Roxagen Tablet

Introduction

Roxagen Tablet 20 mg is an oral drug used to treat anemia associated with chronic kidney disease (CKD). The drug belongs to a class of medicines called hypoxia-inducible factor prolyl (HIF) hydroxylase inhibitors. It is a small molecule inhibitor of HIF hydroxylases, which increases the levels of erythropoietin (EPO) that stimulates erytemplate production in patient’s body to raise the haemoglobin level.

Uses

Roxagen Tablet 20 mg is prescribed for the treatment of anemia in adults with chronic kidney disease (CKD). This includes both maintenance therapy and treatment of anemia in those on dialysis. It can also be used in combination with other medications.

Mechanism of action

Roxagen Tablet 20 mg works by inhibiting HIF hydroxylases, which are enzymes that suppress the activation of hypoxia inducible factors (HIFs) that in turn stimulate the production of erythropoietin (EPO) and other elements of the erythropoietic cascade. This results in an increase in red blood cell production, which boosts hemoglobin levels, and ultimately improves oxygen delivery to cells in the body.

How long does it take to work?

Roxagen Tablet 20 mg begins to take effect within a few days of taking the first dose. Generally, it takes about 4-6 weeks for the full effects to become noticeable in treating CKD-related anemia. Erythropoiesis is expected to occur within 3-4 weeks with full effect achieved at approximately 8-12 weeks.

Absorption

Roxagen Tablet 20 mg is rapidly absorbed into the body after oral administration. Peak plasma concentrations are achieved within 3 hours in healthy volunteers. The bioavailability of roxadustat is 0.55-0.94.

Route of Elimination

Roxagen Tablet 20 mg is eliminated from the body by urinary and fecal pathways. Approximately 73% of the drug is excreted in urine, with the remaining 27% excreted in feces.

Dosage

The appropriate dose of roxadustat must be taken orally three times per week and not on consecutive days. The dose should be individualized to achieve and maintain target Hb levels of 10 to 12 g/dL as described below:

Patients not on erythropoiesis-stimulating agent treatment: For adults, the usual starting dose is 50 mg three times weekly. The recommended starting dose of roxadustat is 70 mg three times per week in patients weighing less than 100 kg and 100 mg three times per week in patients weighing 100 kg and over.

Patients switching from erythropoiesis-stimulating agents: For adults, the usual starting dose is 70 or 100mg three times weekly. The dosage thereafter should be adjusted according to the patient's condition.

Dose adjustment: When dose adjustments are required, increase or decrease the dose according to the "Dose increase/decrease table" and "stepwise Dose adjustment sequence" below. Once adjusted, maintain the dose level for ≥4 weeks. If the hemoglobin concentration increases rapidly (>2.0 g/dL) within 4 weeks of a dose increase, decrease the dose or suspend the treatment immediately.

The stepwise dose adjustments up or down should follow the sequence of the available doses: 20 mg-40 mg-50 mg-70 mg-100 mg-150 mg-200 mg-250 mg-300 mg-400 mg (only for CKD patients on dialysis).

Missed dose: When there is ≥ 24-hour interval until the next scheduled dosing time, take the missed dose immediately and follow the prescribed schedule for subsequent doses. If there is <24 hours until the next scheduled dosing time, skip the missed dose, and take the next dose as scheduled. Do not take 2 doses on the same day.

Method of administration: Roxadustat tablets are to be taken orally with or without food.

The recommended dose of Roxagen Tablet 20 mg for adult patients with anemia associated with CKD and on dialysis is between 2.5 and 15 mg. The optimal dose and duration of therapy depend on individual patient's response to therapy. Generally, the initial dose is 2.5 mg. Dose increase should be in increments of up to 7.5 mg depending on haemoglobin level response. Some patients may require to increase the dose up to 15 mg and in rare cases more than 15 mg. The maximum dose is 30 mg in one day. The conditions and dose should always be designed neurologist. Any change in dose should always follow the doctor’s advice.

Administration

Roxagen Tablet 20 mg is taken orally, with or without food. The capsule can be swallowed whole with a glass of water

Side effect

The most common side effects include fatigue, headache, dizziness, nausea, joint pain, diarrhoea, low blood pressure, thrombocytopenia, and increased creatinine levels. Rare side effects of this medication include anemia, stroke, thrombotic microangiopathy, and hepatotoxicity.

Toxicity

The safety of Roxagen Tablet 20 mg has been studied extensively in clinical trials. There is no evidence that the drug is toxic. In rare cases, it can cause hepatotoxicity. However, this is thought to be mediated by inappropriate use of concurrent medications.

Precaution

Roxagen Tablet 20 mg should be used with caution in patients with cardiovascular disease, hepatic or renal impairment, and those taking other medications that can induce hepatotoxicity. It is also important to follow the doctor's advice while taking the medication and not exceed the recommended dose.

Interaction

Roxagen Tablet 20 mg has been found to interact with certain medications as well as with food. Some medications may lower or increase the effectiveness of the drug, so it is important to let your doctor know of any other medications you are taking. Additionally, some foods can increase or decrease the absorption of the drug, so it is important to avoid certain foods while taking it.

Disease Interaction

Roxagen Tablet 20 mg should be used with caution in patients with high blood pressure, diabetes, or stroke. Additionally, it should not be used in patients with existing malignancy or intolerance to its active ingredients.

Drug Interaction

Roxagen Tablet 20 mg may interact with certain drugs, such as anti-coagulants, non-steroidal anti-inflammatory drugs, antibiotics, diuretics, and anti-fungals. To avoid any potential interactions, it is important to let your doctor know of all medications you are taking before starting this medication.

Food Interactions

Certain foods can increase or decrease the absorption of Roxagen Tablet 20 mg. Therefore, it is best to avoid grapefruits or grape juice while taking this medication. Additionally, alcohol intake should be avoided as it can intensify the side effects of this medication.

Pregnancy Use

Roxagen Tablet 20 mg is considered to be contraindicated in pregnancy, as there is insufficient safety data available. It is best to consult a doctor before taking this medication if you are pregnant.

Lactation Use

Roxagen Tablet 20 mg is not recommended for use in breastfeeding women, as there is a potential risk of adverse effects to the baby. It is best to consult a doctor before taking this medication if you are breastfeeding.

Acute overdose

In cases of overdose, there may be an increased risk of adverse side effects. If the patient has overdosed on Roxagen Tablet 20 mg, it is advisable to seek medical attention immediately.

Contraindication

Roxagen Tablet 20 mg should not be used in patients with systolic heart failure, known hypersensitivity to the active ingredient or any of its excipients; in combination with strong CYP450 3A4 inhibitor or strong士UDP-glucuron Mason transferase (Sister) inhibitor, and in those with an active malignancy or tumour lysis syndrome.

Dose direction

Roxagen Tablet 20 mg should be taken orally, with or without food, as determined by your physician. The capsule may be swallowed whole with a glass of water. Do not chew or crush the capsule. Follow the physician's instructions on the dose and duration of the medication. Do not exceed the recommended dose or discontinue the medication without consulting the doctor.

Storage condition

Roxagen Tablet 20 mg should be kept at room temperature away from direct sunlight and moisture. Keep it out of reach of children. Do not freeze the medication.