Peringatan Keamanan

The intravenous administration of paracetamol in the form of propacetamol has no effect on fertility. There is no evidence of carcinogenic potential in mice but there is a report in female rats at 0.7 times the maximum clinical exposure where there was a report of mononuclear cell leukemia. There is a potential clastogenic effect at doses of 8 times the maximum anticipated clinical exposure.L1523

Propacetamol

DB09288

small molecule experimental

Deskripsi

Propacetamol is a non-opioid analgesic devoid of the major contraindications.A32051 It is a derivative of acetaminophen, or paracetamol, with the molecular formula glycine, N, N-diethyl-,4-(acetylamino)phenyl ester. Propacetamol is a parenteral formulation of paracetamol and thus, it is a prodrug that is completely hydrolyzed to paracetamol.A7892 It is not available in the United States but this prodrug has been widely used in other countries such as France since 1985.L1505

Struktur Molekul 2D

Berat 264.325
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 propacetamol is of 3.6 h.[L1509]
Volume Distribusi The volume of distribution of propacetamol is 1.29 l/kg.[L1509]
Klirens (Clearance) The clearance rate of propacetamol is 0.28 l.h/kg.[L1509]

Absorpsi

The bioavailability of 2g of propacetamol is similar to the bioavailability found in 1 g of intravenous paracetamol. Peak plasma concentration is obtained as and from the end of infusion. Pharmacokinetic analysis with intravenous propacetamol showed a significantly higher and earlier maximum plasma concentration than orally administered paracetamol. The Cmax, Tmax and AUC are 12.72 mcg/ml, 0.25 h and 25.5 mcg.h/ml. After infusion with propacetamol, significant concentrations of paracetamol are observed in cerebrospinal fluid.L1509

Metabolisme

After administration, propacetamol is completely converted by plasma esterases into N, N-diethylglycine and paracetamol. The latest is the active metabolite. It is reported that the active metabolite of propacetamol can be transformed to N-acetil-p-benzoquinone imine by CYP2E1 which is a hepatotoxic metabolite.L1511

Rute Eliminasi

The metabolites of propacetamol are mainly excreted in the urine. From the elimination rate, 90% of the administered dose is excreted in 24 hours mainly as glucuronide and sulfate conjugates. Less than 5% is eliminated as unchanged paracetamol.L1523

Interaksi Obat

1985 Data
Peginterferon alfa-2b The serum concentration of Propacetamol can be increased when it is combined with Peginterferon alfa-2b.
Leflunomide The serum concentration of Propacetamol can be decreased when it is combined with Leflunomide.
Teriflunomide The serum concentration of Propacetamol can be decreased when it is combined with Teriflunomide.
Amlodipine The metabolism of Propacetamol can be decreased when combined with Amlodipine.
Isoetharine The risk or severity of hypertension can be increased when Isoetharine is combined with Propacetamol.
Norepinephrine The risk or severity of hypertension can be increased when Norepinephrine is combined with Propacetamol.
Phenylpropanolamine The risk or severity of hypertension can be increased when Phenylpropanolamine is combined with Propacetamol.
Droperidol The risk or severity of hypertension can be increased when Droperidol is combined with Propacetamol.
Doxapram The risk or severity of hypertension can be increased when Doxapram is combined with Propacetamol.
Atropine The risk or severity of hypertension can be increased when Atropine is combined with Propacetamol.
Linezolid The risk or severity of hypertension can be increased when Linezolid is combined with Propacetamol.
Metaraminol The risk or severity of hypertension can be increased when Metaraminol is combined with Propacetamol.
Furazolidone The risk or severity of hypertension can be increased when Furazolidone is combined with Propacetamol.
Methoxamine The risk or severity of hypertension can be increased when Methoxamine is combined with Propacetamol.
Propiomazine The risk or severity of hypertension can be increased when Propiomazine is combined with Propacetamol.
Orciprenaline The risk or severity of hypertension can be increased when Orciprenaline is combined with Propacetamol.
Phenmetrazine The risk or severity of hypertension can be increased when Phenmetrazine is combined with Propacetamol.
Pseudoephedrine The risk or severity of hypertension can be increased when Pseudoephedrine is combined with Propacetamol.
Ritodrine The risk or severity of hypertension can be increased when Ritodrine is combined with Propacetamol.
Flupentixol The risk or severity of hypertension can be increased when Flupentixol is combined with Propacetamol.
Remifentanil The risk or severity of hypertension can be increased when Remifentanil is combined with Propacetamol.
Bitolterol The risk or severity of hypertension can be increased when Bitolterol is combined with Propacetamol.
Oxymetazoline The risk or severity of hypertension can be increased when Oxymetazoline is combined with Propacetamol.
Diethylpropion The risk or severity of hypertension can be increased when Diethylpropion is combined with Propacetamol.
Naratriptan The risk or severity of hypertension can be increased when Naratriptan is combined with Propacetamol.
Isoprenaline Isoprenaline may increase the neuromuscular blocking activities of Propacetamol.
Arbutamine The risk or severity of hypertension can be increased when Arbutamine is combined with Propacetamol.
Desflurane The risk or severity of hypertension can be increased when Desflurane is combined with Propacetamol.
Isocarboxazid The risk or severity of hypertension can be increased when Isocarboxazid is combined with Propacetamol.
Lisdexamfetamine The risk or severity of hypertension can be increased when Lisdexamfetamine is combined with Propacetamol.
Fenoterol The risk or severity of hypertension can be increased when Fenoterol is combined with Propacetamol.
Pirbuterol The risk or severity of hypertension can be increased when Pirbuterol is combined with Propacetamol.
Ephedra sinica root The risk or severity of hypertension can be increased when Ephedra sinica root is combined with Propacetamol.
Ephedrine The risk or severity of hypertension can be increased when Ephedrine is combined with Propacetamol.
Mephentermine The risk or severity of hypertension can be increased when Mephentermine is combined with Propacetamol.
Procaterol The risk or severity of hypertension can be increased when Procaterol is combined with Propacetamol.
Clenbuterol The risk or severity of hypertension can be increased when Clenbuterol is combined with Propacetamol.
MMDA The risk or severity of hypertension can be increased when MMDA is combined with Propacetamol.
2,5-Dimethoxy-4-ethylamphetamine The risk or severity of hypertension can be increased when 2,5-Dimethoxy-4-ethylamphetamine is combined with Propacetamol.
4-Bromo-2,5-dimethoxyamphetamine The risk or severity of hypertension can be increased when 4-Bromo-2,5-dimethoxyamphetamine is combined with Propacetamol.
Tenamfetamine The risk or severity of hypertension can be increased when Tenamfetamine is combined with Propacetamol.
Chlorphentermine The risk or severity of hypertension can be increased when Chlorphentermine is combined with Propacetamol.
Dextroamphetamine The risk or severity of hypertension can be increased when Dextroamphetamine is combined with Propacetamol.
Phendimetrazine The risk or severity of hypertension can be increased when Phendimetrazine is combined with Propacetamol.
Periciazine The risk or severity of hypertension can be increased when Periciazine is combined with Propacetamol.
Acepromazine The risk or severity of hypertension can be increased when Acepromazine is combined with Propacetamol.
Thioproperazine The risk or severity of hypertension can be increased when Thioproperazine is combined with Propacetamol.
Epicaptopril The risk or severity of hypertension can be increased when Epicaptopril is combined with Propacetamol.
Clorgiline The risk or severity of hypertension can be increased when Clorgiline is combined with Propacetamol.
1-benzylimidazole The risk or severity of hypertension can be increased when 1-benzylimidazole is combined with Propacetamol.
Nialamide The risk or severity of hypertension can be increased when Nialamide is combined with Propacetamol.
Amibegron The risk or severity of hypertension can be increased when Amibegron is combined with Propacetamol.
Naluzotan The risk or severity of hypertension can be increased when Naluzotan is combined with Propacetamol.
Pizotifen The risk or severity of hypertension can be increased when Pizotifen is combined with Propacetamol.
Solabegron The risk or severity of hypertension can be increased when Solabegron is combined with Propacetamol.
Nitrous oxide The risk or severity of hypertension can be increased when Nitrous oxide is combined with Propacetamol.
Xylometazoline The risk or severity of hypertension can be increased when Xylometazoline is combined with Propacetamol.
Dexmethylphenidate The risk or severity of hypertension can be increased when Dexmethylphenidate is combined with Propacetamol.
Isometheptene The risk or severity of hypertension can be increased when Isometheptene is combined with Propacetamol.
Levonordefrin The risk or severity of hypertension can be increased when Levonordefrin is combined with Propacetamol.
Naphazoline The risk or severity of hypertension can be increased when Naphazoline is combined with Propacetamol.
Tetryzoline The risk or severity of hypertension can be increased when Tetryzoline is combined with Propacetamol.
Cinitapride The risk or severity of hypertension can be increased when Cinitapride is combined with Propacetamol.
Tyramine The risk or severity of hypertension can be increased when Tyramine is combined with Propacetamol.
Adrafinil The risk or severity of hypertension can be increased when Adrafinil is combined with Propacetamol.
Isoxsuprine The risk or severity of hypertension can be increased when Isoxsuprine is combined with Propacetamol.
Ifenprodil The risk or severity of hypertension can be increased when Ifenprodil is combined with Propacetamol.
Hexoprenaline The risk or severity of hypertension can be increased when Hexoprenaline is combined with Propacetamol.
Etilefrine The risk or severity of hypertension can be increased when Etilefrine is combined with Propacetamol.
Cirazoline The risk or severity of hypertension can be increased when Cirazoline is combined with Propacetamol.
Synephrine The risk or severity of hypertension can be increased when Synephrine is combined with Propacetamol.
Hydracarbazine The risk or severity of hypertension can be increased when Hydracarbazine is combined with Propacetamol.
Benmoxin The risk or severity of hypertension can be increased when Benmoxin is combined with Propacetamol.
Mebanazine The risk or severity of hypertension can be increased when Mebanazine is combined with Propacetamol.
Octamoxin The risk or severity of hypertension can be increased when Octamoxin is combined with Propacetamol.
Pheniprazine The risk or severity of hypertension can be increased when Pheniprazine is combined with Propacetamol.
Phenoxypropazine The risk or severity of hypertension can be increased when Phenoxypropazine is combined with Propacetamol.
Pivhydrazine The risk or severity of hypertension can be increased when Pivhydrazine is combined with Propacetamol.
Safrazine The risk or severity of hypertension can be increased when Safrazine is combined with Propacetamol.
Caroxazone The risk or severity of hypertension can be increased when Caroxazone is combined with Propacetamol.
Iofetamine I-123 The risk or severity of hypertension can be increased when Propacetamol is combined with Iofetamine I-123.
Racepinephrine The risk or severity of hypertension can be increased when Propacetamol is combined with Racepinephrine.
Amitraz The risk or severity of hypertension can be increased when Propacetamol is combined with Amitraz.
Medetomidine The risk or severity of hypertension can be increased when Propacetamol is combined with Medetomidine.
Xylazine The risk or severity of hypertension can be increased when Propacetamol is combined with Xylazine.
Atipamezole The risk or severity of hypertension can be increased when Propacetamol is combined with Atipamezole.
Ractopamine The risk or severity of hypertension can be increased when Propacetamol is combined with Ractopamine.
Romifidine The risk or severity of hypertension can be increased when Propacetamol is combined with Romifidine.
Detomidine The risk or severity of hypertension can be increased when Propacetamol is combined with Detomidine.
Tetrahydrocannabivarin The risk or severity of hypertension can be increased when Propacetamol is combined with Tetrahydrocannabivarin.
PF-00610355 The risk or severity of hypertension can be increased when Propacetamol is combined with PF-00610355.
Ritobegron The risk or severity of hypertension can be increased when Propacetamol is combined with Ritobegron.
Abediterol The risk or severity of hypertension can be increased when Propacetamol is combined with Abediterol.
Tulobuterol The risk or severity of hypertension can be increased when Propacetamol is combined with Tulobuterol.
Dopexamine The risk or severity of hypertension can be increased when Propacetamol is combined with Dopexamine.
Piclozotan The risk or severity of hypertension can be increased when Propacetamol is combined with Piclozotan.
Idazoxan The risk or severity of hypertension can be increased when Propacetamol is combined with Idazoxan.
Higenamine The risk or severity of hypertension can be increased when Propacetamol is combined with Higenamine.
Reproterol The risk or severity of hypertension can be increased when Propacetamol is combined with Reproterol.
Tramazoline The risk or severity of hypertension can be increased when Propacetamol is combined with Tramazoline.

Target Protein

Prostaglandin G/H synthase 1 PTGS1
Prostaglandin G/H synthase 2 PTGS2
Transient receptor potential cation channel subfamily V member 1 TRPV1
Cannabinoid receptor 1 CNR1

Referensi & Sumber

Artikel (PubMed)
  • PMID: 8116325
    Hans P, Brichant JF, Bonhomme V, Triffaux M: Analgesic efficiency of propacetamol hydrochlorid after lumbar disc surgery. Acta Anaesthesiol Belg. 1993;44(4):129-33.
  • PMID: 24779190
    Jozwiak-Bebenista M, Nowak JZ: Paracetamol: mechanism of action, applications and safety concern. Acta Pol Pharm. 2014 Jan-Feb;71(1):11-23.
  • PMID: 1633071
    Bannwarth B, Netter P, Lapicque F, Gillet P, Pere P, Boccard E, Royer RJ, Gaucher A: Plasma and cerebrospinal fluid concentrations of paracetamol after a single intravenous dose of propacetamol. Br J Clin Pharmacol. 1992 Jul;34(1):79-81.
  • PMID: 14711849
    Allegaert K, Van der Marel CD, Debeer A, Pluim MA, Van Lingen RA, Vanhole C, Tibboel D, Devlieger H: Pharmacokinetics of single dose intravenous propacetamol in neonates: effect of gestational age. Arch Dis Child Fetal Neonatal Ed. 2004 Jan;89(1):F25-8.

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