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Voltaren ampoules
Antirheumatic, anti-inflammatory, analgesic


Composition
Active substance:
Diclofenac sodium (phenylacetic acid derivative)
Presentation and amount of active substance per unit:
i.m.: injection solution; i.v.: concentrate for infusion
One 3 mL ampoule of Voltaren contains 75 mg diclofenac sodium
Excipients:
Mannitol, propylene glycol, water, antioxidant: sodium metabisulfite (E 223) 2.0 mg;
Preservative: benzyl alcohol 120 mg.


Description
Clear, colourless to faintly yellow liquid.


Properties/effects
Mechanism of action
Voltaren ampoules contain diclofenac sodium, a non-steroidal compound with pronounced antirheumatic, antiinflammatory, analgesic, and antipyretic properties.


Inhibition of prostaglandin biosynthesis, which has been demonstrated in experiments, is considered to be fundamental to its mechanism of action. Prostaglandins play an important role in causing inflammation, pain, and fever. Diclofenac sodium in vitro does not suppress proteoglycan biosynthesis in cartilage at concentrations equivalent to the concentrations reached in humans.


Therapeutic effect
In rheumatic diseases, the anti-inflammatory and analgesic properties of Voltaren elicit a clinical response characterised by marked relief from signs and symptoms such as pain at rest, pain on movement, morning stiffness, and swelling of the joints, as well as by an improvement in function. In post-traumatic and postoperative inflammatory conditions, Voltaren rapidly relieves both spontaneous pain and pain on movement and reduces inflammatory swelling and wound oedema. When used concomitantly with opioids for the management of postoperative pain, Voltaren significantly reduces the need for opioids.


In clinical trials, the pronounced analgesic effect has also been demonstrated in moderate and severe pain of nonrheumatic origin, an effect which sets in within 15-30 minutes. Voltaren has also been shown to have a beneficial effect in migraine attacks. Voltaren ampoules are particularly suitable for initial treatment of inflammatory and degenerative rheumatic diseases, and of painful conditions due to inflammation of non-rheumatic origin.

Pharmacokinetics
Absorption
After administration of 75 mg diclofenac by intramuscular injection, mean peak plasma concentrations of about 2.5 µg/mL (8 µmol/L) are reached after about 20 minutes. The amount absorbed is in linear proportion to the size of the dose. When 75 mg diclofenac is administered as an intravenous infusion over 2 hours, mean peak plasma concentrations are about 1.9 µ/mL (5.9 µmol/L). Shorter infusions result in higher peak plasma concentrations, while longer infusions give plateau concentrations proportional to the infusion rate after 3 to 4 hours. In contrast, plasma concentrations decline rapidly once peak levels have been reached following intramuscular injection or administration of gastro-resistant tablets or suppositories. The area under the concentration curve (AUC) after intramuscular or intravenous administration is about twice as large as it is following oral or rectal administration, because about half the active substance is metabolised during its first passage through the liver ("first pass" effect) when administered via the oral or rectal route. Pharmacokinetic behaviour does not change after repeated administration. No accumulation occurs provided the recommended dosage intervals are observed.


Distribution
Altogether 99.7% of diclofenac binds to serum proteins, mainly to albumin (99.4%). The apparent volume of distribution calculated is 0.12-0.17 L/kg. Diclofenac enters the synovial fluid, where maximum concentrations are measured. 2-4 hours after peak plasma values have been reached. The apparent half-life for elimination from the synovial fluid is 3-6 hours. Two hours after reaching peak plasma levels, concentrations of the active substance are already higher in the synovial fluid than in the plasma, and they remain higher for up to 12 hours.


Metabolism
Biotransformation of diclofenac takes place partly by glucuronidation of the intact molecule, but mainly by single and multiple hydroxylation and methoxylation, resulting in several phenolic metabolites (3'hydroxy-, 4'-hydroxy-, 5-hydroxy-, 4',5dihydroxy-, and 3'-hydroxy-4' methoxydiclofenac), most of which are converted to glucuronide conjugates. Two of these phenolic metabolites are biologically active, but to a much lesser extent than diclofenac.


Elimination
Total systemic clearance of diclofenac from plasma is 263 ± 56 mL/min (mean value± SD). The terminal half-life in plasma is 1-2 hours.


Four of the metabolites, including the two active ones, also have short plasma half-lives of 1-3 hours. One metabolite, 3'-hydroxy-4'-methoxy-diclofenac, has a much longer plasma half-life. However, this metabolite is virtually inactive. About 60% of the administered dose is excreted in the urine in the form of metabolites. Less than 1% is excreted as unchanged substance. The rest of the dose is eliminated as metabolites through the bile in the faeces.


Kinetics in special clinical situations
No relevant age-dependent differences in the drug's absorption, metabolism, or excretion have been observed after oral administration. However, in elderly patients a 15-minute intravenous infusion resulted in 50% higher plasma concentrations than expected from the data on young healthy subjects.


In patients suffering from renal impairment, no accumulation of the unchanged active substance can be inferred from the single-dose kinetics when applying the usual dosage schedule. At a creatinine clearance of less than 10 mL/min, the calculated steady-state plasma levels of the hydroxy metabolites are about 4 times higher than in healthy subjects. However, the metabolites are ultimately cleared through the bile.


In patients with impaired liver function (chronic hepatitis or non-decompensated cirrhosis), the kinetics and metabolism of diclofenac are the same as in patients without liver disease.


Indications
Intramuscular injection
Initial treatment of:
- Exacerbations of inflammatory and degenerative forms of rheumatism: rheumatoid arthritis, ankylosing spondylitis, osteoarthritis, spondylarthritis, painful syndromes of the vertebral column, non-articular rheumatism.
- Acute attacks of gout.
- Renal colic and biliary colic.
- Post-traumatic and postoperative pain, inflammation, and swelling.

Intravenous infusion
Treatment or prevention of post-operative pain in a hospital setting.

 

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