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1. Antimicrobial drugs

2. Control of Microbial Growth
• Sterilizing Agents-- kill everything (e.g.
heat, radiation)
• Disinfectants-- kill most things. Too
strong for living tissues (e.g. lysol, NH3)
• Antiseptics-- milder in action. Can be
used topically, but not ingested. (e.g.
alcohol, iodine)
• Chemotherapeutics-- can be ingested
(e.g. penicillin, sulfa drugs)

3. 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).

4. ORIGINS OF ANTISEPTICS
Joseph Lister (1827 - 1912)
• Realised that deaths from operations mostly occurred
from infection contracted during the operation as a result
of unclean practices.
• He started using Carbolic acid (phenol) during operations
to maintain aseptic conditions with significant
improvements.
• Like Semmelweiss he initially encountered opposition,
but use of his methods by the Germans during the Franco-
Prussian war in 1870 provided his major breakthrough
and over the next 10 years, the practise of aseptic surgery
became accepted.

5. Antimicrobials could be
• narrow-spectrum and effective only against a
limited variety of pathogens or broad-
spectrum, affecting many different types of
pathogens
• bactericidal if they kill the susceptible bacteria
or bacteriostatic if they inhibit the growth of
bacteria

6. 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.

7. Requirements for antiseptics
and disinfectants.
• Must have a broad spectrum of action;
• Rapid onset of action;
• Should have a small latency period;
• Should have a high activity;
• Must be chemically resistant;
• High availability and low cost;
• Lack of local irritant or allergic effects on tissues;
• Minimal absorption from the place of their application;
• Low toxicity.

8. Sources of antiseptics
• Early antiseptics were probably
vegetable extracts
– Many spices contain antibacterial
agents
• Essential oils extracted from plants
often have antibacterial properties
• Lister used carbolic acid which
chemically is a solution of phenol
– Phenol was originally extracted from
coal tar.
– Coal tar preparations are still used
today in therapeutic soaps 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.

9. Classification of Antiseptics and
Disinfectants
(according chemical structure)
I. Inorganic substances
1. Halogens:
• Iodine (2%, 3%, 5% alcochol solution)
• Chlorozodin
• Oxychlorosene
• Iodinolum
• Ioddicerinum
• Povidon-Iod (Betadinum)
• Iodophorm
• Lugol’s solution
• Chloramine B
• Chlorhexidine bigluconate
• Pantocidum (Halazone)

10. Hydrogen peroxide
Potassium permanganate
3. Acids and alkalis:
Boric acid
Salicylic acid
Solution of ammonia
4. Metallic salts:
Hydrargyri dichloridum : Hg2Cl2
Hydrargyri amidochloridum: HgNH2Cl
Silver nitrate: AgNO3
Copper sulfate CuSO4
Zinc sulfate ZnSO4
Zinc oxide ZnO

11. Classification continuation
II. Organic substances
1. Phenol derivatives:
• Phenol (Phenolum purum,
Carbolic acid)
• Cresol (Tricresolum)
• Resorcinol
• Thymol
2. Aldehydes:
• Formaldehyde (Formalinum)
• Glutaraldehide
• Hexamethylentetraminum
(Methenamine)
3. Alcochols:
• Spiritus aethylicus (Ethyl alcohol)
Benzylbenzoate
4. Dyes:
• Methylenum blue
• Brilliant green (Viride nitens)
• Etacridin lactate
5. Detergents:
• Aethonium
• Decamethoxin
• Roccal
• Dimexid
6. Tar, resins, products of
petroleum:
• Pix liquida Betulae (Birch tar)
• Ichthyolum
• Liniment by Vishnevsky
7. Nitrofuran derivatives:
• Nitrofurasone (Furacilinum)
8. Antiseptics from medicinal
plants:
• Chlorophyliptum
• Novoimaninum

12. Halogens
Chlorine
• Discovered in 1774 by a Swede, C.W. Scheele
• It is a pale green, toxic, reactive gas
• It is a powerful irritant and toxin
– Used as a gas warfare agent in WWI
– very nasty, inflicting lifelong damage on those who
survived
– The damaged lungs were possibly a factor in the
1918 flu pandemic
• Solution of chlorine in water is both a powerful
bleach and disinfectant
– Semmelweis had used chloride of lime as an
antiseptic

13. Halogens
The mechanism of antimicrobial action
• Denaturation of proteins of the
protoplasm of microbial cells by reacting
with the amino group of the proteins
(phenylalanine, tyrosyl), displacing
hydrogen and oxidaion of sulphydryl
groups.
• Denatured protein loses its activity.
• In the presence of organic substances
halogen’s antimicrobial effect
decreases.

14. Iodines
• Iodine - active bactericidal element.
• At a dilution of 1: 20 000 - kill vegetative forms of bacteria for 1
min,
• the dispute - 15 min.
• Alcoholic solution of Iodine 5% (5 g of Iodine, KI -2g, ethyl
alcohol 95% 100ml)
• An irritant and a distraction action
• INDICATIONS: Disinfection of the surgical field, disinfection of
wounds, the surgeon's hands, in myositis, neuralgia.
• Iodine is partially absorbed into the blood from the skin and
exhibits resorptive effects, especially in children.
• SIDE EFFECT: Chemical burns, dermatitis.

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

16. Halogens (Chlorine disinfectants)
CHLORINE - active bactericidal element is
active in the undissociated form of HOCl
when Cl dissolved in water at neutral and
acidic pH.
• Bleach - not less than 32% of free Cl.
Antimicrobial action - fast, but not for long
• INDICATIONS: 0.2-0.5% sol. for the
disinfection of premises, infective
patients discharge (pus, sputum, urine,
feces).
• Corrosive to metals.

17. CHLORAMINE B - 25-29%
active Cl
CHLORAMINE B - 25-29% active Cl.
INDICATION: eye wash, hand disinfection, douching (0.25-0.5%),
treatment of purulent wounds, burns, pustular skin diseases (0.5-
2%). Disinfection of premises, health products and non-metallic
tool, selection of patients (1.5%).
Deodorizing properties.
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 substances.
N-Chlorobenzenesulfonamide
sodium salt

18. Halogens
CHLORHEXIDINE BIGLUCONATE
(Bisdiguanidine derivative).
• Has the properties of chlorine and
detergent compounds.
• Capable of damaging the plasma
membrane of microorganisms.
• Strong antibacterial and fungicidal
action.
• Bactericidal activity against GR+, Gr-
bacterias, active against Treponema,
gonococci, trichomonas, Proteus.
INDICATIONS: disinfection of the surgical
area, the surgeon's hands, tools, burn
surfaces, septic processes, prevention
of sexually transmitted diseases. In the
form of a tabl. - in infectious and
inflammatory diseases of the mouth and
throat. 0.2% solution inhibits the
formation of plaque and effective in
treating gingivitis.
!!!Can not be used in
conjunction with IODINE!!!
CHLORHEXIDINE is often used
as an active ingredient in
mouthwash pastes to reduce
dental plaque and oral bacteria.
It have an immediate
bactericidal action and a
prolonged bacteriostatic action
due to adsorption onto the
pellicle-coated enamel surface.

19. Chloroazodin
N,N Dichlorodicarbonamidine
It explodes if heated above 155oC
Soluble in water and used for packing of dental caries,
lavage and irrigation
Glyceryltriacetate solution is used as wound dressing
Chlorazodin has long lasting antiseptic action

20. Oxychlorosene Sodium
Complex slowly releases Hypochlorous acid
It is Dodecylbenezenesulphonic acid Sodium salt and
Hypoclorus acid
It has germicidal activity with emulsifying properties of HOCl
such as wetting, emulsifying, keratolytic actions of anionic
detergent
0.1 to 0.5 % are used and dilutions of 0.1% to 0.2 % are
used in urology and opthalmology

21. Iodinolum
Iodinolum.
Structure: iodine — 1 g, iodide potassium — 3 g, polyvinyl alcohol
— 9 g, the water distilled — to 100 g.
Form of release of medicine. Bottles from dark glass with liquid
on 100 ml.
Use and doses of drug. Outwardly 1% solution (for rinsings,
spraying, washings, bandagings, ear drops). Course of treatment
of 2 — 4 weeks.
Effect of the medicine. Under the influence of intercellular lymphs
Iodinolum is split with release of iodine which has antimicrobic and
antiinflammatory effect (see iodine Solution spirit).
Release of iodine happens slowly, thanks to it the irritating
influence decreases and the prodollsitelnost of antimicrobic effect
of iodine increases.
Indications to use. Adenoid disease, purulent otitis, atrophic
rhinitis, chronic periodontitis, trophic and varicose ulcers, purulent
wounds, burns.
Contraindications. Individual hypersensitivity to iodine drugs.
By-effects, treatment of complications and poisoning

22. Ioddicerinum
IODDICERINE (Iodine, dimethyl sulfoxide, glycerol)
Fungicidal, antimicrobial, antiviral, antinecrotic, antioxidant
effect.
!!!The most active Iodine preparation!!!
Doesn’t irritate tissue, does not cause pain reaction, deeply
penetrates into the tissue.
INDICATION: Inflammatory infection (purulent wounds,
infectious ulcers, sore throats, tonsillitis, pulpitis, otitis,
pyoderma, erosion of the mucous membranes, mastitis,
candidiasis, inflammatory diseases of the genital organs).
Topically in the form of tampons, turundul, napkins,
irrigation, washing.

23. Povidon-Iodine (Betadinum)
Povidone-iodine is a broad spectrum antiseptic for topical application in the treatment
and prevention of wound infection. It may be used in first aid for minor cuts, grazes,
burns, abrasions and blisters. Povidone-iodine exhibits longer lasting antiseptic effects
than tincture of iodine, due to its slow absorption via soft tissue, making it the choice for
longer surgeries.
Bacteria do not develop resistance to PVP-I.
Consequently, PVP-I has found broad application in medicine as a surgical scrub; for
pre- and post-operative skin cleansing; for the treatment and prevention of infections in
wounds, ulcers, cuts and burns; for the treatment of infections in associated
with candidal, trichomonal or mixed infections. For these purposes PVP-I has been
formulated at concentrations of 7.5–10.0% in solution, spray, surgical scrub, ointment,
and swab dosage forms.
Because of these critical indications, only sterile povidone-iodine should be used in most
cases.

24. Pantocidum (Halazone)
P-Dichlorosulfamoylbenzoic acid
It is used to disinfect water

25. 2. Phenol

26. 2. Phenols
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).

27. 2. Phenols
• Potency of the disinfectant is determined by Phenolic coefficient.
• Phenolic coefficient is defined as the ratio of dilution of a given test
disinfectant to the dilution of phenol that is required to kill (to same
extent) a strain of Salmonella typhi under carefully controlled time and
temperature.
• Phenolic coefficient of Phenol is always 1. The dilution of a given
disinfectant if 10 times greater than phenol then phenolic coefficent is
10.
• M.O.A: Phenolic compounds used as antiseptics
or disinfectants include pure phenol and substitution products with
halogens and alkyl groups. They act to denature and coagulate proteins
and are general protoplasmic poisons. Phenol (carbolic acid) is one of
the oldest antiseptic agents.

28. Resorcinol
 In small doses has keratoplastic property in the more
annoying - keratolytic.
 Used for the treatment of skin diseases (eczema, seborrhea),
fungal infections (2-5% solutions, 5-20% ointment, paste).
Birch tar
 Has: antimicrobial, keratoplastic, keratolytic and irritant effect.
 Is used to treat a number of skin diseases and scabies.
 Is one of the components of balsamic liniment of Vishnevskiy

29. p-chlorophenol
 p-chlorophenol is used in combination of liquid petrolatum as
an antiseptic and antiirritant.
 Phenolic coefficient is about 4

30. p-chlorophenol
 p-chlorophenol is used in combination of liquid petrolatum as
an antiseptic and antiirritant.
 Phenolic coefficient is about 4

31. p-chloro-m-xylenol
Chloroxylenol, also known as para-chloro-meta-xylenol (PCMX), is
an antiseptic and disinfectant which is used for skin disinfection and cleaning surgical
instruments. It is also used within a number of household disinfectants
and wound cleaner. It is less effective than some other available agents. It is available
as a liquid.
Side effects are generally few but can include skin irritation. It may be used mixed with
water or alcohol. Chloroxylenol is most effective against Gram-positive bacteria. It
works by disruption of the cell wall and stopping the function of enzymes.
Chloroxylenol was first made in 1927. It is on the World Health Organization's List of
Essential Medicines, the most effective and safe medicines needed in a health
system. It is sold in a number of formulations and under a number of brand names
including Dettol.

32. Hexachlorophene
2,2’-methylenebis(3,4,6-trichlorophenol)
Two commercial preparations using hexachlorophene, pHisoDerm and pHisoHex,
were widely used as antibacterial skin cleansers in the treatment of acne,
with pHisoDermdeveloped for those allergic to the active ingredients in pHisoHex.
In the US during the 1960s, both were available over the counter. After the ban
was enacted, pHisoDermwas reformulated without hexachlorophene, and
continued to be sold over-the-counter, while pHisoHex, which contained 3%
hexachlorophene (three times the legal limit imposed in 1972), became available
(and remains available today) as a prescription body wash. In the European
Community countries during the 1970s and 1980s, pHisoHex was available over
the counter. A related product, pHisoAc, was used as a skin mask to dry and peel
away acne lesions. Another preparation, pHiso-Scrub, was a hexachlorophene-
impregnated sponge for scrubbing, has since been discontinued. Several
substitute products (including triclosan) were developed, but none had the germ-
killing capability of hexachlorophene.

33. Cresol
O-cresol
m-cresol p-cresol
•Cresol is mixture of three isomers of methylphenols
•Cresol is obtained from coal tar or petroleum
•The mixture is an antiseptic disinfectant.
•Phenolic coefficient is of 2.5
•Very unpleasant ordor

34. Thymol
Isopropyl-m-cresol
It is extracted from oil of Thymus vulgaris
It is mild fungicidal, used in alcoholic solutions and in dusting powders for tratment
of tinea (ringworm ) infections

35. Eugenol
4-Allyl-2-methoxyphenol
Eugenol is pleasant in taste
Eugenol is possesses both local anesthetic and antiseptic
activity
Its phenolic coefficient is 14.4
Eugenol is used in mouthwashes.

36. Oxidizing agents
• HYDROGEN PEROXIDE
• It is available as 30% and 3% solution. More
common 3% solutions is used.
• H2O2 = 2H + O2
It is decomposed with release of molecular form
of oxygen that is responsible for antimicrobial
effect
• Releasing oxygen makes foam that cleans and
deodorizes putrid wounds and ulcers.
• Catalases present in tissues speeds
decomposition and foaming of hydrogen peroxide
• Hydrogen peroxide is used in treatment of infected
wounds and to stop small bleeding.

37. Hydrogen
peroxide
Indications:
- rinsing the mouth and throat, for the treatment
of wounds that are infected with anaerobic
microflora. Concentrated solutions (20-30%) is
indicated for the treatment of warts, lichen
planus.
Side effects:
- burn mucosa. Not used in deep wounds, and
not introduced into a body cavity - may cause
embolism.

38. Potassium permanganate
• 2KMnO4 + H2O = 2KOH + 2MnO2 + 3O2
It liberates oxygen in atomic form.
• Highly water soluble, used in 1:4000-
1:10000 solution.
• Higher concentrations cause burns and
blistering.
• It promotes rusting.
Clinical uses:
• Gargling, douching, irrigating cavities,
urethra and wounds.
• Stomach wash in alkaloid poisoning.
• In a 2-5% solution is used for burns, bites
of mosquitoes and snakes, for quick
healing of wounds.
• Disinfection of water.

39. Heavy metal compounds.
• Their mechanism of action is the blocking of
sulfhydryl, carboxyl and amino groups of proteins
and enzymes of microorganisms.
• Metal ions are formed by dissociation of the salts,
interaction with these active biosubstrates functional
groups cause their denaturation.
• At a deeper penetration of the substance in the
tissue causes irritated cells and nerve endings
effect, and the extreme manifestation of a
cauterizing effect of metal salts.
• (Pb, ... Al, Zn, Cu, Ag, ... Hg) In such sequence an
increases antimicrobial activity. As antiseptics most
active are metal salts on the right side of the row.

40. Heavy metal compounds.
• With prolonged use of salts of heavy metals can be
cytotoxic effect due to the inhibition of thiol enzymes in
the tissues.
• Symptoms of poisoning with salts of heavy metals: a
chemical burn of GIT mucosa, the weakening of cardiac
activity, collapse, kidney and liver damage.
• In cases of poisoning: gastric lavage with water, tea
solution with activated carbon, Unithiol.
Inside: milk, raw eggs, Unithiol or Tetacin calcium,
Sodium thiosulfate. Symptomatic treatment: cardiac
glycosides, sympathomimetic, plasma expanders,
vasoconstrictors, narcotic analgesics.

41. Acids and alkalis
• Acids: boric acid, salicylic - Shift the pH to the acid side →
protein denaturation of microbial cell protoplasm. Since
proteins of the skin and mucous membranes forming dense,
insoluble albuminates, that is providing anti-microbial, anti-
inflammatory, antifungal effects.
• In high concentrations cauterize tissue (coagulative necrosis )!
• Boric acid: used for washing and rinsing of the mucous
membranes of the mouth, diaper rash, acute and chronic otitis
media, colitis, pyoderma, pediculosis.
• Side effect: It penetrates through the skin and mucous
membranes, especially in children, cumulates. With long-term use
in patients with impaired renal function develops acute and
chronic poisoning (nausea,vomiting, diarrhea, skin rashes,
confusion consciousness, convulsions, oliguria, sometimes shock.
• Salicylic acid: Weak antiseptic, irritant, low concentrations (1-3%)
–keratoplastic, in high (5% -10%) - keratolytic effect.
• Application: Oily seborrhea, acne, eczema, psoriasis, ichthyosis,
warts, corns, etc.

42. Alkalis
• Alkalines: NaHCO3, sodium tetraborate, sol. of
ammonia.
• NaHCO3, sodium tetraborate - melted mucin, a
softening effect. Inflammatory exudate pH shifts to
the alkaline side reduces the manifestations of
inflammation.
• 10% ammonia solution exhibits antiseptic effect,
manifests cleaning properties, dissolves fat. Given
these properties, it is suggested for washing hands
before surgery (25 ml solution of ammonia diluted
in 5 liters of water).
• Inhalation to stimulate the respiratory center.

43. Group of aldehydes and
alcohols
• PREPARATIONS: FORMALDEHYDE SOLUTION,
LIZOFORM, ETHYL ALCOHOL,
HEXAMETHYLENETETRAMINE (METHENAMINE)
Formaldehyde solution (Formalin)
• Has antimicrobial (vegetative forms and spores) and
deodorizing effects.
• MECHANISM OF ACTION: dehydration of microbial
cells protoplasm proteins causing its destruction.
• Is used as a disinfectant and deodorant, skin
treatment with sweating (0.5-1%), disinfection tools
(0.5%). For the preservation of anatomical objects.

44. Aldehydes and alcohols
(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.

45. Ethyl alcohol
• Bactericidal activity starts with alcohol 20% and increases
with concentration. On the spore form does not affect.
• High concentrations of alcohol in the protein environment
form dense protein aggregates.
• 70% - it is more deeply penetrates into the deeper layers of
the epidermis of the skin, sebaceous and sweat glands,
provides a high antiseptic effect (antimicrobial strength of
70% is equal to 3% phenol sol.).
• Application: disinfection of hands and operating field
(70%).
• Sterilization of surgical instruments (90-96%).
• Disinfection of the skin before injection (70%).
• Alcohol compresses for children (20%), adults (40%).
• For the preparation of medicaments.

46. Group of dyes
Ethacridine lactate (rivanol),
Brilliant green,
Methylene blue
• Antimicrobial activity of this group
falls In the protein environment
• The most sensitive Gr + bacteria,
cocci.

47. 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.)

48. Nitrofuran derivatives (furacillin,
furazolidone)
• Spectrum of action: Gr-, Gr + bacteria (staphylococci,
streptococci, dysentery bacillus, intestinal coli, Salmonella
paratyphi, the causative agent of gas gangrene, etc.) and
protozoa (Trichomonas, Giardia).
• Pharmacodynamic: influenced microbes reductase, there is a
restoration of the nitro group and their transformation into toxic
products for cells (inhibition of the respiratory chain, the
destruction of the microbial wall).
• In the presence of pus does not lose effectiveness.
• Apply for external treatment of wounds, skin, mucous
membranes, wash serous and joint cavities, otitis media,
conjunctivitis and others. Eye diseases and orally for the
treatment of bacterial dysentery.

49. Detergents
• Detergents - a substances with a high surface activity.
• Show antiseptic and cleansing action.
• Distinguish anionic and cationic detergents.
• Anionic detergents include ordinary soaps (sodium or
potassium salts of fatty acids).
• As antiseptics mainly used cationic surfactants:
benzalkonium chloride, cetylpyridinium chloride,
miramistim.
• Benzalkonium chloride has antibacterial, antiprotozoal and
spermicidal action (spermicidal effect develops in two stages:
first - the destruction of the flagellum, and then - the gap of the
sperm head, which makes it impossible to fertilization).
• Used for treatment of skin, mucous membranes, wounds,
rinsing the bladder, urethra, and for contraception in women.

50. Miramistim:
• Antiseptic, antiviral, antibacterial agent
• Gr-, Gr +, anaerobes, fungi.
• Reduces the resistance of bacteria and fungi to
antibiotics.
Application: used as a 0.01% solution as an antiseptic
in dental practice for the treatment of infected wounds,
burns, infections of upper respiratory tract, urogenital
system, stimulates local non-specific immunity,
accelerates regeneration.
Cetylpyridinium chloride
in the composition of the drug "Tserigel" is used for
hand washing before surgery.

51. II. Synthetic chemotherapeutic
agents
• Sulfonamides
• Quinolones and Fluroquinolones
• Nitrofuran derivatives

52. Sulfonamides
• Sulfa drugs (SA) - synthetic chemotherapeutic agents,
which are derivatives of sulfanilamide, or amides of
sulfonic acid.
The first preparation of SA: Red Streptocid (1935).
Common
properties of SA:
- Sulfa nucleus;
- Mechanism of
action;
- Spectrum of
antibacterial action.

53. Classification of SA
1. Preparations with the resorptive (system) actions
which are well absorbed in the intestine, creating high
concentrations in the blood and other tissues:
• short-acting drugs (period of half of absorption less
than 10 hours are applied 3-4 times per day,
sometimes even 4-6 times a day in an amount of 4-6
g/day):
• - Sulfadimezin;
• - Etazol;
• - Norsulfazol;
• - Urosulfan.

54. Classification of SA
• drugs with intermediate action (t1/2 = 10 -24 hours):
• - Sulfazin;
• - Sulfamethoxazole.
• long-acting (t 1/2 = 24-28 hours):
• - Sulfadimetoxin;
• - Sulfapiridazin;
• - Sulfamonomethoxine.
• extremely long-acting (t 1/2 of 48 hours):
• - Sulfalen.

55. Classification of SA
2. Preparations of the intestinal action, which are
slowly and incompletely absorbed from the GIT, they
are use for the treatment of intestinal infections (t 1/2
<10 hours).
• - Ftalazol;
• - Sulgin;
• - Ftazin;
3. SA for topical application (readily soluble in water
and is used topically in the eye drops for the
prevention and treatment of gonococcal eye disease
in newborns, as well as for the treatment of
conjunctivitis, blepharitis, corneal ulcers and other
pathologies of the eye).
• -Sulfacil-sodium.

56. Mechanism of action
• Certain microbes require paraaminobenzoic
acid (PABA) to synthesize dihydrofolic acid
which is required to produce purines and
ultimately nucleic acids.
• Sulfonamides, chemical analogs of PABA, are
competitive inhibitors of dihydropteroate
synthetase.
• Sulfonamides therefore are reversible inhibitors
of folic acid synthesis and bacteriostatic not
bacteriocidal.

57. Mechanism of action

58. Conditions necessary for the manifestation of the
antibacterial action of the SA:
• - microorganisms can use SA instead of PABA in the case
when the concentration of the drug in tissues in 2000-5000
times higher than the concentration of PABA;
• - SA efficiency sharply decreases in the presence of pus,
blood and tissue breakdown products due to the PABA high
concentration in these products;
• - SA have antimicrobial action only against those
microorganisms which are themselves synthesized DHFA;
• - In SA resistant microorganisms observed increased synthesis
of PABA;
• - The use of the SA in low concentrations contributes to the
formation of resistant strains of microorganisms and leads to
inefficiency of the SA.

59. SA antimicrobial spectrum
• Currently used SA have broad spectrum, they
inhibit gram-positive and gram-negative
bacteria:Streptococcus pneumoniae, beta-
haemolytic streptococci, E. coli, klebciella,
shigella, salmonella, enterobacter, gonococci,
meningococci, and pneumococci;
• Nocardia,
• Chlamidia,
• Protozoa (toxoplasma and malarial plasmodia).

60. SA pharmacokinetics
• Absorption. Slightly in the stomach and mainly in
the small intestine. Within 30 minutes after the
administration of the SA are found in urine. The
bioavailability is 70-90%.
• Biotransport. Reversibly bind to serum albumin,
an agent which is directly proportional to the degree of
hydrophobicity of the molecule of the drug. SA can
displace from its association another protein drugs,
particularly NSAIDs and endogenous substances
(bilirubin).
• Distribution. Pass through the blood-tissue,
placenta and blood-brain barriers. Also passes into
breast milk.

61. SA pharmacokinetics
• 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.

62. Clinical uses of SA
• Infections of urinary tract
• GIT infections
• Respiratory tract infection
• Pharingitis, gingivitis
• Chlamidial infections
• Wounds, burns
• Toxoplasmosis
• Malaria
• For systemic treatment cotrimoxazole is more often
used nowadays
• Sufonamides are used for prevention of infections.

63. Side effects of sulfonamides
- occur in 3 - 5% of patients and more frequently in children and the
elderly. Complications due to overdose, and patients with
hypersensitivity to the SA.
1. The central nervous system: nausea, vomiting, dizziness, headache
(central genesis), depression, increased fatigue.
2. Blood: leukopenia, thrombocytopenia, agranulocytosis,
methemoglobinemia, hemolytic anemia.
3. Kidneys: oliguria, proteinuria, hematuria, crystalluria.
4. Allergic reactions: fever, itching, rash, pain in the joints.
Prevention of crystalluria:
• - Drink plenty of liquids (3-5 liters per day);
• - drink alkaline mineral water or milk during SA using.
Contraindications: Toxic and allergic reactions to drugs.

64. Combined sulfa drugs
1 - Combination with 5-aminosalicylic acid:
• SALAZOSULFOPIRIDIN
• SALAZOPIRIDAZIN
2 - combined with Trimethoprim:
• Biseptol (trimethoprim + sulfamethoxazole)
• Sulfaton (trimethoprim + sulfadimezin)

65. Combined sulfa drugs
(BISEPTOLUM).
• The mechanism of
action of the combined
drug on the principle of
combined violations of
nucleic acid synthesis
in two points:
1. at the level of DHFA
inclusion in PABA
synthesis;
2. at the level of THFA
formation from DHFA.

66. Combined sulfa drugs
(BISEPTOLUM).
• The second (additional) mechanism is achieved by
use of Trimethoprim (TMP) - antimalarial drug.
• TMP has a similar antimicrobial activity with the SA
and is superior in activity in the 20-100 times. The
most justifiable is a combination of TMP with
sulfamethoxazole in the ratio of 1: 5.
• Thus, the combined preparation ‘Biseptol-480’
created, which is a combination of TMP with
sulfamethoxazole 1: 5 (80 mg + 400 mg).
• This combination has a bactericidal effect, although
each of the components exhibits - bacteriostatic.

67. Features of combined SA drugs
• - Effective even in the case of resistance to SA;
• - Resistance to the combined drugs develops
slowly;
Side effects:
• 1. Dispepsia;
• 2. Skin rash;
• 3. Sometimes superinfection;
• 4. The reduction in reproductive function (rare).

68. Antimicrobials with different
chemical structure.
FLUOROQUINOLONES:
• mono fluorine substitute
1. ciprofloxacin
2. ofloxacin
3. pefloxacin
4. norfloxacin
5. enoxacin
• bifluorine substitute
1. lomefloxacin
2. ofloxacin
3. sparfloxacin
• trifluorine substitute
1. traufloxacin
2. gatifloxacin
3. gemifloxacin
4. moxifloxacin

69. FLUOROQUINOLONES:
The spectrum of action:
• wide, including Pseudomonas aeruginosa, Chlamydia, Giardia,
Trichomonas, Yersinia, anaerobes, anthrax.
Mechanism of action:
• block the enzyme DNA-gyrase, responsible for supercoiling of
the DNA molecule, as well as block the enzyme topoisomerase
type 4, is responsible for the compact folding of the DNA
molecule. This leads to an uncoiling of DNA and the
microorganism death.
Type of antimicrobial action:
• bactericidal

70. FLUOROQUINOLONES:
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

71. Naphthalidine Derivatives
• nalidixic acid
• oxolinic acid
• pipenamic acid

72. 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)

73. Nitrofurans
(classification)
1. The drug is used topically for treatment of wounds and hands, with
anaerobic infections:
• FURACILLIN
• FURAZOLIDONE
2. The drug is used in infectious diseases of the GIT:
• FURAZOLIDONE
3. The drug is used in infectious diseases caused by protozoa:
• FURAZOLIDONE
4. The drug is used in infectious diseases of the kidneys and urinary
tract:
• FURAGIN
• FURADONIN
• SOLOFUR

74. Nitrofurans
The spectrum of action:
• Gr +, protozoa
• and anaerobic.
Mechanism of action:
• are acceptors of H+ ions and enter into competition
with the natural acceptors in the chain of tissue
respiration, as a consequence of violating the
microbial cell respiration and death.
Type of antimicrobial action:
• bactericidal

75. Nitrofurans
Side effects:
• Peripheral paresthesia and paresis
• Hypotension (donors are NO)
• Nausea, diarrhea, vomiting, epigastric
pain, anorexia
• Anemia and leukopenia
• Allergic reactions
Indications: see classification.

76. Derivatives of 8-oxyquinoline
(classification)
1. The drug is used topically for treatment of wounds and
hands:
• SAPROSAN
• HLORHINALDON
2. The drug is used in infectious diseases of the
gastrointestinal tract:
• ENTEROSEPTOL
• MEXAZA
• INTESTOPAN
3. The drug is used in infectious diseases caused by
protozoa:
• ENTEROSEPTOL
• QUINIOFON
• DIYODOHIN
4. The drug is used in infectious diseases of the kidneys and
urinary tract:
• NITROXOLIN (5-NOC)

77. Derivatives of 8-oxyquinoline
The spectrum of action:
• Gr +, fungi, protozoa and anaerobic
Mechanism of action:
• Disrupt the synthesis of NA in the microbial cell;
• Uncouple oxidative phosphorylation processes;
• Communicating with iron enzymes and break breathing
activity of microbial cells;
• All this leads to the death of microorganisms.
Type of antimicrobial action:
• bactericidal
Indication:
• see. classification

78. Derivatives of 8-oxyquinoline
Side effects:
• Peripheral paresthesia and paresis, polyneuritis,
headache, optic nerve damage (irreversible
blindness).
• Dyspepsia, anorexia, itching in the anal area.
• Hyperthyroidism, iodine phenomenon (iodine
poisoning: a runny nose, nasal congestion, cough,
conjunctivitis, acne-like skin rash, treatment - the NaCl
solution).
• Allergic reactions

79. Imidazole derivatives
• Metronidazole
• Tinidazole

80. Imidazole derivatives
The spectrum of action:
• anaerobes, Giardia, amoeba, balantidiums, some
protozoa, Helicobacter pilory
Mechanism of action:
• penetrate into the cells, where the enzymatic action of
metalloproteases separates nitro from them, which
causes the death of the microorganism.
Nature of antimicrobial action:
• bactericidal
Indication:
• generalized anaerobic infection, amoebiasis, amoebic
dysentery, giardiasis, trichomoniasis, balantidiazis,
peptic ulcer and duodenal ulcer.

81. Imidazole 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).

82. Thank you)))