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Pharmacology I > Test 1 part III > Flashcards

Test 1 part III Flashcards

1
Q

what are the 2 categories of selectivity

A
  1. beneficial/therapeutic effects
  2. toxic/adverse effects
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2
Q

due to drug selectivity you should administer the ______________ dose that produces an acceptable benefit

A

lowest

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3
Q

due to selectivity of drugs you should consider attacking receptors in different parts of the body to ________________ and ____________

A

achieve a more therapeutic effect; less toxic benefit

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4
Q

what are the 5 basic mechanisms for transmembrane signaling

A
  1. lipid soluble chemical signal (ligand) passively diffuses through the membrane and acts on intracellular receptor
  2. signal binds to extracellular portion of transmembrane protein and activates enzyme activity on the cytoplasmic side
  3. signal binds to extracellular portion of a transmembrane receptor that is bound to a separate protein (cytoplasmic side) –> signal
  4. signal binds to and directly opens an ion channel d/t ion shift
  5. signal binds to a cell surface receptor linked to an effector enzyme by a G-protein
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5
Q

transmembrane signaling that is done through signal binding extracellularly to transmembrane protein and activates enzymatic activity on the cytoplasmic side is often limited by _______________

A

down-regulation

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6
Q

what are the common 2ndary messengers used with G-protein signal transduction

A

cAMP
IP3
cGMP

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7
Q

what is the function of the secondary messenger in signal tranduction of G-coupled protein being IP3 (inositol -1,4,5-triphosphate)

A

Ca2 release
can work with or against cAMP

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8
Q

what is the function of cAMP as the secondary messenger in signal transduction with G protein

A
  1. mobilization of stored energy
  2. conservation of water
  3. Ca2+ homeostasis
  4. increased HR and contraction of the heart
  5. regulates the production of adrenal and sex steroids
  6. relaxation of smooth muscle`
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9
Q

what is the function of cGMP as the seondary messenger in signal tranduction with Gprotein

A

relaxation of VASCULAR smooth muscle

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10
Q

what are the two principle functions of secondary messengers in signal transduction

A
  1. amplification
  2. flexible regulation
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11
Q

________________ is the attachment of a phosphoryl group to an amino acid during signal transduction (from a secondary messenger) that powerfully enhances the signal by recording a molecular memory that the pathway has been activated

A

amplification

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12
Q

_________________ is the part of signal transduction where 2ndary messengers use the presence or absence of particular kinases or kinase substrates to produce different effects in different cell types

A

flexible regulation

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13
Q

_______________ is also called cytosol or cytoplasmic mixture

A

intracellular volume

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14
Q

intracellular volume accounts for _________ of total body water; and extracellular fluid accounts for ___________ of total body water

A

2/3; 1/3

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15
Q

_________________ accounts for 60-65% of total body water

A

intracellular volume

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16
Q

what are the components of extracellular fluid volume

A

plasma volume and interstitial volume

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17
Q

__________________ is your intravascular fluid that is 95% water.

A

plasma volume

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18
Q

what are the contents of plasma volume

A

95% water
also contains dissolved proteins, gluocse, clotting factors, electrolytes, hormones, and CO2

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19
Q

_________________ is described as the fluid around the tissue cells

A

interstitial volume

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20
Q

fluid that accumulates in interstitial spaces = ________________

A

edema

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21
Q

drugs administered IV are distributed to the __________________ compartment then redistributed to the __________________ compartment; then to the ______________________ compartment for elimination

A

central; peripheral; central

22
Q

what is the formula for volume of distribution

A

Vd = amount of drug in body at equilibrium before elimination starts / plasma concentration of drug

23
Q

____________ relates the amount of drug in the body to the concentration of drug in the blood

A

volume of distribution

24
Q

what are the characteristics/properties of drugs with a small volume of distribution (Vd)

A
  1. bind to plasma binding proteins
  2. poor lipid solubility (hydrophillic)
  3. highly ionized
  4. faster elimination
25
Q

properties of drugs with large volume of distribution (Vd)

A
  1. unbound
  2. highly lipid soluble (lipophillic)
  3. non-ionized
  4. drug diffuses into tissues (low plasma concentration)
  5. long terminal half life
26
Q

what are the mechanisms of tissue permeation (i.e. drug absorption)

A
  1. aqueous diffusion
  2. lipid diffusion
  3. active and facilitated transport
  4. endo/exocytosis
27
Q

what characteristics must a drug possess to permeate to the tissues via aqueous diffusion

A

small molecule, unbound, neutrally charged, and hydrophillic

28
Q

tissue permeation through aqueous diffusion is drive by the ________________, but the process is governed by __________________

A

concentration gradient; Fick’s law of diffusion

29
Q

tissue permeation through the cell via passive diffusion down the concentration gradient describes which mechanism

A

lipid diffusion

30
Q

which method/mechanism of tissue permeation utilizes special carriers fixed in the cell to move the drug molecules against the concentration gradient

A

active transport

31
Q

which method/mechanism of tissue permeation utilizes special carriers fixed in the cell to move the drug molecule through the cell with the concentration gradient

A

facilitated diffusion

32
Q

which method/mechanism of tissue permeation utilizes transport proteins to move the drug molecule through the cell

A

endocytosis/exocytosis

33
Q

the larger (via molecular weight) a drug molecule is, the ________________ it is absorbed

A

slower

34
Q

the more lipid soluble a drug is the ___________ it is absorbed

A

faster

35
Q

as molecular weight of different insulin preparations increases, their ___________ also increases

A

onset

36
Q

a drug needs a molecular weight of at least ______________ for good receptor binding; but a MW > ____________, does not diffuse easily through the body

A

100; 1000

37
Q

ionization = lipid _________________

A

INsolubility

38
Q

a drug in its lipid soluble form will be significantly ________________ via passive diffusion during passage down the renal tubule. Thus, the drug will NOT be ________________

A

reabsorbed; eliminated

39
Q

under normal urine pH conditions of 6.0, what drug would be more easily EXCRETED, a weak acid or a weak base ?

A

weak base

40
Q

weak acids are hydrogen ________________ ,and weak bases are hydrogen ____________

A

donors; acceptors

41
Q

muscle relaxants are a quaternary amine (4 C + 1 H), this makes them permanently charged (i.e. ionized), meaning they are lipid ______________

A

insoluble

42
Q

what is the single most important factor for determining drug concentrations

A

clearance

43
Q

the higher the therapeutic index, the ______________ the drug

A

safer

44
Q

the clinically acceptable risk of toxicity (from a drug) depends on what factor?

A

the severity of the dz

45
Q

__________________ theoretical volume of plasma that is 100% cleared of a drug in a given unit of time

A

clearance

46
Q

what are the units clearance is measured in

A

mL/min

47
Q

most drugs are eliminated via _______________________

A

first order kinetics

48
Q

_______________ is a constant fraction of the drug eliminated per unit of time

A

first order kinetics

49
Q

_______________ is a constant amount of drug eliminated per unit of time

A

zero order kinetics

50
Q

clearance is influenced by what factors?

A

drug dose
organ blood flow
liver and kidney function

Pharmacology I (16 decks)

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