Last Updated on June 3, 2023
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What is Betamethasone?
The active ingredient Betamethasone is a synthetic cortisol-derivative (a glucocorticoid or corticosteroid). It has anti-inflammatory and anti-allergic and suppresses the immune system. They are used in numerous diseases, both chronic and acute. Here you can read everything of interest to the effect of Betamethasone, side effects and use.
GCS. Suppresses the function of white blood cells and tissue macrophages. Limits the migration of leukocytes to the area of inflammation. Violates the ability of macrophages to phagocytosis, as well as to the formation of interleukin-1. Promotes the stabilization of lysosomal membranes, thereby reducing the concentration of proteolytic enzymes in the area of inflammation. Reduces the permeability of capillaries due to the release of histamine. Suppresses the activity of fibroblasts and the formation of collagen.
Inhibits the activity of phospholipase A2, which leads to suppression of the synthesis of prostaglandins and leukotrienes. Suppresses the release of COX (mainly COX-2), which also contributes to a decrease in the production of prostaglandins.
Reduces the number of circulating lymphocytes (T- and B-cells), monocytes, eosinophils and basophils due to their movement from the vascular bed into the lymphoid tissue; suppresses the formation of antibodies.
Betamethasone suppresses pituitary release of ACTH and β-lipotropin, but does not reduce the level of circulating β-endorphin. Oppresses the secretion of TSH and FSH.
With direct application on the vessels has a vasoconstrictor effect.
Betamethasone has a pronounced dose-dependent effect on the metabolism of carbohydrates, proteins and fats. Stimulates gluconeogenesis, promotes the capture of amino acids by the liver and kidneys and increases the activity of gluconeogenesis enzymes. In the liver, betamethasone enhances the storage of glycogen, stimulating the activity of glycogen synthetase and the synthesis of glucose from protein metabolism products. Increasing the glucose level in the blood activates the release of insulin.
Betamethasone suppresses the capture of glucose by fat cells, which leads to activation of lipolysis. However, due to an increase in the secretion of insulin, lipogenesis stimulates, which contributes to the accumulation of fat.
It detains sodium ions and water in the body, stimulates the excretion of potassium ions, reduces absorption of calcium from the digestive tract, cleans calcium ions from the bones, increases the excretion of calcium by the kidneys.
Has catabolic effect in lymphoid and connective tissue, muscles, fatty tissue, skin, bone tissue. Osteoporosis and Itenko-Cushing’s syndrome are the main factors limiting long-term therapy to SCS. As a result of catabolic action, growth can be suppressed in children.
In high doses, betamethasone can increase the excitability of brain tissue and helps lower the threshold of convulsive readiness. Stimulates excess production of hydrochloric acid and pepsin in the stomach, which leads to the development of peptic ulcers.
In systemic application, the therapeutic activity of betamethasone is due to anti-inflammatory, antiallergic, immunosuppressive and antiproliferative action.
With external and local application, the therapeutic activity of betamethasone is due to anti-inflammatory, antiallergic and antiexcudative (due to vasoconstrictor effect) action.
For anti-inflammatory activity exceeds hydrocortisone 30 times, does not have mineralocorticoid activity. The presence of fluorine in the molecule enhances the anti-inflammatory activity of betamethasone.
Betamethasone in the form of dipropionate is characterized by a prolonged action.
Mechanism of action
In the human body’s natural hormone cortisol, also called hydrocortisone, multiple effects. Colloquially called the hormone also “cortisone”, which is not correct, but because this is the inactivated (invalid) form of cortisol.
The following functions has cortisol in the body:
- It increases the production of blood sugar (glucose) in the liver, in order to provide the body in stressful situations fast energy.
- It promotes the breakdown of fat stores, which also provides energy.
- It accelerates protein turnover – and the workings of protein provides energy
- It acts as a resource essential for life stress hormone: cortisol indeed reacts slower than the adrenaline (also a stress hormone), its effects hold for longer at
- It has a dampening effect on the immune system.
Betamethasone is a synthetic cortisol descendant. It affects approximately 25- to 30-fold greater than its natural counterpart. All glucocorticoids are the basis of their potency in classes from 1 (weak activity) divided to 4 (very potent) – Betamethasone is here the class 3 (highly effective) associated
Compared to cortisol Betamethasone is degraded more slowly in the body or inactivated, because it can not be degraded by endogenous enzymes to cortisone.
Pharmacokinetics and metabolism of Betamethasone
Betamethasone is rapidly absorbed from the gastrointestinal tract after ingestion and reaches the highest blood levels within one to two hours. The biological half-life, that is the time in which the effect is to drop to half, with 36 to 54 hours very long. By comparison, the half-life of cortisol is about ten hours
The liver converts Betamethasone into a better soluble compound. This is then excreted via the bile in the feces.
Betamethasone is applied topically for skin diseases such as psoriasis, eczema, allergic or itchy skin reactions () on the skin. In this case, Betamethasone ointment, gel or cream may be used which contain the active substance as so-called ester: In these compounds, fatty acids are attached to the Betamethasone, to enhance the uptake into the skin. Examples include Betamethasone valerate and Betamethasone dipropionate.
is to be administered as an injection (injection) or taken in liquid form, the Betamethasone, Betamethasonhydrogenphosphat is used. It has a far better solubility in water than the pure active ingredient. The applications here are even more comprehensively. Examples are:
- anaphylactic (severe form of allergic reaction)
- fluid retention (with swelling) in the brain (cerebral edema)
- severe acute asthma attacks
- early treatment of severe skin diseases (see above)
- autoimmune diseases
- rheumatoid arthritis
- more severe inflammatory reactions in the body
It is important always that it does not concern bacterial infections, since the attenuation of the immune system might let flare up particularly strongly by Betamethasone infections.
The duration of treatment varies individually.
How to Take Betamethasone?
The most common application form of Betamethasone is the local treatment using Betamethasone ointment for skin diseases. Due to the long duration of action, the ointment must often be applied only once a day.
In addition, often Betamethasone tablets come to use that need to be taken by a medical treatment plan. Here, in general, the dose is increased rapidly at first, then kept constant (plateau-phase), until the condition has subsided, and then reduced slowly to complete the therapy. The tablets are usually taken in the morning because the body’s cortisol levels are highest also in the morning after getting up.
Side effects of Betamethasone
Side effects are primarily expected only on internal use (eg Betamethasone tablets or injections). For local use on the skin only a negligible portion of the drug enters the bloodstream.
The side effects of Betamethasone are dose dependent. At high doses and / or prolonged use the following adverse reactions are possible:
- Moon face, truncal obesity
- Weight gain
- increased blood fat and cholesterol levels
- water retention
- Changes in electrolyte levels in the blood
- skin reactions (thinning of the skin, bleeding, acne, redness, sweating, decreased wound healing)
- muscle weakness
- susceptibility to bone fractures
- mood swings
- blood pressure increase or decrease
- Change in the number of certain blood cells
- weakening of the immune system and susceptibility to infections
Many of these side effects can be effectively avoided if a dose is administered, which is as high as necessary, but as small as possible.
Long-term use of this drug on extensive skin surfaces leads to the development of systemic side effects peculiar to glucocorticosteroids: suppression of the hypothalamic-pituitary-adrenal system with the appearance of secondary adrenal insufficiency, hypercorticism.
Betamethasone is degraded in the body of certain enzymes (especially CYP3A4). The concomitant use of other drugs, which stimulate these enzymes, reduces the effect of Betamethasone. Such drugs are about the antibiotic rifampicin, and the Epilepsy means Phenytoin, Carbamazepine and phenobarbital.
Conversely, the coadministration of drugs which inhibit the enzymes in question, enhance the effect of Betamethasone. This is the case for the anti-fungal agent ketoconazole and itraconazole).
In combination with ACE inhibitors (antihypertensive as Ramipril, Enalapril, Lisinopril) may lead to changes in blood count.
Betamethasone may reduce the blood glucose lowering effect of oral hypoglycaemic agents.
Non-steroidal anti-inflammatory drugs (aspirin, Ibuprofen, Indomethacin), which are often taken as a headache remedy, can cause gastrointestinal bleeding in combination with Betamethasone strengthened.
glucocorticoids such as Betamethasone overcome the placental barrier and are excreted in human milk, therefore it should not be used in pregnancy and lactation. When medically justified confinement before the actual due date Betamethasone is used to encourage the early development of the lungs the unborn child.
How to get?
All medications that contain Betamethasone, subject to medical prescription. But you can buy Betamethasone cream otc in UK online.
Since when Betamethasone is known?
Already in 1855, the scientist Thomas Addison (after the Addison’s disease was named, when it comes to an underactive cortisol-producing adrenal glands) described a disease that was successfully treated with an adrenal extract. The hormone cortisol contained therein was identified in 1936 by the research groups of Kendall and Reichstein. 1948 succeeded for the first time to produce cortisol and in the laboratory. This also offered the opportunity to change its structure in order to optimize the duration of action and to reduce the potential for side effects. This eventually led to the development of Betamethasone.