L6 - Pharmacokinetics (Flipped) Flashcards

1
Q

What is pharmacokinetics?

A

The study of what the body does to a drug

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2
Q

Drug effects depend on…

A

Pharmacokinetics and pharmacodynamincs

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3
Q

Pharmacodynamics is the….

A

mechanism of action and effects on cellular functions: eg. receptors, ion channels, enzymes, transporters.

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4
Q

What do the physiochemical properties of a drug affect in phramacokinetics?

A

Concentration - ADME
Absorption, Distribution, Metabolism, Excretion

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5
Q

What is the diffusion coefficient?

A

Proportional to 1/sqrt

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6
Q

What is the relationshop between drug size and diffusion coefficient?

A

The smaller the drug the higher the diffusion cefficient, and the faster it diffuses.

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7
Q

What are some of the barriers in drug absorption?

A
  • The plasma membrane
  • epitheilial cells, gastrointestinal mucosa or renal tuble (all consit of a layer of tightly connected cells)
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8
Q

What prevents potentially harmful molecules from leaking from the blood into the organs?

A

Periendothelial cells or pericytes

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9
Q

What type of transport is important for small molecule drugs?

A

Diffusion through lipid and carriers, as they dont fit through pores.

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10
Q

What is important for transfer or macromolecules across the BBB?

A

Pinocytosis.

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11
Q

What in the liver and kidneys can be used for the elimination of drugs?

A

Carriers involved in the elimination of toxic materials.

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12
Q

Physiochemical properties of a drug that affect absorption

A
  • Lipid Solubility
  • Diffusivity
  • Diffusion coeffcient
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13
Q

What molecules can move freely in lipids and penetrate cell membranes?

A

Non-polar/ucharged molecules.

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14
Q

What are 4 routes of drug administration?

A
  • Intravenous - most direct route
  • Subcutaneous/Intramuscular - next
    fastest route
  • Intrathecal - A lumbar puncture used to
    produce regional
    anaesthesia.
  • Oral - Most absoprtion happens in the gut
    by passive diffusion.
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15
Q

What is bioavailability?

A

How well the fraction of ingested dose gain access to circulation.
Low if absorption is incompleted or drug is metabolised in the gut or by the liver.

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16
Q

What is the OCT2?

A

Organic Cation Transporter
- A uniporter in proximal tublular cells of
the kidney.
- Also a solute carrier

17
Q

What drugs does the OCT2 deal with?

A

Nephrotoxic drugs such as Cisplatin (anticancer drug)

18
Q

What are the main sites where SLCs (solute carriers) such as OCTs and OATs act?

A
  • The BBB
  • The renal tubule
  • The GI Tract
  • The Biliary tract
  • The placenta
19
Q

What does the effectiveness of a drug depend on?

A
  • Affinity/Efficacy
  • Pharmacokinetics
20
Q

How the drugs is processed in the body depends on?

A
  • Absorption
  • Metbolism
  • Distribution
  • Excretion
21
Q

What is distribution of a drug dependant on?

A

permability and lipid solubility.

22
Q

What is Volume of distribution (Vd)?

A
  • A measure of the volume of fluid that would be required to hold the amount of drug in the body as measured in the plasma.
    Vd = Dose/ concentration in plasma.
23
Q

What molecules can cross the BBB easily

A

Lipid soluble molecules such as caffine and ethanol.

24
Q

How are drugs metabolised in the body?

A

In the liver by 2 biochemical phases

25
Q

What are the 2 phases of drug metabolism?

A

Phase 1 - catabolic reactions - can produce
a more reactive compound.
Phase 2 - Syntheic (anabolic) reactions -
involve conjugation to produce
an inactive product.

26
Q

What does the metabolism of paracetamol produce?

A

Hepatotoxic molecules

27
Q

What does the metabolism of Benzodiazapines produce?

A

long-lived active metabolites

28
Q

What may products of phase 1 reactions have?

A

Increased toxicity and carcinogenity.

29
Q

How are drugs excreted from the body?

A
  • Through urine
  • Excretion in milk
  • Excretion in air
  • Renal excretion - glomerular filtration
    - active tubular secretion
    - Passive diffusion
30
Q

What are saturation kinetics?

A

when the velocity of the reaction increases to a maximal value (plateau) as the concentration of the reactant is increased.