[MID-MEDORG-02] ANTI-INFECTIVE AGENTS

This flashcard is about Anti-Infectives.

John Lister

In 1867, he introduced phenol for antiseptic principles.

(Lister’s principle caused dramatic decrease in postsurgical infections).

Phenol (Carboxylic Acid)

John Lister used this as wash for the hand.

Paul Erlich

Who is the Father of Chemotherapy?

Paul Erlich

Disciple of Robert Koch, began to work with set of antibacterial dyes and anti-parasitic organic arsenicals.

Anti-microbial activity

Paul Erlich’s goal is to develop compounds that retain _________ activity at the expense of toxicity to human host.

Magic bullets

These are antimicrobial agents that selectively attack pathogens without significant toxicity to the host.

Paul Erlich

Who discovered that the anti-microbial properties of dyes are parallel to staining activity (first demonstration of selective toxicity)?

Salvarsan

This is the first anti-syphilitic drug.

Compound 606

Salvarsan is also known as?

Selective Toxicity

Main tenet of modern antimicrobial therapy.

• The property of certain chemicals to kill one type of organism while not harming other.

1920s

What year is the most successful anti-infective agents based on Group-IIB element mercury and the Group-VA elements arsenic and antimony?

Group-IIB element mercury and the Group-VA elements arsenic and antimony

These are the basis for anti-infective agent.

H.W. Thomas

In 1920, he discovered the most successful anti-infective agents based on the group-IIB element mercury and the group-VA element arsenic and antimony, Atoxyl.

Atoxyl

Sodium arsanilate and arsphenamine was used for sleeping sickness and these are drugs derived from synthetic dyes.

• Gentian violet

• Methylene blue

What are some examples of dyes where atoxyl was discovered?

Atoxyl

Somewhat effective were a few chemical conjurers of the quinine molecule.

• Some of these agents represented significant achievements in anti-infective therapy but they also possess some important limitations.

• Mercury

• Arsenic

• Antimony

Atoxyl contains elements used against parasites, exemplifying the use of heavy metals as therapeutic agents despite their potential toxicity.

Germicides

Anti-infective agents that are used locally.

Antisepsis

Definition and Standard for Removing Microorganism:

Application of an agent to living tissue for the purpose of preventing infection.

Disinfection

Definition and Standard for Removing Microorganism:

Chemical or physical treatment that destroys most vegetative microbe or viruses, but not spores, in or inanimate surface.

Decontamination

Definition and Standard for Removing Microorganism:

Destruction or marked reduction in the number of activity of microorganism.

Sanitation

Definition and Standard for Removing Microorganism:

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

Sterilization

Definition and Standard for Removing Microorganism:

A process intended to kill or remove all types of microorganism, including spores, and usually including viruses with an acceptable low probability of survival.

Pasteurization

Definition and Standard for Removing Microorganism:

A process that kill non-sporulating microorganism by hot water or steam at 65-100c.

65-100 degrees Celsius

What is the temperature needed in pasteurization?

• Chemical type of the compound

• Biological property

• Therapeutic indication

What are the Classification of Anti-infectives?

Antiseptics

Local Anti-Infectives:

Applied to living tissue.
Must have low toxicity to be used directly on skin or wounds.

• Bactericidal

• Bacteriostatic

Cidal

Compound that kills bacteria.

Static

Prevents the growth of bacteria.

Disinfectant

Local Anti-Infectives:

Applied to inanimate objects.
Exerts a rapidly lethal action against all potentially pathogenic microorganism and spored.

Coagulation and denaturation of cell protein

What is the mechanism of action of local anti-infectives?

• Antiseptics

• Disinfectant

What are the two (2) local anti-infectives?

• Formalin

• Phenol > Alcohol

Local Anti-Infectives Mechanism of Action:

What are some examples of strong coagulators?

• Iodine

• Cresol

• Phenol

Local Anti-Infectives Mechanism of Action:

What are some examples of denaturants?

Low-enough toxicity

Ideal Anti-Infective:

The ideal level of toxicity for it to be used directly on skin or wounds.

Lethal action

Ideal Anti-Infective:

Exert a rapid and sustained?

Low surface tension

Ideal Anti-Infective:

Ideal surface tension so that it will spread easily into the wound.

Body fluids (pus)

Ideal Anti-Infective:

Retain activity in the presence of?

• Non-irritating

• Non-allergenic

Ideal Anti-Infective:

Characteristics needed for tissues.

Systemic toxicity

Ideal Anti-Infective:

This should lack?

Healing

Ideal Anti-Infective:

This shouldn’t interfere with?

• Alcohol and related compounds

• Phenol and derivatives

• Oxidizing agents

• Halogen containing compounds

• Cationic surfactants

What are the five (5) Classification of Anti-Infective Agents?

Alcohol

Classification of Anti-Infective Agents:

The activity of _______ against microorganisms is the result of their ability to denaturate important proteins and carbohydrates.

Denature

The activity of alcohols against microorganisms is the result of their ability to _______ important proteins and carbohydrates.

• Ethyl alcohol

• Isopropyl alcohol

What are the two (2) most commonly used antiseptics and disinfectants?

Protein and carbohydrate precipitation

What is the mechanism of action of alcohol?

8-carbon atom (octanol)

Structure-Activity Relationship: Alcohol

What is the molecular weight carbon atom of alcohol?

Antibacterial potency increases

Structure-Activity Relationship: Alcohol

MW up to 8-carbon atom (octanol).

Increase penetration to membrane

Structure-Activity Relationship: Alcohol

As the primary chain length increases.

Decreases antibacterial potency

Structure-Activity Relationship: Alcohol

Branching of the alcohol chain.

Primary > Secondary > Tertiary

Structure-Activity Relationship: Alcohol

Isomeric alcohols’ potencies decreases in the order of?

• Ethanol

• Rectified spirit

• Wine spirit

• Grain alcohol

• Spiritus vini rectificatus

What are the five (5) synonyms of ethyl acohol?

95%

What is the % of ethyl alcohol in commercial ethanol?

Azeotrope

Commercial Ethanol (95% EtOH):

This concentration forms an ______ with water that distills at 78.2c

78.2 degrees Celsius

Azeotrope forms with water that distills at temperature?

Grain Fermentation

Method of Preparation: Ethyl alcohol

Synthetically prepared by the sulfuric acid-catalyzed hydration of ethene.

Sulfuric acid-catalyzed hydration of ethene

Grain Fermentation is synthetically prepared by the?

Acetaldehyde

Alcohol is metabolized in the human body by a series of oxidations:

• Nausea, vomiting, and vasodilatory flushing.

Disulfiram (Antabuse)

Alcohol is metabolized in the human body by a series of oxidations:

• Block aldehyde dehydrogenase, allowing acetaldehyde to accumulate.

Antabuse

Disulfiram is also known as?

Ethanol

This is ineffective against spores.

Spores

Ethanol is ineffective against?

• Solvent

• Fuel

• CNS depressant

• Antipyretic

• Germicidal

• Disinfectant

What are the six (6) common uses of ethanol?

25%

What is the % of ethyl alcohol as antipyretic?

60-90%

What is the % of ethyl alcohol as germicidal?

70%

What is the % of ethyl alcohol as disinfectant?

1. Nerves

2. Ganglia

Medicinal Uses: Ethyl alcohol

Injected near (1)___ and (2)___ to alleviate pain.

Narcotic potency

Medicinal Uses: Ethyl alcohol

Ethyl alcohol has low?

• Mild sedative

• A weak vasodilator

• Carminative

What are the internal uses of ethyl alcohol (diluted form)?

Spirits

Pharmaceutical Uses: Ethyl alcohol

Ethanol as the sole solvent.

Tinctures

Pharmaceutical Uses: Ethyl alcohol

Hydroalcoholic mixtures.

Fluid extracts

Pharmaceutical Uses: Ethyl alcohol

Alcohol as cosolvent.

Denatured Alcohol

This kind of alcohol is:

• Intoxicating beverages

• Unfit for human use

• In alc lamps

• Wood alcohol

• Acetone

• Benzene

What are the three (3) denaturants?

Denatured Alcohol

This alcohol is completely denatured with wood alcohol and benzene.

Wood alcohol and Benzene

Denatured Alcohol is completely denatured with?

Methanol

Wood alcohol is also known as?

Rubbing Alcohol

(CH₃CHOHCH₃) — 2 propanol

What alcohol is this?

• Astringent

• Rubefacient

• Mild local anesthetic

What are the uses of Rubbing Alcohol?

68-72%

Rubbing alcohol contains how many % of isopropyl alcohol?

Sulfuric Acid

Preparation of Rubbing Alcohol:

This acid is catalyzed by hydration of propylene.

Isopropyl Alcohol

This alcohol is a disinfectant for the skin and surgical instruments.

Skin and surgical instruments

Isopropyl Alcohol is a disinfectant for the?

50-95%

What is the % of bactericidal property of Isopropyl Alcohol?

60% Ethyl Alcohol

40% Isopropyl Alcohol equals to?

Azeotropic Isopropyl Alcohol

This alcohol is used on gauze pads for sterilization of the skin prior to hypodermic injections.

Dehydrated Alcohol

This is an absolute alcohol.

99% ethanol

Dehydrated alcohol must contain no less than how much (%) ethanol?

Diluted Alcohol

Mixture of alcohol and water containing 41-42% by weight.

41-42%

Diluted alcohol is a mixture of alcohol and water containing % by weight.

• Ethyl alcohol

• Denatured alcohol

• Rubbing alcohol

• Isopropyl alcohol

• Azeotropic Isopropyl alcohol

• Dehydrated alcohol

• Diluted alcohol

What are the seven (7) Types of Alcohol?

Mnemonics: Every Drunk Racoon in Antarctica Dies Daily

Glycerin (Glycerol)

The first polyhydric alcohol which can yield both an aldose and a ketose.

• 1,2,3-propanetriol

Aldose and Ketose

Glycerin (Glycerol) is the first polyhydric alcohol which can yield both?

1,2,3-propanetriol

What is the chemical name of Glycerin (Glycerol)?

Solvent and Humectant

What are the uses of Glycerin (Glycerol)?

Ethylene Oxide (C₂H₄₀)

A gas sterilant and used for temperature sensitive medical equipment.

3-80%

Ethylene Oxide (C₂H₄₀) forms an explosive mixtures in air conditions ranging from (%)?

Carboxide

This contains 10% ethylene oxide and 90% carbon dioxide by volume; without danger of explosion.

• 10% ethylene oxide

• 90% carbon dioxide

Carboxide contains these two (2) sterilant gas mixture?

Germicidal

What is the mechanism of action of Carboxide?