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.

• 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.

Adrenoreceptor agonists

SalbutamolMetabolism: HepaticHalf-Life: 1.6 hours

Excretion: RenalFormula: C13H21NO3

= 239.311

•It is marketed by GlaxoSmithKline as Ventolin, Aerolin or Ventorlin.•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 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 ) .

Salmeterol (Severent )

•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.

C25H37NO4

Terbutaline Sulphate 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.

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.

Orciprenaline Sulphate

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

Drug Comparisons

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 economic impact of asthma

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.

• Some adults find their asthma is made worse by dust or fumes at work. This is known as work-aggravated asthma.

The social impact 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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