ASMALINE

Terbutaline sulfate

USP is a beta-adrenergic agonist bronchodilator available as tablets of 2.5 mg (2.05 mg of the free base) and 5 mg (4.1 mg of the free base) for oral administration.

Terbutaline sulfate is ±-α-[( tert –butylamino) methyl]-3,5-dihydroxybenzyl alcohol sulfate (2:1) (salt).

The molecular formula is (C 12 H 19 NO 3 ) 2.

• H 2 SO and the structural formula is Terbutaline sulfate USP is a white to gray-white crystalline powder.

It is odorless or has a faint odor of acetic acid.

It is soluble in water and in 0.1N hydrochloric acid, slightly soluble in methanol, and insoluble in chloroform.

Its molecular weight is 548.65.

Ingredients: lactose monohydrate, pregelatinized starch, microcrystalline cellulose, povidone, and magnesium stearate. image description.

Tetrabutylene is used in the following cases: air reed cramps associated with lung diseases, such as asthma, reeds inflammation, and lung swelling.

The medication is used with caution, under medical supervision, in the following cases: cardiovascular diseases, because terbutylene may lead to hypertension and an acceleration of heart rate.

Diabetes, where the testoline may increase blood sugar.

In vitro and in vivo pharmacologic studies have demonstrated that terbutaline exerts a preferential effect on beta 2 -adrenergic receptors.

While it is recognized that beta 2 -adrenergic receptors are the predominant receptors in bronchial smooth muscle, data indicate that there is a population of beta 2 -receptors in the human heart, existing in a concentration between 10% to 50%.

The precise function of these receptors has not been established See WARNINGS.

In controlled clinical studies in patients given terbutaline sulfate orally, proportionally greater changes occurred in pulmonary function parameters than in heart rate or blood pressure.

While this suggests a relative preference for the beta 2 -receptors in man, the usual cardiovascular effects commonly associated with other sympathomimetic agents were also observed with terbutaline sulfate.

The pharmacologic effects of beta-adrenergic agonists, including terbutaline, are at least in part attributable to stimulation through beta-adrenergic receptors of intracellular adenyl cyclase, the enzyme which catalyzes the conversion of adenosine triphosphate (ATP) to cyclic 3’, 5’-adenosine monophosphate (cAMP).

Increased cAMP levels are associated with relaxation of bronchial smooth muscle and inhibition of release of mediators of immediate hypersensitivity from cells, especially from mast cells.

Controlled clinical studies have shown that terbutaline sulfate relieves bronchospasm in chronic obstructive pulmonary disease by significantly increasing pulmonary function (e.g., an increase of 15% or more in FEV and in FEF 25%-75% ).

After administration of terbutaline sulfate tablets, a measurable change in flow rate usually occurs within 30 minutes, and a clinically significant improvement in pulmonary function occurs within to 120 minutes.

The maximum effect usually occurs within to 180 minutes.

Terbutaline sulfate also produces a clinically significant decrease in airway and pulmonary resistance, which persists for 4 hours or longer.

Significant bronchodilator action (as measured by airway resistance, FEF 25%-75% or PEFR) has also been demonstrated for up to 8 hours in some studies.

In studies comparing the effectiveness of terbutaline sulfate with that of ephedrine for up to 3 months, both drugs maintained a significant improvement in pulmonary function throughout this period of treatment.

Studies in laboratory animals (minipigs, rodents, and dogs) have demonstrated the occurrence of cardiac arrhythmias and sudden death (with histologic evidence of myocardial necrosis) when beta-agonists and methylxanthines were administered concurrently.

The clinical significance of these findings is unknown.

Oral administration of 5-mg terbutaline sulfate tablets or 5 mg terbutaline sulfate in solution in 17 healthy, adult, male subjects, resulted in mean (SD) peak plasma terbutaline concentration of 8.3 and 8.6 ng/mL, which were observed at median (range) times of 2 (1 to 3) and 1.5 (0.5 to 3.0) hours after dosing.

The mean (SD) AUC values were 54.6 and 53.1 hr•ng/mL, and corresponded to a bioavailability of 103% for the tablet relative to the solution.

After oral administration of terbutaline, 51 to 62 mcg/kg of body weight, to 3 healthy male subjects, peak serum levels of 3.1 to 6.2 ng/mL were observed to 3 hours later.

In the same study, after 3 days only 30% to 50% of the dose was recovered from urine and the remainder from the feces, which may indicate poor absorption.

After an oral dose to asthmatic patients, the elimination half-life of terbutaline was approximately 3.4 hours.

In comparison to oral dosing, subcutaneous administration of 0.5 mg of terbutaline sulfate to 17 healthy, adult, male subjects resulted in a mean (SD) peak plasma terbutaline concentration of 9.6 ng/mL, which was observed at a median (range) time of 0.5 (0.08 to 1.0) hours after dosing.

The mean (SD) AUC and total body clearance values were 29.4 hr•ng/mL, and 311 mL/min, respectively.

The terminal half-life was determined in of the 17 subjects and had a mean (SD) of 5.7 hours.

About 90% of the drug was excreted in the urine at 96 hours after subcutaneous administration, with about 60% of this being unchanged drug.

The sulfate conjugate is a major metabolite of terbutaline, and urinary excretion is the primary route of elimination.

There are no reports of any clinical pharmacokinetic studies investigating dose proportionality, effect of food, or special population studies with terbutaline.

Tyrbutaline is an expanded trachea, relaxing the muscles of respiratory smoothness, by stimulating beta-2 receptors, as well as its light impact on the heart rate.

Tetropthalin is used for adults and children at least 12 years old.

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of the scientific.

The median subcutaneous lethal dose of terbutaline sulfate in mature rats is approximately 165 mg/kg (approximately 90 times the maximum recommended daily oral dose for adults on a mg/m 2 basis).

The median subcutaneous lethal dose of terbutaline sulfate in young rats is approximately 2000 mg/kg (approximately 1100 times the maximum recommended daily oral dose for adults on a mg/m 2 basis).

The expected symptoms with overdosage are those of excessive beta-adrenergic stimulation and/or occurrence or exaggeration of any of the symptoms listed under ADVERSE REACTIONS, e.g., seizures, angina, hypertension or hypotension, tachycardia with rates up to 200 beats per minute, arrhythmias, nervousness, headache, tremor, dry mouth, palpitation, nausea, dizziness, fatigue, malaise, and insomnia.

Hypokalemia may also occur.

There is no specific antidote.

Treatment consists of discontinuation of terbutaline sulfate together with appropriate symptomatic therapy.

The judicious use of a cardioselective beta-receptor blocker may be considered, bearing in mind that such medication can produce bronchospasm.

There is insufficient evidence to determine if dialysis is beneficial for overdosage of terbutaline sulfate.

In the alert patient who has taken excessive oral medication, the stomach should be emptied by induced emesis followed by lavage.

In the unconscious patient, the airway should be secured with a cuffed endotracheal tube before lavage, and emesis should not be induced.

Instillation of activated charcoal slurry may help reduce absorption of terbutaline.

Adequate respiratory exchange should be maintained, and cardiac and respiratory support provided as needed.

The patient should be monitored until signs and symptoms of overdosage have subsided.

Asthma may deteriorate acutely over a period of hours or chronically over several days or longer.

If the patient needs more doses of terbutaline sulfate than usual, this may be a marker of destabilization of asthma and requires reevaluation of the patient and the treatment regimen, giving special consideration to the possible need for anti-inflammatory treatment, e.g., corticosteroids.

The use of beta-adrenergic agonist bronchodilators alone may not be adequate to control asthma in many patients.

Early consideration should be given to adding anti-inflammatory agents, e.g., corticosteroids.

Terbutaline sulfate, like all other beta-adrenergic agonists, can produce a clinically significant cardiovascular effect in some patients as measured by pulse rate, blood pressure, and/or symptoms.

Although such effects are uncommon after administration of terbutaline sulfate at recommended doses, if they occur, the drug may need to be discontinued.

In addition, beta-agonists have been reported to produce electrocardiogram (ECG) changes, such as flattening of the T wave, prolongation of the QTc interval, and ST segment depression.

The clinical significance of these findings is unknown.

Therefore, terbutaline sulfate, like all sympathomimetic amines, should be used with caution in patients with cardiovascular disorders, especially coronary insufficiency, cardiac arrhythmias, and hypertension.

There have been rare reports of seizures in patients receiving terbutaline; seizures did not recur in these patients after the drug was discontinued.

Oral terbutaline sulfate has not been approved and should not be used for acute or maintenance tocolysis. 2.

Terbutaline sulfate is contraindicated in patients known to be hypersensitive to sympathomimetic amines or any component of this drug product.

The usual oral dose of terbutaline sulfate for adults is 5 mg administered at approximately six-hour intervals, three times daily, during the hours the patient is usually awake.

If side effects are particularly disturbing, the dose may be reduced to 2.5 mg three times daily, and still provide a clinically significant improvement in pulmonary function.

The total dose within 24 hours should not exceed 15 mg. Children Terbutaline sulfate is not recommended for use in children below the age of 12 years.

A dosage of 2.5 mg three times daily is recommended for children 12-15 years of age.

The total dose within 24 hours should not exceed 7.5 mg. If a previously effective dosage regimen fails to provide the usual relief, medical advice should be sought immediately as this is often a sign of seriously worsening asthma that would require reassessment of therapy.

Terbutaline sulfate tablets, USP are packaged in bottles of and 1000 tablets.

Descriptions of the 2.5 and 5 mg tablets follow: Tablets 2.5 mg.

• White to off-white, oval tablets, scored on one side and engraved with “T132” on the other side Bottles of 30 NDC 71205-938-30 Bottles of 60 NDC 71205-938-60 Bottles of 90 NDC 71205-938-90 Bottles of 100 NDC 71205-938-00 Bottles of 500 NDC 71205-938-55 Tablets 5 mg.

• White to off-white, round, scored and engraved “T” above and “133” below the score on the scored side.

Bottles of 30 NDC 71205-939-30 Bottles of 60 NDC 71205-939-60 Bottles of 90 NDC 71205-939-90 Bottles of 100 NDC 71205-939-00 Bottles of 500 NDC 71205-939-55 Store at 20°C to 25°C (68°F to 77°F) .

Dispense in a tight, light-resistant container as defined in the USP with a child-resistant closure Manufactured for: TWi Pharmaceuticals USA, Inc.

Paramus, NJ 07652.

There are no adequate and well-controlled studies of terbutaline sulfate in pregnant women.

Published animal studies show that rat offspring exhibit alterations in behavior and brain development, including decreased cellular proliferation and differentiation when dams were treated subcutaneously with terbutaline during the late stage of pregnancy and lactation period.

Terbutaline exposures in rat dams were approximately 6.5 times the common human dose in adults of 15 mg/day, on a mg/m 2 basis.

Oral terbutaline sulfate has not been approved and should not be used for acute or maintenance tocolysis.

In particular, terbutaline sulfate should not be used for tocolysis in the outpatient or home setting.

Serious adverse reactions, including death, have been reported after administration of terbutaline sulfate to pregnant women.

In the mother, these adverse reactions include increased heart rate, transient hyperglycemia, hypokalemia, cardiac arrhythmias, pulmonary edema and myocardial ischemia.

Increased fetal heart rate and neonatal hypoglycemia may occur as a result of maternal administration.

In animal embryofetal developmental studies, no teratogenic effects were observed in offspring when pregnant rats and rabbits received terbutaline sulfate at oral doses up to 50 mg/kg/day, approximately and 65 times, respectively, the maximum recommended daily oral dose for adults, on a mg/m 2 basis.

Terbutaline sulfate should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.

It is not known whether this drug is excreted in human milk.

Therefore, terbutaline sulfate should be used during nursing only if the potential benefit justifies the possible risk to the newborn.

Terbutaline sulfate is not recommended for patients under the age of 12 years because of insufficient clinical data to establish safety and effectiveness See DOSAGE AND ADMINISTRATION.

Clinical studies of terbutaline sulfate did not include sufficient numbers of subjects aged and over to determine whether they respond differently from younger subjects.

Other reported clinical experience has not identified differences in responses between the elderly and younger patients.

In general, dose selection for an elderly patient should be cautious, usually starting at the low end of the dosing range, reflecting the greater frequency of decreased hepatic, renal, or cardiac function, and of concomitant disease or other drug therapy.