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RT Pharmacology Ch 2

Principles of Drug Action

QuestionAnswer
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: -Efficient deliver 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 contraindication do medication delivery is? Hypersensitivity
Created by: DanielleCurrySRT