Anti-Asthmatic Medicines

Asthma

Asthma
Asthma is an inflammatory condition in which there is recurrent
reversible airway obstruction in response to irritant stimuli
that are too weak to affect non-asthmatic subjects,
characterized by attacks of wheezing, shortness of breath and
often nocturnal cough.
Severe attacks are life-threatening
Essential features
o Airway inflammation, which causes bronchial hyper-
responsiveness, which in turn results in recurrent reversible
airway obstruction
 Anti-Asthmatic Drugs
Anti-asthmatic drugs are mainly categorized into two major
groups
o Bronchodilators
o Anti-inflammatory agents
Most drugs acting on respiratory tract are adrenoceptor
agonists, or sympathomimetic agents (bronchodilators) and
corticosteroids (used as ‘controllers’ or anti-inflammatory)
The two categories (above) are not mutually exclusive, that is
some drugs classified as bronchodilators also have some anti-
inflammatory effect
 Treating Acute Asthma
Drugs used in the management of asthma include beta2 adrenoreceptor
agonists like salbutamol or terbutaline. Bronchodilators like
theophyline/aminophyline and corticosteroids or antihistamines.
All patients with acute severe asthma should be given high-flow oxygen (if
available) and an inhaled short-acting beta2 agonist via a large-volume
spacer or nebulizer.
For example, give 4–10 puffs of Salbutamol 100 micrograms/metered
inhalation, each puff inhaled separately via a large-volume spacer, and
repeat at 10–20 minute intervals if necessary.
In all cases, corticosteroid should be given
 Treating Acute Asthma
For adults, give Prednisolone 40–50 mg by mouth for at least 5 days, or
intravenous Hydrocortisone 100 mg every 6 hours until conversion to oral
Prednisolone is possible.
For children, give Prednisolone 1–2 mg/kg by mouth (max. 40 mg) for 3–5
days or intravenous hydrocortisone (under 1 year 25 mg, 1–5 years 50 mg,
6–12 years 100 mg)
every 6 hours until conversion to oral prednisolone is possible.
Patient who has not been taking theophylline may benefit from
aminophylline infusion.
Treatment should never be delayed and patients should never be sedated
 Treating Acute Asthma
Administration of Drugs for Asthma
Inhalation includes pressurized metered dose inhaler of salbutamol. This
route delivers the drug directly to the airways, the dose required is smaller
than when given by mouth and side-effects are reduced. Solutions for
nebulisation are available for use in acute
severe asthma.
Oral, drugs given by mouth for the treatment of asthma include beta2
agonists, corticosteroids and theophyline/aminopyhline.
Parenteral, drugs such as beta 2 agonists, corticosteroids, and aminophylline
can be given by injection in acute severe asthma when administration by
nebulisation is inadequate or inappropriate
 Beta2 Adrenoceptor Agonists
[Sympathomimetics]
The selective beta2-adrenoceptor agonists or selective beta2 stimulants, such as
salbutamol or terbutaline, are the safest and most effective short-acting beta2
agonists for asthma.
Salbutamol
Indications: Is used in asthma and other conditions associated with reversible airway
obstruction
Modes of action
o Salbutamol is a beta2 agonist which acts by stimulating the beta 2 receptors in the
smooth muscles of the bronchi causing relaxation
Formulations/preparations available
o Salbutamol is well absorbed when given orally with a peak plasma concentration
being achieved in about 6 hours
o Therefore, it is available as tablets, syrup, and aerosol/ inhalation
 Salbutamol
Dose
o For chronic asthma 4mg tablet 3-4 times a day by mouth. Or aerosol
inhalation 200micrograms (two puffs) 3-4 times a day
o For acute asthma give by inhalation of nebulized solution 2.5 mg q.i.d
(four ) times a day increased to 5mg if necessary
o For children with mild to moderate asthma give salbutamol orally, 1-5years
1mg t.i.d (three) times day, over five years 2mg t.i.d times a day
o For children with acute severe asthma give nebulized salbutamol 0.1mg
every 4 hours
o Prophylaxis in exercise-induced bronchospasm, 200 micrograms (2 puffs),
child 100 micrograms (1 puff), increased to 200 micrograms (2 puffs) if
necessary.
 Salbutamol
Side effects
o Fine tremor (particularly in the hands), nervous tension,
headache, muscle cramps, and palpitation.
o Other side-effects include tachycardia, peripheral vasodilation.
o Disturbances of sleep and behaviour, urticaria, hypotension,
and collapse have also been reported.
o High doses of beta2 agonists are associated with hypokalaemia
 Salbutamol
Cautions
o Non-steroidal anti-inflammatory drugs (NSAIDs), especially, can precipitate
asthma in sensitive individuals.
o Beta2 agonists should be used with caution in hyperthyroidism,
cardiovascular disease, and hypertension.
o If high doses are needed during pregnancy they should be given by
inhalation because a parenteral beta2 agonist can cause cardiac problems.
o Beta2 agonists should be used with caution in diabetes, monitor blood
glucose.
 QUESTION
For a patient who has been prescribed Salbutamol tabs 2mg 4
times a day for 20 days, how many tablets should she take for
that duration if the strength of Salbutamol tablets available is
4mg?
 Theophylline
Indications for Theophylline
Theophylline is indicated for reversible airways obstruction and
acute severe asthma.
Theophylline is a bronchodilator used for asthma and stable
chronic obstructive pulmonary disease.
It may have an additive effect when used in conjunction with
small doses of beta2 agonists the combination may increase
the risk of side-effects, including hypokalaemia
 Theophylline
Pharmacokinetics for Theophyilline
Theophylline is metabolised in the liver, there is considerable variation in plasma
theophylline concentration particularly in smokers, in patients with hepatic
impairment or heart failure, or if certain drugs are taken concurrently.
The plasma-theophylline concentration is increased in heart failure, cirrhosis, viral
infections, in the elderly, and by drugs that inhibit its metabolism.
The plasma-theophylline concentration is decreased in smokers and in chronic
alcoholism and by drugs that induce liver metabolism.
It is readily absorbed and cleaned by hepatic metabolism.
It has a short elimination half life.
Theophylline is given by injection as aminophylline, a mixture of theophylline with
ethylenediamine, which is 20 times more soluble than theophylline alone.
Aminophylline injection is needed rarely for severe attacks of asthma.
 Theophylline
Formulations/Preparation Available
Theophylline is available as injectable or tablets.
If given by injection, must be given by very slow intravenous injection (over at least 20
minutes) because it is too irritant for intramuscular use.
Side Effects
May cause seizures, tremor, nausea, insomnia, or tachycardia at high drug
concentration.
Allergy to ethylenediamine can cause urticaria, erythema, and exfoliative dermatitis
and convulsion may also occur if given by rapid IV injection.
Dose
Acute severe asthma adults orally 100-300mg 3- 4 times daily after food or by slow
intravenous injection over at least 20 minutes (with close monitoring), 250–500 mg
(5 mg/kg), child 5 mg/kg
 Corticosteroids
Hydrocortisone
Reduces the inflammatory component in chronic asthma and is a life-saving in status
asthmaticus (acute severe asthma).
Does not prevent the immediate response to allergen or other challenges.
The mechanism of action involves decreased formation of mediators like cytokines
and
other inflammatory cells.
They are given by inhalation (e.g. beclometasone), oral prednisolone or intravenous
hydrocortisone.
Prednisolone
Indicated for suppression of inflammatory and allergic disorders.
Dose: 10-20mg orally daily up to 60mg daily
Acute asthma, 30-40mg daily for few days gradually reduced when asthma has been
reduced
Precaution, avoid rapid withdraw
 Epinephrine
Adrenaline (epinephrine) which has both alpha- and beta-
adrenoceptors agonist properties
Used in the emergency management of allergic and
anaphylactic reactions and in the management of
croup(Upper airway infection that blocks breathing)
Dose: 1mg IV every 3-5min PRN; may administer up to 0.2mg/kg
if no response.