Insulin lispro – Drug class, mechanism of action, use, dosage and side effects

Insulin lispro - Drug class, mechanism of action, use, dosage and side effects

What is insulin lispro?

A recombinant human insulin analog produced in a laboratory strain of Escherichia coli, plasmid DNA transfected into the bacteria encodes for analogues of human insulin which may also have a lysine at residue B28 and proline at B29 is called as an insulin lispro. These residues are known to get reversed in endogenous human insulin. It is approved by FDA in 199 and a rapid-acting insulin lispro can be produced by reversal of amino acids (lysine at residue B28 and proline at B29).

Protein structure, molecular formula and weight of insulin lispro

Protein structure:

Protein structure, molecular formula and weight of insulin lispro

Protein chemical formula of insulin lispro: C257H387N65O76S6

Protein average weight: 5808.00 Da

What are the indications of insulin lispro?

Insulin lispro is indicated for the treatment of the diabetes mellitus of type 1 and type 2. This medication is used in conjunction with an intermediate or long-acting insulin. However, it should not be used with a continuous insulin infusion pump.

Mechanism of action of insulin lispro

The primary activity of insulin and insulin analogs is regulation of glucose metabolism, these insulin analogs include insulin lispro. Insulin acts by stimulating the peripheral glucose uptake by skeletal muscle and fat thereby lowering the blood glucose and by inhibiting the hepatic glucose production. Insulin enhances the protein synthesis and inhibit lipolysis and proteolysis.

Pharmacokinetics of insulin lispro

Insulin lispro is absorbed when administered subcutaneously. As compared to regular human insulin, it is absorbed more quickly. In healthy subjects, after 30 to 90 minutes of injection, it reaches peak plasma levels. The site of injection can also change the absorption of the medication. When compared with deltoid or thigh administration, the higher serum drug levels and shorter duration of action was found when administered in the abdomen. Bioavailability of this drug is 0.1 – 0.2 unit/kg = 55% – 77%.

The volume of distribution of this drug when administered intravenously as an injection in bolus form of 0.1 and 0.2 U/Kg dose in healthy subjects divided into two different groups. With an increase in dose, the mean volume of distribution of insulin lispro can be reduced. The metabolic degradation of this medication occurred by a receptor-mediated process and is also cleared in the same way. The elimination half-life of insulin lispro is known to be of 1 hour.

How long does insulin lispro stay in your system?

The elimination half-life of this medication is 1 hour and the elimination of a drug is equaled to 5 times to that of the half-life of the same drug. Therefore, insulin can be eliminated from your body in 5 to 6 hours completely.

Can insulin lispro can be taken in pregnancy?

This comes under a US FDA pregnancy category B which means that this drug is failed to show any risk or harm to the fetus in animals and there are no well-controlled studies are given in pregnant women. One should take this medication only when benefit outweighs the risk.  The monitoring of pregnant women is necessary while she is on this medication.

Can insulin lispro can be taken by nursing mother?

This insulin lispro and may another form of biosynthetic insulin (such as aspart, deteir, glargine, and glulisine) can be excreted into the human milk. If taken by mouth, insulin can be remain inactivated. And if absorbed, it would be destroyed in the digestive tract of the infant. In patients with type 1 diabetes, lactation onset occurs later and the delay is even longer when there is poor glucose control. However, in such diabetic mothers, lactation persists similar in normal mothers once established. In women who breastfeed, the requirements of insulin are generally lower due to glucose being used for milk production. The use is considered acceptable and it is known to be excreted in human milk. Dose adjustment in insulin dose may be required in pregnant women.

What are the side effects of insulin lispro?

Insulin lispro can cause some side effects also and one should not ignore such side effects and should contact the doctor immediately. The common side effects are:

  • Nose infection
  • Throat infection
  • Pain at the site of injection
  • Irritation at the site of injection
  • Joint pain
  • Itching or rashes
  • Weight gain
  • Swelling of lower limbs (legs, feet or ankles)

It can also some serious side effects, therefore one should consider immediate doctor consultation in such cases:

  • Low blood sugar
  • lower potassium levels
  • life-threatening allergic reactions
  • Serious anaphylactic reactions

What are the warnings of insulin lispro?

One should avoid the administration of the insulin lispro if:

  • You are allergic to insulin or any other ingredient present in its formulation.
  • If your blood sugar is very less.
  • You should never use your insulin (such as Humalog KwikPen, Insulin Pens, and Insulin cartridges) with any other person.
  • You should ask your doctor in case:
  • you have low blood sugar levels
  • you have low potassium levels in your blood
  • you have kidney or liver problems
  • you ever suffered from heart failure
  • you are taking thiazolidiones (TZDs) like rosiglitazone-containing drugs (such as Avandia, Avandryl, or Avandamet or Actos (pioglitazone), Actoplus Met, or Oseni

Insulin lispro can not be mixed with any other insulin product whereas any other insulin products can be mixed altogether. You should never mix insulin lispro with any other insulin product even if it comes automatically mixed.

What is the role of insulin lispro in diabetes?

Insulin lispro is similar to human insulin. It has more rapid onset and shorter duration of action as compared to human insulin. Due to this property, there is reduced the risk of hypoglycemia. It improves the dosing convenience for patients with diabetes and also it provides more effective and natural control of blood sugar concentrations. In the treatment of diabetes mellitus, insulin lispro proves a new and effective agent.

How should I use insulin lispro?

  • Always read the instructions carefully before taking the insulin lispro.
  • Do not share reusable pen or cartridges or even syringes with other people, even if the needle have been changed. This may cause serious infection to others and also you can get a serious infection from others.
  • Always follows your doctor’s instruction while you take this medicine.
  • Inject the insulin injection before of after 15 minutes of eating a meal because this medication start eating fast.
  • You should know the type and strength of insulin that you use, you should not change it, until and unless your doctor advise you to so.
  • You should check your blood sugar levels. Keep an eye by regular monitoring, and get the information about the exact level of sugar in the blood and also ask when you should check it.

What are the symptoms of insulin overdose?

You may have following symptoms if you have low blood sugar, therefore check these symptoms:

  • Confusion
  • Anxiety
  • Extreme hunger
  • Fatigue
  • Irritability
  • Sweating or clammy skin
  • Trembling hands

If your blood sugar levels continue to fall, you could have seizures or pass out.

What should be done in case of an insulin overdose?

You should not panic in case of insulin overdose, as this is the condition which can be treated at home. Just follow these steps:

  • In order to keep a record, you should check your blood sugar regularly.
  • In case of hypoglycemia, you can take a high sugar content form such as regular soda, sweetened fruit juice, eat a hard candy, tablets, gel or you can also have glucose paste.
  • Eat something shortly, if you skipped a meal. Your blood sugar can be raised by administering anything with 15 to 20 grams of carbohydrates.
  • Take some rest by taking a break.
  • Recheck your blood sugar after 15 or 20 minutes.If it’s still low, take another 15 to 20 grams of a quick-acting sugar, and eat something if you can.

What should I avoid while using insulin lispro?

Without first talking to your doctor or pharmacist, you should never change the brand of insulin lispro or syringe. You should also avoid drinking alcohol while using this medication. If you drink alcohol while taking insulin, your blood sugar may drop to dangerously low levels.

How to avoid mistakes during insulin lispro use?

You can administer insulin by the means of several things. It most often happens when you:

  1. Misread the syringes or vials, and it is very much common when you are unfamiliar with a new product.
  2. In case you use a wrong type of insulin, for example, you take 30 units of long-acting and 10 units of short-acting insulin. Moreover, there are chances of mixing them together.
  3. You should take insulin but avoid eating. These are the injections which are rapid and short-acting insulin injections that should be just taken before or after meals. After having the meals, your blood sugar levels increase. The administration of short-acting or rapid-acting insulin can lower your sugar to a dangerous level when you take it without eating.
  4. You should inject insulin in an arm or leg just before exercise because physical activity can change the absorption of insulin and can also lower your blood sugar levels. You should avoid injecting the injection at the site of exercise affected area.

Can insulin lispro be taken with furosemide?

The effectiveness of insulin lispro and other diabetic medications can be reduced by furosemide due to their interaction with each other. Yous should monitor your blood sugar closely. During and after treatment with diabetic medications, you may need a dose adjustment. Yous should also let your doctor know about all the other medications that you are already taking, even about vitamins or herbal medicines. Also, avoid stopping this medication without prior consultation with your doctor.

Can you take insulin lispro with metoprolol?

Risk, severity, and duration of hypoglycemia (low blood sugar) can be increased by beta-blockers in patients receiving insulin lispro and certain other anti-diabetic medications. Some symptoms such as tremor, palpitation and rapid heartbeat can be masked by beta blockers which make it more difficult to recognize an oncoming episode. Other symptoms may not be affected such as a headache, dizziness, drowsiness, nervousness, confusion, nausea, hunger, weakness, and perspiration. You may need to monitor your blood glucose levels more frequently, especially if you are prone to developing hypoglycemia. It is important to tell your doctor about all other medications you use, including vitamins and herbs. Do not stop using any medications without first talking to your doctor.

Can you take aspirin with insulin lispro?

Using aspirin together with insulin or certain other diabetes medications may increase the risk of hypoglycemia, or low blood sugar. Symptoms of hypoglycemia include a headache, dizziness, drowsiness, nervousness, confusion, tremor, nausea, hunger, weakness, perspiration, palpitation, and rapid heartbeat. Talk to your doctor if you have any questions or concerns. You may need a dose adjustment or more frequent monitoring of your blood sugar to safely use both medications. It is important to tell your doctor about all other medications you use, including vitamins and herbs. Do not stop using any medications without first talking to your doctor.

Can I drink alcohol during insulin lispro use?

Alcohol may cause hypoglycemia or hyperglycemia in patients with diabetes. Hypoglycemia most frequently occurs during acute consumption of alcohol. Even modest amounts can lower blood sugar significantly, especially when the alcohol is ingested on an empty stomach or following exercise. The mechanism involves inhibition of both gluconeogenesis as well as the counter-regulatory response to hypoglycemia. Episodes of hypoglycemia may last for 8 to 12 hours after ethanol ingestion. By contrast, chronic alcohol abuse can cause impaired glucose tolerance and hyperglycemia. Moderate alcohol consumption generally does not affect blood glucose levels in patients with well controlled diabetes. A disulfiram-like reaction (e.g., flushing, headache, and nausea) to alcohol has been reported frequently with the use of chlorpropamide and very rarely with other sulfonylureas.

Can I take insulin lispro with oral contraceptives containing estradiol?

Estradiol may interfere with blood glucose control and reduce the effectiveness of insulin lispro and other diabetic medications. Monitor your blood sugar levels closely. You may need a dose adjustment of your diabetic medications during and after treatment with estradiol. It is important to tell your doctor about all other medications you use, including vitamins and herbs. Do not stop using any medications without first talking to your doctor.

Can I take insulin lispro with fenofibrate?

Certain drugs such as ACE (angiotensin converting enzyme), ARB (angiotensin receptors blockers), amylin analogs, anabolic steroids, fibrates, MAO (mom anime oxidase) inhibitors such as linezolid, salicylates, selective serotonin reuptake inhibitors (SSRIs), Quinine, sulfonamides, disopyramide, quinidine, propxyphene, and ginseng. These agents (ACE inhibitors, ARBs, fibrates (fenofibrate) and ginseng) increases the insulin sensitivity thereby enhances the risk of hypoglycemia where as some agents stimulates the insulin secretion (MAOIs, quinidine, pentoxifyllne, quinine, ginseng), and some agents such as (SSRIs and insulin-like growth factor) increases the peripheral glucose utilization. At the same time, some agents such as SSRIs, MAOIs, insulin like growth factor inhibits gluconeogenesis, and agents such as amylin analogs, cause the slowing the rate of gastric emptying and suppressing postprandial glucagon secretion. Therefore it is very important to close monitor the patients for the signs and symptoms of hypoglycemia in case patient co-administer the fenofibrate and insuin lispro. The signs and symptoms of hypoglycemia such as headache, dizziness, nausea, hunger, tremor, weakness, sweating, palpitations are the common symptoms of hypoglycemia therefore the patients should be apprised and should let them know how to treat it, and to contact their physician if it occurs.

Can insulin lispro can be taken by the patients suffering from hypokalemia?

During the treatment of insulin, patients may suffer from hypokalemia most often. In patients who are at greater risk of developing hypokalemia, for example patients using potassium-lowering medications, or even the patients who are taking medications which are sensitive to serum potassium concentration, one should use insulin with extreme caution.

Can I eat garlic while using insulin lispro?

Some authors suggest that garlic may potentiate the hypoglycemic effect of insulin and oral antidiabetic agents, although supportive evidence is scarce. While garlic has been used in the treatment of diabetes, data from small, randomized trials in individuals with and without diabetes have not demonstrated clinically significant effects on blood glucose or insulin sensitivity.

Can I take alpha lipoic acid with insulin lispro?

Theoretically, alpha-lipoic acid may potentiate the hypoglycemic effect of insulin and oral antidiabetic agents. Alpha-lipoic acid has been shown to improve insulin sensitivity and glucose utilization in lean and obese patients with type II diabetes. However, one study found no evidence of a pharmacokinetic or pharmacodynamic interaction in 24 healthy volunteers administered glyburide or acarbose with single doses of alpha-lipoic acid. There was no significant difference in plasma insulin and glucose concentrations when glyburide or acarbose were administered with alpha-lipoic acid or without.

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About Miljan Krcobic 363 Articles
Miljan Krčobić. has bachelor degree in Pharmacy.