Tolbutamide

Chemical name

N-[(Бутиламино)карбони��]-4-метилбензолсульфо��амид (in the form of sodium salt)

Gross

C12-H18-N2-O3-S

Characteristics

The white crystalline powder, slightly bitter taste. Nerastvorim water, but is vodo-rastvorimae salts with alkalis, soluble in alcohol.

Of drugs

The drugs-gipoglikemicescoe. It stimulates the release of insulin from beta-kletok pancreas. Decreases glikozilirovannogo level of hemoglobin, reduced concentration of glucose (prandial) in the serum of patients with moderate and severe forms of инсуинсулиннезависим ого Diabetes. Postpishchevu stops giperglikemia increases tolerance to glukoze and Cl free liquid (to a lesser extent). Provides antidiureticescoe little effect. No impact on lipid profile blood plasma. In appointing the dose of 3 g healthy or sick with insulinnezawisimam diabetes gradually reduces the level of glucose in the blood (30% or more during a period of one hour). Restoring baseline fast through a 6-12 hrs (the dose to 6 grams per day is not accompanied by an increase in effect). In experiments on rats and mice have been detected and kartsinoguennogo mutagennogo action. In rats at doses exceeding recommended for the men in 100 times doses found a tertogennogo effect. To examine the effects on fertility are not Provodilosl.bystro drawn from the blood. Away does not affect the removals and the speed of impact. There are in the blood at 20 min. C_max achieved in 3-4 h after 24 h plasma identified only sledove number, the duration of the 12-hour Linking plasma protein-96% - T_1/2 4.5-6.5 h Oxidized to metilnomu radikalu in carboksilnoe inactive derivative (1-butil-3-p-carboksifenilsulfonilmocevina), 75% of which 24 hours to return with urine.

Indications

Diabetes mellitus type 1 (with inefficiency nizkokalorina diet, adequate physical exercise, etc.).

Restrictions on the use of

Diseases of the digestive tract, liver and kidney (continuous monitoring blood glucose), a children's age (safety and efficacy of the children are not identified).

Pregnancy and lactation

Contraindicated. If the pregnancy is important for the removal of one month prior to delivery and the transition to insulinoterapiu. At the time of treatment should stop breastfeeding.

Contraindications

Hypersensitivity, diabetic ketoacidosis, diabetic coma, diabetes mellitus type 2, fever, trauma, operative intervention, pregnancy, breast-feeding.

Side-Effects

From the metabolic : hypoglycaemia, Giponatriemia.so part of the intestine : pain in epigastralna area, anorexia, nausea, vomiting, neuralgia, constipation (to 1.4% of cases). Seldom-holetsaticeski hepatitis (yellow staining skin and skler, discoloration chairs, dark urine, pain in the right подреберье).Аллергиче ские reactions : no more than 1.1% of cases, erythema, skin makulopapulezne, urticaria, Zud.so the Skin : photosensitization (up to 1.1%). From the circulatory system and blood (blood, gemostaz) : 1% of cases and less-lakopenia, agranulozitos, thrombocytopenia, pancitopenia, haemolytic or aplastic Anemia.prochie : headache, changes in taste sensations.

Patient interaction

The weakened mineralo- and glukokortikoida, amphetamines, anti-convulsants (gidantoina derivative), asparaginase, baclofen, calcium antagonists, carboangidraza inhibitors (acetazolamide), hlortalidon, oral contraceptives, epinephrine, etakrinova acid, furosemide, glukagon, salicilata, tiazidnye dioretiki, hormones thyroid, triamteren and other preparations of giperglikemia. Anabolic steroids and androgena increase gipoglikemicescuu activity. Ketonzol, miconazole, sulfinpirazon blocking inachtiwatia and reinforce gipoglikemia. Indirect combined, NPVS, chloramphenicol, klofibrat, guanetidin, MAO inhibitors, probenecid, sulfanilamida, rifampicin increase the concentration of free fraction in the blood (through vzaimovtesnenia of the plasma protein), and up biotransformatia. While alcohol may Development дисульфирамоподобног о syndrome (abdominalnaya pain, nausea, vomiting, headache). Antitireoidnye and mielotoksicskie drugs increases the likelihood of development agranulozitoza; Were, moreover, provoke trombozitopeniu.

Overdosing

Symptoms : Gipoglikemia.lechenie : lifting drug glucose ingestion and / or modification of diet to mandatory monitoring blood glucose; With heavy gipoglikemii (coma, seizures epileptiformnye) immediate hospitalization; A 50% solution of glucose in / in struino while infuziei (in / with drip) 10% glucose solution that ensures the fast above 100 mg / dle. Monitoring blood glucose is a 1-2 day after the release of the patient from a coma. Dialysis ineffective.

Precautions

Translated patient with therapy gipoglikemicakimi means is not required break in treatment. An exception is hlorpropamid with long T_1/2 necessitated suspension of the therapy or the careful monitoring patients within 1-2 weeks because of the increased risk of gipoglikemii. Mode switching from insulinoterapii depends on the dose of hormone : the dose to 20 U of insulin per day it instantly overturned and immediately appoint tolbutamid; Dose of 40 U per day reduces its 30-50% and above 40 U per day-20% (in hospital), and at the same time appoint tolbutamid (with the hypoglycemic effect tolbutamida dose of insulin to lower). Throughout the insulin needed a threefold glucose and acetone in the urine. The glukozurii and / or azetonurii shows insulinzawisimom diabetes and requires translation into insulinoterapiu.

Dosing and Administration

Inside. Initial dose of 1-2 g / day one (morning), or a few tricks. Probably later, a decrease or an increase in dose, depending on the patient. Maximum daily intake - 3 and

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