释义 |
liraglutide Translationsliraglutide
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 See If pancreatitis is suspected, discontinue drug promptly, perform confirmatory tests, and treat appropriately. If pancreatitis is confirmed, don't restart drug. See Monitor patient for signs and symptoms of thyroid tumor. Patient teaching • Instruct patient to take drug without regard to meals. See 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. See 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) liraglutide, Victoza (trade name) Classification Therapeutic: antidiabetics Pharmacologic: glucagon like peptide 1 glp 1 receptor agonists Pregnancy Category: C
IndicationsAdjunct 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.ActionActs 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 effectsImproved glycemic control.PharmacokineticsAbsorption: 55% absorbed following subcutaneous injection.Distribution: Unknown.Protein Binding: >98%.Metabolism and Excretion: Endogenously metabolized.Half-life: 13 hr.Time/action profile (↓ in HbA1c)ROUTE | ONSET | PEAK | DURATION |
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Subcut | within 4 wk | 8 wk | unk |
Contraindications/PrecautionsContraindicated 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 EffectsCentral nervous systemDermatologicEndocrinologic- thyroid C-cell tumors (life-threatening)
Gastrointestinal- pancreatitis (life-threatening)
- diarrhea (most frequent)
- nausea (most frequent)
- vomiting (most frequent)
- constipation
GenitourinaryLocal- hypersensitivity reactions including anaphylaxis and angioedema (life-threatening)
- injection site reactions
InteractionsDrug-Drug interactionConcurrent 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/DosageSubcutaneous (Adults) 0.6 mg once daily initially, may be ↑ at weekly intervals up to 1.8 mg/day.AvailabilitySolution for subcutaneous injection: Pre-filled, multi-dose pen that delivers doses of 0.6 mg, 1.2 mg, or 1.8 mg Nursing implicationsNursing 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 DiagnosesImbalanced 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.
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