Peringatan Keamanan

If a patient has not taken opioids, naloxone does not have a significant effect on patients.A234599,L33724

The oral LD50 in mice and rats is >1 g/kg.L33699 The intraperitoneal LD50 is 80 mg/kg in mice and 239 mg/kg in rats.L33699 The subcutaneous LD50 is 286 mg/kg in mice and 500 mg/kg in rats.L33699

Naloxone

DB01183

small molecule approved vet_approved

Deskripsi

Naloxone is an opioid antagonist medication used to block or reverse the effects of opioid drugs, particularly within the setting of drug overdoses which are rapidly becoming a leading cause of death worldwide.A234594 More specifically, naloxone has a high affinity for ?-opioid receptors, where it acts as an inverse agonist, causing the rapid removal of any other drugs bound to these receptors.A234594 When taken in large quantities, opioid medications such as morphine, hydromorphone, methadone, heroin, or fentanyl are capable of causing life-threatening symptoms such as respiratory depression, reduced heart rate, slurred speech, drowsiness, and constricted pupils.A234594,L33724 If untreated, this can progress to vomiting, absent pulse and breathing, loss of consciousness, and even death.L33724 Naloxone is indicated for the rapid reversal of these symptoms of central nervous system depression in opioid overdose.A234589 It's important to note that naloxone only works on opioid receptors within the body, and is therefore not capable of reversing the effects of non-opioid medications such as stimulants like methamphetamine or cocaine, or benzodiazepines like lorazepam or diazepam.

Also known as the brand name product Narcan, naloxone is currently available by intramuscular (IM) or subcutaneous (SubQ) injection, nasal spray, or intravenous (IV) infusion.L33729,L33739 Naloxone IM injections are commonly available in the form of "kits", which is ideal for making overdose treatment accessible and readily available for administration by minimally trained individuals within the community.L33734 Kits commonly include the supplies necessary to treat an overdose in a non-medical setting such as alcohol swabs, syringes, a rescue breathing mask, and instructions for use. Frequently also carried by medical and emergency personnel and at events known to be associated with heavy drug use like music festivals, naloxone kits are considered a key component of harm reduction strategies. There are over-the-counter nasal sprays available.

When injected intramuscularly (IM), naloxone acts within three to five minutes. Administration of naloxone is associated with very few side effects. Notably, if injected into a person not currently using opioid medications, there would be no noticeable effects at all. However, for individuals using opioid medications or experiencing an overdose, IM injection of naloxone rapidly reverses opioid effects and can cause the injected individual to immediately experience withdrawal symptoms.A234589 Common symptoms of opioid withdrawal include nausea, vomiting, sweating, runny nose, aches, and diarrhea.A234589 Although certainly physically uncomfortable, opioid withdrawal symptoms are not life-threatening; administration of naloxone is, therefore, appropriate for any person appearing to have any symptoms of an opioid overdose. Due to its short duration of action, persons injected with naloxone should be monitored for responsiveness and potentially injected a second time or taken to the hospital.A234589

Naloxone is also available within the combination product Suboxone with the opioid medication buprenorphine.L33714,L33719 Suboxone is used for the maintenance treatment of opioid dependence and addiction.L33714,L33719 When taken orally, naloxone has no pharmacological effect and does not reduce the effectiveness of the opioid effect of buprenorphine.L33714,L33719 The primary purpose of including naloxone within Suboxone is to act as a deterrent to injection, as injected naloxone would rapidly reverse the effects of buprenorphine.L33714,L33719

Naloxone was granted FDA approval on 13 April 1971.L33709

Struktur Molekul 2D

Berat 327.3743
Wujud solid

Peta Jejaring Molekuler
Legenda: ObatTargetGenEnzim(Panah → menunjukkan arah efek / relasi)TransporterCarrier

Profil Farmakokinetik

Waktu Paruh (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.[L33699] In neonates, the mean half life is 3.1 ± 0.5 hours.[L33699]
Volume Distribusi The volume of distribution of naloxone is 200 L.[A234594] Naloxone distributes into tissues rapidly.[L33694] It can also cross the placenta and blood-brain barrier.[L33694]
Klirens (Clearance) The clearance of naloxone is 2500 L/day.[A234594]

Absorpsi

An intranasal dose of naloxone is 42-47% bioavailable.L33694 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.L33694 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.L33694 A 2 mg intravenous dose reaches a Cmax of 26.2 ng/mL with an AUC of 12.8 h\*ng/mL.L33694

Metabolisme

Naloxone primarily undergoes glucuronidation to form naloxone-3-glucuronide.L33694 Naloxone is also N-dealkylated to noroxymorphone or undergoes 6-keto reduction to naloxol.A234584

Rute Eliminasi

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.L33694 The metabolites naloxone-3-glucuronide, noroxymorphone, and naloxol are all detected in the urine.A234584,L33694

Interaksi Makanan

1 Data
  • 1. Take separate from meals. When formulated as a buccal film or sublingual form, avoid eating or drinking until the film has completely dissolved.

Interaksi Obat

812 Data
Cilostazol Cilostazol may decrease the excretion rate of Naloxone which could result in a higher serum level.
Colchicine Naloxone may decrease the excretion rate of Colchicine which could result in a higher serum level.
Fentanyl The therapeutic efficacy of Fentanyl can be decreased when used in combination with Naloxone.
Alprazolam Alprazolam may decrease the excretion rate of Naloxone which could result in a higher serum level.
Midazolam Midazolam may decrease the excretion rate of Naloxone which could result in a higher serum level.
Methylnaltrexone Naloxone may increase the opioid antagonism activities of Methylnaltrexone.
Naloxegol The therapeutic efficacy of Naloxegol can be decreased when used in combination with Naloxone.
Lamotrigine The metabolism of Naloxone can be increased when combined with Lamotrigine.
Primidone The metabolism of Naloxone can be increased when combined with Primidone.
Rifampin The metabolism of Naloxone can be increased when combined with Rifampicin.
Phenobarbital The metabolism of Naloxone can be increased when combined with Phenobarbital.
Tacrolimus Tacrolimus may decrease the excretion rate of Naloxone which could result in a higher serum level.
Icosapent Icosapent may decrease the excretion rate of Naloxone which could result in a higher serum level.
Cefotiam Cefotiam may decrease the excretion rate of Naloxone which could result in a higher serum level.
Mesalazine Mesalazine may decrease the excretion rate of Naloxone which could result in a higher serum level.
Cefmenoxime Cefmenoxime may decrease the excretion rate of Naloxone which could result in a higher serum level.
Cefmetazole Cefmetazole may decrease the excretion rate of Naloxone which could result in a higher serum level.
Pamidronic acid Pamidronic acid may decrease the excretion rate of Naloxone which could result in a higher serum level.
Tenofovir disoproxil Tenofovir disoproxil may decrease the excretion rate of Naloxone which could result in a higher serum level.
Cidofovir Cidofovir may decrease the excretion rate of Naloxone which could result in a higher serum level.
Cefpiramide Cefpiramide may decrease the excretion rate of Naloxone which could result in a higher serum level.
Ceftazidime Ceftazidime may decrease the excretion rate of Naloxone which could result in a higher serum level.
Loracarbef Loracarbef may decrease the excretion rate of Naloxone which could result in a higher serum level.
Cefalotin Cefalotin may decrease the excretion rate of Naloxone which could result in a higher serum level.
Nabumetone Nabumetone may decrease the excretion rate of Naloxone which could result in a higher serum level.
Ketorolac Ketorolac may decrease the excretion rate of Naloxone which could result in a higher serum level.
Tenoxicam Tenoxicam may decrease the excretion rate of Naloxone which could result in a higher serum level.
Cefotaxime Cefotaxime may decrease the excretion rate of Naloxone which could result in a higher serum level.
Tolmetin Tolmetin may decrease the excretion rate of Naloxone which could result in a higher serum level.
Foscarnet Foscarnet may decrease the excretion rate of Naloxone which could result in a higher serum level.
Piroxicam Piroxicam may decrease the excretion rate of Naloxone which could result in a higher serum level.
Fenoprofen Fenoprofen may decrease the excretion rate of Naloxone which could result in a higher serum level.
Valaciclovir Valaciclovir may decrease the excretion rate of Naloxone which could result in a higher serum level.
Sulindac Sulindac may decrease the excretion rate of Naloxone which could result in a higher serum level.
Bacitracin Bacitracin may decrease the excretion rate of Naloxone which could result in a higher serum level.
Amphotericin B Amphotericin B may decrease the excretion rate of Naloxone which could result in a higher serum level.
Cephaloglycin Cephaloglycin may decrease the excretion rate of Naloxone which could result in a higher serum level.
Adefovir dipivoxil Adefovir dipivoxil may decrease the excretion rate of Naloxone which could result in a higher serum level.
Pentamidine Pentamidine may decrease the excretion rate of Naloxone which could result in a higher serum level.
Etodolac Etodolac may decrease the excretion rate of Naloxone which could result in a higher serum level.
Acyclovir Acyclovir may decrease the excretion rate of Naloxone which could result in a higher serum level.
Naproxen Naproxen may decrease the excretion rate of Naloxone which could result in a higher serum level.
Sulfasalazine Sulfasalazine may decrease the excretion rate of Naloxone which could result in a higher serum level.
Phenylbutazone Phenylbutazone may decrease the excretion rate of Naloxone which could result in a higher serum level.
Carprofen Carprofen may decrease the excretion rate of Naloxone which could result in a higher serum level.
Cefaclor Cefaclor may decrease the excretion rate of Naloxone which could result in a higher serum level.
Diflunisal Diflunisal may decrease the excretion rate of Naloxone which could result in a higher serum level.
Ceforanide Ceforanide may decrease the excretion rate of Naloxone which could result in a higher serum level.
Salicylic acid Salicylic acid may decrease the excretion rate of Naloxone which could result in a higher serum level.
Meclofenamic acid Meclofenamic acid may decrease the excretion rate of Naloxone which could result in a higher serum level.
Acetylsalicylic acid Acetylsalicylic acid may decrease the excretion rate of Naloxone which could result in a higher serum level.
Carboplatin Carboplatin may decrease the excretion rate of Naloxone which could result in a higher serum level.
Oxaprozin Oxaprozin may decrease the excretion rate of Naloxone which could result in a higher serum level.
Ketoprofen Ketoprofen may decrease the excretion rate of Naloxone which could result in a higher serum level.
Balsalazide Balsalazide may decrease the excretion rate of Naloxone which could result in a higher serum level.
Cefditoren Cefditoren may decrease the excretion rate of Naloxone which could result in a higher serum level.
Colistimethate Colistimethate may decrease the excretion rate of Naloxone which could result in a higher serum level.
Cefuroxime Cefuroxime may decrease the excretion rate of Naloxone which could result in a higher serum level.
Cefapirin Cefapirin may decrease the excretion rate of Naloxone which could result in a higher serum level.
Cefadroxil Cefadroxil may decrease the excretion rate of Naloxone which could result in a higher serum level.
Cefprozil Cefprozil may decrease the excretion rate of Naloxone which could result in a higher serum level.
Olsalazine Olsalazine may decrease the excretion rate of Naloxone which could result in a higher serum level.
Lumiracoxib Lumiracoxib may decrease the excretion rate of Naloxone which could result in a higher serum level.
Cefamandole Cefamandole may decrease the excretion rate of Naloxone which could result in a higher serum level.
Cefazolin Cefazolin may decrease the excretion rate of Naloxone which could result in a higher serum level.
Cefonicid Cefonicid may decrease the excretion rate of Naloxone which could result in a higher serum level.
Cefotetan Cefotetan may decrease the excretion rate of Naloxone which could result in a higher serum level.
Cefoxitin Cefoxitin may decrease the excretion rate of Naloxone which could result in a higher serum level.
Ceftizoxime Ceftizoxime may decrease the excretion rate of Naloxone which could result in a higher serum level.
Cefradine Cefradine may decrease the excretion rate of Naloxone which could result in a higher serum level.
Magnesium salicylate Magnesium salicylate may decrease the excretion rate of Naloxone which could result in a higher serum level.
Salsalate Salsalate may decrease the excretion rate of Naloxone which could result in a higher serum level.
Choline magnesium trisalicylate Choline magnesium trisalicylate may decrease the excretion rate of Naloxone which could result in a higher serum level.
Cefepime Cefepime may decrease the excretion rate of Naloxone which could result in a higher serum level.
Cefacetrile Cefacetrile may decrease the excretion rate of Naloxone which could result in a higher serum level.
Ceftibuten Ceftibuten may decrease the excretion rate of Naloxone which could result in a higher serum level.
Cefpodoxime Cefpodoxime may decrease the excretion rate of Naloxone which could result in a higher serum level.
Antrafenine Antrafenine may decrease the excretion rate of Naloxone which could result in a higher serum level.
Tiaprofenic acid Tiaprofenic acid may decrease the excretion rate of Naloxone which could result in a higher serum level.
Hydrolyzed Cephalothin Hydrolyzed Cephalothin may decrease the excretion rate of Naloxone which could result in a higher serum level.
Cephalothin Group Cephalothin Group may decrease the excretion rate of Naloxone which could result in a higher serum level.
Oxyphenbutazone Oxyphenbutazone may decrease the excretion rate of Naloxone which could result in a higher serum level.
Latamoxef Latamoxef may decrease the excretion rate of Naloxone which could result in a higher serum level.
Benoxaprofen Benoxaprofen may decrease the excretion rate of Naloxone which could result in a higher serum level.
Metamizole Metamizole may decrease the excretion rate of Naloxone which could result in a higher serum level.
Ceftobiprole Ceftobiprole may decrease the excretion rate of Naloxone which could result in a higher serum level.
Cimicoxib Cimicoxib may decrease the excretion rate of Naloxone which could result in a higher serum level.
Ceftaroline fosamil Ceftaroline fosamil may decrease the excretion rate of Naloxone which could result in a higher serum level.
Lornoxicam Lornoxicam may decrease the excretion rate of Naloxone which could result in a higher serum level.
Aceclofenac Aceclofenac may decrease the excretion rate of Naloxone which could result in a higher serum level.
Zaltoprofen Zaltoprofen may decrease the excretion rate of Naloxone which could result in a higher serum level.
Azapropazone Azapropazone may decrease the excretion rate of Naloxone which could result in a higher serum level.
Salicylamide Salicylamide may decrease the excretion rate of Naloxone which could result in a higher serum level.
Kebuzone Kebuzone may decrease the excretion rate of Naloxone which could result in a higher serum level.
Isoxicam Isoxicam may decrease the excretion rate of Naloxone which could result in a higher serum level.
Indoprofen Indoprofen may decrease the excretion rate of Naloxone which could result in a higher serum level.
Ibuproxam Ibuproxam may decrease the excretion rate of Naloxone which could result in a higher serum level.
Floctafenine Floctafenine may decrease the excretion rate of Naloxone which could result in a higher serum level.
Fenbufen Fenbufen may decrease the excretion rate of Naloxone which could result in a higher serum level.
Etofenamate Etofenamate may decrease the excretion rate of Naloxone which could result in a higher serum level.

Target Protein

Mu-type opioid receptor OPRM1
Delta-type opioid receptor OPRD1
Kappa-type opioid receptor OPRK1
Cyclic AMP-responsive element-binding protein 1 CREB1
Estrogen receptor ESR1
Toll-like receptor 4 TLR4
Liver carboxylesterase 1 CES1

Referensi & Sumber

Synthesis reference: Bianca Brogmann, Silke Muhlau, Christof Spitzley, "Pharmaceutical preparation containing oxycodone and naloxone." U.S. Patent US20050245556, issued November 03, 2005.
Artikel (PubMed)
  • PMID: 5129377
    Weinstein SH, Pfeffer M, Schor JM, Indindoli L, Mintz M: Metabolites of naloxone in human urine. J Pharm Sci. 1971 Oct;60(10):1567-8. doi: 10.1002/jps.2600601030.
  • PMID: 28722939
    Jordan MR, Morrisonponce D: Naloxone .
  • PMID: 29318006
    Rzasa Lynn R, Galinkin JL: Naloxone dosage for opioid reversal: current evidence and clinical implications. Ther Adv Drug Saf. 2018 Jan;9(1):63-88. doi: 10.1177/2042098617744161. Epub 2017 Dec 13.
  • PMID: 30915992
    Papathanasiou T, Springborg AD, Kongstad KT, Staerk D, Moller K, Taylor BK, Lund TM, Werner MU: High-dose naloxone, an experimental tool uncovering latent sensitisation: pharmacokinetics in humans. Br J Anaesth. 2019 Aug;123(2):e204-e214. doi: 10.1016/j.bja.2018.12.007. Epub 2019 Jan 18.
  • PMID: 24106351
    Kumar K, Singh SI: Neuraxial opioid-induced pruritus: An update. J Anaesthesiol Clin Pharmacol. 2013 Jul;29(3):303-7. doi: 10.4103/0970-9185.117045.

Contoh Produk & Brand

Produk: 370 • International brands: 3
Produk
  • Bunavail
    Film • - • Buccal • US • Approved
  • Bunavail
    Film • - • Buccal • US • Approved
  • Bunavail
    Film • - • Buccal • US • Approved
  • Buprenorphine and Naloxone
    Tablet • - • Sublingual • US • Generic • Approved
  • Buprenorphine and Naloxone
    Tablet • - • Sublingual • US • Generic • Approved
  • Buprenorphine and Naloxone
    Tablet • - • Sublingual • US • Generic • Approved
  • Buprenorphine and Naloxone
    Tablet • - • Sublingual • US • Generic • Approved
  • Buprenorphine and Naloxone
    Tablet • - • Sublingual • US • Generic • Approved
Menampilkan 8 dari 370 produk.
International Brands
  • Kloxxado — Hikma Pharmaceuticals PLC
  • Narcanti
  • Narcon

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