Drug reference

rifapentine

Rifamycin · Antimycobacterial

RifamycinAntimycobacterial

CDSCO approved

EXCRETION

—

not curated

INTERACTIONS

12 major

SEVERE in our sources

PREGNANCY

FDA category + note

Top interactionssee all 12 →

Various Cyp And P Glycoprotein SubstratesSevereTextbookG&G 14e · p1271, 1283
AbemaciclibSevereDatabaseDDInter
AbirateroneSevereDatabaseDDInter
AcalabrutinibSevereDatabaseDDInter

Mechanism

Rifapentine, like other rifamycins, enters bacilli and binds to the β subunit of DNA-dependent RNA polymerase (rpoB) to form a stable drug-enzyme complex, suppressing chain formation in RNA synthesis.

Indications

tuberculosis diseaselatent tuberculosis infection

Dosing

Adult: 1200 mg daily (dose used in recent successful phase III trial for TB disease, not currently used for general TB disease treatment)
Renal adjustment: Dose adjustment not specified beyond general clearance mechanisms.

Pharmacokinetics

Half-life

14–18 h

Bioavailability

70%

Protein binding

97%

Metabolism

Microsomal β-esterases and cholinesterases (autoinduction of clearance)

Excretion

Bile and feces (major), urine (minor)

Side effects

Common

rashhepatitisflu-like symptomsElevated aminotransferase levelsGastrointestinal events (nausea, vomiting, diarrhea)Orange discoloration of body fluids

Pregnancy & lactation

Pregnancy

Drug interactions

Various Cyp And P Glycoprotein Substrates

Severe

Textbook

Administration often results in higher clearance for concurrently administered medicines subject to these metabolic and transport pathways, leading to therapeutic failures.

Prior to putting a patient on rifapentine, all the patient’s medications and contraception should be examined for potential interactions (inferred from rifampin management).

Source: G&G 14e · p1271, 1283

Abemaciclib

Severe

Database

Drug interaction classified as: metabolism

Source: DDInter

Abiraterone

Severe

Database

Drug interaction classified as: metabolism

Source: DDInter

Acalabrutinib