Glipizide

Chemical name

N-[2-[4-[[[(Циклогексилами но)карбонил]амино]сул��фонил]фенил]этил]-5-ме тилпиразинкарбоксами д

Gross

C21-H27-N5-O4-S

Characteristics

White powder odourless. Nerastvorim in water and alcohol, but soluble in NaOH solution with a concentration of 0.1 mol / l and it is readily soluble in dimethylformamide.

Of drugs

The drugs-gipoglikemicescoe. It stimulates the release of insulin функционально-активн��х beta-kletok pancreas. Reduces the glikozilirovannogo hemoglobin concentration and prandial glucose in patients with moderate and severe forms of insulinnezawisimogo diabetes. Decreases postpishchevu giperglikemia increases tolerance to glukoze and Cl free liquid (to a lesser extent). Insulinotropony response develops over 30 min after oral admission, the duration of the one-time admission is 24 hours No impact on lipid profile Krovi.v plasma experiments on rats and mice in doses 75 times higher than MRDC not induces carcinogenesis and has no effect on fertility (rats). Studies performed on bacteria, and in vivo, not identified mutant свойств.Быстродейств��ющая form absorbed quickly and completely. Away does not affect the total removals, but it slows down to 40 minutes. C_max determined after 1-3 h after a single reception. T_1/2 is 2-4 hours After receiving medlennoactutei form appears in the blood after 2-3 hours, C_max achieved after 12 hours Associated with blood plasma proteins at 98-99%. The distribution of the on / in a 11-litre, the average T_1/2 for 2-5 hours The Cl after the single in / with the introduction of 3 l / h. Biotransformiroetsa in the liver (the primary pass-slightly). Less than 10% of output unchanged to the urine and feces, about 90% excreted in the form of metabolites in the urine (80%) and faeces (10%).

Indications

Diabetes mellitus type 2, in the absence of effective nizkokalorina diet, adequate physical exercise, etc.; Mikroangiopatia diabetic.

Restrictions on the use of

Diseases of the digestive tract, liver and kidney (continuous monitoring blood glucose), a children's age (the effectiveness and safety of the children have not been established).

Pregnancy and lactation

Contraindicated. If during 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, uvenilny diabetes mellitus type 1 disease, injuries, operative intervention, pregnancy, breast-feeding.

Side-Effects

For medlennoactutei glipizida forms : on the part of the nervous system and sensory organs : dizziness, headache, insomnia, drowsiness, anxiety, depression, sputannosti consciousness, the gait, paresthesia, giperstesia, lifted the eyes, the pain in the eyes, conjunctivitis, haemorrhaging Setchatku.s the circulatory system and blood (blood, gemostaz) : sinkope, incredible, arterial hypertension, Prilivov.so sense of the metabolic : Gipoglikemia.so part of the intestine : anorexia, nausea, vomiting, a feeling of gravity in epigastralna area, neuralgia, constipation, impurity in the blood Stule.so the skin : skin rashes, urticaria, Zud.so the respiratory system : rhinitis, pharyngitis, Despnoe.so the urogenital system : dizuria, declining Libido.prochie : thirst, chemical and peripheral oedema, nelokalizovannaya pain in the whole body, artralgia, mialgia, convulsions, Potlivosti.dl fast form glipizida : On behalf of the nervous system and sensory organs : headache, dizziness, Sonlivosti.so the circulatory system and blood (blood, gemostaz : lakopenia, agranulozitos, thrombocytopenia, pancitopenia, haemolytic or aplastic Anemia.so the metabolism : nesharnyi diabetes, giponatriemia, porfirinova Bolezn.so part of the intestine : nausea, vomiting, pain in epigastralna area, bar, holetsaticeski hepatitis (yellow staining skin and s 12de9 kler, discoloration chair and dark urine, pain in the right podreberie). From the Skin : erythema, skin makulopapulezne, urticaria, Fotosencibilizace.prochie : increased concentration LDG, alkaline phosphatase, indirect cium.

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 gipoglikemicescuu increased activity. Indirect combined, NPVS, chloramphenicol, klofibrat, guanetidin, MAO inhibitors, probenecid, sulfanilamida, rifampicin increase the concentration of free fraction in the blood (due to the displacement of the blood plasma), and up biotransformatia. Ketonzol, miconazole, sulfinpirazon blocking inachtiwatia and reinforce gipoglikemia. While alcohol may Development дисульфирамоподобног о syndrome (abdominalnaya pain, nausea, vomiting, headache). Antitireoidnye and mielotoksicskie drugs increases the likelihood of development agranulozitoza; Past, and-trombozitopenia.

Overdosing

Symptoms : Gipoglikemia.lechenie : lifting drug glucose ingestion and / or modification of diet to mandatory monitoring fast; With heavy gipoglikemii (coma, seizures epileptiformnye) immediate hospitalization, a 50% solution of glucose in / in struino while infuziei (in / with drip) 10% glucose solution to the concentration of glucose in the blood above 5.5 mmol / l; monitoring fast to a 1-2 day after the release of the patient from a coma. Dialysis ineffective.

Precautions

Be wary appoint elderly, the weak and exhausted and sick patients napochechnikova and hypophyseal insufficiency (to avoid gipoglikemicakih initial reactions and supporting dose should not be high).

Dosing and Administration

Inside before or during delivery. DRAM form, 5 mg before breakfast, in the absence of the effect in a few days dose increase to 2.5-5 mg (requiring constant monitoring concentrations of glucose in the blood); Maximum single dose of 15 mg maximum daily dose of 40 mg. Doses higher than 15 mg appointed several receptions. Against the backdrop of the liver, kidneys and in older patients, 2.5 mg. Medlennoactutaya form, 5 mg at the luncheon. To monitor the effectiveness of medlennoactutei every 3 months, the level of glikozilirovannogo hemoglobin. If after three months the effect of inadequate dose increased to 10 mg or 20 mg (the maximum daily intake).

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