Metformin

When ATH:
A10BA02

Characteristic.

Metformin hydrochloride is a white or colorless crystalline powder. It is soluble in water and almost nerastvorim in acetone, ether and chloroform. Molecular weight 165,63.

Pharmacological action.
Hypoglycemic.

Application.

Diabetes mellitus type 2 (especially in cases, accompanied by obesity) the ineffectiveness of correction of hyperglycemia dietary therapy, incl. in combination with sulfonylureas drugs.

Contraindications.

Hypersensitivity, kidney disease or renal failure (creatinine levels more 0,132 mmol/l in men and 0,123 mmol/l in women), expressed human liver; states, accompanied by hypoxia (incl. cardiac and respiratory failure, acute phase of myocardial infarction, acute cerebral circulation insufficiency, anemia); degidratatsiya, infectious diseases, extensive surgery and trauma, Saint Martin's evil, acute or chronic metabolic acidosis, including Diabetic Ketoacidosis with coma or without it, acidosis in history, compliance with a low calorie diet (less 1000 kcal / day), studies using radioactive isotopes, pregnancy, lactation.

Restrictions apply.

Childhood (efficacy and safety of children are not identified), elderly (senior 65 years) age (as a result of slow metabolism it is necessary to assess the risk/benefit ratio). Nor should appoint people, performing heavy physical work (increased risk of laktatnogo azidoza).

Pregnancy and breast-feeding.

When pregnancy is possible, if the effect of therapy outweighs the potential risk to the fetus (adequate and well-controlled studies on the use during pregnancy has not been).

Category actions result in FDA - B. (The study of reproduction in animals revealed no risk of adverse effects on the fetus, and adequate and well-controlled studies in pregnant women have not done.)

At the time of treatment should stop breastfeeding.

Side effects.

From the digestive tract: at the beginning of the course of treatment-anorexia, diarrhea, nausea, vomiting, flatulence, abdominal pain (reduced when administered during a meal); metallic taste in mouth (3%).

Cardio-vascular system and blood (hematopoiesis, hemostasis): in a few cases, megaloblastic anemia (the result of malabsorption of vitamin B12 and folic acid).

Metabolism: gipoglikemiâ; in rare cases, lactate acidosis (weakness, drowsiness, gipotenziya, resistant bradiaritmia, respiratory disorders, abdominal pain, myalgia, gipotermiя).

For the skin: rash, dermatitis.

Cooperation.

Effect of metformin weaken tiazidnye dioretiki and others, corticosteroids, fenotiazinы, glucagon, thyroid hormones, Estrogens, incl. consisting of oral contraceptives, phenytoin, a nicotinic acid, sympathomimetic, calcium antagonists, Isoniazid. In a single dose in healthy volunteers nifedipine increased removals, Cmax and AUC of metformin, Tmax and T1/2 If this is not changed. Gipoglikemicescoe effect increase insulin, sulfonylureas, acarbose, NSAIDs, MAO inhibitors, oxytetracycline, ACE inhibitors, derivatives klofibrata, cyclophosphamide, beta-blockers. Furosemide increases (C)max on 22%. Preparations (amilorid, Digoxin, morphine, prokaynamyd, quinidine, quinones, ranitidine, triamteren and Vancomycin), secreted into the tubules, compete for tubular transport systems and in the long-term therapy may increase Cmax on 60%. Reduces Cmax and T1/2 furosemide on 31 and 42,3% respectively. Zimetidin slows elimination of metformin, as a result of which increases the risk of developing lactic acid acidosis. Incompatible with alcohol (increased risk of acidosis milk).

Overdose.

Symptoms: Lactic acidosis.

Treatment: hemodialysis, simptomaticheskaya therapy.

Dosing and Administration.

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

Precautions.

It continuously monitor kidney function, glomeruljarnuju filter, blood glucose. Particularly careful monitoring of blood glucose is required in the application of metformin in combination with drugs sulfonylureas or insulin (risk of hypoglycemia). Combined treatment with metformin and insulin in hospital should be held prior to the establishment of an adequate dose of each drug. In patients on continuous therapy with metformin should be 1 Once a year to determine the content of vitamin B12 due to a possible reduction of its suction. You must determine the level of lactate in plasma at least 2 once a year, as well as on myalgia. With increasing content of lactate medication overturned. Do not use before surgery and during 2 days after their spending, as well as for 2 days before and after the execution of the diagnostic studies (in/in urografia, angiography etc.).

Cooperation

Active substanceDescription of interaction
AkarʙozaFMR: synergism. Strengthens (mutually) effect.
AmlodipineFMR: antagonizm. Provokes giperglikemia, weakens the effect; with a joint appointment requires constant monitoring of blood glucose concentrations.
BetametazonFMR: antagonizm. Reduces effect; the combined appointment requires constant monitoring of blood glucose concentrations.
BumetanidFMR: antagonizm. Weakens effect (can provoke hyperglycemia); When combined with the appointment of a continuous monitoring glycemia.
VancomycinFKV. Slows excretion (secretiruetsa kanalzami and competes for tubular transport systems), may increase withmax more than half.
VerapamilFMR: antagonizm. Provokes giperglikemia, weakens the effect; When combined with the appointment of a continuous monitoring glycemia.
Gadopentetovaya acidFMR. Against the backdrop of metformin may have a sudden change of kidney.
GidrokortizonFMR: antagonizm. Weakens effect; When combined require increased dose.
GidroxlorotiazidFMR: antagonizm. Weakens effect; joint application requires constant monitoring concentrations of glucose in the blood.
DesogestrelFMR: antagonizm. Weakens effect (can provoke hyperglycemia); joint application requires continuous monitoring of the level of glycemia.
DexamethasoneFMR: antagonizm. Weakens effect; with a joint appointment requires constant monitoring of blood glucose concentrations.
DigoxinFKV. Slows excretion (secretiruetsa kanalzami and competes for tubular transport systems) and can increase Cmax more than half.
DiltiazemFMR: antagonizm. Provokes giperglikemia, weakens the effect; When combined with the appointment of a continuous monitoring glycemia.
DoʙutaminFMR: antagonizm. Reduces effect; with a joint appointment requires constant monitoring of blood glucose concentrations.
DopamineFMR: antagonizm. Weakens effect; with a joint appointment requires constant monitoring of blood glucose concentrations.
IsoniazidFMR: antagonizm. Weakens effect.
IndapamidFMR: antagonizm. Weakens effect; joint application requires constant monitoring concentrations of glucose in the blood.
Insulin dvuhfaznыy [human genetic engineering]FV. FMR: synergism. Strengthens (mutually) effect.
Insulin soluble [pork monocomponent]FMR: synergism. Strengthens (mutually) effect.
YoheksolFMR. Against the backdrop of metformin may have a sudden change of kidney.
Yoksaglovaya acidFMR. Against the backdrop of metformin may have a sudden change of kidney; patients, who will x-ray study using these input parenteral means, metformin should be temporarily cancelled.
YopamydolFMR. Against the backdrop of metformin may have a sudden change of kidney; patients, who will x-ray study using these input parenteral means, metformin should be temporarily cancelled.
KarvedilolFMR: synergism. Do effect; with a joint appointment requires constant monitoring of blood glucose concentrations.
KortizonFMR: antagonizm. Provokes giperglikemia, weakens the effect; the joint appointment of a continuous monitoring glycemia.
LevonorgestrelFMR: antagonizm. Weakens effect; the combined appointment requires constant monitoring of blood glucose concentrations.
Levothyroxine sodiumFMR: antagonizm. Weakens effect; with a joint appointment requires constant monitoring of blood glucose concentrations.
LiotironinFMR: antagonizm. Weakens effect; When combined with the appointment of a continuous monitoring glycemia.
MethylprednisoloneFMR: antagonizm. Provokes giperglikemia, weakens the effect; the joint appointment of a continuous monitoring glycemia.
MorphineFKV. Slows down the selection (secretiruetsa kanalzami and competes for tubular transport systems) and can increase Cmax more than half.
Morphine sulfateFKV. Slows (mutually) allocation (competing for the overall transport system in renal bone).
A nicotinic acidFMR: antagonizm. Weakens effect.
NimodipineFMR: antagonizm. Provokes giperglikemia, weakens the effect; with a joint appointment requires constant monitoring of blood glucose concentrations.
NifedipineFKV. Although it increases the absorption of, FROMmax and prolong the excretion, gipoglikemiceski effect weaken.
NorepinephrineFMR: antagonizm. Weakens effect; combined or consistent application requires greater control over the level of glycemia.
OxytetracyclineFMR: synergism. Do effect.
OctreotideFMR. Changes effect (possible both hypo-, and hyperglycemia); When combined continuous monitoring blood glucose.
PerfenazynFMR: antagonizm. Weakens effect (can provoke hyperglycemia); joint application requires continuous monitoring of the level of glycemia.
Poliestradiola phosphateFMR: antagonizm. Weakens effect (can provoke hyperglycemia); When combined with the appointment of a continuous monitoring glycemia.
PrednisoloneFMR: antagonizm. Weakens effect; with a joint appointment requires constant monitoring of blood glucose concentrations.
ProkaynamydFKV. Slows excretion (secretiruetsa kanalzami and competes for tubular transport systems), can increase Cmax more than half, enhances the effect of.
PromethazineFMR: antagonizm. Weakens effect; with a joint appointment requires constant monitoring of blood glucose concentrations.
RanitidineFKV. FMR. Slows excretion, increases (more than half) Cmax (secretiruetsa kanalzami and competes for tubular transport systems), enhances the effect of.
SalmeterolFMR: antagonizm. Weakens effect; the combined appointment requires constant monitoring of blood glucose concentrations.
SpironolactoneFMR: antagonizm. Weakens effect.
TioridazinFMR: antagonizm. Weakens effect (can provoke hyperglycemia); When combined with the appointment of a continuous monitoring glycemia.
TriamcinoloneFMR: antagonizm. Reduces effect; with a joint appointment requires constant monitoring of blood glucose concentrations.
TrimethoprimFKV. Slows (mutually) deduction: competing for the overall transport system in renal bone.
TrifluoperazineFMR: antagonizm. Weakens effect (can provoke hyperglycemia); socetannoe application requires continuous monitoring of the level of glycemia.
FelodipineFMR: antagonizm. Provokes giperglikemia, weakens the effect; When combined with the appointment of a continuous monitoring glycemia.
PhenylephrineFMR: antagonizm. Weakens effect; combined or consistent application requires greater control over the level of glycemia.
PhenytoinFMR: antagonizm. Weakens effect.
FludrokortizonFMR: antagonizm. Weakens effect; joint application requires constant monitoring concentrations of glucose in the blood.
FluoxetineFMR: synergism. Do effect; the combined appointment of caution (After the abolition fluoksetina possible hyperglycemia, requiring increasing doses).
FlufenazinFMR: antagonizm. Weakens effect (can provoke hyperglycemia); socetannoe application requires continuous monitoring of the level of glycemia.
FurosemidFKV. Although slows excretion and increases withmax и AUC, the effect weakens. Against the backdrop of metformin reduced the 1.3-1.4 times Cmax and T1/2.
QuinidineFKV. Slows excretion (secretiruetsa kanalzami and competes for tubular transport systems), can increase Cmax more than half, enhances the effect of.
ChlorpromazineFMR: antagonizm. Weakens effect (can provoke hyperglycemia); socetannoe application requires continuous monitoring of the level of glycemia.
XlortalidonFMR: antagonizm. Weakens effect (can provoke hyperglycemia); When combined with the appointment of a continuous monitoring glycemia.
CyclophosphamideFMR: synergism. Do effect.
EpinephrineFMR: antagonizm. Weakens effect; combined or consistent application requires greater control over the level of glycemia.
EstradiolFMR: antagonizm. Weakens effect; joint application requires constant monitoring concentrations of glucose in the blood.
Ethacrynic acidFMR: antagonizm. Weakens effect.
EthanolAgainst the backdrop of metformin increases the risk of molernkislogo azidoza; during treatment, the admission of alcohol-containing drinks should be deleted.
EthinylestradiolFMR: antagonizm. Weakens effect (can provoke hyperglycemia); When combined with the appointment of a permanent monitoring of the level of glycemia.
EphedrineFMR: antagonizm. Weakens effect; combined or consistent application requires greater control over the level of glycemia.

 

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