The action of the drug on the human body is called Pharmacodynamics in Medical terminology. To produce its effect and to change the pathological process that is happening the body and to reduce the symptom or cure the disease, the medicine has to function in a specific way. The changes it does to the body at cellular level gives the desired result of treating a disease. Drugs act by stimulating or inhibiting a receptor or an enzyme or a protein most of the times. Medications are produced in such a way that the ingredients target the specific site and bring about chemical changes in the body that can stop or reverse the chemical reaction which is causing the disease.
Pharmacology: Pharmacodynamics: The pharmacologic effects of Lv Ke are at least in part attributable to stimulation through β-adrenergic receptors of intracellular adenyl cyclase, the enzyme that catalyzes the conversion of adenosine triphosphate (ATP) to cyclic-3', 5'-adenosine monophosphate (cyclic AMP). Increased cyclic AMP levels are associated with relaxation of bronchial smooth muscle. Bronchial effects of inhaled Lv Ke can be detected after few minutes and duration of action is normally 4-6 hrs.
Like other β2-adrenoceptor agonists also Lv Ke has cardiovascular effects in some patients as measured by changes in pulse rate, blood pressure, symptoms and electrocardiogram (ECG) changes. These effects can especially be detected after oral and IV administration of Lv Ke. In addition, Lv Ke has some metabolic effects. Especially IV and nebulized Lv Ke decreases serum potassium concentrations although the effect is generally mild and transient.
Pharmacokinetics: After administration of Lv Ke by the inhaled route between 10 and 25% of the dose reaches the lung. The remainder is retained in the delivery system or is deposited in the oropharynx from where it is swallowed. The fraction deposited in the airways is absorbed into the pulmonary tissues and circulation, but is not metabolised by the lung. On reaching the systemic circulation it becomes accessible to hepatic metabolism and is excreted primarily in the urine. The swallowed portion of an inhaled dose is absorbed from the gastrointestinal tract and undergoes considerable first-pass metabolism. Both unchanged drug and conjugate are excreted primarily in the urine. The elimination half-life (t½) of Lv Ke is 2.7-5.5 hrs after oral and inhaled administration.
Toxicology: Preclinical Safety Data: Acute toxicity of Lv Ke is low in the mouse, rat and dog. Lethal dosage (LD50) values in these species have exceeded several thousand fold the intended human therapeutic doses. Reported findings in repeated-dose studies eg, tachycardia, increases in heart weights and hypertrophy of muscle fibres are common to all potent selective β2-agonists and are an expression of excessive β-stimulant action. Cleft palate has been reported in mice but not in rats or rabbits after SC administration. Lv Ke is not mutagenic. Mesovarian leiomyomas, benign tumours of smooth muscle, occur particularly in Sprague-Dawley rats, but not in other species.
How should I take Lv Ke?
This section provides information on the proper use of a number of products that contain albuterol. It may not be specific to Lv Ke. 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 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 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.
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.
Lv Ke administration
Administration of drug is important to know because the drug absorption and action varies depending on the route and time of administration of the drug. A medicine is prescribed before meals or after meals or along with meals. The specific timing of the drug intake about food is to increase its absorption and thus its efficacy. Few work well when taken in empty stomach and few medications need to be taken 1 or 2 hrs after the meal. A drug can be in the form of a tablet, a capsule which is the oral route of administration and the same can be in IV form which is used in specific cases. Other forms of drug administration can be a suppository in anal route or an inhalation route.
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Should be taken on an empty stomach. Take 1 hr before or 2 hr after meals.
Lv Ke pharmacology
Pharmacokinetics of a drug can be defined as what body does to the drug after it is taken. The therapeutic result of the medicine depends upon the Pharmacokinetics of the drug. It deals with the time taken for the drug to be absorbed, metabolized, the process and chemical reactions involved in metabolism and about the excretion of the drug. All these factors are essential to deciding on the efficacy of the drug. Based on these pharmacokinetic principles, the ingredients, the Pharmaceutical company decides dose and route of administration. The concentration of the drug at the site of action which is proportional to therapeutic result inside the body depends on various pharmacokinetic reactions that occur in the body.
When using an aerosol there is a rapid absorption of albuterol (Lv Ke) in the blood, but its concentration in plasma when used in recommended doses are very low or below detection limit.
After oral administration Lv Ke 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. Lv Ke 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 Lv Ke and unintentionally swallowed.
T1/2 from plasma is 2-7 hours. albuterol (Lv Ke) 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).
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