Tìm theo
Methotrimeprazine
Các tên gọi khác (7 ) :
  • (-)-(2R)-3-(2-Methoxy-10H-phenothiazin-10-yl)-N,N,2-trimethylpropan-1-amine
  • (-)-10-(3-(Dimethylamino)-2-methylpropyl)-2-methoxyphenothiazine
  • 2-Methoxytrimeprazine
  • Levomepromazina
  • Levomepromazine
  • Levomepromazinum
  • Methotrimeprazine
Thuốc chống rối loạn tâm thần
Thuốc Gốc
Small Molecule
CAS: 60-99-1
CTHH: C19H24N2OS
PTK: 328.472
A phenothiazine with pharmacological activity similar to that of both chlorpromazine and promethazine. It has the histamine-antagonist properties of the antihistamines together with central nervous system effects resembling those of chlorpromazine. (From Martindale, The Extra Pharmacopoeia, 30th ed, p604)
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C19H24N2OS
Phân tử khối
328.472
Monoisotopic mass
328.16093409
InChI
InChI=1S/C19H24N2OS/c1-14(12-20(2)3)13-21-16-7-5-6-8-18(16)23-19-10-9-15(22-4)11-17(19)21/h5-11,14H,12-13H2,1-4H3/t14-/m1/s1
InChI Key
InChIKey=VRQVVMDWGGWHTJ-CQSZACIVSA-N
IUPAC Name
[(2R)-3-(2-methoxy-10H-phenothiazin-10-yl)-2-methylpropyl]dimethylamine
Traditional IUPAC Name
methotrimeprazine
SMILES
COC1=CC2=C(SC3=C(C=CC=C3)N2C[C@H](C)CN(C)C)C=C1
Độ hòa tan
20 mg/L (at 25 °C)
logP
4.68
logS
-4.22
pKa (Strongest Basic)
9.42
PSA
15.71 Å2
Refractivity
99.83 m3·mol-1
Polarizability
36.77 Å3
Rotatable Bond Count
5
H Bond Acceptor Count
3
H Bond Donor Count
0
Physiological Charge
1
Number of Rings
3
Bioavailability
1
Rule of Five
true
Ghose Filter
true
pKa
9.19
Dược Lực Học : Methotrimeprazine is a phenothiazine with pharmacological activity similar to that of both chlorpromazine and promethazine. It has the histamine-antagonist properties of the antihistamines together with central nervous system effects resembling those of chlorpromazine. (From Martindale, The Extra Pharmacopoeia, 30th ed, p604)
Cơ Chế Tác Dụng : A phenothiazine with pharmacological activity similar to that of both chlorpromazine and promethazine. It has the histamine-antagonist properties of the antihistamines together with central nervous system effects resembling those of chlorpromazine. (From Martindale, The Extra Pharmacopoeia, 30th ed, p604) Methotrimeprazine's antipsychotic effect is largely due to its antagonism of dopamine receptors in the brain. In addition, its binding to 5HT2 receptors may also play a role.
Dược Động Học :
▧ Absorption :
Methotrimeprazine has an incomplete oral bioavailability, because it undergoes considerable first-pass-metabolism in the liver. Oral bioavailability is approximately 50 to 60%.
▧ Metabolism :
Hepatic. Methotrimeprazine is metabolized in the liver and degraded to a sulfoxid-, a glucuronid- and a demethyl-moiety.
▧ Half Life :
Approximately 20 hours.
Độc Tính : Symptoms of overdose include convulsions, spastic movements, and coma.
Chỉ Định : For the treatment of psychosis, particular those of schizophrenia, and manic phases of bipolar disorder.
Tương Tác Thuốc :
  • Amphetamine Decreased anorexic effect, may increase psychotic symptoms
  • Artemether Additive QTc-prolongation may occur. Concomitant therapy should be avoided.
  • Benzphetamine Antipsychotics may diminish the stimulatory effect of Amphetamines. Monitor effectiveness of amphetamine therapy when altering concurrent antipsychotic therapy as antipsychotic agents may impair the stimulatory effect of amphetamines.
  • Brimonidine Brimonidine may enhance the CNS depressant effect of Methotrimeprazine. Methotrimeprazine may enhance the CNS depressant effect of brimonidine. Consider therapy modification.
  • Bromazepam Concomitant therapy may result in additive CNS depressant effects. The dosage of bromazepam should be decreased by 50% prior to initiating concomitant therapy. Monitor for increased CNS depression.
  • Bromocriptine The phenothiazine decreases the effect of bromocriptine
  • Carisoprodol Carisoprodol, a CNS depressant, may enhance the CNS depressant effect of methotrimeprazine. Methotrimeprazine may enhance the CNS depressant effect of CNS Depressants like carisoprodol. Reduce the dosage of CNS depressants by 50% with initiation of concomitant methotrimeprazine therapy. Further CNS depressant dosage adjustments should be initiated only after clinically effective methotrimeprazine dose has been established. Monitor for increased CNS depression with concomitant therapy.
  • Cisapride Increased risk of cardiotoxicity and arrhythmias
  • Dantrolene Concomitant therapy may result in additive CNS depressant effects. The dosage of dantrolene should be decreased by 50% prior to initiating concomitant therapy. Monitor for increased CNS depression.
  • Dexfenfluramine Decreased anorexic effect, may increase psychotic symptoms
  • Dextroamphetamine Decreased anorexic effect, may increase psychotic symptoms
  • Diethylpropion Decreased anorexic effect, may increase psychotic symptoms
  • Donepezil Possible antagonism of action
  • Fenfluramine Decreased anorexic effect, may increase psychotic symptoms
  • Galantamine Possible antagonism of action
  • Gatifloxacin Increased risk of cardiotoxicity and arrhythmias
  • Grepafloxacin Increased risk of cardiotoxicity and arrhythmias
  • Guanethidine Methotrimeprazine may decrease the effect of guanethidine.
  • Isocarboxazid Possible severe adverse reaction with this combination
  • Levofloxacin Increased risk of cardiotoxicity and arrhythmias
  • Lumefantrine Additive QTc-prolongation may occur. Concomitant therapy should be avoided.
  • Mazindol Decreased anorexic effect, may increase psychotic symptoms
  • Methamphetamine Decreased anorexic effect, may increase psychotic symptoms
  • Metrizamide Increased risk of convulsions
  • Paliperidone The CNS depressant agents, paliperidone and methotrimeprazine, may cause additive CNS depressant effects. Monitor for increased CNS depressant effects during concomitant therapy.
  • Pargyline Possible severe adverse reaction with this combination
  • Phendimetrazine Decreased anorexic effect, may increase psychotic symptoms
  • Phenelzine Possible severe adverse reaction with this combination
  • Phenmetrazine Decreased anorexic effect, may increase psychotic symptoms
  • Phentermine Decreased anorexic effect, may increase psychotic symptoms
  • Phenylpropanolamine Decreased anorexic effect, may increase psychotic symptoms
  • Rivastigmine Possible antagonism of action
  • Sparfloxacin Increased risk of cardiotoxicity and arrhythmias
  • Terfenadine Increased risk of cardiotoxicity and arrhythmias
  • Tramadol Additive CNS depressant effects. Decrease dose of tramadol by 50% if initiating methotrimeprazine therapy. Monitor for increased CNS depression and apply further dosage adjustments as required.
  • Tranylcypromine Possible severe adverse reaction with this combination
  • Vigabatrin Additive CNS depression may occur. Dose adjustments may be required if one agent is added to existing therapy with the other agent. Monitor for increased CNS depression during concomitant therapy.
  • Voriconazole Additive QTc prolongation may occur. Consider alternate therapy or monitor for QTc prolongation as this can lead to Torsade de Pointes (TdP).
  • Vorinostat Additive QTc prolongation may occur. Consider alternate therapy or monitor for QTc prolongation as this can lead to Torsade de Pointes (TdP).
  • Zaleplon Additive CNS depressant effects may occur. A dose reduction of zaleplon may be required. Monitor for increased CNS depression during concomitant therapy.
  • Ziconotide Additive CNS depressant effects may occur. A dose reduction of ziconotide may be required. Monitor for increased CNS depression during concomitant therapy.
  • Ziprasidone Additive QTc-prolongation may occur increasing the risk of life-threatening ventricular arrhythmias and torsade de pointes. Concomitant therapy should be avoided.
  • Zolpidem Additive CNS depressant effects. Reduce zolpidem dose by half upon initiation of methotrimeprazine. Zolpidem dose may be adjusted once methotrimeprazine dose has been established. Monitor for increased CNS depression.
  • Zonisamide Additive CNS depressant effects. Reduce zonisamide dose by half upon initiation of methotrimeprazine. Zonisamide dose may be adjusted once methotrimeprazine dose has been established. Monitor for increased CNS depression.
  • Zopiclone Additive CNS depressant effects. Reduce zopiclone dose by half upon initiation of methotrimeprazine. Zopiclone dose may be adjusted once methotrimeprazine dose has been established. Monitor for increased CNS depression.
  • Zuclopenthixol Additive QTc prolongation may occur. Consider alternate therapy or use caution and monitor for QTc prolongation as this can lead to Torsade de Pointes (TdP). Methotrimeprazine, a strong CYP2D6 inhibitor, may increase the serum concentration of zuclopenthixol by decreasing its metabolism. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of zuclopenthixol if methotrimeprazine is initiated, discontinued or dose changed.
Liều Lượng & Cách Dùng : Solution - Intramuscular
Tablet - Oral
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Levoprome
  • Công ty :
    Sản phẩm biệt dược : Neurocil
  • Công ty :
    Sản phẩm biệt dược : Nosinan
  • Công ty :
    Sản phẩm biệt dược : Nozinan
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB01403
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=72287
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46507223
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C07192
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00403
ChemSpider
http://www.chemspider.com/Chemical-Structure.65239.html
PharmGKB
http://www.pharmgkb.org/drug/PA164743234
Wikipedia
http://en.wikipedia.org/wiki/Levomepromazine
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