PCC1 Revision Quiz Cheat Sheet

1. Solubility is one of the most important In order for the drug to reach the physicochemical properties in pharma- site of action and bind to a recepceutics because tor in the body it must be able to dissolve 2. Which of these is the standard order Biological target identification, hit of events in the research phase of dug molecule identification, hit moldiscovey? ecule to lead molecule optimisation, lead molecule optimisation, candidate selection, PCS (pre-clinical safety)assessment 3. What is the role of protein structure in If the structure of a protein target computer-aided drug design? is known, a 3-dimensional computer model of the protein can be developed. 4. What is virtual screening in the context Possible drug candidates can be of drug discovery? rapidly screened for their potential fit to a receptor in a process known as virtual screening. 5. How are drug candidates selected for further evaluation in computer-aided drug design? Drug candidates predicted to mimic the natural ligand and bind to the protein will be highlighted for further evaluation. 6. Activation of phospholipase C results in DAG and Ins(1,4,5) IP3 the production of: 7. Movement of drugs by passive diffusion requires that the molecule is relaacross membrane... tively lipid-soluble - cell membrane composed of lipid bilayer - lipid soluble easily pass through Oral 8. Which of the following routes of administration involves 'first-pass metabolism'? When a drug is taken orally, it is 1/8 absorbed through the GI tract and passes through the liver before reaching the systemic circulation. During this process, the drug may undergo metabolism in the liver before reaching the target tissues. 9. What is intra-thecal? route of administration in which a drug is delivered directly into the spinal canal/ subarachnoid space surrounding the spinal cord. - this method allows the drug to bypass the BBB and act directly on the CNS - it is commonly used for administering medications such as anesthesia, and chemotherapy/ pain management drugs. 10. Generally speaking, extensive False 'first-pass' metabolism is considered to be a positive drug characteristic: - not considered a positive drug characteristic because it can lead to a significant reduction in bioavailability of the drug. - when a drug undergoes extensive metabolism in the liver before reaching systemic circulation, a smaller amount of the active drug may reach the target tissues, reducing its effectiveness and potentially decreasing therapeutic effects 2/8 11. What does it mean by extensive 'first-pass' metabolism? - It occurs when a large portion of a drug is metabolised by enzymes in the liver before it reaches systemic circulation. - drugs that undergo extensive first-pass metabolism may require higher doses to achieve the desired clinical response 12. Safety pharmacology is a discipline that predict the risk of rare lethal aims to events 13. Which of these are considered part of a - the toxicological mechanism of drug molecule's toxicological profiles? action - dose-response relationship - the therapeutic index 14. The effects of coadministration with other drug molecules refer to: - how the drug may interact with other medication = Evaluating this interaction is crucial to ensure the safety and effectiveness of medication. 15. What is a toxicological profile? - helps in evaluating safety and potential risks of a substance 16. Which of the following statement regarding drug toxicity is true: - a drug can act via more than 1 mechanism of action ( both in terms of its pharmacological action and toxicity ) - a single drug molecule can lead to multiple adverse reactions in one/ or more target organs - changes in biochemistry, phys- 3/8 iology, and growth are all examples of clinical manifestations of adverse effects - liver toxicity is commonly encoutered due to the conversion of drugs into reactive metabolites - route of exposure and duration of exposure are key elements of toxicity 17. What is a toxic response? Is a function of drug concentration at the site of action 18. The Nuremberg Code originated from ...... The Nuremberg trials at the end of second WW 19. You are presented with a drug for formulation. It is intended for use in patients suffering from anaphylactic shock and requires urgent treatment. Your API has the following properties: · High potency ·Acceptable water solubility · LopP of 1.58 · Hgh oral bioavailability · Minimal first-pass metabolism · High-volume distribution · Stable in water Solution of injection - it can provide rapid and direct delivery of the medication into the bloodstream, ensuring quick onset of action to address the life-threatening condition. Injectable solution - form of parental administration - administered directly into bloodstream / bypasses GI tract - not have high oral bioavailability Which of the following is an appropriate Solutions for injection - endosage form given the intended use and sure drug is completely dissolved the API properties above? hence have acceptable water solubility 20. What is the difference between oral and - When a drug is administered IV, IV? it bypasses the GI tract and is delivered directly into the bloodsteam. 4/8 - This direct route of administration avoids first-pass metabolism in the liver unlike oral medications typically undergo when absorbed through the GI tract - Therefore, drugs administered intravenously, do not pass through the liver before reaching systemic circulation, allowing for rapid and complete absorption of the medication. 21. What is high oral bioavailability? - refers to the extent and rate at which a drug/susbstance is absorbed and becomes available in the systemic circulation after oral administration. - A drug with high oral bioavailibilty, it is efficently absorbed from the GI tract, allowing a significant amount of administered dose to reach the bloodstream and exert its therapeutic effects. 22. Which has high oral bioavailability oral Oral solution - already dissolved solution/ suspension or Tablet? in dissolved form, allowing for quicker and more complete absorption in the GI tract - Tablets need to disintegrate and dissolve before the drug can be absorbed - oral suspension = have solid 5/8 particles in liquid, need shaking before use. 23. Do transdermal patches have acceptable water solubility? No -designed to be absorbed through skin and into bloodstream - drug is formulated in a way that allows it to penetrate the skin barrier for systemic delivery 24. Do transdermal patches have minimal first-pass metabolism? Yes - they are designed to bypass the first-pass metabolism that occurs when drugs are taken orally. - by delivering the drug directly through the skin and into the bloodstream, transdermal patches avoid metabolism in the liiver before reaching systemic circulation. 25. What is minimal first-pass metabolism? Occurs when a drug is administered through a route that bypasses the GI tract, reducing its metabolism in the liver. 26. Why does oral solution not have minimal first-pass metabolism? - it can reduce bioavailbility before reaches the systemic circulation 27. What does high potency mean? refers to the effectiveness of a drug producing a specific effect at a relatively low dose. A drug with high potency requires a lower dose to achieve the desired therapeutic effect. 6/8 28. What is high-volume distribution? - drug is extensively distributed throughout body tissues 29. Does transdermal patches have a high - they have a low VD compared VD? to oral medications due to slower absorption and localised drug delivery 30. The most active components of plants Secondary metabolites are .... 31. Which of the following is a type of Euro- Directives - type of European pean union legislation? Union legislation that sets out goals that all EU countries must acheve 32. Which of the following is NOT a type of Rapid recognition procedure MA application? 33. You have a new API that has an acceptable pharmacology and toxicology profile as well as favorable physicochemical characteristics. However, it is not stable in water for more than 7 days. Which of the following is a suitable formulation for this drug? A powder for constitution - In contract, a powder formulation can help maintain the stability of the drug until it is ready for administration 34. Why an oral solution may not be suit- The the lquid form of an oral soable for a drug that is not stable for more lution requires the drug to be disthan 7 days? solved in water. - If the drug is not stable in water for an extended period, it may lose potency in the solution over time, affecting its effectiveness. 35. Why a lotion may not be suitable for a drug that is not stable for more than 7 days? 7/8 - lotion have acceptable water potency - high water content - lose potency 8/8