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Semester 2 Pharmacology > Pharmacokinetics 1 > Flashcards

Pharmacokinetics 1 Flashcards

1
Q

What is bioavailability?

A

Fraction of unchanged drug that reaches the systemic circulation

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2
Q

What gives 100% bioavailability?

A

IV injection

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3
Q

What are the four ways small molecules cross cell membranes?

A

1) Diffusing directly through the lipid
2) Diffusing through aqueous pores
3) Transmembrane carrier protein
4) Pinocytosis (mostly macromolecules, not drugs)

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4
Q

Describe lipid diffusion of drugs

A
  • Hydrophilic drugs are soluble in aqueous, polar media

* Lipophilic drugs are soluble in fats and non-polar solutions

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5
Q

What are the polar media?

A
  • blood plasma
  • Cytosol
  • Intersitial fluid
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6
Q

What are the non-polar media?

A
  • Interior of the lipid bilayer

* Fat

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7
Q

Which type of dugs have low lipid solubility?

A

Ionised drugs

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8
Q

What does a drugs ionised:unionised ratio depend on?

A

The pH

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9
Q

What are the main drug properties that affect absorption?

A
  • Lipophilicty

* Ionisation

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10
Q

What are the factors that affect distribution?

A
  • Degree of drug ionisation
  • Lipid solubility
  • ph of compartments
  • Cardiac output and blood flow
  • Capillary permeability
  • Plasma protein binding
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11
Q

What do phosphate groups have a high affinity for? And what does this mean for their distribution?

A
  • Calcium

* Quickly distributed to the skeleton

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12
Q

What are the pharmacological properties of pilocarpine?

A

Non selective muscarinic agonist

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13
Q

What are the pharmacological properties of Bethanechol?

A

Non-selective muscarinic agonist

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14
Q

What are the clinical uses of pilocarpine?

A
  • Constriction of pupils (miosis)
  • Glaucoma (to decrease IOP)
  • Xerostomia (following head/neck radiotherapy)
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15
Q

What are the clinical uses of bethanechol?

A

Bladder and GI hypotonia

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16
Q

What is the structure of bethanechol?

A

Quaternary amine

17
Q

What is the structure of Pilocarpine

A

Tertiary amine

18
Q

What are the 5 stages of drugs in the body

A

1) Liberation
2) Absorption
3) Distribution
4) Metabolism
5) Excretion

19
Q

What are the advantages and disadvantages of oral administration?

A

Advantages:
• Convenient
Disadvantages:
• First pass effect, many barriers and variables

20
Q

What are the advantages and disadvantages of sublingual administration?

A 
Advantages:
• No first pass effect 
Disadvantages:
• Inconvenient
• Small dose limit
• Taste
21
Q

What are the advantages and disadvantages of inhalation administration?

A 
Advantages:
• Fast
• Rapid delivery to blood 
Disadvantages:
• Requires special properties of the drug (atomised, vaporised)
22
Q

What are the advantages and disadvantages of Topical administration?

A 
Advantages:
• Convenient
• Localised
Disadvantages:
• Only local
23
Q

What are the advantages and disadvantages of transdermal administration?

A

Advantages:
• Prolonged release
Disadvantages:
• Skin is a very effective barrier

24
Q

What are the advantages and disadvantages of Intramuscular administration?

A 
Advantages:
• Rapid for aqueous 
• Slow for oil
Disadvantages:
• Painful
• Requires trained personnel
25
Q

What are the advantages and disadvantages of Intravenous administration?

A 
Advantages:
• Direct
• Total dose
• Rapid
Disadvantages:
• Requires a professional
• Infection risk 
• Rapid response
26
Q

What are the two main ways a drug will get across a plasma membrane?

A
  • Diffusing directly across the membrane

* Transmembrane carrier proteins

27
Q

Why will the percentage of unbound warfarin increase if the patient is also taking aspirin?

A

Because of the competition of binding to albumin

28
Q

What does the distribution of a drug throughout the body depend on?

A
  • Permeability across tissue barriers
  • Binding within compartments
  • pH partition
  • Fat:Water partition
29
Q

How many body water compartments are there?

A

4

Semester 2 Pharmacology (11 decks)

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