MEPTIN Procaterol Hydrochloride 5mcg / mL Syrup 60mL
RXDRUG-DRP-5277
Discreet Packaging
FDA-registered Products
FDA-licensed Pharmacies
Indications/Uses
Relief of dyspnea and other symptoms caused by respiratory obstructive disturbance in the following diseases: Bronchial asthma, chronic bronchitis and pulmonary emphysema. Treatment of acute bronchitis.
Dosage/Direction for Use
Tablet/Syrup: Adults: Usual Dose: 50 mcg or 10 mL once before bedtime or twice daily (in the morning and before bedtime). The dosage would be adjusted according to the patient's age and severity of symptoms.
Adults and Children ≥6 years: Usual Dose: 25 mcg or 5 mL once before bedtime or twice daily (in the morning and before bedtime). The dosage would be adjusted according to the patient's age and severity of symptoms. <6 years: (1.25 mcg/kg body weight) 0.25 mL/kg body weight 2-3 times daily (in the morning, early afternoon and before bedtime).
Adults and Children ≥6 years: Usual Dose: 25 mcg or 5 mL once before bedtime or twice daily (in the morning and before bedtime). The dosage would be adjusted according to the patient's age and severity of symptoms. <6 years: (1.25 mcg/kg body weight) 0.25 mL/kg body weight 2-3 times daily (in the morning, early afternoon and before bedtime).
Overdosage
Overdosage with Meptin has been associated with tachycardia, tachycardiac arrhythmia, hypotension, nervousness, tremor, hypokalemia, hyperglycemia and lactic acidosis. In the event of any overdosage-related abnormalities are observed, Meptin should be discontinued and, if required, gastric lavage should be performed to remove any unabsorbed drug. Emergency treatment and general maintenance therapy should also be provided, if needed. In the event of serious tachycardiac arrhythmia has developed, β-blockers eg, propanolol may be effective, but administration of these drugs to asthma patients should be performed with care because β-blockers may increase airway resistance in these patients.
Administration
May be taken with or without food.
Contraindications
History of hypersensitivity to any of the ingredients of Meptin
Special Precautions
Patients with hyperthyroidism (the disease may be exacerbated), hypertension (blood pressure may further increase), heat disease (palpitation, arrhythmia, exacerbation of heart disease and other symptoms may occur), diabetes mellitus (the disease may be exacerbated). Patients who are pregnant or suspected of being pregnant which requires careful administration; an additional important precaution with regards to its use for the long-term management of bronchial asthma. It should be initiated when symptoms are not adequately controlled by inhaled corticosteroids or other asthma medications, the development of acute asthma episodes during its use.
Important: If the desired therapeutic effect of Meptin cannot be achieved at the recommended dose, it should be discontinued.
Continuous administration of excessive amounts of the drug may cause cardiac arrhythmia and cardiac arrest. Special care should therefore be taken not to exceed the recommended dosage of Meptin (at the time of asthma episodes).
The mainstay of long-term management of bronchial asthma is inflammatory agents eg, inhaled corticosteroids. Meptin should therefore be used only as additional therapy for patients whose symptoms are not adequately controlled by inhaled corticosteroid or other asthma medications, or whose disease severity clearly warrants initiation of treatment with Meptin.
As Meptin is not a substitute for inhaled corticosteroids and other anti-inflammatory agents, the patients or their guardian or other legally authorized person should be instructed not to reduce the dosage of inhaled corticosteroids or to stop use of inhaled corticosteroids and switch to monotherapy with Meptin unless specifically instructed to do so by their physician, even if they have felt symptomatic improvement with the use of Meptin.
During the long-term management of bronchial asthma with Meptin, the patient may develop acute asthma episodes. The patient or their guardian or other legally authorized person should therefore be instructed to use adequate drugs other than Meptin eg, short-acting inhaled β2-stimulants, if acute asthma episodes occur during treatment with Meptin. In addition, if the use of such drugs becomes more frequent or sufficient therapeutic effect is not observed with the initial dose of the drugs, the patient's asthma my not be adequately controlled. The patient or the guardian or other legally authorized person should be instructed to consult a physician as soon as possible and receive adequate medication in such cases. In addition, as such conditions may be life-threatening, anti-inflammatory therapy should be consolidated by adequate measures eg, increasing the dosage of inhaled corticosteroids.
Effects on Laboratory Tests: Meptin tends to inhibit skin reactions in allergen tests. Meptin should be withdrawn 12 hrs prior to such tests.
Other Precautions: Similar to other β2-adrenergic agonists, tissue damage in cardiac muscle was noted in oral toxicity studies at Meptin 30 and 10 mg/kg/day, or higher in the subacute and chronic toxicity studies, respectively, using rats. The damage was also observed in dog studies. However, the damage has been reported with other β2-adrenergic agonists in both rats and dogs.
Dietary administration of procaterol hydrochloride for 104 weeks was reported to cause mesovarian leiomyoma in SD rats. The tumor, however, is rat-specific and tends to develop during long-term administration of β2-adrenergic agonists.
Use in pregnancy & lactation: Meptin 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 Meptin during pregnancy has not been established.)
Nursing should be interrupted before starting treatment with Meptin. (Rat studies showed that procaterol hydrochloride is excreted in breast milk.)
Use in children: The safety of Meptin in low birth weight infants and neonates has not been established.
Use in the elderly: Dosage adjustment or other appropriate measures should be considered when prescribing Meptin to elderly patients, because these patients may be physiologically more sensitive to the drug than younger patients.
Important: If the desired therapeutic effect of Meptin cannot be achieved at the recommended dose, it should be discontinued.
Continuous administration of excessive amounts of the drug may cause cardiac arrhythmia and cardiac arrest. Special care should therefore be taken not to exceed the recommended dosage of Meptin (at the time of asthma episodes).
The mainstay of long-term management of bronchial asthma is inflammatory agents eg, inhaled corticosteroids. Meptin should therefore be used only as additional therapy for patients whose symptoms are not adequately controlled by inhaled corticosteroid or other asthma medications, or whose disease severity clearly warrants initiation of treatment with Meptin.
As Meptin is not a substitute for inhaled corticosteroids and other anti-inflammatory agents, the patients or their guardian or other legally authorized person should be instructed not to reduce the dosage of inhaled corticosteroids or to stop use of inhaled corticosteroids and switch to monotherapy with Meptin unless specifically instructed to do so by their physician, even if they have felt symptomatic improvement with the use of Meptin.
During the long-term management of bronchial asthma with Meptin, the patient may develop acute asthma episodes. The patient or their guardian or other legally authorized person should therefore be instructed to use adequate drugs other than Meptin eg, short-acting inhaled β2-stimulants, if acute asthma episodes occur during treatment with Meptin. In addition, if the use of such drugs becomes more frequent or sufficient therapeutic effect is not observed with the initial dose of the drugs, the patient's asthma my not be adequately controlled. The patient or the guardian or other legally authorized person should be instructed to consult a physician as soon as possible and receive adequate medication in such cases. In addition, as such conditions may be life-threatening, anti-inflammatory therapy should be consolidated by adequate measures eg, increasing the dosage of inhaled corticosteroids.
Effects on Laboratory Tests: Meptin tends to inhibit skin reactions in allergen tests. Meptin should be withdrawn 12 hrs prior to such tests.
Other Precautions: Similar to other β2-adrenergic agonists, tissue damage in cardiac muscle was noted in oral toxicity studies at Meptin 30 and 10 mg/kg/day, or higher in the subacute and chronic toxicity studies, respectively, using rats. The damage was also observed in dog studies. However, the damage has been reported with other β2-adrenergic agonists in both rats and dogs.
Dietary administration of procaterol hydrochloride for 104 weeks was reported to cause mesovarian leiomyoma in SD rats. The tumor, however, is rat-specific and tends to develop during long-term administration of β2-adrenergic agonists.
Use in pregnancy & lactation: Meptin 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 Meptin during pregnancy has not been established.)
Nursing should be interrupted before starting treatment with Meptin. (Rat studies showed that procaterol hydrochloride is excreted in breast milk.)
Use in children: The safety of Meptin in low birth weight infants and neonates has not been established.
Use in the elderly: Dosage adjustment or other appropriate measures should be considered when prescribing Meptin to elderly patients, because these patients may be physiologically more sensitive to the drug than younger patients.
Use In Pregnancy & Lactation
Meptin 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 Meptin during pregnancy has not been established.)
Nursing should be interrupted before starting treatment with Meptin. (Rat studies showed that procaterol hydrochloride is excreted in breast milk.)
Nursing should be interrupted before starting treatment with Meptin. (Rat studies showed that procaterol hydrochloride is excreted in breast milk.)
Adverse Reactions
In clinical trials involving 22,575 patients, a total of 644 patients (2.83%) showed adverse reactions, including abnormal laboratory values. (At the time of approval of the initial application, completion of re-examination and approval of an additional indication for oral formulations of Meptin tablet and syrup.
The following summary of data includes adverse reactions reported after marketing without incidence rates.
Clinically Significant Adverse Reactions (*Incidence Unknown): Shock, Anaphylactoid Reactions: Shock or anaphylactoid reactions may occur. Patients should therefore be closely monitored. If abnormal findings are observed, Meptin should be discontinued and appropriate measures taken.
Significant decreases in serum potassium levels have been reported in patients receiving Meptin. If xanthine derivatives, corticosteroids or diuretics are co-administered with this drug in patients with severe asthma, extreme care is necessary to minimize the possibility of aggravating the decrease in serum potassium levels induced by β2-adrenergic agonists. Serum potassium levels should be closely monitored in hypoxic patients, in view of the possible aggravation of cardiac arrhythmias secondary to a decrease in serum potassium levels.
Other Adverse Reactions: The following table shows the adverse reactions for tablets: (see Table 1).
The following summary of data includes adverse reactions reported after marketing without incidence rates.
Clinically Significant Adverse Reactions (*Incidence Unknown): Shock, Anaphylactoid Reactions: Shock or anaphylactoid reactions may occur. Patients should therefore be closely monitored. If abnormal findings are observed, Meptin should be discontinued and appropriate measures taken.
Significant decreases in serum potassium levels have been reported in patients receiving Meptin. If xanthine derivatives, corticosteroids or diuretics are co-administered with this drug in patients with severe asthma, extreme care is necessary to minimize the possibility of aggravating the decrease in serum potassium levels induced by β2-adrenergic agonists. Serum potassium levels should be closely monitored in hypoxic patients, in view of the possible aggravation of cardiac arrhythmias secondary to a decrease in serum potassium levels.
Other Adverse Reactions: The following table shows the adverse reactions for tablets: (see Table 1).
The following table shows the adverse reactions for syrup: (see Table 2).
Drug Interactions
Precautions for co-administration should be administered with care when co-administered with the following drugs: Catecholamines (eg, epinephrine and isoproterenol): The combined use of Meptin with catecholamines may cause arrhythmias or cardiac arrest. Epinephrine, isoproterenol and other catecholamines potentiate the adrenoreceptor stimulating action of Meptin, possibly resulting in the induction of arrhythmias.
Xanthine derivatives (eg, theophylline, aminophylline hydrate and diprophylline): The combined use of xanthine derivatives may aggravate hypokalemia and cardiovascular adverse reactions (eg, tachycardia, arrhythmias) due to β-adrenergic stimulation. If any of these abnormalities are observed, the dose should be reduced or treatment should be discontinued immediately. Xanthine derivatives potentiate the adrenoreceptor-stimulating action of Meptin, possibly resulting in a decrease in serum potassium levels and causing cardiac or vascular adverse reactions. The mechanism responsible for the induction of hypokalemia is not known.
Corticosteroids (eg, betamethasone, prednisolone and hydrocortisone sodium succinate) and diuretics (eg, furosemide): The combined use of Meptin with corticosteroids and diuretics may cause a decrease in serum potassium levels, resulting in arrhythmias. If any of these abnormalities are observed, the dose of the drug should be reduced or treatment should be discontinued immediately. Corticosteroids and diuretics augment the excretion of potassium from the renal tubules, possibly resulting in an excessive decrease in serum potassium levels.
Xanthine derivatives (eg, theophylline, aminophylline hydrate and diprophylline): The combined use of xanthine derivatives may aggravate hypokalemia and cardiovascular adverse reactions (eg, tachycardia, arrhythmias) due to β-adrenergic stimulation. If any of these abnormalities are observed, the dose should be reduced or treatment should be discontinued immediately. Xanthine derivatives potentiate the adrenoreceptor-stimulating action of Meptin, possibly resulting in a decrease in serum potassium levels and causing cardiac or vascular adverse reactions. The mechanism responsible for the induction of hypokalemia is not known.
Corticosteroids (eg, betamethasone, prednisolone and hydrocortisone sodium succinate) and diuretics (eg, furosemide): The combined use of Meptin with corticosteroids and diuretics may cause a decrease in serum potassium levels, resulting in arrhythmias. If any of these abnormalities are observed, the dose of the drug should be reduced or treatment should be discontinued immediately. Corticosteroids and diuretics augment the excretion of potassium from the renal tubules, possibly resulting in an excessive decrease in serum potassium levels.
Caution For Usage
Precautions for Handling: Meptin is supplied in 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.
Storage and Care: Patients should keep Meptin in the dedicated storage container and to cap the container immediately after use. Patients should wipe the mouthpiece (inhalation orifice) or wipe it with a wet cloth. Avoid Meptin to be subject to strong impact and not to disassemble the housing.
Storage and Care: Patients should keep Meptin in the dedicated storage container and to cap the container immediately after use. Patients should wipe the mouthpiece (inhalation orifice) or wipe it with a wet cloth. Avoid Meptin to be subject to strong impact and not to disassemble the housing.
Storage
Store at temperatures not exceeding 30°C. After removal from the aluminum pillow package, keep it stored in the dedicated storage container.
Action
Pharmacology: Bronchodilative Action: The bronchodilative action of procaterol hydrochloride 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 1-5 min after inhalation in conscious guinea pigs and anesthetized dogs, indicating much faster onset of action than the tablet formulation.
Inhaled procaterol hydrochloride dilates not only the central airway but also peripheral airways in pediatric asthma patients.
Duration of Bronchodilative Action: Procaterol hydrochloride had a longer duration of bronchodilative action than isoproterenol, trimetoquinol, orciprenaline and salbutamol in dogs, cats and guinea pigs.
The potency with which procaterol hydrochloride at 10 mcg by inhalation inhibited the increase in airway resistance due to histamine was equal to that of salbutamol at 200 mcg by inhalation in anesthetized dogs. However, procaterol hydrochloride is longer-acting than salbutamol.
Selectivity for β2-Adrenergic Receptors (Organ Selectivity): The selectivity of procaterol hydrochloride for β2-adrenergic receptors in the respiratory system greater than that for such receptors in the cardiovascular system, as compared to isoproterenol, trimetoquinol, orciprenaline and salbutamol in dogs, cats and guinea pigs.
Antiallergic Action: Procaterol hydrochloride exhibited a definite antiallergic action by inhibiting antigen-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 allergen inhalation in bronchial asthma patients, as compared to isoproterenol, trimetoquinol, orciprenaline sulfate and salbutamol sulfate.
The drug also inhibited allergen-induced delayed-type and immediate-type bronchial responses.
Effects on Respiratory Tract System: Procaterol hydrochloride accelerated ciliary activity in the airway of pigeons.
Effect on Exercise-Induced Asthmatic Attacks: Procaterol hydrochloride suppressed treadmill or ergometer exercise- or methacholine-induced asthmatic attacks in patients with bronchial asthma.
Effect on Airway Hypersensitivity: Procaterol hydrochloride inhibited airway hypersensitivity induced by the inoculation of influenza virus C in dogs.
Effect on Vascular Permeability Increase: Procaterol hydrochloride inhibited the acceleration of vascular permeability and edema formation in dorsal subcutaneous air sacs in rats experimentally prepared using various inflammatory chemical agents. Its potency was similar to that of isoproterenol. Procaterol hydrochloride also inhibited pulmonary edema induced by histamine inhalation in guinea pigs, with greater potency than salbutamol sulfate.
Effect on Cough: Procaterol hydrochloride hydrate inhibited substance P-induced cough in normal subjects with upper respiratory tract infection.
Clinical Studies: Meptin 50 mcg tablets were studied in a total of 1,362 patients at 212 institutions throughout Japan. The clinical efficacy rates of the drug administered by single and repeated administration in patients with bronchial asthma were 51.1% (310/607) and 40.1% (188/469), respectively. The efficacy rate for repeated administration in patients with chronic bronchitis or pulmonary emphysema was 20.2% (19/94), and the corresponding value in patients with acute bronchitis was 50% (36/72). Tolerance to the drug was not observed during repeated administration.
Meptin 25 mcg tablets were studied in children with bronchial asthma. The clinical efficacy of the drug single and repeated administration was 59.4% (199/335) and 48% (145/302), respectively. The efficacy of the drug by repeated administration in those with acute bronchitis was 94% (79/84). Tolerance to the drug was not observed during repeated administration.
Meptin syrup was studied in children. The clinical efficacy of the drug by single administration in those with bronchial asthma was 82.9% (34/41), the efficacy by repeated administration in those with bronchial asthma or asthma-like bronchitis was 50.7% (116/229) and the efficacy by repeated administration in those with acute bronchitis was 75.9% (104/137).
Pharmacokinetics: Plasma Concentrations: When Meptin tablet was administered orally to a 6 healthy male subjects as single doses of 50 mcg/subject and 100 mcg/subject, the following plasma concentration curves and pharmacokinetic parameters were obtained.
Plasma Pharmacokinetic Data: 50 mcg tablet: Time to reach maximum plasma concentration (tmax) is 1.1 hr, peak plasma concentration (Cmax) is 97 pg/mL and half-life (t½) is not determined.
100 mcg tablet: Tmax is 1.5 hrs, Cmax is 226 pg/mL and t½ is 3.6 hrs.
When Meptin syrup was administered orally to 44 healthy male subjects at a single dose of 100 mcg/subject as procaterol hydrochloride, in a fasting condition, the following plasma concentration curves and pharmacokinetic parameters were obtained.
Pharmacokinetic parameters of procaterol syrup: Tmax is 1.3±0.7 hrs, Cmax is 263±104 pg/mL, t½ is 41±1.8 hrs and area under the concentration-time curve (AUC) is 1,151±288 pg·hr/mL.
Urinary Excretion: When Meptin was administered orally as single doses of 50 and 100 mcg/subject as procaterol hydrochloride, 9.93% and 11.65% of the dose were excreted into the urine within 24 hrs post-dosing, respectively.
the onset of the bronchodilative action was observed at 1-5 min after inhalation in conscious guinea pigs and anesthetized dogs, indicating much faster onset of action than the tablet formulation.
Inhaled procaterol hydrochloride dilates not only the central airway but also peripheral airways in pediatric asthma patients.
Duration of Bronchodilative Action: Procaterol hydrochloride had a longer duration of bronchodilative action than isoproterenol, trimetoquinol, orciprenaline and salbutamol in dogs, cats and guinea pigs.
The potency with which procaterol hydrochloride at 10 mcg by inhalation inhibited the increase in airway resistance due to histamine was equal to that of salbutamol at 200 mcg by inhalation in anesthetized dogs. However, procaterol hydrochloride is longer-acting than salbutamol.
Selectivity for β2-Adrenergic Receptors (Organ Selectivity): The selectivity of procaterol hydrochloride for β2-adrenergic receptors in the respiratory system greater than that for such receptors in the cardiovascular system, as compared to isoproterenol, trimetoquinol, orciprenaline and salbutamol in dogs, cats and guinea pigs.
Antiallergic Action: Procaterol hydrochloride exhibited a definite antiallergic action by inhibiting antigen-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 allergen inhalation in bronchial asthma patients, as compared to isoproterenol, trimetoquinol, orciprenaline sulfate and salbutamol sulfate.
The drug also inhibited allergen-induced delayed-type and immediate-type bronchial responses.
Effects on Respiratory Tract System: Procaterol hydrochloride accelerated ciliary activity in the airway of pigeons.
Effect on Exercise-Induced Asthmatic Attacks: Procaterol hydrochloride suppressed treadmill or ergometer exercise- or methacholine-induced asthmatic attacks in patients with bronchial asthma.
Effect on Airway Hypersensitivity: Procaterol hydrochloride inhibited airway hypersensitivity induced by the inoculation of influenza virus C in dogs.
Effect on Vascular Permeability Increase: Procaterol hydrochloride inhibited the acceleration of vascular permeability and edema formation in dorsal subcutaneous air sacs in rats experimentally prepared using various inflammatory chemical agents. Its potency was similar to that of isoproterenol. Procaterol hydrochloride also inhibited pulmonary edema induced by histamine inhalation in guinea pigs, with greater potency than salbutamol sulfate.
Effect on Cough: Procaterol hydrochloride hydrate inhibited substance P-induced cough in normal subjects with upper respiratory tract infection.
Clinical Studies: Meptin 50 mcg tablets were studied in a total of 1,362 patients at 212 institutions throughout Japan. The clinical efficacy rates of the drug administered by single and repeated administration in patients with bronchial asthma were 51.1% (310/607) and 40.1% (188/469), respectively. The efficacy rate for repeated administration in patients with chronic bronchitis or pulmonary emphysema was 20.2% (19/94), and the corresponding value in patients with acute bronchitis was 50% (36/72). Tolerance to the drug was not observed during repeated administration.
Meptin 25 mcg tablets were studied in children with bronchial asthma. The clinical efficacy of the drug single and repeated administration was 59.4% (199/335) and 48% (145/302), respectively. The efficacy of the drug by repeated administration in those with acute bronchitis was 94% (79/84). Tolerance to the drug was not observed during repeated administration.
Meptin syrup was studied in children. The clinical efficacy of the drug by single administration in those with bronchial asthma was 82.9% (34/41), the efficacy by repeated administration in those with bronchial asthma or asthma-like bronchitis was 50.7% (116/229) and the efficacy by repeated administration in those with acute bronchitis was 75.9% (104/137).
Pharmacokinetics: Plasma Concentrations: When Meptin tablet was administered orally to a 6 healthy male subjects as single doses of 50 mcg/subject and 100 mcg/subject, the following plasma concentration curves and pharmacokinetic parameters were obtained.
Plasma Pharmacokinetic Data: 50 mcg tablet: Time to reach maximum plasma concentration (tmax) is 1.1 hr, peak plasma concentration (Cmax) is 97 pg/mL and half-life (t½) is not determined.
100 mcg tablet: Tmax is 1.5 hrs, Cmax is 226 pg/mL and t½ is 3.6 hrs.
When Meptin syrup was administered orally to 44 healthy male subjects at a single dose of 100 mcg/subject as procaterol hydrochloride, in a fasting condition, the following plasma concentration curves and pharmacokinetic parameters were obtained.
Pharmacokinetic parameters of procaterol syrup: Tmax is 1.3±0.7 hrs, Cmax is 263±104 pg/mL, t½ is 41±1.8 hrs and area under the concentration-time curve (AUC) is 1,151±288 pg·hr/mL.
Urinary Excretion: When Meptin was administered orally as single doses of 50 and 100 mcg/subject as procaterol hydrochloride, 9.93% and 11.65% of the dose were excreted into the urine within 24 hrs post-dosing, respectively.
MedsGo Class
Antiasthmatic & COPD Preparations
Features
Brand
Meptin
Full Details
Dosage Strength
5mcg /ml
Drug Ingredients
- Procaterol
Drug Packaging
Syrup 60ml
Generic Name
Procaterol Hcl
Dosage Form
Syrup
Registration Number
DRP-5277
Drug Classification
Prescription Drug (RX)
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