Principles of Pharmacology Flashcards

1
Q

What makes a drug a ‘medicine’?

A

The intention of being given with therapeutic effect

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2
Q

What is a drug?

A

A chemical compound that produces biological effects

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3
Q

What is the term for drug substances that are already present in the body? Give two examples.

A

Endogenous

  1. Insulin
  2. Adrenaline
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4
Q

What is the 4-step pathway for discussing and studying the pharmacological effects of a drug?

A
  1. Pharmacodynamics
  2. Pharmacokinetics
  3. Clinical Uses
  4. Adverse effects and Contraindications
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5
Q

Define Pharmacodynamics

A

The drug’s mechanism of action upon the body

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6
Q

Define Pharmacokinetics. Include an explation of the ADME acronym

A

The body’s mechanism of action upon the drug.
Absorption-Distribution-Metabolism-Excretion.

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7
Q

What is the difference between Adverse Effects and Contraindications?

A

Adverse Effects are the non-theraputic, unwanted physiological effects of the drug.

Contraindications are the physiological/social/psychological factors in the patient that act as reasons NOT to prescribe the drug

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8
Q

What are the primary and secondary pharmacodynamic effects of Aspirin/NSAIDs?

A
  1. Analgesic
  2. 2 Anti-pyretic (anti-fever)
  3. 3 Anti-inflammatory
  4. Anti-platelet aggregation
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9
Q

Describe the pharmacodynamic mechanism of Aspirin

A
  1. Inhibits Cyclooxygenase (COX)
  2. COX catalyses Arachidonic Acid into Prostaglandings and Thromboxanes
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10
Q

Describe the 4 main physiological roles of Prostaglandins

A
  1. Sensitise pain nerve endings
  2. Dilates blood vessels (redness/inflammatory)
  3. Increases blood vessel permeability (swelling of Int. fluid comp)
  4. Induces fever
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11
Q

Describe the main physiological role of Thromboxanes

A

Induces increased platelet-aggregation

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12
Q

Drugs often act at ________ which are expressed only in selective tissues, and have the correct chemical structure to bind the drug.

A

Receptor Sites

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13
Q

Name three key effects of drug action as perpetuated by the ‘receptor site’ system.

A

Tissue Selectivity

Chemical Selectivity

Action Amplification (even at v. Small concentrations)

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14
Q

What name is given to the type of drug in which the drug binds to a receptor but DOES NOT induce a biological effect?

A

Antagonist

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15
Q

Define an ‘Agonist’ drug.

A

A drug which binds to a receptor to produce a biological cellular response

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16
Q

Draw a diagram to show the steps and relationship between drug ‘affinity’ and ‘efficacy’ in both agonists and antagonists.

A
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17
Q

Out of agonists and antagonists, which is the only one which can have a measured ‘efficacy’? And why?

A

Agonists. Because only agonists produced a direct biological response, whereas antagonists merely block receptor sites to inhibit the effect of endogenous hormones/enzymes

18
Q

Define KA in the context of drug affinity

A

KA is known as the Equilibrium Constant. Specifically, it outlines the point at which exactly 50% of the receptor sites have been filled.

19
Q

Draw a diagram to outline drug affinity. What type of pattern is formed by the typical data?

A
20
Q

Define the EC50 of a drug. What quality does it measure?

A

The concentration at which 50% of the maximal biological response is achieved. Also designates the drug’s potency.

21
Q

Draw a diagram to show why KA and EC50 are not equal, and explain why?

A
22
Q

What do we call the ‘strength’ of a drug, as determined by a combination of its affinity and efficacy?

A

Potency

23
Q

Define ‘ligand’

A

Defined as any molecule or atom that irreversibly binds to a receptor

24
Q

What are ‘Partial Agonists’?

A

Partial agonists are ligands that bind to the agonist recognition site but trigger a response that is lower than that of a full agonist at the receptor

25
Q

What type of antagonism involves antagonists competing with agonists for the same binding site?

A

Competitive antagonism

26
Q

If KAnt < KA, which will occupy more receptor sites at equal concentrations?

A

Antagonist

27
Q

Draw a diagram outlining ‘Surmountable’ antagonism. Why is there a parallel shift to the right in the present of antagonists?

A

Because the concentration of the agonists must be increased in a linear fashion to induce the same maximal biological response

28
Q

Draw a diagram outlining ‘Insurmountable’ antagonism. Why is there a an antagonist-sensitive component? What are the differences between non-competitive and irreversible antagonism?

A
29
Q

Name the four types of receptors, and give an example of an endogenous or given drug that acts there

A
30
Q

Give an an overview of tissue selectivity

A
31
Q

Give an overview of Chemical Selectivity

A
32
Q

Give an overview of Intercellular communication

A
33
Q

Give an overview of amplification

A
34
Q

Broadly speaking, what are the four categories of receptor families?

A
35
Q

Give three examples of intracellular messengers

A

cAMP (Cyclic AMP)

DAG (Diacylglycerol)

IP3 (Inositol 1,4,5-triphosphate)

36
Q

Give an overview of Ligand gated receptor/channel complexes

Include an:

Example

Structure

Mechanism

Speed

A
37
Q

Give an overview of G-coupled protein receptors.

Include an:

Example

Structure

Mechanism

Speed

A
38
Q

Describe the process of intracellular communication initiated via G-protein coupled receptors

A
39
Q

Draw the basic pathway function of GaS/GaI vs GaQ receptors and how they instigate intracellular communication

A
40
Q

Give a diagrammatic outline of how Intracellular receptors work

A
41
Q

Give an outline of how tyrosine kinase receptors work

A