- BRONCHODILATOR AGENT -

Meptin® Swinghaler®
< Procaterol HCl Hydrate>
Dry Powder Inhaler

COMPOSITION
1. Composition
Meptin Swinghaler contains 2 mg of Procaterol HCl Hydrate, and a single puff delivers 10 µg of
the active ingredient. Each container provides about 200 puffs.

2. Product Description
Meptin Swinghaler is a dry powder inhaler consisting of a white plastic container with a blue
pushbutton and a counter filled with a white powder.

INDICATIONS
Remission of various symptoms caused by respiratory obstructive disturbance from the following
diseases: bronchial asthma, chronic bronchitis, and pulmonary emphysema.

PRECAUTIONS REGARDING INDICATIONS

Meptin Swinghaler is indicated only for symptomatic relief of respiratory conditions, and therefore
the drug should be used only at the onset of asthmatic attacks.

CONTRAINDICATIONS
(Meptin Swinghaler is contraindicated in the following patients.)
Patients with a history of hypersensitivity to any ingredient of this drug.

DOSAGE AND ADMINISTRATION

The usual adult dose is 20 µg (2 puffs) of Procaterol HCl Hydrate. For children the amount should be
reduced to 10 µg (1 puff) of Procaterol HCl Hydrate. The dosage may be adjusted according to the
patient's age and severity of symptoms.
< Precautions >
Patients and parents should be cautioned about the possible risk of serious adverse reactions,
including arrhythmia and cardiac arrest, that may result from excessive use of this drug. The
following information or other appropriate instruction should be given to patients receiving this
drug or their families. (See Overdosage section.)
Take this medication exactly as directed: 2 puffs per dose for adults and 1 puff per dose for
children, no more than 4 times a day (total of 8 puffs per day for adults and 4 puffs per day for
children).

PHARMACOLOGY
1. Bronchodilative Action
The bronchodilative action of Procaterol HCl Hydrate was comparable to or more potent than
that of isoproterenol and more potent than that of salbutamol and orciprenaline, as determined
by inhibition of increased pulmonary resistance in dogs, cats, and guinea pigs. The onset of the
bronchodilative action was observed at 1 to 5 minutes after inhalation in conscious guinea pigs
and anesthetized dogs, indicating much faster onset of action than the tablet formulation.
Inhaled Procaterol HCl Hydrate dilates not only the central airway but also peripheral airways in
pediatric asthma patients.

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 2. Duration of Bronchodilatory Action
Procaterol HCl Hydrate had a longer duration of bronchodilative action than isoproterenol,
trimetoquinol, orciprenaline, and salbutamol in dogs, cats, and guinea pigs. The potency with
which Procaterol HCl Hydrate at 10 µg by inhalation inhibited the increase in airway resistance
due to histamine was equal to that of salbutamol at 200 µg by inhalation in anesthetized dogs.
However, Procaterol HCl Hydrate is longer acting than salbutamol.

3. Selectivity for ß2-Adrenergic Receptors (Organ Selectivity)

The selectivity of Procaterol HCl Hydrate for ß-adrenergic receptors in the respiratory system
was greater than that for such receptors in the cardiovascular system, as compared to
isoproterenol, trimetoquinol, orciprenaline, and salbutamol in dogs, cats, and guinea pigs.

4. Anti-allergic Action
Procaterol HCl Hydrate exhibited a definite anti-allergic action by inhibiting antibody-induced
increase in airway resistance, the PCA reaction, and histamine release from sensitized lung tissues
in guinea pigs and rats, as well as allergen- induced skin reactions, and increases in asthmatic
responses to antibody inhalation in bronchial asthma patients, as compared to isoproterenol,
trimetoquinol, orciprenaline, and salbutamol.

5. Effects on Respiratory Track System

Procaterol HCl Hydrate accelerated ciliary activity in airways of pigeons.

6. Effect on Exercise-Induced Asthmatic Attacks

Procaterol HCl Hydrate suppressed treadmill or ergometer exercise- or methacholine-induced
asthmatic attacks in patients with bronchial asthma.

7. Other
The result of a pharmacodynamic study conducted in patients with bronchial asthma, and using a
pulmonary function parameter (FEV1.0) as an index, demonstrated that Meptin Swinghaler and
Meptin Air have equivalent bronchodilatory action.

PHARMACOKINETICS
Since no pharmacokinetic studies have been conducted for Meptin Swinghaler, the results
summarized below are from pharmacokinetic studies of Meptin Air.

1. Plasma Concentrations
When Meptin Air was administered by inhalation to 6 healthy male subjects as single doses of 40
µg per subject, a peak plasma concentration of 128 pg/mL was attained at 15 minutes post-
dosing, followed by a gradual decline.

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2. Urinary Excretion
When Meptin Air was administered by inhalation as a single dose of 40 µg in 4 puffs per subject,
14.36% of the dose was excreted in the urine within 24 hours post-dosing.

PRECAUTIONS
1. Careful Administration (Meptin Swinghaler should be administered with care in the following
patients.)
(1) Patients with hyperthyroidism (The disease may be exacerbated.)
(2) Patients with hypertension (Blood pressure may further increase.)
(3) Patients with heart disease (Palpitation, arrhythmia, exacerbation of heart disease, and
other symptoms may occur.)
(4) Patients with diabetes mellitus (The disease may be exacerbated.)
(5) Patients during pregnancy or suspected pregnancy (See Use during Pregnancy, Delivery or
Lactation section.)

2. Important Precautions
(1) Meptin Swinghaler is recommended only when patients receiving this drug or their families
are instructed properly on the method of use to prevent potential risk due to excessive use
of the drug.
(2) Continuous use of excessive amounts of this drug may cause cardiac arrhythmia and cardiac
arrest. Special care should therefore be taken not to exceed the recommended dose of this
drug at the time of asthma episodes.
(3) When the drug is administered to patients, they should be properly instructed on the
method of use of this drug and adequately observed for any effects. If the desired
therapeutic effect has not been achieved at the recommended dose, the drug should be
discontinued and replaced with other medication to prevent excessive use, since airway
inflammation may possibly be exacerbated.
(4) Patients and their families should be instructed to consult a physician for emergency
treatment and reassessment of therapy when the recommended dosing schedule is not
effective in relieving severe episodes of asthma.

3. Use in the Elderly

Dosage adjustment or other appropriate measures should be considered when prescribing
Meptin Swinghaler to elderly patients because these patients may be physiologically more
sensitive to the drug than younger patients.

4. Use during Pregnancy, Delivery, or Lactation

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 (1) This drug should be administered to pregnant or possibly pregnant women only if
the expected therapeutic benefit is thought to outweigh any possible risk. (The
safety of this drug during pregnancy has not been established.)
(2) Nursing should be interrupted before starting treatment with the drug. (Rat studies
showed that Procaterol HCl Hydrate is excreted in breast milk.)

5. Pediatric Use
(1) Children should be properly instructed on the method of use and adequately observed for
any effects.
(2) The safety of this drug in premature babies, neonates, and infants has not been established.

6. Effects on Laboratory Tests

This drug tends to inhibit skin reactions in allergen tests. The drug should be withdrawn 12
hours prior to such tests.

7. Overdosage
Administration of this drug to patients in excess of the recommended dose can cause ventricular
arrhythmias (ventricular tachycardia, ventricular fibrillation, and other symptoms), cardiac
arrest, and other severe adverse reactions. Patients should be properly instructed on the dose
and method of administration of the drug. (See Precautions in Dosage and Administration
section and Important Precautions section.)

8. Precautions Concerning Use.

It is especially important that patients understand how to use Meptin Swinghaler appropriately.
Patients should be given the following information.

Patient's Instructions for Use

(1) Open the transparent cover by pushing down both sides of the inhaler.
(2) Hold the inhaler at the button (keep the dose counter facing upwards) and shake
the inhaler up and down vertically for 3~4 times.
(3) Push the button of the inhaler towards the mouthpiece once.
(4) Breathe out and hold your breath.
(5) Place the mouthpiece gently between your teeth and close your lips. Inhale fast and deeply
through your mouth as much as you can, then hold your breath for a few seconds as the
medication is being inhaled. Exhale slowly.
(6) Push the button once more to make the inhaler return to the unloaded condition. (Press
once more to end the session, and the dose will not be wasted.)
(7) Close the cover after use.
(8) If more than one puff has been prescribed, repeat steps 2~6.
(9) Rinse your mouth with water.

9. Other Precautions
(1) Tissue damage in cardiac muscle was noted in oral toxicity study of Procaterol HCl Hydrate
using rats and dogs, similar to other ß2-adrenergic agonists.
(2) Administration of Procaterol HCl Hydrate with diet for 104 weeks was reported to cause
mesovarian leiomyoma in SD rats. However, this tumor is rat- species specific and tends to
develop during long-term use of ß2-adrenergic agonists.

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ADVERSE REACTIONS
There has been no survey conducted to clarify the incidence of adverse reactions for Meptin
Swinghaler. The following adverse reactions have been reported for inhalation formulation including
Meptin Air. In clinical trials involving 6,655 subjects, a total of 101 patients (1.52%) showed adverse
reactions including abnormal laboratory values. The following summary of data includes adverse
reactions reported after marketing without data on the incidence .

(1) Clinically significant adverse reactions (*incidence unknown)

1) Shock, anaphylactoid reactions: Shock or anaphylactoid reactions may occur. Patients should
therefore be closely monitored. If abnormal findings are observed, the drug should be
discontinued and appropriate measures taken.
2) Significant decreases in serum potassium levels have been reported in patients receiving
Procaterol HCl Hydrate. If xanthine derivatives, corticosteroid or diuretics are coadministered
with this drug for patients with severe asthma, extreme care is necessary to minimize the
possibility of aggravating the decrease in serum potassium levels induced by ß2-adrenergic
agonists. Serum potassium levels should be closely monitored for hypoxic patients, in view of
the possible aggravation of cardiac arrhythmias secondary to a decrease in serum potassium
level.

(2) Other adverse reactions

Note 1) If symptoms of hypersensitivity occur, the drug should be discontinued.

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*The incidence rates of adverse reactions reported voluntarily after marketing or those reported in
foreign countries are not known.

DRUG INTERACTIONS
Precautions for coadministration (Meptin Swinghaler should be administered with care when
coadministered with the following drugs.)

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PHYSICOCHEMISTRY
Nonproprietary name:
Procaterol HCl Hydrate

Chemical name:
8-Hydroxy-5-{(1RS,2SR)-1-hydroxy-2-[(1-methylethyl)
amino]butyl}-quinolin-2(1H)-one monohydrochloride hemihydrate

Structural formula:

Molecular
Formula : C16H22N2O3 HCl 1/2H2O
Molecular weight : 335.83

PRECAUTIONS FOR HANDLING

1. Explanation to Patients
 When prescribing this drug, the patient should be provided with the dedicated storage
container and the instructions for use and be given instruction on how to use the product. In
particular, patients who will be receiving this drug for the first time should be given a
full explanation of the inhalation procedure and instructed how to correctly inhale the drug.
 This drug is supplied in an aluminum pillow package to protect it from moisture, and the
patient should be instructed not to open the aluminum pillow package until immediately
before use.
2. Storage and Care
 Patients should be instructed to keep this drug in the dedicated storage container and to cap
the container immediately after use.
 Patients should be instructed to wipe the inhaler mouthpiece (inhalation orifice) with a dry
tissue or something similar when it becomes dirty and to not wash the mouthpiece with
water or wipe it with a wet cloth.
 Patients should be instructed not to subject this drug to strong impact and not to
disassemble the housing.
 Be careful to keep the drug out of the reach of children.

STORAGE
Store below 30°C

PACKAGING
Meptin® Swinghaler® in plastic container device

REG. NO.: DKL1418707967A1

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