower your blood sugar peak: when its effects on your blood sugar are strongest duration: how long it lowers your blood sugar According to the U.S. Food and Drug Administration (FDA), the five types of insulin are: Rapid-acting insulin: This type starts to work just 15 minutes after you take it. It peaks within 30 to 90 minutes, and its effects last for three to five hours. Short-acting insulin: This type takes about 30 to 60 minutes to become active in your bloodstream. It peaks in two to four hours, and its effects can last for five to eight hours. It is sometimes called regular-acting insulin. Intermediate-acting insulin: The intermediate type takes one to three hours to start working. It peaks in eight hours and works for 12 to 16 hours. Long-acting insulin: This type takes the longest amount of time to start working. The insulin can take up to 4 hours to get into your bloodstream. Pre-mixed: This is a combination of two different types of insulin: one that controls blood sugar at meals and another that controls blood sugar between meals. Lo Continue reading >>
Insulin Preparations With Prolonged Effect.
Diabetes Technol Ther. 2011 Jun;13 Suppl 1:S5-14. doi: 10.1089/dia.2011.0068. Insulin preparations with prolonged effect. Diabetes Research Unit, Cardiff University, University Hospital Llandough, Penarth, United Kingdom. [email protected] The discovery of insulin and its clinical application early in the last century dramatically improved the prospects of people with diabetes. However, the limitations of those initial, unmodified insulin preparations were quickly recognized; most notably, their relatively "short action" meant that multiple daily subcutaneous injections were required. This stimulated a concerted effort to modify the properties of insulin in order to extend the duration of its blood glucose-lowering effect, minimize dosing frequency, and decrease the burden of treatment. The first successful attempts to prolong insulin's action were achieved by modifying its formulation with additives such as protamine and zinc, culminating in the production of "intermediate-acting" neutral protamine Hagedorn (NPH) insulin in the 1940s and the lente family of insulins in the 1950s. However, NPH and lente insulins were still associated with several limitations, including considerable variability of effect and a pronounced peak in their time-action profile. In the 1980s, the focus of research moved toward the modification of insulin itself with the aim of producing a "long-acting" insulin that would better satisfy basal insulin requirements over the entire day. Once-daily insulin glargine was the first "long-acting" insulin analog in clinical practice, followed by once- or twice-daily insulin detemir and, more recently, insulin degludec, which is now being evaluated for administration at less frequent intervals. These analogs demonstrate several benefits over "intermediate Continue reading >>
Insulin Actions Times And Peak Times
A good way to improve your glucose levels is to track the peaks and drops in your glucose , so you can figure out why they happened and how to correct them. Once you identify glucose patterns (they ARE there!), you also want to understand when each of your insulins is active and when they typically stop lowering your glucose. This helps you adjust your doses or food intake to stop unwanted ups and downs in your readings. The table below shows the start, peak, and end times for various insulins with some explanations and typical uses for each. When Does My Insulin Peak and How Long Does It Last? designed to peak, covers meals and lowers high BGs Humalog , Novolog and Apidra insulins currently give the best coverage for meals and help keep the glucose lower afterward. Their glucose lowering activity starts to work about 20 minutes after they are taken, with a gradual rise in activity over the next 1.75 to 2.25 hours. Their activity gradually falls over the next 3 hours with about 5 to 6 hours of activity being common with these insulins.Although insulin action times are often quoted as 3-5 hours, the actual duration of insulin action is typically 5 hours or more. See our article Duration of Insulin Action for more information on this important topic. In general, "rapid" insulins are still too slow for many common meals where the glucose peaks within an hour and digestion is complete within 2-3 hours. The best kept secret on stopping post meal spiking is to eake the injection or bolus earlier before the meal and to eat slower low glycemic carbs. Regular insulin still carries its original name of "fast insulin" but its slower action often works better for people who take Symlin or for those who have gastroparesis (delayed digestion). It is also a great choice for those who Continue reading >>
Lantus
Lantus analog by Aventis long-acting new molecular entity U100 Special-pH 4 Action in dogs: onset inconsistent, peak 0.5 to 6 hours, inconsistent, duration about 13hr but inconsistent-beef/pork PZI has longer duration (10-16 h as per Nelson) [1][2][3] Line: Aventis Also known as: Glargine (generic) Similar to: Use and Handling: Shelf Life: 24 months Type: clear When Opened: 28 days at room temp, up to 6 months when stored in the refrigerator (2C to 8C) In Pen: 28 days at room temp. Notes: Protect from light and heat Do Not Freeze, do not refrigerate after opening Do not refrigerate in use cartridges Do not use intravenously [4] Do not use intramuscularly [5] Do not mix with other insulins Do not dilute do not prefill syringe discard if precipitate or cloudiness is seen. Lantus is the brand name for insulin glargine, an insulin analog made by Aventis [6]. Lantus is a very long-acting insulin (lasting up to 24 hours in humans) that uses pH reactions to form micro-precipitates under the skin, which create a time-release action. Dogs normally do not fare well with Lantus. [7][2][8][9] Using it for them can mean using the Lantus as a basal insulin with rapid or fast-acting insulins like Humulin R,Novolin R, Novolog [10] or Humalog as bolus insulin, given at mealtimes. This is how insulin-dependent people use it too. Most dogs receive insulin injections twice a day. Using Lantus would possibly double the number of needed daily injections because of the need for the faster-acting insulin at each meal. Dr. Rand participated in a study [1] on the effects of Lantus on dogs. The same 9 healthy dogs were tested with Lantus, beef/pork PZI and porcine (pork) lente insulin. It was concluded that Lantus does not lower blood glucose reliably in dogs; there was no consistent peak time or Continue reading >>
Long-acting Insulins
Rapid-Acting Analogues Short-Acting Insulins Intermediate-Acting Insulins Long-Acting Insulins Combination Insulins Drug UPDATES: TRESIBA ®- insulin degludec injection [Drug information / PDF] Click link for the latest monograph Dosing: Click (+) next to Dosage and Administration section (drug info link) Initial U.S. Approval: 2015 Mechanism of Action: The primary activity of insulin, including TRESIBA, is regulation of glucose metabolism. Insulin and its analogs lower blood glucose by stimulating peripheral glucose uptake, especially by skeletal muscle and fat, and by inhibiting hepatic glucose production. Insulin also inhibits lipolysis and proteolysis, and enhances protein synthesis. TRESIBA forms multi-hexamers when injected into the subcutaneous tissue resulting in a subcutaneous insulin degludec depot. The protracted time action profile of TRESIBA is predominantly due to delayed absorption of insulin degludec from the subcutaneous tissue to the systemic circulation and to a lesser extent due to binding of insulin-degludec to circulating albumin. INDICATIONS AND USAGE: TRESIBA is indicated to improve glycemic control in adults with diabetes mellitus. Limitations of Use TRESIBA is not recommended for the treatment of diabetic ketoacidosis. Dosing: Individualize dose based on type of diabetes, metabolic needs, blood glucose monitoring results and glycemic control goal. Rotate injection sites to reduce the risk of lipodystrophy. Do not dilute or mix with any other insulin or solution. Administer subcutaneously once daily at any time of day. Do NOT perform dose conversion when using the TRESIBA U-100 or U-200 FlexTouch pens. The TRESIBA U-100 and U-200 FlexTouch pens dose window shows the number of insulin units to be delivered and NO conversion is needed. HOW SUPPLIE Continue reading >>
Selected Important Safety Information
Tresiba® is contraindicated during episodes of hypoglycemia and in patients with hypersensitivity to Tresiba® or one of its excipients Never Share a Tresiba® FlexTouch® Pen Between Patients, even if the needle is changed. Sharing poses a risk for transmission of blood-borne pathogens Monitor blood glucose in all patients treated with insulin. Changes in insulin may affect glycemic control. These changes should be made cautiously and under medical supervision. Adjustments in concomitant oral anti-diabetic treatment may be needed Hypoglycemia is the most common adverse reaction of insulin, including Tresiba®, and may be life-threatening Tresiba® (insulin degludec injection) is indicated to improve glycemic control in patients 1 year of age and older with diabetes mellitus. Tresiba® is not recommended for treating diabetic ketoacidosis or for pediatric patients requiring less than 5 units of Tresiba®. Tresiba® is contraindicated during episodes of hypoglycemia and in patients with hypersensitivity to Tresiba® or one of its excipients Never Share a Tresiba® FlexTouch® Pen Between Patients, even if the needle is changed. Sharing poses a risk for transmission of blood-borne pathogens Monitor blood glucose in all patients treated with insulin. Changes in insulin may affect glycemic control. These changes should be made cautiously and under medical supervision. Adjustments in concomitant oral anti-diabetic treatment may be needed Hypoglycemia is the most common adverse reaction of insulin, including Tresiba®, and may be life-threatening. Increase monitoring with changes to: insulin dose, co-administered glucose lowering medications, meal pattern, physical activity; and in patients with hypoglycemia unawareness or renal or hepatic impairment Accidental mix-ups betwe Continue reading >>
Is Newly Approved Tresiba The Best Long-acting Insulin?
Comparing long-acting insulins? Newly approved Tresiba may come out ahead. With the exception of NPH insulin (the original long-acting insulin—examples include Humulin N and Novolin N), they are all going to cost you. So, if you are already paying big bucks for your long-acting insulin, here are some things to think about: What does a long-acting or basal insulin do for me? This is your baseline insulin, the insulin that is secreted to control your sugars when you are not eating (in the fasting state). Put another way, basal Insulin is used to suppress liver glucose production and help you maintain normal sugars even when you aren’t eating. What are my options? The old-school and well respected NPH insulin has been around forever and is considered intermediate acting. Levemir and Lantus were then joined this year by Toujeo and now Tresiba as the main players. Toujeo is basically Lantus (which was losing its patent) and may not gain any traction in the market. These insulins are typically administered once daily to provide basal insulin levels. Basaglar was just approved by the FDA and think of Basaglar as the Lantus “generic” or copycat–that will be available soon and let’s hope it’s cheaper than Lantus. What is Tresiba? Tresiba (insulin degludec) is the longest acting insulin available and there don’t appear to be any coming down the pipeline that give this duration of coverage. What makes Tresiba a hero is the long duration of action (>40 hours) with less fluctuation in blood levels of the drug. It’s given once a day. Is Tresiba the best long-acting insulin? This can only be answered on an individual basis and along with your provider. Lantus, Levemir and Tresiba may have some modest advantages over NPH (less symptomatic and nighttime hypoglycemia) i Continue reading >>
Insulin Analog
Sujoy Ghosh MD(General Medicine) DM(Endocrinology) MRCP(UK) MRCPS(Glasgow), Andrew Collier BSc MD FRCP(Glasgow & Edinburgh), in Churchill's Pocketbook of Diabetes (Second Edition), 2012 Basal insulin analogues Basal insulin analogues appear to offer no clinically significant improvement in glycaemic control, but are associated with fewer severe hypoglycaemic episodes, particularly nocturnal episodes. Insulin detemir is associated with less weight gain than neutral protamine Hagedorm (NPH) insulin, but many individuals require twice-daily dosing. Basal insulin analogues appear to offer greater patient satisfaction but no clear change in quality of life. Tip box Basal insulin analogues should be used in adults with type 1 diabetes who are experiencing severe or nocturnal hypoglycaemia. In type 1 diabetic patients who are not experiencing severe or nocturnal hypoglycaemia, NPH insulin could be considered. Drug-induced hypoglycaemia Insulin, insulin analogues or insulin secretagogues (sulfonylureas and meglitinides) are by far the most common causes of hypoglycaemia. Precipitating factors are restricted carbohydrate intake and liver and renal impairment. Sulfonylurea drugs can cross the placental barrier and stimulate insulin secretion in the fetus. Life-threatening hypoglycaemia has been reported in newborn infants of diabetic mothers who were treated with chlorpropamide during the third trimester. Sulfonylurea-induced hypoglycaemia may be prolonged, especially in those with renal impairment, lasting for up to seven days and necessitating continuous treatment. Mortality is high, ranging from 7.5 to 8.4%, and in attempted suicide with sulfonylurea drugs, the mortality is even higher with seven deaths out of 20 reported cases. Salicylate overdose has been associated with hyp Continue reading >>
Effect Of Switching Basal Insulin Regimen To Degludec On Quality Of Life In Japanese Patients With Type 1 And Type 2 Diabetes Mellitus
Effect of switching basal insulin regimen to degludec on quality of life in Japanese patients with type 1 and type 2 diabetes mellitus Maintainance of a stable basal insulin level is important for glycemic control in treatment of diabetes mellitus. Recently introduced insulin degludec has the longest duration of action among basal insulin formulations. The purpose of this study was to assess changes in quality of life (QOL) associated with switching the basal insulin regimen to degludec in patients with type 1 and type 2 diabetes mellitus. This 24-week open-label intervention study included type 1 (n = 10) and type 2 (n = 20) diabetes mellitus patients, with adequately controlled hemoglobin A1c (HbA1c), who had received insulin glargine or detemir for at least 6months. The primary outcome was change of QOL from baseline, as assessed by the Diabetes Therapy-Related QOL (DTR-QOL) application, after switching from glargine or detemir to degludec. HbA1c and other parameters were also assessed as secondary outcomes. QOL and HbA1c in patients with type 1 diabetes mellitus were unchanged during this study. In patients with type 2 diabetes mellitus, HbA1c did not change, but total DTR-QOL score was significantly improved from baseline after switching to degludec. The DTR-QOL Factor 2, Anxiety and dissatisfaction with treatment, was significantly improved in patients with type 2 diabetes mellitus and especially in the subgroup receiving basal supported oral therapy (BOT). Switching of the basal insulin regimen from glargine or detemir to degludec significantly improved the QOL of patients with type 2 diabetes mellitus who were receiving BOT, by reducing mental stress or anxiety about their treatment. DegludecGlargineDetemirHbA1cDTR-QOLQOLBOT Strict glycemic control is important Continue reading >>
Kaplan Endocrine System A
The nurse recognizes which symptoms are characteristic of impending diabetic ketoacidosis? Hot, dry, flushed skin, excessive thirst, rapid pulse. The nurse monitors the client diagnosed with type 1 diabetes. The client tells the nurse, "I jog 30 minutes every day but today after my jog I felt nervous, hungry, and had tremors." Which statement by the nurse is best? You should eat cheese and crackers prior to jogging. The nurse cares for a client diagnosed with a syndrome of inappropriate antidiuretic hormone (SIADH). The nurse is most concerned if which is observed? The nurse cares for a client immediately after a thyroidectomy. It is most important for the nurse to contact the health care provider if which is observed? It is important for the nurse to monitor a client with Addison's disease for the development of which condition? The nurse identifies the treatment of choice for severe ketoacidosis in a conscious person in which? The nurse cares for a client with diagnosed with diabetes insipidus. The health care provider prescribes vasopressin. The nurse determines that the medication is effective if which observation is made? A client diagnosed with type 1 diabetes asks the nurse why "a pill" for diabetes can't be taken. Which best describes the action of oral hypoglycemic agents? They stimulate beta cells in the pancreas to release endogenous insulin. The nurse understands that which statement best describes the action of glucocorticoids? the nurse knows that a blood sugar level of 40 mg/dL indicates which condition? On the day of discharge, the client newly diagnosed with type 1 diabetes says to the nurse, "Tell me again, what should I do if I develop a fever?" Which response by the nurse is best? A client is evaluated in the outpatient clinic for hypothyroidism. Th Continue reading >>
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Type I Diabetes Flashcards | Quizlet
INSULIN-DEPENDENT DIABETES MELLITUS (IDDM)....is totally dependant on insulin and accounts for 10% of total diabetics What is another name for Type I diabetes? Type 1 diabetes results from the autoimmune destruction of the ________________. There is a significant diminished insulin output ______________ is the only effective drug in treating Type 1 diabetes. ___________ is a polypeptide that stimulates anabolic processes in muscle, liver and fat cells. It binds to cell-surface receptor to initiate signal propagation within the cell. 1. Regular Insulin (Onset 30-60 mins) (Duration 8-10 hours) 2. NPH Insulin (neutral protamine Hagedorn) (Onset 2-4 hours) (Duration 12-18 hours) 3. Zinc Insulin (Lente) (Onset 2-4 hours) (Duration 12-20 hours) 4. Extended Zinc Insulin (Ultralente) (Onset 6-10 hours) (Duration 18-24 hours) What are the four Standard Insulin preparations and their onset and duration times? TYPE I DIABETES/INSULIN-DEPENDENT DIABETES MELLITUS (IDDM) _______________ occurs when circulating insulin concentrations decline or when target cells in tissues become resistant to the hormone. TRUE! (the pancreas cannot make the insulin since the beta cells are damaged...so they have to be given insulin since the endogenous insulin is not being produced) T or F? We consider type I diabetes to be an autoimmune disease that results from the autoimmune destruction of the pancreatic beta cells. Type I diabetes results from the autoimmune destruction of the _________________. What are the onset and duration times for Regular Insulin? What are the onset and duration times for NPH Insulin (neutral protamine Hagedorn)? What are the onset and duration times for Zinc Insulin (Lente)? What are the onset and duration times for Extended Zinc Insulin (Ultralente)? Extended Zinc Insulin Continue reading >>
Insulin Types
Types of Insulin Insulin types are discussed in the table below. [1] Table 1. Insulin Types (Open Table in a new window) Insulin Type Onset Peak Duration Ultra short acting: insulin lispro, insulin aspart, insulin glulisine Usually taken before a meal to cover the blood glucose elevation from eating Used with longer-acting insulin 12-30 min 0.5-3 hr 3-5 hr Short acting: regular insulin Usually taken about 30 minutes before a meal to cover blood glucose elevation from eating Used with longer-acting insulin 30 min 2.5-5 hr 4-24 hr Intermediate acting: insulin NPH Covers the blood glucose elevations when rapid-acting insulins stop working Often combined with rapid- or short-acting insulin and usually taken twice a day 1-2 hr 4-12 hr 14-24 hr Long acting: insulin glargine, ultralente insulin, insulin detemir Often combined, when needed, with rapid- or short-acting insulin Lowers blood glucose levels when rapid-acting insulins stop working Taken once or twice a day 3-4 hr No defined peak ≥24 hr Continue reading >>
