The action of zoledronate on bone tissue is based partly on its affinity for hydroxyapatite, which is part of the mineral matrix of bone. Zoledronate also targets farnesyl pyrophosphate (FPP) synthase. Nitrogen-containing bisphosphonates such as zoledronate appear to act as analogues of isoprenoid diphosphate lipids, thereby inhibiting FPP synthase, an enzyme in the mevalonate pathway. Inhibition of this enzyme in osteoclasts prevents the biosynthesis of isoprenoid lipids (FPP and GGPP) that are essential for the post-translational farnesylation and geranylgeranylation of small GTPase signalling proteins. This activity inhibits osteoclast activity and reduces bone resorption and turnover. In postmenopausal women, it reduces the elevated rate of bone turnover, leading to, on average, a net gain in bone mass.
Zoledronic acid is used to prevent skeletal fractures in patients with cancers such as multiple myeloma and prostate cancer, as well as for treating osteoporosis. It can also be used to treat hypercalcemia of malignancy and can be helpful for treating pain from bone metastases.
It can be given at home rather than in hospital.
Such use has shown safety and quality-of-life benefits in people with breast
cancer and bone metastases.
Along with its needed effects, a medicine may cause some unwanted effects. Although not all of these side effects may occur, if they do occur they may need medical attention.
Check with your doctor or nurse immediately if any of the following side effects occur:
Incidence not known
Some side effects may occur that usually do not need medical attention. These side effects may go away during treatment as your body adjusts to the medicine. Also, your health care professional may be able to tell you about ways to prevent or reduce some of these side effects. Check with your health care professional if any of the following side effects continue or are bothersome or if you have any questions about them:
Other side effects not listed may also occur in
some patients. If you notice any other effects, check with your healthcare
Dosage Forms & Strengths
IV injectable solution
Hypercalcemia of Malignancy
Zometa: No more than 4 mg IV (infused over >15 minutes) once; may be repeated in 7 days
Monitor serum calcium, and wait at least 7 days before considering retreatment
Multiple Myeloma; Bone Metastases From Solid Tumors
Zometa: 4 mg IV (infused over >15 minutes) every 3-4 weeks
Reduction in incidence of fractures (hip, vertebral, and nonvertebral osteoporosis-related fractures)
Prevention in postmenopausal women
Treatment in men and postmenopausal women
Treatment and prevention
Reclast: 5 mg IV over >15 minutes every year; supplemented with elemental calcium and vitamin D
Reclast: 5 mg IV over >15 minutes once; supplemented with elemental calcium and vitamin D
Renal impairment (Zometa)
Renal impairment (Reclast)
Although certain medicines should not be used together at all, in other cases two different medicines may be used together even if an interaction might occur. In these cases, your doctor may want to change the dose, or other precautions may be necessary. Tell your healthcare professional if you are taking any other prescription or nonprescription (over-the-counter [OTC]) medicine.
Certain medicines should not be used at or around the time of eating food or eating certain types of food since interactions may occur. Using alcohol or tobacco with certain medicines may also cause interactions to occur. Discuss with your healthcare professional the use of your medicine with food, alcohol, or tobacco.
Other Medical Problems
The presence of other medical problems may affect the use of this medicine. Make sure you tell your doctor if you have any other medical problems, especially:
Your doctor may also give you vitamins containing Vitamin D and calcium. Tell your doctor if you are unable to take these supplements.
Drink extra fluids so you will pass more urine while you are using this medicine. This will keep your kidneys working well and help prevent kidney problems. However, it is very important to not drink too much liquid. Talk to your doctor about the right amount of liquids for you.
This medicine comes with a
Medication Guide. It is very important that you read and understand this
information. Be sure to ask your doctor about anything you do not understand.
In deciding to use a medicine, the risks of taking the medicine must be weighed against the good it will do. This is a decision you and your doctor will make. For this medicine, the following should be considered:
Tell your doctor if you have ever had any unusual or allergic reaction to this medicine or any other medicines. Also tell your health care professional if you have any other types of allergies, such as to foods, dyes, preservatives, or animals. For non-prescription products, read the label or package ingredients carefully.
Zoledronic acid injection is not indicated for use in children.
Appropriate studies performed to date have not demonstrated geriatric-specific problems that would limit the usefulness of zoledronic acid injection in the elderly. However, elderly patients are more likely to have age-related kidney problems, which may require caution in patients receiving zoledronic acid injection.
Studies in pregnant women have demonstrated a risk to the fetus. However, the benefits of therapy in a life threatening situation or a serious disease, may outweigh the potential risk.
There are no adequate studies in women for determining
infant risk when using this medication during breastfeeding. Weigh the
potential benefits against the potential risks before taking this medication