Rifampicin


Generic Medicine Info
Indications and Dosage
Intravenous
Leprosy
Adult: In combination with at least 1 other anti-leprosy agent: 10 mg/kg once monthly. Max: 450 mg for patients weighing <50 kg; 600 mg for patients weighing ≥50 kg. Alternatively, 600 mg once monthly.

Intravenous
Tuberculosis
Adult: In combination with other anti-tuberculosis drugs: 10 mg/kg once daily via infusion over 2-3 hours. Max: 600 mg daily.
Child: In combination with other anti-tuberculosis drugs: 10-20 mg/kg once daily. Max: 600 mg daily.

Intravenous
Brucellosis, Legionnaire's disease, Severe staphylococcal infections
Adult: In combination with other antibacterial agents: 600-1,200 mg daily in 2-4 divided doses.

Oral
Brucellosis, Legionnaire's disease, Severe staphylococcal infections
Adult: In combination with other antibacterial agents: 600-1,200 mg daily in 2-4 divided doses.

Oral
Prophylaxis against meningitis due to Haemophilus influenzae
Adult: 20 mg/kg (Max 600 mg) once daily for 4 days.
Child: <1 month 10 mg/kg daily; ≤4 years Same as adult dose.

Oral
Tuberculosis
Adult: In combination with other anti-tuberculosis agents: Recommended dose: 8-12 mg/kg once daily. Usual dose: <50 kg: 450 mg daily; ≥50 kg: 600 mg daily.
Child: In combination with other anti-tuberculosis agents: 10-20 mg/kg daily. Max: 600 mg daily.

Oral
Prophylaxis of meningococcal meningitis
Adult: 600 mg bid for 2 days.
Child: <1 month 5 mg/kg bid; ≥1 month 10 mg/kg bid. Doses to be given for 2 days.

Oral
Leprosy
Adult: In combination with at least 1 other anti-leprosy agent: 600 mg once monthly. Alternatively, 10 mg/kg once monthly. Max: 450 mg for patients weighing <50 kg; 600 mg for patients weighing ≥50 kg.
Hepatic Impairment
Max: 8 mg/kg daily.
Administration
Should be taken on an empty stomach. Best taken on an empty stomach 1 hr before or 2 hr after meals.
Reconstitution
Reconstitute vial labelled as 600 mg with 10 mL sterile water for injection then dilute further with an appropriate volume of compatible solution (e.g. dextrose 5% in water) to a final concentration not exceeding 6 mg/mL.
Incompatibility
Y-site: Diltiazem HCl.
Contraindications
Hypersensitivity to rifampicin or other rifamycins. Jaundice. Concomitant use with saquinavir/ritonavir combination; atazanavir, darunavir, fosamprenavir, saquinavir, tipranavir.
Special Precautions
Patient with current or history of alcoholism, risk factors of vitamin K deficiency (e.g. chronic liver disease, poor nutritional status, receiving prolonged antibacterial or anticoagulant therapy), diabetes mellitus, porphyria. Renal (for doses >600 mg/day) and hepatic impairment. Children and elderly. Pregnancy and lactation.
Adverse Reactions
Significant: Hypersensitivity reactions (e.g. fever, rash, urticaria, angioedema, flu-like syndrome); superinfection (e.g. pseudomembranous colitis), anaemia, leucopenia, thrombocytopenia (with or without purpura), discolouration (yellow, orange, red, or brown) of teeth, urine, sweat sputum, tears; vitamin K-dependent coagulopathy, bleeding.
Eye disorders: Visual disturbances.
Gastrointestinal disorders: Nausea, vomiting.
General disorders and administration site conditions: Chills, fatigue, pyrexia.
Investigations: Increased blood bilirubin, AST, ALT.
Metabolism and nutrition disorders: Facial or peripheral oedema.
Musculoskeletal and connective tissue disorders: Muscle weakness, pain in extremities.
Nervous system disorders: Headache, dizziness, drowsiness, generalised numbness.
Psychiatric disorders: Mental confusion, behavioural changes, inability to concentrate.
Reproductive system and breast disorders: Menstrual disturbances.
Potentially Fatal: Hepatotoxicity (e.g. hyperbilirubinaemia, elevated liver enzymes, jaundice, hepatitis, fulminant liver failure) severe cutaneous reactions (e.g. Stevens-Johnson syndrome, toxic epidermal necrolysis, drug reaction with eosinophilia and systemic symptoms (DRESS), acute generalised exanthematous pustulosis).
IV/Parenteral/PO: C
Patient Counseling Information
This drug may cause permanent staining of soft contact lenses. Remove soft contact lenses during therapy.
Monitoring Parameters
Perform culture and susceptibility tests; consult local institutional recommendations before treatment initiation due to antibiotic resistance risks. Monitor LFTs (AST, ALT, bilirubin) at baseline and periodically (every 2-4 weeks) during therapy in patients with pre-existing hepatic impairment; serum creatinine and CBC at baseline and periodically in patients with baseline abnormalities; sputum culture, chest X-ray 2-3 months into treatment, coagulation tests during therapy in patient at risk of vitamin K deficiency.
Overdosage
Symptoms: Nausea, vomiting, abdominal pain, pruritus, headache, lethargy; unconsciousness (in presence of severe hepatic disease); transient increases in liver enzymes and bilirubin; brownish-red or orange discolouration of the skin, urine, sweat, saliva, tears, faeces; facial or periorbital oedema (particularly in children); liver enlargement, hypotension, sinus tachycardia, ventricular arrhythmias, seizures, cardiac arrest. Management: Supportive and symptomatic treatment. Secure airway and establish an adequate respiratory exchange. Perform gastric lavage within 2-3 hours of ingestion to induce emesis followed by instillation of activated charcoal into the stomach. May administer antiemetic agents to control severe nausea and vomiting. May consider active diuresis, with measured intake and output, to promote excretion. For severe cases, haemodialysis may also be considered.
Drug Interactions
May increase the risk of hepatotoxicity when given with halothane or isoniazid. May decrease the serum concentrations, thus reducing the efficacy of praziquantel. May enhance the adverse effect, particularly bleeding, when given concomitantly with cefazolin and other cephalosporins containing N-methylthiotetrazole side chain. May increase metabolism and decrease serum concentrations and effects of antiarrhythmics (e.g. disopyramide, quinidine), antiepileptics (e.g. phenytoin,), barbiturates, hormone antagonist (e.g. tamoxifen, toremifene), antipsychotics (e.g. haloperidol, aripiprazole), anticoagulants (e.g. warfarin), antifungals (e.g. fluconazole, ketoconazole), other antiretrovirals (e.g. zidovudine, indinavir, efavirenz), hepatitis C antiviral drugs (e.g. daclatasvir), beta-blockers (e.g. bisoprolol), Ca channel blocker (e.g. diltiazem), anxiolytics and hypnotics (e.g. diazepam), certain antibacterials (e.g. chloramphenicol, clarithromycin), corticosteroids, cardiac glycosides, hormonal contraceptives (e.g. oestrogens, progestogens), antidiabetic agents (e.g. glipizide, rosiglitazone), immunosuppressants (e.g. ciclosporin, tacrolimus), thyroid hormone (e.g. levothyroxine), analgesics (e.g. methadone, morphine), selective 5-HT3 receptor antagonists (e.g. ondansetron), statins that are metabolised by CYP3A4 (e.g. simvastatin), TCAs (e.g. amitriptyline, nortriptyline), cytotoxics (e.g. imatinib), enalapril, losartan, irinotecan, theophylline, quinine, riluzole. Absorption may be reduced by antacids. Concomitant use with atovaquone increased plasma concentrations of rifampicin and decreased plasma concentrations of atovaquone. Increased plasma concentrations with probenecid and trimethoprim-sulfamethoxazole.
Potentially Fatal: Increased risk of severe hepatotoxicity with saquinavir/ritonavir combination. May substantially decrease the plasma concentrations and efficacy of atazanavir, darunavir, fosamprenavir, saquinavir, tipranavir which may result in the development of viral resistance.
Food Interaction
Delayed and reduced absorption with food.
Lab Interference
Interferes with standard microbiological assays for serum folate and vitamin B12. Cross-reactivity and false-positive urine screening tests for opiates using the Kinetic Interaction of Microparticles in Solution (KIMS) method (e.g. Roche diagnostic systems, Abuscreen online opiates assay). Interferes with the biliary excretion of contrast media used for visualisation of the gallbladder.
Action
Description: Rifampicin binds to the β subunit of DNA-dependent RNA polymerase leading to inhibition of bacterial RNA synthesis.
Synonym: rifampin.
Duration: ≤24 hours.
Pharmacokinetics:
Absorption: Readily and well absorbed from the gastrointestinal tract. Reduced and delayed absorption with food. Time to peak plasma concentrations: 2-4 hours.
Distribution: Widely distributed in most body tissues and fluids, including CSF. Crosses the placenta and blood-brain barrier; enters breast milk. Plasma protein binding: Approx 80%.
Metabolism: Rapidly metabolised in the liver mainly to active 25-O-deacetylrifampicin; undergoes enterohepatic recirculation.
Excretion: Via faeces (60-65%); urine (approx 30%, with approx 50% as unchanged drug). Elimination half-life: 3-4 hours.
Chemical Structure

Chemical Structure Image
Rifampicin

Source: National Center for Biotechnology Information. PubChem Database. Rifampicin, CID=135398735, https://pubchem.ncbi.nlm.nih.gov/compound/Rifampicin (accessed on Jan. 22, 2020)

Storage
Store between 15-30°C. Protect from light and excessive heat.
MIMS Class
Anti-TB Agents
ATC Classification
J04AB02 - rifampicin ; Belongs to the class of antibiotics. Used in the systemic treatment of tuberculosis.
References
Anon. Rifampin. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 03/06/2020.

Buckingham R (ed). Rifampicin. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 03/06/2020.

Joint Formulary Committee. Rifampicin. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 03/06/2020.

Rifadin 150 mg Capsules (Aventis Pharma Limited). MHRA. https://products.mhra.gov.uk/. Accessed 03/06/2020.

Rifadin Capsule, IV Injection, Powder, Lyophilized, for Solution (Sanofi-Aventis U.S. LLC). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 03/06/2020.

Rifadin for Infusion 600 mg (Aventis Pharma Limited). MHRA. https://products.mhra.gov.uk/. Accessed 03/06/2020.

Sanofi-Aventis New Zealand Limited. Rifadin Capsules, Tablets, Syrup and Infusion data sheet 29 July 2019. Medsafe. http://www.medsafe.govt.nz/. Accessed 03/06/2020.

Disclaimer: This information is independently developed by MIMS based on Rifampicin from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to MIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, MIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2024 MIMS. All rights reserved. Powered by MIMS.com
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