Peringatan Keamanan

Overdosage with diamorphine well characterised by a number of symptoms including respiratory depression, pulmonary oedema, muscle flaccidity, coma or stupor, constricted pupils, cold, clammy skin and occasionally bradycardia and hypotension L4996, L4999. The antidote for heroin overdose or poisoning is naloxone L4996.

Diamorphine

DB01452

small molecule approved illicit investigational

Deskripsi

Diamorphine (heroin) is a narcotic analgesic that may be habit-forming. It is a controlled substance (opium derivative) listed in the U.S. Code of Federal Regulations, Title 21 Parts 329.1, 1308.11 (1987). Sale is forbidden in the United States by Federal statute. (Merck Index, 11th ed) Internationally, diamorphine is controlled under Schedules I and IV of the Single Convention on Narcotic Drugs. As heroin, it is illegal to manufacture, possess, or sell in the United States and the UK. However, under the name diamorphine, heroin is a legal prescription drug in the United Kingdom.

Struktur Molekul 2D

Berat 369.411
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) In humans, administered diamorphine has a half-life of approximately two to three minutes [L4999].
Volume Distribusi Data regarding the volume of distribution specific to diamorphine is not readily accessible or available. However, considering diamorphine is considered a prodrug for morphine, the volume of distribution of morphine has been determined to be approximately 1 to 6 L/kg [F2857].
Klirens (Clearance) Some studies have determined a relatively high systemic diacetylmorphine clearance of about 8.7 +/- 2.6 L/min, suggesting that the intestine, liver, and blood might all collectively take part in the first pass metabolism of diacetylmorphine to morphine [A173683], although such clearance observations were made only in opioid-addicted individuals [A173695]. However, considering diamorphine is considered a prodrug for morphine, the mean adult plasma clearance of morphine is approximately 20 to 30 mL/min/kg [F2857].

Absorpsi

Bioavailability is less than 35% when orally administered A173668. In particular, some studies have determined that the bioavailability of orally administered diamorphine could be as low as 22.9% (16.4-29.4%) on average in opioid-naive subjects A173683. Nevertheless, diamorphine administered by any many medically indicated routes of administration leads to a rapid absorption L4996. Peak serum levels are achieved five to ten minutes subcutaneously, three to five minutes intranasally and intramuscularly, and less than one minute intravenously L4996.

Metabolisme

Once administered into the body, diamorphine undergoes deacetylation via various esterase enzymes to generate active metabolites like 6-monoacetylmorphine and morphine L4996, L4999. In particular, when administered orally, diamorphine undergoes extensive first pass metabolism L4996, L4999.

Rute Eliminasi

The majority of the drug is excreted via the kidney as glucuronides and to a much lesser extent as morphine L4999. About 7-10 % is eliminated via the biliary system into the faeces L4999.

Interaksi Makanan

1 Data
  • 1. Avoid alcohol.

Interaksi Obat

918 Data
Buprenorphine Diamorphine 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 Diamorphine.
Dronabinol Dronabinol may increase the central nervous system depressant (CNS depressant) activities of Diamorphine.
Droperidol Droperidol may increase the central nervous system depressant (CNS depressant) activities of Diamorphine.
Hydrocodone Diamorphine 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 Diamorphine.
Magnesium sulfate The therapeutic efficacy of Diamorphine can be increased when used in combination with Magnesium sulfate.
Methotrimeprazine Diamorphine may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
Metyrosine Diamorphine may increase the sedative activities of Metyrosine.
Minocycline Minocycline may increase the central nervous system depressant (CNS depressant) activities of Diamorphine.
Mirtazapine Diamorphine 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 Diamorphine.
Orphenadrine Diamorphine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
Paraldehyde Diamorphine 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 Diamorphine.
Pramipexole Diamorphine may increase the sedative activities of Pramipexole.
Ropinirole Diamorphine may increase the sedative activities of Ropinirole.
Rotigotine Diamorphine may increase the sedative activities of Rotigotine.
Rufinamide The risk or severity of adverse effects can be increased when Rufinamide is combined with Diamorphine.
Sodium oxybate The risk or severity of CNS depression can be increased when Diamorphine is combined with Sodium oxybate.
Suvorexant Diamorphine 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 Diamorphine.
Thalidomide Diamorphine may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
Zolpidem Diamorphine may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
Alvimopan The risk or severity of adverse effects can be increased when Diamorphine is combined with Alvimopan.
Desmopressin The risk or severity of hyponatremia can be increased when Diamorphine is combined with Desmopressin.
Morphine The risk or severity of adverse effects can be increased when Morphine is combined with Diamorphine.
Codeine The risk or severity of adverse effects can be increased when Codeine is combined with Diamorphine.
Hydromorphone The risk or severity of adverse effects can be increased when Hydromorphone is combined with Diamorphine.
Meperidine The risk or severity of adverse effects can be increased when Meperidine is combined with Diamorphine.
Oxycodone The risk or severity of adverse effects can be increased when Oxycodone is combined with Diamorphine.
Dextropropoxyphene The risk or severity of adverse effects can be increased when Dextropropoxyphene is combined with Diamorphine.
Naltrexone The therapeutic efficacy of Diamorphine can be decreased when used in combination with Naltrexone.
Sufentanil The risk or severity of adverse effects can be increased when Sufentanil is combined with Diamorphine.
Alfentanil The risk or severity of adverse effects can be increased when Alfentanil is combined with Diamorphine.
Fentanyl The risk or severity of adverse effects can be increased when Fentanyl is combined with Diamorphine.
Levorphanol The risk or severity of adverse effects can be increased when Levorphanol is combined with Diamorphine.
Remifentanil The risk or severity of adverse effects can be increased when Remifentanil is combined with Diamorphine.
Diphenoxylate The risk or severity of adverse effects can be increased when Diphenoxylate is combined with Diamorphine.
Oxymorphone The risk or severity of adverse effects can be increased when Oxymorphone is combined with Diamorphine.
Dezocine The risk or severity of adverse effects can be increased when Dezocine is combined with Diamorphine.
Methadyl acetate The risk or severity of adverse effects can be increased when Methadyl acetate is combined with Diamorphine.
Dihydroetorphine The risk or severity of adverse effects can be increased when Dihydroetorphine is combined with Diamorphine.
Bezitramide The risk or severity of adverse effects can be increased when Diamorphine is combined with Bezitramide.
Ethylmorphine The risk or severity of adverse effects can be increased when Diamorphine is combined with Ethylmorphine.
Etorphine The risk or severity of adverse effects can be increased when Diamorphine is combined with Etorphine.
Dextromoramide The risk or severity of adverse effects can be increased when Diamorphine is combined with Dextromoramide.
Desomorphine The risk or severity of adverse effects can be increased when Diamorphine is combined with Desomorphine.
Carfentanil The risk or severity of adverse effects can be increased when Diamorphine is combined with Carfentanil.
Dihydrocodeine The risk or severity of adverse effects can be increased when Diamorphine is combined with Dihydrocodeine.
Alphacetylmethadol The risk or severity of adverse effects can be increased when Diamorphine is combined with Alphacetylmethadol.
Dihydromorphine The risk or severity of adverse effects can be increased when Diamorphine is combined with Dihydromorphine.
Ketobemidone The risk or severity of adverse effects can be increased when Diamorphine is combined with Ketobemidone.
DPDPE The risk or severity of adverse effects can be increased when Diamorphine is combined with DPDPE.
Lofentanil The risk or severity of adverse effects can be increased when Diamorphine is combined with Lofentanil.
Opium The risk or severity of adverse effects can be increased when Diamorphine is combined with Opium.
Normethadone The risk or severity of adverse effects can be increased when Diamorphine is combined with Normethadone.
Piritramide The risk or severity of adverse effects can be increased when Diamorphine is combined with Piritramide.
Alphaprodine The risk or severity of adverse effects can be increased when Diamorphine is combined with Alphaprodine.
Nicomorphine The risk or severity of adverse effects can be increased when Diamorphine is combined with Nicomorphine.
Meptazinol The therapeutic efficacy of Diamorphine can be decreased when used in combination with Meptazinol.
Phenoperidine The risk or severity of adverse effects can be increased when Diamorphine is combined with Phenoperidine.
Phenazocine The risk or severity of adverse effects can be increased when Diamorphine is combined with Phenazocine.
Tilidine The risk or severity of adverse effects can be increased when Diamorphine is combined with Tilidine.
Carfentanil, C-11 The risk or severity of adverse effects can be increased when Diamorphine is combined with Carfentanil, C-11.
Naloxegol The risk or severity of adverse effects can be increased when Diamorphine is combined with Naloxegol.
Benzhydrocodone The risk or severity of adverse effects can be increased when Diamorphine is combined with Benzhydrocodone.
Pegvisomant The therapeutic efficacy of Pegvisomant can be decreased when used in combination with Diamorphine.
Succinylcholine The risk or severity of bradycardia can be increased when Succinylcholine is combined with Diamorphine.
Methadone The risk or severity of adverse effects can be increased when Methadone is combined with Diamorphine.
Fluvoxamine The risk or severity of serotonin syndrome can be increased when Diamorphine is combined with Fluvoxamine.
Citalopram The risk or severity of serotonin syndrome can be increased when Diamorphine is combined with Citalopram.
Duloxetine The risk or severity of serotonin syndrome can be increased when Diamorphine is combined with Duloxetine.
Trazodone The risk or severity of serotonin syndrome can be increased when Diamorphine is combined with Trazodone.
Paroxetine The risk or severity of serotonin syndrome can be increased when Diamorphine is combined with Paroxetine.
Sertraline The risk or severity of serotonin syndrome can be increased when Diamorphine is combined with Sertraline.
Sibutramine The risk or severity of serotonin syndrome can be increased when Diamorphine is combined with Sibutramine.
Nefazodone The risk or severity of serotonin syndrome can be increased when Diamorphine is combined with Nefazodone.
Escitalopram The risk or severity of serotonin syndrome can be increased when Diamorphine is combined with Escitalopram.
Zimelidine The risk or severity of serotonin syndrome can be increased when Diamorphine is combined with Zimelidine.
Dapoxetine The risk or severity of serotonin syndrome can be increased when Diamorphine is combined with Dapoxetine.
Milnacipran The risk or severity of serotonin syndrome can be increased when Diamorphine is combined with Milnacipran.
Desvenlafaxine The risk or severity of serotonin syndrome can be increased when Diamorphine is combined with Desvenlafaxine.
Seproxetine The risk or severity of serotonin syndrome can be increased when Diamorphine is combined with Seproxetine.
Indalpine The risk or severity of serotonin syndrome can be increased when Diamorphine is combined with Indalpine.
Ritanserin The risk or severity of serotonin syndrome can be increased when Diamorphine is combined with Ritanserin.
Alaproclate The risk or severity of serotonin syndrome can be increased when Diamorphine is combined with Alaproclate.
Ethanol Diamorphine may increase the central nervous system depressant (CNS depressant) activities of Ethanol.
Azelastine Diamorphine 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 Diamorphine.
Phentermine Phentermine may increase the analgesic activities of Diamorphine.
Pseudoephedrine Pseudoephedrine may increase the analgesic activities of Diamorphine.
Benzphetamine Benzphetamine may increase the analgesic activities of Diamorphine.
Diethylpropion Diethylpropion may increase the analgesic activities of Diamorphine.
Lisdexamfetamine Lisdexamfetamine may increase the analgesic activities of Diamorphine.
Mephentermine Mephentermine may increase the analgesic activities of Diamorphine.
MMDA MMDA may increase the analgesic activities of Diamorphine.
Midomafetamine Midomafetamine may increase the analgesic activities of Diamorphine.
2,5-Dimethoxy-4-ethylamphetamine 2,5-Dimethoxy-4-ethylamphetamine may increase the analgesic activities of Diamorphine.
4-Bromo-2,5-dimethoxyamphetamine 4-Bromo-2,5-dimethoxyamphetamine may increase the analgesic activities of Diamorphine.

Target Protein

Mu-type opioid receptor OPRM1
Kappa-type opioid receptor OPRK1
Delta-type opioid receptor OPRD1
Liver carboxylesterase 1 CES1

Referensi & Sumber

Artikel (PubMed)
  • PMID: 12404073
    Tschacher W, Haemmig R, Jacobshagen N: Time series modeling of heroin and morphine drug action. Psychopharmacology (Berl). 2003 Jan;165(2):188-93. Epub 2002 Oct 29.
  • PMID: 16433897
    Rook EJ, van Ree JM, van den Brink W, Hillebrand MJ, Huitema AD, Hendriks VM, Beijnen JH: Pharmacokinetics and pharmacodynamics of high doses of pharmaceutically prepared heroin, by intravenous or by inhalation route in opioid-dependent patients. Basic Clin Pharmacol Toxicol. 2006 Jan;98(1):86-96. doi: 10.1111/j.1742-7843.2006.pto_233.x.
  • PMID: 18945270
    Halbsguth U, Rentsch KM, Eich-Hochli D, Diterich I, Fattinger K: Oral diacetylmorphine (heroin) yields greater morphine bioavailability than oral morphine: bioavailability related to dosage and prior opioid exposure. Br J Clin Pharmacol. 2008 Dec;66(6):781-91. doi: 10.1111/j.1365-2125.2008.03286.x.
  • PMID: 11557911
    Rentsch KM, Kullak-Ublick GA, Reichel C, Meier PJ, Fattinger K: Arterial and venous pharmacokinetics of intravenous heroin in subjects who are addicted to narcotics. Clin Pharmacol Ther. 2001 Sep;70(3):237-46. doi: 10.1067/mcp.2001.117981.

Contoh Produk & Brand

Produk: 4 • International brands: 0
Produk
  • Diacetylmorphine Hydrochloride
    Powder, for solution • 200 mg / vial • Intramuscular; Intravenous • Canada • Approved
  • Diacetylmorphine Hydrochloride
    Powder, for solution • 5000 mg / vial • Intramuscular; Intravenous • Canada • Approved
  • Diamorphine Hydrochloride Inj 100mg/ml BP
    Powder, for solution • 100 mg / mL • Intramuscular; Intravenous; Subcutaneous • Canada • Approved
  • Diamorphine Hydrochloride Inj 30mg/ml BP
    Powder, for solution • 30 mg / mL • Intramuscular; Intravenous; Subcutaneous • Canada • Approved

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