Betamethasone Pharmacology

Betamethasone

About Betamethasone
Potent glucocorticoid, Anti-inflammatory, immunosuppressent.
Mechanism of Action of Betamethasone
The drug exerts it`s pharmacological action by penetrating and binding to cytoplasmic receptor protein and causes a structural change in steroid receptor complex. This structural change allows it`s migration in to the nucleus and then binding to specific sites on the DNA which leads to transcription of specific m-RNA and which ultimately regulates protein synthesis. It exerts highly selective glucocorticoid action. It stimulates the enzymes needed to decrease the inflammatory response.
The drug exerts anti-inflammatory and immunosuppressant actions as follows: - 1) Induce lipocortins in macrophages, endothelium, and fibroblasts which inhibits phospholipase A2 and thus decreases the production of Prostaglandins, leukotriens (LT), and platelet activating factor, 2) Causes negative regulation of genes for cytokines in macrophages, endothelial cells and lymphocytes and thus decreases the production of interleukins (IL-1, IL-2, IL-3, IL-6), TNF-alpha, GM-CSF (granulocyte macrophage colony stimulating factor), Gama interferon and suppresses fibroblast proliferation and T-lymphocyte functions and interferes chemotaxis. 3) Decreases the production of acute phase reactants from macrophages and endothelial cells and interferes complement function. 4) Decreases the production of ELAM-1(Endothelial leukocyte adhesion molecule-1) and ICAM-1(intracellular adhesion molecule-1) in endothelial cells. 5) Inhibit IgE mediated histamine and LT-C4 release from basophiles and the effects of antigen-antibody reaction is not mediated 6) Reduces the production of collagenase and stromolysin and thus prevents tissue destruction.
Pharmacokinets of Betamethasone
Absorption: Well absorbed orally, Distribution: Distributed in to muscle, liver, kidney, skin, and intestine. It crosses the placenta and also secreted in breast milk, Metabolism: Metabolized in liver in to inactive metabolites by glucuronide and sulfate conjugation. Excretion: Metabolites are excreted mainly through urine and a small amount is excreted through faeces.
Topical:-Absorption: It is absorbed in to the systemic circulation and the amount is depending on the potency, amount applied and the nature of the skin at the site of application. Absorption increases at the site of skin damage, inflammation or occlusion
Onset of Action for Betamethasone
N/A
Duration of Action for Betamethasone
3 to 25 days
Half Life of Betamethasone
36 to 54 hours
Side Effects of Betamethasone
1.Susceptibility to infection
2.Peptic ulcer
3.Haemorrhage
4.Glycosuria
5.Hyperglycaemia
6.Osteoporosis
7.Atrophy of adrenal cortex(on prolonged therapy)
8.Suppression of adrenocorticotropic hormone
9.Cushing`s syndrome
10.Inhibition of growth in children
11.Amenorrhoea
12.Behavioral disturbances
13.Thromboembolic disorders
14.Myopathy
15.Weakness
16.Lymphocytopenia
17.Muscle wasting
18.Gastrointestinal discomfort
19.Increased appetite
20.Delayed wound healing
21.Headache
22.Euphoria
23.Insomnia
24.Seizures
25.Heart failure
26.Arrhythmias
27.Posterior sub capsular cataract
28.Glaucoma
29.Hirsutism
30.Increased intracranial pressure.
Topcal:
1.Burning
2.Irritation
3.Dryness
4.Erythema
5.Folliculitis
6.Striae
7.Skin atrophy
8.tching
Contra-indications of Betamethasone
1.Hypersensitivity to the drug
2.Untreated infections
3.Systemic fungal infections
Topical:
1.Hypersensitivity to Betamethasone and other corticosteroids
2.Untreated bacterial, virus or fungal infections
3.Acne vulgaris
4.Peri-oral dermatitis
5.Scabies
6.Leg ulcers
7.Tuberculosis of the skin
8. Varicose ulcers
9. Skin lesions caused by infections with ring worm, fungi (e.g. Candida, Tinea) or bacteria (e.g. impetigo)
10.Discoid lupus Erythematosus
Special Precautions while taking Betamethasone
1.Avoid sudden discontinuation of the drug
2.Use lower dosages as much as possible
3.Concurrent vaccination
4.Ocular herpes simplex
5.Primary glaucoma
6.Peptic ulcer
7.Psychosis
8.Tuberculosis
9.Epilepsy
10.Osteoporsis
11.Congestive heart failure
12.Renal impairment
13.Recent myocardial infarction
14.Heart failure
15.Diabetes mellitus
16.Hypothyroidism
17.Cirrhosis
18.Stress
19.Sepsis
20.Hypertension
21.Myasthenia gravis
22.Hepatic impairment
23.Non specific Ulcerative colitis
24.Diverticulitis
25.Recent intestinal anastomosis
26.Thromboembolic disorders
27.Avid contact of the topical dosage form with the eyes
Pregnancy Related Information
Use with caution
Old Age Related Information
Use with caution
Breast Feeding Related Information
Use with caution
Children Related Information
Use with caution
Neonates: Contraindicated
Indications for Betamethasone
1.Inflammatory conditions
2.Allergic reactions
3.Shock
4.Anaphylaxis
5.Intra-articular and soft tissue inflammation
6.Asthma
7.Rheumatoid arthritis
8.Adrenal insufficiency
9.Tuberculous meningitis
10.Respiratory diseases
11.Malignancies
12.Cerebral oedema
13.Collagen diseases
14.Addison`s disease
15.Simmond`s disease
16.Hypopitutarism following adrenalectomy
17.Taenosynovitis.
Interactions for Betamethasone
Barbiturates: Decrease efficacy of Betamethasone
Carbamazepine, Primidone: Decreases efficacy.
Oral contraceptives: Increase efficacy of Betamethasone.
Oestrogens: Decreases efficacy of Betamethasone.
Ketoconazole: Increases efficacy of Betamethasone.
Rifampicin: Decreases efficacy.
Betamethasone effects the actions of the following:
Anticholinesterases: Efficacy antagonised in myasthenia gravis.
Oral anticoagulants: Altered response.
Cyclosporine: Increases efficacy leading to enhanced toxicity.
Digitals glycosides: Increases toxicity associated with hypokalaemia.
Isoniazid: Decreases serum levels.
Salicylates: Decreases serum levels.
Diuretics: Increases efficacy may cause increased hypokalaemia and increased hyperglycaemia.
Non-depolarising muscle relaxants - Altered response.
Somatrem: Growth promoting effect inhibited.
Theophyllines: Altered response of either agent.
IUCD: Contraceptive failure.
Lab. Tests:
a) Increases serum cholesterol levels.
b) Increases urine glucose levels.
c) Decreases Thyroid l 131 uptake; Decreases T3 serum levels.
d) Decreases serum potassium.
Typical Dosage for Betamethasone
Oral: Starts with 0.5 to 6mg/day. Reduces to minimum effective; maintenance dosage.
Children:
1 to 6 years: 25 to 50%
7 to 12 years: 50 to 75%
I.M. or I.V.: 4 to 20mg I.M. or as slow I.V. injection. Repeated if required; up to 4 times daily depending up on the severity of condition.
Children: Administered by slow I.V. injection;
<1year: 1mg
1 to 5 years: 2mg
6 to 12 years: 4mg
Intra-articular or soft tissue injection: 0.5 to 9mg depending up on the severity of the condition.
Topical:
Betamethasone Valerate: Apply to the affected area as thin film 1 - 4 times daily depending upon the severity, skin and rate of absorption.
Dermatoses of the scalp: (Betamethasone Valerate 0.12%): Small amount of foam is applied in to the scalp with gentle massage 2 times a day for up to 2 weeks.
Betamethasone dipropionate: Apply to the affected area as thin film 1 -2times daily
Schedule of Betamethasone
H
Storage Requirements for Betamethasone
Store at room temperature in a well closed; light resistant container. Protect from excess heat and moisture. Keep out of reach of children.
Effects of Missed Dosage of Betamethasone
Take the missed dose as soon as noticed and if it is the time for next dose then skip the missed dose. Continue the regular schedule. Do not double the dose.
Effects of Overdose of Betamethasone
Provide symptomatic treatment and supportive measures.

Home Delivery for Betamethasone in Your City

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However, we do publish a comprehensive directory of Pharmacies, Chemists and Druggists in cities all over India. You can use this directory to find the medicine stores in your city (or area) that provide home delivery services for betamethasone and other medicines and health products. Home delivery services for betamethasone may be free or they may cost you depending on the pharmacy and the minimum order requirements. It would be best to get this clarified while placing the order.

Please be aware that you should take betamethasone only if a doctor has recommended or prescribed it. Some or all pharmacies who provide a home delivery service for medicines might insist on a prescription for betamethasone before they complete the sale. You can get this information while placing the order for betamethasone with the pharmacy.

Betamethasone is a generic medicine name and there are several brands available for it. Some of the brands for betamethasone might be better known than betamethasone itself. If the pharmacy that's willing to deliver medicines to your home doesn't have betamethasone in stock, you can ask for one of the branded alternatives for betamethasone.