Term
| What effects drug absorption and distribution? |
|
Definition
| the route of administration, blood flow at site of absorption, chemical properties of the drug |
|
|
Term
| What is enteral route of administration? |
|
Definition
| through digestive tract, orally or retically |
|
|
Term
| What is the parenteral route of administration? |
|
Definition
| bypasses the digestive tract(injections, inhalers, pumps, etc) |
|
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Term
| What are two things that determine the chemical properties of the drug? |
|
Definition
| lipophilic or hydrophilic |
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Term
| How does blood flow at the site of absorption affect absorption? |
|
Definition
| higher the blood flow, the higher the distribution |
|
|
Term
| What is a natural ligand? |
|
Definition
| normal molecule that binds to a receptor and activates it |
|
|
Term
| What is an artifical ligand? |
|
Definition
| drug molecule that binds to a receptor |
|
|
Term
|
Definition
| activates receptor at same level as natural ligand |
|
|
Term
| Where is the first place that all oral medications go after absorption? |
|
Definition
|
|
Term
| How does absorption of liquid formations occur? |
|
Definition
| immediately bioavaliable, some absorbed into the oral mucosa, no digestion required prior to absorption |
|
|
Term
| What must happen to solid formations? |
|
Definition
| they must be broken down, go through mechanical digestion in the stomach, then be absorbed into the small intestines |
|
|
Term
| All oral forms are distributed to the BLANK before entering BLANK |
|
Definition
| liver, general distribution |
|
|
Term
| What is first pass metabolism? |
|
Definition
| some of the drug is metabolized before it gets into general circulation |
|
|
Term
| What is the pH of the stomach? Small intestines? |
|
Definition
stomach- ~2
intestines 7-8 |
|
|
Term
|
Definition
| inactivates drugs for excretion, but some drugs are activated by this! |
|
|
Term
| Where does enterohepatic circulation take plce? |
|
Definition
| between the small intestine and liver, affects amount absorbed into systemic circulation |
|
|
Term
| Are drugs that aren't metabolized always excreted? |
|
Definition
| no, they can recirculate through the system |
|
|
Term
| What does an antagonist do? |
|
Definition
| binds to a receptor and turns off all activity |
|
|
Term
| Injected formulations are immediately BLANK. |
|
Definition
|
|
Term
| When is the blood flow rate like when distribution is rapid? Slower? |
|
Definition
-distributed rapidly when blood flow rate is high
-slower distribution when blood flow rate is low |
|
|
Term
| What does it mean if a drug has slower release? |
|
Definition
| has extended duration of action, given in place where blood flow is low so it slowly releases into the blood stream |
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|
Term
| If a drug is highly lipophilic what does that mean? |
|
Definition
| a greater percent of bound drug at given time(less active) |
|
|
Term
| Are ions hydrophilic or lipophilic? |
|
Definition
|
|
Term
| What type of administration is used for hydrophilic drugs? |
|
Definition
| parenteral because these can't cross a membrane, |
|
|
Term
| What does it mean if something is hydrophilic? |
|
Definition
| it is water soluble and can be dissolved in plasma |
|
|
Term
|
Definition
| elements or molecules that gain or loose and electron |
|
|
Term
| What type of drugs ionize in solution? |
|
Definition
| weak acids or bases will ionize in solution |
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|
Term
| Does ionization do the same thing for every molecule? |
|
Definition
| no, it creates different properties for individual molecules |
|
|
Term
| What type of charge do ions have? |
|
Definition
| Positive(cation) or negatine(anion) |
|
|
Term
|
Definition
| the pH at which 50% of the drug is ionized |
|
|
Term
| Can ionized drugs cross the plasma membrane? |
|
Definition
| no because they form hydrogen bonds, they easily dissolve in plasma but cannot cross membrane |
|
|
Term
| What happens to nonionized drugs? |
|
Definition
| they are easily absorbed, don't dissolve in plasma, don't have the ability to form hydrogen bonds |
|
|
Term
| What are weak acids like at a lower pH? |
|
Definition
| nonionized, that means they are more lipophilic and can cross membranes (oral formations absorbed in he stomach because the pH is 2) |
|
|
Term
| What are weak bases like at a higher pH? |
|
Definition
| more nonionized(oral formulations absorbed in the small intestine pH of 7-8) |
|
|
Term
| **See notes for m ore information on weak acids and bases** |
|
Definition
|
|
Term
| Why are there a lot of side effects with medications dealing with the brain? |
|
Definition
| because it has to be a high enough dose to where some will get through the blood brain barrier |
|
|
Term
| What does a drug have to be to be able to pass the placenta? |
|
Definition
|
|
Term
| What do lipophilic drugs bind to? |
|
Definition
| plasma proteins, bound drug is not bioavaliable, only free drug is therapeutic |
|
|
Term
| Where are plasma proteins made? |
|
Definition
|
|
Term
| What is the distribution of drugs affected by? (5) |
|
Definition
1.size and blood flow to the organ
2.drug solubility
3.plasma protein binding
4.barriers
5.Etc. |
|
|
Term
| What does anthopathic mean? |
|
Definition
| drug has hyprophobic and hydrophilic properties |
|
|
Term
| Distribution of lipophilic drugs can cause what? |
|
Definition
| drug interactions because of a limited amount of plasma proteins in the blood |
|
|
Term
| What happens when two lipophilic drugs compete for plasma proteins? |
|
Definition
| they will compete and the more lipophilic one will win, drug that looses will not be bound at normal %, this drug is more free |
|
|
Term
| What is another word for drug metabolism? |
|
Definition
|
|
Term
|
Definition
| chemical changes in the drug in order to make excretion more likely, mediated by emzymes |
|
|
Term
| What does metabolism do to the drug? |
|
Definition
polarizes the drug so metabolite will be water soluble
-decreases lopophilicity
-decreases binding to plamsa proteins
-decreases retention in the body |
|
|
Term
| What are the three mechanisms of biotransformation? |
|
Definition
-active drug to inactive metabolite
-inactive prodrug(not active until metabolized) to active metabolite
-active drug to active metabolite |
|
|
Term
| What does a drug+metabolic enzyme produce? |
|
Definition
|
|
Term
| what does an effective drug level mean? |
|
Definition
| that the same amount of drug is going into the body as coming out. |
|
|
Term
| when there is a effective drug level what is decreased? |
|
Definition
|
|
Term
| This is maintaining at least the therapeutic level of the drug in the blood? |
|
Definition
| A steady-state drug level |
|
|
Term
| in order to keep a steady state of drug level the dose can fluctuate ______ but will not ____ _______ the therapeutic level.? |
|
Definition
|
|
Term
| The amount of time necessary for the concentration of the drug to decrease by 50% is called the? |
|
Definition
|
|
Term
| how many half lives are necessary to remove nearly all the drug or to build it to a steady state level? |
|
Definition
|
|
Term
| what is Zero- order Kinetics? |
|
Definition
| is when the drug is eliminated at a constant rate in spite of the amount of drug present (ex. Alcohol, Aspirin) |
|
|
Term
| Why does the body eliminate the drug at a constant rate despite the amount in zero- order kinetic reaction? |
|
Definition
| because some drugs use metabolic enzymes that get saturated and the amount doesn't matter they cannot increase the reaction. |
|
|
Term
| what BAD thing can happen with zero order kinetic reactions? |
|
Definition
| can build up to toxic levels quickly |
|
|
Term
| How many phases of metabolize are there? |
|
Definition
|
|
Term
| Where does phase 1 of metabolism happen in the body? |
|
Definition
|
|
Term
| what kind of drugs go through phase 1 metabolism? |
|
Definition
| lipophilic drugs because they need extra metabolism for easy excretion |
|
|
Term
| are Lipophilic drugs easily retained in the body? |
|
Definition
|
|
Term
| where are the metabolic enzymes located? |
|
Definition
|
|
Term
| is phase 1 metabolism effected by age? |
|
Definition
|
|
Term
| besides age what else affects phase 1 metabolism? |
|
Definition
|
|
Term
| what are 3 types of reactions that a drug can under go in phase 1 metabolism? |
|
Definition
1. oxidation
2. Hydrolysis
3. Reduction |
|
|
Term
| what is metabolism based on? |
|
Definition
|
|
Term
| what does aging cause to happen to enzyme production? |
|
Definition
| decreases, therefor decreasing metabolism |
|
|
Term
| because there is a litmited supply of available enzymes for a drug what will the drug do? |
|
Definition
| end up competing for the enzyme for metabolism |
|
|
Term
| how will Drugs with increased affinity for enzymes bind and metabolize? |
|
Definition
|
|
Term
| How will drugs with a lower affinity bind and metabolize? |
|
Definition
| lower than normal binding and lower than normal metabolism |
|
|
Term
| in metabolism, an increase in enzymes =? |
|
Definition
| an increase in metabolism |
|
|
Term
| in metabolism, a decrease in enzymes =? |
|
Definition
|
|
Term
| If a drug has a low affinity will it have more or less side effects? |
|
Definition
|
|
Term
| During metabolism in the liver in phase 1, a lipophilic drug will cause 2 types of enzymes, what are they? |
|
Definition
|
|
Term
|
Definition
| certain drugs cause an increased production of enzymes, this will lead to faster metabolism |
|
|
Term
|
Definition
| production of enzyme decrease, and metabolism rate decrease. |
|
|
Term
| All drugs go through phase ____ but not all go through phase ___? |
|
Definition
|
|
Term
| Lipophilic drugs go through phase_____? |
|
Definition
|
|
Term
| phase 2 metabolism takes place in the? |
|
Definition
|
|
Term
| what enzymes facilitate the process of phase 2? |
|
Definition
|
|
Term
| What takes place in Phase 2 metabolism? |
|
Definition
| the lipophilic drugs are bound to water soluble compounds such as acids, by doing this they are more easily excreted. |
|
|
Term
| in phase 2 are the same types of enzymes that are in the liver metabolizing the drugs? |
|
Definition
| No, transferase enzymes are in phase 2 |
|
|
Term
| Does age, other drugs or metabolism get affected in phase 2? |
|
Definition
|
|
Term
| what are the 3 types of renal (urine) routes of excretion? |
|
Definition
1. Glomerular filtration
2. Active tubular secretion
3. Passive tubular diffusion |
|
|
Term
| what is Glomerular filtration? |
|
Definition
| metabolite enters filtrate directly from glomerulus into Bowman's capsule |
|
|
Term
| what is active tubular secretion? |
|
Definition
| Pumps that transport metabolites directly into filtrate ager Bowman's capsule |
|
|
Term
| This type of excretion requires Energy? |
|
Definition
|
|
Term
| what is Passive tubular diffusion? |
|
Definition
| Through channels into filtrate after Bowman's capsule. |
|
|
Term
| What excretion route does NOT require energy? |
|
Definition
| Passive tubular diffusion |
|
|
Term
| what is another type of excretion besides Renal? |
|
Definition
|
|
Term
| where does extrarenal take place? |
|
Definition
| Happens outside of Kidneys |
|
|
Term
| what are the different types of extrarenal excretions? |
|
Definition
pulmonary
Biliary
Salivary
Gingival crevicular fluid
sweat or milk |
|
|
Term
| what is the modt common route of excretion? |
|
Definition
|
|
Term
| what is pulmonary excretion? |
|
Definition
|
|
Term
| what is biliary excretion? |
|
Definition
|
|
Term
| what is skin and milk secretion? |
|
Definition
| through the skin as sweat and mammary glands as milk |
|
|
Term
| what types of renal excretion can happen after the glomerulus? |
|
Definition
| Active tubular secretion and Passive tubular diffusion |
|
|
Term
| How does Compliance play a role as a factor affecting frug action within the body? |
|
Definition
| the patient has to take the drug and take it when they are supposed to |
|
|
Term
| How does Psychologic factors play a role as a factor affecting frug action within the body? |
|
Definition
| if a patient believes that the drug will help them and they will get better, they will (the Placebo effect) |
|
|
Term
| How does tolerance of the body play a role as a factor affecting frug action within the body? |
|
Definition
| the body adjust to the the drug, if a tolerance is built up it may take more of the drug to get the same effect as a lower dose did previously. |
|
|
Term
| How does pathologic state play a role as a factor affecting frug action within the body? |
|
Definition
| Depends on how sick the patient is for how quick the drug will work, (state of the body and organs) |
|
|
Term
| How does time play a role as a factor affecting frug action within the body? |
|
Definition
| night = drug lasts longer due to slower metabolism |
|
|
Term
| How does sex play a role as a factor affecting frug action within the body? |
|
Definition
| male vs. female may metabolize the drug faster or slower. |
|
|
Term
| How does genetics play a role as a factor affecting frug action within the body? |
|
Definition
| some people produce more enzymes and metabolize drugs more quickly and vise versa. |
|
|
Term
| How does age/weight play a role as a factor affecting frug action within the body? |
|
Definition
weight plays a role because heavier people with more fat = the lipophilic drugs wanting to stay with the fat longer and not go to the blood stream= slower reactions.
Age- may metabolize faster when young and slower as person ages |
|
|
Term
| How does environment play a role as a factor affecting frug action within the body? |
|
Definition
| altitude, chemicals and other factor in the surroundings can affect the way the drugs react in the body |
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