Procaterol Hydrochloride syrup preparation
COMPOSITION AND DESCRIPTION
1. | Composition Each mL of Meptin syrup contains 5 μg of procaterol hydrochloride. The formulation contains 3% ethyl alcohol used as a solvent. |
2. | Product Description Meptin syrup is a colorless. clear and slight viscous liquid. It has an orange odor and a sweet taste. pH: 3.5 - 4.5 |
INDICATIONS
Remission of various symptoms caused by respiratory obstructive disturbance in the following diseases bronchial asthma. chronic bronchitis. pulmonary emphysema. acute bronchitis, and asthma-like bronchitis.
CONTRAINDICATIONS
(Meptin syrup is contraindicated in the following patients)
Patients with a history of hypersensitivity to any ingredient of this drug.
DOSAGE AND ADMINISTRATION
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 the 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. The recommended usual doses for children younger than 6 years old are listed below.
Children younger than 1 year old: 2-3 mL of Meptin syrup (10-15 μg of procaterol hydrochloride).
Children 1-3 years of age: 3-4 mL of Meptin syrup (15-20 μg of procaterol hydrochloride).
Children 3-6 years of age: 4-5 mL of Meptin syrup (20-25 μg of procaterol hydrochloride).
PHARMACOLOGY
1. | Bronchodilatory Action The bronchodilatory 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. |
2. | Duration of Bronchodilatory Action Procaterol hydrochloride had a longer duration of action than isoproterenol, trimetoquinol, orciprenaline, or salbutamol in dogs, cats, and guinea pigs. |
3. | Selectivity for β2-Adrenergic Receptors (Organ Selectivity) The selectivity of procaterol hydrochloride for β2-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 hydrochloride exhibited a definite anti-allergic action by inhibiting antibody-induced increases 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. The drug also inhibited allergen induced delayed-type and immediate-type bronchial responses. |
5. | Effects on Airway Secretion Procaterol hydrochloride accelerates ciliary activity in the airways of pigeons. |
6. | Inhibitory Effect on Exercise-Induced Asthma Episodes The results of treadmill or ergometer exercise or methacholine loading tests suggest that procaterol hydrochloride suppresses exercise-induced asthma attacks in patients with bronchial asthma. |
7. | Effect on Accelerated Airway Hypersensitivity Procaterol hydrochloride inhibited airway hypersensitivity accelerated by the inoculation of influenza virus C in dogs. |
8. | Inhibitory Effect on Accelerated Vascular Permeability 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 salbutarnol. |
9. | Effect on Cough Procaterol hydrochloride inhibited cough in acute bronchitis induced by the inhalation of substance P. |
PHARMACOKINETICS
1. | Plasma Concentrations When procaterol hydrochloride was administered orally to 6 healthy male subjects at single doses of 50 and 100 μg/ subject. the following plasma concentration curves and pharmacokinetic parameters were obtained. Plasma kinetic data
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2. | Urinary Excretion When procaterol hydrochloride was administered orally as single doses of 50 and 100 μg/subject, 9.93% and 11.65% of the dose were excreted in the urine within 24 hours post-dosing, respectively. |
PRECAUTIONS
1. | Careful Administration (Meptin syrup should be administered with care in the following patients.)
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2. | Important Precautions
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3. | Use in the Elderly Dosage adjustment or other appropriate measures should be considered when prescribing Meptin syrup 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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5. | Pediatric Use The safety of this drug in premature babies and neonates has not been established. (Clinical experience in premature babies and neonates is insufficient.) |
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. | Other Precautions
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ADVERSE REACTIONS
In clinical trials involving 22,757 subjects, a total of 644 patients (2.83%) showed adverse reactions, including abnormal laboratory values. The following summary of data includes adverse reactions reported after marketing without incidence. (Figures are total cases reported from the time to approval up to December 1999) | |||||||||||||||||||||||||||||
1. | Clinically significant adverse reactions (*incidence unknown)
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2. | Other adverse reactions
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Note:
1) If symptoms of hypersensitivity occur, the drug should be discontinued.
* The incidences rate of adverse reactions reported voluntarily after marketing and those reported outside Japan are not known.
DRUG INTERACTIONS
Precautions for co-administration (Meptin syrup should be administered with care when co-administered with the following drugs.)
Drugs | Signs, Symptoms, and Treatment | Mechanism and Risk Factors |
catecholamines (e.g., epinephrine and isoproterenol) | The combined use of this drug with catecholamines may cause arrhythmias or cardiac arrest | Epinephrine, isoproterenol, and other catecholamines potentiate the adrenoreceptor stimulating action of this drug, possibly resulting in the induction of arrhythmias |
Xanthine derivatives (e,g theophylline, aminophylline, and dipropylline) | The combined use of this drug with xanthine derivatives may aggravate hypokalemia and cardiovascular adverse reactions (e.g., tachycardia, arrhythmias) due to 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 this drug, 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 (e.g. betamethasone, prednisolone, and hydrocortisone sodium succinate) and Diuretics (e.g. furosemide) | The combined use of this drug with corticosteroids or diuretics may cause a decrease in serum potassium levels, resulting in arrhythmias. If any of these abnormalities are observed. the dose 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 |
PHYSICOCHEMISTRY
Nonproprietary name:
Procaterol hydrochloride (JAN)
Chemical name:
8-hydroxy-5-[(1 RS,2SR)-1-hydroxy-2-isopropyl-aminobutyl)-2(1 H)quinolinone monohydrochloride hemihydrate.
Structural formula:
Molecular formula: C16H22N2O3 - HCl -1/2H20
Molecular weight: 335.83
STORAGE
Room temperature, protected from light
PACKAGING
Meptin syrup: 60 mL in bottles
Reg. No. : DKL 8618701437A1
HARUS DENGAN RESEP DOKTER
Manufactured by:
PT Otsuka Indonesia
Lawang, East Java
Indonesia
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