liraglutide


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Related to liraglutide: Exenatide

liraglutide

Victoza

Pharmacologic class: Glucagon-like peptide-1 (GLP-1) receptor agonist

Therapeutic class: Hypoglycemic

Pregnancy risk category C

FDA Box Warning

• Liraglutide causes dose-dependent and treatment-duration-dependent thyroid C-cell tumors at clinically relevant exposures in both genders of rats and mice. It's unknown whether drug causes thyroid C-cell tumors, including medullary thyroid carcinoma (MTC), in humans, as human relevance couldn't be ruled out by clinical or nonclinical studies.

• Drug is contraindicated in patients with personal or family history of MTC and in patients with multiple endocrine neoplasia syndrome type 2 (MEN 2).

Action

Activates GLP-1 receptor, a membrane-bound cell-surface receptor coupled to adenylyl cyclase by the stimulatory G-protein, Gs, in pancreatic beta cells and increases intracellular cyclic AMP, leading to insulin release in the presence of elevated glucose levels; also decreases glucagon secretion in a glucose-dependent manner. Mechanism of blood-glucose lowering also involves a delay in gastric emptying.

Availability

Injection: 0.6 mg, 1.2 mg, 1.8 mg (6 mg/ml, 3 ml) in prefilled, multidose pens

Indications and dosages

Adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus

Adults: Initially, 0.6 mg subcutaneously daily for 1 week. After 1 week, increase dosage to 1.2 mg daily. If 1.2-mg dose doesn't result in acceptable glycemic control, dosage can be increased to 1.8 mg daily.

Contraindications

• Personal or family history of medullary thyroid carcinoma

• MEN 2

Precautions

Use cautiously in:

• hepatic or renal impairment

• history of pancreatitis

• concomitant use of oral hypoglycemics

• breastfeeding patients

• children (safety and efficacy not established).

Administration

• Administer without regard to meals.

• Be aware that initial dose is intended to reduce GI symptoms and isn't effective for glycemic control.

• When initiating drug, consider reducing dosage of concomitantly administered oral hypoglycemics to reduce risk of hypoglycemia.

Adverse reactions

CNS: dizziness, headache

CV: hypertension

EENT: sinusitis, nasopharyngitis

GI: nausea, vomiting, diarrhea, constipation, pancreatitis

GU: urinary tract infection

Metabolic: hypoglycemia, hyperosmolar coma, death

Musculoskeletal: back pain

Respiratory: upper respiratory tract infection

Other: influenza

Interactions

Drug-drug. Insulin secretagogues (such as sulfonylureas): increased risk of hypoglycemia

Oral drugs: decreased absorption of these drugs

Drug-diagnostic tests. Blood glucose: decreased level

Patient monitoring

If pancreatitis is suspected, discontinue drug promptly, perform confirmatory tests, and treat appropriately. If pancreatitis is confirmed, don't restart drug.

Monitor patient for signs and symptoms of thyroid tumor.

Patient teaching

• Instruct patient to take drug without regard to meals.

Instruct patient to discontinue drug and immediately notify prescriber if persistent severe abdominal pain occurs that may radiate to the back and may or may not be accompanied by vomiting.

Instruct patient to immediately notify prescriber if signs and symptoms of thyroid tumor occur (such as persistent hoarseness, mass in the neck, difficulty swallowing, or difficulty breathing).

• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs and tests mentioned above.

liraglutide

(lir-a-gloo-tide) ,

Victoza

(trade name)

Classification

Therapeutic: antidiabetics
Pharmacologic: glucagon like peptide 1 glp 1 receptor agonists
Pregnancy Category: C

Indications

Adjunct treatment to diet and exercise in the management of adults with type 2 diabetes mellitus; not recommended as first line therapy, as a substitute for insulin, in patients with type 1 diabetes, or for ketoacidosis.

Action

Acts as an acylated human Glucagon-Like Peptide-1 (GLP-1, an incretin) receptor agonist; increases intracellular cyclic AMP (cAMP) leading to insulin release when glucose is elevated, which then subsides as blood glucose decreases toward euglycemia. Also decreases glucagon secretion and delays gastric emptying.

Therapeutic effects

Improved glycemic control.

Pharmacokinetics

Absorption: 55% absorbed following subcutaneous injection.
Distribution: Unknown.
Protein Binding: >98%.
Metabolism and Excretion: Endogenously metabolized.
Half-life: 13 hr.

Time/action profile (↓ in HbA1c)

ROUTEONSETPEAKDURATION
Subcutwithin 4 wk8 wkunk

Contraindications/Precautions

Contraindicated in: HypersensitivityPersonal or family history of medullary thyroid carcinoma (MTC)/multiple endocrine neoplasia syndrome type 2 (MEN 2) ;Type 1 diabetesDiabetic ketoacidosis Lactation: Avoid use; Pediatric: Not recommended.
Use Cautiously in: History of pancreatitis;History of angioedema to another GLP-1 receptor agonistHepatic/renal impairment; Obstetric: Use only if potential benefit justifies potential risk to fetus.

Adverse Reactions/Side Effects

Central nervous system

  • headache

Dermatologic

  • pruritis
  • rash

Endocrinologic

  • thyroid C-cell tumors (life-threatening)

Gastrointestinal

  • pancreatitis (life-threatening)
  • diarrhea (most frequent)
  • nausea (most frequent)
  • vomiting (most frequent)
  • constipation

Genitourinary

  • acute renal failure

Local

  • hypersensitivity reactions including anaphylaxis and angioedema (life-threatening)
  • injection site reactions

Interactions

Drug-Drug interaction

Concurrent use with agents that increase insulin secretion including sulfonylureas may ↑ the risk of serious hypoglycemia, use cautiously and consider dose ↓ of agent increasing insulin secretion.May alter absorption of concomitantly administered oral medications due to delayed gastric emptying.

Route/Dosage

Subcutaneous (Adults) 0.6 mg once daily initially, may be ↑ at weekly intervals up to 1.8 mg/day.

Availability

Solution for subcutaneous injection: Pre-filled, multi-dose pen that delivers doses of 0.6 mg, 1.2 mg, or 1.8 mg

Nursing implications

Nursing assessment

  • Observe patient taking concurrent insulin for signs and symptoms of hypoglycemic reactions (sweating, hunger, weakness, dizziness, tremor, tachycardia, anxiety).
  • If thyroid nodules or elevated serum calcitonin are noted, patient should be referred to an endocrinologist.
  • Monitor for pancreatitis (persistent severe abdominal pain, sometimes radiating to the back, with or without vomiting). If pancreatitis is suspected, discontinue liraglutide; if confirmed, do not restart liraglutide.
  • Lab Test Considerations: Monitor serum HbA1c periodically during therapy to evaluate effectiveness.

Potential Nursing Diagnoses

Imbalanced nutrition: more than body requirements (Indications)
Noncompliance (Patient/Family Teaching)

Implementation

  • Patients stabilized on a diabetic regimen who are exposed to stress, fever, trauma, infection, or surgery may require administration of insulin.
  • Subcutaneous: Administer once daily at any time of the day, without regard to food. Inject into abdomen, thigh, or upper arm. Solution should be clear and colorless; do not administer solutions that are discolored or contain particulate matter.
    • Initial dose of 0.6 mg/day is increased after 1 wk to 1.2 mg/day. If glycemic control is not acceptable, increase to 1.8 mg/day. Available in a prefilled pen without needle; patient may require Rx for needles.
    • First Time Use for Each New Pen—Follow manufacturer's instructions only once with each new pen or if pen is dropped.

Patient/Family Teaching

  • Instruct patient on use of Victoza pen and to take liraglutide as directed. Pen should never be shared between patients, even if needle is changed. Store pen in refrigerator; do not freeze. After initial use, pen may be stored at room temperature or refrigerated up to 30 days. Keep pen cap on when not in use. Protect from excessive heat and sunlight. Remove and safely discard needle after each injection and store pen without needle attached. Advise patient to read the Patient Medication Guide before starting liraglutide and with each Rx refill.
  • If a dose is missed do not make up, skip and take next scheduled dose the next day. If more than 3 days are missed, reinitiate at 0.6 mg to minimize GI effects. Notify health care professional and increase dose as directed.
  • Inform patient that nausea is the most common side effect, but usually decreases over time.
  • Advise patient taking insulin and liraglutide to never mix insulin and liraglutide together. Give as 2 separate injections. Both injections may be given in the same body area, but should not be given right next to each other.
  • Explain to patient that this medication controls hyperglycemia but does not cure diabetes. Therapy is long-term.
  • Review signs of hypoglycemia and hyperglycemia with patient. If hypoglycemia occurs, advise patient to take a glass of orange juice or 2–3 tsp of sugar, honey, or corn syrup dissolved in water and notify health care professional.
  • Encourage patient to follow prescribed diet, medication, and exercise regimen to prevent hypoglycemic or hyperglycemic episodes.
  • Instruct patient in proper testing of serum glucose and ketones. These tests should be closely monitored during periods of stress or illness, and health care professional should be notified if significant changes occur.
  • Advise patient to tell health care professional what medications they are taking and to avoid taking new Rx, OTC, vitamins, or herbal products without consulting health care professional.
  • Advise patient to notify discontinue liraglutide and health care professional immediately if signs of pancreatitis (nausea, vomiting, abdominal pain) occur.
  • Advise patient to inform health care professional of medication regimen before treatment or surgery.
  • Inform patient of risk of benign and malignant thyroid C-cell tumors. Advise patient to notify health care professional if symptoms of thyroid tumors (lump in neck, hoarseness, trouble swallowing, shortness of breath) or if signs of allergic reaction (swelling of face, lips, tongue, or throat; fainting or feeling dizzy; very rapid heartbeat; problems breathing or swallowing; severe rash or itching) occur.
  • Insulin is the preferred method of controlling blood glucose during pregnancy. Counsel female patients to notify health care professional if pregnancy is planned or suspected or if breast feeding.
  • Advise patient to carry a form of sugar (sugar packets, candy) and identification describing disease process and medication regimen at all times.
  • Emphasize the importance of routine follow-up exams.

Evaluation/Desired Outcomes

  • Improved glycemic control.
References in periodicals archive ?
Liraglutide (Victoza[R] P) European prescribing information.
Liraglutide is injected once a day and Byetta twice daily, although the investment community is more anxious to see liraglutide compared with an experimental version of exenatide that is injected just once a week.
The mean weight loss ranged from 4.8 kg with the lowest 1.2-mg dose of liraglutide to 7.2 kg with the 3.0-mg dose, according to the investigators.
Liraglutide, an incretin mimetic developed by Novo Nordisk A/S for once-daily injection, entered phase III testing in February.
Masked efpeglenatide 4 mg was noninferior to open-label liraglutide. Compared with placebo, greater proportions treated with efpeglenatide ≥1 mg achieved HbA1c <7 percent (61 to 72 percent versus 24 percent).
Therefore, in the present study, to determine whether 5-HT is critical for the weight loss induced by GLP-1 receptor activation in mice, we examined the effects of liraglutide on daily food intake and body weight over 4 days in mice treated with or without the tryptophan hydroxylase inhibitor pchlorophenylalanine (PCPA) for 3 days.
Josef-Hospital in Bochum, Germany, and colleagues randomly assigned 9,340 patients with type 2 diabetes at high risk for cardiovascular events to receive either liraglutide (≤1.8 mg daily; 4,668 patients) or placebo (4,672 patients).
At 26 weeks, mean glycated hemoglobin levels in the liraglutide group had decreased by 0.64 percentage points from baseline, but in the placebo group they had increased by 0.42 percentage points, representing a treatment difference of -1.06 percentage points (P less than .001).
However, even though the 8-week intensive dietary program led to substantial weight loss and significant improvement in pain, additional weight loss of nearly 2.5 kg over 52 weeks of daily liraglutide treatment did not translate into more pain control.
The active substance in Victoza, liraglutide, is an incretin mimetic.
Healthcare company Novo Nordisk reported on Monday the receipt of approval from the US Food and Drug Administration (FDA) for an expanded indication for Victoza (liraglutide) injection to lower blood sugar along with diet and exercise in children and adolescents aged 10-17 years with type 2 diabetes.
"This settlement reflects the comprehensive US patent portfolio for liraglutide. Novo Nordisk will continue to defend our broad intellectual property portfolio for innovative drugs against challenges," said Jesper Brandgaard, executive vice president and head of Biopharm and Legal Affairs of Novo Nordisk.