Antiseptics- Pharmacology of commonly used Antiseptics

 Pharmacology of commonly used Antiseptics

ANITISEPTICS

Antiseptic = agent that causes destruction or inhibition of  growth of micro organisms (bacteria, viruses, fungi) on living surfaces such as skin & mucous membranes.

Disinfectant = agent that causes destruction or inhibition of  growth of microorganisms (bacteria, viruses, fungi) on non living surfaces (instruments, equipments, pieces of furniture, rooms, etc).

Spores are (usually) not destroyed !!!

Antisepsis = use of chemical solutions for disinfection  (prefix: ”anti” = against) e.g. removal of transient microorganisms from the skin and a reduction in the resident  flora.

Asepsis = absence of infectious microoorganisms (prefix: ”a” = absence).

Aseptic techniques – aimed at minimising infection 

The use of sterile instruments.

The use of a gloved no touch technique.

History of antiseptics   

Ignaz Semmelweis (1818 – 1865) Hungarian physician working in Vienna cross contamination → high incidence of  death after childbirth.

He made doctors to wash hands in chloride of lime before touching patients.

Dramatically reduced incidence of childhood fever.

Joseph Lister (1827 – 1912) Brittish surgeoncarbolic acid (phenol) for hands  and wounds during operationsto maintain aseptic conditions→ aseptic surgery.

Properties of antiseptics/disinfectants

1. Microbicidal activity

2. Non staining & good

3. Active against all pathogens

4. Active in presence of pus, blood & exudates

5. Rapid acting

6. Non irritating to tissues / non corrosive

7. Non absorbable

8. Non sensitizing

Mechanisms of action

Disrupt cellular structures and/or processes E.g.

Oxidation of bacterial protoplasm. E.g.  H202, Halogens, potasium permanganate

Coagulation (denaturation) of proteins. E.g.  Phenols, chlorhexidine, alcohols, Aldehydes 

Increasing permeability of bacterial cell Membrane. E.g. Cetrimide, soaps.

Classification

Phenol derivatives

Oxidizing agents

Halogens

Biguanides

Quaternary amonium compounds 

Alcohols

Aldehydes

Acids

Surface antigens metallic salts (Metalls)

Dyes.

Gases.

Miscellaneous. 

Depending on concentration:

Some chemicals can act either as antiseptics or as disinfectants e.g. Phenol solution 0.2% = antiseptic; 1% = disinfectant

Phenol & derivatives

Phenol

Earliest use (19th century), reference Standard 

mechanism: denaturation of bacterial proteins

Uses: disinfection of urine/faeces/pus contaminated surfaces/areas

Extremely irritating, corrosive

Cresol

Methyl derivative of phenol, less damaging to tissues than phenol.

3-10 times more active used for disinfection of utensils, excreta & for washing hands.

Chloroxylenol (Dettol)

Does not coagulate proteins

Non corrosive, Non irritating to skin.

Commercial 4.8 % solution used for surgical antisepsis

Skin cream and soap: 0.8%

Mouth wash 1% .

Oxidizing agents

Peroxides

Short-acting germicidal effect through release of nascent oxygen, which irreversibly alters microbial Proteins.

Little or no action on bacterial sporesnascent oxygen rendered inactive when it combines with organic matter.

e.g. Hydrogen peroxide solution (3%)

Releases oxygen in contact with catalase on wound surfaces and  mucous membranes; effervescent action mechanically helps  remove pus and cellular debris from wounds and is valuable cleaning infected tissue.

Peracetic acid

Broad antimicrobial spectrum (like hydrogen peroxide) +  greater lipid solubility.
Effective against bacteria, yeasts, fungi, and viruses (0.001–0.003%)
sporicidal at 0.25–0.5%
Solutions of 0.2% peracetic acid applied to compresses are effective at reducing microbial populations in severely contaminated wounds.

Potassium permanganate:

Broad antimicrobial properties,  
Effective algicide (0.01%) and virulicide (1%) for  disinfection, but concentrations >1:10,000 tend to irritate tissue.
Old solutions turn chocolate brown and lose their activity 
Stains tissues and clothing brown (disadvantage)

Halogens & halogen containing compounds

Iodine tinctures

2% iodine + 2.4% sodium iodide (NaI) in 50%  ethanol; it is 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

2% iodine + 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. 

Chlorine 

Potent germicidal effect against most bacteria, viruses,  protozoa, and fungi at a concentration of 0.1 ppm, 
but much higher concentrations are required in the presence of  organic matter.
Alkaline pH ionizes chlorine and decreases its activity by reducing its penetrability.
irritant to the skin and mucous membranes
widely used to disinfect water supplies and inanimate objects (eg, utensils, bottles, pipelines)
sodium hypochlorite solutions (bleach) 2–5% 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 
Root canal therapy in dentistry

 Biguanides

Chlorhexidine

Acts by disrupting bacterial cell membrane & denaturation  of bacterial proteins
Non irritant, more active against Gram + bacteria
Used in for surgical scrub, neonatal bath, mouth wash &  general skin antiseptic
Most widely used antiseptic in dentistry 0.12-0.2% oral rinse or 0.5 -1 % tooth paste.

Quaternary amonium compounds

Detergents

destroy bacteria, fungi & viruses by Altering permeability of cell membrane
Efficiently remove dirt and grease
Widely used as antiseptics & disinfectants for surgical instruments, gloves etc.

Soaps

Anionic detergents
Weak antiseptics with cleansing action 
Washing with soap and warm water one of the most effective  methods of preventing disease transmission

Alcohols

Ethanol

Antiseptic, cleansing agent at 40-90%
Act by precipitation of bacterial proteins
Irritant, should not be applied on mucous membranes,  ulcers, open wounds

Aldehydes – Formaldehyde

Also used as sterilization agents!
Used for fumigation
37 % aqueous solution (formalin)
denaturates proteins
Used for preserving dead tissues
Use as antiseptic restricted due to bad odour & irritation
Glutaraldehyde is a better sterilizing Agents 

Acids

Boric acid

weak antiseptic, bacteriostatic
used for mouth wash, irrigation eyes glossitis, 
Adverse effect: vomiting,abdominal pain on systemic absorption

Metals: metallic salts

Silver 

Silver ions precipitate proteins + interfere with essential metabolic  activities of microbial cells
0.1% aqueous silver solution – bactericidal but irritating
0.01% solution – bacteriostatic
0.5% solution – sometimes applied  as a dressing on burns to reduce infection
Colloidal silver compounds – slowly releasing silver ions
more sustained bacteriostatic effect
non-irritant
mild antiseptics, also used in ophthalmic preparations

Dyes

Gentian violet (Crystal violet)

topical antiseptic; commonly used for
Marking the skin for surgery preparation and allergy testing 
Effective against Candida albicans and related infections  such as thrush, yeast infections, tinea, etc.
In resource limited settings, , gentian violet is used to manage  burn wounds, inflammation of the umbilical cord stump  (omphalitis) in neonates, oral candidiasis, mouth ulcers

ACRIFLAVINE 

Active against gram +ve Bacteria gonococci
Store in amber colored bottle
Nonirritant
Use chronic ulcers and wounds

Gases

Ethylene Oxide

Acts by alkylating proteins and nucleic acid
Highly inflammable and explosive.
Used for sterilization of heart – lung machine, plastic equipment,  sutures, dental equipment and cardiac catheters. 
Not used for fumigation as it is explosive.

Formaldehyde

40% solution is called formalin.
Formaldehyde solution is used for disinfection of sputum,  removal of warts, on palms and soles to treat hyperhidrosis,  preservation of anatomical and pathological specimens.
Formaldehyde gas used for fumigation of wards and OT’s  rarely for sterilization of heart instruments and gloves.
In dentistry it is used to harden the residual pulp tissue.

Miscellaneous

Nitrofurazone has bactericidal action on fungi. 
It is  used topically for burns and Ulcers.
Pharmacology of commonly used Antiseptics Notes PDF


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