Acarbose

Drug #25

Acarbose is an oligosaccharide analog. It was the first a-glycoside hydrolase inhibitor to be used therapeutically in regulating intestinal carbohydtare digestion and absorption. Acarbose is isolated from fermentation of Actinomyces in culture broth containing both glucose and maltose. Acarbose is oral hypoglycemic agent. Acarbose is used along with diet in the treatment of diabetes to reduce the high blood sugar level. For maximum therapeutic effects, it must be used along with a proper diet and a regular exercise program. It has been recently approved by the FDA for use.

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Primary Characteristics

It is of Semi Synthetic origin and belongs to D-Glucopyranose.

It belongs to Alpha-Glycoside hydrolase inhibitor pharmacological group on the basis of mechanism of action and also classified in Hypoglycemic Agent pharmacological group. It is also classified under Drugs Afecting Glucose Metabolism .

Molecular Weight: 646 · pK_a: 12.01 · Solubility in Water: very soluble · Solubility in Alcohol: 1 in 10 · Non-proprietary name: Acarbose.

Pharmacokinetics

Absorption: Acarbose has an oral bioavailability is 1.5% (±0.5%).

Distribution: Acarbose has a volume of distribution is 0.32 l/kg. plasma protein binding is 13-18%.

Elimination: it is metabolised via 33%, plasma half-life is 2.8 hr, renal excretion is 35%.

Indications

Acarbose is primarily indicated in conditions like Chronic acidotic states, Diabetes mellitus, Duodenal or benign gastric ulcer associated with H.pylori, Prostate cancer, flare with initial gonadorelin therapy.

Acarbose is also indicated for secondary conditions like Secondry bacterial infection of acute bronchitis.

Contraindications

Acarbose is contraindicated in conditions like Eclampsia.

Dosage

Acarbose's dosage details are as follows:

Dose	Single Dose	Frequency	Route	Instructions
Adult Dosage
62.5 mg	62.5 mg	Every 8h	PO	Before meals
175 mg	175 mg	Every 8h	PO	Drug is effective when high fibre diet is given
Paediatric Dosage (20kg)
0 – 0	—	—	—	Not Recommended in this Age Group
Neonatal Dosage (3kg)
0 – 0	—	—		Not recommended in this age group

Drug Interactions

Unknown3 interactions

4 interactions

Always consult your physician for the change of dose regimen or an alternative drug of choice that may strictly be required.

Side Effects

Acarbose produces potentially life-threatening effects which include Acute Renal Failure. Careful monitoring is needed with proper medical management.

The signs and symptoms that are produced after acute overdosage of Acarbose are Carbohydrate malabsorption.

Acarbose is known to cause more or less tolerable side effects which are usually transient. These include Abdominal distension, Dizziness, Flatulence, Headache, Loose stools, Nausea, Sleepiness, Vertigo, Weakness.

Warnings / Precautions

Acrabose should be used with caution in patients with kidney disease, liver disease, stomach, digestive or intestinal disorders, iron deficiency or if have any allergies. It may be difficult to control blood sugar during times of stress such as fever, infection, injury or surgery, consult the doctor if additional medication may be required, because Acarbose prevents the breakdown of table sugar, patients should have a readily available source of glucose (such as glucose tablets) to treat symptoms of low blood sugar if taking Acarbose in combination with other medications to treat diabetes. Use with caution during pregnancy. This medication is not recommended for use by nursing women.

Available Brands

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Single Ingredient

Tabs

100 mg 50 mg

Storage Conditions

Acarbose should be stored tab.

Drug Classification

1.18.7.2 — Oral hypoglycemics

Manufacturers

Manufacturers of Acarbose in Pakistan:

Bayer Raazee