Active Ingredients: Fluocortolone Pivalate and Hexanoate, Cinchocaine Hydrochloride
Therapeutic actions: Fluocortolone exerts an anti-inflammatory, antiallergenic and antipruritic effect. Capillary dilatation, intercellular oedema and tissue infiltration regress; capillary proliferation is suppressed. As ULTRAPROCT® contains two fluocortolone esters, which start to exert their main effect at different times, a rapidly established and long-lasting effect results (biphasic action). As a local anaesthetic, cinchocaine eases the pain. Pharmacokinetics Because of their different lipophilicity and molecular weights, fluocortolone pivalate and fluocortolone hexanoate diffuse at different rates at the site of inflammation, resulting on the one hand in a rapid onset of action and, on the other, in a protracted duration of action. It can be assumed that, after topical application, the two esters are hydrolysed to free fluocortolone and the corresponding acids at the level of the perianal skin or rectal mucosa -but at the latest after the first liver pass - by esterases occurring ubiquitously in the body. No studies into the degree of systemic availability after rectal use are available for the ULTRAPROCT® formulations themselves. Studies with preparations with a similar composition have shown that less than 15 % of the dose of fluocortolone pivalate applied is absorbed rectally. Absorbed fluocortolone is broken down in the liver into metabolites, the overwhelming majority of which are excreted with the urine. Similarly, the local anaesthetic, cinchocaine has a local analgesic effect. Analgesic effective cinchocaine plasma levels are not a necessary prerequisite. Since no absorption studies are available, risk assessment was perfomed under the assumption of a complete absorption. Under this worst case assumption, the absorbed dose of cinchocaine is too low to elicit adverse effects, when ULTRAPROCT® is applied according to the instructions. Following absorption, cinchocaine is biotransformed into a number of metabolites. The principal metabolic routes are the oxidative de-ethylation of the di-ethylamino function, hydroxylation and oxidative degradation of the butyloxy-chain and the additional formation of unidentified polar metabolites. Even under the assumption of complete absorption, systemic effects can be ruled out when the two formulations are used according to instructions because of the low dosage.
What is it used for?: (Indications:) Haemorrhoids, superficial anal fissures, proctitis. Short term symptomatic relief of haemorrhoids, pruritus ani and vulvae.
Contraindications and cautions: Tuberculous or syphilitic processes in the area to be treated; virus diseases (e. g. vaccinia, chickenpox). Precautions Additional specific therapy is required in fungal infections. Inadvertent contact of the preparation with the eyes should be avoided. Careful handwashing after use is recommended.
Side effects: If ULTRAPROCT® is applied for long periods of time (more than 4 weeks), local concomitant symptoms, such as atrophy of the skin cannot be excluded. Allergic skin reactions may occur in rare cases.