HELESTENE CHRONODOSE

Betamethasone Sodium Phosphate and Betamethasone Acetate Injectable Suspension, USP is a sterile aqueous suspension containing betamethasone 3 mg per milliliter as betamethasone sodium phosphate, and betamethasone acetate 3 mg per milliliter.

Inactive ingredients per mL: dibasic sodium phosphate 7.1 mg; monobasic sodium phosphate 3.4 mg; edetate disodium 0.1 mg; and benzalkonium chloride 0.2 mg as a preservative.

The pH is adjusted to between 6.8 and 7.2.

The formula for betamethasone sodium phosphate is C 22 H 28 FNa 2 O 8 P and it has a molecular weight of 516.40.

Chemically, it is 9-Fluoro-11β,17,21-trihydroxy-16β-methylpregna-1,4-diene-3,20-dione 21-(disodium phosphate).

The formula for betamethasone acetate is

C 24 H 31 FO and it has a molecular weight of 434.50.

Chemically, it is 9-Fluoro-11β,17,21-trihydroxy-16β-methylpregna-1,4-diene-3,20-dione 21-acetate.

The chemical structures for betamethasone sodium phosphate and betamethasone acetate are as follows: Betamethasone sodium phosphate is a white to practically white, odorless powder, and is hygroscopic.

It is freely soluble in water and in methanol, but is practically insoluble in acetone and in chloroform.

Betamethasone acetate is a white to creamy white, odorless powder that sinters and resolidifies at about 165ºC, and remelts at about 200ºC to 220ºC with decomposition.

It is practically insoluble in water, but freely soluble in acetone, and is soluble in alcohol and in chloroform. betamethasone sodium phosphate betamethasone acetate.

Seasonal allergic

Rhinitis after failure of other therapies (generally antihistamine, intranasal corticosteroid or short-dose corticosteroid).

• Antenatal prevention of hyaline membrane disease: induction of fetal maturation.

These are those of local corticosteroids, when the condition justifies a high local concentration.

Any prescription of local injection must be part of the infectious danger, especially of the risk of promoting bacterial proliferation.

• dermatological: cheloid scars.

• ENT: intra-sinusal irrigations in subacute or chronic sinusitis justifying drainage.

• rheumatological: o intra-articular injections: inflammatory arthritis, o oarthrosis in the thrust o peri-articular injections: tendinitis, bursitis o soft injections: tallalgia, carpal canal syndrome, Dupuytren's disease.

(Accuracy is attracted to sportsmen, this specialty containing an active ingredient that may induce a positive reaction of tests performed during anti-doping tests.

Rare cases of anaphylactoid/anaphylaxis reactions with potential shock have occurred in patients treated with parenteral corticosteroids.

Appropriate precautions should be taken in patients who have already experienced allergic reactions to corticosteroids.

A crisis of pheochromocytoma, which may be fatal, has been reported after administration of systemic corticosteroids.

Corticosteroids should not be administered to patients for whom the presence of a pheochromocytoma is suspected or proven only after an appropriate assessment of the benefit/risk ratio.

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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 anti-inflammatory effects in disorders of many organ systems.

A derivative of prednisolone, betamethasone has a 16β-methyl group that enhances the anti-inflammatory action of the molecule and reduces the sodium.

• and water-retaining properties of the fluorine atom bound at carbon 9.

Betamethasone sodium phosphate, a soluble ester, provides prompt activity, while betamethasone acetate is only slightly soluble and affords sustained activity.

Pharmacotherapeutic group: non-associated systemic corticosteroids, ATC code: H02AB01.

Physiological glucocorticoids (cortisone and hydrocortisone) are essential metabolic hormones.

Synthetic corticosteroids, including betamethasone, are used primarily for their anti-inflammatory effect.

At high doses, they decrease the immune response.

Their metabolic and sodium retention effect is less than that of hydrocortisone.

Treatment of acute overdose is by supportive and symptomatic therapy.

For chronic overdosage in the face of severe disease requiring continuous steroid therapy, the dosage of the corticosteroid may be reduced only temporarily, or alternate day treatment may be introduced.

Betamethasone Sodium Phosphate and Betamethasone Acetate Injectable Suspension should not be administered intravenously.

Serious Neurologic Adverse Reactions with Epidural Administration Serious neurologic events, some resulting in death, have been reported with epidural injection of corticosteroids.

Specific events reported include, but are not limited to, spinal cord infarction, paraplegia, quadriplegia, cortical blindness, and stroke.

These serious neurologic events have been reported with and without use of fluoroscopy.

The safety and effectiveness of epidural administration of corticosteroids have not been established, and corticosteroids are not approved for this use.

Rare instances of anaphylactoid reactions have occurred in patients receiving corticosteroid therapy See ADVERSE REACTIONS.

In patients on corticosteroid therapy subjected to any unusual stress, hydrocortisone or cortisone is the drug of choice as a supplement during and after the event.

Average and large doses of corticosteroids can cause elevation of blood pressure, salt and water retention, and increased excretion of potassium.

These effects are less likely to occur with the synthetic derivatives except when used in large doses.

Dietary salt restriction and potassium supplementation may be necessary.

All corticosteroids increase calcium excretion.

Literature reports suggest an apparent association between use of corticosteroids and left ventricular free wall rupture after a recent myocardial infarction; therefore, therapy with corticosteroids should be used with great caution in these patients.

Corticosteroids can produce reversible hypothalamic pituitary adrenal (HPA) axis suppression with the potential for glucocorticosteroid insufficiency after withdrawal of treatment.

Metabolic clearance of corticosteroids is decreased in hypothyroid patients and increased in hyperthyroid patients.

Changes in thyroid status of the patient may necessitate adjustment in dosage.

Infections General Patients who are on corticosteroids are more susceptible to infections than are healthy individuals.

There may be decreased resistance and inability to localize infection when corticosteroids are used.

Infection with any pathogen (viral, bacterial, fungal, protozoan, or helminthic) in any location of the body may be associated with the use of corticosteroids alone or in combination with other immunosuppressive agents.

These infections may be mild to severe.

With increasing doses of corticosteroids, the rate of occurrence of infectious complications increases.

Corticosteroids may also mask some signs of current infection.

Infections ​​​Corticosteroids may exacerbate systemic fungal infections and therefore should not be used in the presence of such infections unless they are needed to control drug reactions.

There have been cases reported in which concomitant use of amphotericin B and hydrocortisone was followed by cardiac enlargement and congestive heart failure.

Latent disease may be activated or there may be an exacerbation of intercurrent infections due to pathogens, including those caused by Amoeba, Candida, Cryptococcus, Mycobacterium, Nocardia, Pneumocystis, and Toxoplasma.

It is recommended that latent amebiasis or active amebiasis be ruled out before initiating corticosteroid therapy in any patient who has spent time in the tropics or in any patient with unexplained diarrhea.

Similarly, corticosteroids should be used with great care in patients with known or suspected Strongyloides (threadworm) infestation.

In such patients, corticosteroid-induced immunosuppression may lead to Strongyloides hyperinfection and dissemination with widespread larval migration, often accompanied by severe enterocolitis and potentially fatal gram-negative septicemia.

Corticosteroids should not be used in cerebral malaria.

Tuberculosis ​ The use of corticosteroids in active tuberculosis should be restricted to those cases of fulminating or disseminated tuberculosis in which the corticosteroid is used for the management of the disease in conjunction with an appropriate antituberculous regimen.

If corticosteroids are indicated in patients with latent tuberculosis or tuberculin reactivity, close observation is necessary as reactivation of the disease may occur.

During prolonged corticosteroid therapy, these patients should receive chemoprophylaxis.

Administration of live or live, attenuated vaccines is contraindicated in patients receiving immunosuppressive doses of corticosteroids.

Killed or inactivated vaccines may be administered.

However, the response to such vaccines cannot be predicted.

Immunization procedures may be undertaken in patients who are receiving corticosteroids as replacement therapy, e.g., for Addison’s disease.

Infections Chickenpox and measles can have a more serious or even fatal course in pediatric and adult patients on corticosteroids.

In pediatric and adult patients who have not had these diseases, particular care should be taken to avoid exposure.

The contribution of the underlying disease and/or prior corticosteroid treatment to the risk is also not known.

If exposed to chickenpox, prophylaxis with varicella zoster immune globulin (VZIG) may be indicated.

If exposed to measles, prophylaxis with immunoglobulin (IG) may be indicated.

If chickenpox develops, treatment with antiviral agents should be considered.

Reports of severe medical events have been associated with the intrathecal route of administration See ADVERSE REACTIONS, Gastrointestinal and Neurologic/Psychiatric sections.

Results from one multicenter, randomized, placebo-controlled study with methylprednisolone hemisuccinate, an IV corticosteroid, showed an increase in early mortality (at 2 weeks) and late mortality (at 6 months) in patients with cranial trauma who were determined not to have other clear indications for corticosteroid treatment.

High doses of corticosteroids, including Betamethasone Sodium Phosphate and Betamethasone Acetate Injectable Suspension, should not be used for the treatment of traumatic brain injury.

Use of corticosteroids may produce posterior subcapsular cataracts, glaucoma with possible damage to the optic nerves, and may enhance the establishment of secondary ocular infections due to bacteria, fungi, or viruses.

The use of oral corticosteroids is not recommended in the treatment of optic neuritis and may lead to an increase in the risk of new episodes.

Corticosteroids should not be used in active ocular herpes simplex.

Betamethasone Sodium Phosphate and Betamethasone Acetate Injectable Suspension is contraindicated in patients who are hypersensitive to any components of this product.

Intramuscular corticosteroid preparations are contraindicated for idiopathic thrombocytopenic purpura.

Benzyl alcohol as a preservative has been associated with a fatal “Gasping Syndrome” in premature infants and infants of low birth weight.

Solutions used for further dilution of this product should be preservative-free when used in the neonate, especially the premature infant.

The initial dosage of parenterally administered Betamethasone Sodium Phosphate and Betamethasone Acetate Injectable Suspension may vary from 0.25 to 9 mg per day depending on the specific disease entity being treated.

However, in certain overwhelming, acute, life-threatening situations, administrations in dosages exceeding the usual dosages may be justified and may be in multiples of the oral dosages.

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.

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 the corticosteroid 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.

In the treatment of acute exacerbations of multiple sclerosis, daily doses of 30 mg of betamethasone for a week followed by 12 mg every other day for 1 month are recommended.

In pediatric patients, the initial dose of betamethasone may vary depending on the specific disease entity being treated.

The range of initial doses is 0.02 to 0.3 mg/kg/day in three or four divided doses (0.6 to 9 mg/m 2 bsa/day).

For the purpose of comparison, the following is the equivalent milligram dosage of the various glucocorticoids: Cortisone, 25 Triamcinolone, 4 Hydrocortisone, 20 Paramethasone, 2 Prednisolone, 5 Betamethasone, 0.75 Prednisone, 5 Dexamethasone, 0.75 Methylprednisolone, 4 These dose relationships apply only to oral or intravenous administration of these compounds.

When these substances or their derivatives are injected intramuscularly or into joint spaces, their relative properties may be greatly altered.

If coadministration of a local anesthetic is desired, Betamethasone Sodium Phosphate and Betamethasone Acetate Injectable Suspension may be mixed with 1% or 2% lidocaine hydrochloride, using the formulations which do not contain parabens.

Similar local anesthetics may also be used.

Diluents containing methylparaben, propylparaben, phenol, etc., should be avoided, since these compounds may cause flocculation of the steroid.

The required dose of Betamethasone Sodium Phosphate and Betamethasone Acetate Injectable Suspension is first withdrawn from the vial into the syringe.

The local anesthetic is then drawn in, and the syringe shaken briefly.

Do not inject local anesthetics into the vial of Betamethasone Sodium Phosphate and Betamethasone Acetate Injectable Suspension.

Bursitis, Tenosynovitis, Peritendinitis In acute subdeltoid, subacromial, olecranon, and prepatellar bursitis, one intrabursal injection of 1 mL Betamethasone Sodium Phosphate and Betamethasone Acetate Injectable Suspension can relieve pain and restore full range of movement.

Several intrabursal injections of corticosteroids are usually required in recurrent acute bursitis and in acute exacerbations of chronic bursitis.

Partial relief of pain and some increase in mobility can be expected in both conditions after one or two injections.

Chronic bursitis may be treated with reduced dosage once the acute condition is controlled.

In tenosynovitis and tendinitis, three or four local injections at intervals of to 2 weeks between injections are given in most cases.

Injections should be made into the affected tendon sheaths rather than into the tendons themselves.

In ganglions of joint capsules and tendon sheaths, injection of 0.5 mL directly into the ganglion cysts has produced marked reduction in the size of the lesions.

Following intra-articular administration of 0.5 to 2 mL of Betamethasone Sodium Phosphate and Betamethasone Acetate Injectable Suspension, relief of pain, soreness, and stiffness may be experienced.

Duration of relief varies widely in both diseases.

Intra-articular Injection of Betamethasone Sodium Phosphate and Betamethasone Acetate Injectable Suspension is well tolerated in joints and periarticular tissues.

There is virtually no pain on injection, and the “secondary flare” that sometimes occurs a few hours after intra-articular injection of corticosteroids has not been reported with Betamethasone Sodium Phosphate and Betamethasone Acetate Injectable Suspension.

Using sterile technique, a 20.

• to 24-gauge needle on an empty syringe is inserted into the synovial cavity and a few drops of synovial fluid are withdrawn to confirm that the needle is in the joint.

The aspirating syringe is replaced by a syringe containing Betamethasone Sodium Phosphate and Betamethasone Acetate Injectable Suspension and injection is then made into the joint.

Recommended Doses for Intra-articular Injection Size of Joint Location Dose (mL) Very Large Hip 1.

• 2 Large Knee, ankle, shoulder 1 Medium Elbow, wrist 0.5.

• 1 Small (metacarpophalangeal, interphalangeal, sternoclavicular) Hand, chest 0.25 to 0.5 A portion of the administered dose of Betamethasone Sodium Phosphate and Betamethasone Acetate Injectable Suspension is absorbed systemically following intra-articular injection.

In patients being treated concomitantly with oral or parenteral corticosteroids, especially those receiving large doses, the systemic absorption of the drug should be considered in determining intra-articular dosage.

In intralesional treatment, 0.2 mL/cm of Betamethasone Sodium Phosphate and Betamethasone Acetate Injectable Suspension is injected intradermally (not subcutaneously) using a tuberculin syringe with a 25-gauge, 1/2-inch needle.

Care should be taken to deposit a uniform depot of medication intradermally.

A total of no more than 1 mL at weekly intervals is recommended.

Disorders of the Foot A tuberculin syringe with a 25-gauge, 3/4-inch needle is suitable for most injections into the foot.

The following doses are recommended at intervals of 3 days to a week.

Diagnosis Betamethasone Sodium Phosphate and Betamethasone Acetate Injectable Suspension Dose (mL) Bursitis under heloma durum or heloma molle 0.25 to 0.5 under calcaneal spur 0.5 over hallux rigidus or digiti quinti varus 0.5 Tenosynovitis, periostitis of cuboid 0.5 Acute gouty arthritis 0.5 to 1.

Kit supplied as: 1 Kit NDC 80425-0347-01 Betamethasone Sodium Phosphate and Betamethasone Acetate Injectable Suspension, USP, 5 mL multiple dose vial; box of one: NDC 0517-0720-01 SHAKE WELL BEFORE USING.

Store at 20°C to 25°C (68°F to 77°F); excursions permitted to 15° to 30°C (59° to 86°F) .

Protect from light.

Rx only AMERICAN

SHIRLEY, NY 11967 Revised September 2015 Distributed by Advanced Rx Pharmacy of Tennessee, LLC.

Corticosteroids have been shown to be teratogenic in many species when given in doses equivalent to the human dose.

Animal studies in which corticosteroids have been given to pregnant mice, rats, and rabbits have yielded an increased incidence of cleft palate in the offspring.

There are no adequate and well-controlled studies in pregnant women.

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

Infants born to mothers who have received corticosteroids during pregnancy should be carefully observed for signs of hypoadrenalism.

Systemically administered corticosteroids appear in human milk and could suppress growth, interfere with endogenous corticosteroid production, or cause other untoward effects.

Caution should be exercised when corticosteroids are administered to a nursing woman.

The efficacy and safety of corticosteroids in the pediatric population are based on the well-established course of effect of corticosteroids, which is similar in pediatric and adult populations.

Published studies provide evidence of efficacy and safety in pediatric patients for the treatment of nephrotic syndrome (> 2 years of age), and aggressive lymphomas and leukemias (> 1 month of age).

Other indications for pediatric use of corticosteroids, e.g., severe asthma and wheezing, are based on adequate and well-controlled trials conducted in adults, on the premises that the course of the diseases and their pathophysiology are considered to be substantially similar in both populations.

The adverse effects of corticosteroids in pediatric patients are similar to those in adults See ADVERSE REACTIONS.

Like adults, pediatric patients should be carefully observed with frequent measurements of blood pressure, weight, height, intraocular pressure, and clinical evaluation for the presence of infection, psychosocial disturbances, thromboembolism, peptic ulcers, cataracts, and osteoporosis.

Pediatric patients who are treated with corticosteroids by any route, including systemically administered corticosteroids, may experience a decrease in their growth velocity.

This negative impact of corticosteroids on growth has been observed at low systemic doses and in the absence of laboratory evidence of HPA axis suppression (i.e., cosyntropin stimulation and basal cortisol plasma levels).

Growth velocity may therefore be a more sensitive indicator of systemic corticosteroid exposure in pediatric patients than some commonly used tests of HPA axis function.

The linear growth of pediatric patients treated with corticosteroids should be monitored, and the potential growth effects of prolonged treatment should be weighed against clinical benefits obtained and the availability of treatment alternatives.

In order to minimize the potential growth effects of corticosteroids, pediatric patients should be titrated to the lowest effective dose.

No overall differences in safety or effectiveness were observed between elderly subjects and younger subjects, and other reported clinical experience has not identified differences in responses between the elderly and young patients, but greater sensitivity of some older individuals cannot be ruled out.