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INTRODUTION OF DICLOFEN DRUG
1. M. AQIB JAVED
BS HEALTH STUDENT
PRESENTATION OF PHARMACOLGY
4/21/2018 1M. AQIB JAVED
2. Introduction of Diclofenac
Diclofenac was first synthesized by
Alfred Sallmann and Rudolf Pfister
and introduced as Voltaren by Ciba-
Geigy (now Novartis) in 1973.
It is a (NSAID) taken or applied to
reduce inflammation and as
an analgesic reducing pain in certain
conditions
.
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3. Mechanism of action
action is thought to be inhibition
of prostaglandin synthesis by inhibition
of (COX). It also appears to exhibit
bacteriostatic activity by inhibiting
bacterial DNA synthesis.
Currently, diclofenac and
acetylsalicylic acid are the only
NSAIDs to show some antibacterial
activity against Gram-negative rods.
4/21/2018 3M. AQIB JAVED
4. Actions of Dicofenac
nflammatory disorders may include
musculoskeletal complaints,
especially arthritis, rheumatoid
arthritis, polymyositis, dermatomyositis,
osteoarthritis, dental
pain, temporomandibular joint (TMJ)
pain, ankylosing, gout attacks and pain
management in cases of kidney
stones and gallstones, post-traumatic
pain, and is effective against menstrual
pain.
4/21/2018 4M. AQIB JAVED
5. Pharmacokinitics
When given orally the absorption
ofdiclofenac is rapid and complete in
GIT. Diclofenac binds extensively to
plasma albumin.
It is proportional to the dose for oral
doses between 25 to 150 mg.
But First Fast Effect greatly effect on
it.
4/21/2018 5M. AQIB JAVED
6. Distribution
distribution diclofenac sodium is 1.4
L/kg. Diclofenac is more than 99%
bound to human serum proteins,
primarily to albumin. Serum protein
binding is achieved with
recommended doses.
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7. Metabolism
Metabolism is manily done by liver.
Excretion:
the excretion of dicofenac is
mainly by the urine.
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8. Side effects
Diclofenac consumption has been
associated with significantly increased
vascular and coronary risk in a study
including coxib, diclofenac, ibuprofen
and naproxen. Upper gastrointestinal
complications were also reported.
Major vascular events were increased
by about a third by diclofenac, chiefly
due to an increase in major coronary
events.
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9. Con….
Compared with placebo, of 1000 patients
allocated to diclofenac for a year, three
more had major vascular events, one of
which was fatal. Vascular death was
increased significantly by diclofenac
Liver: damage occurs infrequently, and is
usually reversible.
NSAIDs "are associated with adverse
renal (kidney) effects caused by the
reduction in synthesis of
renal prostaglandins and may be lead to
ranal failure.
4/21/2018 9M. AQIB JAVED
10. Way of addmistration
Voltaren (diclofenac) 50 mg enteric
coatedtablets
Arthrotec (diclofenac and miosprostol)
50-mg tablets
Dyloject (diclofenac) 2 ml
for IV and IM administration
4/21/2018 10M. AQIB JAVED