Antimicrobial Antimicrobial drugsdrugs

I. Antiseptics and disinfectants.I. Antiseptics and disinfectants.

II. Sulfonamides.II. Sulfonamides.

III. Synthetic chemotherapeutics.III. Synthetic chemotherapeutics.

Kharkov National Medical UniversityDepartment of Pharmacology and Medical Prescription

assistant Gordiychuk D.

Control of Microbial GrowthControl of Microbial Growth

Sterilizing AgentsSterilizing Agents-- kill everything (e.g. -- kill everything (e.g. heat, radiation) heat, radiation)

DisinfectantsDisinfectants-- kill most things. Too -- kill most things. Too strong for living tissues (e.g. lysol, NH3) strong for living tissues (e.g. lysol, NH3)

AntisepticsAntiseptics-- milder in action. Can be -- milder in action. Can be used topically, but not ingested. (e.g. used topically, but not ingested. (e.g. alcohol, iodine) alcohol, iodine)

ChemotherapeuticsChemotherapeutics-- can be ingested -- can be ingested (e.g. penicillin, sulfa drugs)(e.g. penicillin, sulfa drugs)

Medicines with an antimicrobial activity are divided into two groups:

1 – non-selective antimicrobial agents, causes most destructive effect on the majority of microorganisms (antiseptics and disinfectants).

2 - selective antimicrobial drugs (chemotherapeutic agents).

ORIGINS OF ANTISEPTICSORIGINS OF ANTISEPTICS

Joseph Lister (1827 - 1912)Joseph Lister (1827 - 1912) Realised that deaths from operations mostly occurred Realised that deaths from operations mostly occurred

from infection contracted during the operation as a result from infection contracted during the operation as a result of unclean practices. of unclean practices.

He started using Carbolic acid (phenol) during operations He started using Carbolic acid (phenol) during operations to maintain aseptic conditions with significant to maintain aseptic conditions with significant improvementsimprovements..

Like Semmelweiss he initially encountered opposition, Like Semmelweiss he initially encountered opposition, but use of his methods by the Germans during the Franco-but use of his methods by the Germans during the Franco-Prussian war in 1870 provided his major breakthrough Prussian war in 1870 provided his major breakthrough and over the next 10 years, the practise of aseptic surgery and over the next 10 years, the practise of aseptic surgery became accepted. became accepted.

►narrow-spectrumnarrow-spectrum and effective only and effective only against a limited variety of pathogens or against a limited variety of pathogens or broad-spectrumbroad-spectrum, affecting many , affecting many different types of pathogensdifferent types of pathogens

►bactericidalbactericidal if they kill the susceptible if they kill the susceptible bacteria or bacteria or bacteriostaticbacteriostatic if they inhibit if they inhibit the growth of bacteriathe growth of bacteria

Antimicrobials could be Antimicrobials could be

Antiseptics and disinfectants - a group of drugs that are able to inhibit the growth, development

or leads to death of microorganisms in the environment surrounding the patient or on the surface of the body.

Antiseptics - (anti- against; septicas - putrid). This is a group of medicines that are used to eliminate pathogens in the wound (skin, mucous membranes) in the gastrointestinal tract and urinary tract. Causes bacteriocidal or bacteriostatic effect depending on the concentration.

Disinfectants - used for disinfection of medical instruments, utensils, facilities, equipment, etc. Disinfection - a complex of measures aimed at prevention of infection in the wound (in the body as a whole) or to prevent the spread of infection.

• Draw a sharp line between antiseptics and disinfectants is not always possible, because many substances used in low concentrations as antiseptics, and higher - for disinfection.

Requirements for Requirements for antiseptics and antiseptics and disinfectants.disinfectants.

Must have a broad spectrum of action;Must have a broad spectrum of action; Rapid onset of action;Rapid onset of action; Should have a small latency period;Should have a small latency period; Should have a high activity;Should have a high activity; Must be chemically resistant;Must be chemically resistant; High availability and low cost;High availability and low cost; Lack of local irritant or allergic effects on tissues;Lack of local irritant or allergic effects on tissues; Minimal absorption from the place of their Minimal absorption from the place of their

application;application; Low toxicity.Low toxicity.

Sources of antisepticsSources of antiseptics► Early antiseptics were Early antiseptics were

probably vegetable extractsprobably vegetable extracts Many spices contain antibacterial Many spices contain antibacterial

agentsagents► Essential oils extracted from Essential oils extracted from

plants often have plants often have antibacterial propertiesantibacterial properties

► Lister used carbolic acid Lister used carbolic acid which chemically is a solution which chemically is a solution of phenolof phenol Phenol was originally extracted Phenol was originally extracted

from coal tar.from coal tar. Coal tar preparations are still Coal tar preparations are still

used today in therapeutic soaps used today in therapeutic soaps and shampoos.and shampoos.

•To characterize the antimicrobial activity of the antiseptic agents used phenol ratio which indicates action force of the antimicrobial agent in comparison with the phenol.•The difference between antiseptics and disinfectants -The objectives of their application.

Classification of Antiseptics Classification of Antiseptics and Disinfectants and Disinfectants (according (according

chemical structure)chemical structure)I. Inorganic I. Inorganic

substancessubstances 1. Halogens:1. Halogens: Iodine (2%, 3%, 5% Iodine (2%, 3%, 5%

alcochol solution)alcochol solution) IodinolumIodinolum IoddicerinumIoddicerinum Povidon-Iod (Betadinum)Povidon-Iod (Betadinum) IodophormIodophorm Lugol’s solutionLugol’s solution Chloramine BChloramine B Chlorhexidine Chlorhexidine

bigluconatebigluconate Pantocidum (Halazone)Pantocidum (Halazone)

2.2. Oxidizing agents:Oxidizing agents: Hydrogen peroxideHydrogen peroxide Potassium permanganatePotassium permanganate33.. Acids and alkalis:Acids and alkalis: Boric acidBoric acid Salicylic acidSalicylic acid Solution of ammoniaSolution of ammonia4. Metallic salts:4. Metallic salts: Hydrargyri dichloridumHydrargyri dichloridum Hydrargyri amidochloridumHydrargyri amidochloridum Silver nitrateSilver nitrate Copper sulfateCopper sulfate Zinc sulfateZinc sulfate Zinc oxideZinc oxide

Classification continuationClassification continuationII. Organic substancesII. Organic substances1. Aldehydes:1. Aldehydes: Formaldehyde (Formalinum)Formaldehyde (Formalinum) GlutaraldehideGlutaraldehide Hexamethylentetraminum Hexamethylentetraminum

(Methenamine)(Methenamine)2. Alcochols: 2. Alcochols: Spiritus aethylicus (Ethyl Spiritus aethylicus (Ethyl

alcohol)alcohol)3. Phenol derivatives:3. Phenol derivatives: Phenol (Phenolum purum, Phenol (Phenolum purum, Carbolic acid)Carbolic acid) Cresol (Tricresolum)Cresol (Tricresolum) ResorcinolResorcinol ThymolThymol BenzylbenzoatBenzylbenzoat4. Dyes: 4. Dyes: Methylenum blueMethylenum blue Brilliant green (Viride nitens)Brilliant green (Viride nitens) Etacridin lactateEtacridin lactate

5. Detergents:5. Detergents: AethoniumAethonium DecamethoxinDecamethoxin RoccalRoccal DimexidDimexid6. Tar, resins, products of 6. Tar, resins, products of

petroleum:petroleum: Pix liquida Betulae (Birch tar)Pix liquida Betulae (Birch tar) IchthyolumIchthyolum Liniment by VishnevskyLiniment by Vishnevsky7. Nitrofuran derivatives:7. Nitrofuran derivatives: Nitrofurasone (Furacilinum)Nitrofurasone (Furacilinum)8. Antiseptics from medicinal 8. Antiseptics from medicinal

plants:plants: ChlorophyliptumChlorophyliptum NovoimaninumNovoimaninum

ChlorineChlorine Discovered in 1774 by a Swede, C.W. Discovered in 1774 by a Swede, C.W.

ScheeleScheele It is a pale green, toxic, reactive gasIt is a pale green, toxic, reactive gas It is a powerful irritant and toxinIt is a powerful irritant and toxin

Used as a gas warfare agent in WWI Used as a gas warfare agent in WWI very nasty, inflicting lifelong damage on those very nasty, inflicting lifelong damage on those

who survivedwho survived The damaged lungs were possibly a factor in The damaged lungs were possibly a factor in

the 1918 flu pandemicthe 1918 flu pandemic Solution of chlorine in water is both a Solution of chlorine in water is both a

powerful bleach and disinfectant powerful bleach and disinfectant Semmelweis had used chloride of lime as Semmelweis had used chloride of lime as anan

antisepticantiseptic

HalogensHalogens

HalogensHalogensThe mechanism of antimicrobial The mechanism of antimicrobial

actionaction Denaturation of proteins of the Denaturation of proteins of the

protoplasm of microbial cells by protoplasm of microbial cells by reacting with the reacting with the amino group of amino group of the proteinsthe proteins, displacing , displacing hydrogenhydrogen..

Denatured protein loses its activity.Denatured protein loses its activity. In the In the presence of organic presence of organic

substancessubstances halogen’s halogen’s antimicrobial effectantimicrobial effect decreasesdecreases..

IodinesIodines

IodineIodine - active bactericidal element. - active bactericidal element. At a dilution of 1: 20 000 - kill vegetative forms of bacteria for 1 At a dilution of 1: 20 000 - kill vegetative forms of bacteria for 1

min,min, the dispute - 15 min.the dispute - 15 min. Alcoholic solution of Iodine 5%Alcoholic solution of Iodine 5% (5 g of Iodine, KI -2g, ethyl (5 g of Iodine, KI -2g, ethyl

alcohol 95% 100ml)alcohol 95% 100ml) An irritant and a distraction actionAn irritant and a distraction action INDICATIONS:INDICATIONS: Disinfection of the surgical field, disinfection of Disinfection of the surgical field, disinfection of

wounds, the surgeon's hands, in myositis, neuralgia.wounds, the surgeon's hands, in myositis, neuralgia. Iodine is partially absorbed into the blood from the skin and Iodine is partially absorbed into the blood from the skin and

exhibits resorptive effects, especially in children.exhibits resorptive effects, especially in children. SIDE EFFECT: Chemical burns, dermatitis.SIDE EFFECT: Chemical burns, dermatitis.

Halogens (Iodine)Halogens (Iodine) LUGOL'S SOLUTION (Iodine-1 part, 2 part -KI, water-17 part)LUGOL'S SOLUTION (Iodine-1 part, 2 part -KI, water-17 part) INDICATION:INDICATION: Mucos lubrication in pharynhitis and larynhitis. Mucos lubrication in pharynhitis and larynhitis.

IODDICERINE (Iodine, dimethyl sulfoxide, glycerol)IODDICERINE (Iodine, dimethyl sulfoxide, glycerol) Fungicidal, antimicrobial, antiviral, antinecrotic, antioxidant effect.Fungicidal, antimicrobial, antiviral, antinecrotic, antioxidant effect. !!!The most active Iodine preparation!!!!!!The most active Iodine preparation!!! Doesn’t irritate tissue, does not cause pain reaction, deeply penetrates Doesn’t irritate tissue, does not cause pain reaction, deeply penetrates

into the tissue.into the tissue. INDICATION:INDICATION: Inflammatory infection (purulent wounds, infectious Inflammatory infection (purulent wounds, infectious

ulcers, sore throats, tonsillitis, pulpitis, otitis, pyoderma, erosion of ulcers, sore throats, tonsillitis, pulpitis, otitis, pyoderma, erosion of the mucous membranes, mastitis, candidiasis, inflammatory diseases the mucous membranes, mastitis, candidiasis, inflammatory diseases of the genital organs).of the genital organs).

Topically in the form of tampons, turundul, napkins, irrigation, Topically in the form of tampons, turundul, napkins, irrigation, washing.washing.

Halogens (Chlorine Halogens (Chlorine disinfectants)disinfectants)

CHLORINE - active bactericidal element is active in the CHLORINE - active bactericidal element is active in the undissociated form of HOCl when Cl dissolved in water at undissociated form of HOCl when Cl dissolved in water at neutral and acidic pH.neutral and acidic pH.

Bleach - not less than 32% of free Cl. Antimicrobial action - Bleach - not less than 32% of free Cl. Antimicrobial action - fast, but not for longfast, but not for long

INDICATIONS: INDICATIONS: 0.2-0.5% sol. for the disinfection of premises, 0.2-0.5% sol. for the disinfection of premises, infective patients discharge (pus, sputum, urine, feces). infective patients discharge (pus, sputum, urine, feces).

Corrosive to metals.Corrosive to metals.

CHLORAMINE B - 25-29% active Cl.CHLORAMINE B - 25-29% active Cl. INDICATION: INDICATION: eye wash, hand disinfection, douching (0.25-eye wash, hand disinfection, douching (0.25-

0.5%), treatment of purulent wounds, burns, pustular skin 0.5%), treatment of purulent wounds, burns, pustular skin diseases (0.5-2%). Disinfection of premises, health products diseases (0.5-2%). Disinfection of premises, health products and non-metallic tool, selection of patients (1.5%).and non-metallic tool, selection of patients (1.5%).

Deodorizing properties.Deodorizing properties. 4-8mg CHLORAMINE B is able to sterilize 1 liter of water for 4-8mg CHLORAMINE B is able to sterilize 1 liter of water for

15-60 min. (Pantocid), if the water contains a lot of organic 15-60 min. (Pantocid), if the water contains a lot of organic substances.substances.

HalogensHalogensCHLORHEXIDINE BIGLUCONATE (Bisdiguanidine derivative).CHLORHEXIDINE BIGLUCONATE (Bisdiguanidine derivative).

Has the properties of chlorine and detergent compounds.Has the properties of chlorine and detergent compounds. Capable of damaging the plasma membrane of microorganisms.Capable of damaging the plasma membrane of microorganisms. Strong antibacterial and fungicidal action.Strong antibacterial and fungicidal action. Bactericidal activity against GR+, Gr- bacterias, active against Bactericidal activity against GR+, Gr- bacterias, active against

Treponema, gonococci, trichomonas, Proteus.Treponema, gonococci, trichomonas, Proteus.

INDICATIONS:INDICATIONS: disinfection of the surgical area, the surgeon's hands, disinfection of the surgical area, the surgeon's hands, tools, burn surfaces, septic processes, prevention of sexually tools, burn surfaces, septic processes, prevention of sexually transmitted diseases. In the form of a transmitted diseases. In the form of a tabltabl. - in infectious and . - in infectious and inflammatory diseases of the mouth and throat. 0.2% solution inhibits inflammatory diseases of the mouth and throat. 0.2% solution inhibits the formation of plaque and effective in treating gingivitis.the formation of plaque and effective in treating gingivitis.

SIDE EFFECTS: SIDE EFFECTS: Dry hands, itchy skin, dermatitis.Dry hands, itchy skin, dermatitis. !!!Can not be used in conjunction with IODINE!!!!!!Can not be used in conjunction with IODINE!!! CHLORHEXIDINECHLORHEXIDINE is often used as an active ingredient in mouthwash is often used as an active ingredient in mouthwash

pastes to reduce dental plaque and oral bacteria. pastes to reduce dental plaque and oral bacteria. It have an immediate It have an immediate bactericidal actionbactericidal action and a prolonged and a prolonged bacteriostatic bacteriostatic

actionaction due to adsorption onto the pellicle-coated enamel surface. due to adsorption onto the pellicle-coated enamel surface.

Oxidizing agentsOxidizing agents HYDROGEN PEROXIDEHYDROGEN PEROXIDE

It is available as 30% and 3% solution. More It is available as 30% and 3% solution. More common 3% solutions is used.common 3% solutions is used.

HH22OO2 = 22 = 2HH + + OO22 It is decomposed with release of It is decomposed with release of molecular form molecular form

of oxygenof oxygen that is responsible for antimicrobial that is responsible for antimicrobial effecteffect

Releasing oxygen makes foam that cleans and Releasing oxygen makes foam that cleans and deodorizes putrid wounds and ulcers. deodorizes putrid wounds and ulcers.

Catalases present in tissues speeds Catalases present in tissues speeds decomposition and foaming of hydrogen peroxidedecomposition and foaming of hydrogen peroxide

Hydrogen peroxide is used in treatment of infected Hydrogen peroxide is used in treatment of infected wounds and to stop small bleeding.wounds and to stop small bleeding.

HydrogenHydrogen peroxide peroxideIndications:Indications:

- rinsing the mouth and throat, for the treatment - rinsing the mouth and throat, for the treatment of wounds that are infected with anaerobic of wounds that are infected with anaerobic microflora. Concentrated solutions (20-30%) is microflora. Concentrated solutions (20-30%) is indicated for the treatment of warts, lichen indicated for the treatment of warts, lichen planus.planus.

Side effects:Side effects:

- burn mucosa. Not used in deep wounds, and - burn mucosa. Not used in deep wounds, and not introduced into a body cavity - not introduced into a body cavity - may cause may cause embolism.embolism.

Potassium permanganatePotassium permanganate

22KMnOKMnO4 + 4 + HH22OO = 2 = 2KOHKOH + 2 + 2MnOMnO2 + 2 + 33OO22 It liberates It liberates oxygen in atomic form.oxygen in atomic form. Highly water soluble, used in 1:4000-Highly water soluble, used in 1:4000-

1:10000 solution.1:10000 solution. Higher concentrations cause burns and Higher concentrations cause burns and

blistering.blistering. It promotes rusting. It promotes rusting.

Clinical uses:Clinical uses: Gargling, douching, irrigating cavities, Gargling, douching, irrigating cavities,

urethra and wounds.urethra and wounds. Stomach wash in alkaloid poisoning.Stomach wash in alkaloid poisoning. In a 2-5% solution is used for burns, bites In a 2-5% solution is used for burns, bites

of mosquitoes and snakes, for quick of mosquitoes and snakes, for quick healing of wounds.healing of wounds.

Disinfection of water. Disinfection of water.

Heavy metal compounds.Heavy metal compounds. Their mechanism of action is the Their mechanism of action is the blocking of blocking of

sulfhydrylsulfhydryl, , carboxylcarboxyl and and amino groupsamino groups of proteins of proteins and enzymes of microorganisms.and enzymes of microorganisms.

Metal ions are formed by dissociation of the salts, Metal ions are formed by dissociation of the salts, interaction with these active biosubstrates functional interaction with these active biosubstrates functional groups cause their groups cause their denaturationdenaturation. .

At a deeper penetration of the substance in the At a deeper penetration of the substance in the tissue causes irritated cells and nerve endings tissue causes irritated cells and nerve endings effect, and the extreme manifestation of a effect, and the extreme manifestation of a cauterizingcauterizing effect of metal salts. effect of metal salts.

(Pb, ... Al, Zn, Cu, Ag, ... Hg)(Pb, ... Al, Zn, Cu, Ag, ... Hg) In such sequence an In such sequence an increases antimicrobial activity. As antiseptics most increases antimicrobial activity. As antiseptics most active are metal salts on the right side of the row.active are metal salts on the right side of the row.

Heavy metal compounds.Heavy metal compounds. With prolonged use of salts of heavy metals can be With prolonged use of salts of heavy metals can be

cytotoxic effectcytotoxic effect due to the inhibition of thiol enzymes in due to the inhibition of thiol enzymes in the tissues. the tissues.

Symptoms of poisoning with salts of heavy metals:Symptoms of poisoning with salts of heavy metals: a a chemical burn of GIT mucosa, the weakening of cardiac chemical burn of GIT mucosa, the weakening of cardiac activity, collapse, kidney and liver damage.activity, collapse, kidney and liver damage.

In cases of poisoning:In cases of poisoning: gastric lavage with water, tea gastric lavage with water, tea solution with activated carbon, Unithiol.solution with activated carbon, Unithiol.

Inside:Inside: milk, raw eggs, Unit milk, raw eggs, Unithhiol or iol or TTetaetaccin calcium, in calcium, SSodium thiosulfate. odium thiosulfate. Symptomatic treatment:Symptomatic treatment: cardiac cardiac glycosides, sympathomimetic, plasma expanders, glycosides, sympathomimetic, plasma expanders, vasoconstrictorvasoconstrictorss, narcotic analgesics., narcotic analgesics.

Acids and alkalisAcids and alkalis AcidAcidss: boric acid, salicylic: boric acid, salicylic - - Shift the pH to the acid side → Shift the pH to the acid side →

protein denaturation protein denaturation of of microbial cell protoplasm.microbial cell protoplasm. Since Since proteins of the skin and mucous membranes formproteins of the skin and mucous membranes forminging dense, dense, insoluble albuminates, insoluble albuminates, that is that is providing providing anti-microbial, anti-anti-microbial, anti-inflammatory, antifungal effects.inflammatory, antifungal effects.

In high concentrations In high concentrations cauterize tissuecauterize tissue ((coagulative coagulative necrosis )!necrosis )! Boric acidBoric acid:: u used sed for for washing and rinsing of the mucous washing and rinsing of the mucous

membranes of the mouth, diaper rash, acute and chronic otitis membranes of the mouth, diaper rash, acute and chronic otitis media, colitis, pyoderma, pediculosismedia, colitis, pyoderma, pediculosis..

Side effectSide effect:: It penetrates through the skin and mucous It penetrates through the skin and mucous membranes, especially in children,membranes, especially in children, cumulates. With long-term use cumulates. With long-term use in patients with impairedin patients with impaired renal function develops renal function develops acute and acute and chronic poisoningchronic poisoning (nausea,vomiting, diarrhea, skin rashes, (nausea,vomiting, diarrhea, skin rashes, confusionconfusion consciousness, convulsions, oliguria, sometimes shock.consciousness, convulsions, oliguria, sometimes shock.

Salicylic acidSalicylic acid:: Weak antiseptic, irritant, low concentrations (1-3%)Weak antiseptic, irritant, low concentrations (1-3%) ––keratoplastickeratoplastic,, in high (5% -10%) in high (5% -10%) - - keratolytic effect. keratolytic effect.

ApplicationApplication:: Oily seborrhea, acne, eOily seborrhea, acne, ecczema, psoriasis, ichthyosis, zema, psoriasis, ichthyosis, warts, corns, etc.warts, corns, etc.

AAlkalislkalis AlkalinesAlkalines:: NaHCO3, sodium tetraborate, NaHCO3, sodium tetraborate, sol. of sol. of

ammoniaammonia.. NaHCO3, sodium tetraborateNaHCO3, sodium tetraborate - melted mucin, a - melted mucin, a

softening effect. Inflammatory exudate pH shiftsoftening effect. Inflammatory exudate pH shiftss to to the alkaline side reduces the manifestations of the alkaline side reduces the manifestations of inflammation.inflammation.

10% ammonia solution10% ammonia solution e exhibits antiseptic effectxhibits antiseptic effect,, manifests cleaning properties, dissolves fat. Given manifests cleaning properties, dissolves fat. Given these properties, it is suggested for these properties, it is suggested for washing hands washing hands before surgerybefore surgery (25 ml solution of ammonia diluted (25 ml solution of ammonia diluted in 5 liters of waterin 5 liters of water).).

Inhalation to stimulate the respiratory center.Inhalation to stimulate the respiratory center.

Group of (aromatic) phenol, resorcinol, thymol, tar, ichthyol, benzylbenzoate.

Phenol (carbolic acid): 3-5% solution for disinfection of furniture, household items, hospital linen, patients discharge.0.25-1% - sometimes in skin diseases accompanied by itching.0.1-0.5% - conservation of serum and suppository.Readily absorbed through intact skin and mucous membranes, causing intoxication (short-term stimulation of the CNS, respiratory depression and cardiac activity, decrease in body temperature, damage of parenchymal organs).

Organic antiseptics

Organic compoundsOrganic compounds  Phenols  Phenols

ResorcinolResorcinol In small doses has In small doses has keratoplastickeratoplastic property in property in

the more annoying - the more annoying - keratolytickeratolytic.. Used for the treatment of skin diseases Used for the treatment of skin diseases

(eczema, seborrhea), fungal infections (2-5% (eczema, seborrhea), fungal infections (2-5% solutions, 5-20% ointment, paste).solutions, 5-20% ointment, paste).

Birch tarBirch tar Has: antimicrobial, keratoplastic, keratolytic Has: antimicrobial, keratoplastic, keratolytic

and irritant effect.and irritant effect. Is used to treat a number of skin diseases and Is used to treat a number of skin diseases and

scabies.scabies. Is one of the components of balsamic liniment Is one of the components of balsamic liniment

of Vishnevskiyof Vishnevskiy

Group of aldehydes and Group of aldehydes and alcoholsalcohols

PREPARATIONS: PREPARATIONS: FORMALDEHYDE SOLUTIONFORMALDEHYDE SOLUTION,, LIZOFORM, ETHYL ALCOHOL, LIZOFORM, ETHYL ALCOHOL, HEXAMETHYLENETETRAMINE (METHENAMINE)HEXAMETHYLENETETRAMINE (METHENAMINE)

Formaldehyde solution (Formaldehyde solution (FFormalin)ormalin) Has antimicrobial (vegetative forms and spores) Has antimicrobial (vegetative forms and spores)

and deodorizing effectsand deodorizing effects.. MECHANISM OF ACTIONMECHANISM OF ACTION: d: dehydration of microbial ehydration of microbial

cells protoplasm proteins causing its destruction.cells protoplasm proteins causing its destruction. Is used as a disinfectant and deodorant, skin Is used as a disinfectant and deodorant, skin

treatment with sweating (0.5-1%), disinfection treatment with sweating (0.5-1%), disinfection tools (0.5%). For the preservation of anatomical tools (0.5%). For the preservation of anatomical objects.objects.

Aldehydes and alcohols Aldehydes and alcohols (Formaldehyde)(Formaldehyde)

If inhaled formaldehyde - tearing, coughing, shortness of breath, agitation.

In oral poisoning - pain in the mouth, behind the sternum, in epigastric region, hematemesis, thirst, loss of consciousness, cyanosis, coma.

Emergency in poisoning: Inhalation of water vapor, oxygen saturation, gastric lavage 2.3% sol. of Ammonium chloride.

Inward enter: 2-3 tbsp. of activated carbon, 100 ml of 30% solution of magnesium sulfate.

In severe poisoning - forced diuresis, s/c 1 ml 0.1% solution of Atropine sulfate, Promedol, inward - Codeine in tabl.

Ethyl alcoholEthyl alcohol Bactericidal activity starts with alcohol 20% and increases Bactericidal activity starts with alcohol 20% and increases

with concentration. On the spore form does not affect.with concentration. On the spore form does not affect. High concentrations of alcohol in the protein environment High concentrations of alcohol in the protein environment

form dense protein aggregates.form dense protein aggregates. 70% - it is more deeply penetrates into the deeper layers of 70% - it is more deeply penetrates into the deeper layers of

the epidermis of the skin, sebaceous and sweat glands, the epidermis of the skin, sebaceous and sweat glands, provides a high antiseptic effect (antimicrobial strength of provides a high antiseptic effect (antimicrobial strength of 70% is equal to 3% phenol sol.).70% is equal to 3% phenol sol.).

Application: disinfection of hands and operating field Application: disinfection of hands and operating field (70%).(70%).

Sterilization of surgical instruments (90-96%).Sterilization of surgical instruments (90-96%). Disinfection of the skin before injection (70%).Disinfection of the skin before injection (70%). Alcohol compresses for children (20%), adults (40%).Alcohol compresses for children (20%), adults (40%). For the preparation of medicaments.For the preparation of medicaments.

Group of dyesGroup of dyesEthacridine lactate (rivanol), Ethacridine lactate (rivanol),

Brilliant green,Brilliant green,

Methylene blueMethylene blue

Antimicrobial activity of this group Antimicrobial activity of this group falls In the protein environmentfalls In the protein environment

The most sensitive The most sensitive Gr + bacteriaGr + bacteria, , coccicocci..

Ethacridine lactate (rivanol): - used in surgery, gynecology, urology, ophthalmology,

dermatology. For washing of fresh and infected wounds, cavities (pleura, peritoneum), bladder, uterus.

Brilliant green (1-2% water and alcohol sol.):

- for the treatment of skin with scratches, pyoderma, blepharitis, and others.

Methylene blue: - used internally for urinary tract infections (cystitis, urethritis). - I/V 1% sol. 50-100 ml in case of poisoning with hydrocyanic

acid or salts (in large doses translates hemoglobin to methemoglobin which comes into contact with a non-toxic form of cyanide complex cyanmethemoglobin).

- When administered I/V in small doses (0.1-0.15 ml/kg 1% sol.) contrary methylene blue restores methemoglobin in the hemoglobin (with nitrite poisoning, aniline, and others.)

Nitrofuran derivatives Nitrofuran derivatives (fura(furaccililllin, furazolidone)in, furazolidone)

Spectrum of action:Spectrum of action: Gr-, Gr + bacteria Gr-, Gr + bacteria (staphylococci, streptococci, dysentery bacillus, (staphylococci, streptococci, dysentery bacillus, intestinal coli, Salmonella paratyphi, the causative intestinal coli, Salmonella paratyphi, the causative agent of gas gangrene, etc.) and protozoa agent of gas gangrene, etc.) and protozoa (Trichomonas, Giardia).(Trichomonas, Giardia).

Pharmacodynamic:Pharmacodynamic: influenced microbes reductase, influenced microbes reductase, there is a restoration of the nitro group and their there is a restoration of the nitro group and their transformation into toxic products for cells (inhibition of transformation into toxic products for cells (inhibition of the respiratory chain, the destruction of the microbial the respiratory chain, the destruction of the microbial wall).wall).

In the presence of pus does not lose effectiveness.In the presence of pus does not lose effectiveness. ApplyApply for external treatment of wounds, skin, mucous for external treatment of wounds, skin, mucous

membranes, wash serous and joint cavities, otitis membranes, wash serous and joint cavities, otitis media, conjunctivitis and others. Eye diseases and media, conjunctivitis and others. Eye diseases and orally for the treatment of bacterial dysentery.orally for the treatment of bacterial dysentery.

DetergentsDetergents

Detergents Detergents - a substances with a high surface activity.- a substances with a high surface activity. Show antiseptic and cleansing action.Show antiseptic and cleansing action. Distinguish anionic and cationic Distinguish anionic and cationic detergentsdetergents.. Anionic detergentsAnionic detergents include ordinary soaps ( include ordinary soaps (sodium or sodium or

potassium saltspotassium salts of fatty acids). of fatty acids). As antiseptics mainly used cationic surfactants: As antiseptics mainly used cationic surfactants:

benzalkonium chloride, cetylpyridinium chloride, benzalkonium chloride, cetylpyridinium chloride, miramistimmiramistim..

Benzalkonium chlorideBenzalkonium chloride has antibacterial, antiprotozoal and has antibacterial, antiprotozoal and spermicidal action (spermicidal effect develops in two stages: spermicidal action (spermicidal effect develops in two stages: first - the destruction of the flagellum, and then - the gap of the first - the destruction of the flagellum, and then - the gap of the sperm head, which makes it impossible to fertilization).sperm head, which makes it impossible to fertilization).

Used for treatment of skin, mucous membranes, wounds, Used for treatment of skin, mucous membranes, wounds, rinsing the bladder, urethra, and for contraception in women.rinsing the bladder, urethra, and for contraception in women.

Miramistim:Miramistim: Antiseptic, antiviral, antibacterial agentAntiseptic, antiviral, antibacterial agent Gr-, Gr +, anaerobes, fungi.Gr-, Gr +, anaerobes, fungi. Reduces the resistance of bacteria and fungi to Reduces the resistance of bacteria and fungi to

antibiotics.antibiotics.

Application:Application: used as a 0.01% solution as an used as a 0.01% solution as an antiseptic in dental practice for the treatment of antiseptic in dental practice for the treatment of infected wounds, burns, infections of upper infected wounds, burns, infections of upper respiratory tract, urogenital system, stimulates respiratory tract, urogenital system, stimulates local non-specific immunity, accelerates local non-specific immunity, accelerates regeneration.regeneration.

Cetylpyridinium chlorideCetylpyridinium chloride

in the composition of the drug in the composition of the drug "Tserigel""Tserigel" is used is used for hand washing before surgery.for hand washing before surgery.

II. Synthetic II. Synthetic chemotherapeutic agentschemotherapeutic agents

SulfonamidesSulfonamides

Quinolones and Quinolones and FluroquinolonesFluroquinolones

Nitrofuran derivativesNitrofuran derivatives

Sulfonamides Sulfonamides Sulfa drugs (SA) - synthetic chemotherapeutic agents, Sulfa drugs (SA) - synthetic chemotherapeutic agents,

which are derivatives of sulfanilamide, or amides of which are derivatives of sulfanilamide, or amides of sulfonic acid.sulfonic acid.

The first preparation of SA: Red Streptocid (1935).

Common properties of SA:

- Sulfa nucleus;- Mechanism of action;- Spectrum of antibacterial action.

Classification of SAClassification of SA

1. Preparations with the resorptive (system) actions 1. Preparations with the resorptive (system) actions which are well absorbed in the intestine, creating high which are well absorbed in the intestine, creating high concentrations in the blood and other tissues:concentrations in the blood and other tissues:

short-actingshort-acting drugs (period of half of absorption less drugs (period of half of absorption less than 10 hours are applied 3-4 times per day, than 10 hours are applied 3-4 times per day, sometimes even 4-6 times a day in an amount of 4-6 sometimes even 4-6 times a day in an amount of 4-6 g/day):g/day):

- Sulfadimezin;- Sulfadimezin; - Etazol;- Etazol; - Norsulfazol;- Norsulfazol; - Urosulfan.- Urosulfan.

Classification of SAClassification of SA drugs with drugs with intermediate actionintermediate action (t1/2 = 10 -24 hours): (t1/2 = 10 -24 hours): - Sulfazin;- Sulfazin; - Sulfamethoxazole.- Sulfamethoxazole.

• • long-actinglong-acting (t 1/2 = 24-28 hours): (t 1/2 = 24-28 hours): - Sulfadimetoxin;- Sulfadimetoxin; - Sulfapiridazin;- Sulfapiridazin; - Sulfamonomethoxine.- Sulfamonomethoxine.

extremely long-actingextremely long-acting (t 1/2 of 48 hours): (t 1/2 of 48 hours): - Sulfalen.- Sulfalen.

2. Preparations of the 2. Preparations of the intestinal actionintestinal action, which are , which are slowly and incompletely absorbed from the GIT, they slowly and incompletely absorbed from the GIT, they are use for the treatment of intestinal infections (t 1/2 are use for the treatment of intestinal infections (t 1/2 <10 hours).<10 hours).

- Ftalazol;- Ftalazol; - Sulgin;- Sulgin; - Ftazin;- Ftazin;3. 3. SA for topical application SA for topical application (readily soluble in water (readily soluble in water

and is used topically in the eye drops for the and is used topically in the eye drops for the prevention and treatment of gonococcal eye disease prevention and treatment of gonococcal eye disease in newborns, as well as for the treatment of in newborns, as well as for the treatment of conjunctivitis, blepharitis, corneal ulcers and other conjunctivitis, blepharitis, corneal ulcers and other pathologies of the eye).pathologies of the eye).

-Sulfacil-sodium.-Sulfacil-sodium.

Classification of SAClassification of SA

Mechanism of actionMechanism of action Certain microbes require Certain microbes require paraaminobenzoic paraaminobenzoic

acidacid (PABA) to synthesize (PABA) to synthesize dihydrofolicdihydrofolic acid acid which is required to produce purines and which is required to produce purines and ultimately nucleic acids.ultimately nucleic acids.

Sulfonamides, chemical analogs of PABA, are Sulfonamides, chemical analogs of PABA, are competitive inhibitors of competitive inhibitors of dihydropteroate dihydropteroate synthetasesynthetase..

Sulfonamides therefore are reversible Sulfonamides therefore are reversible inhibitors of folic acid synthesis and inhibitors of folic acid synthesis and bacteriostaticbacteriostatic not bacteriocidal. not bacteriocidal.

Mechanism of actionMechanism of action

Conditions necessary for the Conditions necessary for the manifestation of the antibacterial action manifestation of the antibacterial action

of the SA:of the SA:

- microorganisms can use SA instead of PABA in the - microorganisms can use SA instead of PABA in the case when the case when the concentration of the drug in tissues concentration of the drug in tissues in 2000-5000 times higherin 2000-5000 times higher than the concentration of than the concentration of PABA;PABA;

- - SA efficiency sharply decreases in the presence SA efficiency sharply decreases in the presence of pus, blood and tissue breakdownof pus, blood and tissue breakdown products due products due to the PABA high concentration in these products;to the PABA high concentration in these products;

- SA have antimicrobial action only against those - SA have antimicrobial action only against those microorganisms which are themselves synthesized microorganisms which are themselves synthesized DHFA;DHFA;

- In SA resistant microorganisms observed increased - In SA resistant microorganisms observed increased synthesis of PABA;synthesis of PABA;

- The - The use of the SA in low concentrationsuse of the SA in low concentrations contributes to the formation of resistant strains of contributes to the formation of resistant strains of microorganisms and leads to microorganisms and leads to inefficiency of the SAinefficiency of the SA..

SA antimicrobial spectrumSA antimicrobial spectrum Currently used SA have Currently used SA have broad spectrumbroad spectrum, they , they

inhibit inhibit gram-positive and gram-negativegram-positive and gram-negative bacteria:bacteria:Streptococcus pneumoniaeStreptococcus pneumoniae, , beta-beta-haemolytic streptococci,haemolytic streptococci, E. coliE. coli, , klebciellaklebciella, , shigellashigella, , salmonellasalmonella, , enterobacter, gonococci, enterobacter, gonococci, meningococci, meningococci, and and pneumococcipneumococci;;

Nocardia, Nocardia, Chlamidia, Chlamidia, Protozoa (Protozoa (toxoplasmatoxoplasma and and malarial plasmodiamalarial plasmodia). ).

SA pharmacokineticsSA pharmacokinetics               Absorption.Absorption. Slightly in the stomach and Slightly in the stomach and

mainly in the small intestine. Within 30 minutes mainly in the small intestine. Within 30 minutes after the administration of the SA are found in after the administration of the SA are found in urine. The bioavailability is 70-90%.urine. The bioavailability is 70-90%.

          Biotransport.Biotransport. Reversibly bind to serum Reversibly bind to serum albumin, an agent which is directly proportional albumin, an agent which is directly proportional to the degree of hydrophobicity of the molecule to the degree of hydrophobicity of the molecule of the drug. SA can displace from its association of the drug. SA can displace from its association another protein drugs, particularly NSAIDs and another protein drugs, particularly NSAIDs and endogenous substances (bilirubin).endogenous substances (bilirubin).

          Distribution.Distribution. Pass through the blood-tissue, Pass through the blood-tissue, placenta and blood-brain barriers. Also passes placenta and blood-brain barriers. Also passes into breast milk.into breast milk.

          

 Biotransformation. Phase I reactions - acetylation, hydrogen substitution in

the group NH2-acetic acid residue, thereby forming acetylated derivatives which do not have antimicrobial activity in an acidic medium and form crystals that disrupts the function of the kidney (crystalluria).

Reaction Phase II – formation of double binding with glucuronic acid.

Excretion. Advantageously, urine, saliva, to a lesser extent and intestinal contents, but also breast milk.

Are displayed in the form of metabolites and unchanged.

SA pharmacokinetics

Clinical uses of SAClinical uses of SA Infections of urinary tractInfections of urinary tract GIT infections GIT infections Respiratory tract infectionRespiratory tract infection Pharingitis, gingivitisPharingitis, gingivitis Chlamidial infectionsChlamidial infections Wounds, burnsWounds, burns ToxoplasmosisToxoplasmosis MalariaMalaria For systemic treatment For systemic treatment cotrimoxazolecotrimoxazole is more often is more often

used nowadays used nowadays Sufonamides are used for prevention of infections. Sufonamides are used for prevention of infections.

Side effects of Side effects of sulfonamidessulfonamides

- - occur in 3 - 5% of patients and more frequently in children and the occur in 3 - 5% of patients and more frequently in children and the elderly. Complications due to overdose, and patients with elderly. Complications due to overdose, and patients with

hypersensitivity to the SA.hypersensitivity to the SA.1.1. The central nervous systemThe central nervous system: nausea, vomiting, dizziness, headache : nausea, vomiting, dizziness, headache

(central genesis), depression, increased fatigue.(central genesis), depression, increased fatigue.2.2. Blood:Blood: leukopenia, thrombocytopenia, agranulocytosis, leukopenia, thrombocytopenia, agranulocytosis,

methemoglobinemia, hemolytic anemia.methemoglobinemia, hemolytic anemia.3. Kidneys:3. Kidneys: oliguria, proteinuria, hematuria, oliguria, proteinuria, hematuria, crystalluria.crystalluria.4. Allergic reactions:4. Allergic reactions: fever, itching, rash, pain in the joints. fever, itching, rash, pain in the joints.                    

  Prevention of crystalluria:Prevention of crystalluria: - Drink plenty of liquids (3-5 liters per day);- Drink plenty of liquids (3-5 liters per day);

- drink alkaline mineral water or milk during SA using.- drink alkaline mineral water or milk during SA using.

Contraindications: Toxic and allergic reactions to drugs.Contraindications: Toxic and allergic reactions to drugs.

1 - Combination with 5-aminosalicylic 1 - Combination with 5-aminosalicylic acid:acid:

SALAZOSULFOPIRIDINSALAZOSULFOPIRIDIN

SALAZOPIRIDAZINSALAZOPIRIDAZIN

2 - combined with 2 - combined with TTrimethoprim:rimethoprim:

Biseptol (trimethoprim + sulfamethoxazole)Biseptol (trimethoprim + sulfamethoxazole)

Sulfaton (trimethoprim + sulfadimezin)Sulfaton (trimethoprim + sulfadimezin)

Combined sulfa drugsCombined sulfa drugs

Combined sulfa drugsCombined sulfa drugs (BISEPTOLUM)(BISEPTOLUM)..

  The mechanism of The mechanism of action of the combined action of the combined drug on the principle drug on the principle of combined of combined violations of nucleic violations of nucleic acid synthesis in acid synthesis in two points:two points:

1. at the level of DHFA 1. at the level of DHFA inclusion in PABA inclusion in PABA synthesis;synthesis;

2. at the level of THFA 2. at the level of THFA formation from DHFA.formation from DHFA.

Combined sulfa drugsCombined sulfa drugs (BISEPTOLUM)(BISEPTOLUM)..

    The second (additional) mechanism is achieved by The second (additional) mechanism is achieved by use of use of Trimethoprim (TMP) - antimalarial drug.Trimethoprim (TMP) - antimalarial drug.

    TMP has a similar antimicrobial activity with the SA TMP has a similar antimicrobial activity with the SA and is superior in activity in the 20-100 times. The and is superior in activity in the 20-100 times. The most justifiable is a combination of TMP with most justifiable is a combination of TMP with sulfamethoxazole in the ratio of 1: 5.sulfamethoxazole in the ratio of 1: 5.

    Thus, the combined preparation ‘Biseptol-480’ Thus, the combined preparation ‘Biseptol-480’ created, which is a combination of created, which is a combination of TMP with TMP with sulfamethoxazole 1: 5 (80 mg + 400 mg).sulfamethoxazole 1: 5 (80 mg + 400 mg).

This combination has a This combination has a bactericidal effectbactericidal effect, although , although each of the components each of the components exhibits - bacteriostaticexhibits - bacteriostatic..

Features of combined SA Features of combined SA drugsdrugs

- Effective even in the case of resistance to - Effective even in the case of resistance to SA;SA;

- Resistance to the combined drugs develops - Resistance to the combined drugs develops slowly;slowly;

Side effects:Side effects: 1. Dispepsia;1. Dispepsia; 2. Skin rash;2. Skin rash; 3. Sometimes superinfection;3. Sometimes superinfection; 4. The reduction in reproductive function 4. The reduction in reproductive function

(rare).(rare).

Antimicrobials Antimicrobials with with different chemical different chemical

structure.structure.FLUOROQUINOLONES:FLUOROQUINOLONES:

mono fluorine mono fluorine substitutesubstitute

1.1. ciprofloxacinciprofloxacin2.2. ofloxacinofloxacin3.3. pefloxacinpefloxacin4.4. norfloxacinnorfloxacin5.5. enoxacinenoxacin bifluorine substitutebifluorine substitute 1.1. lomeflolomefloxxaaccinin2.2. ofloxacinofloxacin3.3. sparfloxacinsparfloxacin

• trifluorine substitute1. traufloxacin2. gatifloxacin3. gemifloxacin4. moxifloxacin

FLUOROQUINOLONES:FLUOROQUINOLONES:

The spectrum of action:The spectrum of action: wide, including Pseudomonas aeruginosa, Chlamydia, Giardia, wide, including Pseudomonas aeruginosa, Chlamydia, Giardia,

Trichomonas, Yersinia, anaerobes, anthrax.Trichomonas, Yersinia, anaerobes, anthrax.

Mechanism of action:Mechanism of action: block the enzyme DNA-gyrase, responsible for supercoiling of block the enzyme DNA-gyrase, responsible for supercoiling of

the DNA molecule, as well as block the enzyme topoisomerase the DNA molecule, as well as block the enzyme topoisomerase type 4, is responsible for the compact folding of the DNA type 4, is responsible for the compact folding of the DNA molecule. This leads to an uncoiling of DNA and the molecule. This leads to an uncoiling of DNA and the microorganism death.microorganism death.

Type of antimicrobial action:Type of antimicrobial action: bactericidalbactericidal

Indications: trichomoniasis, giardiasis, plague, anthrax, gonorrhea, anaerobic infections, Legionnaires' disease.

Side effects: Excitation of the central nervous system, anxiety, in large

doses - convulsions (disrupt the synthesis of GABA in the CNS).

Dyspepsia, drug-induced hepatitis, swelling of the tongue Tachycardia, shortness of breath Anemia, leukopenia Photodermatitis, itching Disturbances of cartilage in children, so containdicated

for children under 12 years. Hypothyroidism Allergic reactions

FLUOROQUINOLONES:

NaphthNaphthalalidine Derivativesidine Derivatives

nalidixic acidnalidixic acid oxolinic acidoxolinic acid ppipenamipenamicic acid acid

Naphthalidine Derivatives

The spectrum of action: narrow (only Gr- microorganisms)Mechanism of action: blocks the enzyme DNA gyrase, as a consequence

despiralization DNA and death of microorganisms.Indication: when introduced into the body does not leave the

bloodstream, excrited with the urine in unchanged form, so used in infectious diseases of the kidneys and urinary tract infection (pyelonephritis, cystitis, urethritis, prostatitis).

Type antimicrobial action: Bactericidal(Side effects see FLUOROQUINOLONES)

NitrofuransNitrofurans(classification)(classification)

1.1. The drug is used topically for treatment of wounds and hands, with The drug is used topically for treatment of wounds and hands, with anaerobic infections:anaerobic infections:

FURACILLINFURACILLIN FURAZOLIDONEFURAZOLIDONE2. The drug is used in infectious diseases of the GIT:2. The drug is used in infectious diseases of the GIT: FURAZOLIDONEFURAZOLIDONE3. The drug is used in infectious diseases caused by protozoa:3. The drug is used in infectious diseases caused by protozoa: FURAZOLIDONEFURAZOLIDONE4. The drug is used in infectious diseases of the kidneys and urinary 4. The drug is used in infectious diseases of the kidneys and urinary

tract:tract: FURAGINFURAGIN FURADONINFURADONIN SOLOFURSOLOFUR

The spectrum of action:The spectrum of action: Gr +, protozoa Gr +, protozoa and anaerobic.and anaerobic.

Mechanism of action:Mechanism of action: are acceptors of H+ ions and enter into competition are acceptors of H+ ions and enter into competition

with the natural acceptors in the chain of tissue with the natural acceptors in the chain of tissue respiration, as a consequence of violating the respiration, as a consequence of violating the microbial cell respiration and death.microbial cell respiration and death.

Type of antimicrobial action:Type of antimicrobial action: bactericidalbactericidal

NitrofuransNitrofurans

Side effects:Side effects: Peripheral paresthesia and paresisPeripheral paresthesia and paresis Hypotension (donors are NO)Hypotension (donors are NO) Nausea, diarrhea, vomiting, epigastric Nausea, diarrhea, vomiting, epigastric

pain, anorexiapain, anorexia Anemia and leukopeniaAnemia and leukopenia AAllergic reactionsllergic reactions

IndicationsIndications: see classification.: see classification.

NitrofuransNitrofurans

Derivatives of Derivatives of 8-oxyquinoline8-oxyquinoline(classification)(classification)

1.1. The drug is used topically for treatment of wounds The drug is used topically for treatment of wounds and hands:and hands:

SAPROSANSAPROSAN HLORHINALDONHLORHINALDON2. 2. The drug is used in infectious diseases of the The drug is used in infectious diseases of the

gastrointestinal tract:gastrointestinal tract: ENTEROSEPTOLENTEROSEPTOL MEXAZAMEXAZA INTESTOPANINTESTOPAN3. The drug is used in infectious diseases caused by 3. The drug is used in infectious diseases caused by

protozoa:protozoa: ENTEROSEPTOLENTEROSEPTOL QUINIOFONQUINIOFON DIYODOHINDIYODOHIN4. The drug is used in infectious diseases of the 4. The drug is used in infectious diseases of the

kidneys and urinary tract:kidneys and urinary tract: NITROXOLIN (5-NOC)NITROXOLIN (5-NOC)

The spectrum of action:The spectrum of action: GrGr + +,, fungi, protozoa and anaerobic fungi, protozoa and anaerobic

Mechanism of action:Mechanism of action: Disrupt the synthesis of NDisrupt the synthesis of NAA in the microbial cell in the microbial cell;; Uncouple oxidative phosphorylation processesUncouple oxidative phosphorylation processes;; Communicating with iron enzymes Communicating with iron enzymes and and break breathing break breathing

activity of activity of microbial cellsmicrobial cells;; All this leads to the death of microorganismsAll this leads to the death of microorganisms..

Type Type of antimicrobial action:of antimicrobial action:

bactericidalbactericidal

IndIndication:ication: seesee. classification. classification

Derivatives of Derivatives of 8-oxyquinoline8-oxyquinoline

Side effectsSide effects::

Peripheral paresthesia and paresis, polyneuritis, Peripheral paresthesia and paresis, polyneuritis, headache, headache, optic nerve damage (irreversible optic nerve damage (irreversible blindness)blindness)..

Dyspepsia, anorexia, itching in the anal areaDyspepsia, anorexia, itching in the anal area..

HyperthyroidismHyperthyroidism, iodine, iodine phenomenon (iodine phenomenon (iodine poisoning: a runny nose, nasal congestion, cough, poisoning: a runny nose, nasal congestion, cough, conjunctivitis, acne-like skin rash, treatment - the NaCl conjunctivitis, acne-like skin rash, treatment - the NaCl solution)solution)..

Allergic reactionsAllergic reactions

Derivatives of Derivatives of 8-oxyquinoline8-oxyquinoline

Imidazole derivativesImidazole derivatives

MetronidazoleMetronidazole

TinidazoleTinidazole

The spectrum of action:The spectrum of action: anaerobes, Giardia, amoeba, balantidiums, some anaerobes, Giardia, amoeba, balantidiums, some

protozoa, Helicobacter piloryprotozoa, Helicobacter pilory

Mechanism of action:Mechanism of action: penetrate into the cells, where the enzymatic actionpenetrate into the cells, where the enzymatic action of of

metalloproteases separates metalloproteases separates nitronitro fromfrom them, which them, which causes the death of the microorganismcauses the death of the microorganism..

Nature of antimicrobial action:Nature of antimicrobial action: bactericidalbactericidal

IndIndication:ication: generalized anaerobic infection, amoebiasis, amoebic generalized anaerobic infection, amoebiasis, amoebic

dysentery, giardiasis, trichomoniasis, balantididysentery, giardiasis, trichomoniasis, balantidiaazzisis, peptic , peptic ulcer and ulcer and duodenal duodenal ulcerulcer..

ImidazoleImidazole derivatives derivatives

Side effects:

Peripheral paresthesia and paresis, headache, dizziness

Dyspepsia, drug-induced hepatitis, a metallic taste in the mouth

Photodermatitis Antabuse like syndrome (when co-administered with

alcohol patients have hypotension, tachycardia, weakness, dizziness, nausea, uncontrollable vomiting, fear of death, allergic reactions).

Imidazole derivatives

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