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What is the study of pharmaceutical chemistry that focuses on the discovery, synthesis and design of bioactive molecules?
What is the study of pharmaceutical chemistry that focuses on the discovery, synthesis and design of bioactive molecules?
Organic Medicinal
What is the study of how drugs interact with their target?
What is the study of how drugs interact with their target?
Pharmacodynamics
Which of these are examples of drug targets?
Which of these are examples of drug targets?
What type of inhibitor binds to the active site of an enzyme and competes with the endogenous substrate?
What type of inhibitor binds to the active site of an enzyme and competes with the endogenous substrate?
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What type of inhibitor forms a covalent bond to an amino acid residue within the active site of an enzyme, permanently inactivating it?
What type of inhibitor forms a covalent bond to an amino acid residue within the active site of an enzyme, permanently inactivating it?
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What type of inhibitor binds to a site distinct from the active site of an enzyme, inducing a conformational change that affects the enzyme's active site and reduces its activity?
What type of inhibitor binds to a site distinct from the active site of an enzyme, inducing a conformational change that affects the enzyme's active site and reduces its activity?
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What type of inhibitor binds to the enzyme-substrate complex, inhibiting the enzyme's activity?
What type of inhibitor binds to the enzyme-substrate complex, inhibiting the enzyme's activity?
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What is the cellular component that is responsible for mediating a drug's response?
What is the cellular component that is responsible for mediating a drug's response?
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What type of drug mimics the endogenous ligand and activates the receptor?
What type of drug mimics the endogenous ligand and activates the receptor?
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What type of drug binds to the receptor but does not activate it, preventing the endogenous ligand from binding?
What type of drug binds to the receptor but does not activate it, preventing the endogenous ligand from binding?
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What type of drug binds to the receptor but does not elicit the full response of a full agonist?
What type of drug binds to the receptor but does not elicit the full response of a full agonist?
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What type of drug binds to the receptor but has an effect opposite to that of the agonist, inhibiting the natural receptor function?
What type of drug binds to the receptor but has an effect opposite to that of the agonist, inhibiting the natural receptor function?
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Constitutional activity refers to the activity of a receptor in the presence of an endogenous ligand.
Constitutional activity refers to the activity of a receptor in the presence of an endogenous ligand.
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What is the phenomenon that occurs when a receptor is continuously exposed to an agonist and becomes less responsive to subsequent stimulation?
What is the phenomenon that occurs when a receptor is continuously exposed to an agonist and becomes less responsive to subsequent stimulation?
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What is the phenomenon that occurs when a receptor is continuously exposed to an antagonist and becomes more sensitive to subsequent agonist stimulation?
What is the phenomenon that occurs when a receptor is continuously exposed to an antagonist and becomes more sensitive to subsequent agonist stimulation?
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Tolerance is a situation where decreased doses of a drug are required to achieve the same effect over time.
Tolerance is a situation where decreased doses of a drug are required to achieve the same effect over time.
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What is the dependence on a drug, leading to withdrawal symptoms when the drug is discontinued?
What is the dependence on a drug, leading to withdrawal symptoms when the drug is discontinued?
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What is the term for the study of the journey of a drug in the body, encompassing absorption, distribution, metabolism, and excretion?
What is the term for the study of the journey of a drug in the body, encompassing absorption, distribution, metabolism, and excretion?
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What is the process of drug transfer from the site of administration to systemic circulation?
What is the process of drug transfer from the site of administration to systemic circulation?
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What process governs the transfer of a drug from the bloodstream to tissues?
What process governs the transfer of a drug from the bloodstream to tissues?
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What is the process of drug modification by enzymatic reactions within the body?
What is the process of drug modification by enzymatic reactions within the body?
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What is the process of drug elimination from the body?
What is the process of drug elimination from the body?
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Ionized drugs are generally absorbed more readily than unionized drugs.
Ionized drugs are generally absorbed more readily than unionized drugs.
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What is the Henderson-Hasselbalch equation used for?
What is the Henderson-Hasselbalch equation used for?
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What is the name of the enzyme that catalyzes the breakdown of acetylcholine?
What is the name of the enzyme that catalyzes the breakdown of acetylcholine?
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What class of drugs acts as a primary target for antibacterials?
What class of drugs acts as a primary target for antibacterials?
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What class of drugs disrupts the bacterial cell membrane, leading to leakage of essential molecules and cell death?
What class of drugs disrupts the bacterial cell membrane, leading to leakage of essential molecules and cell death?
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What class of drugs inhibits the synthesis of essential proteins in bacteria, leading to cell death?
What class of drugs inhibits the synthesis of essential proteins in bacteria, leading to cell death?
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What group of drugs inhibits DNA replication and transcription in bacteria?
What group of drugs inhibits DNA replication and transcription in bacteria?
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What class of drugs targets enzymes involved in the synthesis of tetrahydrofolic acid, which is essential for nucleic acid synthesis?
What class of drugs targets enzymes involved in the synthesis of tetrahydrofolic acid, which is essential for nucleic acid synthesis?
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What class of drugs acts to reduce stomach acid production, primarily targeting H+/K+ ATPases?
What class of drugs acts to reduce stomach acid production, primarily targeting H+/K+ ATPases?
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What class of drugs targets the synthesis and release of insulin, primarily by stimulating pancreatic beta cells?
What class of drugs targets the synthesis and release of insulin, primarily by stimulating pancreatic beta cells?
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What class of drugs antagonize the action of histamine, primarily by blocking H1 receptors?
What class of drugs antagonize the action of histamine, primarily by blocking H1 receptors?
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What class of drugs are commonly used to relieve pain and inflammation, often acting by inhibiting COX enzymes?
What class of drugs are commonly used to relieve pain and inflammation, often acting by inhibiting COX enzymes?
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Salicylic acid is a precursor to aspirin.
Salicylic acid is a precursor to aspirin.
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What class of drugs acts by inhibiting the activity of the central nervous system, often producing sedation, anxiolysis, and hypnotic effects?
What class of drugs acts by inhibiting the activity of the central nervous system, often producing sedation, anxiolysis, and hypnotic effects?
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What is the name of the class of drugs that act as analgesics and anti-inflammatory agents, but do not inhibit COX enzymes?
What is the name of the class of drugs that act as analgesics and anti-inflammatory agents, but do not inhibit COX enzymes?
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Study Notes
Organic Medicinals
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Organic medicinal study of pharmaceutical chemistry focused on the discovery, synthesis, and design of bioactive molecules.
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Pharmacodynamics studies how drugs interact with targets like enzymes, proteins, lipids, and receptors, and nucleic acids.
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Enzymes as drug targets include active site inhibitors.
- Reversible inhibitors compete with endogenous substrates for active sites.
- Irreversible inhibitors form covalent bonds, permanently inactivating enzymes.
- Allosteric site inhibitors bind to sites other than the active site, inducing a conformational change that inactivates the enzyme.
- Uncompetitive inhibitors bind to the enzyme-substrate complex, preventing the reaction from proceeding.
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Receptors as drug targets are cell components, usually proteins, in cell membranes or cytoplasm.
- Agonists bind to receptors, activating them similarly to endogenous ligands.
- Three requirements for agonist binding: correct functional groups, correct orientation, correct site
- Allosteric modulators bind to sites other than the ligand binding site, indirectly affecting receptor activity. (e.g., benzodiazepines on GABA receptors).
- Antagonists bind to, yet do not activate receptors, preventing endogenous ligands from binding.
- Requirements/strategies for antagonist binding: correct functional groups & the correct binding position
- Other mechanisms: allosteric modulators & umbrella effect
- Partial agonists activate receptors less than endogenous ligands.
- Inverse agonists bind to receptors and inhibit their constitutive activity (activity in the absence of an endogenous ligand).
- Desensitization occurs when receptors become less responsive due to prolonged agonist binding.
- Sensitization occurs when receptors become more responsive due to prolonged antagonist binding.
- Tolerance is a situation where increased doses of a drug are required over time to achieve the same effect, often due to receptor desensitization or dependence.
- Dependence is related to the body's ability to adapt to the presence of a drug. Withdrawal symptoms occur if the drug is stopped due to abnormal levels of target receptor.
- Agonists bind to receptors, activating them similarly to endogenous ligands.
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Nucleic acids as drug targets involve intercalating and non-intercalating agents.
- Intercalating agents slip between DNA base pairs, disrupting replication and transcription.
- Examples include, Podophyllotoxins, Camptothecin
- Non-intercalating agents prevent DNA replication or repair.
- Examples include, Alkylating agents, Nitrogen Mustards, Cyclophosphamide, Cisplatin
- Intercalating agents slip between DNA base pairs, disrupting replication and transcription.
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Other components like the journey of the drug in the body, are examined via pharmacokinetics.
Pharmacokinetics
- Absorption: Transfer of drug from administration site to systemic circulation. Factors influencing absorption include ionization, pH, and lipid solubility.
- Distribution: Transfer of drug from blood to cells. Factors involved include plasma protein binding and drug's ability to enter cells.
- Metabolism: Biotransformation of drugs to more polar metabolites.
- Phase I reactions (e.g., oxidation, hydrolysis): Usually make drugs more polar.
- Phase II reactions (e.g., glucuronidation, sulfation): Conjugate drugs with endogenous molecules to make them more water-soluble, and usually detoxify them.
- Excretion: Removal of drugs from the body. Common pathways include renal excretion and biliary excretion.
Adrenergic Drugs
- Catecholamines are adrenergic compounds with a catechol ring and alkylamine chain.
- Biosynthesis, metabolism, and structure-activity relationships (SAR) are essential characteristics.
Cholinergic Drugs
- Acetylcholine (ACh) is the primary neurotransmitter in the peripheral and central nervous systems.
- Has acetylcholine production, metabolism, and structure-activity relationships (SAR).
- Cholinomimetics and cholinergic antagonists are drugs that affect the acetylcholine system.
Antibacterials
- Antibacterial drugs target various bacterial components, including cell walls and protein synthesis. (Examples include Penicillins, Cephalosporins, Carbapenems, etc)
- General structure-activity relationships (SARs) for various drugs.
Antivirals
- Antiviral drugs are directed at different components of viral replication. (Examples include Acyclovir, Valacyclovir, Desciclovir etc)
Other Anti-cancer Drugs
- Anti-cancer drugs target various cellular processes, including DNA replication and protein synthesis.
- Other, more general, anti-cancer drugs include specific examples, such as methotrexate, 5-fluorouracil, cytarabine, and gemcitabine.
Analgesics
- Analgesics are drugs that relieve pain. Nonsteroidal anti-inflammatory drugs (NSAIDs) are a common class of analgesics.
- General structure-activity relationships (SAR) for several drugs.
Proton Pump Inhibitors (PPIs)
- PPIs are a class of drugs that target the proton pump in the stomach, reducing acid secretion.
Hypoglycemic Agents
- Hypoglycemic agents are drugs that lower blood sugar levels. Examples include insulin, sulfonylureas, and biguanides.
- Some related structural characteristics and mechanisms.
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Description
Explore the fascinating world of organic medicinal chemistry focusing on drug design and synthesis of bioactive molecules. This quiz covers the interaction of drugs with various targets such as enzymes and receptors, including details on inhibitor types and mechanisms. Test your knowledge on pharmacodynamics and the intricate processes behind drug action.
