Filters
Custom request?
Type
Production region
Qualifications
Country of origin
Pholcodine API Manufacturers & Suppliers
4 verified results
Commercial-scale Suppliers
Employees: 500+
All certificates
Employees: 600+
All certificates
All certificates
All certificates
Total market transparency
Supplier trade data access
Buyer / supplier flow comparison
Pholcodine | CAS No: 509-67-1 | GMP-certified suppliers
A medication that provides temporary relief of non-productive dry cough by suppressing cough reflexes without significant respiratory depression or analgesic effects.
Therapeutic categories
Primary indications
- Pholcodine is indicated as a cough suppressant for the temporary relief of non-productive dry cough
- It is stated to present a required label indication of "temporary relief of dry cough
- " Cough is the respiratory movement that occurs after an irritation signal is transmitted to the central nervous system and further stimulates the medulla oblongata
- This stimulation causes a motor output that is sent through motoneurons to the respiratory muscles
Product Snapshot
- Pholcodine is formulated as an oral small molecule available in syrup, lozenge, elixir, solution, and liquid forms
- It is primarily used as a cough suppressant for the temporary relief of non-productive dry cough
- Pholcodine holds approved market status in multiple regions but may also be subject to illicit use concerns
Clinical Overview
Pholcodine acts centrally by targeting the cough center located in the medulla oblongata. Its mechanism involves modulation of peripheral reflexogenic receptors that influence cough initiation. Unlike many opioids, therapeutic doses of pholcodine do not depress respiratory function or induce central nervous system excitation. It exhibits selective action on the neuronal pathways responsible for cough suppression without affecting the respiratory centers.
Pharmacodynamically, pholcodine is noted for its lack of euphoric effects, making psychological dependence unlikely as supported by clinical trials. Compared to codeine, pholcodine can cause a greater degree of respiratory depression and comparable hypotensive effects. Preclinical data also suggest additional pharmacologic actions including histamine release induction, antihistaminic, anticholinergic, anticonvulsant, and mild tranquilizing effects. However, pholcodine exhibits minimal analgesic potency.
Pharmacokinetic properties indicate that pholcodine is predominantly renally excreted; specific absorption, distribution, metabolism, or elimination parameters are limited in published literature. Safety concerns primarily revolve around potential respiratory depression, particularly in overdose scenarios. Pholcodine is not approved in the United States, Canada, and was withdrawn from the UK market in 2008. It remains approved in certain other regions but is controlled due to its opioid nature.
From a sourcing and quality control standpoint, procurement of pholcodine API requires stringent adherence to regulatory guidelines given its classification in various jurisdictions. Suppliers must ensure compliance with material purity, impurity profiling, and appropriate documentation to meet pharmaceutical manufacturing standards and mitigate risks related to opioid misuse or contamination.
Identification & chemistry
| Generic name | Pholcodine |
|---|---|
| Molecule type | Small molecule |
| CAS | 509-67-1 |
| UNII | LPP64AWZ7L |
| DrugBank ID | DB09209 |
Pharmacology
| Summary | Pholcodine acts centrally on the medulla oblongata, specifically targeting the cough center to suppress non-productive dry cough. It exerts its effects primarily through mu, kappa, and delta opioid receptors with a selective impact on cough reflex without significant respiratory depression or CNS excitation at therapeutic doses. Additional pharmacodynamic properties include histamine modulation, anticholinergic, anticonvulsant, and mild tranquilizing actions. |
|---|---|
| Mechanism of action | The mechanism of action of pholcodine is directly performed in the medulla oblongata. In this site, it exerts analgesic properties on the peripheric reflexogenic receptors. This site is commonly known as the "cough center." |
| Pharmacodynamics | The therapeutic doses of pholcodine have been shown not to cause depression of respiration, CNS excitation or other side effects associated with narcotics. It is thought that the impact of pholcodine is selective on the cough center without affecting the respiratory center. Pholcodine is not euphorigenic, and thus, psychological dependence is unlikely. Clinical trials have not shown any evidence of addiction after prolonged administration of pholcodine. It is well reported that pholcodine presents a more considerable respiratory depression effect than codeine and it causes hypotension in the same degree than codeine. Some other noted impacts of pholcodine in preclinical trials are: 1) the induction of histamine release, 2) anti-histaminic effect, 3) anti-acetylcholinic action, 4) anti-convulsant action and 5) mild tranquilizing action. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Mu-type opioid receptor | Humans | antagonist |
| Kappa-type opioid receptor | Humans | antagonist |
| Delta-type opioid receptor | Humans | antagonist |
ADME / PK
| Absorption | After oral administration of 60 mg of pholcodine, the Tmax and Cmax are reported to be 1.3 hours and 26.3 ng/ml. In the same administration, the AUC in plasma and saliva are reported to be 1.67 and 6.61 mg h/l respectively. The absorption of pholcodine is reported to represent approximately 88% of the administered dose. |
|---|---|
| Half-life | After oral administration of 60 mg of pholcodine, the half-life in plasma, saliva and urine are 45, 55 and 45 hours respectively. |
| Protein binding | The protein binding of pholcodine is of approximately of 21-23% and it tends to have a slight variation depending if the administration is chronic. |
| Metabolism | The metabolism of pholcodine seems to be very slow and due to the elimination profile, it is thought that most of the administered dose undergoes metabolism. There is some evidence in preclinical trials that indicate that morphine is a minor metabolite of pholcodine and that it accounts for 1% of the administered dose. |
| Route of elimination | After oral administration of pholcodine, the serum concentration peaks and declines in a monoexponential manner. The percent of the dose excreted unchanged is of approximately 25-30%. Part of the administered dose is composed by metabolites that can be recovered in urine. From the administered dose, the fecal excretion corresponds to the 5% of the administered dose as unchanged pholcodine. |
| Volume of distribution | The reported volume of distribution depends on the pharmacokinetic model and it can be of 265L based on a one-compartment model to 3207L in a two-compartment model. |
| Clearance | After oral administration of 60 mg of pholcodine, the clearance rate was reported to be 126 ml/min. |
Formulation & handling
- Pholcodine is a small molecule oral agent primarily formulated in syrups, elixirs, lozenges, and solutions.
- The compound exhibits moderate water solubility and a low LogP, indicating balanced hydrophilic and lipophilic properties conducive to oral bioavailability.
- Formulation stability considerations should focus on maintaining solution clarity and preventing degradation in liquid oral dosage forms.
Regulatory status
Safety
| Toxicity | Generally, pholcodine is significantly less toxic than codeine. Nonetheless, it is important to consider the significant depressive respiratory effect. |
|---|
- Pholcodine may cause significant respiratory depression
- Appropriate handling to minimize inhalation or accidental exposure is advised
- Use of personal protective equipment is recommended to avoid dermal or mucosal contact due to potential central nervous system effects
Pholcodine is a type of Cough suppressants
Cough suppressants, a subcategory of pharmaceutical active pharmaceutical ingredients (APIs), are commonly used to alleviate coughing symptoms. These medications act on the central nervous system to reduce the urge to cough, providing temporary relief and improving patient comfort. Cough suppressants are widely employed in the treatment of various respiratory conditions, including colds, flu, bronchitis, and allergies.
The primary mechanism of action for cough suppressants involves targeting the cough reflex arc. This reflex arc comprises sensory nerve fibers in the respiratory tract that detect irritants, sending signals to the brainstem to initiate coughing. Cough suppressants work by suppressing this reflex at different points, depending on the specific drug.
One widely used class of cough suppressants is opioid derivatives, such as codeine and hydrocodone. These substances act by binding to opioid receptors in the brain, decreasing the sensitivity of the cough reflex. Another class includes non-opioid agents, such as dextromethorphan, which functions by affecting receptors in the brain called NMDA receptors.
Cough suppressants are available in various formulations, including oral syrups, tablets, and capsules. They are often combined with other active ingredients, such as expectorants or antihistamines, to provide a more comprehensive treatment approach.
While cough suppressants can provide symptomatic relief, it is crucial to use them under proper medical guidance. Certain individuals, such as those with respiratory conditions like chronic obstructive pulmonary disease (COPD) or asthma, may require cautious use or alternative treatment options due to potential side effects or drug interactions.
In conclusion, cough suppressants are an essential subcategory of pharmaceutical APIs utilized to manage coughing symptoms. These medications work by targeting the cough reflex arc in the central nervous system, providing temporary relief from coughing. Careful consideration should be given to appropriate usage and potential contraindications, ensuring safe and effective treatment.
Pholcodine (Cough suppressants), classified under Respiratory Tract Agents
Respiratory Tract Agents are a vital category of pharmaceutical APIs (Active Pharmaceutical Ingredients) designed to treat respiratory conditions and diseases. These agents are specifically formulated to target the respiratory system, which includes the lungs, airways, and nasal passages. They play a crucial role in managing various respiratory disorders, such as asthma, chronic obstructive pulmonary disease (COPD), and allergic rhinitis.
Respiratory Tract Agents encompass a wide range of medications, including bronchodilators, corticosteroids, antihistamines, and mucolytics. Bronchodilators are commonly used to relieve airway constriction and facilitate smooth breathing by relaxing the muscles in the airways. Corticosteroids help reduce inflammation in the respiratory system, alleviating symptoms and preventing exacerbations. Antihistamines work by blocking histamine receptors, thus mitigating allergic reactions that often impact the respiratory tract. Mucolytics aid in loosening and thinning mucus, making it easier to expel from the airways.
These APIs are developed through rigorous research and development processes, ensuring their efficacy, safety, and compliance with regulatory standards. Pharmaceutical manufacturers rely on advanced technologies and stringent quality control measures to produce high-quality Respiratory Tract Agents. These APIs are subsequently incorporated into various dosage forms, including inhalers, nasal sprays, nebulizers, and oral medications.
Respiratory Tract Agents are essential in the management of respiratory conditions, providing relief from symptoms, improving lung function, and enhancing the overall quality of life for patients. They are prescribed by healthcare professionals and often used in combination therapies to achieve optimal results. As respiratory disorders continue to affect a significant portion of the global population, the development and availability of effective Respiratory Tract Agents play a vital role in addressing these health challenges and improving patient outcomes.
Pholcodine API manufacturers & distributors
Compare qualified Pholcodine API suppliers worldwide. We currently have 4 companies offering Pholcodine API, with manufacturing taking place in 4 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 |
|---|---|---|---|---|---|
| Macfarlan Smith | Producer | United Kingdom | United Kingdom | CoA, GMP | 23 products |
| PCAS | Producer | France | Unknown | CEP, CoA, FDA, GMP | 29 products |
| Saneca Pharma | Producer | Slovakia | Slovakia | CEP, CoA, GMP, USDMF | 25 products |
| Temad Co. | Producer | Iran | Iran | CoA, GMP, ISO9001, MSDS, USDMF, WC, WHO-GMP | 24 products |
When sending a request, specify which Pholcodine 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 Pholcodine 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.
