Consists of bromhexine hydrochloride, guaiphenesin, terbutaline sulphate
Actions of Bromhexine hydrochloride (Besilent) in details
Description: Bromhexine hydrochloride (Besilent) enhances mucus transport by reducing mucus viscosity and by activating the ciliated epithelium (mucociliary clearance).
Pharmacokinetics:
Absorption: Rapidly absorbed from the GI tract. Bioavailability: Approx 20%. Time to peak plasma concentration: Approx 1 hr.
Distribution: Widely distributed to body tissues. Crosses blood brain-barrier and placenta (small amounts). Plasma protein binding: >90%.
Metabolism: Extensive hepatic first-pass metabolism.
Excretion: Via urine (approx 85-90%, mainly as metabolites). Terminal elimination half-life: 13-40 hr.
Bromhexine hydrochloride (Besilent) administration
Should be taken with food.
Guaiphenesin (Besilent) pharmacology
The mechanism of action of methocarbamol in humans has not been established, but may be due to central nervous system depression. It has no direct action on the contractile mechanism of striated muscle, the motor end plate or the nerve fiber.
Actions of Terbutaline sulphate (Besilent) in details
Pharmacotherapeutic Group: Antiasthma.
Pharmacology: Terbutaline sulphate (Besilent) is an adrenergic agonist which selectively stimulates β-receptors, thus producing relaxation of bronchial smooth muscle, inhibition of the release of endogenous spasmogens, inhibition of edema caused by endogenous mediators, increased mucociliary clearance and relaxation of the uterine muscle.
Pharmacokinetics: The bronchodilating effect of Terbutaline sulphate (Besilent) tablet and syrup starts about 1 hr after administration and reaches its maximum after 2-3 hrs. The duration of action is longer than that of earlier known similar compounds and lasts for about ≥7 hrs. The bronchospasmolytic effect of inhaled Terbutaline sulphate (Besilent) is rapid in onset producing a significant bronchospasmolytic effect after 30-90 sec. Maximum response is usually achieved about 60 min after administration and significant bronchodilatory activity has been shown to persist for 5-7 hrs.
How should I take Terbutaline sulphate (Besilent)?
Take this medicine exactly as directed by your doctor. Do not take more of it, do not take it more often, and do not take it for a longer time than your doctor ordered. Do not change or stop using this medicine without checking first with your doctor.
You may be taking other medicines for asthma together with terbutaline. Do not stop taking these medicines and do not reduce the dose, even if your asthma seems better, unless you are told to do so by your doctor.
Dosing
The dose of this medicine will be different for different patients. Follow your doctor's orders or the directions on the label. The following information includes only the average doses of this medicine. If your dose is different, do not change it unless your doctor tells you to do so.
The amount of medicine that you take depends on the strength of the medicine. Also, the number of doses you take each day, the time allowed between doses, and the length of time you take the medicine depend on the medical problem for which you are using the medicine.
- For oral dosage form (tablets):
- For prevention of bronchospasm:
- Adults and teenagers—5 milligrams (mg) three times a day. This medicine is taken only during the hours the patient is usually awake. Your doctor may adjust your dose as needed. However, the dose is usually not more than 15 mg per 24 hours.
- Children and teenagers 12 to 15 years of age—2.5 mg three times a day. Your doctor may adjust your dose as needed up. However, the dose is usually not more than 7.5 mg per 24 hours.
- Children younger than 12 years of age—Use is not recommended.
- For prevention of bronchospasm:
Missed Dose
If you miss a dose of this medicine, take it as soon as possible. However, if it is almost time for your next dose, skip the missed dose and go back to your regular dosing schedule. Do not double doses.
Storage
Store the medicine in a closed container at room temperature, away from heat, moisture, and direct light. Keep from freezing.
Keep out of the reach of children.
Do not keep outdated medicine or medicine no longer needed.
Ask your healthcare professional how you should dispose of any medicine you do not use.
Terbutaline sulphate (Besilent) pharmacology
In vitro and in vivo pharmacologic studies have demonstrated that terbutaline exerts a preferential effect on beta2-adrenergic receptors. While it is recognized that beta2-adrenergic receptors are the predominant receptors in bronchial smooth muscle, data indicate that there is a population of beta2-receptors in the human heart, existing in a concentration between 10% to 50%. The precise function of these receptors has not been established. 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 beta2-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 FEV1 and in FEF25%-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 60 to 120 minutes. The maximum effect usually occurs within 120 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, FEF25%-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.
Preclinical
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.
Pharmacokinetics
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 (3.9) and 8.6 (3.6) 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(0-48) values were 54.6 (26.8) and 53.1 (23.5) 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 1 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 (3.6) 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(0-48) and total body clearance values were 29.4 (14.2) hr•ng/mL, and 311 (112) mL/min, respectively. The terminal half-life was determined in 9 of the 17 subjects and had a mean (SD) of 5.7 (2.0) 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.
References
- DailyMed. "TERBUTALINE SULFATE: DailyMed provides trustworthy information about marketed drugs in the United States. DailyMed is the official provider of FDA label information (package inserts).". https://dailymed.nlm.nih.gov/dailyme... (accessed September 17, 2018).
- NCIt. "Terbutaline Sulfate: NCI Thesaurus (NCIt) provides reference terminology for many systems. It covers vocabulary for clinical care, translational and basic research, and public information and administrative activities.". https://ncit.nci.nih.gov/ncitbrowser... (accessed September 17, 2018).
- EPA DSStox. "Terbutaline: DSSTox provides a high quality public chemistry resource for supporting improved predictive toxicology.". https://comptox.epa.gov/dashboard/ds... (accessed September 17, 2018).
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Information checked by Dr. Sachin Kumar, MD Pharmacology
