Teriparatide peptide, a revolutionary breakthrough in osteoporosis treatment, is making waves in the medical community. This synthetic form of parathyroid hormone stimulates bone formation, resulting in increased bone mineral density and reduced risk of fractures. Available in easy-to-use pen injections and cartridges, Teriparatide offers convenience alongside efficacy.
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Teriparatide is a biologically active synthetic form of parathyroid hormone. It's primarily used to treat osteoporosis, a condition that weakens bones and makes them prone to fractures. Unlike other osteoporosis medications that slow the breakdown of bone, Teriparatide works by stimulating new bone formation.
This medication is typically administered through an injection under the skin. It's often prescribed for postmenopausal women who have severe osteoporosis and for men with primary or hypogonadal osteoporosis who are at high risk for fracture. It can also be used in individuals who have failed or are intolerant to other osteoporosis therapies.
Peptide Sequence: Ser Val Ser Glu Ile Gln Leu Met His Asn Leu Gly Lys His Leu Asn Ser Met Glu Arg Val Glu Trp Leu Arg Lys Lys Leu Gln Asp Val His Asn Phe-OH
Molecular Formula: C181H291N55O51S2
Molecular Weight: 4117.77 g·mol−1
PubChem CID: 16129682
Teriparatide is indicated for the treatment of several conditions primarily related to bone health:
Osteoporosis in Postmenopausal Women: Teriparatide is often used to treat severe osteoporosis in women who are at high risk for fracture, typically postmenopausal women who have experienced at least one osteoporotic fracture.
Primary or Hypogonadal Osteoporosis in Men: This peptide is indicated for treating primary or hypogonadal osteoporosis that is severe or associated with a high risk of fracture.
Glucocorticoid-Induced Osteoporosis: It can be used to treat men and women with osteoporosis associated with sustained systemic glucocorticoid therapy (chronic steroid use).
Other forms of Osteoporosis: It may also be prescribed for individuals who have failed or are intolerant to other osteoporosis therapies.
Teriparatide works by stimulating the activity of osteoblasts, the cells responsible for building new bone. It mimics the effects of naturally occurring parathyroid hormone (PTH), which regulates bone calcium and phosphate metabolism.
Our bones are in a constant state of remodeling where old bone is broken down by cells called osteoclasts, and new bone is formed by osteoblasts. In people with osteoporosis, the balance between bone breakdown and formation is disrupted, leading to more bone being broken down than formed. This results in overall bone loss and weakened bones prone to fractures.
Teriparatide tilts the balance back towards the bone formation. When administered daily, it promotes the growth and activity of osteoblasts, leading to increased bone formation. Over time, this can increase bone mineral density and reduce the risk of fractures.
One key aspect of Teriparatide's mode of action is its dosing schedule. While natural PTH can stimulate bone formation and breakdown, the once-daily administration of Teriparatide primarily stimulates bone formation. This is because the drug's effects on osteoblasts are longer lasting than its effects on osteoclasts.
Contraindications:
Teriparatide is not recommended for individuals with open epiphyses, metabolic bone diseases, Paget's Disease of bone, bone metastases, a history of skeletal malignancies, or prior external beam or implant radiation therapy involving the skeleton. In both animal studies and one human case report, there were indications that extended use of Teriparatide for over two years might be associated with the development of osteosarcoma in test subjects.
Teriparatide should not be used in certain situations due to the potential for adverse effects. Here are the main contraindications:
Hypercalcemia: Teriparatide can increase calcium levels in the blood, so it should not be used by individuals who already have high calcium levels in their blood.
Bone Metastases or Skeletal Malignancies: Individuals with bone metastases or a history of skeletal malignancies should avoid using Teriparatide.
Prior Radiation Therapy: Those who have undergone radiation therapy involving the skeleton should not use Teriparatide because of the increased risk of osteosarcoma.
Pre-existing Hyperparathyroidism: As Teriparatide mimics the action of parathyroid hormone, it is not recommended for those with pre-existing hyperparathyroidism.
Severe Renal Impairment: Teriparatide should be used with caution in patients with severe renal impairment due to altered drug metabolism.
Pediatric and Adolescents: Teriparatide is not indicated for use in pediatric and adolescent patients as their bones are still growing.
Pregnancy and Breastfeeding: Teriparatide falls under pregnancy category C, which means it should only be used if the potential benefit justifies the potential risk to the fetus. It's not known whether Teriparatide is excreted in human milk, so caution should be exercised when administering it to a nursing woman.
Teriparatide, by mimicking the action of parathyroid hormone (PTH), plays a significant role in calcium and phosphate homeostasis. Here's how it impacts these crucial minerals:
Calcium Homeostasis: Teriparatide increases serum calcium levels by stimulating osteoblasts (bone-forming cells) and indirectly increasing the number and activity of osteoclasts (bone-resorbing cells). This leads to increased bone resorption and calcium release from the bone into the bloodstream. Additionally, Teriparatide enhances renal calcium reabsorption, increasing serum calcium levels.
The digestive system indirectly increases intestinal absorption of calcium by promoting the conversion of vitamin D into its active form (calcitriol), which is responsible for enhancing calcium absorption in the gut.
Phosphate Homeostasis: While Teriparatide increases the release of phosphate from bones into the bloodstream by stimulating bone resorption, it also enhances renal phosphate excretion. The net effect on serum phosphate levels is usually minimal, as increased bone resorption is counterbalanced by increased renal phosphate excretion.
It's important to note that while transient elevations in serum calcium levels may occur after Teriparatide administration, prolonged hypercalcemia is not typical when Teriparatide is used at the recommended dose. However, serum calcium levels should be monitored during therapy, especially in patients with conditions predisposing them to hypercalcemia.
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