Guanidine API Manufacturers & Suppliers
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Guanidine | CAS No: 113-00-8 | GMP-certified suppliers
A medication that reduces muscle weakness and fatigability in Eaton-Lambert myasthenic syndrome by enhancing neuromuscular transmission through increased acetylcholine activity.
Therapeutic categories
Primary indications
- For the reduction of the symptoms of muscle weakness and easy fatigability associated with the myasthenic syndrome of Eaton-Lambert
- It is not indicated for treating myasthenia gravis
Product Snapshot
- Guanidine is formulated as an oral small molecule tablet
- It is primarily used for the symptomatic reduction of muscle weakness and fatigability associated with Eaton-Lambert myasthenic syndrome
- The product is approved for use in the US market
Clinical Overview
Pharmacodynamically, guanidine acts primarily by enhancing the release of the neurotransmitter acetylcholine in response to nerve impulses, thereby improving neuromuscular transmission. Additionally, it appears to modulate muscle cell membrane excitability by slowing depolarization and repolarization rates. These combined effects contribute to the alleviation of symptoms in Eaton-Lambert syndrome.
Guanidine belongs to the chemical class of guanidines, characterized by the guanidine functional group with a general structure (R1R2N)(R3R4N)C=N-R5. It is also classified pharmacologically as an acetylcholine releasing agent and is a known substrate and inhibitor of several organic cation transporters, including MATE1, MATE2, OAT3 (SLC22A8), OCT1, and OCT2. These interactions may influence its absorption, distribution, metabolism, and excretion (ADME) profile, although detailed pharmacokinetic parameters are not specified here.
Safety considerations for guanidine include monitoring for potential toxicity related to its effects on neuromuscular function and caution in patients with renal impairment due to its renal transporter interactions. It has documented use as a laboratory chemical, notably as a protein denaturant and as a fluorescent probe in chromatographic assays, reflecting its utility beyond clinical applications.
From an API sourcing perspective, guanidine must comply with established pharmacopeial standards to ensure purity and reproducibility. Quality control should emphasize the absence of adulterants and impurities, given its chemical reactivity and biological activity. Reliable suppliers with validated manufacturing processes and full regulatory documentation are essential to support pharmaceutical development and therapeutic use.
Identification & chemistry
| Generic name | Guanidine |
|---|---|
| Molecule type | Small molecule |
| CAS | 113-00-8 |
| UNII | JU58VJ6Y3B |
| DrugBank ID | DB00536 |
Pharmacology
| Summary | Guanidine enhances acetylcholine release following nerve impulses, thereby improving neuromuscular transmission. It also modulates muscle cell membrane excitability by slowing depolarization and repolarization processes. These actions contribute to its use in mitigating muscle weakness and fatigability in Eaton-Lambert myasthenic syndrome. |
|---|---|
| Pharmacodynamics | Guanidine apparently acts by enhancing the release of acetylcholine following a nerve impulse. It also appears to slow the rates of depolarization and repolarization of muscle cell membranes. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Aldehyde dehydrogenase, mitochondrial | Humans | inhibitor |
| Ribonuclease pancreatic | Humans | |
| DNA | Humans |
ADME / PK
| Absorption | Rapidly absorbed and distributed |
|---|---|
| Half-life | 7-8 hours |
| Metabolism | Not metabolized. |
Formulation & handling
- Guanidine is a small molecule intended for oral administration, typically formulated as a tablet.
- High water solubility and low LogP suggest favorable dissolution and absorption profiles in oral formulations.
- Handling as a solid is straightforward; no special stability concerns related to moisture or temperature are indicated.
Regulatory status
| Lifecycle | The active pharmaceutical ingredient (API) is approaching patent expiry in the US, with generic versions anticipated to enter the market, indicating a transition toward a more mature market phase with increased competition. |
|---|
| Markets | US |
|---|
Supply Chain
| Supply chain summary | The manufacturing and supply landscape of Guanidine is currently dominated by a single originator company, Schering Corp., which also handles packaging. Branded products such as Guanidine hydrochloride are primarily marketed in the US, with limited presence in other regions. Patent expiration status is not indicated, suggesting either established generics in the market or limited generic competition at this time. |
|---|
Safety
| Toxicity | LD<sub>50</sub> = 475 mg/kg (oral, rat). Can cause severe gastrointestinal symptoms (nausea, vomiting and diarrhea), bone marrow suppression, renal insufficiency and other hematologic abnormalities (anemia, leucopenia). Severe guanidine intoxication is characterized by nervous hyperirritability, fibrillary tremors and convulsive contractions of muscle, salivation, vomiting, diarrhea, hypoglycemia, and circulatory disturbances. |
|---|
- Handle with appropriate protective equipment to avoid ingestion and minimize exposure, due to potential severe gastrointestinal and hematologic toxicity
- Monitor and control environmental release to prevent exposure-related neurotoxicity and renal impairment
- Store in a secure container to prevent accidental contamination or ingestion, considering the compound’s narrow margin of safety
Guanidine is a type of Adrenergic agents
Adrenergic agents are a subcategory of pharmaceutical active pharmaceutical ingredients (APIs) that target the adrenergic system in the body. This system is responsible for regulating various physiological responses, including heart rate, blood pressure, and smooth muscle contraction.
Adrenergic agents can be further divided into two main groups: adrenergic agonists and adrenergic antagonists. Adrenergic agonists stimulate the adrenergic receptors, leading to an increase in sympathetic nervous system activity. This can result in effects such as vasoconstriction, bronchodilation, and increased heart rate. Adrenergic agonists are commonly used in the treatment of conditions such as asthma, hypotension, and cardiac arrest.
On the other hand, adrenergic antagonists block the adrenergic receptors, thereby inhibiting the effects of sympathetic nervous system activation. These agents are often employed to lower blood pressure, treat certain heart conditions, and manage symptoms associated with conditions like benign prostatic hyperplasia. Adrenergic antagonists can be further classified into alpha-adrenergic antagonists and beta-adrenergic antagonists, based on their selectivity for different adrenergic receptor subtypes.
Pharmaceutical companies extensively utilize adrenergic agents as key components in the development of various medications. Adrenergic APIs offer targeted effects on the adrenergic system, allowing for precise modulation of physiological responses. The understanding of adrenergic agents and their mechanisms of action is vital for the design and optimization of drugs used in the treatment of numerous medical conditions. Researchers and scientists continue to explore and innovate within this subcategory to develop new adrenergic agents with enhanced efficacy and fewer side effects, ultimately improving patient outcomes.
Guanidine (Adrenergic agents), classified under Central Nervous System Agents
Central Nervous System (CNS) Agents are a crucial category of pharmaceutical Active Pharmaceutical Ingredients (APIs) that specifically target the central nervous system. The CNS encompasses the brain and spinal cord, playing a vital role in regulating and controlling various bodily functions, including cognition, movement, emotions, and sensory perception. These agents are designed to interact with specific receptors, enzymes, or ion channels within the CNS to modulate neural activity and restore normal functioning.
CNS agents comprise a diverse range of pharmaceutical APIs, including analgesics, anesthetics, antipsychotics, sedatives, hypnotics, anti-epileptics, and antidepressants. Each subcategory addresses distinct neurological disorders and conditions. For instance, analgesics alleviate pain by targeting receptors in the brain and spinal cord, while antipsychotics are employed to manage psychosis symptoms in mental illnesses such as schizophrenia.
The development of CNS agents involves rigorous research, molecular modeling, and extensive clinical trials to ensure safety, efficacy, and specific target engagement. Pharmaceutical companies invest significant resources in identifying novel drug targets, synthesizing new compounds, and optimizing their pharmacological properties. These agents undergo rigorous regulatory evaluations and must adhere to stringent quality standards and guidelines.
Given the prevalence of CNS disorders globally, the market demand for effective CNS agents is substantial. The development of innovative CNS APIs not only improves patient outcomes but also provides valuable commercial opportunities for pharmaceutical companies. Continued advancements in CNS agent research and development hold the promise of groundbreaking therapies that can improve the quality of life for individuals affected by neurological conditions.
