Term
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Definition
| Disintegration, Dissolution, Rate limiting |
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Term
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Definition
Drug movement to achieve a drug action.
absorption, distribution, metabolism/biotransformation, excretion |
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Term
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Definition
drug action: onset, peak, duration.
Receptors, enzymes, hormones |
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Term
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Definition
| breakdown into a liquid form for absorption. Pharmaceutic |
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Term
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Definition
| dissolving into small particles in the GI fluid. Pharmaceutic |
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Term
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Definition
| Time required for the drug to disintegrate and dissolve. Time can be effected by factors such as ph or coating on the tablet. Pharmaceutic |
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Term
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Definition
| movement of drug particles from the GI tract to the body fluids. Done by 3 mechanisms: passive, active and pinocytosis |
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Term
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Definition
| completed by diffusion, movement from higher to lower concentration. Lipid soluble drugs |
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Term
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Definition
| requires a carrier such as an enzyme or protein. Water soluble drugs |
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Term
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Definition
| process by which cells carry drugs across their membranes by engulfing the drug particle. |
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Term
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Definition
| gi membrane composed of mostly lipids and protein, drugs that are lipid soluble pass rapidly through the GI membrane via passive absorption. |
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Term
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Definition
lipid soluble and nonionized
(blood flow, pain, food, fasting and pH can affect absorption) |
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Term
First-pass effect
Absorption |
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Definition
| some drugs do not go from the GI system into the systemic circulation, but pass directly to the liver where they are metabolized. (Less drug effect) Coumadin, Morphine, Lidocaine and Nitroglycerin. Many of these are not given by mouth due to first pass, you would need large amounts of the drug to get an effect. |
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Term
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Definition
| percentage of drug that reaches the system circulation and therefore can cause an effect. IV yields 100% bio availability. can be effected by the form of drug, gi mucosa, food, pH and changes in liver metabolism. |
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Term
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Definition
| drug becomes available to the body tissues, influenced by blood flow, and protein binding. |
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Term
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Definition
is inactive, only free drug is active and can caous a pharacologic response.
Elavil, Valium, Inderal, Kilantin (vind to protein albumin)malnutrition and low albumin can cause increased effect of the drug because of less binding sites and more free drug. If 2 highly protein bound drugs are given they will compete and on drug will be free and cause an increase effect. |
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Term
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Definition
| drugs are rendered inactive, liver organ of metabolism. Metabolism decreased potential for increase drug and toxicity. |
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Term
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Definition
| time for 1/2 of drug to be eliminated. the longer the 1/2 life, the longer drug is active in the body. digoxin 36hrs, valium 30-80 hrs, dilatin 10-40 hrs |
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Term
Biotransformation
Metabolism |
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Definition
drug metabolism that occurs in the liver
Phase 1 oxidation reaction
Phase 2 Conjugation |
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Term
Phase 1
Oxidation reaction
Metabolism/Biotransformation |
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Definition
| effected by aging and therefore drug clearance is reduced. Valium, barbituates, ibuprofen, demerol, and benzodiazepines. Cytochrone p-450 isoenzyme system is most common system of metabolism catalyzes oxidation or phase 1. (make chemicals more reactive so they can be excreted)substances which induce cytochrome 450 would result in decreased drug. 18 subfamilies of cytochrome 450 and each metabolize different drugs. Different drugs effect cytochrome 450 system and therefor the metabolis of each other is part of the science behind drug-drug interactions. |
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Term
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Definition
| elimination, major route of elimination is urine, therefore the kidney is the major organ of excretion |
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Term
| Factors affecting excretion |
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Definition
| urine pH, alkaline promotes excretion of acid drugs. Aspirin overdose (weak acid) to hasten excretion sodium bicarbonate is given to make urine a weak base. effected by kidney function. |
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Term
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Definition
| most accurate measurement of how well the kidney is functioning. Creatinine clearance decreases with age. (elderly 60ml/min) drugs are excreted more slowly. 24 hour urine, normal 85-135ml/min |
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Term
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Definition
| study of the drug on cellular physiology and biochemistry and the mechanism of action. Primary and secondary effect. |
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Term
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Definition
| onset the time drug starts to work is called the minimum effective concentration., peak action is the highest concentration of the drug., duration is the length of time drug has a pharmacological effect. |
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Term
Time Response Curve:
Duration of action |
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Definition
| MEC reached at T1 and maintained until T3. T2 is peak concentration. Onset is T0-T1, drug is not effective until MEC is reached. |
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Term
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Definition
| most found on cell membranes, proteins, glycoproteins and enzymes. |
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Term
Receptor Theory
Ligand inding domain
4 receptor systems |
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Definition
site on the receptor where the drug binds.
first on or in the cell membrane system. 2)drug opens a ligand gated ion channel (sodium or calcium channel). 3)the G protein requires an enzyme to work. 4) transcription requires activation of DNA inside the cell. |
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Term
| G protein Coupled Receptor |
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Definition
| drug activates the receptor which activates the G protein which activates the pharmacological effect. |
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Term
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Definition
initiating a response on receptors
Example of Isuprel stimulates beta 1 receptors. |
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Term
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Definition
| Blocking a response. Tagamet is an H2 it blocks histamine 2 receptors. |
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Term
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Definition
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Term
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Definition
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Term
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Definition
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Term
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Definition
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Term
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Definition
| Atropine is antichlinergic and would block effects increased heart rate, increased BP, decreased gastric secretions, dilated bronchioles and dilated pupils. |
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Term
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Definition
alpha1 blood vessels increased b/p
beta1 heart increase heart rate
beta2 relax bronchioles |
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Term
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Definition
stimulate
inhibition or kill
irritation
replacement |
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Term
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Definition
| activate enzymes or hormones |
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Term
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Definition
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Term
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Definition
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Term
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Definition
margin of safety of a drug
ration of effective dose to lethal dose and the closer the number is to 1 the greater the toxicity. |
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Term
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Definition
| narrow margin of safety and will need close monitoring (blood levels) Ex. Dilantin or Digoxin |
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Term
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Definition
| between the minimum effective concentration (mec) and the minimum toxic concentration. Digoxin has a narrow therapeutic range (.5-2.0 ng/ml) |
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Term
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Definition
| highest concentration and measures absorption. |
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Term
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Definition
| lowest plasma concentration and measures elimination or excretion. always immediately befor the next dose of medicine. |
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Term
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Definition
| meaning a large initial dose is given to reach the MEC quicker |
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Term
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Definition
| physiological effects not related to the desired effects |
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Term
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Definition
| first undesirable side effect, mild to severe, such as anaphylaxis |
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Term
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Definition
| drug is above the therapeutic range |
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Term
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Definition
| drug tolerance due to repeated doses. |
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Term
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Definition
| altered/modified action or effect of a drug. (adverse, drug incompatibility) |
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Term
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Definition
| Absorption: gastric emptying, gastric pH, drug complexes |
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Term
Narcotics
absorption of drug |
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Definition
| can decrease gi motility, increasing the absorption of other drugs. |
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Term
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Definition
| Higher gastric pH, slow gastric emptying, increased body surface (compared to weight), some drugs are absorbed quicker. (penicillin) Many drugs are based on body surface area. |
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Term
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Definition
| decrease in gastric acidity, blood flow to GI, gastric motility, gastric emptying. Lead to decreased absorption of some drugs. |
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Term
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Definition
| Serum Proteins, highly protein bound drugs: coumadin, pheytoin/valproic acid, and NSAIDs |
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Term
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Definition
| increased proportion of water to muscle, fewer protein binding sites and therefore highly bound drugs must be give to children in small doses with caution. Blood brain barrier not fully developed, drugs may increase CNS effects in children |
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Term
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Definition
| decrease in body water, albumin, glycoproteins. water soluble be more concentrated, highly protein bound drugs or 2 protein bound drugs at one time must be monitored closely. increased effect of these drugs. |
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Term
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Definition
| increase metabolism: cause decrease drug effect. (barbiturates increase beta blockers) |
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Term
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Definition
| decrease metabolism: cause increase drug effects. (erythromycin)Theophylline, Coumadin and tegretol |
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Term
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Definition
| hepatic metabolism is immature until age 1. 1/2 life of drug can be prolonged. |
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Term
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Definition
| Phase 1 oxidation reduced in elderly (can cause multiple drug interactions) all drugs in Phase 1 should be used with careful monitoring (Barbituates, Ibuprofin, Codeine, Valium, Demerol, Coumadin, Lidocaine and some bezodiazepines |
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Term
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Definition
| certain drugs can increase or decrease excretion. Quindine and lasix decrease excretion of digoxin can cause toxicity. Benemid decreases excretion of penicillin. |
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Term
| Changes in pH affects excretion |
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Definition
| alkaline urine promotes excretion of acid drugs such as aspirin and acid promotes excretion of alkaline drugs like Quinidine. |
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Term
| Glomerular filtration rate |
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Definition
| measure of kidney function is 30-40% that of an adult and therefore elimination or excretion is severely decreased. (antibiotics and analgesics) |
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Term
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Definition
| decreased blood flow, GRF, kidney function |
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Term
Pharmacodynamic
additive effect |
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Definition
| 2 drugs result in the sum of 2 drug effects, aspirin and coumadin together caus increased blood thining. |
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Term
Pharmacodynamic:
synergistic effect |
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Definition
| 2 drugs that potentiate each other, phenergan given with demerol increases the effect of demerol. |
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Term
Pharmacodynamic
Antagonistic effect |
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Definition
| effect blocking the effects of another drug |
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Term
| Pharmacodynamic: Pediatric |
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Definition
immaturity of organs in newborns
receptor site sensitivity differs |
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Term
| Pharmacodynamic: Geriatric |
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Definition
| altered receptor response, frequently the dose needs to be altered. Start Low go slow |
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Term
| Substitutions for elderly: Hypnotics |
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Definition
no dalmane, doral
yes prosom, serax,restoril |
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Term
| substitution for elderly: Diuretics |
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Definition
No aldomet, clonidone
yes Ca channel blockers and ace inhibitors |
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Term
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Definition
Coumadin, digoxin
antibacterials: no aminoglycosides, vancomycin
GI: no tagamet, pepcid
antidepressants SSRI's preferred |
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Term
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Definition
| dairy products most common never given with Tetracyclines. Grapefruit juice and cholesterol lowering drugs should never be given together. |
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Term
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Definition
electrolyte changes may also interfere with drug action.
low potassium increases the chances of digoxin toxicity. increased Ca Digoxin. HydroDIURIL promotes K loss Digoxin |
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Term
Drug disease interactions
albuterol
lasix
prednisone
ibuprofen |
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Definition
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Term
| Drug induced photo sensitivity |
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Definition
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Term
OTC Drugs
Ibuprofen
OTc cough Medicines
Aspirin Tylenol |
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Definition
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