I-Splone

I-Splone Uses, Dosage, Side Effects, Food Interaction and all others data.

Prednisolone decreases inflammation by inhibition of migration of polymorphonuclear leukocytes and reversal of increased capillary permeability. It suppresses the immune system by reducing the activity and production of the lymphocytes and eosinophils.

Corticosteroids bind to the glucocorticoid receptor, inhibiting pro-inflammatory signals, and promoting anti-inflammatory signals. Prednisolone acetate has a short duration of action as the half life is 2-3 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 I-Splone
Generic Prednisolone Acetate
Prednisolone Acetate Other Names Prednisolone acetate
Weight 5mg
Type Tablet
Formula C23H30O6
Weight Average: 402.4807
Monoisotopic: 402.204238692
Protein binding

The active metabolite, prednisolone, is 70-90% protein bound in plasma.

Groups Approved, Vet approved
Therapeutic Class Glucocorticoids
Manufacturer Indo Bangla Pharmaceutical
Available Country Bangladesh
Last Updated: September 19, 2023 at 7:00 am
I-Splone
I-Splone

Uses

Prednisolone eye drops is used for the treatment of steroid-responsive inflammation of the palpebral and bulbar conjunctiva, cornea and anterior segment of the globe.

Prednisolone tablet, Injection is used forAllergy and anaphylaxis: bronchial asthma, drug hypersensitivity reactions, serum sickness, angioneurotic oedema, anaphylaxis.

Respiratory disease: allergic pneumonitis, asthma, occupational asthma, pulmonary aspergillosis, pulmonary fibrosis, pulmonary alveolitis, aspiration of foreign body, aspiration of stomach contents, pulmonary sarcoid, drug induced lung disease, adult respiratory distress syndrome, spasmodic croup.

Rheumatic disorders: rheumatoid arthritis, polymyalgia rheumatica, juvenile chronic arthritis, systemic lupus erythematosus, dermatomyositis, mixed connective tissue disease.

Arteritis/collagenosis: giant cell arteritis/polymyalgia rheumatica, mixed connective tissue disease, polyarteritis nodosa, polymyositis.

Blood disorders: haemolytic anaemia (auto-immune), leukaemia (acute and chronic lymphocytic), lymphoma, multiple myeloma, idiopathic thrombocytopenic purpura.

Cardiovascular disorders: post-myocardial infarction syndrome, rheumatic fever with severe carditis.

Endocrine disorders: primary and secondary adrenal insufficiency, congenital adrenal hyperplasia.

Gastro-intestinal disorders: Crohn's disease, ulcerative colitis, persistent coeliac syndrome (coeliac disease unresponsive to gluten withdrawal), auto-immune chronic active hepatitis, multisystem disease affecting liver, biliary peritonitis.

Infections (with appropriate chemotherapy): helminthic infestations, Herxheimer reaction, infectious mononucleosis, miliary tuberculosis, mumps orchitis (adult), tuberculous meningitis, rickettsial disease.

Muscular disorders: polymyositis, dermatomyositis.

Neurological disorders: infantile spasms, Shy-Drager syndrome, sub-acute demyelinating polyneuropathy.

Ocular disease: scleritis, posterior uveitis, retinal vasculitis, pseudo-tumours of the orbit, giant cell arteritis, malignant ophthalmic Graves disease.

Renal disorders: lupus nephritis, acute interstitial nephritis, minimal change glomerulonephritis.

Skin disorders: pemphigus vulgaris, bullous pemphigoid, systemic lupus erythematosus, pyoderma gangrenosum.

Miscellaneous: sarcoidosis, hyperpyrexia, Behçets disease, immunosuppression in organ transplantation.

Prednisolone is used for the treatment of steroid-responsive inflammation of the palpebral and bulbar conjunctiva, cornea and anterior segment of the globe.

I-Splone is also used to associated treatment for these conditions: Inflammation, Inflammatory Conditions, Ocular Infections, Irritations and Inflammations, Ocular Inflammation, Organ Transplant Rejection

How I-Splone 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

I-Splone dosage

The initial dosage of Prednisolone may vary from 5 mg to 60 mg daily depending on the disorder being treated. Divided daily dosage is usually used.

The appropriate individual dose must be determined by trial and error and must be re-evaluated regularly according to activity of the disease.

In general, initial dosage shall be maintained or adjusted until the anticipated response is observed. The dose should be gradually reduced until the lowest dose, which will maintain an adequate clinical response is reached.

During prolonged therapy, dosage may need to be temporarily increased during periods of stress or during exacerbations of the disease. When the drug is to be stopped, it must be withdrawn gradually and not abruptly.

Intermittent dosage regimen: A single dose of Prednisolone in the morning on alternate days or at longer intervals is acceptable therapy for some patients. When this regimen is practical, the degree of pituitary-adrenal suppression can be minimized.

Use in children: Corticosteroids cause growth retardation in infancy, childhood and adolescence, which may be irreversible. Treatment should be administered where possible as a single dose on alternate days.

Specific dosage guidelines-

Allergic and skin disorders: initial doses of 5-15 mg daily are commonly adequate.

Collagenosis: Initial doses of 20-30 mg daily are frequently effective. Those with more severe symptoms may require higher doses.

Rheumatoid arthritis: The usual initial dose is 10-15 mg daily. The lowest daily maintenance dose compatible with tolerable symptomatic relief is recommended.

Blood disorders and lymphoma: An initial daily dose of 15-60 mg is often necessary with reduction after an adequate clinical or haematological response. Higher doses may be necessary to induce remission in acute leukaemia.

Adult: Instill one drop into the conjunctival sac two to four times daily. During the initial 24 to 48 hours, the dosing frequency may be increased if necessary. Care should be taken not to discontinue the therapy before completing the course. 

Paediatri: Safety and effectiveness in pediatric patients have not been established.

Side Effects

Elevation of intraocular pressure (IOP) with possible development of glaucoma and infrequent optic nerve damage, posterior subcapsular cataract formation and delayed wound healing.  Fungal and viral infections of the cornea are particularly may develop coincidentally with long-term applications of steroid.

General side-effects include leucocytosis, hypersensitivity including anaphylaxis, thromboembolism, nausea, and malaise.

Toxicity

The oral LD50 of prednisolone acetate in mice is 1680 mg/kg. Patients experiencing an overdose of oral prednisolone acetate may experience an increased severity in the adverse effects of corticosteroids. Overdose of oral prednisolone acetate 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.

Precaution

Shake the bottle well before use. Prolonged use of corticosteroids may result in damage to the optic nerve and defects in vision. If this product is used for longer period of time, intraocular pressure should be routinely monitored.

Caution is necessary when oral corticosteroids, including Prednisolone, are prescribed in patients with the following conditions like-Tuberculosis, Hypertension, Congestive heart failure, Liver failure, Renal insufficiency, Diabetes mellitus or in those with a family history of diabetes, Osteoporosis, Patients with a history of severe affective disorders and particularly those with a previous history of steroid-induced psychoses, Epilepsy, Peptic ulceration, Previous Steroid Myopathy. 

Undesirable effects may be minimized by using the lowest effective dose for the minimum period and by administering the daily requirement as a single morning dose on alternate days. Frequent patient review is required to titrate the dose appropriately against disease activity.

Interaction

Hepatic microsomal enzyme inducers: Drugs which can cause liver enzyme induction such as phenobarbitone, phenytoin, rifampicin, rifabutin, carbamazepine, primidone and aminoglutethimide may reduce the therapeutic efficacy of corticosteroids by increasing the rate of metabolism. 

Non-steroidal anti-inflammatory drugs: Concomitant administration of ulcerogenic drugs such as indomethacin during corticosteroid therapy may increase the risk of Gl ulceration. 

Anticoagulants: Response to anticoagulants may be reduced or, less often, enhanced by corticosteroids. 

Vaccines: Live vaccines should not be given to individuals with impaired immune responsiveness. The antibody response to other vaccines may be diminished. 

Oestrogens: Oestrogens may potentiate the effects of glucocorticoids and dosage adjustment may be required if oestrogens are added to or withdrawn from a stable dosage regimen. 

Other: The desired effects of hypoglycaemic agents (including insulin), anti-hypertensives and diuretics are antagonised by corticosteroids and the hypokalaemic effect of acetazolamide, loop diuretics, thiazide diuretics and carbenoxolone are enhanced.

Food Interaction

  • Avoid excessive or chronic alcohol consumption. Alcohol may cause gastric irritation.
  • Take with food. Food reduces gastrointestinal irritation.

Volume of Distribution

The volume of distribution of the active metabolite, prednisolone, is 0.22/0.7L/kg.

Elimination Route

Prednisolone acetate oral suspension given at a dose equivalent to 15mg prednisolone has a Cmax of 321.1ng/hr, a Tmaxof 1-2 hours, and an AUC of 1999.4ng*hr/mL. The absorption pharmacokinetics of prednisolone acetate are not significantly different from a comparable dose of prednisolone.

Half Life

Oral prednisolone acetate has a plasma half life of 2-3 hours.

Clearance

Data regarding the clearance of prednisolone acetate is not readily available.

Elimination Route

Prednisolone acetate is predominantly excreted in the urine.

Pregnancy & Breastfeeding use

Pregnancy: I-Splone is pregnancy category C. So, this drug should be used during pregnancy only if clearly needed.

Lactation: Corticosteroids are excreted in small amounts in breast milk and infants of mothers taking pharmacological doses of steroids should be monitored carefully for signs of adrenal suppression.

Contraindication

Prednisolone (Eye drops) is contraindicated in viral diseases of the cornea, conjunctiva and known hypersensitivity to any of the ingredients of Prednisolone (Eye drops) or other corticosteroids.

Systemic infections unless specific anti-infective therapy is employed. Hypersensitivity to any ingredient. Ocular herpes simplex because of possible perforation.

Special Warning

Use in the elderly: Treatment of elderly patients, particularly if long term, should be planned bearing in mind the more serious consequences of the common side effects of corticosteroids in old age, especially osteoporosis, diabetes, hypertension, hypokalemia, susceptibility to infection and thinning of the skin. Close clinical supervision is required to avoid life-threatening reactions.

May need to increase dose in patients with hyperthyroidism to achieve therapeutic effects.

Acute Overdose

A one-time accidental overdose of Prednisolone Ophthalmic Suspension generally will not cause acute problems. Long time overdose may show general side-effects. In accidental overdose sufficient water should be taken to dilute the medication.

Report of acute toxicity and/or death following overdose of glucocorticoids 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 and protect from light. Keep out of the reach of children. Protect from freezing.  Shake well before using.

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FAQ

What is I-Splone used for?

I-Splone is used to treat certain eye conditions due to inflammation or injury. I-Splone works by relieving symptoms such as swelling, redness, and itching. It belongs to a class of drugs known as corticosteroids.

How safe is I-Splone?

Use of this medication for prolonged periods or in high doses may cause serious eye problems.Tell your doctor right away if any of these unlikely but serious side effects occur: vision problems, eye pain.I-Splone may mask the signs of an eye infection.

What are the common side effects of I-Splone?

Common side effects of I-Splone are include:

  • stinging/burning/itching/irritation of the eyes for 1 to 2 minutes when you apply this medication,
  • temporary cloudy vision,
  • increased sensitivity to light,
  • visual disturbance (blurry vision),
  • feeling like something is in your eye, and.
  • allergic reactions.

Is I-Splone safe during pregnancy?

Very little I-Splone in an eye drop form is absorbed into the body and available to affect an unborn baby.I-Splone eye drops are considered safe to use during pregnancy for short periods of time.

Is I-Splone safe during breastfeeding?

Amounts of I-Splone in breastmilk are very low.No adverse effect have been reported in breastfed infants with maternal use of any corticosteroid during breastfeeding.

Can I drink alcohol with I-Splone?

moderate alcohol use may be safe during treatment with I-Splone.

Can I drive after taking I-Splone?

Do not drive, use machinery, or do any activity that requires clear vision until you are sure you can perform such activities safely.

When is the best time to take I-Splone?

It is best to take I-Splone as a single dose once a day, straight after breakfast.

How long does I-Splone take to work for inflammation?

I-Splone generally works very quickly usually within one to four days if the prescribed dose is adequate to reduce your particular level of inflammation. Some people notice the effects ofI-Splone hours after taking the first dose.

Is it better to take prednisone in the morning or at night?

Morning dosages are usually best for I-Splone.
If you are on daily I-Splone, experts recommend taking the dose in the morning, to reduce this risk. Taking I-Splone too late in the evening can cause sleeplessness and insomnia, too.

How often can I use I-Splone?

Adults use one or two drops in the affected eye 2 to 4 times a day. Your doctor may tell you to use the drops more often during the first two days of treatment.

How long is it safe to stay on I-Splone?

Do not stop taking I-Splone if you've been on it for more than 3 weeks or have taken high doses for more than 1 week.

Will I-Splone affect my fertility?

I-Splone can cause reversible decreases in sperm counts and motility, another found no link between steroid treatment and infertility.

What happen If I missed I-Splone?

If you miss a dose, use it as soon as you remember. If it is near the time of the next dose, skip the missed dose. Use your next dose at the regular time. Do not double the dose to catch up.

Can you overdose on I-Splone?

An overdose of I-Splone ophthalmic is not expected to be dangerous. Seek emergency medical attention if anyone has accidentally swallowed the medication.

Can I-Splone affect eyesight?

I-Splone is well known to increase a patient's risk of developing cataract or glaucoma.I-Splone can cause an elevation in eye pressure, which is a major risk factor for developing glaucoma.

Is short term use of I-Splone safe?

When used short-term, I-Splone is generally well-tolerated, and when side effects do occur in this scenario, they usually clear up quickly after treatment ends.

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