Active Pharmaceutical Ingredients

Spectinomycin sulfate and spectinomycin hydrochloride belong to the same species with different acid roots. Spectinomycin is a broad-spectrum antibiotic, which has strong inhibitory ability to both Gram-positive and Gram-negative bacteria.

Molecular Formula：C14H26N2O11S, 4H2O

CAS No.: 64058-48-6

Description

Spectinomycin sulfate tetrahydrate is a white or almost white powder. It is freely soluble in water, insoluble in ethanol (96 per cent).

Application

Spectinomycin sulfate tetrahydrate is a broad-spectrum antibiotic. It has strong inhibitory effect on Gram-positive bacteria and gram-negative bacteria. It is effective against Staphylococcus aureus, Streptococcus hemolyticus, Diplococcus pneumoniae, Proteus vulgaris, Pneumococcus, Mycoplasma microplasm and some solitary bacteria.

Packing and Storage

Preserve in an airtight container. If the substance is sterile, store in a sterile, airtight, tamper- proof container.

Minimum Order

One package

Spectinomycin Sulphate Introduction

Item	Details
Basic Information	Spectinomycin sulphate is an aminocyclitol antibiotic with the CAS number 64058 – 48 – 6. Its chemical formula is likely a sulphate salt form of spectinomycin, although the exact stoichiometry may vary. It is derived from Streptomyces spectabilis, similar to spectinomycin hydrochloride. It appears as a white to off – white powder. It has good solubility in water, which is beneficial for formulating it into injectable solutions, much like the hydrochloride form. The sulphate salt may have different physical and chemical properties compared to the hydrochloride salt, which can impact its stability and formulation in pharmaceutical products.
Pharmacological Action	Similar to spectinomycin hydrochloride, spectinomycin sulphate acts by binding to the 30S subunit of the bacterial ribosome. This binding disrupts the normal function of the ribosome, interfering with protein synthesis. It mainly inhibits the elongation step of protein synthesis by causing misreading of the messenger RNA code, leading to the production of non – functional proteins. It has a relatively narrow – spectrum antibacterial activity, with a primary focus on Neisseria gonorrhoeae, the causative agent of gonorrhea. It is highly effective against both penicillin – sensitive and penicillin – resistant strains of Neisseria gonorrhoeae. It also shows some activity against a few other Gram – negative bacteria, such as some strains of Escherichia coli and Proteus mirabilis, but to a much lesser extent compared to its activity against Neisseria gonorrhoeae.
Clinical Applications	1. Gonorrhea Treatment: – Spectinomycin sulphate is mainly used as an alternative treatment for gonorrhea. In cases where penicillin or cephalosporin – based treatments are contraindicated, such as in patients with severe allergies to these drugs, spectinomycin sulphate can be used. – It is also used in regions where there is a high prevalence of Neisseria gonorrhoeae strains resistant to penicillins and cephalosporins. A single intramuscular injection of spectinomycin sulphate is often sufficient to treat uncomplicated gonorrhea, similar to the hydrochloride form. 2. Other Infections (Limited Use): – In some cases, it may be used off – label for the treatment of certain urinary tract infections caused by susceptible Gram – negative bacteria, especially when other more commonly used antibiotics are not effective. However, this is not a common indication, and its use is mainly restricted to gonorrhea treatment.
Adverse Reactions	1. Injection – Site Reactions: Similar to the hydrochloride form, pain, swelling, and induration at the injection site are common side effects. These reactions are usually mild to moderate and resolve within a few days. 2. Gastrointestinal Effects: Nausea, vomiting, diarrhea, and abdominal pain may occur, although they are relatively less common. These symptoms are usually mild and self – limiting. 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 spectinomycin or related compounds are at a higher risk. 4. Renal Toxicity: Although rare, in some cases, it may cause mild renal function abnormalities, such as a transient increase in serum creatinine levels. However, the overall risk of severe renal toxicity is low. 5. Neurological Effects: Rarely, it can cause dizziness, headache, and in some cases, confusion. These neurological symptoms are usually mild and resolve quickly.
Drug Interactions	1. With Other Antibiotics: There is limited data on significant interactions with other antibiotics. However, as with any antibiotic, concurrent use with other drugs that target the same bacteria may lead to overlapping effects or potential antagonism. 2. With Probenecid: Probenecid can inhibit the renal tubular secretion of spectinomycin (regardless of the salt form), increasing its plasma concentration and half – life. This may enhance the antibacterial effect but also increase the risk of side effects. 3. With Nephrotoxic Drugs: Concurrent use with other nephrotoxic drugs, such as aminoglycosides or non – steroidal anti – inflammatory drugs (NSAIDs), may increase the risk of renal toxicity, although the overall risk is still relatively low.
Differences from Spectinomycin Hydrochloride	1. Chemical Composition: The main difference is the counter – ion. Spectinomycin hydrochloride has chloride ions, while spectinomycin sulphate has sulphate ions. This difference in chemical composition can affect properties such as solubility, stability, and formulation. For example, the solubility and pH of solutions containing the two forms may vary slightly. 2. Formulation and Administration: In some cases, the choice between the two forms may depend on the specific requirements of the formulation. The hydrochloride form may be more commonly used in certain pharmaceutical preparations due to its known solubility and stability characteristics. However, the sulphate form may be preferred in other cases, perhaps due to better compatibility with other excipients in the formulation. 3. Clinical Efficacy and Safety: While the overall antibacterial spectrum and adverse effect profile are similar, there may be subtle differences in clinical efficacy and safety. For example, the rate of absorption or the potential for certain side effects may vary slightly between the two forms. However, more research is needed to fully understand these differences, and in most clinical settings, the choice between the two forms is likely to be based on availability and the specific needs of the patient and the formulation.

 

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