Opium

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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Opium has gradually been superseded by a variety of synthetic opioids and general anesthetics.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

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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 Type	Indication	Combined Product Details	Approval Level	Age Group	Patient Characteristics	Dose Form
Treatment of	Severe diarrhea		••••••••••••		•••••••••• •••••••• •• •••••••••	•••••••• • •••••

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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

Target	Actions	Organism
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

Hover over products below to view reaction partners

• Opium
  • 6-Monoacetylmorphine
    • morphine
      • Morphine glucuronide + morphine-3-glucuronide
        • morphine-3,6-diglucuronide
        • morphine-3,6-diglucuronide

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.

• Approved
• Vet approved
• Nutraceutical
• Illicit
• Withdrawn
• Investigational
• Experimental
• All Drugs

Drug	Interaction
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1,2-Benzodiazepine	The risk or severity of adverse effects can be increased when Opium is combined with 1,2-Benzodiazepine.
Abacavir	Abacavir may decrease the excretion rate of Opium which could result in a higher serum level.
Abametapir	The serum concentration of Opium can be increased when it is combined with Abametapir.
Abatacept	The metabolism of Opium can be increased when combined with Abatacept.
Abiraterone	The 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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Brand Name Prescription Products

Name	Dosage	Strength	Route	Labeller	Marketing Start	Marketing End	Region	Image
Opium Teinture	Tincture	200 g / 1 L	Oral	Laboratoire Atlas Inc	1951-12-31	1996-09-09

Mixture Products

Name	Ingredients	Dosage	Route	Labeller	Marketing Start	Marketing End	Region	Image
Camphorated Opium Tincture	Opium (5 mL / 100 mL) + Benzoic acid (500 mg / 100 mL) + Camphor (300 mg / 100 mL)	Tincture	Oral	D.C. Labs Limited	1951-12-31	2003-07-11
Diban Cap	Opium (12 mg) + Atropine sulfate (9.7 mcg) + Attapulgite (300 mg) + Hyoscyamine sulfate (0.0519 mg) + Pectin (71.4 mg) + Scopolamine (3.3 mcg)	Capsule	Oral	Ayerst Laboratories	1992-12-31	1999-04-12
Diban Cap	Opium (12 mg) + Atropine sulfate (9.7 mcg) + Attapulgite (300 mg) + Hyoscyamine sulfate (0.0519 mg) + Pectin (71.4 mg) + Scopolamine (3.3 mcg)	Capsule	Oral	Wyeth Ayerst Canada Inc.	1998-02-18	2001-01-30
Donnagel-PG Cap	Opium (12 mg / cap) + Attapulgite (300 mg / cap) + Pectin (71.4 mg / cap)	Capsule	Oral	Wyeth Ayerst Canada Inc.	1994-12-31	2002-03-20
Donnagel-PG Liq	Opium (24 mg / 30 mL) + Kaolin (6 g / 30 mL) + Pectin (142.8 mg / 30 mL)	Liquid	Oral	Wyeth Ayerst Canada Inc.	1994-12-31	2001-04-23

Unapproved/Other Products

Name	Ingredients	Dosage	Route	Labeller	Marketing Start	Marketing End	Region	Image
Belladonna and Opium	Opium (30 mg/1) + Belladonna (16.2 mg/1)	Suppository	Rectal	bryant ranch prepack	1994-05-01	Not applicable
Belladonna and Opium	Opium (30 mg/1) + Belladonna (16.2 mg/1)	Suppository	Rectal	Padagis US LLC	1994-05-01	Not applicable
Belladonna and Opium	Opium (30 mg/1) + Belladonna (16.2 mg/1)	Suppository	Rectal	Legacy Pharma Inc.	2020-04-29	Not applicable
Belladonna and Opium	Opium (60 mg/1) + Belladonna (16.2 mg/1)	Suppository	Rectal	Padagis US LLC	1997-04-22	Not applicable
Belladonna and Opium	Opium (30 mg/1) + Belladonna (16.2 mg/1)	Suppository	Rectal	bryant ranch prepack	1994-05-01	Not applicable

Categories

ATC Codes

A07DA02 — Opium

• A07DA — Antipropulsives
• A07D — ANTIPROPULSIVES
• A07 — ANTIDIARRHEALS, INTESTINAL ANTIINFLAMMATORY/ANTIINFECTIVE AGENTS
• A — ALIMENTARY TRACT AND METABOLISM

N02AA02 — Opium

• N02AA — Natural opium alkaloids
• N02A — OPIOIDS
• N02 — ANALGESICS
• N — NERVOUS SYSTEM

Drug Categories

• Alimentary Tract and Metabolism
• Analgesics
• Antidiarrheals
• Antidiarrheals, Intestinal Antiinflammatory/antiinfective Agents
• Antipropulsives
• Antitussive Agents
• Biological Products
• Central Nervous System Agents
• Central Nervous System Depressants
• Complex Mixtures
• Cytochrome P-450 CYP2D6 Substrates
• Cytochrome P-450 CYP3A Substrates
• Cytochrome P-450 CYP3A4 Substrates
• Cytochrome P-450 Substrates
• Drugs that are Mainly Renally Excreted
• Gastrointestinal Agents
• Narcotics
• Natural Opium Alkaloids
• Nervous System
• Opiate Agonists
• Opioid Agonist
• Opioids
• Peripheral Nervous System Agents
• Plant Extracts
• Plant Preparations
• Respiratory System Agents
• Sensory System Agents
• Serotonergic Drugs Shown to Increase Risk of Serotonin Syndrome

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]

External Links

PubChem Substance

347911129

RxNav

7676

Wikipedia

Opium

MSDS

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Clinical Trials

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Phase	Status	Purpose	Conditions	Count	Start Date	Why Stopped	100+ additional columns
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Not Available	Completed	Supportive Care	Surgery	1	somestatus	stop reason	just information to hide
Not Available	Completed	Treatment	Pain	1	somestatus	stop reason	just information to hide
4	Completed	Treatment	Hysterectomy / Postoperative pain	1	somestatus	stop reason	just information to hide
4	Completed	Treatment	Kidney Stones	1	somestatus	stop reason	just information to hide
4	Completed	Treatment	Neonatal drug withdrawal syndrome	1	somestatus	stop reason	just information to hide

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Pharmacoeconomics

Manufacturers

Not Available

Packagers

Not Available

Dosage Forms

Form	Route	Strength
Suppository	Rectal
Tincture	Oral
Capsule	Oral
Liquid	Oral
Solution / drops	Oral
Tablet	Oral
Tincture	Oral	200 g / 1 L

Prices

Not Available

Patents

Not Available

Properties

State

Liquid

Experimental Properties

Property	Value	Source
boiling point (°C)	73.3ºC (Opium 2% tincture)	'MSDS'
water solubility	Soluble (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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Details1. Delta-type opioid receptor

Kind

Protein

Organism

Humans

Pharmacological action

Yes

Actions

Agonist

General Function

G-protein coupled receptor that functions as a receptor for endogenous enkephalins and for a subset of other opioids. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors, such as adenylate cyclase. Signaling leads to the inhibition of adenylate cyclase activity. Inhibits neurotransmitter release by reducing calcium ion currents and increasing potassium ion conductance. Plays a role in the perception of pain and in opiate-mediated analgesia. Plays a role in developing analgesic tolerance to morphine

Specific Function

G protein-coupled enkephalin receptor activity

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.

Details2. Kappa-type opioid receptor

Kind

Protein

Organism

Humans

Pharmacological action

Yes

Actions

Agonist

General Function

G-protein coupled opioid receptor that functions as a receptor for endogenous alpha-neoendorphins and dynorphins, but has low affinity for beta-endorphins. Also functions as a receptor for various synthetic opioids and for the psychoactive diterpene salvinorin A. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors, such as adenylate cyclase. Signaling leads to the inhibition of adenylate cyclase activity. Inhibits neurotransmitter release by reducing calcium ion currents and increasing potassium ion conductance. Plays a role in the perception of pain. Plays a role in mediating reduced physical activity upon treatment with synthetic opioids. Plays a role in the regulation of salivation in response to synthetic opioids. May play a role in arousal and regulation of autonomic and neuroendocrine functions

Specific Function

Dynorphin receptor activity

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.

Details3. Mu-type opioid receptor

Kind

Protein

Organism

Humans

Pharmacological action

Yes

Actions

Agonist

General Function

Receptor for endogenous opioids such as beta-endorphin and endomorphin (PubMed:10529478, PubMed:12589820, PubMed:7891175, PubMed:7905839, PubMed:7957926, PubMed:9689128). Receptor for natural and synthetic opioids including morphine, heroin, DAMGO, fentanyl, etorphine, buprenorphin and methadone (PubMed:10529478, PubMed:10836142, PubMed:12589820, PubMed:19300905, PubMed:7891175, PubMed:7905839, PubMed:7957926, PubMed:9689128). Also activated by enkephalin peptides, such as Met-enkephalin or Met-enkephalin-Arg-Phe, with higher affinity for Met-enkephalin-Arg-Phe (By similarity). Agonist binding to the receptor induces coupling to an inactive GDP-bound heterotrimeric G-protein complex and subsequent exchange of GDP for GTP in the G-protein alpha subunit leading to dissociation of the G-protein complex with the free GTP-bound G-protein alpha and the G-protein beta-gamma dimer activating downstream cellular effectors (PubMed:7905839). The agonist- and cell type-specific activity is predominantly coupled to pertussis toxin-sensitive G(i) and G(o) G alpha proteins, GNAI1, GNAI2, GNAI3 and GNAO1 isoforms Alpha-1 and Alpha-2, and to a lesser extent to pertussis toxin-insensitive G alpha proteins GNAZ and GNA15 (PubMed:12068084). They mediate an array of downstream cellular responses, including inhibition of adenylate cyclase activity and both N-type and L-type calcium channels, activation of inward rectifying potassium channels, mitogen-activated protein kinase (MAPK), phospholipase C (PLC), phosphoinositide/protein kinase (PKC), phosphoinositide 3-kinase (PI3K) and regulation of NF-kappa-B (By similarity). Also couples to adenylate cyclase stimulatory G alpha proteins (By similarity). The selective temporal coupling to G-proteins and subsequent signaling can be regulated by RGSZ proteins, such as RGS9, RGS17 and RGS4 (By similarity). Phosphorylation by members of the GPRK subfamily of Ser/Thr protein kinases and association with beta-arrestins is involved in short-term receptor desensitization (By similarity). Beta-arrestins associate with the GPRK-phosphorylated receptor and uncouple it from the G-protein thus terminating signal transduction (By similarity). The phosphorylated receptor is internalized through endocytosis via clathrin-coated pits which involves beta-arrestins (By similarity). The activation of the ERK pathway occurs either in a G-protein-dependent or a beta-arrestin-dependent manner and is regulated by agonist-specific receptor phosphorylation (By similarity). Acts as a class A G-protein coupled receptor (GPCR) which dissociates from beta-arrestin at or near the plasma membrane and undergoes rapid recycling (By similarity). Receptor down-regulation pathways are varying with the agonist and occur dependent or independent of G-protein coupling (By similarity). Endogenous ligands induce rapid desensitization, endocytosis and recycling (By similarity). Heterooligomerization with other GPCRs can modulate agonist binding, signaling and trafficking properties (By similarity)

Specific Function

Beta-endorphin receptor activity

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.

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Drug created at December 03, 2015 16:51 / Updated at September 18, 2024 17:45