Rifamycin

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Information about Rifamycin

Rifamycin is a nonabsorbable rifampin-like antibacterial agent that is used as treatment of travelers’ diarrhea.

Liver safety of Rifamycin

Rifamycin has minimal oral absorption and has not been implicated in causing liver test abnormalities or clinically apparent liver injury.

Mechanism of action of Rifamycin

Rifamycin (rif" a mye' sin) is a semisynthetic derivative of rifampin specifically designed to have minimal gastrointestinal absorption (<0.1%). It is a broad spectrum antibiotic with activity against both aerobic and anaerobic organisms, both gram negative and gram positive. The antibiotic activity is attributed to rifamycin’s binding to bacterial RNA polymerases, preventing RNA and subsequent protein synthesis. Rifamycin is formulated with enteric coating and a multi-matrix technology that prevents the dissolving until it reaches the cecum where the higher pH (above 7) allows for the delivery of the drug throughout the colon. The delayed dissolution of the tablet prevents the antibacterial activity from acting on small bowel flora and targets it largely at the colon.

FDA approval information for Rifamycin

This delayed release formulation of rifamycin was approved for use as treatment of travelers’ diarrhea in 2018.

Dosage and administration for Rifamycin

Rifamycin is available in tablets of 200 mg under the brand name Aemcolo. The recommended dose is 400 mg (2 tablets) twice daily for 3 days.

Side effects of Rifamycin

Side effects are uncommon but can include headache and constipation. Rare instances of hypersensitivity and Clostridium difficile-associated diarrhea have been described.

Antidiarrheal agents

Antidiarrheal agents include bulk forming agents, hydroscopic agents, bile acid resins, bismuth, inhibitors of intestinal motility, non-absorbed antibiotics and hormones. Bulk forming agents include methylcellulose; hydroscopic agents include pectin and kaolin; bile acid resins are cholestyramine, colestipol and colesevalam; inhibitors of intestinal motility include opioids such as diphenoxylate and loperamide. Antibiotics include rifamycin and rifaximin which are non-absorbed and are used for travelers' diarrhea. Hormones with antidiarrheal activity include octretide and somatostatin. Most antidiarrheal agents are active locally in the small intestine and colon and are largely not absorbed. Some, however, have been implicated in rare causes of liver injury (senna, cascara, cholestyramine). Telotristat is a relatively new agent that inhibits the synthesis of serotonin and is used specifically for the diarrhea of carcinoid syndrome.

Antiemetics are a diverse group of medications that act at different points in the pathways that regulate nausea and vomiting. These include antihistamines, anticholinergic agents, phenothiazines, serotonin type 3 receptor blockers, centrally acting benzamides, cannabinoid receptor agonists, substance P antagonists and miscellaneous.

Anticholinergic Agents

Antihistamines

Cannabinoid Receptor Agonists

Serotonin 5-HT3 Receptor Antagonists

Substance P/Neurokinin 1 Receptor Antagonists

Miscellaneous

Acid peptic disease/antiulcer agents that include antacids, the histamine type 2 receptor blockers (H2 blockers), and the proton pump inhibitors (PPIs). These agents are some of the most commonly taken medications and are very well tolerated, most being available both by prescription and over-the-counter. While many of these drugs are approved for use in duodenal and gastric ulcer disease, their major use is for acid reflux and indigestion.

Histamine H2 Receptor Antagonists (H2 Blockers) Cimetidine, Famotidine, Nizatidine, Ranitidine

Proton Pump Inhibitors

Cathartics, laxatives or agents for constipation include bulk forming agents, osmotic agents, stool wetting agents, nonspecific stimulants, prokinetic agents and agents that increase fluid secretion. Many of these therapies are not systemically absorbed and none are considered particularly hepatotoxic. Naldemedine and naloxegol are opioid antagonists and are used to treat the constipation associated with opioid use.

Inflammatory bowel disease encompasses several disorders, most commonly ulcerative colitis and Crohn colitis. Agents can be classified as 5-aminosalicyclic acid (5-ASA) based agents, immunosuppressive drugs, antitumor necrosis factor agents, corticosteroids, antibiotics and miscellaneous.

5-Aminosalicyclic Acid (5-ASA) Derivatives

Immunosuppressive Agents

Tumor Necrosis Factor Antagonists

Miscellaneous

Irritable Bowel Syndrome Agents Antimuscarinics/Antispasmodics [See Anticholinergic agents

Prokinetic Agents - See Serotonin 5-ht4 receptor agonists Alosetron, Cisapride, Domperidone, Linaclotide, Lubiprostone, Metoclopramide, Plecanatide, Prucalopride, Tegaserod

Other

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