Consumer medicine information

Acarbose Viatris

Acarbose

BRAND INFORMATION

Brand name

Acarbose Viatris

Active ingredient

Acarbose

Schedule

S4

 

Consumer medicine information (CMI) leaflet

Please read this leaflet carefully before you start using Acarbose Viatris.

What is in this leaflet

This leaflet answers some common questions about ACARBOSE VIATRIS. It does not contain all the available information. It does not take the place of talking to your doctor or pharmacist.

All medicines have risks and benefits. Your doctor has weighed the risks of you taking this medicine against the benefits they expect it will have for you.

As ACARBOSE VIATRIS is a prescription medicine, it should only be used under medical supervision.

If you have any concerns about taking this medicine, ask your doctor or pharmacist.

Keep this leaflet with the medicine. You may need to read it again.

What ACARBOSE VIATRIS is used for

ACARBOSE VIATRIS tablets contain the active drug acarbose. They are used for the treatment of diabetes.

Acarbose helps to control your blood sugar levels in conjunction with diet, exercise, weight loss and other measures by slowing down the digestion of carbohydrates (complex sugars) from your diet. This reduces the abnormally high blood sugar levels that occur after each meal.

Ask your doctor if you have any questions about why this medicine has been prescribed for you. Your doctor may have prescribed it for another reason.

Before you take ACARBOSE VIATRIS

When you must not take it

Do not take ACARBOSE VIATRIS if you have an allergy to:

  • acarbose, the active ingredient in ACARBOSE VIATRIS
  • any of the ingredients listed at the end of this leaflet.

Some of the symptoms of an allergic reaction may include:

  • shortness of breath
  • wheezing or difficulty breathing
  • swelling of the face, lips, tongue or other parts of the body
  • rash, itching or hives on the skin.

Do not take ACARBOSE VIATRIS if:

  • you have a severe kidney disorder (creatinine clearance <25 mL/min).
  • you suffer from intestinal obstruction, inflammation or ulceration of the bowel, e.g. ulcerative colitis or Crohn’s disease.
  • you have a hernia or have had previous abdominal surgery. If so, consult your doctor first.

Do not give this medicine to a child under the age of 18 years.

Do not take this medicine after the expiry date printed on the pack and blister. The expiry date is printed on the carton and on each blister after “EXP”. The expiry date refers to the last day of that month. If it has expired return it to your pharmacist for disposal.

Do not take this medicine if the packaging is torn or shows signs of tampering. If the packaging is damaged, return it to your pharmacist for disposal.

If you are not sure whether you should start taking this medicine, talk to your doctor.

Before you start to take it

Tell your doctor if you have allergies to any other medicines, foods, preservatives or dyes.

Tell your doctor if you are pregnant or intend to become pregnant. Like most medicines of this kind, acarbose is not recommended to be used during pregnancy. Your doctor will discuss the risks and benefits of using it if you are pregnant.

Tell your doctor if you are breast-feeding or planning to breast-feed. It is not known whether acarbose passes into breast milk.

If you have not told your doctor about any of the above, tell him/her before you start taking ACARBOSE VIATRIS.

Taking other medicines

Tell your doctor or pharmacist if you are taking other medicines, including any you have bought without a prescription from your pharmacy, supermarket or health food shop.

Some medicines and ACARBOSE VIATRIS may interfere with each other. These include:

  • Neomycin (Neosulf™)
  • Colestyramine (Questran Lite™)
  • Intestinal adsorbents (e.g. charcoal)
  • Digestive enzyme preparations (Cotazym-S Forte™, Creon™, Pancrease™, Viokase™)
  • Digoxin

(™ indicates trademark of the original manufacturer/supplier)

These medicines may be affected by ACARBOSE VIATRIS or may affect how well it works. You may need different amounts of your medicines, or you may need to take different medicines.

Your doctor and pharmacist have more information on medicines to be careful with or avoid while taking this medicine.

You should avoid taking cane sugar (sucrose) and products containing sugar. They may cause stomach discomfort or even diarrhoea if taken while you are on ACARBOSE VIATRIS tablets.

If you are taking other medicines containing sulfonylureas or metformin or tend to have low blood sugar levels, tell your doctor before using ACARBOSE VIATRIS.

If you have not told your doctor or pharmacist about any of the above, tell them before you start taking ACARBOSE VIATRIS.

How to take ACARBOSE VIATRIS

Follow all directions given to you by your doctor or pharmacist carefully. They may differ from the information contained in this leaflet.

If you do not understand the instructions printed on the pharmacist label, ask your doctor or pharmacist for help.

How much to take

To gain the maximum benefit from ACARBOSE VIATRIS it is important that you follow the prescribed diet as well as taking the exact dose prescribed by your doctor. This will help control your blood sugar levels and reduce side effects experienced.

At the start of treatment, your doctor may prescribe a low dose of ACARBOSE VIATRIS. Your doctor will determine the correct dose for you depending on your condition, other medicines and your response to the treatment. The average adult dose is one ACARBOSE VIATRIS 100 mg tablet taken three times daily.

How to take it

Swallow the tablets whole with a little liquid immediately before the meal. If you prefer not to swallow the tablets then chew the tablets with the first few mouthfuls of food.

When to take it

Take your medicine at about the same time each day with breakfast, lunch and dinner. Taking it at the same time each day will have the best effect. It will also help you remember when to take it.

When you first start your treatment, your doctor may recommend that you take your tablets once or twice a day, before increasing your dose to three times a day.

How long to take it

Do not stop taking the tablets unless you are told to do so by your doctor.

This medicine helps to control your condition, but does not cure it. It is important to keep taking your medicine even if you feel well.

If you do not feel well while you are taking them, see your doctor (see SIDE EFFECTS).

If you forget to take it

If you forget to take ACARBOSE VIATRIS at the time you are supposed to, do not take the tablets between meals. Wait until it is time for you to take your next dose and take ACARBOSE VIATRIS with your meal and continue as before. Do not take a double dose.

If you take too much (Overdose)

If you have taken too many ACARBOSE VIATRIS tablets, avoid foods or drinks containing carbohydrates and telephone your doctor or the Poisons Information Centre (Australia: 13 11 26) for advice, or go to Accident and Emergency at the nearest hospital, if you think that you or anyone else may have taken too much ACARBOSE VIATRIS. Do this even if there are no signs of discomfort or poisoning. You may need urgent medical attention.

When ACARBOSE VIATRIS is taken with drinks and/or meals containing carbohydrates, overdosage can lead to diarrhoea and other intestinal symptoms such as flatulence (wind) and abdominal cramps.

While you are taking ACARBOSE VIATRIS

Things you must do

If you are about to be started on any new medicine, remind your doctor and pharmacist that you are taking acarbose.

Tell any other doctors, dentists, and pharmacists who treat you that you are taking this medicine.

Take ACARBOSE VIATRIS exactly as instructed by your doctor. If you do not follow your doctor’s instructions, your blood sugar level may not be controlled.

Things you must not do

Do not take ACARBOSE VIATRIS to treat any other complaints unless your doctor tells you to.

Do not give your medicine to anyone else, even if they have the same condition as you.

Do not stop taking your medicine or lower the dosage without checking with your doctor. If you stop taking it suddenly, your condition may worsen or you may have unwanted side effects.

What to be careful of

Treating hypoglycaemia: (“hypos” or low blood sugar).

As a diabetic you may also be receiving other medicines for your diabetes. If ACARBOSE VIATRIS is prescribed for you in addition to sulfonylureas, metformin or insulin to control your diabetes, your doctor may need to adjust the dosages of these drugs to avoid the occurrence of “hypos” (low blood sugar levels).

When taking ACARBOSE VIATRIS together with these drugs, do not treat a “hypo” with ordinary sugar (sucrose). It will not work fast enough. Instead, you should take some GLUCOSE (also known as dextrose) tablets, honey, syrup or sweets which should be available from your local chemist.

SIDE EFFECTS

Tell your doctor or pharmacist as soon as possible if you do not feel well while you are taking ACARBOSE VIATRIS.

All medicines have side effects. Sometimes they are serious; most of the time they are not.

In serious cases, you may need to obtain medical treatment.

Some patients may experience unwanted side effects during acarbose treatment.

These side effects are more common at the start of the treatment, but some may persist or develop after treatment, or when dosage of acarbose is adjusted by your doctor.

Do not be alarmed by the following lists of side effects. You may not experience any of them.

Ask your doctor or pharmacist to answer any questions you may have.

Tell your doctor or pharmacist if you notice any of the following and they worry you:

  • flatulence (wind)
  • abdominal “rumbling” noises
  • a feeling of fullness
  • softer stools or have diarrhoea; particularly if you have eaten foods containing sugar

The above list includes the more common side effects of your medicine. Normally these symptoms will disappear if you continue treatment and keep to your prescribed diet. These symptoms may get worse if you do not keep to your prescribed diet.

If your symptoms persist for more than 2 or 3 days, or if they are severe, consult your doctor or nearest emergency department particularly in the case of diarrhoea.

Do not take antacids to treat these symptoms as they are unlikely to give you any relief.

This list includes the less common side effects of your medicine.

  • stomach cramps
  • nausea
  • indigestion
  • vomiting
  • increased appetite
  • dizziness
  • loss of appetite

Tell your doctor as soon as possible if you notice any of the following. This list includes rare side effects of your medicine.

  • jaundice (yellowing of the skin)
  • swelling from fluid retention
  • inflammation of the liver (hepatitis)
  • intestinal obstruction
  • decrease in platelet count
  • skin reactions such as redness, rash and urticaria (hives)

If while undergoing treatment with acarbose, you experience any side-effects or symptoms which you think may be due to this medication (whether or not it is mentioned in this leaflet) please inform your doctor or pharmacist as early as possible. You may need medical treatment in some cases.

ACARBOSE VIATRIS tablets may cause an increase in the results of certain liver function tests. Therefore, your doctor may conduct blood tests to monitor your liver function during the first 6 to 12 months of treatment with ACARBOSE VIATRIS.

These effects go away when treatment is stopped.

Tell your doctor or pharmacist if you notice anything that is making you feel unwell.

Other side effects not listed above may also occur in some people.

After taking ACARBOSE VIATRIS

When treatment with ACARBOSE VIATRIS is to be stopped, your prescribing doctor may need to alter the dose of other medication(s) accordingly and monitor your condition.

Storage

Keep your tablets in the pack until it is time to take them. If you take the tablets out of the pack they may not keep well.

Keep your tablets in a cool dry place where the temperature stays below 25°C. Protect from moisture.

Do not store it or any other medicine in the bathroom, near a sink, or on a window-sill.

Do not leave it in the car. Heat and damp can destroy some medicines.

Keep it where children cannot reach it. A locked cupboard at least one-and-a half metres above the ground is a good place to store medicines.

Disposal

If your doctor tells you to stop taking this medicine or the expiry date has passed, ask your pharmacist what to do with any medicine that is left over. Return any unused medicine to your pharmacist.

PRODUCT DESCRIPTION

What it looks like

ACARBOSE VIATRIS tablets are available in a blister pack of 90s in two strengths.

ACARBOSE VIATRIS 50 mg tablets are round, biconvex, white to off-white, marked with “ACA 50” on one side.

ACARBOSE VIATRIS 100 mg tablets are round, biconvex, white to off-white, marked with a score line on one side, and “ACA 100” on the reverse side.

Ingredients

Active ingredient per tablet:

ACARBOSE VIATRIS 50 mg – contains acarbose 50 mg

ACARBOSE VIATRIS 100 mg – contains acarbose 100 mg

Inactive ingredients:

  • microcrystalline cellulose
  • pregelatinised maize starch
  • colloidal anhydrous silica
  • magnesium stearate.

Supplier

ACARBOSE VIATRIS is supplied in Australia by:

Alphapharm Pty Limited trading as Viatris
Level 1, 30 The Bond
30-34 Hickson Road
Millers Point NSW 2000
www.viatris.com.au

Australian Registration Numbers

ACARBOSE VIATRIS 50 mg - AUST R 226796

ACARBOSE VIATRIS 100 mg - AUST R 226797

This document was prepared in
November 2022

Published by MIMS February 2023

BRAND INFORMATION

Brand name

Acarbose Viatris

Active ingredient

Acarbose

Schedule

S4

 

1 Name of Medicine

Acarbose.

2 Qualitative and Quantitative Composition

Each tablet contains 50 mg or 100 mg acarbose.
For the full list of excipients, see Section 6.1 List of Excipients.

3 Pharmaceutical Form

Acarbose Viatris 50 mg are round, biconvex, white to off-white tablets, marked with "ACA 50" on one side.
Acarbose Viatris 100 mg are round, biconvex, white to off-white tablets, marked with a score on one side, and "ACA 100" on the reverse side.

4 Clinical Particulars

4.1 Therapeutic Indications

As an adjunct to prescribed diet and exercise for the management of blood glucose concentrations in non-insulin dependent diabetic patients who are inadequately controlled by diet alone or by diet and oral hypoglycaemic agents.

4.2 Dose and Method of Administration

Since the activity and the tolerability of acarbose varies from individual to individual, the optimal dosage must be individualised.
Acarbose Viatris should be swallowed whole with a little liquid directly before a meal or chewed with the first few mouthfuls of the meal.
In adults, Acarbose Viatris should be started at a low initial dose and be increased slowly to minimise the gastrointestinal side effects. Treatment is usually commenced at 50 mg once daily for the first week, 50 mg twice daily for the second week and 50 mg three times a day for the third week. A further increase of the dose may be necessary after 4 - 8 weeks on the basis of the blood glucose level. The average adult dose is 100 mg Acarbose Viatris three times daily. A further increase to 200 mg Acarbose Viatris three times daily may occasionally be necessary (see Section 4.4 Special Warnings and Precautions for Use).
If gastrointestinal symptoms are not tolerated despite close adherence to the prescribed diet, a reduction in the dose should be considered.
No modification of the adult dosage regimen is necessary in the elderly.

4.3 Contraindications

Hypersensitivity to acarbose and/or any of the inactive tablet constituents, pregnancy and lactation.
Acarbose should not be used in patients under 18 years of age.
Acarbose is contraindicated in patients with severe renal impairment (creatinine clearance < 25 mL/min).
Acarbose should not be used in patients with gastrointestinal disorders associated with malabsorption. It should not be used in patients with inflammatory bowel disease, such as ulcerative colitis and Crohn's disease.
Acarbose should not be used in patients with partial intestinal obstruction, or in patients predisposed to intestinal obstruction or ileus.
Similarly, acarbose should not be used in conditions that could be aggravated by an increased formation of intestinal gas (e.g. Roemheld syndrome, major hernias, intestinal obstruction and intestinal ulcers).

4.4 Special Warnings and Precautions for Use

General.

Ingestion of sucrose and food that contains sucrose can easily lead to considerable intestinal symptoms (e.g. flatulence and bloating), or even diarrhoea during treatment with acarbose, as a result of increased carbohydrate fermentation in the colon (see Section 4.8 Adverse Effects (Undesirable Effects)).

Hypoglycaemia.

Acarbose has an antihyperglycaemic effect, but does not itself induce hypoglycaemia. If acarbose is prescribed in addition to drugs containing sulfonylureas or metformin or in addition to insulin, a fall of blood glucose levels into the hypoglycaemic range may necessitate a suitable decrease in the sulfonylurea, metformin or insulin dose. In individual cases hypoglycaemic shock may occur. In the event of acute hypoglycaemia, it should be borne in mind that cane sugar (sucrose) is broken down into fructose and glucose more slowly during acarbose treatment and is therefore unsuitable for a rapid elimination of hypoglycaemic phenomena. Glucose (i.e. dextrose) should be used in place of cane sugar (sucrose).

Elevated serum transaminase levels.

In clinical trials at doses of 50 mg t.i.d. and 100 mg t.i.d., the incidence of serum transaminase elevations with acarbose was the same as placebo. In long-term studies (up to 12 months, and including acarbose doses up to 300 mg t.i.d.) conducted in the U.S., treatment-emergent elevations of serum transaminases (ALT and/or AST) occurred in 15% of acarbose-treated patients as compared to 7% of placebo-treated patients. The elevations were asymptomatic, reversible, more common in females and in general, were not associated with other evidence of liver dysfunction.
Patients' liver enzyme values should be monitored regularly, preferably at monthly intervals for the first 6 to 12 months after initiation of acarbose therapy. If elevated transaminases are observed, a reduction in dosage or withdrawal of therapy may be warranted, particularly if the elevations persist. In such circumstances, patients should be monitored at weekly intervals until normal values are established.

Use in hepatic impairment.

No data available.

Use in renal impairment.

No data available.

Use in the elderly.

See Section 4.2 Dose and Method of Administration.

Paediatric use.

Since there is insufficient data on the safety and efficacy of acarbose in children, acarbose should not be used in patients under 18 years of age.

Effects on laboratory tests.

Small reductions in haematocrit occurred more often in acarbose-treated patients than in placebo-treated patients but were not associated with reductions in haemoglobin. Low serum calcium and low plasma vitamin B6 levels were associated with acarbose therapy but were thought to be either spurious or of no clinical significance.

4.5 Interactions with Other Medicines and Other Forms of Interactions

General.

Certain drugs tend to produce hyperglycaemia and may lead to loss of blood glucose control. These drugs include diuretics (thiazides, furosemide (frusemide)), corticosteroids, phenothiazines, thyroid products, oestrogens, oral contraceptives, phenytoin, nicotinic acid, sympathomimetics and isoniazid. When such drugs are administered to a patient receiving acarbose, the patient should be closely monitored for loss of blood glucose control.

Oral antidiabetic agents.

When acarbose is prescribed in addition to existing treatment with sulfonylureas, or metformin, the dosage of the sulfonylurea or metformin must be appropriately reduced, should the blood glucose levels fall in the hypoglycaemic range. In individual cases hypoglycaemia-related impairment of consciousness may occur.

Neomycin.

Due to neomycin-induced malabsorption of carbohydrate, concomitant administration of neomycin may lead to an enhanced reduction of postprandial blood glucose and to an increase in the frequency and severity of gastrointestinal adverse reactions. If the symptoms are severe, a temporary dose reduction of acarbose may be warranted.

Colestyramine.

The concomitant administration of colestyramine may enhance the effects of acarbose, particularly the reduction of postprandial insulin levels. If both acarbose and colestyramine therapy are withdrawn simultaneously, caution should be exercised as a rebound phenomenon has been observed in non-diabetic subjects.

Digoxin.

In individual cases, acarbose may affect digoxin bioavailability, which may require dose adjustment of digoxin.

Intestinal adsorbents.

On the basis of general considerations, the simultaneous use of intestinal adsorbents (e.g. charcoal), and digestive enzyme preparations (e.g. amylase, pancreatin) may reduce the effect of acarbose and should be avoided wherever possible.

Antacids.

The concomitant administration of acarbose and antacids does not alter the effect of acarbose. The administration of antacid preparations is unlikely to ameliorate the gastrointestinal symptoms of acarbose and therefore should not be recommended for this purpose.

4.6 Fertility, Pregnancy and Lactation

Effects on fertility.

Fertility studies in rats after oral administration produced no untoward effect on fertility or on the overall capacity to reproduce at oral dose levels of 540 mg/kg/day (approximately half the exposure at the maximal therapeutic dose based on the AUC in rats).
(Category B3)
Studies in rats and rabbits have not yielded any evidence of teratogenic or embryotoxic effects due to acarbose when administered at oral doses up to 540 and 480 mg/kg/day, respectively (approximately half the exposure at the maximal therapeutic dose based on the AUC in rats). At oral doses of 480 mg/kg/day, acarbose caused resorptions in rabbits and increased prenatal losses in rats during organogenesis, but was not teratogenic. There are, however, no adequate and well-controlled studies in pregnant women.
Acarbose should not be administered during pregnancy as no information from controlled clinical studies is available on its use in pregnant women.
Acarbose and/or its metabolites are secreted into milk in rats, with milk levels reaching ten times the maternal plasma levels. No information is available on the concentrations of acarbose or its metabolites which may appear in human milk following administration of acarbose. Consequently, acarbose should not be administered to nursing mothers unless the benefit outweighs the possible risk.

4.7 Effects on Ability to Drive and Use Machines

The effects of this medicine on a person's ability to drive and use machines were not assessed as part of its registration.

4.8 Adverse Effects (Undesirable Effects)

The majority of adverse experiences reported to acarbose are gastrointestinal, such as flatulence, diarrhoea and abdominal pain, which result from the pharmacodynamic action of the drug. The majority of symptoms are of mild or moderate intensity and are dose-dependent. In studies of ≥ 6 months duration, the symptoms occurred early (within 1-2 months of treatment) and improved tolerability with longer duration of treatment was observed. Failure to adhere to the prescribed diabetic diet, however, can lead to an intensification of these symptoms. Rarely, these gastrointestinal events may be severe and be confused with or due to ileus (see Section 4.3 Contraindications). In individual cases hypersensitive skin reactions may occur e.g. erythema, exanthema and urticaria. Rarely, cases of hepatitis and/or jaundice have been reported.
The frequency of adverse drug reactions reported with acarbose based on placebo-controlled studies with acarbose sorted by CIOMS III categories of frequency (placebo-controlled studies in clinical trial database: acarbose N = 8,595; placebo N = 7,278; status: 10 Feb 2006) are summarized in Table 1.
Within each frequency grouping, undesirable effects are presented in order of decreasing seriousness. Frequencies are defined as very common (≥ 1/10), common (≥ 1/100 to < 1/10), uncommon (≥ 1/1,000 to < 1/100) and rare (≥ 1/10,000 to < 1/1,000).
Soft stools are often produced by acarbose, but if the dosage of the individual case is too high, or after simultaneous ingestion of cane sugar, the stools can become unformed or even liquid. Should diarrhoea persist, patients should be closely monitored and the dosage reduced, or therapy withdrawn, if necessary.
In addition events reported as liver disorder, hepatic function abnormal, and liver injury have been received especially from Japan. Five cases of fulminant hepatitis with fatal outcome have been reported in Japan. A relationship to acarbose cannot be excluded.

Post marketing adverse event reports.

Blood and lymphatic system disorders.

Unknown frequency: thrombocytopenia.

Immune system disorders.

Unknown frequency: allergic reaction (rash, erythema, exanthema, urticaria).

Gastrointestinal disorders.

Unknown frequency: subileus/ileus, pneumatosis cystoides intestinalis.

Hepatobiliary disorders.

Unknown frequency: hepatitis.

Elevated serum transaminase levels.

See Section 4.4 Special Warnings and Precautions for Use.

Reporting suspected adverse effects.

Reporting suspected adverse reactions after registration of the medicinal product is important. It allows continued monitoring of the benefit-risk balance of the medicinal product. Healthcare professionals are asked to report any suspected adverse reactions at www.tga.gov.au/reporting-problems.

4.9 Overdose

Overdosage of acarbose taken with food and/or drinks containing carbohydrates, can result in an exacerbation of the intestinal effects, i.e. diarrhoea, flatulence, and tympanism.
In the event of overdose with acarbose in the absence of food, excessive intestinal effects are not expected to occur. Hypoglycaemia is unlikely to occur.
Carbohydrate containing food and/or drinks should be avoided for 4-6 hours following overdosage with acarbose.
Diarrhoea should be treated by standard conservative measures.
For information on the management of overdose, contact the Poisons Information Centre on 13 11 26 (Australia).

5 Pharmacological Properties

5.1 Pharmacodynamic Properties

Mechanism of action.

Acarbose exerts its activity in the intestinal tract. In contrast to sulfonylureas, it has no stimulatory action on the pancreas.
The action of acarbose depends on an inhibition of intestinal enzymes (alpha-glucosidases) involved in the degradation of ingested disaccharides, oligosaccharides, and polysaccharides, but not monosaccharides. Maximal specific inhibitory activity is against sucrase. This leads, dose dependently, to a delayed digestion of the above carbohydrates. The result is that absorbable monosaccharides (dextrose) originating from carbohydrates are released more slowly and hence more slowly taken up into blood. Absorption of monosaccharides is not affected. In this way, acarbose reduces the postprandial rise in blood glucose, the blood-glucose fluctuations in the course of the day become truncated, and the mean blood-glucose level is reduced. Acarbose lowers abnormally high levels of glycosylated haemoglobin.

Clinical trials.

Clinical experience in non-insulin dependent diabetes mellitus (NIDDM) patients on dietary treatment only.

Results from six controlled, fixed-dose, monotherapy studies of acarbose in the treatment of NIDDM, involving 769 acarbose-treated patients, were combined and a weighted average of the difference from placebo in the mean change from baseline in glycosylated haemoglobin (HbA1c) was calculated for each dose level as presented in Table 2.

Clinical experience in NIDDM patients receiving sulfonylureas.

Acarbose was studied as adjunctive therapy to sulfonylurea treatment in two large, placebo-controlled, double-blind, randomised studies of 24 weeks duration, in which 540 patients were included in the efficacy analysis. In addition, acarbose was studied as adjunctive therapy to sulfonylurea treatment in a third study of one year duration, in which patients were stratified according to background therapy. Study 1 (Table 3) involved patients under treatment at entry with diet alone who were subsequently randomised to four treatment groups. At the end of the study, patients in the acarbose + tolbutamide group showed a mean treatment effect on glycosylated haemoglobin (HbA1c) of -1.78% and were receiving a significantly lower mean daily dose of tolbutamide than patients in the tolbutamide-alone group. Also, the efficacy in the acarbose + tolbutamide groups was significantly better than in the other three treatment groups. Study 2 (Table 3) involved patients taking background treatment with maximum daily doses of sulfonylureas. At the end of this study, the mean effect of the addition of acarbose to maximum sulfonylurea therapy was a change in HbA1c of -0.54%. In addition, there was a significantly greater proportion of patients in the acarbose + sulfonylurea group who reduced their sulfonylurea dose as compared to patients in the placebo + sulfonylurea group. In Study 3 (Table 3), the addition of acarbose to a background treatment of sulfonylurea in 96 patients produced an additional change in mean HbA1c of -0.9%.

Clinical experience in NIDDM patients receiving metformin.

Acarbose was also studied as adjunctive therapy to metformin treatment in a one year study (Study 3). In this study (Table 3), the addition of acarbose to 74 patients on metformin treatment produced an additional change in mean HbA1c of -0.8%.
As can be seen by the above studies, acarbose lowers HbA1c levels either alone or in combination with other oral hypoglycaemic agents. Overall 58% of the NIDDM patients studied were women. There is no long-term data on morbidity and mortality.

5.2 Pharmacokinetic Properties

Absorption.

One to 2% of an oral dose of acarbose is absorbed from the gastrointestinal tract as unchanged drug. After the oral administration of 200 mg 14C-labelled acarbose (200 mg) to 6 healthy volunteers, approximately 35% of total radioactivity (changed and unchanged drug) appeared in the urine. An average of 51% of the oral dose was excreted in the faeces as unabsorbed drug-related radioactivity within 96 hours of ingestion. The proportion of active substance excreted in the urine was 1.7% of the administered dose. The low systemic bioavailability of the parent drug is therapeutically desired, because acarbose acts locally within the gastrointestinal tract. Following oral dosing with acarbose, peak plasma concentrations of radioactivity were attained 14 - 24 hours after dosing (586.3 ± 282.7 microgram/L after 20.7 ± 5.2 hours), while peak plasma concentrations of active drug were attained at approximately 1 hour (52.2 ± 15.7 microgram/L after 1.1 ± 0.3 hours). The delayed absorption of acarbose-related radioactivity reflects the absorption of metabolites that may be formed by either intestinal bacteria or intestinal enzymatic hydrolysis.

Metabolism.

Acarbose is metabolised exclusively within the gastrointestinal tract, principally by intestinal bacteria, but also by digestive enzymes. A fraction of these metabolites (approximately 34% of the dose) was absorbed and subsequently excreted in the urine. At least 13 metabolites have been separated chromatographically from urine specimens. The major metabolites have been identified as 4-methylpyrogallol derivatives (i.e. sulfate, methyl, and glucuronide conjugates). One metabolite (formed by the cleavage of a glucose molecule from acarbose) also has α-glucosidase inhibitory activity. This metabolite, together with the parent compound, recovered from the urine, accounts for less than 2% of the total administered dose.

Excretion.

The fraction of acarbose that is absorbed as intact drug is almost completely excreted by the kidneys. When acarbose was given intravenously, 89% of the dose was recovered in the urine as active drug within 48 hours. In contrast, less than 2% of an oral dose was recovered in the urine as active (i.e. parent compound and active metabolite) drug. This is consistent with the low bioavailability of the parent drug. The plasma elimination half-life of acarbose activity is approximately 2 hours in healthy volunteers. Consequently, drug accumulation does not occur with three times a day (t.i.d.) oral dosing.

5.3 Preclinical Safety Data

Genotoxicity.

Acarbose showed no genotoxic potential in a series of assays for gene mutations, chromosomal damage and DNA damage.

Carcinogenicity.

Acarbose increased the incidences of hypernephroid carcinomas and cortical adenomas of the kidneys and Leydig cell tumours in the testes of Sprague-Dawley rats at dietary concentrations of approximately 23 mg/kg/day and under conditions of severe malnutrition developing from glucosidase inhibition (reduced glucose utilisation, loss of isocaloric state).

6 Pharmaceutical Particulars

6.1 List of Excipients

In addition to acarbose, Acarbose Viatris tablets contain the following inactive ingredients: microcrystalline cellulose, pregelatinised maize starch, colloidal anhydrous silica and magnesium stearate.

6.2 Incompatibilities

Incompatibilities were either not assessed or not identified as part of the registration of this medicine.

6.3 Shelf Life

In Australia, information on the shelf life can be found on the public summary of the Australian Register of Therapeutic Goods (ARTG). The expiry date can be found on the packaging.

6.4 Special Precautions for Storage

Store below 25°C. Protect from moisture.

6.5 Nature and Contents of Container

Acarbose Viatris is available in PVC/PE/PVDC/Al blister packs of 90 tablets.

Australian register of therapeutic goods (ARTG).

AUST R 226796 - Acarbose Viatris acarbose 50 mg tablet blister pack.
AUST R 226797 - Acarbose Viatris acarbose 100 mg tablet blister pack.

6.6 Special Precautions for Disposal

In Australia, any unused medicine or waste material should be disposed of by taking to your local pharmacy.

6.7 Physicochemical Properties

Chemical structure.


Acarbose Viatris contains acarbose which is a complex oligosaccharide of microbial origin. Acarbose is made up of an unsaturated cyclitol unit, an amino sugar and a maltose residue. Acarbose is a white or yellowish powder with a molecular weight of 645.6. Acarbose is very soluble in water and has a pKa of 5.1. The empirical formula is C25H43NO18.

CAS number.

56180-94-0.

7 Medicine Schedule (Poisons Standard)

S4: Prescription Only Medicine.

Summary Table of Changes