Glucocorticoid drugs

CHARACTERISTICS OF CERTAIN PREPARATIONS

Depending on the structure of steroids vary in the duration, severity of inflammatory, mineralocorticoid, metabolic and immunosuppressive activity (tab. 5). Moreover, there is no direct correlation between their immunosuppressive and anti-inflammatory action. For example, dexamethasone has potent anti-inflammatory effect and relatively low immunosuppressive activity.

Prednisone

As the activity and other parameters close to prednisolone. Initially prednisone is metabolically inactive drug (a prodrug). It is activated in the liver by hydroxylation and conversion to prednisolone. Therefore it is not recommended for use in severe liver disease. The main advantage of prednisone is its lower cost.

Method of production:

- 5 mg tablets (prednisone).


Prednisolone

Synthetic glucocorticoid, is most commonly used in clinical practice for the treatment of pharmacodynamic and is regarded as the standard drug. By glucocorticoid activity 4 times stronger than hydrocortisone, and on mineralocorticoid activity is inferior. Refers to glucocorticoids with an average duration of action.

Method of production:

- Tablets of 5, 10, 20 and 50 mg (ano-prednisone dekortin H tednisol);
- Prednisolone phosphate, ampoules 1 ml, 30 mg / ml;
- Prednisolone hemisuccinate, powder in ampoules of 10, 25, 50 and 250 mg (dekortin-I salt);
- Prednisolone acetate suspension in vials of 10, 20, 25 and 50 mg (prednigexol).

CORTISONE

The drug is a glucocorticoid natural, biologically inactive. It is activated in the liver, turning into a hydrocortisone. It has a short-term effect. Compared with other glucocorticoids it has a more pronounced mineralocorticoid activity, that is, has a significant effect on water and electrolyte metabolism.
application Features

Mainly used for replacement therapy in adrenal insufficiency in patients with normal liver function.

Method of production:

- Tablets of 25 and 50 mg (cortisone acetate).

Hydrocortisone

Natural glucocorticoid on glucocorticoid activity in 4 times weaker than prednisolone at mineralocorticoid slightly exceeds it. As with cortisone likely to develop edema, sodium retention and potassium loss.

Features of the application

Hydrocortisone is the same as cortisone and not recommended for pharmacodynamic therapy, especially in patients with edema, hypertension, congestive heart failure.
It is used mostly for replacement therapy in primary and secondary adrenal insufficiency. In acute adrenal insufficiency and other urgent conditions the drug of choice is hydrocortisone hemisuccinate.

Method of production:

- Hydrocortisone hemisuccinate, dry chemical or solution in ampoules and bottles of 100 and 500 mg (hydrocortisone-meva, panukort, Solu-kortef);
- Hydrocortisone acetate suspension in ampoules and vials of 25 mg / ml.

METHYLPREDNISOLONE

Compared with prednisone has slightly higher (20%) glucocorticoid activity, minimal mineralocorticoid activity, a lower incidence of adverse reactions (especially mental changes, appetite, ulcerogenic action). It has a higher value than prednisolone.

Features of the application

Just as prednisolone, mainly used for pharmacodynamic therapy. It is preferred in patients with mental disorders, obesity, peptic ulcer disease, as well as during pulse therapy.

Method of production:

- 4 tablets of 16 mg and (Medrol, metipred, urbazon, prednol);
- Methylprednisolone succinate, dry matter in vials and bottles of 8, 20, 40, 125, 250, 500 mg, 1.0 g and 2.0 (metipred, prednol-L, Solu-Medrol);
- Methylprednisolone acetate suspension in bottles of 40 mg (Depo-Medrol, metipred);
- Suleptanat methylprednisolone, ampoules of 50 and 100 mg / ml (promedrol).

Triamcinolone

Is fluorinated glucocorticoid. It has a strong (20%) and the prolonged glucocorticoid action than prednisolone. It does not mineralocorticoid activity. The most common cause unwanted reactions, especially on the part of the muscle tissue ( "triamtsinolonovaya" myopathy) and skin (stretch marks, bleeding, hirsutism).

Method of production:

- Tablets of 2, 4 and 8 mg (berlikort, delfikort, kenakort polkortolon.); triamcinolone acetonide, suspension in vials of 40 mg / ml (kenalog, trikort);
- Triamcinolone hexacetonide, suspension in vials of 20 mg / ml (lederspan).

Dexamethasone

Just as triamcinolone, a fluorinated drug. One of the most potent glucocorticoids: 7 times greater for prednisolone glucocorticoid activity. There has mineralocorticoid activity. Causes severe suppression of the hypothalamic-pituitary-adrenal system, expressed disturbances of carbohydrate, fat, calcium metabolism, stimulating effect, so it is not recommended for long term.

Features of the application

The drug has some specific indications for use: bacterial meningitis; brain edema; in ophthalmology (keratitis, uveitis, etc.); prevention and treatment of nausea and vomiting associated with chemotherapy; Treatment of severe abstinence syndrome in alcoholism; prevention of respiratory distress syndrome in premature (dexamethasone stimulates the synthesis of surfactant in the alveoli of the lungs); leukemia (replacement prednisolone dexamethasone on acute lymphoblastic leukemia significantly reduces the incidence of central nervous system).

Method of production:

- Tablets of 0.5 and 1.5 mg (Daxin, deksazon, kortideks);
- Dexamethasone phosphate, ampoules of 1 and 2 ml, 4 mg / ml (Daxin, deksabene, deksazon, sondeks).

Betamethasone

Fluorinated glucocorticoid, strength and duration of action close to dexamethasone. Glucocorticoid activity are 8-10 times higher than that of prednisolone. It does not mineralocorticoid properties. Several weaker than dexamethasone effect on carbohydrate metabolism.
The most famous drug betamethasone phosphate / dipropionate, intended for intramuscular, intra-articular and periarticular injection. It consists of two esters, one of which - phosphate - is rapidly absorbed from the injection site and provides a fast (within 30 minutes) effect, and the other - dipropionate - absorbed slowly, but provides a sustained action - up to 4 weeks or more. It is a suspension of fine crystals, which can not be administered intravenously.
The water-soluble betamethasone phosphate administered intravenously and subkonyunktivalno.

Method of production:

- Tablets of 0.5 mg (tseleston);
- Betamethasone phosphate, ampoules 1 ml, 3 mg / ml (tseleston);
- Betamethasone acetate, ampoules and vials 1 ml to 5 ml, 3 mg / ml (tseleston hronodoze);
- By vials 1 ml of a suspension containing 7 mg of betamethasone 2 mg as phosphate and 5 mg of dipropionate (diprospan, flosteron).


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