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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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derivatized if necessary and then analyzed using GC-MS to provide
information about its chemical structure and purity.
Nuclear Magnetic Resonance (NMR) Spectroscopy: NMR spectroscopy is a
powerful technique used to elucidate the structure of organic compounds
by analyzing the nuclear spin properties of atoms within the molecule.
Anileridine can be analyzed using proton (^1H) and carbon-13 (^13C)
NMR spectroscopy to confirm its chemical structure and identify any
impurities.
Fourier Transform Infrared (FTIR) Spectroscopy: FTIR spectroscopy is
used to analyze the functional groups present in a compound by
measuring the absorption of infrared radiation. Anileridine can be
analyzed using FTIR spectroscopy to confirm its molecular structure and
identify characteristic functional groups.
Elemental Analysis: Elemental analysis techniques such as combustion
analysis or elemental CHN analysis can be used to determine the
elemental composition of anileridine, providing information about its
purity and chemical formula.
Chemical Reactions: Anileridine can undergo various chemical reactions
that can be used for its identification and characterization. For example, it
can be reacted with specific reagents to form characteristic derivatives,
which can then be analyzed using chromatographic or spectroscopic
techniques.
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BENZETHIDINE
Scientific Name: The scientific name of benzethidine is 4-phenyl-4-(1-phenethyl)
piperidine.
Molecular structure:
Physical properties
Appearance: Benzethidine typically appears as a white to off-white
crystalline powder.
Colour: Benzethidine is typically a white to off-white crystalline powder,
so its color is generally white. However, slight variations in color may
occur depending on factors such as impurities or the specific form of the
compound. Therefore, it's essential to note that while benzethidine is
predominantly white, other shades such as off-white may also be observed
in some cases.
Odour: Benzethidine is odorless.
Taste: Benzethidine has a slightly bitter taste
Melting Point: The melting point of benzethidine is approximately 106.5°C
Boiling Point: The boiling point of benzethidine is approximately 246-
248°C.
Molar mass: The molar mass of benzethidine is approximately 307.45
g/mol.
Solubility:
Water: Benzethidine has limited solubility in water. It is only sparingly
soluble, meaning it dissolves to a small extent in water. This limited
solubility in water is due to the non-polar nature of benzethidine's
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structure, which makes it more soluble in organic solvents such as
ethanol, chloroform, and ether. In aqueous solutions, benzethidine tends
to form suspensions or fine particles rather than completely dissolving.
Alcohol: Benzethidine is moderately soluble in alcohol, particularly in
ethanol. It dissolves to a greater extent in alcohol compared to water due
to the similar polarity of benzethidine and alcohol molecules. However,
the solubility of benzethidine in alcohol is still limited, and it may not fully
dissolve at lower concentrations or temperatures.
Chemical Properties:-
Chemical Formula:- The chemical formula of benzethidine is C20H23N.
Chemcal Classification: Benzethidine is classified as a piperidine
derivative.
Functional Groups: The functional group present in benzethidine is the
piperidine group, which consists of a six-membered heterocyclic ring
containing one nitrogen atom.
PH: Benzethidine does not have a defined pH value as it is not typically
used in aqueous solutions where pH is measured. It is a solid compound
with limited solubility in water, and therefore, its pH is not applicable in
the usual sense.
How it is made? Obtained from:
Benzethidine can be synthesized from 4-phenylpiperidine and phenethyl
bromide via a reaction known as a N-alkylation. The reaction typically involves the
following steps:
Formation of the Grignard Reagent: The synthesis begins with the
preparation of phenethylmagnesium bromide (PhCH2MgBr) by reacting
phenethyl bromide with magnesium metal in anhydrous diethyl ether.
N-Alkylation: Once the Grignard reagent is formed, it is reacted with 4-
phenylpiperidine to introduce the phenethyl group onto the piperidine
nitrogen atom. This reaction results in the formation of benzethidine.
The overall reaction can be represented as follows:
PhCH2MgBr + C10H13N → C20H23N + MgBr2
Benzethidine can be obtained from this reaction mixture through isolation
and purification steps such as solvent extraction, crystallization, and column
chromatography.
Route of Administration: Benzethidine is primarily administered via oral
ingestion, although other routes of administration may also be possible. When
taken orally, benzethidine is typically consumed in the form of tablets or capsules.
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After ingestion, the drug is absorbed through the gastrointestinal tract and enters
the bloodstream, where it exerts its pharmacological effects.
Other potential routes of administration for benzethidine include
intravenous injection and rectal administration, although these routes are less
common and may not be as practical or safe as oral ingestion. Intravenous
injection involves directly injecting benzethidine into a vein, allowing for rapid
absorption and onset of action. Rectal administration involves inserting
benzethidine suppositories into the rectum, where the drug is absorbed through
the rectal mucosa.
Pharmacological Action: Benzethidine is a synthetic opioid analgesic with
pharmacological actions similar to other opioids. Its primary mechanism of action
involves binding to opioid receptors in the central nervous system, particularly
mu-opioid receptors, which are involved in mediating pain perception and
modulation.
Analgesia: Benzethidine exerts potent analgesic effects by activating mu-
opioid receptors in the brain and spinal cord. By binding to these
receptors, benzethidine inhibits the transmission of pain signals, resulting
in pain relief.
Respiratory Depression: Like other opioids, benzethidine can cause
respiratory depression by suppressing the activity of respiratory centers
in the brainstem. This effect can lead to a decrease in the rate and depth of
breathing, which may be dangerous or life-threatening in cases of
overdose.
Euphoria and Sedation: Benzethidine can produce feelings of euphoria and
sedation by activating reward pathways in the brain, leading to a sense of
relaxation and well-being.
Physical Dependence and Tolerance: Prolonged use of benzethidine can
lead to the development of physical dependence, as the body adapts to the
presence of the drug and requires it to function normally. Tolerance may
also develop over time, requiring higher doses of the drug to achieve the
same effects.
Constipation: Benzethidine, like other opioids, can cause constipation by
reducing gastrointestinal motility and increasing water absorption in the
intestines.
Nausea and Vomiting: Nausea and vomiting are common side effects of
benzethidine use, particularly during the initial stages of treatment or at
higher doses.
Cough Suppression: Benzethidine has antitussive properties and can
suppress cough reflex by acting on the cough center in the brainstem.
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Miosis: Benzethidine can cause constriction of the pupil (miosis) due to its
effects on the pupillary constrictor muscles.
Analysis:
Physical Method: Physical methods of analysis for benzethidine involve
techniques aimed at characterizing its physical properties, such as appearance,
melting point, solubility, and spectroscopic analysis. Here are some common
physical methods of analysis for benzethidine:
Appearance: Visual inspection of the physical appearance of benzethidine,
which typically appears as a white to off-white crystalline powder.
Melting Point: Determination of the melting point of benzethidine using a
melting point apparatus. The melting point range provides information
about the purity and identity of the compound.
Solubility: Evaluation of the solubility of benzethidine in various solvents,
including water, ethanol, chloroform, and ether. This information helps in
determining suitable solvents for preparation and analysis.
Thin-Layer Chromatography (TLC): TLC can be used to separate and
analyze benzethidine along with reference standards. Visualization can be
achieved using UV light or chemical staining reagents.
High-Performance Liquid Chromatography (HPLC): HPLC is a technique
for the separation, identification, and quantification of compounds in a
mixture. Benzethidine can be analyzed using HPLC with various detectors
such as UV-Vis or mass spectrometry.
Gas Chromatography-Mass Spectrometry (GC-MS): GC-MS can be used to
analyze benzethidine by separating its components using gas
chromatography and identifying them based on their mass spectra.
Nuclear Magnetic Resonance (NMR) Spectroscopy: NMR spectroscopy can
provide information about the molecular structure of benzethidine by
analyzing the nuclear spin properties of its atoms.
Fourier Transform Infrared (FTIR) Spectroscopy: FTIR spectroscopy can
be used to analyze the functional groups present in benzethidine by
measuring the absorption of infrared radiation.
Chemical method: Chemical methods of analysis for benzethidine involve
techniques aimed at characterizing its chemical properties and composition. Here
are some common chemical methods of analysis for benzethidine:
Thin-Layer Chromatography (TLC): TLC can be used to separate and
analyze benzethidine along with reference standards. Visualization can be
achieved using UV light or chemical staining reagents.
High-Performance Liquid Chromatography (HPLC): HPLC is a technique
for the separation, identification, and quantification of compounds in a
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mixture. Benzethidine can be analyzed using HPLC with various detectors
such as UV-Vis or mass spectrometry.
Gas Chromatography-Mass Spectrometry (GC-MS): GC-MS can be used to
analyze benzethidine by separating its components using gas
chromatography and identifying them based on their mass spectra.
Nuclear Magnetic Resonance (NMR) Spectroscopy: NMR spectroscopy can
provide information about the molecular structure of benzethidine by
analyzing the nuclear spin properties of its atoms.
Fourier Transform Infrared (FTIR) Spectroscopy: FTIR spectroscopy can
be used to analyze the functional groups present in benzethidine by
measuring the absorption of infrared radiation.
Elemental Analysis: Elemental analysis techniques such as combustion
analysis or elemental CHN analysis can be used to determine the
elemental composition of benzethidine, providing information about its
purity and chemical formula.
Chemical Reactions: Benzethidine can undergo various chemical reactions
that can be used for its identification and characterization. For example, it
can be reacted with specific reagents to form characteristic derivatives,
which can then be analyzed using chromatographic or spectroscopic
techniques.
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BENZYLMORPHINE
Scientific Name: It is also known as peronine or 3-Benzylmorphinan.
Molecular Structure:
A) Physical properties:-
Appearance: Benzylmorphine typically appears as a white or off-white
crystalline powder or as small crystals. It is a compound with a molecular
structure represented by the chemical formula C24H25NO3, belonging to
the class of morphinans characterized by a four-ring skeleton with three
benzene rings fused to a nitrogen-containing six-membered ring.
Colour: Benzylmorphine is typically white in color.
Odour: The odor of Benzylmorphine typically does not have a distinct
odour,
But described as having a slight acetic odour.
Taste: Benzylmorphine generally has a slightly bitter taste.
Melting Point: The melting point of Benzylmorphine is approximately
194-198°C (381-388°F).
Boiling Point: The boiling point of Benzylmorphine is approximately 355-
360°C (671-680°F) at standard atmospheric pressure.
Solubility :
Water: Benzylmorphine is sparingly soluble in water. Benzylmorphine is
only slightly soluble in water. This means that it dissolves to a limited
extent in water, forming a clear or slightly cloudy solution. The solubility
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of benzylmorphine in water is relatively low compared to its solubility in
organic solvents like ethanol or chloroform.
Alcohol: Benzylmorphine is more soluble in alcohol than in water. In
alcohol, such as ethanol, compared to water. It dissolves more readily in
alcohol, forming a clear solution.
B) Chemical properties:
Chemical Formula: The chemical formula of Benzylmorphine is
C21H23NO3.
Chemical Classification: Benzylmorphine belongs to the chemical class of
morphinan alkaloids. Which is a type of organic compound containing a
tetracyclic ring structure known as a morphinan skeleton. Morphinan
alkaloids are derived from the opium poppy plant (Papaver somniferum)
and exhibit various pharmacological effects, including analgesic (pain-
relieving) and antitussive (cough-suppressing) properties.
Benzylmorphine specifically contains a benzyl group attached to the
morphinan skeleton, distinguishing it from other morphinan alkaloids.
Functional Group: The functional group present in Benzylmorphine is the
benzyl group, which is characterized by a phenyl ring attached to a
methylene (CH2) group.
PH: The pH of Benzylmorphine is not commonly reported or relevant as it
is typically used as a pharmaceutical compound rather than in a solution
where pH would be a significant factor. Therefore, specific information
regarding the pH of Benzylmorphine may not be readily available.
How it is Made ? From where it is obtained ?
Benzylmorphine is typically synthesized from morphine, which is
obtained from the opium poppy plant (Papaver somniferum). The synthesis
involves the introduction of a benzyl group (C6H5CH2) onto the morphinan
skeleton of morphine through chemical reactions. This process typically involves
the use of various reagents and catalysts to facilitate the desired chemical
transformations. Benzylmorphine can be obtained through laboratory synthesis in
pharmaceutical settings for research or medicinal purposes. It is not commonly
found naturally but is produced synthetically for pharmaceutical use.
benzylmorphine can be obtained through organic synthesis techniques. However,
it is important to note that the synthesis of benzylmorphine outside of regulated
laboratory settings is illegal and highly discouraged due to its classification as a
controlled substance.
Route of Administration: Benzylmorphine, like other opioids, can be
administered through various routes, each with its own onset of action, duration of
effect, and potential side effects. The most common routes of administration for
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benzylmorphine are oral, intravenous (IV), intramuscular (IM), and subcutaneous
(SC).
Oral Administration: Benzylmorphine can be taken orally in the form of
tablets, capsules, or solutions. When taken orally, it is absorbed through
the gastrointestinal tract and metabolized in the liver before reaching
systemic circulation. This route of administration typically has a slower
onset of action compared to parenteral routes.
Intravenous (IV) Administration: Benzylmorphine can be administered
intravenously by injecting it directly into a vein. This route allows for
rapid onset of action as the drug bypasses the gastrointestinal tract and is
immediately distributed throughout the bloodstream. IV administration is
often used in medical settings for acute pain management or in emergency
situations.
Intramuscular (IM) Administration: Benzylmorphine can also be
administered intramuscularly by injecting it into a muscle. This route
provides a relatively rapid onset of action as the drug is absorbed directly
into the bloodstream from the muscle tissue. IM administration is
commonly used when IV access is not available or when sustained release
formulations are needed.
Subcutaneous (SC) Administration: Benzylmorphine can be administered
subcutaneously by injecting it into the fatty tissue layer just beneath the
skin. This route allows for slow and sustained absorption of the drug into
the bloodstream, leading to a prolonged duration of action. SC
administration is often used for chronic pain management or in palliative
care settings.
Pharmacological Action: Benzylmorphine is an opioid analgesic that exerts its
pharmacological actions primarily through interaction with opioid receptors in the
central nervous system (CNS). Here are the detailed pharmacological actions of
benzylmorphine:
Analgesia: Benzylmorphine acts as an analgesic by binding to mu-opioid
receptors in the brain and spinal cord. Activation of these receptors
inhibits the transmission of pain signals and alters the perception of pain,
resulting in pain relief. Benzylmorphine is effective in relieving moderate
to severe pain, including both acute and chronic pain conditions.
Respiratory Depression: Like other opioids, benzylmorphine can cause
respiratory depression by suppressing the activity of the respiratory
centers in the brainstem. This effect can lead to decreased respiratory rate
and depth, which may result in respiratory insufficiency or respiratory
arrest, particularly in high doses or in individuals with compromised
respiratory function.
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Sedation: Benzylmorphine has sedative properties, which can lead to
drowsiness, lethargy, and a general feeling of calmness or relaxation. This
effect is mediated through the modulation of neurotransmitter activity in
the CNS, including the inhibition of noradrenaline release and the
enhancement of GABAergic neurotransmission.
Euphoria and Mood Alteration: Benzylmorphine can induce feelings of
euphoria, well-being, and pleasure, commonly referred to as a "high." This
effect is mediated by the activation of mu-opioid receptors in the brain's
reward pathway, leading to the release of dopamine and other
neurotransmitters associated with pleasure and reward.
Physical Dependence and Tolerance: Prolonged use of benzylmorphine
can lead to the development of physical dependence, where the body
becomes adapted to the presence of the drug and experiences withdrawal
symptoms upon discontinuation. Additionally, tolerance may develop,
requiring higher doses of the drug to achieve the same level of analgesia.
Gastrointestinal Effects: Benzylmorphine can cause constipation by
decreasing gastrointestinal motility through the activation of opioid
receptors in the enteric nervous system. This effect is due to the inhibition
of acetylcholine release and subsequent smooth muscle relaxation in the
gastrointestinal tract.
Cardiovascular Effects: Benzylmorphine can cause peripheral vasodilation
and orthostatic hypotension, leading to a decrease in blood pressure.
These effects are mediated by the release of histamine and the inhibition
of sympathetic nervous system activity.
Antitussive Activity: Benzylmorphine exhibits antitussive (cough-
suppressing) activity by acting on the cough center in the medulla
oblongata of the brainstem. It reduces the sensitivity of the cough reflex
and suppresses coughing.
Analysis:
Physical method: The physical methods of analysis for benzylmorphine involve
techniques used to determine its physical properties and characteristics without
chemical alteration. These methods provide valuable information about the
substance's identity, purity, and physical state. Some common physical methods of
analysis for benzylmorphine include:
Melting Point Determination: Melting point determination is a simple and
widely used method to assess the purity of benzylmorphine. By comparing
the observed melting point with the known literature value, the identity
and purity of the sample can be confirmed.
Boiling Point Determination: Boiling point determination can be used to
characterize the volatility and thermal stability of benzylmorphine.
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