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LO11 PC2 ANTI-INFECTIVE AGENTS

Terminology
Anti-infective aka antimicrobial General term referring to drugs active against
pathogens
Antibiotic aka antibacterial active against bacteria
Chemoprophylaxis prophylactic use of a medication
Pathogenicity ability of an organism to cause disease in a human
Virulence severity of disease that an organism is able to cause; a highly virulent
pathogens causes disease when present in very small numbers
Acquired Resistance when a microbe is no longer affected by an anti-infective
Nephrotoxicity adverse effect on the kidneys
Hepatotoxicity an adverse effect on the liver
Ototoxicity an adverse effect on hearing
Superinfection condition caused when a microorganism grows rapidly as a result
of having less competition in its environment
Common Human Pathogens
o Viruses
o Gram (+) organisms: enterococci,
streptococci and staphylococci
o Gram (-) organisms: E.coli, Bacteroides, Klebsiella, Proteus, Pseudomonas
o Opportunistic
o Community-acquired vs. nosocomial
Common Bacterial Pathogens
o StaphylococciCommon in wounds , URIs and pneumonia (MRSAresistant
strain)
o StreptococciCommon infection in URIs, ear infections & pneumonia
o EnterococciCommon infection in UTIs & wounds (VREresistant strain)
o Escherichia coliUTIs; GI infection most commonly related to contaminated
ground beef
o KlebsiellaCauses respiratory tract infections, UTIs, bloodstream, burn
wound infections
o PneumococciMost common cause of pneumonia in children; otitis media
o ProteusCause UTIs and wound infections
o PseudomonasCause respiratory tract infections, UTIs, wound & burn wound
infections (high resistance to many antibiotics)
Definitions and Standards for Removing Microorganisms (Block and Beale,
11th edition)
Antisepsis Application of an agent to living tissue for the purpose of
presenting infection.
Decontamination Destruction or marked reduction in the number of
activities of microorganisms.
Disinfection Chemical or physical treatment that destroys most
vegetative microbes or viruses, but nut spores, in or on
inanimate
surfaces.
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Sanitization Reduction of microbial load on an


level considered acceptable for public health purposes.

inanimate surface to a

Sterilization A process intended to kill or remove all types of


microorganisms, including spores, and usually including viruses with an
acceptably low probability of survival.
Pasteurization A process that kills non-sporulating microorganisms by hot
water or steam at 65-100 degrees Centigrade.
Sterilants, Antiseptics and Disinfectants
Sterilants, antiseptics and disinfectants are evaluated by:
o intrinsic resistance of the microbe,
o the microbial load,
o the mixture of the population of microorganisms present,
o the amount and nature of organic material present,
o the concentration and stability of the disinfectant or sterilant,
o the time and temperature of exposure,
o the pH,
o the hydration and binding of the agent to the surface.
Extensively used in hospitals and other health care settings for a variety of topical
and hard-surface applications.
Chemical agents present are alcohols, phenols, iodine, and chlorine.
Most demonstrate broad-spectrum antimicrobial activity.
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC88911/

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Antiseptics
Diverse class of compounds
Applied to skin surfaces or mucous membranes for anti-infective effects.
Bacteriocidal or bacteriostatic.
Uses:
o cleansing of skin and wound surfaces after injury,
o preparation of skin surfaces prior to injections or surgical procedures,
o routine disinfection of the oral cavity as part of a program of oral hygiene,
o disinfection of inanimate objects, including instruments and furniture
surfaces.
o For skin cleaning - benzalkonium chloride, chlorhexidine, hexachlorophine,
iodine compounds, mercury compounds, alcohol and hydrogen peroxide.
o Chlorhexidine - oral rinses and preoperative total body washes.
o Benzalkonium chloride and hexachlorophine - hand scrubs or face washes.
o Iodine compounds like tincture of iodine and povidone iodine have the
broadest spectrum compared to all topical anti-infectives, with action against
bacteria, fungi, viruses, spores, protozoa, and yeasts.

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o
o

Hydrogen peroxide acts through the liberation of oxygen gas, which may be
useful for wound cleansing through removal of tissue debris.
Thimerosal (Mersol) is a mercurcontains Hg and has activity against bacteria
and yeasts. Prolonged use may result in mercury toxicity.

Precautions:
o Hypersensitivity reactions for chlorhexidine, benzalkonium and
hexachlorophine.
o Skin dryness and irritation for products containing alcohol.
o Systemic toxicity from ingestion of iodine or mercury compounds.
o Chlorhexidine should not be instilled into the ear.
o Iodine compounds should be used sparingly during pregnancy and lactation
due to risk of infant absorption of iodine with alterations in thyroid function.
o Interactions
o Antiseptics should not be used together with any other topical cream,
solution, or ointment.
http://medical-dictionary.thefreedictionary.com/Antiseptics
Alcohols and related compounds
1 aliphatic alcohols are germicidal.
Potency increases but water solubility decreases with chain length until amyl
alcohol (6 carbons) is reached.
Do not destroy bacterial spores.
70% Ethyl alcohol (ethanol) and 50% isopropyl alcohol (isopropanol) are the most
widely used.
http://www.merckmanuals.com/vet/pharmacology/antiseptics_and_disinfectants/alco
hols.html
Alcohol is produced by fermentation from grain and carbohydrates or by sulfuric
acidcatalyzed hydration of ethylene.
Denatured alcohol is ethanol that has been rendered unfit for use in intoxicating
beverages by the addition of other substances. Completely denatured alcohol
contains added wood alcohol (methanol) and benzene and is unsuitable for internal
or external use.
Specially denatured alcohol is ethanol treated with one or more substances so
that its use may be permitted for a specialized purpose, eg. For preparation of
tincture of iodine.
Isopropanol is slightly more potent than ethanol due to its greater depression of
surface tension.
Rubbing alcohol is a mixture of alcohols, with isopropanol as its principal
ingredient. It is used as a skin disinfectant and rubefacient.
The primary medicinal use of alcohol is external, as an antiseptic, preservative, mild
counter-irritant, or solvent.
http://www.merckmanuals.com/vet/pharmacology/antiseptics_and_disinfectants/alco
hols.html
Alcohol is metabolized in the human body by a series of oxidations.
Alcohol is used in the practice of pharmacy for the preparation of spirits. tinctures,
and fluidextracts. Spirits are preparations containing ethanol as the sole solvent.
Tinctures are hydroalcoholic mixtures.
Dehydrated Ethanol, USP or absolute ethanol contains not less than 99% w/w of
C2H5OH, prepared commercially by azeotropic distillation of an ethanol:benzene
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mixture, with efficient removal of water. This is used primarily as a chemical reagent
or solvent but has been injected for the local relief of pain in carcinomas and
neuralgias.
Isopropyl Alcohol, USP or Isopropanol (2-propanol) is considered a substitute for
ethanol in most cases but must not be ingested. Iso-PrOH is prepared commercially
by the sulfuric acidcatalyzed hydration of propylene. Iso-PrOH is used primarily as
a disinfectant for the skin and for surgical instruments. The alcohol is rapidly
bactericidal from 50 to 95%.
Azeotropic iso-PrOH USP, is used on gauze pads for sterilization of the skin prior
to hypodermic injections and in pharmaceuticals and toiletries as a solvent and
preservative.
Ethylene oxide (EO), has been used to sterilize temperature-sensitive medical
equipment and certain pharmaceuticals that cannot be heat sterilized in an
autoclave. EO effectively destroys all forms of microorganisms at ambient
temperatures. EO forms explosive mixtures in air at concentrations ranging from 3
to 80% by volume. The explosion hazard is eliminated when the gas is mixed with
sufficient concentrations of carbon dioxide.
Carboxide is a commercial sterilant containing 10% EO and 90% carbon dioxide.
The mechanism of the germicidal action of EO probably involves the alkylation
of functional groups in nucleic acids and proteins by nucleophilic opening of the
oxide ring. EO is a nonselective alkylating agent and as such is extremely toxic and
potentially carcinogenic. Exposure to skin and mucous membranes should be
avoided. and inhalation of the gas should he prevented by use of an appropriate
respiratory mask during handling and sterilizalion procedures.

Aldehydes
Formaldehyde Solution, USP - colorless aqueous solution containing not <37%
w/v of HCHO with MeOH added to retard polymerization. Formalin readily undergoes
oxidation and polymerization, leading to formic acid and paraformaldehyde. Thus,
should be stored in tightly closed. light-resistant containers. HCHO must be stored
at temperatures above 15C to prevent cloudiness, which develops at lower
temperatures.
Activity: germicidal action is slow but powerful.
MOA: direct nonspecific alkylalion of nucleophilic functional group (amino. hydroxyl,
and sulfhydryl) in proteins and acids to form carbinol derivatives.
Action not confined to microorganisms.
Side effects - irritating to the mucous membranes; causes hardening of the skin;
with ingestion, GI distress; contact dermatitis; pure form carcinogen.
Glutaraldehyde Disinfectant Solution. USP.
Glutaldehyde (Cidex. a 5-carbon dialdehyde) is used as a solution for sterilization of
equipment and instruments that cannot be autoclaved. Commercial glutaraldehyde
is stabilized in alkaline solution. The preparation has two components,
glutaraldehyde and buffer, mixed together immediately before use. The activated
solution contains 2% glutaraldehyde buffered at pH 7.5 to 8.6. Stabilized
glutaraldehyde solutions retain over 80% of the original activity 30 days after

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preparation, whereas the non-stabilized alkaline solution lose about 44% activity
after 15 days. At higher pH (>8.5), glutaraldehyde polymerizes.
Non-buffered solutions are acidic, possibly because of an acidic proton on the
hemiacetal form.
The acidic solutions are stable but had sporocidal activity.
Phenols and derivatives
Phenolic compounds denature proteins and are general protoplasmic poisons.
Phenol (carbolic acid) bacteriostatic at concentrations of 0.11% ,
bactericidal/fungicidal at 12% , 5% solution kills anthrax spores in 48 hr.
Bactericidal action enhanced by EDTA and warm temperatures; decreased by
alkaline medium (through ionization), lipids, soaps, and cold temperatures.
Concentrations >0.5% exert local anesthetic effect, 5% solution strongly irritating
and corrosive to tissues.
Oral ingestion or extensive application to skin can cause systemic toxicity - CNS and
cardiovascular effects; death may result.
Used for disinfection of equipment or organic materials that are to be destroyed (eg,
infected food and excreta).
Not used much as an antiseptic except to cauterize infected areas, eg, infected
umbilicus of neonates.
Incorporated into cutaneous applications for pruritus, stings, bites, burns, etc,
because of its local anesthetic and antibacterial properties to relieve itching and
control infections.
Liquefied Phenol, USP is phenol containing 10% water. This is a convenient way
of adding phenol to a variety of pharmaceutical preparations because of ease of
measurement and facility of transferring.
p-Chlorophenol is used in combination with camphor in liquid petrolatum as an
external antiseptic and anti-irritant. The compound has a phenol coefficient of ~4.
p-Chloro-m-xylenol (PC-MX: Metasep) is a non-irritating antiseptic agent with
broad-spectrum antibacterial and antifungal properties, marketed at 2%
concentration as a shampoo, and used topically for the treatment of tinea
(ringworm) infections such as athlete's foot (tinea pedis and jock itch (tinea cruris).
Hexachlorophene, USP (pHisoHex) is a biphenol possessing greater potency than
a monophenol.
Increased degree of chlorination, increases its antiseptic potency further.
Hexachlorophene is easily adsorbed onto the skin and enters the sebaceous glands.
Because of this, topical application elicits a prolonged antiseptic effect, even in low
concentrations.
Hexachlorophene is used in concentrations of 2-3% soaps. detergent creams,
lotions, and shampoos for a variety of antiseptic uses.
It is, in general, effective against Gram (+) bacteria, but many Gram (-) bacteria are
resistant.
Banned for OTC antiseptic and cosmetic preparations, but still available by
prescription.
Cresol, NF is actually a mixture of three isomeric methylphenols:

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The mixture occurs as a yellow to brownish-yellow liquid that has a characteristic


odor of creosote.
Obtained from coal tar or petroleum by alkaline extraction into aqueous medium,
acidification, and fractional distillation.
The mixture is an inexpensive antiseptic and disinfectant possessing a phenol
coefficient of 2.5.
Cresol is sparingly soluble in water, although alcohols and other organic solvents
will solubilize it.
Drawback to its use as an antiseptic is its unpleasant odor.
Chlorocresol, NF occurs as colorless crystals. Slightly soluble in water and is
useful only as a preservative.
Thymol. NF or isopropyl m-cresol is extracted from oil of Thymus vulgaris or thyme
by partitioning into alkaline aqueous medium followed by acidification. The crystals
obtained from the mother liquor are large and colorless, with a thyme-like odor. It is
only slightly soluble in water, but extremely soluble in alcohols and other organic
solvents.
It has mild fungicidal properties and is used in alcohol solutions and in dusting
powders for the treatment of tinea (ringworm) infections.
Eugenol, USP obtained from clove oil.
Slightly soluble in water but is miscible with alcohol and other organic solvents.
Possesses both local anesthetic and antiseptic activity and can used to relieve
toothaches. Also used in mouthwashes because of its antiseptic property and
pleasant taste.
Phenol coefficient is 14.4.
Resorcinol, USP. m-Dihydroxybenzene (resorcin) is prepared synthetically. It
crystallizes as white needles or as an amorphous powder that is soluble in water
and alcohol.
Resorcinol is light sensitive and oxidizes readily, much less stable in solution,
especially at alkaline pH.
Resorcinol is only a weak antiseptic (phenol coefficient 0.4), but it is used in 1 to 3%
solutions and in ointments and pastes in concentrations of 10 to 20% for the
treatment of skin conditions such as ringworm, eczema. Psoriasis and seborrheic
dermatitis. It is also a keratolytic agent. This property causes the stratum corneum
of the skin to slough, opening the barriers to penetration for antifungal agents.
Hexylresorcinol, USP 4-Hexylresorcinol, or hexylresorcinol is a white crystalline
substance with a faint phenolic. When applied to the tongue it produces a sensation
of numbness.
Hexylresorcinol is an effective antiseptic, possessing both hactericidal and
fungicidal properties. The phenol coefficient against S. aureus is 98.
Possesses surfactant properties and local anesthetic activity.
It is formulated into throat lozenges because of its mild anesthetic and antiseptic
properties. The compound (in the concentration present in lozenges) is probably not
antiseptic, but the local anesthetic property can anesthetize the larynx.

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Pine tar is a viscid blackish brown liquid, used primarily for antiseptic bandaging of
wounds of the hoof and horn. Pine tar has antimicrobial properties.
Chloroxylenols are broad-spectrum bactericides with more activity against gram(+) than gram (-) bacteria. They are active in alkaline pH; however, contact with
organic matter diminishes their activity. Streptococci are more susceptible than
staphylococci.
Parachloro-metaxylenol (PCMX) and dichlorometaxylenol (DCMX) are most
commonly used members of this group. DCMX > active than PCMX.
A 5% chloroxylenol solution (in -terpineol, soap, alcohol, and water) is diluted with
water (1:4) for skin sterilization and (1:25 to 1:50) for wound cleansing and
irrigation of the uterus and vagina.
PCMX is also combined with hexachlorophene to enhance its antibacterial spectrum
and to prevent contamination by gram-negative organisms.
http://www.merckmanuals.com/vet/pharmacology/antiseptics_and_disinfectants/phe
nols_and_related_compounds.html
Oxidizing agents (OA)
Value as germicidal agents depend on their ability to liberate oxygen in the tissues.
Many are inorganic cornpounds, including H2O2, a number of metal peroxides and
sodium perborate. All react in the tissues to generate oxygen and oxygen radicals.
Other OA, such as KMnO4, denature proteins in microorganisms through a direct
oxidation reaction.
OA are effective against anaerobic bacteria and can be used in cleansing
contaminated wounds. The bubbles that form during the liberation of oxygen help to
dislodge debris.
Effectiveness of OA is limited by their generally poor penetrability into infected
tissues and organic matter. Additionally, the action of the oxidizers is typically
transient.
PEROXIDES
Hydrous Benzoyl Peroxide, USP. Hydrous benzoyl peroxide (Oxy-5. Oxy- 10.
Vanoxide) is a white granular powder. In its pure powder form it is explosive. The
compound is formulated with 30% water for safe handling. Compounded at 5 and
10% concentrations. benzoyl peroxide is both keratolytic and keratogenic. It is used
in the treatment of acne. Benzoyl peroxide induces proliferation of epithelial cells,
leading to sloughing and repair.
Hydrogen peroxide solution (3%) liberates oxygen when in contact with
catalase present on wound surfaces and mucous membranes. The effervescent
action mechanically helps remove pus and cellular debris from wounds and is
valuable for cleaning and deodorizing infected tissue but of short duration and is
limited to the superficial layer of the applied surface.
Hydrogen peroxide is finding increased application as a disinfectant in water
treatment and food processing facilities and for sterilization of dental and surgical
instruments.

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Recently developed accelerated hydrogen peroxide (AHP) formulations are


synergistic blends of 0.52% hydrogen peroxide with anionic and non-ionic
surfactants and stabilizers that possess broad-spectrum antimicrobial activity.
They are effective against bacteria, spores, mycobacteria, viruses, and fungi, with
short contact times.
AHP formulations are non-irritating to eyes and skin and are biodegradable,
decomposing to water and oxygen with no active chemical residues.
They have become leading disinfectants in human hospitals and dental clinics in
recent years.
A disadvantage is the potential to damage soft metals, such as brass, copper, and
aluminum, and carbon-tipped instruments.
Sodium perborate, used in antiseptic solutions and in mouthwashes, acts by
decomposing into sodium metaborate and hydrogen peroxide, which then gradually
liberates oxygen.
Benzoyl peroxide slowly releases oxygen to act as an antiseptic. However, it can
cause skin irritation. It also has keratolytic and antiseborrheic activity, which makes
it useful in treating pyoderma in dogs.
Peracetic acid has been recognized only recently as a useful sterilant and
antiseptic, has broad antimicrobial spectrum and lack of harmful decomposition
products of hydrogen peroxide with greater lipid solubility and freedom from
inactivation by tissue catalase and peroxidase. It has been accepted worldwide in
the food industry, including meat and poultry processing plants and dairies.
It is effective against bacteria, yeasts, fungi, and viruses at conc. of 0.0010.003%
and is sporicidal at 0.250.5%, 0.2% solutions applied to compresses are effective at
reducing microbial populations in severely contaminated wounds.
Potassium permanganate has broad antimicrobial properties, but staining
property is a disadvantage. It is an effective algicide (0.01%) and virucide (1%) for
disinfection, but concentrations >1:10,000 tend to irritate tissues. Easily degraded.
Halogen-containing compounds
Iodine and chlorine are used as topical antimicrobial agents. They owe their activity
to high affinity for protoplasm, where they are believed to oxidize proteins and
interfere with vital metabolic reactions.
Elemental iodine is a potent germicide with a wide spectrum of activity and low
toxicity to tissues. 50 ppm I2 solution kills bacteria in 1 min and spores in 15 min. It
is poorly soluble in water but readily dissolves in ethanol, which enhances its
antibacterial activity.
Iodine tincture contains 2% iodine and 2.4% sodium iodide (NaI) dissolved in 50%
ethanol; and used as a skin disinfectant.
Strong iodine tincture contains 7% iodine and 5% potassium iodide (KI) dissolved
in 95% ethanol; it is more potent but also more irritating than tincture of iodine.
Iodine solution contains 2% iodine and 2.4% NaI dissolved in aqueous solution; it is
used as a nonirritant antiseptic on wounds and abrasions.
Strong iodine solution (Lugol's solution) contains 5% iodine and 10% KI in
aqueous solution.

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Iodophores (eg, Povidone-iodine) are water-soluble combinations of iodine with


detergents, wetting agents that are solubilizers, and other carriers.
They slowly release iodine as an antimicrobial agent and are widely used as skin
disinfectants, particularly before surgery.
They do not sting or stain. Iodophores are nontoxic to tissues but may be corrosive
to metals.
They are effective against bacteria, viruses, and fungi but less so against spores.
Iodophor solutions retain good antibacterial activity at pH <4, even in the presence
of organic matter, and often change color when the activity is lost.
Phosphoric acid is often mixed with iodophores to maintain an acidic medium. They
have been used in teat dips to control mastitis, as dairy sanitizers, and as a general
antiseptic or disinfectant for various dermal and mucosal infections.
Chlorine
Potent germicidal effect against most bacteria, viruses, protozoa, and fungi by
forming undissociated hypochlorous acid (HOCl) in water at acid to neutral pH. It is
effective against most organisms at a concentration of 0.1 ppm, higher
concentrations are required in the presence of organic matter.
Alkaline pH ionizes chlorine and decreases its activity by reducing its penetrability.
Used to disinfect water supplies and inanimate objects (eg, bottles); in dairies,
creameries, and milk houses.
Inorganic chlorides like NaOCl solutions (bleach). 5% NaOCl decomposes, a 25%
NaOCl can be used as a disinfectant, and a more diluted form (0.5%) can be used
for irrigating suppurating wounds, but it dissolves blood clots and delays clotting.
Calcium hypochlorite is used as a disinfectant.
Organic chlorides contain chlorine weakly bonded to nitrogen, which is slowly
released for germicidal activity. They are generally less irritant, more stable, and
more convenient to use than hypochlorite solutions.
http://www.merckmanuals.com/vet/pharmacology/antiseptics_and_disinfectants/oxid
izing_agents.html
Chlorine-containing compounds
Halazone, USP. p-Dichlorosulfamoylbenzoic acid sodium salt is used to disinfect
drinking water.
Chloroazidin. N.N-Dichlorodicarbonamidine (Azochloramid) is used in very dilute
solution to disinfect wounds, as packing for dental caries, and for lavage and
irrigation.
A glyceryltriacetate solution is used as a wound dressing.
The antiseptic action of chloroazodin is long lasting because of its extremely slow
reaction with water.
Oxychiorosene Sodium. Oxychlorosene (Clorpactin) is a complex of the sodium
salt of dodecylbeozenesulfonic acid and hypochiorous acid.
The complex slowly releases hypochlorous acid in solution. It combines the
germicidal properties of HOCI with the emulsifying, wetting, and keratolytic actions
of an anionic detergent. The agent has a marked and rapid -cidal action against
most microorganisms, including both Gram-positive and Gram-negative bacteria,
molds, yeasts. viruses, and spores.

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Oxychiorosene is used to treat localized infections (especially when resistant


organisms are present), to remove necrotic tissue from massive infections or
radiation necrosis, to counteract odorous discharges, to act as an irritant, and to
disinfect cysts and fistulas.
Oxychlorosene is marketed as a powder for reconstitution into a solution.
A typical application uses a 0.1 to 0.5% concentration in water.
Dilutions of 0.1 to 0.2% are used in urology and ophthalmology.
Cationic surfactants
Surfactants lower the surface tension of an aqueous solution and are used as
wetting agents, detergents, emulsifiers, antiseptics, and disinfectants. As
antimicrobials, they alter the energy relationship at interfaces. Based on the
position of the hydrophobic moiety in the molecule, surfactants are classified as
anionic or cationic.
Cationic detergents are a group of alkyl- or aryl-substituted quaternary
ammonium compounds (eg, benzalkonium chloride, benzathonium chloride,
cetylpyridinium chloride) with an ionizable halogen.
Major site of action: cell membrane, where they become adsorbed and cause
changes in permeability.
Activity is reduced by porous or fibrous materials that adsorb them; inactivated by
anionic substances (eg, soaps, proteins, fatty acids, phosphates). Therefore, they
are of limited value in the presence of blood and tissue debris.
They are effective against most bacteria, some fungi (including yeasts), and
protozoa but not against viruses and spores. Aqueous solutions of 1:1,000 to
1:5,000 have good antimicrobial activity, especially at slightly alkaline pH.
Anionic Surfactants
Soaps are dipolar anionic detergents with the general formula RCOONa/K, which
dissociate in water into hydrophilic K+ or Na+ ions and lipophilic fatty acid ions.
NaOH and KOH are strong bases (whereas most fatty acids are weak acids), most
soap solutions are alkaline (pH 810) and may irritate sensitive skin and mucous
membranes.
Soaps emulsify lipoidal secretions of the skin and remove, along with most of the
accompanying dirt, desquamated epithelium and bacteria, which are then rinsed
away with the lather.
The antibacterial potency of soaps is often enhanced by inclusion of certain
antiseptics, eg, hexachlorophene, phenols, carbanilides, or potassium iodide.
They are incompatible with cationic surfactants.
Dyes
Organic dyes were used very extensively as anti-infective agents before the
discovery of the sulfonamides and the antibiotics. A few cationic dyes still find
limited use as antinfectives. These include the triphenylmethane dyes gentian violet
and basic fuchsin and the thiazinc dye methylene blue.
The dyes form colorless leucobase under alkaline conditions. Cationic dyes are
active against Gram-positive bacteria and many fungi. Gram-negative bacteria are
generally resistant. The difference in susceptibility is probably related to the cellular
characteristics that underlie the Gram stain.

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Gentian Violet, USP. Variously known as hexamethyl-p-rosaniline chloride, crystal


violet, methyl violet, and methylrosaniline chloride. It occurs as a green powder or
green flakes with a metallic sheen.
The compound is soluble in water (1:35) and alcohol (1:10) but insoluble in nonpolar
organic solvents.
Uses:
o vaginal suppositories for the treatment of yeast infections.
o 1 to 3% solution for the treatment of ringworm and yeast infections.
o orally as an anthelmintic for strongyloidiasis (threadworm)
o oxyuriasis.
Basic Fuchsln, USP is a mixture of the chlorides of rosaniline and p-rosaniline. It
exists as a green crystalline powder with a metallic appearance. The compound is
soluble in water and in alcohol but insoluble in ether. It is a component of carbol
fuchsin solution (Castellani's paint), which is used topically in the treatment of
fungal infections, notably ringworm and athlete's foot.
Methylene Blue, USP. 3,7-bis(dimethylamino)-phenazathionium chloride (Urised).
The compound occurs as a dark green crystalline powder with a metallic
appearance that is soluble in water (1:25) and alcohol (1:65). Methylene blue has
weak antiseptic properties that make it useful for the treatment of cystitis and
urethritis. The action of methylene blue is considered to be bacteriostatic. The
compound colors the urine and stool blue green.
END OF LECTURE

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