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Viaflex 50mg 30 Caps, Diacereine
DESCRIPTION
Diacerein is an acetylated derivative of rhein, anthraquinone glycoside present in rhubarb root and used since ancient times for its stimulant type laxative properties. Diacerein in "in vitro" and "in vivo" studies in experimental animals have shown the ability to inhibit production of interleukin-1 and the synthesis of metalloproteinases. Is used in the treatment of osteoarthritis, considered as a "disease modifying" drug acting in the long term.
Mechanism of action: diacerein inhibits synthesis and release of IL-1 interleukin modulating effects in experimental models of osteoarthritis and in patients with osteoarthritis of the joints of the hand and knee. IL-1 plays a key role in the pathophysiology of arthritis and cartilage destruction. Also stimulates the expression of NO synthase, increases the release of prostaglandin E2 and IL-6 and IL-8 in human chondrocytes interleukins and promotes cartilage degradation. Therefore, the inhibitory effect of diacerein on IL-1 delays all pathological processes occurring in osteoarthritis. Similarly, diacerein inhibits expression of all enzymes that degrade cartilage. Moreover, diacerein stimulates the expression of TGF-b1 and TGF-b2 which in turn promotes matrix synthesis and remodeling of articular chondrocytes. Finally, diacerein inhibits production of superoxide radicals, as well as the production of neutrophils and the phagocytic activity of these reducing macrophage migration. Unlike the anti-inflammatory (NSAID) diacerein does not inhibit the synthesis of prostaglandins and not cause gastro-toxicity.
Pharmacokinetics after an oral dose, diacerein is hydrolyzed to rhein which is the compound
active. A bioavailability of 35-56% is estimated. Administration with food increases absorption, although delayed the time to peak plasma concentration of 2.4 to 5 hours is attained. Rhein is bound to plasma proteins by 99%, with strong affinity for albumin. However, this binding is not saturable so that they are not afraid of interactions with other drugs. The plasma half-life is from 7 to 8 hours. Is removed by sulfation and binding glucuronides that are excreted by the kidneys.
Toxicity: in acute toxicity studies with oral administration of the drug to rodents, were observed LD50 greater than 2,000 mg / kg. The main clinical symptom was diarrhea. The proportional to the administered dose, laxative action was also the most prominent adverse effects after repeated administration to rats and dogs.
Diacerein not influence in any way on reproduction, nor was teratogenic in the species studied. Both the drug and its metabolite rhein showed no genotoxic activity under "in vitro" and "in vivo". In long-term studies, conducted in rats and mice, no carcinogenic potential was evident.
INDICATIONS AND DOSAGE
Treatment of Osteoarthritis
Oral administration:
Adults: the recommended dose is 50 mg twice daily. If you have gastrointestinal side effects should start treatment with 50 mg every 24 hours during the first week.
Elderly: No need for recommended in elderly subjects variations of the usual dose
Children: Efficacy and safety of diacerein in children have not been demonstrated
Diacerein has a slow onset of action, but with effects that last for at least 2 months after the treatment has been deleted. Following precisely the delay in the initial action (30 to 45 days to reach the analgesic effect), must be taken continuously for at least a month to start observing its beneficial effects. For this reason, it may be necessary to start treatment with analgesic / anti-inflammatory usual whose action is immediate.
Renal impairment: In subjects with moderate renal impairment the daily dose should be reduced by 50% of the recommended for adults. In subjects with severe renal impairment, the use of diacerein is contraindicated
Hepatic impairment: no dosage adjustments are required in patients with moderate hepatic impairment. However, in those with severe impairment of liver function, the use of diacerein is contraindicated
CONTRAINDICATIONS and PRECAUTIONS
Diacerein is contraindicated in patients with hypersensitivity to diacerein or substances of similar structure or any component of the formulation.
Diacerhein is contraindicated in inflammatory bowel disease (ulcerative colitis,
Crohn's disease), intestinal obstruction or pseudo-obstruction, and abdominal pain syndrome of unknown cause
Patients with moderate renal impairment and require the titration need periodic monitoring of kidney function.
Ranking FDA pregnancy risk
The results of the studies carried out on rats have shown that diacerein does not affect fertility or reproductive function. The experiments carried out in rats, mice and rabbits revealed no evidence of teratogenicity or genotoxicicidad. Nor diacerein has shown no effect on parturition or post-natal development of the offspring. However, there are no adequate and well-controlled studies in pregnant women. Because animal reproduction studies are not always permit predicting the response in humans, are not recommended during pregnancy diacerein.
Diacerein, such as drugs of the same group may appear, even in trace amounts in breast milk, so that his administration is not recommended during lactation.
Interactions
Antacids derivatives, magnesium, aluminum and calcium may decrease the gastrointestinal absorption of diacerein. In the case of concomitant administration there must be an interval of at least 2 hours between taking any of these preparations and diacerein.
No drug interactions have been described with warfarin, phenytoin, indomethacin, salicylic acid, glibenclamide, hydrochlorothiazide and NSAIDs. Nor are there in interaction studies with cimetidine and paracetamol.
ADVERSE REACTIONS
Diacerein a drug is well tolerated, with gastrointestinal adverse reactions are the most common: diarrhea, loose stools and abdominal pain. These side effects are generally dose-dependent moderate intensity and disappear within a few days, even without leaving the treatment. Occur in approximately 10-20% of patients during treatment with diacerein. Taking the drug with meals or starting treatment with half the recommended (50 mg / day) daily dose may decrease the incidence thereof. Despite this, 6% of patients discontinued treatment.
Rarely (1-10% of patients) was observed pigmentation recto-colonic mucosa (colonic melanosis).
We observed a darkening of the color of the urine related to the structure of the drug that lacks clinical relevance (10% of patients).
There have been some cases of pruritus, eczema and skin (1-10% of patients) eruption.
Have occurred rarely severe hypokalemia or acute hepatitis (one case).
Described a case of toxic epidermal necrolysis with possible fatal outcome.
