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Bronchial asthma
Individual drugs and status asthmaticus
BRONCHODILATORS
SYMPATHOMIMETICS:
Mechanism of action:
β2 receptor stimulation
Increased cAMP formation
in bronchial muscle cell
Bronchial relaxation
Bronchial asthma therapeutics and status asthmaticus
Use with caution:
Hypertensive
Ischemic heart disease patients
Patients taking digitalis
Salbutamol (Albuterol):
highly selective β2 agonist
not suitable for round-the-clock prophylaxis
Pharmacokinetic & pharmacodynamics:
Oral bioavailability is 50%
Duration of action: 4-6 hrs(oral), 2-3 hrs(inhalational)
Oral therapy reserved for patients unable to use inhalers correctly/adjunct
drug for severe asthma
Side effects:
Muscle tremors(M/C)
Palpitation,
restlessness,
nervousness,
throat irritation
ankle edema
Hypokalaemia
Terbutaline:
Similar to salbutamol
Should not be used on any regular schedule
bronchial hyperreactivity: may even worsen
diminished responsiveness seen after long-term use
Restricted to symptomatic relief of wheezing
Bambuterol:
Biscarbamate ester prodrug of terbutaline
hydrolysed in plasma and lungs by pseudocholinesterase - release the
active drug over 24 hours
Reversible inhibition of pseudocholinesterase
It is indicated in nocturnal and chronic asthma
Salmeterol:
Long acting selective β2 agonist(more lipophilic)
Slow onset of action
Inhalation on a twice daily schedule for
maintenance therapy and for
nocturnal asthma
Concurrent inhaled steroid:
Reduces risk of life-threatening asthma attacks
COPD:
• superior to short-acting β2 agonists
• equivalent to inhaled anticholinergics
• prevent expiratory closure of peripheral airways and
• abolish the reversible component of airway obstruction
Formoterol:
faster onset of action
used on a regular morning-evening schedule for round-the-clock
bronchodilatation
Ephedrine:
has α + β1 + β2 actions
mild slowly developing bronchodilatation lasting for 3–5 hours
not preferred now
low efficacy
frequent side effects
PHOSPHODIESTERASE INHIBITORS:
Methyl xanthines:
Theophyline and its compounds
Mechanism of action:
1. Inhibition of phosphodiesterase (PDE)
2. Blockade of adenosine receptors
3. Interleukin-10 release
4. Effects on gene transcription
5. Effects on apoptosis
6. Histone deacetylase activation
Bronchial asthma therapeutics and status asthmaticus
Theophylline:
Pharmacokinetics:
Well absorbed orally
Crosses placenta & Secreted in milk
V = 0.5 l/kg
50% plasma protein bound
metabolized in liver by demethylation and oxidation(CYP1A2)
t½ in adults is 7–12 hours(3–5 hours in children)
Saturable kinetics
Dose reduction needed: age>60yrs, CHF, pneumonia, liver failure
Adverse effects:
• Narrow margin of safety
Interactions:
Increase metabolism: Smoking (1.6), phenytoin (1.5), rifampicin (1.5),
phenobarbitone (1.2), charcoal broiled meat meal (1.3)
Inhibit metabolism: erythromycin, ciprofloxacin, cimetidine, oral contraceptives,
allopurinol(2/3)
Effect enhanced: furosemide, sympathomimetics, digitalis, oral anticoagulants,
hypoglycaemics
Effect decreased: phenytoin, lithium
should not be mixed: ascorbic acid, chlorpromazine, promethazine, morphine,
pethidine, phenytoin, phenobarbitone, insulin, penicillin G, tetracyclines,
erythromycin
Uses:
Bronchial asthma and COPD:
Benefits by
• bronchodilatation
• by decreasing release of inflammatory mediators
• promoting eosinophil apoptosis
• Improved mucociliary clearance
• stimulation of respiratory drive and
• Augmentation of diaphragmatic contractility
But rarely used now:
• narrow margin of safety
• limited efficacy
• 3rd line or alternative/adjuvant
ANTICHOLINERGICS:
MECHANISM OF ACTION:
Drugs acting on M3 receptors
Activation of vagus nerve
Bronchodialation(primarily larger airways)
Bronchial asthma therapeutics and status asthmaticus
Ipratropium bromide:
short acting(4-6hr)
Inferior to β2 sympathomimetics in asthma but superior in:
asthmatic bronchitis,
COPD(drug of choice)
and psychogenic asthma
Regular prophylactic use(2–4 puffs 6 hourly)
Additive with β2 agonist(combination used in severe asthma)
Tiotropium bromide:
longer acting(24hrs)
More effective in severe COPD (FEV1<50%)
ANTI INFLAMATORY
CORTICOSTEROIDS:
INHALED STEROIDS:
high topical and low systemic activity
indicated in all cases of persistent asthma
Started with 100–200 μg BD
titrated upward every 3–5 days(max-400 μg QID)
Have no role in: acute attack & status
Peak effect in 4-7days
COPD:
Not much effective
High dose in advanced COPD
Adverse effects:
Hoarseness of voice,
dysphonia,
sore throat,
oropharyngeal candidiasis
Minimised by: spacer, gargling, topical nystatin/clotrimazole
Systemic effect rare (dose>600 μg/day)
Mood changes, osteoporosis, growth retardation children, bruising,
petechiae, hyperglycaemia and pituitary-adrenal suppression
Beclomethasone dipropionate:
pMDI & rotacaps
Intranasal spray (50 μg in each nostril BD–TDS): perennial rhinitis
Budesonide:
high topical: systemic activity ratio(high first pass metabolism)
preferred in more severe cases
Fluticasone propionate:
high potency(double of beclomethasone)
Longer duration and negligible oral bioavailability
inhalational dose is 100–250 μg BD (max 1000 μg/day).
Flunisolide:
seasonal and perennial rhinitis
Ciclesonide:
a prodrug that is cleaved by esterases in the bronchial epithelium to
release the active moiety
oral bioavailability is <1%
extensively bound to plasma proteins in circulation
SYSTEMIC STEROID THERAPY:
1. Severe chronic asthma:
prednisolone 20-60mg/day
dose reduction afeter 1-2 wk attempted
2. Status asthmaticus:
high dose of a rapidly acting i.v. glucocorticoid
generally act in 6-24 hrs
shift to oral for 5-7 days & then inhalational
3. COPD:
short course (1–3 week) of oral glucocorticoid for exacerbation
LEUKOTRIENE ANTAGONISTS:
Montelukast and Zafirlukast:
Competitively antagonize cysLT1 receptor
There are ‘responders’ and ‘non responders’ to anti-LT therapy
prophylactic therapy - mild-to-moderate asthma as alternatives to
inhaled glucocorticoids
In severe asthma - additive effect with inhaled steroids
no value in COPD
Side effects:
Headache and rashes
Eosinophilia and neuropathy
Churg-Strauss syndrome
Pharmacokinetic and pharmacodynamics:
Highly plasma protein bound
metabolized by CYP2C9
plasma t½: montelukast = 3–6 hours, zafirlukast = 8–12 hours
Zileuton:
5-LOX inhibitor
blocks LTC4/D4/B4 synthesis
clinical efficacy in asthma is similar to montelukast
duration of action is short and it has hepatotoxic
MAST CELL STABILIZERS:
Sodium cromoglycate: (Cromolyn sodium)
Inhibits degranulation of mast cells
May involve a delayed Cl¯ channel in the membrane of these cells
Not effective in acute attack
Pharmacokinetics:
not absorbed orally
administered as an aerosol through metered dose inhaler
1 mg per dose: 2 puffs 4 times a day
Uses:
1.Bronchial asthma:
prophylactic in mild-to-moderate asthma
Beneficial in extrinsic (atopic) and exercise-induced asthma,
especially in younger patients
Therapeutic benefit develops slowly
Less effective than steroids & seldom used now
2.Allergic rhinitis
3.Allergic conjunctivitis
ANTI-IgE ANTIBODY:
Omalizumab:
Humanized monoclonal antibody against IgE
Administered subcutaneously
In severe extrinsic asthma: reduce exacerbations and steroid
requirement
No benefit: nonallergic asthma
very expensive
reserved for resistant asthma with positive skin tests or raised IgE
levels
Bronchial asthma therapeutics and status asthmaticus
Summary:
STATUS ASTHMATICUS
MANAGEMENT
Characteristics:
Acute exacerbation of asthmatic attack which can be life threatening.
Symptoms like:
increasing chest tightness
Wheezing
Dyspnea
Increased ventilation
Hyperinflation
Tachycardia
Poorly relieved by inhalers
Management:
i. Hydrocortisone hemisuccinate 100 mg i.v. stat, followed by 100–
200 mg 4–8 hourly infusion(may take upto 6 hours to act)
ii. Nebulized salbutamol (2.5–5 mg) + ipratropium bromide (0.5 mg)
intermittent inhalations driven by O2
iii. humidified oxygen inhalation
iv. Salbutamol/terbutaline 0.4 mg i.m./s.c. may be added
v. Intubation and mechanical ventilation, if needed.
vi. intensive antibiotic therapy for chest infection
vii. Saline + sod. bicarbonate/lactate infusion for dehydration and
acidosis management
Bronchial asthma therapeutics and status asthmaticus
Bronchial asthma therapeutics and status asthmaticus
Bronchial asthma therapeutics and status asthmaticus

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Bronchial asthma therapeutics and status asthmaticus

  • 1. Bronchial asthma Individual drugs and status asthmaticus
  • 3. SYMPATHOMIMETICS: Mechanism of action: β2 receptor stimulation Increased cAMP formation in bronchial muscle cell Bronchial relaxation
  • 5. Use with caution: Hypertensive Ischemic heart disease patients Patients taking digitalis
  • 6. Salbutamol (Albuterol): highly selective β2 agonist not suitable for round-the-clock prophylaxis Pharmacokinetic & pharmacodynamics: Oral bioavailability is 50% Duration of action: 4-6 hrs(oral), 2-3 hrs(inhalational) Oral therapy reserved for patients unable to use inhalers correctly/adjunct drug for severe asthma
  • 8. Terbutaline: Similar to salbutamol Should not be used on any regular schedule bronchial hyperreactivity: may even worsen diminished responsiveness seen after long-term use Restricted to symptomatic relief of wheezing
  • 9. Bambuterol: Biscarbamate ester prodrug of terbutaline hydrolysed in plasma and lungs by pseudocholinesterase - release the active drug over 24 hours Reversible inhibition of pseudocholinesterase It is indicated in nocturnal and chronic asthma
  • 10. Salmeterol: Long acting selective β2 agonist(more lipophilic) Slow onset of action Inhalation on a twice daily schedule for maintenance therapy and for nocturnal asthma Concurrent inhaled steroid: Reduces risk of life-threatening asthma attacks
  • 11. COPD: • superior to short-acting β2 agonists • equivalent to inhaled anticholinergics • prevent expiratory closure of peripheral airways and • abolish the reversible component of airway obstruction
  • 12. Formoterol: faster onset of action used on a regular morning-evening schedule for round-the-clock bronchodilatation Ephedrine: has α + β1 + β2 actions mild slowly developing bronchodilatation lasting for 3–5 hours not preferred now low efficacy frequent side effects
  • 13. PHOSPHODIESTERASE INHIBITORS: Methyl xanthines: Theophyline and its compounds Mechanism of action: 1. Inhibition of phosphodiesterase (PDE) 2. Blockade of adenosine receptors 3. Interleukin-10 release 4. Effects on gene transcription 5. Effects on apoptosis 6. Histone deacetylase activation
  • 15. Theophylline: Pharmacokinetics: Well absorbed orally Crosses placenta & Secreted in milk V = 0.5 l/kg 50% plasma protein bound metabolized in liver by demethylation and oxidation(CYP1A2) t½ in adults is 7–12 hours(3–5 hours in children) Saturable kinetics Dose reduction needed: age>60yrs, CHF, pneumonia, liver failure
  • 16. Adverse effects: • Narrow margin of safety
  • 17. Interactions: Increase metabolism: Smoking (1.6), phenytoin (1.5), rifampicin (1.5), phenobarbitone (1.2), charcoal broiled meat meal (1.3) Inhibit metabolism: erythromycin, ciprofloxacin, cimetidine, oral contraceptives, allopurinol(2/3) Effect enhanced: furosemide, sympathomimetics, digitalis, oral anticoagulants, hypoglycaemics Effect decreased: phenytoin, lithium should not be mixed: ascorbic acid, chlorpromazine, promethazine, morphine, pethidine, phenytoin, phenobarbitone, insulin, penicillin G, tetracyclines, erythromycin
  • 18. Uses: Bronchial asthma and COPD: Benefits by • bronchodilatation • by decreasing release of inflammatory mediators • promoting eosinophil apoptosis • Improved mucociliary clearance • stimulation of respiratory drive and • Augmentation of diaphragmatic contractility But rarely used now: • narrow margin of safety • limited efficacy • 3rd line or alternative/adjuvant
  • 19. ANTICHOLINERGICS: MECHANISM OF ACTION: Drugs acting on M3 receptors Activation of vagus nerve Bronchodialation(primarily larger airways)
  • 21. Ipratropium bromide: short acting(4-6hr) Inferior to β2 sympathomimetics in asthma but superior in: asthmatic bronchitis, COPD(drug of choice) and psychogenic asthma Regular prophylactic use(2–4 puffs 6 hourly) Additive with β2 agonist(combination used in severe asthma) Tiotropium bromide: longer acting(24hrs) More effective in severe COPD (FEV1<50%)
  • 24. INHALED STEROIDS: high topical and low systemic activity indicated in all cases of persistent asthma Started with 100–200 μg BD titrated upward every 3–5 days(max-400 μg QID) Have no role in: acute attack & status Peak effect in 4-7days COPD: Not much effective High dose in advanced COPD
  • 25. Adverse effects: Hoarseness of voice, dysphonia, sore throat, oropharyngeal candidiasis Minimised by: spacer, gargling, topical nystatin/clotrimazole Systemic effect rare (dose>600 μg/day) Mood changes, osteoporosis, growth retardation children, bruising, petechiae, hyperglycaemia and pituitary-adrenal suppression
  • 26. Beclomethasone dipropionate: pMDI & rotacaps Intranasal spray (50 μg in each nostril BD–TDS): perennial rhinitis Budesonide: high topical: systemic activity ratio(high first pass metabolism) preferred in more severe cases Fluticasone propionate: high potency(double of beclomethasone) Longer duration and negligible oral bioavailability inhalational dose is 100–250 μg BD (max 1000 μg/day).
  • 27. Flunisolide: seasonal and perennial rhinitis Ciclesonide: a prodrug that is cleaved by esterases in the bronchial epithelium to release the active moiety oral bioavailability is <1% extensively bound to plasma proteins in circulation
  • 28. SYSTEMIC STEROID THERAPY: 1. Severe chronic asthma: prednisolone 20-60mg/day dose reduction afeter 1-2 wk attempted 2. Status asthmaticus: high dose of a rapidly acting i.v. glucocorticoid generally act in 6-24 hrs shift to oral for 5-7 days & then inhalational 3. COPD: short course (1–3 week) of oral glucocorticoid for exacerbation
  • 30. Montelukast and Zafirlukast: Competitively antagonize cysLT1 receptor There are ‘responders’ and ‘non responders’ to anti-LT therapy prophylactic therapy - mild-to-moderate asthma as alternatives to inhaled glucocorticoids In severe asthma - additive effect with inhaled steroids no value in COPD Side effects: Headache and rashes Eosinophilia and neuropathy Churg-Strauss syndrome
  • 31. Pharmacokinetic and pharmacodynamics: Highly plasma protein bound metabolized by CYP2C9 plasma t½: montelukast = 3–6 hours, zafirlukast = 8–12 hours
  • 32. Zileuton: 5-LOX inhibitor blocks LTC4/D4/B4 synthesis clinical efficacy in asthma is similar to montelukast duration of action is short and it has hepatotoxic
  • 33. MAST CELL STABILIZERS: Sodium cromoglycate: (Cromolyn sodium) Inhibits degranulation of mast cells May involve a delayed Cl¯ channel in the membrane of these cells Not effective in acute attack Pharmacokinetics: not absorbed orally administered as an aerosol through metered dose inhaler 1 mg per dose: 2 puffs 4 times a day
  • 34. Uses: 1.Bronchial asthma: prophylactic in mild-to-moderate asthma Beneficial in extrinsic (atopic) and exercise-induced asthma, especially in younger patients Therapeutic benefit develops slowly Less effective than steroids & seldom used now 2.Allergic rhinitis 3.Allergic conjunctivitis
  • 35. ANTI-IgE ANTIBODY: Omalizumab: Humanized monoclonal antibody against IgE Administered subcutaneously In severe extrinsic asthma: reduce exacerbations and steroid requirement No benefit: nonallergic asthma very expensive reserved for resistant asthma with positive skin tests or raised IgE levels
  • 39. Characteristics: Acute exacerbation of asthmatic attack which can be life threatening. Symptoms like: increasing chest tightness Wheezing Dyspnea Increased ventilation Hyperinflation Tachycardia Poorly relieved by inhalers
  • 40. Management: i. Hydrocortisone hemisuccinate 100 mg i.v. stat, followed by 100– 200 mg 4–8 hourly infusion(may take upto 6 hours to act) ii. Nebulized salbutamol (2.5–5 mg) + ipratropium bromide (0.5 mg) intermittent inhalations driven by O2 iii. humidified oxygen inhalation iv. Salbutamol/terbutaline 0.4 mg i.m./s.c. may be added v. Intubation and mechanical ventilation, if needed. vi. intensive antibiotic therapy for chest infection vii. Saline + sod. bicarbonate/lactate infusion for dehydration and acidosis management