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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
Q

What are the differences between different inhaled steroids?

A

Different potencies

26
Q

What are the side effects of inhaled steroids

A

Oral candidiasis
Hoarse voice
Systemic symptoms if long term and high dose therapy

27
Q

What drug can be given to reduce oral candidas?

A

Nystatin - antifungal

28
Q

Who are triple combination inhalers given to?

A

LAMA/LABA/ICS to people with COPD with asthmatic features

29
Q

How do you choice which treatment to give a patient

A

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
Q

When are oral corticoisteroids used in patients with COPD and asthma

A

In severe cases

31
Q

Which oral corticosteroid is most often used in severe asthma or COPD

A

Prednisolone

32
Q

What monitoring must be done for someone on high dose steroids

A

Glucose

33
Q

What adjuvant therapy must be given to a patient who is steroid dependant

A

PPI

Bone protection

34
Q

Who should you wean from oral corticosteroids?

A

> 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
Q

Describe the mechanism of action of methylxanthines

A

Unclear
Relaxant effect on smooth muscle
Increases cAMP - inhibition of phosphodiesterase
Bronchodilator action

36
Q

What are the indications for methylxanthine use?

A

Asthma

COPD

37
Q

Name an IV methylxanthine

A

Aminophylline

38
Q

What is aminophylline used for?

A

Acute exacerbations of asthma

39
Q

Name some oral methylxanthines

A

Theophylline and aminophylline

40
Q

Describe the metabolism and clearance of theophylline

A

Cytochrome P450

Clearance declines with age and comorbidity

41
Q

Describe the therapeutic index of methylxanthines

A

Narrow

42
Q

What is the level of methylxanthines

A

10-20mg/L

43
Q

When do you measure methylxanthine levels

A

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
Q

Which rugs increase the levels of methylxanthine

A

Ciprofloxacin
Erythromycin
Smoking - reduction in dose required by 33%

45
Q

Which drugs decrease the levels of methylxanthine

A

Rifampicin

Ritonavir

46
Q

What are the side effects of methylxanthine

A

Headache
Nausea
Insomnia

47
Q

Describe signs of toxicity of methylxanthine

A 
Vomiting
Headache
Tachycardia
Ventricular arrhythmia 
Convulsions
48
Q

How do you convert IV aminophylline to oral theophylline?

A

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
Q

How do you convert IV aminophylline to oral aminophylline?

A

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
Q

Name some mucolytics

A

Acetylcysteine

Carbocysteine

51
Q

Describe the mechanism of action of mucolytics

A

Reduces goblet cell hyperplasia
Reduces mucus glycoprotein production
Helpful in chronic productive cough

52
Q

Describe the mechanism of action of leukotriene receptor antagonists

A

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
Q

What are the side effects of LTRA

A

Headache
Psychiatric
GI

54
Q

Describe how LTRAs are prescribed

A 
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
Q

Name some LTRAs

A

Montelukast

Zafirlukast

56
Q

Describe the treatment of an acute COPD exacerbation

A

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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