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Semaglutide (Ozempic® Injection)

Semaglutide, marketed as Ozempic®, is a glucagon-like peptide-1 (GLP-1) receptor agonist administered via subcutaneous injection. It is used to manage type 2 diabetes mellitus (T2DM) and has demonstrated cardiovascular benefits. This article details its pharmacology, clinical applications, and safety profile, referencing the British National Formulary (BNF)Lippincott Textbook of Pharmacology, and Lange Basic & Clinical Pharmacology.

Semaglutide mimics endogenous GLP-1, enhancing glucose-dependent insulin secretion from pancreatic β-cells and suppressing glucagon release from α-cells (Lippincott). Key effects include:

  • Slowed Gastric Emptying: Reduces postprandial glucose spikes.
  • Appetite Suppression: Activates brain receptors to promote satiety, aiding weight loss (Lange).
  • Cardiovascular Protection: Shown in trials (e.g., SUSTAIN-6) to reduce major adverse cardiovascular events (MACE) in high-risk patients (BNF).
  1. Type 2 Diabetes Mellitus: Adjunctive to diet/exercise ± other antidiabetic agents (e.g., metformin, insulin).
  2. Cardiovascular Risk Reduction: For patients with T2DM and established cardiovascular disease.
  3. Weight Management: Off-label use due to significant weight loss effects (approved in higher doses as Wegovy®) (BNF).
  • Administration: Subcutaneous injection (abdomen, thigh, or upper arm) once weekly.
  • Titration:
    • Initial: 0.25 mg weekly for 4 weeks (to minimize GI side effects).
    • Maintenance: Increase to 0.5 mg or 1 mg weekly based on glycemic response.
  • Renal/Hepatic Impairment: No dose adjustment needed for mild-to-moderate impairment. Use caution in severe renal impairment (eGFR <30 mL/min/1.73m²) (BNF).
  • Gastrointestinal: Nausea (15–20%), vomiting, diarrhea, constipation.
  • Mild hypoglycemia (with concurrent insulin/sulfonylureas).

Serious:

  • Pancreatitis: Monitor for severe abdominal pain.
  • Diabetic Retinopathy Complications: Risk in patients with pre-existing retinopathy.
  • Thyroid C-Cell Tumors: Contraindicated in personal/family history of medullary thyroid carcinoma (MTC) or multiple endocrine neoplasia type 2 (Lippincott).
  • Acute Kidney Injury: Dehydration-related, especially with nausea/vomiting (Lange).
  • Contraindications:
    • Personal/family history of MTC.
    • Pregnancy (Category C: animal studies show fetal risk; avoid unless benefits outweigh risks).
    • HbA1c, renal function, and signs of pancreatitis.
    • Educate patients on hypoglycemia symptoms if used with insulin/sulfonylureas.

 Discontinue if pregnancy occurs; avoid during breastfeeding (BNF).

  • Insulin/Sulfonylureas: Increased hypoglycemia risk; consider dose reduction.
  • Oral Medications: Delayed absorption of drugs dependent on rapid GI uptake (e.g., antibiotics, oral contraceptives—take 1 hour before semaglutide).
  • Diuretics/NSAIDs: May exacerbate dehydration or renal impairment (Lange).
  • Generic: Semaglutide.
  • Brand Name: Ozempic® (injection); Wegovy® (higher dose for obesity).

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