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Year 1 MBChB > Pharmacology > Flashcards

Pharmacology Flashcards

1
Q

What is pharmacodynamics?

A

Drug action on the body

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2
Q

What is pharmacokinetcs?

A

Body action on a drug

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3
Q

What does an agonist do?

A

Gains a response

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4
Q

What does an antagonist do?

A

Blocks a response

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5
Q

2 steps of receptor activation?

A
  • Affinity (binding to receptor)

- Efficacy (change from bound and inactive to active)

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6
Q

Do agonists vs antagonist possess affinity and efficacy?

A
  • Agonists possess both

- Antagonists only possess affinity

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7
Q

Affinity is determined by?

A

Binding and dissociation rates

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8
Q

A high affinity ligand will have a ….. binding rate compared to …. ?

A

High and low dissociation rate

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9
Q

Efficacy is determined by?

A

Forward beta activation rate vs backwards alpha inactivation rate

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10
Q

A ligand with high efficacy will have a … beta rate and … alpha rate?

A

High and low

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11
Q

An antagonist can be + an agonist can be?

A

Competitive or non-competitive + only competitive

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12
Q

Competitive antagonists + agonists bind to what?

A

Both to the active site/ orthosteric site

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13
Q

Non-competitive antagonists bind to what?

A

Allosteric site

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14
Q

2 shapes of agonist depending on graph + 2 key values?

A
  • Hyperbolic curve on a linear graph or sigmoidal on a log graph
  • EMAX is the highest level of response
  • EC50 is half the maximal response
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15
Q

What are full agonists?

A

Can reach their EMAX

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16
Q

What is a partial agonist?

A

Cannot reach EMAX

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17
Q

Agonist + competitive antagonist effect on curve?

A

Shift to right as more agonist needed to reach EMAX

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18
Q

Agonist + non-competitive antagonist effect on curve?

A

No shift but depression of curve as EMAX/EC50 cannot be reached

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19
Q

Autocrine signalling?

A

Cell signal acts on itself

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20
Q

Paracrine signalling?

A

Cell signal acts on neighbour cells

21
Q

Endocrine signalling?

A

Cell signal moves via blood to target areas of the body

22
Q

4 main types of cell receptors?

A

Ligand-gated, GPCRs, kinase-linked and nuclear (all in the cell membrane except nuclear)

23
Q

Ligand gated channel rate of action?

A

Fast action

24
Q

GPCR rate of action + structure?

A
  • Act slowly
  • NH2 + COOH ends with 7 transmembrane domains
  • Alpha, beta and gamma subunit
  • Alpha subunit has a guanine nucleotide bonding site
25
Q

GPCR signalling summary?

A
  • GTP binds to guanine binding site on alpha unit
  • Alpha unit dissociates from beta and gamma subunit to modify G-protein
  • Signal turned off when GTP is hydrolysed
26
Q

2 main types of GPCR alpha subunits and their actions?

A
  • Gs via sympathetic innervation stimulates adenyl cyclase/ cAMP formation
  • Gi via parasympathetic innervation inhibits adenyl cylase/ cAMP formation
27
Q

Kinase-linked receptor rate of action + main molecule that targets it + relevance to cancer + 2 examples?

A
  • Act slowly
  • Targeted by growth factors
  • Mutations lead to cancer
  • ECGR and PI3K
28
Q

Nuclear receptors mechanism + molecules that target it?

A

Combines with steroid and moves to nucleus to alter genes + steroid hormones

29
Q

Where does drug metabolism occur?

A

In the liver

30
Q

Phase I metabolism reaction + key proteins?

A
  • Catabolic reaction that increases polarity of drug via hydrolysis, oxidation etc.
  • P450 (CYP) monooxygenase proteins
31
Q

Phase II metabolism reaction + common reaction?

A
  • Chemical groups made in phase I are joined

- Glucuronidation is a common reaction

32
Q

3 ways drugs are excreted + short summary + most common method?

A
  • Glomerular filtration (for unbound proteins)
  • Active tubular secretion (via OATs and OCTs) - MOST COMMON (90%)
  • Tubular reabsorption (passive diffusion of reabsorbed drug)
33
Q

2 receptors that parasympathetic fibres act on?

A

Nicotinic ligand-gated channels and muscarinic GPCR

34
Q

What can also be released from parasympathetic fibres apart from ACH + whay they cause?

A

VIP and NO + SM relaxation

35
Q

What can also be released from sympathetic fibres apart from NA?

A

ATP and NPY

36
Q

SM contraction summary?

A
  • GPCR activates PLC
  • PLC produces IP3
  • IP3 binds at SR and releases Ca
  • Ca binds calmodulin
  • Calmodulin activates MLCK
  • MLCK activates mysoin cross bridge
37
Q

SM relaxation summary?

A
  • GPCR activates AC
  • AC forms cAMP
  • cAMP activates PKA
  • PKA activates MLCK and MP
  • Calcium dissociates from calmodulin and MP inactivates cross bridge
38
Q

Skeletal/cardiac contraction summary?

A
  • GPCR activates AC
  • AC produces cAMP
  • cAMP activates PKA
  • PKA activates L-type Ca channels
  • CICR occurs
  • Ca binds tropomyosin C
  • Tropomyosin shifts actin out of cleft
39
Q

Skeletal/cardiac relaxation summary?

A
  • PKA activates phoshoplamban
  • Phospholamban increases CICR and relaxation rate
  • L-type channels close
  • Ca-ATPase reruits Ca back into SE
  • Ca dissociated from tropomysoin C
40
Q

How is cAMP inactivated?

A

Phosphodiesterase (PDE)

41
Q

cAMP role in muscle?

A

Activates PKA

42
Q

PKA action in SM vs skeletal/cardiac?

A

Relaxation vs contraction AND relaxation

43
Q

First order kinetics relationship + curve shape?

A

Rate of elimination = drug concentration + hyperbolic curve

44
Q

Zero order kinetics relationship + curve shape?

A

Cp > Km of enzyme that metabolises it + linear curve

45
Q

Clearance of a drug definition + what is applies to?

A

Volume cleared from plasma over time + only applies to first order kinetics

46
Q

How is Ach vs NA taken back into pre-synaptic neurons?

A

Ach = enzyme degradation vs NA = reuptake channels (U1 and U2)

47
Q

Effects of cocaine and amphetamine?

A

Increases adrenoreceptor stimulation so vascontriction, increased heart rate etc.

48
Q

Sympathetic vs parasympathetic receptors in the smooth muscle + heart + vasculature?

A

Beta 2 and M3 + beta 1 and M2 + alpha 1

Year 1 MBChB (10 decks)

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