MindMap Gallery Medicinal Chemistry-Narcotics
Medicinal chemistry, basic knowledge compilation, the main contents include: general anesthetics (inhalation anesthesia, non-inhalation anesthesia intravenous anesthesia) and local anesthetics (classification of local anesthetics, structure-activity relationship of local anesthesia, key drugs of local anesthetics).
Edited at 2022-06-19 23:52:30This is a mind map about bacteria, and its main contents include: overview, morphology, types, structure, reproduction, distribution, application, and expansion. The summary is comprehensive and meticulous, suitable as review materials.
This is a mind map about plant asexual reproduction, and its main contents include: concept, spore reproduction, vegetative reproduction, tissue culture, and buds. The summary is comprehensive and meticulous, suitable as review materials.
This is a mind map about the reproductive development of animals, and its main contents include: insects, frogs, birds, sexual reproduction, and asexual reproduction. The summary is comprehensive and meticulous, suitable as review materials.
This is a mind map about bacteria, and its main contents include: overview, morphology, types, structure, reproduction, distribution, application, and expansion. The summary is comprehensive and meticulous, suitable as review materials.
This is a mind map about plant asexual reproduction, and its main contents include: concept, spore reproduction, vegetative reproduction, tissue culture, and buds. The summary is comprehensive and meticulous, suitable as review materials.
This is a mind map about the reproductive development of animals, and its main contents include: insects, frogs, birds, sexual reproduction, and asexual reproduction. The summary is comprehensive and meticulous, suitable as review materials.
Narcotics
general anesthetic
inhalation anesthesia
Halothane
Trifluorochlorobromoethane, F3C-CHBRCL
Colorless, clear and easy-flowing liquid, non-flammable and explosive. It can slowly decompose when exposed to light, heat and moist air.
Used for general anesthesia and induction anesthesia, but may cause some damage to the liver
Isoflurane
F3C-CHCL-O-CHF2, 1-chloro-2,2,2-trichloroethyl difluoromethyl ether
Ethers, stable and non-toxic
It has a mild inhibitory effect on myocardium and does not increase sensitivity to the adrenal gland. It has a muscle relaxing effect and enhances non-depolarizing muscle relaxation (tubocurarine).
Ketamine
It has chiral carbon atoms and is optically active. The dextrorotary form is highly active, but its racemate in vitro
Ketamine is primarily metabolized to the active norketamine
Anesthesia has a short effect and is prone to hallucinations. It is abused as a drug and belongs to the management of Class I psychotropic drugs.
Sodium gamma-hydroxybutyrate
Also known as sodium oxybate, white crystalline powder, hygroscopic, easily soluble in water
The anesthetic effect is weak, but the toxicity is low. It is used together with other anesthetics or tranquillizers to induce anesthesia and maintain anesthesia.
Management of Class I psychotropic drugs
Non-inhalational anesthesia (intravenous anesthesia)
local anesthetic
Classification of local anesthetics
Structure-activity relationship of local anesthesia
lipophilic part
In necessary parts, effective local anesthesia is mostly benzene rings or aromatic heterocycles with different substituents. The activity of aromatic heterocycle substitution is less than that of benzene ring substitution.
The effect of introducing electron-donating groups on the benzene ring is enhanced, while the effect of introducing electron-withdrawing groups is weakened.
middle connecting part
The duration and intensity of anesthetic effects are related to
The sequence of action is: -CH2->-NH->-S->-O-
The order of its anesthetic intensity is: -S->-O->-CH2->-NH-
hydrophilic part
Usually the amino part
Tertiary amines are common and easily form soluble salts
Primary amines and quaternary amines are more irritating, and quaternary amines are no longer used due to their curare-like effects.
If the hydrophilic part is a heterocyclic ring, the piperidine ring has the strongest effect
Key drugs of local anesthetics
Procaine hydrochloride
The molecule contains ester bonds and is easily hydrolyzed. After hydrolysis, para-aminobenzoic acid and diethylaminoethanol are generated, and the local anesthetic effect disappears.
Under certain conditions, para-aminobenzoic acid can be further decarboxylated into toxic aniline
It has primary aromatic amine groups and is easily oxidized and discolored.
Local anesthetic, stronger effect, less toxic, shorter effect
It is mainly used clinically for infiltration anesthesia and conduction anesthesia. Due to its poor penetrating power, it is generally not used for topical anesthesia.
Tetracaine hydrochloride
This product has an n-butyl group attached to the nitrogen atom of the primary aromatic amine group, making it a secondary amine.
The structure does not contain primary aromatic amine groups, and is generally not easily oxidized and discolored, and cannot be identified by diazotization coupling reaction.
Hydrolyzability is similar to procaine, but slightly slower
The anesthetic effect is 10-15 times stronger than that of procaine, with strong penetrating power and rapid effect, but it is also highly toxic.
Mostly used for mucosal anesthesia and epidural anesthesia
lidocaine hydrochloride
Contains an amide bond. There are two methyl groups adjacent to the amide bond, creating steric positions that hinder its hydrolysis. Therefore, this product is relatively stable to acids and alkalis, and is difficult to hydrolyze under normal conditions.
It has a strong anesthetic effect, twice that of procaine, with strong penetrating power and fast onset of action. It is considered an ideal local anesthetic and is used for various anesthesia and in the treatment of arrhythmias (Class IB).