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117 Cards in this Set
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Diagnositc use? Example?
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Use: To aid in examination, evaluation, and diagnosis of patient or patient condition.
Example: Fluorescein |
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Prophylactic use? Example?
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Use: to prevent an illness, infection, complication, adverse effect, etc
Example: Proparacaine |
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Treatment use?
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Used in the therapeutic management of disease or medical conditions
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Pharmacokinetics?
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How drugs are absorbed, distributed, biotransformed, metabolized, and excreted
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Pharmacodynamics?
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Properties of drug effects including time to onset of action, time to reach peak effects, duration of action, expected times for drug clearance. Can be impacted by pharmacokinetic changes
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Therapeutic effect?
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Desired pharmacoligic effects of a drug
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Tolerance?
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Decreased effectiveness of a drug over time with repeated use
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Drug idiosyncracy?
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Unusual or unexpected response to a drug
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Altered absorption?
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When a combination of two or more drugs impedes or inhibits the absorption of one or more of the drugs being taken/administered. Drugs may inhibit absorption of other drugs across physiologic membranes.
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Chelation is an example of what? How does it work?
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Example of altered absorption. Works by aluminum, magnesium, calcium, iron-containing medications irreversibly bind to some antibiotics (ORAL FLUOROQUINOLONES)
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How to avoid chelation?
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Take 1 hour before, or 2-3 hours after offending agent.
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Dicloxacillin prevention of absorption example?
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Full vs empty stomach. Full stoomach = 65% absorp, emmpty = 85-100%.
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Additive effects?
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Response of combined drugs is equal to combined responses of the individual drugs (1+1 = 2).
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Synergism? Example?
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Response of combined drugs greater than combined response of individual drugs (1+1=3). Refers to INTENDED CLINICAL EFFECTS, not ADEs
Example: Vancomycin and gentamicin to treat bacterial endocarditis |
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Potentiation? Example?
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A drug with no principal effect enchances effect of second drug (0+1=2).
Example: Amoxicillin with clavulanate |
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Altered excretion? Example?
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Drugs may act on the excretion site to reduce/enchance excretion of specific drugs.
Example: Mannitol added to cisplatinum (mannitol flushes kidney out) |
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Competition for serum protein binding?
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Drugs that bind to serum proteins may compete with other drugs for the binding sites.
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Oral drugs should be what?
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Acid stable, absorbed and passed through intestinal lining
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Long term effect of diabetes on peristalsis?
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Decreases it
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Things which are necessary on a drug Rx?
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Name/address/number of practioner
Name/Address of patient Date of issue, name of drug Rx'd, quantity Rx'd, directions for use, signature and license certification, TPA # and IF REQUESTED by patient: notice for what condition the drug is for |
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A.C. means?
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before meals
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gtt means?
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drop
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H.S. means?
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at bedtime
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P.O. means?
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by mouth
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PRN means?
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as needed
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qD means?
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DONT USE IT, use qDay...means every day
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STAT means?
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now/immediately
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U.D means?
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as directed
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Half life?
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amount of time it takes for 50% of the serum level of a drug to be eliminated
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Distribution half life?
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decrease in drug serum concentration as the result of metabolic and excretion processes
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Continuous infusion time to reach steady state? Effect of increasing rate of infusion?
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4-5 half lives
Increse serum conc of drug at steady state, but not shorten time it takes to get there |
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Intermittent dose results in what kind of graph?
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Get peaks at troughs
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Onset of action?
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time taken for a drug to begin working
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Duration of action?
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period of time in which conc of drug is in therapeutic range
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How does a drug better pass through plasma membranes?
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Lipid soluble, composed of smaller molecular structure, and are NOT ionized
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Passive diffusion require energy? Carrier? Fast for? Slow for?
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Energy: No
carrier: yes quick for: small, nonionicc, lipohilic slow for: large, ionic, hydrophilic |
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Carrier-assisted diffusion require energy? carrier? How are drugs bound to carriers? Is there competition?
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Energy: no
carrier: yes Bound by noncovalent structurally similar can compete |
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Hydrophilic channels energy? carrier? drugs under what size can do this?
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energy: no
carriers: no MW under 200 can do this |
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Onset of action of tropicamide? Absorbs through what?
Blocks what? From what? |
OoA: 15-20 min
absorbs through cornea Blocks sphincter muscle of the iris and accommodative muscle of the ciliary body Blocks from Ach |
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decreased serum free drug usually means what?
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that there is less available drug to concentrate in target organ
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What medication can deposit in the cornea and affect vision? Can also cause what?
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Amiodarone...NEED missing info from andrea
can also cause optic neuropathy/neuritis |
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True/False: Some drugs are excreted in unchanged form?
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True
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Pharmacologic metabolic processes often result in drugs becoming what and what?
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More polar and more water soluble
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Metabolic processes can result in what 3 forms of a drug?
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Less active forms, inactive metabolites, or a more active drug (from a prodrug)
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phase I reactions?
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drugs are oxidized or reduced to a more polar form
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phase II reactions?
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a polar molecular group is conjugated to the drug, which substantially increases its polarity
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What liver microsomal drug oxidation/reduction system is responsible for the metabolism of many drugs?
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P450 system
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Azo-reduction is a ___ reaction?
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Phase I reduction
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Nitro-reduction is a ___ reaction?
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Phase I reduction
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Hydroxylation is a ___ rxn?
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Phase I oxidation
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Dealkylation is a ___ rxn?
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Phase I oxidation
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Oxidation is a ____ rxn?
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Phase I oxidation
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Polarizing atom exchange is a ___ rxn?
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Phase I oxidation
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Alcohol oxidation is a ___ rxn?
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Phase I non-microsomal rxn
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Alcohol reduction is a ___ rxn?
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Phase I non-microsomal rxn
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What pathway is responsible for nearly half of all CYP (liver drug metabolism) activity?
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CYP3A
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CYP enzymess involved in metabolism of ___% of drugs?
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75%
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What are substrates?
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drugs which are metabolized, at least in part, by one or more CYP enzymes
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What are inducers?
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Drugs that induce the production of one or more CYP enzymes. W/ an inducer you need more and more of the drug to get same effect b/c being metabolized quicker each time. Can effect all drugs metabolized by the induced enzyme.
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When are drug interactions more likely to occur when dealing with CYP system?
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When there are substrates and either inhibitors/inducers of same CYP enzymes
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How to check renal fxn? Which is best?
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BUN, and serum creatinine.
Best is SCr. |
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Liver fxn tests?
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ALT, AST, ALK PHOS
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Drug binding to receptor sites can cause what 4 things?
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Activation of cellular fxn, inhibition of cellular fxn, activation of biochemical processes, opening or closing of ionic channels
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Strength of binding to binding site known as?
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affinity
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Strong agonist?
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causes maximal effects even though it may only occupy a small fraction of receptors on a cell
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weak agonist?
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An agonist which must be bound to many more receptors than a strong agonist to produce same effect
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Mixed (partial) agonist?
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A drug which fails to produce maximal effects, even when all of the receptors are occupied by the partial agonist
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Drug potency? Used to compare?
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Amount of drug required to produce 50% of the maximal response that the drug is capable of inducing.
Used to compare drugs in SAME class |
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Drug efficacy? Used to compare?
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Degree to which a drug is able to induce maximal effects.
Used to compare drugs with different MoA |
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Category B?
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Animal-reproduction studies have not demonstrated fetal risk but there are no controlled studies in pregnant women
OR animal-reproduction studies have shown adverse effect that was not confirmed in controlled studies in women in first trimester |
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Category C?
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Studes in animals have shown adverse effects on the fetus and there are no ccontrolled studies in women
OR studies in women and animals are not available |
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Category D?
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Positive evidence of human fetal risk, but benefits from use may be acceptable despite risk.
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Category X?
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Studies in animals or human beings have demonstrated fetal abnormalities or there is evidence of fetal risk based on human experience or both, and risk outweighs benefit
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Skeletal muscle control during voluntary mvmt and conducts sensory information such as pain and touch?
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Somatic nervous system
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Controls cardiac and smooth muscle contraction, as well as glandular secretion?
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Autonomic nervous system
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Which system increases HR, dilates bronchi, decreases secretions?
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sympathetic nervous system
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NT of sympathetic nervous system?
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dopamine, epinephrine, norepi
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What does parasympathetic nervous system do? Main NT?
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decrease HR, stimulates GI fxn
Acetylcholine |
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Autonomic pathway?
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presynaptic neurons go from brain to autonomic ganglia, transmit NS signals to postsynaptic neurons by released Ach. Postsynaptic neurons transmit impulses to end organs by released norepi (sympathetic) or Ach (parasymp)
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Receptor a1 effects?
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Vasoconstriction of arterioles and veins, decreased glandular secretion, constriction of radial muscle, decreased motility
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Receptor a2 effects?
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Decreased symp outflow from brain, decreased NE release, decreased islet cell secretion
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Receptor B1 effects?
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increased heart rate, increased contractility, increased conduction velocity, increased automaticity
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Receptor b2 effects?
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tracheal/bronchial relaxation, uterine relaxation, circulatory dilation
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What receptors does parasymp system use for Ach to bind to?
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muscarinic
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What do epi and norepi bind to in symp system?
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adrenergic receptors
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ACh role in preganglionic neurons?
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transmits symp and parasymp impulses from preganglionic neurons to nicotinic receptors
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ACh causes what?
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Muscle contraction (causes CA++ influx), and acts as a neurotransmitter in the brain
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alpha receptors location? a1? a2?
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vascular smooth muscle tissue
a1: myocardium a2: larger blood vessels (skin, mucosa, gut, kidney) |
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Stimulation of alpha receptors (SNS) does what?
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arteriolar vasoconstriction
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Beta 1 receptors location? b2?
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b1: located in myocardial tissue and in the cardiac conduction system
b2: Located in vascular smooth muscle tissue in the bronchi and the liver |
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Beta 1 receptors location? b2?
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b1: located in myocardial tissue and in the cardiac conduction system
b2: Located in vascular smooth muscle tissue in the bronchi and the liver |
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stimulation of b1 does what? b2?
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b1: increased cardiac contractility and heart rate
b2: coronary and peripheral vasodilation and bronchodilation |
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stimulation of b1 does what? b2?
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b1: increased cardiac contractility and heart rate
b2: coronary and peripheral vasodilation and bronchodilation |
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M3 receptor is what kind of receptor generally? specifically? Which organs? Effect?
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generally: cholinergic receptor
specifically: muscarinic organs: eye, glands effect: increases glandular secretions, causes miosis and accommodation |
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M3 receptor is what kind of receptor generally? specifically? Which organs? Effect?
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generally: cholinergic receptor
specifically: muscarinic organs: eye, glands effect: increases glandular secretions, causes miosis and accommodation |
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muscarinic peripheral receptor blocker?
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atropine
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muscarinic peripheral receptor blocker?
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atropine
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Beta 1 receptors location? b2?
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b1: located in myocardial tissue and in the cardiac conduction system
b2: Located in vascular smooth muscle tissue in the bronchi and the liver |
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prazosin and terazosin are what?
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alpha 1 specific blockers
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prazosin and terazosin are what?
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alpha 1 specific blockers
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stimulation of b1 does what? b2?
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b1: increased cardiac contractility and heart rate
b2: coronary and peripheral vasodilation and bronchodilation |
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M3 receptor is what kind of receptor generally? specifically? Which organs? Effect?
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generally: cholinergic receptor
specifically: muscarinic organs: eye, glands effect: increases glandular secretions, causes miosis and accommodation |
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muscarinic peripheral receptor blocker?
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atropine
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prazosin and terazosin are what?
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alpha 1 specific blockers
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What is propranolol?
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a beta adrenergic blocker, not b1 or b2 specific
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Timolol is a what?
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b1 blocker
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metoprolol, atenolol, and betaxolol are what?
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b1 blockers
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At high doses of b1 blockers what can happen?
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some b2 effects may be seen
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Exogenous Ach used for? Is a what? Use caution in giving to?
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Used for surgical miotiic agent.
Is a direct stimulant of muscarinic receptors caution in asthma, parkinsons |
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Pilocarpine is a? Used for? Effects?
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Is a direct stimulant of muscarinic receptors
Used for treating OAG Causes miosis, changes aqueous outflow. Same cautions as exogenous ACh. |
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Echothiophate is a? Used for? ADEs?
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Is a cholinesterase inhibitor
Used for OAG, accommodative esotropia in children ADEs: miosis, NVD, convulsions, respiratory depression |
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How to reverse effects of echothiophate?
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Atropine or pralidoxime
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Atropine is a what? Causes what?
contraindicated in? |
parasympatholytic
mydriasis and cycloplegia Contraindicated in narrow-angle glaucoma |
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Scopolamine is a? Causes what? Alternative use? contraindicated in?
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Parasympatholytic
Causes cycloplegia and mydriasis Also used transdermally to prevent motion sickness Contraindicated in children under age 12 (hallucinations), and narrow-angle glaucoma |
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phenylephrine is a what? Acts on what receptor? Causes what?
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sympathomimetic
a1 mydriasis without cycloplegia |
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phenylephrine ADEs? Alternative use?
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increase in blood pressure, dizziness, headache
Other use: for red eyes |
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sympathomimetics acting on a2 used for?
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inhibiting NE release in CNS, and local vasoconstrictive effects
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