Monocomponent productsMonocomponent products

11--Capsules: 150 mg, 300 mg ,450mg,600mgCapsules: 150 mg, 300 mg ,450mg,600mg . .

22--Syrup : 100 mg/5 mlSyrup : 100 mg/5 ml

33--Ophthalmic :1% ophthalmic ointmentOphthalmic :1% ophthalmic ointment..

44--I.V. infusion: Powder for injection 600 mgI.V. infusion: Powder for injection 600 mg

RifampicinRifampicin inhibits DNA-inhibits DNA-dependent RNA polymerase dependent RNA polymerase activity in susceptible cells. activity in susceptible cells. Specifically, it interacts with Specifically, it interacts with bacterial RNA polymerase, bacterial RNA polymerase, but does not inhibit the but does not inhibit the mammalian enzymemammalian enzyme . . RifampicinRifampicin may be may be bacteriostatic or bactericidal bacteriostatic or bactericidal depending on the depending on the concentration of drugconcentration of drug

attained at site of infectionattained at site of infection . .

1-The primary indications for rifampicin are for treatment of

tuberculosis and inactive meningitis, along with isoniazid, ethambutol, pyrazinamide and streptomycin. It must be administered regularly daily for several months without break otherwise, the risk of drug-resistant tuberculosis is greatly increased . In fact, this is the primary reason that it is used in tandem with the three aforementioned drugs, particularly isoniazid . This is also the primary motivation behind directly observed therapy for tuberculosis.Rifampicin resistance develops quickly during treatment and rifampicin monotherapy should not be used to treat these infections — it should be used in combination with other antibiotics.

2- for leprosy .

3for Gram positive(Staphylococcus aureus and epidermidis, Streptococcus pyogenes, viridans and pneumoniae) and gram negative bacteria

(Haemophilus influenzae type B) .

4-It has some anti-chlamydial activity.

5 -in vitro activity against some viruses (poxvirus and adenovirus) at high doses .

6- It has recently been used for brucellosis

TuberculosisTuberculosis

IV dosage form is for initial treatment or re treatment IV dosage form is for initial treatment or re treatment when drug cannot be taken by mouthwhen drug cannot be taken by mouth..

AdultAdult

PO/IV 10 mg/kg/day (max, 600 mg/day) or 10 mg/kg 2 PO/IV 10 mg/kg/day (max, 600 mg/day) or 10 mg/kg 2 or 3 times/wk (max, 600 mg)or 3 times/wk (max, 600 mg)..

ChildrenChildren

PO/IV 10 to 20 mg/kg/day (max, 600 mg/day) or 10 to PO/IV 10 to 20 mg/kg/day (max, 600 mg/day) or 10 to 20 mg/kg 2 to 3 times/wk (max, 600 mg)20 mg/kg 2 to 3 times/wk (max, 600 mg)..

LeproyLeproy::600600 mg once monthly,supervised (450 mg for those weighing mg once monthly,supervised (450 mg for those weighing

less than 35 kg)less than 35 kg)..

Haemophilus influenzae type B infectionHaemophilus influenzae type B infection::AdultAdult

2020 mg/kg bodyweight once a day for 4 days. (maximum daily mg/kg bodyweight once a day for 4 days. (maximum daily dose 600 mg)dose 600 mg)..

Children over 3-months oldChildren over 3-months old 2020 mg/kg bodyweight once a day for 4 daysmg/kg bodyweight once a day for 4 days . .

Meningococcal carriersMeningococcal carriersAdultAdult::Meningococcal carriers 600 mg twice daily for two daysMeningococcal carriers 600 mg twice daily for two days . .

ChildrenChildren11 to 12 years 10 mg/kg bodyweightto 12 years 10 mg/kg bodyweight 33 to 12 months 5 mg/kg bodyweightto 12 months 5 mg/kg bodyweight

EyeEye Trachoma (i.e. hyperendemic trachoma or sexually transmitted Trachoma (i.e. hyperendemic trachoma or sexually transmitted trachoma-inclusion conjunctivitis)1% ophthalmic ointment trachoma-inclusion conjunctivitis)1% ophthalmic ointment applied three times daily for six weeksapplied three times daily for six weeks

CardiovascularCardiovascularHypotension; shockHypotension; shock..

CNSCNSHeadache; drowsiness; fatigue; dizziness; inability to concentrate; Headache; drowsiness; fatigue; dizziness; inability to concentrate; mental confusion; generalized numbness; behavioral changes; mental confusion; generalized numbness; behavioral changes; myopathymyopathy..

DermatologicDermatologicRash; pruritus; urticaria; pemphigoid reaction; flushingRash; pruritus; urticaria; pemphigoid reaction; flushing..

EENTEENTVisual disturbances; exudative conjunctivitisVisual disturbances; exudative conjunctivitis..

GIGIHeartburn; epigastric distress; anorexia; nausea; vomiting; gas; cramps; Heartburn; epigastric distress; anorexia; nausea; vomiting; gas; cramps; diarrhea; sore mouth and tongue; pseudomembranous colitis; diarrhea; sore mouth and tongue; pseudomembranous colitis; pancreatitispancreatitis..

GenitourinaryGenitourinaryHemoglobinuria; hematuria; renal insufficiency; acute renal failureHemoglobinuria; hematuria; renal insufficiency; acute renal failure..

HematologicHematologicEosinophilia; transient leukopenia; hemolytic anemia; decreased Eosinophilia; transient leukopenia; hemolytic anemia; decreased hemoglobin; hemolysis; thrombocytopeniahemoglobin; hemolysis; thrombocytopenia..

HepaticHepaticAsymptomatic elevations of liver enzymes and hepatitisAsymptomatic elevations of liver enzymes and hepatitis..

RespiratoryRespiratoryShortness of breath; wheezingShortness of breath; wheezing..

MiscellaneousMiscellaneousAtaxia; muscular weakness; pain in extremities; osteomalacia; Ataxia; muscular weakness; pain in extremities; osteomalacia; myopathy; menstrual disturbances; fever;elevated serum uric acid; myopathy; menstrual disturbances; fever;elevated serum uric acid; possible immunosuppression; abnormal growth of lung tumors; possible immunosuppression; abnormal growth of lung tumors; reduced 25-hydroxycholecalciferol levels; edema of face and reduced 25-hydroxycholecalciferol levels; edema of face and extremities; discolorationextremities; discoloration of body fluids of body fluids..

PregnancyPregnancyCategory CCategory C. .

LactationLactationExcreted in breast milk. Discontinue nursing or drugExcreted in breast milk. Discontinue nursing or drug..

Hepatic FunctionHepatic FunctionDosage adjustment is necessary. Dosage adjustment is necessary. For patients with liver dysfunction, use a dose no exceeding 8 mg/kg bodyweightBody fluidsBody fluidsMedication may cause harmless red-orange discoloration of Medication may cause harmless red-orange discoloration of urine, feces, saliva, sputum, sweat, and tears. Soft contact urine, feces, saliva, sputum, sweat, and tears. Soft contact lenses may be permanently stainedlenses may be permanently stained

11--Rifampicin is contraindicated in known cases of Rifampicin is contraindicated in known cases of

hypersensitivity to the drughypersensitivity to the drug..

22-- It may be contraindicated in pregnancy (because of It may be contraindicated in pregnancy (because of teratogenicity noted in animal studies and since the teratogenicity noted in animal studies and since the effects of drugs on fetus has not been established) effects of drugs on fetus has not been established) except in the presence of a disease such as severe except in the presence of a disease such as severe tuberculosistuberculosis . .

33-- It is contraindicated in alcoholics with severely It is contraindicated in alcoholics with severely

impaired liver function and with jaundiceimpaired liver function and with jaundice . .

AbsorptionAbsorption Rifampicin is readily absorbed fromGIT (90%). Peak Rifampicin is readily absorbed fromGIT (90%). Peak plasma concentration occurs at1.5 to 4hrs after an plasma concentration occurs at1.5 to 4hrs after an oral dose,Absorption decreased 30% when taken with oral dose,Absorption decreased 30% when taken with foodfood..DistributionDistribution::

Intravenous rifampicin has the same distribution as in Intravenous rifampicin has the same distribution as in oral route , Diffuses well into most body tissues and oral route , Diffuses well into most body tissues and fluids, including CSF.Crosses placenta and distributes fluids, including CSF.Crosses placenta and distributes into breast milk. Protein binding is 89%into breast milk. Protein binding is 89%..

T1/2 = three hours range (2 to 5 hours)T1/2 = three hours range (2 to 5 hours)..

This half-life increases with single high doses or This half-life increases with single high doses or with liver disease with liver disease . .

but shortens on repeated dosing because but shortens on repeated dosing because rifampicin is avery effective enzyme inducer rifampicin is avery effective enzyme inducer and increase its own metabolism(as well as that and increase its own metabolism(as well as that of several other drugs) of several other drugs)..

Approximately 85% of rifampicin is Approximately 85% of rifampicin is metabolised by the liver microsomal metabolised by the liver microsomal enzymes to its main and active enzymes to its main and active metabolite -deacetylrifampicinmetabolite -deacetylrifampicin . .

RifampicinRifampicin undergoes enterohepatic undergoes enterohepatic recirculation but not the deacetylated recirculation but not the deacetylated form.Rifampicin increases its own rate form.Rifampicin increases its own rate

of metabolismof metabolism . .RifampicinRifampicin may also be inactivated in may also be inactivated in other parts of the other parts of the body.Formylrifampicin is a urinary body.Formylrifampicin is a urinary metabolite that spontaneously forms in metabolite that spontaneously forms in the urinethe urine..

Primarily through Primarily through bile/fecal (60% to bile/fecal (60% to 65% in feces);renal 65% in feces);renal (6% to 15% excreted (6% to 15% excreted as unchanged, 15% as unchanged, 15% excreted as active excreted as active metabolites, 7% as metabolites, 7% as

inactive metabolites)inactive metabolites)..

Drug InteractionsDrug Interactions

11--Azole antifungal agents, benzodiazepines, Azole antifungal agents, benzodiazepines, beta-blockers, chloramphenicol, beta-blockers, chloramphenicol, clarithromycin, clozapine, oral clarithromycin, clozapine, oral contraceptives, corticosteroids, cyclosporine, contraceptives, corticosteroids, cyclosporine, delavirdine, digitoxin, doxycycline, delavirdine, digitoxin, doxycycline, erythromycin, estrogens, haloperidol, erythromycin, estrogens, haloperidol, hydantoins,losartan, methadone, mexiletine, hydantoins,losartan, methadone, mexiletine, morphine, ondansetron, oral morphine, ondansetron, oral anticoagulants,sulfonylureas, tacrolimus, anticoagulants,sulfonylureas, tacrolimus, theophyllines,TCA,verapamiltheophyllines,TCA,verapamilTherapeutic efficacy may be decreased because Therapeutic efficacy may be decreased because of liver enzyme-inducing properties of of liver enzyme-inducing properties of rifampinrifampin

DigoxinDigoxin May decrease digoxin serum concentrationsMay decrease digoxin serum concentrations..EnalaprilEnalapril May significantly increase BPMay significantly increase BP..HalothaneHalothane Hepatotoxicity and hepatic encephalopathy have been reported Hepatotoxicity and hepatic encephalopathy have been reported with coadministrationwith coadministration..IsoniazidIsoniazid May result in higher rate of hepatotoxicityMay result in higher rate of hepatotoxicity..KetoconazolKetoconazolee May cause treatment failure of either ketoconazole or rifampinMay cause treatment failure of either ketoconazole or rifampin..ProbenecidProbenecid Elevates rifampin levelsElevates rifampin levels..

May inhibit standard microbiological assays for serum May inhibit standard microbiological assays for serum folate and vitamin B 12 . Thus, use alternate assay folate and vitamin B 12 . Thus, use alternate assay methods. Transient abnormalities in LFTs (eg, methods. Transient abnormalities in LFTs (eg, elevation in serum bilirubin, abnormal elevation in serum bilirubin, abnormal bromsulfophthalein excretion, alkaline phosphatase, bromsulfophthalein excretion, alkaline phosphatase, serum transaminases) and reduced biliary excretion of serum transaminases) and reduced biliary excretion of contrast media used for visualization of gallbladder contrast media used for visualization of gallbladder may occur. Therefore, perform these tests before the may occur. Therefore, perform these tests before the

morning dose of rifampinmorning dose of rifampin

SymptomsSymptoms

Nausea, vomiting, increasing lethargy, Nausea, vomiting, increasing lethargy, unconsciousness, liver enlargement, jaundice, unconsciousness, liver enlargement, jaundice, increased direct and total bilirubin levels, increased direct and total bilirubin levels, altered hepatic enzyme levelsaltered hepatic enzyme levels..

11--Instruct patient to take drug on empty stomach, 1 h before or 2 Instruct patient to take drug on empty stomach, 1 h before or 2 

h after mealsh after meals . .

22--Inform patient that body fluids may turn red-orange in color Inform patient that body fluids may turn red-orange in color and that soft contact lenses may become permanently stained. and that soft contact lenses may become permanently stained. Advise patient to wear glasses during course of therapyAdvise patient to wear glasses during course of therapy..

33--Instruct patient to notify health care provider of persistent Instruct patient to notify health care provider of persistent

anorexia, nausea, vomiting, diarrhea, jaundice, fever, change anorexia, nausea, vomiting, diarrhea, jaundice, fever, change in color or consistency of stools, malaise or right upper in color or consistency of stools, malaise or right upper quadrant abdominal pain, unusual bleeding or bruising, quadrant abdominal pain, unusual bleeding or bruising, petechiae, hematuria, bleeding gums, or pallorpetechiae, hematuria, bleeding gums, or pallor . .

44--Tell patient to notify health care provider of drowsiness, Tell patient to notify health care provider of drowsiness, fatigue, dizziness, inability to concentrate, confusion, or visual fatigue, dizziness, inability to concentrate, confusion, or visual

or behavioral changesor behavioral changes..

55--Advise patient who uses oral contraceptives to use Advise patient who uses oral contraceptives to use nonhormonal form of contraception during therapynonhormonal form of contraception during therapy . .

66--Advise patient that drug may cause drowsiness and to use Advise patient that drug may cause drowsiness and to use caution while driving or performing other tasks requiring caution while driving or performing other tasks requiring mental alertnessmental alertness . .

77--Advise patient of importance of medication compliance in Advise patient of importance of medication compliance in treatment of tuberculosis. Medication noncompliance reduces treatment of tuberculosis. Medication noncompliance reduces efficacy and promotes resistanceefficacy and promotes resistance . .

88--Caution patient to avoid alcoholCaution patient to avoid alcohol

99--In patients receiving anticoagulants and rifampicin concurrently, it is recommended that the prothrombin timebe performed daily or as frequently as necessary to establish and maintain the required dose of anticoagulant .