Peringatan Keamanan

The LD50 is 0.78µg/mL in males and 0.98µg/mL in females.A176167

Patients experiencing an overdose present with respiratory depression, somnolence, skeletal muscle flaccidity, cold and clammy skin, miosis, and mydriasis. Symptoms of overdose can progress to pulmonary edema, bradycardia, hypotension, cardiac arrest, and death.L12108 Treat overdose with symptomatic and supportive treatment which may include the use of oxygen, vasopressors, and naloxone.L12108

Morphine

DB00295

small molecule approved investigational

Deskripsi

Morphine, the main alkaloid of opium, was first obtained from poppy seeds in 1805.A176035 It is a potent analgesic, though its use is limited due to tolerance, withdrawal, and the risk of abuse.A176050 Morphine is still routinely used today, though there are a number of semi-synthetic opioids of varying strength such as codeine, fentanyl, methadone, hydrocodone, hydromorphone, meperidine, and oxycodone.

Morphine was granted FDA approval in 1941.L12114

Struktur Molekul 2D

Berat 285.3377
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) Morphine has a half life of 2-3 hours.[A176116]
Volume Distribusi The volume of distribution of morphine is 5.31L/kg.[A176119] Morphine-6-glucuronide has a volume of distribution of 3.61L/kg.[A176119]
Klirens (Clearance) The apparent clearance of intravenous or subcutaneous morphine is 1600 mL/min.[A176164]

Absorpsi

Morphine is absorbed in the alkaline environments of the upper intestine and rectal mucosa.A176119 The bioavailability of morphine is 80-100%.A176164 There is significant first-pass metabolism, therefore oral doses are 6 times larger than parenteral doses to achieve the same effect. Morphine reaches steady-state concentrations after 24-48 hours.A176035 Parenteral morphine has a Tmax of 15 minutes and oral morphine has a Tmax of 90 minutes, with a Cmax of 283nmol/L.A176122,A176164 The AUC of morphine is 225-290nmol\*h/L.A176164

Metabolisme

Morphine is 90% metabolized by glucuronidation by UGT2B7 and sulfation at positions 3 and 6.A176059 Morphine can also be metabolized to codeine, normorphine, and morphine ethereal sulfate.A176119

Rute Eliminasi

70-80% of an administered dose is excreted within 48 hours.A176119 Morphine is predominantly eliminated in the urine with 2-10% of a dose recovered as the unchanged parent drug.A176059 7-10% of a dose of morphine is eliminated in the feces.L12114

Farmakogenomik

2 Varian
ABCB1 (rs1045642)

Patients with this genotype may have an increased analgesic response to morphine.

OPRM1 (rs1799971)

Patients with this genotype may have an increased analgesic response to morphine.

Interaksi Makanan

2 Data
  • 1. Avoid alcohol. Concomitant use may lead to profound sedation, respiratory depression, coma, and death.
  • 2. Take with or without food. There is no significant different in the AUC or Cmax of oral extended release tablets when taken with or without food.

Interaksi Obat

1472 Data
Duloxetine The risk or severity of orthostatic hypotension and syncope can be increased when Morphine is combined with Duloxetine.
Levodopa The risk or severity of hypotension and orthostatic hypotension can be increased when Morphine is combined with Levodopa.
Risperidone Morphine may increase the hypotensive activities of Risperidone.
Ranolazine The serum concentration of Morphine can be increased when it is combined with Ranolazine.
Buprenorphine Morphine 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 Morphine.
Dronabinol Dronabinol may increase the central nervous system depressant (CNS depressant) activities of Morphine.
Droperidol Droperidol may increase the central nervous system depressant (CNS depressant) activities of Morphine.
Hydrocodone Morphine may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Hydroxyzine Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Morphine.
Magnesium sulfate The therapeutic efficacy of Morphine can be increased when used in combination with Magnesium sulfate.
Methotrimeprazine Morphine may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
Metyrosine Morphine may increase the sedative activities of Metyrosine.
Minocycline Minocycline may increase the central nervous system depressant (CNS depressant) activities of Morphine.
Nabilone Nabilone may increase the central nervous system depressant (CNS depressant) activities of Morphine.
Orphenadrine Morphine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
Paraldehyde Morphine may increase the central nervous system depressant (CNS depressant) activities of Paraldehyde.
Perampanel Perampanel may increase the central nervous system depressant (CNS depressant) activities of Morphine.
Pramipexole Morphine may increase the sedative activities of Pramipexole.
Ropinirole Morphine may increase the sedative activities of Ropinirole.
Rotigotine Morphine may increase the sedative activities of Rotigotine.
Rufinamide The risk or severity of adverse effects can be increased when Rufinamide is combined with Morphine.
Sodium oxybate Morphine may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Suvorexant Morphine 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 Morphine.
Thalidomide Morphine may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
Zolpidem Morphine may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
Alvimopan The risk or severity of adverse effects can be increased when Morphine is combined with Alvimopan.
Desmopressin The risk or severity of hyponatremia can be increased when Morphine is combined with Desmopressin.
Codeine The risk or severity of adverse effects can be increased when Morphine is combined with Codeine.
Hydromorphone The risk or severity of adverse effects can be increased when Morphine is combined with Hydromorphone.
Oxycodone The risk or severity of adverse effects can be increased when Morphine is combined with Oxycodone.
Dextropropoxyphene The risk or severity of adverse effects can be increased when Morphine is combined with Dextropropoxyphene.
Sufentanil The risk or severity of adverse effects can be increased when Morphine is combined with Sufentanil.
Levorphanol The risk or severity of adverse effects can be increased when Morphine is combined with Levorphanol.
Remifentanil The risk or severity of adverse effects can be increased when Morphine is combined with Remifentanil.
Diphenoxylate The risk or severity of adverse effects can be increased when Morphine is combined with Diphenoxylate.
Oxymorphone The risk or severity of adverse effects can be increased when Morphine is combined with Oxymorphone.
Dezocine The risk or severity of adverse effects can be increased when Morphine is combined with Dezocine.
Methadyl acetate The risk or severity of adverse effects can be increased when Morphine is combined with Methadyl acetate.
Dihydroetorphine The risk or severity of adverse effects can be increased when Morphine is combined with Dihydroetorphine.
Diamorphine The risk or severity of adverse effects can be increased when Morphine is combined with Diamorphine.
Bezitramide The risk or severity of adverse effects can be increased when Morphine is combined with Bezitramide.
Ethylmorphine The risk or severity of adverse effects can be increased when Morphine is combined with Ethylmorphine.
Etorphine The risk or severity of adverse effects can be increased when Morphine is combined with Etorphine.
Dextromoramide The risk or severity of adverse effects can be increased when Morphine is combined with Dextromoramide.
Desomorphine The risk or severity of adverse effects can be increased when Morphine is combined with Desomorphine.
Carfentanil The risk or severity of adverse effects can be increased when Morphine is combined with Carfentanil.
Dihydrocodeine The risk or severity of adverse effects can be increased when Morphine is combined with Dihydrocodeine.
Alphacetylmethadol The risk or severity of adverse effects can be increased when Morphine is combined with Alphacetylmethadol.
Dihydromorphine The risk or severity of adverse effects can be increased when Morphine is combined with Dihydromorphine.
Ketobemidone The risk or severity of adverse effects can be increased when Morphine is combined with Ketobemidone.
DPDPE The risk or severity of adverse effects can be increased when Morphine is combined with DPDPE.
Lofentanil The risk or severity of adverse effects can be increased when Morphine is combined with Lofentanil.
Opium The risk or severity of adverse effects can be increased when Morphine is combined with Opium.
Normethadone The risk or severity of adverse effects can be increased when Morphine is combined with Normethadone.
Piritramide The risk or severity of adverse effects can be increased when Morphine is combined with Piritramide.
Alphaprodine The risk or severity of adverse effects can be increased when Morphine is combined with Alphaprodine.
Nicomorphine The risk or severity of adverse effects can be increased when Morphine is combined with Nicomorphine.
Meptazinol The therapeutic efficacy of Morphine can be decreased when used in combination with Meptazinol.
Phenoperidine The risk or severity of adverse effects can be increased when Morphine is combined with Phenoperidine.
Phenazocine The risk or severity of adverse effects can be increased when Morphine is combined with Phenazocine.
Tilidine The risk or severity of adverse effects can be increased when Morphine is combined with Tilidine.
Carfentanil, C-11 The risk or severity of adverse effects can be increased when Morphine is combined with Carfentanil, C-11.
Meperidine The risk or severity of adverse effects can be increased when Morphine is combined with Meperidine.
Alfentanil The risk or severity of adverse effects can be increased when Morphine is combined with Alfentanil.
Fentanyl The risk or severity of adverse effects can be increased when Morphine is combined with Fentanyl.
Benzhydrocodone The risk or severity of adverse effects can be increased when Morphine is combined with Benzhydrocodone.
Naloxegol The risk or severity of adverse effects can be increased when Morphine is combined with Naloxegol.
Pegvisomant The therapeutic efficacy of Pegvisomant can be decreased when used in combination with Morphine.
Succinylcholine The risk or severity of bradycardia can be increased when Succinylcholine is combined with Morphine.
Methadone The risk or severity of adverse effects can be increased when Methadone is combined with Morphine.
Mifepristone The serum concentration of Morphine can be increased when it is combined with Mifepristone.
Linezolid The risk or severity of serotonin syndrome can be increased when Linezolid is combined with Morphine.
Desogestrel The metabolism of Morphine can be increased when combined with Desogestrel.
Zidovudine The metabolism of Morphine can be increased when combined with Zidovudine.
Testosterone propionate The metabolism of Morphine can be increased when combined with Testosterone propionate.
Mirtazapine Morphine may increase the serotonergic activities of Mirtazapine.
Nicorandil Nicorandil may increase the hypotensive activities of Morphine.
Fluvoxamine The risk or severity of serotonin syndrome can be increased when Morphine is combined with Fluvoxamine.
Citalopram The risk or severity of serotonin syndrome can be increased when Morphine is combined with Citalopram.
Sertraline The risk or severity of serotonin syndrome can be increased when Morphine is combined with Sertraline.
Sibutramine The risk or severity of serotonin syndrome can be increased when Morphine is combined with Sibutramine.
Zimelidine The risk or severity of serotonin syndrome can be increased when Morphine is combined with Zimelidine.
Dapoxetine The risk or severity of serotonin syndrome can be increased when Morphine is combined with Dapoxetine.
Milnacipran The risk or severity of serotonin syndrome can be increased when Morphine is combined with Milnacipran.
Desvenlafaxine The risk or severity of serotonin syndrome can be increased when Desvenlafaxine is combined with Morphine.
Seproxetine The risk or severity of serotonin syndrome can be increased when Morphine is combined with Seproxetine.
Levomilnacipran The risk or severity of serotonin syndrome can be increased when Morphine is combined with Levomilnacipran.
Indalpine The risk or severity of serotonin syndrome can be increased when Morphine is combined with Indalpine.
Ritanserin The risk or severity of serotonin syndrome can be increased when Morphine is combined with Ritanserin.
Alaproclate The risk or severity of serotonin syndrome can be increased when Morphine is combined with Alaproclate.
Paroxetine The risk or severity of serotonin syndrome can be increased when Morphine is combined with Paroxetine.
Ethanol Morphine may increase the central nervous system depressant (CNS depressant) activities of Ethanol.
Azelastine Morphine may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
Brimonidine Brimonidine may increase the central nervous system depressant (CNS depressant) activities of Morphine.
Phentermine Phentermine may increase the analgesic activities of Morphine.
Pseudoephedrine Pseudoephedrine may increase the analgesic activities of Morphine.
Benzphetamine Benzphetamine may increase the analgesic activities of Morphine.
Diethylpropion Diethylpropion may increase the analgesic activities of Morphine.

Target Protein

Mu-type opioid receptor OPRM1
Kappa-type opioid receptor OPRK1
Delta-type opioid receptor OPRD1
Lymphocyte antigen 96 LY96

Referensi & Sumber

Artikel (PubMed)
  • PMID: 27626479
    Pacifici GM: Metabolism and pharmacokinetics of morphine in neonates: A review. Clinics (Sao Paulo). 2016 Aug;71(8):474-80. doi: 10.6061/clinics/2016(08)11.
  • PMID: 27506251
    Kim J, Ham S, Hong H, Moon C, Im HI: Brain Reward Circuits in Morphine Addiction. Mol Cells. 2016 Sep;39(9):645-53. doi: 10.14348/molcells.2016.0137. Epub 2016 Aug 9.
  • PMID: 25444409
    Beltran-Campos V, Silva-Vera M, Garcia-Campos ML, Diaz-Cintra S: Effects of morphine on brain plasticity. Neurologia. 2015 Apr;30(3):176-80. doi: 10.1016/j.nrl.2014.08.004. Epub 2014 Nov 11.
  • PMID: 24985077
    Klimas R, Mikus G: Morphine-6-glucuronide is responsible for the analgesic effect after morphine administration: a quantitative review of morphine, morphine-6-glucuronide, and morphine-3-glucuronide. Br J Anaesth. 2014 Dec;113(6):935-44. doi: 10.1093/bja/aeu186. Epub 2014 Jul 1.
  • PMID: 15907650
    Lotsch J: Pharmacokinetic-pharmacodynamic modeling of opioids. J Pain Symptom Manage. 2005 May;29(5 Suppl):S90-103. doi: 10.1016/j.jpainsymman.2005.01.012.
  • PMID: 2245160
    Hoskin PJ, Hanks GW: Morphine: pharmacokinetics and clinical practice. Br J Cancer. 1990 Nov;62(5):705-7.
  • PMID: 2057987
    Glare PA, Walsh TD: Clinical pharmacokinetics of morphine. Ther Drug Monit. 1991 Jan;13(1):1-23.
  • PMID: 10718775
    Stuart-Harris R, Joel SP, McDonald P, Currow D, Slevin ML: The pharmacokinetics of morphine and morphine glucuronide metabolites after subcutaneous bolus injection and subcutaneous infusion of morphine. Br J Clin Pharmacol. 2000 Mar;49(3):207-14.
Menampilkan 8 dari 9 artikel.

Contoh Produk & Brand

Produk: 701 • International brands: 3
Produk
  • Arymo ER
    Tablet, film coated, extended release • 15 mg/1 • Oral • US • Approved
  • Arymo ER
    Tablet, film coated, extended release • 30 mg/1 • Oral • US • Approved
  • Arymo ER
    Tablet, film coated, extended release • 60 mg/1 • Oral • US • Approved
  • Astramorph
    Injection • 0.5 mg/1mL • Epidural; Intrathecal; Intravenous • US • Generic • Approved
  • Astramorph
    Injection • 1 mg/1mL • Epidural; Intrathecal; Intravenous • US • Generic • Approved
  • Astramorph
    Injection • 0.5 mg/1mL • Epidural; Intrathecal; Intravenous • US • Generic • Approved
  • Astramorph
    Injection • 0.5 mg/1mL • Epidural; Intrathecal; Intravenous • US • Generic • Approved
  • Astramorph
    Injection • 1 mg/1mL • Epidural; Intrathecal; Intravenous • US • Generic • Approved
Menampilkan 8 dari 701 produk.
International Brands
  • Kapanol — Mayne Pharma/Glaxo
  • MSIR — Purdue Pharma
  • Oramorph — Boeringher Ingelheim

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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