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Clinical pharmacology and therapeutics > Prescribing for respiratory patients > Flashcards

Prescribing for respiratory patients Flashcards

1
Q

Describe the mechanism of action of selective beta 2 agonists

A

Stimulate B2 adrenoreceptors in the smooth muscle of the airway

Simulate adenylyl cyclase - enzyme catalyses adenosine triphosphate (ATP) - cAMP

Increased cAMP activates protein kinase

Inhibition of enzyme myosin light chain kinase, inhibiting smooth muscle contraction

Results in bronchial smooth muscle relaxtion and bronchodilation

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2
Q

Name 2 short acting beta 2 agonists

A

Salbutamol

Terbutaline

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3
Q

How long is the onset of short acting beta 2 agonists

A

5min

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4
Q

How long is the duration of action for short acting beta 2 agonists

A

4-6 hrs

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5
Q

What do beta 2 agonists improve?

A

Symptoms

FEV1

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6
Q

What are the side effects of beta 2 agonists

A

Tremor
Resting sinus tachycardia
Hypokalemia

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7
Q

How does nebulised or inhaled beta 2 agonists cause fewer side effects

A

Less systemic absorption

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8
Q

Name two long acting beta 2 agonists

A

Formeterol

Salmeterol

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9
Q

What is the onset of action for long acting beta 2 agonists

A

15-45 mins formoterol has faster onset of action

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10
Q

Describe the mechanism of action of antimuscarinincs

A

Muscarinic antagonists - bind to muscarinic receptors in bronchial smooth muscle. Inhibits Ach release from parasympathetic nerve endings

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11
Q

What muscarinic receptor subtypes are there?

A

M1-M5

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12
Q

Name some antimuscarinics

A

Ipratropium
Tiotropium
LAMA
SAMA

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13
Q

What does M3 receptor do?

A

Bronchoconstriction

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14
Q

What does M2 receptor do?

A

Limits Ach release

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15
Q

Describe the selectivity of ipratropium

A

No selectivity - blocks M2 and M3

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16
Q

Which muscarinic receptor do we want to block?

A

M3 (not the M2 and M2 limits Ach release by negative feedback)

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17
Q

Describe the selectivity of tiotropium

A

Same affinity for all receptors but selective to M3 due to very slow dissociation from M3 in comparison to M2

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18
Q

Which two antimuscarinics should not be prescribed together?

A

Nebulised LAMA and SAMA

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19
Q

What are the side effects of antimuscarinics?

A

Headache
Dry mouth
GI motility disturbances

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20
Q

What is the onset of tiotropium?

A

2 hours

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21
Q

What is the duration of action of tiotropium?

A

24 hrs

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22
Q

What are the combined bronchodilators used in COPD?

A

LAMA/LABA

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23
Q

Describe the mechanism of action of corticosteroids in asthma

A

Decreased formation of cytokines which activate eosinophils and are responsible for IgE production and expression of IgE receptors

Inhibit induction of COX2 by cytokines - anti inflammatory effect

Inhibit production of leukotrienes - leukotrienes trigger contraction in the smooth muscle and overproduction results in inflammation

24
Q

Name some inhaled steroids used in asthma as preventer therapy

A

Beclomethasone
Budesonide
Fluticasone
Mometasone

25
What are the differences between different inhaled steroids?
Different potencies
26
What are the side effects of inhaled steroids
Oral candidiasis Hoarse voice Systemic symptoms if long term and high dose therapy
27
What drug can be given to reduce oral candidas?
Nystatin - antifungal
28
Who are triple combination inhalers given to?
LAMA/LABA/ICS to people with COPD with asthmatic features
29
How do you choice which treatment to give a patient
How much they improve symptoms Persons preference and ability to use inhaler The drugs potential to reduce exacerbations Side effects Cost Reduce the number of inhalers
30
When are oral corticoisteroids used in patients with COPD and asthma
In severe cases
31
Which oral corticosteroid is most often used in severe asthma or COPD
Prednisolone
32
What monitoring must be done for someone on high dose steroids
Glucose
33
What adjuvant therapy must be given to a patient who is steroid dependant
PPI | Bone protection
34
Who should you wean from oral corticosteroids?
>40mg prednisolone daily for more than a week Repeat doses in evening Received > 3 weeks of treatment Recently received repeated courses Taken a short course within 1 week of stopping long term therapy Adrenal suppression
35
Describe the mechanism of action of methylxanthines
Unclear Relaxant effect on smooth muscle Increases cAMP - inhibition of phosphodiesterase Bronchodilator action
36
What are the indications for methylxanthine use?
Asthma | COPD
37
Name an IV methylxanthine
Aminophylline
38
What is aminophylline used for?
Acute exacerbations of asthma
39
Name some oral methylxanthines
Theophylline and aminophylline
40
Describe the metabolism and clearance of theophylline
Cytochrome P450 | Clearance declines with age and comorbidity
41
Describe the therapeutic index of methylxanthines
Narrow
42
What is the level of methylxanthines
10-20mg/L
43
When do you measure methylxanthine levels
IV- 6 hrs after infusion starts and daily if continues for >24 hrs Oral - 4-6hrs post dose and at least 5 days after starting treatment
44
Which rugs increase the levels of methylxanthine
Ciprofloxacin Erythromycin Smoking - reduction in dose required by 33%
45
Which drugs decrease the levels of methylxanthine
Rifampicin | Ritonavir
46
What are the side effects of methylxanthine
Headache Nausea Insomnia
47
Describe signs of toxicity of methylxanthine
``` Vomiting Headache Tachycardia Ventricular arrhythmia Convulsions ```
48
How do you convert IV aminophylline to oral theophylline?
Calculate the total amount administered in 24 hours by multiplying the hourly infusion rate by 24. This calculation assumes infusion concentration prepared is 1mg/ml. Multiply the total aminophylline dose administered in 24 hours by 0.8, which is the salt correction factor. Divide the total amount administered in 24 hours by the dosing interval for oral administration, e.g. divide by 2 for twice daily dosing.
49
How do you convert IV aminophylline to oral aminophylline?
Calculate the total amount administered in 24 hours by multiplying the hourly infusion rate by 24. This calculation assumes infusion concentration prepared is 1mg/ml. Divide the total amount administered in 24 hours by the dosing interval for oral administration, e.g. divide by 2 for twice daily dosing. It is assumed that oral aminophylline has 100% bioavailability.
50
Name some mucolytics
Acetylcysteine | Carbocysteine
51
Describe the mechanism of action of mucolytics
Reduces goblet cell hyperplasia Reduces mucus glycoprotein production Helpful in chronic productive cough
52
Describe the mechanism of action of leukotriene receptor antagonists
Leukotrienes (LTC4, LTD4, LTE4) are potent inflammatory eicosanoids released from mast cells and eosinophils with bronchoconstrictor and pro-inflammatory actions LTRA bind to cysteinyl leukotriene (CysLT) receptors in airway smooth muscle cells and airway macrophages, and on other pro-inflammatory cells (including eosinophils) Blocking bronchoconstriction and mucous secretion
53
What are the side effects of LTRA
Headache Psychiatric GI
54
Describe how LTRAs are prescribed
``` Asthma step 3+ (NICE) Review response to treatment in 4 to 8 weeks Additive effect only Useful in exercise induced asthma Best taken at night ```
55
Name some LTRAs
Montelukast | Zafirlukast
56
Describe the treatment of an acute COPD exacerbation
Antibiotics - only if infective. Amox/doxy for 5 days Bronchodilators - nebulised salbutamol/ipratropium or salbutamol via aerochamber Corticosteroids - prednisolone 30mg for 5 days

Clinical pharmacology and therapeutics (27 decks)

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