Peringatan Keamanan

The reported LD50 of hydromorphone in the mouse was of 104 mg/kg when given intravenously and 84 mg/kg when given orally.F4181 The reports of overdose with hydromorphone are characterized by respiratory depression, somnolence, skeletal muscle flaccidity, cold and clammy skin, constricted pupils, myosis, mydriasis, bradycardia, hypotension, apnea, circulatory collapse, cardiac arrest, and even death.FDA label

The management of an overdose might require assisted ventilation, supportive measures, as well as cardiac massage and defibrillation. It can be recommended the use of naloxone solely in the cases of respiratory depression. The use of opioid antagonist should be restricted to patients that present respiratory depression as they can produce acute abstinence symptoms.FDA label

Hydromorphone was not shown to be mutagenic nor clastogenic and long-term studies of carcinogenicity studies have not been performed. On the other hand, reduced implantation sites and viable fetuses were noted at a 2X normal concentration.FDA label

Hydromorphone

DB00327

small molecule approved illicit

Deskripsi

Hydromorphone is a pure opioid,A176468 a semi-synthetic hydrogenated ketone derivative of morphine that has been available clinically since 1920. Structurally, hydromorphone derived from morphine in the modification of the hydroxyl group in the carbon 6 to a carbonyl and the absence of a double bond between the carbon 7 and 8. Due to these modifications, it presents a very high potency and comparable side effect profile to the parent compound.A176471 Even though hydromorphone does not present a 6-hydroxyl group, it is categorized under the family of phenanthrenes and it is considered a chemical under the schedule II (medical purposes with high addiction potential).A176495

The first reported approved product containing hydromorphone in the form of hydromorphone hydrochloride was developed by Fresenius Kabi USA and FDA approved in 1984.L5795

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) The half-life of hydromorphone immediate-release is of 2-3 hour while the extended release can range from 8-15 hours.[A176468]
Volume Distribusi The volume of distribution of hydromorphone is reported to be of 4 L/kg.[A176468]
Klirens (Clearance) The mean plasma clearance of hydromorphone is reported to be of 105.7 ml/min.[A176510] The systemic clearance is reported to be of 1.96 L/min.[L5798]

Absorpsi

The immediate release version of hydromorphone reaches its peak concentration after 30-60 minutes while the extended-release version reaches the peak concentration after 9 hours.A176468 When administered orally, hydromorphone is absorbed mainly in the upper small intestine with a bioavailability of 60% due to intensive first-pass metabolism. In the controlled-release version of hydromorphone, the absorption follows a biphasic pharmacokinetic profile. However, even though there are clear distinctions in the absorption pathway of hydromorphone, the AUC of both versions is reported to be of 34 ng.h/ml which indicates an equivalence.A176471 The parenteral administration of hydromorphone, which is the most common pathway, presents an almost immediate absorption as observed by the presence of peak plasma concentration almost immediately. This peak plasma concentration declines rapidly due to fast redistribution into liver, spleen, kidney and skeletal muscle. In the parenteral route, the pharmacokinetic profile is log-linear and dose-dependent and to present a higher bioavailability of 78%.A176471 Other administration routes such as rectal, nasal, intraspinal and transdermal present lower bioavailability and changes in their pharmacokinetic profile.A176471

Metabolisme

The metabolism of hydromorphone is mainly hepatic and it is represented by the generation of hydromorphone-3-glucuronide through glucuronidation reactions.A176468 This primary metabolic pathway is done by the activity of the UDP-glucuronosyltransferase-2B7.A176501 The first-pass hepatic metabolism is so large that it represents 62% of the initial administered dose.A176495 On the other hand, hydromorphone is also characterized by the presence of minor metabolic pathways such as the CYP3A4- and CYP2C9-driven generation of norhydromorphone.A39478

Rute Eliminasi

The main elimination route of hydromorphone is through the urine in the form of the main metabolite hydromorphone-3-glucuronide. The elimination of the parent compound represents 7% of the urine elimination and 1% of the fecal elimination.A176468

Interaksi Makanan

2 Data
  • 1. Avoid alcohol.
  • 2. Take with or without food. Food does not significantly affect absorption.

Interaksi Obat

1631 Data
Buprenorphine Hydromorphone 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 Hydromorphone.
Dronabinol Dronabinol may increase the central nervous system depressant (CNS depressant) activities of Hydromorphone.
Droperidol Droperidol may increase the central nervous system depressant (CNS depressant) activities of Hydromorphone.
Hydrocodone Hydromorphone 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 Hydromorphone.
Magnesium sulfate The therapeutic efficacy of Hydromorphone can be increased when used in combination with Magnesium sulfate.
Methotrimeprazine Hydromorphone may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
Metyrosine Hydromorphone may increase the sedative activities of Metyrosine.
Minocycline Minocycline may increase the central nervous system depressant (CNS depressant) activities of Hydromorphone.
Nabilone Nabilone may increase the central nervous system depressant (CNS depressant) activities of Hydromorphone.
Orphenadrine Hydromorphone may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
Paraldehyde Hydromorphone 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 Hydromorphone.
Pramipexole Hydromorphone may increase the sedative activities of Pramipexole.
Ropinirole Hydromorphone may increase the sedative activities of Ropinirole.
Rotigotine Hydromorphone may increase the sedative activities of Rotigotine.
Rufinamide The risk or severity of adverse effects can be increased when Rufinamide is combined with Hydromorphone.
Sodium oxybate Hydromorphone may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Suvorexant Hydromorphone 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 Hydromorphone.
Thalidomide Hydromorphone may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
Zolpidem Hydromorphone may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
Alvimopan The risk or severity of adverse effects can be increased when Hydromorphone is combined with Alvimopan.
Desmopressin The risk or severity of hyponatremia can be increased when Hydromorphone is combined with Desmopressin.
Morphine The risk or severity of adverse effects can be increased when Morphine is combined with Hydromorphone.
Codeine The risk or severity of adverse effects can be increased when Codeine is combined with Hydromorphone.
Oxycodone The risk or severity of adverse effects can be increased when Hydromorphone is combined with Oxycodone.
Dextropropoxyphene The risk or severity of adverse effects can be increased when Hydromorphone is combined with Dextropropoxyphene.
Naltrexone The therapeutic efficacy of Hydromorphone can be decreased when used in combination with Naltrexone.
Sufentanil The risk or severity of adverse effects can be increased when Hydromorphone is combined with Sufentanil.
Levorphanol The risk or severity of adverse effects can be increased when Hydromorphone is combined with Levorphanol.
Remifentanil The risk or severity of adverse effects can be increased when Hydromorphone is combined with Remifentanil.
Diphenoxylate The risk or severity of adverse effects can be increased when Hydromorphone is combined with Diphenoxylate.
Oxymorphone The risk or severity of adverse effects can be increased when Hydromorphone is combined with Oxymorphone.
Dezocine The risk or severity of adverse effects can be increased when Hydromorphone is combined with Dezocine.
Methadyl acetate The risk or severity of adverse effects can be increased when Hydromorphone is combined with Methadyl acetate.
Dihydroetorphine The risk or severity of adverse effects can be increased when Hydromorphone is combined with Dihydroetorphine.
Diamorphine The risk or severity of adverse effects can be increased when Hydromorphone is combined with Diamorphine.
Bezitramide The risk or severity of adverse effects can be increased when Hydromorphone is combined with Bezitramide.
Ethylmorphine The risk or severity of adverse effects can be increased when Hydromorphone is combined with Ethylmorphine.
Etorphine The risk or severity of adverse effects can be increased when Hydromorphone is combined with Etorphine.
Dextromoramide The risk or severity of adverse effects can be increased when Hydromorphone is combined with Dextromoramide.
Desomorphine The risk or severity of adverse effects can be increased when Hydromorphone is combined with Desomorphine.
Carfentanil The risk or severity of adverse effects can be increased when Hydromorphone is combined with Carfentanil.
Dihydrocodeine The risk or severity of adverse effects can be increased when Hydromorphone is combined with Dihydrocodeine.
Alphacetylmethadol The risk or severity of adverse effects can be increased when Hydromorphone is combined with Alphacetylmethadol.
Dihydromorphine The risk or severity of adverse effects can be increased when Hydromorphone is combined with Dihydromorphine.
Ketobemidone The risk or severity of adverse effects can be increased when Hydromorphone is combined with Ketobemidone.
DPDPE The risk or severity of adverse effects can be increased when Hydromorphone is combined with DPDPE.
Lofentanil The risk or severity of adverse effects can be increased when Hydromorphone is combined with Lofentanil.
Opium The risk or severity of adverse effects can be increased when Hydromorphone is combined with Opium.
Normethadone The risk or severity of adverse effects can be increased when Hydromorphone is combined with Normethadone.
Piritramide The risk or severity of adverse effects can be increased when Hydromorphone is combined with Piritramide.
Alphaprodine The risk or severity of adverse effects can be increased when Hydromorphone is combined with Alphaprodine.
Nicomorphine The risk or severity of adverse effects can be increased when Hydromorphone is combined with Nicomorphine.
Meptazinol The therapeutic efficacy of Hydromorphone can be decreased when used in combination with Meptazinol.
Phenoperidine The risk or severity of adverse effects can be increased when Hydromorphone is combined with Phenoperidine.
Phenazocine The risk or severity of adverse effects can be increased when Hydromorphone is combined with Phenazocine.
Tilidine The risk or severity of adverse effects can be increased when Hydromorphone is combined with Tilidine.
Carfentanil, C-11 The risk or severity of adverse effects can be increased when Hydromorphone is combined with Carfentanil, C-11.
Benzhydrocodone The risk or severity of adverse effects can be increased when Hydromorphone is combined with Benzhydrocodone.
Meperidine The risk or severity of adverse effects can be increased when Hydromorphone is combined with Meperidine.
Alfentanil The risk or severity of adverse effects can be increased when Hydromorphone is combined with Alfentanil.
Fentanyl The risk or severity of adverse effects can be increased when Hydromorphone is combined with Fentanyl.
Naloxegol The risk or severity of adverse effects can be increased when Hydromorphone is combined with Naloxegol.
Pegvisomant The therapeutic efficacy of Pegvisomant can be decreased when used in combination with Hydromorphone.
Succinylcholine The risk or severity of bradycardia can be increased when Succinylcholine is combined with Hydromorphone.
Methadone The risk or severity of adverse effects can be increased when Methadone is combined with Hydromorphone.
Tranylcypromine Tranylcypromine may increase the serotonergic activities of Hydromorphone.
Phenelzine Phenelzine may increase the serotonergic activities of Hydromorphone.
Selegiline Selegiline may increase the serotonergic activities of Hydromorphone.
Moclobemide Moclobemide may increase the serotonergic activities of Hydromorphone.
Isocarboxazid Isocarboxazid may increase the serotonergic activities of Hydromorphone.
Rasagiline Rasagiline may increase the serotonergic activities of Hydromorphone.
Pargyline Pargyline may increase the serotonergic activities of Hydromorphone.
Minaprine Minaprine may increase the serotonergic activities of Hydromorphone.
Iproniazid Iproniazid may increase the serotonergic activities of Hydromorphone.
Nialamide Nialamide may increase the serotonergic activities of Hydromorphone.
Pirlindole Pirlindole may increase the serotonergic activities of Hydromorphone.
Toloxatone Toloxatone may increase the serotonergic activities of Hydromorphone.
Hydracarbazine Hydracarbazine may increase the serotonergic activities of Hydromorphone.
Benmoxin Benmoxin may increase the serotonergic activities of Hydromorphone.
Mebanazine Mebanazine may increase the serotonergic activities of Hydromorphone.
Octamoxin Octamoxin may increase the serotonergic activities of Hydromorphone.
Pheniprazine Pheniprazine may increase the serotonergic activities of Hydromorphone.
Phenoxypropazine Phenoxypropazine may increase the serotonergic activities of Hydromorphone.
Pivhydrazine Pivhydrazine may increase the serotonergic activities of Hydromorphone.
Safrazine Safrazine may increase the serotonergic activities of Hydromorphone.
Caroxazone Caroxazone may increase the serotonergic activities of Hydromorphone.
Furazolidone Furazolidone may increase the serotonergic activities of Hydromorphone.
7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline 7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline may increase the serotonergic activities of Hydromorphone.
Harmaline Harmaline may increase the serotonergic activities of Hydromorphone.
Brofaromine Brofaromine may increase the serotonergic activities of Hydromorphone.
Procaine Procaine may increase the serotonergic activities of Hydromorphone.
Procarbazine Procarbazine may increase the serotonergic activities of Hydromorphone.
Safinamide Safinamide may increase the serotonergic activities of Hydromorphone.
Clorgiline Clorgiline may increase the serotonergic activities of Hydromorphone.
Linezolid Linezolid may increase the serotonergic activities of Hydromorphone.
Mirtazapine Hydromorphone may increase the serotonergic activities of Mirtazapine.

Target Protein

Mu-type opioid receptor OPRM1
Delta-type opioid receptor OPRD1
Kappa-type opioid receptor OPRK1

Referensi & Sumber

Artikel (PubMed)
  • PMID: 29261877
    Abi-Aad KR, Derian A: Hydromorphone .
  • PMID: 18261371
    Kumar MG, Lin S: Hydromorphone in the management of cancer-related pain: an update on routes of administration and dosage forms. J Pharm Pharm Sci. 2007;10(4):504-18.
  • PMID: 18443637
    Trescot AM, Datta S, Lee M, Hansen H: Opioid pharmacology. Pain Physician. 2008 Mar;11(2 Suppl):S133-53.
  • PMID: 21999760
    Overholser BR, Foster DR: Opioid pharmacokinetic drug-drug interactions. Am J Manag Care. 2011 Sep;17 Suppl 11:S276-87.
  • PMID: 15268978
    Benetton SA, Borges VM, Chang TK, McErlane KM: Role of individual human cytochrome P450 enzymes in the in vitro metabolism of hydromorphone. Xenobiotica. 2004 Apr;34(4):335-44. doi: 10.1080/00498250310001657559 .
  • PMID: 22554450
    Drewes AM, Jensen RD, Nielsen LM, Droney J, Christrup LL, Arendt-Nielsen L, Riley J, Dahan A: Differences between opioids: pharmacological, experimental, clinical and economical perspectives. Br J Clin Pharmacol. 2013 Jan;75(1):60-78. doi: 10.1111/j.1365-2125.2012.04317.x.
  • PMID: 15907647
    Murray A, Hagen NA: Hydromorphone. J Pain Symptom Manage. 2005 May;29(5 Suppl):S57-66. doi: 10.1016/j.jpainsymman.2005.01.007.
  • PMID: 23973378
    Perlman R, Giladi H, Brecht K, Ware MA, Hebert TE, Joseph L, Shir Y: Intradialytic clearance of opioids: methadone versus hydromorphone. Pain. 2013 Dec;154(12):2794-800. doi: 10.1016/j.pain.2013.08.015. Epub 2013 Aug 20.

Contoh Produk & Brand

Produk: 277 • International brands: 0
Produk
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