Nositrol

Nositrol Uses, Dosage, Side Effects, Food Interaction and all others data.

Nositrol is a naturally occurring corticosteroid, which causes profound and varied metabolic effects. In addition, they modify body’s immune response to diverse stimuli. Nositrol sodium succinate has the same metabolic and anti-inflammatory actions as hydrocortisone.

Nositrol binds to the glucocorticoid receptor leading to downstream effects such as inhibition of phospholipase A2, NF-kappa B, other inflammatory transcription factors, and the promotion of anti-inflammatory genes.[A187463] Nositrol has a wide therapeutic index and a moderate duration of action. Patients should stop taking the medication if irritation or sensitization occurs.

Trade Name Nositrol
Availability Prescription only
Generic Hydrocortisone
Hydrocortisone Other Names 11beta-hydrocortisone, 17-Hydroxycorticosterone, Cortisol, Hidrocortisona, Hydrocortisone, Hydrocortisonum, Kendall's compound F, Reichstein's substance M
Related Drugs Entyvio, Humira, Zeposia, Colazal, prednisone, albuterol, dexamethasone, methylprednisolone, triamcinolone, prednisolone
Type
Formula C21H30O5
Weight Average: 362.4599
Monoisotopic: 362.20932407
Protein binding

Corticosteroids are generally bound to corticosteroid binding globulin[A187439] and serum albumin[A187436] in plasma. Hydrocortisone is 90.1% bound to proteins in plasma, with 56.2% bound to albumin.

Groups Approved, Vet approved
Therapeutic Class Glucocorticoids
Manufacturer
Available Country Mexico
Last Updated: September 19, 2023 at 7:00 am
Nositrol
Nositrol

Uses

Nositrol is used for the use in the following conditions: Primary or secondary adrenocortical insufficiency, Acute adrenocortical insufficiency, Shock unresponsive to conventional therapy, Congenital adrenal hyperplasia, Hypercalcemia associated with cancer, Nonsuppurative thyroiditis, Rheumatic Disorders, Dermatologic Diseases (Allergic States, Severe seborrheic dermatitis, Severe psoriasis, Pemphigus, Severe erythema multiforme), Control of severe or incapacitating allergic conditions (Bronchial asthma, Contact dermatitis, Atopic dermatitis, Serum sickness, Seasonal or perennial allergic rhinitis, Drug hypersensitivity reactions, Urticarial transfusion reactions, Acute noninfectious laryngeal edema), Ophthalmic Diseases (Herpes zoster ophthalmicus, Iritis, iridocyclitis, Chorioretinitis, Diffuse posterior uveitis and choroiditis, Optic neuritis), Gastrointestinal Diseases, Fulminating or disseminated pulmonary tuberculosis when used concurrently with appropriate antituberculous chemotherapy, Loeffler's syndrome, Aspiration pneumonitis, Hematologic Disorders (Acquired, autoimmune hemolytic anemia, Idiopathic thrombocytopenic purpura in adults, Secondary thrombocytopenia, Erythroblastopenia), Neoplastic Diseases (Leukemias and lymphomas in adults, Acute leukemia of childhood), Edematous States, Acute exacerbations of multiple sclerosis

Nositrol is also used to associated treatment for these conditions: Acute Gouty Arthritis, Acute Otitis Externa, Adrenal Insufficiency, Allergic Rhinitis (AR), Allergic corneal marginal ulcers, Anal Fissures, Ankylosing Spondylitis (AS), Anterior Segment Inflammation, Aspiration Pneumonitis, Asthma, Atopic Dermatitis (AD), Berylliosis, Bullous dermatitis herpetiformis, Chorioretinitis, Choroiditis, Congenital Adrenal Hyperplasia (CAH), Congenital Hypoplastic Anemia, Corneal Inflammation, Crohn's Disease (CD), Dermatitis, Dermatitis exfoliative generalised, Dermatitis, Contact, Dermatomyositis, Dermatosis, Drug hypersensitivity reaction, Epicondylitis, Erythroblastopenia, Hemorrhoids, Herpes Labialis, Hypercalcemia of Malignancy, Idiopathic Thrombocytopenic Purpura, Infection of the Fenestration Cavity, Infection of the Mastoidectomy Cavity, Iridocyclitis, Iritis, Itching caused by Hemorrhoids, Itching of the Anus, Leukemia, Acute, Leukemias, Loeffler's syndrome, Lymphomas NEC, Malignant Lymphomas, Mycosis Fungoides (MF), Ophthalmia, Sympathetic, Optic Neuritis, Pain caused by Hemorrhoids, Pemphigus, Post-traumatic Osteoarthritis, Primary adrenocortical insufficiency, Proctitis, Proteinuria, Psoriatic Arthritis, Rectal inflammations NEC, Rheumatic heart disease, unspecified, Rheumatoid Arthritis, Rheumatoid Arthritis, Juvenile, Seasonal Allergic Conjunctivitis, Secondary adrenocortical insufficiency, Secondary thrombocytopenia, Serum Sickness, Severe Seborrheic Dermatitis, Skin Diseases, Stevens-Johnson Syndrome, Synovitis, Systemic Lupus Erythematosus (SLE), Trichinosis, Tuberculous Meningitis, Ulcerative Colitis, Acquired immune hemolytic anemia, Acute Bursitis, Acute Tenosynovitis, Acute rheumatic carditis, Cryptitis, Disseminated Pulmonary Tuberculosis, Fulminating Pulmonary Tuberculosis, Itching skin, Non-suppurative Thyroiditis, Severe Erythema multiforme, Severe Psoriasis, Subacute Bursitis, Superficial infection of the external auditory canal with inflammation, Symptomatic Sarcoidosis, Systemic Dermatomyositis, Varicella-zoster virus acute retinal necrosis, Palliative

How Nositrol works

The short term effects of corticosteroids are decreased vasodilation and permeability of capillaries, as well as decreased leukocyte migration to sites of inflammation.[A187463] Corticosteroids binding to the glucocorticoid receptor mediates changes in gene expression that lead to multiple downstream effects over hours to days.[A187463]

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.[A187463]

Lower doses of corticosteroids provide an anti-inflammatory effect, while higher doses are immunosuppressive.[A187463] High doses of glucocorticoids for an extended period bind to the mineralocorticoid receptor, raising sodium levels and decreasing potassium levels.[A187463]

Dosage

Nositrol dosage

Tablet: The initial dosage of Nositrol Tablets may vary from 20 mg to 240 mg of hydrocortisone 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, Nositrol Tablets 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 patients.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. It should be kept in mind that constant monitoring is needed in regard to drug dosage. If, after long-term therapy the drug is to be stopped, it is recommended that it be withdrawn gradually, rather than abruptly.

Injection:

  • Adult: By IM injection or slow IV injection or infusion. The initial dose of Nositrol sterile powder is 100 mg to 500 mg, depending on the severity of the condition. This dose may be repeated at intervals of 2, 4 or 6 hours as indicated by the patient's response and clinical condition.
  • Children: By slow IV injection, up to 1 year 25 mg, 1-5 years 50 mg, 6-12 years 100 mg.

Side Effects

Nositrol is generally well tolerated except in prolonged high doses. It may cause cardiac arrhythmia, esophageal candidiasis, menstrual irregularity, decreased carbohydrate & glucose tolerance, fluid retention, increased appetite, weight gain, euphoria, mood swings, depression, insomnia, acne etc.

Toxicity

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. Overdose may be treated by adjusting the dose or stopping the corticosteroid as well as initiating symptomatic and supportive treatment.

Precaution

Nositrol should be used with caution in patients with a history of peptic ulceration as it increases the incidence of peptic ulceration. This drug should be used with caution in patients with congestive heart failure, hypertension, glaucoma, diabetic mellitus and epilepsy.

Interaction

Drug interaction of hydrocortisone has been reported with amphotericin B, potassium-depleting agents, macrolide antibiotics, warfarin, antidiabetics, isoniazid, digitalis glycosides, estrogens, barbiturates, phenytoin, carbamazepine, ketoconazole, aspirin etc.

Food Interaction

  • Avoid alcohol.

Nositrol 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.

Nositrol 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.

Volume of Distribution

Total hydrocortisone has a volume of distribution of 39.82L, while the free fraction has a volume of distribution of 474.38L.

Elimination Route

Oral hydrocortisone at a dose of 0.2-0.3mg/kg/day reached a mean Cmax of 32.69nmol/L with a mean AUC of 90.63h*nmol/L A 0.4-0.6mg/kg/day dose reached a mean Cmax of 70.81nmol/L with a mean AUC of 199.11h*nmol/L. However, the pharmacokinetics of hydrocortisone can vary by 10 times from patient to patient.

Topical hydrocortisone cream is 4-19% bioavailable[8546995] with a Tmax of 24h.

Nositrol retention enemas are have a bioavailability of 0.810 for slow absorbers and 0.502 in rapid absorbers. Slow absorbers take up hydrocortisone at a rate of 0.361±0.255/h while fast absorbers take up hydrocortisone at a rate of 1.05±0.255/h.

A 20mg IV dose of hydrocortisone has an AUC of 1163±277ng*h/mL.

Half Life

Total hydrocortisone via the oral route has a half life of 2.15h while the free fraction has a half life of 1.39h. A 20mg IV dose of hydrocortisone has a terminal half life of 1.9±0.4h.

Clearance

Total hydrocortisone by the oral route has a mean clearance of 12.85L/h, while the free fraction has a mean clearance of 235.78L/h. A 20mg IV dose of hydrocortisone has a clearance of 18.2±4.2L/h.

Elimination Route

Corticosteroids are eliminated predominantly in the urine.[A187436] However, data regarding the exact proportion is not readily available.

Pregnancy & Breastfeeding use

Pregnancy category C. Corticosteroids should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.

Use in nursing mother: Systemically administered corticosteroids appear in human milk and could suppress growth, interfere with endogenous corticosteroid production, or cause other untoward effects. Because of the potential for serious adverse reactions in nursing infants from corticosteroids, a decision should be made whether to continue nursing or discontinue the drug, taking into account the importance of the drug to the mother.

Contraindication

Nositrol is contraindicated in severe systemic fungal infections and patients with known hypersensitivity to any component of this product.

Special Warning

Use in elderly patients: Clinical studies were not done in patients’ aged 65 and above. In general dose selection for an elderly patients should be cautious, usually starting at the low end of the dosing range.

Storage Condition

Store at 15-30°C.

Innovators Monograph

You find simplified version here Nositrol

Nositrol contains Hydrocortisone see full prescribing information from innovator Nositrol Monograph, Nositrol MSDS, Nositrol FDA label

FAQ

What is Nositrol used for?

Nositrol topical is used to treat redness, swelling, itching, and discomfort of various skin conditions.It can also be used as hormone replacement for people who do not have enough of the natural stress hormone, cortisol. Uses include conditions such as adrenocortical insufficiency, adrenogenital syndrome, high blood calcium, thyroiditis, rheumatoid arthritis, dermatitis, asthma, and COPD. It is the treatment of choice for adrenocortical insufficiency.

How safe is Nositrol?

Mild Nositrol treatments are very safe. Most people do not have any side effects when they use them for less than 4 weeks. Some people get a burning or stinging feeling for a few minutes when they put the Nositrol on their skin. This stops happening after you've been using it for a few days.

How does Nositrol work?

Nositrol works by calming down your body's immune response to reduce pain, itching and swelling (inflammation).

What are the common side effects of Nositrol?

The most common side effects of Nositrol tablets are feeling dizzy, headaches, swollen ankles and feeling weak or tired. Taking hydrocortisone tablets can affect your immune system so you're more likely to get infections.

Is Nositrol safe during pregnancy?

Nositrol should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. Topical corticosteroids should not be used extensively on pregnant patients, in large amounts or for extended periods of time.

Is Nositrol safe during breastfeeding?

Nositrol creams that you buy from a pharmacy can be used while you're breastfeeding. As a precaution, if you're breastfeeding, wash off any cream you put on your breasts before feeding your baby. Nositrol butyrate is not normally recommended for breastfeeding women.

Can I drink alcohol with Nositrol?

Yes, you can drink alcohol while taking Nositrol tablets. However, if Nositrol tablets make you feel dizzy, it's a good idea not to drink alcohol as it will make you feel worse.

When is the best time to take Nositrol?

Take the tablets just after eating a meal, or alternatively with a snack. It is usual to take one dose a day, 30 minutes before your breakfast.

How long does Nositrol take to work?

Your skin should start to get better after using Nositrol for a few days. If you're using a treatment you've bought from a pharmacy or shop, speak to your doctor if you still have symptoms after 1 week, or if your skin gets worse at any time.

Does Nositrol work instantly?

Nositrol shots start to work very quickly.

Can I take Nositrol for a long time?

For long-term skin problems such as eczema and psoriasis you may need to use Nositrol for longer. To reduce the risk of side effects your doctor may recommend that you only use Nositrol for a few weeks at a time. Once your skin is better, use moisturisers to keep it from becoming inflamed again.

Does Nositrol weaken the immune system?

Nositrol can weaken your body's response to infection because the drug weakens your immune system. Using this medication may also make it harder for you to know that you have an infection.

What happens when I stop taking Nositrol?

Do not stop taking Nositrol without talking to your doctor. Stopping Nositrol abruptly can cause loss of appetite, an upset stomach, vomiting, drowsiness, confusion, headache, fever, joint and muscle pain, peeling skin, and weight loss.

Can Nositrol make my gain weight?

Most doctors will say that the low doses of Nositrol given for cortisol replacement do not cause weight gain or increase in appetite.

Does Nositrol make me tired?

The most common side effects of Nositrol tablets are feeling dizzy, headaches, swollen ankles and feeling weak or tired.

What happen if I take too much Nositrol?

An overdose of Nositrol is not expected to produce life threatening symptoms. Long term use of high doses can lead to thinning skin, easy bruising, changes in body fat, increased acne or facial hair, menstrual problems, impotence, or loss of interest in sex.

What happen If I missed dose of Nositrol?

If you forget to take a dose, take it as soon as you remember. If you do not remember until the next dose is due, skip the missed dose. Never take 2 doses to make up for a forgotten one.

Does Nositrol make me sleepy?

Nositrol oral tablet doesn't cause drowsiness, but it can cause other side effects.

Does Nositrol help acne?

People often use Nositrol for any skin condition that causes redness and swelling, such as allergies, illness, injury, or acne. Topical Nositrol is not an official acne medication. It doesn't kill the bacteria that causes acne and it won't prevent breakouts.

Does Nositrol cause anxiety?

This study found that acute Nositrol increased anxiety without affecting fear.

Who should not take Nositrol?

You should not use Nositrol if you have a fungal infection anywhere in your body.
Tell your doctor about any illness or infection you have had within the past several weeks.

Does Nositrol clear eczema?

Nositrol  cream is one of the most common eczema treatments. It can help reduce the itching and swelling of eczema flare-ups.

*** Taking medicines without doctor's advice can cause long-term problems.
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