Xopenex HFA

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

Medically reviewed by  A Ras MD.

What is Xopenex HFA?

Xopenex HFA is an inhaled prescription medicine used for the treatment or prevention of asthma in people 4 years of age and older. Xopenex HFA has not been shown to be safe and effective in children younger than 4 years of age.

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.

Who should not use Xopenex HFA?

Do not use Xopenex HFA if you:

• are allergic to levalbuterol, racemic albuterol or any of the ingredients in Xopenex HFA. See the end of this Patient Information leaflet for a complete list of ingredients in Xopenex HFA.

What should I tell my healthcare provider before using Xopenex HFA?

Before you use Xopenex HFA, tell your doctor about all of your medical conditions, including if you:

• have heart problems.
• have high blood pressure.
• have seizures.
• have diabetes.
• have thyroid problems.
• are pregnant or plan to become pregnant. It is not known if Xopenex HFA 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 HFA passes into your breast milk. Talk to your doctor about the best way to feed your baby if you use Xopenex HFA.

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

• other inhaled medicines or asthma medicines
• heart medicines
• medicines that increase urination (diuretics)
• antidepressants
• medicine to treat chronic obstructive pulmonary disease (COPD). Ask your doctor or pharmacist for a list of these medicines if you are not sure.

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

How should I use Xopenex HFA?

• Read the step-by-step Instructions for Use that come with Xopenex HFA.
• Xopenex HFA is for oral inhalation use only.
• Use Xopenex HFA 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 HFA.
• An adult should help a child use Xopenex HFA. Your doctor should show you how your child should use Xopenex HFA.
• Do not use your Xopenex HFA more often than your doctor tells you to.
• Get medical help right away if Xopenex HFA:
  • does not work as well for your asthma symptoms
  • your asthma symptoms get worse
  • you need to use Xopenex HFA more often than usual
• While you are using Xopenex HFA, do not use other inhaled medicines and asthma medicines unless your doctor tells you to.

What are the possible side effects of Xopenex HFA?

Xopenex HFA can cause serious side effects including:

• sudden shortness of breath (bronchospasm). Sudden shortness of breath can happen right away after using Xopenex HFA.
• worsening asthma.
• heart problems.
• death. If you use too much Xopenex HFA you can have heart or lung problems that can lead to death.
• serious allergic reactions. Call your doctor and stop using Xopenex HFA 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 HFA include:

• accidental injury
• bronchitis
• dizziness
• pain
• sore throat
• runny nose
• vomiting
• palpitations
• chest pain
• fast heart rate
• tremors
• nervousness

These are not all the possible side effects of Xopenex HFA.
Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.
You may also report side effects to Sunovion Pharmaceuticals Inc. at 1-877-737-7226.

General information about the safe and effective use of Xopenex HFA

Medicines are sometimes prescribed for purposes other than those listed in a Patient Information leaflet. Do not use Xopenex HFA for a condition for which it was not prescribed. Do not give Xopenex HFA to other people, even if they have the same symptoms that you have. It may harm them.
You can ask your pharmacist or doctor for information about Xopenex HFA that is written for health professionals.

How should I store Xopenex HFA?

• Store Xopenex HFA at room temperature between 68°F to 77°F (20°C to 25°C).
• Do not use or store Xopenex HFA inhaler near heat or open flame. Temperatures above 120°F may cause the canister to burst.
• Do not freeze Xopenex HFA.
• Keep Xopenex HFA out of direct sunlight.
• Do not put a hole in the Xopenex HFA canister.
• Store Xopenex HFA with the mouthpiece down.
• Throw away Xopenex HFA when the dose indicator display window reaches zero “0”, showing that all 200 sprays (actuations) have been used.
• Do not throw Xopenex HFA into a fire or an incinerator.

Keep Xopenex HFA and all medicines out of the reach of children.

What are the ingredients in Xopenex HFA?

Active ingredient: levalbuterol tartrate

Inactive ingredients: propellant HFA-134a, Dehydrated Alcohol USP, Oleic Acid NF

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

PRINCIPAL DISPLAY PANEL – TRADE CARTON – 45 MCG 200 ACTUATIONS

• NDC 63402-510-01 Net Contents: 15g
• 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