Pharmacology Flashcards
What type of hypersensitivity is the immediate phase of an asthma attack?
Type 1 hypersensitivity
What type of hypersensitivity is the delayed phase of an asthma attack?
Type 4 sensitivity
What is a SABA and give 2 examples?
Short acting beta 2 agonist
Salbutamol and terbutaline
Are SABAs used in asthma or COPD?
Mainly asthma but can occasionally be used in COPD
What actions do SABAs have? (5)
1) Relax airway smooth muscle by agonising beta 2 adrenoceptors on airway smooth muscle
2) Decrease mucus secretions by agonising beta 2 adrenoceptors on goblet cells
3) Increase mucocillary clearance
4) Reduction in intracellular Ca++ concentration
5) Activation of large conductance potassium channels => hyperpolarisation
Side effects of SABAs?
Beta agonist tremor
Tachycardia
Hypokalemia
dysrhythmia
What is a LABA and give 2 examples?
Long acting beta agonist
Salmeterol and formoterol
Are LABAs used in asthma or COPD?
Both
First line in COPD
Second line in asthma
You can give a LABA as monotherapy in asthma. True or false?
False- NEVER give a LABA alone
What is a leukotriene?
Leukotrienes are dirived from mast cells and other inflammatory cells and cause mucus secretion, smooth muscle contraction and oedema. Examples include LTC4, LTD4 and LTE4
What is a leukotriene receptor antagonist and give an example?
A drug which binds to Cys Leukotriene receptors preventing the binding of leukotrienes and preventing muscle contraction in the airway.
Montelukast
Are leukotriene receptor antagonists used in asthma or COPD?
Asthma ONLY
Add on therapy against early and delayed bronchospasm
used in moderate - severe asthma
Can be used in allergic rhinitis
How are leukotriene receptor antagonists administered?
Orally
What is the action of methylxanthines and give 2 examples?
Have bronchodilator and anti inflammatory actions
Unknown molecular mechanism which may involve inhibition of isoforms of PDE
Aminophyline and theophyline
Are methylxanthines used in asthma or COPD?
Asthma mostly but can be used in COPD
Why are methylxanthines not used frequently?
High therapeutic index and have many adverse effects involving the CNS, CVS and GI tract.
Drug interactions involving CYP450 (don’t give with erythromycin/ flucloxacillin)
How are methylxanthines administered?
Orally
How do steroids work briefly?
They have trans activating or transrepressing activity of specific inflammatory or anti-inflamatory genes
Are glucocorticoids used in asthma or COPD?
Mostly asthma but also in ACOS- eosinophic mediated COPD
What are the common adverse effects for ICS?
Dysphonia- horse and weak voice
Orophatyngeal candidiasis (oral thrush)
Both due to deposition in the oropharynx
When would an oral steroid such as prednisalone be used?
In severe asthma but always in combination with an ICS and only in the short term due to the side effects
What is a chromone and give an example?
Anti inflammatory drug (non steriodal)
‘Mast cell stabaliser’
Not as effective as ICS
Sodium Chromoglicate
When may a chromone be used?
In children and young adults with asthma (especcialy exercised induced. Given qds
In rhinitis and rhinorrhoea
Give an example of a monoclonal antibody against IgE and its mechanism of action?
Omalizumab IV
Binds to IgE via Fc to prevent IgE binding to Fc receptors on mast cells, eosinophils and basophils
Give an example of a monoclonal antibody against IL5 and its mechanism of action?
Mepolizumab SC
Blocks the effect of TH2 cytokine IL5 which is responsible for eosinophilic inflammation
What is a LAMA and give 2 examples?
Long acting muscarinic antagonist
Tiotropium
Glycopyrronium
How do SAMAs and LAMAs cause smooth muscle relaxation?
The block the M3 muscarinic GPCR found on airway smooth muscle.
Activation of this receptor leads to smooth muscle contrition via Gq/11 and phospholipase C
Give an example of a SAMA?
Ipratropium
Why is ipratropium inferior to other muscasrinic receptor antagonists?
It is non selective so blocks M1, M2 and M3 muscarinic receptors equally. Blockade of M1 and M3 is beneficial but blockade of M2 is not.
Other muscarinic receptor antagonists are M3 selective
Are LAMAs used in asthma or COPD?
COPD first line
Asthma second line
Give 2 examples of ultra LABAs?
Indaterol and Oldaterol
What is a phosphodiesterase 4 inhibitor and give an example?
It inhibits the PDE enzyme. The PDE enzyme breaks down cAMP which promotes smooth muscle relaxation
Roflumilast
Are phosphodiesterase 4 inhibitors used in asthma or COPD?
COPD only
Why are phosphodiesterase 4 inhibitors not commonly used
Not well tolerated
Side effects including headache, nausea, vomiting and weight loss
What may be the cause of glucocorticoid unresponsiveness in COPD?
Oxidative/ nutritive stress due to smoking
What are the advantages of a spacer device?
1) Avoids coordination problems encountered with an MDI
2) Reduces oropharangeal and larngeal side effects
3) Reduces systemic absorption from swallowed fraction
4) Allows people to take 2-3 breaths rather an 1 What is
What is a releiver in asthma?
SABA
What are the 1st line preventers in asthma?
ICS
sodium chromoglicate
What are the 2nd line controllers in asthma?
LABA/LAMA (first choice)
Theophyline
Leukotriene receptor antagonist
Anti IgE/ Anti IL5
What classes of drugs are used to treat rhinitis and rhinorrhoea?
Glucocorticoids (topical spray) Antihistamines (oral) Muscarinic receptor antagonists (topical application) Sodium Chromoglicate Leukotriene receptor antagonists Vasoconstrictors
Give an example of a glucocorticoid used in the treatment of rhinitis and rhinorrhoea?
Beclomethasone, Fluticasone, Prednisalone
Most effective in seasonal allergic rhinitis (SAR) and perennial allergic rhinitis (PAR)
Give an example of a muscarinic antagonist used in the treatment of rhinitis and rhinorrhoea?
Ipratropium
Used in PAR and SAR
Give an example of a antihistamine used in the treatment of rhinitis and rhinorrhoea?
Loretidine, cetirizine and fexofenadine
Used in all allergic rhinitis- SAR, PAR and EAR
Give an example of a leukotriene receptor antagonist used in the treatment of rhinitis and rhinorrhoea?
Montelukast
Used in PAR and SAR
Give an example of a vasoconstrictor used in the treatment of rhinitis and rhinorrhoea?
Oxymetazoline
Short term use for reducing congestion