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Block 1 Pharmocology > How Drugs Act 1 > Flashcards

How Drugs Act 1 Flashcards

1
Q

What is Pharmacolgy

A

The branch of medicine and biology concerned with the study of drug action. More specifically, it is the study of the interactions that occur between a living organism and chemicals that affect normal or abnormal biochemical function.

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2
Q

What is a drug

A

: Broadly defined as any man-made, natural, or endogenous (within the body) molecule which exerts a biochemical and/or physiological effect on the cell, tissue, organ, or organism/A drug is a chemical applied to a physiological system that affects its function in a specific way.

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3
Q

How much does the UK spend on Medical drugs per annum?

A

£10bn p.a.

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4
Q

How much does the UK spend on non Medical drugs per annum?

A

c.a. £30bn p.a. (£500 per person)

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5
Q

Aside from medical drugs, what other drugs is the UK spending money on?

A

Sport enhancement (anabolic steroids, EPO)
Mood change (Alcohol, nicotine, caffeine)
Recreational (cannabis, cocaine, ketamine)
Herbal (St. John’s Wort, Milk Thistle)
Homeopathy (placebo effect)

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6
Q

what do drugs act on and give examples

A

drugs act on target proteins, namely: receptors
enzymes
carriers
ion channels.

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7
Q

what is a rececptor in terms of pharmacoly

A

protein molecules whose function is to recognise and respond to endogenous chemical signals

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8
Q

what are drug targets?

A

Other macromolecules with which drugs interact to produce their effects are known as drug targets

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9
Q

what is the nature f drug specificity

A

reciprocal: individual classes of drug bind only to certain targets, and individual targets recognise only certain classes of drug.

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10
Q

are drugs completely specific in their actions? if not, why?

A

•No drugs are completely specific in their actions. In many cases, increasing the dose of a drug will cause it to affect targets other than the principal one, and this can lead to side effects.

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11
Q

give examples of non receptor targets

A 
Plant Sterols (cholesterol lowering)
Ammonium hydroxide (anti-pruritic)
Alcohol (sedative/hypnotic)
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12
Q

give examples of receptor targets

A

Salbutamol (b2 adrenoceptors)
Sildenafil (PDE5)
Ibuprofen (COX-2)

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13
Q

what confers the specificity of the drug?

A

is the chemical nature of the drug/receptor

Interaction that confers specificity

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14
Q

how are we able to target specific tissue?

A

by choosing the receptors

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15
Q

In Hypertensin, Ramipril is used. What is the receptor

Where is the receptor found and where is the not found

A

Angiotensin converting enzyme (ACE)
Present in smooth muscle in kidney and vasculature
NOT present in gut

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16
Q

In Asthma, Salbutamlol is used. What is the receptor and what can this often get confused with

A

b2 adreneric
Present in airway smooth muscle
NOT present in cardiac muscle (b1)

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17
Q

In Psychosis , Eticlopride l is used. What is the receptor

Where is the receptor found

A

: D2 dopamine receptor

Present in neocortical brain regions

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18
Q

What is timecourse?

A

Time for the drug to reach the receptor
Binding rate constants
Activation/inactivation of receptor
Time for the drug to be removed from tissues

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19
Q

what is pharmacodynamics

A

The study of drug-receptor interactions

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20
Q

what is Dissociation constant

A

the concentration at which half of the drug is bound to the receptor at equilibrium.

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21
Q

what is affinity

A

The strength of noncovalent bonds between drug and receptor (DR), as measured by the dissociation constant (Kd) of the DR complex.

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22
Q

what is specificity

A

the degree to which the effects of a drug are due to the one pharmacological action.

23
Q

what happens at equilibrium dissociation

A

association, Kd = Ka

24
Q

what is Kd

A

equilibrium dissociation constant

25
Q

what is Koff

A

dissociation rate cnstant or ff rate constant

26
Q

what is Kon

A

association constant or on rate constant

27
Q

Agonist

A

: A drug that produces a positive effect when bound to a receptor.

28
Q

Potency

A

The dose of drug required to produce a specific effect of given intensity (depends on efficacy and affinity)

29
Q

Efficacy (Emax):

A

The maximum response achievable from a drug.

30
Q

Inverse agonist:

A

A drug that produces a negative effect when bound to a receptor.

31
Q

Antagonist

A

A drug that reduces the effect of an agonist at a given receptor

32
Q

what happens if binding is linearly proportional to effect

A

50% response = 50% binding (Kd)

33
Q

what are the 4 main types of receptor

A

Ligand gated ion channels
G protein coupled receptors
Receptor Kinases
Nuclear receptors

34
Q

Ligand gated ion channels location

A

Membrane

35
Q

G protein coupled receptors location

A

Membrane

36
Q

Receptor Kinases receptors location

A

Membrane

37
Q

Nuclear receptors location

A

Intracellular

38
Q

Ligand gated ion channels effector

A

ion channel

39
Q

Ligand gated ion channels coupling

A

direct

40
Q

Ligand gated ion channels examples

A

nicotinic AcH GABA

41
Q

Ligand gated ion channels structure

A

Oligiomeric assessmbly of subunits surrounding central pore

42
Q

G protein coupled receptors effector

A

channel or enzyme

43
Q

G protein coupled receptors coupling

A

g protein

44
Q

G protein coupled receptors examples

A

muscarinic AcH receptor, adrenreceptors

45
Q

G protein coupled receptors structure

A

monometric or oligometric assembly f subunits comprising f 7 transmembrane helices with intracellular G protein coipling domain

46
Q

Receptor Kinases effector

A

protein kinases

47
Q

Receptor Kinases receptors coupling

A

direct

48
Q

Receptor Kinases receptors examples

A

insulin growth factors and cytokine receptors

49
Q

Nuclear receptors effector

A

gene transcription

50
Q

Nuclear receptors coupling

A

via DNA

51
Q

Nuclear receptors examples

A

steroid receptors

52
Q

Nuclear receptors structure

A

monomeric structure with separate receptor and DNA binding domains

53
Q

Receptor Kinases effector structure

A

single transmembrane helix linking extracellular receptor domain to intracellular kinase domain

Block 1 Pharmocology (17 decks)

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