Naloxone
Identification
- Summary
Naloxone is an opioid receptor antagonist used to rapidly reverse an opioid overdose. Also included in some drug formulations as an abuse deterrent to prevent injection.
- Brand Names
- Kloxxado, Narcan, Suboxone, Targin, Targiniq, Zimhi, Zubsolv
- Generic Name
- Naloxone
- DrugBank Accession Number
- DB01183
- Background
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.3 More specifically, naloxone has a high affinity for μ-opioid receptors, where it acts as an inverse agonist, causing the rapid removal of any other drugs bound to these receptors.3 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.3,13 If untreated, this can progress to vomiting, absent pulse and breathing, loss of consciousness, and even death.13 Naloxone is indicated for the rapid reversal of these symptoms of central nervous system depression in opioid overdose.2 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.14,16 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.15 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.2 Common symptoms of opioid withdrawal include nausea, vomiting, sweating, runny nose, aches, and diarrhea.2 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.2
Naloxone is also available within the combination product Suboxone with the opioid medication buprenorphine.11,12 Suboxone is used for the maintenance treatment of opioid dependence and addiction.11,12 When taken orally, naloxone has no pharmacological effect and does not reduce the effectiveness of the opioid effect of buprenorphine.11,12 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.11,12
Naloxone was granted FDA approval on 13 April 1971.10
- Type
- Small Molecule
- Groups
- Approved, Vet approved
- Structure
- Weight
- Average: 327.3743
Monoisotopic: 327.147058165 - Chemical Formula
- C19H21NO4
- Synonyms
- (−)-naloxone
- 1-N-Allyl-14-hydroxynordihydromorphinone
- 17-allyl-3,14-dihydroxy-4,5α-epoxymorphinan-6-one
- Nalossone
- Naloxona
- Naloxone
- Naloxonum
- External IDs
- EN 1530 Base
Pharmacology
- Indication
Naloxone nasal sprays are indicated for the reversal of an opioid overdose or suspected opioid overdose: it is intended for immediate administration as emergency therapy in settings where opioids may be present.7,20 Intramuscular, intravenous, and subcutaneous injections are indicated for complete or partial reversal of opioid depression, diagnosis of known or suspected opioid overdose, and as an adjunct therapy in the treatment of septic shock.16
Sublingual tablets and films are formulated with buprenorphine for the treatment of opioid dependence.11,12 Naloxone is also formulated with pentazocine as an oral tablet for severe pain.17
Intramuscular or subcutaneous naloxone autoinjectors are used for the emergency treatment of people 12 years of age and older where the use of high-potency opioids such as fentanyl analogues as a chemical weapon, is suspected.18,19
Naloxone has been used off-label for the treatment of neuraxial opioid-induced pruritus.5
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Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Used in combination to treat Opioid dependence Combination Product in combination with: Buprenorphine (DB00921) •••••••••••• ••••• •••••• Reversal of Opioid overdose ••• ••• Reversal of Opioid overdose •••••••••••• ••••••••• Reversal of Opioid overdose •••••••• ••• Diagnostic agent Opioid overdose •••••••••••• ••••••••• - Associated Therapies
- Contraindications & Blackbox Warnings
- Prevent Adverse Drug Events TodayTap into our Clinical API for life-saving information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events with our Clinical API
- Pharmacodynamics
Naloxone is an opioid receptor antagonist indicated in the reversal of opioid overdoses.7 Naloxone has a shorter duration of action than opioids and multiple doses may be required.3,7 The therapeutic window of naloxone is wide, as it has no effect if a patient has not taken opioids.4,7 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.7
- Mechanism of action
Naloxone is a competitive inhibitor of the µ-opioid receptor.7,12 Naloxone antagonizes the action of opioids, reversing their effects.7 If a patient has not taken opioids, naloxone does not have a significant effect on patients.13
Target Actions Organism AMu-type opioid receptor antagonistHumans ADelta-type opioid receptor antagonistHumans AKappa-type opioid receptor antagonistHumans NCyclic AMP-responsive element-binding protein 1 other/unknownHumans NEstrogen receptor alpha antagonistother/unknownHumans UToll-like receptor 4 inhibitorHumans ULiver carboxylesterase 1 binderHumans - Absorption
An intranasal dose of naloxone is 42-47% bioavailable.7 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.7 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.7 A 2 mg intravenous dose reaches a Cmax of 26.2 ng/mL with an AUC of 12.8 h*ng/mL.7
- Volume of distribution
The volume of distribution of naloxone is 200 L.3 Naloxone distributes into tissues rapidly.7 It can also cross the placenta and blood-brain barrier.7
- Protein binding
Naloxone is approximately 45% bound to albumin, but there is significant binding to other proteins.7,12
- Metabolism
Naloxone primarily undergoes glucuronidation to form naloxone-3-glucuronide.7 Naloxone is also N-dealkylated to noroxymorphone or undergoes 6-keto reduction to naloxol.1
Hover over products below to view reaction partners
- Route of elimination
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.7 The metabolites naloxone-3-glucuronide, noroxymorphone, and naloxol are all detected in the urine.1,7
- 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.8 In neonates, the mean half life is 3.1 ± 0.5 hours.8
- Clearance
The clearance of naloxone is 2500 L/day.3
- Adverse Effects
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- Toxicity
If a patient has not taken opioids, naloxone does not have a significant effect on patients.4,13
The oral LD50 in mice and rats is >1 g/kg.8 The intraperitoneal LD50 is 80 mg/kg in mice and 239 mg/kg in rats.8 The subcutaneous LD50 is 286 mg/kg in mice and 500 mg/kg in rats.8
- Pathways
Pathway Category Naloxone Action Pathway Drug action - Pharmacogenomic Effects/ADRs Browse all" title="About SNP Mediated Effects/ADRs" id="snp-actions-info" class="drug-info-popup" href="javascript:void(0);">
- Not Available
Interactions
- Drug Interactions Learn More" title="About Drug Interactions" id="structured-interactions-info" class="drug-info-popup" href="javascript:void(0);">
- This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Drug Interaction Integrate drug-drug
interactions in your softwareAbacavir Abacavir 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. Acemetacin Acemetacin may decrease the excretion rate of Naloxone which could result in a higher serum level. Acetaminophen Acetaminophen may decrease the excretion rate of Naloxone which could result in a higher serum level. Acetazolamide Acetazolamide may increase the excretion rate of Naloxone which could result in a lower serum level and potentially a reduction in efficacy. - Food Interactions
- Take separate from meals. When formulated as a buccal film or sublingual form, avoid eating or drinking until the film has completely dissolved.
Products
- Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.
- Product Ingredients
Ingredient UNII CAS InChI Key Naloxone hydrochloride F850569PQR 357-08-4 RGPDIGOSVORSAK-STHHAXOLSA-N Naloxone hydrochloride dihydrate 5Q187997EE 51481-60-8 TXMZWEASFRBVKY-IOQDSZRYSA-N - Product Images
- International/Other Brands
- Kloxxado (Hikma Pharmaceuticals PLC) / Narcanti / Narcon
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Evzio Injection, solution 0.4 mg/1 Intramuscular; Subcutaneous Kaleo, Inc 2014-04-03 2018-05-31 US Evzio Injection, solution 2 mg/0.4mL Intramuscular; Subcutaneous kaleo, Inc. 2016-10-19 2021-09-30 US EVZIO(R) NALOXONE HCl Injection, solution 2 mg/0.4mL Intramuscular; Subcutaneous HF Acquisition Co LLC, DBA HealthFirst 2020-01-11 Not applicable US Injectable Naloxone Hydrochloride Solution 1 mg / mL Intramuscular; Intravenous; Subcutaneous Omega Laboratories Ltd Not applicable Not applicable Canada Injectable Naloxone Hydrochloride Solution 0.4 mg / mL Intramuscular; Intravenous; Subcutaneous Omega Laboratories Ltd 2016-08-05 Not applicable Canada - Generic Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Naloxone Hci Injection, solution 0.4 mg/1mL Intramuscular; Intravenous; Subcutaneous Hf Acquisition Co. Llc, Dba Health First 2018-08-18 Not applicable US NALOXONE HCl Spray 4 mg/0.1mL Nasal HF Acquisition Co LLC, DBA HealthFirst 2023-04-10 Not applicable US Naloxone HCl Spray 4 mg/0.1mL Nasal Advanced Rx Pharmacy of Tennessee, LLC 2023-02-08 Not applicable US Naloxone HCl Injection 0.4 mg/1mL Intramuscular; Intravenous; Subcutaneous Renaissance Ssa, Llc 2019-12-28 Not applicable US Naloxone Hydrochloride Injection, solution 0.4 mg/1mL Intramuscular; Intravenous; Subcutaneous Medical Purchasing Solutions, Llc 2017-02-28 2023-08-31 US - Over the Counter Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Naloxone Hydrochloride Spray 4 mg/0.1mL Nasal Padagis Israel Pharmaceuticals Ltd 2023-07-30 Not applicable US Naloxone Hydrochloride Spray 4 mg/0.1mL Nasal A-S Medication Solutions 2023-07-30 Not applicable US Narcan Spray 4 mg/0.1mL Nasal Emergent Devices Inc. 2023-08-28 Not applicable US RiVive Spray 3 mg/0.1mL Nasal Harm Reduction Therapeutics, Inc. 2024-01-02 Not applicable US - Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image APOKLISI Naloxone hydrochloride (5 MG) + Oxycodone hydrochloride (10 MG) Tablet, extended release Oral Neopharmed Gentili S.P.A. 2020-05-28 2022-06-24 Italy APOKLISI Naloxone hydrochloride (5 MG) + Oxycodone hydrochloride (10 MG) Tablet, extended release Oral Neopharmed Gentili S.P.A. 2020-05-28 2022-06-24 Italy APOKLISI Naloxone hydrochloride (2.5 MG) + Oxycodone hydrochloride (5 MG) Tablet, extended release Oral Neopharmed Gentili S.P.A. 2020-05-28 2022-06-24 Italy APOKLISI Naloxone hydrochloride (2.5 MG) + Oxycodone hydrochloride (5 MG) Tablet, extended release Oral Neopharmed Gentili S.P.A. 2020-05-28 2022-06-24 Italy APOKLISI Naloxone hydrochloride (2.5 MG) + Oxycodone hydrochloride (5 MG) Tablet, extended release Oral Neopharmed Gentili S.P.A. 2020-05-28 2022-06-24 Italy
Categories
- ATC Codes
- A06AH04 — Naloxone
- A06AH — Peripheral opioid receptor antagonists
- A06A — DRUGS FOR CONSTIPATION
- A06 — DRUGS FOR CONSTIPATION
- A — ALIMENTARY TRACT AND METABOLISM
- V03AB — Antidotes
- V03A — ALL OTHER THERAPEUTIC PRODUCTS
- V03 — ALL OTHER THERAPEUTIC PRODUCTS
- V — VARIOUS
- Drug Categories
- Alimentary Tract and Metabolism
- Alkaloids
- Analgesics
- Antidotes
- Central Nervous System Agents
- Cytochrome P-450 CYP2C18 Substrates
- Cytochrome P-450 CYP2C19 Substrates
- Cytochrome P-450 CYP3A Inhibitors
- Cytochrome P-450 CYP3A Substrates
- Cytochrome P-450 CYP3A4 Inhibitors
- Cytochrome P-450 CYP3A4 Inhibitors (strength unknown)
- Cytochrome P-450 CYP3A4 Inhibitors (strong)
- Cytochrome P-450 CYP3A4 Substrates
- Cytochrome P-450 Enzyme Inhibitors
- Cytochrome P-450 Substrates
- Drugs for Constipation
- Drugs that are Mainly Renally Excreted
- Heterocyclic Compounds, Fused-Ring
- Morphinans
- Natural Opium Alkaloids
- Nervous System
- Opiate Alkaloids
- Opiate Antagonists
- Opioid Antagonists
- P-glycoprotein substrates
- Peripheral Nervous System Agents
- Peripheral Opioid Receptor Antagonists
- Phenanthrenes
- Sensory System Agents
- UGT1A1 Substrates
- Chemical TaxonomyProvided by Classyfire
- Description
- This compound belongs to the class of organic compounds known as phenanthrenes and derivatives. These are polycyclic compounds containing a phenanthrene moiety, which is a tricyclic aromatic compound with three non-linearly fused benzene.
- Kingdom
- Organic compounds
- Super Class
- Benzenoids
- Class
- Phenanthrenes and derivatives
- Sub Class
- Not Available
- Direct Parent
- Phenanthrenes and derivatives
- Alternative Parents
- Isoquinolones and derivatives / Tetralins / Coumarans / 1-hydroxy-2-unsubstituted benzenoids / Alkyl aryl ethers / Aralkylamines / Piperidines / Tertiary alcohols / Trialkylamines / 1,2-aminoalcohols show 7 more
- Substituents
- 1,2-aminoalcohol / 1-hydroxy-2-unsubstituted benzenoid / Alcohol / Alkyl aryl ether / Amine / Aralkylamine / Aromatic heteropolycyclic compound / Azacycle / Carbonyl group / Coumaran show 19 more
- Molecular Framework
- Aromatic heteropolycyclic compounds
- External Descriptors
- morphinane alkaloid, organic heteropentacyclic compound (CHEBI:7459)
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- 36B82AMQ7N
- CAS number
- 465-65-6
- InChI Key
- UZHSEJADLWPNLE-GRGSLBFTSA-N
- InChI
- InChI=1S/C19H21NO4/c1-2-8-20-9-7-18-15-11-3-4-12(21)16(15)24-17(18)13(22)5-6-19(18,23)14(20)10-11/h2-4,14,17,21,23H,1,5-10H2/t14-,17+,18+,19-/m1/s1
- IUPAC Name
- (1S,5R,13R,17S)-10,17-dihydroxy-4-(prop-2-en-1-yl)-12-oxa-4-azapentacyclo[9.6.1.0^{1,13}.0^{5,17}.0^{7,18}]octadeca-7(18),8,10-trien-14-one
- SMILES
- OC1=CC=C2C[C@H]3N(CC=C)CC[C@@]45[C@@H](OC1=C24)C(=O)CC[C@@]35O
References
- Synthesis Reference
Bianca Brogmann, Silke Muhlau, Christof Spitzley, "Pharmaceutical preparation containing oxycodone and naloxone." U.S. Patent US20050245556, issued November 03, 2005.
US20050245556- General References
- 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. [Article]
- Jordan MR, Morrisonponce D: Naloxone . [Article]
- 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. [Article]
- 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. [Article]
- 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. [Article]
- Link [Link]
- FDA Approved Drug Products: Kloxxado (Naloxone) Nasal Spray [Link]
- Caymen Chemical: Naloxone MSDS [Link]
- International Pharmacopoeia: Naloxone Hydrochloride [Link]
- FDA Approved Drug Products: Narcan (Naloxone) Injection (Discontinued) [Link]
- FDA Approved Drug Products: Suboxone (Buprenorphine, Naloxone) Sublingual, Buccal Film [Link]
- FDA Approved Drug Products: Zubsolv (Buprenorphine, Naloxone) Sublingual Tablet [Link]
- British Columbia CDC: Administration of Naloxone [Link]
- FDA Approved Drug Products: Narcan (Naloxone) Nasal Spray [Link]
- DailyMed: Lifems (Naloxone Hydrochloride) Kit [Link]
- Dailymed: Naloxone Hydrochloride Subcutaneous, Intramuscular, Intravenous Injection [Link]
- DailyMed: Naloxone and Pentazocine Oral Tablet [Link]
- FDA Approved Drug Products: Naloxone Hydrochloride Injection Auto-Injector (referred throughout as NALOXONE AUTO-INJECTOR) for intramuscular or subcutaneous use [Link]
- Kaléo News: FDA Approves Kaléo’s Naloxone Auto-Injector 10 mg for the Treatment of Known or Potential Exposure to Ultra-Potent Weaponized Opioids [Link]
- FDA Approved Drug Products: Naloxone Hydrochloride Nasal Spray [Link]
- FDA Approved Drug Products: NARCAN® (naloxone hydrochloride) Nasal Spray [Link]
- External Links
- Human Metabolome Database
- HMDB0015314
- KEGG Drug
- D08249
- KEGG Compound
- C07252
- PubChem Compound
- 5284596
- PubChem Substance
- 46508816
- ChemSpider
- 4447644
- BindingDB
- 54795
- 7242
- ChEBI
- 7459
- ChEMBL
- CHEMBL80
- ZINC
- ZINC000000389747
- Therapeutic Targets Database
- DAP000097
- PharmGKB
- PA450586
- Guide to Pharmacology
- GtP Drug Page
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- Wikipedia
- Naloxone
- MSDS
- Download (74 KB)
Clinical Trials
- Clinical Trials Learn More" title="About Clinical Trials" id="clinical-trials-info" class="drug-info-popup" href="javascript:void(0);">
Phase Status Purpose Conditions Count 4 Active Not Recruiting Prevention Hypoglycemia / Hypoglycemia Unawareness / Type 1 Diabetes Mellitus 1 4 Active Not Recruiting Treatment Constipation / Postoperative pain 1 4 Completed Health Services Research Human Immunodeficiency Virus (HIV) Infections / Opioid Use Disorder (OUD) 1 4 Completed Other Naloxone 1 4 Completed Prevention Opioid Induced Constipation (OIC) / Postoperative pain 1
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Amphastar Pharmaceuticals
- A-S Medication Solutions LLC
- Bristol-Myers Squibb Co.
- Bryant Ranch Prepack
- Cardinal Health
- Dispensing Solutions
- Diversified Healthcare Services Inc.
- Endo Pharmaceuticals Inc.
- General Injectables and Vaccines Inc.
- Hospira Inc.
- Lake Erie Medical and Surgical Supply
- Letco Medical Inc.
- Mallinckrodt Inc.
- Mckesson Corp.
- Nucare Pharmaceuticals Inc.
- Physicians Total Care Inc.
- Reckitt Benckiser Inc.
- Southwood Pharmaceuticals
- Stat Rx Usa
- Dosage Forms
Form Route Strength Tablet, extended release Oral 2.5 MG Tablet, extended release Oral 20 MG Film Buccal Film Buccal; Sublingual Film, soluble Buccal; Sublingual Injection, solution 0.4 mg/1ml Injection, solution Intramuscular; Subcutaneous 0.4 mg/1 Injection, solution Intramuscular; Subcutaneous 2 mg/0.4mL Spray Nasal 8 mg/0.1mL Solution Parenteral 0.040 mg Injection; kit Parenteral; Topical Injection Intramuscular; Intravenous Injection Intramuscular; Intravenous; Subcutaneous 0.4 mg/ml Solution Parenteral 0.4 mg Solution Intramuscular; Intravenous; Subcutaneous 0.4 mg Spray Nasal 3.6 MG Injection, solution Parenteral 0.4 MG/ML Injection, solution 0.4 MG/ML Injection, solution Intramuscular; Intravenous; Subcutaneous 0.04 MG/2ML Injection, solution Injection, solution 0.04 MG/2ML Liquid Intramuscular; Intravenous; Subcutaneous 0.4 mg / mL Liquid Intramuscular; Intravenous; Subcutaneous 1 mg / mL Inhalant Nasal 4 mg/0.1mL Injection Intramuscular; Intravenous; Subcutaneous 0.4 mg/1mL Injection Intramuscular; Intravenous; Subcutaneous 1 mg/1mL Injection Parenteral 0.4 mg/1mL Injection Parenteral 1 mg/1mL Injection Parenteral 4 mg/1mL Injection, solution Intramuscular; Intravenous; Subcutaneous .4 mg/1mL Injection, solution Intramuscular; Intravenous; Subcutaneous 0.02 mg/1mL Injection, solution Intramuscular; Intravenous; Subcutaneous 0.4 mg/1mL Injection, solution Intramuscular; Intravenous; Subcutaneous 1 mg/1mL Spray, metered Nasal 4 mg/0.1mL Injection 0.44 mg/2ml Powder Not applicable 1 kg/1kg Solution Intramuscular; Intravenous; Subcutaneous 4 mg / 10 mL Injection, solution Intramuscular; Subcutaneous 10 mg/0.4mL Spray Nasal 4 mg/0.25mL Injection Intravenous 0.02 mg/1mL Injection Intravenous 0.4 mg/1mL Injection Intravenous 1 mg/1mL Spray Nasal 2 mg/0.1mL Spray Nasal 4 mg/0.1mL Liquid Intramuscular; Intravenous; Subcutaneous 0.02 mg / mL Solution Intramuscular; Intravenous; Subcutaneous 0.4 mg / mL Spray, metered Nasal 2 mg / 0.1 mL Spray, metered Nasal 4 mg / 0.1 mL Solution 0.4 mg/1ml Injection Spray Nasal 1.8 MG Tablet, extended release Oral Tablet Oral Solution Intramuscular 0.400 mg Spray Nasal 3 mg/0.1mL Solution Intramuscular; Intravenous; Subcutaneous 1 mg / mL Film, soluble Sublingual Tablet Oral; Sublingual Tablet Sublingual Tablet, orally disintegrating Sublingual 2.16 MG Tablet, orally disintegrating Sublingual 8.64 MG Film Sublingual Tablet, film coated, extended release Oral 5 mg Tablet, film coated, extended release Oral 10 mg Tablet, film coated, extended release Oral 20 mg Tablet, film coated, extended release Oral 2.5 mg Tablet, film coated, extended release Oral Solution Oral Spray Nasal Spray Nasal 1.26 MG Injection, solution Intramuscular; Subcutaneous 5 mg/0.5mL Tablet, orally disintegrating Sublingual - Prices
Unit description Cost Unit Naloxone hcl powder 70.9USD g Naloxone 0.4 mg/ml vial 7.07USD ml Naloxone 0.4 mg/ml ampul 4.78USD ml Narcan 0.4 mg/ml ampul 4.58USD ml Naloxone 0.02 mg/ml vial 0.84USD ml DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region US9205082 No 2015-12-08 2022-05-10 US US7579019 No 2009-08-25 2020-01-22 US US6159498 No 2000-12-12 2016-10-18 US US9073933 No 2015-07-07 2025-03-30 US US7674800 No 2010-03-09 2025-03-30 US US7683072 No 2010-03-23 2025-03-30 US US7674799 No 2010-03-09 2025-03-30 US US8475832 No 2013-07-02 2030-03-26 US US8603514 No 2013-12-10 2024-04-03 US US8017150 No 2011-09-13 2023-02-13 US US8425462 No 2013-04-23 2024-11-23 US US8231573 No 2012-07-31 2028-11-25 US US8016788 No 2011-09-13 2025-03-21 US US8206360 No 2012-06-26 2027-02-27 US US9238108 No 2016-01-19 2027-01-22 US US8226610 No 2012-07-24 2029-04-10 US US7918823 No 2011-04-05 2024-11-23 US US8608698 No 2013-12-17 2024-11-23 US US8021344 No 2011-09-20 2029-11-02 US US8361029 No 2013-01-29 2024-11-23 US US8313466 No 2012-11-20 2024-11-23 US US7731690 No 2010-06-08 2025-01-15 US US9278182 No 2016-03-08 2026-02-01 US US7731686 No 2010-06-08 2026-06-01 US US8926594 No 2015-01-06 2026-03-31 US US7749194 No 2010-07-06 2028-10-30 US US9056170 No 2015-06-16 2024-11-23 US US7947017 No 2011-05-24 2028-03-12 US US8939943 No 2015-01-27 2031-02-28 US US8627816 No 2014-01-14 2032-02-04 US US9022022 No 2015-05-05 2031-02-28 US US8147866 No 2012-04-03 2027-07-23 US US8703177 No 2014-04-22 2032-08-20 US US8470361 No 2013-06-25 2030-05-22 US US8454996 No 2013-06-04 2019-09-24 US US8658198 No 2014-02-25 2027-12-03 US US8940330 No 2015-01-27 2032-09-18 US US9259421 No 2016-02-16 2032-09-18 US US9168252 No 2015-10-27 2022-05-10 US US9161937 No 2015-10-20 2022-05-10 US US8969369 No 2015-03-03 2022-05-10 US US9084729 No 2015-07-21 2022-05-10 US US9283216 No 2016-03-15 2022-05-10 US US9056051 No 2015-06-16 2022-05-10 US US8846090 No 2014-09-30 2023-04-04 US US6277384 No 2001-08-21 2018-12-22 US US8822487 No 2014-09-02 2018-12-22 US US8673355 No 2014-03-18 2018-12-22 US US6696066 No 2004-02-24 2018-12-22 US US8846091 No 2014-09-30 2023-04-04 US US9211253 No 2015-12-15 2035-03-16 US US9522919 No 2016-12-20 2025-03-30 US US9517307 No 2016-12-13 2034-07-18 US US9474869 No 2016-10-25 2031-02-28 US US9522188 No 2016-12-20 2035-04-24 US US9655843 No 2017-05-23 2027-07-23 US US9439900 No 2016-09-13 2032-09-18 US US9345701 No 2016-05-24 2022-05-10 US US9511066 No 2016-12-06 2022-05-10 US US9555000 No 2017-01-31 2023-04-04 US US9474750 No 2016-10-25 2018-12-22 US US9283221 No 2016-03-15 2022-05-10 US US9480644 No 2016-11-01 2035-03-16 US US9629965 No 2017-04-25 2035-03-16 US US9561177 No 2017-02-07 2035-03-16 US US9468747 No 2016-10-18 2035-03-16 US US9707226 No 2017-07-18 2035-03-16 US US9687454 No 2017-06-27 2029-08-07 US US9724471 No 2017-08-08 2027-05-23 US US9775838 No 2017-10-03 2035-03-16 US US9737669 No 2017-08-22 2024-11-23 US US9855221 No 2018-01-02 2022-02-14 US US9907793 No 2018-03-06 2023-04-04 US US9931305 No 2018-04-03 2022-02-14 US US10085937 No 2018-10-02 2035-03-16 US US10143972 No 2018-12-04 2031-05-24 US US10220158 No 2019-03-05 2035-03-20 US US10143792 No 2018-12-04 2031-05-24 US US10285910 No 2019-05-14 2022-10-11 US US10314977 No 2019-06-11 2024-11-23 US US10322239 No 2019-06-18 2031-02-28 US US10335549 No 2019-07-02 2025-04-30 US US10737028 No 2020-08-11 2024-11-23 US US10874661 No 2020-12-29 2032-09-18 US US10946010 No 2021-03-16 2032-09-18 US US10973814 No 2021-04-13 2034-08-26 US US10722510 No 2020-07-28 2034-08-26 US US10960155 No 2021-03-30 2026-06-25 US US11020388 No 2021-06-01 2032-09-18 US US11020387 No 2021-06-01 2032-09-18 US US11135216 No 2021-10-05 2029-08-07 US US9814838 No 2017-11-14 2031-02-28 US US11135155 No 2021-10-05 2034-08-26 US US11027072 No 2021-06-08 2039-05-24 US US11433066 No 2012-09-18 2032-09-18 US US11571518 No 2021-06-14 2041-06-14 US US11590286 No 2006-12-12 2026-12-12 US US11617713 No 2014-08-26 2034-08-26 US US11628139 No 2014-08-26 2034-08-26 US US11020343 No 2021-06-01 2032-05-11 US
Properties
- State
- Solid
- Experimental Properties
Property Value Source melting point (°C) 177 °C International Pharmacopoeia water solubility Soluble FDA Label logP 2.09 HANSCH,C ET AL. (1995) - Predicted Properties
Property Value Source Water Solubility 5.64 mg/mL ALOGPS logP 1.47 ALOGPS logP 1.62 Chemaxon logS -1.8 ALOGPS pKa (Strongest Acidic) 10.07 Chemaxon pKa (Strongest Basic) 7.84 Chemaxon Physiological Charge 1 Chemaxon Hydrogen Acceptor Count 5 Chemaxon Hydrogen Donor Count 2 Chemaxon Polar Surface Area 70 Å2 Chemaxon Rotatable Bond Count 2 Chemaxon Refractivity 88.72 m3·mol-1 Chemaxon Polarizability 33.83 Å3 Chemaxon Number of Rings 5 Chemaxon Bioavailability 1 Chemaxon Rule of Five Yes Chemaxon Ghose Filter Yes Chemaxon Veber's Rule No Chemaxon MDDR-like Rule No Chemaxon - Predicted ADMET Features
Property Value Probability Human Intestinal Absorption + 0.9729 Blood Brain Barrier + 0.9787 Caco-2 permeable + 0.8867 P-glycoprotein substrate Substrate 0.8788 P-glycoprotein inhibitor I Non-inhibitor 0.7922 P-glycoprotein inhibitor II Non-inhibitor 0.8382 Renal organic cation transporter Inhibitor 0.5 CYP450 2C9 substrate Non-substrate 0.8522 CYP450 2D6 substrate Substrate 0.5296 CYP450 3A4 substrate Substrate 0.6107 CYP450 1A2 substrate Non-inhibitor 0.9046 CYP450 2C9 inhibitor Non-inhibitor 0.9303 CYP450 2D6 inhibitor Non-inhibitor 0.7886 CYP450 2C19 inhibitor Non-inhibitor 0.9025 CYP450 3A4 inhibitor Non-inhibitor 0.9153 CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.9523 Ames test Non AMES toxic 0.7182 Carcinogenicity Non-carcinogens 0.9583 Biodegradation Not ready biodegradable 0.9968 Rat acute toxicity 2.7231 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.7798 hERG inhibition (predictor II) Non-inhibitor 0.8641
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
- Chromatographic Properties
Collision Cross Sections (CCS)
Adduct CCS Value (Å2) Source type Source [M-H]- 180.7506744 predictedDarkChem Lite v0.1.0 [M-H]- 181.48648 predictedDeepCCS 1.0 (2019) [M+H]+ 180.8025744 predictedDarkChem Lite v0.1.0 [M+H]+ 183.87685 predictedDeepCCS 1.0 (2019) [M+Na]+ 180.7681744 predictedDarkChem Lite v0.1.0 [M+Na]+ 191.71365 predictedDeepCCS 1.0 (2019)
Targets
![](https://go.drugbank.com/assets/locked/DrugTargets2-682eb846d210ae4bf33ca03febccfb57bb1c61318e699b729e5df4dfab2c5b67.png)
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Antagonist
- General Function
- Voltage-gated calcium channel activity
- Specific Function
- Receptor for endogenous opioids such as beta-endorphin and endomorphin. Receptor for natural and synthetic opioids including morphine, heroin, DAMGO, fentanyl, etorphine, buprenorphin and methadone...
- Gene Name
- OPRM1
- Uniprot ID
- P35372
- Uniprot Name
- Mu-type opioid receptor
- Molecular Weight
- 44778.855 Da
References
- Narita M, Suzuki M, Mizoguchi H, Narita M, Yajima Y, Sakurada S, Tseng LF, Suzuki T: Up-regulation of mu-opioid receptor-mediated G-protein activation in protein kinase Cgamma knockout mice following repeated naloxone treatment. Neurosci Lett. 2003 Feb 27;338(2):103-6. [Article]
- Freye E, Latasch L, Von Bredow G, Neruda B: [The opioid tramadol demonstrates excitatory properties of non-opioid character--a preclinical study using alfentanil as a comparison]. Schmerz. 1998 Feb 28;12(1):19-24. [Article]
- Neal CR Jr, Owens CE, Taylor LP, Hoversten MT, Akil H, Watson SJ Jr: Binding and GTPgammaS autoradiographic analysis of preproorphanin precursor peptide products at the ORL1 and opioid receptors. J Chem Neuroanat. 2003 Jul;25(4):233-47. [Article]
- Spetea M, Toth F, Schutz J, Otvos F, Toth G, Benyhe S, Borsodi A, Schmidhammer H: Binding characteristics of [3H]14-methoxymetopon, a high affinity mu-opioid receptor agonist. Eur J Neurosci. 2003 Jul;18(2):290-5. [Article]
- Marek GJ: Behavioral evidence for mu-opioid and 5-HT2A receptor interactions. Eur J Pharmacol. 2003 Aug 1;474(1):77-83. [Article]
- Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
- Helm S, Trescot AM, Colson J, Sehgal N, Silverman S: Opioid antagonists, partial agonists, and agonists/antagonists: the role of office-based detoxification. Pain Physician. 2008 Mar-Apr;11(2):225-35. [Article]
- Goodman AJ, Le Bourdonnec B, Dolle RE: Mu opioid receptor antagonists: recent developments. ChemMedChem. 2007 Nov;2(11):1552-70. [Article]
- van Dorp E, Yassen A, Dahan A: Naloxone treatment in opioid addiction: the risks and benefits. Expert Opin Drug Saf. 2007 Mar;6(2):125-32. [Article]
- Nazzaro C, Rizzi A, Salvadori S, Guerrini R, Regoli D, Zeilhofer HU, Calo G: UFP-101 antagonizes the spinal antinociceptive effects of nociceptin/orphanin FQ: behavioral and electrophysiological studies in mice. Peptides. 2007 Mar;28(3):663-9. doi: 10.1016/j.peptides.2006.11.004. Epub 2006 Dec 11. [Article]
- Economidou D, Fedeli A, Fardon RM, Weiss F, Massi M, Ciccocioppo R: Effect of novel nociceptin/orphanin FQ-NOP receptor ligands on ethanol drinking in alcohol-preferring msP rats. Peptides. 2006 Dec;27(12):3299-306. doi: 10.1016/j.peptides.2006.09.007. [Article]
- FDA Approved Drug Products: Zubsolv (Buprenorphine, Naloxone) Sublingual Tablet [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Antagonist
- General Function
- Opioid receptor activity
- Specific Function
- G-protein coupled receptor that functions as receptor for endogenous enkephalins and for a subset of other opioids. Ligand binding causes a conformation change that triggers signaling via guanine n...
- Gene Name
- OPRD1
- Uniprot ID
- P41143
- Uniprot Name
- Delta-type opioid receptor
- Molecular Weight
- 40368.235 Da
References
- Moncada A, Cendan CM, Baeyens JM, Del Pozo E: Effects of serine/threonine protein phosphatase inhibitors on morphine-induced antinociception in the tail flick test in mice. Eur J Pharmacol. 2003 Mar 28;465(1-2):53-60. [Article]
- Kakinohana M, Marsala M, Carter C, Davison JK, Yaksh TL: Neuraxial morphine may trigger transient motor dysfunction after a noninjurious interval of spinal cord ischemia: a clinical and experimental study. Anesthesiology. 2003 Apr;98(4):862-70. [Article]
- Breljak D, Boranic M, Horvat S: Oligopeptide fragments of the enkephalin molecule interfere with hematopoietic cell colony formation. Int J Immunopathol Pharmacol. 2000 Jan-Apr;13(1):13-19. [Article]
- Chudapongse N, Kim SY, Kramer RE, Ho IK: Nonspecific effects of the selective kappa-opioid receptor agonist U-50,488H on dopamine uptake and release in PC12 cells. J Pharmacol Sci. 2003 Nov;93(3):372-5. [Article]
- Osman AM, Gomma M, Saad AH: A possible role for an enkephalinergic system in the internal defense mechanism of Biomphalaria alexandrina exposed to Schistosoma mansoni. J Egypt Soc Parasitol. 2003 Dec;33(3):841-61. [Article]
- Helm S, Trescot AM, Colson J, Sehgal N, Silverman S: Opioid antagonists, partial agonists, and agonists/antagonists: the role of office-based detoxification. Pain Physician. 2008 Mar-Apr;11(2):225-35. [Article]
- van Dorp E, Yassen A, Dahan A: Naloxone treatment in opioid addiction: the risks and benefits. Expert Opin Drug Saf. 2007 Mar;6(2):125-32. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Antagonist
- General Function
- Opioid receptor activity
- Specific Function
- G-protein coupled opioid receptor that functions as receptor for endogenous alpha-neoendorphins and dynorphins, but has low affinity for beta-endorphins. Also functions as receptor for various synt...
- Gene Name
- OPRK1
- Uniprot ID
- P41145
- Uniprot Name
- Kappa-type opioid receptor
- Molecular Weight
- 42644.665 Da
References
- Peng X, Neumeyer JL: Kappa receptor bivalent ligands. Curr Top Med Chem. 2007;7(4):363-73. [Article]
- van Dorp E, Yassen A, Dahan A: Naloxone treatment in opioid addiction: the risks and benefits. Expert Opin Drug Saf. 2007 Mar;6(2):125-32. [Article]
- Helm S, Trescot AM, Colson J, Sehgal N, Silverman S: Opioid antagonists, partial agonists, and agonists/antagonists: the role of office-based detoxification. Pain Physician. 2008 Mar-Apr;11(2):225-35. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Other/unknown
- General Function
- Transcriptional activator activity, rna polymerase ii transcription factor binding
- Specific Function
- Phosphorylation-dependent transcription factor that stimulates transcription upon binding to the DNA cAMP response element (CRE), a sequence present in many viral and cellular promoters. Transcript...
- Gene Name
- CREB1
- Uniprot ID
- P16220
- Uniprot Name
- Cyclic AMP-responsive element-binding protein 1
- Molecular Weight
- 36687.86 Da
References
- Li J, Li YH, Yuan XR: Changes of phosphorylation of cAMP response element binding protein in rat nucleus accumbens after chronic ethanol intake: naloxone reversal. Acta Pharmacol Sin. 2003 Sep;24(9):930-6. [Article]
- Chartoff EH, Papadopoulou M, Konradi C, Carlezon WA Jr: Dopamine-dependent increases in phosphorylation of cAMP response element binding protein (CREB) during precipitated morphine withdrawal in primary cultures of rat striatum. J Neurochem. 2003 Oct;87(1):107-18. [Article]
- Gao C, Chen LW, Tao YM, Chen J, Xu XJ, Chi ZQ: Effects of ohmefentanyl stereoisomers on phosphorylation of cAMP- response element binding protein in cultured rat hippocampal neurons. Acta Pharmacol Sin. 2003 Dec;24(12):1253-8. [Article]
- Walters CL, Cleck JN, Kuo YC, Blendy JA: Mu-opioid receptor and CREB activation are required for nicotine reward. Neuron. 2005 Jun 16;46(6):933-43. [Article]
- Hawes JJ, Narasimhaiah R, Picciotto MR: Galanin attenuates cyclic AMP regulatory element-binding protein (CREB) phosphorylation induced by chronic morphine and naloxone challenge in Cath.a cells and primary striatal cultures. J Neurochem. 2006 Feb;96(4):1160-8. Epub 2006 Jan 17. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- AntagonistOther/unknown
- General Function
- Zinc ion binding
- Specific Function
- Nuclear hormone receptor. The steroid hormones and their receptors are involved in the regulation of eukaryotic gene expression and affect cellular proliferation and differentiation in target tissu...
- Gene Name
- ESR1
- Uniprot ID
- P03372
- Uniprot Name
- Estrogen receptor
- Molecular Weight
- 66215.45 Da
References
- Farooqui M, Geng ZH, Stephenson EJ, Zaveri N, Yee D, Gupta K: Naloxone acts as an antagonist of estrogen receptor activity in MCF-7 cells. Mol Cancer Ther. 2006 Mar;5(3):611-20. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Transmembrane signaling receptor activity
- Specific Function
- Cooperates with LY96 and CD14 to mediate the innate immune response to bacterial lipopolysaccharide (LPS). Acts via MYD88, TIRAP and TRAF6, leading to NF-kappa-B activation, cytokine secretion and ...
- Gene Name
- TLR4
- Uniprot ID
- O00206
- Uniprot Name
- Toll-like receptor 4
- Molecular Weight
- 95679.19 Da
References
- Lewis SS, Loram LC, Hutchinson MR, Li CM, Zhang Y, Maier SF, Huang Y, Rice KC, Watkins LR: (+)-naloxone, an opioid-inactive toll-like receptor 4 signaling inhibitor, reverses multiple models of chronic neuropathic pain in rats. J Pain. 2012 May;13(5):498-506. doi: 10.1016/j.jpain.2012.02.005. Epub 2012 Apr 20. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Binder
- General Function
- Triglyceride lipase activity
- Specific Function
- Involved in the detoxification of xenobiotics and in the activation of ester and amide prodrugs. Hydrolyzes aromatic and aliphatic esters, but has no catalytic activity toward amides or a fatty acy...
- Gene Name
- CES1
- Uniprot ID
- P23141
- Uniprot Name
- Liver carboxylesterase 1
- Molecular Weight
- 62520.62 Da
References
- Bencharit S, Morton CL, Xue Y, Potter PM, Redinbo MR: Structural basis of heroin and cocaine metabolism by a promiscuous human drug-processing enzyme. Nat Struct Biol. 2003 May;10(5):349-56. [Article]
Enzymes
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- SubstrateInhibitor
- General Function
- Vitamin d3 25-hydroxylase activity
- Specific Function
- Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
- Gene Name
- CYP3A4
- Uniprot ID
- P08684
- Uniprot Name
- Cytochrome P450 3A4
- Molecular Weight
- 57342.67 Da
References
- Fang WB, Chang Y, McCance-Katz EF, Moody DE: Determination of naloxone and nornaloxone (noroxymorphone) by high-performance liquid chromatography-electrospray ionization- tandem mass spectrometry. J Anal Toxicol. 2009 Oct;33(8):409-17. doi: 10.1093/jat/33.8.409. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Substrate
- General Function
- Steroid binding
- Specific Function
- UDPGT is of major importance in the conjugation and subsequent elimination of potentially toxic xenobiotics and endogenous compounds. This isoform glucuronidates bilirubin IX-alpha to form both the...
- Gene Name
- UGT1A1
- Uniprot ID
- P22309
- Uniprot Name
- UDP-glucuronosyltransferase 1-1
- Molecular Weight
- 59590.91 Da
References
- Williams JA, Hyland R, Jones BC, Smith DA, Hurst S, Goosen TC, Peterkin V, Koup JR, Ball SE: Drug-drug interactions for UDP-glucuronosyltransferase substrates: a pharmacokinetic explanation for typically observed low exposure (AUCi/AUC) ratios. Drug Metab Dispos. 2004 Nov;32(11):1201-8. doi: 10.1124/dmd.104.000794. Epub 2004 Aug 10. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Steroid hydroxylase activity
- Specific Function
- Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
- Gene Name
- CYP2C18
- Uniprot ID
- P33260
- Uniprot Name
- Cytochrome P450 2C18
- Molecular Weight
- 55710.075 Da
References
- Fang WB, Chang Y, McCance-Katz EF, Moody DE: Determination of naloxone and nornaloxone (noroxymorphone) by high-performance liquid chromatography-electrospray ionization- tandem mass spectrometry. J Anal Toxicol. 2009 Oct;33(8):409-17. doi: 10.1093/jat/33.8.409. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Steroid hydroxylase activity
- Specific Function
- Responsible for the metabolism of a number of therapeutic agents such as the anticonvulsant drug S-mephenytoin, omeprazole, proguanil, certain barbiturates, diazepam, propranolol, citalopram and im...
- Gene Name
- CYP2C19
- Uniprot ID
- P33261
- Uniprot Name
- Cytochrome P450 2C19
- Molecular Weight
- 55930.545 Da
References
- Fang WB, Chang Y, McCance-Katz EF, Moody DE: Determination of naloxone and nornaloxone (noroxymorphone) by high-performance liquid chromatography-electrospray ionization- tandem mass spectrometry. J Anal Toxicol. 2009 Oct;33(8):409-17. doi: 10.1093/jat/33.8.409. [Article]
Carriers
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Binder
- General Function
- Toxic substance binding
- Specific Function
- Serum albumin, the main protein of plasma, has a good binding capacity for water, Ca(2+), Na(+), K(+), fatty acids, hormones, bilirubin and drugs. Its main function is the regulation of the colloid...
- Gene Name
- ALB
- Uniprot ID
- P02768
- Uniprot Name
- Serum albumin
- Molecular Weight
- 69365.94 Da
References
Transporters
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Sodium-independent organic anion transmembrane transporter activity
- Specific Function
- Mediates the Na(+)-independent transport of organic anions such as sulfobromophthalein (BSP) and conjugated (taurocholate) and unconjugated (cholate) bile acids (By similarity). Selectively inhibit...
- Gene Name
- SLCO1A2
- Uniprot ID
- P46721
- Uniprot Name
- Solute carrier organic anion transporter family member 1A2
- Molecular Weight
- 74144.105 Da
References
- Gao B, Hagenbuch B, Kullak-Ublick GA, Benke D, Aguzzi A, Meier PJ: Organic anion-transporting polypeptides mediate transport of opioid peptides across blood-brain barrier. J Pharmacol Exp Ther. 2000 Jul;294(1):73-9. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Xenobiotic-transporting atpase activity
- Specific Function
- Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
- Gene Name
- ABCB1
- Uniprot ID
- P08183
- Uniprot Name
- Multidrug resistance protein 1
- Molecular Weight
- 141477.255 Da
References
- Mahar Doan KM, Humphreys JE, Webster LO, Wring SA, Shampine LJ, Serabjit-Singh CJ, Adkison KK, Polli JW: Passive permeability and P-glycoprotein-mediated efflux differentiate central nervous system (CNS) and non-CNS marketed drugs. J Pharmacol Exp Ther. 2002 Dec;303(3):1029-37. [Article]
Drug created at June 13, 2005 13:24 / Updated at February 20, 2024 23:55