acarbose

General

Pronunciation:
aye-kar-bose


Trade Name(s)

  • Glucobay Canadian Trade name
  • Precose

Ther. Class.

antidiabetics

Pharm. Class.

alpha glucosidase inhibitors

Indications

Management of type 2 diabetes in conjunction with dietary therapy; may be used with insulin or other hypoglycemic agents.

Action

Lowers blood glucose by inhibiting the enzyme alpha-glucosidase in the GI tract. Delays and reduces glucose absorption.

Therapeutic Effect(s):

Lowering of blood glucose in diabetic patients, especially postprandial hyperglycemia.

Pharmacokinetics

Absorption: <2% systemically absorbed; action is primarily local (in the GI tract).

Distribution: Unknown.

Metabolism and Excretion: Minimal amounts absorbed are excreted by the kidneys.

Half-life: 2 hr.

TIME/ACTION PROFILE (effect on blood glucose)

ROUTEONSETPEAKDURATION
POunknown1 hrunknown

Contraindication/Precautions

Contraindicated in:

  • Hypersensitivity;
  • Diabetic ketoacidosis;
  • Cirrhosis;
  • Serum creatinine >2 mg/dL;
  • Lactation:  Lactation.

Use Cautiously in:

  • OB:   Safety not established in pregnancy
  • Pedi:   Safety and effectiveness not established in children
  • Presence of fever, infection, trauma, stress (may cause hyperglycemia, requiring alternative therapy).

Adverse Reactions/Side Effects

GI: abdominal pain, diarrhea, flatulence, ↑ liver enzymes

* CAPITALS indicate life-threatening.
Underline indicate most frequent.

Interactions

Drug-Drug

  •  Thiazide diuretics  and  loop diuretics,  corticosteroids,  phenothiazines,  thyroid preparations,  estrogens (conjugated),  progestins,  hormonal contraceptives,  phenytoin,  niacin,  sympathomimetics,  calcium channel blockers, and  isoniazid  may ↑ glucose levels in diabetic patients and lead to ↓ control of blood glucose.
  • Effects are↓ by  intestinal adsorbents, including  activated charcoal  and  digestive enzyme preparations (amylase, pancreatin) ; avoid concurrent use.
  • ↑ effects of  sulfonylurea hypoglycemic agents.
  • May ↓ absorption of  digoxin ; may require dosage adjustment.

Drug-Natural Products:

  •  Glucosamine  may worsen blood glucose control.
  •  Chromium and  coenzyme Q-10  may ↑ hypoglycemic effects.

Route/Dosage

PO (Adults): 25 mg 3 times daily; may ↑ every 4–8 wk as needed/tolerated (range 50–100 mg 3 times daily; not to exceed 50 mg 3 times daily in patients ≤60 kg or 100 mg 3 times daily in patients >60 kg).

Availability (generic available)

Tablets: 25 mg, 50 mg, 100 mg

Assessment

  • Observe patient for signs and symptoms of hypoglycemia (sweating, hunger, weakness, dizziness, tremor, tachycardia, anxiety) when taking concurrently with other oral hypoglycemic agents.

Lab Test Considerations:

Monitor serum glucose and glycosylated hemoglobin periodically during therapy to evaluate effectiveness.

  • Monitor AST and ALT every 3 mo for the 1st yr and then periodically. Elevated levels may require dose reduction or discontinuation of acarbose. Elevations occur more commonly in patients taking more than 300 mg/day and in female patients. Levels usually return to normal without other evidence of liver injury after discontinuation.

Toxicity and Overdose:

Symptoms of overdose are transient increase in flatulence, diarrhea, and abdominal discomfort. Acarbose alone does not cause hypoglycemia; however, other concurrently administered hypoglycemic agents may produce hypoglycemia requiring treatment.

Implementation

  • Patients stabilized on a diabetic regimen who are exposed to stress, fever, trauma, infection, or surgery may require administration of insulin.

    • Does not cause hypoglycemia when taken while fasting, but may increase hypoglycemic effect of other hypoglycemic agents.
  • PO Administer with first bite of each meal 3 times/day.

Patient/Family Teaching

  • Instruct patient to take acarbose at same time each day. If a dose is missed and the meal is completed without taking the dose, skip missed dose and take next dose with the next meal. Do not double doses.
  • Explain to patient that acarbose controls hyperglycemia but does not cure diabetes. Therapy is long-term.
  • Review signs of hypoglycemia and hyperglycemia (blurred vision; drowsiness; dry mouth; flushed, dry skin; fruit-like breath odor; increased urination; ketones in urine; loss of appetite; stomachache; nausea or vomiting; tiredness; rapid, deep breathing; unusual thirst; unconsciousness) with patient. If hypoglycemia occurs, advise patient to take a form of oral glucose (e.g., glucose tablets, liquid gel glucose) rather than sugar (absorption of sugar is blocked by acarbose) 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 urine ketones. Monitor closely during periods of stress or illness. Notify health care professional if significant changes occur.
  • Advise patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and to consult with health care professional before taking other medications.
  • Advise patient to inform health care professional of medication regimen before treatment or surgery.
  • Advise patient to carry a form of oral glucose and identification describing disease process and medication regimen at all times.
  • Advise female of reproductive potential to notify health care professional if pregnancy is planned or suspected or if breastfeeding.
  • Emphasize the importance of routine follow-up examinations.

Evaluation/Desired Outcomes

Control of blood glucose levels without the appearance of hypoglycemic or hyperglycemic episodes.

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