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Drug

D1293 | Amantadine

Molecular Formula C10H17N
Molecular Weight 151.25
Structure
State solid
Clearance * 0.2 - 0.3 L/hr/kg * 0.10 +/- 0.04 L/hr/kg [healthy, elderly male]
Volume of distribution * 3 to 8 L/kg [healthy subjects]
Route of elimination It is primarily excreted unchanged in the urine by glomerular filtration and tubular secretion.
Protein binding Approximately 67% bound to plasma proteins over a concentration range of 0.1 to 2.0 µg/mL.
Half life Mean half-lives ranged from 10 to 14 hours, however renal function impairment causes a severe increase in half life to 7 to 10 days.
Absorption Amantadine is well absorbed orally from the gastrointestinal tract.
Description Antiviral

N

N04BB01 Amantadine


[N04BB] Adamantane derivatives


[N04B] DOPAMINERGIC AGENTS


[N04] ANTI-PARKINSON DRUGS


[N] Nervous system

Toxicity Dose Time Species Model Method Action Positive criterion Reference
MEMBRANE POTENTIAL 261.2 µM 30 mins mouse liver mitochondria Rh123 fluorescence (excitation 485 nm, emission 535 nm) are recorded using a fluorescence multi-well plate reader (mCICCP (20 µM) treatments was considered as the 100% baseline for ΔΨm loss) decrease EC20 36
RESPIRATION > 400 µM 60 mins mouse liver mitochondria Oxygen consumption was monitored with 50nM MitoXpress ( an oxygen-sensitive phosphorescent dye) using a spectrofluorimeter (Tecan Infinite 200; λExcitation 380nm; λEmission 650nm). Rotenone (2µM) was used as 100% baseline for complex I inhibition. decrease EC20 36
RESPIRATION > 400 µM 60 mins mouse liver mitochondria Oxygen consumption was monitored with 50nM MitoXpress ( an oxygen-sensitive phosphorescent dye) using a spectrofluorimeter (Tecan Infinite 200; λExcitation 380nm; λEmission 650nm). Oligomycin A (1µM) was used as 100% baseline for complex II inhibition. decrease EC20 36
SWELLING > 800 µM 30 mins mouse liver mitochondria swelling assay: Absorbance at 545 nm using a fluorescence multi-well plate reader (CaCl2 (50 µM) was considered as the 100% baseline for the swelling ) increase EC20 36

Target Dose Time Species Model Method Action Positive criterion Reference
NADH:ubiquinone reductase > 400 µM 60 mins mouse liver mitochondria Oxygen consumption was monitored with 50nM MitoXpress ( an oxygen-sensitive phosphorescent dye) using a spectrofluorimeter (Tecan Infinite 200; λExcitation 380nm; λEmission 650nm). Rotenone (2µM) was used as 100% baseline for complex I inhibition. inhibit EC20 36
Succinate dehydrogenase > 400 µM 60 mins mouse liver mitochondria Oxygen consumption was monitored with 50nM MitoXpress ( an oxygen-sensitive phosphorescent dye) using a spectrofluorimeter (Tecan Infinite 200; λExcitation 380nm; λEmission 650nm). Oligomycin A (1µM) was used as 100% baseline for complex II inhibition. inhibit EC20 36
Cytochrome c > 400 µM 30 mins mouse liver mitochondria Cytochrome c release was evaluated using ELISA kit ( 20 µg/ml Alamethicin was used as 100% baseline) release EC20 36

Pictogram Signal Statements Precautionary Statement Codes
Warning

Aggregated GHS information provided by 133 companies from 7 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.


H226 (63.16%): Flammable liquid and vapor [Warning Flammable liquids]


H302 (100%): Harmful if swallowed [Warning Acute toxicity, oral]


H315 (36.09%): Causes skin irritation [Warning Skin corrosion/irritation]


H319 (36.09%): Causes serious eye irritation [Warning Serious eye damage/eye irritation]


H335 (35.34%): May cause respiratory irritation [Warning Specific target organ toxicity, single exposure


Respiratory tract irritation]


H412 (63.91%): Harmful to aquatic life with long lasting effects [Hazardous to the aquatic environment, long-term 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.


 P210, P233, P240, P241, P242, P243, P261, P264, P270, P271, P273, P280, P301+P312, P302+P352, P303+P361+P353, P304+P340, P305+P351+P338, P312, P321, P330, P332+P313, P337+P313, P362, P370+P378, P403+P233, P403+P235, P405, and P501; (The corresponding statement to each P-code can be found at the GHS Classification page.)
Warning

Aggregated GHS information provided by 4 companies from 3 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.


H302 (25%): Harmful if swallowed [Warning Acute toxicity, oral]


H315 (75%): Causes skin irritation [Warning Skin corrosion/irritation]


H319 (75%): Causes serious eye irritation [Warning Serious eye damage/eye irritation]


H335 (50%): May cause respiratory irritation [Warning Specific target organ toxicity, single exposure


Respiratory tract irritation]


H361 (75%): Suspected of damaging fertility or the unborn child [Warning Reproductive toxicity]


H412 (25%): Harmful to aquatic life with long lasting effects [Hazardous to the aquatic environment, long-term 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, P273, P280, P281, P301+P312, P302+P352, P304+P340, P305+P351+P338, P308+P313, P312, P321, P330, P332+P313, P337+P313, P362, P403+P233, P405, and P501; (The corresponding statement to each P-code can be found at the GHS Classification page.)


  • DrugBank DB00915
    CAS Number 102395-13-1, 281-23-2, 31377-23-8, 665-66-7, 768-94-5
    PubChem Compound 2130