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39 Cards in this Set
- Front
- Back
How does totally body water % of body weight change with age.
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From infants to elderly, it decreases with age.
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How does the fraction of lipophilic drug in fatty tissue change with age
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From infant to elderly, it increases with age.
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How do liver metabolism and renal elimination of a drug change with age?
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Infants and elderly are both less than young adults.
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How will the [] over time of a drug differ between an infant and adult if given IV? Sub Q?
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For IV, adult will decrease [] in blood faster in a exponential fashion while the infant will be slower and linear.
For Sub Q, both adult and infant will have [] resembling a bell curve but the adults will occur quicker and with a lower peak and shorter overall duration. |
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Dose adjustment for weight
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Does required = average does/70 kg x weight of individual.
Does not work for abnormally lean or obese people. |
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Tolerance
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Decreased responsiveness acquired after prior or repeated exposures to a given drug or one closely related in pharmacologic activity.
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Tachyphylaxis
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Acute tolerance acquired during repeated administration of a drug in short intervals, possibly due to depletion of a stored pool of a mediator.
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Pharmacokinetic Tolerance
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When a drug reduces its own absorption or transfer across some barrier, or increases the rate of its own elimination. Could be produced by another drug as well.
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Pharmacodynamic or cellular tolerance
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Reduction in reactivity of the receptor or translation of binding to a biological response. Opposite of supersensitivity.
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Homologous vs Heterozygous Desensitization
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Homologous - Give a drug that works on receptor A, get tolerance. Give a drug that works on receptor B, no tolerance to drug B.
Heterzygous - Give a drug that works on receptor A but creates tolerance for Drug A and Drug B which works on a different receptor. |
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What types of drugs are especially susceptible to tolerance.
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Drugs which effect the nervous system.
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Pathological variables in drug dosage
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Most pharmacokynetics data is derrived for healthy individuals yet drugs are usually given to unhealthy individuals, therefore diseases may effect the drug effect.
Ex. chnages in Body temp, hydration, ph. |
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Idiosyncrasy
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A quantitative and qualitative abnormal drug response with genetic abnormality usually being the underlying mechanism.
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Succinylcholine
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Muscle relaxant used in surgery.
Genetic basis for idiosyncrasy: Defective plasma cholinesterase Disease trait: persistent apnea and paralysis Inheritance: Autosomal Autonomous |
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Isoniazid
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Genetic basis for idiosyncrasy: Deficient acetyltransferase
Disease trait: Increased toxicity Inheritance: Auto recessive |
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Primaquine/antimalarial/sulfonamide/probenecid/chloramphenicol
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Genetic basis for indiosyncrasy: Deficient G-6PD in erythrocytes
Disease trait: Drug induced hemolytic anemia Sex linked |
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Summation
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When 2 drugs elicit the same overt response but by different mechanisms and yet their combination is the algebraic sum of their individual effects.
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Additive Effect
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When the combined effect of drugs which act via the same mech are equal to that predicted by simple addition.
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Synergism
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Joint effect of 2 drugs that is greater than the algerbraic sum of their individual effects.
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Antagonism
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The conjoint effect of 2 drugs is less than the sum of the effects of the drugs acting separately.
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Pharmacological Antagonism
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When one drug prevents the response of another by preventing it from combining with its receptor.
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Physiological Antagonism
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When two drugs acting at different sites couterbalance each other by producing opposite effects on the same phisiological function.
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Biochemical Antagonism
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When one drug indirectly decreases the amount of a second drug present at its site of action.
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Chemical antagonist
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The reaction between 2 drugs to create an inactive product.
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Tetracycline antibiotics
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Have drug interactions which deal with GI absorption.
If mixed with (Al 3+, Ca 2+ Mg 2+ ect (found in milk)) will cause reduced absorbtion of antibiotic due to formation of poorly soluable chelates. |
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Digitalis
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Have drug interactions which deal with GI absorption.
If combined with propantheline or other anticholinergics, will reduce aborption due to reduced gut motility. |
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Anticholinergics + Antichlinergics
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Enhanced anticholinergic effects. Can cause heat stroke, toxic psychosis, and adynamic ileus.
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CNS depressants + CNS depressants
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Enhanced CNS depression; drowsiness
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Neuromuscular blockers + Neuromuscular blockers
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Enhanced neuromuscular blockade, prolonged apnea.
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Beta-adrenoreceptor stimulating bronchodilator + non-selective Beta 2 adrenoreceptor blocker
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Bronchodilator effects antagonized.
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Oral anticoagulants + Barbituates
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Anticoagulent effects reduced via induction.
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Oral contraceptives + Barbiturates, Phenytoin, Rifampicin
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Contraceptive reliability reduced via induction.
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Phenytoin + Chloramphenicol/Disulfiram
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Increased serum phenytoin levels due to enzyme inhibition.
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Pharmaceutical or chemical equivalents
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Drug products that contain identical amounts of the same active ingredient.
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Bioequivalent drug products
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Pharmeceutical equivalents whose rate and extent of absorption seem to be the same.
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Bioavailability
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Rate and extent to which the active drug is absorbed from a drug product and becomes available at the site of drug action.
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Therapeutic equivalence
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2 or more pharmaceutically equivalent drugs produce the same efficacy and toxicity in the same individuals under the same dose.
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Problems with absorbtion, Distribution, biotransformation, and excretion in an infant.
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Absorbtion - Altered absorbtion
Distrib - Incomplete BBB, higher volume of distribution for water soluble drugs Biotransformation - Lower rate of oxidative Rxs and glucuronidase conjugation Excretion - Reduced excretion |
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Problems with absorbtion, Distribution, biotransformation, and excretion in an elderly person
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Distribution - Higher volume of fat soluable drugs stored
Biotransformation - Reduced oxidative metab (no change in glucuronidation) Excretion - Reduced capacity |