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Thursday, 19 October 2017

Diclofenac Side effect discovery chemical structure indication

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DICLOFENAC;-


Diclofenac is a nonsteroidal anti-inflammatory drug (NSAID) taken or applied to reduce inflammation and as an analgesic reducing pain in certain conditions. 

DISCOVERY;-


The name "diclofenac" derives from its chemical name: 2-(2,6-dichloranilino) phenylacetic acid. Diclofenac was first synthesized by Alfred Sallmann and Rudolf Pfister and introduced as Voltaren by Ciba-Geigy  in 1973.
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STRUCTURE

Chemical structure:-


Medical Usease/Indication;-

Carefully consider the potential benefits and risks of diclofenac potassium tablets and other treatment options before deciding to use diclofenac potassium tablets. Use the lowest effective dose for the shortest duration consistent with individual patient treatment goals.
Diclofenac potassium/sodium tablets are indicated:
  • For treatment of primary dysmenorrhea
  • For relief of mild to moderate pain
  • For relief of the signs and symptoms of osteoarthritis
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    immage
  • For relief of the signs and symptoms of rheumatoid arthritis

Contraindications;-

·         Hypersensitivity against diclofenac
·         History of allergic reactions

Side effects;-

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ICON
· Cardiac

· Gastrointestinal

· Hepatic

· Renal

· Mental health



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IMM
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. 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.

Table Pharmacokinetic Parameters for Diclofenac;-
PK Parameter
Normal Healthy Adults (20-52 yrs.)

Mean
Coefficient of Variation (%)

Absolute Bioavailability (%) [N = 7]
55
40

Tmax (hr) [N = 65]
1.0
76

Oral Clearance (CL/F; mL/min) [N = 61]
622
21

Renal Clearance (% unchanged drug in urine) [N = 7]
<1

Apparent Volume of Distribution (V/F; L/kg) [N = 61]
1.3
33

Terminal Half-life (hr) [N = 48]
1.9
29


Pregnancy

Pregnancy Category C;-
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ICON

Reproductive studies conducted in rats and rabbits have not demonstrated evidence of developmental abnormalities. However, animal reproduction studies are not always predictive of human response. There are no adequate and well-controlled studies in pregnant women.

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This product is available in the following dosage forms:-


Capsule
Powder for Solution
Capsule, Liquid Filled
Tablet
Tablet, Enteric Coated
Tablet, Extended Release



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