Zoltranz
Zoltranz Uses, Dosage, Side Effects, Food Interaction and all others data.
Osteoporosis causes the body to remove more bone than it replaces. This means that bones get weaker. Weak bones are more likely to break. Osteoporosis is a bone disease that is quite common in women after menopause. It also affects men. At first, osteoporosis has no symptoms, but people with osteoporosis may develop loss of height and are more likely to break (fracture) their bones, especially the back (spine), wrist, and hip bones. Osteoporosis can be prevented, and with proper therapy it can be treated.
Ibandronic acid inhibits osteoclast activity and reduces bone resorption and turnover. In postmenopausal women, it reduces the elevated rate of bone turnover, leading to a progressive gain in bone mass. The absorption of ibandronate occurs in the upper gastrointestinal tract. After absorption, ibandronate either rapidly binds to bone or is excreted unchanged into urine.
Zoltranz is a nitrogen containing bisphosphonate used to treat and prevent osteoporosis in postmenopausal women. The therapeutic index is wide as overdoses are not especially toxic, and the duration of action is long as the half life can be up to 157 hours. Patients should be counselled regarding the risk of upper GI adverse reactions, hypocalcemia, musculoskeletal pain, osteonecrosis of the jaw, atypical fractures of the femur, and severe renal impairment.
| Trade Name | Zoltranz |
| Availability | Prescription only |
| Generic | Ibandronate |
| Ibandronate Other Names | ácido ibandrónico, Ibandronic acid |
| Related Drugs | Prolia, hydrochlorothiazide, alendronate, calcitonin, estradiol, Fosamax, raloxifene, Boniva, Reclast, Tymlos |
| Weight | 168.75mg |
| Type | Tablet |
| Formula | C9H23NO7P2 |
| Weight | Average: 319.2289 Monoisotopic: 319.094975119 |
| Protein binding | Ibandronate's protein binding in serum varies from 85.7-99.5% over a concentration of 0.5-10ng/mL, but is generally 86% across a concentration range of 20-2000ng/mL. |
| Groups | Approved, Investigational |
| Therapeutic Class | Bisphosphonate preparations |
| Manufacturer | Rotex Medica Pakistan (pvt) Ltd |
| Available Country | Pakistan |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Ibandronic Acid is used for the:
- Treatment of osteoporosis in women (specially postmenopausal)
- Prevention of osteoporosis in women (specially postmenopausal)
- Prevention and treatment of osteoporosis in men
Zoltranz is also used to associated treatment for these conditions: Bone Metastases, Hypercalcemia of Malignancy, Osteoporosis
How Zoltranz works
Bisphosphonates are taken into the bone where they bind to hydroxyapatite. Bone resorption by osteoclasts causes local acidification, releasing the bisphosphonate, which is taken into the osteoclast by fluid-phase endocytosis. Endocytic vesicles become acidified, releasing bisphosphonates into the cytosol of osteoclasts where they act.
Osteoclasts mediate resorption of bone. When osteoclasts bind to bone they form podosomes, ring structures of F-actin. Disruption of the podosomes causes osteoclasts to detach from bones, preventing bone resorption.
Nitrogen containing bisphosphonates such as ibandronate are known to induce apoptosis of hematopoietic tumor cells by inhibiting the components of the mevalonate pathway farnesyl diphosphate synthase, farnesyl diphosphate, and geranylgeranyl diphosphate. These components are essential for post-translational prenylation of GTP-binding proteins like Rap1. The lack of prenylation of these proteins interferes with their function, and in the case of Rap1, leads to apoptosis. ibandronate also activated caspase-3 which contribute to apoptosis.
Dosage
Zoltranz dosage
Intravenous (Adult)-
- Hypercalcaemia of malignancy:2-4 mg as a single infusion over 2 hr. Max: 6 mg.
- Postmenopausal osteoporosis: 3 mg by inj over 15-30 seconds once every 3 mth. Missed dose: Give inj as soon as possible; then re-schedule next inj 3 mth from this inj; should not be given more frequently than once every 3 mth.
- Prophylaxis of skeletal events in patients with breast cancer and bone metastases: 6 mg by infusion over at least 15 min 3-4 wkly.
Oral (Adult)-
- Prophylaxis of skeletal events in patients with breast cancer and bone metastases: 50 mg tablet daily
- Postmenopausal osteoporosis, Prophylaxis of postmenopausal osteoporosis: 150 mg tablet once-a-month on the same date each month, alternatively, 2.5 mg daily. Missed once-monthly dose: If next scheduled dose is >7 days away: Take dose the next morning and return to original schedule; if next dose is<7 days away: Wait until the next scheduled dose; 2 tabs must not be taken w/in the same wk.
Oral Administrations-
- The tablet should preferably be taken on the same date each month.
- To maximize absorption and clinical benefit, Ibandronic acid should be taken at least 60 minutes before the first food or drink or any oral medication or supplementation (including calcium).
- To facilitate delivery to the stomach and reduce the potential for esophageal irritation, Ibandronic acid should be swallowed whole with a full glass of plain water.
- The tablet should not be chewed or sucked.
- Patients should not lie down for 60 minutes after takin Ibandronic acid . However, patients can sit down, walk, exercise or do the regular activities.
- If the once-monthly dose is missed and the patient’s next scheduled Ibandronic acid day is more than 7 days away, the patient should be instructed to take one Ibandronic acid 150 mg tablet in the morning following the date that it is remembered. Then the patient should return to the original schedule.
- If the next scheduled dose is within 7 days, patients should wait until the next dose? and then continue taking one tablet once-a-month as originally scheduled. Two 150 mg tablets should not be taken within the same week.
Side Effects
In a one-year study in patients with osteoporosis treated with ibandronate 150 mg once monthly, the majority of adverse drug reactions observed, were mild to moderate in intensity, and most cases did not lead to cessation of therapy. Common adverse reactions include dyspepsia, nausea, diarrhoea, constipation, abdominal pain, myalgia, headache, mild flu-like symptoms, dizziness, skin rash.
Toxicity
Patients experiencing an overdose may present with hypocalcemia, hypophosphatemia, upset stomach, dyspepsia, esophagitis, and uclers. Oral overdose can be managed by giving patients milk or antacids to bind excess unabsorbed ibandronate. Overdoses can be managed by providing intravenous electrolytes and dialysis is not expected to remove excess drug from serum.
Precaution
Hypocalcemia and other disturbances of bone and mineral metabolism should be effectively treated before starting therapy with Ibandronic Acid. Adequate intake of calcium and vitamin D is important in all patients.
Interaction
It is likely that products containing calcium and other multivalent cations (such as aluminium, magnesium, iron) including milk, food, and antacids are likely to interfere with absorption of ibandronate. Therefore, patients must wait 60 minutes after taking Ibandronic Acid before taking other oral medications.
Food Interaction
- Take on an empty stomach.
- Take with a full glass of water. Do not take this medication with other liquids.
[Moderate] ADJUST DOSING INTERVAL: Food significantly decreases the bioavailability of oral ibandronate.
The manufacturer reports up to a 75% decrease in bioavailability when administered 2 hours after a standard meal.
MANAGEMENT: Oral ibandronate should be administered on an empty stomach (after an overnight fast of at least 6 hours) with a 180 to 240 mL glass of plain water and no other food or drink should be taken for at least 30 minutes after administration.
Zoltranz multivitamins interaction
[Moderate] ADJUST DOSING INTERVAL: Products containing aluminum, calcium, magnesium and other polyvalent cations such as antacids or vitamin with mineral supplements are likely to interfere with the gastrointestinal absorption of oral bisphosphonates.
For example, the bioavailability of tiludronate has been shown to decrease 80% during simultaneous administration with calcium, and 60% when aluminum- or magnesium-containing antacids were administered one hour before tiludronate.
Antacids or other oral medications containing aluminum, calcium, magnesium and other polyvalent cations should be administered at least 30 minutes after the bisphosphonate dose.
Zoltranz Drug Interaction
Moderate: aspirin, aspirin, aspirin, aspirin, calcium / vitamin d, calcium / vitamin dUnknown: omega-3 polyunsaturated fatty acids, omega-3 polyunsaturated fatty acids, atorvastatin, atorvastatin, metoprolol, metoprolol, levothyroxine, levothyroxine, cyanocobalamin, cyanocobalamin, ascorbic acid, ascorbic acid, cholecalciferol, cholecalciferol
Zoltranz Disease Interaction
Major: ONJ, hypocalcemia, upper GI mucosal irritation, renal dysfunctionModerate: asthma
Volume of Distribution
The apparent terminal volume of distribution of ibandronate is 90-368L in headlthy subjects and 103L in postmenopausal women with osteopenia.
Elimination Route
Oral ibandronate is 0.63% bioavailable. In a study of healthy males, a 10mg oral dose had a Tmax of 1.1±0.6h and a Cmax of 4.1±2.6ng/mL. The Tmax is approximately 1 hour, while Cmax varies depending on dose.
A 2mg intravenous dose of ibandronate has an AUC of 316ng*h/mL, a 4mg intravenous dose of ibandronate has an AUC of 581ng*h/mL, and a 6mg intravenous dose of ibandronate has an AUC of 908ng*h/mL.
Half Life
The half life of ibandronate in postmenopausal women ranges from 37-157 hours.
Clearance
The total clearance of ibandronate is 84-160mL/min.
Elimination Route
Zoltranz is predominantly eliminated in the urine and the unabsorbed drug is eliminated unchanged in the feces.
Pregnancy & Breastfeeding use
Use in pregnancy: Pregnancy Category C. There are no adequate and well-controlled studies in pregnant women. It should be used during pregnancy only if the potential benefit justifies the potential risk to the mother and fetus.
Use in nursing mothers: It is not known whether it is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when it is administered to a nursing woman.
Contraindication
Ibandronic Acid is contraindicated in any patient who has shown a hypersensitivity reaction to the drug or to any of the excipients, hypocalcemia and inability to stand or sit upright for at least 1 hour.
Special Warning
Pediatric use: Safety and effectiveness in pediatric patients have not been established.
Geriatric Patients: No dose adjustment is necessary in the elderly.
Patients with Hepatic Impairment: No dose adjustment is necessary.
Patients with Renal Impairment: No dose adjustment is necessary for patients with mild or moderate renal impairment where creatinine clearance is equal to or greater than 30 ml/min.
Acute Overdose
No specific information is available on the treatment of overdose with ibandronic acid. However, oral overdose may result in hypocalcemia, hypophosphatemia, upset stomach, dyspepsia, esophagitis, gastritis. Milk or antacids should be given to bind Ibandronic Acid
Storage Condition
Store in a cool and dry place below 30° C. Protect from light and moisture.
Innovators Monograph
You find simplified version here Zoltranz
Zoltranz contains Ibandronate see full prescribing information from innovator Zoltranz Monograph, Zoltranz MSDS, Zoltranz FDA label
FAQ
What is Zoltranz used for?
Zoltranz is a bisphosphonate medication used in the prevention and treatment of osteoporosis and metastasis-associated skeletal fractures in people with cancer. It may also be used to treat hypercalcemia. It is typically formulated as its sodium salt ibandronate sodium. Zoltranz is used to treat and prevent osteoporosis (thinning of the bone) in women after menopause.
What is Zoltranz used for?
Zoltranz may cause irritation of the esophagus and stomach. Some cases have been severe enough to warrant hospitalization. The risk is greater in people who lie down soon after taking oral Boniva or who don't take it with a full glass of water. Take exactly as directed.
How does Zoltranz work?
This Zoltranz works by slowing bone loss to help maintain strong bones and reduce the risk of broken bones (fractures).
What are the common side effects of Zoltranz?
Common side effect of Zoltranz are include:
- Bladder pain
- bloody or cloudy urine
- chest pain
- cough producing mucus
- difficult, burning, or painful urination
- difficulty with breathing
- fever or chills
- frequent urge to urinate
- lower back or side pain
- nervousness
- pounding in the ears
- shortness of breath
- slow or fast heartbeat
- sneezing
- sore throat
- tightness in the chest
Is Zoltranz safe during pregnancy?
This Zoltranz should not be used during pregnancy unless the benefit outweighs the risk to the fetus. There is a theoretical risk of fetal harm Zoltranz if pregnancy occurs after completing a course of bisphosphonate therapy.
Is Zoltranz safe during breastfeeding?
Zoltranz is poorly absorbed orally (average in adults 6% on an empty stomach, negligible with food), so absorption of Zoltranz by a breastfed infant is unlikely.
Can you drink with Zoltranz?
Do not take any food, beverages, or calcium or vitamin supplements within 60 minutes or longer after taking Zoltranz.
When should be taken of Zoltranz?
Zoltranz should be taken first thing in the morning at least 60 minutes before any food, beverage, or other medicines.
How often can I take Zoltranz?
Zoltranz is usually taken once a day in the morning on an empty stomach and the 150-mg tablet is usually taken once a month in the morning on an empty stomach.
How long does Zoltranz take to work?
Zoltranz usually starts to work after 1 month. However, it may take 6 to 12 months for the medicine to fully protect your bones.
How long does Zoltranz stay in my system?
After a 2-h intravenous infusion, plasma concentrations of alendronate decline rapidly to approximately 5% of initial values within 6 h. About 50% of a systemic dose is excreted unchanged in the urine in the 72 h following administration.
Can I just stop taking Zoltranz?
Do not stop using this medicine suddenly without asking your doctor. Tell your doctor if you do weight-bearing exercises, smoke or drink excessively. Your doctor will need to take these into consideration in deciding your dose.
How long can I take Zoltranz?
Your doctor will determine how long to treat you with this medicine. Zoltranz is often given for only 3 to 5 years.
What happens if I miss a dose?
If you miss a dose of this medicine, skip the missed dose and go back to your regular dosing schedule. Do not double doses. For patients taking the medicine each day: If you miss a dose or forget to use your medicine in the morning, skip the missed dose and take your medicine the next morning.
What happens if I overdose?
Overdose symptoms may include muscle cramps, numbness or tingling, tight muscles in your face, seizure (convulsions), irritability, and unusual thoughts or behavior. Do not take any other medicines including vitamins, calcium, or antacids for at least 30 minutes after taking Zoltranz and cholecalciferol.
Can Zoltranz affect my heart?
Zoltranz and possibly other bisphosphonates, may be associated with an unrecognized risk for significant cardiac arrhythmias.
Is Zoltranz bad for my kidney?
Rapid administration of Zoltranz does not effect renal functioning: evidence from clinical studies in metastatic bone disease and hypercalcaemia of malignancy.
Does affect the liver?
Therapy with the bisphosphonates has been associated with a low rate of serum enzyme elevations during therapy and has been linked to rare instances of clinically apparent liver injury.
