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[MT 6314] - 1st Shifting > Intro 7.5 - 10.5 > Flashcards

Intro 7.5 - 10.5 Flashcards

1
Q

PHARMACOKINETIC PRINCIPLES:

Inactive precursor. They need to be activated by passing through the liver

A

Prodrug

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2
Q

PHARMACOKINETIC PRINCIPLES:

Must be administered and converted to the active drug by biologic process inside the bodyz

A

Prodrug

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3
Q

PHARMACOKINETIC PRINCIPLES:

T/F: To reach its receptors and bring about biologic effect. A drug molecule (eg, sedative) must travel from the site of administration (eg, gastrointestinal tract) to the site of action (eg, brain)

A

True

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4
Q

PHARMACOKINETIC PRINCIPLES:

2 Movements of Drugs in the Body

A

Permeation
Water and Lipid Soluble Drugs

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5
Q

5 Permeation
- Movement of drug molecules into and within the biologic environment

A

○ Aqueous diffusion
○ Lipid diffusion
○ Transport by special carriers
○ Endocytosis
○ Exocytosis

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6
Q

Movement of molecules through the watery
extracellular and intracellular spaces

○ Aqueous diffusion
○ Lipid diffusion
○ Transport by special carriers
○ Endocytosis
○ Exocytosis

A

Aqueous diffusion

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7
Q

Occurs within the LARGER aqueous compartments of the body (eg: interstitial space, cytosol, etc.) and across epithelial membrane tight junctions and the endothelial lining of blood vessels

○ Aqueous diffusion
○ Lipid diffusion
○ Transport by special carriers
○ Endocytosis
○ Exocytosis

A

Aqueous diffusion

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8
Q

The capillaries of the brain, testes, and some other tissues have no pores that permit aqueous diffusion.
○ They may also contain high concentrations of drug export pumps (MDR pump molecules).
○ Hence, they are protected or “sanctuary” sites from many circulating drugs.

○ Aqueous diffusion
○ Lipid diffusion
○ Transport by special carriers
○ Endocytosis
○ Exocytosis

A

Aqueous diffusion

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9
Q

can permit molecules as large as MW 20,000 - 30,000

○ Aqueous diffusion
○ Lipid diffusion
○ Transport by special carriers
○ Endocytosis
○ Exocytosis

A

Aqueous diffusion

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10
Q

Membranes of capillaries with small water filled pores. Passive process

○ Aqueous diffusion
○ Lipid diffusion
○ Transport by special carriers
○ Endocytosis
○ Exocytosis

A

Aqueous diffusion

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11
Q

Driven by the concentration gradient of the permeating drug

○ Aqueous diffusion
○ Lipid diffusion
○ Transport by special carriers
○ Endocytosis
○ Exocytosis

A

Aqueous diffusion

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12
Q

A downhill movement (Governed by Fick’s law)

○ Aqueous diffusion
○ Lipid diffusion
○ Transport by special carriers
○ Endocytosis
○ Exocytosis

A

Aqueous diffusion

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13
Q

Aqueous diffusion:

Fick’s Law Formula

A

Rate = C1 - C2 x Permeability coefficient / Thickness x Area

C1 - higher conc
C2 - lower conc

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14
Q

Movement of molecules through membranes and other lipid structures

○ Aqueous diffusion
○ Lipid diffusion
○ Transport by special carriers
○ Endocytosis
○ Exocytosis

A

Lipid diffusion

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15
Q

Most important factor for drug permeation because of the large number of lipid barriers that separate the compartments of
the body

○ Aqueous diffusion
○ Lipid diffusion
○ Transport by special carriers
○ Endocytosis
○ Exocytosis

A

Lipid diffusion

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16
Q

Aside from Aqueous diffusion, it is also passive process and governed by Fick’s law

○ Aqueous diffusion
○ Lipid diffusion
○ Transport by special carriers
○ Endocytosis
○ Exocytosis

A

Lipid Diffusion

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17
Q

Drugs transported across barriers by mechanisms
that carry similar endogenous substances: Amino acid, peptides, glucose

○ Aqueous diffusion
○ Lipid diffusion
○ Transport by special carriers
○ Endocytosis
○ Exocytosis

A

Transport by special carriers

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18
Q

Special carrier molecules function for:
- substances important in cell function;
- too large or too insoluble in lipids to diffuse passively through membranes ○ eg: peptides, amino acids, and glucose.

○ Aqueous diffusion
○ Lipid diffusion
○ Transport by special carriers
○ Endocytosis
○ Exocytosis

A

Transport by special carriers

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19
Q

Capacity is limited and not governed by Fick’s law

○ Aqueous diffusion
○ Lipid diffusion
○ Transport by special carriers
○ Endocytosis
○ Exocytosis

A

Transport by special carriers

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20
Q

2 types of TRANSPORT BY SPECIAL CARRIERS

A

Active Transport
Facilitated diffusion

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21
Q

What type of Transport by Special Carrier is this:
Needs energy and is against a concentration gradient

  • Active Transport
  • Facilitated diffusion
A

Active Transport

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22
Q

What type of Transport by Special Carrier is this:
No energy required and is downhill

  • Active Transport
  • Facilitated diffusion
A

Facilitated diffusion

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23
Q

The 2 types of Transport by special carriers (Active Transport and Facilitated Diffusion) are ____, _____, ____.
(SIS)

A

Selective
Inhibitable
Saturable

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24
Q

5 Transport molecules important in pharmacology:

A
  • NET (norepinephrine transporter)
  • SERT (serotonin)
  • VMAT (vesicular monoamine transporter)
  • MDR1 (multidrug resistance protein - 1)
  • MRP1 (multidrug resistance-asso ciated protein - 1)
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25
Q

WHAT TRANSPORT MOLECULE IS THIS:
Physiologic function: reuptake from synapse

  • NET (norepinephrine transporter)
  • SERT (serotonin)
  • VMAT (vesicular monoamine transporter)
  • MDR1 (multidrug resistance protein - 1)
  • MRP1 (multidrug resistance-asso ciated protein - 1)
A
  • NET (norepinephrine transporter)
  • SERT (serotonin)
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26
Q

WHAT TRANSPORT MOLECULE IS THIS:
Pharmacologic Significance: Target of cocaine and some tricyclic antidepressants

  • NET (norepinephrine transporter)
  • SERT (serotonin)
  • VMAT (vesicular monoamine transporter)
  • MDR1 (multidrug resistance protein - 1)
  • MRP1 (multidrug resistance-asso ciated protein - 1)
A

NET (norepinephrine transporter)

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27
Q

WHAT TRANSPORT MOLECULE IS THIS:
Pharmacologic Significance: Target of selective serotonin reuptake inhibitors and some tricyclic antidepressants

  • NET (norepinephrine transporter)
  • SERT (serotonin reuptake transsporter))
  • VMAT (vesicular monoamine transporter)
  • MDR1 (multidrug resistance protein - 1)
  • MRP1 (multidrug resistance-asso ciated protein - 1)
A

SERT (serotonin reuptake transsporter))

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28
Q

WHAT TRANSPORT MOLECULE IS THIS:
Physiologic Function: Transport of dopamine and norepinephrine into adrenergic vesicles in nerve endings

  • NET (norepinephrine transporter)
  • SERT (serotonin reuptake transsporter))
  • VMAT (vesicular monoamine transporter)
  • MDR1 (multidrug resistance protein - 1)
  • MRP1 (multidrug resistance-asso ciated protein - 1)
A

VMAT (vesicular monoamine transporter)

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29
Q

WHAT TRANSPORT MOLECULE IS THIS:
Pharmacologic Significance: Target of reserpine and tetrabenazine

  • NET (norepinephrine transporter)
  • SERT (serotonin reuptake transsporter))
  • VMAT (vesicular monoamine transporter)
  • MDR1 (multidrug resistance protein - 1)
  • MRP1 (multidrug resistance-asso ciated protein - 1)
A

VMAT (vesicular monoamine transporter)

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30
Q

WHAT TRANSPORT MOLECULE IS THIS:
Pharmacologic Significance: Increased expression confers resistance to certain anticancer drugs; inhibition increases blood levels of digoxin

  • NET (norepinephrine transporter)
  • SERT (serotonin reuptake transsporter))
  • VMAT (vesicular monoamine transporter)
  • MDR1 (multidrug resistance protein - 1)
  • MRP1 (multidrug resistance-asso ciated protein - 1)
A

MDR1 (multidrug resistance protein - 1)

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31
Q

WHAT TRANSPORT MOLECULE IS THIS:
Physiologic Function: Transport of many xenobiotics out of cells

  • NET (norepinephrine transporter)
  • SERT (serotonin reuptake transsporter))
  • VMAT (vesicular monoamine transporter)
  • MDR1 (multidrug resistance protein - 1)
  • MRP1 (multidrug resistance-asso ciated protein - 1)
A

MDR1 (multidrug resistance protein - 1)

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32
Q

WHAT TRANSPORT MOLECULE IS THIS:
Pharmacologic Significance: Confers resistance to certain anticancer and antifungal drugs

  • NET (norepinephrine transporter)
  • SERT (serotonin reuptake transsporter))
  • VMAT (vesicular monoamine transporter)
  • MDR1 (multidrug resistance protein - 1)
  • MRP1 (multidrug resistance-asso ciated protein - 1)
A

MRP1 (multidrug resistance-asso ciated protein - 1)

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33
Q

Binding to specialized components (receptors) on
cell membranes

○ Aqueous diffusion
○ Lipid diffusion
○ Transport by special carriers
○ Endocytosis
○ Exocytosis

A

Endocytosis

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34
Q

Internalization by infolding of the area of the
membrane and contents of the vesicle are
subsequently released into the cytoplasm

○ Aqueous diffusion
○ Lipid diffusion
○ Transport by special carriers
○ Endocytosis
○ Exocytosis

A

Endocytosis

35
Q

the process by which the substance is bound at a cell-surface receptor, engulfed by the cell membrane, and carried into the cell by pinching off of the newly formed vesicle inside the membrane.

○ Aqueous diffusion
○ Lipid diffusion
○ Transport by special carriers
○ Endocytosis
○ Exocytosis

A

Endocytosis

36
Q

Substance can be released into the cytosol by breakdown of the vesicle

○ Aqueous diffusion
○ Lipid diffusion
○ Transport by special carriers
○ Endocytosis
○ Exocytosis

A

Endocytosis

37
Q

Permits very large or very lipid-insoluble chemicals to enter the cell: B12 with intrinsic factor, Iron with transferrin

○ Aqueous diffusion
○ Lipid diffusion
○ Transport by special carriers
○ Endocytosis
○ Exocytosis

A

Endocytosis

38
Q

Reverse process

○ Aqueous diffusion
○ Lipid diffusion
○ Transport by special carriers
○ Endocytosis
○ Exocytosis

A

Exocytosis

39
Q

Expulsion (or secretion) of membrane-encapsulated material from the cell: Neurotransmitters

○ Aqueous diffusion
○ Lipid diffusion
○ Transport by special carriers
○ Endocytosis
○ Exocytosis

A

Exocytosis

40
Q

Predicts the movement of molecules across a barrier

A

FICK’S LAW OF DIFFUSION

41
Q

FICK’S LAW OF DIFFUSION:

Drug absorption is faster in organs with larger surface areas (eg, _______) than from organs with smaller absorbing areas (eg, ______)

MAS MAKAPAL, MAS MABAGAL

A

small intestine; stomach

42
Q

FICK’S LAW OF DIFFUSION:

Drug absorption is faster from organs with (thick/thin)
membrane barriers (eg, lungs) than those with thick barriers (eg, skin)

A

thin membrane barriers

43
Q

The passive flux of molecules down a concentration gradient is governed by _____.

A

Fick’s law

44
Q

FICK’S LAW OF DIFFUSION:

measure of the mobility of the drug in medium of the
diffusion path

  • Permeability coefficient
  • Thickness
  • area
A

Permeability coefficient

45
Q

FICK’S LAW OF DIFFUSION:

(length of the diffusion path). Is inversely proportional but the area is directly proportional. THE BIGGER THE AREA, FASTER TO ABSORB

  • Permeability coefficient
  • Thickness
  • Area
46
Q

FICK’S LAW OF DIFFUSION:
cross-sectional area of the diffusion path

  • Permeability coefficient
  • Thickness
  • Area
47
Q

WATER AND LIPID SOLUBLE DRUGS
polar; they follow the water diffusion

  • Water soluble
  • Lipid soluble
A

Water soluble

48
Q

WATER AND LIPID SOLUBLE DRUGS
Pag maliit, they can go to the paracellular.
They can diffuse in between cells

  • Water soluble
  • Lipid soluble
A

Water soluble

49
Q

WATER AND LIPID SOLUBLE DRUGS
Pag maliit, they can go to the paracellular.
They can diffuse in between cells

  • Water soluble
  • Lipid soluble
A

Water soluble

50
Q

WATER AND LIPID SOLUBLE DRUGS
non polar; they follow the lipid diffusion

  • Water soluble
  • Lipid soluble
A

Lipid soluble

51
Q

WATER AND LIPID SOLUBLE DRUGS
non polar; they follow the lipid diffusion

  • Water soluble
  • Lipid soluble
A

Lipid soluble

52
Q

WATER AND LIPID SOLUBLE DRUGS
They can traverse in cell membrane
because the cell membrane is lipid bilayer.

  • Water soluble
  • Lipid soluble
A

Lipid soluble

53
Q

WATER AND LIPID SOLUBLE DRUGS:
Aqueous solubility of a drug is a function of the
electrostatic charge (degree of ionization, polarity)
of the molecule.

  • AQUEOUS DIFFUSION
  • LIPID DIFFUSION
  • IONIZATION OF WEAK ACIDS AND WEAK BASES
A

AQUEOUS DIFFUSION

54
Q

WATER AND LIPID SOLUBLE DRUGS:
Water molecules are attracted to charged drug
molecules forming an aqueous shell around them

  • AQUEOUS DIFFUSION
  • LIPID DIFFUSION
  • IONIZATION OF WEAK ACIDS AND WEAK BASES
A

AQUEOUS DIFFUSION

55
Q

WATER AND LIPID SOLUBLE DRUGS:
Lipid solubility of a molecule is inversely proportional to its charge

  • AQUEOUS DIFFUSION
  • LIPID DIFFUSION
  • IONIZATION OF WEAK ACIDS AND WEAK BASES
A

AQUEOUS DIFFUSION

56
Q

WATER AND LIPID SOLUBLE DRUGS:
Many drugs are weak bases or weak acids

  • AQUEOUS DIFFUSION
  • LIPID DIFFUSION
  • IONIZATION OF WEAK ACIDS AND WEAK BASES
A

LIPID DIFFUSION

57
Q

WATER AND LIPID SOLUBLE DRUGS:
pH of the medium determines the fraction of molecules charged (ionized) versus uncharged
(nonionized)

  • AQUEOUS DIFFUSION
  • LIPID DIFFUSION
  • IONIZATION OF WEAK ACIDS AND WEAK BASES
A

LIPID DIFFUSION

58
Q

WATER AND LIPID SOLUBLE DRUGS:
Fraction of molecules in the ionized state can be
predicted by means of the H - H equation

  • AQUEOUS DIFFUSION
  • LIPID DIFFUSION
  • IONIZATION OF WEAK ACIDS AND WEAK BASES
A

LIPID DIFFUSION

59
Q

WATER AND LIPID SOLUBLE DRUGS:
Hendersson - Hasselbach equation (H - H
equation): log (protonated) / (unprotonated) = pka -pH

Protonated means associated with a proton (a
hydrogen ion)

  • AQUEOUS DIFFUSION
  • LIPID DIFFUSION
  • IONIZATION OF WEAK ACIDS AND WEAK BASES
A

LIPID DIFFUSION

60
Q

LIPID DIFFUSION:

T/F: Weak acid has PKA

61
Q

LIPID DIFFUSION:

T/F: Some of our drugs are weak acid and weak base

62
Q

LIPID DIFFUSION:

T/F: If weak acid and weak bases, some of them clings
on to their hydrogen. Pag walang charge, non polar (lipid soluble). Pag may charge, lipid INsoluble (polar)

63
Q

LIPID DIFFUSION:

T/F: Strong acid and strong bases will be separated in a solution because it will ionized

64
Q

WATER AND LIPID SOLUBLE DRUGS:
Some of our drugs are weak acid and weak base

  • AQUEOUS DIFFUSION
  • LIPID DIFFUSION
  • IONIZATION OF WEAK ACIDS AND WEAK BASES
A

IONIZATION OF WEAK ACIDS AND WEAK BASES

65
Q

WATER AND LIPID SOLUBLE DRUGS:
The electrostatic charge of an ionized molecule attracts water dipoles —> polar, relatively water-soluble and lipid-insoluble complex

  • AQUEOUS DIFFUSION
  • LIPID DIFFUSION
  • IONIZATION OF WEAK ACIDS AND WEAK BASES
A

IONIZATION OF WEAK ACIDS AND WEAK BASES

66
Q

IONIZATION OF WEAK ACIDS AND WEAK BASES:

T/F: Because lipid diffusion depends on relatively high lipid solubility, ionization of drugs may reduce their ability to permeate membranes. A very large percentage of the drugs in use are weak acids or weak bases;

67
Q

IONIZATION OF WEAK ACIDS AND WEAK BASES:

T/F: Some of our drugs are weak acid and weak base

68
Q

IONIZATION OF WEAK ACIDS AND WEAK BASES:

T/F: Pag walang charge, non polar. Pag may charge, lipid INsoluble (polar). If uncharged, IT CAN’T pass through (only traverse)

69
Q

IONIZATION OF WEAK ACIDS AND WEAK BASES:

Neutral molecule that can form a cation (+ charged) by combining with a proton (hydrogen ion)

  • Weak Base
  • Weak Acid
70
Q

IONIZATION OF WEAK ACIDS AND WEAK BASES:
Ionized, more polar, more water soluble when they are protonated. Pag acidic ang weak base,

  • Weak Base
  • Weak Acid
71
Q

IONIZATION OF WEAK ACIDS AND WEAK BASES:
can accommodate a proton so pag acidic ang weak base they become positively charged since they absorb the Hydrogen

  • Weak Base
  • Weak Acid
72
Q

IONIZATION OF WEAK ACIDS AND WEAK BASES:
When it is positive in an acidic environment they are water-soluble.

  • Weak Base
  • Weak Acid
73
Q

IONIZATION OF WEAK ACIDS AND WEAK BASES:
Neutral molecule that can
reversibly dissociate into an anion (- charged) and a proton ( hydrogen ion)

  • Weak Base
  • Weak Acid
74
Q

IONIZATION OF WEAK ACIDS AND WEAK BASES:
Not ionized, less polar, less water soluble when they are protonated

  • Weak Base
  • Weak Acid
75
Q

IONIZATION OF WEAK ACIDS AND WEAK BASES:
Weak Acid: T/F

pag acidic yung environment, dadami ang hydrogen, it will hold to their hydrogen so it is uncharged. Protonated weak acid is uncharged

76
Q

IONIZATION OF WEAK ACIDS AND WEAK BASES:
Weak Acid: T/F

If alkaline environment, they release there proton, they become negatively charge. If negatively charge polar, you are water soluble, you stay in the water

77
Q

IONIZATION OF WEAK ACIDS AND WEAK BASES:
Weak Acid: T/F

The protonated form of a weak acid is the neutral, more lipid-soluble form

78
Q

IONIZATION OF WEAK ACIDS AND WEAK BASES:
RNH3+ ⇔ RNH2 + H+

Which part of the equation is Protonated weak base (charged, more water-soluble)

79
Q

IONIZATION OF WEAK ACIDS AND WEAK BASES:
RNH3+ ⇔ RNH2 + H+

Which part of the equation is Unprotonated weak base (uncharged, more lipid-soluble)

80
Q

IONIZATION OF WEAK ACIDS AND WEAK BASES:
RNH3+ ⇔ RNH2 + H+

Which part of the equation is proton

81
Q

IONIZATION OF WEAK ACIDS AND WEAK BASES:
RCOOH ⇔ RCOO- + H+

Which part of the equation is Protonated weak acid (uncharged, more water-soluble)

82
Q

IONIZATION OF WEAK ACIDS AND WEAK BASES:
RCOOH ⇔ RCOO- + H+

Which part of the equation is Unprotonated weak acid (charged, more water-soluble)

83
Q

IONIZATION OF WEAK ACIDS AND WEAK BASES:
More of a weak acid will be in the lipid-soluble form at (acid/basic) pH, while more of a weak base will be in lipid soluble form at alkaline pH

[MT 6314] - 1st Shifting (23 decks)

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