Transcript Antiseptics and disinfectants

Antimicrobial drugs
Kharkiv National Medical University
Department of Pharmacology and Medical Prescription
assistant Gordiychuk D.
I. Antiseptics and disinfectants.
II. Sulfonamides.
Plan of lecture
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I. Antiseptics and disinfectants.
II. Sulfonamides.
III. Combined sulfa drugs.
IV. Antimicrobials with different chemical
structure.
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).
ANTICEPTICS are disinfecting agents with
sufficiently low toxicity for host cells that they
can be used directly on skin, mucous
membranes or wounds.
ANTISEPSIS - it is the use of chemicals to
destroy most pathogenic organisms on
animate surfaces.
Antiseptic drugs are used in:
• The treatment of skin infections
• Prevention of infections in cuts and wounds
• Cleaning the skin area of surgery from
microorganisms
• Profilaxy and treatment of infections in
mucosal areas such as mouth, nose and
vagina that are open to environment
• As a scrub for surgeans and the medical
personnel
Disinfection
DISINFECTANTS are chemical agents that inhibit
or kill microorganisms (surgical apparatus,
periphery of the patient, and the objects used by
the patient).
Disinfection It is the application of chemicals to
destroy most pathogenic organisms on inanimate
surfaces. Can be accomplished by application of
chemical agents, use of physical agents (ionizing
radiation) dry or moist heat, superheated steam
(autoclave, 120̊ C).
NB! 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 antiseptics
and disinfectants.
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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.
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.
Antimicrobials could be
• narrow-spectrum - effective only against a
limited variety of pathogens or broadspectrum, affecting many different types of
pathogens.
• bactericidal if they kill the susceptible bacteria
or bacteriostatic if they inhibit the growth of
bacteria
THE PATHOGENS THAT CAN BE
TRANSMITTED
Human Immunodeficiency Virus (HIV)
Herpes Simplex Virus types 1 and 2
Hepatitis B Virus (HBV)
Streptococci
Staphylococci
Mycobacterium tuberculosis
Cytomegalovirus
Some upper respiratory tract viruses
Disinfectants and antiseptics may be contaminated by resistant spores,
Pseudomonas aeruginosa Serretia marcesnes and may transmit infection.
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.
Classification of Antiseptics and
Disinfectants (according chemical structure)
I. Inorganic substances
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1. Halogens:
Iodine (2%, 3%, 5% alcochol
solution)
Iodinolum
Ioddicerinum
Povidon-Iod (Betadinum)
Iodophorm
Lugol’s solution
Chloramine B
Chlorhexidine bigluconate
Pantocidum (Halazone)
2. Oxidizing agents:
• Hydrogen peroxide
• Potassium permanganate
3. Acids and alkalis:
• Boric acid
• Salicylic acid
• Solution of ammonia
4. Metallic salts:
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Hydrargyri dichloridum
Hydrargyri amidochloridum
Silver nitrate
Copper sulfate
Zinc sulfate
Zinc oxide
Classification cont.
II. Organic substances
1. Aldehydes:
• Formaldehyde (Formalinum)
• Glutaraldehide
• Hexamethylentetraminum
(Methenamine)
2. Alcochols:
• Spiritus aethylicus (Ethyl alcohol)
3. Phenol derivatives:
• Phenol (Phenolum purum,
Carbolic acid)
• Cresol (Tricresolum)
• Resorcinol
• Thymol
• Benzylbenzoat
4. Dyes:
• Methylenum blue
• Brilliant green (Viride nitens)
• Etacridin lactate
5. Detergents:
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Aethonium
Decamethoxin
Roccal
Dimexid
6. Tar, resins, products of
petroleum:
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Pix liquida Betulae (Birch tar)
Ichthyolum
Liniment by Vishnevsky
7. Nitrofuran derivatives:
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Nitrofurasone (Furacilinum)
8. Antiseptics from medicinal
plants:
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Chlorophyliptum
Novoimaninum
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
Halogens
The mechanism of antimicrobial
action
• Denaturation of proteins of the
protoplasm of microbial cells by
reacting with the amino group of
the proteins, displacing hydrogen.
• Denatured protein loses its activity.
NB!!! In the presence of organic
substances halogen’s
antimicrobial effect decreases.
Iodines
• Iodine - active bactericidal element.
• At a dilution of 1: 20 000 - kill vegetative forms of bacteria for 1
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.
Iodine cont.
LUGOL'S SOLUTION
(Iodine-1 part, 2 part -KI, water-17 part)
INDICATION: Mucus lubrication in pharyngitis and laryngitis.
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IODDICERINE
(Iodine, dimethyl sulfoxide, glycerol)
Fungicidal, antimicrobial, antiviral, antinecrotic, antioxidant
effects.
NB!!!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, napkins, irrigation, washing.
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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.
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 tools .
• 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.
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.
SIDE EFFECTS: Dry hands, itchy skin, dermatitis.
• !!!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 pelliclecoated enamel surface.
Halogens
Oxidizing agents
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• 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.
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.
Potassium permanganate
• 2KMnO4 + H2O = 2KOH + 2MnO2 + 3O2
It liberates oxygen in atomic form.
• Highly water soluble, used in 1:40001:10000 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.
Heavy metal compounds
• Their mechanism of action is the blocking of SHgroups, 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.
Heavy metal cont.
• 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, sympathomimetics, plasma expanders,
vasoconstrictors, narcotic analgesics.
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, antiinflammatory, anti-fungal 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.
• Indications: Oily seborrhea, acne, eczema, psoriasis, ichthyosis,
warts, corns, etc.
Alkalis
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.
Organic antiseptics
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Group of (aromatic) phenol, resorcinol,
thimol, tar, ichthiol, 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 COMPOUNDS
Phenols
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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.
Group of aldehydes and
alcohols
FORMALDEHYDE SOLUTION, LISOFORM, 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 of tools
(0.5%). For the preservation of anatomical objects.
Aldehydes and alcohols
(Formaldehyde cont.)
• 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 ALCOHOL
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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.
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.
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
(FURACILLIN, FURAZOLIDONE)
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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.
Detergents
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Detergents - are 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.
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.
SULFONAMIDES
Sulfonamides
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Sulfa drugs (SA) - synthetic chemotherapeutic agents,
which are derivatives of sulfanilamide, or amides of
sulfonic acid.
Common
properties of
SA:
- Sulfa nucleus;
- Mechanism of
action;
- Spectrum of
antibacterial
action.
The first preparation of SA: Red Streptocid (1935).
Classification of SA
I. Preparations with the resorptive (system) action
which are well absorbed in the intestine, creating
high concentrations in the blood and other
tissues:
1.short-acting drugs (t1/2 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;
• - Ethazol;
• - Norsulfazol;
• - Urosulfan.
Classification of SA cont.
2. drugs with intermediate action (t 1/2 = 10 24 hours):
• - Sulfazin;
• - Sulfamethoxazole.
3. long-acting (t 1/2 = 24-28 hours):
• - Sulfadimetoxin;
• - Sulfapiridazin;
• - Sulfamonomethoxine.
4. extremely long-acting (t 1/2 of 48 hours):
• - Sulfalen.
Classification of SA
II. 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;
III. 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.
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
synthase.
• Sulfonamides therefore are reversible inhibitors
of folic acid synthesis and bacteriostatic not
bacteriocidal.
Mechanism of action
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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.
SA antimicrobial spectrum
• Currently used SA have broad spectrum, they
inhibit gram-positive and gram-negative
bacteria:Streptococcus pneumoniae, betahaemolytic streptococci, E. coli, Klebciella,
Shigella, Salmonella, Enterobacter, Gonococci,
Meningococci and Pneumococci;
• Nocardia,
• Chlamidia,
• Protozoa (toxoplasma and malarial plasmodia).
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%.
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Biotransport. Reversibly binds 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).
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Distribution. Pass through the blood-tissue,
placenta and blood-brain barriers. Also passes into
breast milk.
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SA pharmacokinetics (cont.)
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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.
Clinical uses of SA
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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.
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.
COMBINED SULFA DRUGS
1 - Combination with 5-aminosalicylic acid:
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SALAZOSULFOPIRIDIN
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SALAZOPIRIDAZIN
2 - combined with Trimethoprim:
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BISEPTOL, COTRIMOXAZOLE, BACTRIM
(TRIMETHOPRIM + SULFAMETHOXAZOLE)
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SULFATON (TRIMETHOPRIM + SULFADIMEZIN)
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.
Combined sulfa drugs
(BISEPTOLUM).
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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.
Features of combined SA drugs
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- 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).
FLUOROQUINOLONES
Antimicrobials with different
chemical structure.
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5.
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1.
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3.
FLUOROQUINOLONES:
mono fluorine substitute• trifluorine substitute
ciprofloxacin
1. traufloxacin
ofloxacin
2. gatifloxacin
pefloxacin
3. gemifloxacin
4. moxifloxacin
norfloxacin
enoxacin
bifluorine substitute
lomefloxacin
ofloxacin
sparfloxacin
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
FLUOROQUINOLONES cont.
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
Naphthalidine Derivatives



NALIDIXIC ACID
OXOLINIC ACID
PIPENAMIC 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)
Nitrofurans
(classification)
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
1.
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
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.
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)
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
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, acnelike skin rash, treatment - the NaCl solution).

Allergic reactions
Imidazole derivatives

Metronidazole

Tinidazole
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.
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).
Thank you)))