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ALERT: U.S. Boxed Warning
The FDA-approved labeling includes a boxed warning. See Warnings/Precautions section and/or refer to product labeling for additional detail.
Pronunciation
(ter i PAR a tide)
U.S. Brand Names
Index Terms
Generic Available
No
Canadian Brand Names
Pharmacologic Category
Use: Labeled Indications
Treatment of osteoporosis in postmenopausal women at high risk of fracture; treatment of primary or hypogonadal osteoporosis in men at high risk of fracture
Restrictions
An FDA-approved medication guide must be distributed when dispensing an outpatient prescription (new or refill) where this medication is to be used without direct supervision of a healthcare provider. Medication guides are available at http://www.fda.gov/cder/Offices/ODS/medication_guides.htm.
Pregnancy Risk Factor
C
Pregnancy Considerations
Adverse events were observed in animal studies; the effect on human fetal development has not been studied. Teriparatide is not indicated for use in pregnant or premenopausal women.
Lactation
Excretion in breast milk unknown/not recommended
Breast-Feeding Considerations
Indicated for use in postmenopausal women. Studies have not been conducted to determine excretion in breast milk. Not recommended for use in breast-feeding women.
Contraindications
Hypersensitivity to teriparatide or any component of the formulation
Warnings/Precautions
Boxed warnings:
• Osteosarcoma: See “Concerns related to adverse effects” below.
Concerns related to adverse effects:
• Orthostatic hypotension: May cause orthostatic hypotension; use with caution in patients at risk of this effect or in those who would not tolerate transient hypotensive episodes (cerebrovascular disease, cardiovascular disease, hypovolemia, or concurrent medication use which may predispose to hypotension/bradycardia). Transient orthostatic hypotension usually occurs within 4 hours of dosing and within the first several doses.
• Osteosarcoma: [U.S. Boxed Warning]: In animal studies, teriparatide has been associated with an increase in osteosarcoma; risk was dependent on both dose and duration. Avoid use in patients with an increased risk of osteosarcoma (including Paget's disease, prior radiation, unexplained elevation of alkaline phosphatase, or in patients with open epiphyses). Do not use in patients with a history of skeletal metastases, hyperparathyroidism, or pre-existing hypercalcemia. Exclude metabolic bone disease other than osteoporosis prior to initiating therapy. Not for use in patients with metabolic bone disease other than osteoporosis.
Disease-related concerns:
• Cardiovascular disease: Use with caution in patients with cardiovascular disease; limited data available concerning safety and efficacy.
• Hepatic impairment: Use with caution in patients with hepatic impairment; limited data available concerning safety and efficacy.
• Renal impairment: Use with caution in patients with renal impairment; limited data available concerning safety and efficacy.
• Urolithiasis: Use with caution in patients with active or recent urolithiasis.
Special populations:
• Pediatrics: Safety and efficacy have not been established in children.
Other warnings/precautions:
• Appropriate use: Use of teriparatide for longer than 2 years is not recommended.
Adverse Reactions
>10%: Endocrine & metabolic: Hypercalcemia (transient increases noted 4-6 hours postdose [women 11%; men 6%])
1% to 10%:
Cardiovascular: Chest pain (3%), syncope (3%)
Central nervous system: Dizziness (8%), depression (4%), vertigo (4%)
Dermatologic: Rash (5%)
Endocrine & metabolic: Hyperuricemia (3%)
Gastrointestinal: Nausea (9%), dyspepsia (5%), vomiting (3%), tooth disorder (2%)
Neuromuscular & skeletal: Arthralgia (10%), weakness (9%), leg cramps (3%), muscle spasm
Respiratory: Rhinitis (10%), pharyngitis (6%), dyspnea (4%), pneumonia (4%)
Miscellaneous: Antibodies to teriparatide (3% of women in long-term treatment; hypersensitivity reactions or decreased efficacy were not associated in preclinical trials)
Postmarketing and/or case reports: Acute dyspnea, allergic reactions, edema (facial/oral), hypercalcemia >11 mg/dL; injection site reactions (bleeding, bruising, erythema, pain, pruritus, swelling); urticaria
Drug Interactions
There are no known significant interactions.
Ethanol/Nutrition/Herb Interactions
Ethanol: Excessive intake may increase risk of osteoporosis.
Herb/Nutraceutical: Ensure adequate calcium and vitamin D intake.
Storage
Store at 2°C to 8°C (36°F to 46°F); do not freeze. Protect from light. Discard pen 28 days after first injection. Do not use if solution is cloudy, colored or contains solid particles.
Mechanism of Action
Teriparatide is a recombinant formulation of endogenous parathyroid hormone (PTH), containing a 34-amino-acid sequence which is identical to the N-terminal portion of this hormone. The pharmacologic activity of teriparatide is similar to the physiologic activity of PTH, stimulating osteoblast function, increasing gastrointestinal calcium absorption, increasing renal tubular reabsorption of calcium. Treatment with teriparatide increases bone mineral density, bone mass, and strength. In postmenopausal women, it has been shown to decrease osteoporosis-related fractures.
Pharmacodynamics/Kinetics
Distribution: Vd: 0.12 L/kg
Metabolism: Hepatic (nonspecific proteolysis)
Bioavailability: 95%
Half-life elimination: Serum: I.V.: 5 minutes; SubQ: 1 hour
Time to peak, serum: 30 minutes
Excretion: Urine (as metabolites)
Dosage
SubQ: Adults: 20 mcg once daily; Note: Initial administration should occur under circumstances in which the patient may sit or lie down, in the event of orthostasis.
Dosage adjustment in renal impairment: No dosage adjustment required. Bioavailability and half-life increase with Clcr <30 mL/minute.
Administration: Other
Administer by subcutaneous injection into the thigh or abdominal wall. Initial administration should occur under circumstances in which the patient may sit or lie down, in the event of orthostasis.
Monitoring Parameters
Serum calcium, serum phosphorus, uric acid; blood pressure; bone mineral density
Test Interactions
Transiently increases serum calcium; maximal effect 4-6 hours postdose; generally returns to baseline ~16 hours postdose
Patient Education
Do not take any new medication during therapy without consulting prescriber. Use injector pen and dispose of pen exactly as instructed (refer to Forteo® user manual dispensed with the medication); rotate injection sites in thigh or abdominal wall. Sit when administering to reduce possibility of falling or injury. Avoid excess alcohol (may increase risk of osteoporosis) and follow dietary instructions of prescriber. May cause dizziness (use caution when driving or engaged in potentially hazardous tasks until response to drug is known); nausea, vomiting, or upset stomach (small frequent meals or frequent mouth care may help); muscle or skeletal pain, weakness, or cramping (consult prescriber for approved analgesic). Report chest pain or palpitations; respiratory difficulty; or other persistent adverse effects. Pregnancy/breast-feeding precautions: Inform prescriber if you are or intend to become pregnant. Breast-feeding is not recommended.
Geriatric Considerations
No age-related differences in pharmacokinetics have been seen. In studies, no significant difference was seen in either efficacy or adverse effects between older patients and younger patients. Teriparatide should be considered as a last resort in patents who cannot tolerate or have not responded to other treatments for osteoporosis.
Additional Information
Teriparatide was formerly marketed as a diagnostic agent (Perithar™); that agent was withdrawn from the market in 1997. Teriparatide (Forteo®) is manufactured through recombinant DNA technology using a strain of E. coli.
Dental Health: Effects on Dental Treatment
Key adverse event(s) related to dental treatment: Tooth disorder.
Dental Health: Vasoconstrictor/Local Anesthetic Precautions
No information available to require special precautions
Mental Health: Effects on Mental Status
May cause dizziness or depression
Mental Health: Effects on Psychiatric Treatment
May cause orthostasis; use caution with psychotropics. May cause GI side effects; use caution with SSRIs.
Nursing: Physical Assessment/Monitoring
Initial administration should occur where patient may sit or lie down, in the event of orthostasis. Assess results of laboratory tests (eg, calcium and phosphorus levels) prior to and periodically during therapy. Assess therapeutic effectiveness and adverse response (eg, chest pain, hypotension, nausea, vomiting, arthralgia, leg cramps, dyspnea) at beginning of and regular intervals during therapy. Teach patient proper use (administration with injector "pen" and disposal), possible side effects/appropriate interventions (diet with adequate calcium and vitamin D), and adverse symptoms to report.
Dosage Forms
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Injection, solution:
Forteo®: 250 mcg/mL (3 mL) [prefilled syringe, delivers teriparatide 20 mcg/dose]
Pricing: U.S. (www.drugstore.com)
Solution (Forteo)
750 mcg/3 mL (3): $899.44
References
Body JJ, Gaich GA, Scheele WH, et al, “A Randomized Double-blind Trial to Compare the Efficacy of Teriparatide [Recombinant Human Parathyroid Hormone (1-34)] With Alendronate in Postmenopausal Women With Osteoporosis,” J Clin Endocrinol Metab, 2002, 87(10):4528-35.
Neer RM, Arnaud CD, Zanchetta JR, et al, “Effect of Parathyroid Hormone (1-34) on Fractures and Bone Mineral Density in Postmenopausal Women With Osteoporosis,” N Engl J Med, 2001, 344(19):1434-41.
Reeve, J, “Recombinant Human Parathyroid Hormone,” BMJ, 2002, 324(7335):435-6.
International Brand Names
Lexi-Comp.com
Last full review/revision August 2008
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