1. EBL Oral Presentation - Asthma
By: Arun Khurana, Zunnair Alam, Wing Chan, Rachel O’Neill, Elizabeth Warnock. Academic Advisor : Karen Hassell

2. 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

3. Adrenoreceptor agonists
Adrenergic receptor agonists are a class of drugs used to treat asthma and other pulmonary diseases.
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 pressurized-metered dose inhaler.
Asthma causes a large problem for modern society as five million people in the UK are currently receiving treatment for asthma (1.1 million children and 4.3 million adults.)

4. Salbutamol Metabolism: Hepatic Half-Life: 1.6 hours Excretion: Renal
Formula: C13H21NO3  =
It is marketed by GlaxoSmithKline as Ventolin, Aerolin or Ventorlin.
Salbutamol was the first selective Β2-receptor agonist to be marketed — in It was first sold by Allen & Hanburys under the brand name Ventolin.
Salbutamol is specifically indicated by Acute asthma.
The most common side effects are of fine tremor, nervousness , headache, muscle cramps, dry mouth and palpitation.
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 ) .

5. 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
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.
Salameterol in all forms costs £29.26.

6. Terbutaline Sulphate MW:(C12H19NO3)2,H2SO4 =548.6
Form: white to greyish-white crystalline powder.
MW:(C12H19NO3)2,H2SO4
=548.6
M.p.:246° to 248°
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.
Mode of action: Terbutaline works by acting on receptors in the lungs called beta-2 receptors. When salbutamol stimulates these receptors it causes the muscles in the airways to relax. This allows the airways to open. When a patient gets an asthma attack, it is difficult for air to get in and out of the lungs. By opening the airways, salbutamol makes it easier to breathe.
Methods: By mouth, subcutaneous or slow intravenous injection, continuous intravenous infusion, inhalation of powder (Turbohaler®) and inhalation of nebulised solution.
Side Effects: Fine tremor, nervous tension, headache, peripheral vasodilation (widening of the veins) and fast heart rate.

7. 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.
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.

8. Orciprenaline Sulphate
Form: A white crystalline powder
MW: 2(C11H17NO3).H2SO4 =
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 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.
Dose
When treating asthma it is generally it is given by mouth in a dose of 20mg four times daily.
Orciprenaline sulphate also comes in the form of an inhaler.
In cases of severe bronchiospasm, orciprenaline sulphate can be administered directly as an intramuscular injection.
Alupent® is a prescription only sugar-free syrup containing 10mg/5ml orciprenaline sulphate. It has a net price of £6.75 for a 300ml bottle. (BNF, 2008)
Side effects
Orciprenaline suphate, being only partially selective, affects receptors elsewhere in the body and can cause many undesirable side-effects such as arrhythmias, tachycardias and anxiety attacks.
A Public Assessment report published by the MHRA (Medicines and Healthcare products Regulatory Agency) in November 2009 claimed that are too many risks associated with orciprenaline sulphate (Alupent®) and that it should no longer be used in the treatment of asthma. The MHRA is currently working with the manufacturer to carry out a voluntary withdrawal of Alupent® over the next year. The drug will still be available for several months, but it is highly recommended that patients are switched to a more-selective β -2-agonist.

9. 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 white crystalline powder
9.6
Salmeterol
A white to off-white powder
9.9

10. 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 value of a lost school day
Costs of unpaid input
The value of a lost school day – the cost of lost school days should be 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.

11. The social impact of asthma
There were 1,200 deaths from asthma in the UK in On average, three people per day or one person every seven hours dies from asthma.
The effects of asthma on children and adolescent’s social lives are very profound, as they interfere with the children’s ability to play, participate in school activities and 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.
Some adults find their asthma is made worse by dust or fumes at work. This is known as work-aggravated 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.
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.

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