Peringatan Keamanan

Toxic manifestations of amoxapine overdosage differ significantly from those of other tricyclic antidepressants. Serious cardiovascular effects are seldom if ever observed. However, CNS effects, particularly grand mal convulsions, occur frequently, and treatment should be directed primarily toward prevention or control of seizures. Status epilepticus may develop and constitutes a neurologic emergency. Coma and acidosis are other serious complications of substantial amoxapine overdosage in some cases. Renal failure may develop two to five days after toxic overdose in patients who may appear otherwise recovered. Acute tubular necrosis with rhabdomuolysis and myolobinurla is the most common renal complication in such cases. This reaction probably occurs in less than 5% of overdose cases, and typically in those who have experienced multiple seizures.

Amoxapine

DB00543

small molecule approved

Deskripsi

Amoxapine, the N-demethylated derivative of the antipsychotic agent loxapine, is a dibenzoxazepine-derivative tricyclic antidepressant (TCA). TCAs are structurally similar to phenothiazines. They contain a tricyclic ring system with an alkyl amine substituent on the central ring. In non-depressed individuals, amoxapine does not affect mood or arousal, but may cause sedation. In depressed individuals, amoxapine exerts a positive effect on mood. TCAs are potent inhibitors of serotonin and norepinephrine reuptake. In addition, TCAs down-regulate cerebral cortical β-adrenergic receptors and sensitize post-synaptic serotonergic receptors with chronic use. The antidepressant effects of TCAs are thought to be due to an overall increase in serotonergic neurotransmission. TCAs also block histamine H1 receptors, α1-adrenergic receptors and muscarinic receptors, which accounts for their sedative, hypotensive and anticholinergic effects (e.g. blurred vision, dry mouth, constipation, urinary retention), respectively. See toxicity section below for a complete listing of side effects. Amoxapine may be used to treat neurotic and reactive depressive disorders, endogenous and psychotic depression, and mixed symptoms of depression and anxiety or agitation.

Struktur Molekul 2D

Berat 313.781
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) 8 hours
Volume Distribusi Widely distributed in body tissues with highest concentrations found in lungs, spleen, kidneys, heart, and brain. Lower concentrations can be detected in testes and muscle.
Klirens (Clearance) -

Absorpsi

Rapidly and almost completely absorbed from the GI tract. Peak plasma concentrations occur within 1-2 hours of oral administration of a single dose.

Metabolisme

Amoxapine is almost completely metabolized in the liver to its major metabolite, 8-hydroxyamoxapine, and a minor metabolite, 7-hydroxyamoxapine. Both metabolites are phamacologically inactive and have half-lives of approximately 30 and 6.5 hours, respectively.

Rute Eliminasi

60-69% of a single orally administered dose of amoxapine is excreted in urine, principally as conjugated metabolites. 7-18% of the dose is excrete feces mainly as unconjugated metabolites. Less than 5% of the dose is excreted as unchanged drug in urine.

Interaksi Makanan

2 Data
  • 1. Avoid alcohol.
  • 2. Take with food. Food reduces irritation.

Interaksi Obat

1810 Data
Valsartan Amoxapine may decrease the antihypertensive activities of Valsartan.
Remikiren Amoxapine may decrease the antihypertensive activities of Remikiren.
Torasemide Amoxapine may decrease the antihypertensive activities of Torasemide.
Guanadrel Amoxapine may decrease the antihypertensive activities of Guanadrel.
Olmesartan Amoxapine may decrease the antihypertensive activities of Olmesartan.
Nitroprusside Amoxapine may decrease the antihypertensive activities of Nitroprusside.
Minoxidil Amoxapine may decrease the antihypertensive activities of Minoxidil.
Fosinopril Amoxapine may decrease the antihypertensive activities of Fosinopril.
Trandolapril Amoxapine may decrease the antihypertensive activities of Trandolapril.
Benazepril Amoxapine may decrease the antihypertensive activities of Benazepril.
Bosentan Amoxapine may decrease the antihypertensive activities of Bosentan.
Enalapril Amoxapine may decrease the antihypertensive activities of Enalapril.
Cyclothiazide Amoxapine may decrease the antihypertensive activities of Cyclothiazide.
Candoxatril Amoxapine may decrease the antihypertensive activities of Candoxatril.
Eplerenone Amoxapine may decrease the antihypertensive activities of Eplerenone.
Lisinopril Amoxapine may decrease the antihypertensive activities of Lisinopril.
Nitroglycerin Amoxapine may decrease the antihypertensive activities of Nitroglycerin.
Cryptenamine Amoxapine may decrease the antihypertensive activities of Cryptenamine.
Candesartan cilexetil Amoxapine may decrease the antihypertensive activities of Candesartan cilexetil.
Eprosartan Amoxapine may decrease the antihypertensive activities of Eprosartan.
Quinapril Amoxapine may decrease the antihypertensive activities of Quinapril.
Telmisartan Amoxapine may decrease the antihypertensive activities of Telmisartan.
Irbesartan Amoxapine may decrease the antihypertensive activities of Irbesartan.
Deserpidine Amoxapine may decrease the antihypertensive activities of Deserpidine.
Diazoxide Amoxapine may decrease the antihypertensive activities of Diazoxide.
Guanethidine Amoxapine may decrease the antihypertensive activities of Guanethidine.
Epoprostenol Amoxapine may decrease the antihypertensive activities of Epoprostenol.
Hydralazine Amoxapine may decrease the antihypertensive activities of Hydralazine.
Cilazapril Amoxapine may decrease the antihypertensive activities of Cilazapril.
Saprisartan Amoxapine may decrease the antihypertensive activities of Saprisartan.
Spirapril Amoxapine may decrease the antihypertensive activities of Spirapril.
Tienilic acid Amoxapine may decrease the antihypertensive activities of Tienilic acid.
Sitaxentan Amoxapine may decrease the antihypertensive activities of Sitaxentan.
Diethylnorspermine Amoxapine may decrease the antihypertensive activities of Diethylnorspermine.
Pinacidil Amoxapine may decrease the antihypertensive activities of Pinacidil.
Temocapril Amoxapine may decrease the antihypertensive activities of Temocapril.
Riociguat Amoxapine may decrease the antihypertensive activities of Riociguat.
Macitentan Amoxapine may decrease the antihypertensive activities of Macitentan.
Aliskiren Amoxapine may decrease the antihypertensive activities of Aliskiren.
Rauwolfia serpentina root Amoxapine may decrease the antihypertensive activities of Rauwolfia serpentina root.
Enalaprilat Amoxapine may decrease the antihypertensive activities of Enalaprilat.
Angiotensin 1-7 Amoxapine may decrease the antihypertensive activities of Angiotensin 1-7.
Imidapril Amoxapine may decrease the antihypertensive activities of Imidapril.
BQ-123 Amoxapine may decrease the antihypertensive activities of BQ-123.
Dihydralazine Amoxapine may decrease the antihypertensive activities of Dihydralazine.
Zofenopril Amoxapine may decrease the antihypertensive activities of Zofenopril.
Guanoxan Amoxapine may decrease the antihypertensive activities of Guanoxan.
Delapril Amoxapine may decrease the antihypertensive activities of Delapril.
Vincamine Amoxapine may decrease the antihypertensive activities of Vincamine.
Linsidomine Amoxapine may decrease the antihypertensive activities of Linsidomine.
Guanoxabenz Amoxapine may decrease the antihypertensive activities of Guanoxabenz.
Tolonidine Amoxapine may decrease the antihypertensive activities of Tolonidine.
Endralazine Amoxapine may decrease the antihypertensive activities of Endralazine.
Cadralazine Amoxapine may decrease the antihypertensive activities of Cadralazine.
Bietaserpine Amoxapine may decrease the antihypertensive activities of Bietaserpine.
Guanazodine Amoxapine may decrease the antihypertensive activities of Guanazodine.
Methoserpidine Amoxapine may decrease the antihypertensive activities of Methoserpidine.
Guanoclor Amoxapine may decrease the antihypertensive activities of Guanoclor.
Muzolimine Amoxapine may decrease the antihypertensive activities of Muzolimine.
Xipamide Amoxapine may decrease the antihypertensive activities of Xipamide.
Candesartan Amoxapine may decrease the antihypertensive activities of Candesartan.
Tocopherylquinone Amoxapine may decrease the antihypertensive activities of Tocopherylquinone.
Benazeprilat Amoxapine may decrease the antihypertensive activities of Benazeprilat.
Fosinoprilat Amoxapine may decrease the antihypertensive activities of Fosinoprilat.
Ramiprilat Amoxapine may decrease the antihypertensive activities of Ramiprilat.
Perindoprilat Amoxapine may decrease the antihypertensive activities of Perindoprilat.
Quinaprilat Amoxapine may decrease the antihypertensive activities of Quinaprilat.
Furosemide Amoxapine may decrease the antihypertensive activities of Furosemide.
Captopril Amoxapine may decrease the antihypertensive activities of Captopril.
Ambrisentan Amoxapine may decrease the antihypertensive activities of Ambrisentan.
Selexipag Amoxapine may decrease the antihypertensive activities of Selexipag.
Ramipril Amoxapine may decrease the antihypertensive activities of Ramipril.
Perindopril Amoxapine may decrease the antihypertensive activities of Perindopril.
Levamlodipine Amoxapine may decrease the antihypertensive activities of Levamlodipine.
Buthiazide Amoxapine may decrease the antihypertensive activities of Buthiazide.
Azilsartan medoxomil Amoxapine may decrease the antihypertensive activities of Azilsartan medoxomil.
Buprenorphine Amoxapine 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 Amoxapine.
Dronabinol Dronabinol may increase the central nervous system depressant (CNS depressant) activities of Amoxapine.
Droperidol Droperidol may increase the central nervous system depressant (CNS depressant) activities of Amoxapine.
Hydrocodone Amoxapine may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Magnesium sulfate The therapeutic efficacy of Amoxapine can be increased when used in combination with Magnesium sulfate.
Methotrimeprazine Amoxapine may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
Minocycline Minocycline may increase the central nervous system depressant (CNS depressant) activities of Amoxapine.
Nabilone Nabilone may increase the central nervous system depressant (CNS depressant) activities of Amoxapine.
Orphenadrine Amoxapine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
Paraldehyde Amoxapine 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 Amoxapine.
Rotigotine Amoxapine may increase the sedative activities of Rotigotine.
Rufinamide The risk or severity of adverse effects can be increased when Rufinamide is combined with Amoxapine.
Sodium oxybate Amoxapine may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Suvorexant Amoxapine 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 Amoxapine.
Thalidomide Amoxapine may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
Zolpidem Amoxapine may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
Aclidinium The risk or severity of adverse effects can be increased when Amoxapine is combined with Aclidinium.
Mianserin Mianserin may increase the anticholinergic activities of Amoxapine.
Mirabegron The risk or severity of urinary retention can be increased when Amoxapine is combined with Mirabegron.
Potassium chloride The risk or severity of gastrointestinal ulceration can be increased when Amoxapine is combined with Potassium chloride.
Pramlintide The risk or severity of reduced gastrointestinal motility can be increased when Pramlintide is combined with Amoxapine.

Target Protein

Sodium-dependent serotonin transporter SLC6A4
Sodium-dependent noradrenaline transporter SLC6A2
D(2) dopamine receptor DRD2
D(1A) dopamine receptor DRD1
Alpha-2A adrenergic receptor ADRA2A
Alpha-1A adrenergic receptor ADRA1A
Muscarinic acetylcholine receptor M1 CHRM1
Gamma-aminobutyric acid receptor subunit alpha-1 GABRA1
5-hydroxytryptamine receptor 2A HTR2A
5-hydroxytryptamine receptor 2C HTR2C
5-hydroxytryptamine receptor 6 HTR6
5-hydroxytryptamine receptor 7 HTR7
D(3) dopamine receptor DRD3
D(4) dopamine receptor DRD4
Histamine H1 receptor HRH1
Alpha-1 adrenergic receptors ADRA1A
Muscarinic acetylcholine receptor CHRM1
5-hydroxytryptamine receptor 2B HTR2B
5-hydroxytryptamine receptor 3A HTR3A
5-hydroxytryptamine receptor 1A HTR1A
5-hydroxytryptamine receptor 1B HTR1B
Alpha-2 adrenergic receptors ADRA2A
Histamine H4 receptor HRH4
GABA(A) Receptor GABRA1
Sodium-dependent dopamine transporter SLC6A3

Referensi & Sumber

Synthesis reference: Howell, C.F., Hardy, R.A., Jr. and Quinones, N.Q.; US. Patent 3,663,696; May 16, 1972; assigned to American Cyanamid Company Howell, C.F., Hardy, R.A., Jr. and Quinones, N.Q.; U.S. Patent 3,681,357; August 1, 1972; assigned to American Cyanamid Company

Contoh Produk & Brand

Produk: 15 • International brands: 9
Produk
  • Amoxapine
    Tablet • 50 mg/1 • Oral • US • Generic • Approved
  • Amoxapine
    Tablet • 25 mg/1 • Oral • US • Generic • Approved
  • Amoxapine
    Tablet • 50 mg/1 • Oral • US • Generic • Approved
  • Amoxapine
    Tablet • 100 mg/1 • Oral • US • Generic • Approved
  • Amoxapine
    Tablet • 150 mg/1 • Oral • US • Generic • Approved
  • Amoxapine
    Tablet • 25 mg/1 • Oral • US • Generic • Approved
  • Amoxapine
    Tablet • 50 mg/1 • Oral • US • Generic • Approved
  • Amoxapine
    Tablet • 100 mg/1 • Oral • US • Generic • Approved
Menampilkan 8 dari 15 produk.
International Brands
  • Adisen — Kun Wha
  • Amolife
  • Amoxan — Wyeth KK
  • Asendin
  • Asendis
  • Défanyl — Eisai
  • Demolox — Wyeth
  • Oxamine — Psyco Remedies
  • Oxcap

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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