Generic

Metformin Hydrochloride

Indications

Treatment of type 2 diabetes, especially in overweight patients whose diet and exercise alone cannot lead to adequate blood sugar control.

Adults: Metformin can be used as a monotherapy or in combination with other oral hypoglycemic drugs or insulin.

In children and adolescents over 10 years of age: Metformin can be used alone or in combination with insulin.
Diabetic complications have been reduced in overweight adults with type 2 diabetes who used metformin as the first-line treatment after a diet failure.

Pharmacology

Metformin is a biguanide oral hypoglycemic agent used to treat type 2 diabetes. It lowers basal and postprandial blood sugar. Its mechanism of action is different from that of sulfonylureas and it does not produce hypoglycemia. Metformin reduces glucose production in the liver, reduces intestinal glucose absorption, and improves insulin sensitivity by increasing peripheral glucose uptake and utilization.

Dosage & Administration

Metformin immediate release tablet: Dosage of Metformin Hydrochloride must be individualized on the basis of both effectiveness and tolerance, while not exceeding the maximum recommended daily doses.

• Adult: The usual starting dose of Metformin is 500 mg twice a day or 850 mg once a day, given with meals. Dosage increases should be made in increments of 500 mg weekly or 850 mg every 2 weeks, up to a total of 2000 mg per day, given in divided doses. For those patients requiring additional glycemic control, Glucomin may be given to a maximum daily dose of 2550 mg per day. Doses above 2000 mg may be better tolerated given three times a day with meals.
• Children: The usual starting dose of Metformin is 500 mg twice a day, given with meals. Dosage increases should be made in increments of 500 mg weekly up to a maximum of 2000 mg per day, given in divided doses.

Metformin extended release tablet: Swallow Metformin XR tablet whole and never crush, cut or chew.

• Adult: The usual starting dose of Metformin XR is 500 mg once daily with the evening meal. Dose should be increased in increments of 500 mg weekly, up to a maximum of 2000 mg once daily with the evening meal, alternatively increased to 1000 mg twice daily taken with meal. Patient receiving Metformin immediate release tablet may be switched to Metformin extended release tablet up to a maximum recommended daily dose.
• Children: Metformin extended release tablet has not been studied in children.
• Renal impaired patient: Do not use Metformin in patients with eGFR below 30 mL/min/1.73 m². Asses risk/benefit of counting if eGFR falls below 45 mL/min/1.73 m².

Interactions

Combined use with carbonic anhydrase (topiramate, zonisamide) may increase the risk of lactic acidosis. Medicines that reduce the clearance of metformin (ranolazine, dotegravir, cimetidine) can increase the accumulation of metformin. Alcohol can enhance the effect of metformin on lactic acid metabolism.

Contraindications

Allergic to active ingredients or any excipient.
Any type of acute metabolic acidosis (such as lactic acidosis, diabetic ketoacidosis).
Severe renal impairment (GFR <30 ml / min).
Acute conditions that can impair kidney function, such as dehydration, severe infection, shock.
Acute or chronic diseases, which can cause tissue hypoxia, such as: heart or respiratory failure, recent myocardial infarction, shock, liver failure, acute alcoholism, alcoholism.

Side Effects

Blood and lymphatic system disorders: Not known: Hemolytic anemia

Metabolism and nutrition disorders: Very rare: Lactic acidosis. Decrease of vitamin B12 absorption with a decrease of serum levels during long-term use of metformin. Consideration of such etiology is recommended if a patient presents with megaloblastic anemia. Cases of peripheral neuropathy in patients with vitamin B12 deficiency have been reported in post-marketing experience (frequency not known)

Nervous system disorders: Common: Taste disturbance. Not known: Encephalopathy

Gastrointestinal disorders: Very common: Gastrointestinal disorders, such as nausea, vomiting, diarrhea, abdominal pain, and loss of appetite. These undesirable effects occur most frequently during the initiation of therapy and resolve spontaneously in most cases. To prevent them, it is recommended that metformin be taken in 2 or 3 daily doses during or after meals. A slow increase of the dose may also improve gastrointestinal tolerability.

Hepatobiliary disorders: Very rare: Isolated reports of liver function test abnormalities or hepatitis resolving upon metformin discontinuation.

Skin and subcutaneous tissue disorders: Very rare: Skin reactions, such as erythema, pruritus, urticaria.

Pregnancy

Pregnancy: Uncontrolled diabetes during pregnancy (pregnancy or permanent) is associated with an increased risk of birth defects and perinatal mortality. When the patient plans to become pregnant and during pregnancy, it is recommended not to use metformin to treat diabetes, but to use insulin to keep blood glucose levels as close to normal as possible to reduce the risk of fetal malformations.
Breastfeeding: Metformin is secreted in breast milk. No adverse reactions were observed in breastfed newborns / infants. However, due to the limited data available, breastfeeding is not recommended during treatment with metformin. The benefits of breastfeeding and the potential risks of adverse effects in children must be considered, and a decision must be made to stop breastfeeding.

Precautions

It is known that a large amount of metformin hydrochloride is excreted by the kidneys, and the risk of metformin accumulation and lactic acidosis increases as the degree of renal damage increases. Metformin can lower vitamin B12 levels. When combined with insulin or insulin secretagogues, it also increases the risk of hypoglycemia.

Therapeutic Class

Biguanides

Storage Conditions

Keep below 30°C temperature, protected from light & moisture. Keep out of the reach of children.

Pharmaceutical Name

Healthcare Pharmaceuticals Ltd.