Peringatan Keamanan

The oral LD50 in rats is 1500mg/kg and in mice is 280mg/kg.L11199 The intraperitoneal LD50 in rats was 240mg/kg and in mice was 332mg/kg.L11199

Patients experiencing a primidone overdose may present with CNS depression, coma, respiratory depression, suppressed reflexes, suppressed response to pain, hypotension, and decreased urine output.A189510 Overdose should be treated with symptomatic and supportive treatment, including the removal of unabsorbed drug.A189510

Primidone

DB00794

small molecule approved vet_approved

Deskripsi

Primidone is an anticonvulsant used to treat essential tremor as well as grand mal, psychomotor, and focal epileptic seizures.L11112 Primidone was developed by J Yule Bogue and H C Carrington in 1949.A189522

Primidone was granted FDA Approval on 8 March 1954.L11112

Struktur Molekul 2D

Berat 218.2518
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) The half life of primidone is 7-22h in adults, 5-11h in children, and 8-80h in newborns.[A189486]
Volume Distribusi The volume of distribution of primidone is 0.5-0.8L/kg.[A189477,A189486]
Klirens (Clearance) Primidone is cleared at a rate of 30mL/min.[A189492]

Absorpsi

Oral primidone is up to 80% bioavailable with a Tmax if 2-4h.A35660,A189486 A 500mg oral dose of primidone Reaches a Cmax of 2.7±0.4µg/mL with a Tmax of 0.5-7h.A189492 Data regarding the AUC of primidone is not readily available.L11112

Metabolisme

Primidone is metabolized to phenobarbitol and phenylethylmalonamide (PEMA).A35126 This metabolism is largely mediated by CYP2C9,A185927,A35660,A189477 CYP2C19,A38649,A185927,A189477 and CYP2E1.A185927,A189477

Rute Eliminasi

Primidone is 72.9-80.6% recovered in urine.A189507

Interaksi Makanan

2 Data
  • 1. Avoid alcohol.
  • 2. Avoid St. John's Wort.

Interaksi Obat

1865 Data
Aripiprazole The metabolism of Aripiprazole can be increased when combined with Primidone.
Buprenorphine Primidone 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 Primidone.
Dronabinol Dronabinol may increase the central nervous system depressant (CNS depressant) activities of Primidone.
Droperidol Droperidol may increase the central nervous system depressant (CNS depressant) activities of Primidone.
Hydroxyzine Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Primidone.
Magnesium sulfate The therapeutic efficacy of Primidone can be increased when used in combination with Magnesium sulfate.
Methotrimeprazine Primidone may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
Metyrosine Primidone may increase the sedative activities of Metyrosine.
Minocycline Minocycline may increase the central nervous system depressant (CNS depressant) activities of Primidone.
Mirtazapine Primidone may increase the central nervous system depressant (CNS depressant) activities of Mirtazapine.
Nabilone Nabilone may increase the central nervous system depressant (CNS depressant) activities of Primidone.
Orphenadrine Primidone may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
Paraldehyde Primidone may increase the central nervous system depressant (CNS depressant) activities of Paraldehyde.
Pramipexole Primidone may increase the sedative activities of Pramipexole.
Rotigotine Primidone may increase the sedative activities of Rotigotine.
Suvorexant Primidone 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 Primidone.
Thalidomide Primidone may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
Zolpidem Primidone may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
Amphetamine The serum concentration of Primidone can be decreased when it is combined with Amphetamine.
Phentermine The serum concentration of Primidone can be decreased when it is combined with Phentermine.
Pseudoephedrine The serum concentration of Primidone can be decreased when it is combined with Pseudoephedrine.
Benzphetamine The serum concentration of Primidone can be decreased when it is combined with Benzphetamine.
Diethylpropion The serum concentration of Primidone can be decreased when it is combined with Diethylpropion.
Lisdexamfetamine The serum concentration of Primidone can be decreased when it is combined with Lisdexamfetamine.
Mephentermine The serum concentration of Primidone can be decreased when it is combined with Mephentermine.
MMDA The serum concentration of Primidone can be decreased when it is combined with MMDA.
Midomafetamine The serum concentration of Primidone can be decreased when it is combined with Midomafetamine.
2,5-Dimethoxy-4-ethylamphetamine The serum concentration of Primidone can be decreased when it is combined with 2,5-Dimethoxy-4-ethylamphetamine.
4-Bromo-2,5-dimethoxyamphetamine The serum concentration of Primidone can be decreased when it is combined with 4-Bromo-2,5-dimethoxyamphetamine.
Tenamfetamine The serum concentration of Primidone can be decreased when it is combined with Tenamfetamine.
Chlorphentermine The serum concentration of Primidone can be decreased when it is combined with Chlorphentermine.
Methylenedioxyethamphetamine The serum concentration of Primidone can be decreased when it is combined with Methylenedioxyethamphetamine.
Dextroamphetamine The serum concentration of Primidone can be decreased when it is combined with Dextroamphetamine.
Metamfetamine The serum concentration of Primidone can be decreased when it is combined with Metamfetamine.
Iofetamine I-123 The serum concentration of Primidone can be decreased when it is combined with Iofetamine I-123.
Ritobegron The serum concentration of Primidone can be decreased when it is combined with Ritobegron.
Mephedrone The serum concentration of Primidone can be decreased when it is combined with Mephedrone.
Methoxyphenamine The serum concentration of Primidone can be decreased when it is combined with Methoxyphenamine.
Gepefrine The serum concentration of Primidone can be decreased when it is combined with Gepefrine.
2,5-Dimethoxy-4-ethylthioamphetamine The serum concentration of Primidone can be decreased when it is combined with 2,5-Dimethoxy-4-ethylthioamphetamine.
Phendimetrazine The serum concentration of Primidone can be decreased when it is combined with Phendimetrazine.
Dabrafenib The serum concentration of Primidone can be decreased when it is combined with Dabrafenib.
Secretin porcine The therapeutic efficacy of Secretin porcine can be decreased when used in combination with Primidone.
Luliconazole The serum concentration of Primidone can be increased when it is combined with Luliconazole.
Mefloquine The therapeutic efficacy of Primidone can be decreased when used in combination with Mefloquine.
Orlistat Orlistat can cause a decrease in the absorption of Primidone resulting in a reduced serum concentration and potentially a decrease in efficacy.
Chloramphenicol The metabolism of Primidone can be decreased when combined with Chloramphenicol.
Doxycycline The serum concentration of Doxycycline can be decreased when it is combined with Primidone.
Griseofulvin The serum concentration of Griseofulvin can be decreased when it is combined with Primidone.
Mianserin The therapeutic efficacy of Primidone can be decreased when used in combination with Mianserin.
Butalbital The risk or severity of adverse effects can be increased when Primidone is combined with Butalbital.
Pentobarbital The risk or severity of adverse effects can be increased when Primidone is combined with Pentobarbital.
Secobarbital The risk or severity of adverse effects can be increased when Primidone is combined with Secobarbital.
Methohexital The risk or severity of adverse effects can be increased when Primidone is combined with Methohexital.
Amobarbital The risk or severity of adverse effects can be increased when Primidone is combined with Amobarbital.
Barbital The risk or severity of adverse effects can be increased when Primidone is combined with Barbital.
Barbexaclone The risk or severity of adverse effects can be increased when Primidone is combined with Barbexaclone.
Pyridoxine The metabolism of Primidone can be increased when combined with Pyridoxine.
Teniposide The serum concentration of Teniposide can be decreased when it is combined with Primidone.
Voriconazole The serum concentration of Voriconazole can be decreased when it is combined with Primidone.
Metyrapone The serum concentration of Metyrapone can be decreased when it is combined with Primidone.
Phenytoin The metabolism of Primidone can be increased when combined with Phenytoin.
Fosphenytoin The metabolism of Primidone can be increased when combined with Fosphenytoin.
Rufinamide The serum concentration of Primidone can be increased when it is combined with Rufinamide.
Topotecan Primidone may increase the excretion rate of Topotecan which could result in a lower serum level and potentially a reduction in efficacy.
Valproic acid The serum concentration of Phenobarbital, an active metabolite of Primidone, can be increased when used in combination with Valproic acid.
Methadone The risk or severity of adverse effects can be increased when Methadone is combined with Primidone.
Sodium oxybate Primidone may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Methylphenidate The serum concentration of Primidone can be increased when it is combined with Methylphenidate.
Quinine The serum concentration of Primidone can be increased when it is combined with Quinine.
Quinidine The serum concentration of Primidone can be increased when it is combined with Quinidine.
Lamotrigine Primidone may increase the excretion rate of Lamotrigine which could result in a lower serum level and potentially a reduction in efficacy.
Bendamustine The serum concentration of Bendamustine can be increased when it is combined with Primidone.
Pirfenidone The metabolism of Pirfenidone can be increased when combined with Primidone.
Ifosfamide The metabolism of Ifosfamide can be increased when combined with Primidone.
Perampanel The metabolism of Perampanel can be increased when combined with Primidone.
Tetrahydrofolic acid The serum concentration of Primidone can be decreased when it is combined with Tetrahydrofolic acid.
Folic acid The serum concentration of Primidone can be decreased when it is combined with Folic acid.
Leucovorin The serum concentration of Primidone can be decreased when it is combined with Leucovorin.
5-methyltetrahydrofolic acid The serum concentration of Primidone can be decreased when it is combined with 5-methyltetrahydrofolic acid.
Levomefolic acid The serum concentration of Primidone can be decreased when it is combined with Levomefolic acid.
Levoleucovorin The serum concentration of Primidone can be decreased when it is combined with Levoleucovorin.
(6S)-5,6,7,8-tetrahydrofolic acid The serum concentration of Primidone can be decreased when it is combined with (6S)-5,6,7,8-tetrahydrofolic acid.
Triglu-5-formyl-tetrahydrofolate The serum concentration of Primidone can be decreased when it is combined with Triglu-5-formyl-tetrahydrofolate.
(6R)-Folinic acid The serum concentration of Primidone can be decreased when it is combined with (6R)-Folinic acid.
Warfarin The metabolism of Warfarin can be increased when combined with Primidone.
Acenocoumarol The metabolism of Acenocoumarol can be increased when combined with Primidone.
(R)-warfarin The metabolism of (R)-warfarin can be increased when combined with Primidone.
R,S-Warfarin alcohol The metabolism of R,S-Warfarin alcohol can be increased when combined with Primidone.
S,R-Warfarin alcohol The metabolism of S,R-Warfarin alcohol can be increased when combined with Primidone.
(S)-Warfarin The metabolism of (S)-Warfarin can be increased when combined with Primidone.
Liothyronine The metabolism of Liothyronine can be increased when combined with Primidone.
Indomethacin The metabolism of Indomethacin can be increased when combined with Primidone.
Minoxidil The metabolism of Minoxidil can be increased when combined with Primidone.
Raloxifene The metabolism of Raloxifene can be increased when combined with Primidone.
Furosemide The metabolism of Furosemide can be increased when combined with Primidone.
Flurbiprofen The metabolism of Flurbiprofen can be increased when combined with Primidone.
Metronidazole The metabolism of Metronidazole can be increased when combined with Primidone.

Target Protein

Gamma-aminobutyric acid receptor subunit alpha-2 GABRA2
Gamma-aminobutyric acid receptor subunit alpha-3 GABRA3
Gamma-aminobutyric acid receptor subunit alpha-4 GABRA4
Gamma-aminobutyric acid receptor subunit alpha-5 GABRA5
Gamma-aminobutyric acid receptor subunit alpha-6 GABRA6
GABA(A) Receptor GABRA1
Gamma-aminobutyric acid receptor subunit alpha-1 GABRA1
Neuronal acetylcholine receptor subunit alpha-4 CHRNA4
Neuronal acetylcholine receptor subunit alpha-7 CHRNA7
Glutamate receptor 2 GRIA2
Glutamate receptor ionotropic, kainate 2 GRIK2

Referensi & Sumber

Artikel (PubMed)
  • PMID: 24812533
    Rajput AH, Rajput A: Medical treatment of essential tremor. J Cent Nerv Syst Dis. 2014 Apr 21;6:29-39. doi: 10.4137/JCNSD.S13570. eCollection 2014.
  • PMID: 24142589
    Schneider SA, Deuschl G: The treatment of tremor. Neurotherapeutics. 2014 Jan;11(1):128-38. doi: 10.1007/s13311-013-0230-5.
  • PMID: 6798720
    Haidukewych D, Rodin EA: Serial free and plasma valproic acid and phenytoin monitoring and drug interactions. Ther Drug Monit. 1981;3(3):303-7. doi: 10.1097/00007691-198103000-00013.
  • PMID: 24385718
    Hedera P, Cibulcik F, Davis TL: Pharmacotherapy of essential tremor. J Cent Nerv Syst Dis. 2013 Dec 22;5:43-55. doi: 10.4137/JCNSD.S6561.
  • PMID: 29955442
    Marvanova M: Pharmacokinetic characteristics of antiepileptic drugs (AEDs). Ment Health Clin. 2016 Mar 8;6(1):8-20. doi: 10.9740/mhc.2015.01.008. eCollection 2016 Jan.
  • PMID: 29957667
    Patsalos PN, Spencer EP, Berry DJ: Therapeutic Drug Monitoring of Antiepileptic Drugs in Epilepsy: A 2018 Update. Ther Drug Monit. 2018 Oct;40(5):526-548. doi: 10.1097/FTD.0000000000000546.
  • PMID: 7107978
    Lee CS, Marbury TC, Perchalski RT, Wilder BJ: Pharmacokinetics of primidone elimination by uremic patients. J Clin Pharmacol. 1982 Jul;22(7):301-8. doi: 10.1002/j.1552-4604.1982.tb02679.x.
  • PMID: 1523859
    Treston AM, Hooper WD: Urinary metabolites of phenobarbitone, primidone, and their N-methyl and N-ethyl derivatives in humans. Xenobiotica. 1992 Apr;22(4):385-94. doi: 10.3109/00498259209046650.
Menampilkan 8 dari 13 artikel.

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