Pamidronic acid

Chemical name

3-Амино-1-гидроксипроп��лидендифосфоновая acid (and in the form of dinatria pentahydrate)

Gross

C3-H11-N-O7-P2

Characteristics

White or almost white powder. Rat in the water and n 2. solution of sodium hydroxide, moderately soluble in divorced (0.1 g). hydrochloric and acetic acids, virtually nerastvorim in the organic solvent. pH 1% aqueous 8.3.

Of drugs

The drugs-ingibirutee bone resorption. The bone is associated with crystal gidroxiapatita (calcium phosphate) bone and prevent their animals. Stops penetration in the bone tissue osteoclastov predecessors and their transformation into a mature form. Ingibiruet inducyruemuu malignant tumors span osteoclastov and prevents osteoliticescuu bone mass resulting from the tumor process. In gipercalziemii caused by malignant tumors during 7-10 days regulate biochemical parameters : reduces phosphate release from bones, calcium levels in the serum, the calcium / creatinine and гидроксипролин/креат��нин in the urine, etc. When a Pejeta reducyruet (up to 50%) of savorotocna alkaline phosphatase, hydroxyproline in the urine and other biochemical markers process, in the case of mielomna disease and in cancer patients with metastases garments osteoliticski type slows development skeletal changes and reduces the recurrence of the bone violations including pathological fractures and compression of the spinal cord, reduces their accompanying pain syndrome. Is a sign of reparation osteoliticakih pockets by reducing the need for radiation therapy or operational intervention. Against the backdrop of the usual anticancer therapy slows the bone vestiges contributes to the development of osteosclerosa in the affected Ucastkah.posle in / in the hour infusions treat patients 30, 60 and 90 mg C_max reached 0.73, 1.44, 2.61 µ g / ml respectively, the average total Cl - 52-110 ml / min, kidney Cl 27-50 ml / min, T_1/2 - 27-28 hours Associated with the plasma protein by 54%, increasing the concentration of calcium to albuminopexii. There is metabolized. Slowly (indefinitely) netted only by renal excretion. Eliminations in most soft tissue occurs for 1-4 days, the liver and spleen, in the first six months, in the bones, about 300 days. Violation of kidney function reduces the excretion of urine.

Indications

Gipercalziemia caused malignant tumors (epidermoidnyi and neepidermoidnyi origin, and without the garments metastasis, immobilization, primary giperparatireozom) osteit distortive (Pejeta disease), malignant cancerous tumors in the bone and mielomnaya disease that osteoliticakimi defeats bones, osteoporosis, including in the therapy glukokortikoidami, fibrosnaya osteodisplazia (symptomatic therapy).

Contraindications

Hypersensitivity expressed by the human kidney, pregnancy, breast-feeding (at the end of treatment), children's age.

Side-Effects

Increased body temperature (1-2 ^ C within 24 to 48 hours after the infusions), nausea, vomiting, loss of appetite, pain in the abdomen, constipation / diarrhea, neuralgia, the symptoms of gastritis, Generalized pain, pain in the bones, back, and arthralgia mialgii (often with the toxin, mielomna disease), sudorozhny status, dizziness, headache, parestesia, arousal, the orientation, insomnia or drowsiness, lethargy, visual hallucinations, conjunctivitis, увеит (ирит, иридоциклит) склерит, эписклерит, ксантопсия, hypertension / гипотензия, signs левожелудочковой or congestive heart failure and anaemia, лимфоцитопения, thrombocytopenia and лейкопения (mainly with chemotherapy Metastases), гематурия, acute renal failure, the current deterioration of kidney disease, гипокальциемия, гипофосфатемия, гипомагниемия, гипокалиемия / гиперкалиемия, гипернатриемия, change in the functional liver samples increasing the concentration of creatinine and urea in the serum, allergic (rashes, itching) and anaphylactoidnye (bronhospazm, dizziness, swelling Kwinke, anaphylactic shock) reaction flu symptoms (malaise, fever, a feeling of fatigue, tides, sweating), herpes, infection urinary tract and respiratory, local reactions : pain, redness, swelling, seal flebit, throm at introduction.

Patient interaction

Compatible with protivoopujolevami drugs. Calzitonin accelerates the reduction of calcium in крови.Фармацевтическ�� incompatible with the infusion solutions containing calcium (incl. solution periods).

Overdosing

Symptoms : gipocalziemia (paresthesia, tetania Arterial gipotenzia). Treatment : in / with the introduction of calcium glukonata.

Precautions

During the treatment, especially in the frequent infuziah for a long time, a periodic review (standard laboratory and clinical parameters) of the kidneys. In gipercalziemii, mostly at the beginning of the course, it is recommended that monitoring of whey in calcium, phosphate, magnesium, sodium, creatinine; When the signs gipocalziemii, including tetaniu, no therapy. Before or during treatment necessarily adequate rehydration saline solution (including slabovrajenna asimptomaticescoy gipercalziemii); In gipercalziemii induced blood malignizaciei further glukokortikoida apply. When expressed as human kidney solution infuziruut rate not to exceed 20 mg / h. In patients with possible heart failure, it is necessary to avoid excessive salts. During therapy advised to refrain from activities potentially hazardous activities that require greater attention and speed of mental reactions. There should be combined pamidronovu acid with other bifosfonatami; Introduce / in struino.

Dosing and Administration

In / in drip slowly (at the speed of not more than 60 mg / h) in the form of infusions. The homemade solution инфузионного dry matter for the infusions previously dissolved in water for injection (15 mg, 5 ml, 30 mg in 10 ml) and concentrate for the infusions add 10 ml of water and then diluted with 0.45% or 0.9% solution of sodium chloride or 5% glucose solution, in 1000 ml for therapy gipercalziemii, 500 ml, in the other cases; concentration in the solution infuzionnom shall not exceed 90 mgu/250 Ml.pri gipercalziemii, inductively malignizaciei, - dose set individually on the basis of a reference concentration of calcium in the blood. For adults and the elderly, with the concentration of calcium in the blood of less than 3 mmol / l total dose rate is 15-30 mg, in the 3-3.5 mmol / l, 60 mg, in the 3.5-4 mmol / l to 90 mg; Dose introducing / in infuzionno within 2 hours one or more receptions in the next two to four consecutive days; with the admission level of calcium in the blood is reduced by 24 to 48 hours, returning to normal within 3-7 days; in the absence of effects this time, the course repeat. Possible alternative : at a moderate gipercalziemii (the level of calcium in the cell 12-13,5 mg / ml), the original single dose of / in infuzionno-60 mg for 4 h or 90 mg over 24 hours; With a development gipercalziemii (level more calcium 13.5 mg / ml) - 90 mg, a single on / in the center cefuroxim; if necessary (if the calcium is not returned to normal) repeat rate, but not less than 7 days. The maximum dose rate (initial, refresher courses), 90 Mg.pri disease Pejeta-30 mg per day for a hour infusions for 3 consecutive days (total dose of 90 mg); May repeat Kursa.v the vestiges of malignant tumors in the bones, multiple mieloma-90 mg, Once in the form of 2-4-casova in / with infusions every 4 weeks; subject to the use of anticancer therapy in three weeks can be used every three weeks.

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