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Pharmacology > 2.2 - Transport Mechanisms > Flashcards

2.2 - Transport Mechanisms Flashcards

1
Q

– How drugs move across cell membrane

– Drug must be in aqueous solution EXCEPT Pinocytosis

A

Transport Mechanisms

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2
Q

Transport Mechanisms

A
  • Passive Diffusion
  • Carrier-Mediated Transport
  • Convective Transport
  • Ion-Pair Transport
  • Vesicular Transport
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3
Q

– Dominant
– Slowest; NON ENERGY requiring
– ALONG the concentration gradient (DOWNHILL)
– Passage across cell membrane

A

Passive Diffusion

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4
Q

Governing Principle of Passive Diffusion

A

Fick’d Law of Diffusion

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5
Q

dQ/dt

A

Rate of diffusion

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6
Q

D

A

Diffusion coefficient

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7
Q

A

A

Surface area

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8
Q

K

A

Partition coefficient

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9
Q

(CGi - Cp)

A

– Concentration Gradient

– Difference in concentration between 2 immiscible phases

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10
Q

h or l

A

– Length of the membrane

– Membrane thickness

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11
Q

D x A x K. (Cgi - Cp)

A

DIRECTLY Proportional

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12
Q

h

A

INVERSELY Proportional

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13
Q

Factors Affectig Rate of Diffusion

A
  • Surface Area (A)
  • Concentration Gradient (Cgi - Cp)
  • Membrane thickness (h or l)
  • Diffusion Coefficient (D)
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14
Q

Surface Area

A

⬆️A = ⬆️dQ/dt

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15
Q

Concentration Gradient (Cgi - Cp)

A

⬆️(CGi - Cp) = ⬆️dQ/dt

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16
Q

Membrane Thickness (h or l)

A

⬆️h = ⬇️dQ/dt

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17
Q

– Propert of a drug in relation to property of the mebrane

– 2 determinants

A

Diffusion Coefficient

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18
Q

2 determinants

A
  • Particle Size

* Lipophilicity

19
Q

Particle Size

A

⬇️PS = ⬆️ A = ⬆️dQ/dt

20
Q

Lipophilicity

A

⬆️Lipophilicity = ⬆️dQ/dt

21
Q

2 Factors

A
  • Degree of Dissociation/ Ionization

* Partition Coefficient (K)

22
Q

[HA] — LUNA

A

• Non-ionized
• Non-polar
• Lipophilic
A B S O R B E D

23
Q

H + A — WIPE

A

• Ionized
• Polar
• Hydrophilic
E X C R E T E D

24
Q

Ka — DossociatiobnRate Constant

A

⬆️Ka = ⬇️Lipo = ⬇️dQ/dt

25
Q

pKa — -log Ka

A

⬆️pKa = ⬇️Ka = ⬆️lipo = ⬆️dQ/dt

26
Q

Partition Coefficient

— Lipid-H2O coefficient

A

⬆️K = ⬆️Lipo = ⬆️dQ/dt

27
Q

Carrier-Mediated Transport

A
  • Features/ Characteristics

* Examples

28
Q

Features/ Characteristics

A
  • Specificity/ Selectivity
  • Subject to Inhibition, Competition, Antagonism
  • Saturable
29
Q

Carriers recognize specific molecules

A

Selectivity/ Specificty

- Ex: Amino Acid transportrers — Recognized L-dopa but not dopamine

30
Q
  • Ex: A.A Transporters — A.A in food can compete with L-dopa for CNS Transport
A

Subject to Inhibition, Competition, Antagonism

31
Q

– Based on the presence of limited # of carriers

– Displays MICHAELIS-MENTEN Kinetics/ Saturation Kinetics/ Nonlinear Kinetics

A

Subject to Saturability

32
Q

Examples

A
  • Active Transport

* Facilitated Diffusion

33
Q

– Energy requiring
– AGAINST concentration gradient (UPHILL)
– Fastest

A

Active Transport

34
Q

– Non-enwrgy requiring

– ALONG concentration gradient

A

Facilitated transport

35
Q

– Linear
– Concentration INDEPENDENT
– Rate of Accumulation = Rate of Elimination

A

First Order Kinetics

36
Q

– Non-linear
– Concentration DEPENDENT
– Saturable Kinetics
– Michaelis-Menten Kinetics

A

Zero Order Kinetics

37
Q

– Movemement through water-filled PORES/GAP JUNCTIONS

– Only PARACELLULAR transport mechanisms

A

Convective Transport

38
Q

Properties of Convectie Transport

A
  • Pore Size/ Diameter
  • Change of the Pore Lining
  • Movement is by SOLVENT drug
  • Movement is ALONG concentration gradient
39
Q

– 7-10 angstrom

– Allows movement of ions/ molecules with MW 150-400

A

Pore Size/ Diameter

40
Q

– Pure (+) or Pure (-)

– Allows movement of ions with charge OPPOSITE of the pure lining

A

Charge of the Pure Lining

41
Q

– Mesh of transport for large ions — large exogenous ions form a neutral complex with an endogenous oppositely charged ion
– Ex: Quaternary Amines

A

Ion-Pair Transport

42
Q

Vesicular Transport

A
  • Pinocytosis

* Phagocytosis

43
Q 
– Cell EATING
– Small molecules; liquids
– Requirement: Micelle form
– Surfactant: Bile Salts/ Bile Acids
– Vesicle-Mediated
– Requires energy
– Ex: Griseofulvin, ADEL Vitamins
A

Pinocytosis

44
Q

– Cell DRINKING

– Large molecules

A

Phagocytosis

Pharmacology (21 decks)

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