Endocrine System-Oral Antidiabetic drugs-α  Glucosidase inhibitors

Endocrine System
Name of the Oral Antidiabetic drugs-α  Glucosidase inhibitors drugs
  • Acarbose
  • Miglitol
  • voglibose

1.Acarbose

Acarbose
Availability
Tablets: 25 mg, 50 mg, 100 mg
Indications and dosages
➣ Treatment of type 2 (non-insulin dependent) diabetes mellitus when diet alone doesn’t control blood glucose
Adults: Initially, 25 mg P.O. t.i.d. Increase q 4 to 8 weeks as needed until maintenance dosage is reached. Maximum dosage is 100 mg P.O. t.i.d. for adults weighing more than 60 kg (132 lb); 50 mg P.O. t.i.d. for adults weighing 60 kg or less.
Mechanism of Action

Inhibits action of alpha-amylase and alphaglucoside enzymes. Normally, alphaamylase hydrolyzes complex starches to oligosaccharides in the small intestine and alpha-glucoside hydrolyzes oligosaccharides, trisaccharides, and di-saccharides to glucose and other monosaccharides in the brush border of the small intestine. In diabetic patients, acarbose inhibits these actions and delays glucose absorption, reducing blood glucose level after meals

Pharmacokinetics
  • Half-Life: 2 hr
  • Peak Plasma Time: 1 hr
  • Bioavailability: <2 %
  • Metabolism: extensively degraded in the intestine by bacterial and digestive enzymes, glucose units are removed from acarbose molecule
  • Urine: 34 % as inactive metabolites
  • Feces: 51% as unabsorbed drug
Administration
  • Give with first bite of patient’s three main meals.
  • Know that drug prevents breakdown of table sugar (sucrose). Thus, mild hypoglycemia must be corrected with oral glucose (such as D-glucose or dextrose), and severe hypoglycemia may warrant I.V. glucose or glucagon injection.
  • Be aware that drug may be used alone or in combination with insulin, metformin, or sulfonylureas (such as glipizide, glyburide, or glimepiride).
Contraindications
  • Hypersensitivity to drug
  • Renal dysfunction
  • Type 1 diabetes mellitus, diabetic ketoacidosis
  • GI disease
  • Cirrhosis
  • Intestinal obstruction
  • Pregnancy or breastfeeding
Precautions:
  • patients receiving concurrent hypoglycemic drugs
  • children
Adverse reactions
  • GI: diarrhea, abdominal pain, flatulence
  • Metabolic: hypoglycemia (when used with insulin or sulfonylureas)
  • Other: edema, hypersensitivity reaction (rash)
Patient monitoring
  • Monitor patient for hypoglycemia if he’s taking drug concurrently with insulin or sulfonylureas.
  • Stay alert for hyperglycemia during periods of increased stress.
  • Assess GI signs and symptoms to differentiate drug effects from those caused by paralytic ileus.
  • Check 1-hour postprandial glucose level to gauge drug’s efficacy.
  • Monitor liver function test results. Report abnormalities so that dosage adjustments may be made as needed.
Patient teaching
  • Inform patient that drug may cause serious interactions with many common medications, so he should tell all prescribers he’s taking it.
  • Teach patient about other ways to control blood glucose level, such as recommendations regarding diet, exercise, weight reduction, and stress management.
  • Stress importance of testing urine and blood glucose regularly.
  • Teach patient about signs and symptoms of hypoglycemia. Tell him that although this drug doesn’t cause hypoglycemia when used alone, hypoglycemic symptoms may arise if he takes it with other hypoglycemics.
  • Urge patient to keep oral glucose on hand to correct mild hypoglycemia; inform him that sugar in candy won’t correct hypoglycemia.
  • Inform patient that GI symptoms such as flatulence may result from delayed carbohydrate digestion in intestine.
  • Advise patient to obtain medical alert identification and to carry or wear it at all times.
  • 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

  • Acamprosate should start as soon as possible after patient has undergone alcohol withdrawal and achieved abstinence.
  • Continue to give acamprosate even during periods of alcohol relapse.

3.Miglitol

Availability
 Tablets: 25 mg, 50 mg, 100 mg
Indications and dosages
➣ Adjunct to diet in non-insulindependent (type 2) diabetes mellitus or combined with a sulfonylurea when diet plus either miglitol or a sulfonylurea alone doesn’t control hyperglycemia
Adults: 25 mg P.O. t.i.d. with first bite of each main meal. After 4 to 8 weeks, may increase to 50 mg P.O. t.i.d. After 3 months, adjust dosage further based on glycosylated hemoglobin (HbA1c) level, to a maximum of 100 mg P.O. t.i.d.
Mechanism of Action

 Inhibits intestinal glucoside hydrolase enzymes, which normally hydrolyze oligosaccharides and disaccharides to glucose and other monosaccharides. This action delays carbohydrate digestion and absorption and reduces postprandial blood glucose level.

Pharmacokinetics
  • Half-Life: 2 hr
  • Absorption: saturable; 100% at 25 mg; 50-70% for 100 mg
  • Bioavailability: 100%
  • Protein Bound: <4%
  • Vd: 0.18 L/kg
  • Metabolism: none
  • Excretion: urine >95%
Administration
  • Give with first bite of three main meals.
Contraindications
  • Hypersensitivity to drug or its components
  • Insulin-dependent (type 1) diabetes mellitus, diabetic ketoacidosis
  • Chronic intestinal disorder associated with marked digestive or absorptive disorders or conditions that may deteriorate due to increased gas formation
  • Inflammatory bowel disease, colonic ulceration, partial intestinal obstruction, or predisposition to intestinal obstruction
Precautions:
  • Significant renal impairment (safety not established)
  • Fever, infection, trauma, stress
  • Pregnant or breastfeeding patients
  • Children (safety not established).
Adverse reactions

GI: abdominal pain, diarrhea, flatulence

Skin: rash

Patient monitoring
  • Monitor CBC, blood glucose, and HBA1c levels.
  • Watch for hyperglycemia or hypoglycemia, especially if patient also takes insulin or oral sulfonylureas.
Patient teaching
  • Instruct patient to take drug three times daily with first bite of three main meals.
  • Advise patient to take drug as prescribed. If appropriate, tell him he may need insulin during periods of increased stress, infection, or surgery.
  • Teach patient about diabetes. Stress importance of proper diet, exercise, weight control, and blood glucose monitoring.
  • Inform patient that sucrose (as in table sugar) and fruit juice don’t effectively treat miglitol-induced hypoglycemia. Advise him to use dextrose or glucagon instead to raise blood glucose level quickly.
  • Tell patient drug may cause abdominal pain, diarrhea, and gas. Reassure him that these effects usually subside after several weeks.
  • As appropriate, review all other significant adverse reactions and interactions,especially those related to the drugs, tests, and foods mentioned above.
Nursing Considerations
  • Use miglitol cautiously in patient with serum creatinine level above 2 mg/dl.
  • Be aware that some patients with type 2 diabetes also may receive a sulfonylurea as an adjunct to miglitol therapy.
  • Give miglitol with first bite of each meal. Drug must have arrived at site of enzymatic action when carbohydrates reach small intestine.
  • Review patient’s HbA1C level, as appropriate, to monitor long-term glucose control.
  • Monitor patient for evidence of overdose, such as transient increases in abdominal discomfort, diarrhoea, and flatulence (but not hypoglycaemia).

5.Voglibose

Voglibose
Availability
 0.2 mg
Indications
In non-insulin-dependent diabetes mellitus (NIDDM) patients as immunotherapy
In combination with other OHAs
In addition to insulin in diabetes mellitus patients
In prevention of onset of type 2 diabetes mellitus in impaired glucose tolerance (only for Voglibose 0.2 mg Tablets) (However, Voglibose Tablets should be used only when impaired glucose tolerance has not been improved in patients already undergoing appropriate dietary treatment and/or exercise therapy.)
Administration
  • Voglibose should be taken orally immediately before each meal.
  • It is available in conventional and oral disintegrating (ODT) forms, with the ODT formulation potentially improving medication compliance.
Side Effects
  • Diarrhoea
  • Flatulence (gas)
  • Abdominal pain or discomfort
  • Bloating
  • Abdominal fullness
  • Nausea and vomiting
Precautions
  • Intestinal obstruction
  • Digestive disorders
  • Inflammatory disease
  • Ulcers
  • Ketosis
  • Diabetic hypersensitivity
Contraindications

Contraindicated in patients with Hypersensitivity to Voglibose or to any of the excipients; Diabetic ketoacidosis, diabetic pre-coma; Severe infection, before and after operation or with serious trauma; Gastrointestinal obstruction or predisposed to it.

REFERENCES

  1. Robert Kizior, Keith Hodgson, Saunders Nursing Drug handbook,1st edition 2024, Elsevier Publications. ISBN-9780443116070
  2. McGraw Hill- Drug Handbook, Seventh Edition, 2013, McGraw Hill Education Publications,9780071799430.
  3. April Hazard, Cynthia Sanoski, Davi’s Drug Guide for Nurses -Sixteenth Edition 2019, FA Davis Company Publications,9780803669451.
  4. Jones and Bartlet, Pharmacology for Nurses, Second Edition, 2020, Jones and Bartlet Learning Publications, ISBN 9781284141986.
  5. Nursebro.com, Search – Nursebro

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