Teriparatide

Subcutaneous
Osteoporosis in postmenopausal women, Primary osteoporosis in men, Hypogonadal osteoporosis in men, Corticosteroid-induced osteoporosis
Adult: In patients at high risk of fracture, or who have failed or are intolerant to other available osteoporosis therapies: 20 mcg once daily to be injected into the thigh or abdominal wall. Max duration of treatment: 24 months (a treatment course must not to be repeated over a patient's lifetime).
Renal impairment: Severe: Contraindicated.

Hypersensitivity. Pre-existing hypercalcaemia, skeletal malignancies or bone metastases, other metabolic bone diseases (e.g. Paget's disease, hyperparathyroidism), unexplained elevations of alkaline phosphatase, previous implant or external beam radiation therapy to the skeleton, hereditary disorders predisposing to osteosarcoma. Young adults with open epiphyses. Severe renal impairment. Pregnancy.

Patient with active or recent urolithiasis or underlying autoimmune disease. Young adults (including premenopausal women). Hepatic and moderate renal impairment. Lactation. Patient must be supplemented with Ca and vitamin D if dietary intake is inadequate. Concomitant use with warfarin, systemic corticosteroid, or digoxin. Monitoring Parameters Screen for elevated alkaline phosphatase or Paget's disease prior to initiation. Monitor serum Ca (draw sample at least 16 hours post-dose), urinary Ca (in patients with suspected active urolithiasis or pre-existing hypercalciuria); signs and symptoms of orthostatic hypotension; weight and height annually. Evaluate BMD at baseline and approx 1-2 years after initiation of therapy. Consider monitoring of bone turnover biochemical markers (e.g. serum procollagen type 1 N-terminal propeptide [P1NP]) at baseline, 3 months, and 6 months to assess response to treatment. Monitor for chronic back pain.

Significant: Serious calciphylaxis and worsening of previous stable cutaneous calcification; transient orthostatic hypotension, transient and minimal elevations of serum Ca or hypercalcaemia. Rarely, osteosarcoma. Blood and lymphatic system disorders: Anaemia. Cardiac disorders: Palpitations, tachycardia. Ear and labyrinth disorders: Vertigo. Gastrointestinal disorders: Nausea, vomiting, hiatus hernia, GERD, haemorrhoids, dyspepsia. General disorders and administration site conditions: Fatigue, asthenia, chest pain, mild and transient inj site events (e.g. pain, swelling, erythema, localised bruising, pruritis, minor bleeding). Immune system disorders: Hypersensitivity reactions (e.g. angioedema, anaphylaxis). Investigations: Weight increased, alkaline phosphatase increased, cardiac murmur. Metabolism and nutrition disorders: Hypercholesterolaemia, hyperuricaemia. Musculoskeletal and connective tissue disorders: Pain in limb, muscle cramps, arthralgia, myalgia, back cramp or pain. Nervous system disorders: Dizziness, headache, sciatica. Psychiatric disorders: Depression, insomnia. Renal and urinary disorders: Polyuria, urinary incontinence, nephrolithiasis, micturition urgency. Respiratory, thoracic and mediastinal disorders: Dyspnoea, emphysema, pharyngitis, pneumonia, rhinitis. Skin and subcutaneous tissue disorders: Increased sweating. Vascular disorders: Syncope.

Symptoms: Nausea, vomiting, dizziness, headache, weakness, and hypotension. Management: Supportive treatment (e.g. hydration). Monitor serum Ca and phosphorus levels.

Concomitant use with digoxin may increase the risk of digitalis toxicity due to the effect of teriparatide on serum Ca levels.

Teriparatide is a recombinant peptide identical to the N-terminal 34-amino acid sequence of endogenous PTH. It binds to the PTH receptor with the same affinity as the intact endogenous hormone and exerts similar physiologic effects as PTH, including stimulation of bone formation by direct effects on bone forming cells (osteoblasts) and increasing gastrointestinal Ca absorption, renal tubular Ca reabsorption and phosphate excretion in the kidney. Anabolic effects of teriparatide demonstrate as increase in bone strength, skeletal mass, and bone formation and resorption markers.
Absorption: Rapidly and extensively absorbed. Absolute bioavailability: Approx 95%. Time to peak plasma concentration: Approx 30 minutes.
Distribution: Volume of distribution: Approx 0.12 L/kg.
Metabolism: Intact PTH and the N-terminal 34-amino acid sequence of PTH are suspected to undergo nonspecific proteolysis in the liver.
Excretion: Via urine (as metabolites). Elimination half-life: Approx 1 hour.

Subcutaneous: Store between 2-8°C. Do not freeze. Protect from light. Once opened, store between 2-8°C for a max of 28 days.

Agents Affecting Bone Metabolism

H05AA02 - teriparatide ; Belongs to the class of parathyroid hormones and analogues. Used in the management of calcium homeostasis.