Peringatan Keamanan

Oral LD50 is 1570 mg/kg in rats.L50713 The minimum acute lethal or toxic dose in humans is not well established. Nonfatal acute overdoses in adults have been reported with doses ranging from nine to 12 mg of rifampin. Fatal acute overdoses in adults have been reported with doses ranging from 14 to 60 mg. Alcohol or a history of alcohol abuse was involved in some of the fatal and nonfatal reports. Nonfatal overdoses in pediatric patients one to four years of age receiving 100 mg/kg of rifampin for one to two doses have been reported.L50718

Immediate signs and symptoms of overdose include nausea, vomiting, abdominal pain, pruritus, headache, and increasing lethargy. Unconsciousness may occur when there is severe hepatic disease. Brownish-red or orange discoloration of the skin, urine, sweat, saliva, tears, and feces will occur: The intensity of this adverse effect is proportional to the amount of drug ingested.L50718 Rifampin is associated with a risk of hepatotoxicity. Transient increases in liver enzymes and/or bilirubin, liver enlargement, and jaundice may occur.L50718

Rifampin overdose should be responded to with intensive supportive measures and symptomatic treatment. Gastric lavage, active diuresis, extracorporeal hemodialysis, or peritoneal dialysis may be initiated.L50718

Rifampin

DB01045

small molecule approved

Deskripsi

Rifampin, also known as rifampicin, is a broad-spectrum antimicrobial A263748 that was first discovered in 1965 A263753 and clinically used in 1968.A263768 Rifampin is used to treat tuberculosis and works by inhibiting the microbial DNA-dependent RNA polymerase (RNAP).A263768

Struktur Molekul 2D

Berat 822.9402
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) In healthy adults, the mean biological half-life of rifampin in serum averages 3.35±0.66 hours after a 600 mg oral dose, with increases up to 5.08±2.45 hours reported after a 900 mg dose. With repeated administration, the half-life decreases and reaches average values of approximately two to three hours. The half-life does not differ in patients with renal failure at doses not exceeding 600 mg daily, and, consequently, no dosage adjustment is required.[L50718] Following a single 900 mg oral dose of rifampin in patients with varying degrees of renal insufficiency, the mean half-life increased from 3.6 hours in healthy adults to 5.0, 7.3, and 11.0 hours in patients with glomerular filtration rates of 30 to 50 mL/min, less than 30 mL/min, and in anuric patients, respectively.[L50718]
Volume Distribusi Following intravenous administration of a 300 mg and 600 mg dose of rifampin infused over 30 minutes to healthy male volunteers, the volume of distribution at steady state was 0.66 ± 0.14 and 0.64 ± 0.11 L/kg, respectively.[L50718] Rifampin is widely distributed throughout the body. It is present in effective concentrations in many organs and body fluids, including cerebrospinal fluid.[L50718]
Klirens (Clearance) Following intravenous administration of a 300 mg and 600 mg dose of rifampin infused over 30 minutes to healthy male volunteers, the total body clearance was 0.19 ± 0.06 and 0.14 ± 0.03 L/hr/kg, respectively.[L50718]

Absorpsi

Upon oral administration, rifampin is readily absorbed from the gastrointestinal tract.L50718 Peak serum concentrations in healthy adults and pediatric populations vary widely from individual to individual. Following a single 600 mg oral dose of rifampin in healthy adults, the peak serum concentration averages 7 mcg/mL but may vary from 4 to 32 mcg/mL. Absorption of rifampin is reduced by about 30% when the drug is ingested with food.L50718 In healthy male volunteers who received a 300 mg dose of rifampin, the mean Cmax was 9 ± 3 mcg/L. The value. increased to 17.5 ± 5 mcg/L for a 600 mg dose.L50718

Metabolisme

Rifampin is rapidly eliminated in the bile and undergoes progressive enterohepatic circulation to form its primary metabolite, 25-desacetyl rifampin,L50718 which retains about 20% of rifampicin’s antimicrobial activity.A263768 It is suggested that arylacetamide deacetylase is the liver esterase involved in the biotransformation of rifampin to 25-desacetyl rifampin.A263763, A24033 Nearly all the drug in the bile is in its deacetylated form within about six hours of administration. Deacetylation reduces intestinal reabsorption and facilitates elimination.L50718

Rute Eliminasi

Less than 30% of the dose is excreted in the urine as rifampin or metabolites. After absorption, rifampin is rapidly eliminated in the bile, and enterohepatic circulation ensues.L50718

Interaksi Makanan

3 Data
  • 1. Avoid alcohol. Alcohol may lead to an increased risk of severe hepatocellular toxicity.
  • 2. Take on an empty stomach. Absorption of rifampin is reduced by about 30% when the drug is ingested with food.
  • 3. Take with a full glass of water. Oral capsules should be taken with a glass of water.

Interaksi Obat

1131 Data
Sulfamethoxazole The serum concentration of Rifampin can be increased when it is combined with Sulfamethoxazole.
Aripiprazole The metabolism of Aripiprazole can be increased when combined with Rifampicin.
Afatinib The serum concentration of Afatinib can be decreased when it is combined with Rifampicin.
Brentuximab vedotin The serum concentration of Brentuximab vedotin can be decreased when it is combined with Rifampicin.
Dabigatran etexilate The serum concentration of Dabigatran etexilate can be decreased when it is combined with Rifampicin.
Linagliptin The serum concentration of Linagliptin can be decreased when it is combined with Rifampicin.
Paliperidone The serum concentration of Paliperidone can be decreased when it is combined with Rifampicin.
Sofosbuvir The serum concentration of Sofosbuvir can be decreased when it is combined with Rifampicin.
Indomethacin The metabolism of Indomethacin can be increased when combined with Rifampin.
Canagliflozin The serum concentration of Canagliflozin can be decreased when it is combined with Rifampicin.
Deferasirox The metabolism of Deferasirox can be increased when combined with Rifampicin.
Bendamustine The serum concentration of Bendamustine can be increased when it is combined with Rifampicin.
Pirfenidone The metabolism of Pirfenidone can be increased when combined with Rifampicin.
Clopidogrel The therapeutic efficacy of Clopidogrel can be increased when used in combination with Rifampicin.
Ifosfamide The metabolism of Ifosfamide can be increased when combined with Rifampicin.
Ledipasvir The serum concentration of Ledipasvir can be decreased when it is combined with Rifampicin.
Perampanel The metabolism of Perampanel can be increased when combined with Rifampicin.
Pitavastatin The excretion of Pitavastatin can be decreased when combined with Rifampicin.
Warfarin The metabolism of Warfarin can be increased when combined with Rifampicin.
Acenocoumarol The metabolism of Acenocoumarol can be increased when combined with Rifampicin.
(R)-warfarin The metabolism of (R)-warfarin can be increased when combined with Rifampicin.
R,S-Warfarin alcohol The metabolism of R,S-Warfarin alcohol can be increased when combined with Rifampicin.
S,R-Warfarin alcohol The metabolism of S,R-Warfarin alcohol can be increased when combined with Rifampicin.
(S)-Warfarin The metabolism of (S)-Warfarin can be increased when combined with Rifampicin.
Eslicarbazepine acetate The metabolism of Eslicarbazepine acetate can be increased when combined with Rifampicin.
Eslicarbazepine The metabolism of Eslicarbazepine can be increased when combined with Rifampicin.
Ezetimibe The metabolism of Ezetimibe can be increased when combined with Rifampin.
Raloxifene The metabolism of Raloxifene can be increased when combined with Rifampicin.
Minoxidil The metabolism of Minoxidil can be increased when combined with Rifampicin.
Furosemide The metabolism of Furosemide can be increased when combined with Rifampicin.
Naltrexone The metabolism of Naltrexone can be increased when combined with Rifampicin.
Flurbiprofen The metabolism of Flurbiprofen can be increased when combined with Rifampicin.
Ketoprofen The metabolism of Ketoprofen can be increased when combined with Rifampicin.
Abacavir The metabolism of Abacavir can be increased when combined with Rifampicin.
Alvocidib The metabolism of Alvocidib can be increased when combined with Rifampicin.
Ezogabine The metabolism of Ezogabine can be increased when combined with Rifampicin.
Bazedoxifene The metabolism of Bazedoxifene can be increased when combined with Rifampicin.
Gavestinel The metabolism of Gavestinel can be increased when combined with Rifampicin.
Fulvestrant The metabolism of Fulvestrant can be increased when combined with Rifampicin.
Naloxone The metabolism of Naloxone can be increased when combined with Rifampicin.
Delafloxacin The metabolism of Delafloxacin can be increased when combined with Rifampicin.
Liothyronine The metabolism of Liothyronine can be increased when combined with Rifampicin.
Febuxostat The metabolism of Febuxostat can be increased when combined with Rifampicin.
Bosentan The serum concentration of Bosentan can be decreased when it is combined with Rifampicin.
Caspofungin The serum concentration of Caspofungin can be decreased when it is combined with Rifampicin.
Chloramphenicol The metabolism of Chloramphenicol can be increased when combined with Rifampicin.
Citalopram The serum concentration of Citalopram can be decreased when it is combined with Rifampicin.
Dolutegravir The serum concentration of Dolutegravir can be decreased when it is combined with Rifampicin.
Fexofenadine The serum concentration of Fexofenadine can be increased when it is combined with Rifampicin.
Leflunomide The serum concentration of teriflunomide (A77 1726), an active metabolite of Leflunomide, can be increased when used in combination with Rifampicin.
Losartan The serum concentration of Losartan can be decreased when it is combined with Rifampicin.
Nevirapine The metabolism of Nevirapine can be increased when combined with Rifampicin.
Nitrazepam The serum concentration of Nitrazepam can be decreased when it is combined with Rifampicin.
Propofol Rifampicin may increase the hypotensive activities of Propofol.
Raltegravir The serum concentration of Raltegravir can be decreased when it is combined with Rifampicin.
Repaglinide The serum concentration of Repaglinide can be decreased when it is combined with Rifampicin.
Ritonavir The serum concentration of Ritonavir can be decreased when it is combined with Rifampicin.
Romidepsin The serum concentration of Romidepsin can be increased when it is combined with Rifampicin.
Saquinavir The serum concentration of Saquinavir can be decreased when it is combined with Rifampicin.
Cimetidine Cimetidine can cause a decrease in the absorption of Rifampicin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Nizatidine Nizatidine can cause a decrease in the absorption of Rifampicin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Ranitidine Ranitidine can cause a decrease in the absorption of Rifampicin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Famotidine Famotidine can cause a decrease in the absorption of Rifampicin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Methantheline Methantheline can cause a decrease in the absorption of Rifampicin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Aluminium Aluminium can cause a decrease in the absorption of Rifampicin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Magnesium oxide Magnesium oxide can cause a decrease in the absorption of Rifampicin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Sodium bicarbonate Sodium bicarbonate can cause a decrease in the absorption of Rifampicin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Aluminum hydroxide Aluminum hydroxide can cause a decrease in the absorption of Rifampicin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Calcium carbonate Calcium carbonate can cause a decrease in the absorption of Rifampicin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Metiamide Metiamide can cause a decrease in the absorption of Rifampicin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Roxatidine acetate Roxatidine acetate can cause a decrease in the absorption of Rifampicin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Magaldrate Magaldrate can cause a decrease in the absorption of Rifampicin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Magnesium hydroxide Magnesium hydroxide can cause a decrease in the absorption of Rifampicin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Magnesium trisilicate Magnesium trisilicate can cause a decrease in the absorption of Rifampicin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Magnesium carbonate Magnesium carbonate can cause a decrease in the absorption of Rifampicin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Lafutidine Lafutidine can cause a decrease in the absorption of Rifampicin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Lavoltidine Lavoltidine can cause a decrease in the absorption of Rifampicin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Bismuth subnitrate Bismuth subnitrate can cause a decrease in the absorption of Rifampicin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Magnesium silicate Magnesium silicate can cause a decrease in the absorption of Rifampicin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Aluminium acetoacetate Aluminium acetoacetate can cause a decrease in the absorption of Rifampicin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Hydrotalcite Hydrotalcite can cause a decrease in the absorption of Rifampicin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Magnesium peroxide Magnesium peroxide can cause a decrease in the absorption of Rifampicin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Almasilate Almasilate can cause a decrease in the absorption of Rifampicin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Aluminium glycinate Aluminium glycinate can cause a decrease in the absorption of Rifampicin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Aloglutamol Aloglutamol can cause a decrease in the absorption of Rifampicin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Niperotidine Niperotidine can cause a decrease in the absorption of Rifampicin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Calcium silicate Calcium silicate can cause a decrease in the absorption of Rifampicin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Aluminium phosphate Aluminium phosphate can cause a decrease in the absorption of Rifampicin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Dexrabeprazole Dexrabeprazole can cause a decrease in the absorption of Rifampicin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Pantoprazole Pantoprazole can cause a decrease in the absorption of Rifampicin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Lansoprazole Lansoprazole can cause a decrease in the absorption of Rifampicin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Rabeprazole Rabeprazole can cause a decrease in the absorption of Rifampicin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Dexlansoprazole The metabolism of Dexlansoprazole can be increased when combined with Rifampicin.
Sodium zirconium cyclosilicate Sodium zirconium cyclosilicate can cause a decrease in the absorption of Rifampicin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Vonoprazan The therapeutic efficacy of Vonoprazan can be decreased when used in combination with Rifampicin.
Glimepiride The serum concentration of Glimepiride can be decreased when it is combined with Rifampicin.
Acetohexamide The serum concentration of Acetohexamide can be decreased when it is combined with Rifampicin.
Chlorpropamide The serum concentration of Chlorpropamide can be decreased when it is combined with Rifampicin.
Tolazamide The serum concentration of Tolazamide can be decreased when it is combined with Rifampicin.
Glyburide The serum concentration of Glyburide can be decreased when it is combined with Rifampicin.

Target Protein

DNA-directed RNA polymerase subunit beta rpoB
Nuclear receptor subfamily 1 group I member 2 NR1I2

Referensi & Sumber

Synthesis reference: Klaus Jurgen, Joachim Seydel, "Combination preparations containing rifampicin and thioacetazon." U.S. Patent US5104875, issued August, 1973.
Artikel (PubMed)
  • PMID: 32491420
    Beloor Suresh A, Rosani A, Patel P, Wadhwa R: Rifampin. .
  • PMID: 31247337
    Grobbelaar M, Louw GE, Sampson SL, van Helden PD, Donald PR, Warren RM: Evolution of rifampicin treatment for tuberculosis. Infect Genet Evol. 2019 Oct;74:103937. doi: 10.1016/j.meegid.2019.103937. Epub 2019 Jun 24.
  • PMID: 346286
    Acocella G: Clinical pharmacokinetics of rifampicin. Clin Pharmacokinet. 1978 Mar-Apr;3(2):108-27. doi: 10.2165/00003088-197803020-00002.
  • PMID: 9364739
    Jamis-Dow CA, Katki AG, Collins JM, Klecker RW: Rifampin and rifabutin and their metabolism by human liver esterases. Xenobiotica. 1997 Oct;27(10):1015-24. doi: 10.1080/004982597239994.
  • PMID: 21856291
    Nakajima A, Fukami T, Kobayashi Y, Watanabe A, Nakajima M, Yokoi T: Human arylacetamide deacetylase is responsible for deacetylation of rifamycins: rifampicin, rifabutin, and rifapentine. Biochem Pharmacol. 2011 Dec 1;82(11):1747-56. doi: 10.1016/j.bcp.2011.08.003. Epub 2011 Aug 12.
  • PMID: 31049868
    Abulfathi AA, Decloedt EH, Svensson EM, Diacon AH, Donald P, Reuter H: Clinical Pharmacokinetics and Pharmacodynamics of Rifampicin in Human Tuberculosis. Clin Pharmacokinet. 2019 Sep;58(9):1103-1129. doi: 10.1007/s40262-019-00764-2.

Contoh Produk & Brand

Produk: 83 • International brands: 7
Produk
  • IsonaRif
    Capsule • 50 mg/5mL • Oral • US • Generic • Approved
  • Rifadin
    Capsule • 300 mg/1 • Oral • US • Approved
  • Rifadin
    Capsule • 150 mg/1 • Oral • US • Approved
  • Rifadin
    Capsule • 300 mg/1 • Oral • US • Approved
  • Rifadin
    Capsule • 150 mg • Oral • Canada • Approved
  • Rifadin
    Capsule • 300 mg • Oral • Canada • Approved
  • Rifadin Cap 300mg
    Capsule • 300 mg • Oral • Canada • Approved
  • Rifadin IV
    Injection, powder, lyophilized, for solution • 600 mg/10mL • Intravenous • US • Approved
Menampilkan 8 dari 83 produk.
International Brands
  • Rifadine
  • Rifaldin
  • Rifoldin
  • Rimactan
  • Rimactane
  • Rofact
  • Tubocin

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
© 2025 Digital Pharmacy Research - Universitas Esa Unggul