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Pharmacology

Primary Care Provider 3 Part II

QuestionAnswer
Women Creatinine Clearance = wt (kg) x (_______ )/72 x serum creatinine (mg/dl)(x _____) 140-age in years, 0.85 (2/19)
Women have an ________ in body fat. Men have a lean body muscle which could mean a _______ creatinine clearance. increase, higher (2/19)
REMEMBER LEAN BODY MASS MATTERS Creatinine Clearance (2/19)
Men Creatinine Clearance = wt (kg) x (__________)/72 x serum creatinine (mg/dl) 140-age in years (2/19)
Drugs and their metabolites are excreted through _______ and ______, through ____ _____, and in other ways. fecal, respiratory routes, breast milk pg 31 (2/20)
Drugs are metabolized in liver and excreted in bile. Metabolites are also reabsorbed into the blood and excreted in urine, or _______. Consider patients w hepatic insufficiency or failure. Feces pg 31 (2/20)
What route is important in the excretion of anesthetic gases? Respiratory route, has to be breathed out pg 31 (2/20)
Routes of excretion not clinically significant breast milk (not for Mom),________,_______, tears, hair, & _______. saliva, tears skin pg 31 (2/20)
Measure of the rate at which the drug is removed from the body. Clearance pg 31 (2/22)
Vd - volume of distribution affects ________ and ________. clearance, half-life pg 31 (2/22)
Stable concentration of the drug or the drug is being administrated at the same rate at which it is being eliminated. Steady state pg 31
Drugs in adipose tissue are _____ cleared. NOT (2/22)
Administration rate equals elimination rate. Steady state (2/23)
The frequency and amount of the drug must be adjusted to achieve steady state such as Parkinson's medications, ie carbidopa/levodopa (Sinemet). Intermittent administration pg 31 (2/23)
Time between when the drug is given and when it first takes effect is the ________. Latent period pg 31.
Time it first takes effect. Onset of action pg 31
When the drug no longer has an effect, this is known as ____________. termination of action pg 31
During period of time which the drug has its effect. Duration of action pg 31
Minimal Effective Concentration Lowest level of concentration that produces the drug effect pg 31
Highest level the drug reaches. Peak plasma level pg 31
If concentration is high enough to cause ADRs, this level is known as __________. Toxic Level, pg 31
Area between the minimal effective concentration and the toxic concentration. Therapeutic range, pg 31
The amount of time required for the amount of drug in the body to decrease by one half. Half-life of a drug, pg 31 (2/23)
Ibuprofen Benzodiazepine lorazepam
The amount of time required for the amount of drug in the body to decrease by one half. Half-life of a drug, pg 31 (2/23)
Ibuprofen Benzodiazepine lorazepam
Half-life matters - monitor drugs with long half-lives (toxic effects & ARs last a long time). First-Order & Linear Kinetics pg 31 (2/25)
Elimination does not depend on dose or concentration of drug. Nonlinear kinetics or zero-order kinetics pg 32 (2/25)
When the amount of drug concentration exceeds the ability of the liver to metabolize the drug, ______ ______ occurs. nonlinear kinetics pg 32 (2/25)
What kinetics is this? Amount eliminated is constant More difficult to maintain therapeutic range Require close monitoring for toxicity ie phenytoin, theophylline Zero-order/nonlinear kinetics pg 32 (2/25)
A _____ ______ ________ makes toxicity a frequent problem. narrow therapeutic window pg 32 (2/25)
Study of biochemical and physiologic effects of drugs and the mechanisms of their action. THE EFFECT OF THE DRUG ON THE BODY. Pharmacodynamics pg 32 (2/25)
HOW DRUGS MOVE AROUND IN THE BODY Pharmacokinetics (2/26)
Component of the organism that binds to a ligand and produces a change in function in the body. Receptor pg 32 (2/27)
Drugs, neurotransmitters, and hormones are known as ____________. Ligands pg 32 (2/27)
Drugs generally do not create an effect by themselves but through a _________. Receptor pg 32 (2/27)
Propensity of a drug to bind or attach itself to a given receptor site. Drug affinity pg 32 (2/28)
Drug that has affinity for and stimulates physiologic activity or cell receptors normally activated by naturally occurring substances. Agonist pg 32 (2/28)
What drug receptor? Creates biologic response Depends on number of receptors Agonist pg 32 (2/28)
What drug receptor? Blocks or reverses effect of agonist, but has no effect on its own. Antagonist pg 32 (2/28)
Chemical fits receptor site well; chemical response is usually good. Agonist pg 33
Drug attached at drug receptor site but then remains chemically inactive; no chemical drug response is produced. Antagonist pg 33
Drug attached at drug receptor site but only a slight chemical action is produced. Partial agonist pg 33
These drug interactions with a receptor are reversible. Agonist drug interactions pg 33
Drug's ability to produce a therapeutic or intended effect. Efficacy pg 33
The amount of drug in the body that is able to bind the receptor drug not bound to plasma proteins. Free drug pg 33
Dependency of effect on its concentration Potency pg 33
Is a drug more potent than another if less drug is needed to achieve the desired effect? Yes pg 33
Binds to a receptor to inhibit the action of a drug but has no intrinsic action of its own. Antagonist pg 33
Inhibition overcomed by the increased concentration of the agonist. Competitive antagonist pg 33 (2/28)
Prevents the action of the agonist at any concentration. Noncompetitive antagonist pg 33 (2/28)
Actions not mediated by receptors. Interaction with molecules or ions ie Antacids neutralize gastric acid. Non-receptor Drugs (2/29)
Drugs with structures close to normal biologic chemicals incorporated into cellular components; thus altering function, ie Purines. Non-receptor Drugs (2/29)
Any undesirable experience associated with the use of a drug or medical product in a patient. Adverse Event pg 33 (2/30)
Defined by WHO as a response to a drug that is noxious and unintended and occurs at doses normally used for man for prophylaxis, diagnosis, or therapy of disease, or for the modification of physiologic function. ADRs - Adverse Drug Reactions pg 33 (2/30)
Is this a ADR or SE? Undesirable experience associated with a drug, incidence about 28%. ADR (2/30)
Is this a ADR or SE? Probably requires additional care, can be life threatening, ie Pancytopenia from chloramphenicol. ADR - Adverse Drug Reactions pg 33 (2/30)
An additional effect, desirable or undesirable, of a drug that is not the primary purpose of giving the drug. SE - Side effect pg 33 (2/30)
Is this a ADR or SE? Think more mildly troublesome, probably not requiring additional care ie Photosensitivity caused by tetracycline. SE - Side effect pg 33 (2/3)
FDA definition of _______ _______. Events r/t use of a drug: Caused congential abnormality Life-threatening event Required intervention to prevent permanent damage Resulted in death, hospitalization, disability Serious Adverse Drug Reactions pg 34 (2/31)
Serious ADRS are voluntary reported to _____ _____ ____ ____ ______ _______. FDA Medical Products MedWatch Reporting Program: Call (800)FDA-1088 or fax (800)FDA-0178 (or(301)816-8532) pg 37 (2/31)
Hepatotoxic Drugs Nephrotoxic Drugs Drugs Associated with Serious Adverse Effects pg 38, box 3-2, (2/31)
Other Toxicities Anaphylaxis Asthma Blood dyscrasias Damage to 8th cranial nerve Eye Damage Peripheral neuritis Serious Adverse Effects - pg 38, box 3-2 (2/31)
Excessive degree of desired effect or unintended severe SE, ie hypoglycemia from insulin Inherent pharmacologic effect (2/32)
Signs and symptoms of an immunologic response Allergic reaction (2/32)
Inflammation Local irritant effect (2/32)
Inherent pharmacologic effect Allergic reaction Local Irritant effect Types of Adverse Drug Reactions (2/32)
Serious warning requiring drug mfger to print a warning displayed in heavy type and boxed text at the beginning of the package insert. The Black Box pg 37
Each person has a specific genetic composition that may be activated in the P450 enzyme system during metabolism. Precipitation of genetic disorders pg 43 (2/33)
Unintended consequences on other natural substances in the blood or may alter various laboratory tests. ie change color of urine or feces. Drug effects on laboratory tests and blood substances pg 44 (2/33)
Attempts to correlate the peak of drug activity with when it is needed by the body. Chronotherapy pg 44 (2/33)
Controls rhythms in endocrine gland secretion, metabolic processes, and behavioral activity. Cyclic variations caused by these processes often are demonstrated by normal temperature changes throughout the day. Circadian Clock pg 44 (2/33)
Food and drug interactions may occur from activation of the _______ enzyme system or from competition with ________ sites. P450, receptor pg 38 (2/34)
What affects.... Body processes Activation of the P450 enzyme system Competition with receptor sites Food and Drug Interactions (2/34) pg 38
What do these Food and Drug Interactions do? Monoamine oxidase inhibitors Caffeine Competition with receptor sites pg 39 (2/34)
Alters the effectiveness of a drug by altering its availability. ALCOHOL PG 40 (2/35)
What does this pertain to? A single drink Competes with drug for same set of metabolizing enzymes Prolongs and enhances drug's availability Can increase risk of harmful side effects. Acute Dose of Alcohol pg 41 (2/35)
What does this pertain to? May activate drug-metabolizing enzymes. Decreasing drug availability/diminished effects Enzymes remain after absence of alcohol Affects metabolism of drugs for several wks May need higher dose of some medications Chronic (long-term) Alcohol Ingestion pg 41 (2/35)
Enzymes activated by chronic ______ consumption transform some drugs into toxic chemicals that can damage the liver or other organs. alcohol pg 41 (2/35)
What can magnify inhibitory effects of sedatives & narcotics at their sites of action in the brain? Alcohol pg 41 (2/35)
Antacids Antihistamines Nasal decongestants Nicotine replacement products Pain relievers Weight control products Major OTC drug categories used pg 43 (2/36)
Key points about which medicine? People don't consider these as drugs Forget to list them Caution with narrow therapeutic window CAM - Complementary Alternative Medicines or Herbal, OTC pg 43 (2/36)
Most frequent is _________ and less frequent is _________ for toxicity and overdose. Accidental, intentional pg 44 (2/37)
What type of toxicity/overdose is this? Repeat doses Confusion Failure to adjust medication Unsupervised children Accidental Toxicity or Overdose pg 44 (2/37)
AE or treatment failure from taking a drug vs. potential benefit Amount of "acceptable" risk pg 45 (2/38)
Decision regarding what? Educate about drug and R/B Consider severity of disease Consider health literacy Patient and provider joint decision about Risk-Benefit Ratio pg 45 (2/38)
It is a measure of drug safety. Calculated by dividing the toxic (or lethal) dose by the therapeutic (or effective) dose. Therapeutic Index pg 46 (2/39)
Therapeutic index = LD50/ED50 LD50 is the toxic or lethal dose in 50% of the population ED50 is the effective or therapeutic dose in 50% of the population pg 46 (2/39)
Describes the range between the lowest therapeutic concentration and the beginning of toxicity. Therapeutic Window pg 46 (2/39)
What is? Target level dosing Therapeutic Window pg 46 (2/39)
A desired or target steady-state concentration of the drug (usually in plasma) is identified, and a dosage is computed that is expected to achieve this value. Target Level Dosing pg 46 (2/39)
Narrow Therapeutic Window _______ increased monitoring importance to avoid bad outcomes. Equals - Key point about therapeutic window pg 46 (2/40)
Lower limit of the therapeutic range appears to be approx. = to drug concentration that produces about 1/2 of the greatest possible therapeutic effect. Target Level Dosing, the therapeutic objective pg 46 (2/41)
Upper limit is fixed by toxicity, not by efficacy. Target Level Dosing, the therapeutic objective pg 46 (2/41)
Upper limit is no more than 5% to 10% of patients will experience a toxic effect. Target Level Dosing, the therapeutic objective pg 46 (2/41)
What do these relate to? Target level (response) Loading dose Maintenance dose Individualizing dose Therapeutic drug monitoring Calculating the Therapeutic Index pg 46 (2/41)
What does this relate to? Nonpharmacologic therapy is always FIRST! Ensure a clear indication for a specific purpose Start Low and Go Slow Lowest effective dose Only one drug whenever possible Simplify the regimen Use S/E profile 1 drug to tx Practical Application of Pharmacokinetics and Pharmacodynamics to Drug Prescribing pg 47 (2/42)
What does this relate to? Monitor therapeutic effects closely Keep good records Use caution w drugs assoc. w AEs Consider interactions & AEs when assess Stay up-to-date Look it UP! Practical Application of Pharmacokinetics and Pharmacodynamics to Drug Prescribing pg 47 (2/42)
Created by: mareed3