Singapore Drugs Database

Indication

Adjunctive therapy for short-term administration in rheumatoid arthritis.

Mechanism of Action

Unbound glucocorticoids cross cell membranes and bind with high affinity to specific cytoplasmic receptors, modifying transcription and protein synthesis. By this mechanism, glucocorticoids can inhibit leukocyte infiltration at the site of inflammation, interfere with mediators of inflammatory response, and suppress humoral immune responses. The antiinflammatory actions of corticosteroids are thought to involve phospholipase A2 inhibitory proteins, lipocortins, which control the biosynthesis of potent mediators of inflammation such as prostaglandins and leukotrienes.

Pharmacokinetics

Absorption

Oral bioavailability 80-99%

Distribution

Metabolism

Hepatic

Elimination

Toxicity

LD₅₀=2000 mg/kg (orally in rat)

Active Ingredient/Synonyms

(6alpha,11beta)-11,17,21-Trihydroxy-6-methylpregna-1,4-diene-3,20-dione | (6α,11β)-11,17,21-trihydroxy-6-methylpregna-1,4-diene-3,20-dione | 1-dehydro-6alpha-Methylhydrocortisone | 1-dehydro-6α-methylhydrocortisone | 6alpha-Methyl-11beta,17alpha,21-triol-1,4-pregnadiene-3,20-dione | delta(1)-6alpha-Methylhydrocortisone | Medrate | Medrone | Methylprednisolon | Methylprednisolone | Methylprednisolonum | Metilprednisolona | Solomet | Urbason | Methylprednisolone |

Indication

For the treatment of bacterial blepharitis, bacterial bonjunctivitis, corneal injuries, corneal ulcers and meibomianitis. For the prophylaxis of ocular infections following foreign body removal

Mechanism of Action

Framycetin binds to specific 30S-subunit proteins and 16S rRNA, four nucleotides of 16S rRNA and a single amino acid of protein S12. This interferes with decoding site in the vicinity of nucleotide 1400 in 16S rRNA of 30S subunit. This region interacts with the wobble base in the anticodon of tRNA. This leads to interference with the initiation complex, misreading of mRNA so incorrect amino acids are inserted into the polypeptide leading to nonfunctional or toxic peptides and the breakup of polysomes into nonfunctional monosomes.

Active Ingredient/Synonyms

Fradiomycin B | Framicetina | Framycetin | Framycétine | Framycetinum | Neomycin B | Framycetin |

Indication

Echocardiography: Sulfur hexafluoride is indicated for use in adult patients with suboptimal echocardiograms to opacify the left ventricular chamber and to improve the delineation of the left ventricularendocardial border. Ultrasonography of the Liver: Sulfur hexafluoride is indicated for use with ultrasound of the liver in adult and pediatric patients to characterize focal liver lesions.

Mechanism of Action

Within the blood, the acoustic impedance of Lumason microspheres is lower than that of the surrounding non-aqueous tissue. Therefore, an ultrasound beam is reflected from the interface between the microspheres and the surrounding tissue. The reflected ultrasound signal provides a visual image that shows a contrast between the blood and the surrounding tissues.

Pharmacokinetics

Absorption

The pharmacokinetic of the SF6 gas component of Lumason was evaluated in 12 healthy adult subjects (7 men and 5 women). After intravenous bolus injections of 0.03 mL/kg and 0.3 mL/kg of Lumason, corresponding to approximately 1 and 10 times the recommended doses, concentrations of SF6 in blood peaked within 1 to 2 minutes for both doses.

Distribution

In a study of healthy subjects, the mean values for the apparent steady-state volume of distribution of SF6 were 341 L and 710 L for Lumason doses of 0.03 mL/kg and 0.3 mL/kg, respectively. Preferential distribution to the lung is likely responsible for these values.

Metabolism

SF6 undergoes little or no biotransformation; 88% of an administered dose is recovered unchanged in expired air.

Elimination

Active Ingredient/Synonyms

hexafluoridosulfur | Sulfur fluoride | sulfur(6+) fluoride | sulfur(VI) fluoride | Sulphur hexafluoride | Sulfur hexafluoride |