Rimabex

Rimabex Uses, Dosage, Side Effects, Food Interaction and all others data.

Rimabex suppresses initiation of chain formation for RNA synthesis in susceptible bacteria by binding to the β subunit of DNA-dependent RNA polymerase, thus blocking RNA transcription.

Rifampin is an antibiotic that inhibits DNA-dependent RNA polymerase activity in susceptible cells. Specifically, it interacts with bacterial RNA polymerase but does not inhibit the mammalian enzyme. It is bactericidal and has a very broad spectrum of activity against most gram-positive and gram-negative organisms (including Pseudomonas aeruginosa) and specifically Mycobacterium tuberculosis. Because of rapid emergence of resistant bacteria, use is restricted to treatment of mycobacterial infections and a few other indications. Rifampin is well absorbed when taken orally and is distributed widely in body tissues and fluids, including the CSF. It is metabolized in the liver and eliminated in bile and, to a much lesser extent, in urine, but dose adjustments are unnecessary with renal insufficiency.

Trade Name Rimabex
Generic Rifampicin
Rifampicin Other Names Rifampicin, Rifampicina, Rifampicine, Rifampicinum, Rifampin
Weight 100mg/5ml, 450mg
Type Syrup, Tablet
Formula C43H58N4O12
Weight Average: 822.9402
Monoisotopic: 822.40512334
Protein binding

89%

Groups Approved
Therapeutic Class Anti-Tubercular Antibiotics
Manufacturer Cibex (private) Limited
Available Country Pakistan
Last Updated: September 19, 2023 at 7:00 am
Rimabex
Rimabex

Uses

In the treatment of both tuberculosis and the meningococcal carrier state, the small number of resistant cells present within large populations of susceptible cells can rapidly become the predominant type. Bacteriologic cultures should be obtained before the start of therapy to confirm the susceptibility of the organism to rifampinand they should be repeated throughout therapy to monitor the response to treatment. Since resistance can emerge rapidly, susceptibility tests should be performed in the event of persistent positive cultures during the course of treatment. If test results show resistance to rifampin and the patient is not responding to therapy, the drug regimen should be modified.

Rimabex is also used to associated treatment for these conditions: Cholestatic pruritus, MRSA Infection, Prosthetic Joint Infection, Asymptomatic Neisseria meningitidis carrier of the nasopharynx, Initial phase Tuberculosis, Late phase Tuberculosis, Antibacterial therapy

How Rimabex works

Rifampin acts via the inhibition of DNA-dependent RNA polymerase, leading to a suppression of RNA synthesis and cell death.

Dosage

Rimabex dosage

Rifampin can be administered by the oral route or by IV infusion. IV doses are the same as those for oral.

Tuberculosis:

  • Adults: 10 mg/kg, in a single daily administration, not to exceed 600 mg/day, oral or IV
  • Pediatric Patients: 10–20 mg/kg, not to exceed 600 mg/day, oral or IV

It is recommended that oral rifampin be administered once daily, either 1 hour before or 2 hours after a meal with a full glass of water.

Rifampin is indicated in the treatment of all forms of tuberculosis. A three-drug regimen consisting of rifampin, isoniazid, and pyrazinamide is recommended in the initial phase of shortcourse therapy which is usually continued for 2 months. The Advisory Council for the Elimination of Tuberculosis, the American Thoracic Society, and theCenters for Disease Control and Preventionrecommend that either streptomycin or ethambutol be added as a fourth drug in a regimen containing isoniazid (INH), rifampin and pyrazinamide for initial treatment of tuberculosis unless the likelihood of INH resistance is very low. The need for a fourth drug should be reassessed when the results of susceptibility testing are known. If community rates of INH resistance are currently less than 4%, an initial treatment regimen with less than four drugs may be considered.

Following the initial phase, treatment should be continued with rifampin and isoniazid for at least 4 months. Treatment should be continued for longer if the patient is still sputum or culture positive, if resistant organisms are present, or if the patient is HIV positive.

Should be taken on an empty stomach. Best taken on an empty stomach 1 hr before or 2 hr after meals.

Preparation Of Solution For IV Infusion: Reconstitute the lyophilized powder by transferring 10 mL of sterile water for injection to a vial containing 600 mg of rifampin for injection. Swirl vial gently to completely dissolve the antibiotic. The reconstituted solution contains 60 mg rifampin per mL and is stable at room temperature for up to 30 hours. Prior to administration, withdraw from the reconstituted solution a volume equivalent to the amount of rifampin calculated to be administered and add to 500 mL of infusion medium. Mix well and infuse at a rate allowing for complete infusion within 3 hours. Alternatively, the amount of rifampin calculated to be administered may be added to 100 mL of infusion medium and infused in 30 minutes.

Dilutions in dextrose 5% for injection (D5W) are stable at room temperature for up to 8 hours and should be prepared and used within this time. Precipitation of rifampin from the infusion solution may occur beyond this time. Dilutions in normal saline are stable at room temperature for up to 6 hours and should be prepared and used within this time. Other infusion solutions are not recommended.

Side Effects

Facial flushing and itching, with or without a rash, flu-like syndrome characterised by episodes of fever, chills, headache, dizziness, bone pain, shortness of breath, and malaise; GI adverse effects (e.g. nausea, vomiting, anorexia, diarrhoea, epigastric distress), pseudomembranous colitis, eosinophilia, leucopenia, haemolytic anaemia; alterations in kidney function and renal failure, menstrual disturbances, oedema, myopathy, muscular weakness; orange-red discolouration of the urine, faeces, sweat, saliva, sputum, tears, and other body fluids; thrombophlebitis, local irritation and inflammation after prolonged IV infusion. Rarely, eye irritation and visual disturbances, anaphylaxis or shock.

Toxicity

LD50=1570 mg/kg (rat), chronic exposure may cause nausea and vomiting and unconsciousness

Precaution

Rimabex has been shown to produce liver dysfunction. Fatalities associated with jaundice have occurred in patients with liver disease and in patients taking rifampin with other hepatotoxic agents. Patients with impaired liver function should be given rifampin only in cases of necessity and then with caution and under strict medical supervision. In these patients, careful monitoring of liver function, especially SGPT/ALT and SGOT/AST should be carried out prior to therapy and then every 2 to 4 weeks during therapy. If signs of hepatocellular damage occur, rifampin should be withdrawn.

In some cases, hyperbilirubinemia resulting from competition between rifampin and bilirubin for excretory pathways of the liver at the cell level can occur in the early days of treatment. An isolated report showing a moderate rise in bilirubin and/or transaminase level is not in itself an indication for interrupting treatment; rather, the decision should be made after repeating the tests, noting trends in the levels, and considering them in conjunction with the patient's clinical condition.

Rifampin has enzyme-inducing properties, including induction of delta amino levulinic acid synthetase. Isolated reports have associated porphyria exacerbation with rifampin administration.

Interaction

May accelerate the metabolism and reduce the effect of drugs that are metabolised by CYP450 enzymes (e.g. quinidine, phenytoin, theophylline). Decreased concentrations of atovaquone and increased concentrations of rifampicin when taken concomitantly. Concurrent use of ketoconazole and rifampicin may result in decreased serum concentrations of both drugs. May decrease serum concentrations of enalaprilat. Reduced absorption by antacids. Increased risk of hepatotoxicity with halothane or isoniazid.

Food Interaction

  • Avoid alcohol.
  • Take on an empty stomach. Take at least 1 hour before or 2 hours after meals.
  • Take with a full glass of water.

Elimination Route

Well absorbed from gastrointestinal tract.

Half Life

3.35 (+/- 0.66) hours

Clearance

  • 0.19 +/- 0.06 L/hr/kg [300 mg IV]
  • 0.14 +/- 0.03 L/hr/kg [600 mg IV]

Elimination Route

Less than 30% of the dose is excreted in the urine as rifampin or metabolites.

Pregnancy & Breastfeeding use

Pregnancy: When administered during the last few weeks of pregnancy, rifampin can cause post natal hemorrhages in the mother and infant for which treatment with vitamin K may be indicated.

Nursing Mothers: Because of the potential for tumorigenicity shown for rifampin in animal studies, a decision should be made whether to discontinue nursing or discontinue the drug, taking into account the importance of the drug to the mother.

Contraindication

Rimabex is contraindicated in patients with a history of hypersensitivity to rifampin or any of the components, or to any of the rifamycins. Rifampin is contraindicated in patients who are also receiving ritonavir-boosted saquinavir due to an increased risk of severe hepatocellular toxicity.

Rifampin is contraindicated in patients who are also receiving atazanavir, darunavir, fosamprenavir, saquinavir, or tipranavir due to the potential of rifampin to substantially decrease plasma concentrations of these antiviral drugs, which may result in loss of antiviral efficacy and/or development of viral resistance.

Special Warning

Geriatric Use: Clinical studies of Rimabex did not include sufficient numbers of subjects aged 65 and over to determine whether they respond differently from younger subjects. Other reported clinical experience has not identified differences in responses between the elderly and younger patients. Caution should therefore be observed in using rifampin in elderly patients.

Acute Overdose

Nausea, vomiting, abdominal pain, pruritus, headache, and increasing lethargy will probably occur within a short time after ingestion; unconsciousness may occur when there is severe hepatic disease. Transient increases in liver enzymes and/or bilirubin may occur. Brownish-red or orange discoloration of the skin, urine, sweat, saliva, tears, and feces will occur, and its intensity is proportional to the amount ingested.

Liver enlargement, possibly with tenderness, can develop within a few hours after severe overdosage; bilirubin levels may increase and jaundice may develop rapidly. Hepatic involvement may be more marked in patients with prior impairment of hepatic function. Other physical findings remain essentially normal. A direct effect upon the hematopoietic system, electrolyte levels, or acid-base balance is unlikely.

Facial or periorbital edema has also been reported in pediatric patients. Hypotension, sinus tachycardia, ventricular arrhythmias, seizures and cardiac arrest were reported in some fatal cases.

Storage Condition

Store between 15-30° C. Avoid excessive heat and protect from light.

Innovators Monograph

You find simplified version here Rimabex

Rimabex contains Rifampicin see full prescribing information from innovator Rimabex Monograph, Rimabex MSDS, Rimabex FDA label

FAQ

What is Rimabex used for?

Rimabex used to treat several types of bacterial infections.

How safe is Rimabex?

Rimabex is a well-tolerated antibiotic.Many people using this medication do not have serious side effects.Rimabex may rarely cause serious liver disease.

How does Rimabex work?

Rimabex works by killing the bacteria that are causing the infection.

What are the common side effects of Rimabex?

Common side effects of Rimabex are include:

  • temporary discoloration (yellow, reddish-orange, or brown color) of your skin, teeth, saliva, urine, stool, sweat, and tears)
  • itching
  • flushing
  • headache
  • drowsiness
  • dizziness
  • lack of coordination
  • difficulty concentrating
  • confusion
  • changes in behavior
  • muscle weakness
  • numbness
  • pain in the arms, hands, feet, or legs
  • heartburn
  • stomach cramps
  • loss of appetite
  • nausea
  • vomiting
  • diarrhea
  • gas
  • painful or irregular menstrual periods
  • vision changes

Is Rimabex safe during pregnancy?

Rimabex have an excellent safety record in pregnancy and are not associated with human fetal malformations.

Is Rimabex safe during breastfeeding?

The amount of Rimabex in milk is insufficient to treat tuberculosis in the breastfed infant. breastfeeding should not be discouraged in women taking Rimabex.

Can I drink alcohol with Rimabex?

Drinking alcohol while taking Rimabex can hurt your liver. Tell your doctor about other medicines you are taking.

Can I drive after taking Rimabex?

Do not drive a car or operate machinery until you know how this drug affects you. avoid drinking alcohol while taking Rimabex.

What is the best time to take Rimabex?

Rimabex works best on an empty stomach. Take it 1 hour before or at least 2 hours after a meal.

How long does it take to work?

Orally administered Rimabex results in peak plasma concentrations in about 2–4 hours.

How often can I take Rimabex?

When Rimabex is used to treat tuberculosis, it is taken once daily. When Rimabex is used to prevent the spread of Neisseria meningitidis bacteria to other people, it is taken twice daily for 2 days or once daily for 4 days.

What happens if I miss a dose of?

Use the medicine as soon as you can, but skip the missed dose if it is almost time for your next dose. Do not use two doses at one time.

What happens if I overdose?

Seek emergency medical attention,Overdose can cause worsening symptoms such as nausea, vomiting, stomach pain, itching, headache, lack of energy leading to loss of consciousness, and dark or discolored skin, saliva, tears, urine, or stools.

How many Rimabex should I take?

Adults 600 milligrams (mg) 2 times a day for 2 days. Children 1 month of age and older Dose is based on body weight and must be determined by your doctor.

Can Rimabex be taken twice a day?

 For adults, it is recommended that 600 mg Rimabex be administered twice daily for two days.

How long does Rimabex stay in my system?

Rimabex administration, the half-life decreases and reaches average values of approximately 2 to 3 hours.

Can I take Rimabex at night?

Take your Rimabex as often and as long as your doctor or nurse tells you. If your stomach is upset.It is okay to take your Rimabex with a small amount of food or try taking it at bedtime.

Does Rimabex cause liver damage?

If your stomach is upset, it is okay to take your Rimabex with a small amount of food or try taking it at bedtime.

Is Rimabex toxic?

Rimabex has proved to be a valuable antibiotic with relatively few major adverse effects. Its toxicity is predominantly hepatic and immunoallergic in character.

Can Rimabex cause hepatitis?

Rimabex caused significant hepatitis in 7.3% of patients treated for cholestatic liver disease in our centre.

*** Taking medicines without doctor's advice can cause long-term problems.
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