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buzzywords > principles pharmacology > Flashcards

principles pharmacology Flashcards

1
Q

paracrine signals

A

produces by cell, targets nearby cells

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2
Q

what are autocrine signals

A

cell to its own receptors

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3
Q

endocrine signals

A

targets specific cells far away from source (hormones)

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4
Q

hydrophobic ligands

A

cannot freely stay in ECM, brought into cells via carrier proteins

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5
Q

hydrophilic ligands

A

signals move freely through ECM, bind to surface receptors on cell

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6
Q

what are the stages of cell signalling

A

reception - recetor binds to ligand

transduction - receptor protein changes, activates intracellular molecules

cell response

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7
Q

what are the 3 classes of signalling pathways

A
  • G-protein coupled receptors
  • enzyme coupled receptors
  • ion channel receptors
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8
Q

describe ligand-gated ion channels

A
  • response within milliseconds

Steps

  1. Ligand binds to the receptor, channel opens
  2. Ions (Ca2+, Na+, K+) flow through passively
  3. Triggers signalling pathway

ex
- Nicontinic acetylcholine receptors

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9
Q

describe G-protein coupled receptors

A
  • response happens in seconds

signal travels far due to signal amplification

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10
Q

describe the steps for turning a G-protein coupled receptor on

A
  1. Agonist (ligand) activates G-coupled receptor
  2. ⍺ subunit leaves G-protein
  3. GDP exchanged for GTP (guanine nucleotide exchange)
  4. Triggers other proteins in signaling pathway
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11
Q

describe the steps for turning a G-protein coupled receptor off

A
  1. ⍺ subunit hydrolyses GTP → GDP
  2. disactivating G-protein
  3. ⍺ subunit recombines with β𝛾 subunit
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12
Q

example of G-protein coupled receptors

A
  • Adrenoceptors – bound and activated by the neurotransmitters/hormones adrenaline and noradrenaline
  • Adrenalinebinding tob2-adrenoreceptors→ Causes bronchodilation
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13
Q

describe enzyme coupled receptors

A
  • Response occurs in hours
  • Single pass transmembrane proteins
  • multiple pathways activated
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14
Q

what are the functions of the autonomic nervous system

A

Mediates output from whole body except skeletal muscle, regulated by external and internal sensory input, via reflexes

  • maintained homeostasis through negative feedback loop
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15
Q

sympathetic transmitter for preganglionic neurones and postganglionic neurones

A
  • acetylcholine (ACh)
  • noradrenaline (NA)
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16
Q

parasympathetic transmitter for both

A

acetylcholine (ACh)

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17
Q

β1: Gs stimulation of adenylyl cyclase →

A

inc HR and force of contraction

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18
Q

β2: Gs stimulation of adenylyl cyclase →

A

bronchodilation

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19
Q

M1: Gq (stimulation of phospholipase C) →

A

inc stomach acid secretion

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20
Q

M2: Gi (inhibition of adenyl cyclase; opening of K+ channels, closure of Ca2+ channels) →

A

decreased HR

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21
Q

M3: Gq (stimulation of phospholipase C) →

A

bronchoconstriction

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22
Q

what does action potential allow

A

signalling over long distances

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23
Q

lower Ka =

A

greater affinity of ligand for receptor

24
Q

antagonist

A

drug that reduces or inhibits the actions of an agonist by binding to the same receptor

25
Q

potency

A

amount of drug required to produce a desired effect

26
Q

efficacy

A

maximum response achievable from drug

27
Q

EC50

A

concentration of drug where 50% of effect is produced

28
Q

smaller EC50 =

A

more potent

29
Q

partial agonist

A

response is sub-maximal, even when all receptors occupied

30
Q

if both the agonist and partial agonist have similar affinities which one has the greater efficacy

A

the full agonist

31
Q

describe reversible competitive antagonist

A

antagonist competes with agonist for same binding site on receptor
- inhibition can be overcome with increased ligand concentration

32
Q

what is the pKa

A

pH at which 50% of drug is ionised and 50% is unionised

33
Q

lower pKa =

A

stronger acid

34
Q

weak bases are absorbed better in

A

acidic environments

35
Q

weak acids are absorbed better in

A

alkaline environments

36
Q

low Vd =

A

drugs retained in vascular compartments - mostly in plasma

37
Q

high Vd

A

drugs retained in non-vascular compartments – adipose, muscle etc.

38
Q

Vd calculation

A

Vd = Dose / [drug] x plasma

39
Q

what Is albumin

A

most abundant plasma protein, high affinity for hydrophobic drugs

40
Q

where do phase I and II of drug metabolism take place

A

the liver

41
Q

what is the equation for bioavailability (F)

A

quantity of drug reaching systemic circulation (AUC)

divided by

quantity of drug administered (DOSE)

42
Q

what is phase I metabolism

A

change in the drug by oxidation, reduction or hydrolysis

43
Q

what is phase II metabolism

A

involves combination of the drug with polar molecules to form a water-soluble metabolite - conjugate

44
Q

name a drug which goes straight to phase II metabolism

A

Codeine

45
Q

what is drug elimination accomplished by

A

renal filtration of blood plasma

46
Q

what is clearance

A

volume of plasma cleared of drug per unit time

47
Q

clearance equation

A

clearance = rate of drug elimination / [Drug] plasma

48
Q

what is Vmax

A

max. rate of the drug elimination

49
Q

what is Km

A

half of max. rate of elimination

50
Q

t1/2 =

A

0.693 x Vd / CL

51
Q

how many half lives are required to reach steady state

A

5

52
Q

necrosis =

A

cell death

53
Q

internal necrosis

A

ischemia

54
Q

when does coagulative necrosis occur

A

when the tissue becomes hypoxic

55
Q

Liquefactive necrosis

A

Occurs when hydrolytic enzymes completely digest dead cells leaving behind a creamy substance (pus) and dead cells
- brain injury

56
Q

caseous necrosis

A

Occurs when the dead cells disintegrate but are not fully digested
- cheesy
TB

buzzywords (22 decks)

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