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| Any substance that uses chemistry to bring about a biologic change |
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| The study of drugs and their effects when used to prevent, diagnose and treat disease |
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| The subset of pharmacology that deals with harmful effects of substances on living systems |
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| Deadly effects seen at high doses |
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| Unwanted effects seen at therapeutic doses |
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| Pharmacogenetics/ Pharmacogenomics |
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| The study of genetic variations that cause differneces in drug response among individuals or populations |
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| Actions of the DRUG on the BODY/ target organ that determine how the drug is used therapeutically (Ex. Drug decrease bp) |
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| The actions of the BODY on the DRUG. This is the process that determines the concentration of a drug in body fluids/ tissues over time (Ex. Does the body absorb it well- can we give orally vs vein) |
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| FDA: Food and Drug Adminstration |
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| Drugs must be SAFE and EFFECTIVE now;started in 1862; is a scientific, regulatory and public health agency: that regulates food products, drugs, medical devices and cosmetics |
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| FDC: Federal Food, Drug and Cosmetic act of 1938 |
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| Drugs must be proven SAFE before being sold and have adequate DIRECTIONS for safe use |
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| Durham-Humphrey Amendment |
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| 1951: Divided drugs into Prescription (Rx) and Over-the-counter (OTC) |
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| Drugs that can only be given under the supervision of a health care professional; they are not safe for use directly by the pt |
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| Drugs that are labeled so patients can use them safely without a health professional |
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| Kefauver-Haris Drug Amendment |
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| Says drugs must be safe and EFFECTIVE. Beginning in 1962 *some drugs were grandfathered in so some uneffective drugs are still out there |
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| New Drug Development: Starts with an idea found by; |
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Definition
| chemically modifying a known molecule; screening previously found compounds for unrecognized activity; using biotechnology and cloning to make compounds found in the body; combining known drugs to get SYNERGISTIC effect |
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| Once a potential drug is identified |
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| It goes through testing; first test in vitro; EXPENSIVE |
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| Tests in animals are done to try and determine human toxicity; and weigh potential benefits of the drugs vs. the risks of toxicity (test acute, subacute, chronic; carcinogenic potential; mutagenic potential; effect on reproduction; wont catch rare toxicities |
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| length of preclinical testing |
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| Human testing.. must file an application with? |
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| Takes 4-6 years; has 4 trials/ phases |
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| Is the new drug Safe? Do humans/ animals have similar reactions? looks at pharmacokinetics; |
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| Phase I Trial: # /types of people |
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| 25-50 health human volunteers; open trial; the subject and providor know what drug the subject is getting |
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| Is it Effective? Given to those with disease |
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| Characteristics of Phase II clinical |
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| 100-200 pt's with the disease; single blind study (provider knows what drug; subject doesnt) |
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| Phase III Clinical trials |
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| Does it Work? Use info from phase I/II to REFINE/ study EFFECTIVENESS/ TOXICITIES |
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| Characteristics of Phase III |
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| 1000's of patients with the disease; double blind |
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| Submitted when drug passes clinical phases of I,II and III; review lasts ~ 1 year (less for extremely needed drugs/ HIV) |
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| Post marketing surveillance. Occurs after FDA gives approval for release of drug; if there is an AREA OF CONCERN-- company must continue to collect DATA; |
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| Patents on New Drugs Lasts? |
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| 17 years; after the trials a drug has about 14 years to make money. |
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| Generics: After patent's expires anyone can manufacture the drug |
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| Scientific name based on chemical structure; long; ex. acetylsalicylic acid= aspirin |
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| Given by United States Adopted Names Council;gives pharmacologic or chemical info about a drug; must be unique; nonproprietary name (not restricted to the original manufacturer); uses stems (prefixes, suffixes, infixes) to help place drugs in similar groups; international standard |
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| Example of Generic Group Name: olol |
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| B blockers: propranolol, metoprolol, indolol |
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| The original company that creates a drug has exclusive rights to that drug until the patent exprires; then they can create a brand name... But others can create other brand names/ similar drugs |
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| The original company that had the patent names the drug first with brand name and has rights over that name |
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| Example of drug names: 3 types |
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chemical: n-methyl-3-pheny-3 etc
generic: fluoxetine
brand: prozac |
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| When a drug is considered "safe" |
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| It means the potential benefits of the drug outweigh the risk: chemo is not safe; but its better then Ca |
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| Package Insert: a document generated by the manufacturer and approved by the FDA: hard copy found in bottle; large amount of info about drug; Description of drug; clinical pharmacology; indications; contraindications; warnings; black box; precautions; adverse reactions; drug abuse; od; dosage; how supplied |
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| found in prescribing information; include chemical characteristics and pharmacologic group |
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| Absolute contraindications |
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| Relative contraindications |
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| if benefits outweigh risks give the drug even through it may have a negative effect; similar to precautions |
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| in prescribing information: a special type of warning: the most serious and highest level of warning |
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| who to use care with when giving; similar to relative contraindications |
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| Most common ones; or common and serious |
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| Drug Facts and comparsions |
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| unbiased source of drug info; expensive |
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| Physician's desk reference |
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| A bunch of package inserts; commercial reference-increases bias; PDR.net |
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| Great pocket guide; published yearly; 23 tables; |
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| alphabetical site of infection; most common causative organisms |
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| recommendations for antibiotic prophylaxis |
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| Pharmacokinetics: 4 components |
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| Clearance; volume of distribution; half-life; steady state |
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| A measure of the bodies ability to eliminate a drug; (renal; hepatic); single most important factor to influence serum drug levels |
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| Space in the body where drug goes: water soluble (blood); lipid soluble (fatty tissues); |
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| large volume of distribution |
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| drug goes everywhere;all tissue effected |
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| small volume of distribution |
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| only a few tissues exposed |
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| The time it takes to decrease the concentration of the drug in the body by half (50%); takes 5 of them to eliminate the drug; DOSING INTERVAL info |
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| works faster reach steady state fsater, get rid of quicker; cons need to take more often, less conveinent; ibuprofen |
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| 24 hr; Dose less frequently; pro- easier to take- more convenient; cons; onset slower reach steady state slower, get rid of slower; piroxicam |
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| the amount of drug in the blood when it is at a stable level; the amount of druc accumulated or taken is equals the amount of drug eliminated by the body; determined by the dose; and how frequently the drug is given (dose interval);;; a certain % of the drug persists after each interval; after 5 half lives get to this level |
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| How BODY effects DRUGs; focus on change in drug plasma concentration; (absorption, distribution, elimination |
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| The movement of drug into the bloodstream; from site of administratino into circulation; applies to all routes except (topical and IV); bioavailability |
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| the process of a drug leaving the blood steam and going into the organs and tissues |
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| removing drug from blood by metabolism and exretion |
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| measure of absorption; the fraction of the administered dose of a drug that reaches systemic circulation in an active form; if you give 100mg and 50mg gets to the system= 50% bioavailable |
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| Most reliable forms of drug delivery |
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| subcutaneous, intramuscular, intravenenous |
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| circulation, diffusing into interstitial fluid, cells from circulation |
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| factors affecting distribution |
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| organ blood flow, plasma protein binding molecular size, lipid solubility |
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| The rate at which a drug is distributed to various organs after a drug dose is administered depends largely on the proportion of cardiac output received by the organs |
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| brain, heart, liver, kidney |
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| skin, bone, adipose tissue |
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| almost all drugs reversibly bind to plasma proteins (ALBUMIN): as the free (unbound drug diffuses into interstitial fluid and cells, drug molecules dissociate from plasma proteins to maintain balane between free drug and bound drgu |
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| confined to plasma compartment |
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| major factor affecting the extent of drug distribution: blood brain barrier |
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Blood Brain Barrier: tight junctions between the capillary endothelial cells and glial cells that inhibit penetration of drugs into the brain
Only drugs with high lipid solubility can penetrate the blood-brain barrier |
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| 3 organs involved in drug elimination |
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| Gastrointestinal tract, kidneys (most), liver |
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| Drug metabolism: BLANK of drugs is done by the liver to help eliminate drugs. The liver will change (metabolize) a drug so it can be eliminated more easily by the kidney or GI tract. use 2 types (Phase I, Phase II) |
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Definition
Make the drug more polar (this often makes the drugs less interactive with the receptors in the body) and more charged
Usually adding –OH, -NH2, -SH group to the drug
By adding one of these chemical groups to the drugs and making them more charged they can be then excreted by the kidney |
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If phase I reaction does make the drug polar enough then it undergoes a phase II reaction
A phase II reaction adds a compound to a drug such as glucuronic acid, sulfuric acid, acetic acid, or amino acid
Called conjugation
Makes the even more polar so hopefully the kidney can excrete it in the urine |
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| BLANK system is a bunch of very important Phase I liver enzymes responsible for catalyzing most of the drug biotransformation in liver |
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Drugs can increase the cytochrome P450 effect
Cytochromes P450 can increase drug effects
Drugs can decrease the cytochrome P450 effect
Cytochrome P450 can decrease drug effects; difficult to predict; |
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Definition
When meds are given orally they are absorbed in the stomach & intestine. Everything absorbed here goes straight to the liver (portal circulation). So everything taken orally sees the liver before it sees any other part of the body
If the liver changes the drug this can be used many ways therapeutically. Two examples:
With a disease of the intestine give drugs that are inactivated by the liver. So the drug acts in the intestines where the disease is then its inactivated in the liver so rest of body never sees the drug.
Prodrug |
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| Some drugs are destroyed by stomach acid so can’t give it orally. So give a prodrug. The prodrug resists the acid and then the liver changes the prodrug to the active drug |
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| Factors that affect liver metabolism |
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Genetics
Diet: E.g. Charbroiled foods induce liver enzymes, grapefruit juice inhibits enzymes in liver
Age: At extremes of age don’t metabolize at same rate as those in the middle
Sex: E.g. Woman metabolize ETOH (ethanol) more slowly & recommendations for drinking tend to reflect this
Diseases: Especially failure of kidney, liver or heart |
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Study of how genetics affects metabolism of drugs
It’s a hot area of study. It is clinically relevant, but not practical yet so not commonly used. Ex acetylation dominant vs recessive gene |
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| Rate of elimination drugs |
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Definition
Mathematical relationships on how fast drugs get out of body classified one of two clinically important ways
First order elimination
Capacity-limited elimination |
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Definition
PERCENTAGE; This is the presumed relationship with most drugs and is the most important in determining steady state and half-lives
Rate of elimination is directly proportional to the concentration of the drug
Same amount of drug eliminated per fraction of time, and it is a % of drug present, NOT a set amount
50% of drug is eliminated every 2 hours, not 50mg |
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| Capacity limited elimination |
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Definition
HIGH CONCENTARTION: SET AMOUNT NOT %
This is the presumed relationship with most drugs and is the most important in determining steady state and half-lives
Rate of elimination is directly proportional to the concentration of the drug
Same amount of drug eliminated per fraction of time, and it is a % of drug present, NOT a set amount
50% of drug is eliminated every 2 hours, not 50mg (in od situations the drug levels rise FAST--> toxic lethal) |
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| Therapeutic drug monitoring |
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| we can measure the levels of some drugs; but remember seeing the amount of drug is different from seeing the amount interacting with the receptor; when drawing blood level must WAIT 4-5 half lives; only certain drugs monitored; know what your looking for (# thats toxic) |
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| the study of a drugs effects on the body; involves what a drug does to the body to give its effect; pharmacodynamics: many of a drugs effects can be explained through the receptor concept |
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| is the component of a cell or organism that interacts with a drug and initiates the chain of events leading to a drugs observed effects; drugs act by associated with specific molecule in the body= receptor; the association of the drug with the molecule changes the molecule chemically or physically giving the drug effect |
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| the relationship between the dose of a drug and its pharmacologic effect: if a receptor is tightly bound you dont need as much drug:: responsible for the selectivity of a drug;(brain receptor only effects brain) |
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| Types of receptor drug interactions |
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| full agonist, partial agonist, antagonist |
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| binds and activates the receptor to get maximal pharmacologic effect |
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| binds and activates receptor to get less than a maximal pharmacologic effect; (act like an antagonist because it will prevent the full agonist from binding to the receptor and exerting its maximal effect) |
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| Prevents the action of agonist by occupying binding sites on the receptor: binds to receptor doesnt activate it ; have a therapeutic effect on the doy because by binding the receptor doesnt allow other compounds nally found in the body to activate the receptor (estrogen antagonist): (competitive vs irreversible) |
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| reversible antagonist; drug binds and then disociates from the receptor; continuous process of binding/ unbinding; most common/ and most useful; concentration dependent; if you given enough of a drug you can get a high concentration of the drug at the receptor site--> get more effect; (Heroin strong narcotic receptor agonist; give narcan; reverse effect or heroin) |
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drugs bind and never let go of the receptor
Antagonist effect is only overcome when a new receptor is made.
Duration of effect of antagonist depends not on drug concentration but on how quickly the body makes a new receptor. |
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| Drug receptor binding primary action |
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Definition
| of water soluble drugs; drug binds to receptor; receptor is modified sending a message/ causing a change in the cell; most drugs are water solube and cannot diffuse through the lipid membrane so the drug sends a message through the membrane as opposed to acting directly on the cell |
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| can act directly on the cell; because they diffuse through the lipid membrane; hormones |
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| lipid soluble and bind to drug-receptor complexes through diffusing through the cell membrane; binding to the receptor in the nucleus and binding genes to activate them; genes then produce proteins which have a pharmacologic effect; take longer to have effect and get rid of |
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| Desensitization/ Tachyphlaxis |
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Definition
| The initial response to a drug decreases while the pt continues to receive the drug because the receptor number increases |
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| Responses of the body to a dose diminishes over multiple doses. stopping drug and restarting restores the initial response |
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| concentration of a drug needed to reach its maximal effect; Blood pressure drug A is more potent than B if you need 5mg of A to get its maximal effect and 50mg of drug B to get its maximal effect |
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| effect drug has ; Drug B is more efficacious (effective) if it lowers the blood pressure more than drug A at its maximal dose |
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| Is the ratio of desired effect to undesired effect of a drug |
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| : Not a lot of room between therapeutic and toxic effect- high potential for toxicity |
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| : A lot of room between therapeutic and toxic doses, low potential for toxicity |
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| receptor drug interactions |
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Definition
No one drug only binds to one receptor. Most drugs bind to many different sites in the body, so many effects and side effects.
Any one receptor is likely found on many cell types, so activating one receptor has many effects. The same receptor on one type of tissue will give a therapeutic effect and on another tissue give a toxic effect |
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