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BIOPHARM MIDTERM CHAPTER 1-3 > Chapter 2 Part I > Flashcards

Chapter 2 Part I Flashcards

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1
Q

What are the different mechanisms of drug transport

A

passive : simple and facilitated

active: carried mediated

ion pair

pinocytosis

convection

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2
Q

the passage of molecules through a membrane that does not actively participate in the process

A

passive diffusion

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3
Q

the rate of diffusion or transport across a membrane is proportional to the difference in drug concentrations on both sides of the membrane

this is known as

A

ficks first law

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4
Q

ficks first law is

A

dc/dt = -DA (change in c/ change in x)

D= diffusion coefficient
A = surface area

change in c = concentration gradient
change in x = diffusion distance/thickness

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5
Q

the process of absorption is driven by ___ of a drug across a membrane

A

concentration gradient

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6
Q

concentration gradient of a drug is dependent on its

A

aqueous solubility and formulation

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7
Q

carrier mediated transport is mainly for

A

hydrophilic molecules

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8
Q

carrier proteins are ______

A

integral membrane proteins

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9
Q

_____ undergo a conformational change after binding to the substrate

A

carrier proteins

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10
Q

molecules to be transported bind to and take a ride using a membrane protein known as ___ or ____

A

carriers
transporters

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11
Q

_____ is when carrier mediated process occurs only in the presence of a concentration gradient

A

facilitated diffusion

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12
Q
A
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13
Q

in facilitated diffusion, transporter proteins create a __________ through which ions and small hydrophilic molecules pass

A

water filled pore

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14
Q

T or F each carrier protein is specific to just one type of ion or molecule in active transport

A

T

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15
Q

T or F solutes cannot be transported against their concentration gradient in active transport

A

F, they can be

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16
Q

the requirement of active transport is

A

ATP, source of energy

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17
Q

the rate of active transport is determined by

A

michelis menten equation

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18
Q

what is the michaelis menten equation

A

rate of drug absorption =
(C) x Vmax / Km + (C)

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19
Q

what does Km stand for

A

affinity constant of the drug for the carrier

the concentration of drug that produces 1/2 of Vmax

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20
Q

Vmax is equivalent to

A

the maximal rate of absorption

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21
Q

pore transport is

A

the transport of drug through aqueous pores of the biological membrane

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22
Q

what is a another name for pore transport

A

convective transport

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23
Q

what is the diameter of aq pores

A

7-10 angstrom

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24
Q

what type of molecules can pass through the aq pores

A

only low molecular weight molecules can pass - 150 for spherical and 400 for chain like

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25
what are the rate determining steps in absorption of orally administered drugs
rate of dissolution rate of drug permeation through the biomembrane
26
T or F absorption can still take place if there is no dissolution
F, no dissolution = no absoprtion
27
drug in particle form to drug in solution form is
dissolution
28
drug in solution form to drug in blood is
permeation
29
what form of a drug has very limited dissolution
tablet form
30
what form of a drug has the best dissolution
once it has been disintegrated to small particles
31
what is lipinskis rule of 5
a guideline that predicts if a chemical compound can be an orally active drug
32
What is lipinskis rule of 5
1 - Molecular weight drug MW is inversely proportional to drug permeability (<500dA) 2 - lipophilicity LogP drug liphophilicity is directly proportional to drug permeability (does ` exceed 5) 3,4 - number of hydrogen bond donors and acceptors is inversely proportional to drug permeability (no more than 10 H bond acceptors all N or O, no more than 5 H bond donors N-H or O-H)
33
poor permeation and poor absorption happens when
MW > 500 daltpns Lop P is greater than 5 more than 5 h bond donors more than 10 H bond acceptors POLAR SURFACE AREA IS GREATER THAN 140 A2
34
according to lipinskis rule of 5, there may not be more than ___ violation to be an orally active drug
one
35
T or F lipinksis rule of 5 is not applicable for substrates of transporters and natural products
T
36
rates of dissolution and absorption of a variety of drugs are related to their ____
ionization constants
37
particle size affects dissolution rate, ___ and F
absorption
38
which kind of drug can get through the lipid membrane? ionized or non ionized
non ionized
39
why does a non ionized drug get through the membrane more easily
higher lipid solubility
40
a drug dissolves more rapidly when the surface area is increased or decreased?
increased
41
reducing or increasing particle size increases surface area
reducing
42
increased surface area leads to faster
dissolution
43
how can you reduce particle size
miling pulverizing grinding
44
what are the exceptions to decreasing particle size and decreasing solubility
tetracycline - enough solubility erythromycin - destroyed in the gut, small particle size is disadvantage extended release tablets
45
particle size has significant influence on which six drugs
griseofulvin nitroflurantoin spironolactone tolbutamide procaine penicillin
46
the ability of a substance to crystallize into two or more different crystal forms is known as
polymorphism
47
In polymorphism, each of of the crystal forms have the same _____ but different _____ in the crystal lattice
chemical structure conformations
48
T or F physical properties, solubility, and rate of dissolution can be different for different polymorphs
T
49
The energy required for a molecule of drug to escape from a crystal is ______ than it is required to escape from an amorphous powder
much greater
50
the amorphous form of a compound is always ___ soluble than a corresponding crystal form
more
51
the thermodynamically most stable form of a pharmaceutical solid is more or less soluble
less soluble
52
a ______ polymorph is more soluble but less stable
metastable
53
do dissolution rates vary with different salt forms
yes
54
which salt form has the highest solubility
sodium, NAa
55
the measure of a drug's lipophilicity and an indication of its ability to cross cell membranes is
partition coefficient
56
is partition coefficient oil/water or water/oil
oil/water
57
Partition (P) is also known as
distribution coefficient (D)
58
distribution coefficient is
the ratio of concentration of a compound in the two phases of a mixture of two immiscible solvents at equilibrium
59
Po/w =
(Coil/Cwater)equilibrium
60
the partition co efficent is the ratio of concentrations of a _____ compound between an aqueous and organic solvent
unionized
61
how is partition coefficient measured
measured by adjusting the pH so that compound remains predominantly in the unionized form in the solvent
62
lopP is
the log of the ratio of concentrations of the unionized solute in the solvents
63
a drug is lipophilic when P is
greater than 1
64
when P is less than 1 the drug is
hydrophillic
65
membrane permeability is the rate of
drug transport across a biological membrane
66
what information does membrane permeability provide
absorption characteristics of the drug
67
if ionization increases what happens to polarity, partition coefficient, and permeation
increases, decreases, decreases
68
if ionization decreases, what happens to polarity, partition coefficient and permeation
decreases, increases, increases
69
according to FDA, a drug is considered ______ when its highest clinical dose strength is soluble in 250 mL of aq media over a pH range 1-7.5 at 37.5 C
highly soluble
70
according to FDA, a drug is considered _______ if the absorption or an orally administered dose in humans is greater than 90% when determined usng mass balance or in comparison to an IV reference dose
highly permeable
71
Class I drugs are
highly soluble and permeable
72
Class II drugs are
low solubility and highly permeable
73
Class III drugs are
high solubility low permeability
74
Class IV drugs are
low solubility low permeability
75
what is the dosage form approach for Class I drugs
simple solid oral dosage form
76
what is the oral dosage form approach for class II drugs
techniques to increase surface area like particle size reduction, solid solution, solid dispersion or solutions using solvents and surfactants
77
what is the oral dosage form approach for class III drugs
incorporate permeability enhancers to maximize local lumenal concentration
78
what is the oral dosage form approach for class IV drugs
class II and III approach combned
79
from class I to IV, what are the chances of non oral dose being required
increasing chances
80
what are some class I drugs
chloroquine diltiazem metoprolol paracetamol propranolol theophylline verapamil
81
what are some class II drugs
carbamazepine danazol gilbenclamide ketoconazole nifedipine phenytoin troglitazone
82
what are some class III drugs
acyclovir atenolol catopril cimetidine metofrmin neomycin B ranitidine
83
What are some class IV drugs
coenzyme Q cyclosporin A ellagic acid furosemide ritonavir saquinavir taxol
84
what is the list of slowest to fastest absorption in terms of formulation
tablets capsules powders suspensions emulsion liquids
85
tablets are disintegrated from ____ to ____
granules, fine particles, dissolution, drug in solution to drug in blood
86
what are the formulation factors?
dosage form excipients phosphate tablet hardness vs disintegration table coating product age and storage conditions
87
T or F product aging and imporper storage have no effect on bioavailibility
F it does adversely
88
what are some physiologic factors
area of absorptive surface vascularity pH presence of other substances GI motility functional integrity of absorptive surface diseases
89
in case of shock, what route is preferred?
IV
90
vasoconstrictors restrict the
absorption of local anesthesias
91
increase in vascularity increases the
rate and extent of absorption
92
T or F aid pH favors acidic drug absorption, basic pH favors basic drugs
T
93
Do pathophysiologic conditions such as burns increase or decrease the permeability of drugs across the skin
increase
94

BIOPHARM MIDTERM CHAPTER 1-3 (4 decks)

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