What Is Minocycline?

Minocycline, also known as dimethylamine tetracycline or cyclamate, is a broad-spectrum antibacterial tetracycline antibiotic. Can be combined with tRNA to achieve antibacterial effect. Minocycline has a broader antibacterial spectrum and antibacterial activity than similar drugs. The antibacterial spectrum is similar to that of tetracycline, and it has a strong effect on gram-positive bacteria, including tetracycline-resistant Staphylococcus aureus, streptococcus, and gram-negative bacteria. ; It also has a good inhibitory effect on Chlamydia trachomatis and Mycoplasma urealyticum.

Drug Name: Minocycline
Alias: Dimethylamine tetracycline

Foreign name: Minocycline
Drug type: Western medicine

Minocycline Basic Information

Chinese name minocycline

Chinese alias: 4,7-bis (dimethylamino) -1,4,4a, 5,5a, 6,11,12a-octahydro-3,10,12,12a-tetrahydroxy-1,11-dioxy -2-tetrabenzamide; dimethylamine tetracycline; 7-dimethylamino-6-desmethyl-6-deoxytetracycline;

English name: minocycline

English alias: Minocyclin; Minocin; 7-dimethylamino-6-demethyl-6-deoxytetracycline; 4S- (4a, 4aa, 5aa, 12aa) -4,7-bis (dimethylamino) -1,4,4a, 5,5a, 6,11,12a-octahydro-3,10,12,12a-tetrahydroxy-1,11-dioxo-2-naphthacene carboxamide; Minocyclinum;

CAS number: 10118-90-8

Molecular formula: C ₂₃ H ₂₇ N ₃ O ₇

Molecular weight: 457.47600

Exact mass: 457.18500

PSA: 164.63000

LogP: 0.88690

Minocycline physical and chemical properties

Appearance and properties: bright yellow-orange amorphous solid

Density: 1.553 g / cm ³

Boiling point: 659.401ºC at 760 mmHg

Flash point: 352.593ºC

Refractive index: 1.717

Stability: Stable in air when protected from light and moisture; strong light andor moist air causes it to darken hydrochloride potency in solution affected primarily due to epimerization.

Storage conditions: Keep in a cool, dry, dark location in a tightly sealed container or cylinder. Keep away from incompatible materials, ignition sources and untrained indliduals. Secure and label area. Protect containers / cylinders from physical damage. ^[1]

Minocycline Related Drug Information

Minocycline pharmacological action

It is a semi-synthetic tetracycline antibiotic. The antibacterial spectrum is similar to that of tetracycline.

Secondary structure of protein Long-lasting properties. This product has the strongest antibacterial effect among tetracyclines. Oral absorption is rapid and almost complete. Food has no significant effect on its absorption. Oral or intravenous injection of 200mg, the serum drug concentration after about 1 hour is about 2, 25 g / ml, after 12 hours there is still 1, 25 g / ml. Those with normal renal function have a half-life of about 16 hours. Its fat solubility is high, so it easily enters many tissues and body fluids, and the drug concentration is higher in saliva and tear fluid than other tetracyclines. It is more metabolized in the body, and the prototype drugs excreted in the urine are much lower than other tetracyclines. Minocycline is the strongest antibacterial effect among tetracycline antibiotics.

The effect on staphylococcus aureus, pneumococcus, hemolytic streptococcus, Streptococcus grass green, gonococcus, influenza, etc. is 2 to 4 times stronger than tetracycline. It also has certain antibacterial activity against tetracycline-resistant bacteria and some Staphylococcus aureus, Enterococcus faecalis, and E. coli that are resistant to penicillin. invalid. Also. It also has effects on fetal Campylobacter, Chlamydia, Mycoplasma pneumoniae, Rickettsia and Vibrio cholerae. The mechanism of the product used in systemic therapy is not only to effectively inhibit the growth of acne-causing bacteria, but also to inhibit the synthesis and activity of lipase in bacteria, prevent the hydrolysis of triglyceride to free fatty acids, and inhibit the formation of acne.

Minocycline kinetics

This product has high fat solubility, complete oral absorption, and is rarely affected by food; but it is more susceptible to calcium, magnesium, aluminum and other metal ions than other tetracyclines, or chelate with metal ions, or increase gastric pH and reduce drug absorption. . The single oral administration of 0, 2g, the peak plasma concentration within 2 to 3 hours averaged 7 g / ml, which is the highest variety among tetracyclines. The protein binding rate is about 75%. Widely distributed in the body, can penetrate

cephalosporin Lung, kidney, liver, thyroid and other tissues. The product can penetrate the blood-brain barrier, and its concentration in cerebrospinal fluid and brain tissue is higher than that of other tetracyclines. Higher concentrations in urine and bile. The elimination half-life of this product is as long as 16-18 hours. It is excreted mainly through urine and feces. Its excretion rate is significantly lower than that of other varieties, and a considerable amount of drugs are metabolized in the body. In patients with liver failure, the prolongation of minocycline half-life is not obvious.

Minocycline pharmacology and toxicology

[Pharmacology]

This product is a semi-synthetic tetracycline broad-spectrum antibiotic, which is highly effective and long-acting. Among the tetracycline antibiotics, this product has the strongest antibacterial effect. The antibacterial spectrum is similar to that of tetracycline. Tetracycline-resistant golden to Gram-positive bacteria

Urticaria Staphylococcus aureus, Streptococcus, etc., and the Neisseria gonorrhoeae in gram-negative bacteria have a strong effect; the effect on gram-negative bacteria is generally weak; this product also has a good effect on Chlamydia trachomatis and Mycoplasma urealyticum Inhibition. Due to the abuse of tetracycline antibiotics, most common Gram-positive and negative bacteria are resistant to this product. The mechanism of action of this product is to bind to the A position of the 30S subunit of the ribosome, preventing the extension of the peptide chain, thereby inhibiting the protein synthesis of bacteria or other pathogenic microorganisms. This strain is a bacteriostatic agent, but also has a bactericidal effect at high concentrations.

[Toxicology]

This product can cause the thyroid of experimental animals (rats, dogs, and monkeys) to turn black. Chronic treatment of this product in rats resulted in goiter and even thyroid tumor. The product can also cause thyroid hyperplasia in rats and dogs.

Minocycline adaptation symptoms

This product is suitable for susceptible to Staphylococcus, Streptococcus, Pneumococcus, Neisseria gonorrhoeae, Shigella, Escherichia coli, Klebsiella, Proteus, Pseudomonas aeruginosa, Treponema pallidum and Chlamydia The following infections caused by pathogens: Septicemia, bacteremia. 2. Superficial purulent infections: folliculitis, pyoderma, tonsillitis, periarthritis, dacryocystitis, gingivitis, vulvitis, trauma infection, post-operative infection, etc. 3 Deep purulent diseases: mastitis, lymphangiitis, submandibular

Central nervous system Adenitis, osteomyelitis, osteitis. 4 Acute and chronic bronchitis, asthmatic bronchitis, bronchiectasis, bronchial pneumonia, bacterial pneumonia, atypical pneumonia, and pulmonary suppuration. 5. Dysentery, enteritis, infectious food poisoning, cholangitis, cholecystitis. 6. peritonitis. 7. Pyelonephritis, pyelitis, pyelitis, urethritis, cystitis, prostatitis, epididymitis, intrauterine infection, gonorrhea. 8. Otitis media, paranasal sinusitis, submandibular glanditis. 9. syphilis.

It is mainly used for rickettsial disease, mycoplasma pneumonia, lymphogranuloma, chancre, plague, cholera, brucellosis (combined with streptomycin) and so on. It can also be applied to systemic or local infections caused by sensitive strains such as E. coli, Aerobacter, Shigella, Haemophilus influenzae, and Klebsiella. In addition, for infections caused by Neisseria gonorrhoeae, syphilis and Treponema pallidum, listeria, clostridium, anthracnose, actinomycetes, and clostridium, when the patient is not resistant to penicillin, the product (or other tetracycline) can be considered class). This product can also be considered for infections caused by sensitive strains of Streptococcus. As for Staphylococcus aureus, most strains are resistant to this class of drugs. In addition, the product can still be used for adjuvant treatment of amebiasis. Similar to tetracycline or doxycycline, it is mainly used for sexually transmitted diseases caused by acne, rosacea and gonorrhea, chlamydia trachomatis. Although this product has certain curative effects on urinary system, respiratory system and soft tissue infections caused by certain drug-resistant bacteria, meningococcal carriers, otitis media, and sinusitis, etc., it has a lot of adverse reactions, which makes it very difficult for clinical application. Big restrictions.

Dosage and Administration: Adults generally take the first dose of 200mg, and then 100mg orally every 12 hours, or after the first dose, 50mg orally every 6 hours, which is well absorbed and not affected by food. Can be taken after meals. General infection: Adults take the first dose of 0, 2g orally, take 0, 1g every 12h, take before or after meals. Systemic therapy for acne: 50 mg orally once a day, twice a day, for 6 weeks as a course of treatment, the longest course of treatment can be up to 12 weeks. For gonorrhea: 0, 1 g each time, 3 times a day, 10 days as a course of treatment. The oral dose should not be too large, it can be taken after meals.

Minocycline drug interactions

1. Since this product can reduce the activity of prothrombin, the dosage of anticoagulant should be reduced when it is combined with anticoagulant.

2. Because antacids (such as sodium bicarbonate) can reduce the absorption and activity of the product, the product and the antacid should be avoided at the same time.

3. When this product is used in combination with drugs containing aluminum, calcium, magnesium, and iron ions, it can form insoluble complexes and reduce the absorption of the product.

4. When the cholesterol-lowering drug cholestyramine or colestipol is used in combination with this product,

cell May affect absorption of the product.

5. Because barbiturates, phenytoin, or carbamazepine can induce the activity of microsomal enzymes, the blood concentration of this product is reduced, so the dose of this product must be adjusted when combined.

6. General anesthetic mefflurane combined with this product can cause fatal nephrotoxicity.

7. As this product can interfere with the bactericidal activity of penicillin, it should be avoided in combination with penicillin.

8. This product combined with strong diuretics (such as furosemide, etc.) can aggravate renal damage.

9. This product can be used in combination with other hepatotoxic drugs (such as anti-tumor chemotherapy drugs) to aggravate liver damage.

10. The combination of this product with oral contraceptives can reduce the effectiveness of oral contraceptives.

Minocycline adverse reactions

1. Bacterial disorders: This product is more common to cause bacterial disorders. Mild cases cause vitamin deficiency, and secondary infections caused by Candida albicans and other resistant bacteria are often seen. Clostridium pseudomembranous enteritis can also occur.

2. Gastrointestinal reaction: loss of appetite, nausea, vomiting, abdominal pain, diarrhea, stomatitis, glossitis, perianal inflammation, etc .; occasionally esophageal ulcers may occur.

3. Liver damage: occasional nausea, vomiting, jaundice, fatty liver, elevated serum aminotransferase, vomiting and blood in the stool, etc., severe cases can coma and die.

Urinary system Renal damage: It can aggravate renal damage in people with renal insufficiency, leading to an increase in blood urea nitrogen and creatinine values.

5. Affects tooth and bone development: This product can be deposited in teeth and bones, causing yellow staining of teeth, and affecting the normal development of bones of fetuses, newborns and infants.

6. Allergic reactions: mainly manifested as rash, urticaria, drug fever, photosensitive dermatitis and asthma. Rare systemic lupus erythematosus, if it occurs, should be discontinued immediately and treated appropriately.

7. Visible vestibular dysfunction such as dizziness, tinnitus, ataxia with nausea and vomiting (dose-dependent, more common in women than men), which usually occurs in the first few doses, and can usually be recovered after 24-48 hours .

8. Blood system: occasional hemolytic anemia, thrombocytopenia, neutropenia, eosinophilia, etc.

9. Vitamin deficiency: occasional symptoms of vitamin K deficiency (hypothrombin, bleeding tendency, etc.), vitamin B deficiency symptoms (glossitis, stomatitis, loss of appetite, neuritis, etc.).

10 Elevated intracranial pressure: occasionally vomiting, headache, diplopia, optic nerve papillary edema, anterior cranial swelling and other symptoms of elevated intracranial pressure should be discontinued immediately.

11. Shock: Occasionally shock occurs, you must pay attention to observation. If you find symptoms such as discomfort, abnormal mouth feeling, asthma, constipation, tinnitus, etc., you should stop the medicine immediately and take appropriate treatment.

12. Skin: maculopapular rash, erythematous rash, etc .; occasionally exfoliative dermatitis, mixed drug rash, erythema polymorpha, and Steven-Johnson syndrome. Long-term use of this product occasionally causes pigmentation in the nails, skin, and mucous membranes.

13. Other: occasional dizziness, burnout, etc. Long-term use of this product can make the thyroid gland turn brown and black, and abnormal thyroid function is rare. Hearing impairment is rare.

Minocycline side effects

ulcer 1 A few patients have nausea, decreased appetite, glossitis, and gastrointestinal flora disorders.

2 Occasional allergic reactions, and even anaphylactic shock.

3 People with severe infections during late pregnancy may cause liver damage. Use with caution in patients with liver and kidney dysfunction.

4 Children may have yellow teeth stains and anterior ridges. Children under 8 years of age and late pregnancy are contraindicated.

Minocycline contraindications

Not suitable for pregnant women, as liver damage may occur. It is not suitable for children under 8 years old, because it can cause the front canal to bulge and yellow teeth staining. The eighth pair of elderly patients with neurological deficits should be used with caution. Systemic or local immune dysfunction should be avoided as far as possible, and must pay close attention to the occurrence of secondary infection when it must be applied.

Minocycline considerations

1. Hepatic and renal insufficiency, esophageal passage disorders, the elderly, oral malabsorption or inability

thyroid It should be used with caution in those who eat and those who have deteriorated their body condition (because they are prone to cause vitamin K deficiency). 2. Due to vestibular toxicity, this product is no longer used as a treatment drug for Neisseria meningitidis carriers and Neisseria meningitidis infection. 3. Those who are allergic to this product may also be allergic to other tetracyclines. 4. As it can cause dizziness, burnout, etc., car drivers, people engaged in dangerous machine operations and high-altitude operations should avoid taking this product. 5. When the product stays in the esophagus and disintegrates, it can cause esophageal ulcers, so you should drink plenty of water, especially when taking it before going to bed. 6. Patients with acute Neisseria gonorrhoeae urethritis should usually have dark field examination when suspected of early or secondary syphilis. Serum examination should be performed every month for other types of syphilis, and at least 4 months. 7. The dose of patients with severe renal insufficiency should be lower than the usual dose. If long-term treatment is needed, blood concentration should be monitored. 8. Liver and kidney function should be checked regularly during medication. 9. This product is more likely to cause photosensitive dermatitis, so you should avoid sun exposure after medication. 10. Interference with laboratory inspection indicators: (1) When measuring urine catecholamine (Hingerty method) concentration, the measurement result may be high due to the interference of the product with fluorescent light. (2) It may increase the measured values of alkaline phosphatase, serum amylase, serum bilirubin, and serum aminotransferase (AST, ALT). 11. This product can be taken with food, milk or carbonated drinks.

Minocycline dosage

oral. The first dose for adults is 0.2g, and then the product is 0.1g every 12 hours, or 50mg every 6 hours.

Minocycline for pregnant women

[Pregnant and lactating women]

1. The product can enter the fetus through the blood-placental barrier and deposit in the teeth

prostate In the calcareous area of teeth and bone, it causes fetal enamel dysplasia and inhibits fetal bone growth; it has teratogenic effects in animal experiments. Therefore, pregnant women and women who are planning to become pregnant are prohibited.

2. The product has a higher concentration in milk. Although it can form insoluble complexes with calcium in milk and absorbs very little, it can cause permanent discoloration of teeth, poor enamel development, and inhibit the infant's bones. Development and growth, so breastfeeding women should suspend breastfeeding during medication.

Minocycline for children

Because this product can cause permanent discoloration of teeth, enamel dysplasia, and inhibit the development of bones, it is contraindicated in children under 8 years old.

Minocycline related preparations

Minocycline hydrochloride

Hemoglobin Pharmacology

This medicine is a semi-synthetic derivative of a new tetracycline. Microbiology: For Staphylococcus aureus, Anaerobacteria, Klebsiella, Pneumococcus, Gonorrhoeae, Escherichia coli, Proteus, Influenza Bacteria, Pseudomonas, Streptococcus (including type B hemolytic and Grass green type and enterococcus) effective. In addition, clinical isolation and culture tests have shown that the drug is effective against the following microorganisms: Corynebacterium, Mycoplasma pneumoniae, Shigella, Actinomycetes, Listeria, Bacillus anthracis, Bacteroid (deteriorating bacteria), Yersinia pestis, Rod Bartonella, Rickettsia, Bordetella pertussis, Brucella, Norfanella, Streptococcus candida, Amoebic dysentery, Chlamydia trachomatis, Flandishella, Haemophilus ducreyi, Trachoma virus.

dynamics

It is quickly absorbed after oral administration, and its absorption is not significantly affected by food or milk. After taking 150mg once, its blood concentration is generally higher than its

Rheumatism Most of its tetracyclines are 2-4 times higher, and there are still measurable concentrations in blood after 96 hours. When the potency in blood is measured according to standard tetracycline, the potency of 150mg minocycline is within 24 hours and 48 hours. It is 16 times higher than 250 mg of tetracycline, which is mainly due to the longer plasma half-life of the drug. It is widely distributed in various tissues of the body. It has higher concentrations in the brain and cerebrospinal fluid than other tetracyclines. Like the blood concentration, the concentration of this drug in tissues is usually 2-4 times higher than that of tetracyclines.

Adapt to symptoms

Sensitive gram-positive and negative bacteria, rickettsia, chlamydia, mycoplasma, spirochaete, etc.

Respiratory tract Various infections, including: respiratory infections such as bronchitis, lung abscess, bronchitis, bronchiectasis, pneumonia. Genitourinary tract infections such as pyelonephritis, gonorrhea urethritis, cystitis, non-gonococcal urethritis, prostatitis. Skin and soft tissue infections such as abscesses, pustulosis, cellulitis, lymphadenitis, infectious dermatitis, pus dermatitis, folliculitis, wound infections, and multiple edema. Otolaryngology infections such as otitis media and external otitis, tonsillitis, bacterial rhinitis, pharyngitis, paranasal sinusitis. Eye infections such as acute conjunctivitis, blepharitis, and vesiculitis.

Dosage

bacterial Adults: 100mg / day of acne vulgaris, taken once or in divided portions, the course of treatment depends on the condition. Non-gonococcal urethritis 100mg / day, once or dividedly, for 10-14 days. Gonorrhea: Male: The initial dose is 200mg, and then 100mg orally every 12 hours, for at least 4 days. Bacterial culture should be performed within 2-3 days after treatment. Female: Same dose as male, may take 10-14 days. Systemic infection: 100 mg orally once every 12 hours. Prevention of asymptomatic meningococcal carriers: 100 mg / time, orally once every 12 hours. Twice a day for 5 days, usually followed by a course of rifampicin. 50mg / time for children over 8 years old, orally once every 12 hours. Patients with mild to moderate renal insufficiency can be used at the usual dose.

Adverse reactions

Mild mouth and gastrointestinal tract discomfort, skin rash, photosensitive dermatitis, occasional mild dizziness.

Precautions

leukocyte Those with allergies to tetracycline preparations. [Precautions] Occasionally, insensitive microorganisms can multiply excessively. If new infections are found during treatment, appropriate measures should be taken. Use of this medicine during tooth germ development (last 3 months of pregnancy, infants and young children) may cause tooth discoloration (yellow-gray-brown). In patients with acute gonococcal urethritis, early or secondary syphilis is suspected, and dark field examination should be performed. When other types of syphilis are suspected, serological examination should be performed monthly and at least 4 months. Use with caution in children under 8 years. The dosage of patients with severe renal insufficiency should be lower than the general dosage. If long-term treatment is needed, blood concentration monitoring should be done. Effects on pregnancy and lactation: The safety of pregnant women using this drug has not been determined.

Minocycline capsule preparation

dynamics

The product is quickly absorbed after oral administration, and food has no significant effect on the absorption of the product. Oral administration of this product 0, 2g, within 1 to 4 hours (average 2, 2 hours) peak blood concentration (Cmax) of 2, 1 to 5, 1mg / L. This product is highly fat soluble and easily penetrates into many tissues and body fluids, such as thyroid, lung, brain and prostate. The concentration of this product in bile and urine is 10 to 30 times higher than that of blood drug, and in saliva and tear The concentration is higher than other tetracycline antibiotics. The serum protein binding rate was 76% to 83%. It is more metabolized in the body, and the original drug excreted in the urine is much lower than other tetracyclines. The product is excreted slowly, most of it is excreted by the kidneys and bile. The blood elimination half-life (t1 / 2) was 11, 1 to 22, and 1 hour (average of 15 and 5 hours).

Dosage

oral. The first dose for adults is 0, 2g, and then take the product 0, 1g every 12 hours, or 50mg every 6 hours.

Taboo

Those who are allergic to this product and other tetracyclines are prohibited.

Drug response

1. Since this product can reduce the activity of prothrombin, the dosage of anticoagulant should be reduced when it is used in combination with anticoagulant. 2. As antacids (such as sodium bicarbonate) can reduce the absorption and activity of the product, it should be avoided at the same time. 3. When the product is combined with a drug containing aluminum, calcium, magnesium, and iron ions, it can form an insoluble complex, which reduces the absorption of the product. 4. When the cholesterol-lowering drug cholestyramine or colestipol is used in combination with this product, it may affect the absorption of this product. 5. Because barbiturates, phenytoin, or carbamazepine can induce the activity of microsomal enzymes, the blood concentration of this product is reduced, so the dose of this product must be adjusted when combined. 6. General anesthetic mefflurane combined with this product can cause fatal nephrotoxicity. 7. As this product can interfere with the bactericidal activity of penicillin, it should be avoided in combination with penicillin. 8. The combination of this product with strong diuretics (such as furosemide, etc.) can aggravate kidney damage. 9. The combination of this product with other hepatotoxic drugs (such as anti-tumor chemotherapy drugs) can aggravate liver damage. 10. The combination of this product with oral contraceptives can reduce the effect of oral contraceptives.

Minocycline Pharmaceutical Applications

Minocycline arthritis

Rheumatoid arthritis

One study showed that minocycline is an effective disease-modifying antirheumatic drug (DMARD) for patients with early rheumatoid arthritis.

O'Dell et al from the University of Nebraska, Omaha, USA conducted a two-year randomized double-blind study comparing the efficacy of minocycline and hydroxychloroquine in 60 patients with rheumatoid arthritis who were seronegative <1 year. . (Arthritis Rheum 2001, 44: 2235)

Thirty patients received 100 mg minocycline twice daily; another 30 patients received hydroxychloroquine 200 mg twice daily. All patients took small doses of prednisone. After 2 years of treatment, the researchers tested the percentage of patients with a 50% improvement (according to the American College of Rheumatology Standard, ACR50). The results showed that 60% of patients in the minocycline group reached ACR 50 after two years, compared with only 33% of patients in the hydroxychloroquine group (P = 0, 04). In the minocycline group, the prednisone dose was lower than that of the hydroxychloroquine group at 2 years of treatment, which were 0, 81, and 3, 21 mg / d (P <0, 01). Patients in the minocycline group were more likely to discontinue prednisone completely than the hydroxychloroquine group (P = 0, 03).

According to the ACR assessment criteria, the outcome of the minocycline group had a good trend, and there was a significant difference in the evaluation of the disease activity of patients (P = 0, 004).

Minocycline sinusitis

Paranasal sinusitis is a common disease in the otolaryngology department. Due to the special anatomy of the paranasal sinuses, treatment is often difficult to complete. In June-December 1998, 62 patients with paranasal sinusitis were treated with minocycline (metamycin) in the outpatient department, and achieved good results. The following report is as follows:

[Object and Method]

Of the 62 patients, 32 were male and 30 were female, aged 14 to 56 years, with an average age of 35 years. Among them, 40 cases were acute paranasal sinusitis and 22 cases were acute episodes of chronic paranasal sinusitis. All patients underwent paranasal sinus radiography or paranasal sinus CT. Scan confirmed. There were 36 cases of maxillary sinusitis, 12 cases of maxillary sinusitis and ethmoid sinusitis, 6 cases of maxillary sinusitis with ethmoid sinus and sphenoid sinusitis, and 8 cases of maxillary sinusitis with frontal and ethmoid sinusitis. No antibiotics were used within 48 hours before treatment.

Methods The minocycline capsules (100mg / capsule) produced by Suzhou Lida Pharmaceutical Co., Ltd. were used for the first time at 0, 2g, po, and each subsequent time at 0, 1g, bid for 2 weeks, and the symptoms and signs were observed. Maxillary sinus puncture was performed before and after treatment, and pus was cultured for bacteriology; blood and urine routines, liver and kidney functions were examined.

The curative effect evaluation standard is divided into 3 levels: Cure: the symptoms and signs are completely controlled, and the bacteriological examination is normal. Significant effect: Symptoms and signs were significantly improved, and the strains of bacteriological examination were significantly reduced. Ineffective: no obvious changes in symptoms and signs.

result

Among 62 patients, 41 cases were cured, 12 cases were markedly effective, 9 cases were ineffective, the cure rate was 66, 1%, and the total effective rate was 85, 5%. Bacterial culture showed: 11 cases of Streptococcus pneumoniae, 6 cases were cured; Haemophilus influenza 14 cases of Bacillus were cured, 11 cases were cured; 11 cases of Escherichia coli, 9 cases were cured; 16 cases of anaerobic bacteria, 14 cases were cured; 6 cases of Staphylococcus aureus were ineffective. Six patients had mild dizziness, and 8 patients had gastrointestinal discomfort, which were all tolerated without affecting the treatment. The reaction disappeared after stopping the drug. After treatment, blood and urine routines were reviewed, and liver and kidney function were normal.

[Expert discussion]

Minocycline is a new generation of semi-synthetic tetracycline drugs, which has the advantages of broad spectrum, long lasting power, and no photosensitivity. Eating or drinking dairy products while taking it does not affect its absorption. It has high fat solubility, penetrates into the sinus tissue, and can quickly reach and exceed the minimum inhibitory concentration of pathogenic bacteria. It has a good effect on E. coli, Haemophilus influenzae, Streptococcus pneumoniae, Mycoplasma pneumoniae, Clostridium anaerobic, and most of Staphylococcus aureus are resistant to this class of drugs. This group of clinical studies shows that minocycline has good clinical efficacy, has the advantages of convenient oral administration and mild side effects, and is indeed an ideal drug for the treatment of paranasal sinusitis.

Minocycline venereal disease

Minocycline (dimethylamine tetracycline, minocycline, minocin) is a second-generation tetracycline, it is a semi-synthetic tetracycline, chemical name 7-dimethylamino-6-desmethyl-6- Deoxytetracycline. It is used to treat all kinds of mild and moderate infections caused by sensitive pathogens and has good clinical effect.

[General pharmacological effects]

Minocycline is a broad-spectrum antibiotic, which has similar pharmacological effects as tetracycline, but has a stronger effect.

Antibacterial: sensitive to gram-positive and negative bacteria, especially to tetracycline-resistant strains; it also has antibacterial activity against aerobic and anaerobic bacteria; in addition, it has inhibitory effects on mycoplasma and chlamydia. Minocycline is mainly bacteriostatic, but high concentration also has bactericidal effect.

Inhibition of lymphocyte activity: Minocycline can significantly inhibit the mitogen-responsive response of lymphocytes to phytohemagglutinin (PHA);

Anti-inflammatory: Minocycline can inhibit neutrophil chemotaxis and inhibit the oxygen intermediates involved in inflammation;

Anti-collagenase activity: Collagenase activity depends on calcium and zinc. Minocycline can affect calcium and zinc levels through its chelation.

Inhibition of sebum secretion: Minocycline can significantly reduce the level of free fatty acids in the skin of the face. With the extension of treatment time, the more the amount of free fatty acids is reduced, the effect can be maintained after stopping the drug.

Effect on protein metabolism: By blocking the binding of aminothiol-S-RNA to the RNA ribosome complex, it hinders protein synthesis.

Affecting cell adhesion: Minocycline can increase the adhesion and elongation of gingival fibroblasts at doses less than 100 g / ml.

Clinical application

Acne minocycline works well for moderate to severe inflammatory acne. Both double-blind studies with placebo or tetracycline have shown that minocycline has a good clinical effect, the number of propionibacterium acnes bacteria and facial sebum in patients' skin have been significantly reduced, and the effect is maintained after stopping the drug. Chen Renyi treated acne vulgaris with minocycline and tetracycline and compared them. A total of 114 patients were randomly divided into two groups. Among them, 58 patients in the minocycline group took 50 mg orally twice daily, and 54 patients in the tetracycline group. Oral 25mg, 4 times a day in the first week, weekly reduction to once a day in the fourth week. After 4 weeks of administration, the efficacy was judged: 42 cases were cured in the minocycline group, with a total effective rate of 96,55%; 14 cases were cured in the tetracycline group, 21 were effective, 19 were ineffective, and the total effective rate was 64, 81%. The two groups were cured There were significant differences in the rate and total effective rate (P <0, 01). Clinical treatments at home and abroad show that minocycline reduces the concentration of free fatty acids in sebum through antibacterial, anti-inflammatory and inhibition of extracellular lipase, which has a satisfactory curative effect on acne, and its effect is obviously better than tetracycline.

[Skin and soft tissue infections]

Minocycline has a better effect on Staphylococcus epidermidis infections and soft tissue infections caused by S. aureus. Skin infections caused by Mycobacterium marine fish can be cured with minocycline for 2 months. Sawchuk et al. Reported a case of pyoderma-like pyoderma that did not respond to previous therapies. The combined treatment with carbon dioxide laser and long-term minocycline was effective. Branger et al reported that a renal transplant patient with M. haemophilus combined with M. mutans infection was cured by surgical drainage of the ulcer and oral minocycline. Minocycline also has significant effects on actinomycosis and nocardia that are primary to the skin. If patients with actinomycosis are allergic to penicillin, the use of minocycline is effective and does not recur after cure.

[Gangrene pyoderma]

Lynch et al. Reported for the first time 4 cases with minocycline 300mg qid at high doses to obtain significant effects. It also has a significant effect on the special types of this disease, namely recurrent atypical bullous gangrene pyoderma and superficial granulomatous pyoderma.

Edema

Other skin diseases, granulomatous rosacea, with minocycline 100 mg daily for 3 weeks, the symptoms quickly improved; later reduced to 50 mg daily for 4 weeks and cured. Using minocycline alone or minocycline instead of corticosteroids for dystrophic bullous epidermal laxity can significantly reduce new blisters. Muto et al. Reported that 1 case of follicular mucinopathy was effective in the treatment of minocycline and indomethacin, and minocycline and or indomethacin were recommended as the first choice for the treatment of this disease. Tanigaki et al. Used minocycline to treat eosinophilic pustular folliculitis effectively. Liegner used minocycline 100mg once every 12 hours to treat early migratory erythema, the rash subsided 7 days after taking the drug, fever and systemic symptoms disappeared after 10 days, and regular inspections in the future did not show recurrence of clinical or laboratory indicators.

Sexually transmitted diseases

Because minocycline has effects on gonococci, anaerobic bacteria, chlamydia trachomatis, mycoplasma, etc., and the effect is significantly better than penicillin and ampicillin, it is widely used to treat gonorrhea, non-gonococcal urethritis, chlamydia trachomatis cervicitis Other sexually transmitted diseases.

Penicillium

Gonorrhea minocycline is suitable for asymptomatic male urethritis caused by gonococcus. Chen Lin et al. Treated 6 cases of gonorrhea with dimethylamine tetracycline capsules and compared them with doxycycline; the treatment group took orally dimethylamine tetracycline capsules 100mg twice daily; the control group took orally doxycycline tablets 100mg twice daily, of which the treatment group 6 5 cases were cured, 5 cases in the control group were cured, and 1 case progressed without significant difference. Li Jiawen et al. Treated 12 patients with chronic gonorrhea with minocycline, took 100 mg orally twice daily, and stopped taking the drug for 2 weeks, and 10 patients were cured with a cure rate of 83,3%. Clinically, taking minocycline has obvious curative effect on gonorrhea.

Non-gonococcal urethritis (Nongonococcal Urethritis, NGU) has a higher incidence than gonorrhea in western countries, and it is also increasing in China. It is mainly caused by chlamydia and mycoplasma infection, and is often resistant to penicillin. Li Jiawen and other 35 patients with non-gonococcal urethritis were treated with minocycline twice daily, 100 mg once a day for 2 weeks, of which 34 cases were cured, the cure rate was 97,1%. Xia Weizhong treated non-gonococcal urethritis with minocycline and fluazinic acid and compared the results with observations: 35 patients in group A were treated with minocycline twice a day, 100 mg once, 21 days as a course of treatment; group 34 Cases were treated with fluoxacin twice daily, 200 mg once, for a period of 21 days. There were 35 cases in group A, 31 cases were cured, 4 cases were ineffective, the cure rate was 88, 57%; 34 cases in group B, 23 cases were cured, 11 cases were ineffective, the cure rate was 67, 64%, and there were significant differences between the two groups (P <0, 05). Zhang Xibao used minocycline and clarithromycin as a clinical control. Among them, 30 patients in group A received cyclamycin microcapsules 200mg / d, and 32 patients in group B received clarithromycin 500mg / d. It is a course of treatment, generally 1 to 2 courses of treatment. The pathogenic cure rate of group A is 90% (27/30), the effective rate is 10% (3/30), and the total effective rate is 100%.

uterus

Chlamydia trachomatis infection in female genital tract of cervicitis is the most common sexually transmitted disease worldwide, and its incidence is increasing year by year in China. Fan Shangrong treated 40 cases of patients with Chlamydia trachomatis infection of the cervix without concurrent appendicitis or pelvic inflammation with minocycline: oral administration of minocycline 100mg qn to patients and their spouses, doubled for the first time, patients took 14d, spouses took 9d, treatment Two weeks after the completion of the review, the microbial cure rate was 92%, and oral minocycline was effective in treating uncomplicated cervical chlamydia trachomatis infection. Ding Shao is treating 20 patients without comorbidities with Chlamydia trachomatis infection with 7-day therapy with minocycline, taking 100 mg orally twice a day for 2 weeks after 7 days of discontinuation, 1 patient stopped after 5 days due to side effects, and the remaining 14 patients Of these, 13 patients had no obvious symptoms, 11 patients had cervicitis, and 4 patients still had cervical erosion, brittleness, or bleeding after wiping. 93% of the patients had symptoms of STD subsided, and all of the chlamydia antigen tests turned negative, and the results were satisfactory. . Applications in Urology

Urinary tract infections: 30 cases of urinary tract infections treated with minocycline, such as Jiu Yonghong, the results show that the cure rate of this drug is 86, 7%, and the drug sensitivity to Staphylococcus aureus and Escherichia coli Up to 93,3%, the minimum inhibitory concentration for gram-negative and gram-positive bacteria is 0, 5 g / ml ~ 4, 0 g / ml, which is significantly better than gentamicin and ampicillin.

prostate

Chronic prostatitis Liu Dingyi and other patients applied minocycline to treat 37 cases of chronic prostatitis. All patients were treated with minocycline 100 mg orally twice daily for 4 weeks as a course of treatment. Of the 37 cases, 18 cases were cured, accounting for 48 and 6%. 10 cases accounted for 27%, 9 cases were invalid, accounting for 24 and 3%, and the total effective rate was 75 and 6%. Xia Xinhui and others treated 26 cases of chronic gonococcal prostatitis with minocycline, oral administration of 100 mg, twice a day, doubled for the first time, 14 days as a course of treatment. 16 cases were cured, 6 cases were effective, and 4 cases were not effective. In this report, fluoxacin, rifampicin and josamycin were also compared. The efficacy of minocycline was better than other drugs.

side effect

Minocycline has certain side effects. In addition to prolonged gastrointestinal irritation, even if the following side effects occur, it will disappear when minocycline is stopped.

Gastrointestinal reactions In the above cases, a small number of patients experienced varying degrees of dizziness, nausea, vomiting, and abdominal pain.

Allergic reactions can cause itching of the skin, urticaria, fixed drug rash, etc. For example, Su Yuhua reported that symmetrical erythema appeared on the extension of the elbow joint due to the use of minocycline, with a large blister on each. Take the antihistamine after stopping the drug , 1% calamine lotion was applied and subsided after 1 week.

Vitamin B6

Pigmentation Skin pigmentation occurs after long-term use of minocycline, which can be limited blue-gray, lower-limb blue-black or extensive mud brown or dark blue-gray pigment. Lei Tiechi reported two cases of cyanomycin spots on the face caused by taking minocycline, darkening the pigments after sun exposure, stopping and taking vitamin C and vitamin E orally, and reducing the pigmentation after 1 month. Similar symptoms occurred after taking minocycline ; In another case, two weeks after taking the drug, the skin around the lower lip and the glans mucous membrane saw large dark brown stains of coins, and the color reduction was reduced 3 months after treatment.

Conclusion

Due to its high lipophilicity and excellent tissue permeability, minocycline can be widely distributed in various tissues and fluids of the body, its half-life is longer than tetracycline, and its blood concentration is high and its bactericidal ability is strong. At the same time, the drug can be eliminated from the urethra with almost no change, and even if it is broken down, its catabolic substance also has antibacterial activity. Therefore, the drug has the characteristics of high efficiency, broad spectrum, fast-acting, long-acting, and fast oral absorption. It has certain effects in skin diseases, urinary system, and respiratory infections. Although it has certain side effects, it is lighter than tetracyclines and is an anti-infective drug that is worth promoting.

Minocycline related news

In April 2013, Japanese researchers recently discovered that minocycline can prevent men from being seduced and led astray by beautiful women. Professors from Waseda University and Kyushu University in Japan want to test the effect of consciousness change after taking dimethylamine tetracycline. They simulated a "beauty plan" and showed 98 testers 8 attractive photos of women and asked them to evaluate the photos. Chinese beauty can rely on the level.

The men tested were divided into two groups, one group taking dimethylamine tetraorally every 4 days

Cyclin; the other group took a placebo. When showing testers beautiful photos of women, the researchers told male testers that they could have 1,300 yen in control and assigned to the women in each photo. In the test, male test subjects were asked how to evaluate the reliability of each woman in the photo and the charm of their beautiful body. In fact, all the pretty women in the photos have pre-determined betrayal of their male partners, so male testers are playing emotional games with unreliable women, but they were not aware of it before.

The results showed that the trust behavior of male testers increased with the increase of female attractiveness, but this female charm did not affect male testers taking dimethylamine tetracycline. At the same time, the study also found that when the money element is introduced, women's charm will further increase. ^[2]