Loxicodegol API Manufacturers
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Looking for Loxicodegol API 1211231-76-3?
- Description:
- Here you will find a list of producers, manufacturers and distributors of Loxicodegol. You can filter on certificates such as GMP, FDA, CEP, Written Confirmation and more. Send inquiries for free and get in direct contact with the supplier of your choice.
- API | Excipient name:
- Loxicodegol
- Synonyms:
- Cas Number:
- 1211231-76-3
- DrugBank number:
- DB14146
- Unique Ingredient Identifier:
- J2WIV0JMML
General Description:
Loxicodegol, identified by CAS number 1211231-76-3, is a notable compound with significant therapeutic applications. Loxicodegol was developed by Nektar Therapeutics as an opioid analgesic with low abuse potential for the treatment of chronic pain . The lack of abuse potential is believed to be due to the drug's slow rate of entry into brain, a unique characteristic compared to others in the opioid class . This is also thought to be the reason behind the reduced frequency of CNS-mediated adverse effects, like sedation, seen with Loxicodegol. Nektar Therapeutics has filed an application for FDA approval of Loxicodegol for use in the treatment of chronic lower back pain
Indications:
This drug is primarily indicated for: Loxicodegol was developed as an opioid analgesic with low abuse potential for use in treating chronic pain . An application has been filed for FDA approval of Loxicodegol for use in treating chronic lower back pain. Its use in specific medical scenarios underscores its importance in the therapeutic landscape.
Absorption:
The absorption characteristics of Loxicodegol are crucial for its therapeutic efficacy: Loxicodegol has a Tmax of 1.8h and a bioavailability of 34% with oral administration . It enters the brain about 17-70 times more slowly than oxycodone . Loxicodegol is also a p-glycoprotein substrate further reducing its transport into the brain. The drug's ability to rapidly penetrate into cells ensures quick onset of action.
Half-life:
The half-life of Loxicodegol is an important consideration for its dosing schedule: Loxicodegol has a half-life of 4.53 h allowing for a longer duration of action . This determines the duration of action and helps in formulating effective dosing regimens.
Volume of Distribution:
Loxicodegol is distributed throughout the body with a volume of distribution of: Loxicodegol has a steady-state Vd of 4.19 L/kg . This metric indicates how extensively the drug permeates into body tissues.
Clearance:
The clearance rate of Loxicodegol is a critical factor in determining its safe and effective dosage: Loxicodegol has a clearance rate of 59.3 mL/min/kg . It reflects the efficiency with which the drug is removed from the systemic circulation.
Pharmacodynamics:
Loxicodegol exerts its therapeutic effects through: Loxicodegol displays full analgesic activity comparable to that of oxycodone, producing similar acetone-writhing test responses in mice and hot-plate test maximal latencies in rats . The safety profile of Loxicodegol is much improved from that of other opioid analgesics . The incidence of respiratory depression and sedation is reduced compared to oxycodone and morphine. Generalized pruritus occurred in 7.3% and 4.9% of subjects at 200mg and 400mg of Loxicodegol compared to 41.5% with 40mg oxycodone. Nausea occurred in 2.5%, 2.4%, and 7.3% with 100mg, 200mg, and 400mg of Loxecodegol compared to 29.3% with 40mg oxycodone. Lastly, vomiting occurred in 2.4% with both 200mg and 400mg Loxicodegol compared to 24.4% with 40mg oxycodone. Loxicodegol is much less addictive than other opioid analgesics. It produces a only a slight high at dosages of 400mg, peaking at scores only 25% that of oxycodone, with no difference compared to placebo at lower dosages. No differences have been noted between Loxicodegol and saline in self-administration or behavior reinforcement in monkeys or rats. The drug's ability to modulate various physiological processes underscores its efficacy in treating specific conditions.
Mechanism of Action:
Loxicodegol functions by: Loxicodegol is a full agonist at the μ-opioid receptor. It also displays selectivity towards this subtype with an affinity of 237 nM compared to 4150 nM and >100000 nM for the δ- and κ-opioid receptors. The μ-opioid receptor is activated with an EC₅₀ of 12.5 μM. Activation of this receptor produces an inhibitory effect on neurotransmission through Gi/Go coupling . Opioid medications like Loxicodegol inhibit voltage gated Ca²⁺ channel opening presynaptically on C fibres and activate inward-rectifying K⁺ channels post-synaptically on 2nd order neurons, leading to hyperpolarization. Together, these prevent the nociceptive signal from traveling up the spinal cord to the brain. In the brain, opioids work through a mechanism of inhibition of inhibition to allow regulatory neurons to suppress nociception. This mechanism highlights the drug's role in inhibiting or promoting specific biological pathways, contributing to its therapeutic effects.
Categories:
Loxicodegol is categorized under the following therapeutic classes: Alkaloids, Heterocyclic Compounds, Fused-Ring, Opiate Alkaloids, Phenanthrenes. These classifications highlight the drug's diverse therapeutic applications and its importance in treating various conditions.
Loxicodegol is a type of 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.
