glucagon like peptide 1 glp 1 receptor agonists
Adjunct treatment to diet and exercise in the management of adults with type 2 diabetes mellitus (not recommended as first-line therapy).
Stimulates the glucagon-like peptide-1 (GLP-1, an incretin) receptor which leads to a reduction in blood glucose by stimulating insulin release and lowering glucagon secretion (both effects subside as blood glucose decreases toward normal). Also lowers blood glucose by delaying gastric emptying.
Improved glycemic control.
Absorption: 89% absorbed following subcutaneous injection; 0.4–1% absorbed following oral administration.
Distribution: Minimally distributed to tissues.
Protein Binding: >99%.
Metabolism and Excretion: Endogenously metabolized; eliminated in the urine (3% as unchanged drug) and feces.
Half-life: 1 wk.
TIME/ACTION PROFILE (plasma concentrations)
- Personal or family history of medullary thyroid carcinoma;
- Multiple Endocrine Neoplasia syndrome type 2;
- Type 1 diabetes;
- Diabetic ketoacidosis.
Use Cautiously in:
- History of pancreatitis;
- Diabetic retinopathy (↑ risk of complications);
- History of angioedema or anaphylaxis to another GLP-1 receptor agonist;
- History of diabetic retinopathy
- OB: Use only if potential maternal benefit justifies potential fetal risk;
- Lactation: Safety not established in breast feeding;
- Rep: Women of reproductive potential;
- Pedi: Safety and effectiveness not established.
Adverse Reactions/Side Effects
EENT: retinopathy complications
Endo: THYROID C-CELL TUMORS, hypoglycemia
GI: PANCREATITIS, abdominal pain, diarrhea, nausea, cholelithiasis, constipation, ↓ appetite, dyspepsia, flatulence, ↑ amylase, ↑ lipase, vomiting
GU: acute kidney injury
Local: injection site reactions
Misc: HYPERSENSITIVITY REACTIONS (INCLUDING ANAPHYLAXIS AND ANGIOEDEMA)
* CAPITALS indicate life-threatening.
Underline indicate most frequent.
- Concurrent use with agents that increase insulin secretion, including sulfonylureas or insulin , 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.
PO (Adults) 3 mg once daily for 30 days, then 7 mg once daily; after 30 days, may ↑ to 14 mg once daily if additional glycemic control needed.
SC (Adults) 0.25 mg once weekly initially for 4 wk, then 0.5 mg once weekly for 1 wk; may then ↑ dose after 4 wk, if needed, up to 1 mg once weekly.
Solution for injection (prefilled pen): 2 mg/1.5 mL (delivers doses of 0.25 mg, 0.5 mg, or 1 mg), 4 mg/3 mL (delivers dose of 1 mg)
Tablets: 3 mg, 7 mg, 14 mg
- Observe patient taking concurrent insulin for signs and symptoms of hypoglycemic reactions (sweating, hunger, weakness, dizziness, tremor, tachycardia, anxiety, headache, blurred vision, slurred speech, irritability).
- Monitor for pancreatitis (persistent severe abdominal pain, sometimes radiating to the back, with or without vomiting). If pancreatitis is suspected, discontinue semaglutide; if confirmed, do not restart semaglutide.
Lab Test Considerations:
Monitor serum HbA1c periodically during therapy to evaluate effectiveness.
- May ↑ lipase and pancreatic amylase.
- Patients stabilized on a diabetic regimen who are exposed to stress, fever, trauma, infection, or surgery may require administration of insulin.
- SC Administer once weekly on same day each wk, any time of day without regard to meals. May change day of injection as long as time between doses is >48 hrs. Inject into abdomen, thigh, or upper arm, rotating sites each wk. Solution is clear and colorless; do not administer solutions that are discolored or contain particulate matter.
- Instruct patient in correct technique for injection and disposal of materials. Follow manufacturer's instructions for pen use. Pen should never be shared between patients, even if needle is changed. Administer missed doses as soon as remembered within 5 days of missed dose; if >5 days, skip dose and administer next dose on regular scheduled day. Advise patient to read Medication Guide before starting therapy and with each Rx refill in case of changes.
- Advise patient taking insulin and semaglutide to never mix insulin and semaglutide 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 notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and consult health care professional before taking any new medications.
- Advise patient to notify health care professional and discontinue semaglutide immediately if signs of pancreatitis (nausea, vomiting, abdominal pain radiating to back) or hypersensitivity (swelling of face, lips, tongue or throat, problems breathing or swallowing, severe rash or itching, fainting or feeling dizzy, very rapid heartbeat) occur.
- 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) occur.
- Advise patient to inform health care professional of medication regimen before treatment or surgery.
- Advise patient to carry a form of sugar (sugar packets, candy) and identification describing disease process and medication regimen at all times.
- Rep: Insulin is the preferred method of controlling blood glucose during pregnancy. Advise female and male patient of reproductive potential to discontinue semaglutide in women at least 2 mo before a planned pregnancy to allow for long washout period of semaglutide. Counsel female patients to notify health care professional if pregnancy is planned or suspected or if breast feeding.
- Emphasize the importance of routine follow-up exams.
Improved glycemic control.
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