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- Opioid analgesics
- Tapentadol
Tapentadol API Manufacturers & Suppliers
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Tapentadol | CAS No: 175591-23-8 | GMP-certified suppliers
A medication that provides opioid analgesia for severe acute and chronic pain, including diabetic neuropathy, reserved for patients with inadequate response to alternative treatments.
Therapeutic categories
Primary indications
- Tapentadol is indicated for the management of acute pain severe enough to require an opioid analgesic and for which alternative treatments are inadequate
- Due to the risks of addiction, drug abuse, and drug misuse, tapentadol is reserved for patients for whom alternative treatment options are unavailable
- [L47286, L47516, L47521]
- The immediate-release tapentadol oral tablets are approved for use in patients six years and older with a body weight of at least 40 kg
Product Snapshot
- Tapentadol is formulated as oral immediate-release and extended-release tablets, as well as oral solution
- It is primarily used for the management of acute and chronic severe pain, including neuropathic pain associated with diabetic peripheral neuropathy, where alternative treatments are inadequate
- Tapentadol is approved for use in the United States and Canada
Clinical Overview
Pharmacologically, tapentadol exhibits a dual mechanism of action. It functions primarily as a selective mu-opioid receptor (MOR) agonist, with a binding affinity at least tenfold greater for MOR than for delta- or kappa-opioid receptors. This activity mediates classic opioid effects such as analgesia, miosis, reduced gastrointestinal motility, and respiratory depression by diminishing brainstem respiratory center sensitivity to carbon dioxide and electrical stimuli. Additionally, tapentadol inhibits norepinephrine reuptake, thereby increasing synaptic noradrenaline levels and facilitating analgesia through alpha-2 adrenergic receptor activation. While it weakly inhibits serotonin reuptake, this effect does not significantly contribute to its analgesic properties.
Regarding absorption, distribution, metabolism, and excretion (ADME), tapentadol is metabolized primarily through phase II conjugation pathways involving UGT1A9 and UGT2B7 enzymes and undergoes minor cytochrome P450 metabolism via CYP2C19, CYP2C9, and CYP2D6 isoforms. These metabolic pathways necessitate careful consideration of potential drug interactions, particularly with CNS depressants, which amplify risks of respiratory depression and overdose. Tapentadol carries a substantial potential for abuse and addiction, which can result in fatal outcomes, especially when combined with alcohol or other central nervous system depressants.
Tapentadol is marketed globally in immediate-release and extended-release formulations, with approvals dating back to 2008 (immediate-release) and 2011 (extended-release) by the U.S. FDA. The extended-release form is not indicated for as-needed use but for steady, long-term pain control in appropriate patients.
From an API procurement perspective, sourcing tapentadol requires stringent quality controls to ensure compliance with pharmacopeial standards and regulatory requirements. Manufacturers must monitor raw material purity, stereochemical integrity, and residual solvent levels, given the critical impact of these parameters on clinical safety and efficacy. Suppliers should provide detailed documentation of synthesis routes and impurity profiles to support regulatory filings and risk assessments.
Identification & chemistry
| Generic name | Tapentadol |
|---|---|
| Molecule type | Small molecule |
| CAS | 175591-23-8 |
| UNII | H8A007M585 |
| DrugBank ID | DB06204 |
Pharmacology
| Summary | Tapentadol is a centrally-acting analgesic that combines selective mu-opioid receptor agonism with noradrenaline reuptake inhibition, enhancing analgesic effects via alpha-2 adrenergic receptor activation. It exhibits typical opioid pharmacodynamic effects, including respiratory depression and miosis. Tapentadol also has weak serotonin reuptake inhibition, which does not significantly contribute to its analgesic activity. |
|---|---|
| Mechanism of action | Tapentadol is a centrally-acting synthetic analgesic. Although their clinical relevance is unclear, tapentadol is believed to have two main mechanisms of action. Tapentadol is a selective mu-opioid receptor (MOR) agonist: it binds to MOR with an affinity greater than or equal to ten-fold affinity compared to delta- and kappa-opioid receptors. Tapentadol also inhibits noradrenaline reuptake, thereby increasing noradrenaline levels and activating alpha-2 receptors to promote analgesia.[A36596, A260731] Tapentadol is a weak serotonin reuptake inhibitor; however, this action does not contribute to its analgesic effect. |
| Pharmacodynamics | Tapentadol is an opioid agonist that exerts physiological effects commonly caused by the opioid drug class. These effects include miosis, reduced gastrointestinal motility, and peripheral vasodilation. Tapentadol produces respiratory depression by reducing the responsiveness of the brain stem respiratory centers to both increases in carbon dioxide tension and electrical stimulation. Tapentadol has a high potential for misuse and abuse, which can lead to the development of substance use disorder. Abuse of tapentadol poses a risk of overdose and death, which increases with alcohol or other central nervous system depressants. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Mu-type opioid receptor | Humans | agonist |
| Sodium-dependent noradrenaline transporter | Humans | inhibitor |
| Kappa-type opioid receptor | Humans | agonist |
ADME / PK
| Absorption | The mean absolute bioavailability after single-dose administration of tapentadol in a fasted state is approximately 32% due to extensive first-pass metabolism. Maximum serum concentrations of tapentadol are typically observed at around 1.25 hours after dosing. Dose-proportional increases in the Cmax and AUC values of tapentadol have been observed over the 50 to 150 mg dose range. A multiple (every 6 hours) dose study with doses ranging from 75 to 175 mg tapentadol showed a mean accumulation factor of 1.6 for the parent drug and 1.8 for the major metabolite tapentadol- O-glucuronide, which are primarily determined by the dosing interval and apparent half-life of tapentadol and its metabolite. The AUC and Cmax increased by 25% and 16%, respectively, when tapentadol was administered after a high-fat, high-calorie breakfast. Tapentadol may be given with or without food. |
|---|---|
| Half-life | The terminal half-life is about four hours after oral administration. |
| Protein binding | The plasma protein binding is approximately 20%. |
| Metabolism | In humans, about 97% of the parent compound is metabolized. Tapentadol is mainly metabolized by Phase II pathways, and only a small amount is metabolized by Phase I oxidative pathways; thus, drug metabolism mediated by cytochrome P450 system is of less importance than phase II conjugation. The major pathway of tapentadol metabolism is conjugation with glucuronic acid to produce glucuronides.[A260716, L47286] After oral administration, approximately 70% of the drug, of which 55% is the O-glucuronide metabolite and 15% is the sulfate metabolite, is excreted in urine. About 3% of the dose was excreted in urine as the unchanged parent drug. Tapentadol can also undergo CYP2C9- and CYP2C19-mediated demethylation to form N-desmethyl tapentadol, which accounts for 13% of the dose. About 2% of tapentadol can also undergo CYP2D6-mediated hydroxylation to form Hydroxy tapentadol. N-desmethyl tapentadol and Hydroxy tapentadol can further be glucuronidated. Metabolites of tapentadol do not contribute to the pharmacological activity of tapentadol.[A260716, L47286] |
| Route of elimination | Tapentadol and its metabolites are 99% excreted via the kidneys. |
| Volume of distribution | Tapentadol is widely distributed throughout the body. Following intravenous administration, the volume of distribution (V<sub>z</sub>) for tapentadol is 540 ± 98 L. |
| Clearance | The total clearance is 1530 ± 177 mL/min. |
Formulation & handling
- Tapentadol is a small molecule API primarily formulated for oral administration in various tablet and solution forms. It exhibits moderate water solubility and logP, relevant for dissolution and absorption considerations in oral formulations. Food intake does not significantly impact bioavailability, but co-administration with alcohol should be avoided due to increased CNS and respiratory depression risk.
Regulatory status
| Lifecycle | The API is marketed in the US and Canada with key US patents expiring between 2017 and 2025, indicating the product is approaching late-stage market maturity in these regions. |
|---|
| Markets | Canada, US |
|---|
Supply Chain
| Supply chain summary | Tapentadol is supplied by multiple originator companies with branded products primarily available in the US and Canadian markets. Several patents protecting the drug have expired or are due to expire between 2017 and 2025, indicating the presence of existing and potentially upcoming generic competition. This patent landscape supports a manufacturing environment that includes both branded and generic API suppliers. |
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Safety
| Toxicity | Intraperitoneal lowest published toxic dose (TDLO) is 10 mg/kg in rats. Acute overdosage with tapentadol is characterized by respiratory depression, somnolence progressing to stupor or coma, skeletal muscle flaccidity, cold and clammy skin, constricted pupils, and, in some cases, pulmonary edema, bradycardia, hypotension, partial or complete airway obstruction, atypical snoring, and death. Marked mydriasis rather than miosis may be seen due to severe hypoxia in overdose situations. Tapentadol overdose is managed by reestablishing a patent and protected airway and using assisted or controlled ventilation if needed. Other supportive measures can manage circulatory shock and pulmonary edema. Cardiac arrest or arrhythmias will require advanced life-support measures. Opioid antagonists, such as [naloxone], are specific antidotes to respiratory depression resulting from opioid overdose. They should be administered, in multiple doses, depending on patient response. As administration of the recommended usual dosage of the opioid antagonist will precipitate an acute withdrawal syndrome in individuals with physical dependence on opioids, administration of the opioid antagonist should be initiated with care and by titration with smaller than usual doses. |
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- Intraperitoneal administration in rats shows a lowest published toxic dose (TDLO) of 10 mg/kg
- Overdose may result in severe respiratory depression, central nervous system depression, cardiovascular instability, and pulmonary edema
- Handling should consider the risk of opioid-related respiratory depression
Tapentadol 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.
Tapentadol (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.
