Naloxone is a synthetic opioid receptor antagonist and active pharmaceutical ingredient (API) used to rapidly reverse the effects of opioids. It has a high affinity for opioid receptors and is particularly important for reversing opioid-induced respiratory and central nervous system depression.
Naloxone is commonly used in pharmaceutical products as naloxone hydrochloride, the hydrochloride salt of naloxone. It is an established pharmaceutical compound used in emergency opioid overdose management and opioid-related clinical applications.
Naloxone is a specialized opioid antagonist pharmaceutical API used in the development and manufacture of injectable, intranasal and other pharmaceutical dosage forms.
Important API quality attributes include identity, assay, related substances, water content, residue on ignition, residual solvents, elemental impurities and stereochemical purity, as applicable to the pharmaceutical specification.
CAS Number: 465-65-6
Molecular Formula: C19H21NO4
Molecular Weight: 327.37 g/mol
Drug Class: Opioid Antagonist
Therapeutic Class: Opioid Antidote
Therapeutic Area: Emergency Medicine / Anesthesiology
Molecule Type: Synthetic Small Molecule
Common Pharmaceutical Form: Naloxone Hydrochloride
Naloxone acts as a competitive antagonist at opioid receptors, particularly the mu-opioid receptor.
Its pharmacological activity includes:
Naloxone has little or no opioid agonist activity at therapeutic concentrations and can reverse the effects of morphine and other opioid agonists.
Naloxone API is used in pharmaceutical development for:
Naloxone is particularly important in emergency management of suspected or known opioid overdose. It can rapidly antagonize opioid effects and restore respiratory function when opioid-induced respiratory depression is present.
Because naloxone can precipitate acute opioid withdrawal in opioid-dependent individuals, its administration and dosage are determined according to the clinical situation and applicable medical guidance.
Naloxone is a synthetic opioid antagonist and is generally handled as a pharmaceutical active ingredient. Naloxone hydrochloride is commonly used in finished pharmaceutical products.
The API's appearance, water content, particle characteristics and other physicochemical properties should be controlled according to the applicable pharmaceutical specification.
A controlled Naloxone API manufacturing process may involve:
Typical Naloxone API testing may include:
Store Naloxone API in a tightly closed container under controlled pharmaceutical storage conditions, protected from excessive moisture, heat and direct light.
Final storage conditions should be established according to validated stability data and the applicable API specification.
Naloxone is relevant to research involving:
| Parameter | Specification |
|---|---|
| Appearance | White crystalline powder or crystals |
| Identification | IR & HPLC compliant |
| Assay (HPLC) | 98.0% – 102.0% |
| Loss on Drying | NMT 1.0% |
| Residue on Ignition | NMT 0.5% |
| pH (1% Solution) | 5.0 – 7.0 |
| Individual Impurity | NMT 1.0% |
| Total Impurities | NMT 2.0% |
| Water Content | NMT 1.0% |
| Melting Point | 184–187°C |