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the study of how various dosage forms influence the way the body metabolizes drugs and the way in which a drug affects the body
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the study of what happens to a drug from the time it is put into the body until the parent drug and all metabolites have left the body
the focus of pharmacokinetics is drug absorption into, distribution and metabolism within, and excretion from a living organism (ADME) |
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description of how a medication INFLUENCES physiologic processes in the body to provide a therapeutic benefit or mechanism of action
this occurs through either receptor interaction, enzyme interaction, or nonselective interaction |
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complex area applying medication knowledge (including pharmaceutics, pharmacokinetics, and pharmacodynamics) to specific patients and/or patient populations to treat disease and/or medical conditions
types of decisions can be divided into acute, maintenance, supplemental, palliative, supportive, prophylactic, and empiric
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study of natural drug sources |
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study of poisonous and undesirable responses to drugs and chemicals; clinical toxicology refers to the care of the poisoned patient (e.g. overdose, ingestion of chemicals, snake bites, etc.) |
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a drug is any chemical with effects to physiological processes of living organisms; a medicine is a substance or preparation used in treating disease |
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describes the chemical composition and molecular structure of a drug |
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USAN Council-assigned name used in official drug comendiums to list drugs; there is always a generic "name" but the actual generic drug may or may not be available commercially |
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registered trademark and indicates that its commercial use is restricted to the owner of the patent for the drug |
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Active vs. Inactive Dosage Forms |
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active includes the drug component that is directly responsible for the medication's role in treating disease; inactive involves drug components not directly responsible for the treatment of disease, but improve or provide drug stability, affect absorption, improve taste, etc. |
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a group of medications that have a similar chemical makeup and a similar physiologic effect on the body or mechanism of action
all medications in a drug class have the same indication, mechanism of action (MOA), dose, adverse effect, contraindications, monitoring, therapeutic considerations, and medication/drug-specific effects |
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disease and/or medical condition treated by the medication |
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Mechanism of Action (MOA) |
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description of how the medication influences physiologic processes in the body to provide a therapeutic benefit |
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the amount of medication required by the body to produce a therapeutic benefit
acceptable dosing ranges are common and doses are often titrated within this range
some drugs have specific target doses for specific indications |
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Adverse Effect (side effect) |
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undesirable response to medication that can occur when medication levels within the body are either therapeutic (within accepted treatment range) or elevated (toxic)
can be expected or unexpected (allergic reaction) |
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patient situations where the risk of using the desired medication is greater than the benefit of using the medication |
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involves efficacy (is the medication doing what we expect it to do?) and toxicity (is the medication doing more than we expect it to?) |
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Therapeutic Considerations |
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additional information important for medication selection |
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include oral, nasogastric, and gastronomy |
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liquids, elixirs, syrups, suspensions, powders, capsules, tablets, coated tablets, enteric-coated tablets, sustained/controlled release oral formulations
the above are listed in order of fastest to slowest absorption rates |
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Nasogastric (NG) and Gastronomy (G) Tube |
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typically liquid medications or medications that can be crushed and mixed with liquid prior to delivery |
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Definition
administered by syringe, needle, or catheter as well as sublingual or buccal and avoid the GI tract
include IM, SQ, IV, ID, intra-articular, intra-arterial, and intra-thecal
IV and intra-arterial are considered to be 100% absorption |
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Definition
applied to the skin or mucous membranes for a localized target effect (e.g. eyes, ears, nose, rectum, vagina, and lungs)
include patches, creams, lotions, otic, opthalmalic, intranasal, inhalers, and suppositories
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Definition
the movement of a drug from its site of administration into the bloodstream for distribution to the tissues
can be short or long processes depending on route of administration, dissolution rate, and medication characteristics
ends with all or a portion of the drug delivered to the systemic circulation and distribution begins |
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the amount or extent of drug available in the systemic circulation espressed as a percentage
it is effected by the route of administration |
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Factors that Effect Enteral Absorption |
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Definition
First-Pass Effect: liver enzymes metabolize the drug, decreasing the amount of active drug that reaches the systemic circulation thus decreasing bioavailability
Stomach pH, presence or absense of food, patients with portions of small bowel removed, certain medication use, conditions of low blood flow to the stomach or small intestine |
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Factors that Effect Parenteral Absorption |
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Type of injection (IV, IM, SQ), poor local or systemic circulation, cold vs. heat, low blood pressure, dosage formulation |
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refers to the transport of the drug in the body by the bloodstream to its site of action
once the drug is distributed, organs such as kidney and liver begin to metabolize and excrete the drug |
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the total intravascular and extravascular area within the body where medications can be distributed |
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How does blood flow effect distribution? |
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poor circulation results in poor distribution; areas of rapid distribution include areas of high vascularization (e.g. heart, kidneys, brain); areas of slow distribution include areas of low vascularization (e.g. muscle, skin, fat) |
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How does protein-binding affect distribution? |
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Definition
drugs bind to protein in the blood such as albumin, alpha-1 acid glycoprotein, or corticosteriod-binding globulin and these bound drugs are considered pharmacologically inactive as opposed to unbound, "free" drugs
low albumin levels require lower drug dosages; drugs can compete for protein-binding sites and one drug may have a higher "free" drug level than expected |
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How do the water/fat soluble properties of a drug effect distribution? |
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Definition
water-soluble drugs typically remain in the bloodstream and have a smaller volume of distribution
fat-soluble drugs typically leave the bloodstream to reach further targets and have a larger volume of distribution |
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How does the blood-brain barrier effect distribution? |
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Definition
only drugs that are lipophilic or that have a transport system can penetrate the barrier |
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Metabolism (biotransformation) |
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involves the biochemical alteration of a drug into an inactive metabolite, a more soluble compound, or a more potent active metabolite
cytochrome P-450 enzymes in the liver control biochemical reactions involved in drug metabolism and typically target lipid soluble drugs |
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involve competition, induction or inducers that "rev" up metabolism and enzyme activity related to other drugs, or inhibition or inhibitors that reduce metabolic rate of other medications |
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the elimination of drugs from the body, either renal, biliary, or through the sweat and mammary glands |
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the primary route of drug excretion; patients with altered renal function require dosage adjustment |
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excretion of drugs by the intestinal tract in which drugs are taken up into the liver, released in the bile, and eliminated in the feces
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Enterohepatic Recirculation |
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Definition
some lipophilic drugs are reabsorbed into circulation through the intestinal tract before biliary excretion and remain in the body for extended periods of time |
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time required for one half of a given amount of drug in the body to be removed; most drugs are eliminated after five half-lives |
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state in which the amount of drug removed via elimination is equal to the amount of drug absorbed with each dose and typically occurs after 4-5 half lives
once a steady state is achieved, there are consistent levels of drug in the body that correlate with maximum therapeutic benefits |
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time required for a drug to bring about a therapeutic response |
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length of time that the drug concentration is sufficient to bring about a therapeutic response |
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correlate to highest and lowest blood levels of a drug and are an area of therapeutic drug monitoring used to maximize the drug response and minimize the drug toxicity |
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medications are attracted to cell surfaces based on the chemical structures of the medication and the receptor site
when medications bind to a receptor, physiologic processes are affected by either eliciting a cellular response (agonist) or blocking a cellular response (antagonist)
drugs that are most effective are those that mimic endogenous substances
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Definition
these drugs either inhibit or enhance the action of specific enzymes by chemically binding to the enzyme and altering its interaction with its normal targets in the body |
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Nonselective Interactions |
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Definition
these drugs target the cell itself to disrupt the cell membrane or metabolic activites of the cell |
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