Respiratory Drugs Flashcards
Aims of pharmacological treatment for asthma
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.
Mechanism of action for beta 2 agonists eg SABA eg salbutamol
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
Beta 2 agonist SABA
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
Beta 2 agonists side affects
§ 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
Inhaled corticosteroids (ICS)
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
Beta 2 agonists examples
SALBUTAMOL & TERBUTALINE
Inhaled steroids (ICS) asthma treatment examples
Beclomethasone , Budesonide, Ciclesonide, Fluticasone
Acute asthma attack = Prednisolone orally, hydrocortisone IV
Side effects of steroids used to treat asthma (ICS)
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.
Long acting beta 2 agonists (LABA)
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)
Examples of long acting beta 2 agonists (LABA) in asthma treatment
Salmeterol and formoterol
Give examples of different types on inhalers
MDI
MDI with spacer
Diskus
Handihaler
Twisthaler
How is the type of inhaler device decided?
§ 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
How is an inhaler used?
Preparation
1. Hold the inhaler upright.
- Remove the cap from the inhaler and inspect to make sure there is nothing inside the inhaler mouthpiece.
- 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.
- Breathe out gently and slowly away from the inhaler until your lungs feel empty.
- Put your lips around the mouthpiece of the inhaler to create a tight seal.
- Start to breathe in slowly and steadily whilst at the same time pressing the canister on the inhaler once.
- Continue to breathe in slowly until your lungs feel full.
- Remove the inhaler from your mouth and seal your lips.
- Hold your breath for 10 seconds, or as long as you are comfortably able to.
- 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.
What does a combination inhaler contain?
ICS + LABA
Eg of combination inhalers for asthma treatment
Seretide and symbicort
SMART inhalers (single maintenance and deliver therapy)
Uses combined inhaler as maintenance & reliever therapy
§ ICS + LABA
§ Does not use their SABA
§ Fast action of FORMETEROL
Name different types of relievers, controllers, preventers and combination asthma drug therapies.
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
Leukotrines receptor antagonists (LRTA)
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.
Example of leukotrines receptor antagonists (LRTA)
Montelukast (Singulair) and Zafirlukast (Accolate)
leukotrines receptor antagonists (LRTA) side effects
Side effects include
§ gastrointestinal upset,
§ dry mouth and thirst.
§ Hypersensitivity reactions have also been reported with the drug including anaphylaxis, angioedema and skin rashes.
Monoclonal antibody in asthma treatment
§ 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
Step wise management of asthma in adults
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
How is acute asthma treated if hospitalisation is not required?
• 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.
Treatment of acute asthma which required hospitalisation;
”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