Solution for subcutaneous administration.
Syringe Pen 2.4 ml.
Forsteo – an analogue of parathyroid hormone. Recombinant human parathyroid hormone (PTH) obtained using the Escherichia coli strain (using DNA recombination technology). Endogenous PTH, which is a sequence of 84 amino acid residues, is the main regulator of calcium and phosphorus metabolism in bones and kidneys. Forsteo (recombinant human PTH (1-34)) is an active fragment of endogenous human PTH. The physiological effect of PTH is to stimulate the formation of bone tissue through a direct effect on osteoblasts. PTH indirectly increases intestinal absorption and tubular reabsorption of calcium, as well as excretion of phosphates by the kidneys.
The biological effect of PTH is due to binding to specific PTH receptors on the cell surface. Teriparatide binds to the same receptors and has the same effect on bones and kidneys as PTH. A single daily administration of teriparatide stimulates the formation of new bone tissue on the trabecular and cortical (periosteal and / or endosteal) surfaces of the bones with predominant stimulation of osteoblast activity relative to the activity of osteoclasts. This is confirmed by an increase in the content of markers of bone formation in blood serum: bone-specific alkaline phosphatase and procollagen-I carboxyterminal propeptide (PICP). An increase in the content of bone formation markers is accompanied by a secondary increase in the level of bone resorption markers in the urine: N-telopeptide (NTX) and deoxypyridinoline (DPD), which reflects the physiological interaction of bone formation and resorption in skeleton remodeling.
2 hours after the administration of teriparatide, a short-term increase in the concentration of serum calcium is observed, which reaches its maximum value after 4-6 hours and returns to the initial values ââwithin 16-24 hours. In addition, transient phosphaturia and a slight short-term decrease in serum phosphorus may be observed blood.
During treatment with teriparatide, bone mineral density (BMD) of the entire body increases by 5-10% (including in the lumbar spine, the neck of the femur and femur).
Mineralization processes occur without signs of toxic effects on bone tissue cells, and bone tissue formed under the influence of teriparatide has a normal structure (without formation of reticulofibrotic bone tissue and bone marrow fibrosis).
Teriparatide reduces the risk of developing fractures regardless of age, baseline bone metabolism or BMD (a relative reduction in the risk of new fractures is 65%).
Absorption and distribution of
Teriparatide is well absorbed by s / c administration. The absolute bioavailability of the drug is approximately 95%. Cmax of teriparatide is achieved 30 minutes after s / c administration of the drug at a dose of 20 Î¼g and is 4-5 times higher than the VHN level of PTH, followed by a decrease in concentration to undetectable values ââwithin 3 hours.
Vd is approximately 1.7 l / kg.
Like endogenous PTH, teriparatide does not accumulate in bones or other tissues.
Metabolism and excretion of
T1 / 2 teriparatide when s / c administration is about 1 hour, which reflects the time required for absorption.
The peripheral metabolism of PTH occurs predominantly in the liver through non-specific enzymatic mechanisms followed by kidney excretion.
Pharmacokinetics in special clinical cases
No effect of age (age group from 31 to 85 years) on the pharmacokinetics of teriparatide was noted.
In patients with mild or moderate renal failure (CC from 30 to 72 ml / min), the pharmacokinetics of the drug does not change.
Treatment of osteoporosis in postmenopausal women treatment of primary osteoporosis or osteoporosis due to hypogonadism in men.
severe renal failure
metabolic bone disease, with the exception of primary osteoporosis (including hyperparathyroidism and Paget’s disease)
increased activity of alkaline phosphatase of unknown origin
previous radiation therapy of skeletal bone
bone metastases or bone tumors
up to 18 years of age.
in patients in the acute phase of urolithiasis or who have recently experienced it, due to a possible worsening of the condition, calcium excretion with urine
should be monitored in patients with moderate impaired renal function
hypovitaminosis D, clinically significant hypocalcemia.
Use in pregnancy and lactation
The effect of teriparatide treatment on human fetal development has not been studied. You should not prescribe the drug during pregnancy.
No clinical studies have been conducted to find out if teriparatide is excreted in breast milk.
Teriparatide should not be given to nursing mothers.
1 ml of solution for subcutaneous administration contains:
teriparatide 250 mcg,
glacial acetic acid – 0.41 mg,
sodium acetate anhydrous – 0.1 mg,
mannitol – 45.4 mg,
metacresol – 3 mg,
hydrochloric acid solution 10% and / or sodium hydroxide solution 10% – qs,
water d / u – qs up to 1 ml.
Dosage and administration of
Forsteo is prescribed for adults. The dose does not depend on the age of the patient.
The recommended dose of Forsteo is 20 mcg, administered 1 time per day subcutaneously in the thigh or abdomen.
The maximum duration of treatment with Forsteo is 18 months. In the event of a break in treatment with Forsteo, patients can continue treatment with other drugs.
Additional calcium and vitamin D supplements are recommended if they are not adequately supplied with food.
The patient must be trained in the technique of administering the drug (see the instructions for use of the syringe pen).
Rules for using the syringe pen
Forsteo is a solution in the syringe pen for individual use. Each injection requires a new sterile needle. Each Forsteo package contains a Patient Guide detailing how to handle a syringe pen.
Injection needles are not included. The pen can be used with needles for insulin pens (Becton Dickinson).
The drug should be administered immediately after the syringe pen is removed from the refrigerator.
The syringe pen should be refrigerated after each injection.
Side effects of
From the musculoskeletal system: very often ( 10%) – pain in the extremities often ( 1%,
from the hematopoietic system: often ( 1%,
from the metabolism: often ( 1%,
From the nervous system: often ( 1%,
From the psyche: often ( 1%,
Cardiovascular system: often ( 1%,
From the respiratory system: often ( 1%,
From the digestive system: often ( 1%,
From skin and subcutaneous tissue: often ( 1%,
From the urinary system: rarely ( 0.1%,
Allergic reactions are very rare (<0.1%) - shortly after injection there is acute shortness of breath, swelling of the oral cavity / face, generalized rash. General reactions: often ( 1%, Local reactions: rarely ( 0.1%, overdose Symptoms: Overdosage may occur with prolonged hypercalcemia and the development of orthostatic collapse. Nausea, vomiting, dizziness, and headache are also possible. Treatment: There is no specific antidote. In case of suspected overdose, it is recommended to cancel Forsteo drug, control the serum calcium content and conduct symptomatic therapy. Storage conditions The drug should be stored out of the reach of children, in a refrigerator at a temperature of 2 Â° to 8 ° C. Do not freeze. The drug in use should be stored in the refrigerator at a temperature of 2 Â° to 8 ° C for no more than 28 days. Expiration 2 years. Deystvuyuschee substances teriparatide dosage form dosage form injection Lilly France, France