DICLOBRU INJECTIONS 75mg/3ml - Leaflet for physicians
and patients
The medicine should never be administered as an intravenous bolus injection; if it is
necessary to use it intravenously, this medicine must be slowly infused drop by drop and
only by a physician in a hospital
COMPOSITION:
Active ingredients: Diclofenac Sodium 75 mg/3 ml
Other ingredients: propylene glycol, benzyl alcohol, sodium metabisulfite, mannitol, sodium
hydroxyde, water for injection.
PRESENTATION AND PACKAGE: ampoules of 3 ml with clear, colorless liquid free of
visible particles, packed in boxes of 5 or 100 ampoules.
PHARMACOLOGICAL PARTICULARS.
Non-steroidal anti-inflammatory drug belonging to the group of phenylacetic acid derivatives. It
has anti-inflammatory, analgesic and antipyretic effects.
It inhibits cyclooxygenase with resulting blockade of the arachidonic cascade reactions and
disturbance of synthesis of PGE2, PGF2-alfa, thromboxan A2, prostacycline, leukotrienes and
output of lysosomal enzymes: inhibits platelet aggregation, and has a desensitizing effect in
long-term using.
In course treatment of locomotor system diseases, the drug intensively penetrates the joint cavity,
relieves joint pain in rest and movements, improves volume of movements, and decreases
morning constraint and edema of joints.
It relieves pain in rest and movements, morning constraint, edema of joints, improves their
functional activity. In inflammatory processes after operations and traumas, it rapidly relieves
both a spontaneous pain and a pain in movements, decreases an inflammatory edema in the
wound area. After a course treatment of the patients with polyarthritis, the drug concentration in
sinovial liquid and sinovial tissues is higher than that in plasma. By anti-inflammatory activity,
diclofenac is better than acetylsalicylic acid, butadione, ibuprofen; there are data of its more
significant clinical effect and better tolerance compared to indometacin. By rheumatism and
Bechterev’s disease it is equivalent to prednisolone.
Pharmacokinetics. The peak plasma concentration is reached 10-20 minutes after intramuscular
administration. 99 % of the drug is bound to plasma proteins. It freely penetrates tissues and
sinovial liquid where its concentration rises slowly and over 4 hours becomes higher than that in
plasma. Diclobru is metabolized in the liver through conjugation and hydroxylation with
formation of the pharmacologically inactive metabolites. 35 % of metabolites is eliminated with
feces, and 65 % is eliminated via the kidneys as inactive derivatives (less than 1 % is eliminated
as unchanged drug). The plasma half-life elimination is 2 hours, sinovial liquid – 3-6 hours.
INDICATIONS:
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Locomotor system diseases (rheumatic arthritis, arthroses, gout, bursopathy, entesopathy,
deforming osteoarthrosis, synovitis and tendosynovitis, myalgia, myositis)
Spinal diseases (Bechterev's disease, coxarthrosis, ankylosing spondylitis, spondylosis,
ischias, osteochondrosis, disorders of the lumbosacral plexus, radiculitis)
Rheumatism
Neurological diseases (neuralgia and neuritis, migraine attacks)
Posttraumatic pains (sprains, dislocations, contusions, fractures)
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Postoperative pains (after tonsillectomy, operations on the abdominal organs, extraction
of teeth)
Menstrual pains (algodysmenorrhea) and inflammation of ovaritis (salpingitis and
oophoritis), inflammatory diseases of the uterus, of vagina and vulva (pathogenetic
therapy)
Renal and bile colicks
Pathogenetic therapy of the otorhinolaryngologic diseases (inflammation of middle ear,
acute pharyngitis, acute tonsillitis [angina], sinusitis, maxillitis)
Pathogenetic therapy of acute respiratory infections of the upper respiratory tract
Diseases of the vision organs (blepharoconjunctivitis, conjunctivitis, keratoconjunctivitis,
changes in corneal membranes, trauma of the eye and orbit)
POSOLOGY FOR INTRAMUSCULAR INJECTION OR SLOW INFUSION (DROP)
1. Intramuscular injection: Contents of one ampoule to be injected deeply in the buttock.
(do never inject under the skin or directly in bolus in a vein), once a day.
In some cases the daily dose can be increased up to two ampoules per day (one injection in each
buttlock) with interval of minimum 6 hours between two injections. The maximal daily dose is
150 mg. The maximal dose should not be used for more than 5 consecutive days.
2. Slow intravenous drop infusion (fulfilled by a doctor in a hospital only):
immediately before infusion, prepare the following solution: to a 100 – 150 ml of 0.9 % NaCl
solutions for intravenous drop infusions or to a 100-150 ml of 5 % glucose solutions, add 1ml of
a solution for injection of 4.2% of Na Bicarbonate. Add the required quantity of Diclobru in one
of the above mentioned solution.
Verify that you have obtained a clear solution free of any particles, crystals or precipitate.
Use only a clear solution.
The intravenous drop infusion may be fulfilled by one of the following schemes:
- 25-50 mg of Diclobru for one hour. Then Diclobru may be infused with rate 5 mg/h to maintain
a therapeutic effect; 75 mg of Diclobru for two hours.
Never exceed the maximal dose of 150 mg/day.
CHILDREN: NOT RECOMMENDED FOR CHIDRENS
CONTRAINDICATIONS:
- hypersensitivity to diclofenac and other ingredients of the drug or other NSAIDs
- ulcerative disease of the stomach and duodenum
- destructive and inflammatory diseases of the intestines in acute phase
- haemopoiesis disorders or blood disorders "aspirin" bronchial asthma
- porphyria
- last trimester of pregnancy and breast feeding
- children under the age of 14 years
- renal and liver insufficiency
SIDE-EFFECTS:
Gastrointestinal side effects may include in rare cases, nausea, erosive-ulcerative lesions,
bleeding and perforation in the gastrointestinal tract, liver dysfunction, elevated transaminase
levels, jaundice, hepatitis.
Peripheral edema and allergic reactions: rash, pruritus, eczema, bronchospasm, anaphylactic
systemic reactions.
Central and peripheral nervous system side effects: dizziness, headache, tinnitus, insomnia,
nervousness, depression or tiredness, vision disturbances (blurred vision, diplopia).
Urinary tract: nephrotic syndrome, renal insufficiency may occur.
Haemopoiesis system: leucopenia, thrombocytopenia, aplastic anaemia, erythema multiforme,
agranulocytosis, haemolytic anemia.
Other systems: edema in the injection site, local pain and induration, particularly in elderly
diabetics.
PRECAUTIONS:
The drug should be used with caution in diseases of liver, kidneys, gastrointestinal tract in
anamnesis, in dyspeptic symptoms, bronchial asthma, arterial hypertension, heart failure, recent
serious operative interventions, as well as for elderly patients. Patients suffering from
impairment of hepatic, cardiac, or renal function should be carefully monitored. Dosage may
have to be reduces in the elderly.
During prolonged treatment, it is recommended to control hepatic function, peripheral blood
contents, occult blood in feces.
In case of known allergic reactions on NSAIDs or sulfites, diclofenac may be used only in
emergency cases.
During the firs 6 months of pregnancy, the drug should be used by strict indications and in least
dosage.
During the treatment alcohol is not recommended.
Effects on the ability to drive or operate machinery: During the treatment, decrease in speed of
psychomotor reactions is possible.
OVERDOSAGE.
Symptoms: acute headache, motor excitation, dizziness, cramps, convulsions; nausea, vomiting,
blood vomiting, diarrhoea, gastrointestinal erosion, ulceration or bleeding in gastrointestinal
tract; liver disorders; renal insufficiency.
Treatment: Forced diuresis. Symptomatic therapy directed on the blood pressure normalization.
In case of convulsions - diazepam, phenobarbital. Hemodialysis is ineffective.
INTERACTIONS WITH OTHER DRUGS
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Concurrent use of diclofenac with potassium-sparing diuretics may increase blood
potassium level; concurrent use with “loop” diuretics may reduce their diuretic effects
It increases blood lithium level
Concurrent use of digoxin and lithium with diclofenac can provoke increasing of digoxin
and lithium plasma concentrations.
Methotrexate. NSAIDs may decrease protein binding and/or renal elimination of
methotrexate, resulting in increased and prolonged methotrexate plasma concentrations
and increased risk of toxicity; it is recommended to withdraw NSAID therapy before and
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after infusions of methotrexate in high doses.
Cyclosporine: Risk of toxicity may increased
Concurrent use with aspirin is not recommended because administration of two or more
NSAIDs may increase the risk of gastrointestinal toxicity and bleeding Concurrent
administration of two or more NSAIDs may alter the pharmacokinetic profile of at least
one of the medications, which may alter the therapeutic effect and/or increase the risk of
adverse effect; specifically, aspirin decreases the bioavailability of diclofenac [by 50 %]
with lowering plasma diclofenac level.
Anticoagulants, coumarin-or indandione-derivative or heparin or thrombolytic agents:
Inhibition of platelet aggregation by NSAIDs, and the possibility of NSAID-induced
gastrointestinal ulceration or bleeding may be hazardous to patients receiving
anticoagulant or thrombolytic therapy; although with usual doses, diclofenac less likely
than other NSAIDs may significantly alter platelet aggregation
It increases risk of side effects of glucocorticoids (gastrointestinal bleeding)
Antidiabetic agents, oral or insulin: NSAIDs may increase the effect of these
medications; dosage adjustments of the antidiabetic agent may be necessary.
It increases the blood level of quinoline derivatives
Bone marrow depressants. Leukopenic and/or thrombocytopenic effects of these
medications may be increased with concurrent or recent therapy with NSAID; if
necessary, dosage adjustment of the bone marrow depressant should be based on blood
counts
Cefamandole, cefoperazone, plicamycin, valproive acid, colchicin: Concurrent use with
NSAID may increase risk of gastrointestinal bleeding and bleeding in other sites.
SHELF LIFE:Shelf-life is 3 years.
DELIVERY CONDITIONS: On medical prescription.
STORAGE INSTRUCTIONS:
Store below 25°C. Protect from light.
KEEP OUT OF REACH OF CHILDREN.