Xopenex

Generic name: levalbuterol inhalation
Brand names: Xopenex, Xopenex Concentrate, Xopenex HFA
Drug class: Adrenergic bronchodilators

Medically reviewed by  A Ras MD.

What is Xopenex?

Xopenex Inhalation Solution is an inhaled prescription medicine used for the treatment or prevention of bronchospasm in people 6 years of age and older.

Xopenex Inhalation Solution has not been shown to be safe and effective in children younger than 6 years of age.

Xopenex Inhalation Solution is supplied in 3 mL unit-dose vials in three different strengths of levalbulterol (0.31 mg, 0.63 mg, 1.25 mg). The vials do not require dilution before use.

Description

The active component of XOPENEX HFA inhalation aerosol is levalbuterol tartrate, the (R)-enantiomer of albuterol. Levalbuterol tartrate is a relatively selective beta2-adrenergic receptor agonist [see Clinical Pharmacology (12)]. Levalbuterol tartrate has the chemical name (R)-α1-[[(1,1-dimethylethyl)amino]methyl]-4-hydroxy-1,3-benzenedimethanol L-tartrate (2:1 salt), and it has the following chemical structure:

The molecular weight of levalbuterol tartrate is 628.71, and its empirical formula is (C13H21NO3)2 · C4H6O6. It is a white to light-yellow solid, freely soluble in water and very slightly soluble in ethanol.

Levalbuterol tartrate is the generic name for (R)-albuterol tartrate in the United States. XOPENEX HFA inhalation aerosol is a pressurized metered-dose aerosol inhaler (MDI) fitted with a dose indicator, which produces an aerosol for oral inhalation. It contains a suspension of micronized levalbuterol tartrate, propellant HFA-134a (1,1,1,2-tetrafluoroethane), Dehydrated Alcohol USP, and Oleic Acid NF.

After priming with 4 actuations, each actuation of the inhaler delivers 67.8 mcg of levalbuterol tartrate (equivalent to 51.6 mcg of levalbuterol free base) from the valve and 59 mcg of levalbuterol tartrate (equivalent to 45 mcg of levalbuterol free base) from the actuator mouthpiece. Each 15 g canister provides 200 actuations (or inhalations).

Mechanism of Action

Activation of beta2-adrenergic receptors on airway smooth muscle leads to the activation of adenylate cyclase and to an increase in the intracellular concentration of cyclic-3′, 5′-adenosine monophosphate (cyclic AMP). The increase in cyclic AMP is associated with the activation of protein kinase A, which in turn, inhibits the phosphorylation of myosin and lowers intracellular ionic calcium concentrations, resulting in muscle relaxation. Levalbuterol relaxes the smooth muscles of all airways, from the trachea to the terminal bronchioles. Increased cyclic AMP concentrations are also associated with the inhibition of the release of mediators from mast cells in the airways. Levalbuterol acts as a functional antagonist to relax the airway irrespective of the spasmogen involved, thus protecting against all bronchoconstrictor challenges. While it is recognized that beta2-adrenergic receptors are the predominant receptors on bronchial smooth muscle, data indicate that there are beta-receptors in the human heart, 10% to 50% of which are beta2-adrenergic receptors. The precise function of these receptors has not been established [see Warnings and Precautions (5)]. However, all beta-adrenergic agonist drugs can produce a significant cardiovascular effect in some patients, as measured by pulse rate, blood pressure, symptoms, and/or electrocardiographic changes.

What is the most important information I should know about Xopenex?

Xopenex Inhalation Solution is only for use with a nebulizer.

Who should not use Xopenex?

Do not use Xopenex Inhalation Solution if you are allergic to levalbuterol, racemic albuterol, or any of the ingredients in Xopenex. See the end of this guide for a complete list of ingredients in Xopenex Inhalation Solution.

What should I tell my healthcare provider before using Xopenex?

Before you use Xopenex Inhalation Solution, tell your doctor if you have:

• had an allergic reaction to levalbuterol or racemic albuterol
• heart problems
• high blood pressure
• seizures
• diabetes
• thyroid problems
• any other medical conditions
• are pregnant or planning to become pregnant. It is not known if Xopenex Inhalation Solution will harm your unborn baby. Talk to your doctor if you are pregnant or plan to become pregnant.
• are breastfeeding or plan to breastfeed. It is not known if Xopenex Inhalation Solution passes into your breast milk. You and your doctor should decide if you will use Xopenex Inhalation Solution or breastfeed. You should not do both.

Tell your doctor about all the medicines you take including prescription and over-the-counter medicines, vitamins, and herbal supplements. Xopenex Inhalation Solution may affect the way other medicines work, and other medicines may affect how Xopenex Inhalation Solution works.

Especially tell your doctor if you take:

• other asthma medicines
• heart medicines
• medicines that increase urination (diuretics)
• antidepressants
• medicine to treat chronic obstructive pulmonary disease (COPD)

Ask your doctor if you are not sure if any of your medicines are the kinds listed above.

Know the medicines you take. Keep a list of them and show it to your doctor and pharmacist when you get a new medicine.

How should I use Xopenex?

• See the instructions for use that comes with Xopenex
• Use Xopenex Inhalation Solution exactly as your doctor tells you to. Do not change your dose without talking to your doctor first.
• Your doctor will tell you how many times and when to use your Xopenex Inhalation Solution.
• An adult should help a child use Xopenex Inhalation Solution.
• Do not use your Xopenex Inhalation Solution more often than your doctor tells you to.
• Get medical help right away if Xopenex Inhalation Solution:
  • does not work as well for your asthma symptoms or
  • your asthma symptoms get worse or
  • you need to use your Xopenex Inhalation Solution more often than usual
• If you also use another medicine by inhalation, you should ask your doctor for instructions on when to use it while you are also using Xopenex Inhalation Solution.
• Do not mix Xopenex Inhalation Solution with other medicines in your nebulizer.
• Only use Xopenex Inhalation Solution if it is colorless. Throw away the Xopenex Inhalation Solution vial if the liquid medicine is not colorless.
• Do not use Xopenex Inhalation Solution after the expiration date on the vial.

What are the possible side effects of Xopenex?

Xopenex Inhalation Solution can cause serious side effects including:

• sudden shortness of breath (bronchospasm). Sudden shortness of breath can happen right away after using Xopenex Inhalation Solution.
• worsening asthma
• heart problems
• death. If you use too much Xopenex Inhalation Solution you can have heart or lung problems that can lead to death.
• serious allergic reactions. Call your doctor and stop using Xopenex Inhalation Solution right away if you have any symptoms of an allergic reaction such as:
  • swelling of the face, throat or tongue
  • hives
  • rash
  • breathing problems
• low potassium levels in your blood

Call your doctor or go to the nearest hospital emergency room right away if you have any of the serious side effects listed above or if you have worsening lung symptoms.

The most common side effects of Xopenex Inhalation Solution include:

• palpitations
• chest pain
• fast heart rate
• headache
• dizziness
• tremor
• nervousness

Tell your doctor if you have any side effects that bother you or that do not go away.

These are not all the possible side effects of Xopenex Inhalation Solution. For more information, ask your doctor or pharmacist.

Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

General information about the safe and effective use of Xopenex

Medicines are sometimes prescribed for purposes other than those listed in a Patient Information guide. Do not use Xopenex Inhalation Solution for a condition for which it was not prescribed. Do not give Xopenex Inhalation Solution to other people, even if they have the same symptoms that you have. It may harm them.

This Patient Information guide summarizes the most important information about Xopenex Inhalation Solution. If you would like more information, talk with your doctor. You can ask your pharmacist or doctor for information about Xopenex Inhalation Solution that is written for health professionals.

There is a pregnancy exposure registry that monitors pregnancy outcomes in women exposed to asthma medication, including Xopenex, during pregnancy. To enroll in the Asthma & Pregnancy Study or for more information about the registry, call 1-877-311-8972 or visit www.mothertobaby.org/ongoing-study/asthma.

For customer service, call 1-800-932-5676.

To report adverse events, call 1-800-932-5676.

For medical information, call 1-800-932-5676.

How should I store Xopenex?

• Store unopened Xopenex Inhalation Solution vials in the protective foil pouch they come in between 68°F to 77°F (20°C to 25°C).
• Keep Xopenex Inhalation Solution away from light and heat.
• When a Xopenex Inhalation Solution foil pouch is opened, use the vials within 2 weeks.
• When Xopenex Inhalation Solution vials are removed from the foil pouch, use them right away or within 1 week.
• Keep put of reach of children.

What are the ingredients in Xopenex?

Active ingredient: levalbuterol hydrochloride

Inactive ingredients: sodium chloride, sulfuric acid, water and nitrogen

Label

PRINCIPAL DISPLAY PANEL – TRADE CANISTER LABEL – 45 MCG 200 ACTUATIONS

• NDC 63402-510-01 Net Contents: 15 g
• Xopenex HFA®
• (levalbuterol tartrate)
• Inhalation Aerosol
• 45 mcg/actuation
• 200 Metered Inhalations
• FOR ORAL INHALATION WITH Xopenex HFA® ACTUATOR ONLY
• Shake well before using.
• Rx only
• SUNOVION

SRC: NLM .