Midecamycin API Manufacturers

General Description:

Midecamycin, identified by CAS number 35457-80-8, is a notable compound with significant therapeutic applications. Midecamycin is a naturally occurring 16-membered macrolide that fits under the category of acetoxy-substituted macrolide antibiotics. In this molecule, an acetoxy group is substituted on the position 9 of the 16-member ring and on position 4 of the terminal sugar. Until 2017, midecamycin was still under the list of approved antimicrobial active pharmaceutical ingredients by Health Canada.

Indications:

This drug is primarily indicated for: Midecamycin was used for the treatment of infections in the oral cavity, upper and lower respiratory tracts and skin and soft tissue infections. The alone use of midecamycin was mainly used in Europe or Japan. Its use in specific medical scenarios underscores its importance in the therapeutic landscape.

Metabolism:

Midecamycin undergoes metabolic processing primarily in: Midecamycin undergoes extensive biotransformation in the liver and its metabolites are characterized by presenting little to no antimicrobial activity. The main metabolite is formed by a 14-hydroxylation and it can be also detected in urine. This metabolic pathway ensures efficient processing of the drug, helping to minimize potential toxicity and side effects.

Absorption:

The absorption characteristics of Midecamycin are crucial for its therapeutic efficacy: Midecamycin is rapidly and almost completely absorbed when orally administered. It is mainly absorbed in the alkaline intestinal environment. This rapid absorption is due to its liposoluble property which allows for good penetration in the tissues, especially bronchial secretion, prostatic tissue, middle ear exudates and bone tissue. The tissue/serum ratio concentration is greater than 1 which indicates that this product does not stay long in the plasma. After oral administration of 600 mg of midecamycin, the peak serum concentration is 0.8 mg/L and it is attained 1 hour after oral administration. This concentration dereased significantly after 4-6 hours. The drug's ability to rapidly penetrate into cells ensures quick onset of action.

Half-life:

The half-life of Midecamycin is an important consideration for its dosing schedule: The half-life of midecamycin is longer than the first macrolide antibiotics. after intravenous administration, the half-life reported is of 54 minutes. This determines the duration of action and helps in formulating effective dosing regimens.

Protein Binding:

Midecamycin exhibits a strong affinity for binding with plasma proteins: Midecamycin does not bind to plasma proteins in a significant proportion and thus, the bound form can account for about 15% of the administered dose. The acetate form of midecamycin presents a larger protein binding. This property plays a key role in the drug's pharmacokinetics and distribution within the body.

Route of Elimination:

The elimination of Midecamycin from the body primarily occurs through: The major route of elimination of midecamycin is is the liver, followed by a low significance of renal elimination. Urinary concentrations accounts for about 3.3% of the administered dose after 6 hours. Understanding this pathway is essential for assessing potential drug accumulation and toxicity risks.

Volume of Distribution:

Midecamycin is distributed throughout the body with a volume of distribution of: The reported apparent volume of distribution of midecamycin is 7.7 L/kg. This metric indicates how extensively the drug permeates into body tissues.

Clearance:

The clearance rate of Midecamycin is a critical factor in determining its safe and effective dosage: Midecamycin presentas a low renal clearance value. It reflects the efficiency with which the drug is removed from the systemic circulation.

Pharmacodynamics:

Midecamycin exerts its therapeutic effects through: Reports have indicated that midecamycin is active against both erythromycin-susceptible and efflux-mediated erythromycin-resistant strains. The diacetate form of this product reduces gastrointestinal side effects and improves its pharmacokinetic profile. Studies have proved that midecamycin is highly active against Gram-positive organisms. The activity of midecamycin in the form of acetate salt presents a better activity, which seems to be potentiated at pH 7-8, as well as a longer half-life. The drug's ability to modulate various physiological processes underscores its efficacy in treating specific conditions.

Mechanism of Action:

Midecamycin functions by: Midecamycin, as part of the macrolides, act by inhibiting bacterial protein synthesis. More specifically, midecamycin inhibits bacterial growth by targetting the 50S ribosomal subunit preventing peptide bond formation and translocation during protein synthesis. The presence of mutations in the 50S RNA can prevent midecamycin binding. Midecamycin is a broad spectrum antibiotic and thus, it can interact with different bacteria. This mechanism highlights the drug's role in inhibiting or promoting specific biological pathways, contributing to its therapeutic effects.

Classification:

Midecamycin belongs to the class of organic compounds known as aminoglycosides. These are molecules or a portion of a molecule composed of amino-modified sugars, classified under the direct parent group Aminoglycosides. This compound is a part of the Organic compounds, falling under the Organic oxygen compounds superclass, and categorized within the Organooxygen compounds class, specifically within the Carbohydrates and carbohydrate conjugates subclass.

Categories:

Midecamycin is categorized under the following therapeutic classes: Anti-Bacterial Agents, Anti-Infective Agents, Antibacterials for Systemic Use, Antiinfectives for Systemic Use, Cytochrome P-450 CYP3A Inhibitors, Cytochrome P-450 CYP3A Substrates, Cytochrome P-450 CYP3A4 Inhibitors, Cytochrome P-450 CYP3A4 Inhibitors (strength unknown), Cytochrome P-450 CYP3A4 Substrates, Cytochrome P-450 Enzyme Inhibitors, Cytochrome P-450 Substrates, Lactones, Macrolides, Macrolides, Lincosamides and Streptogramins, Polyketides. These classifications highlight the drug's diverse therapeutic applications and its importance in treating various conditions.

Experimental Properties:

Further physical and chemical characteristics of Midecamycin include:

• Water Solubility: Insoluble
• Melting Point: 155 ºC
• Boiling Point: 874 ºC
• logP: 2.22
• pKa: 6.9