IPS1 -Medicinal Chemistry - Anti-nfectives

Proverbs 16:3

Joseph Lister

He introduced sterile surgery

Joseph Lister

He used PHENOL or CARBOLIC ACID as antiseptics for use in surgery and post traumetic infections or ward fever

Paul Ehrlich

He established the concepts of selective toxicity

selective toxicity

Paul Ehrlich established the concepts of _____

Paul Ehrlich

He worked on antibacterial dyes, organo-arsenicals (treatment for syphilis) and the so called "magic bullets"

syphilis

Organo-arsenicals is a treatment for  _____ ? 

Anti-infectives

____- are substances that destroys or kill microorganisms that causes infection

Germicides

____- are compounds that is used “locally to kill microorganisms” aka "local anti-infective agents"

local anti-infective agents

Germicides is also known as  ____ ? 

Antiseptic

[Antiseptic or Disinfectant]

_____ - used in living things

Disinfectant

[Antiseptic or Disinfectant]

_____ - used in non living things

Phenol coefficient

______- is the ratio of a dilution of a given test disinfectant to the dilution of phenol required to kill a given strain of Salmonella typhi

D. Salmonella typhi

Phenol coefficient: is the ratio of a dilution of a given test disinfectant to the

dilution of phenol required to kill a given strain of __________.

A. Pseudomonas aeruginosa

B. Mycobacterium leprae

C. Bacillus subtilis

D. Salmonella typhi

1. primary

2. secondary

3. tertiary

Ranking of Alcohol Effectiveness [most to least effective]

8th carbon only

The antibacterial property of alcohol increases with increasing molecular weight until the _____ carbon only

True

[True or False]

In ALCOHOL; Octanol and above are more solid

decreases

In ALCOHOL  

• Branching ____ [increases/decreases]  solubility

more

In ALCOHOL 

• Straight is ____[more / less] effective than branched

Staphylococcus aureus

______- is the test organism for antibacterial property of alcohol

Ethanol

 Alcohol in pharmacy will always pertain to_____

• Alcohol (95%)

• Ethyl alcohol

• Wine spirit

Ethanol is also known as ____ [3]

Ethanol (Alcohol 95%)

_____- is a clear, colorless, volatile liquid with burning taste and a characteristic odor

Absolute alcohol

99% alcohol is known as ____ ?

azeotropic distillation

Absolute alcohol is prepared by ______ ?

Acetaldehyde

____- is responsible for the side effect of alcohol hangover

Alcohol → (alcohol dehydrogenase) → Acetaldehyde → (aldehyde dehydrogenase) → Acetate

Metabolism of alcohol

Denatured alcohol

[TYPE OF ALCOHOL]

_____- ethanol that has been rendered unfit for use in intoxicating beverages by the addition of other substances

Completely Denatured Alcohol

[TYPE OF ALCOHOL]

_____-  a denatured alcohol that contains methanol and benzene that is unsuitable for external and internal use

Dehydrated Ethanol

[TYPE OF ALCOHOL]

Absolute ethanol is also known as ___ ?

99% w/w

[TYPE OF ALCOHOL]

Dehydrated Ethanol contains NLT  _____ % w/w

• 2-propanol

• propan-2-ol

Isopropyl alcohol is also known as ___ [2]

Isopropyl alcohol

[TYPE OF ALCOHOL]

____- have a slight bitter taste and contains 91% v/v of isopropanol

Isopropyl alcohol

[TYPE OF ALCOHOL]

____- prepared by hydration of propylene with sulfuric acid as catalyst

Sulfuric acid

[Alcohol and Related Compounds]

_____- is a catalyst for hydration of propylene to form isopropyl alcohol

Azeotropic isopropyl alcohol, USP

[TYPE OF ALCOHOL]

_____- used in gauze pads

Ethylene oxide (C₂H₄O)

[Alcohol and Related Compounds]

_____- is a colorless, flammable gas, used to sterilize temperature sensitive medical equipment and certain pharmaceuticals that cannot be autoclaved.

Ethylene oxide (C₂H₄O)

[Alcohol and Related Compounds]

____- is a Non-selective alkylating agent therefore carcinogenic 

carcinogenic 

[Alcohol and Related Compounds]

Ethylene oxide (C₂H₄O) is a Non-selective alkylating agent therefore______

Ethylene oxide (C₂H₄O)

[Alcohol and Related Compounds]

_____- is the most important and simplest epoxide (cyclic: CH₂ - O - CH₂)

• Formol

• Formalin

Formaldehyde, USP is also known as ___ [2]

Formaldehyde, USP

[TYPE OF ALDEHYDE]

_____-

• Contains NLT 37% w/v of formaldehyde (HCHO) with methanol

• Miscible with water and alcohol, cloudy at room temperature

Formaldehyde, USP

[TYPE OF ALDEHYDE]

_____- is use as embalming agent, deodorant, antiseptic, gas preparations is disinfectant for rooms, clothes, and instruments

Methanol

____- is mixed with formaldehyde to retard polymerization of aldehyde to para formaldehyde to prevent ingestion

Cidex

What is the BRAND NAME of Glutaraldehyde Disinfectant Solution?

Glutarol

Glutaraldehyde Disinfectant Solution (Cidex) is also known as ____ ?

Glutaraldehyde Disinfectant Solution

[TYPE OF ALDEHYDE]

_____-  is used as sterilizing solution for equipment and instruments that cannot be autoclaved

Para position

PHENOL  substitution with alkyl, aryl, and halogen in at _____[para / meta] increases bactericidal properties

True

[TRUE or FALSE]

In PHENOL

• The presence of  of straight chain alkyl groups enhances bactericidal activity more than branched groups.

• Alkylated phenols

• Resorcinol

In PHENOL

_______ [2] are less toxic than parent compounds while retaining bactericidal properties

Joseph Lister

Phenol, USP is introduced by _____ ?

surgical alcoholic antiseptic

Phenol, USP is introduced by Joseph Lister (1867) as _______

Phenol, USP

____- is used as the standard to which most germicides are compared.

Phenol, USP

____- is a general “protoplasmic poison ( highly corrosive)

antipruritic

[Phenol and their derivatives]-

Phenolated calamine lotion is used as _____

Phenol-glycerin

[Phenol and their derivatives]

_____- used to cauterize small wounds

• Phenol solution

• Phenol glycerin

Milder phenol is also known as  ___ [2]

Liquefied phenol

[TYPE OF PHENOL]

____- phenol with 10% water

Liquefied phenol

[TYPE OF PHENOL]

____- used as pharmaceutical aid

p-chlorophenol

[TYPE OF PHENOL]

____- 

• PC of 4

• 4 times more effective than phenol

p-chlorophenol

[TYPE OF PHENOL]

____- Used in combination with camphor in liquid petrolatum

camphor

p-chlorophenol is used in combination with _____ in liquid petrolatum

p-chlorophenol

[TYPE OF PHENOL]

____- used externally as antiseptic and anti-irritant.

• PC-MX

• Metasep

p-chloro-m-xylenol BRAND NAMES are ____ [2]

p-chloro-m-xylenol

[TYPE OF PHENOL]

____- is available  as shampoo which is used for the treatment of fungal infection.

Hexachlorophene

[TYPE OF PHENOL]

____- is a bisphenolic, more potent than monophenolic, easily absorbed onto skin and even sebaceous glands

methyl phenol

[Phenol and their derivatives]

Cresol, NF is also known as ____ with Phenol coefficient (PC) of 2.5

2.5 

[Phenol and their derivatives]

Cresol, NF is also known as methyl phenol with Phenol coefficient (PC) of _____ ?

Cresol, NF

[TYPE OF PHENOL]

Yellow to brownish-yellow liquid that has a characteristic creosote odor

Cresol, NF

[TYPE OF PHENOL]

____- is obtained from coal tar or petroleum by alkaline extraction into aqueous medium, acidification and fractional distillation

coal tar or petroleum

[TYPE OF PHENOL]

CRESOL  is obtained from______ or _____  by alkaline extraction into aqueous medium, acidification and fractional distillation

• alkaline extraction into aqueous medium

• acidification

• fractional distillation 

[TYPE OF PHENOL]

CRESOL  is obtained from coal tar or petroleum by ____ [3]

• antiseptic

• disinfectant

[TYPE OF PHENOL]

CRESOL is use as ____ [2]

unpleasant odor

[TYPE OF PHENOL]

What is the disadvantage of  Cresol, NF ?

Lysol

[TYPE OF PHENOL]

____- contains saponated cresol solution

Chlorocresol

4-chloro-3-methylphenol is also known as ____ ?

Chlorocresol

[TYPE OF PHENOL]

____-

• A colorless crystal

• Used as preservative

Thymol

[TYPE OF PHENOL]
Isopropyl m-cresol is also known as _____

Thymol

[TYPE OF PHENOL]

____- is a antifungal for the treatment of Tinea capitis, Tinea corpus.

Eugenol

[TYPE OF PHENOL]

4-allyl-2methylphenol is also known as  _____ 

Resorcinol

[TYPE OF PHENOL]

m-dihyroxybenzene, resorcin is also known as ____

Hexylresorcinol

[TYPE OF PHENOL]

4-allyl-2-methylphenol is also known as ____ 

Stearoptene

[OXIDIZING AGENT]

_____- solidify upon long standing

Eleoptene

[OXIDIZING AGENT]

_____- remain liquid upon standing

• Hydrogen Peroxide (H₂O₂)

• Carbamide Peroxide Topical Solution

• Hydrous Benzoyl Peroxide

Oxidizing Agents [3]

• 10 vol: 3%

• 20 vol: 6%

• 30 vol: 9%

[OXIDIZING AGENT]

Hydrogen Peroxide Volumes [3]

Gly-Oxide

[OXIDIZING AGENT]
Carbamide Peroxide Topical Solution BRAND NAME is _____

• Oxy-5

• Oxy-10

• Vamoxide

• PanOxyl

[OXIDIZING AGENT]

Hydrous Benzoyl Peroxide BRAND NAMES are ___[4]

Hydrous Benzoyl Peroxide

[OXIDIZING AGENT]

_____-  is a white granular powder, explosive (pure) addition of 30% water to make it safer

Hydrous Benzoyl Peroxide

[OXIDIZING AGENT]

USES:  

• keratolytic, keratogenic

• treatment of acne caused by propionic bacterium acnes (an anaerobic) 

Hydrous Benzoyl Peroxide

[OXIDIZING AGENT] 

MOA: induce proliferation of epithelial cells leading to sloughing and repair

• Elemental Iodine

• Iodophors

• Povidone-Iodine

Halogen Containing Compounds - Iodine [3]

Elemental Iodine

[Halogen Containing Compounds - Iodine]

____- is the oldest and one of the most effective and useful germicide

Iodophors

[Halogen Containing Compounds - Iodine]

______- are complexes of iodine with non-ionic and cationic surfactants while retaining the germicidal property and reducing the volatility and irritant property of iodine

Lugol's solution or Strong Iodine

[Halogen Containing Compounds - Iodine]

10% Iodine + Sodium Iodide (NaI) or Potassium iodide (KI)

Lugol's solution

[Halogen Containing Compounds - Iodine]

Strong Iodine Solution is also known as ____

Iodine Solution

[Halogen Containing Compounds - Iodine]

5% Iodine + Sodium Iodide (NaI) or Potassium iodide (KI)

Iodine Tincture

[Halogen Containing Compounds - Iodine]
5% Iodine +  Sodium Iodide (NaI)

Iodine Tincture

[Halogen Containing Compounds - Iodine]
Potassium iodide (KI)+ 50% alcohol

Betadine®

[Halogen Containing Compounds - Iodine]

Povidone-Iodine BRAND NAME is ____

Povidone – Iodine

[Halogen Containing Compounds - Iodine]
____- is a Complex of iodine with Polyvinylpyrrolidone (PVP)