Rifocin: Presentation, Chemical Formula, Mechanism of Action, Indications, Interactions and Side Effects

It is indicated for the treatment of pyodermitis and dermatitis, burns, sores, impetigo, varicose ulcers, abscesses and infected wounds.

It is an antibacterial antibiotic that has Rifamycin as its active substance . The topical rifocin is used to prevent the proliferation of bacteria and to contribute to the healing of skin lesions.

This is used in combination with other antibiotics to prevent bacteria from developing resistance, due to their great ability to mutate.

It is also used for the treatment of asymptomatic carriers of Neisseria meningitidis, in the prophylaxis of H. influenzae type B.

As well as in the treatment of leprosy and infections caused by Legionella, staphylococci and atypical microbacteria.

Presentation

Rifocin can be presented as an injectable or topical solution.

Topical use:

Local use solution for 22ml; Ointment for 20g and spray for 30ml.

Injectable solution in lyophilized powder:

It contains 600 mg.

Chemical formula

  • C43H58N4O12.
  • 3 – [[(4-methyl-1-piperazinyl) imino] methyl] rifamycin.

Mechanism of action

The mechanism of action of the rifocin acts by binding to the beta subunit of DNA-polymerases ribonucleic acid-dependent, preventing this enzyme to bind to DNA, blocking the transcription of ribonucleic acid.

Rifocin fails to bind to the polymerases of eukaryotic cells, thus the synthesis of the patient’s RNA is not affected.

The rifocin is bacteriostatic or bactericidal depending on the concentrations reached in the place where it acts and the susceptibility of the microorganism.

Los microorganisms sensible à la rifocina son, Mycobacterium tuberculosis, M. Marin; M. leprae M. bovis, M. kansasii, y ciertas onions from M. intracellulare, M. avium y coincidence.

Rifocin is highly active against Staphylococcus aureus, Haemophilus influenzae, Neisseria meningitidis and Legionella pneumophila.

It also has some effectiveness, in very high concentrations, against Chlamydia trachomatis, poxvirus, and adenovirus.

Indications

In local or topical form, it is indicated for the treatment of superficial infections:

Burns, boils, pyoderma, infected dermatoses, varicose ulcers, infected dermatoses, varicose ulcers, postplebetic eczematoid dermatitis, atherosclerotic and diabetic and post-surgical wound healing.

In the injectable form, it is indicated in the treatment of tuberculosis and the meningococcal carrier state.

It has been shown that Rifocin is active against strains of aerobic gram-negative microorganisms such as: Neisseria meningitidis and Mycobacterium tuberculosis.

Dose

Topic:

The cavities and wounds should be washed after cleaning and removing the purulent material present in the lesion every 6 to 8 hours.

Injectable:

Tuberculosis
  • Adults

10 mg / kg, once a day, which can not exceed 600 mg / day.

  • Pediatric use

10-20 mg / kg, which can not exceed 600 mg / day.

It is indicated in the treatment of all forms of tuberculosis, it is administered in a combined regimen of three drugs:

Rifampicin, pyrazinamide and isoniazid, in the first phase of treatment that is short duration, adjust and continue for 2 months.

Meningococcal carriers
  • Adults

600 mg twice daily are recommended for two days.

  • Pediatric use

Patients 1 month of age or older, 10 mg / kg is recommended, which can not exceed 600 mg per dose, every 12 hours for two days.

Patients under 1 month of age, 5 mg / kg are recommended every 12 hours for two days.

When administering the treatment of tuberculosis and the meningococcal carrier state, bacteriological cultures should be performed before the initiation of therapy to confirm the susceptibility of the organism to Rifocin.

In the same way they should be done during the whole therapy to monitor the response to treatment, since resistant strains can emerge very quickly.

These sensitivity tests are done when dealing with persistent positive cultures, during the entire course of treatment.

If the results obtained in the tests show resistance to Rifocin and no response to treatment is observed, the regimen of the drugs should be modified, evaluating the need for a fourth medication.

Contraindications

The injectable rifocin should be used with great caution in patients suffering from any liver disease or in the treatment with any other hepatotoxic drug that is able to enhance the specific effects of this drug.

With the use of the rifocin, elevations in the levels of transaminases , alkaline phosphatase and bilirubin, as well as jaundice have been observed .

The use of alcohol on a regular basis may increase the risk of hepatitis induced by the use of Rifocin.

Liver function monitoring is recommended, stopping treatment if symptoms of hepatotoxicity are observed.

Rifocin should not be used in patients who are hypersensitive to the drug or to other types of rifamycins (including rifabutin) because cross-hypersensitivity reactions may occur.

Rifocin tends to color bodily fluids such as urine and tears. Being able to permanently color contact lenses.

Rifocin is in category C risk in pregnancy, being used routinely in the treatment of tuberculosis during pregnancy.

Rifocin is excreted through breast milk, but no adverse effects have been obtained in the infant.

In the case of topical Rifocin, the contraindications are hypersensitivity to rifamycins and jaundice.

Interactions

The rifocin is able to reduce plasma concentrations and the effectiveness of drugs that are metabolized through this system, such as:

  • Verapamilo.
  • Warfarin
  • Zaleplon.
  • Zonisamida.
  • Tocainida.
  • Tramadol.
  • Tacrolimus.
  • Theophylline
  • Sirolimus.
  • Sulfonilureas.
  • Quinidina.
  • Quinine
  • Paracetamol.
  • Progestinas.
  • Propafenona.
  • Propranolol.
  • Methadone.
  • Metoprolol.
  • Mexiletina.
  • Midazolam.
  • Levobupivacaína.
  • Lamotrigina.
  • Thyroid hormones
  • Galantamine.
  • Fentanyl
  • Phenytoin
  • Fosfenitoína.
  • Estazolam.
  • Estramustina.
  • Diazepam.
  • Digoxin
  • Diltiazem.
  • Disopyramide.
  • Carbamazepine
  • Chloramphenicol.
  • Corticosteroids
  • Cyclosporine.
  • Atovaquona.
  • Cevimelina.
  • Alfentanilo.
  • Alosetrón.
  • Alprazolam.

A readjustment should be made in the doses of these drugs when the treatment with rifocin is indicated.

Rifocin is contraindicated in patients receiving saquinavir treatment with ritonavir, atazanavir, darunavir, fosamprenavir, saquinavir, or tipranavir.

The use of rifocin can affect the effectiveness of oral or systemic hormonal contraceptives, so the use of alternative contraceptive methods should be considered.

Warnings

Injectable use

It is demonstrated that Rifocina causes liver dysfunction.

Deaths associated with jaundice have been reported in patients with liver problems and in combination with other hepatotoxic agents.

In patients with hepatic insufficiency, Rifocin should be administered only in cases of extreme need, with caution and under strict medical supervision.

In addition, a very careful monitoring of liver function should be performed, if signs of hepatocellular damage appear, the use of Rifocin should be suspended.

It should be administered with great caution in patients with diabetes mellitus.

Prescribing it in the absence of a proven bacterial infection increases the risk of the development of drug-resistant bacteria.

Rifocin in doses higher than 600 mg has caused a higher incidence of adverse reactions.

By skipping one of the doses or not administering the treatment, it may decrease its effectiveness and increase the likelihood of bacterial resistance developing.

The concomitant use of saquinavir or ritonavir with rifocin is contraindicated because they develop severe hepatocellular toxicity.

Injectable Rifocin should be administered in intravenous infusions only. It should not be done intramuscularly or subcutaneously.

If local irritation and inflammation caused by extravascular infiltration are observed, treatment should be discontinued and administered elsewhere.

Patients treated with rifocin due to tuberculosis should be monitored for liver enzymes, bilirubin, serum creatinine, a complete blood count and a platelet count.

Topical use

Extended topical use may cause sensitization.

In cases of beta-hemolytic streptococcal infections, the complete disappearance of the germs should be evidenced to prevent complications.

Adverse reactions

Adverse reactions may occur in the use of the injectable rifocin, such as:

  • Gastrointestinal : Acidity, anorexia, cramps, epigastric stress, diarrhea, flatulence, jaundice, nausea and vomiting.
  • Hepatic : Elevations of serum bilirubin, alkaline phosphatase, serum transaminases, rarely, hepatitis and abnormal liver function tests.
  • Hematological: Cases of disseminated intravascular coagulation, leukopenia, hemolytic anemia and decreased hemoglobin and, in a few cases, agranulocytosis.
  • Central nervous system: Ataxia, headache, fever, fatigue, dizziness, drowsiness, inability to concentrate, mental confusion, changes in behavior, muscle pain and weakness in the extremities in addition to generalized numbness.
  • Eyepieces: Visual alterations.
  • Endocrine: Menstrual disorders.
  • Renal: Adrenal insufficiency, elevations of serum uric, hemolysis, haemoglobinuria, hematuria, interstitial nephritis, acute tubular necrosis, renal failure and acute renal failure.
  • Dermatological: Mild and self-limiting skin reactions, redness and itching with or without a rash.

In the case of topical Rifocin, allergic skin manifestations such as burning, itching, and erythema are observed.

In which case the medication should be discontinued.

Side effects

The following side effects may occur with the following symptoms:

  • Nausea, itching, headache, vomiting, abdominal pain and increased lethargy occur at a time after ingestion, unconsciousness can occur when there is a serious liver disease.
  • Transient increase in liver enzymes and bilirubin.
  • The coloration of the skin, urine, sweat, saliva, tears and stools are brownish red to orange tones, the intensity is directly proportional to the total amount of drug ingested.
  • Enlargement of the liver, due to a severe overdose.
  • Facial or periorbital edema may occur in pediatric patients.
  • In some cases of sinus tachycardia, hypotension, seizures, ventricular arrhythmias and cardiac arrest.