Diclofenac Uses/Diclofenac is a Nonsteroidal Anti-inflammatory Drug. The mechanism of action of diclofenac is as a Cyclooxygenase Inhibitor. The physiologic effect of diclofenac is by means of Decreased Prostaglandin Production. The chemical classification of diclofenac is Nonsteroidal Anti-inflammatory Compounds.
Diclofenac is a nonsteroidal benzene acetic acid derivative with anti-inflammatory activity. As a nonsteroidal anti-inflammatory drug (NSAID), diclofenac binds and chelates both isoforms of cyclooxygenase (COX-1 and-2), thereby blocking the conversion of arachidonic acid to pro-inflammatory-prostaglandins. This agent also may inhibit COX-2-mediated tumor angiogenesis. When inhibiting COX-2, diclofenac may be effective in relieving pain and inflammation; when inhibiting COX-1, it may produce unacceptable gastrointestinal side effects. This agent may be more active against COX-2 than several other carboxylic acid-containing NSAIDs.
Indications of Diclofenac
Diclofenac tablet is used for the treatment, control, prevention, & improvement of the following diseases, conditions and symptoms
- For the acute and chronic treatment of signs and symptoms of osteoarthritis and rheumatoid arthritis.
- Diclofenac is non-steroidal anti-inflammatory drug (NSAID), indicated in the relief of all grades of pain and inflammation associated with a wide range of conditions, including arthritic conditions, acute musculo-skeletal disorders and other painful conditions resulting from trauma.
- Osteoarthritis
- Rheumatoid arthritis
- Ankylosing spondylitis
- Pain due to specially musculoskeletal system
- Muscles stiffness in spinal
- Muscles stiffness in muscle diseases
- Muscles stiffness in the joint diseases
- Lumbago
- Low back pain
- PLID
- Pain caused by nonaticular rheutism
- Muscles stiffness in nerve diseases
- Morning stiffness
- Multiple joint pain
- Periarthritis of scapulohumerous
- Ischiadynia
Therapeutic Indications of Diclofenac
- Anti-Inflammatory Agents, Non-Steroidal; Cyclooxygenase Inhibitors
- Diclofenac sodium also is used topically as an ophthalmic solution for the treatment of postoperative ocular inflammation in patients undergoing cataract extraction.
- Oral diclofenac sodium has been used for its antipyretic effect in the management of fever, usually associated with infection.
- In one study, the antipyretic effect of usual dosages of diclofenac sodiumas delayed-release (enteric-coated) tablets was about equal to that of usual dosages of aspirin. The drug, however, should not be used routinely as an antipyretic because of its potential adverse effects.
- Diclofenac sodium as delayed-release (enteric-coated) tablets also has been used for the symptomatic relief of dysmenorrhea.
- Diclofenac potassium is used orally in the management of primary dysmenorrhea. Diclofenac potassium;
- Diclofenac also has been used parenterally (a parenteral dosage form is currently not commercially available in the US) for the relief of acute or renal colic, and for relief of postoperative pain (including that associated with gynecologic and orthopedic surgery).
- Diclofenac sodium also has been used orally for symptomatic relief of postoperative (including that associated with dental surgery), postpartum, and orthopedic (including musculoskeletal strains or sprains) pain, and visceral pain associated with cancer.
- Diclofenac epolamine transdermal system is used for symptomatic relief of acute pain due to minor strains, sprains, and contusions.
- Diclofenac potassium is used orally for symptomatic relief of postoperative pain (including that associated with orthopedic, gynecologic, and oral surgery) and orthopedic pain (including musculoskeletal sprains and traumatic joint distortions).
- Oral or topical diclofenac has been used for the symptomatic treatment of infusion-related superficial thrombophlebitis.
- Oral diclofenac also has been used for the symptomatic treatment of acute painful shoulder (bursitis and or tendinitis), sciatic pain, backache, myositis, and radiohumeral bursitis (radiohumeral epicondylitis, tennis elbow).
- The drug has been injected locally (a parenteral dosage form currently is not commercially available in the US) for the relief of myofascial pain in a limited number of patients with fibrositis, but additional study is necessary.
- Oral diclofenac has been effective in a limited number of patients for the symptomatic relief of acute gouty arthritis. The drug does not appear to correct hyperuricemia but has been used instead for its anti-inflammatory and analgesic effects to relieve pain, joint tenderness, and swelling associated with this condition.
- Diclofenac has been used orally with good results in a number of children for the management of juvenile rheumatoid arthritis.
- In the symptomatic treatment of ankylosing spondylitis, oral diclofenac appears to provide relief of spinal pain, tenderness and/or spasm, morning stiffness, and pain at rest (including night pain) and to improve motion, posture, chest expansion, and spinal mobility.
- When used in the symptomatic treatment of rheumatoid arthritis, oral diclofenac has relieved pain and stiffness; reduced swelling, tenderness, and the number of joints involved; and improved mobility and grip strength.
- In the symptomatic treatment of osteoarthritis, diclofenac has relieved pain and stiffness, improved knee joint function, and increased range of and functional activity.Diclofenac appears to be only palliative in these conditions and has not been shown to permanently arrest or reverse the underlying disease process.
- Diclofenac sodium 1% gel is used topically for the symptomatic treatment of osteoarthritis-related joint pain. The gel is used for joints amenable to topical therapy (e.g., hands, knees); the gel has not been evaluated for use on joints of the spine, hip, or shoulder.
- Diclofenac sodium in fixed combination with misoprostol is used orally for anti-inflammatory activity and analgesic effects in the symptomatic treatment of rheumatoid arthritis and osteoarthritis in patients at high risk of developing nonsteroidal anti-inflammatory agent (NSAIA)-induced gastric or duodenal ulcers and in patients at high risk of developing complications from these ulcers.
- Diclofenac sodium is used orally for anti-inflammatory and analgesic effects in the symptomatic treatment of acute and chronic rheumatoid arthritis, osteoarthritis, ankylosing spondylitis, and other inflammatory conditions.
- Diclofenac potassium is used orally for anti-inflammatory and analgesic effects in the symptomatic treatment of acute and chronic rheumatoid arthritis, osteoarthritis, ankylosing spondylitis, and other inflammatory conditions.
- Topical or oral diclofenac has been used for the symptomatic treatment of infusion-related superficial thrombophlebitis.
- Diclofenac sodium is used topically for the treatment of actinic keratoses.
Contra Indications of Diclofenac
- Active peptic ulcer
- Acute rhinitis
- Allergic to thiocolchicoside
- Asthma
- Breastfeeding
- Pregnant
- Urticaria
- Concurrent peptic ulcer, or history of ulcer disease
- Allergy to indomethacin, aspirin, or other NSAIDs
- Patients with nasal polyps reacting with an angioedema to other NSAIDs
- Children under 2 years of age (with the exception of neonates with patent ductus arteriosus)
- Some painkillers, including opioid pain killers;
- Hypnotic drugs;
- Psychotropic drugs;
- Used monoamine oxidase inhibitors (MAOIs) such as phenelzine or tranylcypromine
- Epilepsy;
- Addiction or are recovering from addiction to another medication.
- History of peptic ulcer disease,
- Gastrointestinal bleeding,
- Severe pre-existing renal and liver damage
- Caution: pre-existing bone marrow damage (frequent blood cell counts are indicated)
- Caution: bleeding tendencies of unknown origin
- Caution: Parkinson’s disease, epilepsy, psychotic disorders (indomethacin may worsen these conditions)
- Concurrent with potassium sparing diuretics
- Patients who have a patent ductus arteriosus dependent heart defect (such as transposition of the great vessels)
- Significant hypertension (high blood pressure)
- Concomitant administration of lithium salts (such as lithium carbonate)
Dosage
Strengths: sodium 25 mg; potassium 50 mg; sodium 75 mg; sodium 100 mg; sodium 50 mg; 37.5 mg/mL; potassium 25 mg; sodium; 18 mg; 35 mg
Osteoarthritis
- Diclofenac free acid capsules: 35 mg orally 3 times a day
- Diclofenac potassium immediate-release tablets: 50 mg orally 2 or 3 times a day
- Diclofenac sodium enteric-coated tablets: 50 mg orally 2 or 3 times a day or 75 mg orally 2 times a da
- Maximum dose: 150 mg daily
- Diclofenac sodium extended-release tablets: 100 mg orally once a day
Ankylosing Spondylitis
- Diclofenac sodium enteric-coated and delayed-release tablets: 25 mg orally 4 times a day. An additional 25 mg dose may be administered at bedtime, if necessary
- Maximum dose: 125 mg per day
Dysmenorrhea
- Diclofenac potassium immediate-release tablets: 50 mg orally 3 times a day
Rheumatoid Arthritis
Diclofenac potassium immediate-release tablets
- 50 mg orally 3 or 4 times a day
Diclofenac sodium enteric-coated and delayed-release tablets
- 50 mg orally 3 to 4 times a day or 75 mg orally twice a day
- Maximum dose: 225 mg daily
Diclofenac sodium extended-release tablets
- 100 mg orally once a day
- Maximum dose: 100 mg orally 2 times a day; this would be for the rare patient in whom the benefits outweigh the clinical risks.
Migraine
- Diclofenac potassium for oral solution packets: 50 mg (1 packet) orally once
Pain oral
- 25 mg orally 4 times a day
- Diclofenac free acid capsules: 18 mg or 35 mg orally 3 times a day
Diclofenac potassium immediate-release tablets
- 50 mg orally 3 times a day; an initial dose of 100 mg orally followed by 50 mg oral doses may provide better relief in some patients.
Parenteral
- 37.5 mg IV bolus over 15 seconds every 6 hours as needed for pain
- Maximum Dose: 150 mg per day
Side Effects of Diclofenac
The most common
- GI disorders (e.g. dyspepsia, abdominal pain, nausea, vomiting, diarrhoea, flatulence, constipation,, ulcerative stomatitis, ),indigestion,
- Disturbances of the gut such as diarrhoea, constipation, nausea, vomiting or abdominal pain.
- Drowsiness and lightheadedness
- Nausea and vomiting
- joint pain
- Nausea and vomiting
- Severe stomach ache
- Severe diarrhea
- Vaginal thrush
- Skin rash
- Headache
- Chest pain
- Diarrhea or loose stools
- Difficulty with breathing
- Dizziness
- Heartburn
- Muscle pain
More common
- Abdominal or stomach pain,
- Chills or fever
- Headache,
- Joint or back pain
- Muscle aching or cramping
- Muscle pains or stiffness
- Chest pressure or squeezing pain in chest
- Excessive sweating
- feeling of heaviness, pain, warmth and/or swelling in a leg or in the pelvis
- sudden tingling or coldness in an arm or leg
- Constipation
- Diarrhoea
- Loss of muscle coordination
- Sleepiness or unusual drowsiness
- Clumsiness or unsteadiness
- Drowsiness
Rare
- Anxiety
- change in vision
- seizures
- abnormal or fast heart rate
- weight loss
- chest pain or tightness
- confusion
- cough
- Agitation
- arm, back, or jaw pain
- blurred vision
- chest pain or discomfort
- convulsions
- extra heartbeats, fainting
- blurred vision
- chest pain or discomfort
- convulsions
- extra heartbeats
- hallucinations
- headache
- irritability
- lightheadedness
- mood or mental changes
- muscle pain or cramps
- muscle spasm or jerking of all extremities
- muscle pains or stiffness
- chest pressure or squeezing pain in chest
- discomfort in arms, shoulders, neck or upper back
- pain or discomfort in the chest, upper stomach, or throat
- pale or blue lips, fingernails, or skin
- puffiness or swelling of the eyelids or around the eyes, face, lips, or tongue
- unusual drowsiness, dullness, or feeling of sluggishness
Drug Interactions of Diclofenac
Diclofenac may interact with following drugs, supplements & may change the efficacy of drugs
- antacids (e.g., aluminum hydroxide, calcium carbonate, magnesium hydroxide)
- bisphosphonates (e.g., alendronate, etidronate, risedronate, zoledronic acid)
- antipsychotics (e.g., chlorpromazine, clozapine, haloperidol, olanzapine, quetiapine,risperidone)
- angiotensin converting enzyme inhibitors (ACEIs; e.g., captopril, enalapril, ramipril)
- angiotensin receptor blockers (ARBs; e.g., candasartan, irbesartan, losartan)
- beta-adrenergic blockers (e.g., metoprolol, atenolol)
- baclofen
- barbiturates (e.g., butalbital, phenobarbital)
- benzodiazepines (e.g., alprazolam, diazepam, lorazepam)
- calcium channel blockers (e.g., amlodipine, diltiazem, nifedipine, verapamil)
- celecoxib
- cilostazol
- “azole” antifungals (e.g., itraconazole, ketoconazole, voriconazole)
- clopidogrel
- corticosteroids (e.g., dexamethasone, hydrocortisone, prednisone)
- cyclosporine
- diuretics (water pills; e.g., furosemide, hydrochlorothiazide, triamterene)
- 5-ASA medications (e.g, sulfasalazine)
- glucosamine
- haloperidol
- heparin
- methotrexate
- multivitamins
- other non-steroidal anti-inflammatory medications (NSAIDs; e.g., diclofenac, ibuprofen, ketorolac, naproxen)
- Omega-3 fatty acids
- phenytoin
- phenobarbital
- pentoxifylline
- quinolone antibiotics (e.g., ciprofloxacin, ofloxacin)
- selective serotonin reuptake inhibitors (SSRIs; e.g., citalopram, duloxetine,fluoxetine, paroxetine, sertraline)
- serotonin/norepinephrine reuptake inhibitors (SNRIs; e.g., duloxetine, venlafaxine)
- tricyclic antidepressants (e.g., amitriptyline, clomipramine, desipramine, trimipramine)
- warferin
Pregnancy and Lactation of Diclofenac
FDA Pregnancy Category D
Pregnancy
You should not take Diclofenac Tablets during the last 3 months of pregnancy as it may affect the baby s circulation. If you are in the first 6 months of pregnancy talk to your doctor before taking this medicine as Diclofenac Tablets should only be taken if the benefit is likely to outweigh the risks.Taking Diclofenac Tablets may make it more difficult for you to get pregnant. You should talk to your doctor if you are planning to become pregnant or if you have problems getting pregnant.
Lactation
It is not known if diclofenac passes into breast milk. Due to the potential for harm to a baby, if they are exposed to this medication, breastfeeding must be stopped before starting this medication.
Important information of Diclofenac
You should not use diclofenac if you have a history of allergic reaction to aspirin or NSAIDs (non-steroidal anti-inflammatory drugs).
Diclofenac can increase your risk of fatal heart attack or stroke, especially if you use it long term or take high doses, or if you have heart disease. Do not use this medicine just before or after heart bypass surgery (coronary artery bypass graft, or CABG).
Diclofenac may also cause stomach or intestinal bleeding, which can be fatal. These conditions can occur without warning while you are using this medicine, especially in older adults.
