Dosing & Uses
Dosage Forms & Strengths
IV solution
- 1100 kBq/mL (30 microcurie/mL)
- Available as 6mL/single-use vial
Prostate Cancer
Indicated for treatment of men with castration-resistant prostate cancer with symptomatic bone metastases and no known visceral metastatic disease
55 kBq (1.49 microcurie) per kg IV infused over 1 minute; repeat q4weeks for 6 cycles total
Dosage calculation must be based on decay correction factor of radium-223
Dose calculation
- Volume to be administered should be calculated using the:
- -Patient’s body weight (kg)
- -Dosage level 55 kBq/kg body weight or 1.49 microcurie/kg body weight
- -Radioactivity concentration of the product (1,100 kBq/mL; 30 microcurie/mL) at the reference date
- -Decay correction factor to correct for physical decay of radium-223
- Example: (Body wt in kg x 55 kBq/kg body weight) ÷ (Decay factor x 1,100 kBq/mL) or (Body wt in kg x 1.49 microcurie body weight) ÷ (Decay factor x 30 microcurie/mL)
- Decay correction factor table listed in prescribing information and is based on the vial’s reference date
Dosing Considerations
Safety beyond 6 treatment cycles not established
Safety and efficacy not established
Adverse Effects
>10%
Percentages includes all toxicity grades (1-4)
Anemia (93%)
Lymphocytopenia (72%)
Leukopenia (35%)
Thrombocytopenia (31%)
Nausea (36%)
Diarrhea (25%)
Vomiting (19%)
Neutropenia (18%)
Peripheral edema (13%)
1-10%
Percentages includes all toxicity grades (1-4)
Renal failure and impairment (3%)
Dehydration (3%)
Pancytopenia (2%)
Erythema, pain, and edema at injection site (1%)
Warnings
Contraindications
Pregnancy; radium-223 can cause fetal harm when administered to a pregnant woman based on its mechanism of action; not indicated for use in women and is contraindicated in women who are or may become pregnant
Cautions
May cause myelosuppression and bone marrow failure; perform hematologic evaluation at baseline and prior to every dose; discontinue if life-threatening complications occur despite supportive care for bone marrow failure
Safety and efficacy of concomitant chemotherapy have not been established; outside of a clinical trial, concomitant use with chemotherapy is not recommended due to the potential for additive myelosuppression
Not recommended for use in combination with abiraterone acetate plus prednisone/prednisolone outside of clinical trials; increased fractures and mortality reported
Because of potential effects on spermatogenesis associated with radiation, advise men who are sexually active to use condoms and their female partners of reproductive potential to use a highly effective contraceptive method during and for 6 months after completing treatment
Pregnancy & Lactation
Pregnancy
Safety and efficacy have not been established in females; based on mechanism of action, drug can cause fetal harm when administered to a pregnant female; while there are no human or animal data on use in pregnancy, maternal use of a radioactive therapeutic agent could affect development of a fetus; Advise pregnant females and females of reproductive potential of the potential risk to a fetus
Lactation
Safety and efficacy not established in females; there is no data on presence of radium-223 dichloride in human milk, effects on breastfed child, or on milk production
Pregnancy Categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk. C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done. D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk. X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist. NA: Information not available.Pharmacology
Mechanism of Action
Alpha particle-emitting radiopharmaceutical; contains the heavy metal radium, which mimics calcium and forms complexes with the bone mineral hydroxyapatite at areas of increased bone turnover, such as bone metastases; this causes double-strand DNA breaks that are lethal to the prostate cancer cell at the site of increased bone turnover induced by the cancer
Absorption
Peak blood levels were linear in terms of dose proportionality and time independence in the dose range investigated
Distribution
After IV injection, rapidly cleared from the blood and distributed primarily into bone or is excreted into intestine
No significant uptake was seen in other organs such as heart, liver, kidneys, urinary bladder, and spleen at 4 hours post-injection
Detected in blood post-injection
- 15 minutes: ~20% remains in blood
- 4 hr: ~4% remains in blood
- 24 hr: <1% remains in blood
Detected in bone/intestine post-injection
- 10 minutes: Radioactivity was observed in bone and in intestine
- 4 hr: Percentage of the radioactive dose present in bone and intestine was approximately 61% and 49%, respectively
Metabolism
Isotope that decays and is not metabolized
Elimination
~63% excreted from body within 7 days after injection (after correcting for decay)
Fecal excretion is the major elimination route; at 48 hr after injection, the cumulative fecal excretion was 13% (range 0 -34%), and the cumulative urine excretion was 2% (range 1 -5%)
Administration
IV Administration
Follow procedures for proper handling and disposal of radioactive pharmaceuticals
Inspect visually for particulate matter and discoloration before administering
Ready-to-use IV solution; do not dilute or mix with any solutions
Slow IV injection over 1 minute
Flush IV line/cannula with 0.9% NaCl before and after injection
Storage
Store at room temperature, below 40°C (104°F)
Store in original container or equivalent radiation shielding
Images
Patient Handout
radium Ra 223 dichloride intravenous
RADIUM RA 223 DICHLORIDE - INJECTION
(RAY-dee-um)
COMMON BRAND NAME(S): Xofigo
USES: This medication is used to treat prostate cancer and cancer that has spread to bones. Radium Ra 223 dichloride is a radioactive drug. It works by building up in certain cancer cells and causing them to die.
HOW TO USE: This medication is given by slow injection into a vein by a health care professional. It is given as directed by your doctor, usually every 4 weeks for a total of 6 injections.The dosage is based on your medical condition, weight, lab tests, and response to treatment.To prevent dehydration, it is important to drink plenty of fluids while you are being treated with this drug. Consult your doctor or pharmacist if you have any questions.Because this medication releases some radiation and may be present in the blood, urine, or stool for about 1 week after an injection, avoid contact with your blood, urine, or stool for at least 1 week after your treatment. To avoid splashing, sit down on the toilet seat each time you use the bathroom during the 1-week period after your injection. When you are done, flush the toilet twice. Afterward, wash your hands well with soap and water. Use medical gowns and gloves if you need to clean up any blood, urine, or stool. If any blood, urine, or stool gets on your clothing, wash the clothing right away and separately from your other clothing.
SIDE EFFECTS: Nausea, diarrhea, or vomiting may occur. If any of these effects last or get worse, tell your doctor or pharmacist promptly.Dehydration can occur. The risk is increased if you have vomiting or diarrhea that doesn't stop, and you cannot drink normally. Contact your doctor right away if you notice any symptoms of dehydration, such as unusual dry mouth/thirst, fast heartbeat or dizziness/lightheadedness.People using this medication may have serious side effects. However, you have been prescribed this drug because your doctor has judged that the benefit to you is greater than the risk of side effects. Careful monitoring by your doctor may decrease your risk.Tell your doctor right away if you have any serious side effects, including: easy bruising/bleeding, signs of kidney damage (such as change in amount of urine).This medication may increase the risk of bone fractures. Tell your health care provider right away if you have bone pain or changes in movement.This medication may lower your ability to fight infections. This may make you more likely to get a serious (rarely fatal) infection or make any infection you have worse. Tell your doctor right away if you have any signs of infection (such as sore throat that doesn't go away, fever, chills, cough).A very serious allergic reaction to this drug is rare. However, get medical help right away if you notice any symptoms of a serious allergic reaction, including: rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing.This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.In the US -Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088 or at www.fda.gov/medwatch.In Canada - Call your doctor for medical advice about side effects. You may report side effects to Health Canada at 1-866-234-2345.
PRECAUTIONS: Before using radium Ra 223 dichloride tell your doctor or pharmacist if you are allergic to it; or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.Before using this medication, tell your doctor or pharmacist your medical history.This medication can make you more likely to get infections or may make current infections worse. Stay away from anyone who has an infection that may easily spread (such as chickenpox, COVID-19, measles, flu). Talk to your doctor if you have been exposed to an infection or for more details.Tell your health care professional that you are using radium Ra 223 dichloride before having any immunizations/vaccinations. Avoid contact with people who have recently received live vaccines (such as flu vaccine inhaled through the nose).To lower the chance of getting cut, bruised, or injured, use caution with sharp objects like razors and nail cutters, and avoid activities such as contact sports.This medication may increase your risk for other cancers (such as bone cancers). Talk to your doctor for details.Before having surgery, tell your doctor or dentist about all the products you use (including prescription drugs, nonprescription drugs, and herbal products).Radium Ra 223 dichloride is not recommended for use by women.Males with female partners of childbearing age should ask about reliable forms of birth control while using this medication and for 6 months after stopping treatment. Their female partners should also use reliable forms of birth control for the same amount of time.It is unknown if this medication affects sperm. If you plan to father a child, discuss the risks and benefits of this medication with your doctor.
DRUG INTERACTIONS: Drug interactions may change how your medications work or increase your risk for serious side effects. This document does not contain all possible drug interactions. Keep a list of all the products you use (including prescription/nonprescription drugs and herbal products) and share it with your doctor and pharmacist. Do not start, stop, or change the dosage of any medicines without your doctor's approval.A product that may interact with this drug is: abiraterone.
OVERDOSE: If someone has overdosed and has serious symptoms such as passing out or trouble breathing, call 911. Otherwise, call a poison control center right away. US residents can call their local poison control center at 1-800-222-1222. Canada residents can call a provincial poison control center.
NOTES: Lab and/or medical tests (such as complete blood counts, kidney function) should be done while you are using this medication. Keep all medical and lab appointments.
MISSED DOSE: It is important to get each dose of this medication as scheduled. If you miss a dose, ask your doctor or pharmacist right away for a new dosing schedule.
STORAGE: Not applicable. This medication is given in a hospital or clinic and will not be stored at home.
MEDICAL ALERT: Your condition can cause complications in a medical emergency. For information about enrolling in MedicAlert, call 1-888-633-4298 (US) or 1-800-668-1507 (Canada).
Information last revised March 2023. Copyright(c) 2023 First Databank, Inc.
IMPORTANT: HOW TO USE THIS INFORMATION: This is a summary and does NOT have all possible information about this product. This information does not assure that this product is safe, effective, or appropriate for you. This information is not individual medical advice and does not substitute for the advice of your health care professional. Always ask your health care professional for complete information about this product and your specific health needs.
Formulary
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