xilone
xilone Uses, Dosage, Side Effects, Food Interaction and all others data.
xilone is a glucocorticoid similar to cortisol used for its anti-inflammatory, immunosuppressive, anti-neoplastic, and vasoconstrictive effects.
xilone was granted FDA approval on 21 June 1955.
Corticosteroids bind to the glucocorticoid receptor, inhibiting pro-inflammatory signals, and promoting anti-inflammatory signals. xilone has a short duration of action as the half life is 2.1-3.5 hours. Corticosteroids have a wide therapeutic window as patients make require doses that are multiples of what the body naturally produces. Patients taking corticosteroids should be counselled regarding the risk of hypothalamic-pituitary-adrenal axis suppression and increased susceptibility to infections.
Trade Name | xilone |
Availability | Prescription only |
Generic | Prednisolone |
Prednisolone Other Names | delta-dehydrocortisol, delta-dehydrohydrocortisone, delta-hydrocortisone, delta(1)-Dehydrocortisol, delta(1)-Hydrocortisone, Hydroretrocortine, Metacortandralone, PRDL, Prednisolona, Prednisolone, Prednisolonum |
Related Drugs | Humira, Cosentyx, Gilenya, Tysabri, Vumerity, prednisone, albuterol, doxycycline, fluticasone, methotrexate |
Type | |
Formula | C21H28O5 |
Weight | Average: 360.444 Monoisotopic: 360.193674006 |
Protein binding | Prednisolone's protein binding is highly variable, ranging from 65-91% in healthy patients. |
Groups | Approved, Vet approved |
Therapeutic Class | |
Manufacturer | |
Available Country | |
Last Updated: | September 19, 2023 at 7:00 am |
![xilone xilone](https://www.medicinesfaq.com/media/png/xilone.png)
Uses
xilone is a glucocorticoid used to treat adrenocortical insufficiency, inflammatory conditions, and some cancers.
xilone is indicated to treat endocrine, rheumatic, and hematologic disorders; collagen, dermatologic, ophthalmic, respiratory, and gastrointestinal diseases; allergic and edematous states; and other conditions like tuberculous meningitis.
xilone is also used to associated treatment for these conditions: Acne Rosacea, Acute Gouty Arthritis, Allergic Bronchopulmonary Aspergillosis, Allergic Contact Dermatitis, Allergic corneal marginal ulcers, Alveolitis, Extrinsic Allergic, Anal Fissures, Ankylosing Spondylitis (AS), Aspiration Pneumonitis, Atopic Dermatitis (AD), Bell's Palsy, Berylliosis, Bullous dermatitis herpetiformis, Burns, Chorioretinitis, Choroiditis, Chronic Obstructive Airways Disease Exacerbated, Congenital Adrenal Hyperplasia (CAH), Congenital Hypoplastic Anemia, Conjunctivitis, Corneal Inflammation, Corneal injuries, Corneal ulceration, Crohn's Disease (CD), Cyclitis, Dermatitis exfoliative generalised, Dermatitis, Contact, Dermatomyositis, Dermatosis of the Ear Canal, Drug hypersensitivity reaction, Edema of the cerebrum, Epicondylitis, Erythroblastopenia, Exacerbation of asthma, Eye inflammation caused by Cataract Surgery, Eye inflammation caused by Infection, Herpes Zoster Keratitis, Hot Water Burns (Scalds), Hypercalcemia of Malignancy, Idiopathic Pulmonary Fibrosis (IPF), Idiopathic Thrombocytopenic Purpura, Inflamed External Hemorrhoid, Inflamed Hemorrhoids, Internal, Inflammatory Reaction caused by susceptible Bacterial Infections, Iridocyclitis, Iritis, Itching caused by susceptible Bacterial Infections, Leukemia, Acute, Loeffler's syndrome, Malignant Lymphomas, Multiple sclerosis exacerbation, Mycosis Fungoides (MF), Ocular Inflammation, Ophthalmia, Sympathetic, Optic Neuritis, Otic Eczema, Pemphigus, Perennial Allergic Rhinitis (PAR), Pericarditis, Pneumocystis Jirovecii Pneumonia, Pneumonia, Aspiration, Polymyalgia Rheumatica, Post-traumatic Osteoarthritis, Proctitis, Proteinuria, Pruritus, Pruritus Ani, Psoriatic Arthritis, Pulmonary Tuberculosis (TB), Pure Red Cell Aplasia, Rash, Rejection, Transplant, Relapsing Polychondritis, Rheumatoid Arthritis, Rheumatoid Arthritis, Juvenile, Seasonal Allergic Conjunctivitis, Seasonal Allergic Rhinitis, Secondary Adrenal Insufficiency, Secondary thrombocytopenia, Serum Sickness, Severe Asthma, Sjögren's Syndrome, Skin Infections, Bacterial, Stevens-Johnson Syndrome, Superficial punctate keratitis, Synovitis, Systemic Lupus Erythematosus (SLE), Trichinosis, Tuberculosis (TB), Tuberculous Meningitis, Ulcerative Colitis, Uveitis, Vasculitis, Acquired immune hemolytic anemia, Acute Bursitis, Acute Rheumatic heart disease, unspecified, Acute Tenosynovitis, Allergic skin manifestations, Anal eczema, Exfoliative erythroderma, Idiopathic Bronchiolitis obliterans with organizing pneumonia, Idiopathic eosinophilic pneumonias, Non-suppurative Thyroiditis, Primary adrenocoritical insufficiency, Severe Psoriasis, Severe Seborrhoeic dermatitis, Severe alcoholic liver disease, Steroid-responsive inflammation of the eye, Subacute Bursitis, Susceptible Bacterial Infections, Symptomatic Sarcoidosis, Varicella-zoster virus acute retinal necrosis
How xilone works
The short term effects of corticosteroids are decreased vasodilation and permeability of capillaries, as well as decreased leukocyte migration to sites of inflammation. Corticosteroids binding to the glucocorticoid receptor mediates changes in gene expression that lead to multiple downstream effects over hours to days.
Glucocorticoids inhibit neutrophil apoptosis and demargination; they inhibit phospholipase A2, which decreases the formation of arachidonic acid derivatives; they inhibit NF-Kappa B and other inflammatory transcription factors; they promote anti-inflammatory genes like interleukin-10.
Lower doses of corticosteroids provide an anti-inflammatory effect, while higher doses are immunosuppressive. High doses of glucocorticoids for an extended period bind to the mineralocorticoid receptor, raising sodium levels and decreasing potassium levels.
Toxicity
The intraperitoneal LD50 in rats is 2g/kg and 65mg/kg in mice. The subcutaneous LD50 in rats is 147mg/kg and >3500mg/kg in mice. The oral LD50 in mice is 1680mg/kg. In humans, the oral TDLO in men is 9mg/kg/2W and in women is 14mg/kg/13D.
Patients experiencing an overdose of prednisolone may present with gastrointestinal disturbances, insomnia, and restlessness. Overdose of oral prednisolone may be treated by gastric lavage or inducing vomiting if the overdose was recent, as well as supportive and symptomatic therapy. Chronic overdosage may be treated by dose reduction or treating patients on alternate days. An overdose by the ophthalmic route is not expected to cause problems.
Food Interaction
- Avoid alcohol.
- Take with food. Food reduces irritation.
xilone Cholesterol interaction
[Moderate] Corticosteroids may elevate serum triglyceride and LDL cholesterol levels if used for longer than brief periods.
Patients with preexisting hyperlipidemia may require closer monitoring during prolonged corticosteroid therapy, and adjustments made accordingly in their lipid-lowering regimen.
xilone Hypertension interaction
[Moderate] Corticosteroids may cause hypernatremia, hypokalemia, fluid retention, and elevation in blood pressure.
These mineralocorticoid effects are most significant with fludrocortisone, followed by hydrocortisone and cortisone, then by prednisone and prednisolone.
The remaining corticosteroids, betamethasone, dexamethasone, methylprednisolone, and triamcinolone, have little mineralocorticoid activities.
However, large doses of any corticosteroid can demonstrate these effects, particularly if given for longer than brief periods.
Therapy with corticosteroids should be administered cautiously in patients with preexisting fluid retention, hypertension, congestive heart failure, and Dietary sodium restriction and potassium supplementation may be advisable.
xilone Drug Interaction
Moderate: aspirin, polyethylene glycol 3350Minor: budesonide / formoterol, albuterolUnknown: amoxicillin / clavulanate, diphenhydramine, omega-3 polyunsaturated fatty acids, fluticasone nasal, atorvastatin, pregabalin, esomeprazole, acetaminophen, hydroxychloroquine, montelukast, acetaminophen, cyanocobalamin, ascorbic acid, cholecalciferol, ranitidine, cetirizine
xilone Disease Interaction
Major: GI perforation, infections, prematurity, PUD, vaccinationModerate: (+) tuberculin test, cirrhosis, depression/psychoses, diabetes, electrolyte imbalance, fluid retention, hyperadrenocorticalism, hyperlipidemia, hypothyroidism, liver disease, MI, myasthenia gravis, myopathy, ocular herpes simplex, ocular toxicities, osteoporosis, scleroderma, strongyloidiasis, thromboembolism
Volume of Distribution
A 0.15mg/kg dose of prednisolone has a volume of distribution of 29.3L, while a 0.30mg/kg dose has a volume of distribution of 44.2L.
Elimination Route
Oral prednisolone reaches a Cmax of 113-1343ng/mL with a Tmax of 1.0-2.6 hours. Oral prednisolone is approximately 70% bioavailable.
Half Life
xilone has a plasma half life of 2.1-3.5 hours. This half life is shorter in children and longer in those with liver disease.
Clearance
A 0.15mg/kg dose of prednisolone has a clearance of 0.09L/kg/h, while a 0.30mg/kg dose has a clearance of 0.12L/kg/h.
Elimination Route
xilone is over 98% eliminated in urine.
Innovators Monograph
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