Pharmaceutical Formulations Quiz

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Questions and Answers

What is the main purpose of adding water to benzoyl peroxide in its formulation?

  • To improve its acne treatment efficacy
  • To make it safer to handle (correct)
  • To enhance its explosive properties
  • To increase its keratolytic effects

What type of compounds are iodophors classified as?

  • Oxidants with no germicidal activity
  • Bactericidal and fungicidal complexes (correct)
  • Nonionic surfactants
  • Volatile organic compounds

How does iodine act as a germicide?

  • By destabilizing nucleic acids
  • By increasing protein synthesis
  • By iodination and oxidation of proteins (correct)
  • By increasing cellular metabolism

Why are surfactants mixed with iodine in iodophor formulations?

<p>To retain germicidal properties while reducing irritancy (C)</p> Signup and view all the answers

What property of Povidone-iodine contributes to its effectiveness?

<p>Stable charge-transfer complex formation (B)</p> Signup and view all the answers

What concentration of water is used in the formulation of benzoyl peroxide to ensure safety?

<p>30% (A)</p> Signup and view all the answers

What is the function of iodide salts in iodophors?

<p>To increase the solubility of iodine (B)</p> Signup and view all the answers

At which concentrations is benzoyl peroxide classified as keratolytic and keratogenic?

<p>5% and 10% (C)</p> Signup and view all the answers

What is the primary medicinal use of alcohol?

<p>As an antiseptic (A)</p> Signup and view all the answers

What is the boiling point of the azeotrope formed by commercial ethanol and water?

<p>78.2°C (B)</p> Signup and view all the answers

Which substance is NOT commonly added to denatured alcohol?

<p>Ethyl alcohol (B)</p> Signup and view all the answers

Which process is one way ethanol can be synthesized?

<p>Sulfuric-acid–catalyzed hydration of ethylene (A)</p> Signup and view all the answers

What is the proof of alcohol that qualifies it as ethyl alcohol?

<p>At least 160 proof (D)</p> Signup and view all the answers

What effect does rubbing alcohol have when applied to the skin?

<p>It produces an evaporative cooling effect (B)</p> Signup and view all the answers

What type of alcohol is specially denatured alcohol treated with to allow for specific uses?

<p>Various substances including iodine (D)</p> Signup and view all the answers

Which of the following statements about alcohol is true?

<p>Alcohol refers to ethyl alcohol regardless of its source or process (D)</p> Signup and view all the answers

What is the primary mechanism by which organomercurial compounds exert their antibacterial action?

<p>Interacting with sulfhydryl groups in proteins (C)</p> Signup and view all the answers

Which of the following statements is true regarding the antibacterial efficacy of organomercurials?

<p>They exhibit reduced activity in the presence of serum proteins. (B)</p> Signup and view all the answers

What characteristic of Nitromersol distinguishes it as an antiseptic?

<p>It is nonirritating and nonstaining. (D)</p> Signup and view all the answers

What is a major disadvantage of using mercurials as antiseptics?

<p>They are potentially toxic and less effective than other agents. (D)</p> Signup and view all the answers

Which of the following best describes Thimerosal's antiseptic properties?

<p>It is a weakly bacteriostatic antiseptic. (D)</p> Signup and view all the answers

Why are preservatives necessary in parenteral and ophthalmic preparations?

<p>To prevent microbial contamination during use. (D)</p> Signup and view all the answers

Which statement best reflects the current use of Nitromersol?

<p>It has been largely replaced by superior agents. (B)</p> Signup and view all the answers

How do thiol-containing compounds affect organomercurials?

<p>They can reverse the reaction with organomercurials. (A)</p> Signup and view all the answers

What is the primary role of acetaldehyde in alcohol metabolism?

<p>It causes nausea and vomiting when accumulated. (D)</p> Signup and view all the answers

Which form of alcohol is primarily used as a chemical reagent or solvent?

<p>Dehydrated ethanol (A)</p> Signup and view all the answers

What distinguishes spirits from tinctures in pharmaceutical use?

<p>Spirits use ethanol as the sole solvent, while tinctures are hydro-alcoholic. (C)</p> Signup and view all the answers

Why is absolute alcohol not suitable for ingestion?

<p>Residual benzene from its preparation cannot be removed. (B)</p> Signup and view all the answers

Which of the following statements about isopropyl alcohol is correct?

<p>It is a colorless liquid with a characteristic odor and bitter taste. (B)</p> Signup and view all the answers

What is the primary purpose of disulfiram in relation to alcohol metabolism?

<p>To block aldehyde dehydrogenase and increase acetaldehyde. (D)</p> Signup and view all the answers

What compound is primarily produced during the oxidation of ethanol?

<p>Ethanoic acid (C)</p> Signup and view all the answers

What is the method used to prepare dehydrated ethanol commercially?

<p>Azeotropic distillation of an ethanol-benzene mixture. (C)</p> Signup and view all the answers

What sensation does hexylresorcinol produce when applied to the tongue?

<p>Numbness (A)</p> Signup and view all the answers

What is the main reason hexylresorcinol is included in throat lozenges?

<p>For local anesthetic and antiseptic properties (B)</p> Signup and view all the answers

Which of the following oxidizing agents is specifically mentioned for generating oxygen in tissues?

<p>Hydrogen peroxide (D)</p> Signup and view all the answers

What type of bacteria are oxidizing agents especially effective against?

<p>Anaerobic bacteria (D)</p> Signup and view all the answers

What is one limitation of oxidizing agents as germicidal agents?

<p>Transient action (B)</p> Signup and view all the answers

What is the primary use of carbamide peroxide?

<p>As an antiseptic and disinfectant (B)</p> Signup and view all the answers

What is released when carbamide peroxide is mixed with water?

<p>Hydrogen peroxide (D)</p> Signup and view all the answers

What property of oxidizing agents makes them useful in cleansing contaminated wounds?

<p>The bubbles formed during oxygen liberation (C)</p> Signup and view all the answers

What is the primary use of chlorobutanol in pharmaceuticals?

<p>As a bacteriostatic agent for injections (C)</p> Signup and view all the answers

Which of the following compounds is known for its local anesthetic action?

<p>Benzyl alcohol (A)</p> Signup and view all the answers

What factor significantly affects the effectiveness of benzoic acid as a preservative?

<p>pH of the solution (A)</p> Signup and view all the answers

Sodium propionate is most effective as a preservative at which pH level?

<p>Low pH (C)</p> Signup and view all the answers

Which compound is primarily used in perfumery and occurs naturally in rose oil?

<p>Phenylethyl Alcohol (D)</p> Signup and view all the answers

What characteristic of sodium benzoate allows it to function as a preservative in acidic preparations?

<p>It releases benzoic acid in acidic conditions (B)</p> Signup and view all the answers

Which compound is mentioned as an effective antifungal preservative specifically for syrups and elixirs?

<p>Sorbic acid (C)</p> Signup and view all the answers

Potassium sorbate is used for what purpose in comparison to sorbic acid?

<p>When greater water solubility is required (B)</p> Signup and view all the answers

Flashcards

Commercial Ethanol

Ethanol with a concentration of approximately 95% by volume, forming an azeotrope with water, which means it boils at a constant temperature (78.2°C).

Fermentation

A process where yeast converts sugars into ethanol and carbon dioxide.

Sulfuric Acid-Catalyzed Hydration of Ethylene

A chemical reaction where ethylene (a gas) reacts with water in the presence of sulfuric acid to produce ethanol.

Denatured Alcohol

Ethanol that has been modified to make it undrinkable by adding other substances.

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Completely Denatured Alcohol

Denatured alcohol that contains methanol and benzene, making it unsuitable for any use, even externally.

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Specially Denatured Alcohol

Denatured alcohol mixed with specific substances for specific purposes (e.g., tinctures, mouthwashes, plant extracts).

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Medicinal Use of Alcohol

Using alcohol externally to clean wounds, preserve substances, reduce irritation, or dissolve other substances.

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Anesthetic Effect of Alcohol

Alcohol's ability to numb the skin due to its cooling effect as it evaporates.

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Alcohol Metabolism

The process by which the human body breaks down ethanol (alcohol) into harmless substances. This involves a series of oxidation reactions, starting with ethanol and progressing through acetaldehyde to ethanoic acid.

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Acetaldehyde

A toxic by-product created during alcohol metabolism. It's responsible for symptoms like nausea, vomiting, and facial flushing.

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Disulfiram (Antabuse)

A drug used to treat alcohol dependence. It blocks the breakdown of acetaldehyde, making drinkers experience the unpleasant effects of this toxic compound, acting as a deterrent.

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Spirits (In Pharmacy)

A type of pharmaceutical preparation where ethanol is the primary solvent. Examples include tinctures and fluid extracts.

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Dehydrated Ethanol (Absolute Ethanol)

Ethanol with a purity level of at least 99% w/w. It's primarily used as a chemical reagent and solvent, not for drinking.

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Isopropyl Alcohol (2-propanol)

A colorless liquid with a characteristic odor, often used as a disinfectant for skin and surgical instruments. It's a suitable substitute for ethanol in many cases, but never for ingestion.

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Sulfuric-Acid-Catalyzed Hydration of Propylene

A process used commercially to produce isopropyl alcohol. It involves the reaction of propylene with water in the presence of sulfuric acid.

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Isopropanol

A colorless, volatile liquid with a slightly bitter taste. It is commonly used as an antiseptic and solvent in many pharmaceutical and household products.

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What is Hexylresorcinol?

Hexylresorcinol, also known as 4-Hexylresorcinol is a compound that numbs the tongue when applied. It is an effective antiseptic with both bactericidal and fungicidal properties.

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How do oxidizing agents work as germicides?

Oxidizing agents that kill microorganisms usually work by liberating oxygen in the tissues. Examples include hydrogen peroxide, metal peroxides, and sodium perborate.

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What is Carbamide Peroxide?

Carbamide peroxide is a stable complex of hydrogen peroxide and urea used for both antiseptic and disinfectant purposes.

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What are the uses of Carbamide Peroxide?

It's effectively used for treating oral ulcers and dental care because it releases oxygen bubbles that remove debris.

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What is Hydrous Benzoyl Peroxide?

Hydrous benzoyl peroxide is commonly found in acne treatments. It is a white powdery substance that oxidizes and breaks down acne-causing bacteria.

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What types of bacteria are Oxidizing Agents effective against?

Oxidizing agents can be particularly effective against anaerobic bacteria, which cannot survive with oxygen. They also cleanse wounds by dislodging debris with their oxygen bubbles.

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What are the limitations of oxidizing agents?

The use of oxidizing agents is limited because they may have poor penetration into infected tissues and their action can be short-lived.

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What is KMnO4?

KMnO4 is a powerful oxidizing agent that can denature proteins in microorganisms by directly reacting with them.

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Antibacterial Action

The ability of a substance to kill or inhibit the growth of microorganisms, especially bacteria.

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Lipid Solubility and Organomercurials

Organomercurials, a type of mercury-containing compound used as antiseptics, can penetrate microorganisms and tissues due to their increased lipid solubility.

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Organomercurial Mechanism

Organomercurials form covalent bonds with sulfhydryl (-SH) groups in enzymes and proteins, disrupting their function. This leads to bacteriostatic effects, meaning they inhibit bacterial growth but don't kill them.

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Reversibility of Organomercurial Action

Treatment with thiol-containing compounds like cysteine or dimercaprol (BAL) can reverse the effects of organomercurials by breaking their bonds with sulfhydryl groups.

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Serum Inactivation of Organomercurials

Proteins in serum can inactivate organomercurial antiseptics, reducing their efficacy.

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Ineffectiveness Against Spores

Organomercurials are not very effective against bacterial spores, dormant forms of bacteria with a protective outer layer.

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Disadvantages of Organomercurials

Organomercurial antiseptics have disadvantages, including potential toxicity, limited effectiveness, and the availability of safer alternatives.

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Nitromersol

A non-irritating and non-staining antiseptic used for skin and ocular infections but largely replaced by more effective agents.

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Iodine

A compound with powerful germicidal properties. It is effective against a wide range of bacteria and fungi, and is commonly used as a disinfectant.

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Iodophors

Complexes formed by mixing iodine with nonionic or cationic surfactants. They retain iodine's germicidal power but decrease its volatility and irritation.

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Povidone-Iodine

A specific iodophor where iodine is complexed with polyvinylpyrrolidone (PVP), a nonionic surfactant. It is water-soluble and releases iodine slowly, providing sustained antimicrobial activity.

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Iodine's Mechanism of Action

A powerful oxidizing agent that inactivates proteins by iodination of aromatic residues (phenylalanyl and tyrosyl) and oxidation of sulfhydryl groups.

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Benzoyl Peroxide

A substance used in the treatment of acne. It works by reducing excess oil production, killing bacteria, and promoting skin cell turnover.

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Keratolytic Effect of Benzoyl Peroxide

A property of benzoyl peroxide that encourages the shedding of dead skin cells, promoting a clearer complexion. However, it can cause dryness and flaking.

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Keratogenic Effect of Benzoyl Peroxide

Benzoyl peroxide's potential to increase the growth of new skin cells, sometimes causing irritation or temporary worsening of acne, especially at higher concentrations.

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Benzoyl Peroxide's Explosive Nature

The pure form of benzoyl peroxide is highly explosive. It's diluted with water to create a safer, stable product for topical application.

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Chlorobutanol

Chlorobutanol is an effective bacteriostatic agent commonly used in pharmaceutical products for injection, ophthalmic use, and intranasal administration.

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Benzyl Alcohol

Benzyl alcohol is a preservative frequently included in vials of injectable medications. It's often present in concentrations between 1% and 4%, dissolved in water or saline solution.

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Benzoic Acid (Preservative)

Benzoic acid is an antiseptic agent employed in lotions, ointments, and mouthwashes. It is particularly effective at low pH, often used as a preservative in pharmaceuticals and food items.

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Sodium Benzoate

Sodium benzoate is used as a preservative in acidic liquid formulations. In these preparations, benzoic acid is released, enhancing its effectiveness as a preservative.

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Sodium Propionate

Sodium propionate is a potent anti-fungal preservative. It's most effective in acidic conditions, effectively preventing the growth of mold and fungi.

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Sorbic Acid

Sorbic acid is a widely used antifungal preservative. It is commonly employed in syrups, elixirs, ointments, and lotions, particularly those containing components that encourage mold growth, such as sugars.

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Potassium Sorbate

Similar to sorbic acid, potassium sorbate is used as a preservative when greater water solubility is needed. Both compounds act on the same principle but differ in their solubility characteristics.

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Phenylmercuric Nitrate

Phenylmercuric nitrate is a highly effective preservative and antiseptic agent. It works by inhibiting the growth of microorganisms.

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Study Notes

Local Anti-infectives and Preservatives

  • Local anti-infectives and preservatives are used to prevent bacterial infections.
  • Joseph Lister introduced antiseptic principles using phenol in surgery in 1867.
  • Paul Ehrlich aimed to develop less toxic antimicrobial compounds in 1881.
  • Ehrlich’s discovery of compound 606 (Salvarsan/Arsphenamine) was a breakthrough in treating previously untreatable syphilis.
  • Local antimicrobial properties of phenol and iodine were known before Ehrlich's work.

Antiseptics and Disinfectants

  • Antiseptics kill or prevent growth of microorganisms on living tissue.
  • Disinfectants kill microorganisms on inanimate surfaces (objects).
  • Alcohol is a useful antiseptic.
    • Antimicrobial potency increases with increasing length of carbon chain in primary alcohols up to octanol.
    • Branching of the alcohol chain decreases antimicrobial potency.
    • Isopropyl alcohol is slightly more active than ethyl alcohol against vegetative bacterial growth.
    • Alcohols denature important proteins and carbohydrates.
    • Ethanol is a clear, colorless, volatile liquid with a pleasant odor.
  • Denatured alcohol is ethanol treated with other substances to make it unsuitable for consumption.
    • Completely denatured alcohol contains added wood alcohol and benzene.
  • Isopropyl alcohol, a colorless, volatile liquid is used as a disinfectant.

Other Local Anti-infectives and Preservatives

  • Formaldehyde solution, commonly known as formalin is used as a disinfectant with the ability to inactivate harmful microorganisms rapidly.
  • Formaldehyde (HCHO) leads to the formation of formic acid and paraformaldehyde.
  • It is also used as a disinfectant for water supplies and in surgical instruments.
  • Phenol has an unpleasant odor, but is a powerful antiseptic and disinfectant.
  • Cresol forms a yellow to brownish yellow liquid, which is obtained from coal tar and petroleum. It is an inexpensive antiseptic and disinfectant.
  • Chlorine-releasing compounds are used to disinfect water supplies.
  • Iodophors are used as a water disinfectant and a general antiseptic.
  • Quaternary ammonium compounds are cationic surfactants with antimicrobial activity against many kinds of bacteria.

Preservatives

  • Used in preparations to prevent microbial contamination.
  • Ideal preservatives are effective at low concentrations, non-toxic, compatible with other components, and stable.
  • p-Hydroxybenzoic acid derivatives (parabens) are a common class.
  • Methylparaben, propylparaben, and butylparaben are used to inhibit mold growth, yeast growth, or both.
  • Chlorobutanol is used as a bacteriostatic agent.
  • Benzyl alcohol is commonly used in injectable drugs.
  • Phenylmercuric nitrate is an ingredient in various medical products.

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