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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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- In water: Metopon (5-Methyldihydromorphinone) is sparingly soluble in
water. Its solubility can vary depending on the specific form (e.g., salt
form) and conditions, but generally, it is considered to have limited
solubility in water.
- In alcohol: Metopon (5-Methyldihydromorphinone) is generally soluble
in alcohol. Specifically, it is soluble in ethanol (ethyl alcohol) and other
alcohols to varying degrees depending on the concentration and
conditions. However, the exact solubility can vary based on factors such
as temperature and the specific form of alcohol used.
Chemical properties:
Chemical name: The chemical name of Metopon is 5-(3-Ethyl-4-methyl-
2,5-dioxo-4,5-dihydro-1H-pyrrol-1-yl)-N-ethyl-2-methyl-N-(2-(5-methyl-
1,2,4-oxadiazol-3-yl)ethyl)-2-propenamide. Metopon is a synthetic opioid
analgesic and is structurally related to morphine. As with any medication,
it should only be used under the supervision and prescription of a
qualified healthcare professional.
Chemical classification: Metopon belongs to the chemical class of opioids.
Opioids are substances that act on opioid receptors to produce analgesic
(pain-relieving) effects. They include natural, semi-synthetic, and
synthetic compounds, with examples like morphine, codeine, and fentanyl.
Metopon, being a synthetic opioid analgesic, shares characteristics with
other opioids but has distinct chemical properties specific to its structure.
Functional group: Metopon contains several functional groups in its
chemical structure. One of the prominent functional groups is the amide
group, specifically seen in the presence of the carbonyl (C=O) group
bonded to a nitrogen atom. Additionally, there are alkyl, alkene, and
heterocyclic groups within the molecule. These functional groups
contribute to the pharmacological properties of Metopon as a synthetic
opioid analgesic.
From where it is obtained: Metopon is a semi-synthetic opioid analgesic, and its
development involves the modification of morphine. It is not commonly used in
medical practice due to its high potential for abuse and addiction. Metopon is not
typically available for prescription or use, and its production is regulated due to its
controlled substance status.
Route of administration: Metopon is a synthetic opioid analgesic, and its typical
route of administration is oral. However, it's essential to note that the use of any
prescription medication should be strictly under the guidance and prescription of a
qualified healthcare professional.
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Pharmalogical action: Metopon is an opioid analgesic that exerts its
pharmacological action by binding to opioid receptors in the central nervous
system. It primarily acts as an agonist at these receptors, producing analgesia (pain
relief) by inhibiting the transmission of pain signals. Opioid receptors are found in
various regions of the brain and spinal cord, contributing to the drug's effects on
pain perception and modulation. Metopon is a potent opioid and should be used
with caution under the supervision of a healthcare professional due to its potential
for side effects and dependence.
Analysis:
Physical method: Metopon, being a controlled substance and opioid, is primarily
analyzed using various physical and chemical methods to ensure purity, identify
potential impurities, and determine its physical properties. Here are some
common methods used in the analysis of metopon:
Melting Point Determination: The melting point of metopon can be
determined to verify its identity and purity. The observed melting point
should match the known literature values.
Solubility: Testing the solubility of metopon in different solvents can
provide information about its physical properties and aid in its isolation
and purification.
Crystallography: X-ray crystallography can be used to determine the
crystal structure of metopon, providing detailed information about its
molecular arrangement in solid form.
Nuclear Magnetic Resonance (NMR) Spectroscopy: NMR spectroscopy,
particularly proton (1H-NMR) and carbon-13 (13C-NMR) spectroscopy,
can provide structural information about metopon's carbon and hydrogen
atoms, confirming its identity.
Mass Spectrometry (MS): Mass spectrometry can be used to determine the
molecular weight and structural information of metopon through
fragmentation patterns, aiding in its identification and quantification.
Infrared (IR) Spectroscopy: IR spectroscopy can be employed to identify
functional groups present in metopon, providing additional structural
information.
UV-Vis Spectroscopy: UV-Vis spectroscopy may be used to study the
electronic transitions within metopon, particularly useful for
understanding its absorption properties.
Chemical Method: Metopon, chemically known as 5-Methyldihydromorphinone,
is synthesized through a series of chemical reactions starting from morphine. The
general chemical method involves the following steps:
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Acetylation: Morphine is first acetylated to form diacetylmorphine
(heroin).
Reduction: Diacetylmorphine (heroin) undergoes reduction to produce
dihydromorphine.
Methylation: Dihydromorphine is then methylated at the 5-position to
introduce the methyl group, resulting in metopon (5-
Methyldihydromorphinone).
Purification: The final product, metopon, is purified through appropriate
techniques to obtain the desired chemical compound.
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METHYLDIHYDROMORPHINE
Scientific name: 6-Methyldihydromorphine
Molecular structure:
Physical properties:
Apperance: Methyldihydromorphine, also known as Metopon, typically
appears as a white crystalline powder. This appearance is common among
many pharmaceutical-grade opioids and their derivatives. The powder is
usually odorless and can be dissolved in water or other solvents for
medical use.
Colour: Methyldihydromorphine, also known as Metopon, typically
appears as a white to off-white crystalline powder.
Odour: Methyldihydromorphine, like many opioid compounds, typically
does not have a significant or distinctive odor. Most pure opioids are
usually odorless or have a very faint characteristic chemical smell.
Taste: Methyldihydromorphine, like many opioids, typically has a bitter
taste. This is characteristic of most opioid compounds.
Melting point: The melting point of methyldihydromorphine (metopon) is
approximately 150-152°C (302-306°F).
Boiling point: The boiling point of methyldihydromorphine (metopon) is
approximately 260-270°C (520-518°F) under standard atmospheric
pressure. This can vary slightly depending on factors such as purity and
atmospheric conditions
Molar mass: Molar mass of 5-Methyldihydromorphine (Metopon) is
around 299.358 g/mol.
Solubility:
- In water: Methyldihydromorphine, also known as Metopon, has limited
solubility in water. It is generally considered to be sparingly soluble in
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water. However, its exact solubility can vary depending on factors such
as temperature and pH. If you need precise solubility data for specific
purposes, consulting detailed scientific literature or chemical databases
would be advisable.
- In alcohol: Methyldihydromorphine, also known as Metopon, exhibits
limited solubility in alcohol due to its chemical properties. Generally,
opioids like metopon tend to be more soluble in water than in alcohol.
However, specific solubility data for metopon in alcohol isn't widely
documented. Typically, when using such substances, it's crucial to
consult detailed chemical references or pharmaceutical databases for
precise solubility information for practical applications.
Chemical properties:
Chemical formula: The chemical formula for Methyldihydromorphine is
C19H25NO3.
Chemical classification: Methyldihydromorphine belongs to the chemical
class of opioids. Specifically, it is a derivative of morphine, which is an
alkaloid and a natural opioid analgesic found in the opium poppy plant.
Opioids generally act on the opioid receptors in the body and are known
for their pain-relieving properties.
Functional group: The functional groups present in
Methyldihydromorphine include a tertiary amine group (-N(CH3)2) and
an ether group (-O-). The tertiary amine is part of the morphinan
structure, and the ether group is within the cyclic ring system.
How it is made:
1. Starting Materials: Begin with morphine or another suitable morphinan
alkaloid as a starting material.
2. Protection of Functional Groups: Protect specific functional groups using
chemical protecting agents to prevent undesired reactions during
subsequent steps.
3. Methylation: Introduce a methyl group (CH3) to the sixth carbon atom of
the morphinan ring. This is typically achieved through a methylation
reaction.
4. Further Transformations: Carry out additional chemical transformations
to modify the structure and achieve the desired pharmacological
properties.
5. Deprotection: Remove the protecting groups applied earlier, restoring the
original functional groups as needed.
6. Purification: Purify the synthesized compound through techniques such as
chromatography to isolate the desired Methyldihydromorphine product.
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7. Analysis and Quality Control: Conduct thorough analysis and quality
control measures to ensure the purity and identity of the synthesized
compound.
8. Formulation: If intended for pharmaceutical use, the drug may undergo
further formulation processes to create a suitable dosage form (e.g., tablet,
capsule).
It's important to note that the detailed synthesis process may involve
specific reagents, conditions, and reaction mechanisms that would be described in
scientific literature or patents.
From where it is obtained: Methyldihydromorphine is a semi-synthetic opioid
analgesic. It is derived from morphine, which is obtained from the opium poppy
plant (Papaver somniferum). The synthesis involves chemical modifications of
morphine to produce Methyldihydromorphine.
Route of administration: The route of administration for Methyldihydro
morphine can vary, but it is typically administered orally or through injection. The
specific route depends on the formulation of the drug and the medical context in
which it is used.
Pharmalogical action: Methyldihydromorphine is an opioid analgesic,
structurally related to morphine. Its pharmacological action primarily involves
binding to opioid receptors in the central nervous system, leading to analgesia or
pain relief. This drug acts as an agonist, mimicking the effects of endogenous
opioids, such as endorphins.
The activation of opioid receptors inhibits the release of
neurotransmitters like substance P, reducing pain signals in the spinal cord and
brain. Methyldihydromorphine also has depressant effects on the respiratory
center, potentially causing respiratory depression in higher doses.It's essential to
note that opioids, including Methyldihydromorphine, come with risks of tolerance,
dependence, and addiction. Proper medical supervision and adherence to
prescribed dosages are crucial to manage these risks.
Analysis:
Physical method: Methyldihydromorphine is a semi-synthetic opioid analgesic.
Here's a brief physical analysis:
Appearance: Typically, methyldihydromorphine appears as a white to off-
white crystalline powder or as small crystals.
Solubility: It is soluble in organic solvents like ethanol and chloroform, but
its solubility in water is limited.
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Melting Point: The exact melting point can vary, but opioids generally have
melting points in a range that reflects their crystalline nature and purity
Stability: It should be stored in a dry and cool place, protected from light
and moisture, to maintain stability.
Chemical method: Methyldihydromorphine, also known as Metopon, has the
following chemical analysis:
Chemical Formula: C18H21NO3
Molecular Weight: Approximately 299.36 g/mol
Melting Point: Information varies, typically between 159-161°C
Solubility: Soluble in ethanol, chloroform, and other organic solvents;
sparingly soluble in water
Structure: It is a semi-synthetic opioid derivative of morphine, featuring a
methyl group at the 5-position of the morphinan ring system.
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MORAMIDE INTERMEDIATE
Scientific Name: “3-hydroxy-N, N-diethylmorphinan-6-one.”
Molecular Structure:
Physical Properties: Physical properties of drugs and their intermediates can
vary widely depending on their chemical structure and intended use. Some
common physical properties include:
Colour and Odour: Drugs can vary in colour and odour, which can affect
patient acceptability and compliance.
Melting Point: The temperature at which a solid substance melts. This can
vary depending on the purity of the substance and its crystalline form.
Boiling Point: The temperature at which a liquid substance boils and turns
into a vapour. This is relevant for drugs administered via inhalation or in
solutions.
Solubility: The ability of a substance to dissolve in a solvent, usually
expressed in terms of grams of solute per 100 mL of solvent at a specific
temperature. Solubility affects the formulation and administration of
drugs.
Density: The mass per unit volume of a substance. Density is important for
dosage calculations and formulation of drugs.
Chemical Properties:- Basicity: Moramide intermediates often contain basic
nitrogen atoms, which can undergo protonation reactions. This basicity is crucial
for their pharmacological activity, particularly in interacting with opioid receptors.
Functional groups: Moramide intermediates may contain various
functional groups such as amines, amides, and aromatic rings. These
functional groups contribute to their chemical reactivity and interactions
with other molecules.
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Solubility: The solubility of moramide intermediates can vary depending
on their specific chemical structure. Some intermediates may be soluble in
polar solvents like water, while others may be more soluble in organic
solvents.
Stability: The stability of moramide intermediates is an important
consideration during their synthesis, storage, and use. Some intermediates
may be prone to degradation under certain conditions, such as exposure
to heat, light, or acidic/basic environments.
Reactivity: Moramide intermediates may undergo various chemical
reactions such as hydrolysis, oxidation, or reduction depending on the
functional groups present in their structure. Understanding their
reactivity is crucial for controlling the synthesis and purification
processes.
Pharmacological activity: Moramide intermediates may exhibit opioid-like
pharmacological activity, although their potency and specificity for opioid
receptors can vary. This activity is related to their ability to bind to and
activate opioid receptors in the central nervous system.
Toxicity: Like other opioid compounds, moramide intermediates may
possess inherent toxicity, particularly at higher doses or with prolonged
exposure. Understanding their toxicological profile is essential for
assessing their safety for use in pharmaceutical applications.
Route of Administration: Moramide intermediate is typically administered orally
as a prescription medication. It belongs to the opioid analgesic class and is often
used for the management of moderate to severe pain. Oral administration allows
for controlled absorption of the drug through the gastrointestinal tract, leading to
systemic distribution and therapeutic effects. As with any medication, it's
important to follow the prescribed dosage and administration instructions
provided by a healthcare professional.
Pharmacological Actions: The main pharmacological actions of moramide
intermediate include:
Analgesia: Moramide intermediate relieves pain by binding to opioid
receptors in the brain and spinal cord, inhibiting the transmission of pain
signals and altering the perception of pain.
Sedation: Opioids like moramide intermediate can cause sedation or
drowsiness as a side effect, which can be beneficial for patients
experiencing pain-induced insomnia or anxiety.
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Respiratory Depression: One of the major side effects of opioids is
respiratory depression, where the rate and depth of breathing decrease.
This effect can be potentially dangerous, especially in overdose situations.
Euphoria: Opioids can induce a sense of euphoria or well-being in some
individuals, which contributes to their potential for misuse and addiction.
Physical Dependence and Tolerance: Prolonged use of opioids like
moramide intermediate can lead to physical dependence and tolerance,
requiring higher doses to achieve the same level of pain relief.
Constipation: Opioids commonly cause constipation by slowing down
gastrointestinal motility through actions on opioid receptors in the gut.
Cough Suppression: Some opioids have antitussive (cough-suppressing)
effects, although this is not usually a primary indication for their use.
It's important to note that while opioids like moramide intermediate can
be effective for managing pain, they also carry significant risks, including the
potential for addiction, overdose, and respiratory depression. Therefore, they
should be used cautiously and under the supervision of a healthcare professional.
Analysis:
Nuclear Magnetic Resonance (NMR) Spectroscopy: NMR spectroscopy is a
powerful technique used to elucidate the chemical structure of organic
compounds, including moramide intermediates. By analyzing the unique chemical
shifts and coupling patterns of hydrogen and carbon atoms in the molecule, NMR
can provide detailed information about the connectivity of atoms within the
compound.
High-Performance Liquid Chromatography (HPLC): HPLC is a chromatographic
technique used to separate, identify, and quantify individual components in a
mixture. In pharmaceutical analysis, HPLC is commonly employed to assess the
purity of moramide intermediates and detect any impurities or degradation
products present in the sample. Additionally, HPLC can be coupled with various
detectors such as UV, MS, or ELSD for sensitive detection and characterization.
Mass Spectrometry (MS): Mass spectrometry is a technique used to determine the
molecular weight and structural information of organic compounds. In
pharmaceutical analysis, MS is often coupled with chromatographic techniques like
HPLC (LC-MS) to identify and quantify moramide intermediates and related
compounds. MS can provide valuable information about the presence of impurities,
degradation products, and structural modifications in the sample.
Infrared (IR) Spectroscopy: IR spectroscopy is utilized to analyse the functional
groups present in a compound based on the absorption of infrared radiation. By
comparing the IR spectrum of a moramide intermediate with reference spectra,
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