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  • Eliquis (Apixaban) tablets 5mg 20 tablets, 2.5mg 20 tablets, 5mg 60 tablets, 2.5mg 60 tablets, Eliquis (Apixaban) tablets 5mg 20 tablets, 2.5mg 20 tablets, 5mg 60 tablets, 2.5mg 60 tablets,

Eliquis (Apixaban) tablets 5mg 20 tablets, 2.5mg 20 tablets, 5mg 60 tablets, 2.5mg 60 tablets,

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Eliquis (Apixaban) tablets Anti-coagulants 5mg 20 tablets, 2.5mg 20 tablets, 5mg 60 tablets, 2.5mg 60 tablets,

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Clinico-pharmacological group

(The anticoagulant of direct action – a selective inhibitor of factor Xa)

Release form, composition and packaging

Tablets, film-coated yellow color, round, lenticular, with engraving “893” on one side and “2 1/2” on the other.

Excipients: lactose – 50.25 mg, microcrystalline cellulose – 41 mg croscarmellose sodium – 4 mg, sodium lauryl sulfate – 1 mg, magnesium stearate – 1.25 mg.

The composition of the film shell: Opadry II Yellow 4.0 mg (гипромеллоза15 cps1,48 mg of lactose monohydrate 1.24 mg titanium dioxide 0.8 mg, triacetin 0,32 mg, dye iron oxide yellow 0,16 mg)

10 PCs. – blisters (1) – packs of cardboard.

10 PCs. – blisters (2) – packs of cardboard.

10 PCs. – blisters (6) – packs cardboard.

10 PCs. – blisters (10) – packs of cardboard.

Pharmacological action

The anticoagulant of direct action – a selective inhibitor of factor Xa of blood coagulation.The mechanism of action of apixaban to inhibit the activity of FXa. As a result, apixaban changes the values of indicators of blood coagulation system: prolongs the prothrombin time, MHO and activated partial thromboplastin time (APTT). Changes in these indicators when using the drug in a therapeutic dose is minor and individual. Therefore, their use to assess the pharmacodynamic activity of apixaban is not recommended.The inhibition of the FXa activity apixaban proved by using a chromogenic test using a Rotachrom heparin. The change in anti-FXa activity is directly proportional to the increase in the concentration of apixaban in plasma, with maximum activity observed at achievement of apixaban Cmax in blood plasma. A linear relationship between concentration and anti-FXa activity of apixaban recorded in a wide range of therapeutic doses of the drug. Changes in anti-FXa activity when changing the dose and concentration of apixaban more pronounced and less variable than indicators of blood coagulation. Expected minimum and maximum anti-FXa activity apixaban in equilibrium, when applied in a dose of 2.5 mg 2 times/day is 1.KITE/ml (5/95 percentile – 0.67 IU/ml – 2.4 IU/ml) and 0.84 IU/ml (5/95 percentile -0.37 IU/ml – 1.8 IU/ml), respectively, which correlates with variability in the interval between taking doses of the drug (less than 1.6 times). On the background of therapy with apixaban do not require routine monitoring of its concentration in the blood plasma, however the test anti-FXaа the effectiveness Rotachrom can be useful for making decisions about continuing therapy.Mechanism bastiaensen is a powerful direct inhibitor of FXa, reversible and selectively blocks the active site of the enzyme, intended for oral administration. For the implementation of the antithrombotic effect of apixaban not required the presence of antithrombin III. Apixaban inhibits free and bound FXa, and the activity of prothrombinase. Apixaban has no direct effect on platelet aggregation, but indirectly inhibits platelet aggregation, indutsirovannaya. By inhibiting the activity of FXa, apixaban prevents the formation of thrombin and blood clots.ФармакокинетикаВсасываниеАбсолютная the bioavailability of apixaban reaches 50% when applied in doses up to 10 mg. Apixaban is rapidly absorbed from the gastrointestinal tract, Cmax is achieved within 3-4 hours after oral administration. Food intake has no effect on the values of area under the curve “concentration-time” (AUC) or Cmax of apixaban. Apixaban pharmacokinetics for doses of up to 10mg is linear. When taking apixaban in doses above 25 mg marked limitation of drug absorption, which is accompanied by a decrease in its bioavailability. Metabolism of apixaban are characterized by low or moderate inter – and vnutricinovialnoe variability (the corresponding values of the coefficient of variation of 20% and 30%, respectively).Raspredelennye of apixaban with proteins of human blood plasma is approximately 87 %, the volume of distribution (Vss) is approximately 21 L. Metabolism and videnablyudenie 25% of the dose is excreted as metabolites, most of through the bowel. Renal excretion of apixaban approximately 27% of its total clearance.Total clearance of apixaban is approximately 3.3 l/hour, T1/2 about 12 hours Of o-demethylation and hydroxylation at the 3-oxopiperidine balance are the main pathways of biotransformation of apixaban. Apixaban mainly metabolized with the participation of isoenzyme CYP3A4/5, to a lesser extent of CYP1A2 isoenzymes, 2С8, 2C9, 2C19 and 2J2. Unmodified apixaban is the main substance circulating in the human blood plasma, the active circulating in blood metabolites are not available. In addition, apixaban is a substrate of transport proteins, P-glycoprotein 70 and protein resistance of breast cancer (BCRP).Dysfunction of pooncarie renal function has no effect on the Cmax of apixaban. However, there was a higher concentration of apixaban, korrelirovala with the degree of loss of kidney function, estimated by the values of creatinine clearance(CC). Patients with impaired kidney light (QC – 51 ml/min to 80 ml/min), medium (QC – 30 ml/min to 50 ml/min) and severe (CC – 15 ml/min to 29 ml/min), AUC values of apixaban in plasma was increased by 16%, 29% and 44%, respectively, compared with persons who had normal values of KK. The impairment of renal function did not exert obvious effects on the relationship between the concentration of apixaban in plasma and its anti-FXa activity.Research apixaban in patients with a creatinine clearance of <,, 15=”” p=””>,

The liver

Research apixaban in severe hepatic impairment or active pathology of the hepatobiliary system were not conducted.

In the study of the pharmacokinetics and pharmacodynamics of apixaban its single admission to the dose of 5 mg in patients with hepatic impairment mild and moderate severity (class A and b child-Pugh, respectively) and healthy volunteers has been shown that hepatic insufficiency has no effect on these parameters. Changes in anti-FXa activity and MHO patients with hepatic impairment moderate and healthy volunteers were comparable.

Use in elderly patients

At patients of elderly age (over 65 years) was observed higher values of drug concentration in the blood plasma than in younger patients: the mean value of the AUC were approximately 32% higher. Dose adjustment of the drug in elderly patients is not required.

Floor

The exposition of apixaban in women was 18% higher than that of men. Correction of the dose depending on patient gender is not required.

Race and ethnicity

The results obtained in the studies of the first phase, indicated the absence of significant differences in the pharmacokinetics of apixaban between representatives of Caucasoid, Mongoloid and Negroid races. The results of the analyses of the pharmacokinetics in different populations, performed the studies, which included patients treated with apixaban after elective hip or knee joint correspond to the results of studies of the first phase. Correction of the dose depending on the race or ethnicity of the patient is not required.

Body weight

In patients with body weight more than 120 kg apixaban concentration in plasma was approximately 30% lower than in patients with a body weight of 65 kg to 85 kg, patients weighing less than 50 kg, this figure was approximately 30% higher. Dose adjustment depending on the body mass of the patient is not required.

The dependence of the parameters of pharmacokinetics and pharmacodynamics

The dependence between the parameters of pharmacokinetics and pharmacodynamics (including anti-FXa activity, MHO, prothrombin time, APTT) of apixaban and its concentration in blood plasma have been studied for a wide range of doses (from 0.5 mg to 50 mg). It was shown that the relationship between the concentration of apixaban and the FXa activity is best described using a linear model. The dependence of the parameters of the pharmacokinetics and pharmacodynamics of apixaban estimated in patients undergoing planned hip or knee joint, consistent with such observed in healthy volunteers.

Dosage

Inside on 1 tab. (2.5 mg) 2 times/day regardless of food intake (first appointment within 12 -24 h after surgery).

In patients undergoing hip replacement surgery, the recommended duration of treatment is 32 to 38 days, the knee joint is 10 to 14 days.

In the case of pass receiving medication should be taken as soon as possible and to continue reception 2 times/day in accordance with a source schema.

In patients with impaired renal function mild, moderate or severe with a reduction in QC of up to 15 ml/min correction dose is not required. Data on the use of the drug in patients with KK<,, 15=”” b=””>, are missing. The use of the drug Eliquis in this category of patients is not recommended.

Use caution when taking the drug Liquidazione with hepatic impairment mild and moderate severity (grade A or b child-Pugh), thus dose adjustment is not required. The use of the drug in patients with severe hepatic impairment is not recommended.

Dose adjustment of the drug in elderly patients is not required.

Dose adjustment depending on the body mass of the patient is not required.

Correction of the dose depending on patient gender is not required.

Correction of the dose depending on the race or ethnicity of the patient is not required.

Overdose

The antidote is not known. In case of overdose increases the risk of bleeding. In the framework of controlled clinical studies apixaban taken orally to healthy volunteers in doses up to 50 mg/day for 3 to 7 days (25 mg, 2 times/day for 7 days or 50 mg 1 times/day for 3 days), 10 times higher than the maximum recommended human dose, clinically important adverse effects were not noted.

In case of overdose of this drug you can consider the use of activated carbon.

Drug interactions

The effect of other drugs on the pharmacokinetics of apixaban

Inhibitors of CYP3A4 and P-glycoprotein

The combination of apixaban with ketoconazole (dose 400 mg 1 times/day), a potent inhibitor of both CYP3A4 and P-glycoprotein, led to an increase in the average AUC values of apixaban 2 times and the average value of Cmax – 1.6 times. Dose adjustment of apixaban when it is combined with ketoconazole is not required, but apixaban should be used with caution in patients receiving systemic therapy asalouye antifungal agents, particularly ketoconazole or other potent inhibitors of CYP3A4 and P-glycoprotein.

Drugs moderately reduce the rate of excretion of apixaban or inhibiting the CYP3A4 and/or P-glycoprotein, is expected to lead to an increase in the concentration of apixaban in blood plasma, to a lesser extent. For example, diltiazem(a moderate inhibitor of CYP3A4 and a weak inhibitor of P-glycoprotein) in a dose of 360 mg 1 time/day, led to an increase in average AUC values of apixaban 1.4 times and the average values of Cmax – 1.3 times. Naproxen (inhibitor of P-glycoprotein) when used in a dose of 500 mg in healthy volunteers caused an increase in the average values of AUC and Cmax of apixaban in 1.5 and 1.6 times, respectively. It was noted the increase in the values of indicators of blood coagulation. However, against the background of this combination there was no effect of naproxen on platelet aggregation associated with a violation of arachidonic acid metabolism, and clinically significant lengthening of bleeding time.

Dose adjustment of apixaban in combination with moderate inhibitors of CYP3A4 and/or P-glycoprotein is not required.

Inducers of CYP3A4 and P-glycoprotein

The combination of apixaban with rifampicin (a potent inducer of CYP3A4 and P-glycoprotein) led to a decrease in the average values of AUC and Cmax of apixaban approximately 54% and 42%, respectively. Apparently, the combination of apixaban with other powerful inducers of CYP3A4 and P-glycoprotein (in particular, phenytoin, carbamazepine, phenobarbital or drugs St. John’s wort) may also lead to a decrease in the concentration of apixaban in blood plasma. Dose adjustment of apixaban when it is combined with the group is not required, however, to combine these tools with caution.

Anticoagulants, thrombocyte aggregation inhibitors and IPVP

After combined administration of enoxaparin (once daily, in the dose of 40 mg) and apixaban (once, at a dose of 5 mg) was observed an additive effect of these funds on the activity of FXa.

Signs of a pharmacokinetic or pharmacodynamic interaction of apixaban with acetylsalicylic acid (at a dose of 325 mg, 1 times/day) in healthy humans were observed.

Combining apixaban with clopidogrel (at a dose of 75 mg 1 times/day) or a combination of clopidogrel (75 mg) and acetylsalicylic acid (162 mg, 1 times/day) in phase I clinical studies do not lead to an increase in bleeding time, further inhibition of platelet aggregation or increase of indicators of blood coagulation system (prothrombin time, MHO, and APTT) compared to the use of these antiplatelet agents in monotherapy.

However, caution should be exercised with simultaneous use of apixaban with NSAIDs (including acetylsalicylic acid), due to the fact that these drugs increase the risk of bleeding.

It is not recommended to simultaneously apply medications, which may be associated with the development of serious bleeding, such as unfractionated heparin or derivatives of heparin (including low molecular weight heparins), oligosaccharides, inhibiting FXa(e.g., fondaparinux), direct thrombin II inhibitors (e.g., desirudin), tromboliticaskie drugs, the receptor antagonists to glycoprotein IIb/IIa, thienopyridine (e.g., clopidogrel), dipyridamole, dextran, sulfinpirazon, vitamin K antagonists and other anticoagulants. It should be noted that unfractionated heparin may be used in doses necessary to support the patency of venous or arterial catheter.

Combination with other drugs

No clinically significant pharmacokinetic or pharmacodynamic interaction of apixaban with atenolol or famotidine. Combining apixaban (at a dose of 10 mg) with atenolol (100 mg) did not lead to the development of clinically meaningful changes in pharmacokinetics parameters of apixaban, but it was accompanied by a decrease in average values of AUC and Cmax of apixaban 15% and 18%, respectively, compared to the monotherapy regime. The purpose of apixaban (at a dose of 10 mg) with famotidine (40 mg) did not affect the AUC or Cmax values of apixaban.

The influence of apixaban on the pharmacokinetics of other drugs

In studies in vitro apixaban not inhibited the activity of isoenzymes CYP1A2, CYP2A6, CYP2B6, CYP2C8, CYP2C9, CYP2D6 or CYP3A4 (inhibitory concentration (IC50) >,, 45 mmol/l); however, there is a weak suppression of the activity of the isoenzyme CYP2C19 (IC50 >, and 20 µmol/l) apixaban in concentrations much higher than the Cmax of the drug in the plasma during clinical use. Apixaban is not an inducer of isoenzymes CYP1A2, CYP2B6, CYP3A4/5 at concentrations up to 20 µmol/L. In this regard, it is expected that when used together, it will not affect the clearance of drugs metabolized by these isoenzymes. In addition, apixaban not inhibited to a significant extent the activity of P-glycoprotein.

In studies in healthy volunteers apixaban not changed to a large extent the pharmacokinetics of digoxin, naproxen, or atenolol.

Pregnancy and lactation

There are limited data on drug Eliquis during pregnancy. The use of apixaban during pregnancy is not recommended.

There is no information on the excretion of apixaban or its metabolites in breast milk in humans. If necessary, the drug Eliquis during lactation breastfeeding should be discontinued.

Side effects

Adverse reactions were observed in 11% of patients receiving apixaban at a dose of 2.5 mg 2 times/day. As with other anticoagulants, bleeding may occur in patients with risk factors, such as organic lesion assoc ated with the bleeding. The most frequent side effects were anemia, bleeding, bruising, nausea. Adverse reactions developed in patients undergoing orthopedic surgery, the therapy with apixaban presented below.

Further, under adverse reactions is understood: often – >,, 1/100, <,, 1=”” 10=”” -=””>,, 1/1000, <,, 1=”” 100=”” -=””>,, 1/10000, <,, 1=”” 1000=”” p=””>,

The blood and lymphatic system: often – anemia (including postoperative and hemorrhagic, accompanied by appropriate changes in the laboratory results), rarely – thrombocytopenia (reduction in platelets).

The immune system: rarely – hypersensitivity.

From the body of the vision: rarely – bleeding in the tissue of the eyeball (including hemorrhage into the conjunctiva).

Of the cardiovascular system: often-bleeding (including hematoma, and vaginal and urethral hemorrhage), infrequent – hypotension (including hypotension during the procedure).

The respiratory system: rare – nasal bleeding, and rarely hemoptysis.

From the digestive tract: often – nausea, infrequently – gastrointestinal bleeding (including vomiting with blood and melena), the presence of unaltered blood in the stool, rarely rectal bleeding, bleeding from the gums.

The liver and biliary tract: rarely – increased activity of transaminases (including increased ALT activity), increased activity of AST, gamma glutamyl transpeptidase, abnormal changes in liver function tests, increased activity of alkaline phosphatase in the blood, increasing the concentration of bilirubin in the blood.

From the side of musculoskeletal system: rare – muscle bleeding.

From the urinary system: rare – hematuria (including relevant changes of laboratory results).

Other: often – trauma, rarely – bleeding and bleeding after performing invasive procedures (including hematoma after the procedure, bleeding from the postoperative wound hematoma in the region of the puncture of the vessel and the installation location of the catheter), the presence of wound drainage, bleeding in the incision area (including a hematoma in the incision area), bleeding during surgery.

Terms and conditions storage

The drug should be stored out of reach of children at temperature not exceeding 25°C. shelf Life – 3 years.

Testimony

— prevention of venous thromboembolism in patients after elective hip or knee arthroplasty.

Contraindications

— hypersensitivity to the active substance or auxiliary components

— clinically significant active bleeding,

— liver disease, accompanied by disturbances in the blood coagulation system and a clinically significant risk of bleeding,

— severe disturbances of liver function,

— impaired renal function with KK less 15 ml/min, and the use in patients on dialysis,

— pregnancy,

— breastfeeding,

— the age 18 years.

It is not recommended to simultaneously apply apixaban with drugs, which may be associated with the development of serious bleeding.

Caution: apixaban should be used with caution when performing spinal, epidural anesthesia or puncture, and in patients receiving systemic therapy with potent inhibitors of CYP3A4 and P-glycoprotein, such as asalouyeh antifungal agents (e.g. ketoconazole, Itraconazole, voriconazole and Posaconazole), HIV protease inhibitors (eg, ritonavir). Also use caution when applying apixaban with strong inducers of CYP3A4 and P-glycoprotein (in particular, rifampicin, phenytoin, carbamazepine, phenobarbital or St. John’s wort preparations).

The risk of bleeding

The drug should be used with caution in conditions characterized by increased bleeding risk: congenital or acquired bleeding disorders, active ulcerative gastrointestinal disease, bacterial endocarditis, thrombocytopenia, thrombocytopathy, hemorrhagic stroke in the medical history, recent surgical intervention on the brain or spinal cord, and organs of vision, severe uncontrolled arterial hypertension.

In addition, caution should be exercised with simultaneous use of apixaban with NSAIDs (including acetylsalicylic acid), due to the fact that these drugs increase the risk of bleeding.

Surgical intervention associated with hip fracture

In the context of clinical research Aliquis not been used in patients undergoing urgent surgery for the hip fracture, therefore its effectiveness and safety in these patients has not been studied.

Special instructions

As the use of other anticoagulants, careful monitoring of patients, host Eliquis, on the subject of development of hemorrhage. With the development of severe bleeding the drug Eliquis should be abolished. With the development of hemorrhagic complications, you must cancel the treatment and to perform a survey to identify the source of bleeding. If necessary, prescribe appropriate treatment, in particular surgical hemostasis or transfusion of fresh frozen plasma.

Performing spinal, epidural anesthesia or puncture, patients receiving Eliquis

When performing spinal or epidural anesthesia or diagnostic puncture of these areas in patients receiving antithrombotic agent for prevention of thromboembolism, there is the risk of developing epidural or spinal hematomas, which, in turn, can cause persistent or irreversible paralysis. This risk may be increased when using the installed epidural catheter in the postoperative period or in case of parallel use of other drugs affecting hemostasis. Established epidural or subarachnoid catheters should be removed at least 5 hours before the first dose of the drug Eliquis.

Similar increased risk can be observed when performing traumatic or repeated punctures epidural or subarachnoid spaces. Requires frequent monitoring of patients for the development of the manifestations of dysfunction of the nervous system (in particular numbness or weakness of the lower extremities, dysfunction of the bowel or bladder). With the development of these disorders need an emergency examination and treatment. Before performing interventions on the epidural or subarachnoid spaces in patients receiving anticoagulants, incl. with the purpose of prevention of thrombosis, requires evaluation of the ratio of the potential benefits and risks.

Effects on ability to drive vehicles and management mechanisms

Eliquis not render essential influence on ability to driving and working with machinery.

Use in impaired renal function

In patients with impaired renal function mild, moderate or severe with a reduction in QC of up to 15 ml/min correction dose is not required. Data on the use of the drug in patients with KK<,, 15=”” b=””>, are missing. The use of the drug Eliquis in this category of patients is not recommended

Use in hepatic impairment

Use caution when taking the drug Liquidazione with hepatic impairment mild and moderate severity (grade A or b child-Pugh), thus dose adjustment is not required. The use of the drug in patients with severe hepatic impairment is not recommended.

Additional Information

SKU ml5217
Manufacturer Bristol-Myers Squibb
The purpose of the medication Anti-coagulants
Weight kg. 0.05

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