Acarbose: Drug information - UpToDate https://www.uptodate.com/contents/acarbose-drug-information/print?s...

Official reprint from UpToDate®

www.uptodate.com ©2019 UpToDate, Inc. and/or its affiliates. All Rights Reserved.

Acarbose: Drug information

Copyright 1978-2019 Lexicomp, Inc. All rights reserved.

(For additional information see "Acarbose: Patient drug information" and see "Acarbose: Pediatric drug
information")

For abbreviations and symbols that may be used in Lexicomp (show table)

Brand Names: US
Precose

Brand Names: Canada

Glucobay

Pharmacologic Category
Antidiabetic Agent, Alpha-Glucosidase Inhibitor

Dosing: Adult

Diabetes mellitus, type 2: Note: Dosage must be individualized on the basis of

effectiveness and tolerance. Oral: Initial dose: 25 mg 3 times daily with the first bite of each
main meal (may also initiate at 25 mg once daily with gradual titration to 25 mg 3 times
daily as tolerated); increase dose at 4- to 8-week intervals based on 1-hour postprandial
glucose or glycosylated hemoglobin levels and tolerance until maintenance dose of 50 to
100 mg 3 times daily is reached (maximum dose: ≤60 kg: 50 mg 3 times daily; >60 kg: 100
mg 3 times daily)

Postprandial hyperinsulinemic hypoglycemia after gastric bypass surgery (off-

label): Oral: 25 to 100 mg 3 times daily just prior to the start of each meal, or if more
frequent meals may consider 25 to 50 mg up to 6 times daily. Administer in conjunction
with dietary modifications aimed at reducing the glycemic index of each meal (Frankhouser
2013; Mordes 2015; Ritz 2012; Valderas 2012)

1 of 9 04/18/2019, 9:20 AM
Acarbose: Drug information - UpToDate https://www.uptodate.com/contents/acarbose-drug-information/print?s...

Dosing: Renal Impairment: Adult

Serum creatinine ≤2 mg/dL or CrCl ≥25 mL/ minute/1.73 m2: There are no dosage
adjustments provided in the manufacturer’s labeling.

Serum creatinine >2 mg/dL or CrCl <25 ml/minute/1.73 m2: Use is not recommended;
systemic AUC increased 6-fold in patients with CrCl <25 mL/ minute/1.73 m2.

Dosing: Hepatic Impairment: Adult

There are no dosage adjustments provided in the manufacturer's labeling; contraindicated in
patients with cirrhosis.

Dosing: Pediatric

(For additional information see "Acarbose: Pediatric drug information")

Note: Dosage must be individualized on the basis of effectiveness and tolerance.

Diabetes mellitus, type 2: Children ≥10 years and Adolescents: Very limited data
available: Oral: Initial dose: 25 mg 3 times daily with the first bite of each main meal;
may also initiate at 25 mg once daily with gradual titration to 25 mg 3 times daily as
tolerated; then increase in 25 mg/dose increments in 2 to 4 week intervals as
tolerated. Weight-based maximum dose: ≤60 kg: 50 mg/dose, >60 kg: 100 mg/dose.
Clinical trials in pediatric patients are lacking; dosing based on expert reported clinical
experience; overall dosing is similar to that used in adult patients (DeFronzo 1999;
Jacobson-Dickman 2005; Kliegman 2016)

Dumping syndrome (reactive hypoglycemia) after Nissen fundoplication: Limited

data available: Infants ≥4 months and young children who have failed nutritional
manipulations: Oral: Initial dose: 12.5 to 25 mg before each bolus feeding of formula
containing complex carbohydrates. Increase in 12.5 to 25 mg/dose increments until
postprandial serum glucose stable (>60 mg/dL was used in clinical reports). Reported
dose range: 12.5 to 100 mg/dose. Dosing based on a few small studies (total n=11).
Acarbose was well tolerated in most patients; except a few patients experienced
flatulence (De Cunto 2011; Ng 2001; Zung 2003).

Dosing: Geriatric
Refer to adult dosing.

Dosage Forms: US
Excipient information presented when available (limited, particularly for generics); consult
specific product labeling.

2 of 9 04/18/2019, 9:20 AM
Acarbose: Drug information - UpToDate https://www.uptodate.com/contents/acarbose-drug-information/print?s...

Tablet, Oral:

Precose: 25 mg, 50 mg, 100 mg

Generic: 25 mg, 50 mg, 100 mg

Generic Equivalent Available: US

Yes

Dosage Forms: Canada

Excipient information presented when available (limited, particularly for generics); consult
specific product labeling.

Tablet, Oral:

Glucobay: 50 mg, 100 mg [contains CORN STARCH]

Administration: Adult
Oral: Administer with the first bite of each main meal.

Administration: Pediatric
Oral: Administer with first bite of each main meal

Use: Labeled Indications

Diabetes mellitus, type 2: Adjunct to diet and exercise to improve glycemic control in
adults with type 2 diabetes mellitus (noninsulin dependent, NIDDM)

Guideline recommendations: Alpha-glucosidase inhibitors (eg, acarbose) are generally not

used in patients with type 2 diabetes, but may be tried in specific situations (ADA 2017a).

Use: Off-Label: Adult

Postprandial hyperinsulinemic hypoglycemia after gastric bypass surgery

Medication Safety Issues

Sound-alike/look-alike issues:

Precose may be confused with PreCare

International issues:

Precose [US, Malaysia] may be confused with Precosa brand name for
Saccharomyces boulardii [Finland, Sweden]

3 of 9 04/18/2019, 9:20 AM
Acarbose: Drug information - UpToDate https://www.uptodate.com/contents/acarbose-drug-information/print?s...

Adverse Reactions

>10%: Gastrointestinal: Frequency and intensity of flatulence (74%) tend to abate with
time; diarrhea (31%) and abdominal pain (19%) tend to return to pretreatment levels over
time

1% to 10%: Hepatic: Increased serum transaminases (≤4%)

<1%, postmarketing, and/or case reports: Edema, erythema, hepatic injury, hepatitis,
intestinal obstruction, jaundice, pneumatosis cystoides intestinalis, skin rash,
thrombocytopenia, urticaria

Contraindications
Hypersensitivity to acarbose or any component of the formulation; diabetic ketoacidosis;
cirrhosis; inflammatory bowel disease, colonic ulceration, partial intestinal obstruction, patients
predisposed to intestinal obstruction; chronic intestinal diseases associated with marked
disorders of digestion or absorption; 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) and hyperbilirubinemia may occur (dose-related).
These elevations were asymptomatic, reversible, more common in females, and, in
general, were not associated with other evidence of liver dysfunction. Fulminant
hepatitis (may be fatal) has been reported. If elevations are observed, a reduction in
dosage or withdrawal of therapy may be indicated, particularly if the elevations persist.

• Hypoglycemia: Hypoglycemia is unlikely to occur with acarbose monotherapy but

may occur with combination therapy (eg, sulfonylureas, insulin, metformin). In patients
taking acarbose, oral glucose (dextrose) should be used instead of sucrose (cane
sugar) in the treatment of mild-to-moderate hypoglycemia since the hydrolysis of
sucrose to glucose and fructose is inhibited by acarbose.

Disease-related concerns:

• Hepatic impairment: Use with caution in patients with hepatic impairment.

• Renal impairment: Not recommended in patients with significant impairment (serum

creatinine >2 mg/dL or CrCl <25 mL/minute/1.73 m2).

4 of 9 04/18/2019, 9:20 AM
Acarbose: Drug information - UpToDate https://www.uptodate.com/contents/acarbose-drug-information/print?s...

• 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:

• Drug-drug interactions: Potentially significant interactions may exist, requiring dose

or frequency adjustment, additional monitoring, and/or selection of alternative therapy.
Consult drug interactions database for more detailed information.

Other warnings/precautions:

• Appropriate use: Diet: Increased intake of sucrose (cane sugar) and food that
contains sucrose during treatment can lead to GI symptoms (eg, flatulence and
bloating), loose stools, and occasionally diarrhea. If a diabetic diet is not followed, the
GI side effects may be intensified. If severe symptoms develop in spite of adherence
to a diabetic diet, temporarily or permanently reduce dose.

• Patient education: Diabetes self-management education (DSME) is essential to

maximize the effectiveness of therapy.

Metabolism/Transport Effects
None known.

Drug Interactions
(For additional information: Launch drug interactions program)

Alpha-Lipoic Acid: May enhance the hypoglycemic effect of Antidiabetic Agents. Risk C:
Monitor therapy

Androgens: May enhance the hypoglycemic effect of Blood Glucose Lowering Agents.
Exceptions: Danazol. Risk C: Monitor therapy

Digoxin: Acarbose may decrease the serum concentration of Digoxin. Risk C: Monitor
therapy

Direct Acting Antiviral Agents (HCV): May enhance the hypoglycemic effect of Antidiabetic
Agents. Risk C: Monitor therapy

Guanethidine: May enhance the hypoglycemic effect of Antidiabetic Agents. Risk C:

Monitor therapy

Hyperglycemia-Associated Agents: May diminish the therapeutic effect of Antidiabetic

Agents. Risk C: Monitor therapy

Hypoglycemia-Associated Agents: Antidiabetic Agents may enhance the hypoglycemic

5 of 9 04/18/2019, 9:20 AM
Acarbose: Drug information - UpToDate https://www.uptodate.com/contents/acarbose-drug-information/print?s...

effect of Hypoglycemia-Associated Agents. Risk C: Monitor therapy

Maitake: May enhance the hypoglycemic effect of Blood Glucose Lowering Agents. Risk C:
Monitor therapy

Monoamine Oxidase Inhibitors: May enhance the hypoglycemic effect of Blood Glucose
Lowering Agents. Risk C: Monitor therapy

Neomycin: May enhance the adverse/toxic effect of Acarbose. Neomycin may decrease
the metabolism of Acarbose. Risk C: Monitor therapy

Pegvisomant: May enhance the hypoglycemic effect of Blood Glucose Lowering Agents.
Risk C: Monitor therapy

Prothionamide: May enhance the hypoglycemic effect of Blood Glucose Lowering Agents.
Risk C: Monitor therapy

Quinolones: May enhance the hypoglycemic effect of Blood Glucose Lowering Agents.
Quinolones may diminish the therapeutic effect of Blood Glucose Lowering Agents.
Specifically, if an agent is being used to treat diabetes, loss of blood sugar control may
occur with quinolone use. Risk C: Monitor therapy

Ritodrine: May diminish the therapeutic effect of Antidiabetic Agents. Risk C: Monitor
therapy

Salicylates: May enhance the hypoglycemic effect of Blood Glucose Lowering Agents. Risk
C: Monitor therapy

Selective Serotonin Reuptake Inhibitors: May enhance the hypoglycemic effect of Blood
Glucose Lowering Agents. Risk C: Monitor therapy

Thiazide and Thiazide-Like Diuretics: May diminish the therapeutic effect of Antidiabetic
Agents. Risk C: Monitor therapy

Pregnancy Risk Factor

B (show table)

Pregnancy Implications

Adverse events have not been observed in animal reproduction studies. Less than 2% of an
oral dose of acarbose is absorbed systemically, which should limit fetal exposure.

In women with diabetes, maternal hyperglycemia can be associated with congenital

malformations as well as adverse effects in the fetus, neonate, and the mother (ACOG 2005;

6 of 9 04/18/2019, 9:20 AM
Acarbose: Drug information - UpToDate https://www.uptodate.com/contents/acarbose-drug-information/print?s...

ADA 2018c; Metzger 2007). To prevent adverse outcomes, prior to conception and throughout
pregnancy, maternal blood glucose and HbA1c should be kept as close to target goals as
possible but without causing significant hypoglycemia (ADA 2018c; Blumer 2013). Agents other
than acarbose are currently recommended to treat diabetes in pregnant women (ADA 2018c).

Breast-Feeding Considerations
It is not known if acarbose is present in breast milk.

Breastfeeding is not recommended by the manufacturer. However, <2% of an oral dose of

acarbose is absorbed systemically in adults, which may limit the amount that could distribute
into breast milk.

Monitoring Parameters
Postprandial glucose, hemoglobin A1c (at least twice yearly in patients who have stable
glycemic control and are meeting treatment goals; quarterly in patients not meeting treatment
goals or with therapy change [ADA 2018a]), serum creatinine; serum transaminase levels every
3 months during the first year of treatment and periodically thereafter.

Reference Range

Recommendations for glycemic control in nonpregnant adults with diabetes (ADA 2018a):

HbA1c: <7% (a more aggressive [<6.5%] or less aggressive [<8%] HbA1c goal may be
targeted based on patient-specific characteristics)

Preprandial capillary blood glucose: 80 to 130 mg/dL

Peak postprandial capillary blood glucose: <180 mg/dL

Recommendations for glycemic control in older adults (≥65 years) with diabetes (ADA
2018b):

HbA1c: <7.5% (healthy); <8% (complex/intermediate health); <8.5% (very

complex/poor health) (individualization may be appropriate based on patient and
caregiver preferences)

Preprandial capillary blood glucose: 90 to 130 mg/dL (healthy); 90 to 150 mg/dL

(complex/intermediate health); 100 to 180 mg/dL (very complex/poor health)

Bedtime capillary blood glucose: 90 to 150 mg/dL (healthy); 100 to 180 mg/dL
(complex/intermediate health); 110 to 200 mg/dL (very complex/poor health)

Mechanism of Action

7 of 9 04/18/2019, 9:20 AM
Acarbose: Drug information - UpToDate https://www.uptodate.com/contents/acarbose-drug-information/print?s...

Competitive inhibitor of pancreatic α-amylase and intestinal brush border α-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 and Pharmacokinetics

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)

Pharmacodynamics and Pharmacokinetics: Additional Considerations

Renal function impairment: In patients with CrCl <25 mL/minute/1.73 m2, the Cmax was ~5
times higher, and the AUC was 6 times larger.

Pricing: US

Tablets (Acarbose Oral)

25 mg (per each): $0.90 - $0.91

50 mg (per each): $0.88 - $0.98

100 mg (per each): $1.16 - $1.17

Tablets (Precose Oral)

25 mg (per each): $1.12

50 mg (per each): $1.21

100 mg (per each): $1.45

Disclaimer: A representative AWP (Average Wholesale Price) price or price range is provided
as reference price only. A range is provided when more than one manufacturer's AWP price is

8 of 9 04/18/2019, 9:20 AM
Acarbose: Drug information - UpToDate https://www.uptodate.com/contents/acarbose-drug-information/print?s...

available and uses the low and high price reported by the manufacturers to determine the
range. The pricing data should be used for benchmarking purposes only, and as such should
not be used alone to set or adjudicate any prices for reimbursement or purchasing functions or
considered to be an exact price for a single product and/or manufacturer. Medi-Span expressly
disclaims all warranties of any kind or nature, whether express or implied, and assumes no
liability with respect to accuracy of price or price range data published in its solutions. In no
event shall Medi-Span be liable for special, indirect, incidental, or consequential damages
arising from use of price or price range data. Pricing data is updated monthly.

Brand Names: International

Abacus (LK); Acarb (LK); Acarbay (IN); Acarbocin (NZ); Acarose (EG, QA, SA); Acarsel (VN);
Acrose (IL); Beixi (CN); Capribose (ID); Carbotrap (ID); Carlipin (HK); Decarbay (TW); Deglu
(TW); Dexebryl (EG); Diabose (LK); Dibose (MY); Eclid (ID); Garbose (MY); Glibos (TW);
Glicobase (IT); Glucar (IN, LK, MY); Gluco A (BD); Glucobay (AE, AR, AT, AU, BB, BD, BE, BF,
BG, BH, BJ, BM, BR, BS, BZ, CH, CI, CL, CO, CR, CY, CZ, DE, DK, DO, EC, EG, ES, ET, FI,
GB, GH, GM, GN, GR, GT, GY, HK, HN, HR, HU, IE, IN, IQ, IR, IS, IT, JM, JO, JP, KE, KR, LB,
LR, LU, LY, MA, ML, MR, MT, MU, MW, MX, MY, NE, NG, NI, NL, NO, NZ, OM, PA, PE, PH,
PK, PL, PR, PT, PY, QA, RO, RU, SA, SC, SD, SE, SG, SI, SL, SN, SR, SV, SY, TH, TN, TR,
TT, TW, TZ, UG, UY, VE, VN, YE, ZA, ZM, ZW); Glucor (FR); Glucorid (MY); Glumida (ES);
Glycovate (PH); Hasanbose (VN); Incardel (MX); Kaboping (CN); Kertonbose (TW); Precose
(MY, TW); Prepostal (EG); Rebose (IN); Renabos (BD); Sincrosa (MX); Sugatrol (BD);
Tardensone (TW)

For country abbreviations used in Lexicomp (show table)

Use of UpToDate is subject to the Subscription and License Agreement.

Topic 9219 Version 193.0

9 of 9 04/18/2019, 9:20 AM