rifampicin


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Related to rifampicin: ethambutol, Pyrazinamide

rifampin

 [rif-am´pin]
a semisynthetic derivative of rifamycin, with the antibacterial actions and uses of the rifamycin group; administered orally or intravenously.

rifampin (rifampicin (UK))

Rifadin, Rofact (CA)

Pharmacologic class: Rifamycin derivative

Therapeutic class: Antitubercular

Pregnancy risk category C

Action

Inhibits RNA synthesis by blocking RNA transcription in susceptible organisms (mycobacteria and some gram-positive and gram-negative bacteria)

Availability

Capsules: 150 mg, 300 mg

Powder for injection: 600 mg/vial

Indications and dosages

Tuberculosis

Adults: 10 mg/kg/day (up to 600 mg/day) P.O. or I.V. infusion as a single dose

Children: 10 to 20 mg/kg/day (up to 600 mg/day) P.O. or I.V. infusion as a single dose

Asymptomatic Neisseria meningitidis carriers

Adults: 600 mg P.O. or I.V. infusion b.i.d. for 2 days

Children ages 1 month and older: 10 mg/kg/day P.O. or I.V. infusion (up to 600 mg/day) q 12 hours for 2 days

Infants younger than 1 month old: 5 mg/kg P.O. or I.V. infusion q 12 hours for 2 days

Off-label uses

Mycobacterium avium intracellulare complex infection

• Brucellosis

Haemophilus influenzae type B

• Severe staphylococcal bone and joint infections

• Prosthetic valve endocarditis caused by coagulase-negative staphylococci

• Leprosy

• Prophylaxis in high-risk close contact of patients with N. meningitidis infections

Contraindications

• Hypersensitivity to drug or other rifamycin derivatives

Precautions

Use cautiously in:

• porphyria

• history of hepatic disease

• concurrent use of other hepatotoxic drugs

• pregnant or breastfeeding patients.

Administration

• Add 10 ml of sterile water to vial to yield a 60-mg/ml solution for I.V. infusion.

• Further dilute in 100 ml of dextrose 5% in water (D5W) and infuse over 30 minutes, or add to 500 ml of D5W and infuse over 3 hours.

• Give oral doses with a full glass of water 1 hour before or 2 hours after a meal.

• For an adult who can't swallow capsules or for a young child, mix capsule contents with syrup, shake well, and administer.

• If patient can't receive dextrose, use normal saline solution to dilute. Don't use other I.V. solutions.

Adverse reactions

CNS: ataxia, confusion, drowsiness, fatigue, headache, asthenia, psychosis, generalized numbness

EENT: conjunctivitis; discolored tears, saliva, and sputum

GI: nausea, vomiting, diarrhea, abdominal cramps, dyspepsia, epigastric distress, flatulence, discolored feces, anorexia, sore mouth and tongue, pseudomembranous colitis

GU: discolored urine

Hematologic: eosinophilia, transient leukopenia, hemolytic anemia, hemolysis, disseminated intravascular coagulation (DIC), thrombocytopenia

Hepatic: jaundice

Metabolic: hyperuricemia

Musculoskeletal: myalgia, joint pain

Respiratory: dyspnea, wheezing

Skin: flushing, rash, pruritus, discolored sweat, erythema multiforme, toxic epidermal necrolysis, Stevens-Johnson syndrome

Other: flulike symptoms, hypersensitivity reactions including vasculitis

Interactions

Drug-drug. Barbiturates, beta-adrenergic blockers, cardiac glycosides, clarithromycin, clofibrate, cyclosporine, dapsone, diazepam, doxycycline, fluoroquinolones (such as ciprofloxacin), haloperidol, levothyroxine, methadone, progestins, quinine, tacrolimus, theophylline, tricyclic antidepressants, zidovudine: increased metabolism of these drugs Chloramphenicol, corticosteroids, disopyramide, efavirenz, estrogens, fluconazole, hormonal contraceptives, itra-conazole, ketoconazole, nevirapine, quinidine, opioid analgesics, oral hypoglycemics, phenytoin, quinidine, ritonavir, theophylline, tocainide, verapamil, warfarin: decreased efficacy of these drugs Delavirdine, indinavir, nelfinavir, saquinavir: decreased blood levels of these drugs

Hepatotoxic drugs (including isoniazid, ketoconazole, pyrazinamide): increased risk of hepatotoxicity

Drug-diagnostic tests. Alanine aminotransferase, alkaline phosphatase, aspartate aminotransferase, bilirubin, blood urea nitrogen, uric acid: increased levels

Dexamethasone suppression test: interference with results

Direct Coombs' test: false-positive result

Folate, vitamin B12 assay: interference with standard assays

Hemoglobin: decreased value

Liver function tests: abnormal values (transient)

Sulfobromophthalein uptake and excretion test: delayed hepatic uptake and excretion

Drug-behaviors. Alcohol use: increased risk of hepatotoxicity

Patient monitoring

• Monitor kidney and liver function tests, CBC, and uric acid level.

Watch for signs and symptoms of bleeding tendency, especially DIC.

• Assess for signs and symptoms of hepatic impairment.

• Monitor bowel movements for diarrhea, which may signal pseudomembranous colitis.

Patient teaching

• Advise patient to take oral dose 1 hour before or 2 hours after meals. If drug causes significant GI upset, instruct him to take it with meals. To further minimize GI upset, teach him to eat small, frequent servings of food and drink plenty of fluids.

Instruct patient to immediately report easy bruising or bleeding, fever, malaise, appetite loss, nausea, vomiting, or yellowing of skin or eyes.

• Tell patient drug may color his tears, urine, and other body fluids reddish or brownish orange. Instruct him not to wear contact lenses during therapy, because drug may stain them permanently.

• Instruct patient not to drink alcohol.

• Caution patient to avoid driving and other hazardous activities until he knows how drug affects concentration and alertness.

• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs, tests, and behaviors mentioned above.

rifampicin

(rĭ-făm′pĭ-sĭn)
n.

rifampicin

An antibiotic drug used mainly to treat TUBERCULOSIS and LEPROSY, but also LEGIONNAIRES' DISEASE, PROSTATITIS, ENDOCARDITIS and OSTEOMYELITIS. Rifampicin acts by inhibiting transcription of bacterial nucleic acid. It interferes with the action of oral contraceptives. The drug is on the WHO official list. Brand names are Rifadin and Rimactane.
References in periodicals archive ?
MDR patients are defined as patients who are found to be resistant to isoniazid and rifampicin drugs.
From this study we conclude that due to advent of CB-NAAT, diagnosis of tuberculosis and Rifampicin resistant TB is earlier (Within 2 hrs.) and simpler than any other conventional cultural method.
Qualitative data are presented as frequencies of occurrence and the concentrations of rifampicin in plasma as mean with 95% confidence interval.
Evaluation of molecular detection of extrapulmonary tuberculosis and resistance to rifampicin with GeneXpertA(r) MTB/RIF.
Pharmacokinetic/ pharmacodynamic analysis of an intensified regimen containing rifampicin and moxifloxacin for tuberculous meningitis.
Rifampicin and the other antimycobacterial drugs were discontinued.
[1] A meta-analysis of GeneXpert MTB/RIF for resistance testing in 566 tissue samples from 13 studies reported the prevalence of rifampicin resistance to be 5.4%.
Conclusion: GeneExpert MTB/RIF is an efficient method to detect mycobacterium TB along with Rifampicin sensitivity in cervical lymph node tissue specimens.
CBNAAT also diagnosed 12 (8.75%) cases of Rifampicin resistance among the 137 Myobacterium tuberculosis positive cases.
Isoniazid 0.2 [micro]g/ml Ethambutol 2 [micro]g/ml Streptomycin 4 [micro]g/ml Rifampicin 40 [micro]g/ml Result
tuberculosis infection resistant to a single antituberculosis drug, MDR-TB as resistant to both isoniazid and rifampicin, and poly-resistant TB as resistant to more than one anti-tuberculosis drug (other than the combination of isoniazid and rifampicin).
Almost all rifampicin resistance is caused due to mutation in rpoB gene while mutations in the katG and inhA genes confer high-level and low-level INH resistance, respectively [6].