Selectively inhibits the medullary cough center to produce a rapid and long-lasting antitussive effect. The antitussive effect is powerful. The antitussive strength is 1/4 of morphine. The therapeutic dose has no respiratory depressant effect.

The analgesic intensity is 1/10-1/7 of morphine, which is stronger than general antipyretic, analgesic and anti-inflammatory drugs.

Severe, non-phlegm dry cough and moderate pain when other antitussives are ineffective, especially suitable for pleurisy patients with dry cough and chest pain

Continuous application can develop tolerance and dependence

Not suitable for patients with poor respiratory function, excessive phlegm and pregnant women

Reflexively causes the secretion of respiratory glands to increase, allowing sputum to be sucked out and facilitated coughing up.

Acidify blood and body fluids

It is often combined with other drugs to form compound preparations and is used clinically for patients with acute and chronic respiratory inflammation who have sticky phlegm that is difficult to cough up.

It is contraindicated in patients with peptic ulcer, metabolic acidosis and severe liver and kidney dysfunction.

Cleavage of disulfide bonds in mucin

It is used in emergencies with difficulty in the respiratory tract caused by a large amount of sticky sputum blocking the trachea, or for those who have difficulty coughing up sputum due to surgery. Administer by tracheal instillation or injection.

For non-emergency coughs with thick sputum and difficulty, use aerosol inhalation

It has a special smell of garlic, which is irritating to the respiratory tract and can easily cause choking and even bronchospasm.

Used alternately or combined with isoproterenol, it can reduce the occurrence of adverse reactions and improve the efficacy.

Not suitable for asthma patients

Directly injecting or dripping into the trachea will quickly produce a large amount of thin sputum, which can easily block the trachea. Therefore, before instilling into the trachea, preparations must be made to aspirate and expel phlegm, and cooperate with the suction and expulsion in time. Do not drip or inject directly into the trachea without a sputum suction device. , to prevent sputum suction from blocking the trachea

It is not suitable to be used in combination with penicillins, cephalosporins and tetracyclines as it may reduce the antibacterial activity of these antibiotics.

Prevent and treat bronchial asthma, wheezing bronchitis, emphysema, etc. accompanied by bronchospasm

Oral administration to prevent asthma, and multiple aerosol inhalation or intravenous administration to control acute attacks

Its sustained and controlled release preparation can prolong the action time and is suitable for those who prevent sudden attacks of asthma at night.

Excessive use can cause arrhythmia, and long-term use can reduce the density of β2 receptors in bronchial smooth muscle, which can easily lead to tolerance, which not only reduces the efficacy, but also aggravates asthma.

Use with caution in patients with high blood pressure, cardiac insufficiency, diabetes and hyperthyroidism

Prevention and treatment of chronic bronchial asthma, oral administration

For acute attacks or persistent states of severe asthma, intravenous infusion is used, combined with beta-agonists and adrenocortical hormones to improve the efficacy.

Asthmatic bronchitis, emphysema, and bronchitis caused by other obstructive lung diseases

It has cardiotonic and diuretic effects and is used as an auxiliary treatment for cardiogenic asthma and cardiogenic edema.

Relaxes biliary smooth muscle and is used to treat biliary colic

Can dilate peripheral blood vessels and excitatory centers

Oral administration may cause gastrointestinal reactions, which can be alleviated by taking them after meals; intramuscular injection may cause local redness, swelling and pain.

Long-term application may develop tolerance

central excitability

Acute poisoning - a safe dose must be used and the injection must be diluted and injected slowly

It is contraindicated in patients with hypotension, shock, and acute myocardial infarction.

Long-term application has no inhibitory effect on adrenocortical function, and can be used in patients with moderate or severe asthma at low doses for long periods of time or high doses for short periods of time.

It is not suitable to be used as a rescue drug for acute attacks and persistent asthma. It can be used as a treatment drug for intermittent asthma attacks and chronic asthma.

Inhalation administration tends to leave medicinal liquid in the pharynx. Long-term inhalation may cause hoarseness in a few patients and infection of the oral cavity and pharynx. Rinsing the mouth repeatedly after aerosol inhalation can significantly reduce the incidence.

Drug of choice for chronic asthma

When neutralizing gastric acid, it is easy to produce a large amount of carbon dioxide, increase the pressure in the stomach, and cause reactions such as abdominal distension and belching. Patients with severe ulcer disease are at risk of gastrointestinal perforation.

It should not be used alone to treat hyperacidity and is often used in combination with other drugs.

Intravenous infusion can alkalize body fluids and is used for metabolic acidosis

Oral or intravenous infusion can also be used to rescue acidic drug poisoning such as barbiturates and aspirin, and to alkalize urine to accelerate its excretion.

Combining with aminoglycoside antibiotics to treat urinary tract infections can enhance its antibacterial effect

Neutralizes gastric acid quickly and powerfully

After neutralizing gastric acid, a large amount of carbon dioxide is produced. Calcium ions entering the intestine can cause the release of gastrin, which in turn leads to increased rebound gastric acid secretion.

Has astringent effect and can cause constipation

A gel can form in the gastric juice and cover the surface of the ulcer and mucosa, preventing gastric acid and pepsin from contacting the ulcer surface and gastric mucosa, playing a protective role.

No ulcer surface protection effect

Oral administration has a cathartic effect and can produce mild diarrhea. Combined with aluminum hydroxide, it can relieve

Pharmacological effects

Clinical application

Adverse reactions

interaction

second generation

The therapeutic amount does not affect serum prolactin and androgen concentrations, does not cause endocrine disorders, and has no adverse reactions to the central nervous system.

Too fast intravenous injection can slow down the heart rate, inhibit myocardial contractility, and lead to bradycardia.

It is contraindicated for children under 8 years old, and should be used with caution by women. The half-life is significantly prolonged in patients with liver and kidney dysfunction.

three generations

Potent, long-acting H2 receptor antagonist

Take before meals

It has a strong inhibitory effect on gastric acid secretion caused by basal gastric acid, insulin, and pentagastrin, and it also has the effect of relieving gastrointestinal smooth muscle spasm.

For gastric and duodenal ulcers

Combination with cimetidine may enhance efficacy

It can competitively block gastrin receptors, antagonize the effect of gastrin, inhibit the secretion of gastric acid and pepsin, and at the same time increase the synthesis of hexosamines in the gastric mucosa, which has a protective effect on the gastric mucosa and can promote the healing of gastric ulcers.

Mainly used for gastric and duodenal ulcers and gastritis

generation

Take on an empty stomach

It easily enters gastric parietal cells and selectively forms an enzyme inhibitor complex with H-K-ATPase to inhibit its function of transporting H to the gastric cavity, thereby inhibiting gastric acid secretion.

It has a strong inhibitory effect on gastric acid secretion in both normal people and patients with ulcer disease. One administration can inhibit gastric acid secretion for more than 24 hours.

It can increase gastric mucosal blood flow and inhibit Helicobacter pylori, which is beneficial to ulcer healing.

Suitable for gastric and duodenal ulcers, Zollinger-Ellison syndrome and reflux esophagitis

It is not advisable to take it with antacids. For those with reduced liver function, the dosage should be reduced as it can inhibit the activity of liver enzymes.

Second generation proton pump inhibitors

It is better than omeprazole in inhibiting gastric acid secretion and anti-Helicobacter pylori. It has a faster onset of action, similar uses and adverse reactions to omeprazole.

three generations

It is more effective than the previous two generations of drugs in inhibiting gastric acid secretion, relieving symptoms, and curing mucosal damage, and has mild adverse reactions.

After oral administration, bismuth oxide colloid is formed in an acidic environment, covering the ulcer surface and basal granulation tissue, forming a strong insoluble protective film, blocking gastric acid, pepsin, etc. from irritating and corroding the ulcer surface.

Inhibit pepsin activity, promote gastric mucus secretion, protect ulcer surface, and facilitate ulcer repair and anastomosis

Combined with antacids to produce a synergistic effect to inhibit Helicobacter pylori

For peptic ulcer and chronic gastritis, the efficacy is equivalent to that of H2 receptor antagonists. Because it has both gastric mucosal protection and anti-Helicobacter pylori effects, the recurrence rate is low.

There may be ammonia smell in the mouth during taking the medicine, which can make the mouth, tongue and stool black. Occasionally, nausea and vomiting may occur, which will disappear after stopping the medicine.

Antacids and milk can interfere with its action and reduce its efficacy; they also affect the absorption of tetracycline, so they should not be taken together.

Not suitable for people with renal insufficiency and pregnant women

Blocks M1 receptors, reduces the sensitivity of labyrinth receptors and inhibits the conduction of the vestibulocerebellar pathway, producing anti-motion sickness and preventing nausea and vomiting.

Pre-anesthetic administration, motion sickness, vomiting, Parkinson's disease, etc.

It has no obvious effect on central dopamine receptors, but can selectively block peripheral dopamine receptors, with high gastrointestinal selectivity, enhance esophageal peristalsis and the tension of the lower esophageal sphincter, prevent gastro-esophageal reflux, and enhance gastric and upper intestinal peristalsis. , strengthen gastrointestinal motility, prevent duodenal-gastric reflux, have gastrointestinal motility and efficient antiemetic effects

Mainly used for functional dyspepsia, reflux esophagitis, chronic atrophic gastritis, bile reflux gastritis and gastroparesis caused by slow gastric emptying.

Used for nausea and vomiting caused by dysmenorrhea, migraine, craniocerebral trauma or intracranial lesions, tumor chemotherapy or radiotherapy, food and other factors.

Take medication before esophagoscopy and gastroscopy to prevent nausea and vomiting during the examination

Can increase prolactin levels and return to normal on their own after stopping the drug

Injection administration can cause cardiac arrhythmias

Pregnant women and those who are allergic to this drug are prohibited from using it. Use with caution in infants.

It should not be used in combination with anticholinergic drugs, otherwise the efficacy will be reduced

Blocks gastrointestinal dopamine receptors, promotes the release of acetylcholine from gastrointestinal cholinergic nerves, strengthens smooth muscle movement from the esophagus to the proximal small intestine, and exerts gastrointestinal motility effects

Blocks dopamine receptors in the medulla oblongata's emetic chemoreceptor area, producing a strong central antiemetic effect

Blocks hypothalamic dopamine receptors, reduces the release of prolactin inhibitory factors, thereby increasing serum prolactin levels, and has a certain prolactin effect

Chronic functional dyspepsia, reflux esophagitis, bile reflux gastritis, and diabetic gastroparesis

Used for nausea and vomiting caused by tumor chemotherapy or radiotherapy, stomach diseases, brain diseases, dysmenorrhea, postoperative surgery, drugs, pregnancy, etc.

postpartum oligogalactia

Large doses or long-term use can cause extrapyramidal reactions, mainly manifested as Parkinson's syndrome, which can be counteracted by central anticholinergics such as trihexyphenidyl.

hyperprolactinemia

Injectable administration can cause orthostatic hypotension

More side effects

It has high selectivity for gastrointestinal M receptors and has fewer side effects. It is mainly used clinically to treat gastrointestinal spasmodic diseases.

local effect

Systemic effects

Too fast or excessive intravenous injection and excessive Mg2 in the blood may easily cause poisoning, which may manifest as a sharp drop in blood pressure, loss of tendon reflexes, respiratory depression or even cardiac arrest and death. If this occurs, immediate intravenous calcium rescue and artificial respiration should be performed at the same time.

When used for catharsis, it has a strong effect, irritating the intestinal wall and causing pelvic congestion. Pregnant women, menstruating women, and patients with acute abdomen are contraindicated.

Magnesium sulfate can inhibit the central nervous system after being absorbed in a small amount. Therefore, it should not be used as a cathartic when poisoning with central nervous system inhibitor drugs. Sodium sulfate should be used as a cathartic to prevent aggravation of poisoning. It is mainly excreted by the kidneys. It is forbidden or used with caution in patients with renal insufficiency.

Excites uterine smooth muscle

Promote milk excretion

Large doses can induce short-term relaxation of vascular smooth muscles, causing a temporary decrease in blood pressure, and have a mild anti-diuretic effect.

inducing labor, inducing labor

Postpartum hemostasis (replaced by ergometrine)

lactation

Occasionally nausea, vomiting, arrhythmia, drop in blood pressure, etc.

Overdose can cause high-frequency or even sustained tonic contractions of the uterus, which can lead to intrauterine asphyxia or uterine rupture.

Strictly control the dosage, and adjust the intravenous drip speed in time according to uterine contractions, fetal heart rate and maternal conditions to avoid uterine tonic contractions.

Strictly control the indications. It is contraindicated for women with abnormal birth canal, abnormal fetal position, cephalopelvic disproportion, placenta previa, history of cesarean section or more than 3 pregnancies to avoid fetal asphyxia or uterine rupture.

Oxytocin and ergometrine have a synergistic effect. Their combined use can cause uterine rupture due to excessive muscle tone. Calcium channel blockers can reduce the efficacy of oxytocin, so avoid using them together.

The contraction effect on the uterus in early and mid-pregnancy is much stronger than that of oxytocin, and it is more effective on the uterus in late pregnancy. It is most sensitive to the uterus before labor, and can cause high-frequency and large-scale uterine smooth muscle contractions that can lead to abortion.

Dinoprostone not only enhances the rhythmic contraction of uterine smooth muscle, but also relaxes the cervix, causing the uterus to produce spasms similar to those during childbirth.

Produce functional dissolution of the ovarian corpus luteum, degenerate the corpus luteum, promote its atrophy and dissolution, reduce the production and secretion of progesterone, cause the level of progesterone in the blood to drop sharply, and cause the endometrium to fall off and form menstruation.

Affect fallopian tube activity and prevent fertilized eggs from implanting

Ergometrine

Ergotamine

Ergot

Ergometrine has the fastest and strongest effect

The intensity of the effect depends on the functional status of the uterus. It is stronger on the pregnant uterus than on the non-pregnant uterus, and is strongest on the uterus during labor and newly postpartum.

The effect is stronger than oxytocin and long-lasting. A slightly larger dose can cause uterine tonic contractions.

There is no significant difference in the excitatory effects on the uterus and cervix, so it cannot be used to induce or expedite labor.

Ergotamine can directly act on blood vessels, constricting both veins and arteries. It can also constrict cerebral blood vessels, reduce cerebral artery pulsation amplitude, and is used to relieve migraines.

Dihydroergotine, the hydride of ergot poison, has the effect of blocking α-receptors and inhibiting the vasomotor center, and can dilate blood vessels.

Used for uterine bleeding caused by postpartum, dilation and curettage, menorrhagia, etc.

Intramuscular injection of ergometrine uses its ability to produce tonic contractions of uterine smooth muscle to mechanically compress the blood vessels in the muscle layer to stop bleeding. If necessary, repeat the administration once after 30 minutes.

Utilizing the uterine-stimulating effect of ergometrine, especially its sensitivity to the newly born postpartum uterus, it accelerates uterine contraction and recovery.

Ergot fluid extract is often used

Mainly used in combination with caffeine, ergotamine can produce synergistic effects

Caffeine has the effect of constricting cerebral blood vessels and promoting the absorption of ergotamine

Do not use large doses for a long time in the treatment of migraine, otherwise it will damage the endothelial cells of blood vessels and cause necrosis of the limbs. Limit the use to 2-4 days.