Pethidine API Manufacturers & Suppliers
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Meperidine | CAS No: 57-42-1 | GMP-certified suppliers
A medication that provides effective management of moderate to severe acute pain, including postoperative and labor pain, with applications in regional anesthesia and shivering control.
Therapeutic categories
Primary indications
- Used to control moderate to severe pain
Product Snapshot
- Meperidine is available as oral and parenteral small molecule formulations, including tablets, capsules, syrups, injections, and solutions
- It is primarily used for the management of moderate to severe pain
- Meperidine is approved for use in key regulatory markets including the US and Canada
Clinical Overview
Pharmacodynamically, meperidine acts as a kappa-opioid receptor agonist with additional local anesthetic properties. It has a higher affinity for kappa-opioid receptors compared to morphine and produces analgesia through modulation of synaptic transmission. Binding to opioid receptors inhibits adenylate cyclase activity, resulting in decreased intracellular cAMP levels and subsequent suppression of nociceptive neurotransmitter release, such as substance P and dopamine. Meperidine also modulates neuronal excitability by closing N-type voltage-operated calcium channels and opening inwardly rectifying potassium channels, leading to neuronal hyperpolarization. Compared to morphine, meperidine has a slightly faster onset and shorter duration of action, and it typically causes less smooth muscle spasm, constipation, and cough reflex depression.
Meperidine's local anesthetic-like chemical structure enables its use in regional anesthesia techniques, such as intravenous regional anesthesia, peripheral nerve blocks, and intraarticular, epidural, and spinal analgesia. Additionally, it has a unique clinical application in alleviating postoperative shivering and amphotericin B-induced shaking chills.
Regarding safety, prolonged meperidine use can lead to dependence of the morphine type, with withdrawal symptoms appearing more rapidly but lasting a shorter duration than those of morphine. Meperidine is metabolized hepatically, involving cytochrome P450 enzymes such as CYP2D6 and CYP3A4, and is primarily eliminated renally. Due to its metabolism and potential for drug interactions, careful substrate and inducer profiling is necessary during therapy.
Meperidine is classified among high-risk opioids and central nervous system depressants. It is also a substrate for P-glycoprotein and has serotonergic activity, indicating a potential risk for serotonin syndrome if coadministered with serotonergic agents.
Notable pharmaceutical brands containing meperidine vary globally, reflecting regional regulatory approvals and usage patterns.
From a sourcing and quality perspective, procurement of meperidine API requires stringent compliance with pharmacopeial standards and regulatory guidelines. The intrinsic risks associated with opioid APIs necessitate robust control measures for purity, residual solvents, and impurity profiles, alongside secure supply chain management to mitigate diversion and ensure consistent quality for pharmaceutical manufacturing.
Identification & chemistry
| Generic name | Meperidine |
|---|---|
| Molecule type | Small molecule |
| CAS | 57-42-1 |
| UNII | 9E338QE28F |
| DrugBank ID | DB00454 |
Pharmacology
| Summary | Meperidine is a synthetic phenylpiperidine opioid that primarily acts as a kappa-opioid receptor agonist, modulating G-protein coupled receptor signaling to inhibit adenylate cyclase activity and reduce neurotransmitter release involved in nociception. It also exhibits local anesthetic properties linked to its chemical structure and interacts with multiple receptor systems including NMDA and muscarinic acetylcholine receptors. Meperidine produces analgesia for moderate to severe acute pain while showing distinct pharmacodynamic effects compared to morphine, including less smooth muscle spasm and a faster onset of action. |
|---|---|
| Mechanism of action | Meperidine is primarily a kappa-opiate receptor agonist and also has local anesthetic effects. Meperidine has more affinity for the kappa-receptor than morphine. Opiate receptors are coupled with G-protein receptors and function as both positive and negative regulators of synaptic transmission via G-proteins that activate effector proteins. Binding of the opiate stimulates the exchange of GTP for GDP on the G-protein complex. As the effector system is adenylate cyclase and cAMP located at the inner surface of the plasma membrane, opioids decrease intracellular cAMP by inhibiting adenylate cyclase. Subsequently, the release of nociceptive neurotransmitters such as substance P, GABA, dopamine, acetylcholine and noradrenaline is inhibited. Opioids also inhibit the release of vasopressin, somatostatin, insulin and glucagon. Opioids close N-type voltage-operated calcium channels (OP2-receptor agonist) and open calcium-dependent inwardly rectifying potassium channels (OP3 and OP1 receptor agonist). This results in hyperpolarization and reduced neuronal excitability. |
| Pharmacodynamics | Meperidine is a synthetic opiate agonist belonging to the phenylpiperidine class. Meperidine may produce less smooth muscle spasm, constipation, and depression of the cough reflex than equivalent doses of morphine. The onset of action is lightly more rapid than with morphine, and the duration of action is slightly shorter. The chemical structure of meperidine is similar to local anesthetics. Meperidine is recommended for relief of moderate to severe acute pain and has the unique ability to interrupt postoperative shivering and shaking chills induced by amphotericin B. Meperidine has also been used for intravenous regional anesthesia, peripheral nerve blocks and intraarticular, epidural and spinal analgesia. Meperidine is considered a second-line agent for the treatment of acute pain. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Kappa-type opioid receptor | Humans | |
| Glutamate receptor ionotropic, NMDA 1 | Humans | antagonist |
| Glutamate receptor ionotropic, NMDA 2B | Humans | antagonist |
ADME / PK
| Absorption | The oral bioavailability of meperidine in patients with normal hepatic function is 50-60% due to extensive first-pass metabolism. Bioavailability increases to 80-90% in patients with hepatic impairment (e.g. liver cirrhosis). Meperidine is less than half as effective when administered orally compared to parenteral administration. One study reported that 80-85% of the drug administered intramuscularly was absorbed within 6 hours of intragluteal injection in health adults; however, inter-individual variation and patient-specific variable appear to cause considerable variations in absorption upon IM injection. |
|---|---|
| Half-life | Initial distribution phase (t<sub>1/2 α</sub>) = 2-11 minutes; terminal elimination phase (t<sub>1/2 β</sub>) = 3-5 hours. In patients with hepatic dysfunction (e.g. liver cirrhosis or active viral hepatitis) the t<sub>1/2 β</sub> is prolonged to 7-11 hours. |
| Protein binding | 60-80% bound to plasma proteins, primarily albumin and α<sub>1</sub>-acid glycoprotein. The presence of cirrhosis or active viral hepatitis does not appear to affect the extent of protein binding. |
| Metabolism | Meperidine is metabolized in the liver by hydrolysis to meperidinic acid followed by partial conjugation with glucuronic acid. Meperidine also undergoes N-demethylation to normeperidine, which then undergoes hydrolysis and partial conjugation. Normeperidine is about half as potent as meperidine, but it has twice the CNS stimulation effects. |
| Route of elimination | Excreted in the urine. The proportion of drug that is excreted unchanged or as metabolites is dependent on pH. When urine pH is uncontrolled, 5-30% of the meperidine dose is excreted as normeperidine and approximately 5% is excreted unchanged. Meperidine and normeperidine are found in acidic urine, while the free and conjugated forms of meperidinic and normperidinic acids are found in alkaline urine. |
| Volume of distribution | Meperidine crosses the placenta and is distributed into breast milk. |
Formulation & handling
- Meperidine is a small molecule opioid available in both oral and parenteral injectable forms including intramuscular, intravenous, and subcutaneous routes.
- The compound exhibits moderate water solubility and a LogP indicating balanced lipophilicity suitable for formulation in aqueous solutions and oral dosage forms.
- Food does not significantly impact the absorption of meperidine, but co-administration with alcohol should be avoided due to potential interactions.
Regulatory status
| Lifecycle | The API's primary patents have expired, enabling generic manufacturing in both the US and Canadian markets. As a result, product availability is expected to increase with competitive pricing and established clinical use. |
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| Markets | US, Canada |
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Supply Chain
| Supply chain summary | Meperidine is produced by numerous originator and generic manufacturers with a long-established presence primarily in the US and Canadian markets. The branded product Demerol is globally recognized but is mainly marketed in North America. Given the multiple manufacturers and absence of exclusivity, patent expiration has led to existing generic competition in these regions. |
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Pethidine 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.
Pethidine (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.
