Peringatan Keamanan

CNS and respiratory depression which may progress to Cheyne-Stokes respiration, areflexia, constriction of the pupils to a slight degree (though in severe poisoning they may wshow paralytic dilation), oliguria, tachycardia, hypotension, lowered body temperature, and coma. Typical shock syndrome (apnea, circulatory collapse, respiratory arrest, and death) may occur.

Phenobarbital

DB01174

small molecule approved investigational

Deskripsi

A barbituric acid derivative that acts as a nonselective central nervous system depressant. It promotes binding to inhibitory gamma-aminobutyric acid subtype receptors, and modulates chloride currents through receptor channels. It also inhibits glutamate induced depolarizations.

Struktur Molekul 2D

Berat 232.2353
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) 53 to 118 hours (mean 79 hours)
Volume Distribusi -
Klirens (Clearance) -

Absorpsi

Absorbed in varying degrees following oral, rectal or parenteral administration. The salts are more rapidly absorbed than are the acids. The rate of absorption is increased if the sodium salt is ingested as a dilute solution or taken on an empty stomach.

Metabolisme

Hepatic (mostly via CYP2C19).

Rute Eliminasi

Data eliminasi belum tersedia.

Interaksi Makanan

4 Data
  • 1. Administer vitamin supplements.
  • 2. Avoid alcohol.
  • 3. Limit caffeine intake.
  • 4. Take on an empty stomach. Taking this medication on an empty stomach increases the speed of absorption.

Interaksi Obat

1912 Data
Aripiprazole The metabolism of Aripiprazole can be increased when combined with Phenobarbital.
Buprenorphine Phenobarbital 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 Phenobarbital.
Dronabinol Dronabinol may increase the central nervous system depressant (CNS depressant) activities of Phenobarbital.
Droperidol Droperidol may increase the central nervous system depressant (CNS depressant) activities of Phenobarbital.
Hydroxyzine Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Phenobarbital.
Magnesium sulfate The therapeutic efficacy of Phenobarbital can be increased when used in combination with Magnesium sulfate.
Methotrimeprazine Phenobarbital may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
Metyrosine Phenobarbital may increase the sedative activities of Metyrosine.
Minocycline Minocycline may increase the central nervous system depressant (CNS depressant) activities of Phenobarbital.
Mirtazapine Phenobarbital 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 Phenobarbital.
Orphenadrine Phenobarbital may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
Paraldehyde Phenobarbital may increase the central nervous system depressant (CNS depressant) activities of Paraldehyde.
Pramipexole Phenobarbital may increase the sedative activities of Pramipexole.
Rotigotine Phenobarbital may increase the sedative activities of Rotigotine.
Suvorexant Phenobarbital 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 Phenobarbital.
Thalidomide Phenobarbital may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
Zolpidem Phenobarbital may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
Amphetamine The serum concentration of Phenobarbital can be decreased when it is combined with Amphetamine.
Phentermine The serum concentration of Phenobarbital can be decreased when it is combined with Phentermine.
Pseudoephedrine The serum concentration of Phenobarbital can be decreased when it is combined with Pseudoephedrine.
Benzphetamine The serum concentration of Phenobarbital can be decreased when it is combined with Benzphetamine.
Diethylpropion The serum concentration of Phenobarbital can be decreased when it is combined with Diethylpropion.
Lisdexamfetamine The serum concentration of Phenobarbital can be decreased when it is combined with Lisdexamfetamine.
Mephentermine The serum concentration of Phenobarbital can be decreased when it is combined with Mephentermine.
MMDA The serum concentration of Phenobarbital can be decreased when it is combined with MMDA.
Midomafetamine The serum concentration of Phenobarbital can be decreased when it is combined with Midomafetamine.
2,5-Dimethoxy-4-ethylamphetamine The serum concentration of Phenobarbital can be decreased when it is combined with 2,5-Dimethoxy-4-ethylamphetamine.
4-Bromo-2,5-dimethoxyamphetamine The serum concentration of Phenobarbital can be decreased when it is combined with 4-Bromo-2,5-dimethoxyamphetamine.
Tenamfetamine The serum concentration of Phenobarbital can be decreased when it is combined with Tenamfetamine.
Chlorphentermine The serum concentration of Phenobarbital can be decreased when it is combined with Chlorphentermine.
Methylenedioxyethamphetamine The serum concentration of Phenobarbital can be decreased when it is combined with Methylenedioxyethamphetamine.
Dextroamphetamine The serum concentration of Phenobarbital can be decreased when it is combined with Dextroamphetamine.
Metamfetamine The serum concentration of Phenobarbital can be decreased when it is combined with Metamfetamine.
Iofetamine I-123 The serum concentration of Phenobarbital can be decreased when it is combined with Iofetamine I-123.
Ritobegron The serum concentration of Phenobarbital can be decreased when it is combined with Ritobegron.
Mephedrone The serum concentration of Phenobarbital can be decreased when it is combined with Mephedrone.
Methoxyphenamine The serum concentration of Phenobarbital can be decreased when it is combined with Methoxyphenamine.
Gepefrine The serum concentration of Phenobarbital can be decreased when it is combined with Gepefrine.
2,5-Dimethoxy-4-ethylthioamphetamine The serum concentration of Phenobarbital can be decreased when it is combined with 2,5-Dimethoxy-4-ethylthioamphetamine.
Phendimetrazine The serum concentration of Phenobarbital can be decreased when it is combined with Phendimetrazine.
Dabrafenib The serum concentration of Phenobarbital 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 Phenobarbital.
Luliconazole The serum concentration of Phenobarbital can be increased when it is combined with Luliconazole.
Mefloquine The therapeutic efficacy of Phenobarbital can be decreased when used in combination with Mefloquine.
Orlistat Orlistat can cause a decrease in the absorption of Phenobarbital resulting in a reduced serum concentration and potentially a decrease in efficacy.
Chloramphenicol The metabolism of Phenobarbital can be decreased when combined with Chloramphenicol.
Doxycycline The serum concentration of Doxycycline can be decreased when it is combined with Phenobarbital.
Griseofulvin The serum concentration of Griseofulvin can be decreased when it is combined with Phenobarbital.
Mianserin The therapeutic efficacy of Phenobarbital can be decreased when used in combination with Mianserin.
Pentobarbital The risk or severity of adverse effects can be increased when Phenobarbital is combined with Pentobarbital.
Methohexital The risk or severity of adverse effects can be increased when Phenobarbital is combined with Methohexital.
Amobarbital The risk or severity of adverse effects can be increased when Phenobarbital is combined with Amobarbital.
Barbexaclone The risk or severity of adverse effects can be increased when Phenobarbital is combined with Barbexaclone.
Pyridoxine The metabolism of Phenobarbital can be increased when combined with Pyridoxine.
Teniposide The serum concentration of Teniposide can be decreased when it is combined with Phenobarbital.
Voriconazole The serum concentration of Voriconazole can be decreased when it is combined with Phenobarbital.
Prilocaine The risk or severity of methemoglobinemia can be increased when Phenobarbital is combined with Prilocaine.
Metyrapone The serum concentration of Metyrapone can be decreased when it is combined with Phenobarbital.
Rufinamide The serum concentration of Phenobarbital can be increased when it is combined with Rufinamide.
Topotecan Phenobarbital may increase the excretion rate of Topotecan which could result in a lower serum level and potentially a reduction in efficacy.
Acetazolamide The serum concentration of Phenobarbital can be decreased when it is combined with Acetazolamide.
Valproic acid The serum concentration of Phenobarbital, an active metabolite of Phenobarbital, 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 Phenobarbital.
Sodium oxybate Phenobarbital may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Methylphenidate The serum concentration of Phenobarbital can be increased when it is combined with Methylphenidate.
Quinine The serum concentration of Phenobarbital can be increased when it is combined with Quinine.
Quinidine The serum concentration of Phenobarbital can be increased when it is combined with Quinidine.
Lamotrigine Phenobarbital may increase the excretion rate of Lamotrigine which could result in a lower serum level and potentially a reduction in efficacy.
Ifosfamide The metabolism of Ifosfamide can be increased when combined with Phenobarbital.
Perampanel The metabolism of Perampanel can be increased when combined with Phenobarbital.
Tetrahydrofolic acid The serum concentration of Phenobarbital can be decreased when it is combined with Tetrahydrofolic acid.
Folic acid The serum concentration of Phenobarbital can be decreased when it is combined with Folic acid.
Leucovorin The serum concentration of Phenobarbital can be decreased when it is combined with Leucovorin.
(6S)-5,6,7,8-tetrahydrofolic acid The serum concentration of Phenobarbital can be decreased when it is combined with (6S)-5,6,7,8-tetrahydrofolic acid.
Triglu-5-formyl-tetrahydrofolate The serum concentration of Phenobarbital can be decreased when it is combined with Triglu-5-formyl-tetrahydrofolate.
(6R)-Folinic acid The serum concentration of Phenobarbital can be decreased when it is combined with (6R)-Folinic acid.
5-methyltetrahydrofolic acid The serum concentration of Phenobarbital can be decreased when it is combined with 5-methyltetrahydrofolic acid.
Levoleucovorin The serum concentration of Phenobarbital can be decreased when it is combined with Levoleucovorin.
Warfarin The metabolism of Warfarin can be increased when combined with Phenobarbital.
Acenocoumarol The metabolism of Acenocoumarol can be increased when combined with Phenobarbital.
(R)-warfarin The metabolism of (R)-warfarin can be increased when combined with Phenobarbital.
R,S-Warfarin alcohol The metabolism of R,S-Warfarin alcohol can be increased when combined with Phenobarbital.
S,R-Warfarin alcohol The metabolism of S,R-Warfarin alcohol can be increased when combined with Phenobarbital.
(S)-Warfarin The metabolism of (S)-Warfarin can be increased when combined with Phenobarbital.
Minoxidil The metabolism of Minoxidil can be increased when combined with Phenobarbital.
Raloxifene The metabolism of Raloxifene can be increased when combined with Phenobarbital.
Furosemide The metabolism of Furosemide can be increased when combined with Phenobarbital.
Ezetimibe The metabolism of Ezetimibe can be increased when combined with Phenobarbital.
Ketoprofen The metabolism of Ketoprofen can be increased when combined with Phenobarbital.
Abacavir The metabolism of Abacavir can be increased when combined with Phenobarbital.
Alvocidib The metabolism of Alvocidib can be increased when combined with Phenobarbital.
Ezogabine The metabolism of Ezogabine can be increased when combined with Phenobarbital.
Bazedoxifene The metabolism of Bazedoxifene can be increased when combined with Phenobarbital.
Gavestinel The metabolism of Gavestinel can be increased when combined with Phenobarbital.
Raltegravir The metabolism of Raltegravir can be increased when combined with Phenobarbital.
Dolutegravir The serum concentration of Dolutegravir can be decreased when it is combined with Phenobarbital.
Fulvestrant The metabolism of Fulvestrant can be increased when combined with Phenobarbital.

Target Protein

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
NMDA receptor GRIN1
Nuclear receptor subfamily 1 group I member 2 NR1I2

Referensi & Sumber

Synthesis reference: Tong Sun, Shawn Watson, Rajesh Manchanda, "PHENOBARBITAL SALTS; METHODS OF MAKING; AND METHODS OF USE THEREOF." U.S. Patent US20100035904, issued February 11, 2010.
Artikel (PubMed)
  • PMID: 15329080
    Kwan P, Brodie MJ: Phenobarbital for the treatment of epilepsy in the 21st century: a critical review. Epilepsia. 2004 Sep;45(9):1141-9.
  • PMID: 11687150
    Taylor S, Tudur Smith C, Williamson PR, Marson AG: Phenobarbitone versus phenytoin monotherapy for partial onset seizures and generalized onset tonic-clonic seizures. Cochrane Database Syst Rev. 2001;(4):CD002217.
  • PMID: 12535420
    Tudur Smith C, Marson AG, Williamson PR: Carbamazepine versus phenobarbitone monotherapy for epilepsy. Cochrane Database Syst Rev. 2003;(1):CD001904.
  • PMID: 16142991
    Kalviainen R, Eriksson K, Parviainen I: Refractory generalised convulsive status epilepticus : a guide to treatment. CNS Drugs. 2005;19(9):759-68.
  • PMID: 15495087
    Booth D, Evans DJ: Anticonvulsants for neonates with seizures. Cochrane Database Syst Rev. 2004 Oct 18;(4):CD004218.
  • PMID: 26496779
    Pacifici GM: Clinical Pharmacology of Phenobarbital in Neonates: Effects, Metabolism and Pharmacokinetics. Curr Pediatr Rev. 2016;12(1):48-54. doi: 10.2174/1573397111666151026223914.

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Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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