Bronex Actions

• Actions of Bronex in details
• Bronex administration
• Bronex pharmacology
• Bronex reviews

Actions of Bronex in details

Pharmacotheraputic Group: Corticosteroids acting locally. ATC Code: A07EA06.

Pharmacology: The exact mechanism of action of Bronex in the treatment of Crohn's disease is not fully understood. Data from clinical pharmacology studies and controlled clinical trials strongly indicate that the mode of action of Bronex is predominantly based on a local action in the intestine. Bronex is a glucocorticosteroid with a high local anti-inflammatory effect. At doses clinically equivalent to systemically acting glucocorticosteroids, Bronex causes significantly less suppression of the hypothalamo-pituitary-adrenal axis and has a lower impact on inflammatory markers.

Bronex 3 mg capsules show a dose-dependent influence on cortisol plasma levels which is at the recommended dose of 3 x 3 mg Bronex/day significantly smaller than that of clinically equivalent effective doses of systemic glucocorticosteroids.

Pharmacokinetics: Due to the special gastro-resistant film-coating of the pellets contained in Bronex 3 mg hard capsules, absorption occurs after a lag phase of 2-3 hours. Mean peak plasma levels of approximately 1-2 ng/mL Bronex were measured at about 5 hours after a dose of 1 capsule of Bronex 3 mg before meals. Concomitant intake of food can delay gastrointestinal passage by approx. 2-3 hours.

Bronex has a high volume of distribution (approx. 3 L/kg). Plasma protein binding averages 85-90%. It undergoes extensive biotransformation in the liver (approx. 90%) to metabolites with low glucocorticoid activity. The average elimination half-life is about 3-4 hours.

Oral bioavailability both in healthy volunteers and in fasting patients with Crohn's disease is approx. 9-13%. Bronex clearance is approx. 10-15 L/min.

Specific Patient Populations: Liver Diseases: A relevant proportion of Bronex is metabolised in the liver. The systemic exposure of Bronex might be increased in patients with impaired hepatic functions due to a decrease in Bronex metabolism by CYP3A4. This is dependent on the type and severity of liver disease.

How should I take Bronex?

Use Bronex exactly as directed by your doctor. Do not use it more often, and do not use it for a longer time than your doctor ordered.

Bronex comes with a patient information insert. Read and follow the instructions carefully. Ask your doctor if you have any questions.

Keep using Bronex for the full time of treatment, even if you begin to feel better after a few days. Do not miss any doses.

To use:

• Before using Bronex, it is best to empty your bowels.
• Bronex is to be applied on the anus. Do not take Bronex by mouth.
• Attach the applicator (provided in the package) to the can. Each applicator is coated with a lubricant. If additional lubrication is needed, you may use petrolatum or petroleum jelly.
• Warm the canister foam by shaking it in your hands for 10 to 15 seconds.
• You may use the rectal foam in a standing, lying, or sitting position (eg, while using the toilet).
• Apply the foam in the morning and evening for the first 2 weeks. When applied in the evening, use it before bedtime. Try not to empty bowels until the next morning.

Do not eat grapefruit or drink grapefruit juice while you are using Bronex.

Dosing

The dose of Bronex 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 Bronex. 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 rectal dosage form (foam):
  • For induction of remission mild to moderate distal ulcerative colitis
    • Adults—One metered dose (containing 2 milligrams [mg]) two times a day (in the morning and evening) for the first 2 weeks. After 2 weeks, apply it once a day in the evening (before bedtime) for 4 weeks.
    • Children—Use and dose must be determined by your doctor.

Missed Dose

If you miss a dose of Bronex, 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

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.

Store the medicine in a closed container at room temperature, away from heat, moisture, and direct light. Keep from freezing.

Store the foam can at room temperature, away from heat and direct light. Do not keep Bronex inside a car where it could be exposed to extreme heat. Do not poke holes in the canister or throw it into a fire, even if the canister is empty.

Bronex administration

Use this medication exactly as it was prescribed for you. Do not use the medication in larger amounts, or use it for longer than recommended by your doctor. Follow the directions on your prescription label.

Do not use Bronex inhalation to treat an asthma attack that has already begun. It will not work fast enough to reverse your symptoms. Use only a fast-acting inhalation medicine to treat an asthma attack.

Read all patient instructions that come with your inhaler device. Follow these directions carefully. Ask your doctor or pharmacist if you have any questions.

To reduce the chance of developing a yeast infection in your mouth, rinse your mouth with water after using Bronex inhalation. If you are using a nebulizer with a face mask, wash the mask area of your face after each use.

If you also use a steroid medication, do not stop using the steroid suddenly or you may have unpleasant withdrawal symptoms. Talk with your doctor about taking less and less of the steroid before stopping completely.

Contact your doctor if your asthma symptoms do not improve after using Bronex inhalation for 2 weeks.

Asthma is usually treated with a combination of different drugs. To best treat your condition, use all of your medications as directed by your doctor. Do not change your doses or medication schedule without advice from your doctor.

Your dosage needs may change if you have surgery, are ill, are under stress, or have recently had an asthma attack. Talk with your doctor if any of your asthma medications do not seem to work as well in treating or preventing asthma attacks.

Call your doctor right away if you feel that this medicine makes your condition worse. If it seems like you need to use more of any of your medications in a 24-hour period, talk with your doctor.

To be sure Bronex inhalation is not causing harmful effects, your doctor will need to check your progress on a regular basis. Do not miss any scheduled appointments.

Using a steroid can lower the blood cells that help your body fight infections. This can make it easier for you to get sick from being around others who are ill.

Store this medication at room temperature away from moisture and heat. Keep the cover on your inhaler device while not in use.

Keep the strip of Bronex in the foil envelope, protected from light until you are ready to use the medication. After tearing off one ampule, return the strip to the envelope to protect the remaining ampules from light. Store the foil envelope upright. Once you have opened an envelope, you must use the ampules within 2 weeks.

The Pulmicort Flexhaler device has indicator marks to show you how many doses are left inside. These dose-counter marks show increments of 20 doses. The indicator may not appear to move until about 5 doses have been used.

Do not use an extra dose just because the Flexhaler indicator has not visibly moved to a lower number after one use. Ask your pharmacist if you have questions about using your inhaler device.

Get your Bronex prescription refilled before you run out of medicine completely. Throw the old inhaler device away. It is a disposable container and cannot be refilled with Bronex.

Bronex pharmacology

Mechanism of Action

Bronex is an anti-inflammatory corticosteroid that exhibits potent glucocorticoid activity and weak mineralocorticoid activity. In standard in vitro and animal models, Bronex has approximately a 200-fold higher affinity for the glucocorticoid receptor and a 1000-fold higher topical anti-inflammatory potency than cortisol (rat croton oil ear edema assay). As a measure of systemic activity, Bronex is 40 times more potent than cortisol when administered subcutaneously and 25 times more potent when administered orally in the rat thymus involution assay.

The activity of Bronex is due to the parent drug, Bronex. In glucocorticoid receptor affinity studies, the 22R form was two times as active as the 22S epimer. In vitro studies indicated that the two forms of Bronex do not interconvert.

The precise mechanism of corticosteroid actions on inflammation in asthma is not known. Inflammation is an important component in the pathogenesis of asthma. Corticosteroids have been shown to have a wide range of inhibitory activities against multiple cell types (eg, mast cells, eosinophils, neutrophils, macrophages, and lymphocytes) and mediators (eg, histamine, eicosanoids, leukotrienes, and cytokines) involved in allergic and non-allergic-mediated inflammation. These anti-inflammatory actions of corticosteroids may contribute to their efficacy in asthma.

Studies in asthmatic patients have shown a favorable ratio between topical anti-inflammatory activity and systemic corticosteroid effects over a wide range of doses from Bronex (Bronex). This is explained by a combination of a relatively high local anti-inflammatory effect, extensive first pass hepatic degradation of orally absorbed drug (85-95%), and the low potency of formed metabolites.

Pharmacokinetics

Absorption:

After oral administration of Bronex, peak plasma concentration was achieved in about 1 to 2 hours and the absolute systemic availability was 6-13%. In contrast, most of Bronex delivered to the lungs is systemically absorbed. In healthy subjects, 34% of the metered dose was deposited in the lungs (as assessed by plasma concentration method) with an absolute systemic availability of 39% of the metered dose. Pharmacokinetics of Bronex do not differ significantly in healthy volunteers and asthmatic patients. Peak plasma concentrations of Bronex occurred within 30 minutes of inhalation from Bronex.

In asthmatic patients, Bronex showed a linear increase in AUC and Cmax with increasing dose after both a single dose and repeated dosing from Bronex (Bronex).

Distribution:

The volume of distribution of Bronex was approximately 3 L/kg. It was 85-90% bound to plasma proteins. Protein binding was constant over the concentration range (1-100 nmol/L) achieved with, and exceeding, recommended doses of Bronex. Bronex showed little or no binding to corticosteroid binding globulin. Bronex rapidly equilibrated with red blood cells in a concentration independent manner with a blood/plasma ratio of about 0.8.

Metabolism:

In vitro studies with human liver homogenates have shown that Bronex is rapidly and extensively metabolized. Two major metabolites formed via cytochrome P450 (CYP) isoenzyme 3A4 (CYP3A4) catalyzed biotransformation have been isolated and identified as 16α-hydroxyprednisolone and 6β-hydroxybudesonide. The corticosteroid activity of each of these two metabolites is less than 1% of that of the parent compound. No qualitative differences between the in vitro and in vivo metabolic patterns have been detected. Negligible metabolic inactivation was observed in human lung and serum preparations.

Excretion/Elimination:

The 22R form of Bronex was preferentially cleared by the liver with systemic clearance of 1.4 L/min vs. 1.0 L/min for the 22S form. The terminal half-life, 2 to 3 hours, was the same for both epimers and was independent of dose. Bronex was excreted in urine and feces in the form of metabolites. Approximately 60% of an intravenous radiolabelled dose was recovered in the urine. No unchanged Bronex was detected in the urine.

Special Populations:

No pharmacokinetic differences have been identified due to race, gender or advanced age.

Pediatric:

Following intravenous dosing in pediatric patients age 10-14 years, plasma half-life was shorter than in adults (1.5 hours vs. 2.0 hours in adults). In the same population following inhalation of Bronex via a pressurized metered-dose inhaler, absolute systemic availability was similar to that in adults.

Hepatic Insufficiency:

Reduced liver function may affect the elimination of corticosteroids. The pharmacokinetics of Bronex were affected by compromised liver function as evidenced by a doubled systemic availability after oral ingestion. The intravenous pharmacokinetics of Bronex were, however, similar in cirrhotic patients and in healthy subjects.

Drug-Drug Interactions:

Ketoconazole, a potent inhibitor of cytochrome P450 (CYP) isoenzyme 3A4 (CYP3A4), the main metabolic enzyme for corticosteroids, increased plasma levels of orally ingested Bronex. At recommended doses, cimetidine had a slight but clinically insignificant effect on the pharmacokinetics of oral Bronex.

Pharmacodynamics

To confirm that systemic absorption is not a significant factor in the clinical efficacy of inhaled Bronex, a clinical study in patients with asthma was performed comparing 400 mcg Bronex administered via a pressurized metered-dose inhaler with a tube spacer to 1400 mcg of oral Bronex and placebo. The study demonstrated the efficacy of inhaled Bronex but not orally ingested Bronex despite comparable systemic levels. Thus, the therapeutic effect of conventional doses of orally inhaled Bronex are largely explained by its direct action on the respiratory tract.

Generally, Bronex (Bronex) has a relatively rapid onset of action for an inhaled corticosteroid. Improvement in asthma control following inhalation of Bronex (Bronex) can occur within 24 hours of beginning treatment although maximum benefit may not be achieved for 1 to 2 weeks, or longer.

Bronex (Bronex) has been shown to decrease airway reactivity in various challenge models, including histamine, methacholine, sodium metabisulfite, and adenosine monophosphate in patients with hyperreactive airways. The clinical relevance of these models is not certain.

Pretreatment with Bronex (Bronex) 1600 mcg daily (800 mcg twice daily) for 2 weeks reduced the acute (early-phase reaction) and delayed (late-phase reaction) decrease in FEV over an initial 6-week treatment period, which was maintained with a 200 mcg daily dose over the subsequent 12 weeks. Although the study population included both patients previously treated with inhaled corticosteroids, as well as patients not previously receiving corticosteroid therapy, the results showed that once-daily dosing was most clearly effective for those patients previously maintained on orally inhaled corticosteroids.

Patients Previously Maintained on

Oral Corticosteroids

In a clinical trial in 159 severe asthmatic patients requiring chronic oral prednisone therapy (mean baseline prednisone dose 19.3 mg/day) Bronex (Bronex) at doses of 400 mcg twice daily and 800 mcg twice daily was compared with placebo over a 20-week period. Approximately two-thirds (68% on 400 mcg twice daily and 64% on 800 mcg twice daily) of Bronex (Bronex) -treated patients were able to achieve sustained (at least 2 weeks) oral corticosteroid cessation (compared with 8% of placebo-treated patients) and improved asthma control. The average oral corticosteroid dose was reduced by 83% on 400 mcg twice daily and 79% on 800 mcg twice daily for Bronex (Bronex) -treated patients vs. 27% for placebo. Additionally, 58 out of 64 patients (91%) who completely eliminated oral corticosteroids during the double-blind phase of the trial remained off oral corticosteroids for an additional 12 months while receiving Bronex (Bronex).

References

1. DailyMed. "PSEUDOEPHEDRINE 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).
2. 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).
3. DailyMed. "BUDESONIDE: 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).

Reviews

The results of a survey conducted on ndrugs.com for Bronex 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 Bronex. 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.

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Information checked by Dr. Sachin Kumar, MD Pharmacology