Zometa

Zometa – inhibitor of a resorption of a bone tissue at metastasises in a bone.

Form of release and structure

Dosage forms:

• Concentrate for preparation of solution for infusions: transparent colourless liquid (on 5 ml in plastic colourless bottles, in a cardboard pack 1 bottle);
• Solution for infusions: colourless transparent liquid (on 100 ml in plastic bottles, in a cardboard pack 1 bottle).

Active ingredient of Zometa – zoledronovy acid:

• 1 bottle of a concentrate – 4,264 mg of monohydrate of zoledronovy acid that is equivalent to the content of 4 mg of zoledronovy acid anhydrous;
• 1 bottle of solution – 4 mg.

Auxiliary components:

• Concentrate: sodium citrate, Mannitolum, nitrogen, water for injections;
• Solution: Mannitolum, sodium citrate a dihydrate, water for injections.

Indications to use

• Metastasises in a bone of malignant widespread tumors (a breast cancer, a prostate cancer), a multiple myeloma, including prevention of decrease in risk of a compression of a spinal cord, pathological changes, hypercalcemias against the background of a tumor, and the needs for carrying out surgeries on a bone or radiation therapy;
• The hypercalcemia caused by a malignant new growth.

Contraindications

• Period of pregnancy and breastfeeding;
• Children's age;
• Hypersensitivity to bisfosfonata and components of drug.

With care Zomet should appoint at the expressed abnormal liver functions.

Use of drug at a renal failure at patients with the hypercalcemia caused by a malignant tumor is possible if the potential advantage of therapy prevails over the existing risk. Administration of drug by the patient with heavy renal failures is not recommended: at creatinine level in blood serum more than 265 µmol/l at patients with metastasises in a bone, and more than 400 µmol/l at the hypercalcemia caused by a malignant tumor.

Route of administration and dosage

The concentrate to preparation of solution for infusions and solution for infusions is applied by intravenous (in/in) drop by introductions.

Solution for cultivation of a concentrate should not contain calcium! Solution for infusion is prepared with observance of rules of an asepsis. Just before introduction contents of 1 bottle of a concentrate should be parted in 100 ml 0,9% of solution of sodium of chloride or 5% of solution of a dextrose. It is possible to store unused solution no more than 24 hours from the moment of preparation at a temperature of 2-8 °C, and before introduction it should be brought to room temperature, previously having got from the refrigerator.

I will sweep up it is impossible to mix with calciferous or any bivalent cations solutions (Ringer's solution a lactate) and with other medicines therefore for administration of solution of zoledronovy acid it is necessary to use separate system for infusions.

Drop in/in introduction not less than 15 minutes have to last.

The recommended dosing:

• Metastasises in a bone of widespread malignant tumors and a multiple myeloma: on 4 mg of 1 times in 3-4 weeks. It is necessary to appoint drug with a concomitant use in 500 mg of calcium and 400 international units (IU) of vitamin D a day;
• The hypercalcemia caused by a malignant tumor (level of content of calcium with correction on concentration of albumine more than 12 mg/dl or 3 mmol/l): 4 mg;
• Treatment a metastasis in a bone at patients with easy or moderate renal failures (the clearance of creatinine (CC) of 30-60 ml/min.): at KK: 30-39 ml/min. – 3 mg, 40-49 ml/min. – 3,3 mg, 50-60 ml/min. – 3,5 mg of zoledronovy acid.

Before Zometa's introduction, in parallel or after it the patient should appoint introduction of normal saline solution to provide adequate hydration.

Before each administration of drug it is necessary to define concentration of serumal creatinine, at a renal failure introduction of the next dose should be postponed. Parameters of a renal failure:

• Patients with normal (less than 1,4 mg/dl) reference values of creatinine – at increase in level of concentration of serumal creatinine on 0,5 mg/dl;
• Patients with the initial level of creatinine more than 1,4 mg/dl – at increase in content of serumal creatinine on 1 mg/dl.

It is possible to resume treatment in a former dose only after recovery of concentration of creatinine to initial (plus or minus of 10%) level.

Side effects

• Bodies of a hemopoiesis: often – anemia; sometimes – a leukopenia, thrombocytopenia; seldom – a pancytopenia;
• Urinary system: often – renal failures; sometimes – a hamaturia, an acute renal failure, a proteinuria;
• Nervous system: often – a headache; sometimes – disturbances of flavoring feelings, dizziness, a giposteziya, paresthesias, a hyperesthesia, frustration of a dream, feeling of alarm, a tremor; seldom – confusion of consciousness;
• Alimentary system: often – anorexia, nausea, vomiting; sometimes – dryness in a mouth, abdominal pains, diarrhea, a lock, stomatitis, dyspepsia;
• Organ of sight: often – conjunctivitis; sometimes – "blurring" of sight; very seldom – an episcleritis, a uveitis;
• Musculoskeletal system: often – a mialgiya, ostealgias, generalized pains, an arthralgia; sometimes – muscular spasms;
• Respiratory system: sometimes – cough, short wind;
• Cardiovascular system: sometimes – the expressed decrease or increase in the arterial pressure (AP); seldom – bradycardia;
• Immune system: sometimes – hypersensitivity reactions; seldom – a Quincke's disease;
• Dermatological reactions: sometimes – a skin itch, the increased perspiration, rash (including erythematic and macular);
• Laboratory indicators: very often – a hypophosphatemia; often – a hypocalcemia, increase in concentration of creatinine and urea in blood serum; sometimes – a hypopotassemia, a hypomagnesiemia; seldom – a hypernatremia, a hyperpotassemia;
• Others: often – a grippopodobny syndrome (a fever, a febricula, heat, disease state), fever; sometimes – thorax pain, peripheral hypostases, an adynamy, increase in body weight; very seldom – the decrease in the ABP causing a faint or a circulator collapse (generally at patients with risk factors), a bronkhokonstriktion, drowsiness development, fibrillation of auricles, anaphylactic reactions or shock, a small tortoiseshell;
• Local reactions: irritation, pain, hypostasis, in a drug injection site – formation of infiltrate.

Special instructions

At Zometa's appointment at a renal failure at patients with the hypercalcemia caused by a malignant new growth, the main criterion for evaluation of expediency of therapy excess of advantage of use of drug over potential risk is.

Before each administration of solution it is required to determine the level of content of creatinine in blood serum.

At bone metastasises at patients with a renal failure weak and moderate severity treatment should be begun with introduction of the lowered doses. At emergence of functional disorder of kidneys during treatment it is possible to continue therapy only after recovery to initial (a plus-minus of 10%) the level of concentration of creatinine.

Because of risk of development of complications from cardiovascular system against the background of an overhydratation of the patient administration of drug should be begun only after assessment of a condition of hydration of an organism. In case of disturbances the patient should enter normal saline solution to, into time or after drug infusion.

Zometa's use needs to be accompanied with constant control of level of content of creatinine, phosphorus, calcium, magnesium in blood serum. At development of a hypophosphatemia, hypocalcemia or hypomagnesiemia to the patient in addition appoint introduction of appropriate means.

At administration of drug for prevention of decrease in risk of a compression of a spinal cord, pathological changes, the hypercalcemia caused by a tumor, it is necessary to consider decrease in need for carrying out surgical interventions on a bone or radiation therapy that the therapeutic effect occurs in 2-3 months of treatment.

Treat the risk factors influencing development of renal failures: the previous renal failure, dehydration, repeated introduction of bisfosfonat, use of nefrotoksichny means, too bystry administration of solution of Zometa.

During treatment carrying out any dental manipulations therefore before purpose of drug of the patient has to undergo dental inspection is not recommended, cure problem teeth and receive recommendations of need of strict observance of rules of hygiene of a mouth.

Oncological patients have a risk of osteomyelitis, infectious and inflammatory pathologies of an oral cavity, a jaw osteonecrosis against the background of antineoplastic therapy.

Treat risk factors of an osteonecrosis of a jaw: cancer and the treatment accompanying it (use of corticosteroids, chemotherapy, radiation therapy), the accompanying pathologies (including anemia, the previous oral cavity disease, a coagulopathy, infections).

Against the background of use of zoledronovy acid development of a strong passing joint pain, muscles and bones is possible.

Contraindicated simultaneous use of Aklasta whose active ingredient is zoledronovy acid.

Influence of drug on ability of the patient to control of vehicles and mechanisms is not established.

Medicinal interaction

Clinically significant interaction at Zometa's combination to antineoplastic drugs, diuretics, antibiotics, analgetics and other means of antineoplastic therapy is noted.

It is established that zoledronovy acid does not inhibit enzymes of system _{of P450 cytochrome} and has no considerable linkng with proteins of plasma.

It is necessary to be careful at use in a combination with aminoglycosides (as because of simultaneous effect of drugs the risk of increase in level of concentration of calcium increases in a blood plasma) and the medicines having the expressed nephrotoxic effect.

At a multiple myeloma the combination to a thalidomide promotes increase in risk of renal failures.

Drug pharmaceutical is incompatible with infusion kaltsiysoderzhashchy solutions, including Ringer's solution.

For Zometa's introduction it is authorized to use glass bottles, infusional systems, polyvinyl chloride, plastic and polypropylene bags from 0,9% solution of sodium of chloride or 5% dextrose solution.

Terms and storage conditions

To store at a temperature up to 30 °C. To protect from children.

Period of validity – 3 years.