Diclofenac (Voltaren): Pharmacological Properties, Pharmacokinetics, Indications, List of Ingredients, Pediatric Use, Contraindications and Side Effects, Effects on Ability to Drive and Use Machines, Administration during Pregnancy or Breast-Feeding, Storage Requirements
- Diclofenac Description
- Composition and Forms of Issue
- Key Indications
- Dosage and Administration
- Diclofenac Analogues
- Possible Side-Effects
- Interactions with Other Drugs
- Anti-cancer Characteristics
- Contraindications to Use
- Safety Note
- Administration during Pregnancy or Breast-Feeding
- Pediatric Use
- Use by Elderly Patients
- Storage Requirements
Pain is a main sign of any chronic and systemic diseases. Therefore, very often struggle against pain syndrome falls to dermatologists, neurologists and therapists share. In order to eliminate this problem, non-steroidal anti-inflammatory agents prove to be the most efficient remedies. They take analgesic, antithermic and anti-inflammatory effects. Therapists often prescribe Diclofenac for chronic pain treatment. Diclofenac belongs to the group of non-steroidal anti-inflammatory agents with active substance, diclofenac. This non-narcotic anaesthetic medication is used for external and internal application for treatment of arthronosis, osteochondrosis, and various pain syndromes. Diclofenac is issued in the forms of tablets covered with enteric coating, ampules, gels and ointments. Diclofenac is an international brand name of the medication.
Composition and Forms of Issue
Diclofenac solution for intramuscular injection
Solution is transparent, toned, with slight smell of benzyl alcohol. 1ml of solution contains diclofenac sodium 25mg, 1 ampule (3ml) – 75mg. Auxiliary agents: benzyl alcohol, water for injections.
Diclofenac film-coated tablets
1 tablet contains diclofenac sodium 25mg and 50mg, 10, 20, 30, 50 or 100pcs in a package.
Diclofenac retard tablets
1 tablet contains diclofenac sodium 75 and 150ng, 20, 30, 100pcs in a package.
Diclofenac rectal suppositories
1 suppository contains diclofenac – 25, 50, 100mg. Auxiliary agents: 1,2-propylene glycol, aerosol, witepsol, 10 pcs in a package.
Ointment is of 1% white or almost white color with slight specific smell. 1g of ointment contains 10g of diclofenac sodium. Auxiliary agents: polyethylene oxide-400, polyethylene oxide-4000, 1,2-propylene glycol, nipagin, nipasol; 30 or 40 in aluminum tubes, 1 tube in a cardboard package.
Diclofenac gel 1%
1g of gel contains diclofenac sodium 10mg; in tubes 40, 60 g, 1 tube in a cardboard package.
Diclofenac gel 5%
1g of gel contains diclofenac sodium 50mg; in tubes 50, 100 g, 1 tube in a cardboard package.
Diclofenac is indicative in the following cases:
- Musculoskeletal system disorders (rheumatoid arthritis, psoriasic juvenile chronic arthritis, rheumatoid spondylitis, gouty arthritis, rheumatic soft tissue involvement, ostheoarthrosis of peripheric joints and spine including radicular syndrome, peritenditis, bursitis);
- Pain syndrome of mild and moderate severity: neuralgic pain, myoneuralgia, lumboischialgia, post-traumatic pain syndrome accompanied by inflammation, post-surgery pain, headache, migraine, algodismenorrhea, adnexitis, proctitis, toothache.
- As a part of complex therapy, Diclofenac is indicative to treat inflammatory infections of ear, throat and nose with severe pain syndrome (pharyngitis, tonsillitis, otitis).
- Feverish syndrome.
Dosage and Administration
Solution for intramuscular introduction
Diclofenac is injected intramuscularly at the beginning of treatment course in the dose of 75mg (1 ampule) and maximally – 150mg (2 ampules) per day for adults only and only in cases when a fast therapeutic effect is essential. Generally, injections are prescribed within 1-5 days. In case of therapy continuation, a patient switches over tableted, capsulized and suppository form of Diclofenac. Intramuscular injections may be combined with medication’s peroral or rectal intake. In this case, maximal daily dosage must not surpass 150mg.
Diclofenac should be taken perorally during or after food acceptance with small amount of water. Adults and teenagers above 15 years of age should administer Diclofenac by 20-25mg 2-3 times per day. Upon achieving optimal therapeutic effect, a dosage is gradually decreased, and a patient switches over supporting therapy in dosage of 50mg per day. Maximal daily dosage is 150 mg.
Adults are recommended taking from 50 up to 150mg of Diclofenac per day divided into 2-3 intakes. In case of absence of other prescriptions, it is recommended taking the drug in the capacity of initial therapy in the dose of 75-100mg divided into 2-3 separate intakes. For children over 6 years of age, the daily dosage is up to 2 mg/kg of body weight divided into 2-3 intakes. In case of juvenile chronic arthritis, daily dose may be increased up to 3 mg/kg of body weight.
Suppositories should be taken rectally. Adults must use 100mg once a day or 50mg twice a day or 25mg 3-4 times per day. Maximal daily dose is 150mg. Children over 12 years of age may use 50mg 1-2 times per day or 25mg 2-3 times per day.
Ointment and gel are applied 2-4 g with a thin coat above the focus of inflammation and are slightly rubbed in. The frequency of use is 2-3 times per day. Maximal daily dosage should not surpass 8g. Therapy course is no longer than 14 days. Importance of prolonged treatment is determined by a therapist.
The analogues of Diclofenac generally contain one and the same active substance. Among them are Diclofenac Retard, Voltaren, Ortophenum, Naklofen SR.
Diclofenac Possible Side-Effects
From the part of gastro-intestinal tract:
- Oftener than 1% – abdominal pains, feeling of abdominal distension, diarrhea, nausea, uncleared bowels, flatulency, increase in liver enzymes, peptic ulcer with possible complications (bleeding, perforation), gastro-intestinal bleeding;
- More seldom than 1% – vomit, hepatitis, melena, fecal blood, esophageal affection, recurrent oral ulceration, xerosis (including mouth), hepatitis (peracute course is possible), hepatic necrosis, fibroid induration, hepatonephric syndrome, change of appetite, pancreatitis, colitis.
From the part of nervous system:
- Oftener than 1% – headache, vertigo;
- More seldom than 1% – sleep disorder, drowsiness, depression, irritability, aseptic meningitis (very often among patients suffering from erythema centrifugum or other systematic diseases of conjunctive tissue), convulsions, overall weakness, disorientation, nightmares, and apprehension.
From the part of sensory organs:
- Oftener than 1% – buzzing in ears;
- More seldom than 1% – blurring of vision, diplopia, taste perversion, reversible or irreversible loss of hearing, scotoma.
From the part of skin integument:
- Oftener than 1% – itching, rash;
- More seldom than 1% – baldness, urticarial fever, weeping dermatitis, toxic dermatitis, herpes iris (including Stevens Johnson’s syndrome), toxic epidermal necrolysis (Lyell’s syndrome), increased pholosensibility, punctulated effusion of blood.
From the part of urinary system:
- Oftener than 1% – fluid retention;
- More seldom than 1% – nephrotic syndrome, proteinuria, oligohydruria, hematocyturia, interstitial nephritis, renal papillary necrosis, acute kidney failure, azotemia.
Blood-making organs and immune system:
- Oftener than 1% – anemia (including hemolytic and aplastic anemia), leucocytopenia, thrombocytopenia, eosinophilia, agranulocytic angina, thrombocytopenic purpura, impairment of infectious process development (including development of flesh-eating disease).
From the part of respiratory system:
- More seldom than 1% – cough, bronchial spasm, swelling of the larynx, pneumonitis.
From the part of cardio-vascular system:
- More seldom than 1% – increase of arterial blood pressure, backward heart failure, premature ventricular contraction, chest pains.
- More seldom than 1% – anaphylactoid reaction, acute serum sickness (peracute course), lip and tongue edema, allergic vacuities.
Interactions with Other Drugs
- Diclofenac increases concentration in blood plasma of digoxin, methotrexate, lithium medications, and cyclosporine.
- The drug reduces the effect of diuretics; on the setting of potassium-sparing diuretics, the risk of hyperglycemia enhances; on the setting of anticoagulants, thrombolytic agents (streptokinase, urokinase) – risk of bleeding is possible (oftener from gastro-intestinal tract).
- Diclofenac decreases the effect of hypotensive and sleeping medicines;
- The medication enhances the possibility of adverse effects occurrence of other non-steroidal anti-inflammatory agents and glucocorticosteroids (bleeding in gastro-intestinal tract), toxicity of methotrexate and nephrotoxicity of cyclosporine.
- Acetylsalicylic acid decreases concentration of Diclofenac in blood.
- Simultaneous intake with paracetamol increases the risk of nephrotoxic effects of Diclofenac.
- Diclofenac reduces the effect of antihyperglycaemic agents.
- Cefamandole, cefoperazone, cefotetan, valproic acid, and plicamycin increase the frequency of hypoprotrombinemia development.
- Cyclosporine and gold preparations enhance Diclofenac influence on synthesis of prostaglandins in kidneys which increases nephrotoxicity.
- Simultaneous intake with ethanol, colchicine, corticotrophin, and tutsan medicines increases the risk of bleeding in gastro-intestinal tract.
- Diclofenac enhances the effect of medicines causing photosensibilization.
- Medications blocking tubular secretion enhance Diclofenac concentration in blood plasma and increase its toxicity.
According to numerous research studies, it was stated that Diclofenac was among the strong candidates for application in the capacity of chemotherapy. During trials, the results of patients treated with this medication were collated. Patients taking Diclofenac had the decrease of metastasis formation. Patients with tumors of breast, lungs and kidneys observed the slowing down of disease progression. According to specialists anti-tumor effects of Diclofenac were first of all connected with its direct action as a cyclooxygenase inhibitor. Also, its anti-tumor activity may be explained by its effects inhibiting the growth of nourishing tumor vessels, immunomodulation, inhibiting of thrombocytes activity and glucose metabolism.
Contraindications to Use
Patients suffering from the following disorders, diseases or conditions are counter-indicative to Diclofenac treatment:
- Erosive ulcer gastro-intestinal tract disorders (in the exacerbation phase);
- Gastro-intestinal bleeding;
- Aspirin-sensitive asthma;
- Impaired haemopoiesis;
- Bleeding abnormalities (including hemophilia);
- Under-age (up to six years of age);
- Lactation period;
- Hypersensitivity to ingredients (as well as to other non-steroidal anti-inflammatory agents).
Diclofenac should be taken carefully by patients suffering from anemia, bronchial asthma, backward heart failure, arterial hypertension, edema syndrome, hepatic or renal disorder, alcoholism, inflammatory bowel diseases, erosive ulcer gastro-intestinal tract disorders in non-exacerbation phase, diabetes, post-surgery condition, induced porphyria, elderly age, diverticulitis, systemic diseases of conjunctive tissue.
Safety Note on Diclofenac
Within the therapy course with Diclofenac, systematic control of peripheral blood, hepatic and renal function, feces examination for blood presence should be conducted. Patients taking Diclofenac should refuse any activity requiring heightened level of awareness and fast psychic and motor reactions, as well as alcoholic beverages.
Overdose may be characterized by the following symptoms: vomit, headache, labored breathing, impaired judgment, among children – myoclonic seizures, nausea, abdominal pain, bleeding, hepatic and renal function impairment.
Recommended therapy includes gastric lavage, absorbent carbon administration, symptomatic therapy, aggressive diuretic administration. Hemodialysis is of low efficiency.
Administration during Pregnancy and Breast-Feeding
Diclofenac is counter-indicative during pregnancy. If the administration of Diclofenac is required, the question of ablactation should be solved.
Diclofenac is counter-indicative to children under six years of age.
Use by Elderly Patients
Elderly patients should take Diclofenac with due care.
Do not store above 25°С. Keep out of reach of children and animals. Keep out of direct sunlight. Expiration period is three years.