Opium

Identification

Summary

Opium is a medication used to treat moderate to severe pain.

Generic Name
Opium
DrugBank Accession Number
DB11130
Background

Opium is the first substance of the diverse group of the opiates. It has been known for a long time, and the first evidence of a poppy culture dates from 5 thousand years by the Sumerians. During the years, opium was used as a sedative and hypnotic, but it was determined to be addictive.1

Opium is extracted from Papaver somniferum, which is more known as poppies. This plant is an integrant of the Papaveraceae family, and it is characterized by solitary leaves and capsulated fruits. Therefore, opium is a sticky brown resin obtained by collecting and drying the latex that exudes from the poppy pods.13

Once extracted, opium contains two main groups of alkaloids; the psychoactive constituents which are in the category of phenanthrenes and alkaloids that have no central nervous system effect in the category of isoquinolines. Morphine is the most prevalent and principal alkaloid in opium, and it is responsible for most of the harmful effects of opium.14

Opium has gradually been superseded by a variety of synthetic opioids and general anesthetics. Some of the isolated derivatives of opium are morphine, noscapine, strychnine, veratrine, colchicine, codeine, and quinine.2 Opium is a prohibited drug of abuse in most countries, but the illegal production of this drug and its derivatives keeps being registered. There is some legal production of opium in different countries for the obtention of alkaloids by extraction.15

Type
Small Molecule
Groups
Approved, Illicit
Synonyms
  • Opio
  • Opium
  • Papaver somniferum exudate
  • Papaver somniferum resin
External IDs
  • IDS-NO-001

Pharmacology

Indication

Opium and its derivatives are the most commonly used medications for the treatment of acute and chronic pain. Opium and its alkaloid-derivatives can also be used as tranquilizers, antitussives and in the treatment of diarrhea.11 The direct use of opium is not common nowadays but the use of some of its derivatives such as morphine and codeine, as well as the use of a tincture of opium for severe diarrhea can be seen in medical practice.12

Illegal use of opium has been registered to be for both recreational and medicinal purposes.3

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Associated Conditions
Indication TypeIndicationCombined Product DetailsApproval LevelAge GroupPatient CharacteristicsDose Form
Treatment ofSevere diarrhea•••••••••••••••••••••• •••••••• •• ••••••••••••••••• • •••••
Contraindications & Blackbox Warnings
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Pharmacodynamics

Opioids can reduce the intensity and unpleasant feeling of pain. The unspecific effect of opium to the different opioid receptors produce the generation of various effects such as sedation, euphoria, dysphoria, respiratory depression, constipation, pruritus, nausea, and vomiting. It is reported that the secondary effects tend to be diminished as long-term use tolerance is developed. Some reports have also shown an opioid-driven impairment of the hypothalamic function that can result in a loss of libido, impotence, and infertility. Patients have reported a sensation of stress relief even in presence of pain as well as the presence of sedation, hypoventilation, cough inhibition, prolonged apnea, myosis and respiratory obstruction.9

In the cardiovascular system, there are reports of peripheral vasodilatation, including cutaneous causing flushing of the face, neck, and thorax, impaired sympathetic reflexes and postural hypotension. In the gastrointestinal and urogenital system, the increase in smooth muscle tone has been shown to produce reduced peristalsis, delayed gastric emptying and urinary retention.9

Mechanism of action

Opium produces its effects by activating specific G protein-coupled receptors in the brain, spinal cord, and peripheral nervous system. There are three major classes of opioid receptors being δ-opioid, κ-opioid and μ-opioid. Opium will generate an agonist activity which will later open the potassium channels and prevent the opening of voltage-gated calcium channels. This activity causes a reduction in neuronal excitability and inhibits the release of pain neurotransmitters.9

The addictive character of opium is related to the binding to the μ-opioid receptors, which will activate dopaminergic neurons in the ventral tegmental area of the midbrain and thus, enhance the dopamine release in the nucleus accumbens. This mechanism involves the reward activity of the mesolimbic dopaminergic pathway.10

TargetActionsOrganism
ADelta-type opioid receptor
agonist
Humans
AKappa-type opioid receptor
agonist
Humans
AMu-type opioid receptor
agonist
Humans
Absorption

After oral administration, opium bioavailability is poor.9 In the form of opioid tincture, the Cmax and AUC of opium are between 16-24 mg/ml and 3237-6727 ng/ml.h, respectively.4

Volume of distribution

Opium presents a large volume of distribution that exceeds the total body water.9

Protein binding

The protein binding of the alkaloids that form opium, such as morphine and codeine, can range from 20-60% depending on the specific alkaloid. The highest binding proteins for opium alkaloids are albumin and beta-globulin II.5

Metabolism

Opium contains 50 different alkaloid opiates. The most common metabolism of opiates is to be ultimately converted to morphine which is further converted to morphine-3,6-diglucuronide.16 Opioids are metabolized vastly by the enzyme CYP 2D6 and any mutation in this kind of enzyme or coadministration with drugs that interfere with this enzyme may generate a change in the metabolism speed.18 For years, because of this metabolism pathway, it was very hard to differentiate between illicit heroin users and involuntary exposure to poppy seeds. The original tests for this differentiations were based in the presence of morphine in urine without evidence of 6-monoacetylmorphine. Now it is known the presence of a glucuronide metabolite only in the consumption of heroin called ATM4G and this allows a clear differentiation of the consumption of illegal heroin and poppy seed ingestion.6

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Route of elimination

Opium is a mixture of different alkaloids including morphine and codeine. After a single ingestion of opium preparations, codeine and morphine can be found excreted in urine. The presence of codeine and morphine in urine seems to be detectable 2-12 hours and 2-36 hours post administration, respectively. The urinary excretion of morphine and codeine seems to be longer as the dose of opium is increased. After multiple dosages of opium, the presence of codeine and morphine in urine could be detected even after 48 and 84 hours post administration, respectively.7 After ingestion of poppy seeds, it is possible to collect morphine and codeine in urine 3-25 hours and 3-22 hours after administration, respectively.8

Half-life

The half-life of opium ranges between 3-10 hours.9

Clearance

Not Available

Adverse Effects
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Toxicity

Some toxicity concerns from the consumption of opium are the generation of addiction, physical dependence and tolerance to the effect. Studies regarding the opioid tolerance in the treatment of chronic pain have not been systematically investigated. There are also concerns about the opioid-driven modification of endocrine function, currently reported as lower testosterone levels, loss of libido, amenorrhea and infertility.17

Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
DrugInteraction
1,2-BenzodiazepineThe risk or severity of adverse effects can be increased when Opium is combined with 1,2-Benzodiazepine.
AbacavirAbacavir may decrease the excretion rate of Opium which could result in a higher serum level.
AbametapirThe serum concentration of Opium can be increased when it is combined with Abametapir.
AbataceptThe metabolism of Opium can be increased when combined with Abatacept.
AbirateroneThe metabolism of Opium can be decreased when combined with Abiraterone.
Food Interactions
  • Avoid alcohol. Concomitant use of opium with alcohol may cause additive CNS depressive effects.

Products

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dosage, form, labeller, route of administration, and marketing period.
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Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
Opium TeintureTincture200 g / 1 LOralLaboratoire Atlas Inc1951-12-311996-09-09Canada flag
Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing EndRegionImage
Camphorated Opium TinctureOpium (5 mL / 100 mL) + Benzoic acid (500 mg / 100 mL) + Camphor (300 mg / 100 mL)TinctureOralD.C. Labs Limited1951-12-312003-07-11Canada flag
Diban CapOpium (12 mg) + Atropine sulfate (9.7 mcg) + Attapulgite (300 mg) + Hyoscyamine sulfate (0.0519 mg) + Pectin (71.4 mg) + Scopolamine (3.3 mcg)CapsuleOralWyeth Ayerst Canada Inc.1998-02-182001-01-30Canada flag
Diban CapOpium (12 mg) + Atropine sulfate (9.7 mcg) + Attapulgite (300 mg) + Hyoscyamine sulfate (0.0519 mg) + Pectin (71.4 mg) + Scopolamine (3.3 mcg)CapsuleOralAyerst Laboratories1992-12-311999-04-12Canada flag
Donnagel-PG CapOpium (12 mg / cap) + Attapulgite (300 mg / cap) + Pectin (71.4 mg / cap)CapsuleOralWyeth Ayerst Canada Inc.1994-12-312002-03-20Canada flag
Donnagel-PG LiqOpium (24 mg / 30 mL) + Kaolin (6 g / 30 mL) + Pectin (142.8 mg / 30 mL)LiquidOralWyeth Ayerst Canada Inc.1994-12-312001-04-23Canada flag
Unapproved/Other Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing EndRegionImage
Belladonna and OpiumOpium (30 mg/1) + Belladonna (16.2 mg/1)SuppositoryRectalLegacy Pharma Inc.2020-04-29Not applicableUS flag
Belladonna and OpiumOpium (60 mg/1) + Belladonna (16.2 mg/1)SuppositoryRectalPadagis US LLC1997-04-22Not applicableUS flag
Belladonna and OpiumOpium (30 mg/1) + Belladonna (16.2 mg/1)SuppositoryRectalbryant ranch prepack1994-05-01Not applicableUS flag
Belladonna and OpiumOpium (60 mg/1) + Belladonna (16.2 mg/1)SuppositoryRectalLegacy Pharma Inc.2020-04-29Not applicableUS flag
Belladonna and OpiumOpium (30 mg/1) + Belladonna (16.2 mg/1)SuppositoryRectalbryant ranch prepack1994-05-01Not applicableUS flag

Categories

ATC Codes
A07DA02 — OpiumN02AA02 — Opium
Drug Categories
Classification
Not classified
Affected organisms
  • Humans and other mammals

Chemical Identifiers

UNII
37M3MZ001L
CAS number
8008-60-4

References

General References
  1. Duarte DF: [Opium and opioids: a brief history.]. Rev Bras Anestesiol. 2005 Feb;55(1):135-46. [Article]
  2. Huxtable RJ, Schwarz SK: The isolation of morphine--first principles in science and ethics. Mol Interv. 2001 Oct;1(4):189-91. [Article]
  3. Lee S, Park Y, Han E, Choi H, Chung H, Oh SM, Chung KH: Thebaine in hair as a marker for chronic use of illegal opium poppy substances. Forensic Sci Int. 2011 Jan 30;204(1-3):115-8. doi: 10.1016/j.forsciint.2010.05.013. Epub 2010 Jun 16. [Article]
  4. Somogyi AA, Larsen M, Abadi RM, Jittiwutikarn J, Ali R, White JM: Flexible dosing of tincture of opium in the management of opioid withdrawal: pharmacokinetics and pharmacodynamics. Br J Clin Pharmacol. 2008 Nov;66(5):640-7. doi: 10.1111/j.1365-2125.2008.03277.x. [Article]
  5. Judis J: Binding of codeine, morphine, and methadone to human serum proteins. J Pharm Sci. 1977 Jun;66(6):802-6. [Article]
  6. Chen P, Braithwaite RA, George C, Hylands PJ, Parkin MC, Smith NW, Kicman AT: The poppy seed defense: a novel solution. Drug Test Anal. 2014 Mar;6(3):194-201. doi: 10.1002/dta.1590. Epub 2013 Dec 12. [Article]
  7. Liu HC, Ho HO, Liu RH, Yeh GC, Lin DL: Urinary excretion of morphine and codeine following the administration of single and multiple doses of opium preparations prescribed in Taiwan as "brown mixture". J Anal Toxicol. 2006 May;30(4):225-31. [Article]
  8. Struempler RE: Excretion of codeine and morphine following ingestion of poppy seeds. J Anal Toxicol. 1987 May-Jun;11(3):97-9. [Article]
  9. Lee M. and Abrahams M. (2012). Clinical pharmacology (11th ed.). Churchill Livingstone.
  10. Michael-Titus A., Revest P. and Shortland P. (2010). The nervous system (2nd ed.). Churchill Livingstone.
  11. Hanna M., Ouanes J. and Garcia V. (2014). Practical Management of Pain (5th ed.). Mosby.
  12. Le Coutuer P. and Burreson J. (2003). Napoleon's Buttons: 17 molecules that changed history. Tarcher.
  13. Chemical and engineering news [Link]
  14. Encyclopedia [Link]
  15. WHO [Link]
  16. NZIC [Link]
  17. FDA Reports [Link]
  18. Health partners [Link]
PubChem Substance
347911129
RxNav
7676
Wikipedia
Opium
MSDS
Download (252 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4CompletedTreatmentHysterectomy / Postoperative pain1
4CompletedTreatmentKidney Stones1
4CompletedTreatmentNeonatal drug withdrawal syndrome1
4CompletedTreatmentVaginal Surgery1
4TerminatedTreatmentOveractive Bladder Syndrome (OABS)1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
FormRouteStrength
SuppositoryRectal
TinctureOral
CapsuleOral
LiquidOral
Solution / dropsOral
TabletOral
TinctureOral200 g / 1 L
Prices
Not Available
Patents
Not Available

Properties

State
Liquid
Experimental Properties
PropertyValueSource
boiling point (°C)73.3ºC (Opium 2% tincture)'MSDS'
water solubilitySoluble (Opium 2% tincture)'MSDS'
Predicted Properties
Not Available
Predicted ADMET Features
Not Available

Spectra

Mass Spec (NIST)
Not Available
Spectra
Not Available
Chromatographic Properties
Collision Cross Sections (CCS)
Not Available

Targets

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Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Agonist
General Function
Opioid receptor activity
Specific Function
G-protein coupled receptor that functions as receptor for endogenous enkephalins and for a subset of other opioids. Ligand binding causes a conformation change that triggers signaling via guanine n...
Gene Name
OPRD1
Uniprot ID
P41143
Uniprot Name
Delta-type opioid receptor
Molecular Weight
40368.235 Da
References
  1. Lee M. and Abrahams M. (2012). Clinical pharmacology (11th ed.). Churchill Livingstone.
  2. Michael-Titus A., Revest P. and Shortland P. (2010). The nervous system (2nd ed.). Churchill Livingstone.
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Agonist
General Function
Opioid receptor activity
Specific Function
G-protein coupled opioid receptor that functions as receptor for endogenous alpha-neoendorphins and dynorphins, but has low affinity for beta-endorphins. Also functions as receptor for various synt...
Gene Name
OPRK1
Uniprot ID
P41145
Uniprot Name
Kappa-type opioid receptor
Molecular Weight
42644.665 Da
References
  1. Lee M. and Abrahams M. (2012). Clinical pharmacology (11th ed.). Churchill Livingstone.
  2. Michael-Titus A., Revest P. and Shortland P. (2010). The nervous system (2nd ed.). Churchill Livingstone.
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Agonist
General Function
Voltage-gated calcium channel activity
Specific Function
Receptor for endogenous opioids such as beta-endorphin and endomorphin. Receptor for natural and synthetic opioids including morphine, heroin, DAMGO, fentanyl, etorphine, buprenorphin and methadone...
Gene Name
OPRM1
Uniprot ID
P35372
Uniprot Name
Mu-type opioid receptor
Molecular Weight
44778.855 Da
References
  1. Lee M. and Abrahams M. (2012). Clinical pharmacology (11th ed.). Churchill Livingstone.
  2. Michael-Titus A., Revest P. and Shortland P. (2010). The nervous system (2nd ed.). Churchill Livingstone.

Enzymes

Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Substrate
General Function
Steroid hydroxylase activity
Specific Function
Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic...
Gene Name
CYP2D6
Uniprot ID
P10635
Uniprot Name
Cytochrome P450 2D6
Molecular Weight
55768.94 Da
References
  1. Health partners [Link]
Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Substrate
General Function
Vitamin d3 25-hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
Gene Name
CYP3A4
Uniprot ID
P08684
Uniprot Name
Cytochrome P450 3A4
Molecular Weight
57342.67 Da
References
  1. Gesell A, Rolf M, Ziegler J, Diaz Chavez ML, Huang FC, Kutchan TM: CYP719B1 is salutaridine synthase, the C-C phenol-coupling enzyme of morphine biosynthesis in opium poppy. J Biol Chem. 2009 Sep 4;284(36):24432-42. doi: 10.1074/jbc.M109.033373. Epub 2009 Jun 30. [Article]

Carriers

Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Binder
General Function
Toxic substance binding
Specific Function
Serum albumin, the main protein of plasma, has a good binding capacity for water, Ca(2+), Na(+), K(+), fatty acids, hormones, bilirubin and drugs. Its main function is the regulation of the colloid...
Gene Name
ALB
Uniprot ID
P02768
Uniprot Name
Serum albumin
Molecular Weight
69365.94 Da
References
  1. Judis J: Binding of codeine, morphine, and methadone to human serum proteins. J Pharm Sci. 1977 Jun;66(6):802-6. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Binder
General Function
Identical protein binding
Specific Function
Component of the class I major histocompatibility complex (MHC). Involved in the presentation of peptide antigens to the immune system.
Gene Name
B2M
Uniprot ID
P61769
Uniprot Name
Beta-2-microglobulin
Molecular Weight
13714.43 Da
References
  1. Judis J: Binding of codeine, morphine, and methadone to human serum proteins. J Pharm Sci. 1977 Jun;66(6):802-6. [Article]

Drug created at December 03, 2015 16:51 / Updated at March 18, 2024 16:48