Risedronic acid - instructions for use, dose, side effects, contraindications

Clinical and pharmacological group: & nbsp

Correctors of bone and cartilage tissue metabolism

Included in the formulation

Rizarteva

pills inwards

TEVA, LLC Russia

Risendros®

pills inwards

Zentiva c.s. Czech Republic

АТХ:

M.05.B.A Bisphosphonates

M.05.B.A.07 Risedronic acid

Pharmacodynamics:

Binding to hydroxyapatite at the cellular level, inhibition of osteoclast activity, decreased bone resorption.

Pharmacokinetics:Absorption throughout the digestive tract is complete, not dose dependent. F 0.63%; decreases with food intake. Admission 30 minutes before breakfast or 2 hours after lunch reduces absorption by 55%, the appointment for 1 hour before breakfast reduces absorption by 30% compared with taking the drug on an empty stomach (refrain from water and food 10 hours before and 4 hours after intake) . Relationship with plasma proteins 24%. The volume of distribution is 6.3 l / kg. 60% of the dose is accumulated in the bone tissue. It is not metabolized in the body. The half-life in the initial phase is 1.5 hours, in the final phase it is 480 hours. C_max 1 h. Cl 105 ml / min, total clearance 122 ml / min, independent of the drug concentration; there is a linear relationship between renal clearance and CC. Elimination with feces in unchanged form or kidneys (within 24 hours - 50% of the absorbed dose, 28 days - 85% of the absorbed dose).

Indications:

Postmenopausal osteoporosis (prevention and treatment), osteoporosis in the presence of glucocorticosteroids (prevention and treatment in men and women).

ICD-10

XIII.M80-M85.M81.0 Postmenopausal osteoporosis

XIII.M80-M85.M81.1 Osteoporosis after removal of ovaries

XIII.M80-M85.M81.4 Medicinal osteoporosis

Contraindications:

Renal insufficiency (decrease in QC less than 30 ml / min), hypocalcemia, age under 18 years (efficacy and safety of application not established).

Carefully:

Diseases of the gastrointestinal tract in the phase of exacerbation, including esophagitis, gastritis, duodenitis, peptic ulcer and duodenal ulcer, hypoparathyroidism, hypovitaminosis D, malabsorption of calcium, renal failure (QC more than 30 ml / min).

Pregnancy and lactation:

Use in pregnancy is possible only if the intended benefit to the mother exceeds the potential risk to the fetus.

During breastfeeding, the drug should be discontinued.

Recommendations FDA category C.

Dosing and Administration:

Inside, 30 minutes before breakfast or 2 hours after eating, squeezed 200 ml of water. With deforming osteitis adults - 30 mg / day once for 2 months. In the case of recurrence of the disease or a decrease in the activity of AP, it is possible to repeat the course of treatment after 2 months. For osteoporosis (postmenopauznom or on the background of taking GCS), the recommended dose for adults is 5 mg / day.

Side effects:

From the digestive system: pain in the abdomen (incl.gastralgia), dysphagia, belching, glossitis, esophagitis, duodenitis, ulcers of the esophagus and stomach, colitis, diarrhea or constipation, nausea; sometimes - a violation of the liver.

From the nervous system: headache, dizziness, asthenia, unusual fatigue, cramps of the calf muscles, myasthenia gravis.

From the sense organs: acute iritis (flushing of the sclera, pain in the eyes), amblyopia, blurred vision, dry eye mucosa, ringing in the ears.

Allergic reactions: skin rash.

Other: pain in the bones, arthralgia, bronchitis (cough), sinusitis, chest pain, peripheral edema, minor transient hypocalcemia and hypophosphatemia.

Overdose:

Symptoms: hypocalcemia.

Treatment: gastric lavage, antacids or milk inside (to reduce absorption), intravenously preparations of Ca²⁺, symptomatic therapy.

Interaction:

Preparations containing Ca²⁺, Mg²⁺, Al³⁺, Fe²⁺, antacids - reduced absorption of the drug.

NSAIDs are a risk of digestive tract disorders.

Special instructions:

With CC <30 ml / min, the drug should be discontinued, as there is a significant delay in risedronate in the bones.

Risedronate at a dose of 2.5 mg / day for 48 weeks is more effective and safer than etidronate (42-week cycles of 200 mg / day with 10-week intervals) in the treatment of involutional osteoporosis.

It is easier to carry alendronate, if there are side effects from the digestive tract when using alendronate, risedronate may be the drug of choice.

In the treatment of postmenopausal osteoporosis in combination with statins with concomitant lipid metabolism, a greater increase in the mineral density of the lumbar spine as compared with risedronate without statins.

It is inferior in effectiveness to alendronate in the treatment of postmenopausal osteoporosis.

Effective for the treatment of osteoporosis of the lumbar spine and hip neck in early menopause caused by chemotherapy for breast cancer.

Instructions

Risedronic acid (Acidum risedronicum)

Postmenopausal osteoporosis (prevention and treatment), osteoporosis in the presence of glucocorticosteroids (prevention and treatment in men and women).