Bioquinol indications. Antisyphilitic drugs. Classification. Pharmacological characteristics of drugs of various groups (mechanism of action, side effects). Similar drugs

Analogues (generics, synonyms)

Bismoverol

Recipe (International)

Rp.: Sol. Biochinolum 100 ml

D.S. according to the scheme

pharmachologic effect

It has a therapeutic effect in spirochetosis (human diseases caused by microorganisms of a spiral form), as well as anti-inflammatory and resolving effects.

Mode of application

For adults: Intramuscularly in the upper outer quadrant of the buttocks, in a two-stage way. Before injection, the vial is heated in warm water and shaken thoroughly. With syphilis - 3 ml every fourth day. Heading dose - 40-50 ml. The highest single dose for adults is 3 ml (every 3 days). Children according to age.
With nonspecific lesions of the central nervous system, 2 ml every other day. Heading dose - 30-40 ml, depending on the stage of the process.

Indications

All forms of syphilis (in combination with penicillin preparations);
- non-specific lesions of the central nervous system: arachnoencephalitis (inflammation of the membranes and tissues of the brain), meningomyelitis (simultaneous inflammation of the membranes and tissues of the spinal cord), etc.;
- trauma of the skull.

Contraindications

Age up to 6 months.
- kidney disease
- liver
- hemorrhagic diathesis (increased bleeding)
- severe forms of tuberculosis
- decompensation of cardiac activity (a sharp decrease in the pumping function of the heart)


- hypersensitivity to quinine.

Side effects

Possible drooling
- gingivitis (inflammation of the mucous membrane of the gums)
- stomatitis (inflammation of the oral mucosa)
- dermatitis (skin inflammation), bismuth nephropathy (kidney damage due to biyoquinol treatment)
- albuminuria (protein in the urine)
- polyneuritis (multiple inflammation of the peripheral nerves) and trigeminal neuritis (inflammation of the facial nerve).

Release form

In bottles of 100 g.

ATTENTION!

The information on the page you are viewing was created for informational purposes only and does not promote self-treatment in any way. The resource is designed to familiarize healthcare professionals with additional information about certain medicines, thereby increasing their level of professionalism. The use of the drug Bioquinol"mandatory provides for a consultation with a specialist, as well as his recommendations on the method of application and dosage of the medicine you have chosen.

Dosage forms: 8% suspension of quinine bismuth iodine in neutralized peach or olive oil. In vials of 100 ml.

Medicinal properties: Anti-inflammatory.

Storage: List B.

Indications for the use of Bioquinol

All forms of syphilis (in combination with penicillin preparations), non-syphilitic lesions of the central nervous system (arachnoencephalitis, meningomyelitis, etc.), skull injuries.

Contraindications

Bioquinol is forbidden to be taken under the age of 6 months. Diseases of the kidneys, liver, hemorrhagic diathesis, severe forms of tuberculosis, cardiac decompensation, gingivitis, stomatitis, hypersensitivity to quinine.

Side effects

Bioquinol can cause salivation, the appearance of a dark blue border along the edge of the gums, gingivitis, stomatitis, dermatitis, bismuth nephropathy, albuminuria, polyneuritis and trigeminal neuritis.

Instructions for use

V/m. To avoid getting into the vessel before injection, the vial is heated in warm water and shaken thoroughly. With syphilis, 2-3 ml is administered 1 time in 2-3 days (at the rate of 1 ml per day). The course dose is 40-50 ml.

The highest single dose for adults is 3 ml (1 time in 3 days). With nonspecific lesions of the central nervous system, 2 ml every other day. The heading dose is 30-40 ml, depending on the stage of the process.

Price in pharmacies

The price of Bioquinol in different pharmacies can vary significantly. This is due to the use of cheaper components and the pricing policy of the pharmacy chain.

Antisyphilitic there are drugs used to treat syphilis with the aim of selectively influencing its causative agent, pale treponema (Treponemapallidum). They belong to the group of protispirochetosis drugs, they are also prescribed for the treatment of other spirochetosis (for example, relapsing fever) and leptospirosis.

For drug therapy of all stages of syphilis, antibiotics are used. In the later stages of syphilis, iodine compounds are also prescribed to accelerate the resorption of rubbers. (potassium iodide ) or bismuth preparations (biyoquinol and bismoverol).

History reference. The first specific antisyphilitic drugs were organic compounds of arsenic ( salvarsan , novarsenol and others), which were invented by the founder of chemotherapy, the famous German scientist, Nobel laureate Paul Ehrlich in 1910.

P. Ehrlich suggested the effectiveness of such a compound in the treatment of trypanosomiasis ("sleeping sickness") to study the prosyphilitic activity of arsenic compounds. Due to high toxicity and insufficient efficacy, arsenic preparations have not been used in clinical practice for a long time.

(1854-1915)

Classification of antisyphilitic drugs

Origin antisyphilitic drugs are divided into

1. Antibiotics:

Benzylpenicillin preparations (salts benzylpenicillin - sodium, novocaine, benzathine or bicillin-1) and other penicillin antibiotics ( ampicillin, oxacillin)

Cephalosporins ( cefazolin, ceftriaxone)

Macrolides and azalides ( erythromycin, josamycin, azithromycin)

Tetracyclines (doxycycline).

2. Synthetic compounds:

Bismuth preparations ( biyoquinol, bismoverol).

By efficiency Antisyphilitic antibiotics are divided into 3 groups:

1. Fixed assets (and rows).

2. Alternative means (second row).

3. Reserve funds.

Fixed assets. Antisyphilitic drugs and a number of drugs are benzylpenicillin (sodium, potassium salts, as well as benzathine benzylpenicillin other Bicillin), which are used intramuscularly. These antibiotics quickly kill the causative agent of syphilis, Treponema pallidum - they exhibit a treponemocidal effect. The causative agent of syphilis does not acquire resistance to antibiotics.

In some patients, at the beginning of antibiotic therapy, within a few hours after the first injection, the general condition of the patient worsens with the development of symptoms of intoxication - body temperature rises, headache, tachycardia, myalgia, and general weakness occur. Such a side effect of antibiotic therapy was called the Jarisch-Herxheimer Reaction (Jarisch - Herxheimer Reaction - named after the Austrian and German dermatologists who first described it after the use of mercury preparations in patients with syphilis. In the domestic literature it is known as the Herxheimer - Yarish - Lukashevich reaction). The reaction can also occur during antibiotic therapy of other infectious diseases due to the bactericidal action of antimicrobial agents - through the mass death of microorganisms and the rapid entry into the blood of a large number of endotoxins of dead bacteria. This side effect of antibiotic therapy is transient, disappears within one day, can be prevented and does not require special additional treatment. In the case of a general severe condition of the patient, for example, due to a syphilitic lesion of the aortic valve, the patient is given desensitizing agents - glucocorticoids in advance, before the start of antisyphilitic antibiotic therapy, to prevent the occurrence of the Jarisch-Herxheimer reaction.

Alternative means(means of the II series) is macrolides (erythromycin, josamycin) and tetracycline (doxycycline), they are used mainly for allergies to penicillins. Erythromycin is inferior in effectiveness to other drugs of the second row; in addition, it does not pass the hematoplacental barrier and does not have a therapeutic effect on the fetus. Therefore, newborns (in the case of pregnant women treated with erythromycin) are treated with benzylpenicillin preparations.

Rarely prescribed other antibiotics penicillin row (ampicillin, amoxicillin, oxacillin) and cephalosporins (cefazolin, ceftriaxone), which have a wide spectrum of antimicrobial activity, when there is a need for the simultaneous treatment of concomitant infections. Ceftriaxone has the ability to accumulate in the brain in high concentrations, so it is prescribed for neurosyphisis.

Reserve antisyphilitic drugs(means of the III row) consider azalides (azithromycin). In terms of effectiveness, reserve and alternative drugs are inferior to benzylpenicillin preparations.

Bismuth preparations. Complex preparations of bismuth (biyoquinol, bismoverol) are specific antisyphilitic drugs - they act on pale trepoiem and do not show a broad antibacterial effect. The type of antibacterial action is bacteriostatic (treponemostatic type of action). The mechanism of action is due to the blocking of sulfhydryl groups (SH-groups) of microbial enzymes. In terms of activity and speed of onset of the effect, bismuth preparations are inferior to antibiotics.

Bioquinol(biiochinolum) is an 8% suspension of quinine iodobismuthate in neutralized peach oil, i.e. contains bismuth (bi), iodine (io) and quinine (chin) in peach oil (oe). It has additional anti-inflammatory and resolving effects. It is produced in vials for parenteral (intra-hypnotic) injections of 100 mx, administered intramuscularly at 2 (3) ml 1 time in 2 (3) days, that is, at the rate of 1 ml per day.

Bismoverol(bismoverolum) - 7% suspension of the basic bismuth salt of monobismuth-tartaric acid in neutralized peach (or olive) oil.

Bismuth preparations are prescribed for all forms of syphilis in combination with antibiotics. They are especially effective in neurosyphilitic lesions. Bismuth preparations also have anti-inflammatory and resolving effects, so they are used for non-syphilitic lesions of the central nervous system (arachnoencephalitis, meningomyelitis, residual effects after cerebral strokes). They are not absorbed from the digestive tract, so they are administered intramuscularly. It is excreted mainly by the kidneys, as well as in small amounts by the intestines and sweat glands.

Side effects: gingivitis, stomatitis, the appearance of a gray border along the edge of the gums (bismuth border), gray spots on visible mucous membranes, colitis, diarrhea, dermatitis, nephropathy (relatively frequent, usually disappear after discontinuation of the drug), hepatitis. When using bismuth preparations, it is necessary to monitor the condition of the oral mucosa, kidney and liver function.

Classification of antisyphilitic drugs

1. Preparations of benzylpenicillin:

A) short-acting (benzylpenicillin sodium and potassium salts)

B) long-acting (novocaine salt of benzylpenicillin, bicillins)

2. Other antibiotics (tetracycline, erythromycin, cephaloridine)

3. Bismuth preparations (biyoquinol, bismoverol)

The main place in the treatment of syphilis is occupied by drugs benzylpenicillin. For this purpose, both short-acting (benzylpenicillin sodium or potassium salt) and long-acting (benzylpenicillin novocaine salt, bicillins) preparations are used. Benzylpenicillin has a rapid and pronounced

treponemicidal action. The development of resistance to it in pale treponema was not noted. Benzylpenicillin preparations are effective for syphilis at all its stages. They are prescribed in courses, the duration of which is determined by the form and stage of the disease.

In case of intolerance to benzylpenicillin (for example, due to allergic reactions), other antibiotics, tetracyclines, as well as erythromycin, azithromycin, ceftriaxone, can be used to treat syphilis. However, they are inferior in effectiveness to benzylpenicillin preparations.

In addition to antibiotics, in the treatment of syphilis, bismuth preparations. These include biyoquinol (8% slurry of quinine iodobismuthate in neutralized peach oil) and bismoverol (suspension of the basic bismuth salt of monobismuth tartaric acid in neutralized peach oil). Unlike antibiotics, the spectrum of action of bismuth preparations is limited to the causative agent of syphilis. In activity, they are inferior to benzylpenicillin. Their treponemostatic effect is associated with the inhibition of enzymes containing sulfhydryl groups. The therapeutic effect of bismuth preparations develops much more slowly than benzylpenicillin. Bismuth preparations are not absorbed from the gastrointestinal tract, and therefore they are administered intramuscularly.

They are excreted mainly by the kidneys, as well as in small amounts by the intestines and sweat glands. Bismuth preparations are used for all forms of syphilis.

Side effects are relatively rare. Typical for the action of these drugs is the appearance of a dark border along the edge of the gums (the so-called bismuth border). Perhaps the development of gingivitis, stomatitis, colitis, diarrhea, dermatitis. Rarely, kidney and liver damage is observed.

When using bismuth preparations, it is necessary to monitor the condition of the oral mucosa, kidney and liver function.



In the later stages of syphilis, gum is prescribed to accelerate the resorption iodine compounds(potassium iodide).

Preparations


Benzylpenicillin preparations

Benzylpenicillin is an antibiotic that is a waste product of various species of the fungus Renicillinum. In medical practice, it is used in the form of sodium, potassium, novocaine salts of benzylpenicillin.

Benzylpenicillin is active mainly against gram-positive cocci (staphylococci, pneumococci, streptococci), gram-negative cocci (gonococci, meningococci), anthrax, diphtheria bacilli, spirochetes and some pathogenic fungi. Antibiotic-resistant Gram-negative bacteria (Escherichia, Pseudomonas aeruginosa, Klebsiella, Salmonella, Shigella), Mycobacterium tuberculosis, Rickettsia, viruses, protozoa.

Mechanism of action.

Antibiotics of the penicillin group are specific inhibitors of cell wall biosynthesis, and the selectivity of their action is determined by some features of the structure of the bacterial cell wall, compared with the animal. Under the influence of bacteriostatic concentrations of the antibiotic, growing cells stop dividing, their morphology changes dramatically. Microbes significantly increase, swell or take an elongated shape. The altered cells disintegrate with the formation of small particles and die. The basis of the antibacterial action is the suppression of the synthesis of murein - the supporting polymer of the cell wall.

Penicillin inhibits the last step in cell wall synthesis by preventing the formation of peptide cross-links between linear murein chains. Due to the structural similarity of penicillin to the peptide substrate of the cell wall, the antibiotic competes with it for the active site of transpeptidase.



Penicillin is used in the form of aqueous solutions (sodium, potassium soluble salts) or suspensions (novocaine, bicillin and other sparingly soluble salts).

After i / m administration, sodium and potassium salts of benzylpenicillin are absorbed very quickly. The concentration in the blood reaches a maximum after 15 minutes and lasts 3-4 hours.

Penicillin easily crosses the placenta, and 1-6 hours after administration to the mother's body, its concentration in the bloodstream of the fetus is 25-30% (from 10-50%) of the level in maternal blood. Penicillin is excreted in the urine (50-70%), as well as in saliva, sweat, milk and bile.

Side effects.

Headache, fever, urticaria, rash on the skin and mucous membranes, joint pain, eosinophilia, angioedema, there may be anaphylactic shock. With severe allergic reactions, adrenaline, glucocorticoids, antihistamines, penicillinase are prescribed. In anaphylactic shock: the introduction of adrenaline, diphenhydramine, calcium chloride, the use of cardiac drugs, the inhalation of oxygen, warming, after removing from the state of shock, penicillinase is administered.

Benzylpenicillin novocaine salt.

Novocaine salt is a long-acting drug that provides a therapeutic concentration of penicillin in the blood for up to 12 hours. It is excreted from the body with urine.

Bismuth preparations

Bioquinol - 8% suspension of quinine iodobismuthate in neutralized peach oil.

Bioquinol is used to treat various forms of syphilis, mainly in combination with antibiotics of the penicillin group. Enter intramuscularly. Due to the presence of anti-inflammatory and absorbable properties in biyoquinol, it is used in the treatment of non-syphilitic lesions of the central nervous system: arachnoencephalitis, meningomyelitis, etc. Side effects: the appearance of gingivitis and stomatitis, a gray border appears relatively often along the edge of the gums and around individual teeth (especially carious). Perhaps the appearance of gray spots on the mucous membrane of the cheeks, tongue, palate. Very often there is nephropathy, which disappears after discontinuation of the drug.

Bismoverol .

Used to treat patients with syphilis, usually in combination with antibiotics of the penicillin group. Enter intramuscularly.

Contraindications and side effects are the same as when using biyoquinol.