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39 Cards in this Set

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