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32 Cards in this Set
- Front
- Back
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body fat
muscle liver kidney bone |
What are some "other storage sites" for distribution of drug?
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other storage sites
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often requires more drug
may be redistributed to and from storage sites low vascularity of adipose causes it to saturate more slowly...may pull drug from brain, etc. |
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Kg
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Distribution of dose given per ____ of body weight.
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Metabolism
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aka biotransformation
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Metabolism
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The chemical alterations of a drug by the body.
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Metabolism
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-usually done by liver (also blood enzymes, intestinal mucosa, skin, lung, etc.)
Smooth ER or microsomal fraction acts to oxidize drug, reduce drug or conjugate drug with other molecule. (cytochrome P450 group most common: note that it is inducible) -usually changed to less active chemical -if changed to more active form, that form is ususally later metabolized again to a less active form. -often new chemical is more ionized and, therefore, more readily eliminated (not reabsorbed) |
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liver
skin Smooth conjugate inducible less eliminated |
-usually done by ______(also blood enzymes, intestinal mucosa, _____, lung, etc.)
_______ ER or microsomal fraction acts to oxidize drug, reduce drug or ________ drug with other molecule. (cytochrome P450 group most common: note that it is __________) -usually changed to ____ active chemical -if changed to more active form, that form is ususally later metabolized again to a less active form. -often new chemical is more ionized and, therefore, more readily __________(not reabsorbed) |
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Pathology
Age Genetic Drug exposure |
What are some "special patient considerations" for metabolism?
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hepatic
renal cardiovascular |
What is the pathology that you need to look for before inducing P450 system?
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Age
Special patient considerations P450 system (metabolism) |
Infants: immature enzyme systems
aged: degenerating enzyme systems |
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Genetic
(special patient considerations) (metabolism) |
Some individuals are more or less able to metabolize a drug.
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Drug exposure
(special patient considerations) metabolism |
may depress or activate liver
- other prescribed medications may affect biotransformation -alcohol and tobacco use both induce the P450 system -currently prescribed drug may enventually cause "metabolic" tolerance |
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Tolerance
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effectiveness of a dose decreases (more required to maintain effect).
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biotransformation
induce metabolic |
may depress or activate liver
- other prescribed medications may affect ______________ -alcohol and tobacco use both ______ the P450 system -currently prescribed drug may enventually cause "__________" tolerance |
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Excretion
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Drug eliminated from the body.
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Possible routes of Excretion
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kidney
bile to feces (note: enterohepatic circulation possible) sweat glands saliva lungs mother's milk |
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acidic
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Milk is more ______ than plasma so it ionizes or "traps" alkaline drugs.
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cumulative effects
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For any drug, knowing excretion rate is important if to avoid ___________ _______.
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Renal excretion rate
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______ _________ _____ for drugs depends upon health of kidneys and: filtration, secretion, and reabsorption.
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kidneys
filtration secretion reabsorption |
What does renal excretion rate depend on?
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filtration
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depends upon good circulation (GFR)
concentration of unbound drug in plasma |
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secretion
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often by active transport and carrier mediated
depends upon drug maturity of the individual (infants, aged etc) |
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reabsorption
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often passive
fat soluble vs. water soluble size and shape of water soluble molecule ionization and the effects of pH |
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Clearance
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ml/min or L/hr
calculated volume of fluid in the body This calculation is more informative than simply measuring the amount removed because it compensates for plasma concentration. |
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renal clearance
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Physiologist refers to "______ _________" - how effective is the kidney.
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total clearance
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Pharmacologist refer to "_____ __________" = metabolic + renal + other excretion.
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clinicians
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In practice, ________ use "renal clearance" to estimate individual patient renal function.
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Physiological state of the patient
Pathological state "Receptor" or "cellular" tolerance |
What does the ability of the active site to respond to a given concentration surrounding the receptors depend on?
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Physiological state of the patient
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-diurnal rhythms (sleeping pill)
-hormonal preparation |
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Pathological state
(The active site response differs) |
digitalis works better on failing heart
aspirin decreases body temperature only if elevated. |
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"Receptor" or "cellular" tolerance
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"down regulation" at receptor level
In addition to increased biotransformation, sometimes the body acquires capacity to function "normally" even when blood concentration of a drug is still high. *Receptor # may change. *Internal responses (perhaps in second messenger system) may change * Leads to physical dependence on the drug. |
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receptor
blood concentration physical |
"down regulation" at ________ level
In addition to increased biotransformation, sometimes the body acquires capacity to function "normally" even when _____ __________ of a drug is still high. *Receptor # may change. *Internal responses (perhaps in second messenger system) may change * Leads to ________ dependence on the drug. |
