Oxycodone

Oxycodone is a semisynthetic opioid analgesic, renowned for its efficacy in the management of moderate to moderately-severe pain conditions. Developed as an alternative to older opiate-based analgesics, oxycodone has become a pivotal player in pain management both as a standalone agent and in combination with other analgesics, notably acetaminophen.

Oxycodone

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OxyContin branded oxycodone 10mg (OC side)

Pharmacology and Mechanism of Action

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Derived from thebaine, a natural alkaloid sourced from the resin of poppy seeds (Papaver somniferum), oxycodone operates by primarily targeting and activating the μ (mu) type opiate receptor in the central nervous system. This agonistic interaction results in a cascade of neurotransmitter activities culminating in pain modulation and suppression.

Oxycodone's effectiveness in alleviating pain makes it a primary choice for both acute and chronic pain management scenarios. Its history dates back to its synthesis in 1917, and after undergoing comprehensive evaluations, it received the US FDA approval in 1991.

Dosage, Formulations, and Administration

Oxycodone's oral bioavailability ensures its presence in multiple formulations tailored to varied clinical needs:

• Immediate-Release Tablets: Available in 5, 7.5, 10, and 20 mg doses.
• Extended-Release Tablets (OxyContin): Designed for 24-hour pain management, available in doses ranging from 10 to 80 mg.
• Capsules: Typically available in 5 mg.
• Suppositories: For patients unable to ingest orally, available in 10 and 20 mg.
• Oral Solutions: Varied concentrations available to cater to specific patient needs.

Combination Therapies and Brand Associations

For synergistic pain relief, oxycodone is often combined with other non-opioid analgesics. The most prevalent combination is with acetaminophen, but associations with aspirin and ibuprofen also exist. Widely recognized brand formulations include:

• Percocet (Oxycodone and Acetaminophen)
• Tylox (Oxycodone and Acetaminophen)
• Endocet (Oxycodone and Acetaminophen)

Adverse Effects and Clinical Cautions

While oxycodone's therapeutic relevance is unquestionable, its use can result in several side effects:

• Central Nervous System: Sedation, mental clouding, euphoria, agitation, headache, and dizziness.
• Respiratory: Notable respiratory depression, particularly in overdose scenarios.
• Gastrointestinal: Nausea, vomiting, constipation, diarrhea, and abdominal distension.
• Dermatological: Itching and occasional rashes.

Chronic exposure may lead to physical dependency, and abrupt cessation can induce withdrawal symptoms characterized by insomnia, restlessness, pain, and flu-like symptoms.

Regulatory and Abuse Concerns

Given its psychoactive properties, oxycodone falls under the Schedule II category of controlled substances. This DEA classification acknowledges its therapeutic potential but concurrently underscores its abuse liability.

Regrettably, oxycodone misuse has surged in recent decades. Certain formulations can be manipulated for intravenous administration, heightening abuse risks. This misuse trajectory sometimes culminates in illicit drug-seeking behaviors, with heroin becoming a cheaper, more accessible alternative in some regions.

To counteract this, pharmaceutical endeavors are underway to develop tamper-resistant oxycodone formulations to reduce its misuse potential.

Summary

Oxycodone stands as a testament to the duality of drug development - a potent pain modulator with undeniable therapeutic merit, yet a potential conduit for substance abuse and dependency. Its clinical use necessitates vigilant monitoring, patient education, and an unwavering commitment to ensuring patient safety and welfare.

• Dailymed label info on Oxycodone
• FDA Oxycodone

Oxycodone Resources
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• Alfentanil
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Opiate antagonists:

• Nalmefene
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