NSAID: Diclofenac

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Description,Types, Sid-effects,Non-steroidal anti-inflammatory drug,Contraindication


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DiCLOFENAC 1/23/2013 Faisal Asif 1

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Faisal Asif State University of Bangladesgh UG08-15-09-043 15 th batch. 1/23/2013 2


Description Diclofenac Tablets are a benzeneacetic acid derivative. The chemical name is 2-[(2,6-dichlorophenyl)amino] benzeneacetic acid, monosodium salt. The molecular weight is 318.14. Its molecular formula is C14H10Cl2NNaO2, and it has the following structural formula: Synonyms Diclofenac Acid Diclofenac Potassium Diclofenac Sodium ISV-205 1/23/2013 3

Mechanism of action:

Mechanism of action The anti-inflammatory effects of diclofenac are believed to be due to inhibition of both leukocyte migration and the enzyme cyclooxygenase (COX-1 and COX-2), leading to the peripheral inhibition of prostaglandin synthesis. As prostaglandins sensitize pain receptors, inhibition of their synthesis is responsible for the analgesic effects of diclofenac. Antipyretic effects may be due to action on the hypothalamus, resulting in peripheral dilation, increased cutaneous blood flow, and subsequent heat dissipation . 1/23/2013 4

Pharmacodynamics :

Pharmacodynamics Diclofenac Sodium Extended-release Tablets are a no steroidal anti-inflammatory drug (NSAID) that exhibits anti-inflammatory, analgesic, and antipyretic activities in animal models. The mechanism of action of Diclofenac Sodium Extended-release Tablets, like that of other NSAIDs, is not completely understood but may be related to prostaglandin synthetize inhibition. 1/23/2013 5

Absorption :

Absorption Diclofenac is 100% absorbed after oral administration compared to IV administration as measured by urine recovery. However, due to first-pass metabolism, only about 50% of the absorbed dose is systemically available (see Table 1 ). When Diclofenac Sodium Extended-release Tablets are taken with food, there is a delay of 1 to 2 hours in the Tmax and a two-fold increase in Cmax values. The extent of absorption of diclofenac, however, is not significantly affected by food intake. Table 1. Pharmacokinetic Parameters for Diclofenac PK Parameter Normal Healthy Adults (18 to 48 yrs.) Mean Coefficient of Variation (%) Absolute Bioavailability (%) [N = 7] 55 40 Tmax ( hr ) [N = 12] 5.3 28 Oral Clearance (CL/F; mL/min) [N = 12] 895 56 Renal Clearance (% unchanged drug in urine) [N = 7] <1 – Apparent Volume of Distribution (V/F; L/kg) [N = 56] 1.4 58 Terminal Half-life (hr) [N = 56] 2.3 48 1/23/2013 6


Types Voltaren injection (Diclofenac Injection) 3ml: 75 mg Manufacturer COMPOSITION: Each ml contains: Diclofenac sodium ……………………………..25mg Diclofenac Potassium Paracetamol Tablets Diclofenac potassium……..100mg Paracetamol ……………..500mg 1/23/2013 7


Type……. Composition. Each Lofnac 100 mg Enteric Coated Tablet contains: DICLOFENAC SODIUM USP 100 mg Each Lofnac 50 mg Enteric Coated Tablet contains: DICLOFENAC SODIUM USP 50 mg Diclofenac Sodium Complex Vitamin B Tablets dolo -META B tablet s (Vitamins B1+B6+B12+Diclofenac Sodium) COMPOSITION: Each film-coated tablet contains Diclofenac Sodium 50mg Vitamin B1 50 mg Vitamin B6 100mg Vitamin B12 100 mcg Diclofenac Cream 1% Each gram of the cream contains 10mg of Diclofenac sodium 1/23/2013 8

How should I take diclofenac? :

How should I take diclofenac? Take diclofenac exactly as prescribed by your doctor. Do not take in larger or smaller amounts or for longer than recommended. Follow the directions on your prescription label. If you switch brands of diclofenac, your dose needs may change. Follow your doctor's instructions about how much medicine to take . Call your doctor if your headache does not completely go away after taking Cambia. Do not take a second dose of diclofenac powder without your doctor's advice. Do not crush, chew, or break an enteric-coated pill. Swallow the pill whole. The enteric-coated pill has a special coating to protect your stomach. Breaking the pill could damage this coating. If you use diclofenac long-term, your liver function will need to be checked with frequent blood tests. Visit your doctor regularly. Store diclofenac at room temperature away from moisture and heat. 1/23/2013 9

Route of elimination:

Route of elimination Diclofenac is eliminated through metabolism and subsequent urinary and biliary excretion of the glucuronide and the sulfate conjugates of the metabolites. Little or no free unchanged diclofenac is excreted in the urine. Approximately 65% of the dose is excreted in the urine and approximately 35% in the bile as conjugates of unchanged diclofenac plus metabolites. 1/23/2013 10

Contraindications :

Contraindications Hypersensitivity against diclofenac History of allergic reactions ( bronchospasm , shock , rhinitis , urticaria ) following the use of aspirin or another NSAID Third-trimester pregnancy Active stomach and/or duodenal ulceration or gastrointestinal bleeding Inflammatory intestinal disorders such as Crohn's disease or ulcerative colitis Recently , a warning has been issued by the FDA not to use for the treatment of patients recovering from heart surgery Severe liver insufficiency (Child-Pugh Class C) Severe renal insufficiency ( creatinine clearance <30 ml/min) Caution in patients with pre-existing hepatic porphyria , as diclofenac may trigger attacks Caution in patients with severe, active bleeding such as cerebral hemorrhage NSAIDs in general should be avoided during dengue fever , as it induces (often severe) capillary leakage and subsequent heart failure. 1/23/2013 11

Diclofenac – the mystery solved :

Diclofenac – the mystery solved Although the drug, diclofenac, has been used in human medicine for decades, it has only recently been introduced for veterinary use in India and Pakistan. Vultures appear to have been exposed to the drug while scavenging livestock carcasses . Several anomalies remained with the new theory: experiments suggested that diclofenac had a rapid effect on birds, with death following a few days after exposure, while birds observed in the field lingered for several weeks. As few as one in 760 carcasses containing diclofenac at a dose lethal to vultures would be sufficient to cause the observed decline in vulture numbers (30% per year). Clearly, even small-scale usage of the drug can have catastrophic consequences . 1/23/2013 12

References :

References http:// www.drugbank.ca/drugs/DB00586 23.1.2013 http:// en.wikipedia.org/wiki/Diclofenac#Trade_names 20.2013 http:// www.drugs.com/diclofenac.html 20.1.2013 http:// www.birdlife.org/action/science/species/asia_vulture_crisis/diclofenac.html 23.1.2013 1/23/2013 13

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