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Medication Safety Issues
Sound-alike/look-alike issues:
Precose® may be confused with PreCare®
International issues:
Precose® may be confused with Precosa® which is a brand name for Saccharomyces boulardii in Denmark, Finland, Norway, and Sweden
Pronunciation
(AY car bose)
U.S. Brand Names
Generic Available
Yes
Canadian Brand Names
Pharmacologic Category
Pharmacologic Category Synonyms
Use: Labeled Indications
Adjunct to diet and exercise to lower blood glucose in patients with type 2 diabetes mellitus (noninsulin dependent, NIDDM)
Pregnancy Risk Factor
B
Pregnancy Considerations
Adverse events have not been reported in animal reproduction studies; therefore, acarbose is classified as pregnancy category B. Low amounts of acarbose are absorbed systemically which should limit fetal exposure. Maternal hyperglycemia can be associated with adverse effects in the fetus, including macrosomia, neonatal hyperglycemia, and hyperbilirubinemia; the risk of congenital malformations is increased when the Hb A1c is above the normal range. Diabetes can also be associated with adverse effects in the mother. Poorly-treated diabetes may cause end-organ damage that may in turn negatively affect obstetric outcomes. Physiologic glucose levels should be maintained prior to and during pregnancy to decrease the risk of adverse events in the mother and the fetus. Acarbose has been studied for its potential role in treating GDM; however, only limited information is available describing pregnancy outcomes. Until additional safety and efficacy data are obtained, the use of oral agents is generally not recommended as routine management of GDM or type 2 diabetes mellitus during pregnancy. Insulin is the drug of choice for the control of diabetes mellitus during pregnancy.
Lactation
Excretion in breast milk unknown/not recommended
Breast-Feeding Considerations
It is not known if acarbose is found in breast milk; however, low amounts of acarbose are absorbed systemically in adults, which may limit the amount that could distribute into breast milk. Breast-feeding is not recommended by the manufacturer.
Contraindications
Hypersensitivity to acarbose or any component of the formulation; patients with diabetic ketoacidosis or cirrhosis; patients with inflammatory bowel disease, colonic ulceration, partial intestinal obstruction, or in patients predisposed to intestinal obstruction; patients who have chronic intestinal diseases associated with marked disorders of digestion or absorption, and in patients who have conditions that may deteriorate as a result of increased gas formation in the intestine
Warnings/Precautions
Concerns related to adverse effects:
• Elevated serum transaminases: Treatment-emergent elevations of serum transaminases (AST and/or ALT) occurred in up to 14% of acarbose-treated patients in long-term studies. These serum transaminase elevations appear to be dose related. At doses >100 mg 3 times/day, the incidence of serum transaminase elevations greater than 3 times the upper limit of normal was 2-3 times higher in the acarbose group than in the placebo group. These elevations were asymptomatic, reversible, more common in females, and, in general, were not associated with other evidence of liver dysfunction. Fulminant hepatitis has been reported rarely.
Disease-related concerns:
• Renal impairment: Use not recommended in patients with significant impairment (Scr >2 mg/dL); use with caution in other patients with renal impairment.
• Stress-related states: It may be necessary to discontinue acarbose and administer insulin if the patient is exposed to stress (ie, fever, trauma, infection, surgery).
Concurrent drug therapy issues:
• Sulfonylureas/insulin: In combination with a sulfonylurea or insulin will cause a further lowering of blood glucose and may increase the hypoglycemic potential of the sulfonylurea or insulin.
Special populations:
• Pediatrics: Safety and efficacy have not been established in children.
Adverse Reactions
>10%:
Gastrointestinal: Diarrhea (31%) and abdominal pain (19%) tend to return to pretreatment levels over time; frequency and intensity of flatulence (74%) tend to abate with time
Hepatic: Transaminases increased (?4%)
Postmarketing and/or case reports: Edema, erythema, exanthema, hepatitis, ileus/subileus, jaundice, liver damage, rash, urticaria
Drug Interactions
Corticosteroids (Orally Inhaled): May diminish the hypoglycemic effect of Antidiabetic Agents. In some instances, corticosteroid-mediated HPA axis suppression has led to episodes of acute adrenal crisis, which may manifest as enhanced hypoglycemia, particularly in the setting of insulin or other antidiabetic agent use. Risk C: Monitor therapy
Corticosteroids (Systemic): May diminish the hypoglycemic effect of Antidiabetic Agents. In some instances, corticosteroid-mediated HPA axis suppression has led to episodes of acute adrenal crisis, which may manifest as enhanced hypoglycemia, particularly in the setting of insulin or other antidiabetic agent use. Risk C: Monitor therapy
Digoxin: Acarbose may decrease the serum concentration of Digoxin. Risk C: Monitor therapy
Herbs (Hypoglycemic Properties): May enhance the hypoglycemic effect of Hypoglycemic Agents. Risk C: Monitor therapy
Luteinizing Hormone-Releasing Hormone Analogs: May diminish the therapeutic effect of Antidiabetic Agents. Risk C: Monitor therapy
Pegvisomant: May enhance the hypoglycemic effect of Antidiabetic Agents. Risk C: Monitor therapy
Somatropin: May diminish the hypoglycemic effect of Antidiabetic Agents. Risk D: Consider therapy modification
Ethanol/Nutrition/Herb Interactions
Ethanol: Limit ethanol.
Storage
Store at <25°C (77°F). Protect from moisture.
Mechanism of Action
Competitive inhibitor of pancreatic ?-amylase and intestinal brush border ?-glucosidases, resulting in delayed hydrolysis of ingested complex carbohydrates and disaccharides and absorption of glucose; dose-dependent reduction in postprandial serum insulin and glucose peaks; inhibits the metabolism of sucrose to glucose and fructose
Pharmacodynamics/Kinetics
Absorption: <2% as active drug; ~35% as metabolites
Metabolism: Exclusively via GI tract, principally by intestinal bacteria and digestive enzymes; 13 metabolites identified (major metabolites are sulfate, methyl, and glucuronide conjugates)
Bioavailability: Low systemic bioavailability of parent compound; acts locally in GI tract
Half-life elimination: ~2 hours
Time to peak: Active drug: ~1 hour
Excretion: Urine (~34% as inactive metabolites, <2% parent drug and active metabolite); feces (~51% as unabsorbed drug)
Dosage
Oral:
Adults: Dosage must be individualized on the basis of effectiveness and tolerance while not exceeding the maximum recommended dose
Initial dose: 25 mg 3 times/day with the first bite of each main meal; to reduce GI effects, some patients may benefit from initiating at 25 mg once daily with gradual titration to 25 mg 3 times/day as tolerated
Maintenance dose: Should be adjusted at 4- to 8-week intervals based on 1-hour postprandial glucose levels and tolerance. Dosage may be increased from 25 mg 3 times/day to 50 mg 3 times/day. Some patients may benefit from increasing the dose to 100 mg 3 times/day.
Maintenance dose ranges: 50-100 mg 3 times/day.
Maximum dose:
?60 kg: 50 mg 3 times/day
>60 kg: 100 mg 3 times/day
Patients receiving sulfonylureas or insulin: Acarbose given in combination with a sulfonylurea or insulin will cause a further lowering of blood glucose and may increase the hypoglycemic potential of the sulfonylurea or insulin. If hypoglycemia occurs, appropriate adjustments in the dosage of these agents should be made.
Dosing adjustment in renal impairment:
Clcr <25 mL/minute: Peak plasma concentrations were 5 times higher and AUCs were 6 times larger than in volunteers with normal renal function.
Significant renal dysfunction (Scr >2 mg/dL): Use is not recommended.
Administration: Oral
Should be administered with the first bite of each main meal.
Monitoring Parameters
Postprandial glucose, glycosylated hemoglobin levels, serum transaminase levels should be checked every 3 months during the first year of treatment and periodically thereafter, renal function (serum creatinine); blood pressure
Reference Range
Recommendations for glycemic control in adults with diabetes:
Hb A1c: <7%
Preprandial capillary plasma glucose: 70-130 mg/dL
Peak postprandial capillary blood glucose: <180 mg/dL
Dietary Considerations
Take with food (first bite of meal).
Patient Education
Do not take any new medication during therapy unless approved by prescriber. Take this medication exactly as directed, with the first bite of each main meal. Do not change dosage or discontinue this medicine without first consulting prescriber. Do not take other medications with or within 2 hours of this medication unless advised by prescriber. Avoid alcohol. It is important to follow dietary and lifestyle recommendations of prescriber. You will be instructed in signs of hypo- or hyperglycemia by prescriber or diabetic educator. If combining acarbose with other diabetic medication (eg, sulfonylureas, insulin), keep source of glucose (sugar) on hand in case hypoglycemia occurs. May cause mild side effects during first weeks of acarbose therapy (eg, bloating, flatulence, diarrhea, abdominal discomfort); these should diminish over time. Report severe or persistent side effects, fever, extended vomiting or flu, or change in color of urine or stool. Breast-feeding precaution: Consult prescriber if breast-feeding.
Geriatric Considerations
No specific trials in older adults have been conducted; mean age in clinical trials has been <60 years; monitor change in preprandial blood glucose concentrations to account for potential age-related changes in postprandial glucose. In clinical trials, elderly had serum concentrations 1.5 times those of younger adults. Patients with Clcr <25 mL/minute had serum concentrations 5 times those with normal renal clearance. No clinical significance can be attributed to this at this time. No adjustments in dose are recommended. Intensive glucose control (Hb A1c <6.5) has been linked to increased all cause and cardiovascular mortality, hypoglycemia requiring assistance, and weight gain in adult type 2 diabetes. For elderly patients with diabetes who are relatively healthy, attaining target goals for aspirin use, blood pressure, lipids, smoking cessation, and diet and exercise may be more important than normalized glycemic control.
Cardiovascular Considerations
Acarbose produces a slight but statistically significant reduction in Hb A1c (~1%) and fasting plasma glucose (~25 mg/dL). In general, acarbose may be used in combination with other agents (eg, sulfonylurea, metformin) or as monotherapy for patients with Type 2 diabetes. Therapy should be titrated slowly to minimize gastrointestinal side effects.
Dental Health: Effects on Dental Treatment
No significant effects or complications reported
Dental Health: Vasoconstrictor/Local Anesthetic Precautions
No information available to require special precautions
Mental Health: Effects on Mental Status
May cause drowsiness
Mental Health: Effects on Psychiatric Treatment
Antipsychotics and tricyclic antidepressants may decrease the effects of acarbose. Monoamine oxidase inhibitors, SSRIs, and nefazodone may increase the effects of acarbose.
Nursing: Physical Assessment/Monitoring
Assess potential for interactions with other prescriptions, OTC medications, or herbal products patient may be taking. Assess results of laboratory tests, therapeutic effectiveness, and adverse response on a regular basis throughout therapy. Teach patient proper use (or refer patient to diabetic educator), possible side effects/appropriate interventions (eg, importance of adequate hydration), and adverse symptoms to report.
Dosage Forms
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Tablet: 25 mg, 50 mg, 100 mg
Precose®: 25 mg, 50 mg, 100 mg
Pricing: U.S. (www.drugstore.com)
Tablets (Acarbose)
25 mg (100): $81.99
50 mg (100): $87.99
100 mg (100): $89.99
Tablets (Precose)
25 mg (90): $85.52
50 mg (90): $88.49
100 mg (90): $102.58
References
American Diabetes Association, “Standards of Medical Care in Diabetes -- 2008,” Diabetes Care, 2008, 31(Suppl 1):12-54.
Balfour JA and McTavish D, “Acarbose: A Reappraisal,” Drugs, 1993, 46(6):1025-54.
Bischoff H, “Pharmacology of ?-Glucosidase Inhibition,” Eur J Clin Invest, 1994, 24(Suppl 3):3-10.
Scheen AJ, de Magalhaes AC, Salvatore T, et al, “Reduction of the Acute Bioavailability of Metformin by the ?-Glucosidase Inhibitor Acarbose in Normal Man,” Eur J Clin Invest, 1994, 24(Suppl 3):50-4.
International Brand Names
Lexi-Comp.com
Last full review/revision September 2008
Content last modified September 2008
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