Risedronic acid is a Bisphosphonate. The chemical classification of risedronic acid is Diphosphonates. Risedronate Sodium is the sodium salt of the risedronic acid, a synthetic pyridinyl bisphosphonate. Risedronic acid binds to hydroxyapatite crystals in bone and inhibits osteoclast-dependent bone resorption.
Risedronic acid often used as its sodium salt risedronate sodium (USAN) is a bisphosphonate used to strengthen bone, treat osteoporosis caused by menopause, steroid use, or gonadal failure. This medicine is for use when you have a high risk of bone fracture due to osteoporosis or prevent osteoporosis, and treat Paget’s disease of bone.
Risedronate is a pyridinyl bisphosphonate that inhibits osteoclast-mediated bone resorption and modulates bone metabolism and is indicated for the treatment and prevention of osteoporosis in postmenopausal women.
Mechanism of Action of Risedronic acid
The action of risedronate on bone tissue is based partly on its affinity for hydroxyapatite, which is part of the mineral matrix of bone. Risedronate also targets farnesyl pyrophosphate (FPP) synthase. Nitrogen-containing bisphosphonates (such as pamidronate, alendronate, risedronate, ibandronate, and zoledronate) appear to act as analogs 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 signaling 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.
Indications of Risedronic acid
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For the treatment of Paget’s disease of the bone (osteitis deformans), postmenopausal and glucocorticoid-induced osteoporosis
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Treatment of postmenopausal osteoporosis, to reduce the risk of vertebral fractures and the treatment of established postmenopausal osteoporosis, to reduce the risk of hip fractures
- Prevention of osteoporosis
- Paget’s disease
- Treatment of osteoporosis in men to prevent fractures
- Treatment of osteoporosis in post-menopausal women to prevent fractures
- Treatment of osteoporosis in men to prevent fractures
- Prevention and treatment of corticosteroid-induced osteoporosis and prevention of bone loss in post-menopausal women considered at risk of developing osteoporosis.
- Prophylaxis and treatment of female osteoporosis
- Bone destruction
- Prevention and treatment of corticosteroid-associated osteoporosis together with supplements of calcium and vitamin D
- Treatment for osteogenesis imperfecta in patients of 18 years or older
- Dental implants coating (experimental)
- Treatment for osteogenesis imperfecta in patients of 18 years or older
- Dental implants coating (experimental)
- Osteoporosis caused by glucocorticoid
- For the treatment of Paget’s disease of bone (osteitis deformans).
- Indicated as an aid in the treatment of clinical signs of lameness associated with bone spavin in combination with a controlled exercise regime in horses over 3 years of age.
Contra-Indications of Risedronic acid
- Acute inflammations of the gastrointestinal tract (esophagitis, gastritis, ulcerations)
- Clinically manifest osteomalacia
- Certain malformations and malfunctions of the esophagus (strictures, achalasia)
- Inability to stand, walk, or sit for 30 minutes after oral administration
- Renal impairment with a creatinine clearance below 30ml/min
- Hypersensitivity to alendronate or another ingredient
- Hypocalcemia
- Pregnancy and breastfeeding
- Patients below 18 yrs. of age, as no clinical data exists
- Signs of colic, which is usually self-limiting, occurs in 30-45% of horses.
- Tachycardia
- Electrolyte disturbances – primarily calcium, magnesium, and potassium, which can last for several hours. Caution should be used in horses with disease processes that could be affected by electrolyte disturbances, such as hyperkalemic periodic paralysis or cardiac disease.
- Kidney damage – it is eliminated by the kidney and is not recommended for use in animals with impaired renal function.
- Less serious reactions include stiffness of the neck, decreased appetite, fever, and increased urination.
The dosage of Risedronic acid
Strengths: 5 mg; 30 mg; 35 mg; 75 mg; 150 mg;
Treatment Of Postmenopausal Osteoporosis
The recommended regimen is:
- one 5 mg tablet orally, taken daily
or - one 35 mg tablet orally, taken once-a-week
or - one 75 mg tablet orally, taken on two consecutive days for a total of two tablets each month
or - one 150 mg tablet orally, taken once-a-month
Prevention Of Postmenopausal Osteoporosis
The recommended regimen is
- one 5 mg tablet orally, taken daily
or - one 35 mg tablet orally, taken once-a-week
or - alternatively, one 75 mg tablet orally, taken on two consecutive days for a total of two tablets each month may be considered
or - alternatively, one 150 mg tablet orally, taken once-a-month may be considered
Treatment To Increase Bone Mass In Men With Osteoporosis
The recommended regimen is
- one 35 mg tablet orally, taken once-a-week
Treatment And Prevention Of Glucocorticoid-Induced Osteoporosis
The recommended regimen is
- one 5 mg tablet orally, taken daily
Paget’s Disease
-30 mg orally once a day for 2 months
Side Effects of Risedronic acid
The most common
- Abdominal or stomach pain
- feeling of heaviness, pain, warmth and/or swelling in a leg or in the pelvis
- sudden tingling or coldness in an arm or leg
- Burning, itching, stinging, redness, or other sign of irritation at the application site ,rash
- Indigestion
- Constipation
- High blood pressure
- Nausea ,vomiting,
- painful or swollen gums
- numbness or heavy feeling in the jaw
- dull, aching pain in the hip, groin, or thigh
- liver problems,
- stomach pain,
- Dizziness
- headache,
- reversible hair loss or thinning, and
- fever.
Common
- chills or fever
- headache, severe and throbbing
- joint or back pain
- muscle aching or cramping
- muscle pains or stiffness
- chest pressure or squeezing pain in chest
- excessive sweating
- sudden drowsiness or need to sleep
- sharp pain when taking a deep breath
- coughing up blood
- rust colored urine
- liver problems–nausea, upper stomach pain, itching, tired feeling, loss of appetite, dark urine, clay-colored stools, jaundice (yellowing of the skin or eyes)
- decreased amount of urine
Rare
- Anxiety
- change in vision
- chest pain or tightness
- confusion
- a cough
- Agitation
- arm, back, or jaw pain
- blurred vision
- chest pain or discomfort
- convulsions
- extra heartbeats
- hallucinations
- a headache
- irritability
- lightheadedness
- muscle pain or cramps
- muscle spasm or jerking of all extremities
- severe pain in your upper stomach spreading to your back, nausea, and vomiting;
Drug Interactions Risedronic acid
The risedronic acid may interact with following drugs, supplements & may change the efficacy of drugs
- NSAIDs (nonsteroidal anti-inflammatory drugs) such as ibuprofen, naproxen
- aspirin
- antacids
- proton pump inhibitors such as esomeprazole, lansoprazole, omeprazole, pantoprazole,
- H2 blockers such as cimetidine, famotidine, nizatidine, ranitidine
- hormone therapy such as estrogens and estrogen agonist/blockers
- cancer chemotherapy treatments
- steroids such as dexamethasone, methylprednisolone, and prednisone
- calcium supplements
- aluminum supplements
- magnesium supplements
- iron supplements
If you must take these medicines, wait at least 30 minutes after taking risedronate.
Pregnancy & Lactation of Risedronic acid
FDA pregnancy category C
Pregnancy
Risedronate is not intended for use during pregnancy. If you become pregnant while taking this medication, contact your doctor immediately.
Lactations
It is not known if risedronate passes into breast milk. If you breastfeeding mother and are taking this medication, it may affect your baby. Talk to your doctor about whether you should continue breast-feeding. The safety and effectiveness of using this medication have not been established for children.
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