Revolade 25mg Novartis anti-bleeding amarga trombosit ing getih (28 tablet)

Bentuk sediaan Kothak 4 blister x 7 tablet
Spesifikasi Eltrombopag

Komposisi

Informasi komposisi	Isi
Eltrombopag	25 mg

Migunakake

indications Revolade drug indications for treatment in the following cases: Treatment of patients from 1 year of age and older suffers from primary immune platelet (Primary Immune Thrombocytopenia - ITP) lasting from 6 months or more from diagnosis and resistance to other treatments (for example, corticosteroids, immune globulin). Strong treatment earlier and not suitable for hematoma stem cells. ATC code: B02bx 05. Mechanism of impact: TPO is the main cytokine related to the regulation of the production of platelets (megakaryopoies) and the production of endogenous platelets, and endogenous ligand for TPO-R. Eltrombopag interacts with TPO-R's piercing area in humans and onset the same signal communication but is not the same as the transmission of thrombopoietin (TPO), which stimulates the proliferation and differentiation from the precursor cells of the bone marrow. Dynamic pharmacokinetics Eltrombopag's concentration data in plasma are collected in 88 patients with immune thrombocytopenia in examinations 100773A and tra100773b are combined with data from 111 healthy adults in population pharmacokinetic analysis. Estimated AUC (0-τ) and CMAX of Eltrombopag in relatively blood for patients with thrombocytopenia are presented (Table 1). Table 1: Average geometry (95%trust) of Eltrombopag pharmacokinetics parameters in plasma in a stable state in adults with immunomemosis. dose of Eltrombopag, 1 time/day auc (0- τ) a, μg. (39, 58) 3.78 (3.18; 4,49) 198) 12.7 (11,0; 14.5) absorption and bioavailability Eltrombopag is absorbed with a peak concentration of 2 to 6 hours after drinking. Use Eltrombopag simultaneously with antacids and other products containing multi -chemotherapy cations such as dairy products and mineral supplements significantly reducing Eltrombopag levels (see the dose and usage). The absolute use of Eltrombopag has not been established after drinking. Based on the excretion of urine and metabolic substances eliminated in the stool, the oral absorption estimate of drug -related substances after the single dose of 75 mg of Eltrombopag solution is at least 52%. Distribution Eltrombopag is highly connected to human plasma proteins (> 99.9%), mainly with albumin. Eltrombopag is a substrate for BCRP, but not a substrate for p-glycoprotein or Oatp1b1. Biological metabolism Eltrombopag is metabolized mainly through cutting, oxidizing and assembling with glucuronic acid, glutathione, or cysteine. In human radioactive isotope, Eltrombopag accounts for about 64% of Aucinf of radioactive carbon in plasma. Metabolic substances account for small quantities due to glucuronide and oxidation are also detected. In vitro studies show that CYP1A2 and CYP2C8 are responsible for the oxidation metabolism of Eltrombopag. Uridine diphosphoglucuronyl Transferase UGT1A1 and UGT1A3 is responsible for glucuronide and bacteria in the lower digestive tract may be responsible for the cutting line. Elimination The amount of Eltrombopag is widely metabolized. The main excretion path of Eltrombopag is in feces (59%) and 31% of the dose found in urine in the form of metabolites. Eltrombopag is not detected in urine. Eltrombopag does not change excretion through feces accounting for about 20% of the dose. Eltrombopag's plasma semi -discharged time is approximately 21 - 32 hours. pharmacokinetic interaction Based on a human study with Eltrombopag, which has a radioactive isotope, the glucuronide plays a small role in the metabolism of Eltrombopag. Studies on microsomes of human liver cells confirm UGT1A1 and UGT1A3 are enzymes responsible for glucuronids Eltrombopag. Eltrombopag is an inhibitor of some In vitro uGT enzymes. Clinically, not predicting significant drug interactions associated with glucuronid due to the limited contribution of each individual enzyme UGT in the glucuronide elrombopag. About 21% of Eltrombopag dose can be metabolized by oxidation. Studies on human liver cell microsomes identify CYP1A2 and CYP2C8 are enzymes that play the role of Eltrombopag oxidation. Eltrombopag does not inhibit or induce CYP enzymes based on in vitro and in vivo data (see the interaction, cavalry of the drug). In vitro studies prove that Eltrombopag is an inhibitor of OatP1B1 transport agent and is a inhibitor of BCRP and Eltrombopag transportation that increases the concentration of rosuvastatin as the substrate of OATP1B1 and BCRP in a clinical interaction study (see the interactive section, the cavalry of the drug). In clinical studies with Eltrombopag, it is recommended to reduce the dose of statin by 50%. Eltrombopag makes chelate multi -chemotherapy cations such as iron, calcium, magnesium, aluminum, selenium and zinc (see the dose and usage and interaction, the cavalry of the drug). In vitro studies have shown that Eltrombopag is not a substrate for OATP1B1 is the organic polypeptide polypeptide but it is a transportation inhibitor (IC50 value is 2.7 μm (1.2 μg/ml). In Vitro studies also show that Eltrombopag is the substance and inhibitor of breast cancer protein (BCRP) (BCRP) (BCRP) (BCRP) (BCRP) (BCRP) (BCRP) (BCRP) is 2.7 μm (1.2 μg/ml)). Special patient groups kidney failure Eltrombopag's pharmacokinetics was studied after taking Eltrombopag for adult patients with kidney failure. After using the single dose of 50 mg, the AUC0-∞ of Eltrombopag is 32% to 36% lower in patients with mild to moderate and lower renal impairment patients than 60% in patients with severe renal failure compared to healthy volunteers. There is a significant variation and duplication of concentration between patients with renal impairment and healthy volunteers. Eltrombopag concentration (active ingredient) does not connect to this high protein -connected drug has not been measured. Patients with renal function should be cautious when using Eltrombopag and closely monitor, for example by testing serum creatinine and/or urine analysis. Effectiveness and safety of Eltrombopag have not been identified in patients with both renal failure and medium to severe liver and liver failure. Hepatic failure Eltrombopag's pharmacokinetics was studied after taking Eltrombopag for adult patients with liver failure. After using the single dose of 50 mg, the AUC0-∞ of Eltrombopag is higher than 41% in patients with mild liver failure and 80% to 93% higher in patients with medium to severe liver failure compared to healthy volunteers. There is a significant coincidence and variability of concentrations between patients with liver failure and healthy volunteers. Eltrombopag concentration (active ingredient) does not connect to this high protein -connected drug has not been measured. Effect of liver failure on Eltrombopag's pharmacokinetics after repeated use has been evaluated through population pharmacokinetic analysis in 28 healthy adults and 714 patients with liver failure (673 patients infected with HCV and 41 patients with chronic liver disease due to other raw disease). Of the 714 patients, 642 patients with mild liver failure, 67 patients with average liver failure and 2 patients with severe liver failure. Compared to healthy volunteers, mild liver failure patients with AUC (0-τ) of Eltrombopag in plasma is about 111% higher (95% confidence range: 45% to 283%) and patients with average liver failure with AUC value (0-τ) of Eltrombopag in plasma higher than 183% (95% confidence range: 95% to 459%). Therefore, Eltrombopag should not be used in patients with immunomemosis with liver failure (Child-Pugh score ≥ 5) unless the expected benefits are greater than the risk of being defined of the portal vein thrombosis (see the dose and usage and cautious ways). For patients infected with HCV starting to use Eltrombopag at a dose of 25 mg, 1 time/day (see the dose and usage). Race The influence of Asian races (such as Japanese, China, Taiwan and South Korea) on Eltrombopag's pharmacokinetics has been evaluated by using population pharmacokinetics analysis on 111 healthy adults (31 Asian patients) and 88 ITP patients (18 Asian patients). Based on the estimated pharmacokinetic analysis of population pharmacokinetics, Asian ITP patients with AUC (0-τ) Eltrombopag plasma is about 49% higher than non-Asian patients, mainly whites (see the dose and usage). Gender The effect of gender on Eltrombopag's pharmacokinetics has been evaluated using the pharmacokinetic analysis of population population over 111 healthy adults (14 women) and 88 ITP patients (57 women). Based on the estimated pharmacokinetics analysis of population, female ITP patients with AUC (0-τ) Eltrombopag plasma is about 23% higher than that of male ITP patients, when they have not been corrected according to body weight difference. The population of children (from 1 to 17 years old) Eltrombopag's pharmacokinetics is evaluated on 168 children with ITP used 1 time/day in 2 studies, tra108062/petit and tra115450/Petit-2. Eltrombopag's apparent clearance in plasma (Cl/F) increases with body weight. The influence of race and gender on Eltrombopag's CL/F estimates in plasma is homogeneous between children and adults. Patients with Asian children with immunity reduced AUC (0-τ) of Eltrombopag in plasma is about 43% higher than non-Asian patients. Patients with female immune platelets are valid for AUC (0-τ) of Eltrombopag in plasma is about 25% higher than that of male patients. Eltrombopag's pharmacokinetics parameters in children with ITP are shown in Table 2. Table 2: Geometric average average (95%confidence interval) of Eltrombopag pharmacokinetics parameters in plasma in a stable state in children with immunomemosis (the dose regimen of 50 mg, 1 time/day) Age cmax (µg/ml) auctau (µg.

12 to 17 years old (n = 62) 6,80 (6,17; 7,50) 103 (91,1; 116) (9,42; 11,2) 153 (137; 170) 1 to 5 years old (n = 38) (10,4; 12,9) 162 (139; 187) AUC (0-τ) and CMAX are based on the estimation of population pharmacokinetics.

Sadurunge njupuk Revolade 25mg Novartis anti-bleeding amarga trombosit ing getih (28 tablet)

How to use Revolade drugs used oral, should take pills at least 2 hours before or 4 hours after using any product such as antacids, dairy products (or other calcium -containing foods), or additional minerals containing multi -chemotherapy (for example, iron, calcium, magnesi, aluminum, aluminum and zinc). Instructions for use, processing and cancellation: There is no special requirement on drug treatment after use. Dosage Eltrombopag treatment should be started and maintained under the supervision of a doctor who has experience in the treatment of hematology and its complications. The requirements of the dose of Eltrombopag must depend on the patient based on the number of platelets of the patient. The goal of Eltrombopag treatment is not normalization of platelets. Oral mixture can lead to higher Eltrombopag levels than the tablet formula (see the pharmacokinetic properties). When converting between the tablet formula and the oral mixture, should monitor the number of platelets weekly for 2 weeks. immune platelets (Nguyen Phat) Should use the lowest dose of Eltrombopag to achieve and maintain platelets ≥ 50,000/µl. Adjust the dose based on platelet quantity response. Do not use Eltrombopag to normalize the number of platelets. In clinical studies, the number of platelets usually increases within 1 to 2 weeks after starting to use Eltrombopag and decreases within 1 to 2 weeks after stopping treatment. Group of adults and children from 6 to 17 years old: Eltrombopag's recommended starting dose is 50 mg once a day. For patients with Asian origin (such as Chinese, Japan, Taiwan, South Korea or Thailand), it is advisable to start using Eltrombopag at a decrease of 25 mg once daily (see the pharmacokinetic characteristics). Group of children from 1 to 5 years old: Eltrombopag's recommended starting dose is 25 mg once daily. Monitor and adjust the dose: After starting to use Eltrombopag, the dose must be adjusted to achieve and maintain the number of platelets ≥ 50,000/µl when necessary to reduce the risk of bleeding. Do not exceed the dose of 75 mg/day. Should regularly monitor clinical tests on hematology and liver during the Eltrombopag treatment process and the dose regimen of Eltrombopag are adjusted based on the number of platelets as stated in Table 3. week). After that, every month should evaluate the total blood formula including the number of platelets and peripheral blood spread. Table 3. Adjust the dose of Eltrombopag in patients with immune platelets (ITP) The number of platelets adjust the dose or response 2 weeks of treatment increased by 25 mg of daily dose to maximum 75 mg/day. ≤ 150,000/µl Use the lowest dosage of Eltrombopag and/or immunomemosis treatment at the same time to maintain the number of platelets to avoid or reduce bleeding. ≤ 250,000/µl Discount 25 mg of daily dose. Wait 2 weeks to evaluate the effectiveness of this dose and any next dose adjustment. Increase the frequency of platelet tracking 2 times/week. When platelet quantity ≤ 100,000/µl, start treatment with daily dose decreased by 25 mg. ♦ For patients who use 25 mg of Eltrombopag 1 time a day, should consider taking a dose of 25 mg, 1 time every two days. can be used Eltrombopag along with other immune platelet treatment drugs. The dose regimen of the drugs should be adjusted at the same time, when appropriate medical, to avoid increasing the number of platelets excessive during Eltrombopag treatment. It is necessary to wait at least 2 weeks to see the effect of any dose adjustments to the platelet response of the patient before considering other dose adjustments. Adjust the standard Eltrombopag dose, decrease or increase, will be 25 mg, 1 time/day. Stop treatment: Should stop treatment with Eltrombopag if the platelet number does not increase to sufficient to avoid serious bleeding clinically after 4 weeks of Eltrombopag treatment at a dose of 75 mg, 1 time/day. Patients should be clinically assessed periodically and the continued treatment should be decided by the doctor on the basis of each patient. In patients who have not cut spleen, should include assessments related to spleen cutting. A platelet reduction may occur during treatment. Severe property anemia: Starting dose mode: Should start using Eltrombopag at a dose of 50 mg once a day. For patients with Asian origin, Eltrombopag should be started at a reduction of 25 mg once daily (see pharmacokinetic properties). Do not start treatment when the patient has abnormalities in cell genetics of chromosomes No. 7. Monitor and adjust the dose: Hematology responds requires a dose titration, usually up to 150 mg and may take up to 16 weeks after starting using Eltrombopag (see clinical research section). Eltrombopag dose should be adjusted by an increase of 50 mg every 2 weeks when necessary to achieve the target number of platelets ≥ 50,000/µl. For patients using 25 mg, 1 time/day, the dose should be increased to 50 mg/day before increasing the dose of 50 mg. Do not exceed the dose of 150 mg/day. Should regularly monitor clinical and liver clinical tests during the Eltrombopag treatment process and adjust the dose regimen of Eltrombopag based on platelet quantities as stated in Table 4. Table 4: Adjust the dose of Eltrombopag in patients with severe property anemia

The number of platelets adjust the dose or response For patients taking 25 mg once daily, increasing the dose to 50 mg daily before increasing the dose of 50 mg. ≥ 50,000/µl to ≤ 150,000/µl use the lowest dosage of Eltrombopag to maintain platelet quantities. Wait 2 weeks to evaluate the effectiveness and any subsequent dose adjustment. At least 1 week. When platelet quantity ≤ 100,000/µl, start treatment with daily dose decreased by 50 mg. For patients who achieve 3 lines, including regardless of blood transfusion, lasting for at least 8 weeks: Eltrombopag dose can be reduced by 50%. If the number is still stable after 8 weeks with a decrease in doses, stop using Eltrombopag and monitor blood formula. If the number of platelets drops to

Efek sisih

Safety Revolade wis dievaluasi nggunakake double blind, re control studies karo plasebo, tra100773A lan B, tra102537 (Raise) lan tra113765, sing 403 pasien nggunakake Revolade lan 179 pasien sing nggunakake plasebo, saliyane data saka studi open-labeled, rampung yaiku tra108053 lan tra108057. trau11240. Pasien sing wis ngombe obat nganti 8 taun (ing riset ekstensif). Reaksi salabetipun serius sing paling penting yaiku keracunan ati lan trombosis/trombosis. Reaksi salabetipun paling umum dumadi ing paling ora 10% pasien kalebu mual, diare lan tambah alanine aminotransferase.

Keamanan Revolade ing pasien bocah-bocah (saka 1 nganti 17 taun) sadurunge wis diobati karo trombosit kekebalan sing wis dibuktekake ing rong studi. Petit2 (tra115450) punika 2 -part, pindho wuta, mbukak, acak, kontrol label karo plasebo. Patients dibagi kanthi acak 2: 1 lan nggunakake Revolade (n = 63) utawa plasebo (n = 29) nganti 13 minggu ing tataran acak sinau. Petit (tra108062) minangka studi 3-bagean, staggered, open-label, pindho, acak, label kontrol karo plasebo. Pasien dibagi kanthi acak 2: 1 lan nggunakake Revolade (n = 44) utawa plasebo (n = 21) nganti 7 minggu. Cathetan reaksi salabetipun padha karo cathetan reaksi sing ditemoni ing wong diwasa kanthi sawetara reaksi saleh tambahan, ditandhani ♦. Reaksi salabetipun sing paling umum ing bocah-bocah saka umur 1 taun lan luwih dikurangi dadi trombosit kekebalan (≥ 3% lan luwih gedhe tinimbang plasebo) yaiku infeksi saluran napas ndhuwur, nasofaringitis, watuk, mriyang, nyeri weteng, nyeri cangkem - tenggorokan, lara untu lan irung meler.

anemia proliferasi abot ing pasien diwasa:

Keamanan Eltrombopag ing anemia proletar abot wis dievaluasi ing studi klompok siji, mbukak longan (n = 43) sing 11 pasien (26%) diobati> 6 sasi lan 7 pasien (21%) sing diobati> 1 taun. Reaksi salabetipun serius sing paling penting yaiku neutropenia kanthi demam lan bakteri / infeksi. Reaksi salabetipun paling umum dumadi ing paling ora 10% pasien kalebu sirah, pusing, watuk, nyeri tutuk lan tenggorokan, mual, diare, nyeri abdomen, hiperpentine, nyeri sendi, nyeri ing anggota awak, lemes lan mriyang.

Dhaptar reaksi salabetipun:

Reaksi tetanèn ing studi babagan trombosit imun ing wong diwasa (n = 763), studi babagan pengurangan trombosit kekebalan ing bocah-bocah (n = 171), studi babagan medali emas (n = 1,520), studi babagan anemia hyperplasher abot (SAA) (n = 43) lan laporan sawise -sales kapacak ing ngisor iki dening klompok MEDDRA lan frekuensi. Ing saben sistem organ, reaksi salabetipun obat kasebut diatur kanthi frekuensi, pisanan reaksi sing paling umum. Klasifikasi frekuensi sing cocog kanggo saben reaksi obat sing saleh saka obat kasebut adhedhasar konvensi ing ngisor iki (Cioms III): Umum banget (≥ 1/10); Umum (≥ 1/100 nganti

Klompok pasien penurunan trombosit imun (ITP)

Infeksi lan parasit

Umum banget: Nasomitis ♦, infeksi saluran napas ndhuwur ♦.

Jarang: Kanker Rektum Rektum.

Kelainan getih lan sistem limfatik

Umum: Anemia, sel Eosin kaya eosin, leukemia, trombosit, hemoglobin mudhun, jumlah sel getih putih suda.

Jarang: Hipersensitivitas.

Umum: Ngurangi Hemoto, nyuda napsu, hiperurisemia.

Umum: Gangguan turu, depresi.

Umum: Persepsi, perasaan, rasa ngantuk, migren (Migrain).

Umum: mripat garing, sesanti burem, nyeri mripat, mundhut sesanti.

Umum: Sakit kuping, pusing.

Gangguan jantung

Kurang: tachycardia, infark miokard akut, kelainan kardiovaskular, biru ungu, sinus tachycardia, interval QT jangka panjang ing tengah tengah.

Umum: trombosis vena jero, hematoma, kobong panas.

Umum banget: Ho ♦.

Umum: tutuk - tenggorokan, irung meler ♦.

Umum banget: mual, diare ♦. tutuk.

Gangguan ati

Umum banget: Tambah alanin aminotransferase †.

Umum: ruam, rambut rontog, tambah kringet, gatal-gatal ing awak, bintik hemoragik

Umum: nyeri otot, kram otot, nyeri muskuloskeletal, nyeri balung, nyeri punggung.

Umum: proteinuria, hypertreatinine, thrombosis microchun karo gagal ginjel ‡.

Umum: Menstruasi.

Umum: Demam*, nyeri dada, kelemahane; * Umum banget ing trombosit kekebalan (ITP) ing bocah-bocah.

Umum: tambah alkali fosfatase ing getih.

Jarang: Sunburn.

†: Tambah alanine aminotransferase lan aspartate aminotransferase bisa kedadeyan bebarengan, sanajan ing frekuensi sing luwih murah.

‡: Istilah iki digabungake karo istilah prioritas kalebu karusakan ginjel akut lan gagal ginjel.

Klompok pasien sing sinau anemia abadi abot (SAA)

Gangguan getih lan sistem limfatik

Umum: Leukemia netral, infark limpa.

Umum: kakehan zat besi, nyuda napsu, hipoglikemia, nambah napsu.

Gangguan mental

Umum: kuatir, depresi.

Gangguan sistem saraf

Umum banget: sirah, pusing.

Umum: mata garing, katarak, jaundice ing mripat, sesanti burem, gangguan sesanti, fenomena mabur.

Umum banget: watuk, lara tutuk - tenggorokan, irung meler.

Umume: mimisan.

Umume banget: diare, mual, getihen untu, nyeri weteng.

Umum banget: nambah transaminase. Kasus karusakan ati amarga obat-obatan wis dilaporake ing pasien sing kena infeksi immunominals (ITP) lan hepatitis C (HCV).

Umum: Bintik-bintik getih, ruam, gatal, urtikaria, karusakan kulit, ruam inlaid.

Umum banget: nyeri sendi, nyeri ing perangan awak, kejang otot.

Umum: nyeri punggung, nyeri otot, nyeri balung.

Umum: Urine duwe warna ora normal.

Umum banget: lemes, mriyang, hawa adhem

Umum: tambah creatine phosphokinase ing getih.

Pènget

Sadurunge nggunakake obat sampeyan kudu maca instruksi kasebut kanthi teliti lan deleng informasi ing ngisor iki.

contraindicated

Obat Revolade contraindicated ing kasus ing ngisor iki:

Contraindicated kanggo pasien kanthi hipersensitifitas marang Eltrombopag utawa bahan bantu obat kasebut.

Ati-ati nalika nggunakake

Risiko keracunan kanggo ati

Panganggone Eltrombopag bisa nyebabake kelainan fungsi ati lan keracunan kanggo ati abot, ngancam nyawa (deleng reaksi salabetipun). Konsentrasi alanine aminotransferase (ALT) kudu diukur, aspartate aminotrasferase (AST) lan bilirubin serum sadurunge miwiti nggunakake eltrombopag, saben 2 minggu ing fase penyesuaian dosis lan saben wulan sawise dosis stabil wis ditemtokake. Eltrombopag nyegah UGT1A1 lan OATP1B1, sing bisa nyebabake bilirubin getih ora langsung.

Yen konsentrasi bilirubin mundhak, luwih becik nindakake bagean. Sampeyan kudu ngevaluasi tes serum kanggo fungsi ati sing ora normal kanthi mbaleni tes sajrone 3 nganti 5 dina. Yen kelainan diidentifikasi, tes serum kudu dipantau nganti ora normal pulih, stabil utawa bali menyang tingkat wiwitan. Eltrombopag kudu mandheg yen konsentrasi ALT mundhak (≥ 3 kaping wates ndhuwur tingkat normal [X ULN] ing pasien kanthi fungsi ati normal, utawa ≥ 3 kaping tingkat awal utawa> 5 kaping ULN, tingkat ngisor, ing pasien kanthi transaminase mundhak sadurunge perawatan) lan:

kemajuan, utawa

terus-terusan ≥ 4 minggu, utawa

kanthi bilirubin langsung, utawa

kanthi gejala klinis karusakan ati utawa bukti mundhut ati.

Ati-ati nalika njupuk eltrombopag kanggo pasien sing nandhang penyakit ati. Ing pasien kanthi hemorrhage immunominal (spontan) (ITP) lan anemia properti abot (SAA), dosis Eltrombopag kudu diwiwiti luwih murah. Perlu ngawasi kanthi rapet nalika digunakake kanggo pasien sing gagal ati (ndeleng dosis lan panggunaan).

komplikasi trombosis/trombolitik

Resiko trombosis (TEE) ditemokake mundhak ing pasien sing nandhang penyakit ati kronis (CLD) sing diobati karo 75 mg Eltrombopag sapisan dina sajrone 2 minggu kanggo nyiapake prosedur invasif. 6 saka 143 (4%) pasien diwasa kanthi Tee Tee nggunakake Eltrombopag (kabeh vena lawang) lan 2 saka 145 (1%) pasien ing klompok plasebo karo Tee (pasien ing sistem vena portal lan pasien infark miokard). 5 saka 6 pasien sing diobati karo Eltrombopag nandhang trombosis kanthi trombosit> 200.000 / µl lan sajrone 30 dina saka dosis terakhir Eltrombopag. Eltrombopag ora dituduhake kanggo thrombocytopenia ing pasien karo penyakit ati kronis kanggo nyiapake prosedur invasif.

Ing studi klinis karo Eltrombopag babagan trombositopen sing nyuda kekebalan (spontan) (ITP) (ITP), kedadeyan embolisasi trombotik wis diamati ing trombosit sing kurang lan normal. Ati-ati kudu ati-ati nalika nggunakake eltrombopag kanggo pasien sing duwe faktor risiko trombosis sing dikenal kalebu nanging ora winates ing faktor risiko genetik (umpamane, faktor V Leiden) utawa dipikolehi (contone, kekurangan antithrombin III (ATIII), sindrom fosfolipid), umur dhuwur, pasien kanthi tahap dinamis sing dawa, ganas lan ganas, Seni / ciloko, obesitas. Perlu ngawasi kanthi rapet jumlah trombosit lan nimbang nyuda dosis utawa mungkasi perawatan karo Eltrombopag yen jumlah trombosit ngluwihi level target (ndeleng dosis lan panggunaan).

Perlu ditimbang kanggo ngimbangi keuntungan-manfaat mekanis ing pasien kanthi risiko trombosis (TEE) amarga ana sebab apa wae. Ora ana kasus yen tee wis dideteksi saka riset klinis kanggo resistensi kanggo perawatan, nanging ora bisa ngilangi risiko kedadeyan kasebut ing klompok pasien iki amarga mbatesi jumlah pasien sing katon. Amarga dosis paling dhuwur diijini dituduhake kanggo pasien SAA (150 mg / dina) lan amarga sifat reaksi kasebut, TEES samesthine bakal kedadeyan ing klompok pasien iki.

Aja nggunakake eltrombopag ing pasien karo komite hemorrhage sing nyuda kekebalan (spontan) (ITP) kanthi gagal ati (Anak-Pugh ≥ 5 luwih dhuwur tinimbang keuntungan sing dikarepake. Nalika perawatan dianggep cocok, sampeyan kudu ati-ati nalika nggunakake Eltrombopag kanggo pasien sing gagal ati (ndeleng dosis lan cara nggunakake lan reaksi salabetipun).

getihen sawise mungkasi perawatan karo eltrombopag

Trombosit bisa kedadeyan maneh ing pasien kanthi hemorrhage kurang kekebalan (spontan) (ITP) sawise mungkasi perawatan karo Eltrombopag. Sawise mandheg nggunakake Eltrombopag, jumlah trombosit bali menyang tingkat asli sajrone 2 minggu ing umume pasien nambah risiko pendarahan lan ing sawetara kasus bisa nyebabake getihen. Risiko iki mundhak yen mandheg ngobati karo Eltrombopag nalika ana antikoagulan utawa anti-platelet. Disaranake yen sampeyan mungkasi perawatan karo Eltrombopag, miwiti perawatan imunosupresan (spontan) miturut pandhuan perawatan saiki. Perawatan medis tambahan bisa uga kalebu mungkasi perawatan karo obat antikoagulan lan/utawa obat anti-koleksi plateletik, pembalikan antikoagulan, utawa dhukungan trombosit. Kudu ngawasi jumlah trombosit saben minggu sajrone 4 minggu sawise mungkasi perawatan karo Eltrombopag.

Pembentukan retikulin sumsum balung lan risiko fibrosis balung

Eltrombopag bisa nambah risiko wutah utawa kemajuan serat reticulin ing sumsum balung. Makna temuan iki, uga karo reseptor Thrombopoietin liyane (TPO-R), durung ditemtokake.

Sadurunge miwiti perawatan karo Eltrombopag, perlu mriksa tes kaca getih perifer kanthi ketat kanggo nemtokake tingkat awal kelainan ing morfologi sel. Sawise nemtokake dosis stabil Eltrombopag, tes rumus getih total kudu ditindakake kanthi jumlah sel getih putih (WBC) saben wulan. Yen pengamatan diamati yen sel diwasa utawa sel dysplasia diamati, perlu kanggo mriksa tes pendarahan perifer kanggo morfologi anyar utawa luwih elek (contone, sel getih abang sing dibentuk ing banyu lan sel getih abang kanthi inti, leukosit diwasa) utawa ngurangi sel getih. Yen pasien ngalami morfologi anyar utawa luwih abot utawa luwih abot utawa ngurangi sel getih, Eltrombopag kudu dihentikan lan kudu dianggep biopsi sumsum balung, kalebu pewarnaan kanggo fibrosis.

Kemajuan sindrom displasia sumsum (MDS) sing ana

Ana keprihatinan teoritis yen pemilik TPO-R bisa ngrangsang progresi tumor ganas saka hematologi sing ana kayata sindrom displasma sumsum. Isomer TPO-R minangka faktor pertumbuhan sing nyebabake ekspansi sel prekursor kanggo nggawe trombosit, diferensiasi lan produksi trombosit. TPO-R diwujudake utamane ing permukaan sel saluran akar. Ing studi klinis kanthi isomer TPO-R ing pasien sindrom displasia sumsum (MDS), kasus paningkatan sementara ing jumlah sel lan kasus kemajuan MDS menyang leukemia sumsum akut (AML) wis dilaporake. Diagnosis perdarahan kekebalan (spontan) (ITP) (ITP) (ITP) (SAA) ing pasien diwasa lan wong tuwa kudu ditemtokake kanthi ngilangi entitas klinis liyane sing nuduhake tanda-tanda pengurangan trombosit, utamane diagnosis sindrom displasia meduler.

Perlu kanggo nimbang implementasine nyedhot sumsum balung lan biopsi ing proses penyakit lan perawatan, utamane ing pasien sing umure luwih saka 60 taun - wong kanthi gejala sistemik utawa pratandha abnormal kayata tambah getih perifer. Efisiensi lan safety Revolade durung ditemtokake kanggo ngobati trombositopenia amarga sindrom myeloma. Revolade ora bisa digunakake minangka tambahan kanggo studi klinis kanggo trombositopenia amarga sindrom dysplasma sumsum.

Abnormalitas genetik sel lan kemajuan menyang sindrom myeloma (MDS)/Leukemia sumsum akut (AML) ing pasien anemia properti abot (SAA).

Abnormalitas genetik sel dikenal dumadi ing pasien anemia properti abot (SAA). Ora jelas apa Eltrombopag bakal nambah risiko genetika sel ing pasien kanthi anemia properti sing abot. Ing fase-phase studi klinis babagan anemia anti-properti sing abot karo Eltrombopag kanthi dosis wiwitan 50 mg / dina (tambah saben 2 minggu nganti 150 mg / dina) (ELT112523), tingkat kelainan anyar ing genetika sel diamati ing 17,1% pasien diwasa [7/41 (4 sing duwe infeksi rantai 7)]. Wektu tengah nalika sinau nganti abnormal genetis sel yaiku 2,9 sasi.

Ing fase-phase studi klinis anemia anti-dinamis abot karo Eltrombopag ing dosis 150 mg / dina (kanthi owah-owahan ras utawa umur minangka nyatakake) (ELT116826), tingkat anyar cytotromas abnormal diamati ing 22,6% pasien diwasa [7/31 (kang 3 pasien duwe owah-owahan ing kromosom 7)]. Kabeh pasien 7 duwe sistem sitotoksik normal ing wiwitan. Enem pasien kanthi kelainan sitotoksik ing sasi kaping 3 nalika njupuk Eltrombopag lan pasien sing ora normal cytotromagnines ing sasi kaping 6.

Ing studi klinis karo Eltrombopag ing anemia prolaps abot, 4% pasien (5/133) didiagnosis sindrom displasma sumsum. Wektu rata-rata nganti diagnosis yaiku 3 wulan saka wiwitan perawatan Eltrombopag. Kanggo pasien sing ngalami perawatan anemia anti-properti sing abot karo terapi imunosupresif sadurunge, utawa perawatan sing kuat karo terapi imunosupresif, dianjurake kanggo mriksa sumsum balung kanthi nyedhot sumsum balung kanggo tes cytopenic sadurunge miwiti nggunakake Eltrombopag, ing 3 sasi perawatan lan 6 sasi sabanjure. Yen dideteksi kelainan anyar ing genetika sel, perlu kanggo ngevaluasi yen terus nggunakake Eltrombopag cocok utawa ora.

Owah-owahan visual

Katarak sing diamati ditemokake ing studi babagan keracunan Eltrombopag ing rodents (pirsani bagean data safety non-klinis). Ing studi kontrol ing pasien sing kena infeksi virus hepatitis C, trombositopenia sing diobati karo interferon (n = 1,439), kemajuan katarak asli kasedhiya utawa kedadeyan katarak ing klompok Eltrombopag 8% lan ing klompok plasebo yaiku 5%. Kasus pendarahan retina, biasane ing 1 utawa 2, wis dicathet ing pasien sing kena infeksi virus hepatitis C nggunakake Interferon, Ribavirin lan Eltrombopag (2% ing Eltrombopag lan 2% ing klompok plasebo). Pendarahan dumadi ing permukaan retina (preretinal), ing ngisor retina (sbretinal), utawa ing jaringan retina. Dianjurake kanggo ngawasi mata pasien.

ngluwihi kisaran QT/QT (QTC)

Sinau babagan QTC babagan sukarelawan sehat sing njupuk dosis 150 mg Eltrombopag saben dina ora nuduhake signifikansi klinis kanggo kutub jantung. Ekstensi QTC wis dilapurake ing studi klinis ing pasien kanthi pendarahan imunosupresif (spontan) (ITP). Pentinge klinis saka QTC iki ora dingerteni.

ilang kanggo nanggepi Eltrombopag

Kekirangan saka respon utawa non-maintenance minangka respon platelet kanggo perawatan Eltrombopag ing dosis sing disaranake kudu ningkatake panyebabe, kalebu reticulin sumsum balung.

Klompok pasien bocah

Peringatan lan ati-ati ing ndhuwur babagan trombositopenik (spontan) (ITP) sing nyuda kekebalan uga ditrapake kanggo klompok pasien bocah.

mengaruhi tes laboratorium

Eltrombopag dicelup kanthi dhuwur lan mulane nduweni kemampuan kanggo mengaruhi sawetara tes laboratorium. Perubahan warna serum lan pengaruh ing tes total bilirubin lan bun wis dilaporake ing pasien nggunakake Revolade. Yen asil observasi laboratorium lan klinis ora konsisten, tes kanthi cara liya bisa mbantu nemtokake validitas asil kasebut.

Gunakake obat kanggo wanita nalika meteng lan lactation

Wanita ngandhut:

Ora ana data utawa data sing diwatesi babagan panggunaan eltrombopag ing wanita ngandhut. Pasinaon kewan nuduhake keracunan kanggo reproduksi. Resiko sing ora dingerteni kanggo wong.

Aja nyaranake nggunakake Revolade nalika meteng.

Wanita bisa ngandhut, kontrasepsi ing lanang lan wadon:

Ora dianjurake kanggo nggunakake Revolade ing wanita sing cenderung ora nggunakake kontrasepsi.

wanita sing nyusoni:

Ora cetha apa Eltrombopag/metabolit bakal diekskripsikake menyang ASI. Pasinaon kewan nuduhake yen Eltrombopag bisa disekresi menyang susu (pirsani data safety non-klinis); Mulane, ora bisa ngilangi risiko nyusoni. Sampeyan kudu mutusake apa arep mandheg nyusoni utawa nerusake / nyingkiri perawatan karo Revolade, kanthi nggatekake keuntungan nyusoni lan mupangat kanggo nambani wanita.

Reproduksi:

Kemampuan kanggo ngasilake tikus lanang utawa wadon ora kena pengaruh ing tingkat pajanan sing padha karo tingkat pajanan ing manungsa. Nanging, ora bisa ngilangi risiko kanggo wong (ndeleng data keamanan non-klinis).

Efek obat kasebut ing nyopir lan ngoperasikake mesin

Interaksi obat

Efek Eltrombopag ing obat liya:

Inhibitor HMG Reduktase HMG:

Gunakake Eltrombopag 75 mg, 1 wektu / dina suwene 5 dina kanthi dosis siji 10 mg rosuvastatin minangka substrat OATP1B1 (Polypeptide ngirim anion organik - Polipeptida Pengangkut Anion Organik, OATP) lan BCRP (Protein Tahan Kanker Payudara) kanggo 39 Healthy Healthy Health of Rosu(3%). 90%: 82%, 126%) lan AUC (wilayah ing sangisore kurva) 0-∞ 55% (90%rentang sing bisa dipercaya: 42%, 69%). Interaksi uga samesthine karo inhibitor HMG-COA Reductase liyane, kalebu Atorvastatin, Fluvastatin, Lovastatin, Pravastatin lan Simvastatin. Nalika digunakake bebarengan karo Eltrombopag, disaranake kanggo nyuda dosis statin lan ngawasi kanthi ati-ati reaksi salabetipun statin (deleng sipat farmakokinetik).

substrat OATP1B1 lan BCRP:

Ati-ati nalika nggunakake Eltrombopag lan substrat OATP1B1 (contone, methotrexate) lan BCRP (contone, Topotecan lan Methotrexate) (ndeleng sifat farmakokinetik).

Substrat sitokrom p450:

Ing panliten nggunakake mikrosom ati manungsa, Eltrombopag (nganti 100 μm) nuduhake yen ora ana inhibitor enzim in vitro CYP450 1A2, 2A6, 2C19, 2D6, 2E1, 3A4/5, lan 4A9/11 lan CYP2C8 lan CYP2C9/11 minangka inhibitor CYP2C8 lan CYP2clita. Eksplorasi. Gunakake Eltrombopag 75 mg, 1 wektu / dina kanggo 7 dina kanggo 24 wong sehat sing ora nyandhet utawa ngindhuksi metabolisme polutan kanggo 1A2 (kafein), 2C19 (omeprazole), 2C9 (Flurbipfen) utawa 3A4 (Midazolam) ing manungsa. Ora ana interaksi klinis sing dikarepake nalika Eltrombopag lan substrate CYP450 digunakake bebarengan (deleng karakteristik farmakokinetik).

Inhibitor Protease HCV:

Ora ana pangaturan dosis nalika nggunakake Eltrombopag karo Telaprevir utawa Boceprevir. Dosis tunggal Eltrombopag 200 mg karo Telaprevir 750 mg saben 8 jam ora ngganti konsentrasi Telaprevir ing plasma.

Njupuk dosis siji Eltrombopag 200 mg bebarengan karo BoCeprevir 800 mg saben 8 jam ora ngganti AUC (0-τ) BoCeprevir ing plasma nanging nambah cmax nganti 20%, lan nyuda cmin (konsentrasi plasma paling murah) 32%. Pentinge klinis ngurangi cmin durung ditemtokake, dianjurake kanggo ngawasi klinis lan nguji inhibitor emas.

Efek obat liya ing Eltrombopag:

siklosporin:

Ngurangi konsentrasi Eltrombopag wis diamati nalika digunakake bebarengan karo 200 mg lan 600 mg Ciclosporin (inhibitor BCRP (protein anti kanker payudara) Ciclosporin nyuda CMAX saka Eltrombopag 39% lan nyuda Aucinf saka Eltrombopag 24%. Eltrombopag karo cyclosporin bisa ditambahake adhedhasar trombosit kasebut.

Kation multi-kimia (kelat):

eltrombopag chelate kanthi kation polimerisasi kayata wesi, kalsium, magnesium, aluminium, selenium lan seng. Gunakake dosis siji Eltrombopag 75 mg karo antacid sing ngemot kation multi-kemoterapi (1524 mg aluminium hidroksida lan 1425 mg Magnesi karbonat) nyuda AUC0-∞ saka Eltrombopag ing plasma 70% (90% linuwih: 64%, 76%) lan nyuda CMTROX ing plasma 907% 76%).

Sampeyan kudu nggunakake Eltrombopag paling sethithik 2 jam sadurunge utawa 4 jam sawise nggunakake produk apa wae kayata antacid, produk susu, utawa suplemen mineral sing ngemot kation sinema supaya ora nyuda penyerapan Eltrombopag kanthi signifikan amarga kimia chelate (deleng bagean dosis lan panggunaan lan sifat farmakokinetik).

lopinavir/ritonavir:

Panggunaan Eltrombopag bebarengan karo Lopinavir/Ritonavir bisa nyuda tingkat Eltrombopag. Panaliten ing 40 sukarelawan sehat nuduhake yen panggunaan simultan saka dosis siji Eltrombopag 100 mg kanthi dosis bola-bali Lopinavir / Ritonavir 400/100 mg, 2 kali / dina nyebabake nyuda AucinF Eltrombopag ing plasma 17% (90% kisaran keandalan: 6,6%, 26%). Mula, ati-ati nalika nggunakake Eltrombopag karo Lopinavir/Ritonavir.

Kudu ngawasi kanthi teliti jumlah trombosit kanggo mesthekake manajemen medis sing cocok kanggo dosis Eltrombopag nalika miwiti utawa mungkasi perawatan karo Lopinavir/Ritonavir. CYP1A2 lan CYP2C8: Eltrombopag dimetabolisme liwat akeh dalan kalebu CYP1A2, CYP2C8, UGT1A1, lan UGT1A3 (pirsani karakteristik farmakokinetik). Inhibitor utawa induksi enzim sing ora mesthi mengaruhi konsentrasi eler ing plasma kanthi signifikan, dene inhibitor utawa induksi pirang-pirang enzim bisa nambah konsentrasi Eltrombopag (contone Fluvoxamine) utawa nyuda tingkat Eltrombopag (contone Rifampicin).

Inhibitor Protease HCV:

Asil panaliten interaktif farmakokinetik (PK) nuduhake yen panggunaan BoCeprevir 800 mg bebarengan saben 8 jam utawa Telaprevir 750 mg saben 8 jam kanthi dosis tunggal Eltrombopag 200 mg ora ngganti tingkat Eltrombopag ing plasma kanthi signifikan klinis.

Trombosit imunologis (ITP):

Obat-obatan sing digunakake ing perawatan ngurangi kekebalan kanthi kombinasi karo Eltrombopag ing studi klinis kalebu kortikosteroid, danazol, lan/utawa azathioprine, immunoglobulin (imunoglobulin) intravena (IVIG), lan Anti-D Immunoglobulin. Sampeyan kudu ngawasi jumlah trombosit nalika nggabungake eltrombopag karo obat liya ing perawatan trombosit kekebalan kanggo ngindhari jumlah trombosit ing njaba ruang lingkup sing disaranake (ndeleng dosis lan cara nggunakake).

Interaksi karo panganan:

Gunakake tablet utawa wêdakakêna Eltrombopag kanthi dhaharan multi-kalsium (contone, dhaharan produk susu) kanthi signifikan nyuda AUC0 -∞ lan CMtrombopag ing plasma. Kontras, nggunakake Eltrombopag 2 jam kepungkur utawa 4 jam sawise mangan kanthi akeh kalsium utawa panganan sing kurang kalsium [

Panganan kanthi kandungan kalsium sing sithik ( Kavaleri:

Amarga ora ana studi babagan korélasi obat kasebut, mula ora nyampur obat iki karo obat liya.

Panyimpenan

Ninggalake papan sing adhem, aja nganti cahya, suhu ngisor 30⁰C.

Obat liyane

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