Nalox
Nalox Uses, Dosage, Side Effects, Food Interaction and all others data.
Nalox is a pure opioid antagonist that acts competitively at opioid receptors. While the mechanism of action of naloxone is not fully understood, the preponderance of evidence suggests that naloxone antagonizes the opioid effects by competing for the same receptor sites, especially the opioid mu receptor. Recently, naloxone has been shown to bind all three opioid receptors (mu, kappa and gamma) but the strongest binding is to the mu receptor.
Nalox is an opioid receptor antagonist indicated in the reversal of opioid overdoses. Nalox has a shorter duration of action than opioids and multiple doses may be required. The therapeutic window of naloxone is wide, as it has no effect if a patient has not taken opioids. Patients treated with naloxone may experience opioid withdrawal and a person administering naloxone should be aware that reversal of opioid overdoses may not resolve all the symptoms a patient is experiencing if other drugs are involved.
| Trade Name | Nalox |
| Availability | Prescription only |
| Generic | Naloxone |
| Naloxone Other Names | Nalossone, Naloxona, Naloxone, Naloxonum |
| Related Drugs | Subutex, Sublocade, Zubsolv, Probuphine, Buprenex, Bunavail, Narcan Nasal Spray, Evzio, nalmefene, Kloxxado |
| Weight | 0.4mg/ml, |
| Type | Injection |
| Formula | C19H21NO4 |
| Weight | Average: 327.3743 Monoisotopic: 327.147058165 |
| Protein binding | Naloxone is approximately 45% bound to albumin, but there is significant binding to other proteins. |
| Groups | Approved, Vet approved |
| Therapeutic Class | Antidote preparations |
| Manufacturer | Samarth Life Sciences Pvt Ltd, Haji Medicine Co, |
| Available Country | India, Pakistan, |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Nalox is used for the complete or partial reversal of opioid depression, including respiratory depression, induced by natural and synthetic opioids, including propoxyphene, methadone and certain mixed agonist-antagonist analgesics: nalbuphine, pentazocine, butorphanol, and cyclazocine. Nalox is also used for diagnosis of suspected or known acute opioid overdosage. Nalox may be useful as an adjunctive agent to increase blood pressure in the management of septic shock
Nalox is also used to associated treatment for these conditions: Opioid Dependence, Opioid Overdose, Pruritus, Respiratory Depression, Septic Shock, Severe Pain, Moderate Pain, Suspected Opioid Overdose
How Nalox works
Nalox is a competitive inhibitor of the µ-opioid receptor. Nalox antagonizes the action of opioids, reversing their effects. If a patient has not taken opioids, naloxone does not have a significant effect on patients.
Dosage
Nalox dosage
Reversal of central depression from opioid use during surgery:
- Adult:100-200 mcg at intervals of 2-3 minute, titrate dose according to response while maintaining analgesia.
- Child:5-10 mcg IV at 2-3 min intervals.
Opioid overdosage:
- Adult:0.4-2 mg repeated if necessary at 2-3 min intervals. If there is no response after a total of 10 mg has been given, consider the possibility of overdosage with other drugs. Reduce dose for opioid-dependent patients: 0.1-0.2 mg. IM/SC routes may be used (at IV doses) if IV admin is not feasible.
- Child:Initially 10 mcg/kg IV followed by 100 mcg/kg IV if necessary. Alternatively, 0.4-0.8 mg IM or SC, repeated as necessary, if IV admin is not feasible.
Opioid-induced depression in neonates due to obstetric analgesia:
- Child:10 mcg/kg IV, IM or SC repeated at 2-3 min intervals if necessary or 60 mcg/kg as a single IM dose.
Intravenous:
- Reversal of central depression from opioid: Stable in 0.9% sodium chloride and 5% dextrose inj at 4 mcg/ml for 24 hr.
- Opioid overdosage: Stable in 0.9% sodium chloride and 5% dextrose ing at 4 mcg/ml for 24 hr.
Parenteral: Stable in 0.9% sodium chloride and 5% dextrose inj at 4 mcg/ml for 24 hr.
Side Effects
Occur secondarily to reversal (withdrawal) of narcotic analgesia and sedation. Mental depression, apathy, inability to concentrate, sleepiness, irritability, anorexia, nausea, and vomiting in high oral doses during initial treatment of opiate addiction.
Toxicity
If a patient has not taken opioids, naloxone does not have a significant effect on patients.
The oral LD50 in mice and rats is >1 g/kg. The intraperitoneal LD50 is 80 mg/kg in mice and 239 mg/kg in rats. The subcutaneous LD50 is 286 mg/kg in mice and 500 mg/kg in rats.
Precaution
Patients physically dependent on opioids, or who have received large doses of opioids (acute withdrawal syndrome may be precipitated). Pregnancy and lactation.
Interaction
Decreased effect of opioid analgesics.
Food Interaction
- Take separate from meals. When formulated as a buccal film or sublingual form, avoid eating or drinking until the film has completely dissolved.
Nalox Disease Interaction
Major: CV disordersModerate: liver disease, renal, septic shock
Volume of Distribution
The volume of distribution of naloxone is 200 L. Nalox distributes into tissues rapidly. It can also cross the placenta and blood-brain barrier.
Elimination Route
An intranasal dose of naloxone is 42-47% bioavailable. An 8 mg dose of nasal naloxone reaches a Cmax of 12.3-12.8 ng/mL, with a Tmax of 0.25 hours, and an AUC of 16.7-19.0 h*ng/mL. A 0.4 mg intramuscular dose reaches a Cmax of 0.876-0.910 ng/mL, with a Tmax of 0.25 hours, and an AUC of 1.94-1.95 h*ng/mL. A 2 mg intravenous dose reaches a Cmax of 26.2 ng/mL with an AUC of 12.8 h*ng/mL.
Half Life
The mean half life of naloxone hydrochloride is 1.8-2.7 hours intranasally, 1.4 hours intramuscularly, and 1.2 hours intravenously. In neonates, the mean half life is 3.1 ± 0.5 hours.
Clearance
The clearance of naloxone is 2500 L/day.
Elimination Route
After oral or intravenous administration, naloxone is 25-40% eliminated in the urine within 6 hours, 50% in 24 hours, and 60-70% in 72 hours. The metabolites naloxone-3-glucuronide, noroxymorphone, and naloxol are all detected in the urine.
Pregnancy & Breastfeeding use
Pregnancy Category C. Either studies in animals have revealed adverse effects on the foetus (teratogenic or embryocidal or other) and there are no controlled studies in women or studies in women and animals are not available. Drugs should be given only if the potential benefit justifies the potential risk to the foetus.
Storage Condition
Store at 25° C. Protect from light.
Innovators Monograph
You find simplified version here Nalox
Nalox contains Naloxone see full prescribing information from innovator Nalox Monograph, Nalox MSDS, Nalox FDA label
