Drug Profile
2. Brand(s):
| Brand Name | Manufacturer | Dosage Form | Pack Size | MRP |
| Instaren | | Tablet | 20’s | Rs 75 |
| Instaren (SR) | | Tablet | 20’s | Rs 140 |
| Kayfen | KCL | Tablet | 50*10 | Rs 270 |
| Klodic | Nabiqasim | Tablet | 20’s | Rs 67.79 |
| Maxit | Hilton | Tablet | 20’s | Rs 95.43 |
| Maxit | Hilton | Injection | 10 Ampules | Rs 142.15 |
3. Pharmacological Group:
NSAID
4. Formulations:
Diclofenac sodium
Diclofenac potassium
5. General Information:
Diclofenac is in a group of drugs called nonsteroidal anti-inflammatory drugs (NSAIDs). Diclofenac works by reducing hormones that cause inflammation and pain in the body.Diclofenac is used to treat pain or inflammation caused by arthritis or ankylosing spondylitis.
6. Dosage Form
Solids
| Tablets◘ |
| Capsules | ||
| Hard Capsules | Soft Capsules | Modified Released Capsules |
| Uncoated Tablets◘ | Coated Tablets | Modified Released Tablets ◘ | Sublingual Tablets |
| Powders | |
| Powders for suspension | Powders for Inhalers |
| Others |
| Liquids | Syrup | Oral drops | Nasal Drops | Topical Solutions | Eye Preparations | Ear Preparations | Others |
| Parenterals Preparations ◘ | Injections ◘ | Infusions | Powders for injection | Others |
| Topical Solids | Ointment | Creams | lotions | Gels | Pastes | Others |
6. Therapeutic Uses:
Inflammation and Rheumatoid Arthritis, Painful condition in Gynaecology.
7. Information for the user:
i. How to take:
Take this medication exactly as it was prescribed for you. Do not take the medication in larger amounts, or take it for longer than recommended by your doctor. Follow the directions on your prescription label.
ii. Frequency & Time of Doses:
50-75mg qid
iii. Recommended Dosage Range:
| Neonates/ Children | Adult | Geriatric | Dose according to clinical condition |
| 0.5 to 2 mg/kg body weight in two to three divided doses | 100 to 150 mg tid | Dose should be reduced due to less functionality of Liver and kidney | |
iv. Onset of effect:
2hrs
v. Duration of Action:
6-8 hrs
vi. Diet Advice:
Drinking too much alcohol may increase the amount of uric acid in the blood and lessen the effects of Diclofenac. Taking too much vitamin C may make the urine more acidic and increase the possibility of kidney stones forming while you are taking Diclofenac. Therefore, check with your doctor before you take vitamin C while taking this medicine.
vii. Storage:
Store diclofenac at room temperature away from moisture and heat.
Viii: Missed Dose:
Take the missed dose as soon as you remember. If it is almost time for your next dose, skip the missed dose and take the medicine at your next regularly scheduled time. Do not take extra medicine to make up the missed dose.
ix. Stopping the drug:
Stopping the Drug at once after the completion of therapy may not produce any harmful symptoms but a low dose regime is required to avoid relapse.
x. Exceeding the dose (overdose):
Seek emergency medical attention if you think you have used too much of this medicine. Symptoms of a diclofenac overdose may include nausea, vomiting, stomach pain, drowsiness, black or bloody stools, coughing up blood, shallow breathing, fainting, or coma.
8. Possible Adverse Effects:
Chest pain, weakness, shortness of breath, slurred speech, problems with vision or black,
Tarry stools, nausea.
9. Contraindications:
Diclofenac tablets are contraindicated in patients with known hypersensitivity to Diclofenac.
Diclofenac tablets should not be given to patients who have experienced asthma, urticaria, or allergic-type reactions after taking aspirin or other NSAIDs. Severe, rarely fatal, anaphylactic-like reactions to NSAIDs have been reported in such patients).
10. Interactions:
| Drug-Drug Interactions | Drug-Food Interactions |
| warfarin (Comedians); cyclosporine (Neoral, Sandimmune)lithium (Eskalith, Lithobid); methotrexate (Rheumatrex, Trexall);diuretics (water pills) such as furosemide | Using alcohol or tobacco with Allopurinol may cause interactions to occur. Vit C rich food can leads to Kidney stones. |
11. Prolonged Use:
If you take diclofenac for a long period of time, your doctor may want to check you on a regular basis to make sure this medication is not causing harmful effects. Do not miss any scheduled visits to your doctor.
12. Special Precautions:
Allergic to any drugs, or if you have: a history of heart attack, stroke, or blood clot; heart disease, congestive heart failure, high blood pressure, a history of stomach ulcers or bleeding, Liver or kidney disease, Asthma, a bleeding or blood clotting disorder or if you smoke.
ii. Pregnancy:
FDA pregnancy category C. This medication may be harmful to an unborn baby. Tell your doctor if you are pregnant or plan to become pregnant during treatment. Taking diclofenac during the last 3 months of pregnancy may result in birth defects. Do not take diclofenac during pregnancy unless your doctor has told you to.
iii. Breast Feeding/Lactation:
Diclofenac can pass into breast milk and may harm a nursing baby. Do not use this medication without telling your doctor if you are breast-feeding a baby.
iv. Infants & Children:
Do not give this medicine to a child without the advice of a doctor. v. Over 60:
Elderly patient more strongly then other adults. They should take lower effective dose for their conditions.
Vi. Driving & Hazardous work:
A few patients may experience the dizziness or drowsiness or disturbance of vision. In case of such effect avoid driving and machine work.
vii. Alcohol:
Do not drink alcohol while taking diclofenac. Alcohol can increase the risk of stomach bleeding caused by diclofenac.
13. Pharmacological Properties:
13. (I). Pharmacodynamic Properties:
Diclofenac is an NSAID which is believed to work through inhibition of cyclooxygenase (COX), thus inhibiting prostaglandin synthesis. There are at least 2 variants of cyclooxygenase (COX-1 and COX-2). Diclofenac inhibits both COX-1 and COX-2. It appears that its analgesic, antipyretic, and anti-inflammatory activity are achieved principally through COX-2 inhibition; whereas COX-1 inhibition is responsible for its unwanted effects on platelet aggregation and the GI mucosa.
13. (ii). Pharmacokinetic Properties:
i. Absorption:
Completely absorbed from Gastro resistant tablet after their passage through stomach in the intestine.
ii. Distribution:
| Bioavailability | %Protein binding | Half Life | Volume of distribution | Blood Brain Barrier | Placental Barrier |
| 95% | 99.7 % | 2hrs | 0.12 to 0.5 liter/kg | | Crosses |
iii. Metabolism
| Site of Metabolism | Active Metabolites |
| Hepatic | Glucuronide conjugates. |
iv. Elimination:
| Elimination Half Life | Route of Elimination |
| 1-2 hours | 60% in urine and rest through bile and faeces as metabolites. |
15. Preclinical Safety Data:
Diclofenac did not influence neither fertility of parent animals (rats) nor the –pre –peri, and post natal development of offspring. No teratogenic effect was detected in mice, rat and rabbits.
No mutagenic effect could be demonstrated in various in vitro and in vivo experiments and no carcinogenic potential in long term studies was detected in rats and mice.
16. Instructions for Handling:
Throw away any medication that is outdated or no longer needed. Talk to your pharmacist about the proper disposal of your medication.
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