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Primary Care Provider 3 Part I

Study of the action of drugs in the body, including the processes of absorption, distribution, metabolism, and elimination. What the body does to the drug. Pharmacokinetics (2/3) pg 21
Study of the biochemical and physiological effects of drugs and the mechanisms of their action. The effect of the drug on the body. Pharmacodynamics (2/3) pg 32
Offical name assigned by manufacturer - approved by the U.S. Adopted Name Council (USAN). Generic Name (2/5) or nonproprietary name pg 21
Patent name given to the medicine by the company that is marketing the drug. Trade Name pg 21 (2/5)
Describes the drug's chemical composition and molecular structure. Chemical Name pg 21 (2/5)
How much of the drug is administered reaches its site of action. Bioavailability pg 21
Means two drug products (1) contain the same active ingredients; (2) are identical in strength or concentration, dosage form, and route of administration; and (3) essentally the same rate and extent of bioavailability. Bioequivalence pg 21
Legally the generic drug must have ______% of the proprietary drug. plus or minus 20% pg 22
Influences dissolution rate of solid form of drug. Formulation of the drug - factors that affect absorption pg 22
The higher concentration, the more ______ the drug is absorbed. quickly - concentration of drug pg 22 factors that affect absorption
Nonionized drugs are more _______ soluble and may readily diffuse across cell membranes. lipid - pg 22 (2/8)
Ionized drugs are lipid ________ and _______. insoluble, nondiffusible - pg 22 (2/8)
These drug formulations are more readily absorbable. Lipophilic pg 22 (2/8)
________ drugs become nonionized in the acidity of the stomach and then diffuse across membranes. Acidic pg 22 (2/8)
Basic drugs ________ tend to ionize and are not well absorbed in the stomach, but they may be better absorbed in the small intestine. alkaloids pg 22 (2/8)
A change in the pH of the stomach will affect the ________ of many drugs. absorption pg 22 (2/8)
Poor GI absorption may occur. Irritation to the GI mucosa may result. Destruction of drugs b/c of digestive enzyme and low gastric pH. Drug and food interactions may occur. Disadvantages of ORAL ingestion of medications. pg 22 ( 2/8)
Some drugs nonionic and have high ______ solubility are readily absorbed by the _____ _______. lipid, oral mucosa. pg 22 (2/8)
Drugs absorbed sublingually are advantageous because they avoid the ____ ______ phenomenon; therefore, the drug reaches site of action quicker. ie sublinqual nitroglycerin first-pass pg 23 (2/8)
Lipid-soluble drugs may not be absorbed because the skin acts as a ______ ______. lipid barrier pg 23 (2/8)
Skin that is _____ intact will absorb drugs more readily. NOT pg 23 (2/8)
Important to apply ________ medication to intact, healthy skin to ensure the correct absorption. intact pg 23 (2/8)
Mucous membranes also readily absorb drugs more readily than intact skin because of increased __________. vascularlity pg 23 (2/8)
Topical administration has the same advantage of avoiding the ____ ____ metabolism of the drug through the liver. first-pass pg 23 (2/8)
One advantage to ______ is that less first-pass metabolism of the drug occurs than oral preparations. rectal pg 23 (2/8)
Rectal absorption tends to be more _________ and ___ ______ than oral absorption, and some drugs cause rectal irritation. inconsistent, less complete pg 23 (2/8)
Disadvantage of ____ ____ include problems with regulating exact dose and many patients have difficulty in self-administering. inhalation therapy pg 23 (2/8)
Pulmonary absorption uses a larger surface area, making absorption ________. rapid pg 23 (2/8)
Ophthalmic should be instilled in the pouch of the lower eyelid. Anything formulated for the eye can be used anywhere else in the _____. body pg 23 (2/8)
Decreased circulation will result in _______ drug absorption. ie insulin injected into thigh muscle, followed by exercise will produce more rapid absorption of insulin. decreased pg 23 (2/8)
Random movement of drug molecules from high to low concentration. Passive diffusion pg 24 (2/8)
Molecules that are moderately sized, water soluble, or ionic across cell membranes. Active transport pg 24 (2/8)
The _______ the concentration, the more rapid the diffusion across the membrane. higher pg 24 (2/8)
If drug not _________, steady state is attained when concentration of ____ drug is the same on both side of the membrane. electrolyte, free pg 24 (2/8)
Lipids pass through membranes better than ______ molecules do. hydrophic pg 24 (2/8)
Nonionized drugs are more ______ soluble and may readily diffuse across cell membrane. lipd pg 24 (2/9)
Ionized drugs are lipid ________ and nondiffusible. insoluble pg 24 (2/9)
Acidic drugs such as aspirin become _________ in the acidic environment of the stomach and thus can diffuse across the membranes. nonionized pg 24 (2/9)
Basic drugs such as alkaloids ________ in the stomach and are not well absorbed. These drugs are better absorbed in a less acidic environment such as the small intestine. ionize pg 24 (2/9)
Particle going from low to high concentration. Particles need help entering the membrane b/c selectively impermeable. Very large particles enter and exit the cell. Active transport is a process used in the cell in all 3 situations. pg 24 (2/9)
Description of the amount of space into which a drug can be spread or distributed. Calculated volume or size of a compartment necessary to account for the total amount of drug in the body if present throughout the body at same concentration in plasma. Volume of distribution (Vd) pg 25 (2/9)
The larger the Vd, the _____ drug there is in the tissue. more pg 25 (2/9)
Water-soluble drugs have a Vd similar to the ______ volume b/c they are distributed in the blood. plasma pg 25 (2/9)
Water soluble drugs Vd ______ plasma volume. equals (2/9)
Plasma volume for a normal adult is ____ to _____ liters. 3 to 5 pg 25 (2/9)
_________ drugs have a larger Vd. Lipophilic pg 24 (2/9)
Plasma protein binding, obesity, edema, and tissue binding. Factors affecting volume of distribution pg 25 (2/9)
Geriatric patients often have relatively less muscle and more fat, placing them at risk for accumulation of ________ drugs in the adipose tissue. lipophilic pg 25 (2/9)
If geriatric patients lose weight and take the same dose, they could become ______. This can be a particular problem with lipophilic benzodiazepines. toxic pg 25 (2/9)
In these patients, ______ _______ drugs have a smaller Vd, resulting in increased blood concentrations. Effect even greater if patient is dehydrated. water-soluble pg 25 (2/9)
Excess fluid in interstitial spaces such as edema will affect the ________ of water-soluble drugs. distribution pg 25 (2/9)
In obesity, ________ drugs are distributed into adipose tissue and tend to accumulate. Little drug available elsewhere to produce an effect. ie phenobarbital fat soluble becomes trapped in fatty tissue causing low levels. lipophilic pg 25 (2/9)
Fat-soluble drugs are slowly released from the fat into the bloodstream, so they have a _____ duration of action. May prolong duration of s/e. longer pg 25 (2/9)
Drugs highly _____ bound (>90%) have a volume of distribution that is about the same as the amount of plasma. This is a small volume of distribution. protein pg 25 (2/9)
If _________ serum albumin, more active drug is available for _____ ______ drugs. decreased, protein-bound pg 25 (2/10)
If two _____ _____ drugs are used, the most _____ protein-bound drug will tend to ______ the other. Examples are furosemide and cephalosporins. protein-bound, tightly, displace pg 25 (2/10)
Albumin concentrations ________ slightly with age in most elderly patients, changes affect drug therapy in chronically ill or malnourished. decrease, pg 25 (2/10)
Most common protein that binds to various acidic drugs. Albumin, pg 25 (2/10)
Some drugs have significant ______ binding, which may result in ______ free concentrations when _______ is significantly reduced. protein, greater, albumin pg 25 (2/10)
Highly protein bound drugs to albumin should be prescribed in ______ doses for patients with _____ serum albumin values. reduced, low pg 25 (2/10)
Tissue binding - Some drugs have an _______ for specific tissue. Ciprofloxacin and tetracycline have an ________ for _______. affinity, affinity, bone pg 26 (2/10)
Endothelial cells of brain capillaries do not have intercellular _______ and ________. (CNS) pores, vesicles, pg 26 (2/10)
Will easily pass the blood-brain barrier, limited only by cerebral blood flow. (CNS) Lipophilic drugs, pg 26 (2/10)
Passive distribution of these drugs are restricted in the brain/CNS. Hydrophilic drugs pg 26 (2/10)
These drugs cross the blood-brain barrier easily and likely to cause CNS side effects such as confusion and drowsiness. Highly fat-soluble drugs pg 25 (2/10)
Biotransformation AKA - Metabolism pg 26 (2/11)
Chemical inactivation of a drug through conversion to a more water-soluble compound that can be excreted primarily in liver, lungs, and GI tract. Biotransformation pg 26 (2/11)
Makes drug more hydrophilic through oxidation, reduction, or hydrolysis. Phase I pg 26 (2/11)
What phase is the cytochrome P450 enzyme system part of? Phase I pg 26 (2/11)
Glucuronidation is called _________. Phase II pg 26 (2/11)
Phase II involves _______ (attachment of particles to the molecule), making it a highly _____ ______ substance with little or no pharmacologic activity. conjugation, water-soluble pg 25 (2/11)
If blood flow to liver is ________, drugs will be metabolized more slowly, leading to a _______ duration of action. decreased, longer pg 26 (2/11)
Blood Flow Matters Biotransformation (metabolism) Phase I (2/12)
Blood Flow Doesn't matter Biotransformation (metabolism) Phase II (2/12)
What phase of Biotransformation includes Oxidation, reduction, or hydrolysis makes the drug more hydrophic Cytochrome P450 enzyme system Biotransformation (metabolism) Phase I (2/12)
What phase of Biotransformation includes Glucuronidation, process is conjugation (2 things together to make a new) and produces highly water-soluble inactive substance (usually). Biotransformation (metabolism) Phase II (2/12)
These drugs pass easily through membranes including renal tubules, making them difficult to excrete. Lipophilic drugs pg 26 (2/12)
Biotransformation changes this drug to active and transforms it into a hydrophilic inactive compound that is readily excreted. Lipophilic drug pg 26 (2/12)
This system is found in ribosomes, but concentrated in liver, intestine, and lungs. Divided into groups according to similarity. Most important in predictable interactions. Cytochrome P450 Enzyme System pg 26 (2/13)
CYP 2D6 CYP 3A3/4 CYP 1A2 CYP 2C9/10 CYP 2C19 Most important enzyme groups in human drug interactions. pg 26 (2/13)
CYP 34A CYP 2D6 CYP 2C19 CYP 2C9 CYP 1A2 CYP 2E1 Six P450 enzymes account for metabolism of nearly all clinically important drugs. Pg 26 (2/14)
The P450 enzyme system is not the same in every individual. Each person receives genetic material that determines individual variations in the enzyme system; this is called ______________. Genetic Polymorphism pg 26 (2/14)
A drug which is affected by alteration of its enzyme metabolism. Substrate pg 27 (2/14)
Drug causes alteration in the enzyme metabolism of another drug by being an __________. inhibitor or inducer pg 27 (2/14)
Cytochrome P450 enzyme system may speed up reaction b/c it causes the drug to change to a more _______ substance. hydrophilic pg 27 (2/14)
Drug which causes the enzyme to metabolize more slowly or decreases the capacity of the enzyme pathway is called ________. Inhibitor pg 27 (2/15)
More drug can increase toxicity. Alteration in Phase I. Two mechanisms - competition and metabolic. MORE DRUG IN SYSTEM. Inhibitor pg 27 (2/15)
Less drug and less effectiveness. Less common than inhibition. Self induction (carbamazepine) LESS DRUG IN SYSTEM. Inducer pg 27 (2/15)
Drug that causes the enzymes to metabolize the substrate more quickly. Causes acceleration in the enzyme metabolism of another drug. Inducer pg 27 (2/15)
Increase enzyme activity by increasing the number of CYP 450 enzymes. Inducer pg 27 (2/15)
Same drug can be both a ______ and an ______ or ______. substrate, inducer, inhibitor pg 27 (2/15)
AKA: Glucuronidation Phase II of Biotransformation pg 27 (2/16)
In Phase II, a chemical group/compound is added to the drug by ________ ________. Groups are highly polar or ionized. Makes them ______ soluble and generally _______. covalent linkage, water, inactive pg 27 (2/16)
Expected results of Phase II Biotransformation: glucronidation. Water soluble and (usually) inactive pg 27 (2/16)
A chemical that is pharmacologically inactive until biotransformed into a active metabolite, ie enalapril or angiotensin-converting enzyme inhibitor. Doesn't work as a medication at all. Prodrug pg 30, (2/16)
Large amounts of drug must be given for a sufficient dose to remain after the liver. Known as First Pass, Phase II pg 27 (2/17)
Oral drugs pass directly to liver via hepatic portal blood flow; also ______, but not ______. rectal, sublinqual pg 27 (2/17)
Nitroglycerin Estrogen Extensively metabolized by sublinqual and transdermal patches. Need smaller dose since doesn't pass thru liver. (2/17)
Alternative routes to avoid the liver on first pass. Makes it possible to give a smaller amount of drug and be effective. Sublingual or topical pg 30 (2/17)
Process by which drugs and metabolites are removed from the body, primarily kidney and some liver. Excretion AKA Elimination pg 30 (2/18)
Does a drug filter into the tubule if it is bound to a protein? NO pg 30
Pencillin A drug which can be both secreted and actively reabsorbed. pg 30
Glomeruler filtration Tubular secretion Partial reabsorption Renal elimination functions (2/18)
This pH will increase the excretion of acidic molecules in urine. Alkalination pg 31
This pH will increase the secretion of basic molecules in urine. Acidification pg 31
Reduced glomerular filtration rate in kidneys causes the drug to remain in blood ______. longer pg 31 (2/18)
Necessary to calculate in patients with kidney damage to modify the dosage of medication. LEAN BODY MASS MATTERS. Estimated Creatinine Clearance pg 31 (2/19)
Created by: mareed3