Pharmacology Competency 1

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The Ideal Drug

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Effectiveness, safety, selectivity, reversible action, predictability, ease of administration, low cost, chemical stability...
No drug is ideal.

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Pharmaceutical Phase

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Includes Disintegration and Dissolution. Drug becomes a solution so it can cross biologic membrane. Skipped when given by parenteral or subq.

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Disintegration

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Tablet breaks into smaller pieces

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Dissolution

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Smaller pieces are dissolved into liquid. Drugs in liquid form are already in solution.

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Rate limiting

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the time it takes the drug to disintegrate and dissolve to become available for the body to absorb.

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Enteric coated drugs

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resist disintegration in gastric acid of stomach so it has extended release when it does not disintegrate till it hits alkaline environment of small intestine

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Pharmacokinetics

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the process of drug movement to achieve drug action. Four phasess are absorption, distribution, metabolism, and excretion.

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Absorption

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movement of drug particles from GI tract to body fluids by passive absorption, active absorption, or pinocytosis.

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Passive Absorption

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mostly by diffusion, (movement from high concentration to lower concentration). Does not require energy to move across membrane.

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Active Absorption

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requires a carrier such as an enzyme or protein to move the drug against a concentration gradient. Energy required.

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Pinocytosis

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Process by whihc cells carry a drug across their membrane by engulfing the drug particles

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Lipid soluble

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GI membrane composed mostly of lipid and protein so lipid soluble pass rapidly through. aborbed faster than water soluble and ionized.

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Water soluble

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needs a carrier, either an enzyme or protein to pass through the membrane.

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First Pass (hepatic) effect

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some drugs pass to the liver before systemic circulation via the portal vein. Such as Warfarin and morphine.

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Bioavailability

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subcategory of absorption. percentage of administered drug dose that reaches systemic circulation. occurs after absorption and hepatic drug metabolism. for oral its less than 100% but for IV its usually 100%.

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Absorption factors

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the drug form, route of admin, GI mucosa motility, food and other drugs, changes in liver metabolism caused by dysfunction or inadequate hepatic blood flow. Age, pregnancy, disease state.

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Distribution

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Process by which drug becomes available to body fluids and body tissues. Influenced by blood flow, drugs affinity to the tissue, and protein binding effect. dose and concentration in body.

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Protein Binding effect

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high protein bound, moderate high, moderate, and low. When a percent of the drug binds to proteins such as albumin, the bound drug becomes inactive until the free drug is eliminated and then it can be released from the protein.

Hint 18

Check protein binding percentage of all drugs administered to client. Also check client plasma protein and albumin levels.

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Metabolism

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Can be metabolized in both the GI tract and liver, liver is primary.

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Half-life

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time it takes for one half of the drug concentration to be eliminated.

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Creation Clearance

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Most accurate test to determine renal function. Metabolic by-product of muscle that is excreted by the kidneys. when creatinine clearance is decreased, durg dosage likewise may need to be decreased. Normal creatinine clearance is 85-133 mL/min

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Pharmacodynamics -

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study of drug concentration and its effects on the body.

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LFT

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Liver function test used to check metabolism

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Onset of action

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time it takes to reach the minimum effective concentration (MEC) after the drug is administered

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Peak action

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drug reaches its highest blood or plasma concentration

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Duration of action

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length of time the drug has a pharmacological effect

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Time-response curve

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evaluates three parameters of drug action: the onset of drug action, peak action, and duration of action.

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Chrytochrome p450

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works as catalysts to the process that breaks down drugs. Enzymes can be inhibited which is longer drug activity. induced is shorter. Grapefruit juice.

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Metabolic enzymes

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smoking and alcohol cause less of drug reaction, longer to heal wounds, less affected by the drug

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Agonist

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drugs that produce a response

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antagonists

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drugs that block a response

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Excretion

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mainly from kidneys, labs BUN and creatinine, decreased renal function leads to increase in duration and intensity of meds. increased BUN can be false high due to dehydration

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Therapeutic index (TI)

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estimates the margin of safety of a drug through the use of a ratio that measures the effective dose in 50% of persons or animals and the lethal dose in 50% of animals. the close the ratio is to 1 the greater the toxicity.
TI= LD50/ED50

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Low therapeutic index

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narrow margin of safety. plasma drug levels need to be monitored.

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High therapeutic index

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wide margin of safety less danger of producing toxic effects.

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Therapeutic range

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drug concentration in plasma should be effective in concentration in the plasma for obtaining desired drug action and min toxic concentration.

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Peak drug level

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highest plasma concentration of drug at a specific time. indicate rate of absorption.

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Trough drug level

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lowest plasma concentration of a drug, measures the rate at which the drug is eliminated. Drawn immediately before the next dose of drug is given, regardless of route.

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Loading dose

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large initial dose given to achieve a rapid minimum effective concentration in plasma.

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Pharmacogenetics

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scientific discipline studying how the effect of a drug action varies from a predicted drug response because of genetic factors or hereditary influence.

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Tachyphylaxis

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rapid decrease in response to the drug. "acute tolerance" can be narcotics, barbiturates, laxatives, psychotropics.

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placebo effect

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psychological benefit from a compound that may not have the chemical structure of a drug effect.

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to avoid toxic effects the nurse needs to know

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half-life, protein-biding percentage, normal side effects, and therapeutic ranges of the drug.

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special considerations with children

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gastric pH more alkaline, skin has thinner, smaller muscle mass, decreased plasma protein in infants, incomplete development of blood brain barrier, liver immaturity, decreased renal excretion, dosage adjustments, dose by weight and age.

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special considerations for older adults

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absorption time is slower and delayed, decreased plasma proteins, decreased body water, decreased liver and renal functions, smaller muscle mass. health problems, cognitive problems, sensory changes, financial concerns, difficulty managing

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idiosyncratic reactions

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occur rarely and unpredictably in the population. the cause is not known. sometimes they are listed as an adverse side effect but very rare

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paradoxical reaction

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when a drug has the opposite effect to what you would imagine. like add medicine causes a child to become hyper.

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teratogenic

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can harm or influence a growing fetus