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Proteases - drug of the choice in the pharmacotherapy of lymphedema

Machanova1 M., Wald2 M., Prausova3 J., Bechyne4 M., Adamek2 J. Proteases - drug of the choice in the pharmacotherapy of lymphedema. 1 Oncology Department, Liberec Hospital, 2 Department of Surgery, 2nd Medical Faculty UK, Prague, 3 Oncology Department, Faculty Hospital Motol, Prague, 4 Dermatology Clinic, Faculty Hospital Bulovka, Prague. 2000


In the oncological literature of the past decades mainly the survival time was emphasized. Currently the quality of patients' life during and after the treatment also becomes more and more important. Each physician dealing with the treatment of malignant tumors could confirm that some percentage of complications during radical treatment is unavoidable. However, it is important that treatment benefits prevail the risk of serious and unpleasant complications. Or, if such complications occur, they could be positively influenced by treatment. Lymphedema is one of the complications which affect mostly patients treated by combined treatment of surgery and radiotherapy.
Lymphedema, both primary and secondary (regardless of its cause), is a sign of serious lymph circulation disorders in particular area. If it is not treated adequately and in time, it leads to the irreversible damage of lymphatic system followed by complications, such as relapsing skin inflammations, fibrotization, tissue induration etc. Similar condition, more difficult to diagnose, appears during visceral disorders of lymphatic system.
Lymphedema can form shortly after the surgery or during radiation treatment.
However, it can also develop after few years. Mechanism of this disease is based on gradual decrease of the transport capacity of lymphatic system in particular area.
Lymphostasis causes a damage of valvulae and endothelium of lymphatic vessels. Their permeability increases, lymph flow is slowed down and lymphatic plugs are formed. Edema is formed as a result of extravazation of proteins and fibrin. Consequently, number of fibroblasts increases, neovascularization appears, and more cells typical for chronic inflammations occur. Number of collagen fibres also increases and sclerotization of tissue starts. All these mechanisms acting together multiply their effect and form a vicious circle of the disease. Thus, elephantiasis can insconspicuously develop.
Older conceptions of pharmacotherapy of lymphedema consisted of symptomatic treatments (diuretics, venopharmacs). In many cases they just aimed at prophylaxis or therapy of complications (antibiotics, antimycotics). Later on an immunomodulating therapy was also tried. Treatment by diuretics, which is unfortunately used up to these days, is currently considered by number of authors to be harmful and from the pathophysiology of lymphedema and macroorganism point of view medicaly wrong.
Use of proteases (hydrolases), administered orally but acting systemically (that means within the whole organism), introduced a fundamental change in the attitude towards the pharmacology of lymphedema. Combinations of plant and animal proteases are usually used: papain, bromelain, trypsin, chymotrypsin and event. pancreatin, amylase, lipase and rutoside (in our country registered preparations: Wobenzym® coated tablets, Phlogenzym® tbl.).
These combined enzyme preparations show effect on almost all pathophysiological mechanisms causing lymphedema. These drugs are, therefore, able to break the circulus vitiosus and normalize lymphatic circulation in the affected area. In the case of fully developed lymphedema at the stage III and IV they are able to improve significantly nutrient supply to already induced and sclerotized tissue.

What is a concrete relationship between pharmacological effects of proteases and pathophysiology of lymphedema?

Proteolytic and mainly fibrinolytic effect of proteases leads to a lysis of lymphatic plugs and restoring of lymphatic passages which can then more easily remove products of proteolysis of extravazally deposited fibrin and other proteins.
Significant antiedematous and edemaprotective effect of proteases, strenghtened by rutoside, improves rheological properties of lymph (and blood) and ensures improvement in the transporting capacity of lymphatic system and microcirculation. Activation of macrophages ensures a fast removal of proteolysis products. Activation of NK cells and other components of cellular and humoral immunity significantly positively influences chronic inflammatory processes in the indured tissue.
Analgetic effect is evoked by proteases both directly - by peptidolytic cleavage of pain mediators and indirectly - by lowering of oncotic pressure and restriction of inflammatory reaction.
Rheological effects (lowering of serum and plasma viscosity, lowering of thrombocyte aggregation and increase in flexibility of erythrocytes) ensure a better arterial blood supply and easier venous drainage.
Very important is also the vehiculum effect: proteases increase concentrations of antibiotics in blood and tissues and, therefore, facilitate a faster cure of acute and chronic infections.
Marta I. Korpan and Veronika Fialka from UNI Klinik fuer Physikalische Medizin und Rehabilitation, Wien conducted in 1993-95 a controlled randomized clinical study Wobenzym versus diuretics on female patients suffering from lymphedema after the breast ablation for carcinoma. Duration of the trial was 7 weeks and volumometric parameters were evaluated. Results of the treatment in the Wobenzym group were significantly better than in the group treated by diuretics.
Additionally, significantly more pain-free patients were found in the Wobenzym group.
The most frequent localization of lymphedema connected with malignant tumor and its treatment is the edema of homolateral arm during breast carcinoma. According to various authors a frequency of this complication is 7-30%. Thanks to better and moderate surgical techniques and more accurate radiation treatment the current statistics reveal better results than the older studies. A frequency of occurrence of breast carcinoma increases. Thus, the risk of formation and development of lymphedema refers to a big number of patients and represents a serious health and psychosocial problem. Every year there is approx. 4000 newly registered cases of breast carcinoma in the Czech Republic. Therefore, 270-1150 patients is under the risk of developing lymphedema.
Particular groups of patients:
l. M. Machanova
2. M. Bechyne, J. Tomanova, R. Bechynova
3. J. Adamek, J. Prausova, M. Wald
4. M.I. Korpan, V. Fialka