Pharmacology Flashcards

1
Q

What is affinity?

A

A measure of molecules attraction to a receptor

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2
Q

What is efficacy?

A

The ability of a molecule to elicit the response at the receptor

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3
Q

What type of receptors are nicotinic ACh receptors?

A

Ligand gated

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4
Q

What type of receptors are adrenergic receptors?

A

G protein coupled receptors

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5
Q

How do G protein coupled receptors illicit a response from an effector?

A
  1. No signalling, receptor unoccupied, G protein binds GDP
  2. Agonist activates receptor. G protein couples with receptor. GDP dissociates from alpha subunit, and GTP binds to it. Alpha subunit dissociates from G protein and couples with effector, modifying its activity to turn on the signal
  3. Alpha subunit hydrolyses GTP to GDP and G protein alpha subunit recombines with beta-gamma subunit, turning off the signal
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6
Q

What type of receptor are insulin receptors?

A

Kinase associated receptors

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7
Q

How do kinase associated receptors work?

A

Autophosphorylisation of tyrosine

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8
Q

What type of receptor are steroid receptors?

A

Nuclear receptors

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9
Q

How do nuclear receptors work?

A

They diffuse across the cell membrane to the nucleus and bring about changes in transcription bring about their effect

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10
Q

What do depolarisation and repolarisation mean?

A

Depolarisation - membrane potential becomes more positive

Repolarisation - membrane potential becomes more negative

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11
Q

What are the stages of action potential?

A
  1. Resting potential due to sodium outside the cell and negative protein inside the cell
  2. Ligand such as ACh binds to ligand gated Na channel allowing Na influx and causing depolarisation
  3. Once threshold is reaches voltage gated Na channels open - further Na influx - AP
  4. Potassium efflux causes repolarisation
  5. Voltage goes below resting potential - refractory period where no further AP can occur
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12
Q

Where in CNS do sympathetic and parasympathetic neurones flow from?

A

Sympathetic - thoracic-lumbar

Parasympathetic - cranio-sacral

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13
Q

What neurotransmitter are the pre and postganglionic neurone s for sympathetic neurones, and which receptors do they act on?

A

Pre - ACh on nicotinic receptors (ligand gated)

Post - usually noradrenaline on alpha or beta adrenoreceptors (GPRC)

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14
Q

What neurotransmitter are the pre and postganglionic neurone s for PARAsympathetic neurones, and which receptors do they act on?

A

Pre - ACh on nicotinic receptors (lignand gated)

Post - ACh on muscarinic receptors (GPCR)

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15
Q

Do parasympathetic or sympathetic neurones have a short pre-ganglionic neurone and a long post-ganglionic neurone?

A

Sympathetic

Parasympathetic have long pre-ganglionic, short post-ganglionic

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16
Q

What does absorption of drugs depend on?

A

Solubility
Lipid:water coefficient
Chemical stability
Degree of ionisation

17
Q

What is the main fate of drugs?

A

Distribution

18
Q

Why are some drugs confined to plasma, and what is an example of such drugs?

A

Too large to get past capillaries or bound to plasma protein

Heparin

19
Q

Why are some drugs confined to interstitial fluid and plasma, and what is an example of such drugs?

A

Can get past capillaries but not lipid soluble so can’t get past cell membrane
Amoxicillin

20
Q

Why can some drugs be distributed in all fluids and what is an example of such drugs?

A

Small and lipophilic

Ethanol

21
Q

What are the two sites of excretion?

A

Hepatic

Renal

22
Q

What is clearance?

A

Volume of drug cleared from the plasma in a unit of time

23
Q

What is half life?

A

Time taken for plasma concentration to reduce by half

24
Q

What is steady state dose

A

The stage where rate of administration = rate of elimination

25
Q

How many half lives does it take for steady state to be achieved?

A

5

26
Q

In which way do IV and oral administration achieve steady state?

A

IV - smooth curve

Oral - has peaks and troughs but steady state on average

27
Q

What is a therapeutic window?

A

Between minimum drug to be effective and maximum before side effects

28
Q

What is the difference between pharmacodynamics and pharmacokinetics?

A

Dynamics - what the drug does to the body

Kinetics - what the body does to the drug

29
Q

Which receptors are acted on by hydrophilic and hydrophobic proteins?

A

Hydrophilic - kinase linked

Hydrophobic - steroid

30
Q

What is pKa?

A

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

31
Q

What is phase 1 of drug metabolism?

A

Oxidation, reduction and hydrolysis to make a drug more polar
Adds chemically reactive group to allow conjugation

32
Q

What is phase 2 of drug metabolism?

A

Conjugation - adds an endogenous compound to further increase polarity

33
Q

What is key in drug oxidation?

A

Cytochrome P450