1. Systemic Procaterol (Meptin) as a CONTROLLER for Asthma
PART 1
Good day to you doctor.
Today I would like to discuss with you Procaterol (Meptin) as a controller medication for your patients with Asthma.
I will be focusing on the Systemic Forms of Meptin, particularly the Tablet Format: 25mcg and 50mcg tablets.

2. INFLAMMATION Environmental Risk Factors
Definition of Asthma
Environmental Risk Factors
Airway Hyperresponsiveness Airway Limitation Symptoms
Triggers
INFLAMMATION
As you know well, doctors, asthma is defined as a chronic inflammatory disorder of the airways, characterized by inflammation, airway hyperresponsiveness, and reversible airway obstruction.
In susceptible individuals, the inflammation leads to an increase in airway responsiveness to various stimuli, and causes recurrent symptoms associated with airway obstruction that is often reversible either spontaneously or with treatment.
Global Strategy for Asthma Management and Prevention, 1995

3. Common Asthma Triggers
Allergens 1
Respiratory Tract Infections
Irritants (Dust, Strong Odor, etc.)
Temperature Change
Emotion / Stress
Exercise / Physical Activity 2 3 4 5 6
The most common stimuli or asthma triggers are listed here in this slide.
As an exposure of asthmatic subjects to the stimuli induces asthmatic episodes, identification and control or avoidance of these stimuli are far most important in the management of asthma, which can reduce manifestation of symptoms and may decrease airway inflammation and hyperresponsiveness in a long-term.

4. Philippine Consensus Report on the Diagnosis & Management of Asthma
Step 2: Mild, Persistent
Controller:
Daily medication:
- Inhaled Corticosteroids up to 800 mcg/day
or Cromolyn Sodium
Alternative Controller:
-Long-Acting b2 Agonist or Sustained Release Theophylline
None
Step 1: Mild, Intermittent
Reliever:
- Inhaled Short-Acting b2 Agonist as needed, not > 3x/week
Alternative Reliever:
- Short-Acting Oral bronchodilator (b2 Agonist or Theophyllime)
- Inhaled Short-Acting b2 Agonist as needed, not > 3-4x/day
Step 4: Severe, Persistent
- Add Ipratropium Bromide
- Inhaled Corticosteroids 800-2,000 mcg/day
- Long-Acting Bronchodilator
(Inhaled or Oral b2 Agonist, Sustained Release Theophylline)
- Oral Long-Acting b2 Agonist + Theophylline
- Oral Steroid > 7.5 mg/day, daily or alternate day
Step 3: Moderate, Persistent
- Add Long-Acting Bronchodilator
- Low Dose Oral Steroid < 7.5 mg/day, daily or alternate day
As discussed earlier, the underlying condition of asthma is inflammation. It is, therefore, important to address the inflammation in the management of asthma.
In order to address these problems, the Philippine Consensus Report in the Diagnosis & Management of Asthma recommends the use of controllers, which are mainly steroids and anti-inflammatory agents as the first choice.
However, once you are faced with any of the situations wherein you do not want to increase dosage of the controller given to your patients, the condition of your patients is not properly controlled by the controller given, or you do not want to use steroids even in a form of inhaler, like for your pediatric cases, the consensus recommends to use any of the oral or long-acting bronchodilators as an additional controller.

5. Treatment Modality for Asthma
Steroids
Anti-inflammatory drugs
Oral/Long acting bronchodilators
Anti-inflammatory effects
Reduce airway hyperreactivity
Sustained bronchodilation
Inflammation
Airway Hyperreactivity
Controller
Bronchoconstriction
Asthmatic attack
Reliever
Knowing that the underlying conditions of asthma are inflammation and airway hyperresponsiveness, I hope you will agree with us that bronchodilators having the following features are more recommended as an additional controller to steroids or anti-inflammatory drugs;
1. Anti-inflammatory effect,
2. Reduces airway hyperresponsiveness, and
3. Sustained bronchodilating action.
Inhaled Bronchodilators
Rapid onset of action
Potent bronchodilation

6. Site of Action of Anti-asthmatic Drugs
GTP
cGMP
GMP
Anti-cholinergic Agents
Inhibition
Guanylate Cyclase
Bronchoconstriction
Phosphodiesterase
Adenylate Cyclase
Bronchodilation
Xanthine Derivatives
b2 Stimulants
Activation
Inhibition
ATP
cAMP
AMP
As you know well, we have three bronchodilators available in the market now, which are beta 2 stimulants or agonists, xanthine derivatives, and anti-cholinergic agents.
Our product, Procaterol, Meptin belongs to the beta 2 stimulant category.
Release
Inhibition
Bronchoconstriction
Mucous edema
Mast cell
Histamine, LTs
Inhibition
Inhibition
DSCG, DCC
Anti-histaminic agents
Illustration Text Book of Clinical Medicine - Respiratory Medicine

7. Features of Meptin Syrup & Tablets
as A Controller
Long Duration of Bronchodilating Action
Anti-inflammatory Effect
Our product, Procaterol, Meptin has the following features, which meet the criteria for a bronchodilator as a controller in the management of asthmatic patients, as discussed in the previous slide;
1. Long duration of bronchodilating action,
2. Anti-inflammatory effect, and
3. Reduces airway hyperreactivity.
For the course of my next visits, I will be tackling individually these three functions of Procaterol.
Reduces Airway Hyperreactivity

8. Bronchodilating Action of Procaterol
Method of Administration: Intraduodenal
(%)
Procaterol (n=8) 0.3μg/kg
Salbutamol (n=8) 3μg/kg
Orciprenaline (n=4) .10μg/kg
Terbutaline (n=4) 0.3μg/kg
Trimetoquinol (n=4). 3μg/kg 60
Inhibition of Airway Resistance
mean±S.E. 30
As you can see in this slide, Procaterol has a longer duration of bronchodilating action of more than 8 hours, which is much longer than those of salbutamol and terbutaline. 1 2 3 4 5 6 8
(hr.)
Postｰadministration
Kawamura et al: Unpublished Data (Internal Use)

9. Duration of Action of Meptin Tablets60 70 80 90
100
110
120
130
140
150
160
(%)
START
Meptin 0.1mg
Metaproterenol 20mg
Salbutamol 4mg
Trimetoquinol 6mg
Control
FEV1.0
Meptin tablet
50 µg
This slide shows another evidence demonstrating the long duration of action of our product, Procaterol, Meptin lasting up to more than 12 hours, thus proving its beneficial effect especially when given at bedtime to patients suffering from nocturnal asthma. PM AM
Yakura, T. et. al.: Gendai Iryo. 10:1499 (1978)

10. Results of Clinical Study with Meptin
Improvement of Sleep
(%)
100
n = 94 (Acute Pediatric Bronchitis)
Meptin 25mcg tablets 50
Clinical results have shown that our product, Procaterol, Meptin improved sleep in almost 50% of the patients in this study on the first day of administration, and in almost 100% of them on the 3rd day.
This long duration of action of our product, Procaterol, Meptin not only provides restful sleep at night to asthmatic patients, but also benefits to their parents in case of pediatric patients and other relatives tasked with taking care of them as they don’t have to wake up in the wee hours of the morning just to attend to the need of the patient undergoing an attack. 53 1 53 2 53 3 53 4 52 5 50 6 48 7 44
(Days)
(n)
Matsuyama et. al.: Clinical Pediatrics, 43 (2), 373 (1990)

11. Dosage and Administration:
Meptin® Syrup
The usual adult dosage is 10 ml of Meptin® Syrup (50 µg of procaterol hydrochloride) once before bed or twice (in the morning and before bed) a day by oral route.
The dosage in children 6 years of age or older is 5 ml of Meptin® Syrup (25 µg of procaterol hydrochloride) once before bed or twice (in the morning and before bed) a day by the oral route.
The dosage in children less than 6 years of age is 0.25 ml of Meptin® Syrup (1.25 µg of procaterol hydrochloride) per Kg body weight once before bed or twice (in the morning and before bed) a day by the oral route.
The dosage may be adjusted according to the patient’s age and severity of symptoms.
Meptin® Syrup
The usual adult dosage is 10 ml of Meptin® Syrup (50 µg of procaterol hydrochloride) once before bed or twice (in the morning and before bed) a day by oral route.
The dosage in children 6 years of age or older is 5 ml of Meptin® Syrup (25 µg of procaterol hydrochloride) once before bed or twice (in the morning and before bed) a day by the oral route.
The dosage in children less than 6 years of age is 0.25 ml of Meptin® Syrup (1.25 µg of procaterol hydrochloride) per Kg body weight once before bed or twice (in the morning and before bed) a day by the oral route.
The dosage may be adjusted according to the patient’s age and severity of symptoms.

12. Dosage and Administration:
Meptin® Tablet 50 µg
The usual adult dosage of Meptin® Tablet is one tablet (50 µg), orally once before bed or twice (in the morning and before bed) per day.
The dosage should be adjusted according to the patient’s age and severity of symptoms.
Meptin® Tablet 25 µg
The usual dose of Meptin® 25 µg tablet is two tablets (50 µg) once before bed or twice (in the morning and before bed) per day by the oral route.
The dosage in children 6 years of age or older is one tablet (25 µg), once before bed or twice (in the morning and before bed) per day by the oral route. The dosage should be adjusted according to the patient’s age and severity of symptoms.
This slide is just a reminder of the proper dosage and administration of Meptin Tablets.
Meptin® Tablet 50 µg
The usual adult dosage of Meptin® Tablet is one tablet (50 µg), orally once before bed or twice (in the morning and before bed) per day.
The dosage should be adjusted according to the patient’s age and severity of symptoms.
Meptin® Tablet 25 µg
The usual dose of Meptin® 25 µg tablet is two tablets (50 µg) once before bed or twice (in the morning and before bed) per day by the oral route.
The dosage in children 6 years of age or older is one tablet (25 µg), once before bed or twice (in the morning and before bed) per day by the oral route. The dosage should be adjusted according to the patient’s age and severity of symptoms.

13. MEPTIN: ORAL & INHALED DURATION OF ACTION ORAL: 10 to 12 hours
ONSET OF
ACTION
ORAL:
30 to 60 minutes
INHALED:
3 to 5 minutes
Meptin is available in both oral and inhaled form. The difference is in the duration and onset of action for your patients.

14. Thank you for your time in listening to my presentation, doctor.
As you can see, here is the line up of our respiratory products.
Meptin Syrup, Tablets, and Swinghaler, together with Budesonide Obucort, are all approved for the relief of asthma symptoms.
Meptin has been, and ever will be the reliable choice through the years for Asthma management and control.