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Description
Bambuterol is a long-acting beta-adrenoceptor agonist used in the treatment of asthma. It is a prodrug of terbutaline. Bambuterol is a carbamate ester that is terbutaline in which both of the phenolic hydroxy groups have been protected as the corresponding N,N-dimethylcarbamates. A long-acting beta-adrenoceptor agonist used in the treatment of asthma; it is a prodrug for terbutaline. It has a role as a beta-adrenergic agonist, a prodrug, a bronchodilator agent, an anti-asthmatic drug, an EC 3.1.1.7 (acetylcholinesterase) inhibitor, a sympathomimetic agent and a tocolytic agent. It is a carbamate ester and a member of phenylethanolamines. It is functionally related to a terbutaline.
Properties and Characteristics of Bambuterol
| Drug class | Long-Acting Beta 2 Adrenergic Receptor Agonist, Anti-Asthmatic Drugs |
| Brand Names | Bamberol, Betaday, Buterol, Aerodyl, Baburol, Bambec, Bamberol, Bambudil, Bambutol, Betaday, Buterol, Dilator, Muterol, Oxeol Paranova, Oxéol |
| Synonyms | Bambuterol, 81732-65-2, Bambec, Bambuterolum, Bambuterolum [Latin], Oxeol, Bambuterol [BAN:INN], Bambuterol (INN), terbutaline bisdimethylcarbamate, CHEBI:553827 |
| Molecular Formula | C18H29N3O5 |
| Molecular Weight | 367.4 g/mol |
| IUPAC Names | [3-[2-(tert-butylamino)-1-hydroxyethyl]-5-(dimethylcarbamoyloxy)phenyl] N,N-dimethylcarbamate |
| Structural formula of main components |  |
| Pure active ingredient | Terbutaline |
| Appearance | off-white |
| Melting Point | 222-224°C |
| Solubility | 4.69e-01 g/L |
| Excretion | Bambuterol and its metabolites are mainly excreted via the kidneys as urine |
| Available as | Tablets and Syrups |
| Storage | Store at 4° C |
| Prescription | Prescription is required |
Bambuterol Benefits & Uses
Bambuterol is used to treat the following:
- Asthma
- COPD and other airways-related problems
What are the side effects of Bambuterol?
A patient can suffer from the following side effects:
- Nausea
- Vomiting
- Skin Rash
- Flu-Like Symptoms
- Diarrhoea
- Sleeplessness
- Headache
- Palpitations
- Muscle Cramps
Mechanism of action
The pharmacologic effects of bambuterol are at least in part attributable to stimulation through beta-adrenergic receptors (beta 2 receptors) of intracellular adenyl cyclase, the enzyme that catalyzes the conversion of adenosine triphosphate (ATP) to cyclic AMP. Increased cyclic AMP levels are associated with relaxation of bronchial smooth muscle and inhibition of release of mediators of immediate hypersensitivity from cells, especially from mast cells.
Dosage of Bambuterol
Adults:
Initial dose: 10mg to 20mg once daily at bedtime.
The 10mg dose may be increased if necessary to 20mg after 1 to 2 weeks.
In patients who have previously tolerated beta-2 agonists well, the recommended starting dose, as well as maintenance dose, is 20mg.
Patients with Renal Impairment:
In patients with moderate to severely impaired renal function (GFR < 50 ml/min), it is recommended that the starting dose of bambuterol should be halved. Further doses should be adjusted according to response.
Overdose symptoms
Symptoms: Headache, anxiety, tremor, nausea, tonic muscle cramps, palpitations, tachycardia and cardiac arrhythmias. Management: Consider gastric lavage and activated charcoal in severe cases. Determine acid-base balance, blood glucose and electrolytes. Monitor BP, heart rate and rhythm.
For haemodynamically significant cardiac arrhythmias, the preferred antidote is a cardioselective β-blocker, but should be used with caution in patients with history of bronchospasm. Admin a vol expander when the β2-mediated reduction in peripheral vascular resistance significantly contributes to the fall in BP.
Warnings
Warnings for special population
Pregnancy: This medicine is not recommended for use in pregnant women unless absolutely necessary. All the possible risks and benefits should be discussed with the doctor before using this medicine.
Breast-feeding: This medicine is not recommended for use in breastfeeding women unless necessary. All the risks and benefits should be discussed with the doctor before using this medicine. If the medicine is used, the infant should be monitored closely for any undesirable side effects.
General warnings
Use in pediatrics: This medicine should be used with extreme caution in children and only under the supervision of a healthcare professional. It is not recommended for use in patients less than 2 years of age.
Seizure disorder: This medicine should be used with caution in patients with a known history of seizure disorder due to the increased risk of recurrent seizures. Report any unusual symptoms to the doctor immediately. Appropriate dose adjustments or replacement with a suitable alternative may be required based on the clinical condition.
Glaucoma: This medicine should be used with caution in patients with pre-existing glaucoma due to the increased risk of worsening of the patient’s condition. Appropriate patient education, dose adjustments, or replacement with a suitable alternative may be required based on the clinical condition.
Heart diseases: This medicine should be used with caution in patients with pre-existing heart diseases due to the increased risk of worsening of the patient’s condition. Close monitoring of heart function, vital signs, or electrolyte levels may be necessary based on the clinical condition. Appropriate dose adjustments or replacement with a suitable alternative may be required in some cases based on the clinical condition.
Hyperthyroidism: This medicine should be used with caution in patients with pre-existing hyperthyroidism due to the increased risk of worsening of the patient’s condition. Close monitoring of thyroid hormone levels, appropriate dose adjustments, or replacement with a suitable alternative may be required based on the clinical condition.
Driving and operating machinery: This medicine may cause symptoms such as drowsiness, dizziness, a shakiness of arms and legs, muscle stiffness, etc. in some patients. It is advised that you do not perform any activities such as driving a vehicle or operating machinery if you experience any of these symptoms during treatment with this medicine.
Other medicines: This medicine may interact with many other medicines and may cause severe adverse effects. Hence, it is advised that you report all your current medicines, including any herbs and supplements, to the doctor before beginning treatment with this medicine.