Respiratory Drugs Flashcards

1
Q

Aims of pharmacological treatment for asthma

A

Complete control defined as - § No Daytime symptoms
§ No Night-time wakening due to asthma § No need for rescue medication
§ No asthma attacks
§ No exacerbations
§ No Limitations on activity including exercise § Normal lung function(FEV1 &/or PEF >80%) § Minimal side effects from the medication.

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2
Q

Mechanism of action for beta 2 agonists eg SABA eg salbutamol

A

They are selective to beta 2 receptors on the lungs

Salbutamol is a bronchodilator which acts on B2 receptors
Stimulation of adenylate cyclase
Increase cAMP production

Bronchodilating affects:
Phosphorylase’s the myosin kinase
Relaxation of smooth muscle
Causing bronchodilation

Anti bronchoconstriction affects:
Mast cell membrane stabilisation
No histamine release
No bronchoconstriction

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3
Q

Beta 2 agonist SABA

A

Reliever
§ SALBUTAMOL & TERBUTALINE
§ Short acting
§ Onset of action is rapid (often within 5 - 15 minutes)
§ Produce bronchodilation for up to six hours.
§ Inhaler , Nebuliser, Intravenous, Oral

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4
Q

Beta 2 agonists side affects

A

§ TREMOR
§ Fine skeletal muscle tremor from stimulation of B2 adrenoceptors.

§ TACHYCARDIA and Palpitations - possible arrhythmias

§ HYPOKALAEMIA
§ due to promotion of potassium uptake into cells. § Cautions include CV, prolonged QT, decreased K

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5
Q

Inhaled corticosteroids (ICS)

A

Preventer not a reliever
§ Most effective class of drug in the treatment of chronic asthma
§ Some improvements in asthma symptoms within 24 hours
§ Maximum effect after 1-2 weeks.
§ Short term and long term anti-inflammatory effects
§ Supress inflammation and the immune response
§ Commence – if using SABA >3 times a week
- Asthma symptoms present >3 times a week -Woken at night once a week
§ Beclomethasone , Budesonide, Ciclesonide, Fluticasone

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6
Q

Beta 2 agonists examples

A

SALBUTAMOL & TERBUTALINE

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7
Q

Inhaled steroids (ICS) asthma treatment examples

A

Beclomethasone , Budesonide, Ciclesonide, Fluticasone
Acute asthma attack = Prednisolone orally, hydrocortisone IV

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8
Q

Side effects of steroids used to treat asthma (ICS)

A

Main :
§ oral candidiasis due to steroid depositing in oropharyngeal area.
§ Prevent by using spacer device or by gargling after use of the inhaler.
§ dysphonia (hoarseness)
- caused by deposition of the inhaled steroid on vocal
cords
and myopathy of laryngeal muscles.
§ This occurs in 1/3 of patients using inhaled corticosteroids.
§ However should be less troublesome if using breath- actuated delivery.

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9
Q

Long acting beta 2 agonists (LABA)

A

Controllers
Eg salmeterol and formoterol (prolonged receptor activity)

Longer acting - for up to 12 hours
§ Slower onset of action then a short acting beta2-adrenoreceptor agonist.
§ SHOULD NOT be used without the concurrent use of inhaled steroid
(either as a separate inhaler or in a LABA/ICS combination inhaler)

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10
Q

Examples of long acting beta 2 agonists (LABA) in asthma treatment

A

Salmeterol and formoterol

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11
Q

Give examples of different types on inhalers

A

MDI
MDI with spacer
Diskus
Handihaler
Twisthaler

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12
Q

How is the type of inhaler device decided?

A

§ CAN THE PATIENT USE IT!!! Compliance is critical
§ Determined by the choice of drug & strength
§ Should be assessed by a competent healthcare professional.
§ Titrated against clinical response to ensure optimum efficacy.
§ Patient specific plan – increase / decrease inhaler
§ Reassess inhaler technique as part of structured clinical review.
§ In children MDI and spacer are the preferred method of delivery of B2 agonists or inhaled corticosteroids

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13
Q

How is an inhaler used?

A

Preparation
1. Hold the inhaler upright.

  1. Remove the cap from the inhaler and inspect to make sure there is nothing inside the inhaler mouthpiece.
  2. Shake the inhaler well.

Inhalation
4. Sit or stand up straight and slightly tilt your chin up. This position helps the medication to better reach the lungs.

  1. Breathe out gently and slowly away from the inhaler until your lungs feel empty.
  2. Put your lips around the mouthpiece of the inhaler to create a tight seal.
  3. Start to breathe in slowly and steadily whilst at the same time pressing the canister on the inhaler once.
  4. Continue to breathe in slowly until your lungs feel full.
  5. Remove the inhaler from your mouth and seal your lips.
  6. Hold your breath for 10 seconds, or as long as you are comfortably able to.
  7. Breathe out gently, away from your inhaler.

Final steps
12. Once you have finished using your inhaler, replace the cap. If you’ve used an inhaler that contains steroids, rinse your mouth with water to reduce the chance of side effects.

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14
Q

What does a combination inhaler contain?

A

ICS + LABA

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15
Q

Eg of combination inhalers for asthma treatment

A

Seretide and symbicort

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16
Q

SMART inhalers (single maintenance and deliver therapy)

A

Uses combined inhaler as maintenance & reliever therapy
§ ICS + LABA
§ Does not use their SABA
§ Fast action of FORMETEROL

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17
Q

Name different types of relievers, controllers, preventers and combination asthma drug therapies.

A

Relievers:
Short acting beta agonists
Salbutamol
Fenoterol

Anticholingergics
Ipatropium bromide
Tiotropium

Controllers:
Long acting beta agonists
Salmeterol
Formoterol

Preventers:
Inhaled corticosteroids (ICS)
Ciclesonide
Beclomethasone
Budesonide
Fluticasone

Leukotriene receptor antagonist:
Montelukast (tablets)

Combinations:
Budesonide + formoterol
Fluticasone + salmeterol

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18
Q

Leukotrines receptor antagonists (LRTA)

A

Add on to other medications
Montelukast (Singulair) and Zafirlukast (Accolate)
§ Inhibit the leukotriene induced bronchoconstriction by blocking leukotriene receptors.
§ Most useful in mild to moderate asthma, exercise induced asthma and asthma provoked by NSAIDs including aspirin.

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19
Q

Example of leukotrines receptor antagonists (LRTA)

A

Montelukast (Singulair) and Zafirlukast (Accolate)

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20
Q

leukotrines receptor antagonists (LRTA) side effects

A

Side effects include
§ gastrointestinal upset,
§ dry mouth and thirst.
§ Hypersensitivity reactions have also been reported with the drug including anaphylaxis, angioedema and skin rashes.

21
Q

Monoclonal antibody in asthma treatment

A

§ Eg Omalizumab (Xolair)is a monoclonal antibody
§ Used in the treatment of severe and persistent asthma that cannot be controlled by existing regimens available to treat asthma.
§ Subcutaneous injection
§ It binds specifically to IgE and removes both circulating and tissue IgE.
§ Leads to a reduction of high affinity IgE receptors on mast cells, basophil cells and dendritic cells.
§ Treatment with the drug gradually reduces airway inflammation in asthma with a peak response after 12-16 weeks.
§ Specialist respiratory consultants & shared care

22
Q

Step wise management of asthma in adults

A

SABA as required (unless using MART)- consider moving up if using three + doses a week
low dose ICS- regular preventer
Initial add on therapy = Add inhaled LABA to low dose ICS
Additional controller therapies = increase ICS to medium dose or add LTRA, if no responses to LABA consider stopping
Specialist therapies- refer patients for specialist care

23
Q

How is acute asthma treated if hospitalisation is not required?

A

• Use a short-acting beta-2 agonist via a large- volume spacer to relieve acute symptoms.

• For an adult, give 4 puffs initially, followed by 2 puffs every 2 minutes according to response, up to 10 puffs.

• For a child, give a puff every 30–60 seconds, up to 10 puffs. Each puff should be given one at a time and inhaled with five tidal breaths. Repeat every 10–20 minutes according to clinical response.

• Consider advising quadrupling inhaled corticosteroid (ICS) at the onset of an asthma attack and for up to 14 days in order to reduce the risk of needing prescribed oral steroids.

24
Q

Treatment of acute asthma which required hospitalisation;

A

”O SHIT ME”
Oxygen - maintain Sats 94-98%

Salbutamol – high dose back to back nebs 2.5-5mg
Hydrocortisone 100mg ( or prednisolone 40mg)
Ipratropium 4-6 hourly
Theophylline / Aminophylline

Magnesium sulphate
Escalate early

25
Q

Obs for moderate acute asthma

A

Increasing symptoms
PEF >50-75% of best or predicted
No features of acute severe asthma

26
Q

Obs for acute severe asthma

A

Any one of:
PEF 33-50% best or predicted
Resp rate greater or equal to 25
Heart rate greater or equal to 110
Inability to complete sentences in one breath

27
Q

Obs for life threatening asthma

A

In a patient with severe asthma, anyone of the following:
PEF less 33% best or predicted
SpO2 < 92%
PaO2 <8KPa
‘Normal’ PaCO2 (4.6-6.0 kPa)
Altered conscious level
Exhaustion
Arrhythmia
Hypotension
Cyanosis
Silent chest
Poor resp effort

28
Q

Obs for near fatal asthma

A

Raised PaCO2 and or requiring mechanical ventilation with raised inflation pressures

29
Q

What should be measured in an initial assessment of acute asthma?

A

Clinical features: breathlessness, tachycardia, cyanosis, silent chest
PEF or FEV1
Pulse oximetry
ABG
CXR sometimes

30
Q

How is magnesium used in the treatment of severe asthma?
And what are the side effects?

A

§ Treatment of severe asthma in adults if life-threatening features are present.
§ Adjunct in very severe cases of life-threatening asthma if PEF <50%.
§ Bronchodilates by blocking calcium channels in smooth muscle cell membranes, therefore reducing calcium influx into the cell.

§ Side effects
§ including atrioventricular block so administration requires the patient to have continuous ECG monitoring.
§ Other side effects include potentiation of the hypotensive effects of calcium channel blockers

31
Q

What additional therapy can be added to control exercise induced asthma?

A

If exercise induced asthma is a specific problem in patients taking ICS who are otherwise well controlled, consider adding one of the following therapies –
§ Leukotriene receptor antagonist
§ Long acting B2 agonist (LABA)
§ Sodium cromoglicate or nedocromil sodium
§ Oral B2 agonists
§ Theophylline (aminophylline)

Immediately before exercise, inhaled short acting B2 agonists are the drug of choice

32
Q

Aims of COPD treatment

A

§ To make an accurate diagnosis of COPD
§ Treat bronchospasm and obstruction
§ Treatment of hypoxia and respiratory failure
§ Treat Infection if present
§ To provide Smoking Cessation
§ To Provide pulmonary rehabilitation
§ Manage acute exacerbations of COPD
§ Assessment for long term oxygen therapy
§ Ensure yearly Influenza & pneumococcal vaccines

33
Q

Initial treatment for COPD

A

§ For breathlessness and/or exercise limitation use as required short acting beta 2-agonts such as salbutamol or terbutaline.

§ And/or a short acting antimuscarinic drug such as Ipratropium use as required

§ Short acting beta2 agonists can be continued with any further additional treatment
§ Short acting antimuscarinic antagonists however must be stopped if longer acting muscarinic agents (such as Tiotropium) are introduced.

34
Q

Antimuscarinics in COPD management

A

Eg sama/lama
Ipatropium/tiotropium
§ Main benefit is in the treatment of COPD and are of less benefit in mild to moderate asthma.
§ Nebuliser for severe exacerbations of asthma
§ Antimuscarinic drugs have a slower onset of action (30-60minutes) compared to salbutamol (5-10 minutes)
§ Given exclusively by inhalation (dry powder or aerosol) or via a nebuliser. (caution glaucoma)

35
Q

LAMA (long acting anti muscuranic) in COPD management

A

§ Its effect last 24 hours
§ Side effects include
§ dry mouth (suck on boiled sweets)
§ in men in particular - difficulties in passing urine
§ Used once daily and should not be used with any short acting antimuscarinic drug such as Ipratropium (Atrovent).
§ Aclidinium (Ekilira Genuair) is a further new LAMA to the UK market.
§ The drug is used twice daily usually morning and evening
§ Tiotropium (Spiriva) & Glycopyrronium (Seebri breezhaler)

36
Q

Role of inhaled steroids in COPD

A

§ Controversial and is the subject of ongoing debate.
§ Not recommended as monotherapy as they
§ have only modest effect in relieving dyspnoea and improving lung function
§ less effect than long-acting bronchodilators.

§ Some suggestion that use of ICS inhalers in COPD patients increases the risk of serious pneumonia.
§ The risk is particularly increased and dose dependent with the ICS, fluticasone

37
Q

Oral corticosteroids for COPD

A

Prednisolone

Maintenance use of oral corticosteroid therapy in COPD is not recommended
Some patients with advanced COPD may require maintenance oral corticosteroids when these cannot be withdrawn following an exacerbation.
The does of oral corticosteroids should be kept as low as possible
For exacerbations usually 30mg Prednisolone for 5 to 7 days

38
Q

THEOPHYLLINE /
AMINOPHYLLINE for COPD MANAGEMENT

A

§ Vasodilator, anti-inflammatory and apparently an immunomodulatory actions.
§ Additive effect with short or long acting beta2- adrenoceptors and prolong the duration and action of the drugs compared to when used alone.
§ Narrow therapeutic index
§ Aminophylline hydrolysed rapidly after
absorption from the gut to theophylline
§ Measurement of theophylline concentrations is valuable as a guide to effective dosing of the drug.

39
Q

Theophylline side effects

A

§ Gastrointestinal upsets include nausea, vomiting and diarrhoea.
§ CNS stimulation,
§ including insomnia, irritability and occasional seizures at very high plasma concentrations
§ Cardiac stimulation
§ can produce various arrhythmias at higher doses or unexpected higher blood levels.
§ Hypokalaemia can occur acutely after IV injection which can also promote cardiac arrhythmias
§ Drug interactions with many drugs.
§ such as ciprofloxacin, erythromycin, clarithromycin, fluconazole, and ketoconazole can all precipitate theophylline toxicity.

40
Q

When should cor pulmonale be considered in COPD patients?

A

A diagnosis of Cor pulmonale should be considered if patients have:
§ Peripheral oedema,
§ Raised venous pressure
§ systolic parasternal heave
§ A loud pulmonary second heart sound.

41
Q

Nebulisers in COPD patients

A

§ Patients with distressing/ disabling breathlessness despite maximal therapy using inhalers should be considered for nebuliser therapy.
§ Should not be prescribed without an assessment of the patient’s and/or carer’s ability to use the device.

42
Q

Long term oxygen therapy for COPD

A

§ LTOT is indicated in patients with COPD who have PaO2 less than 7.3kPa when stable or a PaO2 greater than 7.3 and less than 8 kPa when stable and one of the following
§ Secondary polycythaemia
§ Nocturnal hypoxaemia (oxygen saturation (SaO2) of arterial blood less than 90% for more than 30% of the time)
§ Peripheral oedema or pulmonary hypertension
§ Reminder – Clinicians should always be aware that inappropriate oxygen therapy in patients with COPD may cause respiratory depression (type 2 Respiratory Failure)

43
Q

Mucolytics for COPD patients

A

§ Used in patients with chronic productive cough with thick viscous sputum.
§ Not be used routinely to prevent exacerbations in patients with stable COPD.
§ Carbocisteine should be avoided in those patients with history of peptic ulceration.
§ Can cause bleeding from the GI tract (blood in vomit or black tarry stools)
§ Carbocisteine & Erdosteine

44
Q

Acute exacerbation of COPD treatment

A

§ Oxygen – Sats 88-92% if risk of retaining C02
§ Steroids – 30mg for 7-14 days
§ Bronchodilators – salbutamol & ipratropium

§ Antibiotics – if purulent sputum
First choice oral antibiotics include:
§ Amoxicillin 500 mg three times a day for 5 days.
§ Doxycycline 200 mg on first day, then 100mg once a day for 5-day course
in total.
§ Clarithromycin 500 mg twice a day for 5 days.
§ Aminophylline
§ Consider RESCUE PACKS on discharge - ANTIBIOTICS & STEROIDS
§ END stage – opioids / benzodiazepines

45
Q

When should low dose antibiotic be used for a patient with COPD?

A

§ Oral prophylactic antibiotic therapy eg low dose azithromycin 500mg
§ Consider azithromycin (usually 250 mg 3 times a week)
for people with COPD if they:
• donotsmokeand
• haveoptimisednon-pharmacologicalmanagementand inhaled therapies, relevant vaccinations and (if appropriate) have been referred for pulmonary rehabilitation and
• continuetohave1ormoreofthefollowing,particularlyifthey have significant daily sputum production:
• frequent(typically4ormoreperyear)exacerbationswith sputum production
• prolongedexacerbationswithsputumproduction • exacerbationsresultinginhospitalisation.

46
Q

Dexamethasone for covid treatment

A

¡ Dexamethasone is a corticosteroid
¡ Given to patients hospitalised for COVID-19 who are requiring supplemental O2 therapy to maintain O2 saturations of >92%
¡ Dose: 6mg PO
¡ Given for 10 days or the duration the patient is on O2, whichever is shorter
¡ No proven benefit to patients who do not require O2

47
Q

TOCILIZUMAB/SARILUMAB for covid treatment

A

For very immuno suppressed
¡ Monoclonal antibody
¡ IL-6 Inhibitor
¡ Established use in inflammatory arthritis
¡ Works to block the IL-6 release in the inflammatory cascade
¡ Causes immunosuppression – patients are at increased risk of
developing infections for the following 12 weeks

48
Q

Remdesivir for covid (viral) treatment

A

REMDESIVIR
¡ Blocks an enzyme required for viral replication
¡ Given for 3-5 days
¡ Only useful in first 10 days of illness as it works to shorten the illness
¡ Can cause abnormal LFTs – must check!
Becca doesn’t like as can be more harm than good (shorten illness by 2days but affect liver a lot)