Transcript Orciprenaline Sulphate

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
• 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.
Salbutamol
Metabolism: Hepatic
Half-Life: 1.6 hours
Excretion: Renal
Formula: 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 )
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.
Terbutaline Sulphate
Form: white to greyish-white crystalline
powder.
MW:(C12H19NO3)2,H2SO4
=548.6
M.p.:246° to 248°
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•
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•
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 beta2 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.
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.
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.
Drug Comparisons
Drug
State
pKa
Terbutaline Sulphate
A white to greyish-white 8.7, 10.0, 11.0
crystalline powder
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
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 social impact of asthma
• There were 1,200 deaths from asthma in the UK in 2006. 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.
Thank you for listening to our presentation. We
hope you found it informative. Please feel free to
ask any questions.