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66 Cards in this Set

  • Front
  • Back
what does exercise or stress cause? (concerning norepi & epi)
- inc norepi release from sympathetic nerve terminals --> inc in widespread sympathetic tone in target organs
- inc epi release from adrenal medulla --> inc in widespread sympathetic tone in target organs
what are the naturally occuring catecholamines?
what is a sympathomimetic?
a drug which mimics the action of either epi or norepi (NE)
which adrenergic receptor is selectively agonized by dobutamine (dobutrex)?
what is/are the most important b1 site(s)?
-heart --> inc HR & contractility
-kidney --> inc renin secretion
which adrenergic receptor is selectively agonized by albuterol, metroproterenol (alupent)?
what is/are the most important b2 site(s)?
-bronchial tree --> bronchodilation
-skeletal muscle --> vasodilation
which adrenergic receptor is seletively agonized by phenylephrine?
what is/are the most important a1 site(s)?
-skin & skeletal muscle --> vasoconstriction
-nasal mucosa --> vasoconstriction --> decongestion
-nasal glands --> dec secretions
which adrenergic receptor is selectively agonized by clonidine, methyldopa and others?
what is/are the most important a2 site(s)?
-vasomotor center-medulla --> dec HR & BP
what are the classic sympathomimetic drugs?
what does epi do?
inc BP by 1) positive inotropy & chronotopy which --> CO and 2) potent a1 vasopressor action in many vascular beds
what does a positive inotropy cause?
causes the heart to beat more forcefully
what does NE do?
-same effects as epi
-inc TPR --> inc systolic and diastolic BP
what does isoproterenol do?
-same effects as epi on the heart but...
-has only b1 and b2 activity, no a activity, therefore...
-potent bronchodilator
-inc HR and contractility
-slight inc in systolic BP due to inc CO
-may be used in cardiogenic shock
what type of adrenergic activity does isoproterenol have and which does it lack?
only has b1 and b2 activity, lacks a activity
what does dopamine do at low doses?
-renal vasodilation
-no change in TPR
-used to keep kidneys working in cardiogenic shock
what does dobutamine do?
-has selective b1 action
-used in cardiogenic shock for its positive inotropy
what are other sympathomimetics that are not catecholamines, but are similar in structure?
what does phenylephrine do?
-mydriatic (a1) and decongestant (a1)
what does ephedrine do?
-pressor agent (a1) used:
-intra-operatively if BP is low
-in chronic orthostatic hypotension
-as a decongestant (a1)
-release of stored catecholamines
-enters the CNS --> mild amphetamine-like stimulation
what does oxymetazoline do?
-decongestant (a1)
what does amphetamine do?
-release of store catecholamines
-enters CNS well --> stimulates mood and alertness, depresses apetite
what does methamphetamine do?
-enters CNS well --> stimulates mood and alertness, inspires motorcycle gangs
what does phenylpropanolamine do?
-weak amphetamine variant, therefore a weak mood stimulant
-safe as an appetite suppressant, but may cause severe HTN in large doses
why were the sympathomimetics involved in the Fen-Phen diet withdrawn from the market?
too many cases of valvulopathy and/or pulmonary hypertension.
what does methylphenidate do?
used for ADHD in children
what is another name for methylphenidate?
what does pemoline do?
used for ADHD in children
what is another name for pemoline?
what is adderall?
used for adult ADHD
what does cocaine do?
-a local anesthetic with sympathomimetic action because it decreases NE reuptake at synapses
-enters CNS very well
what are the adverse side effects of cocaine?
-MI & stroke
-dec fetal brain development
-other fetal abnormalities
what are the 4 sympathomimetics that make your nose feel good?
what is the most common decongestant? the least common?
-pseudoephedrine - MOST COMMON
-oxymetazoline - LEAST COMMON
what sympathomimetic is used as a therapeutic application for asthma and COPD?
-b2 agonists
what is the prototype sympathomimetic for asthma and COPD?
what can cause "palpitations" in a patient?
b2 agonists
anaphylactic shock is what type of hypersensitivity reaction?
-type I, IgE-mediated
what does anaphylactic shock cause?
-bronchospasm & hypersecretions --> bad dyspnea
-cardiovascular collapse
-can happen to anyone you give any drug or perscription to
what is the drug of choice for tx anaphylactic shock?
-epi because it causes vasoconstriction (a1), stimulates heart (b1), bronchodilation (b2)
-also give antihistamine (benadryl inj.) and a steroid
what is the tx for HTN?
-clonidine (catapres) & methyldopa (aldomet) are a2 agonists
how do a2 agonists effect HTN?
-cause 1) inc in vagal parasympathetic act to the heart --> slows it and dec it contractility & 2) a dec in sympathetic activity to the heart and peripheral vasculature --> dec HR and contractility further & dec TPR by dilating vessels
-all of which dec BP
what is given for premature labor?
-ritodrine and terbutaline, which are b2 agonists --> relax the uterus
what is pharmacokinetics?
describes the movement of a drug around the body
what happens after a drug is administered?
What Parameters Do We Use To Describe the “Fate of a Drug”?
•Volume of distribution (VD)
•Clearance (Cl)
•Half-life (t ½)
•Bioavailability (F)
•Protein binding (PB)
what is pharmacokinetics?
"what the body does to the drug"
what is pharmacodynamics?
"what the drug does to the body"
what is Volume of Distribution (Vd)?
•The “apparent” volume in which the drug is distributed
•Actually relates the amount of drug in the body to the measured concentration in the plasma (or blood)
what is the equation for Vd?
Vd = dose / Co
what is clearance?
•Volume of plasma (or blood) from which drug is removed (or cleared) per unit time
what is hepatic clearance?
–Volume………cleared by the liver
what is renal clearance?
–Volume………cleared by the kidney
t/f: clearance is usually constant
what is the equation for total clearance?
Cl(hepatic) + Cl(renal) + Cl(lung) + Cl(other organs)
what is half-life?
•Time taken for drug concentration to decline by one-half
•Refers to elimination or terminal half-life
what is fractional availability?
• The fraction of unchanged drug reaching the systemic circulation following administration
•For IV administration, F = 1
•For oral administration, F is often < 1
what is first pass effect?
•The fraction or percentage of an orally administered drug removed on the first pass through the gastrointestinal wall and/or liver before reaching the systemic circulation
–First Pass = 1 – fractional bioavailability
what is an example of alternations in absorption?
what is chelation?
•Irreversible binding of drugs in the GI tract
•Tetracyclines, quinolone antibiotics - ferrous sulfate (Fe+2), antacids (Al+3, Ca+2, Mg+2), dairy products (Ca+2)
•Usually separating administration of chelating drugs by 2+ hours decreases interaction effect
•Dose tetracycline 1 hour before or 2 hours after dairy products
what is Interindividual Variability?
•There are wide interindividual differences in drug metabolizing ability which may arise from genetically determined differences in the basal level of expression of an enzyme
•Poor metabolizers will have high plasma concentrations of parent compounds and low concentration of metabolites
what are the most common single agent drug interactions?
what are the Dose-Effect Parameters?
POTENCY: The sensitivity of an organ or tissue to the drug
EFFICACY: The maximum effect
what is the dose response curve?
-relates the amount administered to the response
-response may be measured as % responding or as intensity of response.
-it's sigmoidal in shape