Mycalcitonin

Synthetic salmon calcitonin.

Chemistry Properties: Calcitonin is a polypeptide hormone secreted by the parafollicular cells (C cells) of the thyroid gland in mammals. Calcitonin, from any source, is a 32-amino acid polypeptide chain with a disulfide bridge and a molecular weight of about 3600. Prolinamide at the carboxyl terminus, glycine at position 28, and 7 of the first 9 amino acids are common to all calcitonins, but the remaining amino acid sequence may differ considerably from that of human calcitonin, depending on the species.
Mycalcitonin contains a chemical synthetic polypeptide of 32-amino acids in the same linear sequence that found in salmon origin, calcitonin. Potency of salmon calcitonin is expressed in term of International Unit (IU). Each activation of metered dose spray will deliver 0.09 mL of Mycalcitonin solution which contains salmon calcitonin 200 IU.

Pharmacology: Pharmacodynamics/Pharmacokinetics: The hypocalcemic and hypophosphatemic effects of calcitonin are caused predominantly by direct inhibition of osteoclastic bone resorption. Some evidence suggests that calcitonin stimulates formation of bone by osteoblasts. Although calcitonin inhibits the effects of parathyroid hormone (PTH) on osteolysis, it does not act as a global inhibitor of PTH. It does not block activation of bone-cell adenylyl cyclase by PTH and does not inhibit PTH-induced uptake of Ca²⁺ into bone. The actions of calcitonin are not blocked by inhibitors of RNA and protein synthesis. Calcitonin interacts directly with receptors on osteoclasts to produce a rapid and profound decrease in ruffled border surface area, thereby diminishing resorptive activity.
Depressed bone resorption leads to reduced urinary excretion of Ca²⁺, Mg²⁺, and hydroxyproline. Plasma phosphate concentrations also are lowered, due also to increased urinary phosphate excretion. Direct renal effects of calcitonin vary with species. In human beings, calcitonin promotes excretion of Ca²⁺, phosphate, and Na⁺.

Pain Associated with Acute Osteoporotic Vertebral Compression Fractures; Paget's Disease.

Intranasal: Pain Associated with Acute Osteoporotic Vertebral Compression Fractures: 200 IU daily.
Paget's Disease: 200 IU daily although 200 IU twice daily may be required initially in a few cases. Dose reduction may also be attempted after a time in patients using the intranasal form of therapy.
Alternating nostrils daily is recommended for nasal spray administrations.

There have been no evidences of severe adverse reactions due to overdosage.

Hypersensitivity to calcitonin and/or compositions of Mycalcitonin.

As a polypeptide, calcitonin very occasionally causes local or generalized hypersensitivity reactions. In patients with a history of such reactions, a skin test before beginning treatment with the drug may be needed.
Nasal examinations should be performed before treatment begins and any time that nasal complaints occur.
Chronic rhinitis may increase the bioavailability of the intranasally administered calcitonin and patients with this condition should be carefully monitored if they are using the nasal spray.
There is report that long-term use of calcitonin raises cancer risk.
Use in Children: Human calcitonin or salmon calcitonin has been used rarely in children with Juvenile Paget's Disease, but the relationship of these pediatric bone disorders to Paget's Disease in adults has not been established. Currently, there are inadequate safety and efficacy data to support the use of calcitonin in children.

Animal reproduction studies have not been performed with human calcitonin, but salmon calcitonin has been shown to decrease fetal birth weight in rabbits when given in dosages 14-56 times the recommended human dosage. Because calcitonin does not cross the placenta, this adverse fetal effect may result from metabolic effects of calcitonin in the pregnant animal. It is not known whether human calcitonin or salmon calcitonin can cause fetal harm when administered to pregnant woman, and the drugs should be used during pregnancy only when the potential benefits justify the possible risks to the fetus.
There is the evidence that calcitonin passes into breast milk although drug distributed into milk and ingested by the infant is likely to be inactivated in the GI tract and therefore unlikely to be absorbed by the nursing infant. Because studies to determine GI absorption of calcitonin in nursing infants have not been performed to date, calcitonin is not recommended for nursing mother.

Nausea and vomiting are common. Side effects are less common with the intranasal than with the injectable form.

There are no known interactions with other drugs.

Instructions For Use: Please read the instructions and the different parts of nasal spray carefully, to know how to use the nasal spray.
The different parts of the nasal spray: 1. Cap: Protects contamination. Replace the cap every time after used.
2. Jet: The tiny hole from which the medicine sprays out.
3. Nozzle: The part the patient inserts into the nostril.
4. Pump: The part the patient presses down to operate the spray.
5. Counter (for 14 doses only): Display the status for ready to use and display how many puffs the patient has already taken.
6. Dip tube: The tube inside the spray bottle that draws up the medicine when the patient presses the pump.
7. Bottle: Contains enough medicine for at least 14 or 28 metered doses.
Using the nasal spray: Remove the cap.
Do not shake the nasal spray bottle.
Bend the head forward slightly and insert the nozzle into one of the nostrils. Try to hold the nasal spray upright.
Press the pump firmly once only and breathe in deeply through the nostril to keep the medicine in the nose.
If the patient takes two puffs at a time, repeat this procedure for the other nostril.
After use, clean the nozzle with a tissue paper and replace the cap.
Checking the counter (for 14 doses only): Every time the patient uses the nasal spray, the number in the dose counter window will change. The displayed number tells how many puffs the patient has already taken. The nasal spray is guaranteed to deliver 14 metered doses. The patient may be able to obtain 2 additional doses.
When the dose counter window shows a red 16, 16 puffs have been used and the nasal spray is finished. The patient may notice that a little medicine is left in the nasal spray bottle, but this is normal.
Preparing a new nasal spray for use: NEVER shake the nasal spray bottle as this could cause air bubbles which may affect the dose (for 28 doses only).
First, remove the cap.
Hold the nasal spray bottle upright in one or two hands and press down firmly on the pump 3 times.
This primes the new nasal spray bottle by clearing air out of the dip tube. The patient will only need to do this once when starting a new nasal spray bottle.
Do not worry if a little medicine sprays out, this is normal.
Always follow the doctor's instructions.
14 doses: As the patient presses the pump, watch the changes in the dose counter window.
When a green is showing in the counter window, the new nasal spray is ready to use.
Follow the instructions for 'Using the nasal spray'.

Unopened nasal spray bottle should be kept in a refrigerator (2-8°C). Once opened, the nasal spray bottle must be kept at room temperature; it should be kept in the upright position and used for a maximum of 4 weeks.

Agents Affecting Bone Metabolism

H05BA01 - calcitonin (salmon synthetic) ; Belongs to the class of anti-parathyroid hormones, calcitonin preparations. Used in the management of calcium homeostasis.

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