Name of the Oral Antidiabetic drugs- Meglitinide /phenylalanine Analogues drugs
- Repaglinide
- Nateglinide
1.Repaglinide
| Repaglinide |
| Availability Tablets: 0.5 mg, 1 mg, 2 mg |
| Indications and dosages ➣ Adjunct to diet and exercise in type 2 (non-insulin-dependent) diabetes mellitus uncontrolled by diet and exercise alone, or combined with metformin in type 2 diabetes mellitus uncontrolled by diet, exercise, and either repaglinide or metformin alone Adults: 0.5 to 4 mg P.O. before each meal; may adjust at 1-week intervals based on blood glucose response. Maximum daily dosage is 16 mg |
Mechanism of Action
Stimulates release of insulin from functioning pancreatic beta cells. In patients with type 2 diabetes mellitus, a shortage of these cells decreases blood insulin levels and causes glucose intolerance. By interacting with the adenosine triphosphatase (ATP)–potassium channel on the beta cell membrane, repaglinide prevents potassium from leaving the cell. This causes the beta cell to depolarize and the cell membrane’s calcium channel to open. As a result, calcium moves into the cell and insulin moves out. The extent of insulin release is glucose dependent; the lower the glucose level, the less insulin is secreted from the cell.
Pharmacokinetics
- Bioavailability: 56%
- Peak plasma time: 1 hr
- Protein bound: >98%
- Metabolized extensively in liver, by CYP3A4 and CYP2C8
- Half-life: 1 hr
- Excretion: Feces (90%); urine (8%)
Administration
- Give 15 to 30 minutes before meals. Administer two, three, or four times daily, if needed, to adapt to patient’s meal pattern
Contraindications
- Hypersensitivity to drug or its components
- Diabetic ketoacidosis
- Type 1 (insulin-dependent) diabetes mellitus
- Administration with gemfibrozil
Precautions:
- Renal or hepatic impairment; adrenal or pituitary insufficiency; stress caused by infection, fever, trauma, or surgery
- Concurrent use of CYP2C8 inhibitors (such as trimethoprim, gemfibrozil, montelukast)
- Concurrent use of CYP3A4 inhibitors (such as ketoconazole, itraconazole, erythromycin)
- Concurrent use of CYP3A4 or CYP2C8 inducers (such as rifampin, barbiturates, carbamazepine)
- Elderly or malnourished patients
- Pregnant or breastfeeding patients
- Children.
Adverse reactions
- CNS: headache, paresthesia
- CV: angina, chest pain
- EENT: sinusitis, rhinitis
- GI: nausea, vomiting, diarrhea, constipation, dyspepsia
- GU: urinary tract infection
- Metabolic: hyperglycemia, hypoglycemia
- Musculoskeletal: joint pain, back pain
- Respiratory: upper respiratory infection, bronchitis
- Other: tooth disorder, hypersensitivity reaction
Patient monitoring
- Monitor blood glucose and glycosylated hemoglobin levels.
- Monitor patient’s meal pattern. Consult prescriber about adjusting dosage if patient adds or misses a meal.
- Assess for angina, shortness of breath, or other discomforts.
- Watch for signs and symptoms of bronchitis and upper respiratory, urinary, and EENT infections.
Patient teaching
- Tell patient to take 15 to 30 minutes before each meal.
- Instruct patient to monitor blood glucose level carefully. Teach him to recognize signs and symptoms of hypoglycemia and hyperglycemia.
- Advise patient to report signs and symptoms of infection.
- As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs, foods, and herbs mentioned above.
Nursing Considerations
- Be aware that repaglinide shouldn’t be used with NPH insulin because the combination may increase the risk of angina.
- Expect to check HbA1c level every 3 months, as ordered, to assess patient’s long-term control of blood glucose level.
- During times of increased stress, such as from infection, surgery, or trauma, monitor blood glucose level often and assess need for additional insulin
2.Nateglinide
| Nateglinide |
| Availability Tablets: 60 mg, 120 mg |
| Indications and dosages ➣ To decrease glucose levels in type 2 (non-insulin-dependent) diabetes mellitus not adequately controlled by diet and exercise Adults: 120 mg P.O. t.i.d. up to 30 minutes before meals, or 60 mg P.O. t.i.d. if patient is near glycosylated haemoglobin (HbA1c) goal |
Mechanism of Action
Increases insulin secretion via binding K+ channels on beta islet cells. Reduces postprandial hyperglycemia. Amount of insulin released is dependent upon existing glucose levels.
Pharmacokinetics
- Half-Life: 1.2-3 hr
- Duration: 4 hr
- Urine: 83%
- Feces: 10%
- Peak Plasma Time: < 1hr
- Bioavailability: 72-75%
- Protein Bound: 97-99%
- Metabolism: by hepatic cytochrome P450 CYP2C9 (70%) & CYP3A4 (30%)
Administration
- Give 30 minutes before meals. If meal is missed, don’t give dose.
- Know that drug may be given alone or with metformin
Contraindications
- Hypersensitivity to drug or its components
- Diabetic ketoacidosis
- Type 1 (insulin-dependent) diabetes mellitus
Precautions:
- Renal or hepatic impairment, adrenal or pituitary insufficiency
- Elderly or malnourished patients
- Pregnant or breastfeeding patients.
Adverse reactions
- CNS: dizziness
- GI: diarrhea
- Metabolic: hypoglycemia
- Musculoskeletal: back pain, joint pain
- Respiratory: upper respiratory tract infection, bronchitis, coughing
- Other: flulike symptoms, trauma
Patient monitoring
- Monitor blood glucose and HbA1c levels.
- Assess pulmonary status for bronchitis, upper respiratory infection, and flulike signs and symptoms.
- Monitor musculoskeletal status. Check for back pain and arthropathy.
- Note GI complaints and identify nutritional deficiencies.
Patient teaching
- Instruct patient to take dose up to 30 minutes before each main meal.
- Advise patient not to skip a meal. If he does, tell him to also skip accompanying nateglinide dose, to prevent hypoglycemia.
- Teach patient how to monitor blood and urine for glucose and ketones, as prescribed.
- Instruct patient to report adverse CNS effects and signs and symptoms of respiratory infection.
- Caution patient to avoid driving and other hazardous activities until he knows how drug affects sensation and balance.
- As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs and tests mentioned above.
Nursing Considerations
- Give nateglinide 1 to 30 minutes before meals to reduce the risk of hypoglycemia.
- Monitor fasting glucose and HbA1c levels periodically, as ordered, to evaluate treatment effectiveness.
- Monitor patient often in event of fever, infection, trauma, or surgery because transient loss of glucose control may occur, requiring an alteration in therapy.
REFERENCES
- Robert Kizior, Keith Hodgson, Saunders Nursing Drug handbook,1st edition 2024, Elsevier Publications. ISBN-9780443116070
- McGraw Hill- Drug Handbook, Seventh Edition, 2013, McGraw Hill Education Publications,9780071799430.
- April Hazard, Cynthia Sanoski, Davi’s Drug Guide for Nurses -Sixteenth Edition 2019, FA Davis Company Publications,9780803669451.
- Jones and Bartlet, Pharmacology for Nurses, Second Edition, 2020, Jones and Bartlet Learning Publications, ISBN 9781284141986.
- Nursebro.com, Search – Nursebro
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