ISOBUTALINE
ISOBUTALINE Uses, Dosage, Side Effects, Food Interaction and all others data.
ISOBUTALINE is a relatively selective β2-adrenergic bronchodilator that has little or no effect on alpha-adrenergic receptors. The drug has exerts a preferential effect on β2-adrenergic receptors but stimulates beta-adrenergic receptors less selectively than relatively selective β2-agonists. ISOBUTALINE appears to have a greater stimulating effect on beta-receptors of the bronchial, vascular, and uterine smooth muscles (β2 receptors) than on the beta-receptors of the heart (β1 receptors). This drug relaxes smooth muscle and inhibits uterine contractions, but may also cause some cardiostimulatory effects and CNS stimulation.
The pharmacologic effects of terbutaline are at least in part attributable to stimulation through beta-adrenergic receptors of intracellular adenyl cyclase, the enzyme that catalyzes the conversion of adenosine triphosphate (ATP) to cyclic- 3',5'- adenosine monophosphate (c-AMP). Increased c-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.
ISOBUTALINE is a beta-2 adrenergic receptor agonist indicated to treat reversibly bronchospasm in asthmatic patients with bronchitis and emphysema. It has a short duration as the inhaled form is taken up to three times daily, and the therapeutic window is wide.
| Trade Name | ISOBUTALINE |
| Availability | Prescription only |
| Generic | Terbutaline |
| Terbutaline Other Names | Terbutalin, Terbutalina, Terbutaline, Terbutalinum |
| Related Drugs | Dupixent, Xolair, ProAir Digihaler, albuterol, dexamethasone, methylprednisolone, nifedipine, Symbicort, Breo Ellipta, Ventolin |
| Type | |
| Formula | C12H19NO3 |
| Weight | Average: 225.2842 Monoisotopic: 225.136493479 |
| Protein binding | Terbutaline is not highly bound to protein in plasma. |
| Groups | Approved |
| Therapeutic Class | Short-acting selective β2-adrenoceptor stimulants |
| Manufacturer | |
| Available Country | |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Used to open up the airways in people with asthma, bronchitis and other breathing problems.Used to relieve trouble breathing upon exertion.For the prevention and reversal of bronchospasm in patients 12 years of age and older with reversible, obstructive airway disease.Symptomatic management of reversible bronchospasm associated with bronchitis and emphysema.
ISOBUTALINE is also used to associated treatment for these conditions: Asthma, Bronchospasm, Chronic Cough (CC), Chronic Obstructive Pulmonary Disease (COPD), Cough, Premature Labour, Productive cough, Airway secretion clearance therapy
How ISOBUTALINE works
ISOBUTALINE is a selective beta-2 adrenergic receptor agonist. Agonism of these receptors in bronchioles activates adenylyl cyclase, increasing intracellular cyclic adenosine monophosphate (cAMP). Increased cAMP decreases intracellular calcium, activating protein kinase A, inactivating myosin light-chain kinase, activating myosin light-chain phosphatase, and finally relaxing smooth muscle in the bronchiole.
Dosage
ISOBUTALINE dosage
The recommended adult dose for treating asthma, emphysema or bronchitis is 2.5-5 mg 3 times daily approximately 6 hours apart while awake. The maximum dosage is 15 mg/day. Shake the inhaler several times and uncap the mouthpiece. Breathe out fully. For best results, hold the inhaler 1 to 2 inches in front of your open mouth or attach a spacer to the inhaler and place the spacer in your mouth, above your tongue and past your teeth. Take a deep, slow breath as you push down on the canister. Hold your breath for 10 seconds, then exhale slowly. Use nebulizer machine for better response.
Side Effects
Dry mouth, irritated throat, nausea, dizziness, headache, heartburn, loss of appetite, altered taste sensation, restlessness, anxiety, nervousness, trembling, and sweating may occur but should subside as your body adjusts to the medication.
Toxicity
Patients experiencing an overdose may present with abdominal pain, agitation, palpitations, seizures, angina, hypertension, hypotension, tachycardia, arrhythmias, nervousness, headache, tremor, dry mouth, nausea, dizziness, fatigue, malaise, insomnia. Discontinue treatment with terbutaline and initiate symptomatic and supportive therapy.
Precaution
Before you use this drug, tell your doctor if you have: any allergies, heart disease, high blood pressure, an overactive thyroid gland, seizures, diabetes. Tell your doctor if you ever had a bad reaction to albuterol, bitolterol, ephedrine, epinephrine, isoetharine, isoproterenol, metaproterenol, pseudoephedrine, or pirbuterol or other similar agents. Tell your doctor if you are pregnant before using this medication. ISOBUTALINE is excreted into breast milk. Consult with your doctor before breast-feeding. ISOBUTALINE is not recommended for children under the age of 6. Caution is advised in the elderly.
Interaction
Tell your doctor of all nonprescription and prescription medications you take, including: beta-blockers (e.g., propranolol, timolol), all asthma drugs, antidepressants, MAO inhibitors (e.g., furazolidone, linezolid, phenelzine, selegiline, tranylcypromine), diuretics (e.g., hydrochlorothiazide). Many nonprescription medications contain pseudoephedrine or ephedrine, so check the labels carefully. Do not take any of these medications without consulting your doctor. Do not start or stop any medicine without doctor or pharmacist approval.
Food Interaction
No interactions found.ISOBUTALINE Hypertension interaction
[Moderate] Adrenergic bronchodilators can stimulate cardiovascular beta- 1 and beta- 2 receptors, resulting in adverse effects such as tachycardia, palpitation, peripheral vasodilation, blood pressure changes, and ECG changes (e.g., flattening of the T wave; prolongation of the QT interval; ST segment depression).
Direct stimulation of cardiac tissues is mediated by beta- 1 receptors and thus less likely to occur with beta-2-selective agents such as albuterol.
However, beta-2-selectivity is not absolute and can be lost with larger doses.
High dosages of these agents have been associated with precipitation or aggravation of angina, myocardial ischemia, and cardiac arrhythmias.
Therapy with adrenergic bronchodilators should be administered cautiously in patients with sensitivity to sympathomimetic amines, hyperthyroidism, and The recommended dosages should not be exceeded.
ISOBUTALINE Drug Interaction
Moderate: epinephrine, furosemide, promethazine, oxytocin, budesonide / formoterolUnknown: aspirin, diphenhydramine, misoprostol, carboprost, ipratropium, methylergonovine, naloxone, acetaminophen, metoclopramide, rho , tiotropium, cyanocobalamin, ascorbic acid, cholecalciferol, phytonadione
ISOBUTALINE Disease Interaction
Volume of Distribution
ISOBUTALINE has a mean volume of distribution of 1.6 L/kg.
Elimination Route
A 0.5 mg subcutaneous dose of terbutaline reaches a mean Cmax of 9.6 ± ng/mL, with a median Tmax of 0.5 hours, and a mean AUC of 29.4 ± 14.2 h*ng/mL. A 5 mg oral terbutaline tablet reaches a mean Cmax of 8.3 ± 3.9 ng/mL with a median Tmax of 2 hours, and a mean AUC of 54.6 ± 26.8 h*ng/mL. A 5 mg oral terbutaline solution reaches a mean Cmax of 8.6 ± 3.6 ng/mL, with a median Tmax of 1.5 hours, and a mean AUC of 53.1 ± 23.5 h*ng/mL.
Oral terbutaline has an oral bioavailability of 14-15%.
Half Life
An oral dose of terbutaline has an elimination half life of 3.4 hours, while a subcutaneous dose has an elimination half life of 2.9 hours.
Clearance
The average clearance of terbutaline is 3.0 mL/min/kg.
Elimination Route
An oral dose of terbutaline is 40% eliminated in the urine after 72 hours. The major metabolite in the urine was the sulphate conjugated form of terbutaline. Parenteral doses of terbutaline are 90% eliminated in the urine, with approximately 2/3 as the unchanged parent drug. Less than 1% of a dose of terbutaline is eliminated in the feces.
Pregnancy & Breastfeeding use
Although no teratogenic effects have been observed in animals or in patients, ISOBUTALINE should only be administered with caution during the first trimester of pregnancy. ISOBUTALINE is secreted via breast milk, but effect on the infant is unlikely at therapeutic doses.
Contraindication
Do not use ISOBUTALINE if
- You are allergic to any ingredient in ISOBUTALINE or to a sympathomimetic amine (eg, epinephrine, albuterol).
- You need to treat prolonged (more than 48 to 72 hours) premature labor.
Special Warning
ISOBUTALINE is not approved for use by children younger than 6 years of age.
Storage Condition
Store at room temperature between 15 to 30° C. Keep away from moisture and sunlight. Do not puncture. Keep away from the reach of children.
Innovators Monograph
You find simplified version here ISOBUTALINE
FAQ
What is ISOBUTALINE used for?
ISOBUTALINE is used to prevent and treat wheezing, shortness of breath, and chest tightness caused by asthma, chronic bronchitis, and emphysema. ISOBUTALINE is in a class of medications called beta agonists. It works by relaxing and opening the airways, making it easier to breathe.
Does ISOBUTALINE work well?
ISOBUTALINE works well by relaxing and opening the airways, making it easier to breathe.
What are the common side effects of ISOBUTALINE?
the common side effects of ISOBUTALINE are include:
- uncontrollable shaking of a part of the body
- nervousness
- dizziness
- drowsiness
- difficulty falling asleep or staying asleep
- weakness
- headache
- nausea
- sweating
- dry mouth
Is ISOBUTALINE safe during pregnancy?
ISOBUTALINE injection should only be given to women who are in a hospital and should not be used to treat premature labor for longer than 48 to 72 hours. ISOBUTALINE has caused serious side effects, including death, in pregnant women who took the medication for this purpose.
What are the common side effects of ISOBUTALINE ?
ISOBUTALINE use of inhaled bronchodilators is acceptable during breastfeeding because of the low bioavailability and maternal serum levels after use.ISOBUTALINE use as a tocolytic agent might decrease the duration of breastfeeding.
Can I drive after taking ISOBUTALINE?
If you are taking high doses of this medicine, you should not drive or use machinery. If you are unsure, talk to your doctor.
How long does ISOBUTALINE stay in my system?
ISOBUTALINE excreted in the urine at 96 hours after subcutaneous administration.
How quickly should ISOBUTALINE work?
ISOBUTALINE need 12 to 72 hours to begin to work. Using ISOBUTALINE delays delivery for several days (at least) and allows time for work.
Does ISOBUTALINE make me tired?
ISOBUTALINE make you tired with include nervousness, shaking (tremor), dizziness, drowsiness or headache may occur.
What happens if I miss a dose?
Take the missed dose as soon as you remember it. However, if it is almost time for the next dose, skip the missed dose and continue your regular dosing schedule. Do not take a double dose to make up for a missed one.
How should ISOBUTALINE be used?
ISOBUTALINE comes as a tablet to take by mouth. The tablets are usually taken three times a day, once every six hours.
Can ISOBUTALINE cause chest pain?
ISOBUTALINE may cause chest pain also common adverse effects include with palpitations, rapid heart rate, tremor or nervousness.
Does ISOBUTALINE cause hypertension?
ISOBUTALINE may increase your heart rate and blood pressure.
Can I take ISOBUTALINE long time?
Oral ISOBUTALINE should no longer be taken. Long term (more than 72 hours) of ISOBUTALINE is no longer recommended.
Can my overdose on ISOBUTALINE?
Overdose symptoms may include chest pain, fast or irregular heartbeats, trouble sleeping, tiredness, a seizure, or fainting.
Does ISOBUTALINE make I shake?
The most common side-effect of ISOBUTALINE is feeling shaky.
How long does it take for oral ISOBUTALINE to work?
Your child should begin to breathe easier within 5 to 10 minutes after taking ISOBUTALINE.
Does ISOBUTALINE cause hypokalemia?
ISOBUTALINE induce profound hypokalemia by stimulating cellular potassium uptake and both drugs cause significant renal sodium and fluid retention and cardiac arrhythmias.
How many times can I get ISOBUTALINE?
ISOBUTALINE usually taken three times a day, once every six hours.
How is ISOBUTALINE eliminated from the body?
ISOBUTALINE is extensively metabolized to the glucuronic acid conjugate which is eliminated via bile and urine .
What happens when I stop taking ISOBUTALINE?
If you stop taking the drug suddenly or don’t take it at all: Your symptoms could get worse. This could lead to serious breathing problems.
