Ultraproct Pomada 15g, Fluocortolon, Cinchocaine
INDICATIONS: hemorrhoids, anal fissures surface proctitis.
Pharmacokinetics in humans:
Pharmacodynamics: The fluocortolone exerts an anti-inflammatory, anti-allergic and antipruritic. Reverts capillary dilation, intercellular edema and tissue infiltration. The capillary proliferation is suppressed.
Since Ultraproct esters containing two fluocortolone, they begin to exert their main effect at different times, an effect of rapid onset and prolonged duration (biphasic action).
As a local anesthetic, relieves pain cinchocaine.
Pharmacokinetics Due to their differences in lipophilicity and molecular weight, and fluocortolone pivalate fluocortolone caproate diffuse at different speeds in the area of inflammation, resulting in one hand a rapid onset of action and, on the other hand, prolonged duration of the same.
Presumably, after topical application, the two esters are hydrolyzed to free fluocortolone corresponding acids and perianal skin or rectal mucosa, but no later than after the first pass in the liver, by esterases present in all the body.
No studies on the extent of systemic availability after rectal application specific formulations Ultraproct. Prepared studies have shown similar composition that is absorbed rectally least 15% of the dose applied fluocortolone pivalate.
The fluocortolone absorbed is degraded in the liver to metabolites, mostly eliminated in urine.
Like corticosteroid, cinchocaine exerts its analgesic effect locally. It is a necessary prerequisite for the existence of plasma cinchocaine effective analgesics. Since there are no available absorption studies, risk assessment was made assuming complete absorption. In the worst case, cinchocaine absorbed dose is too low to cause adverse effects when Ultraproct is applied according to the instructions.
After absorption, cinchocaine is biotransformed into different metabolites. Of particular importance is the radical oxidative desethylation di-ethylamino, hydroxylation and oxidative chain degradation oxibutílica additional training and unidentified polar metabolites.
Even on the assumption that complete absorption occurs can discard the occurrence of systemic effects when the two formulations are used in accordance with the instructions, due to its low dose.
CONTRAINDICATIONS tuberculous or syphilitic processes in the area of treatment viral diseases (eg vaccínide, chickenpox).
PRECAUTIONS: If in the area to treat a yeast infection there is additional need specific treatment.
Avoid contact with the ocular conjunctiva. It is recommended to wash hands thoroughly after application.
RESTRICTIONS OF USE DURING PREGNANCY AND BREASTFEEDING experimental clinical trials in animals with glucocorticoids have shown reproductive toxicity.
A number of epidemiological studies suggest that there could be possibly increased risk of cleft lip and palate in newborns of women who were treated with systemic corticosteroids during the first trimester of pregnancy.
Lip and palate are a rare disorder, and if that glucocorticoids are teratogenic, they may be responsible for an increase of only one or two cases per 1,000 women treated during pregnancy. The information regarding the use of topical glucocorticoids during pregnancy is inadequate, however, expect a lower risk, since systemic availability of topically applied corticosteroids is very low.
As a general rule should not apply topical preparations containing corticosteroids during the first trimester of pregnancy. You should carefully consider the clinical indication Ultraproct treatment and should carefully weigh the risk-benefit ratio in pregnant women and during lactation. In particular, avoid prolonged treatment.
Excretion with milk in effective amounts of active glucocorticoids is unlikely.
ADVERSE REACTIONS: In long-term treatment (more than 4 weeks) can not exclude the possibility that local secondary manifestations appear, for example, skin atrophy.
In rare cases, allergic skin reactions.
DRUG INTERACTIONS AND OTHER GENDER: None known so far.
CHANGES IN RESULTS OF LABORATORY TESTS: None known so far.
PRECAUTIONS IN RELATION TO EFFECTS Carcinogenesis, Mutagenesis, Impairment of Fertility: In studies of systemic tolerance after repeated administration of the ester hydrochloride fluocortolone and cinchocaine Ultraproct content, there were no findings that could make use prohibitive prescribed preparation.
Not anticipated recognized symptoms of intolerance for highly effective local anesthetics, due to the low amount of bioavailable cinchocaine hydrochloride after repeated topical administration of the required therapeutic dose.
Embryotoxicity studies with typical results showed Ultraproct of glucocorticoids, that is, in the appropriate test systems embryolethal effects are induced and / or teratogenic. Based on these findings, special care should be taken when prescribing Ultraproct during pregnancy.
No data on experimental animal studies or epidemiological to assess the teratogenic potential cinchocaine hydrochloride. However, in analogy with local anesthetics of amide acid structure similar in effect and not embryotoxic effects are expected in humans after topical administration of the dose required for therapy. Based on the results obtained in bacterial mutagenicity tests in mammals, both in vitro and in vivo, is considered cinchocaine hydrochloride is not genotoxic.
The research fluocortolone a bacterial test system for the detection of point mutagenic effects, showed no evidence of genotoxic potential. Since there are no relevant indications of mutagenic potential for any of the substances glucocorticoids, are not expected such effects with the fluocortolone esters. In investigations in search of specific mutagenic cinchocaine hydrochloride in bacterial or mammalian cells, we found no relevant indications of genotoxic potential.
There have been no specific evidence of tumorigenicity with the active ingredients in Ultraproct. According to the knowledge of the structures, the mechanism of the pharmacological effect and the results of toxicity studies after repeated administration, no signs of tumorigenic potential.
No local intolerance reactions observed in dogs after repeated rectal administration of the combination of active principles in the form of suppositories. Many years Ultraproct therapeutic use in humans have shown no undesirable local effects worth mentioning. Side effects that have been reported sporadically are mainly related to suspected contact allergy.
DOSAGE AND ADMINISTRATION: Before applying Ultraproct which should preferably after defecation should carefully cleaned the anal region. The speed improvement usually seen should not lead to complete the treatment prematurely. To avoid relapse, after being gone for the inconvenience, treatment should be continued for one week at least, but with longer intervals (one application per day). However, care should be taken that the treatment duration does not exceed four weeks.
Generally ointment was applied 2 times a day, with the exception of the first day of treatment in which to achieve rapid elimination of the inconvenience can be prepared using the 4 times.
For each application of ointment sufficient amount the size of a pea, which runs a finger in the anal region and the anal ring, winning with a fingertip sphincter resistance. To be used intrarectal use accompanying the applicator container by screwing the ointment tube. Given very swollen processes and therefore particularly painful, can be, however, desirable to use the principle finger treatment for intrarectal application.
Prolapsed nodules should be coated with a thick layer of ointment and carefully replaced the finger pressing inward.
MANIFESTATIONS AND MANAGEMENT OF OVERDOSE OR ACCIDENTAL INGESTION: According to the results of acute toxicity studies with ester hydrochloride cinchocaine fluocortolone and should not be expected risk of acute intoxication due to the unique application of rectal or perianal Ultraproct, even in the case of inadvertent overdosing. After oral ingestion inadvertent prepared (for example, after ingestion of a few grams of ointment), one must rely primarily systemic effects cinchocaine hydrochloride, according to the dose can also be manifested as severe cardiovascular symptoms (depression or cessation of heart function) and central nervous system symptoms (seizures, inhibition or cessation of respiratory function.
PRESENTATION: Box with 15 g tube rectal cannula.
RECOMMENDED STORAGE: Store at room temperature to no more than 30 º C and dry.
Drug Name: Ultraproct
Comparable patent medicine: Ultraproct
Active substance: fluocortolone pivalate / caproate fluocortolone / Cinchocaine
Concentration: 0.918mg / 0.945mg / 5000 mg
Prolonged release tablets: No
Box 15g tube and rectal cannula
Made in: Italy