What Is Teriparatide?

Teriparatide stimulates bone formation and bone resorption, which can reduce the incidence of fractures in postmenopausal women. Depending on the method of administration, it can also increase or decrease bone density. Continuous infusion can lead to a continuous increase in parathyroid hormone PTH concentration, and therefore a stronger bone resorption effect than a daily injection that only causes a transient increase in serum parathyroid hormone PTH concentration. In addition, this drug does not inhibit the platelet aggregation response of the adenosine diphosphate induction pathway or the collagen induction pathway.

Drug Name: Teriparatide

Foreign name: Teriparatide acetate
Drug type: Treatment of osteoporosis drugs

· Teriparatide · General Information

Chinese name: teriparatide

Chinese alias: teriparatide acetate / recombinant human parathyroid hormone (1-34); teriparatide acetate; teriparatide acetate 52232-67-4

English name: Teriparatide acetate

English alias: Teriparatide Acetate; Teriparatideacetate; Parathyroid Hormone Fragment 1-34 human; Parathyroid Hormone Fragment (1-34); PARATHYROID HORMONE (PTH) HUMAN 1-34, MIN 95%;

PARATHYROID HORMONE (1-34); Teriparatide acetate / Human PTH (1-34); Parathyroid hormone (1-34) (human); Parathyroid Hormone (1-34), human; LTS05731 PTH (1-34) (HUMAN) ACETATE; Teriparatideacetate / HumanPTH (1-34); Teripartide acetate; PARATHYROID HORMONE (1-34) HUMAN; PTH (1-34) (HUMAN); PTH (1-34) (HUMAN); Teriparatide

CAS number: 52232-67-4

Molecular formula: C ₁₈₁ H ₂₉₁ N ₅₅ O ⁵¹ S ₂ .C ₂ H ₄ O ₂

Molecular weight: 4177.77000 ^[1]

Teriparatide Teriparatide Related Drug Sheet Information

Teriparatide pharmacological effects

This drug [hPTH (1-34)] is a synthetic peptide hormone, a 1-34 amino acid fragment of human parathyroid hormone PTH, which is an endogenous parathyroid hormone PTH containing 84 amino acids with biological activity N-terminal region. The immunological and biological characteristics of this medicine are completely the same as endogenous parathyroid hormone PTH and bovine parathyroid hormone PTH (bPTH). This medicine stimulates bone formation and bone resorption, can reduce the incidence of fractures in postmenopausal women, and can also increase or decrease bone density depending on the method of administration. Continuous infusion can lead to a continuous increase in parathyroid hormone PTH concentration, and therefore a stronger bone resorption effect than a daily injection that only causes a transient increase in serum parathyroid hormone PTH concentration. In addition, this drug does not inhibit the platelet aggregation response of the adenosine diphosphate induction pathway or the collagen induction pathway.

Pharmacokinetics

The drug reaches its peak blood concentration 0.5 hours after subcutaneous injection, and it takes effect within 3 months (bone mineral density), and the bioavailability is 95%. The duration after a single intramuscular injection was 6 hours. The volume of distribution after intravenous injection was 0.1 L / kg. This medicine may be broken down into fragments by liver non-specific proteolytic enzymes, and then excreted by the kidney, with a renal clearance of 90%. The overall clearance of this drug is about 90L / h for men and about 60L / h for women. The parent compound elimination half-life is 1 hour for subcutaneous administration and 5 minutes for intravenous administration.

Dosage form and specifications

Teriparatide injection 3ml: 750µg. ^[2]

Teriparatide indications

For primary osteoporosis and hypogonadal osteoporosis, postmenopausal osteoporosis.

Teriparatide contraindications

Those who are allergic to this product are prohibited.

Teriparatide considerations

1. Use with caution: (1) active or newly occurring urolithiasis. (2) Patients with tumor bone metastasis or history of bone malignancy. (3) Metabolic bone diseases other than osteoporosis. (4) Open callus. (5) Patients with Paget's disease. (6) Previous patients with hypercalcemia. (7) Those who have previously received bone radiation therapy. (8) Those with unknown causes of increased alkaline phosphatase. (9) Patients with an increased baseline risk of osteosarcoma. 2. The impact of drugs on children: Children's medication safety data are limited and should be used with caution. 3. The impact of the drug on pregnancy: The US Food and Drug Administration (FDA) has rated the drug's pregnancy safety as C. The safety of pregnant women's medication is not clear, and the advantages and disadvantages of pregnant women's medication should be weighed. 4. The effect of the drug on breastfeeding: It is not clear whether the drug is secreted into the milk. The drug should be weighed against the pros and cons in the breastfeeding women. 5. Check and monitor before and after administration and during administration: (1) Serum calcium, phosphorus and urine calcium concentrations (changes in serum 1,25-dihydroxyvitamin D, calcium ions, and phosphate concentrations in patients should be detected after intravenous infusion). (2) Detection of specific indicators of bone formation and bone resorption [such as serum bone-specific alkaline phosphatase (bone formation), procollagen 1-carboxy-terminal propeptide (bone formation), urine N-terminal peptide (bone resorption)]. (3) Determination of bone mineral density (absorptiometry). (4) Test whether the patient has hypothyroidism. 6. Subcutaneous administration may cause orthostatic hypotension, and patients should give the initial dose while sitting or lying down. 7. This medicine is not recommended for more than 2 years. 8. Patients should use this medicine with caution when receiving digitalis treatment.

Teriparatide adverse reactions

1. Cardiovascular system: decreased blood pressure (including symptomatic orthostatic hypotension, caution should be used when the symptoms occur), which usually occurs when starting several doses. 2. Central nervous system: dizziness (8%), depression (4%), numb tingling sensation (less than 2%), and transient and mild headache are visible. 3. Metabolic / endocrine system: increased blood calcium (transient increase, 6% for men, 11% for women), decreased blood calcium (only case report), increased blood uric acid (about 3%), parathyroid glands Functional decline (only case reports). 4. Musculoskeletal System: This medicine can cause leg pain spasms (3%) and joint pain (10%) when treating osteoporosis. 5. Gastrointestinal tract: When treating osteoporosis with this medicine, 8.5% of patients develop nausea. Nausea, abdominal cramps, desire to defecate, diarrhea, and metallic taste in the mouth occur in less than 2% of patients using this medicine acetic acid injection. 6. Skin: Pain (intravenous injection), erythema (intradermal, subcutaneous injection), pruritus (subcutaneous injection), urticaria (intramuscular injection) can be seen during injection. 7. Others: About 3% of osteoporosis patients develop anti-teriparatide antibodies 1 year after administration [patients do not appear to have adverse sequelae or reduced drug efficacy (such as bone mineral density)].

Teriparatide dosage

1. Conventional dose: (1) Intravenous infusion: Osteoporosis: The rate is 75ng / (kg · h) for 24 hours. (2) Intramuscular injection: osteoporosis: 100 g per day for 5 to 6 months. (3) Subcutaneous injection: Postmenopausal osteoporosis in women or primary or hypogonadal osteoporosis in men: The recommended dose is 20 µg / time, once per day. 2. Dose at renal insufficiency: The single dose pharmacokinetics of patients with mild to moderate renal impairment will not be significantly affected, which suggests that these patients do not need to adjust the dosage. Patients with severe renal impairment observed significant elimination half-life and a significant increase in the area under the curve (about 75%), and it is unclear whether it caused an increase in the incidence of clinically-related adverse reactions, and there are no guidelines for dosage. 3. Dose for the elderly: In the range of 31 to 85 years old, increasing age has no significant effect on the pharmacokinetics of this drug, and there is no need to adjust the dose ^[3] . 4. Orally, 10 mg (1 tablet) each time, twice daily, or 20 mg (2 tablets) each time, twice daily.