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Файл:Ординатура / Хирургия / Библиотека им академика М.И. Перельмана / Книга_5491_Библиотеки_им_академика_М_И_Перельмана
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Thebaine:
Carbonyl group (C=O): Thebaine contains a ketone functional group (C=O)
in its molecular structure.
Ether group (C-O-C): Similar to morphine and codeine, thebaine also
contains ether linkages in its structure.
Amino group (-NH2): Thebaine contains an amino group, contributing to
its basic properties.
PH: around 5.0 to 7.0.
How it is Made ? /From whether it is obtained?: Opium is obtained from the
opium poppy plant (Papaver somniferum) through a process known as opium
harvesting. Here's an overview of how opium is obtained:
Cultivation: Opium poppy plants are cultivated in regions with suitable
climates and soil conditions. The cultivation process involves sowing
poppy seeds in well-drained soil and providing adequate water and
sunlight for growth.
Growth and Flowering: The opium poppy plants grow over a period of
several months, eventually reaching a height of about 3 to 5 feet. During
the flowering stage, the plants produce large, showy flowers with petals
that range in color from white to purple.
Opium Harvesting: Opium is harvested from the opium poppy plants by
making shallow incisions or cuts in the mature seed pods (also known as
poppy pods) using a special harvesting tool called a "lancet." The milky
latex sap, which contains alkaloids such as morphine and codeine, oozes
out of the incisions and is collected on the surface of the pods.
Drying: The collected opium sap is left to dry on the surface of the poppy
pods, where it forms a dark, sticky residue. This residue is scraped off the
pods and further dried in the sun or in controlled indoor environments to
reduce moisture content and increase shelf stability.
Processing: Once dried, the opium may undergo additional processing
steps to improve its purity or concentrate its active alkaloids. These
processing steps may include grinding the dried opium into a fine powder
or extracting specific alkaloids using solvent-based techniques.
Packaging and Distribution: The processed opium is typically packaged in
airtight containers or wrapped in protective material to prevent moisture
absorption and degradation. It is then distributed for various purposes,
including medicinal use, research, or illicit trade.
Route of Administration:
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Oral ingestion: One of the most common and traditional methods of
consuming opium is by swallowing it. Opium can be consumed directly in
its raw form or processed into various products such as tinctures, teas, or
pills. When ingested orally, opium is absorbed through the gastrointestinal
tract, leading to slower onset of effects compared to other routes of
administration.
Smoking: Opium can be smoked by heating it and inhaling the vapors.
Traditionally, opium was smoked in pipes or hookahs, although this
method of administration has become less common in modern times.
Smoking opium results in rapid absorption of its active compounds
through the lungs, leading to a quicker onset of effects compared to oral
ingestion.
Inhalation: In addition to smoking, opium can be inhaled in the form of
vapor or fumes. This method involves heating opium on a hot surface or
using specialized vaporization devices to produce inhalable vapors.
Inhalation allows for rapid absorption of opium's active compounds
through the respiratory system.
Injection: While less common, opium alkaloids such as morphine and
codeine can be dissolved in a solution and injected intravenously or
intramuscularly. Injection provides rapid delivery of opium's effects by
bypassing the digestive and respiratory systems, leading to a quick onset
of action.
Pharmacological Action:
Analgesia: Morphine and codeine are potent analgesics that act primarily
by binding to opioid receptors in the central nervous system. They
modulate pain perception by inhibiting the transmission of pain signals
and altering pain processing in the brain and spinal cord.
Sedation: Opium alkaloids such as morphine have sedative properties,
leading to feelings of relaxation, drowsiness, and tranquility. These effects
are mediated through the activation of opioid receptors in the brain,
resulting in a decrease in arousal and alertness.
Euphoria: Opium and its alkaloids can produce feelings of euphoria and
well-being, particularly at higher doses or with prolonged use. This
euphoric effect is mediated by the activation of reward pathways in the
brain, resulting in pleasurable sensations and mood elevation.
Respiratory depression: One of the most significant side effects of opium
and its alkaloids is respiratory depression, which can lead to shallow
breathing or even respiratory arrest in severe cases. This effect is
mediated by the suppression of respiratory centers in the brainstem.
Cough suppression: Codeine, in particular, is known for its antitussive
(cough-suppressant) effects. It acts on cough centers in the brain to reduce
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the urge to cough, making it useful for treating dry, non-productive
coughs.
Gastrointestinal effects: Opium and its alkaloids can affect gastrointestinal
motility, leading to constipation, nausea, and vomiting. These effects are
mediated by the activation of opioid receptors in the gastrointestinal tract,
resulting in decreased peristalsis and gastric emptying.
Dependence and tolerance: Prolonged use of opium and its alkaloids can
lead to the development of tolerance, dependence, and addiction.
Individuals may require higher doses of opium to achieve the same effects
over time, and cessation of use can lead to withdrawal symptoms such as
anxiety, agitation, and flu-like symptoms.
Methods of Analysis
The analysis of opium can involve various aspects, including its chemical
composition, purity, potency, and pharmacological effects. Here are some key
components of the analysis of opium:
Chemical Composition: Opium is a complex mixture of alkaloids, organic
compounds, and other substances derived from the opium poppy plant.
Analyzing the chemical composition of opium involves identifying and
quantifying its alkaloid constituents, such as morphine, codeine, thebaine,
and others. Techniques such as chromatography (e.g., gas
chromatography, liquid chromatography) and spectroscopy (e.g., mass
spectrometry, infrared spectroscopy) are commonly used for chemical
analysis.
Purity: Determining the purity of opium involves assessing the
concentration of its active constituents relative to other compounds
present in the mixture. High-performance liquid chromatography (HPLC)
and thin-layer chromatography (TLC) are often used to quantify the
alkaloid content and assess the purity of opium samples.
Potency: Opium potency refers to its strength or effectiveness in
producing pharmacological effects, such as analgesia or sedation. Potency
can vary depending on factors such as the concentration of alkaloids and
the specific alkaloid profile of the opium sample. Pharmacological assays
and bioassays may be used to determine the potency of opium samples.
Pharmacological Effects: Analyzing the pharmacological effects of opium
involves studying its interactions with biological receptors and systems in
the body. In vitro studies using cell-based assays and in vivo studies using
animal models can be used to assess the pharmacological activity of opium
and its alkaloid constituents.
Toxicological Profile: Assessing the toxicological profile of opium involves
evaluating its potential for adverse effects and toxicity. Studies may
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include acute toxicity testing, chronic toxicity studies, and assessments of
mutagenicity and carcinogenicity. Toxicological analysis helps to identify
potential risks associated with opium use and inform safety
considerations.
Contaminants and Adulterants: Opium samples may be analyzed for the
presence of contaminants, such as pesticides, heavy metals, and microbial
contaminants, which can pose health risks to consumers. Adulterants,
such as other plant materials or synthetic substances, may also be
detected and quantified using analytical techniques.
Physical Method: Physical methods for analyzing opium focus on characterizing
its physical properties without altering its chemical composition. Here are some
common physical methods used for opium analysis:
Macroscopic Examination: Visual inspection of opium samples can provide
information about their appearance, including color, texture, and
consistency. Variations in these characteristics can indicate differences in
opium samples, such as purity, age, or processing methods.
Microscopic Examination: Microscopic techniques, such as microscopy
and polarized light microscopy, can be used to examine the morphological
characteristics of opium, including the presence of plant debris, cellular
structures, and the distribution of alkaloid crystals. Microscopic analysis
can help identify adulterants or contaminants in opium samples.
Melting Point Determination: Melting point determination can provide
information about the purity and identity of opium samples. However,
since opium is a complex mixture of compounds, it does not have a well-
defined melting point. Instead, melting point analysis may be used for
specific opium alkaloids, such as morphine or codeine, to assess their
purity.
Solubility Tests: Solubility tests involve dissolving opium samples in
various solvents, such as water, ethanol, chloroform, or ether, and
observing their solubility properties. Differences in solubility can indicate
the presence of specific compounds or impurities in opium samples.
Density Measurement: Density measurement can provide information
about the mass per unit volume of opium samples. Variations in density
may indicate differences in composition or purity between opium samples.
Density measurements can be performed using a suitable method, such as
a pycnometer or density meter.
Thin-Layer Chromatography (TLC): TLC is a chromatographic technique
used to separate and analyze the components of opium samples based on
their differential migration on a thin layer of adsorbent material. TLC can
be used for qualitative analysis of opium alkaloids and impurities.
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Ultraviolet (UV) Spectroscopy: UV spectroscopy can be used to analyze
opium samples by measuring the absorbance of ultraviolet light at specific
wavelengths. UV spectroscopy can provide information about the
presence of certain compounds or functional groups in opium samples.
Chemical Method: Chemical methods for analyzing opium involve techniques that
induce chemical reactions or alterations in the compounds present in the sample
to characterize its properties or identify its constituents. Here are some common
chemical methods used for opium analysis:
Alkaloid Extraction: Opium contains various alkaloids, including
morphine, codeine, and thebaine, which are the primary active
constituents. Chemical methods involve extracting these alkaloids from
the opium matrix using solvents such as ethanol, methanol, or chloroform.
Acid-base extraction techniques may also be employed to selectively
isolate alkaloids based on their solubility properties.
Chromatography: Chromatographic techniques, such as high-performance
liquid chromatography (HPLC) or gas chromatography (GC), are
commonly used for opium analysis. HPLC can separate and quantify
individual alkaloids present in opium samples, providing information
about their concentration and purity. GC can be used to analyze volatile
compounds or derivatives of opium alkaloids.
Spectroscopy: Spectroscopic methods, such as infrared spectroscopy (IR)
or nuclear magnetic resonance spectroscopy (NMR), can provide
structural information about the compounds present in opium. IR
spectroscopy can identify functional groups, while NMR spectroscopy can
determine the molecular structure of opium alkaloids and other
constituents.
Colorimetric Assays: Colorimetric assays involve using specific chemical
reagents to produce color changes in opium samples based on the
presence of certain compounds. For example, the Dragendorff reagent can
be used to detect alkaloids in opium by forming colored precipitates.
Acid-Base Titration: Acid-base titration techniques can be used to
determine the alkaloid content or total alkalinity of opium samples. Opium
alkaloids are basic compounds that can react with acids to form salts,
allowing for quantification based on the volume of acid required for
neutralization.
Mass Spectrometry: Mass spectrometry (MS) techniques can be used to
identify and quantify compounds present in opium samples based on their
mass-to-charge ratios. Liquid chromatography coupled with mass
spectrometry (LC-MS) or gas chromatography-mass spectrometry (GC-
MS) are powerful tools for opium analysis, providing high sensitivity and
specificity.
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OXYCODONE
Scientific name:
(4R,4aS,7aR,12bS)-4a-hydroxy-9-methoxy-3-methyl-2,4,5,6,7a,13-hexahydro-1H-
4,12-methanobenzofuro[3,2-e]isoquinolin-7-one.
Molecular structure:
Physical Properties
Appearance: Solid form: White, crystalline, odorless powder
Colour: White, Blue, Pink, Peach, Green
Odour: odorless
Taste: bitter taste
M.p: 197-198°C
B.p: 300°C to 310°C (572°F to 590°F)
Molar mass: 351.83 g/mol
Solubility:
Highly soluble in water: Dissolves readily in water (1 g in 6-7 mL).
Slightly soluble in alcohol: Sparingly soluble in ethanol.
Nearly insoluble in nonpolar solvents: Practically insoluble in ether and
other nonpolar solvents.
Chemical Properties
Chemical formula: C18H21NO4
Chemical classification: Oxycodone is classified as a semi-synthetic opioid
analgesic. Opioids are a class of drugs that act on opioid receptors in the
central nervous system to produce analgesia (pain relief), sedation, and
other effects. Oxycodone is derived from the opioid alkaloid thebaine,
which is found in the opium poppy plant. It is synthesized through a series
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of chemical reactions from thebaine, resulting in a semi-synthetic
compound with opioid properties. Oxycodone is commonly used for the
management of moderate to severe pain and is available in various
formulations, including immediate-release and extended-release
formulations. Its classification as an opioid reflects its pharmacological
mechanism of action and therapeutic use in pain management.
Functional group: The functional groups present in the chemical structure
of oxycodone are:
- Alcohol (Hydroxyl) Group (-OH): Oxycodone contains one alcohol
functional group, which is represented by the hydroxyl (-OH) group. This
functional group is attached to one of the carbon atoms in the molecule.
The hydroxyl group is important for the pharmacological activity of
oxycodone and can participate in various chemical reactions, including
esterification and hydrolysis.
- Ether Group (-O-): Oxycodone contains one ether functional group,
which is represented by the oxygen atom (-O-) linking two carbon atoms
in the molecule. The ether linkage is part of the morphinan skeleton of
oxycodone and contributes to its overall chemical structure and
properties.
- Ketone Group (Carbonyl) (C=O): Oxycodone contains one ketone
functional group, which is represented by the carbonyl group (C=O)
attached to one of the carbon atoms in the molecule. The ketone group is
part of the cyclic structure of oxycodone and plays a role in its
pharmacological activity and chemical reactivity.
PH: 1.4-4
How It Is Made ?/From Whether It Is Obtained?
Oxycodone is a semi-synthetic opioid, meaning it is derived from natural
sources but undergoes chemical modification in a laboratory setting to produce the
final compound. The synthesis of oxycodone typically involves several chemical
steps starting from thebaine, an alkaloid found in the opium poppy plant. Here is a
general overview of how oxycodone is synthesized:
Extraction of Thebaine: The process begins with the extraction of thebaine
from opium poppy plants. Opium latex, obtained from the poppy pods,
undergoes extraction and purification to isolate thebaine, which serves as
the starting material for oxycodone synthesis.
Chemical Modification: The thebaine is subjected to chemical reactions in
the laboratory to modify its structure and convert it into oxycodone. These
reactions typically involve functional group transformations, such as
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reduction, oxidation, and esterification, to introduce or modify specific
chemical moieties in the molecule.
Purification: After the chemical modification steps, the crude reaction
mixture is purified to isolate the desired oxycodone product from other
reaction by-products and impurities. Purification techniques may include
crystallization, chromatography, and recrystallization to obtain high-
purity oxycodone.
Formulation: Once the oxycodone compound is obtained in pure form, it
can be formulated into various pharmaceutical dosage forms, such as
tablets, capsules, or solutions, for administration to patients.
Pharmaceutical excipients are often added to the formulation to improve
stability, bioavailability, and patient acceptability.
Oxycodone is primarily synthesized in pharmaceutical laboratories under
controlled conditions to ensure product quality, purity, and safety. The synthesis
process may involve several intermediate compounds and chemical reagents, and
it requires expertise in organic chemistry and pharmaceutical science.
Route of Administration:
Oral: Oral administration is the most common route for oxycodone. It is
typically available in immediate-release (IR) or extended-release (ER)
formulations in the form of tablets or capsules. Immediate-release
oxycodone is often prescribed for the management of acute pain and is
usually taken every 4 to 6 hours as needed. Extended-release formulations
are designed to provide around-the-clock pain relief and are taken at
scheduled intervals, such as once or twice daily.
Sublingual: Sublingual administration involves placing oxycodone tablets
under the tongue, where they dissolve and are absorbed through the
mucous membranes into the bloodstream. This route may be used for
certain immediate-release formulations to achieve rapid onset of action.
Buccal: Buccal administration involves placing oxycodone tablets between
the cheek and gum, where they dissolve and are absorbed through the
buccal mucosa into the bloodstream. This route may also be used for
certain immediate-release formulations to achieve rapid onset of action.
Rectal: Rectal administration involves inserting oxycodone suppositories
or rectal solutions into the rectum, where they are absorbed through the
rectal mucosa into the bloodstream. This route may be used when oral
administration is not feasible or when rapid onset of action is desired.
Intravenous (IV): Intravenous administration of oxycodone involves
injecting a solution of the medication directly into a vein. This route is
typically reserved for use in hospital settings for the management of
severe pain or when rapid onset of action is required.
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Intramuscular (IM): Intramuscular administration of oxycodone involves
injecting a solution of the medication into a muscle. This route may be
used in certain clinical situations, although it is less common than oral or
intravenous administration.
Pharmacological Action:
Oxycodone exerts its pharmacological actions primarily through
interactions with opioid receptors in the central nervous system. Here are the key
pharmacological actions of oxycodone:
Analgesia: Oxycodone is a potent analgesic, meaning it relieves pain by
modulating the perception of pain signals in the brain and spinal cord. It
acts predominantly on mu-opioid receptors, which are distributed
throughout the central and peripheral nervous systems. By binding to
these receptors, oxycodone inhibits the transmission of pain signals and
alters the response to pain, resulting in pain relief.
Sedation: Oxycodone can produce sedative effects, leading to feelings of
relaxation, drowsiness, and decreased alertness. These effects are
mediated by its actions on mu-opioid receptors in regions of the brain
involved in regulating arousal and wakefulness.
Euphoria: Like other opioids, oxycodone has the potential to produce
feelings of euphoria or well-being, particularly at higher doses or when
used recreationally. Euphoria is thought to result from the activation of
mu-opioid receptors in brain reward pathways, leading to the release of
dopamine and other neurotransmitters associated with pleasure and
reward.
Respiratory Depression: One of the most serious side effects of oxycodone
and other opioids is respiratory depression, which can lead to decreased
breathing rate and shallow breathing. Respiratory depression occurs due
to the suppression of respiratory centers in the brainstem by activation of
mu-opioid receptors. This effect is dose-dependent and can be life-
threatening if not managed appropriately.
Constipation: Oxycodone commonly causes constipation as a side effect.
This occurs because opioids inhibit the release of neurotransmitters
involved in bowel motility and fluid secretion, leading to decreased
peristalsis and increased water absorption in the intestines.
Miosis: Oxycodone, like other opioids, can cause constriction of the pupils
(miosis) due to activation of the parasympathetic nervous system. Miosis
is a characteristic clinical sign of opioid intoxication and can help
healthcare providers recognize opioid overdose.
Cough Suppression: Oxycodone has antitussive properties and can
suppress cough reflexes by acting on opioid receptors in the brainstem.
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This effect is utilized in certain cough medications that contain oxycodone
as an active ingredient.
Analysis
Physical Method: Physical methods for analyzing oxycodone can involve
techniques that characterize its physical properties or determine its presence in a
sample without altering its chemical structure. Here are some physical methods
commonly used for oxycodone analysis:
Melting Point Determination: This method involves measuring the
temperature at which oxycodone melts. The melting point of a substance
is a characteristic physical property that can help identify and assess its
purity.
Solubility Testing: Solubility testing involves determining the solubility of
oxycodone in different solvents or solvent mixtures. This information can
be useful for formulating oxycodone-containing pharmaceuticals or
assessing its purity.
Crystallography: X-ray crystallography is a technique used to determine
the three-dimensional structure of oxycodone crystals. This method
provides detailed information about the arrangement of atoms in the
crystal lattice.
Differential Scanning Calorimetry (DSC): DSC is a thermal analysis
technique used to measure the heat flow associated with physical and
chemical changes in oxycodone. This method can provide information
about its melting behavior, crystalline transitions, and stability.
Nuclear Magnetic Resonance (NMR) Spectroscopy: NMR spectroscopy is a
powerful technique used to study the molecular structure and dynamics of
oxycodone in solution. It can provide information about chemical shifts,
coupling constants, and molecular conformation.
Infrared (IR) Spectroscopy: IR spectroscopy is used to analyze the
vibrational modes of oxycodone molecules. It can provide information
about functional groups present in the molecule and is often used for
qualitative identification.
Ultraviolet-visible (UV-Vis) Spectroscopy: UV-Vis spectroscopy is used to
analyze the absorption of light by oxycodone molecules in the ultraviolet
and visible regions of the electromagnetic spectrum. This method can
provide information about the electronic structure and concentration of
oxycodone in solution.
Particle Size Analysis: This method involves measuring the size
distribution of oxycodone particles in a sample. Particle size analysis is
important for optimizing drug formulation and assessing the physical
properties of pharmaceutical preparations.
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