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Rifampicin (trade names include Rifampin, Rifadin, Rifaldin, Rifamtibi, Rifasynt, Rifoldin, Rimactane, Rimaped, Rimycin, Rofact) is an antibiotic from drugs for treatment of tuberculosis pharmacological group. This medicine is used for the treatment of several types of bacterial infections, including tuberculosis, Mycobacterium tuberculosis, Mycobacterium bovis, Mycobacterium avium complex, methicillin-resistant Staphylococcus aureus (MRSA), Chlamydia pneumoniae, Neisseria meningitidis (meningococcal) infections, tick-borne pathogens Borrelia burgdorferi and Anaplasma phagocytophilum, Listeria species, Neisseria gonorrhoeae, Haemophilus influenzae, meningitis, Legionnaires' disease, Legionella pneumophila, primary amoebic meningoencephalitis caused by Naegleria fowleri, pruritus caused by primary biliary cholangitis, leprosy, vaccinia virus, in biotechnology as bacterial RNA polymerase inhibitor. Rifampicin inhibits bacterial DNA-dependent RNA synthesis by inhibiting bacterial DNA-dependent RNA polymerase.
Pharmacological and medical categories:
Anti tuberculosis drugs
J - Antiinfectives for systemic use
J04 - Antimycobacterials
J04A - Drugs for treatment of tuberculosis
J04AB - Antibiotics
J04AB02 - Rifampicin
Tuberculosis - A15-A19
Leprosy [Hansen's disease] - A30
Listeriosis - A32
Meningococcal infection - A39
Other bacterial diseases, not elsewhere classified - A48
Legionnaires' disease - A48.1
Gonococcal infection - A54
Other spirochetal infections - A69
Lyme disease - A69.2
Spotted fever [tick-borne rickettsioses] - A77
Other viral infections characterized by skin and mucous membrane lesions, not elsewhere classified - B08
Other protozoal diseases, not elsewhere classified - B60
Naegleriasis - B60.2
Streptococcus, Staphylococcus, and Enterococcus as the cause of diseases classified elsewhere - B95
Methicillin resistant Staphylococcus aureus infection as the cause of diseases classified elsewhere - B95.62
Other bacterial agents as the cause of diseases classified elsewhere - B96
Hemophilus influenzae [H. influenzae] as the cause of diseases classified elsewhere - B96.3
Meningitis due to other and unspecified causes - G03
Pneumonia due to other infectious organisms, not elsewhere classified - J16
Chlamydial pneumonia - J16.0
Pruritus - L29
Indications and usage:
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 rifampin and 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.
To reduce the development of drug-resistant bacteria and maintain the effectiveness of rifampin and other antibacterial drugs, rifampin should be used only to treat or prevent infections that are proven or strongly suspected to be caused by susceptible bacteria. When culture and susceptibility information are available, they should be considered in selecting or modifying antibacterial therapy. In the absence of such data, local epidemiology and susceptibility patterns may contribute to the empiric selection of therapy.
Dosage and administration:
Rifampin can be administered by the oral route or by IV infusion. IV doses are the same as those for oral.
Signs and Symptoms
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.
Treatment Intensive support measures should be instituted and individual symptoms treated as they arise. The airway should be secured and adequate respiratory exchange established. Since nausea and vomiting are likely to be present, gastric lavage within the first 2 to 3 hours after ingestion is probably preferable to induction of emesis. Following evacuation of the gastric contents, the instillation of activated charcoal slurry into the stomach may help absorb any remaining drug from the gastrointestinal tract. Antiemetic medication may be required to control severe nausea and vomiting.
Active diuresis (with measured intake and output) will help promote excretion of the drug.
For severe cases, extracorporeal hemodialysis may be required. If this is not available, peritoneal dialysis can be used along with forced diuresis.
Rifampicin 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.
This medication 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.
Rifampin 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.
Rifadin should be used with caution in patients with a history of diabetes mellitus, as diabetes management may be more difficult.
Prescribing rifampin in the absence of a proven or strongly suspected bacterial infection or a prophylactic indication is unlikely to provide benefit to the patient and increases the risk of the development of drug-resistant bacteria.
For the treatment of tuberculosis, rifampin is usually administered on a daily basis. Doses of rifampin greater than 600 mg given once or twice weekly have resulted in a higher incidence of adverse reactions, including the "flu syndrome" (fever, chills and malaise), hematopoietic reactions (leukopenia, thrombocytopenia, or acute hemolytic anemia), cutaneous, gastrointestinal, and hepatic reactions, shortness of breath, shock, anaphylaxis, and renal failure. Recent studies indicate that regimens using twice-weekly doses of rifampin 600 mg plus isoniazid 15 mg/kg are much better tolerated.
Rifampin is not recommended for intermittent therapy; the patient should be cautioned against intentional or accidental interruption of the daily dosage regimen since rare renal hypersensitivity reactions have been reported when therapy was resumed in such cases.
Rifampicin has enzyme induction properties that can enhance the metabolism of endogenous substrates including adrenal hormones, thyroid hormones, and vitamin D. Rifampin and isoniazid have been reported to alter vitamin D metabolism. In some cases, reduced levels of circulating 25-hydroxy vitamin D and 1,25-dihydroxy vitamin D have been accompanied by reduced serum calcium and phosphate, and elevated parathyroid hormone.
Adverse reactions, side effects:
Heartburn, epigastric distress, anorexia, nausea, vomiting, jaundice, flatulence, cramps, and diarrhea have been noted in some patients. Although Clostridium difficile has been shown in vitro to be sensitive to rifampin, pseudomembranous colitis has been reported with the use of rifampin (and other broad spectrum antibiotics). Therefore, it is important to consider this diagnosis in patients who develop diarrhea in association with antibiotic use.
Transient abnormalities in liver function tests (e.g., elevations in serum bilirubin, BSP, alkaline phosphatase, serum transaminases) have been observed. Rarely, hepatitis or a shock-like syndrome with hepatic involvement and abnormal liver function tests has been reported.
Thrombocytopenia has occurred primarily with high dose intermittent therapy, but has also been noted after resumption of interrupted treatment. It rarely occurs during well supervised daily therapy. This effect is reversible if the drug is discontinued as soon as purpura occurs. Cerebral hemorrhage and fatalities have been reported when rifampin administration has been continued or resumed after the appearance of purpura.
Rare reports of disseminated intravascular coagulation have been observed.
Leukopenia, hemolytic anemia, and decreased hemoglobin have been observed.
Agranulocytosis has been reported very rarely.
Central Nervous System
Headache, fever, drowsiness, fatigue, ataxia, dizziness, inability to concentrate, mental confusion, behavioral changes, muscular weakness, pains in extremities, and generalized numbness have been observed.
Psychoses have been rarely reported.
Rare reports of myopathy have also been observed.
Visual disturbances have been observed.
Menstrual disturbances have been observed.
Rare reports of adrenal insufficiency in patients with compromised adrenal function have been observed. Renal Elevations in BUN and serum uric acid have been reported. Rarely, hemolysis, hemoglobinuria, hematuria, interstitial nephritis, acute tubular necrosis, renal insufficiency, and acute renal failure have been noted. These are generally considered to be hypersensitivity reactions. They usually occur during intermittent therapy or when treatment is resumed following intentional or accidental interruption of a daily dosage regimen, and are reversible when rifampin is discontinued and appropriate therapy instituted.
Cutaneous reactions are mild and self-limiting and do not appear to be hypersensitivity reactions. Typically, they consist of flushing and itching with or without a rash. More serious cutaneous reactions which may be due to hypersensitivity occur but are uncommon.
Occasionally, pruritus, urticaria, rash, pemphigoid reaction, erythema multiforme including Stevens-Johnson Syndrome, toxic epidermal necrolysis, vasculitis, eosinophilia, sore mouth, sore tongue, and conjunctivitis have been observed.
Anaphylaxis has been reported rarely.
Edema of the face and extremities has been reported. Other reactions reported to have occurred with intermittent dosage regimens include "flu syndrome" (such as episodes of fever, chills, headache, dizziness, and bone pain), shortness of breath, wheezing, decrease in blood pressure and shock. The "flu syndrome" may also appear if rifampin is taken irregularly by the patient or if daily administration is resumed after a drug free interval.
Healthy subjects who received rifampin 600 mg once daily concomitantly with saquinavir 1000 mg/ritonavir 100 mg twice daily (ritonavir-boosted saquinavir) developed severe hepatocellular toxicity. Therefore, concomitant use of these medications is contraindicated.
Enzyme Induction: Rifampin is known to induce certain cytochrome P-450 enzymes. Administration of rifampin with drugs that undergo biotransformation through these metabolic pathways may accelerate elimination of coadministered drugs. To maintain optimum therapeutic blood levels, dosages of drugs metabolized by these enzymes may require adjustment when starting or stopping concomitantly administered rifampin.
Rifampin has been reported to substantially decrease the plasma concentrations of the following antiviral drugs: atazanavir, darunavir, fosamprenavir, saquinavir, and tipranavir. These antiviral drugs must not be co-administered with rifampin.
Rifampin has been reported to accelerate the metabolism of the following drugs: anticonvulsants (eg, phenytoin), digitoxin, antiarrhythmics (eg, disopyramide, mexiletine, quinidine, tocainide), oral anticoagulants, antifungals (eg, fluconazole, itraconazole, ketoconazole), barbiturates, beta-blockers, calcium channel blockers (eg, diltiazem, nifedipine, verapamil), chloramphenicol, clarithromycin, corticosteroids, cyclosporine, cardiac glycoside preparations, clofibrate, oral or other systemic hormonal contraceptives, dapsone, diazepam, doxycycline, fluoroquinolones (eg, ciprofloxacin), haloperidol, oral hypoglycemic agents (sulfonylureas), levothyroxine, methadone, narcotic analgesics, progestins, quinine, tacrolimus, theophylline, tricyclic antidepressants (eg, amitriptyline, nortriptyline) and zidovudine. It may be necessary to adjust the dosages of these drugs if they are given concurrently with rifampin.
Patients using oral or other systemic hormonal contraceptives should be advised to change to nonhormonal methods of birth control during rifampin therapy.
Rifampin has been observed to increase the requirements for anticoagulant drugs of the coumarin type. In patients receiving anticoagulants and rifampin concurrently, it is recommended that the prothrombin time be performed daily or as frequently as necessary to establish and maintain the required dose of anticoagulant.
Other Interactions: When the two drugs were taken concomitantly, decreased concentrations of atovaquone and increased concentrations of rifampin were observed.
Concurrent use of ketoconazole and rifampin has resulted in decreased serum concentrations of both drugs. Concurrent use of rifampin and enalapril has resulted in decreased concentrations of enalaprilat, the active metabolite of enalapril. Dosage adjustments should be made if indicated by the patient's clinical condition.
Concomitant antacid administration may reduce the absorption of rifampin. Daily doses of rifampin should be given at least 1 hour before the ingestion of antacids.
Probenecid and cotrimoxazole have been reported to increase the blood level of rifampin.
When rifampin is given concomitantly with either halothane or isoniazid, the potential for hepatotoxicity is increased. The concomitant use of rifampin and halothane should be avoided. Patients receiving both rifampin and isoniazid should be monitored close for hepatotoxicity.
Plasma concentrations of sulfapyridine may be reduced following the concomitant administration of sulfasalazine and rifampin. This finding may be the result of alteration in the colonic bacteria responsible for the reduction of sulfasalazine to sulfapyridine and mesalamine.
C - Australia
C - United States (Risk cannot be ruled out)
Salts and other forms:
Synonyms, international and chemical names:
Brands, generics, trade names:
Benemicin - Polfa
Rifacept - Concept Pharmaceuticals
Rifadin - Sanofi-Aventis, Pfizer, Sandoz
Rifaldin - Sanofi-Aventis
Rifamtibi - Sanbe Farma
Rifasynt - Medochemie, Komedic, Medline, Star Medical Supplies
Rifoldin - Sanofi-Aventis
Rifwell - Wellona Pharma
Rimactane - Novartis, F.P. Marketing, IDS Group, Medical Supplies, Malaysia, Orphan Pharmaceutical, Sandoz, Zuellig Pharma
Rimaped - Pediatrica, United Laboratories
Rimycin - Alphapharm
Rofact - Valeant Pharmaceuticals, ICN Pharmaceuticals
Tubocin - Antibiotic Company
Rifampicin main article on Wikipedia: https://en.wikipedia.org/wiki/Rifampicin
Rifampicin compound on PubChem: https://pubchem.ncbi.nlm.nih.gov/compound/Rifampicin
Rifampicin Sodium compound on PubChem: https://pubchem.ncbi.nlm.nih.gov/compound/Rifampicin-sodium
Rifampicin on DrugBank: https://www.drugbank.ca/drugs/DB01045
Rifampicin Sodium on DrugBank: https://www.drugbank.ca/salts/DBSALT001014
Rifampin FAQ on MedlinePlus (revised 04/15/2019): https://medlineplus.gov/druginfo/meds/a682403.html
Rifadin (Rifampin) capsules and Rifadin IV (Rifampin) lyophilized powder for injection drug label info on DailyMed (revised March 26, 2021): https://dailymed.nlm.nih.gov/dailymed/lookup...
Rifampin containing drugs on Drugs-About.com: https://drugs-about.com/ing/rifampin.html
Rifampicin for sale on Pharma Doctor: https://pharma-doctor.com/rifampicin.html
Rifampicin international drug names on Drugs.com: https://www.drugs.com/international/rifampicin.html
Rifadin (Rifampin capsules USP) and Rifadin IV (Rifampin for injection USP) official prescribing information from the U.S. FDA (revised November 2010): https://www.accessdata.fda.gov/drugsatfda_docs/label...
Rifadin (Rifampin capsules USP) and Rifadin IV (Rifampin for injection USP) product monograph from Sanofi-Aventis pharmaceutical company (revised October 2020): http://products.sanofi.us/rifadin/Rifadin.pdf
Rifampin medication guide from Drugs.com (revised June 26, 2020): https://www.drugs.com/mtm/rifampin.html
Rifampicin 300 mg capsules patient information leaflet on Medicines.org.uk (revised December 2019): https://www.medicines.org.uk/emc/files/pil.8789.pdf
Revised: June 2021
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