RECIPE:
Metformin HCl ................................................ .................. 500 mg
Glibenclamid ... .................................... 2.5 mg
Excipients q.s ... .............................................. 1 member
(Avicel, lactose, PVP K30, croscarmellose sodium, magnesium stearate, HPMC, PVA, PEG 6000, titanium dioxide, talc, yellow iron oxide color, red iron oxide color).
DOSAGE FORM: Film-coated tablets.
PRESENTATION: Box of 3 blisters x 10 tablets.
PHARMACODYNAMICS: GliritDHG 500mg / 2.5mg is a drug to treat type 2 diabetes, with the main active ingredient is metformin combined with glibenclamide. Metformin belongs to the biguanid group, whose mechanism of peripheral action is to increase the use of glucose in cells, improve the association of insulin with receptors, inhibit glucose synthesis in the liver and reduce intestinal absorption of glucose. Metformin has no hypoglycemic effect in people without diabetes. In people with diabetes, metformin reduces hyperglycemia but does not cause catastrophic hypoglycemic events unless fasting or a synergistic combination. Glibenclamide is a sulfonylurea that reduces blood glucose levels, mainly by stimulating pancreatic beta cells to increase endogenous insulin secretion. During short-term treatment, the blood glucose level decreases because the drug reduces the glucose flow of the liver into the blood and increases the insulin effect on peripheral target cells. With long-term use of glibenclamide, blood insulin levels drop to the levels they were before treatment, but glucose tolerance continues to improve. Although the mechanisms of action of metformin and glibenclamide are different, they complement one another and may have synergistic effects on glycemic control when monotherapy does not control blood sugar as required.
PHARMACOKINETICS: Metformin is slowly and incompletely absorbed from the gastrointestinal tract. The absolute bioavailability of 500 mg metformin orally on fasting is approximately 50 - 60%. There is no proportion to the dose when increasing the dose, due to reduced absorption. Food reduces the rate of absorption and slows down the absorption of metformin. Metformin is not metabolized in the liver and is not excreted in the bile. Metformin is excreted by the kidneys as a non-metabolized form. The plasma half-life is 1.5 - 4.5 hours.
Glibenclamide is well absorbed from the gastrointestinal tract. Food does not affect the rate and extent of absorption of the drug. Duration of effect is 45 - 60 minutes and reaches a maximum within 1.5 - 3 hours. The volume of distribution of glibenclamide is about 0.125 liters / kg, the average elimination half-life is 1.4 - 1.8 hours, and may be prolonged in patients with hepatic or renal impairment. It is usually possible to take the medication only once a day. Glibenclamide is completely metabolized in the liver to active metabolites and excreted in urine and feces.
INDICATIONS: Treatment of type 2 diabetes mellitus to control blood sugar, combined with diet and exercise.
CONTRAINDICATIONS: Patients with a history of hypersensitivity to metformin, glibenclamide, sulfonamides, diuretics with active ingredient sulfonamide or probenecid or any of its ingredients.
Insulin-dependent diabetes mellitus (type 1 diabetes). Type 2 diabetes mellitus for people under 18. Complicated diabetes mellitus. Diabetes when stressed.
Patients with acute catabolic state, severe infection, sepsis, trauma, severe respiratory disease with hypoxemia, hyperglycemia with or without coma, severe acidosis due to hyperglycemia, impairment congestive heart, cardiovascular collapse, acute myocardial infarction.
Severe liver or kidney damage, severe malnutrition. Exacerbations of chronic disease.
Patients with severe renal impairment (eGFR less than 30 mL / minute / 1.73 m2) [see Warnings and precautions].
Patients with acute or chronic metabolic acidosis, including diabetic ketoacidosis.
PRECAUTIONS: Adherence to the diet and medication are crucial for successful treatment and to prevent undesirable changes in blood glucose levels.
Hypoglycemia is more likely to occur when you eat less, exercise excessively, prolong, or when drinking alcohol, or when used in combination with another blood glucose lowering medication.
Undernourished, hardened brain arteries.
Lactic acidosis
After-sales surveillance has documented metformin-associated lactic acidosis, including fatalities, hypothermia, hypotension, persistent bradycardia. The onset of metformin-associated lactic acidosis is usually not easily detected, accompanied by atypical symptoms such as malaise, myalgia, respiratory failure, drowsiness and abdominal pain. Lactic acidosis associated with metformin is characterized by increased lactate concentration in the blood (> 5 mmol / L), anion gap (without evidence of urinary or diabetic ketoacidosis), an increase in the lactate / pyruvate ratio and plasma metformin levels generally increase> 5µg / mL.
Measures to minimize the risk and management of metformin acid lactic acidosis in high-risk patients are detailed in the drug use leaflet (Dosage and administration, Contraindications, Warnings and precautions, Drug Interactions and Drug Use on special subjects).
If lactic acidosis is suspected of being related to metformin, stop using metformin, promptly take the patient to hospital and take preventive measures. In patients who have been treated with metformin, have been diagnosed with lactic acidosis or are suspected of having a high likelihood of lactic acidosis, it is recommended that fast dialysis be used to correct the acidosis situation and to remove the accumulated metformin ( metformin hydrochloride can be dialysed with a clearance of 170 mL / min under good hemodynamic conditions). Dialysis can reverse symptoms and recover.
Educate patients and family members about the symptoms of lactic acidosis and if these symptoms occur, discontinue the medication and report these symptoms to the doctor.
For each factor that increases the risk of metformin-associated lactic acidosis, recommendations are made to minimize the risk and manage the metformin-associated lactic acidosis, specifically as follows:
Renal impairment: Lactic acidosis associated with metformin during after-sales drug monitoring occurs primarily in patients with severe renal impairment. The risk of metformin accumulation and lactic acidosis associated with metformin increases with the severity of renal failure because metformin is eliminated mainly by the kidneys. Clinical recommendations based on the patient's renal function include [see Dosage and administration, Clinical pharmacology]:
- Before starting treatment with metformin it is necessary to estimate the patient's glomerular filtration rate (eGFR).
- Metformin contraindicated in patients with eGFR below 30 mL / minute / 1.73 m2 [see section Contraindications].
- It is not recommended to start treatment with metformin in patients with eGFR ranging from 30-45 mL / min / 1.73 m2.
- Collect data on eGFR at least once a year in all patients using metformin, in patients with an increased risk of renal failure (e.g., elderly), renal function should be assessed. more often.
- In patients on metformin and with an eGFR of less than 45 mL / min / 1.73 m2, assess the risks and benefits of continuing the regimen.
Drug interactions: Concomitant use of metformin with certain medications may increase the risk of metformin-associated lactic acidosis: patients with impaired renal function lead to significant hemodynamic changes, affecting weight. by acid-base or by increasing metformin accumulation [see Drug Interactions section]. Therefore, consider monitoring patients more often.
Patients aged 65 years and older: The risk of metformin-associated lactic acidosis increases with the age of the patient because elderly patients are more likely to have liver, kidney, and heart failure than younger patients. Renal function should be assessed more frequently in elderly patients.
Perform diagnostic tests using contrast medicine: Intravascular injection in patients receiving metformin may lead to acute impairment of renal function and cause lactic acidosis. Stop metformin before or at the time of the scan using iodine-containing contrast media in patients with eGFR of 30-60 mL / min / 1.73 m2, patients with a history of impairment liver, alcoholism, heart failure or patients will use contrast dye containing iodine by the artery. Re-evaluate eGFR 48 hours after the scan and use metformin again if kidney function is stable.
Surgery or other procedures: Storing food and fluids during surgery or performing other procedures may increase the risk of volume reduction, hypotension and kidney failure. Metformin should be temporarily discontinued when the patient has a restricted food or fluid intake.
Inhaled hypoxia: Afterschool monitoring has documented a number of metformin-associated lactic acidosis occurring in acute congestive heart failure (especially when accompanied by reduced perfusion and hypoxemia. ). Cardiovascular insufficiency (shock), acute myocardial infarction, sepsis and other conditions associated with hypoxia are associated with lactic acidosis and may also cause pre-renal blood nitrogen. When these events occur, stop metformin.
Alcohol consumption: Alcohol may affect the effect of metformin on lactate metabolism and may thereby increase the risk of metformin-associated lactic acidosis. Warn patients not to drink alcohol while using metformin.
Hepatic Impairment: Patients with hepatic impairment may develop metformin acid-related lactic acidosis due to impaired lactate elimination leading to increased lactate levels in the blood. Therefore, metformin should be avoided in patients who have been diagnosed with liver disease through clinical or laboratory evidence.
PREGNANT WOMEN AND LACTATION: The drug is contraindicated on these subjects.
The development of lactic acidosis is related to metformin due to a decrease in lactate elimination leading to an increase in lactate levels in the blood. Therefore, metformin should be avoided in patients who have been diagnosed with liver disease through clinical or laboratory evidence.
PREGNANT WOMEN AND LACTATION: The drug is contraindicated on these subjects.
DRIVING AND OPERATING MACHINERY: Be cautious when driving and operating machinery because of the risk of hypoglycemia.
INTERACTIONS: Glirit hypoglycemic effect of GliritDHG 500mg / 2.5mg may be increased in combination with sulfonamides, salicylates, phenylbutazone, nonsteroidal anti-inflammatory drugs, fluoroquinolones, cumarin derivatives, beta blockers, monoaminoxydase inhibitors, perhexilin, chloramphenicol, clofibrate and fenofibrate, sulfinpyrazone, probenecid, pentoxifylin, cyclophosphamid, azapropazon, tetracyclin, angiotensin converting enzyme, alcohol, fluconazol, miconazol, eniproflolo
The hypoglycemic effect of GliritDHG 500mg / 2.5mg may be reduced when combined with thiazide diuretics, ethacrynic acid, oral contraceptives containing estrogen / gestagen, phenothiazine derivatives, isoniazid, nicotinic acid (high dose). ), sympathomimetics, thyroid preparations and corticosteroids, salbutamol or terbutalin (intravenously).
Increased toxicity when combined with: cationic (amiloride, digoxin, morphine, procainamide, quinidine, quinine, ranitidine, triamterene, trimethoprim and vancomycin), cimetidine.
UNWANTED EFFECTS:
Usually dose-related and usually occur at the beginning of treatment:
Common: anorexia, nausea, vomiting, diarrhea, epigastric, constipation, heartburn; ban, urticaria, sensuality with light.
Uncommon: dysplasia of blood, aplastic anemia, hemolytic anemia, myelosuppression, thrombocytopenia, agranulocytosis, lactic acidosis.
Rarely: Temporary vision loss.
Inform your doctor unwanted effects encountered when using the drug.
OVERDOSE AND TREATMENT: Hypoglycemic reactions may occur due to an overdose, an interaction with certain medications or a mistake in eating. Manifestations: headache, irritation, restlessness, excessive sweating, insomnia, tremor, behavioral disorders, less alertness, agility.
Remedy by eating sugar (about 20 - 30 g) and immediately notify the doctor. If the patient is in a coma, either saccharose or glucose solution can be injected into the stomach or infused glucose into a vein.
DOSAGE AND ADMINISTRATION: Take the drug about 30 minutes before a meal.
The recommended dose of Metformin
The starting dose for patients not taking metformin is 500 mg, once daily, orally. If the patient does not experience adverse gastrointestinal reactions and needs to increase the dose, an additional 500 mg may be administered at intervals of 1 to 2 weeks. Dosage of metformin should be considered adjusted on a patient-by-patient basis based on patient efficacy and tolerance and does not exceed the maximum recommended dose of 2000 mg / day.
Dosage of GliritDHG
Initial dosage: usually take 1 tablet of GliritDHG 500mg / 2.5mg 30 minutes before breakfast. If you need to adjust the dose, after 2 weeks, increase to 1 tablet of GliritDHG 500mg / 5mg
Maximum dose: 2000 mg / 20 mg / day (4 tablets GliritDHG 500mg / 5mg / day). Drink before meals.
Each dose should be explored individually to avoid hypoglycemia.
Patients must follow the diet according to the instructions of the treating doctor.
Recommended use of the drug in patients with renal insufficiency
Assess renal function before initiating treatment with metformin and evaluate periodically thereafter.
Metformin is contraindicated in patients with eGFR below 30 mL / minute / 1.73 m2
Treatment with metformin is not recommended in patients with eGFR ranging from 30-45 mL / min / 1.73 m2.
In patients who are on metformin and have an eGFR of less than 45 mL / min / 1.73 m2, assess the risk - benefit of continued treatment.
Stop using metformin if the patient has an eGFR that falls below 30 mL / minute / 1.73 m2 [see Contraindications, Warnings and Precautions section].
Stop using metformin when doing imaging tests using iodine-containing contrast media
In patients with an annual eGFR of 30 - 60 mL / minute / 1.73 m2, in patients with a history of liver disease, alcoholism or heart failure, or in patients who will receive contrast drugs photodiodes contain iodine via arteries, stop metformin before or at the time of carrying out diagnostic imaging tests using iodine-containing contrast media. Re-evaluate the eGFR after 48 hours of metformin scan if the kidney function is stable [see Warnings and precautions].
Or as directed by a physician.
Read the directions carefully before use.
If you need further information, please consult your doctor.
This drug is for a doctor's prescription.
Expiry date: 36 months from date of manufacture.
Storage conditions: Store in dry places, not exceeding 30oC, protect from light.
Standard: TCCS....
Treatment of hypertension, especially in patients with metabolic complications such as diabetes. Treatment of chronic stable angina, coronary angina.
Atorlip is used in the following cases: increased total cholesterol, increased LDL-cholesterol, increased triglycerides.
Atorlip is used in the following cases: increased total cholesterol, increased LDL-cholesterol, increased triglycerides.
Primary hypertension for uncontrolled blood pressure subjects with monotherapy.
