Buy Zavedos® lyophilisate 5 mg vial 1 pc.
  • Buy Zavedos® lyophilisate 5 mg vial 1 pc.

Zavedos® [Idarubicin]

Pfizer
539 Items
2019-09-19
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$162.94
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Clinical Pharmacology

Antineoplastic drug from the group of anthracycline antibiotics. Idarubicin, integrating into the DNA molecule, interacts with topoisomerase II and inhibits the synthesis of nucleic acids. Idarubicin has a high lipophilicity and is characterized by a higher rate of penetration into cells than doxorubicin and daunorubicin.

The main metabolite of idarubicin - idarubitsinol has antitumor activity and has less pronounced cardiotoxicity than idarubitsin.

Pharmacokinetics

Suction

When ingestion absorption is high. Time to reach Cmax - 2-4 h. Bioavailability - 18-39%. With a / in the introduction of Cmax achieved within a few minutes.

Distribution

The capture of idarubicin by the nucleated cells of the blood and bone marrow in patients with leukemia goes very quickly and almost coincides with its appearance in the blood plasma. The concentrations of idarubicin and idarubitsinol in the nucleated cells of the blood and bone marrow are more than 100–200 times higher than the corresponding concentrations in the blood plasma.

Metabolism and excretion

Idarubicin is rapidly metabolized to the active metabolite of idarubicinol.

Excreted mainly in the form of idarubicinol with bile, as well as with urine in unchanged form (1-2%) and in the form of idarubicinol (4.6%).

T1/2 idarubitsina after ingestion is 10-35 hours, after the on / in the introduction - 11-25 hours. Idarubitsinol is characterized by a longer T1/2 - 33-60 h when administered orally and 41-69 h - with a / in the introduction. The rate of elimination of idarubicin and idarubicinol from plasma and cells almost coincides (terminal T1/2 idarubitsina of cells is about 15 hours, and idarubitsinola - about 72 hours).

Indications

  • Acute non-lymphoblastic or myeloblastic leukemia in adults (first-line therapy for the induction of remission, as well as for relapses or resistant cases);
  • acute lymphoblastic leukemia in adults and children (second-line therapy);
  • common breast cancer (with the ineffectiveness of first-line chemotherapy, which does not include anthracyclines).

Composition

1 bottle contains:

Active substances: idarubicin hydrochloride 5 mg.

Excipients: lactose.

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Zavedos® [Idarubicin]

Dosage and Administration

The drug is administered IV (very slowly) within 5-10 minutes. To reduce the risk of extravasation, it is recommended to administer Zavodos through the system tube for IV injection (during the infusion of 0.9% sodium chloride solution).

Capsules are ingested, squeezed with a small amount of water. Can be taken with food. The capsule should be swallowed whole (do not get through, do not dissolve, do not chew).

In acute non-lymphoblastic leukemia (ONLL) adults receive the drug IV a dose of 12 mg / m2 body surface area daily for 3 days (in combination with cytarabine) or 8 mg / m2 daily for 5 days as monotherapy or in combination with other anticancer drugs. If it is impossible IV the introduction of idarubitsin for oral use of 30 mg / m2/ day for 3 days as monotherapy or 15-30 mg / m2 daily for 3 days in combination with other anti-leukemia drugs.

In acute lymphoblastic leukemia adults are prescribed 12 mg / m2, children - 10 mg / m2; the drug is administered intravenously daily for 3 days as monotherapy.

For advanced breast cancer the drug is administered orally as a monotherapy at the rate of 45 mg / m2 in one day or 15 mg / m2/ day for 3 days every 3-4 weeks depending on the hematological status of the patient. In combination chemotherapy, the drug is used at a dose of 35 mg / m.2 in one day.

All the above schemes should be used taking into account the hematological status of the patient, as well as the doses of other cytotoxic drugs used in combination therapy.

When violations of the liver and kidneys data on the use of the drug Zavedos limited. At elevated levels of bilirubin and / or creatinine in serum, it is recommended to use the drug in reduced doses.

When the content of bilirubin in the serum in the range of 1.2-2 mg%, the dose of anthracyclines is usually reduced by 50%, above 2 mg% - the drug is canceled.

Rules for the preparation and administration of the solution

Only water for injection is used as a solvent for Zavedos®. To prepare a solution of 5 mg of the drug is dissolved in 5 ml of water for injection.

Adverse reactions

Since the cardiovascular system: phlebitis, thrombophlebitis and thromboembolism, incl. pulmonary embolism. A manifestation of early (acute) cardiotoxicity is sinus tachycardia and / or ECG changes (nonspecific changes in the ST segment or T wave). Tachyarrhythmias can also occur, including ventricular premature beats and ventricular tachycardia, bradycardia, AV blockade, and blockade of the bundle of His. The occurrence of these phenomena is not always a prognostic factor for the development of subsequently delayed cardiotoxicity, they are rarely clinically significant and do not require the abolition of Zavidos therapy. Late (delayed) cardiotoxicity is usually noted during the last courses of therapy or several months or years after completion of therapy. Late cardiomyopathy is manifested by a decrease in the left ventricular ejection fraction and / or symptoms of congestive heart failure (shortness of breath, pulmonary edema, hypostatic edema, cardiomegaly and hepatomegaly, oliguria, ascites, exudative pleurisy, canter rhythm). Subacute events (pericarditis / myocarditis) may also occur. The most severe form of cardiomyopathy caused by anthracyclines is life-threatening, congestive heart failure, which limits the total dose of the drug.

From the hemopoietic system: leukopenia, neutropenia, thrombocytopenia, anemia. The number of neutrophils and platelets usually reaches the lowest values ​​by 10-14 days after the administration of the drug, the restoration of the blood picture is observed during the third week. Dose-dependent reversible leukopenia and neutropenia are manifestations of toxicity, which limits the dose of the drug.The clinical manifestation of severe myelosuppression can be chills, infections, sepsis / septicemia, septic shock, hemorrhage, and tissue hypoxia.

From the digestive system: nausea, vomiting, anorexia, dehydration, mucositis, stomatitis, esophagitis, abdominal pain, heartburn, erosion / ulcers of the gastrointestinal mucosa, diarrhea, colitis (including neutropenic enterocolitis with perforation), increased activity of liver enzymes and increased bilirubin level . Rarely on the background of the drug intake was observed the development of severe complications of the gastrointestinal tract (perforation, bleeding).

From the urinary system: red urine staining within 1-2 days after taking the drug.

Dermatological reactions: alopecia, rash, pruritus, hyperpigmentation of the skin and nails, hypersensitivity of irradiated skin ("radiation response"), urticaria and peripheral erythema.

Allergic reactions: hot flashes to the face, anaphylaxis.

Local reactions: when the drug gets under the skin - blistering, severe cellulite, necrosis of the surrounding soft tissues.

Other: hyperuricemia due to rapid lysis of tumor cells ("tumor lysis syndrome"), secondary leukemia with or without a preleukemic phase (most often observed when using anthracyclines in combination with antitumor agents that violate the structure of DNA) with a latent period of 1 to 3 years.

Carefully: the drug should be prescribed for myocarditis, chickenpox, shingles, gout or urate nephrolithiasis (in history), infections, leukopenia, thrombocytopenia, elderly patients (over 60 years).

Drug interactions

Combined chemotherapy using Zavos and other drugs of similar effect can lead to an additive toxic effect, especially in relation to the hematopoietic system / bone marrow and gastrointestinal tract.

An additive myelosuppressive effect can also be observed if radiation therapy was performed on the background or 2-3 weeks prior to Zavedos® therapy.

Combined use with other cardiotoxic or cardiovascular medicines (for example, calcium channel blockers) requires careful monitoring of heart function throughout the entire treatment period.

Changes in liver function as a result of concomitant therapy can disrupt idarubicin metabolism, as well as its pharmacokinetics, therapeutic efficacy and / or increase its toxicity.

When combined with uricosuric drugs increases the risk of nephropathy.

Pharmaceutical interaction.

Zavedos® can not be mixed with other drugs. Pharmaceutically incompatible with any solutions with alkaline pH - idarubicin is destroyed.

The drug should not be mixed with heparin due to the possible formation of a precipitate.

Pregnancy and Lactation

Zavedos® is contraindicated during pregnancy and lactation (breastfeeding).

Patients of childbearing age who receive therapy with Zaredos should use reliable contraceptive methods.

Special instructions

Zavedos® should only be used under the supervision of a physician experienced in cytotoxic chemotherapy.

Before starting to use the drug, Zavedos should be convinced that the patient has no signs of acute toxicity (stomatitis, neutropenia, thrombocytopenia, generalized infections) resulting from previous therapy with cytotoxic drugs.

Before and during each cycle of therapy, it is necessary to carefully monitor the peripheral blood pattern with leukocyte count.

To reduce the risk of severe toxic heart damage, it is recommended that Zavodos regularly monitor its function prior to and during therapy (using the same evaluation method throughout the observation period), including evaluation of the left ventricular ejection fraction using echocardiography or multichannel radioisotope angiography , as well as ECG monitoring. Heart function monitoring should be especially careful in patients with risk factors, as well as in patients receiving high cumulative doses of anthracyclines. If there are signs of cardiotoxicity, Zavodos treatment should be stopped immediately.Risk factors for cardiotoxicity include cardiovascular diseases in the active or latent phase, previous or concomitant radiation therapy of the mediastinum or pericardial area, prior therapy with other anthracyclines or anthracenedions, simultaneous use of other drugs that suppress the contractile ability of the heart. However, cardiotoxicity due to the use of the drug may develop at lower cumulative doses and regardless of the presence or absence of risk factors for the development of cardiotoxicity. It is assumed that the toxicity of idarubicin and other anthracyclines and anthracenediones is additive.

Limit cumulative doses of Zavodos with a / in the introduction and ingestion has not yet been established. Cases of the development of cardiomyopathy were reported in approximately 5% of patients with intravenous injection of a cumulative dose of 150-290 mg / m2. Available data on patients who took Zavodos orally in a total cumulative dose of up to 400 mg / m2 suggest a low probability of developing cardiotoxicity.

Since impaired liver and / or kidney function may affect the distribution of idarubicin, it is necessary to monitor liver and kidney function (with determination of the level of bilirubin and creatinine in blood serum) before and during treatment.

Before prescribing Zavidos capsules to patients with an increased risk of bleeding and / or gastrointestinal perforation, the ratio of the perceived benefits of using the drug and the risk of complications should be assessed.

Patients taking Zavedos inside should be carefully monitored, as gastrointestinal bleeding and severe damage to the gastrointestinal tract mucosa may develop.

In connection with the possible development of hyperuricemia during therapy, it is recommended to determine the level of uric acid, potassium, calcium, phosphate and creatinine in the blood serum. Conducting preventive measures (hydration, alkalization of urine, taking allopurinol) allows you to minimize the risk of complications associated with tumor lysis syndrome.

After injection into the veins of small diameter or after repeated injections into the same vein, phlebosclerosis can develop. The risk of phlebitis / thrombophlebitis at the injection site can be reduced by strictly following the recommendations for the introduction of the drug.

At the first signs of extravasation (burning or soreness at the injection site), the infusion should be stopped immediately and then resumed into another vein before the full dose is administered.

When working with Zavedos, it is necessary to follow the rules for handling cytotoxic substances.

In case of accidental contact with the skin, immediately wash it off with plenty of water and soap or sodium bicarbonate solution; in case of accidental ingestion of the drug in the eyes - flush the eyes with plenty of water for at least 15 minutes.

The surface contaminated with the preparation is recommended to be treated with a dilute solution of sodium hypochlorite (containing 1% chlorine).

Overdosage

Symptoms: manifestations of acute cardiotoxicity in the first 24 hours (late cardiotoxicity can be observed several months after anthracycline overdose) and severe myelosuppression (within 1-2 weeks).

Treatment: conduct symptomatic therapy.

  • Brand name: Zavedos®
  • Active ingredient: Idarubicin
  • Dosage form: Lyophilisate for preparation of solution for IV introductions.
  • Manufacturer: Pfizer
  • Country of Origin: USA

Studies and clinical trials of Idarubicin (Click to expand)

  1. An “all-oral” combination therapy in chronic lymphocytic leukemia including the oral idarubicin
  2. A Phase II study of oral idarubicin as a treatment for metastatic hormone-refractory prostate carcinoma with special focus on prostate specific antigen doubling time
  3. Long-term follow-up of three randomized trials comparing idarubicin and daunorubicin as induction therapies for patients with untreated acute myeloid leukemia
  4. Remission induction therapy of untreated acute myeloid leukemia using a non-cytarabine-containing regimen of idarubicin, etoposide, and carboplatin
  5. A new effective treatment for indolent lymphoma: a pilot study with fludarabine, idarubicin and prednisone combination (FLIDA)
  6. A prospective randomized trial of doxorubicin versus idarubicin in the treatment of advanced breast cancer
  7. A phase II study of idarubicin in the treatment of measurable gastric cancer
  8. Treatment of myelodysplastic syndromes with daily oral idarubicin. A phase I–II study
  9. Simultaneous determination of doxorubicin, daunorubicin, and idarubicin by capillary electrophoresis with laser-induced fluorescence detection
  10. Arsenic trioxide- and idarubicin-induced remissions in relapsed acute promyelocytic leukaemia: Clinicopathological and molecular features of a pilot study
  11. High-dose cytosine arabinoside and idarubicin treatment of chronic myeloid leukemia in myeloid blast crisis
  12. Idarubicin, cytarabine, and topotecan in patients with refractory or relapsed acute myelogenous leukemia and high-risk myelodysplastic syndrome
  13. Continuous infusion of intermediate-dose cytarabine and fludarabine with idarubicin for patients younger than 60 years with resistant acute myeloid leukemia: A prospective, multicenter phase II study
  14. FLAIE (fludarabine, cytarabine, idarubicin, and etoposide), a four drug induction chemotherapy for adult acute myeloid leukemia: A single center experience
  15. Salvage therapy for acute myeloid leukemia with fludarabine, cytarabine, and idarubicin with or without gemtuzumab ozogamicin and with concurrent or sequential G-CSF
  16. A single, high dose of idarubicin combined with cytarabine as induction therapy for adult patients with recurrent or refractory acute lymphoblastic leukemia
  17. Idarubicin and standard-dose cytosine arabinoside in adults with recurrent and refractory acute lymphocytic leukemia
  18. A phase 1-2 study of a farnesyltransferase inhibitor, tipifarnib, combined with idarubicin and cytarabine for patients with newly diagnosed acute myeloid leukemia and high-risk myelodysplastic syndrome
  19. Phase 1 study of arsenic trioxide, high-dose cytarabine, and idarubicin to down-regulate constitutive signal transducer and activator of transcription 3 activity in patients aged <60 years with acute myeloid leukemia
  20. Phase 2 randomized study of p53 antisense oligonucleotide (cenersen) plus idarubicin with or without cytarabine in refractory and relapsed acute myeloid leukemia
  21. Differential antigenotoxic and cytoprotective effect of amifostine in idarubicin-treated mice
  22. Activity of topoisomerase inhibitors daunorubicin, idarubicin, and aclarubicin in the Drosophila Somatic Mutation and Recombination Test
  23. Oral idarubicin in the treatment of acute myelogenous leukaemia and the blast phase of chronic myeloid leukaemia

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