Actions of Centesol in details
Centesol contains a selective β2-adrenergic receptor agonist, Centesol. Centesol acts especially on the bronchi where it relaxes the smooth muscles. The effect of Centesol is mediated by cyclic adenosine monophosphate. Centesol also inhibits the release of histamine and some other mediators in the lungs and accelerates ciliary clearance of the bronchi.
Inhaled Centesol acts rapidly and maximum response is reached in 30-60 min. Following oral inhalation, the fraction that is distributed to the lung (approximately 10-25%) is rapidly seen in the circulation as free unmetabolized drug. The plasma concentrations of inhaled Centesol are, however, lower than those produced by oral dose. At the doses used in inhalation therapy, the adverse reactions to Centesol are clearly less than in oral therapy.
Centesol and its metabolites are rapidly excreted in the urine and faeces, with about 80% of the dose being recovered in urine within 24 hrs. The elimination t½ of Centesol is 2.7-5.5 hrs after oral and inhaled administration.
When shifting from freon-based metered-dose aerosols to other drug dispensing devices, it is optimal to offer the patient a dispensing device, which does not require adjustment of the dose of the antiasthmatic. It is easiest for the patient to manage a new drug dispenser, which resembles as closely as possible his/her previous aerosol dispenser.
The Centesol powder dispensed by Easyhaler has been shown to exhibit clinically equivalent bronchodilatation to the optimally used Centesol aerosol when equal metered doses are administered.
How should I take Centesol?
This section provides information on the proper use of a number of products that contain albuterol. It may not be specific to Centesol. Please read with care.
Use this medicine only as directed by your doctor. Do not use more of it and do not use it more often than your doctor ordered. Also, do not stop using this medicine or any asthma medicine without telling your doctor. To do so may increase the chance for breathing problems.
The albuterol inhalation solution (eg, Accuneb®) should be used with a jet nebulizer that is connected to an air compressor with good air flow. The inhalation solution and nebulizer will come with patient instructions. Read and follow these instructions carefully. Ask your doctor if you have any questions.
To use the inhalation solution in the nebulizer:
- Use one container of solution or mix the exact amount of solution using the dropper provided for each dose.
- Place the inhalation solution in the medicine reservoir or nebulizer cup on the machine.
- Connect the nebulizer to the face mask or mouthpiece.
- Use the face mask or mouthpiece to breathe in the medicine.
- Use the nebulizer for about 5 to 15 minutes, or until the medicine in the nebulizer cup is gone.
- Clean all the parts of the nebulizer after each use.
The albuterol inhalation aerosol (eg, Proair® HFA) and albuterol inhalation powder (eg, Proair® Respiclick™) is used with a special inhaler that comes with patient instructions. Read the directions carefully before using this medicine. If you or your child do not understand the directions or are not sure how to use the inhaler, ask your doctor to show you what to do. Also, ask your doctor to check you or your child on a regular basis to make sure you are using it properly.
To use the inhalation aerosol:
- The inhaler should be at room temperature before you use it.
- Insert the metal canister firmly and fully into the clear end of the Proair® HFA mouthpiece. This mouthpiece should not be used with other inhaled medicines.
- Remove the cap and look at the mouthpiece to make sure it is clean.
- Shake the inhaler well and test spray it in the air 3 times before using it for the first time or if the inhaler has not been used for more than 2 weeks.
- To inhale this medicine, breathe out fully, trying to get as much air out of the lungs as possible. Put the mouthpiece just in front of your mouth with the canister upright.
- Open your mouth and breathe in slowly and deeply (like yawning), and at the same time firmly press down once on the top of the canister.
- Hold your breath for about 10 seconds, then breathe out slowly.
- If you are supposed to use more than one puff, wait 1 minute before inhaling the second puff. Repeat these steps for the second puff, starting with shaking the inhaler.
- When you have finished all of your doses, rinse your mouth with water and spit the water out.
- Clean the inhaler mouthpiece at least once a week with warm running water for 30 seconds, and dry it completely.
- If you need to use the inhaler before it is completely dry, shake off the excess water, replace the canister, and spray it 2 times in the air away from the face. Use your regular dose.
- After using the inhaler, wash the mouthpiece again and dry it completely.
- If the mouthpiece becomes blocked, washing it will help.
To use the inhalation powder:
- Take the inhaler from the foil pouch before you use it for the first time.
- The inhaler provides about 200 inhalations. The dose counter will change to red when there are "20" doses left. Call your doctor or pharmacist for a refill of prescription or medicine.
- Make sure the cap is closed before using this medicine. Do not open the cap unless you are going to use it.
- Hold the inhaler upright as you open the cap fully until you hear a "click". Your inhaler is now ready to use.
- To inhale this medicine, breathe out fully, trying to get as much air out of the lungs as possible. Put the mouthpiece fully into your mouth and close your lips around it.
- Breathe in through your mouth as deeply as you can until you have taken a full deep breath.
- Do not block the vent above the mouthpiece with your lips or fingers.
- Hold your breath for about 10 seconds or as long as you comfortably can.
- Remove the inhaler from your mouth and check the dose counter to make sure you received the medicine.
- Close the cap firmly over the mouthpiece after using the inhaler. Always close the cap after each use.
- If you are supposed to use more than one puff, repeat these steps for the second puff, starting with opening the cap fully.
- Keep the inhaler clean and dry at all times. Do not wash or put any part of the inhaler in water.
- If you need to clean the mouthpiece, wipe it gently with a dry cloth or tissue.
Dosing
The dose of this medicine will be different for different patients. Follow your doctor's orders or the directions on the label. The following information includes only the average doses of this medicine. If your dose is different, do not change it unless your doctor tells you to do so.
The amount of medicine that you take depends on the strength of the medicine. Also, the number of doses you take each day, the time allowed between doses, and the length of time you take the medicine depend on the medical problem for which you are using the medicine.
- For inhalation aerosol dosage form (inhaler):
- For treatment or prevention of bronchospasm:
- Adults, teenagers, and children 4 years of age and older—Two puffs every 4 to 6 hours as needed.
- Children younger than 4 years of age—Use and dose must be determined by your child's doctor.
- For prevention of exercise-induced bronchospasm:
- Adults, teenagers, and children 4 years of age and older—Two puffs taken 15 to 30 minutes before exercise.
- Children younger than 4 years of age—Use and dose must be determined by your child's doctor.
- For treatment or prevention of bronchospasm:
- For inhalation powder dosage form (inhaler):
- For treatment or prevention of bronchospasm:
- Adults, teenagers, and children 12 years of age and older—Two puffs every 4 to 6 hours as needed.
- Children younger than 12 years of age—Use and dose must be determined by your child's doctor.
- For prevention of exercise-induced bronchospasm:
- Adults, teenagers, and children 12 years of age and older—Two puffs taken 15 to 30 minutes before exercise.
- Children younger than 12 years of age—Use and dose must be determined by your child's doctor.
- For treatment or prevention of bronchospasm:
- For inhalation solution dosage form (used with a nebulizer):
- For prevention of bronchospasm:
- Adults and children older than 12 years of age—2.5 milligrams (mg) in the nebulizer 3 or 4 times per day as needed.
- Children 2 to 12 years of age—0.63 to 1.25 mg in the nebulizer 3 or 4 times per day as needed.
- Children younger than 2 years of age—Use and dose must be determined by your child's doctor.
- For prevention of bronchospasm:
Missed Dose
If you miss a dose of this medicine, take it as soon as possible. However, if it is almost time for your next dose, skip the missed dose and go back to your regular dosing schedule. Do not double doses.
Storage
Store the canister at room temperature, away from heat and direct light. Do not freeze. Do not keep this medicine inside a car where it could be exposed to extreme heat or cold. Do not poke holes in the canister or throw it into a fire, even if the canister is empty.
Keep the medicine in the foil pouch until you are ready to use it. Store at room temperature, away from heat and direct light. Do not freeze.
Store the medicine in a closed container at room temperature, away from heat, moisture, and direct light. Keep from freezing.
Keep out of the reach of children.
Do not keep outdated medicine or medicine no longer needed.
Ask your healthcare professional how you should dispose of any medicine you do not use.
Throw away Proair® Respiclick™ 13 months after opening the foil pouch, when the dose counter reaches "0", or after the expiration date, whichever comes first.
Centesol administration
Should be taken on an empty stomach. Take 1 hr before or 2 hr after meals.
Centesol pharmacology
When using an aerosol there is a rapid absorption of albuterol (Centesol) in the blood, but its concentration in plasma when used in recommended doses are very low or below detection limit.
After oral administration Centesol Cyclocaps is well absorbed from the gastrointestinal tract. Plasma protein binding is 10%. Metabolised with "first pass" through the liver and possibly in the wall of the intestine, the main metabolite - inactive sulfate conjugate. Centesol is not metabolised in the lungs, thus its ultimate metabolism and excretion following inhalation depends on the method of application, which defines the relationship between inhaled Centesol and unintentionally swallowed.
T1/2 from plasma is 2-7 hours. albuterol (Centesol) is rapidly excreted in the urine as metabolites and unchanged substance, in small amounts excreted in the feces.
References
- DailyMed. "ALBUTEROL: DailyMed provides trustworthy information about marketed drugs in the United States. DailyMed is the official provider of FDA label information (package inserts).". https://dailymed.nlm.nih.gov/dailyme... (accessed September 17, 2018).
- NCIt. "Albuterol: NCI Thesaurus (NCIt) provides reference terminology for many systems. It covers vocabulary for clinical care, translational and basic research, and public information and administrative activities.". https://ncit.nci.nih.gov/ncitbrowser... (accessed September 17, 2018).
- EPA DSStox. "Albuterol: DSSTox provides a high quality public chemistry resource for supporting improved predictive toxicology.". https://comptox.epa.gov/dashboard/ds... (accessed September 17, 2018).
Reviews
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Information checked by Dr. Sachin Kumar, MD Pharmacology