Terbutaline

Terbutaline Uses, Dosage, Side Effects, Food Interaction and all others data.

Terbutaline 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. Terbutaline 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.

Terbutaline 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 Terbutaline
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
Weight 1mg/ml, 2.5mg, 5mg
Type Oral, Subcutaneous, Tablet, Injectable Solution, Oral Tablet, Oral/injection
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 United States
Last Updated: September 19, 2023 at 7:00 am
Terbutaline
Terbutaline

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.

Terbutaline 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 Terbutaline works

Terbutaline 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

Terbutaline 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. Terbutaline is excreted into breast milk. Consult with your doctor before breast-feeding. Terbutaline 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.

Terbutaline 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.

Terbutaline Disease Interaction

Moderate: cardiovascular, diabetes, hypokalemia, seizures

Volume of Distribution

Terbutaline 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, Terbutaline should only be administered with caution during the first trimester of pregnancy. Terbutaline is secreted via breast milk, but effect on the infant is unlikely at therapeutic doses.

Contraindication

Do not use Terbutaline if

  • You are allergic to any ingredient in Terbutaline or to a sympathomimetic amine (eg, epinephrine, albuterol).
  • You need to treat prolonged (more than 48 to 72 hours) premature labor.

Special Warning

Terbutaline 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 Terbutaline

FAQ

What is Terbutaline used for?

Terbutaline is used to prevent and treat wheezing, shortness of breath, and chest tightness caused by asthma, chronic bronchitis, and emphysema. Terbutaline is in a class of medications called beta agonists. It works by relaxing and opening the airways, making it easier to breathe.

Does Terbutaline work well?

Terbutaline works well by relaxing and opening the airways, making it easier to breathe.

What are the common side effects of Terbutaline?

the common side effects of Terbutaline 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 Terbutaline safe during pregnancy?

Terbutaline 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. Terbutaline has caused serious side effects, including death, in pregnant women who took the medication for this purpose.

What are the common side effects of Terbutaline ?

Terbutaline use of inhaled bronchodilators is acceptable during breastfeeding because of the low bioavailability and maternal serum levels after use.Terbutaline use as a tocolytic agent might decrease the duration of breastfeeding.

Can I drive after taking Terbutaline?

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 Terbutaline stay in my system?

Terbutaline excreted in the urine at 96 hours after subcutaneous administration.

How quickly should Terbutaline work?

Terbutaline need 12 to 72 hours to begin to work. Using Terbutaline delays delivery for several days (at least) and allows time for work.

Does Terbutaline make me tired?

Terbutaline 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 Terbutaline be used?

Terbutaline comes as a tablet to take by mouth. The tablets are usually taken three times a day, once every six hours.

Can Terbutaline cause chest pain?

Terbutaline may cause chest pain also common adverse effects include with palpitations, rapid heart rate, tremor or nervousness.

Does Terbutaline cause hypertension?

Terbutaline may increase your heart rate and blood pressure.

Can I take Terbutaline long time?

Oral Terbutaline should no longer be taken. Long term (more than 72 hours) of Terbutaline is no longer recommended.

Can my overdose on Terbutaline?

Overdose symptoms may include chest pain, fast or irregular heartbeats, trouble sleeping, tiredness, a seizure, or fainting.

Does Terbutaline make I shake?

The most common side-effect of Terbutaline is feeling shaky.

How long does it take for oral Terbutaline to work?

Your child should begin to breathe easier within 5 to 10 minutes after taking Terbutaline.

Does Terbutaline cause hypokalemia?

Terbutaline 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 Terbutaline?

Terbutaline usually taken three times a day, once every six hours.

How is Terbutaline eliminated from the body?

Terbutaline is extensively metabolized to the glucuronic acid conjugate which is eliminated via bile and urine .

What happens when I stop taking Terbutaline?

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.

http://classyfire.wishartlab.com/tax_nodes/C0000000
http://classyfire.wishartlab.com/tax_nodes/C0002448
http://classyfire.wishartlab.com/tax_nodes/C0000134
http://classyfire.wishartlab.com/tax_nodes/C0001286
http://classyfire.wishartlab.com/tax_nodes/C0000137
http://classyfire.wishartlab.com/tax_nodes/C0003899
http://classyfire.wishartlab.com/tax_nodes/C0004647
http://classyfire.wishartlab.com/tax_nodes/C0004646
http://classyfire.wishartlab.com/tax_nodes/C0002279
http://classyfire.wishartlab.com/tax_nodes/C0001661
http://classyfire.wishartlab.com/tax_nodes/C0001897
http://classyfire.wishartlab.com/tax_nodes/C0002228
http://classyfire.wishartlab.com/tax_nodes/C0004557
http://classyfire.wishartlab.com/tax_nodes/C0004150
http://classyfire.wishartlab.com/tax_nodes/C0003073
https://www.ebi.ac.uk/chebi/searchId.do?chebiId=CHEBI:9449
http://www.hmdb.ca/metabolites/HMDB0015009
http://www.genome.jp/dbget-bin/www_bget?cpd:C07129
https://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=5403
https://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46506887
https://www.chemspider.com/Chemical-Structure.5210.html
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=25770
https://mor.nlm.nih.gov/RxNav/search?searchBy=RXCUI&searchTerm=10368
https://www.ebi.ac.uk/chebi/searchId.do?chebiId=9449
https://www.ebi.ac.uk/chembldb/index.php/compound/inspect/CHEMBL1760
http://bidd.nus.edu.sg/group/cjttd/ZFTTDDRUG.asp?ID=DAP000246
http://www.pharmgkb.org/drug/PA451616
http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=560
http://www.rxlist.com/cgi/generic3/terbutaline.htm
https://www.drugs.com/cdi/terbutaline.html
https://en.wikipedia.org/wiki/Terbutaline
*** Taking medicines without doctor's advice can cause long-term problems.
Share