Source: Health Products Regulatory Authority (IE) Revision Year: 2021 Publisher: Dompé Farmaceutici S.p.A., Via San Martino 12-12/a, 20122 Milano, Italy
Pharmacotherapeutic group: Anti-inflammatory and antirheumatic products, non-steroids, drug, propionic acid derivatives
ATC code: M01AE03
Sprintafen Lysine Salt has a higher solubility compared with Sprintafen acid.
The mechanism of action of NSAIDs is related to the reduction in prostaglandin synthesis caused by inhibition of the enzyme cyclooxygenase.
More specifically, NSAIDs inhibit the transformation of arachidonic acid into cyclic endoperoxides, PGG2 and PGH2, the precursors of prostaglandins PGE1, PGE2, PGF2a and PGD2, prostacyclin PGI2 and thromboxanes (TxA2 and TxB2). Inhibition of prostaglandin synthesis may also interfere with other mediators such as quinines, causing an indirect action in addition to the direct action.
Sprintafen Lysine Salt has a potent analgesic effect, on account of both its anti-inflammatory and central effects. Painful inflammatory conditions are resolved or reduced, thereby favouring articular motility.
In a pharmacokinetic study on 30 subjects, peak plasma concentrations of 3.61 μg/ml (SD 1.17 μg/ml) were achieved 15-30 minutes after administration.
No accumulation has been observed following repeated administrations of Sprintafen.
When Sprintafen is administered with food, its total bioavailability (AUC) is not altered; however, the rate of absorption is slowed.
95-100% of Sprintafen binds with plasma proteins (primarily albumin).
Plasma clearance values are between 0.06 and 0.08 L/kg/h and the apparent distribution value is 0.1-0.4 L/kg.
Sprintafen is extensively metabolised by the hepatic microsomal enzymes, primarily by conjugation and only marginally by means of hydroxylation. The resulting metabolites have no pharmacological activity. h3. Elimination
The product is eliminated rapidly and primarily via the kidneys. It has a plasma half-life of approximately 1.5 hours. 60-80% of a dose of Sprintafen 25 mg tablets is excreted in urine as a glucoronide metabolite within 24 hours.
The LD50 of Sprintafen lysine salt following oral administration in rats and mice was 102 and 444 mg/kg, respectively, equal to 30-120 times the active anti-inflammatory and analgesic dose for the animal. For intraperitoneal administration, the LD50 of Sprintafen lysine salt is 104 and 610 mg/kg in rats and mice, respectively.
Prolonged treatment with oral Sprintafen lysine salt in rats, dogs, and monkeys, at doses equal to or higher than the therapeutic doses, did not cause any toxicity. Gastrointestinal and renal alterations were reported at high doses, in line with the known side effects of non-steroidal anti-inflammatory drugs in animals. In one prolonged toxicity study on oral or rectal administration in rabbits, Sprintafen was seen to be better tolerated when administered via the rectal route than via the oral route. In a tolerability study conducted in rabbits via the intramuscular route, Sprintafen lysine salt was seen to be well tolerated.
In teratogenesis, fertility, reproduction, and post-natal toxicity studies, Sprintafen was seen to have no teratogenic effect or negative effect on the reproductive function.
Sprintafen lysine salt was not reported as being mutagenic during in vitro genotoxicity tests. Carcinogenesis studies on Sprintafen in mice and rats showed no carcinogenic effect.
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