Enplate 250 mcg
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Pharmacological action – stimulating thrombopoiesis.
Pharmacodynamics
Romiplostim is an Fc-peptidylated protein (peptide antibody) involved in signaling and activation of intracellular transcription through binding to thrombopoietin (TPO) receptors (also known as cMpl) and inducing increased platelet formation. The peptide antibody molecule consists of an Fc-fragment of human immunoglobulin IgG1, in which each single-chain subunit is covalently linked at the C-end to a peptide chain containing two TPO receptor-binding fragments.
The amino acid sequence of romiplostim is not homologous to the amino acid sequence of endogenous TPO. No cross-reactivity of antibodies to Romiplostim with endogenous TPO was observed in preclinical and clinical studies.
Clinical efficacy
The efficacy and safety of Romiplostim has been evaluated with a treatment duration of up to 3 years. In clinical trials, treatment with Romiplostim resulted in a dose-dependent increase in platelet count. The time to maximum effect on platelet counts was about 10-14 days and was independent of the dose. After a single p/c administration of romiplostim at a dose of 1 to 10 mcg/kg in patients with idiopathic (immune) thrombocytopenic purpura (ITP), the peak platelet count was 1.3-14.9 times the baseline platelet count within 2-3 weeks. The response to treatment varied in all patients. The majority of patients with ITP who received romiplostim at doses ranging from 1 to 3 mcg/kg for 6 weeks had platelet counts ranging from 50 to 450 × 109/L. Of the 271 patients with ITP who received romiplostim in clinical trials, 55 (20%) were 65 years of age or older, and 27 (10%) were 75 years of age or older. In placebo-controlled trials, no differences in safety and efficacy were found between older and younger patients.
Results from basic placebo-controlled studies
The safety and efficacy of romiplostim was evaluated in two placebo-controlled, double-blind studies in adult patients with ITP who received at least one course of treatment before participating in the study and who represented the full spectrum of the ITP patient population. Both studies followed a similar design. Patients (over 18 years of age) were randomized in a 2:1 ratio and received a starting dose of romiplostim of 1 mcg/kg or placebo, respectively. Patients received a single weekly injection for 24 weeks. Doses were adjusted to maintain platelet counts (50 to 200 × 109/L). In both studies, efficacy was determined by an increase in the number of patients in whom a sustained increase in platelet count was achieved. The average weekly dose in patients with splenectomy was 3 mcg/kg, and 2 mcg/kg in patients with preserved spleen.
In both studies, a significantly higher proportion of patients who received romiplostim showed a sustained response in the form of increased platelet counts compared to patients who received placebo. In placebo-controlled studies after the first 4 weeks of romiplostim, platelet counts were maintained at ≥50 × 109/L in 50-70% of patients during the 6-month treatment period. In the placebo group, only 0-7% of patients showed an increase in platelet count during the 6-month treatment period. In both studies, patients already receiving therapy for ITP according to the established regimen continued to use these drugs for the entire study period (corticosteroids, danazol and/or azathioprine). At the beginning of the study 21 patients with preserved spleen and 18 patients who underwent splenectomy received therapy with drugs for ITP (predominantly corticosteroids). In all patients (100%) after splenectomy who received romiplostim it was possible to reduce the dose of corticosteroids by more than 25%, or even to cancel standard therapy for ITP at the end of treatment, compared with 17% of patients who received placebo. In 73% of patients with preserved spleen who received romiplostim, it was possible to reduce the dose by more than 25%, or even to cancel standard therapy for ITP at the end of treatment, compared with 50% of patients who received placebo.
Bleeding Events
An inverse relationship between bleeding events and platelet counts was observed throughout the clinical ITP treatment program. All clinically significant bleeding events (≥3 grade) occurred at platelet counts < 30 × 109/L. All cases of bleeding ≥ grade 2 occurred at platelet counts < 50 × 109/L. There were no statistically significant differences between all observed bleeding events among patients receiving Enplat or placebo. In two placebo-controlled studies, 9 patients experienced bleeding that was considered serious, (5 [6%] romiplostim, 4 [9.8%] placebo; relative risk [romiplostim/placebo] = 0.59; 95% confidence interval = (0.15; 2.31)). Bleeding events of grade 2 or higher occurred in 15% of patients receiving romiplostim and 34% of patients receiving placebo (relative risk; [romiplostim/placebo]=0.35; 95% confidence interval = (0.14; 0.85)).
Pharmacokinetics
The pharmacokinetics of romiplostim are based on the target-mediated distribution of the drug, which is probably due to receptors for thrombopoietin (TPO) located on the surface of platelets and other platelet-derived cells, such as megakaryocytes.
Absorption
After p/c administration of 3 to 15 µg/kg romiplostim, Cmax in plasma in patients with idiopathic (immune) thrombocytopenic purpura (ITP) was noted after 7-50 h (mean, 14 h). Plasma drug concentrations varied among patients and did not correlate with the administered dose. Plasma concentrations of Romiplostim are probably inversely related to platelet counts.
Distribution
The distribution volume of romiplostim in healthy volunteers after IV administration decreased nonlinearly from 122; 78.8 to 48.2 mL/kg for IV doses of 0.3; 1.0 and 10 µg/kg, respectively. This nonlinear decrease in volume of distribution is consistent with the target-mediated binding of romiplostim (megakaryocyte and platelet receptors), which can be saturated at higher doses.
The T1/2 of Romiplostim in patients with ITP varies from 1 to 34 days (average, 3.5 days). The plasma excretion of Romiplostim depends in part on the expression of TPO receptors on platelets. As a consequence of the dose received, patients with high platelet counts show low plasma concentrations and vice versa. In another study involving patients with ITP, no cumulation was observed after 6 weeks of weekly use of romiplostim (3 mcg/kg).
Particular patient groups
There have been no studies of the pharmacokinetics of Romiplostim in patients with renal and hepatic impairment. Presumably, the pharmacokinetics of Romiplostim are not affected by age, body weight and sex to a clinically significant degree.
Indications
Enplate is used to treat adult patients with ITP with or without preserved spleen who have not responded to previous therapy with corticosteroids or immunoglobulins.
Enplate is also used to treat children over 1 year of age with chronic ITP with or without preserved spleen who have not responded to previous therapy with corticosteroids or immunoglobulins.
If there is no improvement or you feel worsened, you should consult a physician.
Active ingredient
Romiplostim
Composition
The drug Enplate contains:
- The active ingredient is Romiplostim.
Each vial of Enplate, 250 mcg, powder for preparation of a solution for subcutaneous injection, contains 375 mcg of Romiplostim. An excess of the contents of each vial ensures the administration of 250 µg of Romiplostim. The 0.5 ml of the resulting solution will contain 250 µg of Romiplostim (the drug concentration will be 500 µg/ml).
- The excipients are mannitol (E421), sucrose, L-histidine, hydrochloric acid (for pH regulation) and polysorbate 20.
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How to take, the dosage
Always use the drug in full accordance with your physician’s recommendations.
Check with your doctor if you have any doubts.
Application in adults and children (ages 1 to 17 years)
Recommended dosage
The starting dose is 1 microgram of Enplet per kilogram of body weight (once a week). Your physician will tell you how much Enplatelet you should receive. In order to increase your platelet count, injections of Enplatelet should be given once a week. Your physician will take regular blood samples to assess the platelet response. The dose will be adjusted if necessary.
When your platelet count is under control, your physician will continue to check your blood regularly. The dose may be adjusted to maintain the correct platelet count over time.
Application in children (ages 1 to 17 years)
In addition to determining your platelet count, your doctor will also measure your body weight regularly to adjust the dose.
The route and/or route of administration
Enplet is used under the direct supervision of your doctor, who will carefully monitor the dose you are getting.
Enplet is given once a week as a subcutaneous injection.
If you have used more Enplate than you should
The doctor who treats you will make sure you are getting the correct dose of Enplate. You may not experience any physical symptoms if you use a higher dose of Enplate, but your platelet count may become very high, increasing your risk of blood clots. Therefore, if your doctor suspects that a higher dose of Enplate is being used, it is recommended that you watch for any signs or symptoms of adverse reactions and get appropriate treatment immediately.
If you have used less Enplate than you should
The attending physician will make sure you are getting the correct dose of Enplate. You may not experience any physical symptoms if you use a lower dose of Enplate, but your platelet count may decrease, resulting in an increased risk of bleeding. Therefore, if your physician suspects you are using a lower dose of Enplate, it is recommended that you watch for any signs and symptoms of adverse reactions and get appropriate treatment immediately.
If you forget to use Enplate
If you miss a dose of Enplate, your healthcare provider will arrange with you when the next dose should be given.
If you stop using Enplate
If you stop using Enplate, you may experience a recurrence of thrombocytopenia (decreased platelet count). Your doctor will decide if you can stop using Enplatelet.
Contact your doctor if you have any questions about the use of the drug.
Interaction
Tell your doctor if you are taking, have recently taken or may start taking any other medications.
If you are also taking medications that prevent blood clots (anticoagulants or antiaggregants), the risk of bleeding increases. Your doctor will discuss this with you.
If you are taking corticosteroids, danazol and/or azathioprine to treat ITP, you can either reduce the dose of these drugs or stop them while you are taking Enplate.
Special Instructions
Consult with your doctor, pharmacist, or nurse before using Enplatelet:
- If you are at increased risk of blood clots or if it runs in your family.
The following factors also increase your risk of blood clots:
- liver problems;
- older age (≥65 years);
- bedridden
- malignant neoplasms
- previous surgery or trauma;
- obesity (overweight);
- smoking.
If your platelet count is very high, these factors may increase your risk of blood clots. Your doctor will adjust the dose of Enplatelet to rule out an excessive increase in your platelet count.
- Cessation of Enplatelet may cause a recurrence of thrombocytopenia (decreased platelet count). Your platelet count will need to be monitored if Enplatelet is discontinued. Your doctor will also discuss with you the precautions you need to follow.
Trackability
To improve the traceability of biological medicines, you must accurately document the name and series number of the drug used.
Bone marrow changes (increased reticulin concentration and possible bone marrow fibrosis
The long-term use of Enplate may cause bone marrow changes. These changes can lead to abnormal blood cells or decreased blood cell production. A mild form of these changes in the bone marrow, characterized by increased reticulin concentrations, has been noted in clinical trials of Enplate. It is unknown whether these changes progress to a more severe form (fibrosis). Signs of changes in the bone marrow may be abnormalities detected in blood tests. Your doctor will determine if the abnormal blood test results mean that bone marrow tests need to be done or if Enplate should be discontinued.
Mistakes when using Enplate
Medical errors when using Enplate may be over- or under-dosing. Guidelines for dose calculation and adjustment should be followed.
The administration of too high doses of the drug may result in an excessive increase in platelet counts, which may cause thrombotic/thromboembolic complications. If there is an excessive increase in the platelet count, Enplatelet should be discontinued, and the platelet count should be monitored.
The administration of an insufficient dose may result in a lower than expected platelet count and the possibility of bleeding. It is recommended that platelet counts be monitored when using Enplatelet.
Progression of malignant blood diseases
Your doctor may decide to do a bone marrow biopsy if he or she feels it is necessary to confirm the diagnosis of IPS and rule out other diseases such as myelodysplastic syndrome (MDS). If Enplate is used with MDS, the number of blast cells may increase and MDS may evolve into acute myeloid leukemia (a type of malignant blood disease).
Loss of response to romiplostim therapy
. If there is a loss or lack of platelet response to Romiplostim therapy, your doctor will determine the causes, including whether there is increased reticulin deposition in the bone marrow and whether your body is producing antibodies that neutralize the activity of Romiplostim.
Effects on red and white blood cells
During the use of Romiplostim, there can be changes in the number of red (decrease) and white (increase) blood cells. Your doctor may recommend that you have regular blood tests to check these numbers.
Children and adolescents
Enplet is not recommended for use in children under 1 year of age.
Other medicines and Enplate
Tell your doctor if you are taking, have recently taken, or might start taking any other medicines.
If you are also taking medicines that prevent blood clots (anticoagulants or antiaggregants), there is an increased risk of bleeding. Your doctor will discuss this with you.
If you are taking corticosteroids, danazol and/or azathioprine to treat ITP, you can either reduce the dose of these drugs or stop them while you are taking Enplate.
Driving and operating machinery
Talk to your doctor before you start driving or operating machinery, as some adverse reactions to the drug (such as dizzy spells) may affect your ability to do so safely.
Synopsis
The active ingredient of Enplate is Romiplostim. Romiplostim belongs to the hemostatic agents, and its action is based on stimulating the production of platelets, specific cells whose work is necessary to stop bleeding. Romiplostim is used for low platelet counts in patients with primary immune thrombocytopenia (ITP). ITP is a condition in which the body’s immune system destroys its own platelets. Platelets are blood cells that help repair tissue damage and form blood clots. A significant decrease in the number of platelets can lead to bruising and cause serious bleeding.
The principle of Enplatelet is the stimulation of the bone marrow (a blood-producing organ inside the bones that produces blood cells) to increase the number of platelets. Such stimulation should help to prevent the appearance of hematomas and prevent bleeding against ITP.
Contraindications
Do not use Enplate:
– If you are allergic to Romiplostim or any other drug components (listed in Section 6 of the package insert);
– If you are allergic to other drugs that are manufactured using DNA technology with the bacterium Escherichia coli (E coli).
Side effects
Like all medicines, this medicine can cause adverse reactions, but not everyone has them.
The most serious adverse reactions that can occur with Enplate are listed below:
Frequent – may occur in no more than 1 in 10 people (may be detected by blood and urine tests):
- low blood platelet counts (recurrence of thrombocytopenia and bleeding after stopping treatment);
Frequent – may occur in no more than 1 in 10 people
- bone marrow disorders, including increased bone marrow fibers (increased levels of reticulin deposits);
infrequent – may occur in no more than 1 in 10 people (may be detected by blood and urine tests):
- the number of platelets in the blood can rise to very high levels (overdose), which can increase the risk of clotting; Or platelet counts may decrease (underdose), which may increase the risk of bleeding (medication errors);
Frequency is unknown – based on available data, the incidence cannot be determined:
- increase in blast cells and worsen myelodysplatic syndrome to acute myeloid leukemia, which is a type of malignant blood disease (progression of existing myelodysplatic syndrome to acute myeloid leukemia).
If you develop any of the above symptoms, stop using Enplate immediately and see your doctor, or seek medical advice.
Possible adverse reactions in adult patients with ITP
Very common – may occur in more than 1 in 10 people:
- headache;
- hypersensitivity (allergic reaction);
- infection of the upper respiratory tract.
Frequent – may occur in no more than 1 in 10 people:
- disruption of sleep (insomnia);
- dizziness;
tingling or numbness in the hands and feet (paresthesia);
- migraine;
- reddening of the skin (hot flashes);
- pulmonary artery thrombosis (pulmonary embolism);
- nausea;
- diarrhea;
- abdominal pain;
- disordered digestion (dyspepsia);
- constipation;
- cutaneous itching (pruritus);
- subcutaneous hemorrhage (ecchymosis);
- bruises (contusions);
- rash;
- Joint pain (arthralgia);
- muscle pain or weakness (myalgia);
- pain in the hands and feet;
- muscular cramps;
- back pain;
- bone pain;
- fatigue (fatigue);
- reactions at the injection site;
- oedema of the hands and feet (peripheral oedema);
- pain;
- weakness (asthenia);
- increased body temperature (pyrexia);
- chills;
- bruises;
- swelling of the face, lips, mouth, tongue, or throat, which may prevent swallowing or breathing (angioedema);
- gastroenteritis;
- sensation of palpitations;
- inflammation of the sinuses (sinusitis);
- inflammation of the pathways through which air enters the lungs (bronchitis).
Frequent – may occur in no more than 1 in 10 people (may be detected by blood and urine tests):
- anemia.
Infrequent – may occur in no more than 1 in 100 people:
- Bone marrow insufficiency, bone marrow disease resulting in scarring (myelofibrosis), enlarged spleen (splenomegaly), vaginal bleeding, rectal bleeding, oral bleeding, injection site bleeding;
- heart attack (myocardial infarction), increased heart rate;
- dizziness or dizziness (vertigo);
- Eye problems, including ocular hemorrhage (conjunctival hemorrhage), difficulty focusing or blurring of the visual field (accommodation disorder, congestion disk or eye disorders), blindness, itching in the eye, increased lacrimation, visual disturbances;
- Digestive problems, including vomiting, bad breath, difficulty swallowing (dysphagia), poor digestion or heartburn (gastroesophageal reflux disease), blood in stools (hematochezia), abdominal discomfort, mouth ulcers or blisters (stomatitis), discoloration of teeth;
- decreased body weight, weight gain, alcohol intolerance, loss of appetite (anorexia or decreased appetite), dehydration;
- flu, local infection, inflammation of nasal passages and throat (nasopharyngitis);
- pain and swelling of joints due to uric acid, which is produced during the breakdown reactions in digestion (gout);
- muscle tension, muscle weakness, shoulder pain, muscle twitching;
- depression, unusual dreams;
- hair loss (alopecia), sensitivity to light (photosensitivity reaction), acne, skin allergic reaction upon contact with an allergen (contact dermatitis), skin rashes and blisters (eczema), dry skin, redness on the skin (erythema), increased skin flaking (exfoliative rash) abnormal hair growth, thickening and itching of the skin due to scratching (prurigo), subcutaneous hemorrhage or bleeding (purpura), papular rash, itchy skin rash, generalized itchy rash (urticaria), skin nodules, unusual body odor;
- .blood circulation problems, including blood clots inside the liver (portal vein thrombosis), deep vein thrombosis, low blood pressure (hypotension), high blood pressure, blockage of blood vessels (peripheral artery embolism) decreased blood flow in the hands, ankles or feet (peripheral ischemia), swollen veins and the formation of blood clots in them, sometimes accompanied by a particular painfulness when touching the veins (phlebitis or superficial thrombophlebitis), thrombus formation (thrombosis);
- a rare syndrome in which there is periodic burning pain in the feet and hands, accompanied by redness and increase in their temperature (erythromelalgia).
infrequent – may occur in no more than 1 in 10 people (may be detected by blood and urine tests):
- a rare type of anemia in which red blood cell, white blood cell, and platelet levels are reduced (aplastic anemia);
- increased white blood cell count (leukocytosis);
- changes in the results of some blood tests (increased levels of transaminases, increased levels of lactate dehydrogenase in the blood);
- cancer of leukocytes (multiple myeloma);
- protein in the urine.
Possible adverse reactions in children with ITP
Very common – may occur in more than 1 in 10 people:
- infection of the upper respiratory tract;
- pain in the mouth and throat (pain in the oropharynx);
- rinitis (itching, runny or stuffy nose);
- pain in the upper abdomen;
- diarrhea;
- rash;
- high body temperature (pyrexia);
- bruises (bruises).
Frequent – may occur in no more than 1 in 10 people:
- gastroenteritis;
- pain and discomfort in the throat when swallowing (pharyngitis);
- inflammation of the eye (conjunctivitis);
- ear infection;
- inflammation of the sinuses (sinusitis);
- edema of the extremities, hands or feet;
- subcutaneous haemorrhage or bleeding (purpura);
- a pruritic rash (urticaria).
infrequent – may occur in no more than 1 in 100 people:
- high platelet count (thrombocytosis)
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Pregnancy use
If you are pregnant or breastfeeding, think you may be pregnant, or are planning a pregnancy, talk to your doctor or pharmacist before using this medicine. Enplate is not recommended for use during pregnancy unless prescribed by your doctor.
It is not known if Romiplostim penetrates into breast milk. Enplate is not recommended for use during breastfeeding. When deciding whether to stop breastfeeding or Romiplostim therapy, consider the benefits of breastfeeding for the baby and the benefits of Romiplostim therapy for the mother.
Consult your physician before using any medication.
Weight | 0.031 kg |
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Shelf life | 3 years |
Conditions of storage | Store the product out of the reach of children where they cannot see it. Do not use after the expiration date printed on the carton and vial label after "Expired until:". The expiration date is the last day of that month. Store between 2 and 8°C. Do not freeze. Store in the original package (carton) to protect it from light. The product can be stored outside the refrigerator for 30 days at a temperature not exceeding 25 °C in the original package (carton pack). After dilution: for 24 hours at 25 °C or for 24 hours at 2 to 8 °C in the original package (carton pack) to protect from light. Do not dispose of any medicines in the sewer system or with household waste. Ask your pharmacy technician how to dispose of medicines that Do not throw them away. |
Manufacturer | Pateon Inc, Canada |
Medication form | solution for injection |
Brand | Pateon Inc |
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