Tìm theo
Primidone
Các tên gọi khác (8 ) :
  • 5-Phenyl-5-ethyl-hexahydropyrimidine-4,6-dione
  • Desoxyphenobarbital
  • Mysoline
  • Primaclone
  • Primidon
  • Primidona
  • Primidone
  • Primidonum
Thuốc chống co giật, chống động kinh
Thuốc Gốc
Small Molecule
CAS: 125-33-7
ATC: D08AC04, N03AA03, S03AA05, S01AX08, R01AX07, R02AA18
ĐG : Amerisource Health Services Corp. , http://www.amerisourcebergen.com
CTHH: C12H14N2O2
PTK: 218.2518
An antiepileptic agent related to the barbiturates; it is partly metabolized to phenobarbital in the body and owes some of its actions to this metabolite. Adverse effects are reported to be more frequent than with phenobarbital. (From Martindale, The Extra Pharmacopoeia, 30th ed, p309)
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C12H14N2O2
Phân tử khối
218.2518
Monoisotopic mass
218.105527702
InChI
InChI=1S/C12H14N2O2/c1-2-12(9-6-4-3-5-7-9)10(15)13-8-14-11(12)16/h3-7H,2,8H2,1H3,(H,13,15)(H,14,16)
InChI Key
InChIKey=DQMZLTXERSFNPB-UHFFFAOYSA-N
IUPAC Name
5-ethyl-5-phenyl-1,3-diazinane-4,6-dione
Traditional IUPAC Name
primidone
SMILES
CCC1(C(=O)NCNC1=O)C1=CC=CC=C1
Độ tan chảy
281.5 °C
Độ hòa tan
500 mg/L (at 22 °C)
logP
0.91
logS
-2.64
pKa (strongest acidic)
11.5
pKa (Strongest Basic)
-6.2
PSA
58.2 Å2
Refractivity
59.04 m3·mol-1
Polarizability
22.44 Å3
Rotatable Bond Count
2
H Bond Acceptor Count
2
H Bond Donor Count
2
Physiological Charge
0
Number of Rings
2
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Primidone is a barbiturate with anticonvulsant properties. Primidone, either alone or used concomitantly with other anticonvulsants, is indicated in the control of grand mal, psychomotor, and focal epileptic seizures. It may control grand mal seizures refractory to other anticonvulsant therapy. Primidone raises electro- or chemoshock seizure thresholds or alters seizure patterns in experimental animals. Primidone per se has anticonvulsant activity as do its two metabolites, phenobarbital and phenylethylmalonamide (PEMA). In addition to its anticonvulsant activity, Primidone potentiates that of phenobarbital in experimental animals.
Cơ Chế Tác Dụng : An antiepileptic agent related to the barbiturates; it is partly metabolized to phenobarbital in the body and owes some of its actions to this metabolite. Adverse effects are reported to be more frequent than with phenobarbital. (From Martindale, The Extra Pharmacopoeia, 30th ed, p309) Primidone is a GABA receptor agonist. The mechanism of Primidone's antiepileptic action is not known.
Dược Động Học :
▧ Absorption :
90 to 100%
▧ Protein binding :
70%
▧ Metabolism :
Hepatic
▧ Half Life :
3-23 hours
Độc Tính : Symptoms of an overdose typically include sluggishness, incoordination, difficulty in thinking, slowness of speech, faulty judgment, drowsiness or coma, shallow breathing, staggering, and in severe cases coma and death.
Chỉ Định : For the treatment of epilepsy
Tương Tác Thuốc :
  • Acenocoumarol The barbiturate, primidone, decreases the anticoagulant effect of acenocoumarol.
  • Aminophylline The barbiturate, primidone, decreases the effect of aminophylline.
  • Anisindione The barbiturate, primidone, decreases the anticoagulant effect of anisindione.
  • Asenapine Primidone is a CYP1A2 inducer and may increase metabolism of asenapine.
  • Bendamustine CYP1A2 metabolism may result in increased levels of active metabolites, decreases levels of bendamustine.
  • Betamethasone The barbiturate, primidone, may decrease the effect of the corticosteroid, betamethasone.
  • Chlorotrianisene The enzyme inducer, primidone, decreases the effect of the hormone agent, chlorotrianisene.
  • Clomifene The enzyme inducer, primidone, decreases the effect of the hormone agent, clomifene.
  • Conjugated Estrogens The enzyme inducer, primidone, decreases the effect of the hormone agent, conjugated estrogens.
  • Cortisone acetate The barbiturate, primidone, may decrease the effect of the corticosteroid, cortisone acetate.
  • Cyclosporine The barbiturate, primidone, increases the effect of cyclosporine.
  • Dexamethasone The barbiturate, primidone, may decrease the effect of the corticosteroid, dexamethasone.
  • Dicoumarol The barbiturate, primidone, decreases the anticoagulant effect, dicumarol.
  • Diethylstilbestrol The enzyme inducer, primidone, may decrease the effect of the hormone agent, diethylstilbestrol.
  • Doxycycline The anticonvulsant, primidone, decreases the effect of doxycycline.
  • Dyphylline The barbiturate, primidone, decreases the effect of dyphylline.
  • Estradiol The enzyme inducer, primidone, decreases the effect of the hormone agent, estradiol.
  • Estradiol valerate/Dienogest Affects CYP3A4 metabolism, decreases or effects levels of Estradiol valerate/Dienogest.
  • Estriol The enzyme inducer, primidone, decreases the effect of the hormone agent, estriol.
  • Estrone The enzyme inducer, primidone, decreases the effect of the hormone agent, estrone.
  • Estropipate The enzyme inducer, primidone, decreases the effect of the hormone agent, estropipate.
  • Ethinyl Estradiol This product may cause a slight decrease of contraceptive effect
  • Etravirine Etravirine, when used concomitantly with Primidone (primarily metabolized to phenobarbital), may experience a decrease in serum concentration. It is recommended to avoid concurrent therapy.
  • Felbamate Felbamate may increase the effect and toxicity of primidone.
  • Felodipine The barbiturate, primidone, decreases the effect of felodipine.
  • Fludrocortisone The barbiturate, primidone, may decrease the effect of the corticosteroid, fludrocortisone.
  • Folic Acid Folic acid decreases the effect of anticonvulsant, primidone.
  • Gefitinib The CYP3A4 inducer, primidone, may decrease the serum concentration and therapeutic effects of gefitinib.
  • Griseofulvin The barbiturate, primidone, decreases the effect of griseofulvin.
  • Hydrocortisone The barbiturate, primidone, may decrease the effect of the corticosteroid, hydrocortisone.
  • Levonorgestrel Phenobarbital decreases the effect of levonorgestrel
  • Medroxyprogesterone Acetate The enzyme inducer, primidone, may decrease the effect of the hormone, medroxyprogesterone.
  • Megestrol acetate The enzyme inducer, primidone, may decrease the effect of the hormone, megestrol.
  • Mestranol This product may cause a slight decrease of contraceptive effect
  • Methadone The barbiturate, primidone, decreases the effect of methadone.
  • Methoxyflurane The barbiturate, primidone, increases the renal toxicity of methoxyflurane.
  • Methylprednisolone The barbiturate, primidone, may decrease the effect of the corticosteroid, methylprednisolone.
  • Metoprolol The barbiturate decreases the effect of metabolized beta-blocker
  • Metronidazole The barbiturate, primidone, decreases the effect of metronidazole.
  • Nifedipine The barbiturate, primidone, decreases the effect of the calcium channel blocker, nifedipine.
  • Norethindrone This product may cause a slight decrease of contraceptive effect
  • Oxtriphylline The barbiturate, primidone, decreases the effect of oxtriphylline.
  • Paramethasone The barbiturate, primidone, may decrease the effect of the corticosteroid, paramethasone.
  • Prednisolone The barbiturate, primidone, may decrease the effect of the corticosteroid, prednisolone.
  • Prednisone The barbiturate, primidone, may decrease the effect of the corticosteroid, prednisone.
  • Propranolol The barbiturate decreases the effect of metabolized beta-blocker
  • Quinestrol The enzyme inducer, primidone, decreases the effect of the hormone agent, quinestrol.
  • Quinidine The anticonvulsant, primidone, decreases the effect of quinidine.
  • Roflumilast Affects CYP3A4 metabolism, decreases level or effect of roflumilast. Also decreases the level or effect of roflumilast by affecting CYP1A2 metabolism.
  • Rufinamide Increases clearance of rufinamide thus decreasing plasma concentration of rufinamide.
  • Telithromycin Primidone may decrease the plasma concentration of Telithromycin. Consider alternate therapy.
  • Temsirolimus Primidone may increase the metabolism of Temsirolimus decreasing its efficacy. Concomitant therapy should be avoided.
  • Theophylline The barbiturate, primidone, decreases the effect of theophylline.
  • Tramadol Primidone may decrease the effect of Tramadol by increasing Tramadol metabolism and clearance.
  • Trazodone The CYP3A4 inducer, Primidone, may decrease Trazodone efficacy by increasing Trazodone metabolism and clearance. Monitor for changes in Trazodone efficacy/toxicity if Primidone is initiated, discontinued or dose changed.
  • Tretinoin The strong CYP2C8 inducer, Primidone, may increase the metabolism and clearance of oral Tretinoin. Consider alternate therapy to avoid failure of Tretinoin therapy or monitor for changes in Tretinoin effectiveness and adverse/toxic effects if Primidone is initiated, discontinued or dose changed.
  • Triamcinolone The barbiturate, primidone, may decrease the effect of the corticosteroid, triamcinolone.
  • Triprolidine The CNS depressants, Triprolidine and Primidone, may increase adverse/toxic effects due to additivity. Monitor for increased CNS depressant effects during concomitant therapy.
  • Vandetanib Decreases levels of vandetanib by affecting CYP3A4 metabolism. Contraindicated.
  • Verapamil The barbiturate, primidone, decreases the effect of the calcium channel blocker, verapamil.
  • Voriconazole The barbiturate, primidone, decreases the effect of voriconazole.
  • Warfarin The barbiturate, primidone, decreases the anticoagulant effect of warfarin.
Liều Lượng & Cách Dùng : Tablet - Oral
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty : Desitin
    Sản phẩm biệt dược : Liskantin
  • Công ty : Unia
    Sản phẩm biệt dược : Mizodin
  • Công ty :
    Sản phẩm biệt dược : Mylepsinum
  • Công ty : AstraZeneca
    Sản phẩm biệt dược : Mysoline
  • Công ty : Psicofarma
    Sản phẩm biệt dược : Pridona
  • Công ty : Apsen
    Sản phẩm biệt dược : Primid
  • Công ty : Rekah
    Sản phẩm biệt dược : Prysoline
  • Công ty : Alkaloida
    Sản phẩm biệt dược : Sertan
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00794
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=4909
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46507775
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C07371
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00474
ChemSpider
http://www.chemspider.com/Chemical-Structure.4740.html
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0527-1301-01
PharmGKB
http://www.pharmgkb.org/drug/PA451105
Wikipedia
http://en.wikipedia.org/wiki/Primidone
RxList
http://www.rxlist.com/cgi/generic2/primid.htm
Drugs.com
http://www.drugs.com/cdi/primidone.html
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