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Actonel - Clinical Pharmacology



Mechanism of Action:

ACTONEL has an affinity for hydroxyapatite crystals in bone and acts as an antiresorptive agent. At the cellular level, ACTONEL inhibits osteoclasts. The osteoclasts adhere normally to the bone surface, but show evidence of reduced active resorption (e. g., lack of ruffled border).
Histomorphometry in rats, dogs, and minipigs showed that ACTONEL treatment reduces bone turnover (activation frequency, i. e., the rate at which bone remodeling sites are activated) and bone resorption at remodeling sites.



Absorption after an oral dose is relatively rapid (tmax ~1 hour) and occurs throughout the upper gastrointestinal tract. The fraction of the dose absorbed is independent of dose over the range studied (single dose, 2.5 to 30 mg; multiple dose, 2. 5 to 5 mg). Steady-state conditions in the
serum are observed within 57 days of daily dosing. Mean absolute oral bioavailability of the 30-mg tablet is 0.63% (90% CI: 0.54% to 0.75%) and is comparable to a solution.

The extent of absorption of a 30-mg dose (three 10-mg tablets) when administered 0.5 hours before breakfast is reduced by 55% compared to dosing in the fasting state (no food or drink for 10 hours prior to or 4 hours after dosing). Dosing 1 hour prior to breakfast reduces the extent of absorption by 30% compared to dosing in the fasting state. Dosing either 0.5 hours prior to breakfast or 2 hours after dinner (evening meal) results in a similar extent of absorption. ACTONEL is effective when administered at least 30 minutes before breakfast.
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