Enzyme preparations: 5-alpha reductase inhibitors
In prostate tissue, type I enzyme has little biological activity.
The enzyme 5-alpha reductase type II is localized in the prostate, testicles and their appendages, glans penis, scrotum, seminal vesicles, liver, and chest. It is most active in prostate tissue and converts the male sex hormone testosterone into the more potent androgen dihydrotestosterone (DHT). The isoenzymes (or isoenzymes) of this enzyme differ in amino acid sequence, but perform the same catalytic function. Both isoenzymes are detected in normal prostatic tissue. In benign prostatic hyperplasia (BPH), their overexpression is noted, which leads to hyperplasia of stromal and epithelial cells in the transition zone and paraurethral glands. Excessive production of DHT can lead to androgen-dependent conditions such as BPH, prostate cancer, acne, alopecia, etc. Finasteride and Dutasteride are used to treat and prevent the progression of BPH, reduce its size, improve urination and reduce the risk of acute urinary retention. After the use of these drugs, the concentration of DHT in the blood serum and in prostate tissue is effectively reduced, and apoptosis of prostatic epithelial cells is induced. With long-term course use, the volume of the prostate decreases by an average of 15–25%, the peak flow rate of urination increases and, thus, the severity of symptoms decreases and the mechanical component of obstruction in BPH is eliminated. Finasteride (Finasteride) - TN “Alfinal”, “Prosteride”, “Penester” , table. 5 mg, is a synthetic derivative of 4-azandrostane, a competitive specific inhibitor of type II 5-alpha reductase. In patients with BPH who took Finasteride at a dose of 5 mg/day. over a 3-year period, there was a decrease in serum DHT concentrations of approximately 70% and a decrease in prostate volume of approximately 27% compared to baseline values. PSA concentrations decreased by approximately 50% compared to baseline values, which helps reduce the growth of prostate epithelial cells. Serum testosterone concentrations increased by approximately 10–20%.
It was found that long-term (more than 4 years) use of Finasteride in patients reduced the risk of developing urological complications and surgical interventions by 51%. The drug has no affinity for androgen receptors, does not affect the lipid profile and the levels of cortisol, estradiol, prolactin, thyroid-stimulating hormone and thyroxine in the blood plasma. Food intake does not affect bioavailability, which is 80%. The maximum concentration in blood plasma is reached approximately 2 hours after oral administration. The recommended dose is 1 tablet. 1 per day. Absorption is independent of food intake. Duration of treatment is up to 6 months; if necessary, treatment can be continued until a pharmacotherapeutic effect is achieved.
Important! When using the drug, the following side effects can often develop: impotence, decreased libido, ejaculation disorders, decreased ejaculate volume, skin rash, urticaria, angioedema of the lips and face. However, in most patients these phenomena were transient.
Dutasteride (Dutasteride) - TN "Dutasteride Bacter", "Avodart" , caps. 0.5 mg - dual 5-alpha reductase inhibitor, suppresses the activity of 5-alpha reductase isoenzymes type I and II. The maximum effect of Dutasteride on reducing the concentration of DHT is dose-dependent and is observed 1–2 weeks after the start of treatment: when taking the drug at a dose of 0.5 mg per day, the average concentration of DHT in the blood serum is reduced by 85 and 90%, respectively. After taking one dose (0.5 mg), the maximum concentration of Dutasteride in the blood serum is achieved within 1–3 hours. Absolute bioavailability is about 60%, relative to a 2-hour IV infusion. Bioavailability is independent of food intake and has a high degree of binding to plasma proteins (>99.5%). It has a large distribution volume - from 300 to 500 liters. When taken daily, the concentration of the drug in the blood serum reaches 65% of the stable level after 1 month and approximately 90% of the stable level after 3 months.
The capsule of the drug should be swallowed whole without chewing or opening, since its contents may cause irritation of the oropharyngeal mucosa. Dutasteride does not have a specific antidote, so if an overdose is suspected, it is sufficient to carry out symptomatic and supportive treatment.
Bovhyaluronidase azoximer (Bovhyaluronidasum azoximerum) - TN "Longidaza" , lyophilisate for the preparation of injection solution. 1500 IU or 3000 IU, applied subcutaneously or intramuscularly. 1 ampoule or bottle contains a conjugate of the proteolytic enzyme hyaluronidase with a high-molecular carrier, possessing the full range of pharmacological properties inherent in drugs with hyaluronidase activity. The specific substrate of hyaluronidase is glycosaminoglycans - “cementing” substances of connective tissue. As a result of hydrolysis, the viscosity of glycosaminoglycans, which are capable of binding water and metal ions, decreases. As a result, tissue permeability increases, trophism improves, swelling decreases, hematomas resolve, the elasticity of scarred areas increases, contractures (Latin contractura - tightening, narrowing) and adhesions (overgrowth of connective tissue) are eliminated. The effect is most pronounced in the initial stages of the pathological process.
The clinical effect of bovhyaluronidase azoximer is significantly superior, and its allergenic and irritant properties are reduced compared to native hyaluronidase. Conjugation increases the enzyme's resistance to temperature and inhibitors, increases its activity, which leads to prolongation of action. The enzymatic activity of the drug is maintained when heated to 37°C for 20 days, while native hyaluronidase loses its activity within 24 hours under the same conditions. Bovhyaluronidase azoximer has chelating, antioxidant, anti-inflammatory, immunomodulatory activity and has an antifibrotic effect.
Important! Contraindications include hypersensitivity to the drug, acute infectious diseases, malignant neoplasms, age under 18 years, acute renal failure. Methods of application are selected by the doctor depending on the diagnosis, severity of the disease, clinical course, and age of the patient.
Combination drugs
Currently, there are two combination drugs on the pharmaceutical market containing the α1A-blocker tamsulosin with 5-alpha reductase inhibitors - finasteride and dutasteride. When using combination drugs together, caution is recommended, because Concomitant use of these drugs may potentially lead to symptomatic hypotension. Patients should be informed about the possibility of symptoms associated with orthostatic hypotension, such as severe dizziness, blurred vision, cramps in the arms and legs, confusion, weakness, sweating, etc.
Tamsulosin + Finasteride - TN "Soniride Duo" , produced in a set: tamsulosin (modified release capsule, 0.4 mg) and finasteride (table, film coating, 5 mg). Soniride Duo is intended for the treatment and control of symptoms of benign prostatic hyperplasia (BPH) when combination treatment is necessary for the purpose of:
- achieving regression in the size of the prostate gland, improving urination and reducing symptoms of the lower urinary tract caused by BPH;
- slowing the clinical progression of the disease and reducing the incidence of acute urinary retention and the need for surgical treatment, including transurethral resection of the prostate and prostatectomy.
Important! Soniride Duo can only be used if the prostate gland is enlarged (prostate volume is more than 40 cm3). With such an enlarged prostate, combination treatment alleviates the symptoms of BPH and slows the clinical progression of the disease more effectively than monotherapy with these drugs. For the full therapeutic effect, long-term use of the drug Soniride Duo is necessary.
Tamsulosin + Dutasteride - TN "Duodart", caps. 0.5 mg + 0.4 mg is a combination of two components with complementary mechanisms of action that help eliminate symptoms in patients with BPH. The modified release formulation contains a soft gelatin capsule containing dutasteride and a pellet containing tamsulosin hydrochloride. Application: for the treatment and prevention of progression of BPH by reducing its size, eliminating symptoms, increasing the speed of urination, reducing the risk of acute urinary retention and the need for surgical intervention. Duodart is taken 1 capsule of each component 1 time per day, after approximately 30 minutes. after the same meal. Capsules should be taken whole, without chewing or opening them, with water. Bioequivalence was found between Duodart and the simultaneous administration of separate capsules of dutasteride and tamsulosin.
Important! Contact of the contents of the hard capsule inside the soft gelatin with the mucous membrane of the oral cavity can cause inflammation in the latter.
Similar products and their costs
Popular analogues of Afalaza include:
- Speman;
- Uroprofit;
- Finast;
- Tadenan;
- Prostamol Uno.
Speman
Speman is classified as a combination preparation containing substances of plant origin.
The medicine is produced in India on the basis of 9 components, such as: orchis root, astercanthus longifolia, velvet bean fruits, pearl parmelia, compass lettuce shoots, laptenia stem, tribulus fruits, beautiful argyrea, mosaic gold.
Speman stimulates the formation of sperm, increases the motility of male germ cells, and has prostatotropic and anti-inflammatory effects.
The average price for the drug is 300-350 rubles.
Uroprofit
A Russian-made product produced by. The main components of the medicine are herbal components: cranberry fruits, bearberry leaves, horsetail. In addition, the drug contains arbutin, proangocyanidins, and vitamin C. The active substances not only have antimicrobial, antispasmodic and diuretic effects, but also prevent the development of urolithiasis.
The herbal remedy normalizes urination, reduces the risk of recurrence of cystitis, and helps improve the condition of the urinary tract. The release form of Uroprofit is capsules. The average price is 340 rubles.
Finast
This is an Indian hormonal antitumor drug. The main active ingredient is finasteride. Auxiliary components include lactose, sodium docusate, corn starch, MCC, magnesium stearate, sodium carboxymethyl starch. Indications for use of Finasta:
- treatment of benign prostate tumors, as a result of which its size decreases and the pathological process slows down;
- treatment of symptoms of prostatic hyperplasia, normalization of urine outflow.
The product should not be taken by people who are allergic to any of the components of the drug. Finast is contraindicated in patients with prostate cancer. The drug should absolutely not be used to treat women.
The product is available in the form of tablets coated with a protective coating. The cost ranges from 350 to 400 rubles.
Tadenan
A drug produced in France. The medicine contains only 2 components: African plum bark extract and peanut oil. The product has a beneficial effect on the functioning of the prostate gland, helping to eliminate urinary disorders such as:
- nocturia;
- dysuria;
- pollakiuria.
The tablets relieve inflammation around the gland tissue, restoring its physiological functions. Tadenan is also effective after surgery; it helps to minimize the risk of relapse of the disease. The drug is intended for the treatment of men; there is no data on the effect of Tadenan on the female body.
The product is available in gelatin capsules. The medicine can be found on sale at a price of 190 rubles.
Prostamol Uno
This is a German substitute for Afalaza. The main active ingredient is an alcoholic extract of sabal palm fruits. The product has anti-edema, anti-androgenic and anti-inflammatory effects. Prostamol Uno is used for urinary dysfunction caused by prostate adenoma. The drug slows down the growth of the hypertrophied gland, but does not reduce it.
The medicine is available in capsules for oral use. The cost of tablets is high and ranges from 1800 to 2000 rubles.
Doctors recommend not to self-medicate, but to go to the hospital to select a suitable analogue of Afalaza.
Specific antibody preparations
Humanity has long discovered the effect of antibodies. These are special molecules that are produced by cells of the immune system to recognize foreign antigens. Subsequently, antigen binding and destruction occurs. Antibodies are specific. This means that they recognize only their antigen or determinant group (a separate fragment). One antigen may contain several such determinant groups and different antibodies will be formed to them. When an antigen is introduced into the body, a large number of different types of antibodies are formed, directed exclusively at one type of antigen. This allows for adequate immune protection. Antibodies are widely used in the treatment of many diseases.
Afalaza, tab. d/rass. - complex preparation, includes active ingredients - antibodies to endothelial NO synthase, affinity-purified, 0.006 g each, and antibodies to prostate-specific antigen (PSA), affinity-purified, 0.006 g each, which are applied to lactose in the form of a mixture of three active aqueous-alcoholic dilutions of the substance, respectively 10012, 10030, 100200 times. The combined use of components in the drug is accompanied by a synergistic effect.
Affinity-purified antibodies to prostate-specific antigen modify the functional activity of endogenous PSA. The regulatory influence of the antigen on functional and metabolic processes in prostate tissue is enhanced.
The drug has a pronounced anti-inflammatory, decongestant and vegetative stabilizing effect. The combined use of components improves spermatological indicators: increasing the concentration of sex hormones, the number of sperm and their motility, reducing the viscosity of seminal fluid, normalizing prostate secretions. Regenerative and repair processes are activated in patients who have undergone surgery and the likelihood of developing complications after surgery is reduced. It is possible to carry out a second course of treatment after 1–4 months. The course of treatment and dosage (primary and repeated) is determined by the attending physician.
"Afala" , tab. d/rass. — the active component of the drug is affinity-purified antibodies to prostate-specific antigen, 0.003 g each. When using the drug, inflammation and swelling are reduced, urodynamics are improved, the volume of residual urine is reduced, dysuric disorders are reduced and the tone of the lower urinary tract and the functional state in the prostate gland are normalized. The drug is used for BPH stages I and II. The drug is part of the complex therapy of acute and chronic prostatitis, as an anti-inflammatory and analgesic. It is used for dysuric disorders, such as frequent urge to urinate, including at night, difficulty urinating, pain or discomfort in the perineal area.
Important! Contraindication is increased individual sensitivity to the components of the drug. Not recommended for use in patients under 18 years of age due to insufficient data on efficacy and safety for this age. Afala does not affect the ability to drive vehicles and other potentially dangerous mechanisms.
Features of the product
A common drug prescribed to prevent the development of prostate adenoma is afolase. The effectiveness of the drug has been confirmed in practice. This medicine has an affordable price. It can be bought at a pharmacy without a prescription.
The main components of the product are two types of antibodies. The instructions for use of the product describe in detail its pharmacological effects. When taken, a targeted medicine increases blood flow in the tissues of the prostate gland and penis. The active ingredients have a positive effect on endothelium, ensuring an improvement in the general condition of blood vessels. During treatment, functional and metabolic processes are normalized, inflammation and swelling are relieved.
The active substances included in the drug are affinity purified. That is, they undergo special processing to remove other proteins and components of the donor's DNA. This guarantees the absolute safety of the drug. When taking it, the risks of negative side reactions of the body are minimized.
