Buy Aranesp solution 20 mcg 0.5 ml syringe, 1 pc.
  • Buy Aranesp solution 20 mcg 0.5 ml syringe, 1 pc.

Aranesp® [Darbepoetin Alfa]

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Clinical Pharmacology

Pharmacodynamics
Darbepoetin alfa stimulates erythropoiesis by the same mechanism as endogenous erythropoietin. Darbepoetin alfa contains five N-linked carbohydrate chains, while the endogenous hormone i recombinant human erythropoietins (rhEpo) have only three chains. Additional sugar residues, from a molecular point of view, do not differ from those presented in the endogenous hormone. Due to the increased carbohydrate content, darbepoetin alfa has a longer half-life in comparison with rhEpo and, consequently, greater in vivo activity.
Despite these changes in the molecular structure, darbepoetin alfa retains a very narrow specificity for the erythropoietin receptor.

Preclinical safety data.
In all studies in rats and dogs, the use of Aranesp significantly increased the concentration of hemoglobin, hematocrit, erythrocytes and reticulocytes, which corresponds to the expected pharmacological effect. Adverse events with the introduction of very high doses of the drug were considered as a result of enhanced pharmacological action (decrease in tissue blood flow due to an increase in blood viscosity). This included myelofibrosis and spleen hypertrophy, as well as expansion of the QRS complex on the ECG in dogs, without disturbing the cardiac rhythm and affecting the QT interval. Aranesp did not possess any genotoxic potential and did not affect the proliferation of non-hematological cells either in vitro or in vivo. In chronic toxicity studies, there was no tumorogenic or unexpected mitogenic response in any of the studied tissue types. In long-term animal studies, the carcinogenic potential of darbepoetin alfa was not evaluated.
In tests conducted on rats and rabbits, there was no clinically significant effect on pregnancy, fetal / fetal development, childbirth, or postnatal development. The level of penetration of the drug through the placenta was minimal. No changes in fertility were noted.

Pharmacokinetics
Due to the increased carbohydrate content, the concentration of circulating darbepoetin alpha in the blood exceeds the minimum concentration necessary for stimulating erythropoiesis for a longer time compared with equivalent doses of rhpc, which allows reducing the frequency of darbepoetin alpha administration while maintaining the equivalent level of the biological response.

Patients with chronic renal failure.
The pharmacokinetics of darbepoetin alfa has been studied in patients with chronic renal failure with intravenous and subcutaneous administration of the drug. Its half-life was 21 hours (standard deviation (CO) 7.5) when administered intravenously. The clearance of darbepoetin alfa was 1.9 ml / hour / kg (CO 0.56), and the volume of distribution (Opc) was approximately equivalent to plasma volume (50 ml / kg). After subcutaneous administration of the drug, its bioavailability corresponded to 37%. With monthly subcutaneous administration of darbepoetin alfa at a dose of 0.6 to 2.1 μg / kg, its half-life was 73 hours (CO 24). The longer half-life of darbopoetin alfa when administered subcutaneously, compared with intravenous, is due to absorption kinetics. During clinical studies, minimal accumulation of the drug was observed with any route of administration. In preclinical studies, it was demonstrated that renal clearance of darbepoetin is minimal (up to 2% of total clearance) and does not affect the half-life of the drug from serum.
The route of administration does not affect the dose of darbepoetin alfa necessary to maintain the hemoglobin achieved.

Cancer patients receiving chemotherapy.
After subcutaneous administration of the drug in a dose of 2.25 mcg / kg to adult cancer patients, the average maximum concentrations of darbepoetin alpha, which are 10.6 ng / ml (CO 5.9), were set on average for 91 hours (CO 19.7).These parameters corresponded to the linear pharmacokinetics of the dose in a wide range of values ​​(from 0.5 to 8 mcg / kg with weekly administration and from 3 to 9 mcg / kg with the introduction once every two weeks). Pharmacokinetic parameters did not change with repeated dosing for 12 weeks (weekly or biweekly). It was noted the expected moderate increase (less than 2-fold) serum concentration of the drug when it reaches an equilibrium state, but there were no signs of its accumulation during repeated administration. PK studies were performed involving patients with chemotherapy-induced anemia, which, in combination with chemotherapy, received subcutaneous injections of darbepoetin alpha at a dose of 6.75 mcg / kg every three weeks. In this study, the mean (SB) half-life was 74 (CO 27) hours.

Indications

- treatment of anemia associated with chronic renal failure in adults and children 11 years and older;
- treatment of symptomatic anemia in adult oncological patients with non-myeloid malignant neoplasms receiving chemotherapy.

Composition

The active substance in one pre-filled syringe pen (SureClick) Darbepoetin alfa (recombinant): 20 μg (40 μg / ml)
Excipients in 1 ml of solution: sodium dihydrogen phosphate monohydrate - 2.118 mg, sodium hydrogen phosphate - 0.661 mg, sodium chloride - 8.182 mg, polysorbate 80 - 0.05 mg, water for injection - up to 1 ml

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Aranesp® [Darbepoetin Alfa]

Dosage and Administration

Treatment with Aranesp should be carried out by doctors who have experience in prescribing for the above indications.
Aranesp (SureClick) is supplied ready for use in pre-filled syringe pens. PZShR intended only for subcutaneous injections. Instructions on the use of the drug, its handling and the order of its destruction are given in the section Specific instructions for use.
Treatment of anemia in patients with chronic renal failure.
Aranesp can be administered subcutaneously or intravenously. Subcutaneous administration is preferable for non-hemodialysis patients to prevent puncture of peripheral veins. The goal of therapy is to increase the hemoglobin content to a level in excess of 110 g / l. For each patient, an individual selection of the required hemoglobin above 110 g / l is necessary. It is necessary to avoid increasing hemoglobin by more than 20 g / l over 4 weeks or hemoglobin above 140 g / l. Clinical studies have shown that the individual response of the patient may be different. However, at the initial stages, the following recommendations should be followed, for both adults and children, with subsequent optimization of therapy depending on clinical indications.
Treatment with Aranesp includes two stages, a phase of correction and a supporting phase:

Phase correction.
The initial dose for subcutaneous or intravenous administration should be 0.45 mcg / kg body weight for a single weekly dose. Alternatively, for patients not receiving dialysis, subcutaneous administration of the drug is allowed at an initial dose of 0.75 mcg / kg body weight every two weeks. If the increase in hemoglobin concentration is insufficient (less than 10 g / l in 4 weeks), the dose of the drug is increased by approximately 25%. Increasing the dose should not be administered more often than once every four weeks.
If the hemoglobin concentration increases by more than 25 g / l over four weeks, the dose of Aranesp should be reduced by 25-50%, depending on the rate of hemoglobin increase. If the hemoglobin content exceeds 140 g / l, therapy should be interrupted until hemoglobin decreases below 130 g / l, and then resume the introduction of the drug in a dose reduced by about 25% compared to the previous one. Hemoglobin should be measured weekly or biweekly until it stabilizes. Subsequently, hemoglobin can be assessed periodically.

The supporting phase.
During the maintenance phase, you can continue a single weekly administration of the drug Aranesp or switch to the introduction every two weeks. When transferring patients on dialysis from weekly injections to the administration regimen once every two weeks, the initial dose should be twice the dose administered once a week. For patients who do not receive dialysis, once the desired hemoglobin concentration is achieved while the drug is given every two weeks, it can be given subcutaneously once a month using an initial dose twice the previous dose given once every two weeks.
Titration of the dose in order to maintain the desired hemoglobin concentration should be made as often as required.

For each patient, an individual selection of the required hemoglobin above 110 g / l is necessary. If it is necessary to optimize the dose of Aranesp to maintain the required hemoglobin, it is recommended to increase it by approximately 25%. If there is an increase in hemoglobin of more than 20 g / l in 4 weeks, the dose should be reduced by approximately 25%, depending on the rate of increase. If the hemoglobin content exceeds 140 g / l, therapy should be interrupted until the concentration decreases below 130 g / l, and then resume the introduction of the drug in a dose less than about 25% compared to the previous one.
After any change in dose or mode of administration, the hemoglobin content should be monitored every 1 or 2 weeks. Changing the dose during the maintenance phase should be performed no more than once every two weeks.
When changing the route of administration of the drug should use the same dose of the drug and monitor the concentration of hemoglobin every 1-2 weeks to maintain the desired level of hemoglobin.
Patients receiving weekly one, two or three injections of rhEpo can be transferred to the mode of a single weekly administration of Aranesp or its introduction once every two weeks. The initial weekly dose of Aranesp (mcg / week) is determined by dividing the total weekly rhEpo dose (IU / week) by 200. The initial dose of Aranesp (mcg / two weeks) in the once-two-week administration regimen is determined by dividing the total cumulative dose of rhEp, administered over a two-week period, at 200. In view of the known individual variability, it may be necessary to titrate doses for individual patients to obtain the optimal therapeutic effect.
When replacing rchEpo on the drug Aranesp. measurement of hemoglobin level should be performed at least once a week or two weeks, and the method of administration of the drug should remain unchanged.

Treatment of symptomatic anemia in cancer patients.
Aranesp should be administered subcutaneously to patients with anemia (with a hemoglobin concentration of ≤ 110 g / l.)
The recommended starting dose is 500 mcg (6.75 mcg / kg) once every three weeks. If the clinical response after nine weeks is inadequate (fatigue, hemoglobin content), further therapy may be ineffective.
Alternatively, once a week, the drug can be administered at a dose of 2.25 μg / kg body weight.
Aranesp is discontinued approximately four weeks after the completion of chemotherapy.
Hemoglobin content should not exceed 130 g / l.
After reaching the target hemoglobin, the dose should be reduced by 25-50% to maintain hemoglobin at an appropriate level. If necessary, further dose reduction is allowed to prevent an increase in hemoglobin concentration of more than 130 g / l.
If the rate of increase of hemoglobin exceeds 20 g / l for 4 weeks, the dose should be reduced by 25-50%.

Adverse reactions

General provisions.
In connection with the use of darbepoetin alfa, rare cases of the development of potentially significant serious allergic reactions have been described, including dyspnea, skin rashes and urticaria.
Patients with chronic renal failure.
The undesirable effects developing in the treatment of Aranesp include arterial hypertension and vascular access thrombosis. However, in the combined safety database, none of these phenomena was associated with a change in hemoglobin (less than 120 vs.> 120 g / l) or with a rate of increase in hemoglobin (less than 10, from 10 to less than 20, from 20 to less than 30 and> 30 g / l of hemoglobin for 4 weeks).
Pain at the site of subcutaneous injection was recorded more often than when using rhepo.
Discomfort at the injection site, as a rule, was mild and temporary and developed mainly after the first injection.
The adverse effects that are considered to be associated with the use of Aranesp are as follows:

Body system Detection rate Adverse reaction to the drug
Central Nervous System / Peripheral Nervous System Often found (> 1%, ≤10%) Headache
The cardiovascular system Often found (> 1%, ≤10%) Hypertension
Vascular pathology Often found (> 1%, ≤10%) Vascular access thrombosis
Injection site Often found (> 1%, ≤10%) Pain at the injection site


In very rare cases, convulsions were observed in patients with chronic renal failure receiving Aranesp.In some cases, in connection with the use of Aranesp, partial red cell aplasia (PCCA) has been described, caused by the neutralizing effect of anti-erythropoietin antibodies.
All other treatment-related adverse events were observed with a 1% frequency and less frequently (not often or rarely). Most of them had mild or moderate severity and corresponded to comorbidities in such patients.

Cancer patients.
The incidence of arterial hypertension and cardiovascular events was comparable in cancer patients who received placebo, rhEpo or Aranesp, when Aranesp was administered subcutaneously. In addition, these adverse events were not associated with either hemoglobin content (less than 130 vs.> 130 g / l), or with a rate of hemoglobin increase (> 20 g / l for four weeks). In cancer patients who received Aranesp, the incidence of thromboembolic complications, including deep vein thrombosis and pulmonary embolism, increased compared with patients who received placebo.

In general, adverse events with the use of Aranesp in cancer patients who received concomitant chemotherapy corresponded to the underlying disease and chemotherapy used to treat it.
The adverse effects that are considered to be associated with the use of Aranesp are as follows:

Body system Detection rate Adverse reaction to the drug
Musculoskeletal system Often found (> 1%, ≤10%) Arthralgia
Organism as a whole Often found (> 1%, ≤10%) Peripheral edema
Injection site Often found (> 1%, ≤10%) Pain at the injection site
Vascular pathology Often found (> 1%, ≤10%) Thromboembolic reactions


The most commonly reported adverse event deemed to be associated with the use of Aranesp (less than 5%) was pain at the injection site. Discomfort at the injection site was usually mild and temporary.

Contraindications

Hypersensitivity to darbepoetin alfa, rhEpo or to any component of the drug. Poorly controlled arterial hypertension.

Carefully

  • Liver disease;
  • sickle cell anemia;
  • epilepsy.

Drug interactions

The clinical data obtained so far do not contain indications of the interaction of Aranesp with other substances. However, it is known that its interaction with drugs characterized by a high degree of affinity for erythrocytes, such as cyclosporine, tacrolimus, is potentially possible. With the simultaneous appointment of darbepoetin alfa with any similar drugs, the level of their content in blood serum should be monitored with a dose modification in case of an increase in hemoglobin concentration.
Due to the fact that compatibility studies have not been carried out, Aranesp should not be mixed or administered as an infusion along with other medications.

Pregnancy and Lactation

Adequate and strictly controlled clinical studies on the safety of using Aranesp during pregnancy have not been conducted. With caution and after careful assessment of the expected benefits of therapy for the mother and the potential risk to the fetus, the drug should be prescribed to pregnant women. If necessary, the appointment of Aranesp during lactation breastfeeding should be stopped.

Special instructions

General provisions.
In order to confirm the effectiveness of erythropoiesis, all patients should determine the iron content before and during treatment with the goal of prescribing, if necessary, additional therapy with iron preparations.
The lack of response to the use of Aranesp should serve as an incentive to identify causal factors. The effectiveness of substances stimulating erythropoiesis decreases with a lack of iron, folic acid or vitamin B12 in the body, as a result of which their level must be adjusted.The erythropoietic response can also be weakened in the presence of concomitant infectious diseases, symptoms of inflammation or cases of trauma, hidden blood loss, hemolysis, severe aluminum intoxication, concomitant hematological diseases or bone marrow fibrosis. The number of reticulocytes should be considered as one of the evaluation parameters. If the typical reasons for the lack of response are excluded, and the patient has reticulocytopenia, a bone marrow examination should be performed. If the picture of the bone marrow corresponds to the PKKA picture, it is recommended to perform a study for the presence of antibodies to erythropoietin.
PCCA, caused by the neutralizing effect of anti-erythropoietin antibodies, has been described in connection with the use of recombinant erythropoietic proteins, including darbepoetin alfa. These antibodies have been shown to cross-react with all erythropoietic proteins. In the case of the diagnosis of PCCA, treatment with Aranesp should be stopped without a subsequent transfer of the patient to a therapeutic regimen that includes another recombinant erythropoietic protein (see the Adverse Effects section).
In all studies of Aranesp, the exclusion criterion was active liver disease, so there are no data on the use of the drug in patients with impaired liver function. Since the liver is considered the main route of excretion of Aranesp and rhEpo, these drugs should be prescribed with caution in patients with liver pathology.
Abuse of Aranesp in healthy individuals can lead to an excessive increase in hematocrit. Such events can be associated with life-threatening complications of the cardiovascular system.
The protective cap of the needle on PZShR contains in its composition natural dehydrated rubber (a derivative of latex), which may be the cause of an allergic reaction.

Patients with chronic renal failure.
The use of supplementary therapy with iron preparations is recommended for all patients in whom the serum ferritin concentration does not exceed 100 mcg / l or the transferrin saturation level is below 20%. Blood pressure should be monitored in all patients, especially at the beginning of Aranesp use. Patients should be aware of the importance of adhering to the recommendations on the use of antihypertensive drugs and dietary restrictions. If blood pressure is poorly controlled during the corresponding procedures, it is possible to reduce the hemoglobin content by reducing the dose of Aranesp or temporarily ceasing its administration (see the section Dosage and administration).
In patients with chronic renal failure and clinical symptoms of coronary heart disease or congestive heart failure, target hemoglobin levels should be determined individually. In such patients, the maximum hemoglobin content should not exceed 120 g / l, unless the severity of the symptoms (for example, angina) requires a different solution.
During the application of Aranesp should be regularly monitored for serum potassium. An increase in potassium concentration has been described in several patients receiving Aranesp, but a causal relationship has not been established. If you identify increased or increasing concentrations of potassium, the introduction of Aranesp should be discontinued until its normalization.
Patients suffering from epilepsy should be prescribed Aranesp with caution, as there are reports of the development of seizures in patients with chronic renal failure who received Aranesp.

Cancer patients
Effect on tumor growth.
Erythropoietins are growth factors that mainly stimulate the production of red blood cells. Erythropoietin receptors can be expressed on the surface of various tumor cells.As in the case of any growth factors, there is an assumption that erythropoietins are capable of stimulating the growth of malignant neoplasms of any type. In two controlled clinical studies on the use of erythropoietin in patients with various forms of cancer, including head and neck and breast cancer, an unexplained increase in mortality was demonstrated.
In patients with solid tumors or lymphoproliferative malignant diseases with an increase in hemoglobin levels above 130 g / l, the dose adjustment scheme described in the section Dosage and administration should be strictly followed in order to minimize the potential risk of thromboembolic events. It is also necessary to regularly monitor the number of platelets and hemoglobin concentration in the blood.
Special instructions for use

Aranesp is a sterile product made without preservatives. One syringe pen should be administered no more than one dose of the drug. Any amount of the drug remaining in the pre-filled syringe pen should be destroyed.
Before the introduction of the drug solution Aranesp should be monitored for the presence of visible particles. It is allowed to use only colorless, transparent or slightly opalescent solution. Do not shake the solution. Before the introduction should wait for warming up the PZSHR to room temperature.
To avoid discomfort at the injection site, it is necessary to change the injection site.
Any quantities of unused product or its waste must be destroyed in accordance with local requirements.

Overdosage

The boundaries of the therapeutic dose of the drug Aranesp are very wide. Even with very high serum concentrations of the drug, no overdose symptoms were observed.
In case of detection of polycythemia, the administration of Aranesp should be temporarily stopped (see the section Dosage and administration). If clinically indicated, phlebotomy can be performed.

  • Brand name: AnviMax®
  • Active ingredient: Paracetamol, Ascorbic acid, Rimantadine, Rutozid, Loratadine, Calcium gluconate
  • Dosage form: Effervescent pills [with cranberry taste and aroma], effervescent pills [with raspberry taste and aroma]. On 10 pills in a tub from polypropylene complete with a cover from polyethylene with a silica gel insert.
    On 1 tuba together with the application instruction in a pack from a cardboard.
  • Manufacturer: FarmVILAR FPK

Studies and clinical trials of Darbepoetin Alfa (Click to expand)
  1. Recurrent skin reaction secondary to darbepoetin alfa for two months in a patient with chronic lymphocytic leukemia
  2. Darbepoetin alfa 300 or 500 μg once every 3 weeks with or without intravenous Iron in patients with chemotherapy-induced anemia
  3. A randomized, active-control, pilot trial of front-loaded dosing regimens of darbepoetin-alfa for the treatment of patients with anemia during chemotherapy for malignant disease
  4. A randomized controlled trial of darbepoetin alfa administered as a fixed or weight-based dose using a front-loading schedule in patients with anemia who have nonmyeloid malignancies
  5. A randomized, active-control, pilot trial of front-loaded dosing regimens of darbepoetin-alfa for the treatment of patients with anemia during chemotherapy for malignant disease
  6. Anemia Management in Adult Chronic Hemodialysis Patients Using Darbepoetin Alfa Protocol
  7. The efficacy of monthly administration of darbepoetin alfa in Saudi hemodialysis patients
  8. Timing of the administration of intravenous darbepoetin alfa during the dialysis session: Does it impact efficacy?
  9. Physical and biophysical effects of polysorbate 20 and 80 on darbepoetin alfa
  10. A Multicenter, Open Study Evaluating the Impact of Darbepoetin Alfa on Anaemia and Quality of Life, in Cancer Patients Undergoing Radiotherapy
  11. Comparison of Darbepoetin Alfa and Epoetin Alfa for Radiotherapy(RT) or Chemoradiotherapy(CT/RT)-Induced Anemia
  12. The impact of timing of chemotherapy relative to darbepoetin alfa (DA) on DA pharmacokinetics (PK) and hematologic effects
  13. Development and evaluation of a population pharmacokinetic (PK) model for darbepoetin alfa in healthy subjects
  14. The development and validation of a sensitive, dual-flow cell, SPR-based biosensor immunoassay for the detection, semi-quantitation, and characterization of antibodies to darbepoetin alfa and epoetin alfa in human serum
  15. P92 Current practice use of darbepoetin alfa in the management of chemotherapy-induced anaemia in patients < 65 and ≥65 years: interim data from CHOICE, an international, observational study
  16. Randomized, dose-finding study of darbepoetin alfa in anaemic patients with lymphoproliferative malignancies
  17. Efficacy and safety of darbepoetin alfa in anaemic patients with lymphoproliferative malignancies: a randomized, double-blind, placebo-controlled study
  18. NOVEL ERYTHROPOIESIS STIMULATING PROTEIN (DARBEPOETIN ALFA) ADMINISTERED ONCE EVERY OTHER WEEK CORRECTS ANAEMIA IN PATIENTS WITH CKD
  19. Randomized trial of darbepoetin alfa for treatment of renal anemia at a reduced dose frequency compared with rHuEPO in dialysis patients
  20. Darbepoetin alfa: A new therapeutic agent for renal anemia
  21. Extended dosing of darbepoetin alfa in peritoneal dialysis patients
  22. Pharmacokinetic evaluation of darbepoetin alfa for the treatment of pediatric patients with chemotherapy-induced anemia

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