DRUGS & SUPPLEMENTS
NSAIDs, a derivative of phenylacetic acid, Diclofenac has a pronounced anti-inflammatory, analgesic and mild antipyretic effect. The mechanism of action is associated with inhibition of COX activity - the main enzyme metabolism of arachidonic acid, which is a precursor of prostaglandins, which play a major role in the pathogenesis of inflammation, pain and fever. Analgesic effect is due to two mechanisms: peripheral and central (due to inhibition of prostaglandin synthesis in the central and peripheral nervous system).
Inhibits synthesis of proteoglycan in cartilage.
In rheumatic diseases, Diclofenac reduces joint pain at rest and in motion, as well as morning stiffness and swelling of the joints, helps to increase range of motion; reduces post-traumatic and postoperative pain, and inflammatory edema.
Inhibits platelet aggregation. With prolonged use has a desensitizing effect.
When used topically in ophthalmology reduces swelling and pain in inflammatory processes non-infectious etiology.
After intake is absorbed from the gastrointestinal tract. Eating slows down the rate of absorption, extent of absorption is not changed. About 50% of the active substance is metabolized in the "first passage" through the liver. When used rectally absorption is slower. Time to reach Cmax in plasma after oral administration is 2-4 hours depending on the used dosage form, after rectal - 1 h, I.M. administration - 20 min. The concentration of active substance in plasma is a linear function of the applied dose.
Not cumulative. Plasma protein binding is 99.7% (predominantly albumin). Penetrates into synovial fluid, Cmax is achieved in 2-4 hours later than in plasma.
To a large extent metabolized to form several metabolites, among which two pharmacologically active, but to a lesser extent than Diclofenac.
Systemic clearance of the active substance is about 263 ml / min. T1/2 from plasma is 1-2 h, from synovial fluid - 3-6 h. Approximately 60% of the dose was excreted as metabolites by the kidneys, less than 1% excreted in the urine as unchanged, while the rest is displayed in the form of metabolites with bile.
Why is Diclofenac prescribed?
Articular syndrome, degenerative and chronic inflammatory diseases of musculoskeletal system (osteochondrosis, osteoarthritis, periartropatii), post-traumatic inflammation of soft tissue and musculoskeletal system (sprains, bruises). Pain in the spine, neuralgia, myalgia, arthralgia, pain and inflammation after surgery or injury, pain in gout, migraine, algomenorrhea, pain with Bursitis, proctitis, colic (biliary and renal), pain in infectious and inflammatory diseases of ENT organs.
For local use: the inhibition of miosis during surgery for cataract prevention of cystoid macular edema associated with removal and lens implantation, inflammatory eye non-infectious nature, post-traumatic inflammation in penetrating and nonpenetrating wound of the eyeball.
Dosage and administration
For oral use for adult single dose is 25-50 mg 2-3 times / 24 h. Frequency of admission depends on the dosage form employed, the severity of the disease and is 1-3 times / 24 h, rectally - 1 times / 24 h, for the treatment of acute conditions or the exacerbation of chronic edema use intramuscular in dose of 75 mg.
For children older than 6 years and adolescents daily dose is 2 mg / kg.
Topical applied at a dose of 2-4 g (depending on the size of painful area) on the affected area 3-4 times / 24 h.
When used in ophthalmology frequency and duration of administration are determined individually.
The maximum oral daily dose for adults is 150 mg.
Diclofenac side effects
Digestive system: nausea, vomiting, anorexia, abdominal pain and discomfort in the epigastrium, flatulence, constipation, diarrhea, and in some cases - erosive-ulcerative lesions, gastrointestinal bleeding and perforation; rarely - abnormal liver function. When rectal administration - in isolated cases were observed inflammation of the colon bleeding, exacerbation of ulcerative colitis.
From the side of the central nervous system and peripheral nervous system: dizziness, headache, agitation, insomnia, irritability, fatigue, rarely - paresthesia, visual disturbances, tinnitus, insomnia, cramps, irritability, tremors, mental disorders, depression.
Hemopoietic system: rarely - anemia, leukopenia, thrombocytopenia, agranulocytosis.
Urinary system: rarely - renal failure; in predisposed patients may be swelling.
Dermatological reactions: rarely - hair loss.
Allergic reactions: skin rash, itching, when used in the form of eye drops - itching, redness, photosensitivity.
Local reactions: in the place of I.M. introducing possible burning, in some cases - the formation of infiltration, abscess, necrosis of adipose tissue in the rectal administration may be local irritation, the appearance of mucous discharge mixed with blood, painful defecation, when used externally, in rare cases - itching, redness, rash, burning sensation, when applied topically in ophthalmology may be a transient burning sensation and / or temporary blurred vision immediately after instillation.
With long-term topical use and / or drawing on a vast surface of body are possible systemic side effects due to resorptive action of Diclofenac.
known hypersensitivity to Diclofenac sodium or to any accessory ingredient that is part of the drug Diclofenac;
anamnestic information about the attacks of bronchial asthma, urticaria, acute rhinitis associated with the use of aspirin or other NSAIDs;
hemodyscrasia unknown origin;
children under 6 years
pregnancy (III trimester);
increased sensitivity to sulfite (for injection solution).
children under age 15 - tablets of 50 mg to 18 years - injection.
Using during pregnancy and breastfeeding
Use during pregnancy and lactation is possible in cases where the potential benefits for the mother exceeds than the potential risk to the fetus or newborn.
With extreme caution is used in diseases of liver, kidney, gastrointestinal history, dyspepsia, asthma, hypertension, heart failure, after major surgery, as well as elderly patients.
When referring to a history of allergic reactions to NSAIDs Diclofenac and sulfites are used only in urgent cases. In the course of treatment requires systematic monitoring of liver function and kidney picture of peripheral blood.
Do not recommended the use for rectal patients with diseases of anorectal region or anorectal bleeding in history. Topical should be applied only to intact skin areas.
Avoid contact with Diclofenac in the eye, or on mucous membranes. Patients who use contact lenses, eye drops should be applied no earlier than 5 minutes after removing the lenses.
Not recommended for children under 6 years.
During the period of treatment drugs for systemic use is not recommended alcohol consumption.
During the period of treatment may decrease the speed of psychomotor reactions. With worsening blurred vision after application of eye drops should not be driving and doing other potentially danger activities.
Diclofenac drug interactions
At simultaneous application with Diclofenac antihypertensive drugs may be weakening their actions.
There are few reports on the occurrence of seizures in patients taking both NSAIDs and antibacterial drugs quinolic series.
At simultaneous application with GCS and increased risk of side effects from the digestive system.
With simultaneous use of diuretics may decrease diuretic effect. With the simultaneous use of potassium-sparing diuretics may increase the concentration of potassium in the blood.
With simultaneous use with other NSAIDs may increase the risk of side effects.
There are reports of hypoglycemia or hyperglycemia in patients with diabetes who engaged in Diclofenac together with hypoglycemic drugs.
When applied simultaneously with acetylsalicylic acid may decrease the concentration of Diclofenac in plasma.
Although clinical studies have not found the influence of Diclofenac on the action of anticoagulants, describes the individual cases of bleeding when used with Diclofenac and warfarin.
With simultaneous use may increase digoxin, lithium, and phenytoin in blood plasma.
The absorption of Diclofenac from the gastrointestinal tract is reduced by simultaneous application with kolestiraminom, to a lesser extent - with colestipol.
With simultaneous use may increase the concentration of methotrexate in plasma and increased its toxicity.
With simultaneous application of Diclofenac could not affect the bioavailability of morphine, but the concentration of the active metabolite of morphine may be enhanced in the presence of Diclofenac, which increases the risk of side effects metabolites of morphine, including respiratory depression.
When applied simultaneously with pentazocine described a case of great convulsions, and rifampicin - may decrease the concentration of Diclofenac in plasma, with ceftriaxone - increases excretion of ceftriaxone in bile; with cyclosporine - may increase cyclosporine nephrotoxicity.
Diclofenac in case of emergency / overdose
Symptoms: may cause hypotension, renal failure, convulsions, gastrointestinal irritation or respiratory depression. Treatment: There is no specific antidote. In acute poisoning as soon as possible to stop drug absorption from the gastrointestinal tract. There is indicated gastric lavage, activated charcoal appointment and conduct of other symptomatic and supportive therapy. The use of forced diuresis, dialysis or blood transfusion is not justified because NSAIDs largely associated with serum proteins and possess extensive metabolism.
In a dry, protected from light place, at temperature not above 25°C.Common expiration date for Diclofenac tablets: 3 years.
Diclofenac pharmaceutical active ingredients containing related brand and generic drugs:
Active ingredient is the part of the drug or medicine which is biologically active. This portion of the drug is responsible for the main action of the drug which is intended to cure or reduce the symptom or disease. The other portions of the drug which are inactive are called excipients; there role is to act as vehicle or binder. In contrast to active ingredient, the inactive ingredient's role is not significant in the cure or treatment of the disease. There can be one or more active ingredients in a drug.
Diclofenac available forms, composition, doses:
Form of the medicine is the form in which the medicine is marketed in the market, for example, a medicine X can be in the form of capsule or the form of chewable tablet or the form of tablet. Sometimes same medicine can be available as injection form. Each medicine cannot be in all forms but can be marketed in 1, 2, or 3 forms which the pharmaceutical company decided based on various background research results.
Composition is the list of ingredients which combinedly form a medicine. Both active ingredients and inactive ingredients form the composition. The active ingredient gives the desired therapeutic effect whereas the inactive ingredient helps in making the medicine stable.
Doses are various strengths of the medicine like 10mg, 20mg, 30mg and so on. Each medicine comes in various doses which is decided by the manufacturer, that is, pharmaceutical company. The dose is decided on the severity of the symptom or disease.
Diclofenac destination | category:
Destination is defined as the organism to which the drug or medicine is targeted. For most of the drugs what we discuss, human is the drug destination.
Drug category can be defined as major classification of the drug. For example, an antihistaminic or an antipyretic or anti anginal or pain killer, anti-inflammatory or so.
Diclofenac Anatomical Therapeutic Chemical codes:
A medicine is classified depending on the organ or system it acts [Anatomical], based on what result it gives on what disease, symptom [Therapeutical], based on chemical composition [Chemical]. It is called as ATC code. The code is based on Active ingredients of the medicine. A medicine can have different codes as sometimes it acts on different organs for different indications. Same way, different brands with same active ingredients and same indications can have same ATC code.
Diclofenac pharmaceutical companies:
Pharmaceutical companies are drug manufacturing companies that help in complete development of the drug from the background research to formation, clinical trials, release of the drug into the market and marketing of the drug.
Researchers are the persons who are responsible for the scientific research and is responsible for all the background clinical trials that resulted in the development of the drug.
Frequently asked QuestionsCan i drive or operate heavy machine after consuming Diclofenac?
Depending on the reaction of the Diclofenac after taken, if you are feeling dizziness, drowsiness or any weakness as a reaction on your body, Then consider Diclofenac not safe to drive or operate heavy machine after consumption. Meaning that, do not drive or operate heavy duty machines after taking the capsule if the capsule has a strange reaction on your body like dizziness, drowsiness. As prescribed by a pharmacist, it is dangerous to take alcohol while taking medicines as it exposed patients to drowsiness and health risk. Please take note of such effect most especially when taking Primosa capsule. It's advisable to consult your doctor on time for a proper recommendation and medical consultations.Is Diclofenac addictive or habit forming?
Medicines are not designed with the mind of creating an addiction or abuse on the health of the users. Addictive Medicine is categorically called Controlled substances by the government. For instance, Schedule H or X in India and schedule II-V in the US are controlled substances.
Please consult the medicine instruction manual on how to use and ensure it is not a controlled substance.In conclusion, self medication is a killer to your health. Consult your doctor for a proper prescription, recommendation, and guidiance.
ReviewsDrugs.com conducted a study on Diclofenac, and the result of the survey is set out below. It is noteworthy that the product of the survey is based on the perception and impressions of the visitors of the website as well as the views of Diclofenac consumers. We, as a result of this, advice that you do not base your therapeutic or medical decisions on this result, but rather consult your certified medical experts for their recommendations.
One visitor reported usefulHow is the drug Diclofenac useful in reducing or relieving the symptoms? How useful is it?
According to the survey conducted by the website sDrugs.com, there are variable results and below are the percentages of the users that say the medicine is useful to them and that say it is not helping them much. It is not ideal to continue taking the medication if you feel it is not helping you much. Contact your healthcare provider to check if there is a need to change the medicine or if there is a need to re-evaluate your condition. The usefulness of the medicine may vary from patient to patient, depending on the other diseases he is suffering from and slightly depends on the brand name.
Three visitors reported time for resultsWhat is the time duration Diclofenac drug must be taken for it to be effective or for it to reduce the symptoms?
Most chronic conditions need at least some time so the dose and the drug action gets adjusted to the body to get the desired effect. The stastistics say sDrugs.com website users needed 5 days to notice the result from using Diclofenac drug. The time needed to show improvement in health condition after using the medicine Diclofenac need not be same for all the users. It varies based on other factors.
Three visitors reported age
The information was verified by Dr. Arunabha Ray, MD Pharmacology