Exam 3- Pharam - Section 1 Flashcards

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1
Q

Study of drug movement of drugs in the body across biological membranes from the time of absorption until elimination

A

Drug deposition

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2
Q

4 stages of drug deposition

A

1) Absorption
2) Distribution
3) Biotransformation (Metabolism)
4) Excretion

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3
Q

Factors affecting the deposition of drugs:

A
  • biological cell membranes
  • concentration gradient
  • pump mechanism
  • site of admin
  • total body water
  • plasma protein binding
  • disease
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4
Q

Properties of a cell membrane:

A
  • phospholipid bilateral
  • membrane proteins
  • cell junctions (gap, tight)
  • aqueous pores
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5
Q

4 Mechanisms of transport across a membrane

A

1) Passive diffusion
2) Facilitated diffusion
3) Active Transport
4) Pinocytosis

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6
Q

Mechanism:

  • moves down conc. Gradient
  • NO energy required
  • most common form
A

Passive Diffusion

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7
Q

3 Mechanisms of passive diffusion

A
  • Transmembrane
  • Paracellular
  • Simple
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8
Q

Transmembrane passive diffusion

A

-movement by passive diffusion through aqueous protein channels in the cell membrane

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9
Q

Paracellular mechanism of passive diffusion

A
  • movement via filtration through intracellular aqueous pores
  • tissues that have barrier mechanism have tight intracellular junctions
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10
Q

Simple mechanism of Passive diffusion

A
  • movement through lipid membrane

- majority of drugs move through the body via this route

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11
Q

Mechanism:

  • moves down concentration gradient
  • requires a carrier
  • NO energy required
  • Saturable
A

Facilitated diffusion

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12
Q

Example of facilitated diffusion

A

Glucose transport in muscle

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13
Q

Mechanism:

  • Moves uphill Low-High
  • Requires energy (ATP)
  • requires a carrier
  • selectivity
  • saturable
  • competitive inhibitions by co-transported compounds
A

Active transport

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14
Q

2 classifications of active transport

A
  • Primary

- Secondary

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15
Q

Primary Active Transport

A
  • Na+/ K+ ATPase
  • transport pump
  • Most abundant active transport pump in the body
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16
Q

Secondary Active Transport

A
  • Na+ dependent glucose transporter in renal tubules
  • Na+ transported, glucose is hitch hiker
  • Glucose sized keyhole next to Na+ port
17
Q

Pinocytosis

A
  • endocytosis or “cell drinking”
  • drug dissolved in water
  • can be toxic
18
Q

Example of Pinocytosis

A

Sequestration of aminoglycoside antibiotics (amikacin, gentamicin) in renal tubules
**can cause renal damage and can be renal toxins

19
Q

Factors affecting Simple Diffusion

A

1) concentration gradient
2) lipid solubility
3) degree of ionization

20
Q

Drugs move across membranes from high to low “down hill”

A

Concentration gradient

21
Q

Lipid solubility

A
  • lipid membrane limits diffusion
  • need to be lipophilic to enter lipid portion
  • **higher lipid solubility of the drug= faster crossing cell membranes
  • non-lipid solvable drugs are more dependent on molecular size
22
Q

Degree of Ionization

A
  • drugs cross bio membrane in non-ionized form (more lipid solvable form)
  • Rate of diffusion depends on degree of ionization
23
Q

What does the degree of ionization depends on?

A
  • pH of the drug
  • pKa of the drug
  • ph of the environment in vivo
24
Q

______ is the pH of a drug at which 50% of the drug is ionized and 50% is non-ionized

A

pKa

25
Q

Weak acids are more ionized in __________ solutions.

A

Alkaline

26
Q

Weak bases are more ionized in ________ solutions

A

Acidic

27
Q

_________ is a proton donor, and contributes h+ to a solution

A

Acid

28
Q

_______is a proton acceptor and binds or buffers H+ in a solution

A

Base

29
Q

What is the most abundant and most important buffer system?

A

Bicarbonate - carbonic acid buffer system

30
Q

CO2 + H2O H2CO3 HCO3- + H+

A

The Ubiquitous Equation

31
Q

Non-carbonate buffers

A
  • Proteins
  • Phosphates
  • Ammonia
32
Q

The buffer system for Intracellular fluid (ICF)

A

Phosphate + Protein (mostly Hgb) > carbonic acid

33
Q

The buffer system for Interstitium fluid?

A

Carbonic acid > protein > phosphate

34
Q

What is the buffer system for Cerebrospinal (CSF) ?

A

Carbonic acid

35
Q

What is the buffer system for Renal tubular filtrate?

A

Carbonic acid > phosphate > Ammonia

36
Q

The buffer system for plasma (intravascular) fluid?

A

Carbonic acid > phosphate > protein