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- Analgesics
- Opioid analgesics
- Remifentanil
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Remifentanil | CAS No: 132875-61-7 | GMP-certified suppliers
A medication that provides rapid, ultra-short-acting analgesia during induction and maintenance of general anesthesia for effective pain management in surgical procedures.
Therapeutic categories
Primary indications
- For use during the induction and maintenance of general anesthesia
Product Snapshot
- Remifentanil is available as an injectable solution and lyophilized powder formulation for intravenous administration
- It is primarily indicated for use during the induction and maintenance of general anesthesia
- The product is approved for commercial use in regulatory markets including the United States and Canada
Clinical Overview
Pharmacologically, remifentanil functions as a selective mu-opioid receptor agonist. Activation of these receptors results in reduced sympathetic nervous system tone, producing analgesia and respiratory depression. Its pharmacodynamic profile includes an extremely rapid onset of action, with blood-brain equilibration occurring within approximately one minute. Peak opioid effects are achieved quickly, and the duration of analgesic action is brief due to rapid metabolism. The effects and side effect profile, which include typical opioid-mediated responses such as bradycardia, respiratory depression, and hypotension, are dose-dependent and reversible by opioid antagonists like naloxone.
The mechanism of action involves remifentanil binding to central mu-opioid receptors, modulating nociceptive pathways to provide analgesia while attenuating autonomic responses during surgical stimulation. Its metabolic clearance is unique among opioids; remifentanil is rapidly hydrolyzed by nonspecific plasma and tissue esterases, leading to a short context-sensitive half-life. This metabolism results in predictable and easily titratable pharmacokinetics, with minimal risk of accumulation even after prolonged infusion.
Safety considerations include the risk of respiratory depression, hypotension, bradycardia, and potential for serotonin syndrome when combined with serotonergic drugs. Due to its high potency and rapid onset, careful monitoring in controlled clinical environments is essential. Remifentanil is classified among high-risk opioids and should be managed accordingly during anesthesia protocols.
From a sourcing perspective, remifentanil API procurement requires rigorous quality control to ensure purity, potency, and stability, given its sensitivity and clinical application in acute care settings. Compliance with international pharmacopeial standards and stringent manufacturing practices is necessary to maintain consistent therapeutic performance and patient safety.
Identification & chemistry
| Generic name | Remifentanil |
|---|---|
| Molecule type | Small molecule |
| CAS | 132875-61-7 |
| UNII | P10582JYYK |
| DrugBank ID | DB00899 |
Pharmacology
| Summary | Remifentanil is a potent opioid analgesic that acts primarily as a µ-opioid receptor agonist, with additional activity at delta and kappa opioid receptors. It exhibits a rapid onset and ultra-short duration of action due to quick blood-brain equilibration. Its pharmacodynamic effects include dose-dependent analgesia and sedation, which can be reversed by opioid antagonists such as naloxone. |
|---|---|
| Mechanism of action | Remifentanil is a µ-opioid agonist with rapid onset and peak effect, and short duration of action. The µ-opioid activity of remifentanil is antagonized by opioid antagonists such as naloxone. |
| Pharmacodynamics | Remifentanil is an opioid agonist with rapid onset and peak effect and ultra-short duration of action. The opioid activity of remifentanil is antagonized by opioid antagonists such as naloxone. The analgesic effects of remifentanil are rapid in onset and offset. Its effects and side effects are dose dependent and similar to other opioids. Remifentanil in humans has a rapid blood-brain equilibration half-time of 1 ± 1 minutes (mean ± SD) and a rapid onset of action. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Mu-type opioid receptor | Humans | agonist |
| Delta-type opioid receptor | Humans | agonist |
| Kappa-type opioid receptor | Humans | agonist |
ADME / PK
| Half-life | 1-20 minutes |
|---|---|
| Protein binding | 70% (bound to plasma proteins) |
| Metabolism | By hydrolysis of the propanoic acid-methyl ester linkage by nonspecific blood and tissue esterases. |
| Route of elimination | Remifentanil is an esterase-metabolized opioid. The carboxylic acid metabolite is essentially inactive (1/4600 as potent as remifentanil in dogs) and is excreted by the kidneys with an elimination half-life of approximately 90 minutes. |
| Volume of distribution | * 350 mL/kg * 452 ± 144 mL/kg [neonates] * 223 ± 30.6 mL/kg [adolescents] |
| Clearance | * 40 mL/min/kg [young, healthy adults] |
Formulation & handling
- Remifentanil is a small molecule alpha amino acid derivative administered exclusively via intravenous injection or parenteral routes.
- The API is provided as both lyophilized powder and solution formulations requiring appropriate reconstitution and sterile handling for injection.
- Alcohol should be avoided due to potential enhancement of sedative and CNS depressant effects; no oral administration is applicable.
Regulatory status
| Lifecycle | The active pharmaceutical ingredient (API) entered the market following patent expiry in the United States in 2018 and is currently marketed in both the United States and Canada. This indicates a mature market phase with potential generic competition. |
|---|
| Markets | Canada, US |
|---|
Supply Chain
| Supply chain summary | Remifentanil is manufactured by a limited number of originator companies and is marketed primarily in North America, including Canada and the US. Branded products are available mainly in these regions, with multiple formulations under consistent naming. The expiration of key US patents indicates the presence or potential for generic competition in the market. |
|---|
Remifentanil is a type of Opioid analgesics
Opioid analgesics are a subcategory of pharmaceutical Active Pharmaceutical Ingredients (APIs) that are commonly used for pain management. These potent substances interact with specific receptors in the central nervous system, producing analgesic effects and reducing the perception of pain. Opioid analgesics are derived from opium alkaloids or synthetic compounds that mimic their effects. They are classified based on their strength, with some being classified as strong opioids (e.g., morphine, fentanyl) and others as weak opioids (e.g., codeine, tramadol). These APIs work by binding to opioid receptors, primarily located in the brain, spinal cord, and gastrointestinal tract. By activating these receptors, opioid analgesics modulate pain signals, resulting in pain relief. Additionally, they can induce feelings of euphoria, sedation, and respiratory depression, which can be both beneficial and potentially harmful.
Due to their potency and potential for abuse, opioid analgesics are tightly regulated substances. They are primarily prescribed for acute and chronic pain management, such as post-surgical pain, cancer pain, and severe injuries. However, their misuse and addiction potential have led to a public health crisis in many countries.
In conclusion, opioid analgesics are a subcategory of pharmaceutical APIs that play a crucial role in pain management. While they provide effective pain relief, their use requires careful monitoring and adherence to prescribing guidelines to mitigate the risks associated with their potential for abuse and addiction.
Remifentanil (Opioid analgesics), classified under Analgesics
Analgesics are a category of pharmaceutical Active Pharmaceutical Ingredients (APIs) that are commonly used to relieve pain. They are designed to alleviate discomfort by targeting the body's pain receptors or by reducing inflammation. Analgesics are widely utilized in the medical field to manage various types of pain, ranging from mild to severe.
One of the primary classes of analgesics is nonsteroidal anti-inflammatory drugs (NSAIDs). NSAIDs work by inhibiting the production of prostaglandins, substances that contribute to pain and inflammation. This class includes well-known drugs like ibuprofen and naproxen. Another class of analgesics is opioids, which are derived from opium or synthetic compounds that mimic the effects of opium. Opioids act on the central nervous system to reduce pain perception and provide potent pain relief. Examples of opioids include morphine, codeine, and oxycodone.
Analgesics are available in various forms, such as tablets, capsules, creams, and injections, allowing for different routes of administration based on the patient's needs. They are commonly used to manage pain associated with conditions like arthritis, headaches, dental procedures, and post-operative recovery.
It is important to note that analgesics should be used under medical supervision, as improper use or overuse can lead to adverse effects, including gastrointestinal complications, addiction, and respiratory depression in the case of opioids. Therefore, it is crucial for healthcare professionals to assess each patient's individual needs and prescribe the appropriate analgesic and dosage.
In summary, analgesics are a vital category of pharmaceutical APIs used to alleviate pain by targeting pain receptors or reducing inflammation. With various classes and forms available, they provide valuable options for pain management when used responsibly and under medical guidance.
