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To deal with vomiting caused by different reasons, how to choose 10 types of antiemetics?

 Last Update: 2022-04-22
 Source: Internet
 Author: User

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Nausea and vomiting is one of the most common clinical symptoms.
It seems simple, but it is not easy to find the cause
.

Nausea and vomiting is a complex physiological reflex process through the synergistic action of stomach, esophagus, oral cavity, diaphragm and abdominal muscles, so that gastric contents are excreted through esophagus and oral cavity

Nausea and vomiting is one of the most common clinical symptoms.

Nausea and vomiting is a special supervisory feeling, manifested as stomach discomfort and fullness, usually a prelude to vomiting, often accompanied by salivation and repeated swallowing, and in severe cases accompanied by headache, dizziness, sweating, and pale complexion and increased heart rate

There are many causes of nausea and vomiting, which are clinically divided into reflex vomiting and central vomiting

The treatment of nausea and vomiting

2.
Nausea and Vomiting Treatment 2.
Nausea and Vomiting Treatment

Because there are many diseases that cause nausea and vomiting, it should not be used blindly until the cause is not clear
.

The treatment principles of nausea and vomiting include etiological treatment, symptomatic treatment and correction of water and electrolyte imbalance

Because there are many diseases that cause nausea and vomiting, it should not be used blindly until the cause is not clear

If the cause of nausea and vomiting is clear, treatment of the underlying disease can be controlled

A variety of neurotransmitters and receptors are involved in the occurrence of nausea and vomiting.

1) Antihistamines

H1 receptor blockers commonly used by antihistamines inhibit the gag reflex mainly by inhibiting the vomiting center and acting on cholinergic neurons in the vestibular nucleus and reticular structure
.

H1 receptor blockers mainly include promethazine, meclizine, chlorpheniramine, astemizole and other drugs

2) Anticholinergics

There are many types of anticholinergic drugs, such as atropine , anisodamine , and scopolamine .
Atropine and anisodamine mainly reduce the excitability of the vagus nerve, increase the tension of the cardiac sphincter , relieve gastrointestinal spasm, prevent vomiting and reflux, and are often used to prevent preoperative vomiting .
And scopolamine is a post-ganglionic anticholinergic drug, which can inhibit the central nervous system, has effects on sedation, hypnosis and antiemetic, and has a good effect on nausea and vomiting caused by motion sickness .
However, anticholinergic drugs also have some adverse effects, such as dry mouth, flushing, and increased heart rate .

3) Drugs that promote gastrointestinal motility

Currently commonly used drugs are metoclopramide, domperidone, cisapride and erythromycin
.
Metoclopramide, a derivative of procainamide, blocks dopamine receptors, thereby reducing the urge to nausea and vomiting
.
At the same time, metoclopramide can promote pyloric peristalsis, dilate the pyloric canal, shorten gastric emptying time, and enhance the sensitivity of gastric smooth muscle to acetylcholine, thereby improving gastric peristalsis
.

4) 5-HT antagonists

90% of 5-HT in the body is secreted by chromaffin cells in the gastrointestinal mucosa, which can activate the 5-HT3 receptors in the intestinal mucosa and central CTZ , while 5-HT3 receptor antagonists selectively block peripheral and central 5 -HT3 receptors.
-HT3 receptor, thereby effectively controlling vomiting caused by chemotherapy .

At present, selective 5-HT3 receptor antagonists have been synthesized and widely used in clinical practice
.
Among them, commonly used drugs for 5-HT3 receptor antagonists include ondansetron, gripristone, tropisetron and the like
.
5-HT3 receptor antagonists were first used for vomiting caused by chemotherapy, and of course, it is also effective for vomiting caused by radiotherapy and surgery
.
When patients are ineffective against other antiemetics, 5-HT3 receptor antagonists are used
.
5-HT3 receptor antagonists are widely tolerated and have few adverse reactions, usually mild and moderate headache, dizziness, constipation and diarrhea
.

5) Phenothiazines

Phenothiazines mainly exert antiemetic effects by selectively inhibiting CTZ or (and) directly reducing the excitability of the medulla oblongata emesis center.
Commonly used drugs include chlorpromazine, promethazine, perphenazine, trifluoperazine and Prochlorperazine,
etc.
This class of drugs has a good effect on nausea and vomiting caused by certain drugs (such as opioids, anesthetics and chemotherapy drugs), and is also effective on cardiac vomiting caused by radiotherapy and gastrointestinal lesions
.

Chlorpromazine is the most commonly used clinically, and its only mechanism of action is mainly to inhibit CTZ , and it can also counteract the emetic effect of apomorphine
.
Preoperative application of chlorpromazine can reduce postoperative nausea and vomiting vocalization rate by 50% ; if the drug is used therapeutically after operation, nausea and vomiting symptoms can be controlled in about 30% of patients .
Promethazine has sedative and strong antihistamine effect, can inhibit CTZ and vestibular system .

6) Butyryl benzene drugs

Butyrylbenzene drugs mainly produce strong anti-emetic effects by inhibiting CTZ in the central nervous system, and have a good effect on the prevention and treatment of postoperative nausea and vomiting.
Commonly used drugs are haloperidol, droperidol and so on
.
Intramuscular injection of haloperidol 1 mg , within 1 to 5 hours, 80% to 100% of postoperative nausea and vomiting can be controlled
.
The antiemetic effect of droperidol is better than that of haloperidol.
The drug takes effect in 5 to 8 minutes after intravenous injection, and the best effect lasts for 3 to 6 hours
.
However, butyrylphenone drugs often have adverse reactions such as drowsiness, anxiety, delayed extrapyramidal reactions, delayed postoperative recovery, respiratory depression and hypotension
.

7) Cannabinoids

The mechanism of action of cannabinoids is not clear, it may be related to the frontal lobe, reflex inhibition of the medulla oblongata vomiting center related to mental activity
.
Commonly used drugs in this category include tetrahydrocannabinoids and peptafenone, which are mainly used for the antiemetic effect of chemotherapy drugs-induced nausea and vomiting
.
Oral administration of heptaphenone 30 minutes before chemoprevention is 80% effective against nausea and vomiting .
Its effect is significantly better than that of phenothiazines, but these drugs have more adverse reactions, such as drowsiness, dry mouth, and blurred vision.
etc.
_

8) NK1 receptor antagonists

Substance P ( substance P , SP ) is a polypeptide containing 11 amino acids and belongs to the tachykinin (also known as neurokinin) family.
The tachykinin receptors include NK-1 , NK-2 and NK-3 , of which P The substance has the strongest affinity with NK-1 .
SP is emetic, and selective NK-1 receptor antagonists can inhibit its emetic .

The main drugs for NK1 receptor antagonists are aprepitant and fosaprepitant
.
Aprepitant is the first NK1 receptor antagonist approved for clinical use
.
Combined use with 5-HT3 receptor antagonists further reduces cisplatin-induced acute and delayed emesis
.
The Professional Committee of Cancer Rehabilitation and Palliative Care of the Chinese Anti-Cancer Association released the 2014 edition of the " Guidelines for the Prevention and Treatment of Vomiting Related to Cancer Treatment in China ", which proposed the principle of prevention-based treatment and recommended the " triple regimen " - aprepitant, 5 - HT3 Antibody antagonists, combined with dexamethasone as the first-line chemotherapy and antiemetic treatment, this program is basically consistent with the US NCCN guidelines
.
Aprepitant is well tolerated, and common adverse reactions include anorexia, weakness, fatigue , constipation, diarrhea, nausea and vomiting, and the incidence is between 10 % and 18% .

The main drugs for NK1 receptor antagonists are aprepitant and fosaprepitant
.
Aprepitant is the first NK1 receptor antagonist approved for clinical use
.
Combined use with 5-HT3 receptor antagonists further reduces cisplatin-induced acute and delayed emesis
.
The Professional Committee of Cancer Rehabilitation and Palliative Care of the Chinese Anti-Cancer Association released the 2014 edition of the "Guidelines for the Prevention and Treatment of Vomiting Related to Cancer Treatment in China " , proposing the principle of prevention-based treatment, and recommending the " triple regimen " - aprepitant, 5-HT3 Receptor antagonists, combined with dexamethasone as first-line chemotherapy and antiemetic treatment, this program is basically consistent with the US NCCN guidelines
.
Aprepitant is well tolerated, and common adverse reactions include anorexia, weakness, fatigue , constipation, diarrhea, nausea and vomiting, and the incidence is between 10 % and 18% .

9) Glucocorticoids

Glucocorticoids can be used to treat chemotherapy-related vomiting and also to relieve nausea and vomiting caused by increased intracranial pressure.
The commonly used drug is dexamethasone
.
However, the mechanism of action of glucocorticoids has not yet been clarified, and some studies suggest that it may have anti-inflammatory and antitoxin effects, reduce peripheral nerve damage, maintain normal gastrointestinal motility, and reduce delayed vomiting
.
In addition, some scholars believe that the antiemetic effect is achieved by inhibiting the production and release of 5-HT through both peripheral and central pathways .

10 ) Benzodiazepines _

Short-acting benzodiazepines are often used to relieve nausea, but their antiemetic effect is weak, and the drug of choice is lorazepam
.
These drugs are mainly used for sedation and anti-anxiety, so they have a good effect on nausea and vomiting related to anxiety, and can also improve the efficacy of other antiemetic drugs, and can also prevent vomiting
.

References

1.
Wang Mengjun .
Research and development status and development trend of antiemetic drugs [J].
Shanghai Pharmaceuticals , 2014, 35(17):6.

2.
Yu Jieping , Shen Zhixiang , Luo Hesheng .
Practical Gastroenterology ( Second Edition ) ( Essential ) [M].
Science Press , 2007.

2.
Yu Jieping , Shen Zhixiang , Luo Hesheng .
Practical Gastroenterology Digestion ( Second Edition ) ( Essential ) [M].
Science Press , 2007.
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