Proctosan® [Heparin, Polydocanol, Prednisone]

Actual information

Proctosan Neo is a combined preparation for the treatment of hemorrhoids, available in the form of rectal suppositories and ointments. it includes the detergent polydocanol, the direct anticoagulant heparin and the synthetic glucocorticoid prednisolone. heparin in the composition of this drug improves local blood circulation, has decongestant and absorbable properties and prevents the development of thrombophlebitis of hemorrhoids. polydocanol exhibits sclerosing, antipruritic and analgesic effects. prednisone has pronounced anti-inflammatory properties, helps eliminate itching and swelling. Thus, proctosan neo causes relief of the main symptoms of hemorrhoids, and is also used for proctological diseases such as anal fissure, eczema and thrombophlebitis of the veins of the perianal region. the drug can be used both in the acute period and for the prevention of exacerbations of hemorrhoids, to prepare for surgical treatment of hemorrhoids and after surgery.

Hemorrhoids is recognized as one of the most common diseases among the general population (Lohsiriwat V., 2015). The true prevalence of hemorrhoids is unknown. However, recent data indicate an increase in the prevalence of this disease over time. In 1990, an epidemiological study of hemorrhoids in the United States revealed that its prevalence was 4.4%, whereas in the XXI century. studies in South Korea and Austria showed a prevalence of this disease at 14.4% (Lee J.H. et al., 2014) and 38.9% (Riss S. et al., 2012), respectively. It has been found that 25% of Britons and 75% of Americans report hemorrhoids at least once in their lives (Baker H., 2006; Tucker H. et al., 2008), this risk is especially high in pregnant women and the elderly.

Hemorrhoids are described in the literature as an increase and / or distal displacement of the cavernous vascular plexuses of the rectum, as well as the parts of the anal mucosa, loose connective tissue and smooth muscles of the rectum wall that cover them (Thomson WH, 1975; Lohsiriwat V., 2012; Lohsiriwat V. , 2013).

Clinically characterized by painless rectal bleeding during bowel movements with prolapse of the anal tissue or without it. As a rule, hemorrhoids can be divided into 2 types: internal and external. External hemorrhoids usually do not require special treatment, except when it causes the patient discomfort or causes the development of acute thrombosis. Therapeutic tactics in the case of hemorrhoids may include a therapeutic approach: local therapy and / or oral administration of drugs that affect the venous wall, as well as changes in lifestyle and diet. In the case of the ineffectiveness of these measures or with severe hemorrhoids, sclerotherapy, ligation of hemorrhoids or surgical interventions are indicated. Surgical treatment is indicated for internal hemorrhoids of stage III – IV or when non-surgical therapeutic approaches have failed or led to complications (Lohsiriwat V., 2015). Studies have shown that there is a tendency to self-medicate, rather than seek proper medical care, among people with hemorrhoids or those who mistakenly believed that they had hemorrhoids (Rohde H., Christ H., 2004). According to the 2012 Google Zeitgeist annual survey, hemorrhoids were the most common health problem in the United States, ahead of gastroesophageal reflux disease and sexually transmitted diseases. The danger of self-medication in this case is also associated with the low quality of information that patients can find on the Internet on this issue (Yeung T.M., D’Souza N.D., 2013). Therefore, clinicians should advise and treat patients with hemorrhoids using evidence-based medicine and medical care standards. Almost the majority of patients with external hemorrhoids can be effectively treated using non-surgical measures by a general practitioner, gastroenterologist or general surgeon on an outpatient basis.Surgical intervention is indicated for severe hemorrhoids or the ineffectiveness of other methods of treatment (Lohsiriwat V., 2012).

Painless rectal bleeding is the most common manifestation of hemorrhoids. It can be accompanied by prolapse of anal tissue, hemorrhoidal nodes. Blood usually does not mix with feces, but is clearly visible on the surface and has a bright red color, since the hemorrhoid plexus has a large number of arteriovenous shunts (Aigner F. et al., 2009). Hemorrhoid patients may experience pain in the anus. However, in fact, severe anal pain in a patient with hemorrhoids is more likely due to anal fissure and anorectal abscess.

An accurate history and a thorough physical examination, sigmoidoscopy and anoscopy are necessary for the diagnosis of hemorrhoids. Differential diagnosis may require sigmoidoscopy or colonoscopy, especially in patients who are at risk for colorectal cancer (Lohsiriwat V., 2013; Lohsiriwat V., 2012).

Heparin

Heparin is a sulfated polysaccharide that prevents blood coagulation (Onishi A. et al., 2016). The more than 100-year history of the study and clinical use of heparin began in 1916 when a 26-year-old medical student named Jay McLean impressed his mentor William Howell, professor of physiology at Johns Hopkins University, saying that he discovered "antithrombin" (Messmore HL et al., 2004). Another important date in the history of the study of heparin was 1918 (Rák K., 1998) - the year when Emmett Holt and William Howell gave the substance the name “heparin” (Ong CS et al., 2019 ) Commercial production began shortly after it was opened in the 1920s, and advanced cleaning methods led to animal studies and the first clinical studies in the 1930s (Barrowcliffe T.W. 2012). In 1928, Charles Best, MD, in Toronto, Canada, organized a group of chemists, physiologists, and surgeons to focus on heparin development. This group determined which animal tissues were the best source, carried out purification and identification, and determined the pharmacological properties of in vitro. By 1935, they were ready for human research. By 1941, scientists reported a group of 700 patients who received glycosaminoglycan treatment called heparin (Messmore H. L. et al., 2004). Studying the chemical structure of heparin turned out to be a difficult task, but the structure of the main disaccharide unit was established by the 1960s, but knowledge of the heterogeneity and structure of heparin chains continued to accumulate over the next 20 years (Barrowcliffe T.W., 2012). The introduction of new tests for laboratory monitoring has made it possible to clarify the dose of heparin for clinical use in the 1960s and 1970s. The use of heparin allowed the development of hemodialysis and pulmonary bypass surgery, as well as the prophylaxis of deep vein thrombosis in surgical patients (Messmore H. L. et al., 2004). In 1976, it was found that only one third of the heparin chains has a high affinity for antithrombin, and subsequent studies have revealed a unique pentasaccharide sequence that is necessary for binding of antithrombin and anticoagulant activity. This pentasaccharide was synthesized in 1983. The clinical use of heparin continued to expand, and the two main developments were the use of low doses of heparin for the prevention of deep vein thrombosis and pulmonary embolism, as well as the development of low molecular weight heparin as a separate drug (Barrowcliffe T.W., 2012). Already in the 1960s, the possibility of topical use of heparin in proctology for the treatment of hemorrhoids (Ogawa P., de Figueiredo JC, 1966), as well as its use for the treatment of anorectal diseases in combination with glucocorticoids (Forni G., Nanni Costa P. , 1962).

Prednisone

Prednisolone is a synthetic glucocorticoid widely used in medicine.The pharmacokinetics of prednisone is dose dependent (Frey B.M., Frey F.J., 1990).

The clinical response to the administration of prednisone is due to its affinity for specific receptors in the tissues (Frey F.J., 1987). Prednisolone has versatile properties. Among them, a decrease in the migration of pro-inflammatory cells to the focus of inflammation, suppression of the function of these cells. Prednisone also reduces tissue edema by reducing histamine release and lower capillary permeability. It also inhibits collagen synthesis, affects carbohydrate metabolism, reduces antibody production, and has a catabolic effect in tissues. The effect of prednisolone on water-salt metabolism lies in the fact that it promotes the elimination of K ions⁺ and Ca²⁺, at the same time traps Na ions⁺, which leads to fluid retention in the body. The clinical effects of prednisolone include anti-inflammatory, decongestant, anti-allergic (these effects of prednisolone appear in the drug Proctosan Neo), and in high doses - immunosuppressive and antiproliferative.

In the 60s of the twentieth century. rectal administration of prednisolone was even proposed to be used in the treatment of bronchospastic syndrome (Adelmann G., 1967).

Polydocanol

Polydocanol is the most commonly used sclerosant for sclerotherapy worldwide (Doganci S. et al., 2016). It is a detergent, that is, it causes protein denaturation upon contact, and polydocanol also has an antipruritic and analgesic effect, since it reduces sensitivity by interrupting the transmission of impulse. In recent years, polydocanol has been widely used for the treatment of hemorrhoids (Fernandes V., Fonseca J., 2019; Rosa B., 2019), complications of hemorrhoids and their treatment (Santos-Antunes J. et al., 2016), as well as for varicose sclerotherapy expansion of veins and spider veins. The efficacy and safety of the use of this drug as an alternative treatment for varicose veins of the esophagus and stomach, tendinopathy and epicondylitis, vascular malformations, varicocele, hydrocele and spermatocele, aneurysmal bone cysts, itching, gastrointestinal bleeding, simple renal cysts, are currently being studied. reducing the frequency and severity of radio-induced dermatitis (Ebrahimi SRS et al., 2017). A recent in vivo study on the chorion-allantoic membrane model of chickens examined the ability of polydocanol to inhibit vascular growth. It was found that polydocanol has an antiangiogenic effect (p0.05). This effect of polydocanol is particularly interesting in light of the data on the probability of the contribution of microvessel neoplasm to the pathophysiology of hemorrhoids (Chung Y. C. et al., 2004).

Proctosan Neo It is an effective local remedy for the treatment of hemorrhoids, anal fissures, itching and eczema of the anal area. Its effect is due to the complementary effects of the components of this drug. Given the systemic absorption of its components, one should bear in mind a possible overdose (despite the fact that it is unlikely), as well as the fact that the drug is contraindicated in the first trimester of pregnancy. To avoid the development of systemic side effects of prednisone Proctosan neo should not be used for more than 2 weeks in a row. The drug is dispensed without a prescription, however, it is not recommended to use it as a self-medication. If there is no regression of symptoms after a few days of admission, you should consult a doctor again.