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S1 Pharmacology > Basic Drug Pharmacology > Flashcards

Basic Drug Pharmacology Flashcards

1
Q

What 4 main kinds of regulatory proteins are commonly involved as primary drug targets ?

A

• Receptors
• Enzymes
• Carrier molecules (transporters)
• Ion channels

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2
Q

What is a receptor ?

A
  • a target molecule through which soluble physiological mediators produce their effect
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3
Q

What is the process of drug-receptor interaction?

A
  1. Ligand binds to a receptor.
  2. Forms a ligand-receptor complex.
  3. Triggers a response or multiple responses.
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4
Q

What are the 4 main receptor classes + their response times in drug-receptor interactions ?

A
  • ligand-gated ion channels = minutes
  • G - protein coupled receptors = seconds
  • enzyme - linked receptors = hours
  • intracellular receptors = hours
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5
Q

What are key points about drug-receptor interactions ?

A
  • drugs exhibit high structure and specificity to produce pharmacological effects.
  • interact with receptor sites located in macromolecules with protein-like properties and specific 3D shapes
  • a minimum three-point attachment is required for a drug to bind effectively to a receptor site.
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6
Q

What types of bonds are involved in drug-receptor interactions, and how common are covalent bonds?

A
  • any bond can be involved in drug-receptor interactions
  • covalent bonds are very tight and practically irreversible
  • so they are rare because drug-receptor interaction is reversible , except in a toxic situation
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7
Q

What are the 3 main types of receptor binding experiments ?

A
  • Kinetic experiments = measure binding of one or more radioligand concentrations over a series of time points
  • Saturation experiments = measure binding of increasing concentrations of radioligand
  • Competition/modulation experiments = measuring radioligand binding at equilibrium in the presence of increasing concentrations of a non-labeled compound
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8
Q

What is an agonist in drug-receptor interactions ?

A
  • a substance that interacts with a specific cellular constituent
  • elicits an observable biological response
  • can be endogenous (neurotransmitter) or exogenous (outside body )
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9
Q

What is a partial agonists in drug-receptor interactions ?

A
  • acts on the same receptor as agonists,
    however, regardless of its dose it cannot produce the same maximal biological response as a full agonist
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10
Q

What is an inverse agonist (negative antagonist) ?

A
  • acts on the same receptor of the agonist yet produces an inverse effect
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11
Q

What is a spare receptor in drug-receptor interactions ?

A
  • receptor that exists in excess of what is needed to produce a full biological effect
  • not different from other receptors
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12
Q

What is intrinsic activity in drug-receptor interactions ?

A
  • proportionality constant of the ability of the agonist to activate the receptor compared to the maximally active compound ( most effective) in the series being studied
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13
Q

What is an antagonist ?

A
  • Inhibits the effect of an agonist but has no
    biological activity of its own.
  • may compete on the same receptor site that the agonist occupies or it may act on allosteric site.
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14
Q

What are the 4 types of antagonists ?

A
  • Competitive: antagonist binds to same site as agonist in a reversible manner.
  • Noncompetitive: antagonist binds to the same site as agonist irreversibly.
  • Allosteric: antagonist and agonist bind to different site on same receptor
    • Physiologic: Two drugs have opposite effects through differing mechanism
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15
Q

What is a heteroreceptor in drug receptor interactions ?

A
  • receptor that regulates the synthesis and/or
    the release of chemical mediators other than its own ligand.
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16
Q

What is an autoreceptor ?

A
  • macromolecule typically found in the nerve
    ending that regulates the synthesis and/or the release of its own ligand
17
Q

What is receptor down-regulation ?

A
  • agonist induces a decrease in no of receptors available for binding
18
Q

What is receptor up regulation ?

A
  • agonist induces an increase in the number of receptors available for binding
19
Q

What is affinity ?

A
  • the ability of a drug to combine with a receptor
  • it is proportional to the binding equilibrium constant KD
  • ligand of low affinity requires higher conc of drug to produce the same effect
  • both agonists and antagonists have affinity to the receptor
20
Q

What is efficacy ?

A
  • measure of the biochemical or physiological effect that results from the drug binding to the target
  • represents the maximum effect the drug can produce
21
Q

What is potency + what does it depend upon ?

A
  • refers to the dose of a drug required to produce a specific effect, usually 50% of the maximum effect
  • depends upon both affinity + efficacy
22
Q

What are ligands ?

A
  • substances, molecules or compounds which bind to receptors present in the body
  • eg acetyl chole, adrenaline, noradrenaline, neurotransmitters
23
Q

What are the effects of ligands on the receptor ?

A
  • resemble the natural ligand, activating the receptor in a similar way
  • block the natural ligand, preventing it from binding and activating the receptor
24
Q

What are 2 properties do agonists have ?

A
  • Affinity for receptor
    • Capability to produce chain reactions in the cells having capability of intrinsic activity or efficacy
25
Q

What do agonists cause ?

A
  • when binding to receptors they cause activation of receptors
26
Q

What is the action of a drug ?

A
  • biochemical or physiological mechanisms by which the drug produces a response in the body.
  • e.g - the action of penicillin is to interfere with cell wall synthesis in bacteria.
27
Q

What is the effect of a drug ?

A
  • the observable consequence of a drug action
  • e.g - the effect of penicillin is the death of the
    bacteria.
28
Q

What does a dose-response curve represent?

A
  • shows the relationship between the dose of a drug and the magnitude of its effect
29
Q

What is the threshold in a dose-response curve?

A
  • threshold is the smallest dose of a drug that produces a measurable effect.
30
Q

What is the ceiling in a dose-response curve?

A
  • the maximum effect that a drug can produce, even with increasing doses.
31
Q

What does ED50 stand for?

A
  • ED50 stands for Effective Dose 50
  • the dose of a drug required to produce 50% of the drug’s maximal response.

S1 Pharmacology (33 decks)

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