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163 Cards in this Set
- Front
- Back
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the study of the absorption, distribution, metabolism and excretion of drugs (what the body does to the drug)
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Pharmacokinetics
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the formulation and preparation of drugs
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Pharmaceutics
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the study of the economic impact of drugs
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Pharmacoeconomics
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the study of the harmful effects of chemicals
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Toxicology
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the study of the medicinal uses of naturally occurring compounds
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Pharmacognosy
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the preparation and dispensing of drugs
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Pharmacy
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genetic influences by and on drugs
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Pharmacogenetics
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physiological and biochemical mechanism of action of drugs
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Pharmacodynamics
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identifies discrete genetic differences among individuals that play a critical role in drug response
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Pharmacogenomics
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bind to a receptor and block the function that receptor serves
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Antagonists
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bind to a receptor and stimulate the function that receptor serves
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Agonists
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competes with normal chemicals found in the body for place on receptor
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competetive
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when the amt of the drug falls below the natural chemical level the drug falls off the receptor and is replaced by the natural chemical
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competitive antagonist
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bind and do their job but never come off
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noncompetitive antagonists
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TD50
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Toxic dose in 50% of the population
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LD50/ED50
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Therapeutic Index
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____ the therapeutic index the safer the drug.
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Higher
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Therapeutic index of 1 means...
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the same dose that causes an effect might also kill someone.
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Name the bonds from strongest to weakest.
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Covalent
Ionic Hydrogen Hydrophobic Van der Waals |
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How many half lives does it take to get full elimination of the drug?
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4
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describes the attraction the drug has for the target receptor
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Potency (affinity)
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The _____ the affinity the weaker the attraction-need to give more drug.
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lower
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describes whether the drug has the ability to produce the effect you want
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efficacy
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What four things does the dose response curve tell you?
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potency (affinity), efficacy, variablity, slope
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states that the amount will vary depending on things such as time of day given, amt of sleep person has, anxiety, etc.
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variability
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indirect measure of the safety
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slope
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What is the therapeutic range?
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range that you need to have an effect without any toxicity
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stimulation of cells with agonists that results in state of desensitization
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down regulation
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administration of an antagonist that results in an increase in the number of receptors
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up regulation
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alteration in the therapeutic action of a drug by concurrent administration of other exogenous chemicals.
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interaction
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the combined effect of two drugs acting via the same mechanism is equal to that expcted by simple addition of their individual actions
1+1=2 |
addition
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the combined effect of two drugs is greater than the algebraic sum of their individual effects
1+1=3 |
synergism
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the enhancement of the action of one drug by a second drug that has no detectable action of its own
1+0=3 |
potentiation
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the action of one drug opposes the action of another
1+1=0 |
antagonism
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the pH at which the drug will exist in solution as 50% ionized and 50% unionized
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pKa
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bases in acidic pH are...
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ionized
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pKa is a measure of
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ionization
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drugs that are water soluable are...
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ionized
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pH=pKa
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50% ionized/ 50%unionized
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A change in the tissue sensitivity to a drugs action due to an adaptive mechanism
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functional tolerance/ pharmacodynamic tolerance
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A change in the drug level due to an adaptive change in the absorption, distribution, metabolism or excretion of the drug (ie enzyme induction or inhibition)
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Dispositional tolerance/ pharmacokinetic tolerance
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activates a receptor but cannot produce a maximum response. It may also be able to partially block the effects of full agonists.
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Partial agonist
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the relationship between the number of receptors stimulated and the response is usually nonlinear. A maximal or almost maximal response can often be produced by activation of only a fraction of the receptors present.
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Spare receptor concept
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A molecule that is able to bind and form a complex with a receptor to produce a biologic response.
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Ligand
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the liver makes more enzymes to help metabolize the drug if it is in the body consistantly
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enzyme induction
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the liver makes less enzymes that lead to less metabolism of drug leading to an increase in their effects
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enzyme inhibition
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places glucuronic acid on the drug-when the glucose goes through the kidneys and is eliminated in the urine it drags the grug along with it
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conjugation
can also be coupled with glycine, acetate, sulfate, and others |
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What phase metabolism is conjugation and synthesis?
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Phase 2
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What phase metabolism is oxidation, reduction and hydrolysis?
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Phase 1
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This type of metabolism typically forms inactive and readily excretable products
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Phase 2
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These types of reactions can form chemically reactive products that can be toxic or carcinogenic
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Phase 1
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this type of metabolism is catalyzed by the cytochrome P-450 system of enzymes
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oxidative
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the addition of water to an ester or amide to break the bond and form two smaller molecules.
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hydrolysis
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Phase 1 reactions usually result in a ______ compound that is easily excreted by the kidneys.
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more polar
transforms a lipid-soluable compound to a water-soluable one |
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In phase 1 reactions, by placing a ______ or _____ group on drug molecules it enables phase 2 reactions to occur.
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hydroxy or carboxy
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Nonionized forms are lipid soluable which means they can diffuse across cell membranes such as the blood-brain barrier, gastric, and placental barriers. T/F
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True
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Ionized molecules are unable to penetrate lipid cell membranes because...
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of their low lipid solubility. This is a result of the electric charges on the molecules that repel sections of the cell membranes with similar charges, preventing their diffucsion across the membrane.
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proton donors
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acids
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proton acceptors
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bases
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What is the neurotransmitter released by the sympathetic preganglionic nerve?
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ACh
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What is the neurotransmitter released by the parasympathetic preganglioinic nerve?
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ACh
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What is the neurotransmitter released by the sympathetic postganglionic nerve?
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NE
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What is the neurotransmitter released by the parasympathetic postganglionic nerve?
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ACh
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What are the receptor sites at the preganglionic synapse of the sympathetic nerve?
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nicotinic cholinergic
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What are the receptor sites at the preganglionic synapse of the parasympathetic nerve?
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nicotinic cholinergic
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What are the receptor sites at the postganglionic synapse of the sympathetic nerve?
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Adrenergic receptors
alpha beta dopamine |
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What are the receptor sites at the postganglionic synapse of the parasympathetic nerve?
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muscarinic cholinergic receptor
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If you give a drug that mimics NE at the postganglionic sympathetic site the drug is called what?
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sympathomimetic
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If you give a drug that blocks an alpha, beta, or dopa receptor it is called what?
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sympatholytic
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Another way to say adrenergic agonist is...
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sympathomimetic
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Another term for adrenergic antagonist is...
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sympatholytic
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Two other terms for parasympatholytic are...
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anticholinergic or antimuscarinic
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A drug that mimics ACh at the muscarinic receptor on the postganglionic parasympathetic neuron is called what?
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parasympathomimetic
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A drug that blocks a muscarinic receptor site at the parasympathetic postganglionic synapse is what?
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parasympatholytic
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parasympathetic is
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stimulatory
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sympathetic is
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inhibitory
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from the beginning of induction to the loss of consciousness
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Stage 1 (analgesia)
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from the loss of consciousness to onset of automatic rhythmicity of vital signs and response to stimulation is exaggerated
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Stage 2 (excitement)
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from the end of Stage 2 to end of respiration
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Stage 3 (surgical anesthesia)
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cessation of respiration to death
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Stage 4 (medullary paralysis/ death)
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loss of consciousness
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stage 1
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loss of lash reflex
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stage 3
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loss of cornea reflex
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stage 3
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complete analgesia
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stage 1
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loss of airway reflexes
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stage 3
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overdose
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stage 4
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hypertensive, tachycardic
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stage 2
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loss of tracheal reflex
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stage 3
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loss of pain
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stage 1
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relaxed muscle tone
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stage 3
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The ____ you breath the _____ you go to sleep.
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faster; faster
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concentration effect
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The higher the concentration the faster it works (faster you go to sleep)
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property of anesthetic drug that will tell you the speed of induction and emergence
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blood gas coefficient
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Ventilation perfusion deficit ______ the delivery of all anesthetics. The drugs that have a ___ blood/gas coefficient are affected more than the ______ drugs.
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slows; low; slower
(the faster the drug works the more you will notice a difference) |
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If you give two gases at the same time, the fast drug will make the slow drug go in faster than it would if it were being given alone.
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Second gas effect
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What is the only drug that can be given to produce the 2nd gas effect?
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Nitrous Oxide
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What are the 6 factors that are related to the lungs that effect the induction time?
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Ventilation
Concentration Blood gas solubility V/Q problems Second gas effect N2O diffusions into closed spaces |
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What happens to the induction time if there is an increase in the cardiac output?
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makes the patient go to sleep slower. It affect the slow induction agents (those with high blood gas solubility) more than the faster agents.
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The higher the gas flow rates via the anesthesia machine...
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the faster the anesthetic will reach the patient thus the faster the patient will go to sleep.
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MAC of Sevoflurane
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2
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Blood/Gas Partition Coefficient:
Sevoflurane |
0.6
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Oil/Gas Partition coefficient:
Sevoflurane |
50
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the minimum alveolar concentration required to achieve surgical anesthesia in 50% of patients exposed to a noxious stimulus
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MAC
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The ___ the blood/gas coefficient the faster the rise of the anesthetic in the lungs.
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lower
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What happens to the FA/FI ratio the faster you breath? how does this effect the rate of induction?
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the FA/FI ratio increases causing you to go to sleep faster
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How is alveolar concentration of the gas related to the brain concentration?
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Alveolar concentration = brain concentration of the agent
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FA-fraction in the alveoli shows...
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how much gas is in the lungs
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FI-fraction of inspired gas show what?
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How much the dial is adjusted to
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Name areas/situations that would be problematic with the use of nitrous oxide.
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pneumothorax
bowel obstruction inner ear surgery neurosurgical procedures with air injections air embolism ocular surgery that requires gas injection (within 4 wk of surgery) |
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Increase in cardiac output ____ the onset of all anesthetics. The agents with the _____ blood/gas coefficients are affected the most.
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Slows; highest (those that are more soluable-slower to induce)
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State why the induction time is longer when the cardiac output is increased.
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If more blood passes through the lungs, more blood is available to remove anesthetic and therby lower the FA/FI ratio.
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Term that describes how much of the drug you administer will get into the blood.
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bioavailability
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What is the main purpose behind metabolizing drugs in the liver?
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to make then water soluable so they can be excreted in the kidneys
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If someone is enzyme induced this means they will metabolize drugs...
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faster.
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If someone takes a drug that is an enzyme inhibitor, it means they will metabolize some drugs...
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slower.
(There be more of a drug effect because the drug is hanging around longer) |
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If someone is an alchoholic, they will require (more/less) drug. Why?
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More because they are enzyme induced. They have more enzymes which metabolize drugs faster requiring more drug.
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If someone is enzyme induced this means they will metabolize drugs...
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faster.
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Liver metabolizes most of the drug and only releases some of it into the blood stream
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First pass metabolism
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How do you avoid the first pass metabolism effect with drugs?
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don't give as an oral medication
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What are the two reasons for tolerance?
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Functional tolerance and
Dispositional tolerance |
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What percentage of the cardiac output goes to the vessel rich group?
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75%
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What percentage of the cardiac output goes to the muscles?
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19%
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What percentage of the cardiac output goes to the fat?
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6%
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Never give less than ___ % O2 when under anesthesia.
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30%
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Oil/gas partition coefficient is an indication of...
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the potency of the anesthetic.
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The (higher/lower) the number the more potent the anesthetic.
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higher
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The more potent the drug the (more/less) drug you have to give.
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less
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The greater the alveolar ventilation, the faster the patient achieves anesthesia.
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Ventilation effect
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The higher the concentration of anesthetic delivered, the faster anesthesia is achieved.
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Concentration effect
(also referred to as overpressuring) |
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The indicator of an anesthetic's speed of onset and emergence. The higher the coefficient, the ____ the anesthetic.
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Blood/gas solubility coefficient
slower |
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The indicator of an anesthetic's potency. The higher the coefficient the _____ potent the agent.
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Oil/gas solubility coefficient
more |
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The phenomenon in which two anesthetics of varying onset speeds are administered together. A high concentration of a ____ anesthetic such as N2O is administered with a ____ second anesthetic gas. The _____ gas achieves anesthetic levels more quickly than if it had been given alone.
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Second gas effect;
faster; slower; slower |
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Occurs when high concentrations of N2O are administered. At the end of the procedure when N2O is discontinued, it leaves the body very rapidly, causing a transient dilution of the O2 and CO2 in the lungs. Hypocarbia and hypoxia may occur.
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Diffusion hypoxia
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_____ in cardiac output ____ the speed of onset of all anesthetics. The _____ soluble anesthetics are affected to a much greater extent than the ______ soluble anesthestics. This is called the _________.
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Increases; decrease; more; less
Cardiac output effect |
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Ventilation-perfusion abnormalities ______ the speed of onset of all anesthetics and affect the _____ soluble agents to a much greater degree than the ______ soluble agents.
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less; more
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Do children go to sleep faster or slower than adults? Why?
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Children achieve anesthesia more rapidly because of a higher respiratory rate and vessel rich group blood flow. However, the required doses are higher in children.
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What affect does obesity have on receiving anesthetic agents?
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Obesity has minimal clinical effects on anesthetic induction; however, emergence may be slower due to the deposition of anesthetics in fat. (also called the reservoir effect)
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State the amount Sevoflurane that is metabolized by the body.
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Sevoflurane 5-7%
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ED50
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effective dose in 50% of the population
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LD50
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lethal dose in 50% of the population
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acids in acidic pH are...
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nonionized
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bases in basic pH are...
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nonionized
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acids in basic pH are...
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ionized
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Drugs that are lipid soluable are...
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nonionized
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MAC of isoflurane
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1.15
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MAC of Nitrous Oxide
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105
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MAC of Desflurane
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5.8
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MAC of Halothane
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.075
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Oil/Gas Partition coefficient:
Isoflurane |
99
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Oil/Gas Partition coefficient:
Nitrous Oxide |
1.4
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Oil/Gas Partition coefficient:
Desflurane |
18.7
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Oil/Gas Partition coefficient:
Halothane |
224
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Blood/Gas Partition coefficent:
Isoflurane |
1.4
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Blood/Gas Partition coefficent:
Nitrous Oxide |
0.47
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Blood/Gas Partition coefficent:
Desflurane |
0.42
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Blood/Gas Partition coefficent:
Halothane |
2.3
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Another name for Isoflurane
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Forane
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Another name for Desflurane
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Suprane
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Another name for Halothane
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Fluothane
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State the amount of Isoflurane that is metabolized by the body.
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<1%
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State the amount of Desflurane that is metabolized by the body.
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<0.1%
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State the amount of Nitrous Oxide that is metabolized by the body.
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Trace amounts
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Another name for Sevoflurane
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Ultane
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