Drug Nomenclature and Discovery
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Drug Nomenclature and Discovery

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Questions and Answers

What is the main purpose of generic drug names?

  • To identify the chemical structure of the drug
  • To provide easy branding for pharmaceutical companies
  • To comply with regulatory standards
  • To discuss the functionalities of the drug (correct)

    • Which of the following suffixes typically indicates an antiviral drug in its generic name?

  • -avir (correct)
  • -cillin
  • -statin
  • -mab

    • Which name is primarily used for regulatory purposes and is often lengthy?

  • Trade name
  • Chemical name (correct)
  • Generic name
  • Brand name

    • What distinguishes biopharmaceuticals from biologics?

    <p>Biopharmaceuticals include modern design techniques</p> Signup and view all the answers

    Which process is key in discovering suitable chemical candidates for drugs?

    <p>Bioassays screening</p> Signup and view all the answers

    What aspect is primarily involved in medicinal chemistry?

    <p>Optimizing existing chemical products</p> Signup and view all the answers

    Which of the following statements is true regarding brand names of drugs?

    <p>Brand names depend on the manufacturer</p> Signup and view all the answers

    What is one method to optimize a chemical product in medicinal chemistry?

    <p>Adding a functional group</p> Signup and view all the answers

    What is the role of carbidopa in relation to levodopa?

    <p>It prevents the conversion of levodopa to dopamine outside the brain.</p> Signup and view all the answers

    How does aspirin reduce the toxicity of salicylic acid?

    <p>By converting it into an ester.</p> Signup and view all the answers

    What is one reason dopamine cannot be administered directly into the body?

    <p>It will be decomposed by biological mechanisms.</p> Signup and view all the answers

    What structural feature of azathioprine aids in its effectiveness?

    <p>An electron-withdrawing -NO2 group.</p> Signup and view all the answers

    What is the purpose of high-throughput screening in medicinal chemistry?

    <p>To favor computational analysis over traditional methods.</p> Signup and view all the answers

    In molecular mechanics, which two aspects do computers model during virtual screening?

    <p>Ligands and receptors.</p> Signup and view all the answers

    What characterizes a 'native conformation' of a molecule?

    <p>It reflects the conformation usually observed in real-time situations.</p> Signup and view all the answers

    What does CADD stand for in the context of medicinal chemistry?

    <p>Computer-Aided Drug Design.</p> Signup and view all the answers

    What is the primary focus of drug discovery?

    <p>To find a target for drug intervention to resolve a problem</p> Signup and view all the answers

    Which technique measures binding interactions by detecting changes in heat generation?

    <p>Isothermal titration calorimetry</p> Signup and view all the answers

    Why does the binding of two molecules in ITC generate less heat?

    <p>The bound state stabilizes the molecules, leading to less energy release</p> Signup and view all the answers

    What does stereospecific reaction depend on?

    <p>The conformation of the reactant</p> Signup and view all the answers

    How is target specificity and selectivity important in drug development?

    <p>It restricts drug action to a specific receptor/enzyme type</p> Signup and view all the answers

    What is a characteristic of surface plasmon resonance (SPR) in drug testing?

    <p>The signal increase is proportional to the candidate and ligand concentration</p> Signup and view all the answers

    What can be inferred about stereoselectivity?

    <p>It shows a preference towards a specific candidate among similar options</p> Signup and view all the answers

    What is one drawback of using agonists in drug therapy?

    <p>Agonists increase the likelihood of undesirable side effects</p> Signup and view all the answers

    What is the primary focus of molecular docking in drug design?

    <p>To determine the binding interaction between a drug molecule and its target protein</p> Signup and view all the answers

    Which approach aims to improve the drug-receptor interaction by analyzing functional groups?

    <p>Structure-Activity Relationship</p> Signup and view all the answers

    What does QSAR aim to quantify regarding a drug?

    <p>The relationship between physical properties and biological activity</p> Signup and view all the answers

    What is one common side effect of drugs that lack selectivity?

    <p>Unintended binding to non-target receptors</p> Signup and view all the answers

    What is the estimated success rate of drug discovery in pharmaceutical research?

    <p>50%</p> Signup and view all the answers

    How has penicillin production improved over the years?

    <p>Through advancements in X-rays and filtration techniques</p> Signup and view all the answers

    Which condition is mentioned as an example of drug discovery efforts?

    <p>Parkinson's disease</p> Signup and view all the answers

    What challenge is associated with creating a drug for Parkinson's disease?

    <p>Dopamine also affects other systems outside of the brain</p> Signup and view all the answers

    Why do amides still participate in hydrogen bonding despite being able to prevent amines' nitrogen from forming hydrogen bonds?

    <p>Amides can form hydrogen bonds through either their hydrogen or oxygen.</p> Signup and view all the answers

    What impact does the deprotonation of carboxylic acid have on its ability to form hydrogen bonds?

    <p>It prevents it from becoming a hydrogen bond donor.</p> Signup and view all the answers

    What is the primary reason aryl halides do not react directly with alkyl amines under standard conditions?

    <p>The aromatic system stabilizes the carbon-halogen bond.</p> Signup and view all the answers

    Which feature of aryl halides contributes to their lower reactivity compared to alkyl halides?

    <p>Aryl halides have poor leaving groups in aromatic systems.</p> Signup and view all the answers

    What type of conformational aspect does an alkene exhibit, and how does this affect its rigidity?

    <p>Alkenes are rigid and cannot be rotated easily.</p> Signup and view all the answers

    Why are alkyl halides known to have a strong affinity with nucleophilic groups?

    <p>Alkyl halides can easily lose their halide group.</p> Signup and view all the answers

    In terms of SN2 reactions, what aspect of the planar aromatic ring affects the reactivity of aryl halides?

    <p>The ring prevents backside attack due to its planar geometry.</p> Signup and view all the answers

    How does rigidity play a role in the binding of a molecule to receptors?

    <p>Rigidity can help lock a molecule into the required conformation for ideal binding.</p> Signup and view all the answers

    Study Notes

    Drug Nomenclature

    • Generic names don't have capitalized letters and are used to discuss the functionality of a drug.
    • Brand names have their first letters capitalized and don't reveal much about the drug.
    • Three main names for drugs: Chemical name (IUPAC), generic name, and trade name.
    • Chemical names are complex and mainly used for regulations.

    Drug Discovery

    • Generic names are used for advertising drugs.
    • Brand names depend on the company selling the drugs.
    • Biologics involve extracting natural biological sources for drug repurposing.
    • Biopharmaceuticals use modern biotechnological and computational techniques for modifying existing pharmaceuticals.
    • Early drug development is based on the observation of natural products.
    • Medicinal chemistry focuses on optimizing existing chemical products, such as enhancing a molecule's affinity to its target.

    Drug Design and Optimization

    • Bioassays are used to screen the activity of various chemicals against a predetermined target.
    • Drug design can be done on targets obtained from tissues or genes extracted from patients.
    • Molecular docking is a computational technique that predicts how drugs bind to specific sites on target proteins.
    • Optimization of drugs aims to increase selectivity and effectiveness.
    • Structure-Activity Relationship (SAR) studies how a drug's functional groups interact with target receptors.
    • Quantitative Structure-Activity Relationship (QSAR) quantifies the physical properties of a drug and their impact on its biological activity.

    Drug Discovery Techniques

    • Drug discovery is a challenging process, with a success rate estimated at 50%.
    • Nuclear Magnetic Resonance (NMR) bioassays compare regular protein signals with signals after the addition of a potential drug candidate.
    • Surface Plasmon Resonance (SPR) measures binding events by detecting changes in light reflection at a metal surface.
    • Isothermal Titration Calorimetry (ITC) measures the heat changes that occur when molecules bind, providing information about binding affinity.
    • Stereospecific reactions occur when the product of a chemical reaction depends on the specific conformation of the reactant.
    • Stereoselectivity describes a compound's preference for reacting with certain candidates.
    • Target specificity and selectivity ensure a drug only targets a specific receptor or enzyme in a specific area of the body.

    Agonists and Antagonists

    • Agonists are drugs that mimic the action of natural compounds.
    • Antagonists block the action of natural compounds.
    • A pitfall of agonists is that changing the molecule's conformation can change its binding outcome.
    • Amide-analogue alkenes are similar to regular alkenes and cannot be rotated.

    Drug Metabolism and Modifications

    • Deprotonation of carboxylic acid prevents it from being a hydrogen bond donor.
    • Ester hydrolysis in vivo can be different from in vitro.
    • Alkyl halides have a strong affinity for nucleophilic groups.
    • Aryl halides typically don't react directly with alkyl amines under standard conditions.
    • Azathioprine prolongs its interaction with glutathione by creating an electron-deficit area.
    • Valium prolongs its activity by having a hydrophobic methyl group instead of a hydrogen atom.
    • Aspirin masks salicylic acid's toxic phenolic group by turning it into an ester.
    • Carbidopa acts as a sentry drug, inhibiting the conversion of levodopa to dopamine outside the brain, but not in the brain.
    • Dopamine cannot be administered directly because it is quickly deactivated and metabolized in the body.

    Computational Medicinal Chemistry

    • Molecular mechanics uses computational analysis to study drugs.
    • High-throughput screening has favoured computational analysis over bioassays.
    • Computational Drug Design (CADD) models the structure, energy, and binding of ligands and receptors.
    • Native conformation refers to the conformation of a molecule in its natural environment, typically aqueous.
    • Native conformations are considered stable.

    Studying Drug Molecules

    • Space-filling representation model shows the space occupied by each atom in a molecule.
    • The computer models two key aspects: ligand and receptors.
    • Energy calculation is done through modelling.

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    PHM2006 Medicinal Chemistry for Pharmaceutical Professionals PDF

    Description

    Explore the intricacies of drug nomenclature, including the differences between generic names, brand names, and chemical names. This quiz covers foundational concepts in drug discovery and design, focusing on biologics, biopharmaceuticals, and medicinal chemistry. Test your knowledge of how these elements influence the pharmaceutical landscape.

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