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Drug

D0087 | Naltrexone

Molecular Formula C20H23NO4
Molecular Weight 341.4
Structure
State solid
Clearance * ~ 3.5 L/min [after IV administration]
Volume of distribution * 1350 L [intravenous administration]
Route of elimination Both parent drug and metabolites are excreted primarily by the kidney (53% to 79% of the dose), however, urinary excretion of unchanged naltrexone accounts for less than 2% of an oral dose and fecal excretion is a minor elimination pathway. The renal clearance for naltrexone ranges from 30 to 127 mL/min and suggests that renal elimination is primarily by glomerular filtration.
Protein binding 21% bound to plasma proteins over the therapeutic dose range.
Half life 4 hours for naltrexone and 13 hours for the active metabolite 6 beta-naltrexol.
Absorption Although well absorbed orally, naltrexone is subject to significant first pass metabolism with oral bioavailability estimates ranging from 5 to 40%.

N

A

N07BB04 Naltrexone


[N07BB] Drugs used in alcohol dependence


[N07B] DRUGS USED IN ADDICTIVE DISORDERS


[N07] OTHER NERVOUS SYSTEM DRUGS


[N] Nervous system

N02AA56 Oxycodone and naltrexone


[N02AA] Natural opium alkaloids


[N02A] OPIOIDS


[N02] ANALGESICS


[N] Nervous system

A08AA62 Bupropion and naltrexone


[A08AA] Centrally acting antiobesity products


[A08A] ANTIOBESITY PREPARATIONS, EXCL. DIET PRODUCTS


[A08] ANTIOBESITY PREPARATIONS, EXCL. DIET PRODUCTS


[A] Alimentary tract and metabolism

Pictogram Signal Statements Precautionary Statement Codes
Danger

Aggregated GHS information provided by 73 companies from 9 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.


H302 (47.95%): Harmful if swallowed [Warning Acute toxicity, oral]


H312 (23.29%): Harmful in contact with skin [Warning Acute toxicity, dermal]


H317 (35.62%): May cause an allergic skin reaction [Warning Sensitization, Skin]


H332 (26.03%): Harmful if inhaled [Warning Acute toxicity, inhalation]


H334 (23.29%): May cause allergy or asthma symptoms or breathing difficulties if inhaled [Danger Sensitization, respiratory]


H341 (12.33%): Suspected of causing genetic defects [Warning Germ cell mutagenicity]


H400 (52.05%): Very toxic to aquatic life [Warning Hazardous to the aquatic environment, acute hazard]


Information may vary between notifications depending on impurities, additives, and other factors. The percentage value in parenthesis indicates the notified classification ratio from companies that provide hazard codes. Only hazard codes with percentage values above 10% are shown.


 P201, P202, P261, P264, P270, P271, P272, P273, P280, P281, P285, P301+P312, P302+P352, P304+P312, P304+P340, P304+P341, P308+P313, P312, P321, P322, P330, P333+P313, P342+P311, P363, P391, P405, and P501; (The corresponding statement to each P-code can be found at the GHS Classification page.)
Warning

H302: Harmful if swallowed [Warning Acute toxicity, oral]


 P264, P270, P301+P312, P330, and P501; (The corresponding statement to each P-code can be found at the GHS Classification page.)

  • Alcohol abuse

  • Alcoholism

  • Drug dependence

  • Anxiety (0.02)

  • Vomiting (0.03)

  • Headache

  • Nausea

    • (-)-Naltrexone (-)naltrexone (1S,5R,13R,17S)-4-(cyclopropylmethyl)-10,17-dihydroxy-12-oxa-4-azapentacyclo[9.6.1.0^{1,13}.0^{5,17}.0^{7,18}]octadeca-7(18),8,10-trien-14-one
    (1S,5R,13R,17S)-4-(cyclopropylmethyl)-10,17-dihydroxy-12-oxa-4-azapentacyclo[9.6.1.0^{1,13}.0^{5,17}.0^{7,18}]octadeca-7,9,11(18)-trien-14-one (4R,4aS,7aR,12bS)-3-(cyclopropylmethyl)-4a,9-bis(oxidanyl)-2,4,5,6,7a,13-hexahydro-1H-4,12-methanobenzofuro[3,2-e]isoquinoline-7-one;hydrochloride (4R,4aS,7aR,12bS)-3-(cyclopropylmethyl)-4a,9-dihydroxy-2,4,5,6,7a,13-hexahydro-1H-4,12-methanobenzofuro[3,2-e]isoquinoline-7-one
    (4R,4aS,7aR,12bS)-3-(cyclopropylmethyl)-4a,9-dihydroxy-2,4,5,6,7a,13-hexahydro-1H-4,12-methanobenzofuro[3,2-e]isoquinoline-7-one;hydrochloride (5alpha)-17-(Cyclopropylmethyl)-3,14-dihydroxy-4,5-epoxymorphinan-6-one 16590-41-3
    17-(Cyclopropylmethyl)-4,5-epoxy-3,14-dihydroxmorphinan-6-one, (5.alpha.)- 17-(Cyclopropylmethyl)-4,5-epoxy-3,14-dihydroxymorphinan-6-one 17-(Cyclopropylmethyl)-4,5alpha-epoxy-3,14-dihydroxymorphinan-6-one
    3,14-dihydroxy-17-(cyclopropylmethyl)-4,5alpha-epoxymorphinan-6-one 4-(cyclopropylmethyl)-10,17-dihydroxy-12-oxa-4-azapentacyclo[9.6.1.0~1,13~.0~5,17~.0~7,18~]octadeca-7(18),8,10-trien-14-one 5S6W795CQM
    88088-EP2270005A1 88088-EP2275420A1 88088-EP2298761A1
    88088-EP2298776A1 88088-EP2305648A1 AB00174152-14
    AB00174152_17 AKOS015994596 AR-270/43507956
    BCP07022 BDBM50000787 BDBM60212
    BIDD:GT0405 BPBio1_000146 BRD-K88172511-003-21-1
    BRD-K88172511-310-03-8 BRN 3596648 BSPBio_000132
    C07253 CAS-16590-41-3 CCRIS 3506
    CHEBI:7465 CHEMBL19019 CS-0880
    Celupan D05113 DB00704
    DQCKKXVULJGBQN-XFWGSAIBSA-N DSSTox_CID_26313 DSSTox_GSID_46313
    DSSTox_RID_81532 DTXSID4046313 EINECS 240-649-9
    EN-1639A [AS HYDROCHLORIDE] FT-0696752 GTPL1639
    HMS2089O11 HS-0002 HSDB 6750
    HY-76711 LS-92094 MCULE-7032963403
    Morphinan-6-one, 17-(cyclopropylmethyl)-4,5-alpha-epoxy-3,14-dihydroxy- Morphinan-6-one, 17-(cyclopropylmethyl)-4,5-epoxy-3,14-dihydroxy-, (5alpha)- N-Cyclopropylmethyl-14-hydroxydihydromorphinone
    N-Cyclopropylmethylnoroxymorphone NCGC00024427-03 NCGC00024427-04
    NCGC00024427-05 NCGC00162274-02 Naltrexon
    Naltrexona Naltrexona [INN-Spanish] Naltrexone (USAN/INN)
    Naltrexone [USAN:INN:BAN] Naltrexone base anhydrous Naltrexone solution, 1.0 mg/mL in methanol, ampule of 1 mL, certified reference material
    Naltrexonum Naltrexonum [INN-Latin] Nemexin
    PDSP2_000847 PTI-555 Prestwick0_000116
    Prestwick1_000116 Prestwick2_000116 Prestwick3_000116
    PubChem24168 Q409587 ReVia
    SC-94535 SCHEMBL34681 SMP1_000206
    SPBio_002071 Tox21_112007 Tox21_112007_1
    UM-792 UNII-5S6W795CQM US9107954, naltrexone
    Vivitrex Vivitrol Vivitrol (TN)
    W-5099 ZINC1773 cid_5485201
    cyclopropylmethyl(dihydroxy)[?]one naltrexone naltrexone (ReVia)

    DrugBank Name Naltrexone
    DrugBank DB00704
    CAS Number 16590-41-3, 16676-29-2
    PubChem Compound 5360515
    KEGG Compound ID C07253
    KEGG Drug D05113
    PubChem.Substance 46505333
    ChEBI 7465
    PharmGKB PA450588
    ChemSpider 4514524
    BindingDB 50000787.0
    TTD DAP000379
    Wikipedia Naltrexone
    DPD 20300

    1. Dykens et al. (2007)