Core Drugs Of Asthma Flashcards

1
Q

what are the main drugs used to treat asthma ?

A

Salbutamol

Fluticasone

Mometasone

Budesonide

Montelukast

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2
Q

what is the mechanic of action of Salbutamol?

A

Agonist at the β2 receptor on airway smooth muscle cells. Activation reduces Ca2+ entry and this prevents smooth muscle contraction.

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3
Q

what is the drug target of Salbutamol?

A

Beta 2 (β2) adrenergic receptor

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4
Q

what are the side effects of Salbutamol?

A

Palpitations/ agitation

Tachycardia/ Arrythmias

Hypokalaemia (at higher doses)



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5
Q

what are some facts about Salbutamol?

A

Salbutamol is a short acting beta agonist (SABA). It’s half life is 2.5-5hours.



Beta 2 selectivity is not absolute – as a result, cardiac (beta 1) effects can be seen.

Hypokalaemia can be caused via an effect on sodium/ potassium ATPase. This effect can be exacerbated by coadministration with corticosteroids



In 2020, salbutamol was the 12th most commonly prescribed drug in the West London area

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6
Q

what is the mechanic of action of Fluticasone?

A

Very powerful drugs. Multiple actions on many different cell types. Fluticasone directly decreases inflammatory cells such as eosinophils, monocytes, mast cells, macrophages, and dendritic cells. It reduces the number of these cells and also the number of cytokines they produce.

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7
Q

what is the drug target of Fluticasone?

A

Glucocorticoid receptor

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8
Q

what are the side effects of Fluticasone?

A

Local side effects:

Sore throat, hoarse voice, opportunistic oral infections



Systemic side effects:

Growth retardation in children

Hyperglycaemia

Decreased bone mineral density

Immunosuppression

Effects on mood

(Many others)

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9
Q

what are some facts about Fluticasone?

A

Greater affinity for the glucocorticoid receptor compared to cortisol.

Oral bioavailability <1%. Therefore, any systemic delivery via the inhaled route is predominantly through the pulmonary vasculature.

In 2020, fluticasone was the 72nd most commonly prescribed drug in the West London area

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10
Q

what is the mechanic of action of Mometasone?

A

Very powerful drugs. Multiple actions on many different cell types. Mometasone directly decreases inflammatory cells such as eosinophils, monocytes, mast cells, macrophages, and dendritic cells. It reduces the number of these cells and also the number of cytokines they produce.

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11
Q

what is the drug target of Mometasone?

A

Glucocorticoid receptor

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12
Q

what are the side effects of Mometasone?

A

Local side effects:

Sore throat, hoarse voice, opportunistic oral infections



Systemic side effects:

Growth retardation in children

Hyperglycaemia

Decreased bone mineral density

Immunosuppression

Effects on mood

(Many others)



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13
Q

what are some facts about Mometasone?

A

Greater affinity for the glucocorticoid receptor compared to cortisol.


Oral bioavailability <1%. Therefore, any systemic delivery via the inhaled route is predominantly through the pulmonary vasculature.


In 2020, mometasone was the 62nd most commonly prescribed drug in the West London area





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14
Q

what is the mechanic of action of Budesonide?

A

Very powerful drugs. Multiple actions on many different cell types. Budesonide directly decreases inflammatory cells such as eosinophils, monocytes, mast cells, macrophages, and dendritic cells. It reduces the number of these cells and also the number of cytokines they produce

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15
Q

what is the drug target of Budesonide?

A

Glucocorticoid receptor

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16
Q

what are the side effects of Budesonide?

A

Local side effects:

Hoarse voice, opportunistic oral infections



Systemic side effects:

Growth retardation in children

Hyperglycaemia

Decreased bone mineral density

Immunosuppression

Effects on mood

(Many others)



17
Q

what are some facts about Budesonide?

A

Oral bioavailability >10%. Therefore, inhaled budesonide will still result in some systemic absorption through the gastro-intestinal tract.



Less potent than fluticasone and mometasone





In 2020, budesonide was the 71st most commonly prescribed drug in the West London area



18
Q

what is the mechanic of action of Montelukast?

A

Antagonism of CysLT1 leukotriene receptor on eosinophils, mast cells and airway smooth muscle cells decreases eosinophil migration, broncho-constriction and inflammation induced oedema

19
Q

what is the drug target of Montelukast?

A

CysLT1 leukotriene receptor

20
Q

what are the side effects of Montelukast?

A

Mild side effects:

Diarrhoea

Fever

Headaches

Nausea or vomiting



Serious side effects:

Mood changes

Anaphylaxis



21
Q

what are some facts about Montelukast?

A

For prophylaxis of exercise-induced bronchoconstriction, montelukast should be administered at least 2 hours before initiating exercise.



In 2020, montelukast was the 95th most commonly prescribed drug in the West London area