Cough and Cold drugs / Respiratory drugs Flashcards
name the 2 categories of anti-asthmatics and the drug classes with drug names
controller (anti-inflammatory)
- inhaled corticosteroids e.g. fluticasone
- leukotriene pathway inhibitor e.g. montelukast/zileuton
- anti-IgE monoclonal antibody e.g. omalizumab
- anti-IL5/IL-4R monoclonal antibody e.g. other zumabs
reliever (bronchodilator)
- b2 agonists (SABA, LABA, ultra LABA) e.g. salbutamol, salmeterol/formoterol, idacaterol
- muscarinic antagonists e.g. ipratropium bromide, tiotropium bromide
- methylxanthine e.g. theophylline
fluticasone
drug class + MOA + uses + side effects
Drug class: inhaled corticosteroids (controller)
MOA: nuclear receptor to decrease transcription of inflammatory cytokines
Uses: first line prophylactic for asthma (inhaled)
Side effects: oropharyngeal candidiasis, throat infections, easy bruising (thrombocytopenia)
montelukast/zileuton
drug class + MOA + uses + side effects
Drug class: leukotriene pathway inhibitor (controller)
MOA: inhibits5- lipo oxygenase enzyme to prevent production of leukotrienes
Uses: more for aspirin-induced asthma
Side effects: shunting to other pathways
omalizumab
drug class + MOA + uses
Drug class: anti-IgE monoclonal antibody (controller)
MOA: IgE is an important antibody in immunity and inflammation and hence binding to it to inhibit it can prevent stimulation of immunity/inflammation (such as prevention of mast cell degranulation)
Clinical uses: prophylaxis and treatment of chronic asthma
other zumabs (drug class + MOA + uses)
Drug class: anti-IL5/IL4R monoclonal antibody (controller)
MOA: binds to the cytokine sth inhibit immunity-induced inflammation
clinical uses: treatment for severe asthma that does not respond to the above
mechanism of action of B2 agonists
increase adenyl cyclase and cAMP = decrease calcium concentration = smooth muscle relaxation
also has additional functions: mast cell stabilisation + increase mucociliary clearance
salbutamol
drug class + uses + duration of action
Drug class: short acting BA
Uses: bronchiole smooth muscle relaxation
Duration of action: rapid (3-6 hours)
salmeterol/formoterol (drug class + MOA + duration of action)
Drug class: long acting BA
MOA/uses: maintenance and prevention
Duration: taken twice daily (12 hours)
indacaterol (drug class + MOA + duration of action)
Drug class: ultra long acting BA
MOA/uses: only used in COPD (together with tiotropium bromide as a bronchodilator)
Duration: once daily (24 hours)
ipratropium bromide/tiotroprium bromide (drug class + MOA + uses + side effects)
Drug class: muscarinic inhibitor
MOA: inhibit m3-mediated bronchoconstriction and reduce secretions
Uses: tiotropium is a first-line bronchodilator in COPD (along with indacaterol)
Side effects: unpleasant taste and dry mouth (affects compliance) + urinary retention in elderly
theophylline (drug class + MOA + side effects)
Drug class: methylxanthines
MOA: inhibits PDE4 enzyme, resulting in cAMP accumulation and hence broncho-relaxation (similar to B2 agonist)
also has additionally anti-inflammatory effects on mast cells and T cells (once again, similar to B2 agonists)
Side effects: has a narrow therapeutic window + drug-drug interaction with antimicrobials
first line asthmatic therapy when there is an attack
ICS-formoterol is the preferred reliever of choice
double whammy in one puff:
- controller: inhaled corticosteroid
- reliever: formoterol (rapid acting that lasts for 3-6 hours)
maintenance therapy for asthma
ICS-LABA with SABA salbutamol for reliever when necessary
do we regularly use indacaterol?
no, as it is a long-acting BA and is only used for COPD (along with tiotroprium bromide)
what do we give if asthma is poorly controlled (even with ICS-LABA)?
we give theophylline as an adjunct therapy
why do we have to give ICS along with LABA for long-term maintenance therapy?
over time, LABA can cause tolerance by down regulation of receptors and if an attack was to occur, the patient would not be susceptible to salbutamol = increased risk of athsma-related death.
hence we have to give ICS in order to increase B2 receptor level
what are the drug classes for cough/cold?
to reduce blocked nose, you make the mucus more watery and you increase the excretion of it. worse come to worse, you try to decrease production of mucus.
make mucus more watery:
- expectorants
- mucolytics
increase excretion of mucus:
- decongestants
- mucokinetics
decrease production of mucus:
- antihistamines
- mucoregulators
to reduce cough, you suppress the cough center.
suppress cough center:
- suppressant
what are the drug examples for each cough/cold drug class?
suppressant:
codeine, dextromethorphan
expectorant:
guaiphenesin
mucolytic:
aerosolised N-acetylcysteine
carbocisteine
decongestant:
pseudoephedrine
oxymetazoline
B2 agonists:
salbutamol, salmeterol, ambroxol
anti-histamine:
1st gen - diphenhydramine
2nd gen - cetirizine. loratadine, fexofenadine
muscarinic inhibitor:
ipratropium bromide, tiotropium bromide
codeine (drug class and MOA)
drug class: suppressant/antitussive
MOA: works as an opioid receptor agonist and suppresses cough center in brainstem
dextromethorphan (drug class and MOA)
drug class: suppressant/antitussive
MOA: works as an opioid receptor agonist and suppress cough center in brainstem
side effect of suppressants e.g. codeine and dextromethorphan
shuts down GIT and urinary tract - constipation/urinary retention
addition as codeine is converted to morphine in the body
contraindications of codeine and dextromethorphan
codeine is not given in those < 18 due to addiction problem but dextromethorphan is not given to children < 4 due to sedation, GI disturbance and CVS disturbance
guaiphenesin (drug class and MOA)
Drug class: expectorant
MOA: increases water content of mucus to make it looser and easier to expel
contraindication of guaiphenesin
cannot be used in young children < 2 years old
aerosolised n-acetylcysteine and carbocisteine (drug class and MOA)
Drug class: mucolytics
MOA: breaks down disulphide bonds and makes mucus less viscous
additional anti-inflammatory effect
pseudoephedrine/oxymetazoline (drug class and MOA)
Drug class: decongestant
MOA: a1 agonist; increase vasoconstriction of nasal passage
diphenhydramine/cetirizine/fexofenadine (drug class and MOA)
Drug class: anti-histamine
MOA: H1 antagonist; decrease secretions and vasodilator
ipratropium bromide/tiotropium bromide (drug class and MOA)
Drug class: muscarinic antagonists
MOA: m3 antagonist; decrease mucus hyper secretion (does not inhibit basal secretion)
