Active Pharmaceutical Ingredients

Thiamphenicol is a broad-spectrum antibiotic of chloramphenicol, which has stronger effect on Gram-negative bacteria than positive bacteria. Its chemical structure is similar to that of chloramphenicol. Its methylsulfone group replaces the nitro group of chloramphenicol, so its toxicity is reduced, and its antibacterial effect in the body is 2.5-5 times stronger than that of chloramphenicol.

Molecular Formula：C12H15Cl2NO5S

Molecular Weight：356.2

CAS No.: 15318-45-3

Description

Thiamphenicol is a fine, white or yellowish-white, crystalline powder or crystals. It is slightly soluble in water, very soluble in dimethylacetamide, freely soluble in acetonitrile and in dimethylformamide, soluble in methanol, sparingly soluble in acetone and in anhydrous ethanol, slightly soluble in ethyl acetate.

Application

Thiamphenicol is a broad-spectrum antibiotic of chloramphenicol, which has stronger effect on Gram-negative bacteria than positive bacteria. Its chemical structure is similar to that of chloramphenicol. Its methylsulfone group replaces the nitro group of chloramphenicol, so its toxicity is reduced, and its antibacterial effect in the body is 2.5-5 times stronger than that of chloramphenicol.

In clinic, thiamphenicol is mainly used in the treatment of respiratory, urinary, hepatobiliary, typhoid and other intestinal surgery, obstetrics and Gynecology and ENT infection, especially for mild infection. Thiamphenicol has strong antibacterial activity against Gram-positive bacteria such as pneumococci and hemolytic streptococcus, and it has strong antibacterial activity against Gram-positive bacteria such as Neisseria gonorrhoeae, diplococcus meningitidis, pulmonary Bacteroides, Escherichia coli, Vibrio cholerae, dysentery and influenza, it also has certain antibacterial activity against anaerobic bacilli, Rickettsia and amoeba, the mechanism of action is the same as that of chloramphenicol.

Thiamphenicol also has a strong immunosuppressive effect and is an excellent immunosuppressant. Its mechanism of action is significantly different from other immunosuppressive agents, and its immunosuppressive effect is several times higher than that of chloramphenicol.

Packing and Storage

Preserve in an airtight container, protected from light.

Minimum Order

One package

Thiamphenicol Introduction

Item	Details
Basic Information	Thiamphenicol is a broad – spectrum antibiotic with the CAS number 15318 – 45 – 3. Its chemical formula is C₁₂H₁₅Cl₂NO₅S. It appears as a white or almost white, odorless, and bitter – tasting crystalline powder. It has relatively poor solubility in water but better solubility in organic solvents like ethanol and propylene glycol. This solubility profile impacts its pharmaceutical formulation, often requiring special techniques to ensure proper delivery in medications.
Pharmacological Action	Thiamphenicol acts by binding to the 50S subunit of the bacterial ribosome. It inhibits the peptidyl transferase activity, which is essential for the formation of peptide bonds during protein synthesis. By blocking this step, it prevents the elongation of the polypeptide chain, ultimately inhibiting bacterial protein synthesis. It has a broad – spectrum antibacterial activity. Against Gram – positive bacteria, it is effective against Staphylococcus aureus (including some methicillin – resistant strains), Streptococcus pneumoniae, and Streptococcus pyogenes. Against Gram – negative bacteria, it shows activity against Escherichia coli, Klebsiella pneumoniae, Salmonella species, and Shigella species. It also has activity against some anaerobic bacteria and rickettsiae.
Clinical Applications	1. Respiratory Tract Infections: – It can be used to treat community – acquired pneumonia, targeting pathogens such as Streptococcus pneumoniae and Haemophilus influenzae. – For acute exacerbations of chronic bronchitis, thiamphenicol can combat bacteria like Haemophilus influenzae and Moraxella catarrhalis. 2. Gastrointestinal Tract Infections: – Thiamphenicol is effective in treating gastrointestinal infections caused by Salmonella and Shigella species. It can be used for the treatment of typhoid fever, paratyphoid fever, and bacillary dysentery. – In some cases, it may also be used for treating traveler’s diarrhea caused by susceptible bacteria. 3. Urinary Tract Infections: – It can be used to treat urinary tract infections caused by susceptible Gram – negative bacteria such as Escherichia coli and Klebsiella pneumoniae. 4. Eye and Ear Infections: – In ophthalmic and otolaryngology practice, thiamphenicol can be used in topical preparations to treat eye infections like conjunctivitis and ear infections such as otitis externa when caused by susceptible organisms. 5. Other Infections: – It may be used for treating rickettsial infections such as Rocky Mountain spotted fever, although other antibiotics are more commonly preferred.
Adverse Reactions	1. Hematological Effects: One of the most significant concerns with thiamphenicol is its potential to cause hematological disorders. It can lead to reversible bone marrow suppression, which may present as a decrease in red blood cells, white blood cells, and platelets. In rare cases, it can cause aplastic anemia, which is a life – threatening condition where the bone marrow fails to produce sufficient blood cells. 2. Gastrointestinal Effects: Nausea, vomiting, diarrhea, abdominal pain, and anorexia are common side effects. These symptoms are usually mild to moderate and may be due to the drug’s effect on the normal gut flora and direct irritation of the gastrointestinal mucosa. 3. Allergic Reactions: Allergic reactions can occur, ranging from mild rashes, itching, and hives to severe anaphylactic shock. Patients with a history of allergic reactions to thiamphenicol or related compounds are at a higher risk. 4. Neurological Effects: In some cases, it can cause headache, dizziness, and in rare cases, more severe neurological symptoms such as peripheral neuropathy. 5. Gray Baby Syndrome (in Neonates): In neonates, especially premature infants, thiamphenicol can cause gray baby syndrome. This syndrome is characterized by hypotension, ashen – gray skin color, and in severe cases, circulatory collapse. The immature liver and kidneys in neonates are unable to effectively metabolize and excrete the drug, leading to its accumulation and subsequent toxicity.
Drug Interactions	1. With Oral Anticoagulants: Thiamphenicol can enhance the anticoagulant effect of oral anticoagulants like warfarin. It may inhibit the normal gut flora that produces vitamin K, which is necessary for the synthesis of clotting factors. Patients taking both drugs need to have their prothrombin time or international normalized ratio (INR) monitored closely. 2. With Oral Hypoglycemic Agents: Concurrent use with oral hypoglycemic agents may increase the risk of hypoglycemia. Thiamphenicol may enhance the effect of these agents, leading to low blood sugar levels. Patients need to monitor their blood sugar levels closely. 3. With Other Nephrotoxic Drugs: Concurrent use with other nephrotoxic drugs, such as aminoglycosides or non – steroidal anti – inflammatory drugs (NSAIDs), can increase the risk of nephrotoxicity. 4. With Chloramphenicol: Since thiamphenicol is structurally related to chloramphenicol, concurrent use may increase the risk of hematological toxicity.
Special Population Considerations	1. Pregnant Women: The use of thiamphenicol during pregnancy is generally not recommended, especially in the third trimester. It can cross the placenta and may cause harm to the developing fetus, including potential hematological effects. However, in some cases where the benefits outweigh the risks, it may be used with careful monitoring. 2. Breastfeeding Women: Thiamphenicol is excreted in breast milk. Breastfeeding should be avoided during treatment with thiamphenicol as it may cause adverse effects in the nursing infant, especially in terms of potential hematological and gastrointestinal effects. 3. Children: In children, the risk of hematological side effects, including bone marrow suppression, needs to be carefully considered. The use of thiamphenicol should be based on a careful assessment of the benefits and risks, and close monitoring of blood cell counts may be required. 4. Patients with Renal or Hepatic Impairment: In patients with significant renal or hepatic impairment, the metabolism and clearance of thiamphenicol may be affected. Dosage adjustment may be necessary, and close monitoring of serum drug levels and organ function is recommended.

 

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