药品详细

Primidone(扑米酮)

基本信息
剂型规格
适应症
药理
临床
理化性质
相互作用
文档
专利
Pathway
文献
序列

化学结构式图

中文名

扑米酮

英文名

Primidone

分子式

C₁₂H₁₄N₂O₂

化学名

5-ethyl-5-phenyl-1,3-diazinane-4,6-dione

分子量

Average: 218.2518
Monoisotopic: 218.105527702

CAS号

125-33-7

ATC分类

D08A 未知;S03A 未知;S01A 抗感染药;R01A 未知;R02A 未知;N03A 未知

药物类型

small molecule

阶段

approved

商品名

同义名

基本介绍

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)

生产厂家

Amneal pharmaceutical
Dr reddys laboratories ltd
Impax laboratories inc
Lannett co inc
Mutual pharmaceutical co inc
Valeant pharmaceuticals international
Vintage pharmaceuticals inc
Watson laboratories inc
West ward pharmaceutical corp
Xcel pharmaceuticals

封装厂家

Amerisource Health Services Corp.
Amneal Pharmaceuticals
Astellas Pharma Inc.
Atlantic Biologicals Corporation
Avkare Incorporated
Cardinal Health
Comprehensive Consultant Services Inc.
Doctor Reddys Laboratories Ltd.
Global Pharmaceuticals
Heartland Repack Services LLC
Impax Laboratories Inc.
Kaiser Foundation Hospital
Lake Erie Medical and Surgical Supply
Lannett Co. Inc.
Major Pharmaceuticals
Murfreesboro Pharmaceutical Nursing Supply
Mutual Pharmaceutical Co.
Patheon Inc.
PCA LLC
Pharmaceutical Packaging Center
Pharmaceutical Utilization Management Program VA Inc.
Pharmacy Service Center
Physicians Total Care Inc.
Prepak Systems Inc.
Professional Co.
Qualitest
Remedy Repack
Resource Optimization and Innovation LLC
Richmond Pharmacy
Valeant Ltd.
Vangard Labs Inc.
Vintage Pharmaceuticals Inc.
Watson Pharmaceuticals
West-Ward Pharmaceuticals

参考

Synthesis Reference

Not Available

General Reference

Murphy K, Delanty N: Primary Generalized Epilepsies. Curr Treat Options Neurol. 2000 Nov;2(6):527-542. Pubmed
Kagitani-Shimono K, Imai K, Okamoto N, Ono J, Okada S: Unverricht-Lundborg disease with cystatin B gene abnormalities. Pediatr Neurol. 2002 Jan;26(1):55-60. Pubmed
Brown GM, Stone GH, Rathbone MP: Primidone and rapid cycling affective disorders. Lancet. 1993 Oct 9;342(8876):925. Pubmed
Schaffer LC, Schaffer CB, Caretto J: The use of primidone in the treatment of refractory bipolar disorder. Ann Clin Psychiatry. 1999 Jun;11(2):61-6. Pubmed
Young MC, Hughes IA: Loss of therapeutic control in congenital adrenal hyperplasia due to interaction between dexamethasone and primidone. Acta Paediatr Scand. 1991 Jan;80(1):120-4. Pubmed

剂型

规格

化合物类型

Type	small molecule

Classes

Barbiturates
Phenethylamines
Lactams

Substructures

Barbiturates
Carbonyl Compounds
Amino Ketones
Benzene and Derivatives
Carboxylic Acids and Derivatives
Aminals and Derivatives
Pyrimidines and Derivatives
Phenethylamines
Heterocyclic compounds
Aromatic compounds
Carboxamides and Derivatives
Lactams

适应症

药理

Indication

For the treatment of epilepsy

Pharmacodynamics

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.

Mechanism of action

Primidone is a GABA receptor agonist. The mechanism of Primidone's antiepileptic action is not known.

Absorption

90 to 100%

Volume of distribution

Not Available

Protein binding

70%

Metabolism

Hepatic

Important The metabolism module of DrugBank is currently in beta. Questions or suggestions? Please contact us.

Substrate	Enzymes	Product
Primidone	Cytochrome P450 2C19	Phenobarbital	Details

Route of elimination

Not Available

Half life

3-23 hours

Clearance

Not Available

Toxicity

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.

Affected organisms

Humans and other mammals

Pathways

Not Available

理化性质

Properties

State

solid

Experimental Properties

Property	Value	Source
melting point	281.5 °C	PhysProp
water solubility	500 mg/L (at 22 °C)	YALKOWSKY,SH & DANNENFELSER,RM (1992)
logP	0.91	HANSCH,C ET AL. (1995)
logS	-2.64	ADME Research, USCD

Predicted Properties

Property	Value	Source
water solubility	1.04e+00 g/l	ALOGPS
logP	0.62	ALOGPS
logP	1.12	ChemAxon
logS	-2.3	ALOGPS
pKa (strongest acidic)	11.5	ChemAxon
pKa (strongest basic)	-6.2	ChemAxon
physiological charge	0	ChemAxon
hydrogen acceptor count	2	ChemAxon
hydrogen donor count	2	ChemAxon
polar surface area	58.2	ChemAxon
rotatable bond count	2	ChemAxon
refractivity	59.04	ChemAxon
polarizability	22.44	ChemAxon

药物相互作用

Drug	Interaction
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.
Dicumarol	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	The enzyme inducer, primidone, may decrease the effect of the hormone, medroxyprogesterone.
Megestrol	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.

食物相互作用

Avoid alcohol.
Avoid high doses of caffeine.
Take with food to reduce gastric irritation.

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