Consists of Bromhexine, Guaifenesin, Terbutaline
Actions of Bromhexine (Cherrymint) in details
Bromhexine (Cherrymint) is a synthetic derivative of the herbal active ingredient vasicine. Preclinically, it has been shown to increase the proportion of serious bronchial secretion. Bromhexine (Cherrymint) enhances mucus transport by reducing mucus viscosity and by activating the ciliated epithelium (mucociliary clearance).
In clinical studies, Bromhexine (Cherrymint) showed a secretolytic and secretomotor effect in the bronchial tract area, which facilitates expectoration and eases cough. Pharmacokinetics: Bromhexine (Cherrymint) is absorbed well by the enteral route, the absorption half-life of a Bromhexine (Cherrymint) solution is 0.4 hrs. Following oral intake of Bromhexine (Cherrymint) tablets, the peak plasma concentration is reached within approximately 1 hr (tmax). Bromhexine (Cherrymint) is subject to a first-pass effect of 75-80%; the absolute bioavailability of oral dosage forms is therefore given as 20-25% (37,40). Food before administration of Bromhexine (Cherrymint) enhances the bioavailability of the compound.
Following pre-oral administration, Bromhexine (Cherrymint) shows dose linearity in the dose range 8-32 mg. At least 10 different Bromhexine (Cherrymint) metabolites have been discovered in the plasma, including the pharmacologically active metabolite ambroxol.
There is a high level of plasma protein-binding at 95-99% and a large distribution volume of 7 L/kg body weight (IV administration). Bromhexine (Cherrymint) accumulates in the lung rather than in the plasma.
The dominant elimination half-life is given as 1 hr, the terminal elimination half-life is 13-40 hrs. Following oral administration of 8 mg, the plasma levels fell after 8-12 hrs to 1.5 ng/mL and 0.2 ng/mL, respectively. For the most part, Bromhexine (Cherrymint) is excreted renally in the form of metabolites that pass through the kidneys while only minor amounts of 0-10% parent compound are found in unchanged form in the urine. After 24 hrs and 5 days, 70% and 88% of the oral dose, respectively is recovered in the urine, 4% is excreted with the feces.
Bromhexine (Cherrymint) does not cumulate as the long terminal elimination half-life is not dominant. Steady-state levels are reached after 3 days at the latest.
In animal studies, Bromhexine (Cherrymint) penetrates the cerebrospinal fluid and the placenta. It is expected that the compound is excreted in breast milk.
Reduced clearance of Bromhexine (Cherrymint) parent substance can be expected in the case of severe liver disease; in the case of severe renal insufficiency, cumulation of metabolites cannot be ruled out; pharmacokinetic studies for these conditions are not available.
Toxicology: Acutely, Bromhexine (Cherrymint) HCl has a very low index of toxicity:
Oral LD
50 values were >5 g/kg in rats, >4 g/kg in rabbits, >10 g/kg in dogs and >1 g/kg in newborn rats. The intraperitoneal LD50 in rats was 2 g/kg. The LD50 values for the syrup formulation were >10 mL/kg in mice and rats. No clinical signs were observed at these acute doses.In repeated oral dose toxicity studies over 5 weeks, mice tolerated 200 mg/kg [no observed adverse effect level (NOAEL)]. At 2000 mg/kg, mortality was high. The few surviving mice showed a reversible increase in liver weight and serum cholesterol. Rats tolerated 25 mg/kg over 26 or 100 weeks, while at 500 mg/kg, convulsions and deaths occurred. The centrilobular hepatocytes were enlarged due to vacuolic change. Another 2-year study confirmed that doses up to 100 mg/kg are well-tolerated, while at 400 mg/kg, convulsions occurred sporadically in a few rats. Dogs tolerated 100 mg/kg (NOAEL) orally over 2 years. Bromhexine (Cherrymint) syrup (0.8 mg/mL) was well-tolerated up to 20 mg/kg in rats, but there was a reversible centrilobular simple fatty change of liver. An IM dose of 8 mg injectable solution was locally and systemically well-tolerated in dogs treated for 6 weeks.
Bromhexine (Cherrymint) was neither embryotoxic nor teratogenic in segment II at oral doses up to 300 mg/kg (rat) and 200 mg/kg (rabbit). Fertility was not impaired in segment II at doses up to 300 mg/kg. The “NOAEL” during the peri- and postnatal development in segment II was 25 mg/kg.
A single intra-articular injection of 4 mg Bromhexine (Cherrymint) was well-tolerated in rabbits and dogs. The lesions after IM injection in rabbits compared well with those after physiological saline solution. In vitro, 1 mL injectable solution showed a hemolytic action when mixed with 0.1 mL human blood.
In 2 studies (Ames and micronucleus tests), Bromhexine (Cherrymint) had no mutagenic potential. Bromhexine (Cherrymint) did not show a tumorigenic potential in the 2-year studies on rats given up to 400 mg/kg and on dogs given up to 100 mg/kg.
Bromhexine (Cherrymint) administration
Should be taken with food.
Actions of Guaifenesin (Cherrymint) in details
Guaifenesin (Cherrymint) may act as an irritant to gastric vagal receptors, and recruit efferent parasympathetic reflexes that cause glandular exocytosis of a less viscous mucus mixture. Cough may be provoked. This combination may flush tenacious, congealed mucopurulent material from obstructed small airways and lead to a temporary improvement in dyspnea or the work of breathing.
How should I take Guaifenesin (Cherrymint)?
Use Guaifenesin (Cherrymint) exactly as directed on the label, or as prescribed by your doctor. Do not use in larger or smaller amounts or for longer than recommended.
Do not give Guaifenesin (Cherrymint) to a child younger than 4 years old. Always ask a doctor before giving a cough or cold medicine to a child. Death can occur from the misuse of cough and cold medicines in very young children. Drink extra fluids to help loosen the congestion and lubricate your throat while you are taking this medication. Take Guaifenesin (Cherrymint) with food if it upsets your stomach.
Measure the liquid form of Guaifenesin (Cherrymint) with a special dose-measuring spoon or cup, not a regular table spoon. If you do not have a dose-measuring device, ask your pharmacist for one.
Do not crush, chew, break, or open a controlled-release, delayed-release, or extended-release tablet or capsule. Swallow it whole. Breaking or opening the pill may cause too much of the drug to be released at one time.
Store Guaifenesin (Cherrymint) at room temperature away from moisture, heat, and direct sunlight.
Guaifenesin (Cherrymint) administration
Oral: Administer with a large quantity of fluid to ensure proper action.
ER tablet: Do not break, crush, or chew ER tablet.
Bariatric surgery: Some institutions may have specific protocols that conflict with these recommendations; refer to institutional protocols as appropriate. Switch to IR tablet or oral solution.
Granules: Empty contents of packet onto tongue and swallow; for best taste, do not chew granules.
Guaifenesin (Cherrymint) pharmacology
Guaifenesin (Cherrymint) is an expectorant which increases the output of phlegm (sputum) and bronchial secretions by reducing adhesiveness and surface tension. The increased flow of less viscous secretions promotes ciliary action and changes a dry, unproductive cough to one that is more productive and less frequent. By reducing the viscosity and adhesiveness of secretions, Guaifenesin (Cherrymint) increases the efficacy of the mucociliary mechanism in removing accumulated secretions from the upper and lower airway.
Actions of Terbutaline (Cherrymint) in details
Pharmacology: Pharmacotherapeutic Group: Selective β2-agonist. ATC Code: R03AC03.
Pharmacodynamics: Terbutaline (Cherrymint) is an adrenergic agonist which predominantly stimulates β2-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.
The tertiary butyl group attached to the terminal nitrogen of the Terbutaline (Cherrymint) molecule is thought to confer selective stimulation of the pulmonary β2-receptors and only relatively minor stimulation of cardiac β1-receptors. The presence of the 2 phenolic hydroxyl groups in the meta positions confers resistance to metabolism by the enzyme catechol-o-methyl transferase.
The active drug is released gradually from Terbutaline (Cherrymint) prolonged-release tablets, leading to a prolonged bronchodilatation which in clinical trials has been demonstrated for up to 12 hrs.
The potent bronchospasmolytic effect is rapid in onset and reaches a maximum about 30 min after SC injection, 1 hr after aerosol and 2-3 hrs after oral administration. The duration of action is between 4 and 5 hrs.
Inhaled Terbutaline (Cherrymint) acts within a few minutes and has a duration for up to 6 hrs.
Pharmacokinetics: There is a considerable first-pass metabolism in the intestinal wall and in the liver. The bioavailability is around 10%. Maximum plasma concentration of Terbutaline (Cherrymint) is reached within 2-6 hrs, somewhat later after dosing in the evening.
About 20-30% of the metered-dose is deposited in the lungs at a normal inhalation flow rate.
Terbutaline (Cherrymint) is metabolised mainly by conjugation with sulfuric acid and excreted as the sulphate conjugate. No active metabolites are formed.
Metabolism of Terbutaline (Cherrymint) sulphate which is ingested orally or swallowed following inhalation is principally by conjugation in the GI mucosa. The drug is absorbed unchanged from the respiratory tract and is excreted mainly eg, in the urine. Practically all of an administered dose of Terbutaline (Cherrymint) is eliminated after 72 hrs.
How should I take Terbutaline (Cherrymint)?
A nurse or other trained health professional will give you Terbutaline (Cherrymint). Terbutaline (Cherrymint) is given as a shot under your skin (usually into the shoulder area).
Terbutaline (Cherrymint) may sometimes be given at home to patients who do not need to be in a hospital or clinic. If you are using Terbutaline (Cherrymint) at home, your doctor will teach you or someone who cares for you how to prepare and inject the medicine. Be sure that you understand exactly how the medicine is prepared and injected.
Use Terbutaline (Cherrymint) only as directed. Do not use more of it and do not use it more often than your doctor ordered. To do so may increase the chance of side effects.
If you are using Terbutaline (Cherrymint) for asthma, you should use another medicine that works faster for an asthma attack that has already started. If you do not have another medicine to use for an acute attack or if you have any questions about this, check with your doctor.
Dosing
The dose of Terbutaline (Cherrymint) 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 Terbutaline (Cherrymint). 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 injection dosage form:
- For prevention of bronchospasm:
- Adults and teenagers—0.25 milligrams (mg) injected under your skin. Your doctor may increase your dose as needed. However, the dose is usually not more than 0.5 mg within 4 hours.
- Children younger than 12 years of age—Use is not recommended.
- For prevention of bronchospasm:
Missed Dose
If you miss a dose of Terbutaline (Cherrymint), 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 unopened vials of Terbutaline (Cherrymint) at room temperature, away from heat and direct light. Do not freeze. An open vial of medicine must be used right away.
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.
Throw away used needles in a hard, closed container that the needles cannot poke through. Keep this container away from children and pets.
Terbutaline (Cherrymint) administration
IV: Use infusion pump.
Oral: Administer around-the-clock to promote less variation in peak and trough serum levels
Inhalation: Terbutaline (Cherrymint) Turbuhaler [Canadian product]: After removing lid, patient should hold inhaler upright and turn blue grip as far as it will go in one direction then turn it back to original position. Clicking sound indicates that inhaler is ready for use. Patient should exhale fully but not into the inhaler and then place mouthpiece gently between teeth, close lips around inhaler and inhale deeply. Inhaler should be removed from mouth prior to exhaling. Instruct patients to rinse mouth with water after each inhalation as some medication may stick to the inside of the mouth and throat. If inhaler is dropped or shaken, or if patient exhales into the inhaler after a dose is loaded, the dose will be lost and a new dose should be loaded and inhaled. Outside of mouthpiece should be cleaned once weekly with a dry tissue. Instruct patient to keep inhaler dry. First appearance of red mark in dose indicator (window underneath mouthpiece) indicates that 20 doses remain. When red mark reaches bottom of dose indicator no doses remain and Turbuhaler should be discarded.
SubQ: Extravasation management, sympathomimetic vasopressors (off-label use): Stop vesicant infusion immediately and disconnect IV line (leave needle/cannula in place); gently aspirate extravasated solution from the IV line (do NOT flush the line); remove needle/cannula; elevate extremity. Infiltrate extravasation area with Terbutaline (Cherrymint) solution 1 mg diluted with 10 mL (large extravasation site) or 1 mg diluted in 1 mL (small/distal extravasation site) of 0.9% sodium chloride into extravasation site (Stier 1999).
Terbutaline (Cherrymint) pharmacology
In vitro and in vivo pharmacologic studies have demonstrated that Terbutaline (Cherrymint) 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 (Cherrymint) 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 (Cherrymint) sulfate.
The pharmacologic effects of beta-adrenergic agonists, including Terbutaline (Cherrymint), 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 (Cherrymint) 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 (Cherrymint) 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 (Cherrymint) 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 (Cherrymint) 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 (Cherrymint) sulfate tablets or 5 mg Terbutaline (Cherrymint) sulfate in solution in 17 healthy, adult, male subjects, resulted in mean (SD) peak plasma Terbutaline (Cherrymint) 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 (Cherrymint), 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 (Cherrymint) was approximately 3.4 hours.
In comparison to oral dosing, subcutaneous administration of 0.5 mg of Terbutaline (Cherrymint) sulfate to 17 healthy, adult, male subjects resulted in a mean (SD) peak plasma Terbutaline (Cherrymint) 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 (Cherrymint), 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 (Cherrymint).
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).
- DailyMed. "GUAIFENESIN; HYDROCODONE BITARTRATE: 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).
Reviews
The results of a survey conducted on ndrugs.com for Cherrymint are given in detail below. The results of the survey conducted are based on the impressions and views of the website users and consumers taking Cherrymint. We implore you to kindly base your medical condition or therapeutic choices on the result or test conducted by a physician or licensed medical practitioners.User reports
1 consumer reported administration
When best can I take Cherrymint, on an empty stomach, before or after food?ndrugs.com website users have also released a report stating that Cherrymint should be taken After food. In any case, this may not be the right description on how you ought to take this Cherrymint. Kindly visit your doctor for more medical advice in this regard. Click here to see other users view on when best the Cherrymint can be taken.
Users | % | ||
---|---|---|---|
After food | 1 | 100.0% |
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Information checked by Dr. Sachin Kumar, MD Pharmacology