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Chemical name

Rifamycin, 3 -[[(4 - methyl - 1 - piperazinyl) imino] methyl].

Category

Antibacterial (antimycobacterial, antileprosy agent).

Mechanism of action

Rifampin, a semisynthetic broad - spectrum bactericidal antibiotic, inhibits bacterial RNA synthesis by binding strongly to the beta subunit of DNA - dependent RNA polymerase, preventing attachment of the enzyme to DNA and thus blocking initiation of RNA transcription.

Indications

- Tuberculosis (treatment) - It is indicated in combination with other antituberculosis medications in the treatment of all forms of tuberculosis, including tuberculous meningitis.
- Leprosy (treatment) - It is used in combination with other agents in the treatment of leprosy (Hansen's disease).
- Meningococcal infections (prophylaxis) - It is indicated in the treatment of close contacts of patients with proved or suspected infection caused by Neisseria meningitidis.

Precautions to consider

Risk - benefit should be considered when the following medical problems exist:
Hepatic function impairment - Hypersensitivity to rifampin - Alcoholism, active or in remission.

Pregnancy / Breast - feeding

Rifampin crosses the placenta. It is recommended that pregnant women with tuberculosis be treated for a minimum of 9 months with multidrug therapy, including rifampin. FDA pregnancy category C.
Rifampin is distributed into breast milk. Problems in humans have not been documented.

Drug interactions

Rifampin is known to induce the hepatic microsomal enzymes that metabolize various drugs listed in the table below. The therapeutic effects of these drugs may be decreased.

Rifampin Drug Interactions Due to Hepatic Microsomal Enzyme Induction
Acetaminophen Corticosteroids Mexiletine
Anticoagulants, oral Cyclosporine Quinidine
Barbiturates Digitoxin Sulfones
Benzodiazepines Disopyramide Sulfonylureas
Beta - blockers Estrogens Theophyllines
Chloramphenicol Hydantoins Tocainide
Clofibrate Methadone Verapamil
Contraceptives, oral    

Combinations containing any of the following medications, may also interact with this medication: Diazepam, Isoniazid, Probenecid, Phenytoin, Trimethoprim.

Side / Adverse effects

Those indicating need for medical attention: Incidence less frequent: "Flu - like" syndrome - hypersensitivity.
Incidence rare: Blood dyscrasias - hepatitis (yellow eyes or skin) - hepatitis prodromal symptoms - interstitial nephritis.
Those not indicating need for medical attention:
Incidence more frequent: Reddish orange to reddish brown discoloration of urine, feces, saliva, sputum, sweat and tears. Tears discolored by rifampin may also discolor soft contact lenses.

Administration and dosage

Usual adult and adolescent dose: Tuberculosis - In combination with other antituberculosis medication: Oral, 600 mg once a day for the entire treatment period; or 10 mg per kg of body weight, up to 600 mg, two or three times a week, depending on the treatment regimen.
Meningococcal infection (prophylaxis) - Oral, 600 mg two times a day for two days.
Usual adult prescribing limits: Up to 600 mg daily.
Children 1 month of age and over: Tuberculosis - In combination with other antituberculosis medications: Oral, 10 to 20 mg per kg of body weight, up to 600 mg, once a day; or 10 to 20 mg per kg of body weight, up to 600 mg, two or three times a week, depending on the treatment regimen.
Meningococcal infection (prophylaxis): Oral, 10 mg per kg of body weight every twelve hours for two days.

How supplied

1 - Capsules: Box of 100 capsules. Each capsule contains 300 mg rifampin.
2 - Capsules: Box of 100 capsules. Each capsule contains 150 mg rifampin.

Storage

Store below 30°C, protect from direct light and moisture.
Oral drops: Store in a cool place, protect from light and freezing.

References

1 - USP DI Vol: 1 (1997) - pages: 2528-2533.
2 - Drug facts and comparisons (1994).
3 - USP 23 page: 1381.
   
 

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