|The primary site of drug metabolism & excretion is the?||Kidney|
|Routes of drug administration:||-Enteral -Parenteral -Inhalation -Transdermal -Topical|
|Enteral routes of administration:||Most common rout is by mouth (oral) -Tablet -Capsule -Elixir -Suspension|
|Parenteral routes of administration:||-Intravenous IV -Intramuscular IM -Subcutaneous SC -Intrathecal IT -Intraosseous IO *Solution *Suspension *Sub-lingual *Suppository *Depot (bypass first-pass & GI)|
|Transdermal routes of administration:||-Patch -Paste|
|Inhalation routes of administration||-Aerosol -Gas *for either systemic or local effect|
|Topical routes of administration||-Powder -Lotion -Ointment -Solution -Eye drops -Nasal spray|
|Agonist||Chemical or drug that binds to a receptor and creates an effect on the body.|
|Antagonist||Chemical or drug that binds to a receptor bud does not create an effect on the body; it blocks the receptor site from accepting an agonist.|
|Bioavailability||Amount of drug that reaches the systemic circulation.|
|Drug Administration||Method by which a drug is made available to the body.|
|First-pass Effect||Initial metabolism in the liver of a drug taken orally before the drug reaches the systemic circulation. *High first-pass effect = Low systemic side effect|
|Hypersensitivity||Allergic or immune-mediated reaction to a drug, which can be serious, requiring airway maintenance or ventilatory assistance.|
|Idiosyncratic Effect||Abnormal or unexpected reaction to a drug, other than an allergic reaction, as compared with the predicted effect.|
|Lung Availability/Total Systemic Availability Ratio (L/T ratio)||Amount of drug that is made available to the lung out of the total available to the body. *Tells you how effective inhalation of medication will be and the amount of systemic side effects *L/T ration should be as close to 1 as possible|
|Pharmacodynamics||Mechanisms of drug action by which a drug molecule causes its effect in the body. *What the medication does to the body|
|Pharmacokinetics||Time course and disposition of a drug in the body, based on its absorption, distribution, metabolism, and elimination. *What the body does to the medication|
|Receptor||Cell component that combines with a drug to change or enhance the function of the cell.|
|Structure-activity relationship (SAR)||Relationship between a drug’s chemical structure and the outcome it has on the body.|
|Synergism||Drug interaction that occurs from two or more drug effects that are greater than if the drugs were given alone. *1+1=3 *Sleeping Pill/Sedative + Alcohol|
|Additivity||Occurs when two drugs act on the same receptors, and the combined effect is the simple linear sum of the effects of the two drugs, up to a maximal effect. 1+1+2 *Anticoagulant+Alcohol|
|Potentiation||A special case of synergism in which one drug has no effect but can increase the activity of the other drug. *1+0=2|
|Tachyphylaxis||Rapid decrease in response to a drug.|
|Therapeutic Index (TI)||Difference between the minimal therapeutic and toxic concentrations of a drug; the small the difference, the greater change the drug will be toxic. *Ratio between LD50 & ED50 *Narrow = Dangerous *Wide = Less Dangerous|
|Tolerance||Decreasing intensity of response to a drug over time.|
|Absorption/Mechanisms by which drugs move across membrane barriers:||-Aqueous diffusion -Lipid diffusion -Carrier-mediator transport -Pinocytosis|
|Mucosoal barrier consists of:||-AW surface liquid -Epithelial cells -Basement membrane -Interstitium -Capillary vascular network|
|Bioavailability is influenced by:||-Absorption -Inactivation by stomach acids -Metabolic degradation -Blood flow to site of absorption|
|Primary site of drug metabolism and biotransformation:||Liver|
|Drug Distribution||The process by which a drug is transported to its sites of action, eliminated, or stored.|
|Volumes of major body compartments:||Vascular – 5L Interstitial Fluid – 10L Intracellular Fluid – 20L Fat – 14-25L|
|Clearance||A measure of the ability of the body to rid itself of a drug *AKA Total systemic or plasma clearance|
|Plasma Clearance (CLp)||Hypothetical volume of plasma that is completely cleared of all drug over a given period. *L/hr or L/hr/kg|
|Factors increasing L/T ratio:||-Efficientdeliver devices -Inhaled drugs with high first-pass metabolism -Mouth washing, including rinsing and spitting -Use of a reservoir device|
|Chemical Antagonism||Direct chemical interaction between drug and biologic mediator, which inactivates the drug.|
|Functional Antagonism||Can occur when two drugs each produce an effect, and the two effects cancel each other.|
|Competitive Antagonism||Occurs when a drug has affinity for a receptor but no efficacy and at the same time blocks the active agonist from binding to and stimulating the receptor.|
|Maintenance Dose||Rate at which medication must be replaced to maintain steady plasma levels. *Calculated dose and schedule *Small doses must be given more frequently|
|Time-Plasma Curve||Concentration of the drug in plasma over time; helps to determine the choice of medication for a clinical situation, and a dosing schedule.|
|Plasma Half-Life||Amount of time the body takes to completely metabolize and eliminate 50% of the dose *1:50%, 2:25%, 3:12.5%, 4:6.25%, 5:3.12%, 6:1.56%, 7:0.78%, 8:0.39%, 9:0.19%|
|EC50 or ED50||Effective concentration or dose of a medication that produces 50% of the drugs maximal response.|
|The most common route of drug distribution:||The Circulatory System|
|Which of the following is the most dangerous TI number: 2, 37, 25||2 (narrow)|
|The most common route of medication administration to the general out patient population is?||Oral|
|Which of the four major body compartments contains the smallest volume in liters?||Vascular 5L|
|What is the most important liver enzyme?||Cytochrome P450|
|What is the relationship from chemical activity to its clinical activity?||Structure Activity Relationship (SAR)|
|The most significant documented contraindicationdo medication delivery is?||Hypersensitivity|
|What is an agonist||Chemical that binds to a receptor and creates an effect on the body|
|What is Synergism||Two drugs given together have a greater effect than when alone|
|Tachyphylaxis||Rapid decrease in response to a drug|
|Enteral route||Literally means small intestines|
|Parenteral||Any route except enteral: IV etc|
|Pharmacokinetic phase||time a drug takes to be absorbed, distributed and eliminated from body|
|Bioavailability||% of drug that reaches systemic circulation|
|First-pass effect||effect of liver on a drug|
|Factors affecting Lung availability/total systemic availability||1. Efficiency of device used 2. Inhaled drugs with firs-pass effect 3. Mouthwashing 4. Use of a reservoir|
|Potency||Concentration or dose of drug that produces 50% of the drugs max response.|
|Pharmacogenetics||Hereditary differences in the way the body handles specific drugs|
|Idiosyncratic effect||effect that is opposite of the expected, or absent|
Respiratory Pharmacology Chapter 2 Practice Questions:
1. 5 Routes of administration: enteral, parenteral, inhalation, transdermal, topical
2. Absorption of pharmacokinetic phase: when drugs are given by mouth they must be dissolved in the stomach or intestines and absorbed into the blood stream. Once dissolved they must cross a lipid membrane to enter the blood stream. When the drugs are given via inhalation they must cross the lining of the respiratory tract (lipid membrane) to enter circulation. Depends on drugs ability to cross the cell membranes and resist the stomach, liver, and intestine break down. the less breakdown here the more goes to the systemic metabolism. The rate of absorption depends on the route of administration. Drugs taken orally take longer to be absorbed because they have to be broken down into small particles before they can go to the blood stream.
3. Agonist: Chemical or drug that binds to a receptor and creates an effect on the body
4. Agonist VS Antagonist: agonist are drugs that have an affinity for a receptor that causes a specific response. agonist activate the receptor. antagonist combine at the same receptor site but don’t cause activation of the receptor. antagonist block the action at the receptor site. it would be great if all we worried about were drugs and receptor sites. but by saying that it is that simple all drugs would exert the same effect when they bind to specific sites. drugs have an intrinsic activity that corresponds to their potency. a particular drug may have an intrinsic activity of 1(full agonist) or a .5 (partial agonist). the drug with the intrinsic activity of 1 would be a drug that gives a full response. (more potent action). a drug that has an intrinsic activity of 0 would be an antagonist.
5. Antagonist: Chemical or drug that binds to a receptor but does not create an effect on the body; it blocks the receptor site from accepting an agonist.
6. Aqueous Diffusion: occurs in the aqueous compartments of the body such as interstitial. spaces or within a cell. movement or transport of molecules is restricted by size. diffusion is the concentration gradient.
7. bioavailability: amount of drug that reaches the systemic circulation
8. Biovalibiity: term used to indicate how much of the drug actually reaches the systemic circulation. it is influenced by absorption but also inactivation caused by stomach acids and metabolic degradation. blood flow also play into factor
9. Carrier Mediated Transport: carrier molecules embedded in the membranes can transport substances such as amino acids, sugars, or naturally occurring peptides and the drugs that resemble these substances
10. chemical antagonism: 2 direct chemical interaction one drug inactivates another drug
11. Competitive antagonism: Drug has infinity for receptor but no efficacy and blocks a drug that does have efficacy
12. Cytochrome P450: major enzyme in the liver that metabolized p450 oxidase system. Certain drugs can INCREASE the amounts of enzymes, thereby increasing the rate of metabolism in the liver. Certain drugs can DECREASE the amounts of enzymes, thereby decreasing the rate of metabolism in the liver. Interactions of drugs in important to know for regulating therapeutic effects.
13. describe the method by which a drug dose is made available to the body: drug formulations and additives; drug additives; gelatin (gelatin allows for swallowing); drug coatings; aerosolized drugs can have preservatives, propellants, carrier agents; they can have an oil base or powder base plus the actual medication
14. Distribution: The movement of a drug through the blood stream into the tissues and then to the cells
15. drug administration: method by which a drug is made available to the body
16. drug interactions: chemical antagonism; functional antagonism; competitive antagonism; synergism; additibity; potentiation
17. ED50: the dose at which 50% of the response to the drug occurs (produces 50% of the response to the maximal effects)
18. enteral: use of the intestine
19. first pass effect: When a drug is taken orally and absorbed into the blood from the stomach or intestines the portal vein drains this blood directly into the liver. If a drug is highly metabolized by the liver enzymes it may become inactive before it reaches its target site.
Blood from the liver is drained by hepatic veins into the inferior vena cava and general circulation
20. first-pass effect: initial metabolism in the liver of a drug taken orally before the drug reaches the systemic circulation.
21. functional antagonism: 2 drugs produce and effect and cancel effect and cancel each other
22. half life of drugs: the time required for the plasma concentration of a drug to decrease by one half. half life is a determining factor of the length of action a drug will have. how long blood or plasma to decrease from full concentration to 50%
23. how can enteral be delivered: Oral: pills- single dose med use powered drug mixed with a syrup usually round oval. Tablets- made by compressing or molding powder with a bulk filling material under high pressure most are scored to allow for cutting in half. if it isn’t scored don’t cut in half as dosage may not be right. Tablets can be buffered or chewable
Capsules- encased in a hard or soft shell. mostly cylindrical in shape the drug inside can be powdered granulated liquid or combination of. these should not be crushed or dissolved and should be swallowed whole. Elixirs- usually have alcohol sugar and a flavoring agent example is an aspirin with codeine. Suspensions- is mixed with a liquid but the drug is not dissolved. Rectal: suppositories; sublingual/buccal; ng tube.
24. how can inhalation be delivered: gas, aerosol, metered dose inhaler, nebulizer solution, dry powder inhalers. Some consider in halation a form of topical. it helps to avoid systemic side effects, and the delivery this way provides a rapid absorption
25. how can parenteral be delivered: Injection. intramuscular (im); gets the drug to the circulatory slower than and IV but more rapid than oral. subcutaneous (SC); is between dermis and epidermis. intravenous (IV). solution; direct to a vein can be bolus or steady infusion; suspension; depot. Intrathecal (IT) (spinal fluid). Intraosseous (IO) (bone marrow). If clear or water based infusion is rapid, but if oil based or cloudy solutions have a slower rate of absorption. Parental carries the risk of infection, pain, or local irritation
26. How can Topical be delivered: powder; lotion; ointment; solution
27. How can Transdermal be delivered: Patch (should be rotated to prevent adverse affects). slow sustained release provides sustained blood leves throughout the day. Nitro, Nicoderm
28. how do we elimination: the primary site of drug excretion is the kidney; diseases affecting kidney or liver can affect drug clearance from the body; may refer to total systemic clearance or plasma clearance.; other ways to excrete is through bile in GI tract; air exhaled through the lungs; tears; sweat; feces; salvia
29. hypersensitivity: allergic or immune-mediated reaction to a drug, which can be serious, requiring airway maintenance or ventilatory assistance
30. idiosyncratic effect: abnormal or unexpected reaction to a drug, other than an allergic reaction, as compared with the predicted effect.
31. inhalation: taking a substance, typically in the form of gases, fumes, vapors, mists, aerosols, or dust, into the body by breathing in.
32. Insolubile: (ionized) (have positive and negative charges separated on the molecule)
Not susceptible to being dissolved
33. L|T ratio: proportion of drug available from the lung, out of the total systemically available drug; formula (lung does)/lung dose+gi dose); the higher that ratio the more efficient the aerosol drug delivery to the respiratory tract
34. LD50: the dose at which 50% of population had lethal effects
35. Lipid Diffusion: Epithelial cells have lipid membranes and a drug must be lipid soluble to diffuse across such a membrane. drugs can be lipid soluble or lipid insoluble. Lipid insoluble drugs are ionized (have positive and negative charges separated on the molecule). Acids: + (proton donator) (Carries positive chg). Bases: – (proton acceptor) (Carries neg. chg)
36. local effect: limited to the area of treatment inhaled drug to treat constricted airways)
37. lung availability/total systemic availability ratio L/T ratio): amount of drug that is made available to the lung out of the total available to the body
38. mechanisms for absorption: aqueous diffusion; lipid diffusion; carrier mediated transport; pinocytosis; factors affecting absorption
39. Metabolism: The process by which drug molecules are metabolized or biotransformed. Phase 1: converts active drug to water soluble form. Phase 2: combines a substance with a metabolite to form a polar conjugate.
40. The more_____ a drug is in its state (water or lipid) the more it is absorbed systemically: soluble
41. parenteral: any way other than the intestine, most commonly an injection (intravenous, intramuscular, subcutaneous, or intraosseous)
42. Pharmacodynamic phase: what the drug does to the body
-once a particular drug is absorbed and distributed, the drug action requires drug presence at a particular receptor site.
43. pharmacodynamics: mechanisms of drug action by which a drug molecule causes its effects in the body
44. pharmacogenetics: study of genetic factors and their influence on drug response
45.The Pharmacokinetic phase: Elimination; plasma clearance; maintenance dose; plasma half-life; time plasma curves.
46. Pharmacokinetic phase of inhaled aerosol drugs: local versus systemic effect; inhaled aerosols in pulmonary disease; distribution of inhaled aerosols; oral portion(stomach), inhaled portion.
47. Pharmacokinetics: time course and disposition of a drug in the body, based on its absorption, distribution, metabolism, and elimination
48. Phases of Drug action: drug admin (how we are going to give our drug and what dose); pharmacokinetic phase (how the drug is absorbed, distributed, metabolized, and eliminated); pharmacodynamics phase (the drug and receptor); effect (what happens)
49. Pinocytosis: the mechanism by which cells ingest extracellular fluid and its contents that then allows them to move across the membrane barrier.
50. Pinocytosis is referred to as: active transport
51. plasma concentrations: -to achieve a steady level of drug in the body, dosing must equal the rate of elimination
52. positive reaction for two drugs: synergism when two drugs react on the same receptor by different mechanisms and effects up to maximal effect. additivity two drugs on the same receptor and the combined effect is a simple linear sum of effects up to maximal effect. potentioation special case of synergism in which one drug has no effect but can increase the activity of the other drug.
53. potency: drug potency refers to the amount of drug required to produce the response desired. when the response is measured against the concentration, a dose response relationship can be seen. the lower the dose required to provide a certain effect, the more potent the drug is
54. receptor: cell component that combines with a drug to change or enhance the function of the cell
55. Routes of administration can affect absorption: drugs that are taken oral take the longest to be absorbed. drugs were given parentally bypass the liver and directly enter the systemic circulation. drugs give IM absorption is quicker that subcutaneous. surface area affects absorption greater the blood flow the quicker it moves systemically. first, pass effect
56. Site of Biotransformation or Metabolism: The liver is the principal organ for drug metabolism. It contains enzymes that convert lipid soluble drugs into water-soluble metabolites
57.Soluble: (non-ionized) Susceptible to being dissolved
58. structure activity relationship (SAR): the relationship between a drug’s chemical structure and the outcome it has on the body
59. synergism: drug interaction that occurs from 2 or more drug effects that are greater than if the drugs were given alone. additive effect two drugs act on the same receptor and combined effect is the sum of two drugs. potentiation is synergism but a special case one drug has no effect but can increase the activity of the other drug
60. systemic effect: pertains to the whole body, whereas the target for the drug is not local, possibly causing side effects ( capsule of acetaminophen for a headache)
61. tachyphylaxis: rapid decrease in response to a drug
62. therapeutic index (TI): difference between the minimal therapeutic and toxic concentrations of a drug; the smaller the difference, the greater chance the drug will be toxic
63. TI therapeutic index: the ratio of LD50 to ED50
64. Time response curve: concentration of a drug over time displayed graphically. and 25 mg is the amount needed to achieve some therapeutic effect (critical threshold); how long is the drug therapeutic
65. tolerance: decreasing intensity of response to a drug over time
66. topical: use of the skin or mucous membrane (lotion)
67. transdermal: use of the skin (patch)
68. types of antagonisms: chemical inactivates a drug; functional two drugs each produce and effect and then cancel out the effects of each other; competitive when a drug has an affinity for the receptor but blocks the active agonist from binding and stimulation the receptor
69. Weak acids _______ H ions it is neutral or non-ionized and is lipid soluble: donate
70. Weak base _____ H ions is ionized and is not lipid soluble.: gains
71. what are the mucosal barriers to the respiratory track: airway surface liquid; epithelial cells; basement membrane; interstitium; capillary vascular network
72. What effects distribution: depends on blood flow to the kidney, the drugs ability to leave the blood and the ability to enter the CNS quickly. Others will have to cross the blood brain barrier and will take longer to get to the CNS. The purpose of the blood brain barrier is to prevent toxin and poisons from reaching the brain. this can make it hard if trying to treat a brain infection.
73. what factors affect absorption: -the route is determined by the barriers that a drug must cross. water soluble drugs easily cross membrane barriers and can be given by mouth. lipid soluble drugs would be favored to give by IV.