Rolisporin Actions


Actions of Rolisporin in details

infoThe action of the drug on the human body is called Pharmacodynamics in Medical terminology. To produce its effect and to change the pathological process that is happening the body and to reduce the symptom or cure the disease, the medicine has to function in a specific way. The changes it does to the body at cellular level gives the desired result of treating a disease. Drugs act by stimulating or inhibiting a receptor or an enzyme or a protein most of the times. Medications are produced in such a way that the ingredients target the specific site and bring about chemical changes in the body that can stop or reverse the chemical reaction which is causing the disease.


Pharmacology: Rolisporin sodium is a β-lactam antibiotic from the 3rd generation cephalosporin group.

Rolisporin is a broad-spectrum cephalosporin antibiotic resistant to β-lactamases. It is active against gram-positive aerobes (Staphylococcus metis, Streptococcus, Streptococcus pneumoniae), gram-negative aerobes (Borrelia burgdorferi, Branhamella catarrhalis, Citrobacter freundii, Citrobacter koseri, Enterobacter, Escherichia coli, Haemophilus influenzae, Klebsiella, Morganella morganii, Neisseria including N. meningitidis and N. gonorrheae, Proteus mirabilis, Proteus multocida, Proteus vulgaris, Providencia, Salmonella, Serratia, Shigella, Yersinia) and anaerobes (Clostridium perfringens, Fusobacterium, Peptostreptococcus, Prevotella).

Pharmacokinetics: Distribution: After IV infusion of a single dosage of 1 g, the maximum serum concentration is in average about 168 mg/L after 30 min. After IM injection of the same dosage, a serum peak of 80 mg/L is reached within 2 or 3 hrs.

The IM and IV routes are bioequivalent (similar areas under the curve). Rolisporin administered by IM route has an absolute bioavailability near 100%. The distribution volume of Rolisporin is 7-12 L. The diffusion of Rolisporin is good in the interstitial liquid, the tissues and the organic liquids (especially the cerebrospinal fluid, bile, bones, bronchial secretions, infectious areas of the ENT sphere).

Protein-Binding: The binding of Rolisporin to serum proteins (albumin) is reversible and saturable. It may vary from 80-95% in the range of therapeutic concentrations. As the albumin rate is lower, the proportion of free Rolisporin in the interstitial liquid is consequently higher than in the plasma.

Metabolism: Rolisporin is very poorly metabolized. The intestinal flora only transforms it to inactive metabolites.

Excretion: Rolisporin is excreted by urinary and biliary routes. The total serum clearance is 10-22 mL/min. The renal clearance is 5-12 mL/min. Fifty to 60% of Rolisporin is excreted as unchanged form in the urine whereas around 40-50% is excreted in the bile. In adults, the elimination t½ is about 8 hrs long.

Pharmacokinetics in Particular Clinical Conditions: In newborns, the quantity of Rolisporin remaining in the urine corresponds to about 70% of the administered dosage.

In newborns <8 days, the average elimination t½ is generally 2 or 3 times higher than in young adults; it is shorter in newborns 3-12 months.

In children and newborns, after a single IM injection of 50 mg/kg, the peak serum concentration of Rolisporin is reached after 5.4 hrs (192±135mg/L).

In children and newborns, after a single IM injection, the diffusion in the middle ear is good with rates higher than the MIC of main bacillus responsible for middle ear acute disease during at least 48 hrs. After a single injection of 50 mg/kg, the total concentration of Rolisporin in the middle ear liquid is about 5 mg/L after 1.5 hrs (33±20 mg/L), after the 15th hr, stable on the 24th hr (35±12 mg/L) and is still about 19±7mg/L after 48 hrs.

In patients with renal or hepatic insufficiency, Rolisporin pharmacokinetics is very much different and the elimination t½ is only very poorly increased. If only the renal function is concerned, then the Rolisporin biliary elimination is increased. If only the hepatic function is concerned, the renal elimination is increased.

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.

Rolisporin administration

infoAdministration of drug is important to know because the drug absorption and action varies depending on the route and time of administration of the drug. A medicine is prescribed before meals or after meals or along with meals. The specific timing of the drug intake about food is to increase its absorption and thus its efficacy. Few work well when taken in empty stomach and few medications need to be taken 1 or 2 hrs after the meal. A drug can be in the form of a tablet, a capsule which is the oral route of administration and the same can be in IV form which is used in specific cases. Other forms of drug administration can be a suppository in anal route or an inhalation route.

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 pharmacology

infoPharmacokinetics of a drug can be defined as what body does to the drug after it is taken. The therapeutic result of the medicine depends upon the Pharmacokinetics of the drug. It deals with the time taken for the drug to be absorbed, metabolized, the process and chemical reactions involved in metabolism and about the excretion of the drug. All these factors are essential to deciding on the efficacy of the drug. Based on these pharmacokinetic principles, the ingredients, the Pharmaceutical company decides dose and route of administration. The concentration of the drug at the site of action which is proportional to therapeutic result inside the body depends on various pharmacokinetic reactions that occur in the body.

Rolisporin is a cephalosporin/cephamycin beta-lactam antibiotic used in the treatment of bacterial infections caused by susceptible, usually gram-positive, organisms. Rolisporin has in vitro activity against gram-positive and gram-negative aerobic and anaerobic bacteria. The bactericidal activity of Rolisporin results from the inhibition of cell wall synthesis and is mediated through Rolisporin binding to penicillin binding proteins (PBPs). Rolisporin is stable against hydrolysis by a variety of beta-lactamases, including penicillinases, and cephalosporinases and extended spectrum beta-lactamases.


  1. EPA DSStox. "Ceftriaxone: DSSTox provides a high quality public chemistry resource for supporting improved predictive toxicology.". (accessed September 18, 2017).
  2. 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.". (accessed September 18, 2017).


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Information checked by Dr. Sachin Kumar, MD Pharmacology

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