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Lormetazepam | CAS No: 848-75-9 | GMP-certified suppliers
A medication that treats short-term insomnia by promoting sleep onset and maintenance with minimal next-day sedation, supporting central nervous system depressant applications.
Therapeutic categories
Primary indications
- For the treatment of short-term insomnia
Product Snapshot
- Lormetazepam is available as oral tablets, capsules, coated tablets, solution/drops, and parenteral injection solution formulations
- It is primarily indicated for the short-term treatment of insomnia
- The drug is approved for use in key regulatory markets including FDA and EMA regions
Clinical Overview
Pharmacodynamically, lormetazepam acts as a central nervous system (CNS) depressant, exerting anxiolytic, muscle relaxant, sedative, and hypnotic properties. As a short-acting benzodiazepine, lormetazepam’s clinical profile includes minimal residual sedation upon awakening, which may be advantageous in minimizing next-day impairment.
The mechanism of action involves modulation of the GABAA receptor complex. Specifically, lormetazepam binds at the interface of the α and γ subunits of GABAA receptors containing γ2 and α1, α2, α3, or α5 subunits. This binding enhances the receptor's affinity for the inhibitory neurotransmitter GABA, resulting in increased chloride ion influx into neurons. The subsequent neuronal hyperpolarization decreases excitability, contributing to the therapeutic CNS depressant effects.
Pharmacokinetic data relevant to absorption, distribution, metabolism, and excretion (ADME) indicates that lormetazepam is orally bioavailable, with a relatively short elimination half-life consistent with its short-acting classification. Metabolism occurs primarily via hepatic pathways, with metabolites excreted renally.
Safety considerations include potential risks typical of benzodiazepine use such as dependence, withdrawal phenomena, and CNS depression. Its short-term use is generally recommended to minimize tolerance and dependence risks. Caution is advised in populations with respiratory impairment, hepatic insufficiency, or concomitant CNS depressant use.
From a regulatory and chemical standpoint, lormetazepam is classified among benzodiazepinones and other centrally acting sedative-hypnotics, consistent with its fused-ring heterocyclic structure.
In terms of API procurement, suppliers should ensure compliance with pharmacopeial standards for identity, purity, and potency. Stringent quality control is necessary to confirm the absence of impurities and degradation products, given the compound’s clinical use in CNS indications and regulatory scrutiny associated with benzodiazepines. Reliable sourcing is critical to maintain consistency in formulation and therapeutic outcomes.
Identification & chemistry
| Generic name | Lormetazepam |
|---|---|
| Molecule type | Small molecule |
| CAS | 848-75-9 |
| UNII | GU56C842ZA |
| DrugBank ID | DB13872 |
Pharmacology
| Summary | Lormetazepam is a short-acting benzodiazepine that acts as a positive allosteric modulator of GABA(A) receptors by binding to the benzodiazepine site between the α and γ subunits. This interaction enhances chloride ion influx, leading to neuronal hyperpolarization and decreased central nervous system excitability. Its pharmacodynamic effects include anxiolytic, muscle relaxant, sedative, and hypnotic actions primarily used for short-term management of insomnia. |
|---|---|
| Mechanism of action | Lormetazepam, as a benzodiazepine, binds to the regulatory site between the α and γ subunits of γ-aminobutryic acid (GABA) A receptors with γ2 and α1, α2, α3, or α5 subunits . This facilitates the opening of the chloride channel allowing chloride ions to flow into the neuron resulting in hyperpolarization. Hyperpolarized neurons require greater simulation to reach their action potential threshold. The general inhibitory effect on neuronal depolarization produces the effects of lormetazepam. |
| Pharmacodynamics | Lormetazepam is a benzodiazepine which reduces central nervous system (CNS) activity [L927, T28]. It produces anxiolytic, muscle relaxant, sedative and hypnotic effects. Because it is a short-acting benzodiapine, it does not produce significant sedation after waking. |
Targets
| Target | Organism | Actions |
|---|---|---|
| GABA(A) Receptor | Humans | positive allosteric modulator |
| GABA(A) Receptor Benzodiazepine Binding Site | Humans | ligand |
ADME / PK
| Half-life | The terminal phase half life is 11 h . |
|---|---|
| Metabolism | Metabolised to an inactive metabolite via glucuronide conjugation |
Formulation & handling
- Lormetazepam is a small molecule benzodiazepine primarily formulated for oral administration as tablets, capsules, and oral solutions.
- Due to its low water solubility and moderate lipophilicity (LogP 3.39), formulation strategies should address dissolution and bioavailability enhancement.
- Parenteral formulations exist, requiring sterile handling and stability considerations for injectable solutions.
Regulatory status
Safety
| Toxicity | The primary manifestation of overdosage ranges from drowsiness to coma and symptoms may include ataxia, hypotension, hypotonia, respiratory depression which may lead to death . Experimental LD50 values are as follows : Mouse - 780 mg/kg (intraperitoneal), 1790 mg/kg (oral), 10000 mg/kg (subcutaneous). Rat - 6250 mg/kg (intraperitoneal), 10000 mg/kg (oral), 10000 mg/kg (intraperitoneal). |
|---|
- Exposure may result in central nervous system depression, including drowsiness, ataxia, hypotonia, respiratory depression, and in severe cases, coma or fatality
- Handle with appropriate protective equipment to minimize risk of accidental ingestion or injection
- Experimental LD50 values indicate variable toxicity depending on administration route and species, with lower toxicity observed via oral and subcutaneous routes
Cefalexin Monohydrate is a type of Cephalosporins
Cephalosporins are a class of pharmaceutical active ingredients (APIs) widely used in the field of antibiotics. They belong to the beta-lactam family, which also includes penicillins. Cephalosporins are derived from a fungus called Acremonium cephalosporium and are known for their potent antimicrobial properties.
These APIs are commonly used to treat a wide range of bacterial infections, including respiratory tract infections, skin and soft tissue infections, urinary tract infections, and even meningitis. Cephalosporins work by inhibiting the synthesis of bacterial cell walls, leading to the disruption of bacterial growth and ultimately their destruction.
Cephalosporins are classified into generations based on their antimicrobial spectrum and activity against specific bacteria. The first-generation cephalosporins are effective against Gram-positive bacteria, while subsequent generations show broader activity against both Gram-positive and Gram-negative bacteria.
Pharmaceutical companies manufacture cephalosporins in various formulations, including tablets, capsules, injectable solutions, and suspensions. They are often prescribed by healthcare professionals and are available under different brand names in the market.
It is important to note that like other antibiotics, cephalosporins should be used judiciously to prevent the development of antibiotic resistance. Proper dosage and adherence to treatment guidelines are crucial to maximize their effectiveness and minimize the risk of resistance.
In conclusion, cephalosporins are a vital category of APIs widely used in the treatment of bacterial infections. Their broad spectrum of activity and effectiveness make them an essential tool in modern medicine.
Cefalexin Monohydrate API manufacturers & distributors
Compare qualified Cefalexin Monohydrate API suppliers worldwide. We currently have 2 companies offering Cefalexin Monohydrate API, with manufacturing taking place in 2 different countries. Use the table below to review supplier type, countries of origin, certifications, product portfolio and GMP audit availability.
| Supplier | Type | Country | Product origin | Certifications | Portfolio |
|---|---|---|---|---|---|
| Bayer | Producer | Germany | Germany | CoA, GMP | 42 products |
| Cambrex | Producer | Italy | United States | CoA, GMP | 104 products |
When sending a request, specify which Cefalexin Monohydrate API quality you need: for example EP (Ph. Eur.), USP, JP, BP, or another pharmacopoeial standard, as well as the required grade (base, salt, micronised, specific purity, etc.).
Use the list above to find high-quality Cefalexin Monohydrate API suppliers. For example, you can select GMP, FDA or ISO certified suppliers. Visit our help page to learn more about sourcing APIs via Pharmaoffer.
