Liraglutide functions as the GLP-1 (glucagon-like peptide 1) receptor agonist. The Food and Drug Administration (FDA) approved Liraglutide on January 25, 2010. It is an acylated synthetic glucagon-like peptide-1 analog. The upsurge in cyclic AMP (adenosine monophosphate) enables the glucose-dependent discharge of Insulin, hinders the glucose-dependent discharge of glucagon, and delays gastric emptying to improve controlling of blood sugar.
Uses of Liraglutide:
Liraglutide injection is utilized with a diet and workout schedule to regulate blood sugar levels in grown-ups and kids of age ten years and older with type 2 diabetes when further medicines did not maintain levels adequately. Liraglutide injection is also utilized to decrease the chance of a heart attack, stroke, or death in grown-ups with type 2 diabetes mellitus and heart and blood vessel disease. Liraglutide injection is not utilized to manage type 1 diabetes or diabetic ketoacidosis in grown-ups.
Dosage and Administration:
Injection 6 mg per mL solution in a pre-filled, multiple-dosage pen that provides dosages of 0.6 mg, 1.2 mg, or 1.8 mg.
Warnings and Precautions:
- Risk of Thyroid C-Cell Tumors - Issues of medullary thyroid carcinoma (MTC) in cases managed with Liraglutide have been declared in the postmarketing time. Liraglutide is contraindicated in cases with an individual or familial history of MTC or in cases with multiple endocrine neoplasia syndrome type 2. Advise the patients about the possible chance for MTC with the usage of Liraglutide and inform them of manifestation of thyroid tumors like a neck mass, dysphagia, dyspnea, and constant hoarseness. Frequent monitoring of serum calcitonin or thyroid ultrasound is of unsure value for earlier findings of MTC in cases managed with Liraglutide. Such monitoring may improve the chance of unneeded procedures due to lower test particularity for serum calcitonin and the increased incidence of thyroid disorder. Particularly elevated serum calcitonin may demonstrate MTC, and if serum calcitonin is estimated and seen to be advanced, the patient should be additionally assessed. Cases with thyroid nodules reported on physical assessment or neck imaging should also be additionally assessed.
- Pancreatitis - Acute pancreatitis, involving fatal and non-fatal hemorrhagic or necrotizing pancreatitis, has been marked in cases managed with Liraglutide. After beginning Liraglutide therapy, assess the patient for manifestations like constant extreme abdominal aches, periodically radiating to the back, which can or cannot be accompanied by vomiting. If pancreatitis is supposed to occur, Liraglutide should immediately be stopped, and proper treatment should be started. If pancreatitis is verified, Liraglutide should not be continued.
- Do Not Share Liraglutide Pens Between Patients - Liraglutide pens must never be transferred between patients, even if the needle is switched. Pen-sharing induces a chance of the spread of blood-borne pathogens.
- Usage With Medications Known to Cause Hypoglycemia - Patients accepting Liraglutide in a mixture with an Insulin secretagogue or Insulin might have an elevated chance of hypoglycemia. Decreasing the dosage of Sulfonylurea or Insulin may reduce the chance of hypoglycemia in the amount of Sulfonylurea.
- Renal Impairment - There have been postmarketing notifications of acute renal failure and aggravating chronic renal failure, which might periodically need hemodialysis in Liraglutide-treated cases.
- Hypersensitivity Reactions - There have been postmarketing information on severe hypersensitivity responses like anaphylactic responses and angioedema in cases managed with Liraglutide. If a hypersensitivity response happens, stop Liraglutide therapy immediately per the standard of supervision and observe until manifestations settle. Do not utilize it in cases with a prior hypersensitivity response to Liraglutide.
- Acute Gallbladder Disease - In some cases, Liraglutide managed cases present acute possibilities of gallbladder disorder, such as cholelithiasis or cholecystitis. The majority of circumstances need hospitalization or cholecystectomy. If cholelithiasis is present, gallbladder investigations and relevant clinical follow-up need to be demonstrated.
Use in Specific Populations
1. Pregnancy - Liraglutide should be utilized while pregnant only if the possible advantage explains the possible hazard to the fetus.
- Disease-Associated Maternal and Embryo or Fetal Risk - Inadequately managed diabetes in pregnancy improves the maternal hazard for diabetic ketoacidosis, preeclampsia, involuntary abortions, preterm delivery, stillbirth, and delivery difficulties due to fetal macrosomia. Poorly controlled cases of diabetes increase the fetal hazard for neural tube faults, cardiovascular malformations, stillbirth, and macrosomia-associated morbidity.
- Lactation: Developmental and health advantages of breastfeeding should be regarded along with the mother's clinical requirement for Liraglutide and any possible adverse impacts on the breastfed baby from Liraglutide or from the underlying motherly state.
2. Pediatric Use - The safety and efficacy of Liraglutide have not been demonstrated in pediatric patients. Liraglutide is not suggested for usage in pediatric cases.
3. Geriatric Use - No general disparities in safety or effectiveness were seen between these cases and younger cases. Still, the greater sensitivity of some older cases was reported.
4. Renal Impairment - No dosage correction of Liraglutide is suggested for cases with renal impairment. There has been postmarketing information on acute renal failure and the deepening of chronic renal failure, which might periodically need hemodialysis.
5. Hepatic Impairment - No dosage correction of Liraglutide is suggested for cases with hepatic impairment.
6. Gastroparesis - Liraglutide slows gastric emptying.
What Is Type 2 Diabetes?
Type 2 diabetes is a chronic disorder with high sugar or glucose in the blood. Type 2 diabetes is the most familiar type of diabetes. Insulin hormone is made in the pancreas by a special type of cell known as beta cells. Insulin is required to drive blood sugar into cells. In the inner portion of the cells, glucose is reserved and subsequently utilized for energy. In type 2 diabetes, the fat cells, liver cells, and muscle cells do not react perfectly to Insulin. Therefore, blood sugar does not get into these cells to be reserved for energy. When sugar cannot penetrate cells, a high sugar level is created in the blood. This is known as hyperglycemia. The body is incapable of using glucose for energy. This directs to the manifestation of type 2 diabetes. Type 2 diabetes typically evolves gradually over time. Most individuals with the disorder are overweight on the diagnosis. Enhanced fat makes it more difficult for the body to utilize Insulin correctly. Type 2 diabetes can also evolve in individuals who are not overweight. This is additionally typical in more aged grown-ups.
What Is Liraglutide?
Liraglutide is an injectable medication for grown-ups with type 2 diabetes mellitus; It is used along with diet and exercise to lower blood sugar levels. The recent therapy for cardiovascular disease may decrease the chance of major cardiovascular circumstances like heart attack, stroke, or death. Liraglutide is not a replacement for Insulin or usage in individuals with type 1 diabetes or diabetic ketoacidosis. It is not comprehended if Liraglutide can be utilized with mealtime Insulin. It is not understood if Liraglutide is secure and effective for usage in kids.
What Is the Most Significant Information That Should Be Known About Liraglutide?
- Liraglutide may generate serious side effects involving - potential thyroid tumors, including cancer. Discuss with the healthcare provider in case of any lump or swelling in the neck, hoarseness of voice, problem in swallowing, or shortness of breath. These may be manifestations of thyroid cancer.
- Do not utilize Liraglutide if any family member has ever had a kind of thyroid cancer known as medullary thyroid carcinoma (MTC) or in case of an endocrine system condition.
How Should Liraglutide Be Used?
Refer to the instructions for usage that comes with Liraglutide. Utilize Liraglutide precisely as the healthcare provider advises. Healthcare providers should show how to utilize Liraglutide before using it for the foremost time. Liraglutide is injected subcutaneously into the stomach, thigh, or upper arm. Do not inject Liraglutide into a muscle or vein. Use Liraglutide one time daily, at any daytime.
- Missed Dose: In case of a missed dosage of Liraglutide, have the missed dose at the following scheduled dose. Do not have both doses of Liraglutide at the same time.
Liraglutide may be accepted with or without food. Do not mix Insulin and Liraglutide jointly in the same injection. An injection of Liraglutide and Insulin can be given in the same body area but not exactly next to each other. Change the injection area with a separate injection. Do not use an identical area for each injection. Do not share the Liraglutide pen with others, even if the needle has been changed. It can deliver others a severe disease or get a severe disease from them. The dosage of Liraglutide and other diabetes medications may need to be adjusted because of alterations in the level of physical activity, weight change, raised stress, disease, alteration in diet, or additional medication intake.
Who Should Not Use Liraglutide?
- Do not use Liraglutide if the patient or any of the family have ever had a kind of thyroid cancer called medullary thyroid carcinoma (MTC) or if the patient has an endocrine system disorder known as multiple endocrine neoplasia syndrome type 2.
- Allergy to Liraglutide.
What Should Be Informed to the Healthcare Provider Before Using Liraglutide?
Prior to the usage of Liraglutide, inform the healthcare provider about the following:
- If there are any other medical conditions involving pancreas disease, kidney disorders, or liver diseases.
- Have extreme issues with the stomach, like delayed emptying of the stomach called gastroparesis or difficulties with digesting food.
- Pregnant or intend to become pregnant. It is not comprehended that Liraglutide will harm an unborn baby. Inform the healthcare provider in case of pregnancy while utilizing Liraglutide.
- Breastfeeding or plan to breastfeed. It is not understood if Liraglutide passes into the breast milk. Converse with the healthcare provider about the most suitable way to feed the baby while utilizing Liraglutide.
- Notify the healthcare provider about all the medications that are being taken by the patient, involving over-the-counter medication medications and herbal supplements.
- Liraglutide may influence how certain medications work, and certain drugs may impact how Liraglutide functions. Prior to the usage of Liraglutide, consult with healthcare providers about low blood sugar and how to handle it.
- Inform the healthcare provider in case of taking additional medicines to treat diabetes, involving Insulin or Sulfonylureas. Comprehend the medications that they are taking.
What Are the Side Effects of Liraglutide?
- Pancreatitis - Inflammation of the pancreas is called pancreatitis. Discontinue the usage of Liraglutide and contact the healthcare provider immediately in case of extreme ache in the stomach region that does not go away, with vomiting or without vomiting. The patient may sense the ache from the abdomen to the back.
- Hypoglycemia - Lower blood sugar is called hypoglycemia. The risk of getting reduced blood sugar may be increased in case of usage with Liraglutide with any other medication that can induce lower blood sugar, like Sulfonylurea or Insulin.
Manifestations of Reduced Blood Sugar May Involve:
- Dizziness or light-headedness.
- Altered vision.
- Anxiety and irritability.
- Mood transitions.
- Slurred speech.
- Confusion or sleepiness.
- Shakiness or weakness.
- Rapid heartbeat.
In cases with kidney issues, loose motions, nausea, and vomiting may induce fluid loss, which may worsen kidney problems.
Serious Allergic Reactions:
Quit using Liraglutide and acquire medical assistance immediately in case of manifestations of a serious allergic response involving:
- Swelling of face, lips, tongue, or throat.
- Difficulties in breathing or swallowing.
- A remarkably fast heartbeat.
- Excruciating rash.
Gallbladder issues have occurred in some cases of Liraglutide. Inform the healthcare provider Immediately in case of manifestations of gallbladder issues involving:
- An ache in the right or middle upper stomach region.
- Nausea and vomiting.
- Skin or the white portion of the eyes turns yellow.
The most typical side effects of Liraglutide involve nausea, diarrhea, vomiting, reduced appetite, indigestion, and constipation. Inform healthcare providers about any side effects that induce difficulty or do not go away. However, these are not all the probable side effects of Liraglutide.
General Information About the Safe and Effective Usage of Liraglutide:
Medications are periodically prescribed for objectives other than those documented in a drug guide. Do not take Liraglutide for a disorder for which it was not specified. Do not deliver Liraglutide to other individuals, even if they have the exact manifestation. It may hurt them.
Instructions for Using Liraglutide:
Initially, read the medication manual that arrives with the Liraglutide pen and then read these patient Instructions for usage for details about how to use the Liraglutide pen correctly.
Do not share the Liraglutide pen with others, even if the needle has been altered. It may transmit a serious infection.
- Do not share the Liraglutide pen with others, even if the needle is changed.
- Consistently use a fresh needle for separate injections.
- Do not reuse or share the needles with others.
- Keep the Liraglutide pen and all medications out of the reach of children.
- If the Liraglutide pen is dropped, then repeat.
- Be cautious not to distort or impair the needle.
- Do not use the cartridge scale to estimate how much Liraglutide to inject.
- Be careful when using utilized needles to control needle stick injuries.
- The Liraglutide pen can be used for up to 30 days after the usage for the first time.
First-Time Use for Each New Pen:
Step 1 - Check the Pen:
- Take the new Liraglutide pen out of the refrigerator.
- Wash hands with soap and water prior to the usage.
- Inspect the pen label prior to each use to make certain that it is the right one.
- Pull off the pen lid.
- Inspect Liraglutide in the cartridge.
- The fluid should be transparent, odorless, and free of particles. If not, do not use it.
- Wipe the stopper with an alcohol swab.
Step 2 - Attach the Needle:
- Clear the protective tab from the outermost needle cap.
- Press the outer cap comprising the needle directly onto the pen, then tighten the needle on until safe.
- Pull off the outermost needle cap. Do not throw it away.
- Pull off the internal needle cap and throw it away.
- A tiny dot of fluid may arise, which is normal.
Step 3 - Dial to the Flow Check Symbol:
- This action is accomplished only one time for each fresh pen and is exclusively needed at the foremost time at the usage of the new pen.
- Turn the dose selector till the flow check symbol (--) lines up with the arrow.
- The flow assessment mark does not distribute the quantity the healthcare provider prescribes.
Step 4 - Prepare the Pen:
- Hold the pen with the needle pointing upper.
- Tap the cartridge slowly with the finger to obtain any air bubbles to the cartridge's top portion. Hold the needle pointing up and push the dosage button until 0 mg lines up with the pointer. Repeat steps 3 and 4, up to six times, until a drop of Liraglutide seems to be at the needle tip.
Step 5 - Inspect the Pen:
- Take the Liraglutide pen.
- Wash hands with soap and water prior to the usage.
- Inspect the pen label before each usage to confirm it is the right one.
- Pull off the pen cap.
- Check Liraglutide in the cartridge.
- The fluid should be transparent, odorless, and free of particles. If not, do not use it.
- Wipe the stopper with a swab.
Step 6 - Attach the Needle:
- Clear the protecting tab from the outer needle cap.
- Press the external needle cap comprising the needle directly onto the pen, then tighten the needle till it is safe.
- Pull off the external needle cap. Do not discard it away.
- Pull off the internal needle cap and discard it. A little drop of fluid may arise. This is standard.
Step 7 - Dial the Dose:
- Liraglutide pen can deliver a dosage of 0.6 mg (initial dose), 1.2 mg, or 1.8 mg. Be certain about the dose of Liraglutide specified.
- Twist the dose selector till the right dose lines up with the pointer.
- A "click" sound is heard at all times when turning the dose selector.
- Do not put the dosage by estimating the number of clicks that are heard.
- If the wrong dose has been opted, alter it by twisting the dose selector backward or forward till the right dose lines up with the pointer.
- Be cautious to avoid pressing the dosage button while turning the dose selector. This may induce Liraglutide to come out.
Step 8 - Injecting the Dose:
- Insert a needle into the stomach skin, thigh, or top part of the arm.
- Utilize the injection method indicated by the healthcare provider.
- Do not inject Liraglutide into a vein or muscle.
- Push down on the dose button's center to inject until zero mg lines up with the pointer.
- Be cautious to avoid touching the dosage presentation with the other fingers.
- This may stop the injection.
- Maintain the dosage button pushed down and confirm that the needle is kept under the skin for six seconds to confirm the full dose is injected.
- Keep the thumb on the injection control till the needle is removed from the skin.
- Change the injection areas within the site chosen per dose.
- Do not use the exact injection area per injection.
Step 9 - Withdraw a Needle: A drop of Liraglutide is seen at the needle tip. This is standard, and it does not impact the dose just accepted. If blood seems after taking the needle out of the skin, place little pressure, but do not massage the area.
Step 10 - Remove and Dispose of the Needle: Cautiously place the external needle cap on the needle.
How to Unscrew the Needle?
- Securely release the needle from the Liraglutide pen after every usage.
- Keep the utilized Liraglutide pen and needles in an FDA-cleared sharps disposal receptacle immediately after usage.
- Do not dispose of the loose needles and pens in the household trash.
- In case of not having an FDA-cleared sharps disposal receptacle, a household receptacle can be used.
- When the disposal receptacle is nearly full, follow the community procedures for the immediate disposal of the sharps disposal receptacle.
- Do not reuse or share the needles with others.
Caring for Liraglutide Pen:
- Following releasing the needle, place the pen cap on the Liraglutide pen and keep the Liraglutide pen without the needle connected.
- Do not attempt to fill the Liraglutide pen again, as it is previously filled and is disposable.
- Do not attempt to restore the pen or pull it separately.
- Maintain the Liraglutide pen out of dust, dirt, and liquids.
- If cleaning is required, wipe the pen's exterior with a neat and moist cloth.
How Should Liraglutide Be Stored?
- Keep the fresh, new Liraglutide pen in the refrigerator at 36 degrees F (Fahrenheit) to 46 degrees F.
- If Liraglutide is held outside of refrigeration before the initial use, it should be utilized or discarded within 30 days.
- Do not freeze Liraglutide or take it if it has been frozen.
- Do not keep Liraglutide close to the refrigerator's cooling part.
Pen in Use:
- Keep the Liraglutide pen for 30 days at 59 degrees F to 86 degrees F or in a refrigerator at 36 degrees F to 46 degrees F when taking the pen out of the house.
- It should be thrown away if Liraglutide has been revealed to temperatures more than 86 degrees Fahrenheit.
- Guard the Liraglutide pen against heat and sunlight.
- Hold the pen cap on when the Liraglutide pen is not in use.
- Utilize a Liraglutide pen for only 30 days.
- Discard a used Liraglutide pen after 30 days, even if some medication is left in the pen.
Liraglutide is an acylated receptor agonist of the human glucagon-like peptide-1 (GLP-1) receptor with 97 percent amino acid series homology to endogenous human GLP-1(7-37). GLP-1(7-37) illustrates less v than 20 percent of the total circulating endogenous GLP-1, such as GLP-1(7-37). Liraglutide triggers the GLP-1 receptor, a membrane-bound cell-surface receptor connected to adenylyl cyclase with the G-protein, in beta cells of the pancreas. Liraglutide improves intracellular cyclic AMP (cAMP), directing Insulin discharge in raised glucose concentrations. This Insulin discharge decreases as glucose concentrations decline and procedure euglycemia. Liraglutide also reduces glucagon secretion in a glucose-dependent style. The mechanism of glucose reduction also includes a delay in gastric emptying.
GLP-1 (7-37) has a half-life of around two minutes.
Liraglutide's pharmacodynamic profile is compatible with its pharmacokinetic profile followed after a single subcutaneous intake as Liraglutide reduced fasting, before meals, and postprandial glucose the whole day.
- Glucose-Dependent Insulin Secretion - A single Liraglutide dose of 7.5 mcg/kg did not alter glucagon response to reduced glucose concentrations.
- Gastric Emptying - Liraglutide induces a delay of gastric emptying, thus decreasing the rate at which postprandial glucose occurs in the circulation.
- Cardiac Electrophysiology (Qtc) - The result of Liraglutide on cardiac repolarization experimented in a QTc analysis. Liraglutide at constant state concentrations with everyday amounts up to 1.8 mg did not induce QTc prolongation.
- Absorption - Complete bioavailability of Liraglutide following subcutaneous intake is around 55 %.
- Distribution - The mean volume of distribution following the intravenous administration of Liraglutide is 0.07 L/kg. Liraglutide is considerably bound to plasma protein.
- Metabolism - Liraglutide is endogenously metabolized in a comparable way to big proteins without a distinct organ as a major route of elimination.
- Elimination - Most of the radioactivity of urine and feces was eliminated in the initial six to eight days. Following subcutaneous intake of one dosage of Liraglutide, the mean apparent clearance is around 1.2 L/h with an elimination half-life of around 13 hours, creating Liraglutide appropriate for once-daily intake.
- Elderly - Age had no impact on the pharmacokinetics of Liraglutide, depending on a pharmacokinetic study.
- Gender - Depending on the effects of people's pharmacokinetic investigations, women have 25 % more inferior weight-modified clearance of Liraglutide compared to males.
- Race and Ethnicity - Race and ethnicity had no impact on the pharmacokinetics of Liraglutide based on the effects of people's pharmacokinetic examinations.
- Body Weight - Body weight particularly impacts the pharmacokinetics of Liraglutide depending on the results of population pharmacokinetic examinations. The disclosure of Liraglutide reduces with an addition in baseline body weight.
- Renal Disorder - The one-dose Liraglutide pharmacokinetics was assessed in cases with contrasting degrees of renal impairment.
Liraglutide has a lower possibility for pharmacokinetic drug interactions associated with cytochrome P450 (CYP) and plasma protein binding.
- Digoxin - The simultaneous administration with Liraglutide reduced Digoxin AUC by 16 %; Cmax reduced by 31 %. Digoxin median period to maximal concentration was slowed from one hour or more.
- Lisinopril - The co-administration with Liraglutide decreased Lisinopril AUC by 15 %, and Cmax was reduced by 27 %. Lisinopril median Tmax was slowed from six hours to eight hours with Liraglutide.
- Atorvastatin - Liraglutide did not alter the broad disclosure (AUC) of Atorvastatin after a single dose of Atorvastatin 40 mg, taken five hours after the dosage of Liraglutide at a constant state. Atorvastatin Cmax was reduced by 38 %, and median Tmax was slowed from one hour to three hours with Liraglutide.
- Acetaminophen - Liraglutide did not alter the total exposure (AUC) of Acetaminophen following a single dosage of Acetaminophen 1000 mg, taken eight hours after the dose of Liraglutide at a constant state. Acetaminophen Cmax was reduced by 31 %, and median Tmax was slowed up to 15 minutes.
- Griseofulvin - Liraglutide did not alter the total exposure of Griseofulvin following the co-administration of a single dosage of Griseofulvin 500 mg with Liraglutide at a constant state. Griseofulvin Cmax advanced by 37 %, while median Tmax did not alter.
- Oral Contraceptives - A single dosage of an oral contraceptive mixture product comprising 0.03 mg Ethinylestradiol and 0.15 mg Levonorgestrel was taken under provided states and seven hours after the dosage of Liraglutide at constant circumstances. Liraglutide reduced Ethinylestradiol and Levonorgestrel Cmax by 12 % and 13 %, respectively.
- Insulin Detemir - No pharmacokinetic relations were marked between Liraglutide and Insulin detemir at the time of different subcutaneous Insulin detemir injections of 0.5 units per kilogram, and Liraglutide 1.8 mg were taken in cases with type 2 diabetes.
Frequently Asked Questions