Peringatan Keamanan

LD50=~900 mg/kg (Orally in rats); LD50=90 mg/kg (Orally in women); Signs of overdose include motor unrest, muscular twitching and rigidity, tremor, ataxia, convulsions, hyperpyrexia, vertigo, mydriasis, vomiting, cyanosis, hypotension, shock, tachycardia, cardiac arrhythmias, impaired cardiac conduction, respiratory depression, and disturbances of consciousness up to deep coma.

Maprotiline

DB00934

small molecule approved investigational

Deskripsi

Maprotiline is a tetracyclic antidepressant with similar pharmacological properties to tricyclic antidepressants (TCAs). Similar to TCAs, maprotiline inhibits neuronal norepinephrine reuptake, possesses some anticholinergic activity, and does not affect monoamine oxidase activity. It differs from TCAs in that it does not appear to block serotonin reuptake. Maprotiline may be used to treat depressive affective disorders, including dysthymic disorder (depressive neurosis) and major depressive disorder. Maprotiline is effective at reducing symptoms of anxiety associated with depression.

Struktur Molekul 2D

Berat 277.4033
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) Average ~ 51 hours (range: 27-58 hours)
Volume Distribusi Maprotiline and its metabolites may be detected in the lungs, liver, brain, and kidneys; lower concentrations may be found in the adrenal glands, heart and muscle. Maprotiline is readily distributed into breast milk to similar concentrations as those in maternal blood.
Klirens (Clearance) -

Absorpsi

Slowly, but completely absorbed from the GI tract following oral administration.

Metabolisme

Hepatic. Maprotiline is metabolized by N-demethylation, deamination, aliphatic and aromatic hydroxylations and by formation of aromatic methoxy derivatives. It is slowly metabolized primarily to desmethylmaprotiline, a pharmacologically active metabolite. Desmethylmaprotiline may undergo further metabolism to maprotiline-N-oxide.

Rute Eliminasi

Approximately 60% of a single orally administered dose is excreted in urine as conjugated metabolites within 21 days; 30% is eliminated in feces.

Interaksi Makanan

2 Data
  • 1. Limit caffeine intake.
  • 2. Take with or without food.

Interaksi Obat

1987 Data
Deferasirox The serum concentration of Maprotiline can be increased when it is combined with Deferasirox.
Peginterferon alfa-2b The serum concentration of Maprotiline can be increased when it is combined with Peginterferon alfa-2b.
Leflunomide The serum concentration of Maprotiline can be decreased when it is combined with Leflunomide.
Teriflunomide The serum concentration of Maprotiline can be decreased when it is combined with Teriflunomide.
Buprenorphine Maprotiline may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
Doxylamine Doxylamine may increase the central nervous system depressant (CNS depressant) activities of Maprotiline.
Dronabinol Dronabinol may increase the central nervous system depressant (CNS depressant) activities of Maprotiline.
Droperidol Droperidol may increase the central nervous system depressant (CNS depressant) activities of Maprotiline.
Hydrocodone Maprotiline may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Magnesium sulfate The therapeutic efficacy of Maprotiline can be increased when used in combination with Magnesium sulfate.
Methotrimeprazine Maprotiline may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
Metyrosine Maprotiline may increase the sedative activities of Metyrosine.
Minocycline Minocycline may increase the central nervous system depressant (CNS depressant) activities of Maprotiline.
Nabilone Nabilone may increase the central nervous system depressant (CNS depressant) activities of Maprotiline.
Orphenadrine Maprotiline may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
Paraldehyde Maprotiline may increase the central nervous system depressant (CNS depressant) activities of Paraldehyde.
Perampanel Perampanel may increase the central nervous system depressant (CNS depressant) activities of Maprotiline.
Pramipexole Maprotiline may increase the sedative activities of Pramipexole.
Ropinirole Maprotiline may increase the sedative activities of Ropinirole.
Rotigotine Maprotiline may increase the sedative activities of Rotigotine.
Rufinamide The risk or severity of adverse effects can be increased when Rufinamide is combined with Maprotiline.
Sodium oxybate Maprotiline may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Suvorexant Maprotiline may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
Tapentadol Tapentadol may increase the central nervous system depressant (CNS depressant) activities of Maprotiline.
Thalidomide Maprotiline may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
Zolpidem Maprotiline may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
Aclidinium The risk or severity of adverse effects can be increased when Maprotiline is combined with Aclidinium.
Mianserin Mianserin may increase the anticholinergic activities of Maprotiline.
Mirabegron The risk or severity of urinary retention can be increased when Maprotiline is combined with Mirabegron.
Potassium chloride The risk or severity of gastrointestinal ulceration can be increased when Maprotiline is combined with Potassium chloride.
Pramlintide The risk or severity of reduced gastrointestinal motility can be increased when Pramlintide is combined with Maprotiline.
Secretin porcine The therapeutic efficacy of Secretin porcine can be decreased when used in combination with Maprotiline.
Tiotropium The risk or severity of adverse effects can be increased when Maprotiline is combined with Tiotropium.
Topiramate The risk or severity of hyperthermia and oligohydrosis can be increased when Maprotiline is combined with Topiramate.
Umeclidinium The risk or severity of adverse effects can be increased when Maprotiline is combined with Umeclidinium.
Benzylpenicilloyl polylysine Maprotiline may decrease effectiveness of Benzylpenicilloyl polylysine as a diagnostic agent.
Betahistine The therapeutic efficacy of Betahistine can be decreased when used in combination with Maprotiline.
Hyaluronidase (ovine) The therapeutic efficacy of Hyaluronidase (ovine) can be decreased when used in combination with Maprotiline.
Hyaluronidase (human recombinant) The therapeutic efficacy of Hyaluronidase (human recombinant) can be decreased when used in combination with Maprotiline.
Hyaluronidase The therapeutic efficacy of Hyaluronidase can be decreased when used in combination with Maprotiline.
Methadone The risk or severity of adverse effects can be increased when Methadone is combined with Maprotiline.
Glycopyrronium The risk or severity of adverse effects can be increased when Maprotiline is combined with Glycopyrronium.
Rasagiline The risk or severity of adverse effects can be increased when Rasagiline is combined with Maprotiline.
Pargyline The risk or severity of adverse effects can be increased when Pargyline is combined with Maprotiline.
Hydracarbazine The risk or severity of adverse effects can be increased when Hydracarbazine is combined with Maprotiline.
Benmoxin The risk or severity of adverse effects can be increased when Benmoxin is combined with Maprotiline.
Mebanazine The risk or severity of adverse effects can be increased when Mebanazine is combined with Maprotiline.
Octamoxin The risk or severity of adverse effects can be increased when Octamoxin is combined with Maprotiline.
Pheniprazine The risk or severity of adverse effects can be increased when Pheniprazine is combined with Maprotiline.
Phenoxypropazine The risk or severity of adverse effects can be increased when Phenoxypropazine is combined with Maprotiline.
Pivhydrazine The risk or severity of adverse effects can be increased when Pivhydrazine is combined with Maprotiline.
Safrazine The risk or severity of adverse effects can be increased when Safrazine is combined with Maprotiline.
Caroxazone The risk or severity of adverse effects can be increased when Caroxazone is combined with Maprotiline.
Furazolidone The risk or severity of adverse effects can be increased when Furazolidone is combined with Maprotiline.
7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline The risk or severity of adverse effects can be increased when 7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline is combined with Maprotiline.
Harmaline The risk or severity of adverse effects can be increased when Harmaline is combined with Maprotiline.
Brofaromine The risk or severity of adverse effects can be increased when Brofaromine is combined with Maprotiline.
Procarbazine The risk or severity of adverse effects can be increased when Procarbazine is combined with Maprotiline.
Safinamide The risk or severity of adverse effects can be increased when Safinamide is combined with Maprotiline.
Procaine The risk or severity of adverse effects can be increased when Procaine is combined with Maprotiline.
Phenelzine The risk or severity of adverse effects can be increased when Phenelzine is combined with Maprotiline.
Minaprine The risk or severity of adverse effects can be increased when Minaprine is combined with Maprotiline.
Selegiline The risk or severity of adverse effects can be increased when Selegiline is combined with Maprotiline.
Moclobemide The risk or severity of adverse effects can be increased when Moclobemide is combined with Maprotiline.
Isocarboxazid The risk or severity of adverse effects can be increased when Isocarboxazid is combined with Maprotiline.
Clorgiline The risk or severity of adverse effects can be increased when Clorgiline is combined with Maprotiline.
Iproniazid The risk or severity of adverse effects can be increased when Iproniazid is combined with Maprotiline.
Nialamide The risk or severity of adverse effects can be increased when Nialamide is combined with Maprotiline.
Pirlindole The risk or severity of adverse effects can be increased when Pirlindole is combined with Maprotiline.
Toloxatone The risk or severity of adverse effects can be increased when Toloxatone is combined with Maprotiline.
Linezolid The risk or severity of serotonin syndrome can be increased when Linezolid is combined with Maprotiline.
Dicoumarol The risk or severity of adverse effects can be increased when Maprotiline is combined with Dicoumarol.
Phenindione The risk or severity of adverse effects can be increased when Maprotiline is combined with Phenindione.
Phenprocoumon The risk or severity of adverse effects can be increased when Maprotiline is combined with Phenprocoumon.
4-hydroxycoumarin The risk or severity of adverse effects can be increased when Maprotiline is combined with 4-hydroxycoumarin.
Coumarin The risk or severity of adverse effects can be increased when Maprotiline is combined with Coumarin.
Ethyl biscoumacetate The risk or severity of adverse effects can be increased when Maprotiline is combined with Ethyl biscoumacetate.
Fluindione The risk or severity of adverse effects can be increased when Maprotiline is combined with Fluindione.
Clorindione The risk or severity of adverse effects can be increased when Maprotiline is combined with Clorindione.
Diphenadione The risk or severity of adverse effects can be increased when Maprotiline is combined with Diphenadione.
Tioclomarol The risk or severity of adverse effects can be increased when Maprotiline is combined with Tioclomarol.
(S)-Warfarin The risk or severity of adverse effects can be increased when Maprotiline is combined with (S)-Warfarin.
Tedizolid phosphate The risk or severity of serotonin syndrome can be increased when Tedizolid phosphate is combined with Maprotiline.
Abiraterone The serum concentration of Maprotiline can be increased when it is combined with Abiraterone.
Botulinum toxin type A The risk or severity of adverse effects can be increased when Maprotiline is combined with Botulinum toxin type A.
Glucagon Maprotiline may increase the gastrointestinal motility reducing activities of Glucagon.
Sulpiride Maprotiline may increase the anticholinergic activities of Sulpiride.
Botulinum toxin type B The risk or severity of adverse effects can be increased when Maprotiline is combined with Botulinum toxin type B.
Mirtazapine Maprotiline may increase the serotonergic activities of Mirtazapine.
Eluxadoline The risk or severity of constipation can be increased when Maprotiline is combined with Eluxadoline.
Ramosetron The risk or severity of constipation can be increased when Maprotiline is combined with Ramosetron.
Cyproterone acetate The metabolism of Maprotiline can be increased when combined with Cyproterone acetate.
Ethanol Maprotiline may increase the central nervous system depressant (CNS depressant) activities of Ethanol.
Azelastine Maprotiline may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
Brimonidine Brimonidine may increase the central nervous system depressant (CNS depressant) activities of Maprotiline.
Zimelidine The risk or severity of adverse effects can be increased when Maprotiline is combined with Zimelidine.
Dapoxetine The risk or severity of adverse effects can be increased when Maprotiline is combined with Dapoxetine.
Seproxetine The risk or severity of adverse effects can be increased when Maprotiline is combined with Seproxetine.
Citalopram The risk or severity of QTc prolongation can be increased when Maprotiline is combined with Citalopram.
Sertraline The risk or severity of adverse effects can be increased when Maprotiline is combined with Sertraline.

Target Protein

Sodium-dependent noradrenaline transporter SLC6A2
Histamine H1 receptor HRH1
Muscarinic acetylcholine receptor M1 CHRM1
Muscarinic acetylcholine receptor M2 CHRM2
Muscarinic acetylcholine receptor M3 CHRM3
Muscarinic acetylcholine receptor M4 CHRM4
Muscarinic acetylcholine receptor M5 CHRM5
Alpha-1 adrenergic receptors ADRA1A
5-hydroxytryptamine receptor 2A HTR2A
5-hydroxytryptamine receptor 2C HTR2C
5-hydroxytryptamine receptor 7 HTR7
D(2) dopamine receptor DRD2
Alpha-2 adrenergic receptors ADRA2A

Referensi & Sumber

Belum ada data referensi/link/attachment untuk obat ini pada database. Jalankan import DrugBank untuk mengisi field referensi.

Contoh Produk & Brand

Produk: 18 • International brands: 2
Produk
  • Ludiomil
    Tablet • 25 mg/1 • Oral • US • Approved
  • Ludiomil
    Tablet • 50 mg/1 • Oral • US • Approved
  • Ludiomil
    Tablet • 75 mg/1 • Oral • US • Approved
  • Ludiomil Tab 10mg
    Tablet • 10 mg • Oral • Canada • Approved
  • Ludiomil Tab 25mg
    Tablet • 25 mg / tab • Oral • Canada • Approved
  • Ludiomil Tab 50mg
    Tablet • 50 mg / tab • Oral • Canada • Approved
  • Ludiomil Tab 75mg
    Tablet • 75 mg / tab • Oral • Canada • Approved
  • Maprotiline Hydrochloride
    Tablet, film coated • 25 mg/1 • Oral • US • Generic • Approved
Menampilkan 8 dari 18 produk.
International Brands
  • Deprilept
  • Psymion

Sekuens Gen/Protein (FASTA)

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