Included in the formulation
Included in the list (Order of the Government of the Russian Federation No. 2782-r of 30.12.2014):VED
АТХ:H.05.A.A.02 Teriparatide
Pharmacodynamics:Teriparatide - recombinant human parathyroid hormone (PTH). Endogenous PTH is the main regulator of calcium and phosphorus metabolism in bones and kidneys, stimulates the formation of bone tissue (by primarily enhancing the activity of osteoblasts in relation to osteoclast activity), indirectly increases intestinal absorption and tubular calcium reabsorption, as well as kidney phosphate excretion. The biological effect of PTH is due to binding to specific PTH receptors on the cell surface. Teriparatide - an active fragment of endogenous human PTH, which binds to the same receptors and exerts the same effect on bones and kidneys as PTH. All other agents for the treatment of osteoporosis work on a different principle - they inhibit the process of bone destruction, but do not stimulate the formation of young bone tissue, and on the background of treatment with teriparatide, bone mineral density (BMD) increases.The processes of mineralization occur without signs of toxic effects on its cells, the formed bone tissue has a normal structure (without the formation of reticulofibrous bone tissue and bone marrow fibrosis). Teriparatide reduces the risk of fractures regardless of age, baseline bone metabolism or BMD (relative risk reduction of new fractures is 65%).
Pharmacokinetics:Well absorbed with n / to the introduction. Absolute bioavailability is 95%, Vd is 1.7 l / kg. Cmax is achieved 30 minutes after the SC administration at a dose of 20 μg and exceeds the upper limit of the normal level of PTH by 4-5 times, for 3 hours the concentration decreases to undetectable values. The half-life at the n / k introduction is 1 hour, which reflects the time required for absorption. Peripheral metabolism occurs predominantly in the liver through nonspecific enzymatic mechanisms followed by excretion by the kidneys. Do not accumulate in bones or other tissues (just like endogenous PTH).
Age (in the group of patients from 31 to 85 years) does not affect the pharmacokinetics of teriparatide.In patients with mild or moderate renal insufficiency (QC from 30 to 72 ml / min), the pharmacokinetics of the drug does not change. The recommended dose of teriparatide does not depend on sex, although the systemic exposure of teriparatide in men is 20-30% lower than that of women.
Indications:Treatment of osteoporosis in postmenopausal women; treatment of primary osteoporosis or osteoporosis due to hypogonadism in men; treatment in men and women of osteoporosis with an increased risk of fractures due to prolonged systemic therapy of glucocorticosteroids.
XIII.M80-M85.M80.0 Postmenopausal osteoporosis with pathological fracture
XIII.M80-M85.M80.1 Osteoporosis with a pathological fracture after removal of the ovaries
XIII.M80-M85.M80.4 Medicinal osteoporosis with pathological fracture
XIII.M80-M85.M80.5 Idiopathic osteoporosis with pathological fracture
XIII.M80-M85.M81.0 Postmenopausal osteoporosis
XIII.M80-M85.M81.1 Osteoporosis after removal of ovaries
XIII.M80-M85.M81.4 Medicinal osteoporosis
XIII.M80-M85.M81.5 Idiopathic osteoporosis
XIII.M80-M85.M81.8 Other osteoporosis
XIII.M80-M85.M82.1 * Osteoporosis in endocrine disorders (E00-E34 +)
Contraindications:Hypersensitivity; previous hypercalcemia; severe renal insufficiency; metabolic diseases of bones,with the exception of primary osteoporosis (including hyperparathyroidism and Paget's disease); unclosed growth zones; increased activity of AP of unknown origin; previous radiation therapy of bones of the skeleton; metastases in bone or bone tumors in history; pregnancy, lactation; age to 18 years.
Do not use for the prevention of osteoporosis or in the lungs of its forms in order to avoid the occurrence of osteosarcoma. Assign in case of severe disease.
Carefully:Urolithiasis (in acute stage or recently transferred); moderately expressed renal failure, hypovitaminosis D, hypocalcemia (clinically significant), simultaneous reception of cardiac glycosides.
Pregnancy and lactation:Studies in animals have shown a negative effect on the fetus. Adequate and controlled studies in pregnant women have not been conducted. Use in pregnant women is contraindicated. If necessary, use during lactation should stop breastfeeding.
Action category for the fetus by FDA - FROM.
Dosing and Administration:Assign to adults, the dose does not depend on the age of the patient.and is 20 mcg, is administered 1 time / day p / to the area of the thigh or abdomen. The maximum duration of treatment is 24 months. The efficacy and safety of teriparatide in therapy for more than 2 years has not been studied; as a result, a course of therapy lasting more than 24 months during the life of the patient is not recommended.
It is recommended supplemental calcium and vitamin D, if they are supplied with food in insufficient quantities.
Side effects:From the cardiovascular system: often - a feeling of heartbeat, lowering blood pressure; infrequently - a tachycardia.
From the respiratory system: often shortness of breath; infrequently - emphysema.
From the digestive system: often - nausea, vomiting, hiatal hernia, gastroesophageal reflux disease; infrequently - hemorrhoids.
From the skin and subcutaneous tissues: often - increased sweating.
From the musculoskeletal system: very often - pain in the limbs; often - muscle cramps; infrequently - myalgia, arthralgia, pain or spasm in the back.
From the side of the kidneys and urinary tract: infrequent - urinary incontinence, polyuria, imperative urge to urinate, urolithiasis; rarely - renal dysfunction / kidney failure.
Allergic reactions: very rarely - shortly after injection, acute shortness of breath, hives, chest pain, swelling (mostly peripheral).
Common reactions: often - weakness, pain in the chest, asthenia.
Local reactions: rarely - erythema at the injection site, reaction at the injection site ..
Laboratory and instrumental data: infrequently - an increase in body weight, noises in the heart, an increase in the concentration of alkaline phosphatites.
Overdose:Symptoms: hypercalcemia with delayed onset, development of orthostatic hypotension. Nausea, vomiting, dizziness, headache are also possible.
Treatment: there is no special antidote. If suspicion of overdose is recommended, the discontinuation of teriparatide, monitoring the content of serum calcium and symptomatic therapy.
Interaction:Clinically significant interactions with hydrochlorothiazide, furosemide, digoxin, atenolol, as well as with sustained-release preparations (diltiazem, nifidipine, felodipine, nisoldipine) were not noted.
Co-administration of teriparatide with raloxifene or hormone replacement therapy does not affect the serum calcium and urine levels of calcium.
Single administration of teriparatide has no effect on the pharmacodynamics of digoxin. However, patients receiving digoxincaution should be exercised in the application of teriparatide, as the latter can cause a transient increase in the concentration of calcium in the blood (and thus be a predisposing factor in the development of intoxication with digitalis preparations).
Special instructions:Blood sampling for determining the calcium content in the blood should be performed no earlier than 16 hours after the last administration of teriparatide (a short-term increase in the serum calcium content may be observed). Constant monitoring of the concentration of calcium during treatment is not required.
When receiving teriparatide, rare episodes of short-term orthostatic hypotension can occur which occur within 4 hours after its administration, pass independently when the patient is placed in the supine position and is not a contraindication to further treatment.
Due to the lack of clinical data for long-term treatment with teriparatide, the recommended treatment period should not exceed 24 months.
Special patient groups
In patients with hypercalcemia, the effect was not studied, therefore teriparatide should not be prescribed to such patients because of the possibility of progression of hypercalcemia. Before the start of treatment, hypercalcemia should be excluded, however, regular monitoring of serum calcium concentration is not required.
In children of childhood, the effect was not studied, therefore teriparatide Do not use in children, adolescents, or young people with open epiphyseal growth zones (risk of osteosarcoma).
In patients with active course of urolithiasis, the effect was not studied. In acute its course or recent exacerbation, apply teriparatide Do not follow the risk of exacerbation of the disease.
Care should be exercised in patients with impaired renal function of moderate severity. With a mild degree of renal dysfunction, extreme caution is not required.
Data on the use of teriparatide in patients with impaired liver function are absent, and therefore teriparatide this group of patients should be treated with caution.
In patients with stable course of CHF after application of two doses of teriparatide at 20 μg clinically significant changes in pharmacokinetics, blood pressure, heart rate or other safety indicators were not revealed. Dose adjustments for the use of the drug in patients with CHF I-III functional class (according to NYHA) is not required.
Impact on the ability to drive vehicles and manage mechanisms
In some patients who took teriparatide, transient phenomena of orthostatic arterial hypotension or dizziness were noted. Patients with such symptoms should refrain from managing the vehicles and mechanisms until the symptoms disappear.