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Ch. 1 Drug Action

Pharm 1

Name the 3 phases of a drug taken by mouth? Pharmaceutic(dissolution), Pharmacokinetic, Pharmacodynamic
In what phase does the drug become a solution so that it can cross the biologic membrane? The Pharmaceutic Phase
What is a Parenterally given dosage? This med dosage is one that is given and is administered by a route that bypasses the GI Tract (ex-IV, IM:Intramuscular, SubQ:subcutaneous)
What are the 4 phases that make up the Pharmacokinetic phase? Absorption, distribution, metabolism, excretion
In order for a med in pill form to be absorbed what must it go through first? pill goes through disintegration then dissolution (occurs in GI tract and happens in the Pharmaceutic phase)
These are added to drugs to allow them to be a certain size, shape and to enhance drug dissolution so they can be readily absorbed.(ex: K, Na) Excipients
When smaller particles of drugs are dissolved in GI fluids before absorption what is it called? Dissolution
What is the time it takes for the drug to disintegrate and dissolve to become available for the body to absorb called? Rate Limiting
Drugs are absorbed more rapidly in a acidic or alkaline fluids? absorbed in a Acidic fluid of 1 or 2
The young and old have more or less gastric acidity? Less! so drugs are absorbed slower in the stomach!
Which drugs resist disintegration in the gastric acid of the stomach? Enteric-coated drugs(breakdown may not occur until they reach the alkaline environment of the small intestine)
Which drugs should not be crushed because it would alter the place and time of absorption? Enteric-coated drugs
What is the process of drug movement to achieve drug action called? Pharmacokinetic
Name the 3 types of Absorption that move drug particles from the GI tract to the the body fluids? Passive(diffusion from high to low con.), Active(Needs a carrier enzyme or Protein and ATP to move from low to high), Pinocytosis(drug engulfed and carried across membrane)
Which drugs pass rapidly through the GI membrane? Lipid soluble ones
The GI tract is made mostly of what? lipids and proteins
What do water-soluble drugs need to pass through the cell membrane? They need enzyme or protein carriers
Large particles pass readily through the cell membrane when? If they are non-ionized(no + or - charge)
What can destroy some drugs like Penicillin G? Gastric Acid
How can drug lose be offset? By giving larger Partial doses
Which drugs do not pass through the GI tract or the Liver? Parenteral drugs, eyedrops,eardrops, nasal sprays, respiratory inhalants, transdermal drugs, and sublingual drugs
What drugs are absorbed through the skin and into the systemic system? TDD Transdermal drugs
Which drugs are absorbed under the tongue to avoid first-pass metabolism that occurs in the liver? Sublingual drugs
Which drugs are absorbed faster? lipid soluble and nonionized ones
what can affect drug absorption? blood flow, pain , hunger, stress, fasting, food and Ph
Drugs given Intramuscular-IM are absorbed faster because they have more blood vessels? True Ex:Deltoids
When drugs are taken orally they may not pass directly into the systemic system but may go where? to the intestinal lumen to the liver via the Portal Vein
In here drugs can be metabolized into a inactive form and be excreted in urine(this decreases the amount of active drugs available) In the Liver
What are drug Metabolites? these are drugs that have been metabolized by the Liver and are equally or more active than the original drug. they cause a increased pharmacologic response.
What is the first-pass effect? This is when drugs pass to the liver first and most of the drug dose would be destroyed.
What are some examples of first-pass metabolism drugs? Coumadin(warfarin),Morphine, Lidocaine, some Nitroglycerins
What is Bioavailability? This is the% of administered drug dose that reached the systemic circulation. Its a subcategory of absorption.
What is the % of bioavailability of oral drugs? LESS THAN 100%
What is the % of bioavailability of IV drugs? 100%
What is the % of bioavailability of first-pass hepatic metabolic oral drugs on entering the systemic circulation? 20-40%
A decrease in liver function or decrease in hepatic blood flow can do what to bioavailability of of a drug? It can cause a increase in drug bioavailability if the drug is metabolized by the liver.
How does drug toxicity occur with some oral drugs? occurs if they are absorbed rapidly which will cause a increase in the drug concentration.
Slow absorption of oral drugs causes what? less drug available and causes a decrease in drug serum concentration.
This is the process by which drugs become available to body fluids and body tissues Distribution
What can affect drug distribution? blood flow, drugs affinity to the tissue, protein-binding effect.
Volume of drug distribution Vd is dependent on what? drug dose and concentration in body
Drugs with a larger Vd stay in the body longer because of? their loner half-life
What protein do most drugs bind with? Albumin
highly bound protein drugs are what %? >89%(11% is active)
moderately-high bound protein drugs are what %(this part is inactive and cant cause a pharmacologic response)? 61-89%
moderately bound protein drugs are what %? 30-60%
What % are low protein-bound drugs? <30%
What are free drugs? these are drugs that are not bound to proteins, they are active and can cause a pharmacologic affect.
should 2 highly protein-bound drugs be given together? No! because they would cause a increase in the amount of free drugs and thus possible toxicity would occur.
When protein levels decrease what happens? it decreases the # of protein-binding sites and can cause an increase in the amount of free drug in the plasma.
How is drug dose prescribed? it is done by the % in which the drug binds to protein
What are Anticonvulsants? these are drugs that prevent epileptic or convulsive seizures. they bind to Albumin
which Antidysrhythmics bind to the protein component Globulin? Lidocaine, Quinidine(prevent disturbances in rhythmic pattern of brain waves)
Who has hypoalbuminemia because of low serum albumin levels, which results in fewer protein-binding sites? The elderly because of malnutrition
When there is a decrease in plasma proteins(albumin)what happens? you get a decrease in protein-binding sites, which will permit more free drug in the circulation and may become life threatening.
What is the primary site of drug metabolism? The liver(also GI tract )
How do liver diseases like Hepatitis & Cirrhosis alter drug metabolism? they inhibit the drug-metabolism enzymes in the liver,metabolism rate decreases and excess drug accumulation can occur and lead to toxicity.
What is the time it takes for one half of the drug concentration to be eliminated called? half-life(t1/2)--> affected by metabolism and elimination.
Liver or Kidney dysfunction does what to the half-life of a drug? It prolongs the half-life, and less drug is metabolized and eliminated.
a short half-life of a drug is how long? 8 hours
A long half-life of a drug is how long? 24 hours or longer. takes several days before drug is completely eliminated from body. EX: Digoxin
Steady-state serum concentration is predictive of what? Therapeutic drug effect
The main route of drug elimination occurs where? in the Kidneys(urine)-Filters unbound drugs, water-soluble drugs, and unchanged drugs
The Urine pH(4.5-8) influences what? drug excretion
Acidic urine promotes excretion of what? weak base drugs
Alkaline urine promotes excretion of what? weak acids drugs(aspirin)
This is a metabolic byproduct of muscle that is excreted by the kidneys. Creatinine
What is CLcr or Creatinine clearance? This is a test to determine Renal function. If renal function is decreased then drug dosage needs to be decreased. in the elderly the CLcr may be around 60 ml/min.
What is the normal level for CLcr? 85-135 ml/min. This value decreases with age.
What is Pharmacodynamic Phase? This is the study of drug concentration and its effects on the body.
When you have a drug response what may occur? You may get primary and secondary responses(these may be undesirable)
Drug response is the relationship between what? the minimal versus the maximal dose needed to produce the desired response. all drugs have different values at which they will be effective.
When looking at pharmacodynamics what 3 things do we need to know about the drug? We need to know the drugs onset of action(time to reach minimum effective concentration-MEC), peak action(drug reaches its highest blood or plasma concentration, duration of action(length time the drug has a pharmacologic effect)
Where are drug binding sites primarily found? proteins, glycoproteins, proteolipids, enzymes
Name the 4 types of receptor families? 1. kinase-linked 2. ligand-gated ion channels 3.G protein-coupled receptor 4. nuclear receptor
Which receptor site has receptor in cell nucleus and has prolonged activation? Nuclear receptors
This is the site on the receptor in which drugs bind. This is Ligand-binding domain
Ligand-gated ion channels have drugs where? These receptors have drugs that span the cell membrane that cause the channels to open and allow ion, usually K and Ca to flow in and out.
This type of receptor is on the cell surface and the drug activates the enzyme inside the cell and a response is activated. These are kinase-linked receptors
What do G protein-coupled receptor systems have? drug-->that activates---> receptor---> activates---> G protein----> activates----> effector
What do Agonist do? these are drugs that produce a response
What do drug antagonists do? these drugs block a response
antagonists and agonists drugs lack what? they lack specific and selective effects
The receptors that are located in eyes,lungs,heart, bladder and blood vessels are called what? Cholinergic receptors (and the drug affect all anatomic sites (ex- eyes, lungs etc.) of location, has 1 receptor site type)
Drugs that affect various sites(but have the same type of receptor-cholinergic) are what? Nonspecific drugs
non-selective drugs affect what? these drugs affect various receptors(ex-alpha-1 sites, Beta-1 sites, or Beta-2 sites)
If a drug produces a response without acting on a receptor how does it do this? it inhibits the production of hormones or the activity of enzyme activity.
what are the 4 categories of drug action? 1. stimulation or depression 2. replacement 3. inhibition or killing of organisms 4. irritation(laxatives irritate the lining of the colon to increase defecation and peristalsis)
whats the half-life of a). penicillin and b). Digoxin(a antidysrhymthic) 1=2hrs b=36 hrs.
If a drug with a long half-life is given 2 or more times a day what will happen? drug accumulation occurs and drug toxicity will occur.
what is ED? the Effective Dose in 50% of people /animals, in ratio form
LD is what? this is the lethal dose in 50% of people/animals. the closer it is to 1 the more lethal
TI(therapeutic Index)= LD/ED
drugs with a high TI are? in a wide margin of safety and have less chances of producing toxicity
Peak drug levels indicate what? the rate of absorption of the drug.
Through drug levels indicate what? the rate of elimination of the drug
Tachyphylaxis refers to what? this is a rapid decrease in response to a drug.
Which drug classes can cause Tachyphlyaxis? narcotics, barbiturates, laxatives, and psychotrophic agents
What is Placebo effect? This is a psychologic benifit from a compound that may not have the chemical structure of a drug effect.
Created by: VRoberts