Actions of Yalone in details
Pharmacology: Pharmacodynamics: Yalone is a synthetic glucocorticoid and a methyl derivative of prednisolone. It is a moderately potent glucocorticoid with only slight mineralocorticoid activity. Yalone is a potent anti-inflammatory agent with the capacity to profoundly inhibit the immune system. Yalone 4 mg is equivalent to about 5 mg of prednisolone in terms of anti-inflammatory activity. In addition, Yalone has a lesser tendency to induce sodium and water retention compared with prednisolone.
Pharmacokinetics: The pharmacokinetics of Yalone is linear, independent of the route of administration.
After oral administration, Yalone achieves its maximum plasma concentration in about 1.5-2.3 hrs across doses in healthy adults. Mean oral time to peak concentration is achieved in about 1.1-2.2 hrs. The oral bioavailability of Yalone is 82-89%.
Yalone is widely distributed throughout the body and is described by a 2-compartment model. The mean volume of distribution of Yalone ranges from 41-61.5 L in adult volunteers.
Similar to many CYP3A4 substrates, Yalone may also be a substrate for the adenosine triphosphate (ATP)-binding cassette (ABC) transport protein p-glycoprotein which may influence tissue distribution and interactions with other medicines.
Yalone is widely distributed into tissues and is bound to plasma protein (approximately 77%). It crosses the blood-brain barrier into the central nervous system with peak CSF levels being 5-6% of the corresponding plasma levels. It also crosses the placenta and is secreted in breast milk.
Yalone is extensively metabolized in the liver to inactive metabolites, mainly 20α-hydroxymethylprednisolone and 20β-hydroxymethylprednisolone. Metabolism in the liver occurs primarily via the CYP3A4 enzyme.
The mean elimination half-life (t½) for total Yalone is in the range of 1.8-5.2 hrs.
Radiolabeled 6-Yalone was administered IV to 6 cancer patients. Seventy-five percent (75%) of total radioactivity was recovered in the urine after 96 hrs and 9% in the feces after 5 days. Twenty percent (20%) of the total dose was excreted in the bile; however, the time course was not cited.
How should I take Yalone?
Take Yalone exactly as directed by your doctor. Do not take more of it, do not take it more often, and do not take it for a longer time than your doctor ordered. To do so may increase the chance for unwanted effects.
If you use Yalone for a long time, do not suddenly stop using it without checking first with your doctor. You may need to slowly decrease your dose before stopping it completely.
Dosing
The dose of Yalone 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 Yalone. 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 oral dosage form (tablets):
- Dose depends on medical condition:
- Adults—At first, 4 to 48 milligrams (mg) per day. Your doctor may adjust your dose as needed.
- Children—Use and dose must be determined by your doctor.
- Dose depends on medical condition:
Missed Dose
If you miss a dose of Yalone, 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 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.
Yalone administration
Take exactly as prescribed by your doctor. Do not take in larger or smaller amounts or for longer than recommended. Follow the directions on your prescription label.
Your doctor may occasionally change your dose to make sure you get the best results from this medication.
Your steroid medication needs may change if you have unusual stress such as a serious illness, fever or infection, or if you have surgery or a medical emergency. Tell your doctor about any such situation that affects you.
This medication can cause unusual results with certain medical tests. Tell any doctor who treats you that you are using Yalone.
Do not stop using Yalone suddenly, or you could have unpleasant withdrawal symptoms. Ask your doctor how to avoid withdrawal symptoms when you stop using Yalone.
Wear a medical alert tag or carry an ID card stating that you take Yalone. doctor, dentist, or emergency medical professional who treats you should know that you take steroid medication.
Store at room temperature away from moisture and heat.
Yalone pharmacology
Glucocorticoids, naturally occurring and synthetic, are adrenocortical steroids that are readily absorbed from the gastrointestinal tract.
Naturally occurring glucocorticoids (hydrocortisone and cortisone), which also have salt-retaining properties, are used as replacement therapy in adrenocortical deficiency states. Their synthetic analogs are primarily used for their potent anti-inflammatory effects in disorders of many organ systems.
Glucocorticoids cause profound and varied metabolic effects. In addition, they modify the body’s immune response to diverse stimuli. Yalone is a potent anti-inflammatory steroid with greater anti-inflammatory potency than prednisolone and even less tendency than prednisolone to induce sodium and water retention.
Yalone sodium succinate has the same metabolic and anti-inflammatory actions as Yalone. When given parenterally and in equimolar quantities, the two compounds are equivalent in biologic activity. Following the intravenous injection of Yalone sodium succinate, demonstrable effects are evident within one hour and persist for a variable period. Excretion of the administered dose is nearly complete within 12 hours. Thus, if constantly high blood levels are required, injections should be made every 4 to 6 hours. This preparation is also rapidly absorbed when administered intramuscularly and is excreted in a pattern similar to that observed after intravenous injection.
References
- DailyMed. "METHYLPREDNISOLONE: 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. "Methylprednisolone: 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. "Methylprednisolone: DSSTox provides a high quality public chemistry resource for supporting improved predictive toxicology.". https://comptox.epa.gov/dashboard/ds... (accessed September 17, 2018).
Reviews
The results of a survey conducted on ndrugs.com for Yalone are given in detail below. The results of the survey conducted are based on the impressions and views of the website users and consumers taking Yalone. We implore you to kindly base your medical condition or therapeutic choices on the result or test conducted by a physician or licensed medical practitioners.User reports
Consumer reported administration
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Information checked by Dr. Sachin Kumar, MD Pharmacology
