W20 - Lung Medication Flashcards

1
Q

what does understanding and probing structure activity relationships involve

A

studies to determine the atoms or functional groups that are important to a drugs activity

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2
Q

what can these studies lead to

A

identification of the pharmacophore

groups that are identified to be essential for activity

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3
Q

What is the relevence of beta 2 adrenoreceptor in the treatment of asthma

A

beta 2 adrenoreceptor activation leads to smooth muscle relaxation and since they line the bronchial smooth muscle this leads to dilation of the airways which is important for the treatment of asthma.

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4
Q

what were the natural starting point for the development of adrenergic beta 2 agonists

A

adrenaline and noradrenaline

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5
Q

what are some examples of beta 2 agonists

A

salbutamol dobutamine and xamoterol

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6
Q

what molecular target are adrenergic receptors

A

G protein linked receptors

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7
Q

what is the importance of serine in relationship to adrenaline and noradrenaline

A

serine residue interacts with the phenolic groups of the catecholamine via hydrogen bonding

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8
Q

what is the importance of the aromatic ring of the phenylamine residue in relationship to adrenaline and noradrenaline

A

interacts with the catechol ring via van der waals interactiosn

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9
Q

what is the importance of the aspartic residue in relationship to adrenaline and nor adrenaline

A

interacts with the protonated nitrogen of the catecholamine by ionic bonding

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10
Q

why is adrenaline no longer used to treat asthma

A

short duration of action

no selectivity for b2 receptors as it swtiches on all possible adrenergic receptors

leading to side effects mainly in the cardiovascular system

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11
Q

what was adrenaline replaced by

A

isoprenaline

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12
Q

what was the downside of isoprenaline

A

no selectivity between the different types of beta receptors so side effects still evident

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13
Q

how do we provide selectivity to distinguish between the different beta receptors

A

introducing alkyl substituents to the side chain linking the aromating ring and the amine or varying the alkyl substituents on the nitrogen

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14
Q

what is the short duration of isoetharine a result of

A

drugs being taken up by tissues and methylated by the metabolic enzyme catechol o methyltransferase COMT to form an inactive ether

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15
Q

What part of the molecules of isoetharine was the target of COMT

A

the OH on the phenyl ring.

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16
Q

what was essential to note before replacing the meta phenol

A

the group replacing it is still able to bind to the receptor and retain biological activity

but

would not be recognised by the metabolic enzyme

17
Q

what is chiral swtiching

A

mostly relates to racemic drugs that have been on the market for several years and are approaching the end of their patent life