Zestanid
Zestanid Uses, Dosage, Side Effects, Food Interaction and all others data.
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.
Corticosteroids bind to the glucocorticoid receptor, inhibiting pro-inflammatory signals, and promoting anti-inflammatory signals. Corticosteroids have a wide therapeutic window as patients may 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 | Zestanid |
Availability | Prescription only |
Generic | Methylprednisolone |
Methylprednisolone Other Names | Methylprednisolon, Methylprednisolone, Methylprednisolonum, Metilprednisolona |
Related Drugs | Humira, Otezla, Cosentyx, Dupixent, Gilenya, Tysabri, Xolair, Trelegy Ellipta, Vumerity, ProAir Digihaler |
Type | |
Formula | C22H30O5 |
Weight | Average: 374.4706 Monoisotopic: 374.20932407 |
Protein binding | Methylprednisolone is 76.8% protein bound in plasma and does not significantly bind to corticosteroid binding protein. Methylprednisolone is bound to human serum albumin in plasma. |
Groups | Approved, Vet approved |
Therapeutic Class | Glucocorticoids |
Manufacturer | |
Available Country | Peru |
Last Updated: | September 19, 2023 at 7:00 am |
![Zestanid Zestanid](https://www.medicinesfaq.com/media/png/zestanid.png)
Uses
Methyl Prednisolone Tablets are used for the following conditions:
Endocrine Disorders: Primary or secondary adrenocortical insufficiency, Congenital adrenal hyperplasia, Nonsuppurative thyroiditis, Hypercalcemia associated with cancer
Rheumatic Disorders: As adjunctive therapy for short-term administration (to tide the patient over an acute episode orexacerbation) in: Rheumatoid arthritis, including juvenile rheumatoid arthritis (selected cases may require low-dose maintenance therapy), Ankylosing spondylitis, Acute and subacute bursitis, Synovitis of osteoarthritis, Acute nonspecific tenosynovitis, Post-traumatic osteoarthritis, Psoriatic arthritis, Epicondylitis, Acute gouty arthritis
Collagen Diseases: During an exacerbation or as maintenance therapy in selected cases of: Systemic lupus erythematosus Systemic dermatomyositis (polymyositis), Acute rheumatic carditis
Dermatologic Diseases: Bullous dermatitis herpetiformis, Severe erythema multiforme (Stevens-Johnson syndrome), Severe seborrheic dermatitis, Exfoliative dermatitis, Mycosis fungoides, Pemphigus, Severe psoriasis
Allergic States: Control of severe or incapacitating allergic conditions intractable to adequate trials of conventional treatment: Seasonal or perennial allergic rhinitis, Drug hypersensitivity reactions, Serum sickness, Contact dermatitis, Bronchial asthma, Atopic dermatitis
Ophthalmic Diseases: Severe acute and chronic allergic and inflammatory processes involving the eye and its adnexa such as: Allergic corneal marginal ulcers, Herpes zoster ophthalmicus, Anterior segment inflammation, Diffuse posterior uveitis and choroiditis, Sympathetic ophthalmia, Keratitis, Optic neuritis, Allergic conjunctivitis Chorioretinitis, Iritis and iridocyclitis
Respiratory Diseases: Symptomatic sarcoidosis, Berylliosis, Loeffler’s syndrome not manageable by other means, Fulminating or disseminated pulmonary tuberculosis when used concurrently with appropriate antituberculous chemotherapy, Aspiration pneumonitis
Hematologic Disorders: Idiopathic thrombocytopenic purpura in adults, Secondary thrombocytopenia in adults, Acquired (autoimmune) hemolytic anemia, Erythroblastopenia (RBC anemia), Congenital (erythroid) hypoplastic anemia
Neoplastic Diseases: For palliative management of: Leukemias and lymphomas in adults, Acute leukemia of childhood
Edematous States: To induce a diuresis or remission of proteinuria in the nephrotic syndrome, without uremia, of the idiopathic type or that due to lupus erythematosus.
Gastrointestinal Diseases: To tide the patient over a critical period of the disease in: Ulcerative colitis, Regional enteritis
Nervous System: Acute exacerbations of multiple sclerosis
Zestanid is also used to associated treatment for these conditions: Acne Rosacea, Acute Gouty Arthritis, Adrenal cortical hypofunctions, Adrenocortical Hyperfunction, Allergic corneal marginal ulcers, Alopecia Areata (AA), Ankylosing Spondylitis (AS), Anterior Segment Inflammation, Aponeurosis contusion, Arthritis, Aspiration Pneumonitis, Asthma, Atopic Dermatitis (AD), Berylliosis, Bronchial Asthma, Bullous dermatitis herpetiformis, Bursitis, Chorioretinitis, Choroiditis, Congenital Adrenal Hyperplasia (CAH), Congenital Hypoplastic Anemia, Corneal Inflammation, Cushing's Syndrome, Degenerative Joint Disease, Dermatitis exfoliative generalised, Dermatitis, Contact, Discoid Lupus Erythematosus (DLE), Drug hypersensitivity reaction, Edema, Edema of the cerebrum, Epicondylitis, Erythroblastopenia, Gouty Arthritis, Hypercalcemia, Idiopathic Thrombocytopenic Purpura, Inflammation, Inflammatory Reaction of the Cysts, Iridocyclitis, Iritis, Keloid Scars, Leukemia, Acute, Lichen Planus (LP), Lichen simplex chronicus, Loeffler's syndrome, Malignant Lymphomas, Multiple sclerosis exacerbation, Mycosis Fungoides (MF), Necrobiosis lipoidica diabeticorum, Nummular Eczema, Ocular Inflammation, Ophthalmia, Sympathetic, Optic Neuritis, Pemphigus, Perennial Allergic Rhinitis (PAR), Polymyositis, Post-traumatic Osteoarthritis, Psoriatic Arthritis, Psoriatic plaque, Pure Red Cell Aplasia, Regional Enteritis, Rheumatoid Arthritis, Rheumatoid Arthritis, Juvenile, Sarcoidosis, Seasonal Allergic Conjunctivitis, Seasonal Allergic Rhinitis, Seborrheic Dermatitis, Eczematous, Secondary thrombocytopenia, Serum Sickness, Severe Allergic Asthma, Severe Seborrheic Dermatitis, Stevens-Johnson Syndrome, Synovitis, Systemic Lupus Erythematosus (SLE), Temporal Arteritis, Tendonitis exacerbated, Transfusion Reactions, Trichinosis, Tuberculosis (TB), Tuberculosis Meningitis, Tumors Metastatic to Brain, Ulcerative Colitis, Uveitis, Acquired immune hemolytic anemia, Acute nonspecific tenosynovitis, Acute rheumatic carditis, Cystic tumors of aponeurosis, Cystic tumors of tendon, Idiopathic eosinophilic pneumonias, Inflammatory dermatoses of the scalp, Localized Hypertrophic, Inflammatory, Infiltrated granuloma annulare lesions, Non-suppurative Thyroiditis, Severe Psoriasis, Systemic Dermatomyositis, Varicella-zoster virus acute retinal necrosis
How Zestanid 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.
Dosage
Zestanid dosage
The initial dosage of Methyl Prednisolone Tablets may vary from 4 mg to 48 mg of Methyl Prednisolone per day depending on the specific disease entity being treated. In situations of less severity lower doses will generally suffice while in selected patients higher initial doses may be required. The initial dosage should be maintained or adjusted until a satisfactory response is noted. If after a reasonable period of time there is a lack of satisfactory clinical response, Methyl Prednisolone should be discontinued and the patient transferred to other appropriate therapy. It should be emphasized that dosage requirements are variable and must be individualized on the basis of the disease under treatment and the response of the patient. After a favorable response is noted, the proper maintenance dosage should be determined by decreasing the initial drug dosage in small decrements at appropriate time intervals until the lowest dosage which will maintain an adequate clinical response is reached. It should be kept in mind that constant monitoring is needed in regard to drug dosage. Included in the situations which may make dosage adjustments necessary are changes in clinical status secondary to remissions or exacerbations in the disease process, the patient's individual drug responsiveness, and the effect of patient exposure to stressful situations not directly related to the disease entity under treatment; in this latter situation it may be necessary to increase the dosage of Zestanid for a period of time consistent with the patient's condition. If after long-term therapy the drug is to be stopped, it is recommended that it be withdrawn gradually rather than abruptly.
Multiple Sclerosis: In treatment of acute exacerbations of multiple sclerosis daily doses of 200 mg of prednisolone for a week followed by 80 mg every other day for 1 month have been shown to be effective (4 mg of methylprednisolone is equivalent to 5 mg of prednisolone).
Side Effects
Short courses of Zestanid are usually well-tolerated with few, mild side effects. Long term, high doses of Zestanid may produce predictable and potentially serious side effects. Whenever possible, the lowest effective doses of Zestanid should be used for the shortest length of time to minimize side effects. Alternate day dosing also can help reduce side effects. Side effects of Zestanid and other corticosteroids range from mild annoyances to serious irreversible body damage. Side effects include fluid retention, weight gain, high blood pressure, potassium loss, headache, muscle weakness, hair growth on the face, glaucoma, cataracts, peptic ulceration, growth retardation in children, convulsions and psychic disturbances including depression, euphoria, insomnia etc.
Toxicity
The oral LD50 in rats is >4g/kg. The intraperitoneal LD50 in mice is 2292mg/kg and in rats is 100mg/kg.
Data regarding acute overdoses of glucocorticoids are rare. Chronic high doses of glucocorticoids can lead to the development of cataract, glaucoma, hypertension, water retention, hyperlipidemia, peptic ulcer, pancreatitis, myopathy, osteoporosis, mood changes, psychosis, dermal atrophy, allergy, acne, hypertrichosis, immune suppression, decreased resistance to infection, moon face, hyperglycemia, hypocalcemia, hypophosphatemia, metabolic acidosis, growth suppression, and secondary adrenal insufficiency. Treat acute overdoses with symptomatic and supportive therapy, while chronic overdoses will require temporarily reduced dosages.
Precaution
Adrenocortical insufficiency may persist for months after discontinuation of therapy; therefore, in any situation of stress occurring during that period, hormone therapy should be reinstituted. Since mineralocorticoid secretion may be impaired, salt and/or a mineralocorticoid should be administered concurrently. There is an enhanced effect of corticosteroids on patients with hypothyroidism and in those with cirrhosis. Corticosteroids should be used cautiously in conjunction with corticosteroids in hypoprothombinemia. Growth and development of infants and children on prolonged corticosteroid therapy should be carefully observed.
Interaction
Erythromycin, Clarithromycin, Phenobarbital, Phenytoin, Rifampin and Ketoconazole inhibit the metabolism of Zestanid. Estrogens including birth control pills, can increase the effect of corticosteroids by 50 %. Cyclosporin reduces the metabolism of Zestanid while Zestanid reduces the metabolism of Cyclosporin. Zestanid may increase or decrease the effect of blood thinners (e.g. Warfarin). For all these interactions, the dose of Zestanid may need to be lowered.
Food Interaction
- Avoid alcohol.
- Take with food. Food reduces GI irritation.
[Moderate] MONITOR: Grapefruit juice may increase the plasma concentrations of orally administered drugs that are substrates of the CYP450 3A4 isoenzyme.
The proposed mechanism is inhibition of CYP450 3A4-mediated first-pass metabolism in the gut wall by certain compounds present in grapefruit.
Because grapefruit juice inhibits primarily intestinal rather than hepatic CYP450 3A4, the magnitude of interaction is greatest for those drugs that undergo significant presystemic metabolism by CYP450 3A4 (i.e., drugs with low oral bioavailability).
In general, the effect of grapefruit juice is concentration-, dose- and preparation-dependent, and can vary widely among brands.
Certain preparations of grapefruit juice (e.g., high dose, double strength) have sometimes demonstrated potent inhibition of CYP450 3A4, while other preparations (e.g., low dose, single strength) have typically demonstrated moderate inhibition.
Pharmacokinetic interactions involving grapefruit juice are also subject to a high degree of interpatient variability, thus the extent to which a given patient may be affected is difficult to predict.
MANAGEMENT: Patients who regularly consume grapefruit or grapefruit juice should be monitored for adverse effects and altered plasma concentrations of drugs that undergo significant presystemic metabolism by CYP450 3A4.
Grapefruit and grapefruit juice should be avoided if an interaction is suspected.
Orange juice is not expected to interact with these drugs.
Zestanid 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.
Zestanid 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.
Zestanid Drug Interaction
Moderate: aspirinMinor: albuterol / ipratropium, albuterol, alprazolamUnknown: diphenhydramine, duloxetine, omega-3 polyunsaturated fatty acids, cyclobenzaprine, fluticasone nasal, escitalopram, pregabalin, guaifenesin, acetaminophen / hydrocodone, acetaminophen, montelukast, acetaminophen, cyanocobalamin, ascorbic acid, cholecalciferol, cetirizine
Zestanid 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
The average volume of distribution of methylprednisolone is 1.38L/kg.
Elimination Route
Oral methylprednisolone has 89.9% the bioavailability of oral methylprednisolone acetate, while rectal methylprednisolone has 14.2% the bioavailability. Intravitreal methylprednisolone has a Tmax of 2.5h. Approximately 1/10 of an oral or IV dose of methylprednisolone will reach the vitreous humor. Further data regarding the absorption of methylprednisolone are not readily available.
Half Life
Zestanid has a half life of 2.3h.
Clearance
The average plasma clearance of methylprednisolone is 336mL/h/kg.
Elimination Route
Zestanid and its metabolites have been collected in urine in humans. A study in dogs showed 25-31% elimination in urine and 44-52% elimination in feces.
Pregnancy & Breastfeeding use
Pregnancy category C. Either studies in animals have revealed adverse effects on the foetus (teratogenic or embryocidal or other) and there is no controlled studies in women and animals are not available. Drugs should be given only if the potential benefit justifies the potential risk to the fetus.
Lactation: Zestanid has not been adequately evaluated in nursing mothers.
Contraindication
Systemic fungal infections and known hypersensitivity to components.
Acute Overdose
Report of acute toxicity and/or death following overdose of glucocorticoid are rare. No specific antidote is available; treatment is supportive and symptomatic. Serum electrolytes should be monitored.
Storage Condition
Store in a cool dry place, away from light. Keep out of reach of children
Innovators Monograph
You find simplified version here Zestanid
FAQ
What is Zestanid used for?
Zestanid is used to treat a number of different conditions, such as inflammation, severe allergies, adrenal problems, arthritis, asthma, blood or bone marrow problems, eye or vision problems, lupus, skin conditions, kidney problems, ulcerative colitis, and flare-ups of multiple sclerosis.Zestanid is a synthetic glucocorticoid, primarily prescribed for its anti-inflammatory and immunosuppressive effects. It is either used at low doses for chronic illnesses or used concomitantly at high doses during acute flares.
How safe is Zestanid?
Zestanid can make you more likely to get infections or may worsen any current infections. Avoid contact with people who have infections that may spread to others. Consult your doctor if you have been exposed to an infection or for more details.
How does Zestanid work?
Zestanid works by decreasing inflammation and changing your body's immune response. This reduces the inflammation caused by your condition.
What are the common side effects of Zestanid?
Common side effects of Zestanid are include:
- upset stomach
- stomach irritation
- vomiting
- headache
- dizziness
- insomnia
- restlessness
- depression
- anxiety
- acne
- increased hair growth
- easy bruising
- irregular or absent menstrual periods
Is Zestanid safe during pregnancy?
Zestanid may be safe in pregnancy. However, use of these drugs in pregnant patients should be considered carefully and avoided unless deemed necessary.
Can I drink alcohol with Zestanid?
Alcohol and Zestanid can each irritate the digestive tract and cause peptic ulcers. Combining the two may be asking for trouble, especially if you're already prone to indigestion or stomach upset.
Can I drive after taking Zestanid?
Do not drive or operate machinery until you know how Zestanid will affect you.
Should Zestanid be taken on an empty stomach?
Zestanid may cause an upset stomach, so it's recommended to take it with food or milk.
How long does Zestanid take to work?
Zestanid has a rapid onset. It reaches its peak effect within one to two hours after an oral dose, and within one hour of an intravenous dose.
How often can I take Zestanid?
After taking 160 mg per day for 1 week, your doctor will reduce your dosage to 64 mg taken every other day for one month.
Does Zestanid make me sleepy?
Zestanid oral tablet doesn't cause drowsiness, but it can cause other side effects.
Who should not take Zestanid?
You should not use Zestanid if you have a fungal infection anywhere in your body.Before taking methylprednisolone, tell your doctor about all of your medical conditions, and about all other medicines you are using.
What happens if I overdose?
Seek emergency medical attention. An overdose of Zestanid is not expected to produce life threatening symptoms. However, long term use of high steroid doses can lead to symptoms such as thinning skin, easy bruising, changes in the shape or location of body fat, increased acne or facial hair, menstrual problems, impotence, or loss of interest in sex.
What happen If I missed dose of Zestanid?
If you miss a dose, take it as soon as you remember. If your next dose of Zestanid should be taken soon, just take that dose. Don't double up, or take more than one dose at a time.
What happen If I stop taking Zestanid?
If you abruptly stop taking Zestanid or taper off too quickly, you might experience Zestanid withdrawal symptoms: Severe fatigue, Weakness, Body aches.
How long does Zestanid stay in your system?
It is metabolized by the liver into inactive metabolites which are excreted in the urine. The half-life of Zestanid is 18 to 36 hours which means it may take 2 to 7 days to fully eliminate the drug from the body.
Will Zestanid affect my conception?
Maternal Zestanid doses of up to 40 mg daily are considered unlikely to affect the baby.
Can Zestanid affects my heart ?
Zestanid can cause bradycardia (slowed heartbeats) and other heart rhythm problems in some people.
Can Zestanid affect my kidneys?
Administration of Zestanid did not influence renal growth.
Can Zestanid increase liver enzymes?
increase liver enzymes rare, hepatotoxicity related to Zestanid should be considered in patients who develop elevated enzyme levels while receiving this steroid.