Betamethasone is a corticosteroid medicine that has strong anti-inflammatory effects. It is used in autoimmune and inflammatory conditions.

Betamethasone Uses (Indications):

• Intramuscular:

  • Allergic states:

    • It is effective in controlling severe allergic conditions intractable to adequate trials of conventional treatment in asthma, atopic dermatitis, contact dermatitis, drug hypersensitivity reactions, perennial or seasonal allergic rhinitis, serum sickness, transfusion reactions.

  • Dermatologic diseases:

    • It is indicated for various dermatological conditions including bullous dermatitis herpetiformis, exfoliative erythroderma, mycosis fungoides, pemphigus, severe erythema multiforme (Stevens-Johnson syndrome)

  • Endocrine disorders:

    • It is used for the management of congenital adrenal hyperplasia, hypercalcemia in malignancy, nonsuppurative thyroiditis.
    • The drug of choice in primary or secondary adrenocortical insufficiency is hydrocortisone/cortisone. Synthetic analogs can be concurrently used with mineralocorticoids where applicable; in infancy, mineralocorticoid supplementation is of particular importance.

  • Gastrointestinal diseases:

    • It is indicated for the management of regional enteritis and ulcerative colitis.

  • Hematologic disorders:

    • Acquired (autoimmune) hemolytic anemia, Diamond-Blackfan anemia, pure red cell aplasia, selected cases of secondary thrombocytopenia also needs additional therapy.

  • Neoplastic diseases:

    • It is given as palliative treatment of leukemias and lymphomas.

  • Nervous system:

    • Acute exacerbations of multiple sclerosis; cerebral edema secondary to a primary or metastatic brain tumor or craniotomy can be managed by betamethasone.

  • Ophthalmic diseases:

    • Sympathetic ophthalmia, temporal arteritis, uveitis, and ocular inflammatory conditions unresponsive to topical corticosteroids need betamethasone for control.

  • Renal diseases:

    • In patients with idiopathic nephrotic syndrome, in order to induce diuresis or remission of proteinuria or that due to lupus erythematosus, betamethasone is effective.

  • Respiratory diseases:

    • It is given in combination with ATT for fulminating or disseminated pulmonary tuberculosis. It is also used for idiopathic eosinophilic pneumonia, symptomatic sarcoidosis, or berylliosis.

  • Rheumatic disorders:

    • Short term therapy is advised as adjunctive therapy to tide the patient over an acute episode or exacerbation in acute gouty arthritis; acute rheumatic carditis; ankylosing spondylitis; psoriatic arthritis; rheumatoid arthritis, including juvenile rheumatoid arthritis, treatment of dermatomyositis, polymyositis, and systemic lupus erythematosus.

  • Miscellaneous:

    • Trichinosis with neurologic or myocardial involvement, tuberculous meningitis with subarachnoid block or impending block when used with appropriate antituberculous chemotherapy.

  • Intra-articular or soft tissue administration:

    • In order to tide the patient over an acute episode or exacerbation in acute gouty arthritis, acute and subacute bursitis, acute nonspecific tenosynovitis, epicondylitis, rheumatoid arthritis, synovitis of osteoarthritis, it is given as adjunct short term therapy.

  • Intralesional:

    • It is effective for treating keloids, alopecia areata, discoid lupus erythematosus, localized hypertrophic, infiltrated, inflammatory lesions of granuloma annulare, lichen planus, lichen simplex chronicus, and psoriatic plaques, necrobiosis lipoidica diabeticorum.

Off Label Use of Betamethasone in Adults:

• Accelerate fetal lung maturation.

Betamethasone dose in adults:

• Usual dosage range:

  • Initial: 0.25 to 9 mg Intramuscular daily.

Note:

• Dosage is based on severity and patient response and expressed as a combined amount of betamethasone sodium phosphate and betamethasone acetate;
• 1 mg is equivalent to betamethasone sodium phosphate 0.5 mg and betamethasone acetate 0.5 mg.

Betamethasone Indication-specific dosing:

Betamethasone Off label treatment dose of Antenatal fetal maturation:

• 12 mg I/M once daily for a total of 2 doses.
• Women between 24 and 34 weeks of gestation, including those with ruptured membranes or multiple gestations, who are at risk of delivering within 7 days should have a single course of betamethasone.
• Some women in beginning at 23 weeks gestation or late preterm (between 34 0/7 weeks and 36 6/7 weeks gestation) should also have a single course.
• A single repeat course may be considered in some women with pregnancies less than 34 weeks gestation at risk for delivery within 7 days and who had a course of antenatal corticosteroids more than 2 weeks given previously.

Betamethasone dose in the treatment of Bursitis (other than of foot), tenosynovitis, and peritendinitis:

• 3 to 6 mg Intrabursal (0.5 to 1 mL) for one dose.
• Acute exacerbations of chronic conditions need several doses.
• Repeated injections need dose reduction.

Betamethasone dose in dermatological diseases:

• 2 mg/cm² Intralesional (0.2 mL/cm²) for one dose.
• The maximum: 6 mg [1 mL] weekly.

Betamethasone dose in the treatment of Foot disorders:

• 5 mg to 6 mg Intra-articular (0.25 to 1 mL) per dose at 3 to 7-day intervals.

• The dose is based upon condition:

  • Bursitis:

    • 3 -5 mg (0.25 to 0.5 mL).

  • Tenosynovitis:

    • 3 mg (0.5 mL).

  • Acute gouty arthritis:

    • 3-6 mg (0.5 to 1 mL).

Betamethasone dose in the treatment of Multiple sclerosis:

Note: High-dose Intravenous or oral methylprednisolone is required for acute exacerbations of multiple sclerosis.

• 30 mg Intramuscular daily for 1 week, followed by 12 mg every other day for 4 weeks.

Betamethasone dose in the treatment of Rheumatoid and osteoarthritis:

• 3 mg to 12 mg Intra-articular (0.5 to 2 mL) for one dose.

• The dose is based upon the joint size:

  • Very large (eg, hip):

    • 6 to 12 mg (1 to 2 mL).

  • Large (eg, knee, ankle, shoulder):

    • 6 mg (1 mL).

  • Medium (eg, elbow, wrist):

    • 3 mg to 6 mg (0.5 to 1 mL).

  • Small (eg, inter- or metacarpophalangeal, sternoclavicular):

    • 5 mg to 3 mg (0.25 to 0.5 mL).

Betamethasone Dose in Childrens

Note:

• In order to prevent HPA axis suppression, short term therapy with the lowest effective dose should be given.
• The dose depends on severity and patient response.
• Dosages expressed as a combined amount of betamethasone sodium phosphate and betamethasone acetate;
• 1 mg is equivalent to betamethasone sodium phosphate 0.5 mg and betamethasone acetate 0.5 mg.

Betamethasone General dosing in the treatment of inflammatory and allergic conditions:

• Infants, Children, and Adolescents:

  • Initial: 0.02 to 0.3 Intramuscular mg/kg/day (0.6 to 9 mg/m²/day) in 3 or 4 divided doses

Betamethasone Intralesional dose in a larger Infantile hemangioma:

• Infants and Children:

  • Dosage dependent upon the size of lesion:

    • Commonly reported:

      • 6 mg administered as a 6 mg/mL concurrently with triamcinolone injection divided into multiple injections along the lesion perimeter,
      • reported range: 1.5 to 18 mg/dose;
      • doses usually administered every 8 to 14 weeks;
      • reported range: 6 to 25 weeks.

Betamethasone Pregnancy Risk Category: C

• Betamethasone can cross the placenta. It is partially metabolized in the placenta by placental enzymes into an inactive metabolite.
• If steroids are administered in the first trimester, oral clefts and decreased birth weight can be seen.
• However, this information is contradictory and depends on the maternal dose/indication.
• Hypoadrenalism can result from corticosteroid administration during pregnancy.
• It is used for premature membrane rupture in preterm infants or premature labor to induce antenatal fetal lungs maturation.
• Antenatal corticosteroid administration has been shown to decrease the risk of intraventricular hemorhage, necrotizing Enterolitis, neonatal death, and respiratory distress syndrome.
• The single course is recommended for women between 24- and 34 weeks gestation, who are at high risk of giving birth within one week.
• This includes those with ruptured membranes, multiple gestations, or those who have had previous pregnancies.
• It is administered once to women who are pregnant at 23 weeks and at high risk of giving birth within 7 days.
• It is recommended that women between the ages of 34 and 36 7/7 weeks, who are at high risk of preterm birth within 7 days, and have not received corticosteroids before, receive it as a single course. 
• Tocolytics are not recommended as an additional therapy.
• Women with intrauterine infections, multiple gestations, pregestational diabetics, and women who have had a cesarean section previously at term, should not be given late preterm corticosteroids.
• It is not recommended to take multiple courses.
• Women with pregnancies of less than 34 weeks and at high risk of delivery within 7 days are required to receive a single course.
• It is not recommended to use a repeat course for women who have ruptured membranes during pregnancy.
• For the treatment of rheumatic diseases, the lowest effective dose should be administered to a pregnant woman.
• You may also use intra-articular dosing during pregnancy.

Use betamethasone while breastfeeding

• Breast milk contains corticosteroids.
• An antenatal betamethasone treatment can lead to delayed milk production after birth and decreased volume.
• This effect was observed in women who were between 28 and 34 weeks gestation.
• Antenatal steroid therapy does not affect milk production if the birth took place within 3 days or more than 10 days.
• Breastfed babies can experience side effects such as growth suppression when taking maternal steroid therapy.
• Therefore, breastfeeding mothers should not be given betamethasone.
• You can breastfeed while taking corticosteroids, but you must monitor your infant closely for any adverse reactions.

Betamethasone Dose adjustment in renal disease:

No dose adjustments have been recommended by manufacturers in patients with kidney disease.

Betamethasone Dose adjustment in liver disease:

No dose adjustments have been recommended by the manufacturer in patients with liver disease.

Side effects of Betamethasone:

• Cardiovascular:

  • Bradycardia
  • Cardiac Arrhythmia
  • Cardiomegaly
  • Circulatory Shock
  • Edema
  • Embolism (Fat)
  • Hypertension
  • Hypertrophic Cardiomyopathy
  • Myocardial Rupture (Following Recent MI)
  • Syncope
  • Tachycardia
  • Thromboembolism
  • Thrombophlebitis
  • Vasculitis

• Central Nervous System:

  • Abnormal Sensory Symptoms
  • Arachnoiditis
  • Depression
  • Emotional Lability
  • Euphoria
  • Headache
  • Increased Intracranial Pressure
  • Insomnia
  • Malaise
  • Meningitis
  • Myasthenia
  • Neuritis
  • Neuropathy
  • Paraplegia
  • Paresthesia
  • Personality Changes
  • Pseudotumor Cerebri
  • Psychic Disorder
  • Seizure
  • Spinal Cord Compression
  • Vertigo

• Dermatologic:

  • Acne Vulgaris
  • Allergic Dermatitis
  • Atrophic Striae
  • Diaphoresis
  • Ecchymoses
  • Erythema
  • Exfoliation Of Skin
  • Fragile Skin
  • Hyperpigmentation
  • Hypertrichosis
  • Hypopigmentation
  • Skin Atrophy
  • Skin Rash
  • Subcutaneous Atrophy
  • Suppression Of Skin Test Reaction
  • Thinning Hair
  • Urticaria
  • Xeroderma

• Endocrine & Metabolic:

  • Amenorrhea
  • Calcinosis
  • Cushingoid State
  • Decreased Glucose Tolerance
  • Decreased Serum Potassium
  • Fluid Retention
  • Glycosuria
  • Growth Suppression (Pediatric)
  • Hirsutism
  • HPA-Axis Suppression
  • Hypokalemic Alkalosis
  • Impaired Glucose Tolerance/Prediabetes
  • Insulin Resistance (Increased Requirements For Insulin Or Oral Hyperglycemic Agents)
  • Moon Face
  • Negative Nitrogen Balance
  • Protein Catabolism
  • Sodium Retention
  • Weight Gain

• Gastrointestinal:

  • Abdominal Distention
  • Change In Bowel Habits
  • Hiccups
  • Increased Appetite
  • Intestinal Perforation
  • Nausea
  • Pancreatitis
  • Peptic Ulcer
  • Ulcerative Esophagitis

• Genitourinary:

  • Bladder Dysfunction
  • Spermatozoa Disorder (Decreased Motility And Number)

• Hematologic & Oncologic:

  • Petechia

• Hepatic:

  • Hepatomegaly
  • Increased Liver Enzymes

• Hypersensitivity:

  • Anaphylactoid Reaction
  • Anaphylaxis
  • Angioedema

• Infection:

  • Infection (Decreased Resistance)
  • Sterile Abscess

• Local:

  • Injection Site Reaction (Intra-Articular Use).
  • Postinjection Flare (Intra-Articular Use)

• Neuromuscular & Skeletal:

  • Amyotrophy
  • Aseptic Necrosis Of Femoral Head
  • Aseptic Necrosis Of Humeral Head
  • Bone Fracture
  • Charcot Arthropathy
  • Lipotrophy
  • Myopathy
  • Osteoporosis
  • Rupture Of Tendon
  • Steroid Myopathy

• Ophthalmic:

  • Blindness
  • Blurred Vision
  • Cataract
  • Exophthalmos
  • Glaucoma
  • Increased Intraocular Pressure
  • Papilledema

• Respiratory:

  • Pulmonary Edema

• Miscellaneous:

  • Wound Healing Impairment

Contraindications to Betamethasone:

• Hypersensitivity to any ingredient of the formulation
• I/M is not recommended for immune thrombocytopenia, also known as idiopathic-thrombocytopenic purpura.

Canadian labeling: Additional contraindications not in US labeling

• Cerebral malaria
• Vaccinia
• Herpes simplex eyelidus
• Systemic fungal infections
• Use in areas where there is local infection
• There is not much evidence of cross-reactivity between glucocorticoids and allergens. 
• Cross-sensitivity is possible due to similarities in chemical structure and/or drugcologic actions. However, this cannot be ruled out.

Warnings and precautions

• Suppression of the adrenals:
  • Hypercortisolism, or suppression of the hypothalamic-pituitary-adrenal (HPA) axis, can be caused by prolonged therapy or higher doses. This in turn can lead to adrenal crisis.
  • Always withdraw corticosteroids slowly and stop abruptly.
  • Switching from systemic corticosteroids or inhaled products can lead to adrenal insufficiency and/or increased allergic symptoms.
  • Asthmatic patients with inadequate adrenal function can cause fatalities.
  • Prednisone may make adult patients more susceptible if they are taking >20mg of prednisone daily (or an equivalent).
  • Systemic steroids are more effective than aerosol steroids for treating patients with trauma surgery or infection.
  • Patients suffering from suppression of the HPA-axis should be given adequate supplementation with natural steroids rather than betamethasone in stressful situations.

• Anaphylactoid reactions

  • Patients who have received corticosteroids have had rare cases of anaphylactoid reactions.

• Immunosuppression:

  • Extended steroid therapy can increase the risk of secondary infections, masked acute infections (fungal infections), prolongation or exacerbation or limitation of immunity to killed or inactivated vaccinations.
  • Infection exacerbation (may be fatal) or activation of special pathogens such as Amoeba Candida, Cryptococcus Mycobacterium Nocardia Pneumocystis Strongyloides and Toxoplasma may occur.
  • Particularly avoid Amebiasis and Strongyloidesinfections.
  • Ocular herpes easyx should not be treated with steroids. Avoid exposure to chickenpox and measles.
  • Steroids should not be used to treat viral hepatitis and cerebral malaria fungal infections.
  • Patients with latent tuberculosis and reactivated TB should be closely monitored.
  • Avoid steroid use in active TB. Only fulminating and disseminated TB should be treated with antituberculosis medication.
  • Before starting corticosteroids, it is important to rule out amoebiasis in patients who have recently traveled to tropical climates or undiagnosed diarrhea.

• Kaposi Sarcoma:

  • Kaposi's Sarcoma may develop when you are on prolonged corticosteroid therapy. This warrants withdrawal.

• Myopathy

  • Patients with neuromuscular transmission disorder may experience acute myopathy if they are exposed to high-dose corticosteroids. This can affect the eyes and/or the respiratory muscles.
  • Recovery may be delayed if creatine kinase levels are not monitored.

• Psychiatric disorders:

  • Steroids can cause depression, euphoria and insomnia as well as mood swings, personality changes, and mood swings.
  • Corticosteroid treatment can worsen pre-existing mental conditions.

• Cardiovascular disease

  • Systemic steroids can cause fluid retention and electrolyte disturbances, so it is important to be cautious when using them in hypertension or heart failure.
  • It is possible to make dietary changes.
  • Steroid therapy may cause left ventricular wall rupture. Patients with MI should be careful.

• Diabetes:

  • Glucose production/regulation can be altered with steroids resulting in hyperglycemia, therefore it should be cautiously used in patients with DM.

• Gastrointestinal Disease:

  • Patients with GI diseases such as diverticulitis, fresh intestinal anastomoses and peptic ulcerative colitis are at greater risk of perforation.
  • Avoiding ethanol can cause irritation of the gastric mucosal.

• Head injury

  • Patients with head injuries can experience increased mortality if they are given high doses of IV methylprednisolone. High-dose corticosteroids should not be used to treat them.

• Hepatic impairment

  • Patients with cirrhosis or hepatic impairment should be cautious about prolonged therapy as it can cause fluid retention.

• Myasthenia gravis:

  • Initial steroid therapy may lead to myasthenia gravis exacerbation, so it is important to be cautious.

• Ocular disease:

  • Steroid therapy for prolonged periods can lead to increased intraocular pressure open angle glaucoma (IOP) and cataracts.
  • It is important to have an ophthalmic examination every other day.
  • Optic neuritis can be treated with this method, but it is not recommended.

• Osteoporosis

  • Extended therapy or high doses of corticosteroid may lead to osteoporotic fractures and increased bone loss.

• Renal impairment

  • Patients with impaired renal function should be cautious when taking steroids.

• Seizure disorders:

  • Seizures can occur in patients with an adrenal crisis.
  • Steroids should not be used in patients who have a history of seizure disorders.

• Thyroid disease:

  • Thyroid status changes can require dose adjustment.
  • The level of steroid metabolic clearance in hyperthyroidism is higher than that in hypothyroidism.

How to administer Betamethasone?

• In order to give suspension along with a local anesthetic, it should be mixed in a syringe with 1% or 2% lidocaine HCl (without parabens) or similar parabens-free local anesthetic.
• The dose of betamethasone suspension should be withdrawn from the vial into the syringe and the local anesthetic should be drawn into the syringe followed by shaking of the syringe.
• The local anesthetic should not be injected directly into the suspension vial.

Intramuscular:

• Injectable sodium phosphate/acetate suspension should not be given Intravenous or epidurally.

Intrabursal:

• Tendinitis tenosynovitis: Inject into affected tendon sheaths (not directly into tendons).

Intradermal:

• A uniform depot should be injected by using a 25-gauge 1 mL (eg tuberculin) syringe with a 1/2 inch needle. It should not be given subcutaneously.

Mechanism of action of Betamethasone:

• Betamethasone can be used to control the rate of protein synthesization. It's responsible for the inhibition of migration polymorphonuclear lymphocytes, and fibroblasts.
• It reverses capillary permeability at the cellular level and lysosomal stability at the cellular level, which prevents or controls inflammation.

Protein binding:

• 64%.

Metabolism:

• Occurs in the liver.

Half-life elimination:

• 6.5 hours.

Time to peak serum:

• Intravenous: 10 to 36 minutes.

Excretion:

• Urine (<5% as unchanged drug).

International Brands of Betamethasone:

• Bei Shi Li
• Betacort
• Betagen
• Betanoid
• Betasone
• Betnelan
• Betnesol
• Bufencon
• Celestan Depot
• Celeston
• Celeston Chronodose
• Celestone
• Celestone Chronodose
• Celestone Soluspan
• Cidoten
• Corteroid
• Cortixyl
• Depot
• Dacam RL
• Diprofos Depot
• Diprophos
• Diprosone Depot
• Diprospan
• Flosetron
• Inflacor
• Lenasone
• Metamar
• Solu Celestan
• Vistamethasone
• Walacort
• X-Beta

Betamethasone Brand Names in Pakistan: