intrinsic resistance

acquire drug resistance

Being resistant to one drug is also resistant to other antibacterial drugs with different structures and different targets, which is one of the important reasons for the failure of antibacterial drug treatment.

Administer small doses multiple times to maintain drug administration, thereby prolonging drug concentration

There is often a first dose effect, often doubling the first dose to improve antibacterial activity

Avoid use if it is teratogenic or obviously toxic to the fetus.

Avoid using it if it is toxic to both the mother and fetus. When there are definite indications for use, it needs to be used under blood concentration monitoring.

The drug has low toxicity, has no obvious effects on the fetus and mother, and has no teratogenic effect. It can be used when there is infection during pregnancy.

Aminoglycosides, quinolones, tetracyclines, chloramphenicol, sulfonamides, etc. should be avoided

Breastfeeding should be suspended when using any antibacterial drugs

The renal function of the elderly is physiologically reduced. When receiving antibacterial drugs that are mainly excreted by the kidneys, the dosage should be reduced according to the reduced renal function.

Elderly patients should choose antibacterial drugs with low toxicity and bactericidal effect. Drugs with high nephrotoxicity should be avoided as much as possible - such as aminoglycosides

Aminoglycosides have obvious ototoxicity and nephrotoxicity and should be avoided as much as possible.

Vancomycin has certain ototoxicity and nephrotoxicity and can only be used when there are clear indications.

Tetracyclines can cause yellowing of teeth and enamel hypoplasia and should not be used for children under 8 years old.

Quinolones should be avoided in minors under 18 years of age due to their possible effects on bone development.

The liver and kidneys of newborns are immature, so chloramphenicol should be banned and the use of highly toxic antibacterial drugs should be avoided. When there are indeed indications for use, blood drug concentration must be monitored and the dosage regimen adjusted accordingly.

Avoid or disable the use of antibacterial drugs that may cause serious adverse reactions, such as sulfonamides and furans

Drugs that are mainly excreted by the kidneys need to be used in reduced doses

Adjust dosage regimen according to age

Intramuscular injection of antibiotics in neonates can easily cause local induration and affect drug absorption, so intramuscular injection is not suitable.

Directly affects the effect of antibacterial treatment. For example, in patients with agranulocytosis and infection, antibacterial drugs are less effective.

For patients with debilitating diseases, malnutrition or large doses of corticosteroids and other drugs that lower immune function, quick-acting bactericidal drugs should be used and given a reasonable dose and course of treatment to ensure efficacy and prevent recurrence.

Try to avoid the use of nephrotoxic antibacterial drugs. When there are indeed indications for use, the dosage regimen must be adjusted, such as amphotericin b, vancomycin, and aminoglycoside antibiotics. It is best to avoid their use.

Select antibacterial drugs with no nephrotoxicity or low nephrotoxicity based on the severity of infection, type of pathogenic bacteria and drug susceptibility test results.

Adjust the dosage and method according to the patient's degree of renal function decline and the excretion route of antibacterial drugs in the human body, and monitor blood drug concentrations if possible

Drugs that are mainly cleared by the liver, but have no obvious toxicity, should be used with caution and reduced dosage if necessary

The drug is mainly cleared or metabolized by the liver and can cause toxic reactions. Patients with reduced liver function should avoid using it.

Drugs are eliminated by the liver and kidneys. There are patients with decreased liver function and renal function. However, the drug itself is not very toxic. When using such drugs, the dosage needs to be reduced.

The drug is mainly excreted by the kidneys, and patients with reduced liver function do not need to adjust the dose.

It may be effective if used to prevent infection caused by one or two specific pathogenic bacteria invading the body; if the purpose is to prevent the invasion of any bacteria, it is often ineffective.

Preventing infections that occur over a period of time may be effective; long-term preventive medication often fails to achieve the goal

If the patient's primary disease can be cured or alleviated, preventive drugs may be effective. For example, in patients with immune deficiency, preventive drugs should be used as little or as little as possible.

Circumstances in which prophylactic antimicrobials are not usually used routinely

Purpose

in principle

People with recurrence of rheumatic fever should use benzathine penicillin or penicillin G as a prophylaxis to kill hemolytic streptococci in the throat. People who are allergic to penicillin can use erythromycin instead.

Epidemic cerebrospinal meningitis can be prevented with sulfadiazine or rifampicin

Eye drops of 1% silver nitrate or erythromycin are often given to newborns to prevent ophthalmia caused by gonorrhea or chlamydia trachomatis.

Intermittent application of SMZ-TMP prevents recurrent urinary tract infections

Penicillin or ampicillin may be used before oral, urinary tract, or cardiac surgery

Penicillin can be used to prevent the occurrence of gas gangrene when patients with complex trauma, war injuries, or vasculitis obliterans undergo amputation.

Metronidazole plus gentamicin or kanamycin should be used before or after colon surgery to prevent various aerobic or anaerobic bacterial infections after surgery.

Exert synergistic antibacterial effects to improve efficacy

Delay or reduce the development of drug resistance

Expand antibacterial spectrum

Serious infections that cannot be effectively controlled by a single antibacterial drug

Mixed infections that cannot be effectively controlled by a single antibacterial drug

Serious infection with unknown pathogenic bacteria

Those who take medicine for a long time are prone to develop drug resistance

Classification

Collaboration

Penicillin G

Acid-resistant penicillins

Enzyme-resistant penicillins

Broad spectrum penicillins

Broad-spectrum penicillins against Pseudomonas aeruginosa

Penicillins against Gram-negative bacilli

Broad antibacterial spectrum

Strong antibacterial effect

penicillinase-resistant

High efficacy

Low toxicity

The incidence of allergic reactions is lower than that of penicillins

Combined with PBPs, it inhibits the synthesis of bacterial cell wall mucopeptides. It is a bactericidal drug during the breeding period and has a synergistic effect with aminoglycoside antibiotics.

first generation

second generation

Third Generation

Fourth Generation

Stable to β-lactamase from generation to generation

The toxicity to the kidneys is getting lower from generation to generation

The first three generations are less effective against Gram-positive bacteria than the previous generation, while the antibacterial effect against Gram-negative bacteria is getting stronger with each generation.

The fourth generation has strong antibacterial activity against both Gram-positive and Gram-negative bacteria.

allergic reaction

Nephrotoxicity - first and second generation

gastrointestinal reactions

disulfiram-like reaction

Coagulopathy

clavulanic acid

sulbactam

tazobactam

Imipenem

Meropenem

Panipenem

Laxocephalosporin

Fluoxycephalosporin

aztreonam

carolimus

Irreversibly binds to the target site of the 50S subunit of bacterial ribosomes and inhibits bacterial protein synthesis.

A fast-acting bacteriostatic agent

The drug of choice for the treatment of mycoplasma pneumonia, Legionnaires' disease, diphtheria, and whooping cough is "The First Choice Red of One Hundred Air Forces" (Archie can be substituted)

Treat penicillin-resistant Staphylococcus aureus infections and other infections of the respiratory tract, soft tissue, and urinary tract caused by other sensitive bacteria

As an alternative to penicillin-allergic patients for the following infections

Strong irritation

liver damage

A few patients may develop allergic drug rash, drug fever, tinnitus, temporary deafness, etc.

Sterilization rate and sterilization duration are concentration-dependent

Only effective against aerobic bacteria, strong against aerobic Gram-negative bacilli

PAE with longer duration, concentration dependent

It has a first-contact effect and can quickly kill sensitive bacteria when exposed to this type of drug for the first time. When exposed to the same drug again or multiple times, the bactericidal effect is significantly reduced.

In alkaline environment, antibacterial activity is enhanced

There is partial or complete cross-resistance between drugs in this class

Mainly inhibits bacterial protein synthesis

It can also destroy the integrity of bacterial cell membranes, increase permeability, and cause the important contents of the bacteria to leak out and cause death.

Stationary phase bactericide

Mainly used for systemic infections caused by sensitive aerobic Gram-negative bacilli

Ototoxicity

nephrotoxicity

neuromuscular blockade

allergic reaction

tetracycline

Oxytetracycline

Chlortetracycline

Demeclocycline

Metacycline

Doxycycline

minocycline

Superinfection, hemolytic anemia

Sterilizes bacteria by inhibiting bacterial DNA gyrase and interfering with bacterial DNA replication.

Antibacterial spectrum

Suitable for infections of the genitourinary tract, respiratory tract, intestinal tract, bones, joints, skin and soft tissues caused by sensitive bacteria

It can replace penicillins and cephalosporins in the treatment of systemic infections. It can replace macrolides in the treatment of mycoplasma pneumonia, chlamydial pneumonia, and Legionnaires' disease. It can be used as the first choice drug for the treatment of typhoid fever.

gastrointestinal reactions

central nervous system reaction

Allergic Reaction-Photosensitivity

cartilage damage

Other adverse reactions

Quinolones can form complexes with multivalent metal ions, etc., thereby reducing absorption, so they should not be taken with foods or drugs containing these ions.

Antacids, anticholinergics, and H2 receptor blockers can reduce gastric acidity and reduce the absorption of quinolones, so they should be avoided.

When quinolones can inhibit the metabolism of caffeine, warfarin and theophylline in the liver, the blood drug concentration will increase and toxic reactions will occur, so combined use should be avoided.

Quinolones increase the central nervous system toxicity of NSAIDs and should be avoided in combination

Avoid combining with alkaline drugs. Quinolones can cause crystalluria, especially in alkaline urine, which can increase kidney damage.

The combined use of sefloxacin with phenothiazines, tricyclic antidepressants and antiarrhythmic drugs may increase the risk of arrhythmias and is prohibited from combined use.

The first quinolone

Mainly used for genitourinary tract, gastrointestinal tract infections and gonorrhea (acute) caused by sensitive bacteria

The in vitro antibacterial activity is the strongest among clinically applied quinolones.

Commonly used for respiratory, urogenital and gastrointestinal infections caused by sensitive bacteria

It is also used to treat infections in the mouth, skin, soft tissue, bones and joints.

Allergies and joint pain are occasionally seen, and it is contraindicated by athletes and the elderly.

Can increase methylxanthine concentration and cause toxic reactions

Used for infections of the urinary tract, respiratory tract, biliary tract, skin and soft tissue, ear, nose, throat and eyes caused by sensitive bacteria

It is also effective against Mycobacterium tuberculosis that is resistant to streptomycin, isoniazid, and para-aminosalicylic acid, and can be used as a second-line drug for the treatment of tuberculosis.

Occasionally mild central nervous system toxicity

It can be used for the prevention of surgical infections in the respiratory tract, urinary tract, pelvis, abdominal cavity, skin and soft tissue, ear, nose, throat and oral cavity caused by sensitive bacteria.

The dose is only 1/2 of ofloxacin

The adverse reactions are much lower than ofloxacin, and the main adverse reactions are gastrointestinal reactions.

The antibacterial activity in vivo is stronger than norfloxacin and ofloxacin, but not as good as fleroxacin.

It can be used to treat urogenital system, skin and soft tissue, respiratory tract, and eye infections. It is also suitable for the treatment of chlamydia infection and tuberculosis.

This type of drug is most likely to cause photosensitivity reactions, so sunlight should be avoided during use.

Administer once daily

The in vitro antibacterial activity is slightly lower than that of ciprofloxacin, but the in vivo antibacterial activity is stronger than existing quinolones.

Mainly used for the treatment of infectious diseases or secondary infections of the genitourinary system, respiratory system, gynecology, and surgery caused by sensitive bacteria.

three generations

Its activity against Gram-positive bacteria is significantly better than that of ciprofloxacin, and it is effective against penicillin- and cephalosporin-resistant Streptococcus pneumoniae. It is also more effective against Gram-negative bacteria, mycoplasma, chlamydia, anaerobic bacteria, and Mycobacterium tuberculosis.

A few patients have phototoxic reactions and may also produce QT prolongation, so use with caution

Four generations

Clinically, it can be used for acute and chronic bronchitis and upper respiratory tract infections caused by certain sensitive bacteria. It can also be used for infections of the genitourinary system and skin and soft tissues.

Photosensitivity reaction is mild

For respiratory and urinary tract infections, skin, soft tissue and ear, nose and throat infections

Virtually no potential for phototoxicity

It can be divided into three categories: anti-systemic infection drugs (easily absorbed by the intestines), anti-intestinal infection drugs (difficult to be absorbed by the intestines) and external drugs.

Antibacterial effect

Mechanism

Adverse reactions

Moderately effective sulfonamides

Easily penetrates the blood-brain barrier, preventive drug for Neisseria meningitidis meningitis

Also used to treat nocardiosis and combined with pyrimethamine for the treatment of toxoplasmosis

Combined use with trimethoprim can produce synergistic antibacterial effects

Crystals are easy to precipitate in the kidneys and damage the kidneys. You should alkalize your urine and drink more water to prevent it.

The concentration in cerebrospinal fluid is lower than SD and can be used to prevent epidemic cerebrospinal meningitis.

Suitable for urinary tract infections caused by sensitive bacteria such as Escherichia coli

Mainly used in combination with trimethoprim to produce synergistic antibacterial effects and expand the scope of clinical indications

During medication, attention should be paid to damage to the urinary system

Often breaks down into sulfapyridine and 5-aminosalicylic acid

5-aminosalicylic acid has certain anti-inflammatory and immunomodulatory effects

Oral/enema can be used for acute and chronic ulcerative colitis and Crohn's disease

Suppositories for ulcerative proctitis

Strong against Pseudomonas aeruginosa and effective against Staphylococcus aureus and Clostridium tetani

Suitable for burns or large-area trauma infections

If there is local pain and burning sensation, its hydrochloride salt may cause acidosis if used on a large area. Its acetate salt should be used.

It is more effective against Pseudomonas aeruginosa than sulfamilon

Used to prevent and treat wound infections of second- and third-degree burns or scalds

Eye drops are used to treat trachoma, keratitis and conjunctivitis, etc.

Not for use in systemic infections

Mainly used for acute lower urinary tract infections caused by sensitive bacteria, chronic bacteriuria and recurrent chronic urinary tract infections

Gastrointestinal reactions and allergic reactions are common

Long-term use of large doses can cause headaches, dizziness, etc., and even peripheral neuritis.

Patients lacking glucose-6-phosphate dehydrogenase can cause hemolytic anemia. Neonates and those lacking this enzyme are contraindicated.

It is used for dysentery, enteritis, and cholera caused by sensitive bacteria. It can also be used for typhoid, paratyphoid, giardiasis, trichomoniasis, etc. It can also treat gastric and duodenal ulcers caused by Helicobacter pylori.

Amino derivatives of tricyclodecane

It can specifically inhibit influenza A virus and is mainly used for the prevention and treatment of influenza A.

It has anti-tremor paralysis effect and can be used in the treatment of Parkinson's disease

It can specifically inhibit influenza A and is mainly used for the prevention and treatment of influenza A.

It is phosphorylated by HSV thymidine activating enzyme and host cell kinase in infected cells to generate acyclovir triphosphate, which can competitively inhibit viral DNA polymerase and can also be incorporated into viral DNA to block viral DNA synthesis.

The drug of choice for HSV (herpes simplex virus) infection

Effective in treating hepatitis B when combined with immunomodulators (alpha-interferon)

Phlebitis may be seen during intravenous infusion

After entering infected cells, it is first activated into ganciclovir triphosphate, and then competes with guanosine triphosphate for the corresponding enzyme, thereby inhibiting the synthesis of viral DNA.

Stronger against cytomegalovirus than acyclovir

It is mainly used to prevent and treat cytomegalovirus (CMV) infection in patients with immunodeficiency and immunosuppression. It can also be used to prevent and treat CMV infection in organ transplant recipients and AIDS patients.

Can induce bone marrow suppression

It can improve the shortcomings of low bioavailability of oral administration of acyclovir

Has replaced acyclovir as the first-line drug for the treatment of herpes zoster and genital herpes

Mainly used to treat uncomplicated herpes zoster

It can accelerate wound healing, shorten the course of herpetic neuralgia, and also has an effect on genital herpes. It is currently the most effective drug for treating genital herpes.

Inhibits viral DNA polymerase, thereby inhibiting viral growth

Intravenous administration can be used to treat cytomegalovirus retinitis in patients with immunodeficiency, and can also be used to treat skin and mucosal infections caused by herpes simplex virus. It is effective in patients with HIV infection and herpes zoster that is resistant to acyclovir.

Adverse reactions include kidney damage and hypocalcemia

The most effective drug against influenza virus currently

Mainly used to treat influenza A and B, respiratory and cytotoxic viruses, pneumonia and bronchitis, herpes, adenovirus pneumonia, hepatitis A and C, etc.

It has a strong teratogenic effect, so it is contraindicated in the first 3 months of pregnancy.

A type of biologically active glycoprotein produced by body cells under the stimulation of viral infection or other inducers.

Mainly used to prevent and treat chronic hepatitis, but also used for respiratory viral infections, herpetic keratitis, herpes zoster, herpes simplex, cytomegalovirus infection, malignant tumors, etc.

Competitively inhibits thymidylate synthase, blocking DNA synthesis

Only topical application is used to treat acute herpetic keratitis and other herpetic eye diseases caused by herpes simplex virus. It is less effective in chronic ulcerative parenchymal herpetic keratitis and ineffective in herpetic keratoiritis.

There may be local pain, edema, etc., and long-term use may cause corneal opacity or stained spots, etc.

Hydrolyzed to adefovir in the body to exert antiviral effects

Treatment of adult chronic hepatitis B patients with active replication of hepatitis B virus and compensated liver function with persistently elevated transaminases. It is especially suitable for those who require long-term medication or who have developed resistance to lamivudine.

Thymidine derivatives

The first drug used to treat HIV infection

Competitively inhibits HIV-1 reverse transcriptase, hinders proviral DNA synthesis, and is incorporated into the DNA being synthesized to terminate the elongation of the viral DNA chain and inhibit HIV replication.

The drug of choice for the treatment of AIDS can reduce or alleviate AIDS and related syndromes. Most people advocate cocktail therapy, that is, combined drug therapy.

Adverse reactions are mainly bone marrow suppression

Cytosine derivatives

Effective against zidovudine-resistant human immunodeficiency virus

Often used in combination with stavudine or zidovudine to treat HIV infection

It can inhibit the replication of hepatitis B virus (HBV) and effectively treat chronic HBV infection. It is currently one of the most effective drugs for the treatment of HBV infection.

Adverse reactions mainly include headache, insomnia, fatigue and gastrointestinal discomfort.

Deoxycytidine derivatives

It can effectively treat HIV infection. When used alone, it is not as effective as zidovudine. It can be used in combination with zidovudine and a protease inhibitor.

It is mainly used for AIDS and AIDS-related syndromes, and can also be used in combination with zidovudine to treat HIV-infected patients whose clinical status has worsened.

The main adverse reactions are dose-dependent peripheral neuritis and occasionally pancreatitis.

Can directly inhibit HIV-1 reverse transcriptase, but has no activity against HIV-2 DNA polymerase

This type of drug is prone to develop drug resistance when used alone, and is often used in combination with nucleotide reverse transcriptase inhibitors and protease inhibitors, which can synergistically inhibit HIV replication.

The main adverse reaction is rash

By inhibiting HIV protease, it prevents the cleavage of precursor proteins, leading to the accumulation of immature non-infectious virus particles, thereby producing an antiviral effect and effectively fighting HIV.

ritonavir

nelfinavir

saquinavir

Candida albicans infection, coccidioidomycosis infection and cryptococcal meningitis are the first choice drugs for the treatment of cryptococcal meningitis in AIDS patients. Combined with flucytosine, the efficacy can be enhanced.

Various skin tinea and onychomycosis

Prevent fungal infections in patients with organ transplantation, leukemia, leukopenia, etc.

Mild gastrointestinal reaction

rash

Elevated transaminases

primary extraerythrocytic stage

secondary extraerythrocytic phase

intraerythrocytic phase

Gametophyte formation

Sporozoite formation

Chloroquine

Quinine

pyronaridine

artemisinin

Artesunate

Artemether

Primachloroquine

Pyrimethamine

Clinical application

Adverse reactions

It has good curative effect on amoebic dysentery and extraintestinal amebiasis, with low toxicity. It can also be used to treat vaginal trichomoniasis and anaerobic bacterial infections.

Mostly hydrolyzed in the intestinal lumen or intestinal mucosa

After ingestion, it mainly relies on its unabsorbed part to kill amoeba cysts. It has good effects on those who have no symptoms or only have mild symptoms. It is currently the most effective cysticide.

Also effective against chronic amoebic dysentery, but less effective against extraintestinal amebiasis.

Large doses can cause miscarriage

Can be used to treat mild, chronic amoebic dysentery and asymptomatic cyst discharge

For patients with acute amoebic dysentery, it can be combined with metronidazole and emetine to improve the cure rate.

Ineffective against extraintestinal amoebiasis

Gastrointestinal reaction, mild thyroid enlargement, sulfonate allergy

Long-term use of large doses can cause severe visual impairment

The two drugs have a direct killing effect on amoeba trophozoites

Emetine is highly irritating and can cause vomiting when taken orally. It can only be injected into deep muscles. In addition, it is severely toxic to the myocardium.

This medicine is only used to treat acute amoebic epilepsy and extraintestinal amebiasis in severe cases where metronidazole is ineffective.

Effective against amoebic liver abscess and lung abscess, but not effective against amoebic dysentery

Only used for amebic hepatitis or liver abscess where metronidazole is ineffective or inappropriate, and should be combined with anti-intestinal amoebiasis drugs to prevent recurrence.

The drug of choice against intestinal nematodes

It is contraindicated for pregnant women and those under 2 years old. Use with caution in patients with severe liver, kidney, heart dysfunction and active ulcer disease.

It can be divided into the early phase of DNA synthesis (G1 phase), the DNA synthesis phase (S phase), the late DNA synthesis phase (G2 phase) and the mitosis phase (M phase).

When the drug-sensitive tumor cells in the proliferation phase are killed, the cells in the G0 phase can enter the proliferation phase, which is the root cause of tumor recurrence.

It can only kill tumor cells in a certain proliferation stage, and its selectivity is relatively high. It can be divided into two categories: one is drugs that act on the S phase, such as methotrexate, cytarabine, mercaptopurine, etc.; the other is drugs that act on the M phase, such as vinblastine, vincristine, etc.

It can kill cells in all stages of proliferating cell groups. This class of drugs has poor selectivity and has little effect on non-proliferating cell populations. Drugs include alkylating agents, anti-tumor antibiotics, platinum, etc.

Drugs that directly affect DNA structure and function

Drugs that interfere with nucleic acid biosynthesis

Drugs that interfere with the transcription process and prevent RNA synthesis: such as daunorubicin, doxorubicin, actinomycin D, etc.

Drugs that inhibit protein synthesis and function

Drugs that regulate hormone balance in the body: such as adrenocortical hormones, androgens, estrogen, etc.

Targeted anti-tumor drugs: such as gefitinib, erlotinib, rituximab, trastuzumab, etc.

Alkylating agents: such as cyclophosphamide, thiotepa, busulfan, nitrogen mustard, etc.

Anti-metabolites: such as methotrexate, fluorouracil, mercaptopurine, hydroxyurea, etc.

Anti-tumor antibiotics: such as daunorubicin, mitomycin, bleomycin, actinomycin D, etc.

Anti-tumor botanicals: such as vinblastine, vincristine, paclitaxel, hydroxycamptothecin, etc.

Hormone drugs: such as adrenocortical hormones, androgens, estrogen, tamoxifen, etc.

Molecular targeted drugs: small molecule compounds: gefitinib, erlotinib, monoclonal antibodies: rituximab, trastuzumab, cetuximab

Others: such as cisplatin, carboplatin, asparaginase

Pharmacological effects

Clinical application

Adverse reactions

Sulfonate alkylating agent

A small dose can significantly inhibit granulocyte production. It is the first choice drug for the treatment of chronic myelogenous leukemia. It is ineffective against acute myeloid leukemia and has no obvious effect on other tumors.

With bone marrow suppression, individual patients may develop pulmonary fibrosis, cataracts, amenorrhea, testicular atrophy, teratogenesis, etc.

Binds to the bases in the DNA molecules of tumor cells to hinder the division of tumor cells

Used to treat breast cancer, ovarian cancer, bladder cancer, etc.

There is bone marrow suppression, few gastrointestinal reactions, and little local irritation.

Used for malignant lymphoma, leukemia, sarcoma, lung cancer, breast cancer, testicular cancer, etc.

For malignant tumors that are resistant to cyclophosphamide, this drug is still effective, has a high chemotherapy index, and has a lower incidence of adverse reactions than cyclophosphamide.

Combined with the urinary tract protective agent mesna, it can reduce damage to the urinary system

Competitively inhibits the activity of dihydrofolate reductase, blocks the reduction of dihydrofolate into tetrahydrofolate, and blocks the carrying of one-carbon groups, thus hindering DNA biosynthesis.

Can interfere with RNA and protein synthesis

Mainly used for acute leukemia in children

After entering the body, it is converted into 5-fluorouracil deoxynucleoside, which inhibits thymidylate synthase, causing deoxythymidylate deficiency and hindering DNA biosynthesis.

Its metabolites can be incorporated into RNA, interfere with the synthesis of RNA and protein, and have certain effects on cells in G1 and G2 phases.

It is mainly used for digestive tract cancer and breast cancer, and is also effective for ovarian cancer, cervical cancer, chorioepithelial cancer, and bladder cancer.

Adverse reactions: gastrointestinal reactions, including bloody diarrhea in severe cases; bone marrow suppression, alopecia, ataxia and other reactions; occasionally liver and kidney damage

It is converted into xanthine nucleotides and thioinosinic acid in the body, which interferes with purine metabolism and hinders DNA synthesis. It is most sensitive to cells in S phase.

Has a strong immunosuppressive effect

It is effective in the treatment of acute lymphoblastic leukemia in children, and is also used in the treatment of choriocarcinoma, malignant hydatidiform mole, malignant lymphoma, multiple myeloma, autoimmune diseases, etc.

Gastrointestinal reactions and bone marrow suppression, occasionally liver and kidney damage

It has teratogenic effects and is contraindicated by pregnant women.

Ribonucleotide reductase inhibitor, selectively acts on S phase cells, preventing the reduction of cytidylic acid to deoxycytidylic acid, thereby inhibiting DNA synthesis.

For chronic myelogenous leukemia and melanoma

Adverse reactions include bone marrow suppression and gastrointestinal reactions, etc.

Can be teratogenic, contraindicated by pregnant women

Selectively inhibits DNA polymerase activity and prevents cellular DNA biosynthesis; it can be incorporated into DNA and RNA to interfere with DNA replication and RNA function.

The main drug used to treat acute myeloid leukemia or monocytic leukemia in adults

May cause bone marrow suppression, gastrointestinal reactions, and intravenous injection may cause phlebitis

By directly embedding into the base pairs of the DNA double helix chain, it combines with DNA to form a complex, hindering the function of RNA polymerase, preventing RNA biosynthesis, inhibiting protein synthesis, thereby inhibiting the growth of tumor cells.

Used for chorioepithelial carcinoma, neuroblastoma, rhabdomyosarcoma, nephroblastoma, Hodgkin's disease, etc.

Gastrointestinal reactions are more common, can inhibit bone marrow, can cause teratogenesis, and a few may cause hair loss, dermatitis, etc.

It can complex with copper/iron ions to convert oxygen molecules into oxygen free radicals, causing DNA single-strand or double-strand breaks, hindering DNA replication, and interfering with cell division and reproduction.

It has a good effect on squamous epithelial cancer and is also used for lymphoma and testicular cancer.

Mild bone marrow suppression, severe pulmonary toxicity, can cause interstitial pneumonia and pulmonary fibrosis

Its alkylating group can cross-link with the DNA double strand, preventing its replication and causing it to break.

It is used to treat solid tumors, such as gastric cancer, colon cancer, lung cancer, pancreatic cancer, etc. It is a commonly used drug to treat malignant tumors of the digestive tract.

Have bone marrow suppression and gastrointestinal reactions

Intravenous administration should prevent leakage to avoid tissue necrosis

Directly embed into DNA molecules, destroy the template function of DNA, prevent the transcription process, and inhibit DNA replication and RNA synthesis.

For the treatment of acute lymphoblastic leukemia and acute myelogenous leukemia

Cardiotoxic reactions and bone marrow suppression

For the treatment of drug-resistant acute leukemia, malignant lymphoma and various solid tumors

The most serious toxic reaction: causing myocardial degeneration and myocardial interstitial edema

Bone marrow suppression, gastrointestinal reactions, hair loss, etc.

Vinblastine-VLB, vincristine-VCR, vindesine-VDS, vinorelbine-NVB

Pharmacological effects

Clinical application

Adverse reactions

By specifically promoting tubulin polymerization and inhibiting its depolymerization, it prevents spindle formation and affects the mitosis of tumor cells.

It has a good effect on metastatic ovarian cancer and breast cancer, and has a certain sequential effect on lung cancer, esophageal cancer, brain tumors, and lymphoma.

The main adverse reactions are bone marrow suppression and gastrointestinal reactions, as well as cardiotoxicity and nervous system toxicity.

It is clinically used to treat locally advanced or metastatic breast cancer and non-small cell lung cancer, and is used in combination with a variety of drugs to treat a variety of tumors.

It can inhibit the initial stage of protein synthesis, decompose ribosomes, and also inhibit cell mitosis, which has a significant effect on cells in the S phase.

It is used for acute myeloid leukemia, and can also be used for chronic myelogenous leukemia, acute monocytic leukemia, malignant lymphoma, etc.

Adverse reactions mainly include bone marrow suppression and gastrointestinal reactions, but also tachycardia, myocardial damage, hair loss, etc.

Can specifically inhibit the activity of DNA topoisomerase I, thus interfering with DNA structure and function

It is a non-specific drug of the cell cycle and has a stronger effect on the S phase than the G1 and G2 phases.

Hydroxycamptothecin has certain effects on various malignant tumors such as primary liver cancer, gastric cancer, bladder cancer, and rectal cancer.

Topoxicam is suitable for patients with metastatic ovarian cancer who have failed initial chemotherapy and sequential chemotherapy, and patients with chemotherapy-sensitive small cell lung cancer who have failed first-line chemotherapy.

Irinotecan is suitable for the treatment of patients with advanced colorectal cancer and has certain effects on bone cancer, cervical cancer, gastric cancer, ovarian cancer, small cell lung cancer, etc.

Includes podophyllotoxin, semisynthetic etoposide, and teniposide

Can bind to tubulin, affect cell mitosis, and inhibit the growth and reproduction of tumor cells.

Semi-synthetic products mainly interfere with DNA topoase II, causing DNA chain breakage and causing cell death.

The combination of etoposide and cisplatin is effective in treating small cell lung cancer and testicular cancer; teniposide is used for childhood leukemia, especially for infant monocytic leukemia.

The main adverse reactions are bone marrow suppression and gastrointestinal reactions, and large doses can cause liver toxicity.

Commonly used drugs include prednisone, prednisolone, dexamethasone, etc.

By inhibiting lymphoid tissue, it promotes lymphocyte lysis, which is effective but not long-lasting and prone to drug resistance.

It is used for acute lymphoblastic leukemia and malignant lymphoma, and is also used for chronic lymphocytic leukemia. It is not effective for other tumors.

Short-term medication can relieve symptoms such as fever caused by tumors

This type of drug can suppress immunity and easily cause infection and tumor spread, so it is necessary to combine sufficient amounts of effective antibacterial drugs and anti-malignant tumor drugs.

The estrogen drug commonly used to treat malignant tumors is diethylstilbestrol

Can inhibit the hypothalamus and pituitary gland, reduce androgen secretion, and directly antagonize androgens

It is used to treat prostate cancer and can also be used for menopausal patients with extensive metastasis of breast cancer.

Commonly used ones include methyltestosterone, testosterone propionate, etc.

It can directly antagonize the effects of estrogen, inhibit the secretion of pituitary follicle-stimulating hormone, and oppose the stimulating effect of prolactin on the breast, thus inhibiting tumor growth and causing tumor regression.

Mainly used to treat advanced breast cancer, especially those with bone metastasis.

It can also promote protein synthesis, which can improve the general symptoms of late-stage patients.

Progestins commonly used to treat malignant tumors include medroxyprogesterone and megestrol, which can inhibit the pituitary gland through negative feedback and reduce the production of luteinizing hormone, adrenocorticotropic hormone and other growth factors.

For the treatment of breast cancer, endometrium cancer, prostate cancer and kidney cancer

Antiestrogens, which compete with estradiol for estrogen receptors and inhibit the growth of estrogen-dependent tumor cells.

For the treatment of breast and ovarian cancer

Selective estrogen receptor modulator, competitively binds to estrogen receptors and inhibits the growth of estrogen receptor-positive breast cancer

For the treatment of estrogen receptor-positive metastatic breast cancer in menopausal women

Orally administered nonsteroidal antiandrogens, mainly used for prostate cancer

It can bind to the intracellular kinase domain of the receptor, compete for the enzyme substrate ATP, and block the kinase activity of EGFR and its downstream signaling pathways.

For second-line treatment of advanced or metastatic non-small cell lung cancer

The main adverse reactions include gastrointestinal reactions and skin symptoms such as papules and itching, and occasionally fatal interstitial pneumonia.

Inhibits the binding of ATP to intracellular protein tyrosine kinase, inhibits EGFR autophosphorylation, thereby blocking signal transduction and intervening in cell proliferation, differentiation and other processes.

Can be used as a third-line treatment for locally advanced or metastatic non-small cell lung cancer that has failed two or more chemotherapy regimens.

Adverse reactions are similar to those of gefitinib

Rituximab can specifically bind to CD20 to cause B cell lysis, thereby inhibiting B cell proliferation and inducing apoptosis of mature B cells.

For the treatment of non-Hodgkin lymphoma

Adverse reactions are mainly signs and symptoms related to infusion, and most occur during the first infusion.

It inhibits the growth and metastasis of tumor cells by binding to human epidermal growth factor receptor-2 (HER2) and downregulating the expression of HER2 gene.

It is used to treat metastatic breast cancer with overexpression of HER2, metastatic breast cancer that has received one or more chemotherapy regimens, etc.

Adverse reactions mainly include abdominal pain, chest pain, muscle pain, edema, gastrointestinal reactions, nervous system reactions, etc.

It can block intracellular signal transduction pathways by inhibiting tyrosine kinases, thereby inhibiting cancer cell proliferation and inducing cancer cell apoptosis.

In combination with irinotecan for the treatment of metastatic rectal cancer that overexpresses EGFR and is resistant to irinotecan-based chemotherapy.

Allergic reactions are more common

It can hydrolyze asparagine in serum and reduce the supply of asparagine to tumor cells, thereby inhibiting tumor cell growth.

For the treatment of acute lymphoblastic leukemia

Common adverse reactions are gastrointestinal reactions, bleeding and psychiatric symptoms, and allergic reactions may also occur.

First generation - cisplatin, second generation - carboplatin, both drugs are cell cycle non-specific drugs

This type of drug mainly forms cross-links with the bases on DNA, destroys the structure and function of DNA, and prevents cell division and proliferation.

It has a broad anti-tumor spectrum and is effective against a variety of solid tumors. It can be used for head and neck squamous cell carcinoma, ovarian cancer, bladder cancer, prostate cancer, lung cancer, breast cancer, etc. It is a commonly used drug in combination chemotherapy.

Third-generation oxaliplatin acts on DNA by producing alkylated complexes to form intra- and inter-strand cross-links, thereby inhibiting DNA synthesis and replication. It can be used in combination with fluorouracil and leucovorin to treat metastatic colon cancer and Rectal cancer, adjuvant treatment for stage III colon cancer after complete resection of the primary tumor.

There are gastrointestinal reactions, bone marrow suppression, nephrotoxicity and neurotoxicity, etc.