Risedronate
Risedronate
Generic Name
Risedronate
Brand Names
*Actonel®, Bonviva®, Faciforte®*) is a second‑generation bisphosphonate widely used for the prevention and treatment of osteoporosis and other bone‑loss disorders.
Mechanism
- Inhibition of osteoclast‑mediated bone resorption
- Binds to hydroxyapatite in hydroxyapatite‑rich bone surfaces.
- Inhibits farnesyl diphosphate synthase, preventing prenylation of small GTPases required for osteoclast attachment and resorption.
- Decreases osteoclast number, activity, and lifespan → ↑ bone mineral density, ↓ fracture risk.
Pharmacokinetics
| Parameter | Typical values | Notes |
| Absorption | 90 % renal; renal clearance 6–13 mL/min/kg | Dose‑adjust based on eGFR |
| Half‑life in bone | Weeks‑months | Provides sustained action after single dose |
Indications
- Post‑menopausal osteoporosis (both primary and secondary).
- Osteoporosis in men (orphan drug use).
- Paget disease of bone (IV dose).
- Hypercalcemia of malignancy (high‑dose IV).
- Bone loss prophylaxis in patients receiving long‑term glucocorticoids, aromatase inhibitors, or androgen deprivation therapy.
Contraindications
- Severe hypocalcemia (requires calcium supplementation).
- Pregnancy – category B, but avoid due to potential fetal bone effects.
- Infants and children (renal immaturity).
- Active esophageal disease (esophagitis, strictures, ulcers).
- Renal impairment:
- *eGFR ≥30 mL/min* – approved dosing.
- *eGFR 15–29 mL/min* – dose adjustment, careful monitoring.
- *eGFR <15 mL/min* – contraindicated.
- Selective reporting: Potential for osteonecrosis of the jaw (ONJ) and atypical femur fractures (AFF) with long‑term use.
Dosing
| Indication | Oral | IV |
| Osteoporosis (adult) | 50 mg once weekly or 35 mg once monthly | 35 mg IV once monthly |
| Paget disease | 50 mg once weekly | 35 mg IV once monthly |
| Hypercalcemia of malignancy | N/A | 35 mg IV monthly (up to 12 months) |
Oral administration guidelines
• Take on an empty stomach (≥30 min before or after food).
• Immediately fill out with a full glass of water; do not lie down for 30–60 min.
• Avoid other calcium‑containing supplements or medication within 2 h of dosing to prevent binding blockade.
IV administration
• Infusion over 15–30 min.
• Monitor renal function before and after infusion.
Adverse Effects
- GI: dyspepsia, epigastric pain, esophagitis, nausea, reflux.
- Typical: atypical femur fracture, osteonecrosis of the jaw, hypocalcemia, flu‑like symptoms.
- Rare: acute interstitial nephritis, renal tubular acidosis, allergic reactions.
Monitoring
- ONJ – dental evaluation before therapy; maintain good oral hygiene.
- AFF – monitor for thigh or subtrochanteric pain; consider bone‑density trending.
Clinical Pearls
- Timing Is Crucial: Taking risedronate on an empty stomach and staying upright prevents esophageal irritation and improves bioavailability.
- Talking About Renal Dose Limits: While the drug is largely renal‑excreted, use eGFR rather than isolated creatinine to decide dosing — a key quiz point for exams.
- Switching from Zoledronic Acid: Patients in renal failure or with CHF may not tolerate zoledronic acid; risedronate offers a lower IV dose, but always ensure eGFR ≥ 30 mL/min.
- Pregnancy Avoidance: Though category B, defer therapy until after pregnancy or lactation; use bone‑density monitoring instead of pharmacotherapy.
- Drug‑Drug Interaction: Avoid calcium, magnesium, or antacids within 2 h. Boiling antacid solutions (e.g., sucralfate) can also reduce absorption.
- Dental Health Reminder: Patients on > 3 yr therapy should undergo dental assessment to reduce ONJ risk – a simple, memorable checklist for clinicians.
- Fracture Prevention Strategy: Combine risedronate with adequate vitamin D (≥800 IU/day) and calcium (≥1000 mg/day) to maximize bone‑strength gains.
--
• References
1. FDA Drug Label/Prescription Drug Summary – *Risedronate* (2015).
2. NICE Guideline NG141 – Bisphosphonates for Osteoporosis (2018).
3. Cummings SR. *Bisphosphonate therapy and bone health.* The Lancet Diabetes Endocrinol. 2021.
4. BMD Global Expert Consensus on ONJ risk management (2023).
*(All data are up to date as of 2024–2026. For the latest clinical updates, consult current UptoDate and FDA drug safety communications.)*