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Файл:Ординатура / Хирургия / Библиотека им академика М.И. Перельмана / Книга_5733_Библиотеки_им_академика_М_И_Перельмана
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Chemical Method:
Chemical methods for analyzing oxycodone involve techniques that focus
on its chemical properties and interactions. Here are some chemical methods
commonly used for oxycodone analysis:
High-Performance Liquid Chromatography (HPLC): HPLC is a powerful
analytical technique used to separate, identify, and quantify components
in a mixture. It is commonly used for the analysis of oxycodone in
pharmaceutical formulations and biological samples. HPLC analysis of
oxycodone typically involves a chromatographic column, a mobile phase
(solvent), and a detector, such as UV or mass spectrometry.
Gas Chromatography (GC): GC is another chromatographic technique used
for the analysis of volatile and semi-volatile compounds. While less
commonly used for oxycodone analysis compared to HPLC, GC can be
employed for specific applications, such as the analysis of oxycodone
metabolites in biological samples.
Mass Spectrometry (MS): Mass spectrometry is a technique used to
identify and quantify compounds based on their mass-to-charge ratio.
Mass spectrometry can be coupled with chromatographic techniques (e.g.,
LC-MS or GC-MS) for sensitive and selective detection of oxycodone and its
metabolites in complex matrices.
Titration: Titration is a classical chemical method used to determine the
concentration of a substance in a solution by reacting it with a
standardized reagent. While less common for oxycodone analysis
compared to chromatographic and spectrometric techniques, titration
methods may be employed for certain applications, such as the
determination of oxycodone content in pharmaceutical formulations.
Colorimetric Assays: Colorimetric assays involve the use of color changes
to detect and quantify analytes in a sample. These assays may rely on
specific chemical reactions between oxycodone and reagents that produce
color changes proportional to the concentration of oxycodone present.
Thin-Layer Chromatography (TLC): TLC is a simple and cost-effective
chromatographic technique used for qualitative analysis of compounds.
While less sensitive and specific compared to HPLC and GC, TLC can be
used for rapid screening of oxycodone and related compounds in samples.
Electrophoresis: Electrophoretic techniques, such as capillary
electrophoresis (CE), can be used for the separation and analysis of
charged species, including oxycodone and its metabolites. CE offers high
separation efficiency and can be coupled with sensitive detection methods
for quantitative analysis.
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OXYMORPHONE
Scientific name: 4,5α-Epoxy-3,14-dihydroxy-17-methylmorphinan-6-one
Molecular structure:
Physical Properties
Appearance: Solid form: White to off-white crystals or crystalline powder.
Solution form: Colorless liquid (when dissolved in water).
Colour: white, green, blue, pink, and peach
Odour: distinct odor
Taste: bitter in taste
M.p: 285-300°C (545-572°F)
B.p: 518.6°C
Molar mass: 285.34 g/mol
Solubility:
Moderately soluble in water: Dissolves in approximately 4 parts water (1 g
in 4 ml).
Sparingly soluble in alcohol: Only slightly dissolves in alcohol.
Practically insoluble in non-polar solvents: Essentially insoluble in
substances like ether and chloroform.
Chemical Properties
Chemical formula: C17H19NO4
Chemical classification: Oxymorphone belongs to the class of compounds
known as opioids or narcotic analgesics. Opioids are a group of substances
that act on opioid receptors in the central nervous system to produce
analgesic (pain-relieving), sedative, and euphoric effects. They are
commonly used for the management of moderate to severe pain but can
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also have significant risks and side effects, including respiratory
depression, tolerance, dependence, and addiction.
More specifically, oxymorphone is a semi-synthetic opioid derived from
morphine. It is structurally related to morphine but differs in its chemical
structure, particularly at the C-6 position, where oxymorphone has a ketone group
instead of a hydroxyl group. This modification results in increased potency and
bioavailability compared to morphine. Oxymorphone is used clinically for the relief
of moderate to severe pain and is available in various formulations, including
immediate-release and extended-release formulations for oral administration, as
well as injectable formulations for parenteral administration.
Functional group: The functional groups present in oxymorphone are:
Ketone Group (-C=O): The ketone group is present at the C-6 position of
the morphinan ring structure in oxymorphone. It is represented by the
carbonyl group (-C=O), where the carbon atom is double-bonded to an
oxygen atom. This functional group contributes to the pharmacological
activity of oxymorphone and plays a role in its chemical reactivity.
Hydroxyl Group (-OH): Oxymorphone contains several hydroxyl groups (-
OH) attached to the morphinan ring structure. These hydroxyl groups
contribute to the molecule's solubility and may also participate in
hydrogen bonding interactions with other molecules.
Amino Group (-NH-): Oxymorphone contains an amino group (-NH-)
attached to the morphinan ring structure. This functional group can act as
a weak base and may undergo protonation in acidic environments to form
oxymorphone salts, such as oxymorphone hydrochloride.
PH: 7.4 is 0.98
How It Is Made?/From Whether It Is Obtained?
Oxymorphone is primarily synthesized from thebaine, which is a natural
alkaloid found in opium poppy plants. The synthesis involves several chemical
steps to modify the structure of thebaine and convert it into oxymorphone. Here is
a simplified outline of the synthesis process:
Isolation of Thebaine: Thebaine is extracted from opium poppy plants,
which contain a variety of alkaloids including morphine and codeine.
Thebaine is separated from other alkaloids through extraction and
purification processes.
Chemical Modification: Thebaine undergoes chemical reactions to
introduce functional groups and modify its molecular structure. These
reactions typically involve oxidation, reduction, and rearrangement
reactions to transform thebaine into oxymorphone.
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Purification: After the chemical modification steps, the crude product is
purified to isolate oxymorphone from other reaction by-products and
impurities. Purification techniques may include chromatography,
crystallization, and filtration.
Formulation: Once purified, oxymorphone may be formulated into various
pharmaceutical dosage forms, such as tablets, capsules, or injectable
solutions, for use in clinical settings.
Oxymorphone is primarily obtained through chemical synthesis in
laboratory settings. It is not typically obtained directly from natural sources like
opium poppy plants, as the concentration of oxymorphone in opium is much lower
compared to other alkaloids like morphine and codeine. Therefore, chemical
synthesis is the most practical method for producing oxymorphone on a
commercial scale.
Route of Administration: Oxymorphone can be administered through several
routes, depending on the specific formulation and the patient's needs. The routes
of administration for oxymorphone include:
Oral: Oxymorphone is commonly available in immediate-release and
extended-release tablet formulations for oral administration. Oral
administration is convenient and suitable for patients who can swallow
pills. Immediate-release tablets provide rapid onset of action, while
extended-release formulations offer around-the-clock pain relief.
Intravenous (IV): Oxymorphone is available as an injectable formulation
for intravenous administration. IV administration is typically used in
hospital settings for patients who require rapid pain relief or for those
who cannot tolerate oral medications.
Intramuscular (IM): In certain situations, oxymorphone may be
administered via intramuscular injection. This route of administration is
less common than oral or IV administration and may be used when IV
access is not available or when rapid absorption is desired.
Subcutaneous (SC): Subcutaneous injection of oxymorphone is less
common but may be used in certain clinical scenarios. Subcutaneous
administration involves injecting the medication into the fatty tissue layer
beneath the skin, where it is absorbed gradually into the bloodstream.
Transdermal: While not a common route of administration for
oxymorphone, transdermal patches containing oxymorphone may be
available in some regions. These patches deliver the medication through
the skin and are typically used for sustained pain relief over an extended
period.
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Pharmacological Action: The pharmacological actions of oxymorphone primarily
stem from its activity as an opioid analgesic. Here are the key pharmacological
actions of oxymorphone:
Analgesia: Oxymorphone is a potent agonist of the mu-opioid receptors in
the central nervous system. Activation of these receptors inhibits the
transmission of pain signals and alters the perception of pain, resulting in
analgesia. Oxymorphone is effective in relieving moderate to severe pain,
including acute and chronic pain conditions.
Central Nervous System Depression: Like other opioids, oxymorphone can
cause central nervous system depression, including sedation and
drowsiness. These effects contribute to its pain-relieving properties but
can also lead to side effects such as dizziness and impaired cognitive
function.
Respiratory Depression: Oxymorphone can depress respiratory function
by decreasing the sensitivity of the respiratory center in the brainstem to
carbon dioxide levels. This effect can lead to respiratory depression,
characterized by decreased respiratory rate and depth. Severe respiratory
depression can be life-threatening and requires medical intervention.
Euphoria and Sedation: Oxymorphone can produce feelings of euphoria,
relaxation, and well-being, particularly at higher doses or with misuse.
These effects are mediated by the activation of mu-opioid receptors in
reward pathways in the brain.
Gastrointestinal Effects: Oxymorphone can cause constipation due to its
effects on opioid receptors in the gastrointestinal tract, leading to
decreased gastrointestinal motility and increased water absorption in the
colon. Other gastrointestinal effects may include nausea, vomiting, and
bloating.
Physical Dependence and Tolerance: Prolonged use of oxymorphone can
lead to the development of physical dependence, characterized by
withdrawal symptoms upon discontinuation of the drug. Additionally,
tolerance may develop, requiring higher doses of oxymorphone to achieve
the same level of pain relief over time.
Cardiovascular Effects: Oxymorphone may cause changes in heart rate and
blood pressure, although these effects are generally less pronounced
compared to other opioids.
Analysis
Analysis of oxymorphone can involve various approaches depending on
the specific context and requirements. Here are several aspects of analysis related
to oxymorphone:
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Quantitative Analysis: Quantitative analysis methods are used to
determine the concentration or content of oxymorphone in
pharmaceutical formulations, biological samples, or illicit substances.
Techniques such as high-performance liquid chromatography (HPLC), gas
chromatography (GC), and mass spectrometry (MS) are commonly
employed for accurate quantification.
Qualitative Analysis: Qualitative analysis methods are used to confirm the
presence of oxymorphone in a sample without necessarily quantifying its
concentration. Techniques such as thin-layer chromatography (TLC),
infrared spectroscopy (IR), and ultraviolet-visible spectroscopy (UV-Vis)
can provide qualitative information about the identity of oxymorphone in
a sample.
Purity and Impurity Analysis: Purity analysis involves determining the
degree of purity of oxymorphone in a sample, while impurity analysis
focuses on identifying and quantifying impurities or degradation products.
These analyses are crucial for ensuring the quality and safety of
pharmaceutical formulations. Techniques such as chromatography,
spectroscopy, and titration may be used for purity and impurity analysis.
Stability Testing: Stability testing involves assessing the chemical stability
of oxymorphone formulations under various storage conditions over time.
This analysis helps determine the shelf life and storage requirements of
pharmaceutical products containing oxymorphone.
Metabolite Analysis: In pharmacokinetic studies, metabolite analysis
involves identifying and quantifying the metabolites of oxymorphone in
biological samples such as blood, urine, or tissue. This analysis provides
insights into the metabolism and elimination of oxymorphone in the body.
Formulation Analysis: Formulation analysis involves evaluating the
composition and characteristics of oxymorphone-containing
pharmaceutical formulations, including excipient compatibility,
dissolution properties, and physical stability.
Forensic Analysis: Forensic analysis of oxymorphone may involve
identifying and quantifying oxymorphone in illicit drugs, forensic samples,
or toxicology specimens. Techniques such as chromatography, mass
spectrometry, and immunoassays may be used for forensic analysis.
Environmental Analysis: Environmental analysis may involve detecting
and quantifying oxymorphone and its metabolites in environmental
samples such as water, soil, or wastewater. This analysis helps assess the
environmental impact of oxymorphone use and disposal.
Physical Method: Physical methods for analyzing oxymorphone typically involve
techniques that assess its physical properties, such as appearance, solubility,
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melting point, and spectroscopic characteristics. Here are some common physical
methods used for oxymorphone analysis:
Appearance and Color: Visual inspection of the physical appearance and
color of oxymorphone tablets, powders, or solutions can provide
preliminary information about its identity and purity. Any deviations from
the expected appearance may indicate degradation or adulteration.
Solubility: Determination of the solubility of oxymorphone in various
solvents, including water, ethanol, and organic solvents, can provide
information about its physical and chemical properties. Solubility tests
may involve observing the dissolution behavior of oxymorphone in
different solvents under controlled conditions.
Melting Point: Measurement of the melting point of oxymorphone using a
melting point apparatus can provide information about its purity and
crystalline structure. The melting point range of oxymorphone
hydrochloride is typically reported to be between approximately 285-
300°C (545-572°F).
Differential Scanning Calorimetry (DSC): DSC is a thermal analysis
technique used to study the thermal behavior of materials, including
melting, crystallization, and phase transitions. DSC can be used to
determine the melting point and thermal stability of oxymorphone
samples.
X-ray Powder Diffraction (XRPD): XRPD is a technique used to analyze the
crystalline structure of materials by measuring the diffraction pattern of
X-rays scattered by the sample. XRPD can be used to identify the
crystalline form of oxymorphone and assess its purity.
Spectroscopic Methods: Spectroscopic techniques, such as infrared
spectroscopy (IR) and ultraviolet-visible spectroscopy (UV-Vis), can
provide information about the molecular structure and chemical bonds
present in oxymorphone. These techniques can be used for qualitative and
quantitative analysis of oxymorphone in pharmaceutical formulations and
other samples.
Particle Size Analysis: Particle size analysis techniques, such as laser
diffraction or microscopy, can be used to characterize the particle size
distribution of oxymorphone powders or suspensions. Particle size
analysis is important for ensuring consistency and uniformity in
pharmaceutical formulations.
Chemical Method: Chemical methods for analyzing oxymorphone involve
techniques that assess its chemical properties, composition, and reactions. Here
are some common chemical methods used for oxymorphone analysis:
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High-Performance Liquid Chromatography (HPLC): HPLC is a widely used
technique for the separation, identification, and quantification of
compounds in a mixture. In HPLC analysis of oxymorphone, the sample is
typically injected into a chromatographic column, where it is separated
based on its interaction with a stationary phase and a mobile phase.
Detection can be performed using UV, fluorescence, or mass spectrometry
detection.
Gas Chromatography (GC): GC is another chromatographic technique used
for the separation and analysis of volatile and semi-volatile compounds. In
GC analysis of oxymorphone, the sample is vaporized and injected into a
chromatographic column, where it is separated based on its partition
between a stationary phase and a carrier gas. Detection is typically
performed using a detector such as a flame ionization detector (FID) or
mass spectrometer.
Mass Spectrometry (MS): MS is a powerful technique for the identification
and quantification of compounds based on their mass-to-charge ratio. In
MS analysis of oxymorphone, the compound is ionized and fragmented,
and the resulting mass spectrum is used to identify the compound. MS can
be coupled with chromatographic techniques such as HPLC or GC for
enhanced sensitivity and selectivity.
Nuclear Magnetic Resonance (NMR) Spectroscopy: NMR spectroscopy is
used to elucidate the molecular structure of compounds based on their
interaction with a magnetic field. In NMR analysis of oxymorphone, the
compound is dissolved in a suitable solvent and subjected to NMR
spectroscopy, which provides information about the chemical
environment of the atoms in the molecule.
Titration Methods: Titration methods, such as acid-base titrations, can be
used to determine the concentration of oxymorphone hydrochloride in
pharmaceutical formulations. In acid-base titration, a standardized
solution of acid or base is added to the sample until the equivalence point
is reached, and the amount of acid or base consumed is used to calculate
the concentration of oxymorphone hydrochloride.
Gravimetric Analysis: Gravimetric analysis involves the measurement of
mass to determine the concentration or purity of a compound. In
gravimetric analysis of oxymorphone, the compound may be precipitated
as a solid and then weighed to determine its concentration or purity.
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PARA-FLUOROFENTANYL
Scientific name:
N-(4-fluorophenyl)-N-[1-(2-phenylethyl)piperidin-4-yl]propanamide
Molecular structure:
Physical Properties
Appearance: white to off-white crystalline powder or as a solid material
Colour: white to off-white crystalline powder
Odour: distinctive odor.
Taste: bitter taste
M.p: 103-105ºC
B.p: 479.2ºC at 760mmHg
Solubility: It may have varying solubility in different solvents, but specific
solubility data may not be readily available
Molar mass: 354.469 g·mol−1
Chemical Properties
Chemical formula: C22H28FN3O
Chemical cla Para-fluorofentanyl belongs to the chemical class of synthetic
opioids. Specifically, it is an analog of fentanyl, which is a potent synthetic opioid
analgesic. Synthetic opioids are chemically synthesized compounds that act on
opioid receptors in the central nervous system to produce analgesic (pain-
relieving) effects. Within the broader category of opioids, para-fluorofentanyl falls
under the subclass of fentanyl analogs. These compounds are structurally related
to fentanyl but may have modifications to their chemical structure, such as the
addition or substitution of functional groups, which can affect their potency,
pharmacokinetics, and pharmacodynamics.
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Due to its structural similarity to fentanyl, para-fluorofentanyl shares
many pharmacological properties with other opioids, including analgesia, sedation,
respiratory depression, and euphoria. However, as a synthetic opioid, para-
fluorofentanyl may exhibit differences in potency, duration of action, and side
effect profile compared to natural opioids like morphine or semi-synthetic opioids
like oxycodone.
It's important to note that para-fluorofentanyl and other synthetic opioids
are associated with a high risk of overdose and addiction, and their use should be
strictly regulated and monitored by healthcare professionals. Additionally, para-
fluorofentanyl is often encountered in the context of illicit drug use, where it may
be sold under various street names and formulations, posing significant risks to
public health and safety.
Classification:
Functional group: The functional groups present in para-fluorofentanyl are:
Amide Group (-CONH-): The amide group is a functional group consisting
of a carbonyl group (C=O) bonded to a nitrogen atom (N) and another
atom or group of atoms. In para-fluorofentanyl, the amide group is part of
the main structure of the molecule, linking the phenethylamine moiety to
the piperidine ring.
Phenyl Group (-C6H5): The phenyl group is a hydrocarbon ring structure
consisting of six carbon atoms bonded together in a hexagonal ring, with
five of the six carbon atoms bonded to hydrogen atoms. In para-
fluorofentanyl, the phenyl group is part of the phenethylamine moiety,
contributing to the overall structure of the molecule.
Piperidine Ring: The piperidine ring is a saturated six-membered
heterocyclic ring containing five carbon atoms and one nitrogen atom. In
para-fluorofentanyl, the piperidine ring serves as the central ring
structure, connecting the phenethylamine moiety to the propanamide
moiety.
Fluorine Atom (-F): While not a traditional functional group, the fluorine
atom in para-fluorofentanyl is chemically significant as it is directly
attached to one of the phenyl rings, substituting for a hydrogen atom. This
substitution alters the pharmacological properties of the molecule
compared to fentanyl and other fentanyl analogs.
How It Is Made ?/From Whether It Is Obtained?
Para-fluorofentanyl is a synthetic compound, meaning it is manufactured
through chemical synthesis rather than being obtained from natural sources. The
exact synthetic route for para-fluorofentanyl may vary depending on the specific
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