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Pharmacology
Primary Care Provider 3 Part II
Question | Answer |
---|---|
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) |