Metformin

Chemical name

N,N-Диметилимиддикарбо имиддиамид (and as hydrochloride)

Gross

C4-H11-N5

Characteristics

White or colourless crystalline powder. It is soluble in water and almost nerastvorim in acetone, ether and chloroform.

Of drugs

The drugs-gipoglikemicescoe. Lowers glucose concentration (prandial and after meals) in the blood and the level of haemoglobin glikozilirovannogo increases tolerance to glukoze. Decreases intestinalnuu absorption of glucose, its products in the liver potenziruet sensitivity insulino peripheral tissues (increases glucose uptake and metabolism). Do not alter the secretion of insulin beta-kletkami islets pancreas (insulin level, as measured prandial and daily insulin response may even decline). Normalizes lipid profile blood plasma in patients insulinnezawisimam diabetes : Reduce the triglycerides, cholesterol and reasonable (as defined prandial), and does not alter the levels of high density lipoprotein etc. densities. 4-3 or reduce estate тела.Экспериментальн��е animal studies in doses three times greater than MRDC converted on the surface of the body, not identified mutagenic, carcinogenic, teratogenic properties and the impact on Fertilnosti.bystro drawn from the blood. Absolute bioavailability (prandial) is 50-60%. C_max (approximately 2 µ g / ml or 15 micromole) in the plasma is achieved in 2 hours Away C_max reduced by 40% and slowed its achievement in 35 minutes. Suction blood from the end on the 6900 and the concentration in the blood is gradually lowered (plasma level within 24 to 48 hours at less than 1 µ g / ml). The volume of distribution (for the dose 850 mg) 654 is 358 litres. Light is associated with plasma proteins, can accumulate in the salivary glands, the liver and kidneys. Report the news (kanaltsevaya secretia) unchanged to (90% per day). Kidney Cl-79 ml / min. T_1/2 is 6.2 hrs (plasma), and 17.6 hours (blood) (the difference can be explained by the capacity of koumoulirovati in erythrocytes). Older prolongiruetsa T_1/2 and C_max increases. When violations of kidney longer T_1/2 and reduced kidney Cl.

Indications

Diabetes mellitus type 2, with the ineffectiveness of correction io dietterapiei, incl. in combination with sulfonylureas drugs; diabetes mellitus type 1 as a supplement to insulinoterapii.

Restrictions on the use of

Children's (the effectiveness and safety of the children to be determined) and the elderly (over 65 years), age (as a result of a slow metabolism, it is necessary to weigh the benefit / risk).

Pregnancy and lactation

Contraindicated. At the time of treatment should stop breastfeeding.

Contraindications

Hypersensitivity, kidney disease or renalnaya insufficiency (creatinine level of more than 0.132 mmol / l for men and 0.123 mmol / L in women) expressed liver disorder, cardiac and respiratory distress, the acute phase of myocardial infarction, infectious diseases, extensive operations and injuries, chronic alcoholism, acute or chronic metabolic acidosis, including diabetic ketoacidosis with coma or not, the research use of radioactive isotopes of iodine, pregnancy, breast-feeding.

Side-Effects

For part of the intestine : at the beginning of treatment (5-20%), anorexia, diarrhoea, nausea, vomiting, flatulence, abdominalnaya pain (reduced to the reception at meal times); Metallic taste (not more than 3% of cases). From the circulatory system and blood (blood, gemostaz) : in a few cases, megaloblastnaya anaemia (the result of vitamin intake B_12 and folic acid). From metabolism : in extremely rare cases, lactate acidosis (weakness, drowsiness, gipotenzia, reflected bradiaritmia, respiratory violations, the pain in the abdomen, mialgia, hypothermia), Gipoglikemia.so the skin : skin and dermatitis.

Patient interaction

Effect weaken tiazidnye etc. dioretiki, corticosteroids, fenotiazina, hormones thyroid, estrogena, oral contraceptives, phenytoin, nikotinova acid simpatomimetiki, calcium antagonists, isoniazid. The increase insulin, sulfonylureas derivatives, acarboza, NPVS, MAO inhibitors, auxitetratziklin, ACE inhibitors, derivatives klofibrata, cyclophosphamide, beta-adrenoblokatora. Furosemide C_max increases by 22%. Nifedipin increases removals C_max, prolong down. Drugs (amiloride, digoxin, morphine, procainamide, quinidine, quinine, ranitidine, triamteren and vancomycin), secretirutesa in bone compete for tubularnae transportation systems, and long-term therapy can increase C_max by 60%. Decreases C_max and T_1/2 furosemida at 31% and 42.3%, respectively. Incompatible with alcohol (elevated risk of dairy azidoza).

Overdosing

Symptoms : lactate Azidoz.lechenie : Hepatology, symptomatic therapy.

Precautions

It continuously monitor kidney function, glomeruljarnuu filter, the level of glucose in the blood. The once a year to determine the content of vitamin B_12. In translating the patient to the vial, he appointed immediately after the previous product, except for the replacement of hlorpropamida (a week break for treatment from long T_1/2 preparation). Do not use before surgery, and within two days after the elections, as well as during the two days before and after the diagnosis (in / in urografia, angiography, etc.). Nor should appoint people doing difficult physical work (due to increased risk of lactatnogo azidoza).

Dosing and Administration

Inside during or after delivery. Dose selected individually, but not more than 3 g / day in a few receptions.

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