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Actions of Rolisporin in details
Pharmacology: Pharmacokinetics: Rolisporin is administered as IV and IM injection. The mean elimination half-life (t½) in healthy adults is about 6-9 hrs and is much longer than any other cephalosporins or cephamycins. The t½ does not alter with change in the route of administration.
Rolisporin was completely absorbed following IM administration with mean maximum plasma concentrations (Cmax) occurring between 2 and 3 hrs post-dosing. Multiple IV or IM doses ranging from 0.5-2 g at 12- to 24-hr intervals resulted in 15-36% accumulation of Rolisporin above single dose values.
Thirty-three percent (33%) to 67% of a Rolisporin dose was excreted in the urine as unchanged drug and the remainder was secreted in the bile and ultimately found in the feces as microbiologically inactive compounds. After a 1 g IV dose, average concentrations of Rolisporin, determined from 1-3 hrs after dosing, were 581 mcg/mL in the gallbladder bile, 788 mcg/mL in the common duct bile, 898 mcg/mL in the cystic duct bile, 78.2 mcg/g in the gallbladder wall and 62.1 mcg/mL in the concurrent plasma.
Over a 0.15-3 g dose range in healthy adult subjects, the values of elimination t½ ranged from 5.8-8.7 hrs; apparent volume of distribution from 5.78-13.5 L; plasma clearance from 0.58-1.45 L/hr; and renal clearance from 0.32-0.73 L/hr. Rolisporin is reversibly bound to human plasma proteins, and the binding decreased from a value of 95% bound at plasma concentrations of <25 mcg/mL to a value of 85% bound at 300 mcg/mL. Rolisporin crosses the blood placenta barrier.
Infants and Children: Elimination t½ in neonates is prolonged (almost equal to adults) but decreases with increasing postnatal age.
In patients with renal failure, non-renal elimination may compensate.
Microbiology: Antibacterial Activity: Rolisporin for injection has a broad spectrum activity in vitro which includes gram-positive and gram-negative aerobic and some anaerobic bacteria.
Rolisporin has a high degree of stability in presence of β-lactamases, both penicillinases and cephalosporinases of gram-negative and gram-positive bacteria.
Rolisporin shows good in vitro activity against the following organisms.
Gram-Negative Aerobes: Enterobacter aerogenes, Enterobacter cloacae, Escherechia coli, Haemophilus influenzae (including Ampicillin resistant strains), Haemophilus parainfluenzae, Klebsiella spp (including K. pneumoniae), Neisseria gonorrhoeae (including penicillinase and non-penicillinase producing strains); Proteus mirabilis, P. vulgaris, Morganella morganii, Serratia marcescens, Pseudomonas aeruginosa.
Gram-Positive Aerobes: Staphylococcus aureus including penicillinase-producing strains, Staphylococcus epidermidis, Streptococcus pyogenes (Group A β-hemolytic), Streptococcus agalactiae (Group B streptococci), Streptococcus pneumoniae.
Gram-Negative Aerobes: Citrobacter freundii, Citrobacter diversus, Providencia spp, Salmonella spp, Shigella spp, Acinetobacter calcoaceticus.
Anaerobes: Bacteroides spp, Clostridia (but most Clostridium difficile strains are resistant).
How should I take Rolisporin?
A nurse or other trained health professional will give you Rolisporin. Rolisporin is given as a shot into one of your muscles or through a needle placed in one of your veins.
Use exactly as prescribed by your doctor. Do not use in larger or smaller amounts or for longer than recommended. Follow the directions on your prescription label.
Rolisporin is injected into a muscle, or into a vein through an IV. You may be shown how to use an IV at home. Do not self-inject this medicine if you do not fully understand how to give the injection and properly dispose of used needles, IV tubing, and other items used to inject the medicine.
Rolisporin must be given slowly, and the IV infusion can take at least 30 minutes to complete.
You may need to mix Rolisporin with a liquid (diluent) before using it. If you are using the injections at home, be sure you understand how to properly mix and store the medication. Use only the diluent your doctor has recommended.
After mixing your medicine, you will need to use it within a certain number of hours or days. This will depend on the diluent and how you store the mixture (at room temperature, in a refrigerator, or frozen). Carefully follow the mixing and storage instructions provided with your medicine. Ask your pharmacist if you have questions.
Do not mix Rolisporin in the same injection with other antibiotics, or with any diluent that contains calcium, including a TPN (total parenteral nutrition) solution.
If you use other injectable medications, be sure to flush your intravenous catheter between injections of each medication.
Use this medicine for the full prescribed length of time. Your symptoms may improve before the infection is completely cleared. Skipping doses may also increase your risk of further infection that is resistant to antibiotics. Rolisporin will not treat a viral infection such as the common cold or flu.
This medication can cause unusual results with certain lab tests for glucose (sugar) in the urine. Tell any doctor who treats you that you are using Rolisporin.
Store unmixed Rolisporin powder at room temperature, away from moisture, heat, and light.
If your medicine was provided in a frozen form or was frozen after mixing, thaw it in a refrigerator or at room temperature. Do not warm in a microwave or boiling water. Use the medicine as soon as possible after thawing it. Do not refreeze.
Rolisporin is a prodrug and must be activated by bacterial catalase. Specficially, activation is associated with reduction of the mycobacterial ferric KatG catalase-peroxidase by hydrazine and reaction with oxygen to form an oxyferrous enzyme complex. Once activated, isoniazid inhibits the synthesis of mycoloic acids, an essential component of the bacterial cell wall. At therapeutic levels isoniazid is bacteriocidal against actively growing intracellular and extracellular Mycobacterium tuberculosis organisms. Specifically isoniazid inhibits InhA, the enoyl reductase from Mycobacterium tuberculosis, by forming a covalent adduct with the NAD cofactor. It is the INH-NAD adduct that acts as a slow, tight-binding competitive inhibitor of InhA.
- EPA DSStox. "Ceftriaxone: DSSTox provides a high quality public chemistry resource for supporting improved predictive toxicology.". https://comptox.epa.gov/dashboard/dsstox... (accessed September 18, 2017).
- NCIt. "Ceftriaxone: NCI Thesaurus (NCIt) provides reference terminology for many systems. It covers vocabulary for clinical care, translational and basic research, and public information and administrative activities.". https://ncit.nci.nih.gov/ncitbrowser/Con... (accessed September 18, 2017).
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