The drug for treatement of osteoporosis??
Ans: Bisphosphonates. Mechanism of action
of Bisphosphonates? Ans: Bisphosphonates
block bone resorption. Bisphosphonates bind strongly to the hydroxyapatite in
the bone and interferes with osteoclasts, which are the bone cells that break
down bone. The bisphosphonate molecules are incorporated into newly formed bone
as they are analogs of pyrophosphate. Compared to other drugs, bisphosphonates
stay in the body a very long time. Most drugs are excreted or metabolized by
the body in a day or two. Bisphosphonates stay in the body for years through
cycles of bone absorption.
·
Bisphonates:--Most are taken orally,
as a pill, either once a day or once a week. Bisphosphonates can be given intravenously
5 mg IV injection performed by infusion clinic once yearly.
Such formulations are available for
patients who cannot tolerate oral bisphosphonates. Some patients cannot
sit upright for 30 to 60 minutes which is a requirement for some drugs. The
bisphosphonate zoledronate can be administered through a patch.
They have been widely used for years and
although there can be side effects; the medical profession considers them
generally safe and effective. Bisphosphonates are employed for:
·
treatment and prevention of
postmenopausal osteoporosis
·
treatment to increase bone mass
in men with
osteoporosis
·
treatment and prevention of
glucocorticoid induced osteoporosis
·
treatment of Paget’s disease
·
prevention of Skeletal Related
Events (bone problems caused by cancer metastasis)
·
treatment of the hypercalcemia of malignancy
Non-approved but known (off label)
uses
·
Vitamin D overdose
·
Osteoporosis caused by spinal
injury.
Fosamax with D (alendronate with Vitamin D) manufactured by Merck
Dosage and Forms:
·
once weekly – 70mg/5,600U tablet
·
once weekly - 70mg/2,800U tablet
Actonel (risedronate) manufactured by Procter and Gamble /
Sanofi-Aventis .The patent expired in 2011 and
generic forms are now available. Dosage and Forms:
5mg, 35mg, 75mg and 150mg tablet
·
5mg tablet daily or
·
35mg tablet weekly or
·
75mg tablet taken on 2 consecutive
days one time each month or
·
150mg tablet monthly
Non-approved but known (off label)
uses
·
Hypercalcemia
·
Bone Cancer or Bone Metastases
Residronate: Is dispensed as Resical
kit (otsira) –The small tab of Residronate have to be taken in empty stomach
with 200 ml of water and she should not lie down for 1 hr. The other tablets in
the kit are Calcium tab 1 tab BD to be
consumed on week days.
A similar product in Kit formulations are available in the name of
Xtra Cal srong Kit(Pulse). Risofos Kit (Cipla) Approx cost 100/- per Kit. The pink
tab t be taken on Sunday morning as described and rest calcium tablets to e
taken n BD schedule calcium tablets .
May be supplemented by Vit D if deficient.
Actonel with Calcium (risedronate with calcium)
Dosage and Forms:
Blister Package containing one (1) 35mg Actonel and six (6) 1250mg calcium
carbonate tablets
o Actonel taken on day 1 and calcium taken on days 2 - 7
·
The
generic ames are .
·
Alendronate (Fosamax)
·
Alendronate plus Vitamin D.
·
Risedronate (Actonel)
·
Risedronate plus Calcium.
·
Ibandronate (Boniva)
·
zoledronic acid (Reclast, Zometa)
·
Etidronate (Didronel)
·
Pamidronate (Aredia)
What
is Hydroxyapatite? Ans: Hydroxyapatite is a calcium phosphorus
compound that makes up about half of bone mass.
Alendronate (Fosamax), developed by Merck
Market Share and Sales:
Over 10 million prescriptions for alendronate were written in the US in 2016.
Merck's patent expired more than a decade ago. Generic alendronate from other
manufacturers now domainates the market.
Dosage and Forms:
10mg and 70mg tablet
·
10mg
tablet daily or
·
70mg tablet weekly
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