DEXACURE Tablet Ref.[115635] Active ingredients: Dexamethasone

Source: Registered Drug Product Database (NG)  Revision Year: 2022  Publisher: Unicure Pharmaceutical Ltd, Ikofa Village, Lagos - Benin Expressway, Ikofa, Ijebu - Ode, Email: unicurepharms@163.com

5.1. Pharmacodynamic properties

Pharmacotherapeutic group: Corticosteroids for systemic use, Glucocorticoids
ATC code: H02AB02

Dexamethasone is a synthetic glucocorticoid whose anti-inflammatory potency is 7 times greater than prednisolone. Like other glucocorticoids, Dexamethasone also has anti-allergic, antipyretic and immunosuppressive properties. Dexamethasone has practically no water and salt-retaining properties, and is therefore particularly suitable for use in patients with cardiac failure or hypertension. Because of its long biological half-life (36-54 hours), DEXACURE Dexamethasone is especially suitable in conditions where continuous glucocorticoid action is desired.

5.2. Pharmacokinetic properties

Absorption

Corticosteroids, are, in general, readily absorbed from the gastro-intestinal tract. They are also well absorbed from sites of local application. Water-soluble forms of corticosteroids are given by intravenous injection for a rapid response; more prolonged effects are achieved using lipid-soluble forms of corticosteroids by intramuscular injection.

Distribution

Corticosteroids are rapidly distributed to all body tissues. They cross the placenta and may be excreted in small amounts in breast milk.

Most corticosteroids in the circulation are extensively bound to plasma proteins, mainly to globulin and less so to albumin. The corticosteroid-binding globulin has high affinity but low binding capacity, while the albumin has low affinity but large binding capacity. The synthetic corticosteroids are less extensively protein bound than hydrocortisone (cortisol). They also tend to have longer half-lives.

Bio transformation and Elimination

Corticosteroids are metabolised mainly in the liver but also in the kidney, and are excreted in the urine. The slower metabolism of the synthetic corticosteroids with their lower protein-binding affinity may account for their increased potency compared with the natural corticosteroids.

5.3. Preclinical safety data

In animal studies, cleft palate was observed in rats, mice, hamsters, rabbits, dogs and primates: not in horses and sheep. In some cases these divergences were combined with defects of the central nervous system and of the heart. In primates, effects in the brain were seen after exposure. Moreover, intra-uterine growth can be delayed. All these effects were seen at high dosages.

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