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EBL Oral Presentation - Asthma
By: Arun Khurana, Zunnair Alam, Wing Chan, Rachel O’Neill, Elizabeth Warnock.
Academic Advisor : Karen Hassell
Topics to be covered in this
presentation
• Adrenoreceptor Agonists
• Drugs used in treatment of asthma
– Salbutamol
– Salmeterol
– Terbutaline Sulphate
– Ephedrine Hydrochloride
– Orciprenaline Sulphate
• States of drugs and pKa values
• Socio-economic impacts of asthma
Adrenoreceptor agonists
• 5 million people in the UK are
currently receiving treatment for
asthma
 1.1 million children
 4.3 million adults
• Adrenergic receptor agonists are a
class of drugs used to treat asthma
and other pulmonary diseases.
Adrenoreceptor agonists
• These drugs act on the
adrenogenic receptors
causing smooth muscles to
relax, which results in
dilation of bronchial
passages.
• Beta-2 adrenergic agonists
are most often
administered by inhaling
from a pressurizedmetered dose inhaler.
Salbutamol
Metabolism: Hepatic
Half-Life: 1.6 hours
Excretion: Renal
Formula: C13H21NO3 = 239.311
•Salbutamol was the first selective Β2-receptor agonist to be marketed — in 1968. It was
first sold by Allen & Hanburys under the brand name Ventolin.
•Salbutamol is specifically indicated by Acute asthma.
•The selectivity of Salbutamol depends on the dose given. Inhalation of drugs aids selectivity
as it delivers small but effective doses to the airways thus helping in minimizing systemic
exposure. After inhalation, the onset of drug action takes an intermediate amount of time (
bronchodilation is produced for about 6 hours ) .
Salbutamol
• It is marketed by
GlaxoSmithKline as Ventolin,
Aerolin or Ventorlin.
•
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The most common side effects :
fine tremor
nervousness
headache
muscle cramps
dry mouth
palpitation.
Salmeterol (Severent )
C25H37NO4
•Salmeterol helps to treat and manage Bronchospams, Nocturnal asthma, Chronic
Asthma and Chronic obstructing pulmonary disease (COPD). It is known as a
“LABA”.
•Salmeterol works by attaching itself to particular beta 2 receptors. Specific
secondary binding sites on the beta 2 receptors are targeted by Salmeterol
molecules. As a result of this bronchial muscle is relaxed, bronchodilatation is
promoted
Salmeterol (Severent )
• The dosage of Salmeterol depends on which problem it is being used to
treat. In the form of Inhalers it can treat:
• Asthma- 50 micrograms (1 blister/2 puffs) twice daily. COPD- 50 micrograms
(1 blister/2 Puffs) twice daily.
• Salmeterol in all forms costs £29.26.
Terbutaline Sulphate
Form: white to greyish-white crystalline
powder.
MW:(C12H19NO3)2,H2SO4
=548.6
M.p.:246° to 248°
• Terbutaline sulfate is a synthetic sympathomimetic amine
• Uses-Terbutaline sulfate is used as a relatively short-acting bronchodilator
in the symptomatic treatment of bronchial asthma and of reversible
bronchospasm that may occur in association with chronic obstructive
pulmonary disease (COPD), including chronic bronchitis and emphysema.
Subcutaneous terbutaline is about as effective as an equal subcutaneous
dose of epinephrine in improving pulmonary function.
Terbutaline Sulphate
• Dose: 500micrograms (1
inhalation), up to 4 times daily.The
inhaled form of terbutaline starts
working within 15 minutes and
can last up to 6 hours.
• Methods: By mouth,
subcutaneous or slow intravenous
injection, continuous intravenous
infusion, inhalation of powder
(Turbohaler®) and inhalation of
nebulised solution.
Ephedrine Hydrochloride
•Melting Point: 216oC-222oC
•Molecular formula: C10H15NO,HCl =201.7
•It exists as colourless crystals or a white crystalline
powder.
Ephedrine hydrochloride helps to relieve the symptoms caused by asthma.
It helps to relax the smooth muscles present in the lungs, this is turn allows the bronchial
discharge to flow out from the bronchial tubes to generate more cough.
Dosage:
This medication should be taken 3 times a day, by mouth. It may take a few hours before
the full benefit of the drug takes effect.
Ephedrine Hydrochloride
Athletes all over the world use ephedrine
chloride not only to boost energy levels, but
to help lower their weight by the reduction
of body fat. Ephedrine noticeably stimulates
the central nervous system, increasing the
heart rate and has an overall heat producing
effect on most tissues in the body.
Orciprenaline Sulphate
Form: A white crystalline powder
MW: 2(C11H17NO3).H2SO4 = 520.29
Melting point: about 205°C
When treating asthma it is given by mouth in a dose of 20mg four times daily.
It also comes in the form of an inhaler or in severe cases of bronchiospasm it can
be administered directly as an intramuscular injection.
Orciprenaline suphate, being only partially selective, affects receptors elsewhere
in the body and can cause undesirable side-effects such as arrhythmias,
tachycardias and anxiety attacks.
A report published by the MHRA in November 2009 decided that orciprenaline
sulphate (Alupent®) should no longer be used in the treatment of asthma.
Orciprenaline Sulphate
• Orciprenaline sulphate is a
sympathomimetic agent with partially
selective β -adrenoceptor stimulant
activity. It is used as a bronchodilator
in the treatment of reversible airways
obstruction (asthma) and in some
patients with chronic obstructive
pulmonary disease. On inhalation, the
onset of action is usually within 30
minutes and can last from 1 to 5
hours.
Drug Comparisons
Drug
State
pKa
Terbutaline Sulphate
A white to greyish-white
crystalline powder
8.7, 10.0, 11.0
Orciprenaline Sulphate
A white crystalline
powder
9.0, 10.1, 11.4
Salbutamol
A white powder
9.3, 10.3
Ephedrine Hydrochloride Colourless crystals or a
9.6
white crystalline powder
Salmeterol
A white to off-white
powder
9.9
The economic impact of asthma
Direct costs
• Hospital costs
• Costs of home care
• Alternative medicine
• Nursing home costs
• Ambulance callouts
Indirect costs
• Time spent by others caring for sick
relatives
• Physical resources – e.g. the number of
missing days lost or the number of
premature deaths
• Short-term absence due to sickness
• Long-term absence such as early
retirement
The economic impact of asthma
• The value of a lost school day
 measured as a reduction in the earning
resulting from how the disease affects the
returns on education.
 The time lost from work for parents who have
to care for their sick children should also be
counted.
• Costs of unpaid input
 When a person is suffering from an illness,
the household atmosphere maybe affected as
the sick member of the household is unable
to contribute to the financial stability, leading
to placement of added pressure on the
remaining family members.
The social impact of asthma
•
There were 1,200 deaths from asthma in the UK in
2006.
 On average, 3 people per day or
 1 person every 7 hours.
•
The effects of asthma on children and adolescent’s
social lives are very profound, as they interfere with
children’s ability to
 play, participate in school activities
 form friendships and relationships.
Studies show that one in three 7 year old children who suffered from asthmatic
symptoms had missed more than 50 days' schooling as a direct result of asthma.
School absence can lead to psychological problems as a result of the child feeling
different, inferior or being overprotected. These problems can in turn exacerbate the
symptoms of asthma.
The social impact of asthma
• Some adults find their asthma is made
worse by dust or fumes at work. This is
known as work-aggravated asthma.
For this type of asthma, employees
should talk to their employer as soon as
possible about relocating so that they
are no longer exposed to the sensitizer
that's causing their asthma.
Thank you for listening to our presentation. We
hope you found it informative. Please feel free to
ask any questions.