Rifampin (Rifampicin)

Table of contents

  • Brand Names
  • Drug Combinations
  • Chemistry
  • Pharmacologic Category
  • Mechanism of Action
  • Therapeutic Use
  • Unlabeled Use
  • Pregnancy and Lactation Implications
  • Contraindications
  • Warnings and Precautions
  • Adverse Reactions
  • Caution and personalized dose adjustment in patients with the following genotypes
  • Other genes that may be involved
  • Substrate of
  • Inhibits
  • Induces
  • Drug Interactions
  • Nutrition/Nutraceutical Interactions
  • Dosage
  • Pharmacokinetics and Pharmacodynamics
  • Special Considerations

Brand Names

Europe

Austria: Eremfat, Rifoldin, Rimactan; Belgium: Rifadine; Bulgaria: Tubocin; Cyprus: Rifaren, Rifasynt, Syntoren; Czech Republic: Arficin, Benemicin, Eremfat; Denmark: Rimactan; Finland: Rimapen; France: Rifadine, Rimactan; Germany: Eremfat, Rifa, Rifampicin, Rimactan; Greece: Rifadin, Rifaldin; Hungary: Rifamed; Ireland: Rifadin, Rimactane; Italy: Rifadin, Rifampic; Latvia: Benemicin; Lithuania: Benemicin, Tubocin; Luxembourg: Rifadine, Rimactan; Malta: Eremfat, Rifadin, Rifampcin, Rifasynt; Netherlands: Rifadin, Rifampicine; Poland: Rifampicyna; Portugal: Rifadin, Rifex; Romania: Rifampicina, Sinerdol; Slovakia: Benemicin; Slovenia: Arficin; Spain: Rifaldin, Rimactán; Sweden: Rifadin, Rimactan; UK: Rifadin, Rimactane.

North America

Canada: Rifadin, Rofact; USA: Rifadin, Rifampin.

Latin America

Argentina: Rifadin, Rifampicina; Brazil: Monicil-Rifampicina, Rifaldin, Rifamp; Mexico: Alfiral, Eurifam, Finamicina, Pestarin, Rifadin, Rifampicina, Rimactan, Turifam.

Asia

Japan: Aptecin, Rifadin, Rimactane.

Drug combinations

Rifampin and Isoniazid

Rifampin and Trimethoprim

Rifampin, Isoniazid, and Pyrazinamide

Rifampin, Ethambutol, Isoniazid, and Pyrazinamide

Chemistry

Rifampin: C~43~H~58~N~4~O~12~. Mw: 822.94. (1) Rifamycin, 3-[[(4-methyl-1-piperazinyl)imino]methyl]-; (2) 5,6,9,17,19,21-Hexahydroxy-23-methoxy-2,4,12,16,18,20,22-heptamethyl-8-[N-(4-methyl-1-piperazinyl)formimidoyl]-2,7-(epoxypentadeca[1,11,13]trienimino)naphtho[2,1-b]furan-1,11(2H)-dione 21-acetate. CAS-13292-46-1 (1968).

Pharmacologic Category

Antimycobacterials; Antituberculosis Agents. Miscellaneous Antibacterials; Rifamycins. (ATC-Code: J04AB02).

Mechanism of action

Inhibits bacterial RNA synthesis by binding to β-subunit of DNA-dependent RNA polymerase, blocking RNA transcription.

Therapeutic use

Management of active tuberculosis in combination with other agents. Elimination of meningococci from nasopharynx in asymptomatic carriers.

Pregnancy and lactiation implications

Due to risk of tuberculosis to fetus, treatment recommended when probability of maternal disease is moderate to high. Postnatal hemorrhages reported in infant and mother with isoniazid administration during last few weeks of pregnancy. Enters breast milk (not recommended in nursing women).

Unlabeled use

Prophylaxis of Haemophilus influenzae type b infection. Legionella pneumonia. Used in combination with other anti-infectives in treatment of staphylococcal infections. Treatment of M. leprae infections.

Contraindications

Hypersensitivity to rifampin, any rifamycins, or any component of the formulation. Concurrent use of amprenavir, saquinavir/ritonavir (possibly other protease inhibitors).

Warnings and precautions

Regimens of >600 mg once or twice weekly associated with high incidence of adverse reactions including flu-like syndrome. May cause thrombocytopenia, leukopenia, or anemia with regimens >600 mg once or twice weekly. Hypersensitivity reactions occurred in patients taking >600 mg once or twice weekly. Prolonged use may result in fungal or bacterial superinfection, including C. difficile-associated diarrhea and pseudomembranous colitis. Use with caution in history of alcoholism (even if ethanol consumption is discontinued during therapy), and in liver impairment. Do not use for meningococcal disease, only for short-term treatment of asymptomatic carrier states. Use with caution in porphyria (exacerbations reported due to enzyme-inducing properties), and in patients receiving concurrent medications associated with hepatotoxicity. Do not administer I.V. form via I.M. or SubQ routes. Soft contact lenses should be removed during therapy (permanent staining may occur). Urine, feces, saliva, sweat, tears, and CSF may be discolored to red/orange.

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