Anti infectives 4.1

Did not include alcohols and cationic surfactants, gi tapul kog input hehe

Joseph Lister (in 1867)

He introduced antiseptic principles for surgery and post traumatic injury

Phenol (Carbolic Acid)

He used ____________ (__________) as a wash for the hands, as a spray on an incision site, andonbandages applied to wounds. Lister’s principles caused a dramatic decrease in the incidenceof postsurgical infections

Paul Erlich

The father of chemotherapy

Selective toxicity

The property of certain chemicals to destroy one form of live without harming another, was the cornerstone of modern antimicrobial chemotherapy

Robert Koch

Paul Erlich was a disciple of ______________

Gerntian violet

Name the chemical

Methylene blue

Name the chemical

Selective toxicity

The main tenet of modern antimicrobial chemotherapy

sulfonamides and penicillins

Ehrlich’s seminal discovery paved the way for the development of the ___________ and __________ and the elucidation of the mechanisms of selective toxicity.

Cinchona

Herbal remedy for malaria

Ipecac

herbal remedy for amebic dysentery

Salvarsan

Ehrlich’s discovery of compound 606, the effective anti syphilitic drug ______________, was a breakthrough in the treatment of a serious, previously untreatable disease.

Group IIB-Mercury
Group VA - Arsenic & Antimony

Until the 1920s, most successful anti-infective agents were based on the group-___ element ____ and the group-___elements ________ and _________.

Atoxyl (Sodium arsanilate and arsphenamine)

______________(______________________) was used for sleeping sickness

Trypanosomiasis

This is a vector-borne parasitic disease caused by protozoans, transmitted by bites of tse tse flies (glossina)

Atoxyl

Name the compound

Arsphenamine

Name the compound

Germicides

Anti-infective agents that are used locally are called __________, and within this classification, there are two primary subtypes and several other definitions of sanitization.

Antiseptics

___________ are compounds that kill (-cidal) or prevent the growth of (-static) microorganisms when applied to living tissue.

1. Low toxicity
2. Exert a rapid and sustained action
3. Low surface tension
4. Retain activity in presence of body fluids
5. Non-irritating to tissues
6. Non-allergenic
7. Does not interfere with healing

Ideal Characteristics of an antiseptic agent (7)

1. Bacitracin
2. Polymyxin
3. silver sulfadiazine
4. Neomycin

A few antibiotics, such as _______, ____________, _______________, and ___________, are poorly absorbed through the skin and mucous membranes and are used topically for the treatment of local infections.

Disinfectant

An agent that prevents transmission of infection by the destruction of pathogenic microorganisms when applied to inanimate objects

1. Exert rapid lethal action to pathogenic microorganisms and spores
2. Good penetrating properties into organic matter
3. Shares compatibility with organic compounds (esp soaps)
4. Not inactivated by living tissues
5. Non corrosive
6. Aesthetically pleasing

6 Characteristics of an ideal Disinfectant

Washing of hands

The most important means of preventing transmission of infectious agents from person to personorfrom regions of high microbial load, such as the mouth, nose, or gut, to potential sites of infection is simply ________________

Skin disinfectants with soap and water

These are usually used as preoperative surgical scrubs and sterilants for surgical incisions.

Chemotherapy

It is the study and the use of chemical agents that are selectively more toxic to invading organisms than to the host.

1. Chemical type
2. Biological property
3. Therapeutic indication

3 Chemotherapeutic agents are classified according to their:

Antibiotics

Anti infectives from natural source to semi-synthetic

Antimicrobials

Anti infectives produced from synthetic substance

Antisepsis

Application of an agent to living tissue to prevent infection

Decontamination

Destruction or marked reduction in the number or activity of microorganisms

Disinfection

The chemical or physical treatment that destroys most vegetative microbes or viruses, but not spores, in or on inanimate surfaces

Sanitization

The reduction of microbial load on an inanimate surface to a level considered acceptable for public health purposes

Sterilization

The process intended to kill or remove all types of microorganisms, including spores, and usually viruses with an acceptably low probability of survival

Pasteurization

A process that kills nonsporulating microorganisms by hot water or steam at 65 to 100 degrees Celsius

Phenol Coefficient test

A standardized test in which the dilution of the chemical agent being evaluated that kills a standard number of bacteria in 10 min is compared to the dilution of phenol that accomplished the same task

Salmonella typhii, and Staphylococcus aureus

Phenol Coefficient test has some faults in that the standard test organisms are ___________________, and _______________ and not the gram-negative bacteria that are usually associated with nosocomial infections.

1. Infections acquired in the hospital
2. An organism can become resistant to disinfectants and in some cases, the disinfectant has become a source of infection for the susceptible person

2 Nosocomial infection

1. Oxidizing agents
2. Dehydrating agents
3. Alkylating agents
4. Sulfhydryl Combining agents
5. Agents affecting permeability

5 Modes of action

1. Halogens (Chlorine and Iodine)
2. Hydrous benzoyl peroxide
3. Acids

Examples of oxidizing agents

Alcohol

Example of dehydrating agent

1. Ethylene oxide
2. Formaldehyde
3. Glutaraldehyde

Examples of Alkylating agents

1. Anionic and Cationic detergents
2. Non-ionic detergents
3. Phenols
4. Chlorhexidine

Examples of agents affecting permeability

KMnO4

Other oxidizing agents, such as ___________, denature proteins in microorganisms through a direct oxidation reaction

Oxidizing agents

These are effective against anaerobic bacteria and can be used in cleansing contaminated wounds.

Elemental iodine (I2)

the oldest germicide still in use today

Iodine Tincture

2% iodine in 50% alcohol with sodium iodide

Lugol’s Solution

AKA Strong iodine solution (5% iodine in water with potassium iodide)

Iodine Solution

2% iodine in water with sodium iodide

Phenylalanyl and Tyrosyl

sulfhydryl groups

Iodine is one of the most effective and useful of the germicides. It acts to inactivate proteins by iodination of aromatic residues (_________ and _________) and oxidation (______ groups).

Iodophors

are complexes of iodine with non-ionic or cationic surfactants (solubilizers); the complex reduce the volatility of I2 and remove its irritant properties, have both bactericidal and fungicidal properties.

Povidone Iodine

This is a charge-transfer complex of iodine with the nonionic surfactant PVP (polyvinylpyrrolidone).

Povidone Iodine

is used as an aqueous solution for presurgical disinfection of the incision site, can also be used to treat infected wounds and damage to the skin, and it is effective for local bacterial and fungal infections

Povidone iodine

Name this compound

True

True or false?

Povidone iodine is extremely water soluble and releases iodine very slowly

10%

In povidone iodine, approximately ___% of the iodine in the complex is bioavailable.

Chlorine and Chloride releasing compounds

These compounds have been used in the disinfection of water supplies for more than a century.

HClO - Hypochlorous acid

the active germicidal species that is formed when chlorine is dissolved in water led to the development and use of the first inorganic hypochlorite salts such as NaOCl and Ca(OCl)2.

organic N-chloro compounds

Later, __________ were developed as disinfectants. These compounds release hypochlorous acid when dissolved in water, especially in the presence of acid.

Sodium Salt of Halazone

The sodium salt of _________, is used to disinfect drinking water.

Halazone

p-Dichlorosulfamoylbenzoic acid, photosensitive compound with a faint chlorine odor

Halazone

Name this compound

Chloroazodin

Name this compound

Chloroazodin

N,N-dichlorodicarbonamidine (Azochloramid), yellow crystalline solid with a faint odor of chlorine, unstable to light or heat. It will explode if heated above 155 Celsius

False, the antiseptic action of chloroazodin is long lasting because of its extremely slow reaction with water.

True or False?

The antiseptic action of chloroazodin is fast because of its extremely fast reaction with water.

Oxychlorosene

Name this compound

Oxycholorosene (Chlorpactin)

is a complex of the sodium salt of dodecylbenzenesulfonic acid and hypochlorous acid. The complex slowly releases hypochlorous acid in solution.

Oxycholorosene (Chlorpactin)

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.

Oxycholorosene (Chlorpactin)

Used to treat localized infections, 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.

0.1 to 0.5% - Typical Application
0.1 to 0.2% - Urology and Ophthalmology

A typical application uses a ________% concentration in water. Dilutions of _____% are used in urology and ophthalmology.

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 to make it safer to handle.

It is used in the treatment of acne

Benzoyl Peroxide

This induces proliferation of epithelial cells, leading to sloughing and repair

Hydrous Benzoyl Peroxide

Name the compound

Tinea or ringworm

Dermatophytoses are collectively called

Keratolytic agents - Salicylic acid or other α-hydroxy compounds

The skin is a formidable barrier to drug penetration, and many of the topical agents work best if an adjuvant is added that opens the barrier function of the skin. _____________ such as ___________ or other ________________ perform this function reasonably well.

Sebum

Adults have an acidic, fatty substance in and on the skin called ____________

antifungal

Sebum functions as a natural ______ agent, part of the innate immune system.

Propionic acid

an antifungal agent that is nonirritating and nontoxic. After application, it is present in perspiration in low concentration (0.01%).

Zinc Propionate

Occurs as an anhydrous form and as a monohydrate, salt is unstable to moisture, and is used as a fungicide, particularly on adhesive tape.

Undecylenic acid (Desenex, Cruex)

Obtained from destructive distillation of castor oil. A viscous yellow liquid.

Insoluble in water, but soluble in alcohol and most organic solvents

can be used in concentrations up to 10% in solutions, ointments, powders, and emulsions for topical administrations.

the preparations should never be applied to mucous membranes because it is a severe irritant

Benzoic acid

This possesses appreciable antifungal effects, but it cannot penetrate the outer layer of theskin in infected areas. Therefore, when used as an antifungal agent, this must be admixed with a keratolytic agent.

Whitfield’s Ointment, USP

An old preparation that is still in use is _________________. This ointment contains benzoic acid (6%) and salicylic acid (6%) in a petrolatum base. The cure rates from preparations like these are low.

Salicylic acid - pKa 2.5

is a strong aromatic acid (pKa ____) with both antiseptic and keratolytic properties

occurs as white, needle like crystals or a fluffy crystalline powder, depending on how the compound was brought out of solution.

used externally in ointments and solutions for its antifungal and keratolytic properties.

only slightly soluble in water but is soluble in most organic solvents.

m-Hydroxyphenol (resorcinol)

possesses antiseptic and keratolytic activity. It occurs as white, needlelike crystals and has a slightly sweet taste

is soluble in water, alcohols, and organic solvents.

Ethylene Oxide (C2H4O)

Name this compound

Ethylene Oxide (C2H4O)

has been used to sterilize temperature sensitive medical equipment and certain pharmaceuticals that cannot be heat sterilized in an autoclave.

Ethylene Oxide (C2H4O)

a colorless, flammable gas that liquefies at 12°C

Ethylene Oxide (C2H4O)

readily through porous materials and very effectively destroys all forms of microorganisms at ambient temperatures

Ethylene Oxide (C2H4O)

forms explosives mixtures in air at concentrations ranging from 3% to 80% by volume.

CO2

Mixed to Ethylene oxide to eliminate explosion hazard

Ethylene Oxide

is a nonselective alkylating agent, and for that reason is extremely toxic and potentially carcinogenic.

Formalin

is a colorless aqueous solution that officially contains not less than 37% w/v of formaldehyde(HCHO), with methanol added to retard polymerization

Formic acid, and paraformaldehyde

Formaldehyde readily undergoes oxidation and polymerization, leading to ___________ and _______________, respectively, so the preparation should be stored in tightly closed, light-resistant containers

15 degrees Celsius

Formalin must be stored at temperatures above ______ to prevent cloudiness, which develops at lower temperatures

Action is slow but powerful

The germicidal action of formaldehyde is (slow/fast) but (weak/powerful).

Top - Formic Acid
Bottom - Paraformaldehyde

Name these compounds