What Is Acyclovir?
Acyclovir is a synthetic purine nucleoside analog. It is mainly used for various infections caused by herpes simplex virus, and can be used for HSV infections in primary or recurrent skin, mucous membranes, external genital infections and immunodeficiency patients. As the drug of choice for the treatment of HSV encephalitis, reducing morbidity and reducing mortality are better than arabinose. Can also be used for herpes zoster, Epstein-Barr virus, and chickenpox infections in immunodeficiency patients. For topical application only to the skin, less skin absorption of acyclovir.
- Drug Name
- Acyclovir
- Alias
- Open-chain guanine nucleoside; acyclovir; acyclovir; acyclovir; acyclic guanine nucleoside; 9- (2-hydroxyethoxymethyl) guanine;
- Foreign name
- Acyclovir; acycloguanosine; Poviral; aclovir;
- Whether prescription drugs
- prescription
- Main indications
- Herpes simplex virus infection
- Dosage
- 0.1 g
- Adverse reactions
- Itchy skin or hives.
- Main medication contraindications
- Can cause nephrotoxicity in combination with zidovudine
- Dosage form
- White crystalline powder
- Character
- The product is a white tablet
- CAS number
- 59277-89-3
- Molar mass
- 225.21
- Chemical formula
- C8H11N5O3
- Solubility (water)
- Slightly soluble in water
- Acyclovir is a synthetic purine nucleoside analog. It is mainly used for various infections caused by herpes simplex virus, and can be used for HSV infections in primary or recurrent skin, mucous membranes, external genital infections and immunodeficiency patients. As the drug of choice for the treatment of HSV encephalitis, reducing morbidity and reducing mortality are better than arabinose. Can also be used for herpes zoster, Epstein-Barr virus, and chickenpox infections in immunodeficiency patients. For topical application only to the skin, less skin absorption of acyclovir.
Introduction to Acyclovir Compounds
Acyclovir Basic Information
- Phonetic name: AXILUOWEI
- Chinese name; Acyclovir
- English name: Acyclovir
- Acyclovir molecular formula
- Chinese alias: acyclovir, glycosylguanosine, hydroxyethoxyguanosine, suitable therapy, infusion therapy, acyclic guanine nucleoside, acycloguanine, acycloguanosine, 9- ( 2-hydroxyethoxymethyl) guanine Acyclovir, Acycloguanosine, ZOVIRAX.
- CAS: 59277-89-3
- Molecular formula: C 8 H 11 N 5 O 3
- Molecular weight: 225.21
- Exact mass: 225.08600
- PSA: 119.05000
- Drug Category: Antiviral Drug Category: Antiviral
Acyclovir physical and chemical properties
- Appearance and properties: white to light yellow crystal powder
- Density: 1.77
- Melting point: 256-257 ° C
- Boiling point: 595ºC at 760 mmHg
- Stability: stable, but incompatible with strong oxidants
- Storage conditions: storeroom is ventilated, low temperature and dry, stored separately from food ingredients
Aciclovir Safety Information
- Customs code: 2933790090
- WGK Germany: 2
- Danger category code: R36 / 37/38
- Safety instructions: S22-S24 / 25
- RTECS number: UP0791400
- Dangerous goods mark: Xi [1]
Acyclovir production method
- Method 1: Preparation of N-7 (or 9) -diacetylguanine using guanine nucleoside as raw material 283g of guanine nucleotides, 1.03L of 10mol acetic anhydride and 210ml of 2mol acetic acid were added to a 5L three-necked flask, and heated to reflux After 1h, add 17.2g of 0.2mol PTS, reflux for 1h, recover acetic anhydride and acetic acid by distillation under reduced pressure, add 600ml of ethyl acetate to the concentrated solution, reflux for 1.5h, and filter after cooling to obtain the product. Guanine nucleotides [acetic anhydride, acetic acid, PTS] N-7- (or 9) -diacetylguanine N-acetyl-9-[(2-acetoxyethoxy) methyl] guanine Add 200 g of N-7 (or 9) -diacetylguanine, 282 g of 2-oxo-1,4-butanediol diacetate, 9 g of PTSA, and 1.2 L of toluene into the three-necked flask. After refluxing for 24 hours, quickly cool To 0 ° C, filter and dry to get the product. N-7 (or 9) -diacetylguanine [2-oxo-1,4-butanediol diacetate, PTSA, toluene] N-acetyl-9-[(2-acetoxyethoxy Of methyl) methyl] guanine acycloguanosine N-acetyl-9-[(2-acetoxyethoxy) methyl] guanine 0.5mol, 2.7L of 25% methylamine aqueous solution was placed on the three neck In the bottle, react for 0.5 h at 35-37 ° C under stirring, concentrate to dryness under reduced pressure, add 350 ml of ethanol to dissolve, filter, wash the filter cake with ethanol, and dry to obtain a crude product. Recrystallized with 40 times water to obtain fine products. N-acetyl-9-[(2-acetoxyethoxy) methyl] guanine [methylamine] [35-37 ° C, 0.5h] acycloguanosine
- Method 2: Preparation of N, N-diacetylguanine using guanine as raw material, put 5g of guanine in a round bottom flask, add 81ml of acetic anhydride, stir and mix, add a small amount of acetic acid and zinc acetate, heat and reflux for 16h, cool The acetic acid was recovered under reduced pressure, cooled in an ice bath, filtered, washed with ethanol, and dried to obtain a product. Guanine [acetic anhydride, acetic acid, zinc acetate] N, N-diacetylguanine 1,3-dioxapentane Preparation After mixing 248 g of ethylene glycol and 120 g of paraformaldehyde, slowly add concentrated sulfuric acid under stirring. 22.1g, reflux for 3h after the addition, cool the reaction solution to room temperature, transfer to a separatory funnel, add sodium chloride saturated salting out, separate the organic phase, dry after distillation, and collect the 74-76 ° C fraction, which is the product. Preparation of ethylene glycol [paraformaldehyde, concentrated sulfuric acid] 1,3-dioxane N-acetyl-9-[(2-acetoxyethoxy) methyl] guanine 31 g of acetic anhydride, acetic acid Mix 5g 2g p-toluenesulfonic acid, cool to below 10 ° C with stirring, add 24g dioxane and keep the temperature not more than 40 ° C, cool to room temperature, add 78ml toluene and 15g N, N-diacetylguanine, stir Reflux for 1 h, cool to room temperature, add chloroform, filter, and dry to obtain the product. N, N-Diacetylguanine [1,3-dioxane, PST, acetic anhydride, acetic acid, toluene] N-acetyl-9-[(2-acetoxyethoxy) methyl] bird Preparation of Purine Acycloguanosine N-acetyl-9-[(2-acetoxyethoxy) methyl] guanine obtained in the previous step was mixed with 120 ml of a 40% methylamine aqueous solution, and heated under stirring for 1 h. After cooling It was filtered, and the filtrate was concentrated under reduced pressure, washed with ethanol, and filtered to obtain a crude product, which was recrystallized from water to obtain a pure acyclovir. N-acetyl-9-[(2-acetoxyethoxy) methyl] guanine [methyl] acyclic guanosine. The 2-chloro-9-(-2-hydroxyethoxymethyl) adenine is reacted with sodium nitrite to obtain the 2-chloro-9- (2-hydroxyethoxymethyl) hypoxanthine (melting point> (310 ° C) saturated with liquid ammonia, and acycloguanosine was formed by heating at 125 ° C for 5h in a closed atmosphere.
- Method 1: Use guanine as raw material. Mix guanine and acetic anhydride, add a small amount of acetic acid and zinc acetate, and stir to reflux. The excess acetic anhydride was evaporated under reduced pressure, cooled to 0 ° C, and filtered. The filter cake was washed with ethanol and water, and dried to obtain N, N, -diacetylguanine in a yield of 92.6%. Mix acetic anhydride, acetic acid and p-toluenesulfonic acid and cool to below 10 ° C. Dioxane is added under stirring, and the internal temperature is controlled below 40 ° C. Cool to room temperature, add toluene and N, N'-diacetylguanine, and stir to reflux. Cool to room temperature, add chloroform, and filter. The filter cake was washed with chloroform, dried, and then dissolved in a 40% methylamine aqueous solution and stirred under reflux. Cool, filter, and concentrate the filtrate under reduced pressure to a slurry. After cooling, wash with ethanol and filter. The filter cake was recrystallized from water to obtain acyclovir with a yield of 75% and a melting point of 255 to 258 ° C. N, N'-diacetylguanine can also be catalyzed with 2-oxo-1,4-butanediol diacetate in dimethyl sulfoxide with p-toluenesulfonic acid. Chromatography was performed to obtain the diacetate of acyclovir, followed by hydrolysis in a methanol solution of saturated ammonia to obtain acyclovir. The total yield in terms of guanine was 43%.
- Method 2: After guanine trimethyl silylation, and then react with 2-benzyloxyethoxymethyl chloride, remove the benzyl group to obtain acyclovir, with a yield of 24% [1] .
Acyclovir uses
- This product is a purine nucleoside derivative that inhibits DNA synthesis. Its anti-herpes virus activity is 160 times stronger than that of adenosine arabinoside. It is clinically used for herpes simplex virus encephalitis, herpes virus keratitis and external genital infections, varicella-zoster virus infection of AIDS and cytomegalovirus infection, chronic hepatitis B, etc. [1] .
Acyclovir Pharmacopoeia Standard
Acyclovir source (name), content (potency)
- This product is 9- (2-hydroxyethoxymethyl) guanine. Calculated on dry basis, containing C8H11N5O3 shall not be less than 98.0%.
Acyclovir traits
- This product is white crystalline powder; odorless and tasteless.
- This product is slightly soluble in glacial acetic acid or hot water, almost insoluble in ether or dichloromethane; easily soluble in sodium hydroxide test solution.
Acyclovir identification
- (1) In the chromatogram recorded under the content determination item, the retention time of the main peak of the test solution should be consistent with the retention time of the main peak of the reference solution.
- (2) The infrared light absorption spectrum of this product should be consistent with the control spectrum (Figure 213 of "Infrared Spectra of Drugs").
Acyclovir check
- Clarity and color of the solution
- Take 0.50g of this product and add 10ml of 1% sodium hydroxide solution to dissolve. The solution should be clear and colorless; if it is turbid, compare with No. 1 turbidity standard solution (Appendix B of Part Two of the 2010 Pharmacopoeia). For injection) or compared with the turbidity standard solution No. 2 (Appendix B of Part Two of the Pharmacopoeia, 2010 Edition), it must not be more concentrated (for oral and external use); if it develops color, it is compared with the yellow colorimetric standard solution No. 1 (2010 Edition Pharmacopoeia II) (Appendix A, Method 1) must not be deeper (for injection) or deeper than Yellow Standard Colorimetric Solution No. 2 (Appendix A, Method 1 of Pharmacopoeia, 2010 Edition 2), and must not be deeper (for oral, external use).
- relative substance
- Take this product, add dimethyl sulfoxide to dissolve and dilute it to make a solution containing 10mg per 1ml, and test according to thin layer chromatography (Appendix VB of Part Two of the Pharmacopoeia, 2010 Edition). Pipette 5l of the above solution and place it on a thin layer of silica gel GF254. On the plate, use chloroform-methanol-concentrated ammonia solution (80: 20: 2) as the developing agent, unfold, dry, and inspect under an ultraviolet light (254nm). Except for the main spots, no other spots of impurities can be seen.
- Guanine and other related substances
- Weigh about 40mg of this product accurately, put it in a 200ml measuring bottle, add 2ml of 0.4% sodium hydroxide solution to dissolve, add 25ml of 0.1% (V / V) phosphoric acid solution, dilute to the mark with water, shake well, and use it as the test solution. ; Accurately measure 1ml, place in a 100ml volumetric flask, add 5ml of 0.1% phosphoric acid solution, dilute to the mark with water, shake well, as a control solution; also accurately weigh 10mg of guanine reference substance, place in a 50ml volumetric flask, add 0.4% Dissolve 5ml of sodium hydroxide solution, add 5ml of 0.1% phosphoric acid solution, dilute to the mark with water, and shake well, and use it as a stock solution of guanine reference; accurately measure 1ml, put it in a 100ml measuring bottle, dilute to the mark with water, shake well, As a guanine impurity reference solution. Measured according to high performance liquid chromatography (Appendix V D of Part Two of the Pharmacopoeia, 2010 edition), using octadecylsilane bonded silica as the filler; using water as the mobile phase A and methanol as the mobile phase B, and performing gradient washing according to the following table Detach; column temperature: 35 ° C; detection wavelength: 254nm. Take appropriate amounts of the guanine reference solution and the control solution, mix them in equal volumes, shake well, and inject 20 l into the liquid chromatograph to adjust the chromatographic system and detection sensitivity. The resolution between the acyclovir peak and the guanine peak should be greater than 3.0 ; The height of the acyclovir peak is about 10% of full scale. Then accurately measure 20 l each of the test solution, the guanine reference solution and the control solution, and inject them into the liquid chromatograph respectively to record the chromatogram. If there is an impurity peak in the chromatogram of the test solution, the amount of guanine should be calculated based on the peak area of the external standard method, which should not exceed 0.7%; the sum of the peak areas of other impurities should not be greater than the main peak area of the control solution (1.0%).
| Time (minutes) | Mobile phase A (%) | Mobile phase B (%) |
| 0 | 94 | 6 |
| 15 | 94 | 6 |
| 40 | 65 | 35 |
| 41 | 94 | 6 |
| 51 | 94 | 6 |
- Loss on drying
- Take this product and dry it at 105 to constant weight, and the weight loss shall not exceed 6.0% (Appendix L of Part Two of the Pharmacopoeia of 2010 Edition).
- Residue on ignition
- Take 1.0g of this product and check it according to law (Appendix N of Part Two of the 2010 Pharmacopoeia). The residual residue shall not exceed 0.1%.
- Heavy metal
- Take the residue left under the burning residue and inspect it according to law (Appendix H of the 2010 edition of the Pharmacopoeia, the second method). The heavy metal must not exceed ten parts per million [2] .
Determination of acyclovir content
- It was determined by high performance liquid chromatography (Appendix D, Part Two of the Pharmacopoeia, 2010 Edition).
- Chromatographic conditions and system suitability tests
- Octadecylsilane-bonded silica gel was used as the filler; methanol-water (10:90) was used as the mobile phase; the detection wavelength was 254 nm. Take 5ml of acyclovir reference solution, add 1ml of guanine reference solution under guanine and other related substances, shake well, inject 20l into the liquid chromatograph, record the chromatogram, acyclovir peak and bird The resolution of the purine peaks should meet the requirements.
- Assay
- Take about 50mg of this product, weigh it accurately, put it in a 50ml measuring bottle, add 5ml of 0.4% sodium hydroxide solution to dissolve, dilute with water to the mark, shake well, take 2ml of precision measurement, put it in a 100ml measuring bottle, and dilute to the mark with water , Shake well, accurately measure 20 l, inject it into the liquid chromatograph, record the chromatogram; also take an appropriate amount of acyclovir reference substance, and measure in the same way. Calculate the peak area according to the external standard method.
Acyclovir Categories
- Antiviral drugs.
Acyclovir storage
- Shaded and sealed [3] .
Acyclovir preparation
- (1) Acyclovir tablets
- (2) Acyclovir ointment
- (3) Acyclovir eye ointment
- (4) Acyclovir eye drops
- (5) Acyclovir for injection
Acyclovir Drug Analysis
- Method name: Acyclovir API-Acyclovir-High Performance Liquid Chromatography
- Scope of application: This method uses high-performance liquid chromatography to determine the content of acyclovir in the acyclovir drug substance.
- This method is applicable to acyclovir drug substance.
- Principle of the method: The test product is dissolved in 0.4% sodium hydroxide solution and diluted with water. It is subjected to chromatographic separation by high-performance liquid chromatography, and the peak area of acyclovir is measured at a wavelength of 254 nm with an ultraviolet absorption detector, and its calculated content.
- Reagent:
- 1. methanol.
- 2.0.4% sodium hydroxide solution.
- equipment:
- Instrument
- 1.1 HPLC
- 1.2 Column
- Octadecylsilane bonded silica as filler
- 1.3 UV absorption detector
- Chromatographic conditions
- 2.1 Mobile phase: methanol water = 10 90
- 2.2 Detection wavelength: 254nm
- 2.3 Column temperature: room temperature
- Sample preparation:
- Preparation of reference solution
- Accurately weigh the appropriate amount of acyclovir reference substance, and use the preparation method of the test solution to prepare a solution containing 20 & micro; g per 1mL, which is the reference substance solution.
- 2. Preparation of test solution
- Weigh about 50mg of the test product accurately, place it in a 50mL measuring flask, add 5mL of 0.4% sodium hydroxide solution to dissolve, dilute with water to the mark, shake well, take 2mL precisely, place in a 100mL measuring bottle, and dilute to the mark with water. Shake well to prepare the test solution.
- Note: "Precision weighing" means that the weighed weight should be accurate to one thousandth of the weighed weight. "Precision measurement" means that the accuracy of measuring the volume should meet the accuracy requirements of the volume pipette in national standards.
- Operation steps: Precisely draw 20 mL of each of the reference solution and the test solution, inject them into a high-performance liquid chromatograph, and measure the peak area of acyclovir (C8H11N5O3) with a UV absorption detector at a wavelength of 254 nm, and calculate its content [ 4] .
Acyclovir drug description
Acyclovir pharmacology and toxicology
- Antiviral drugs. In vitro tests for herpes simplex virus, varicella zoster virus, cytomegalovirus, etc.
- Acyclovir
- Interfering with viral DNA polymerase and inhibiting viral replication;
- Under the action of DNA polymerase, it binds to the growing DNA strand and causes the extension of the DNA strand to be interrupted. The product has a special affinity for the virus, but has low toxicity to mammalian host cells. In vitro cell transformation assays have been reported to be carcinogenic, but no animal carcinogenic evidence has been found in animal experiments. Some animal experiments show that high concentrations of drugs can cause mutations, but there is no basis for chromosomal changes.
- The carcinogenic and mutagenic effects of this product are unclear. Large-dose injections can cause testicular atrophy and decrease sperm counts in animals. The drug can pass through the placenta, and animal experiments have confirmed that it has no effect on embryos [5] .
Acyclovir pharmacokinetics
- Oral absorption is poor, about 15% to 30% is absorbed by the gastrointestinal tract. The effect of eating on blood concentration was not significant. Can be widely distributed in various tissues and body fluids, including brain, kidney, lung, liver, small intestine, muscle, spleen, milk, uterus, vaginal mucosa and
- Acyclovir
Acyclovir indication
- 1. Herpes simplex virus infection: used orally for the first and recurrent cases of genital herpes virus infection; the product is administered orally for recurrent cases for prevention. Injections are for people who are immunocompromised. Treatment of initial and recurrent mucosal skin infections and prevention of recurrent cases; also used for the treatment of herpes simplex encephalitis.
- 2. Herpes zoster: Oral for the treatment of mild cases of herpes with immunodeficiency and immunodeficiency. The injection is used for the treatment of patients with severe herpes in immunodeficiency patients.
- 3. Treatment of chickenpox in immunocompromised persons.
- 4. Topical application for the initial treatment and recurrence of herpes simplex mucosal skin herpes simplex infection caused by herpes simplex virus and immunodeficiency patients.
- 5. Treatment of acute retinal necrosis with its sodium salt. Nucleotide antivirals for the treatment of:
- Herpes simplex keratitis;
- herpes simplex;
- with herpes;
- Use its sodium salt to treat acute retinal necrosis. It is mainly used for superficial and deep keratitis caused by herpes simplex virus and shingles virus.
Acyclovir clinical application
- 1. Herpes simplex virus infection: used for the first and recurrent cases of genital herpes virus infection.
- Acyclovir
- 2. Herpes zoster: Taken for the treatment of mild cases of herpes zoster and immunodeficiency patients with normal immune function.
- 3. Treatment of chickenpox in immunocompromised persons.
- Aciclovir is catalyzed by viral thymidine kinase (TK enzyme) and kinases in cells in infected cells to generate acyclovir triphosphate and inhibit viral DNA polymerase. In addition, once acyclovir triphosphate is incorporated into the DNA of the virus that is being extended, it results in the suspension of DNA synthesis. Drug-resistant virus strains have been found clinically and experimentally. The formation of drug resistance is related to the mutation of the virus thymidine kinase gene. [5]
Acyclovir dosage
- Oral dosage
- The skin and mucous membranes of genital herpes and immunodeficiency patients, herpes simplex 200mg orally once a day
- Acyclovir
- Shingles: Adults usually use 800mg once a day, 5 times a day for a total of 7-10 days.
- For patients with renal insufficiency, the creatinine clearance rate is less than 10ml / min, 150mg every 24 hours; when the creatinine clearance rate is 10-15ml / min, 300mg every 12-24 hours; for those with creatinine clearance> 50ml / min, 300mg every 8 hours. Pediatric doses have not been established.
- Intravenous infusion
- Severe genital herpes is treated for 5 days every 5 hours according to body weight. Immunodeficiency patients with skin herpes simplex or severe shingles, 5mg / kg every 8 hours, intravenous drip for more than 1 hour, a total of 7-10 days.
- Herpes simplex encephalitis, 10 mg / kg every 8 hours for a total of 10 days.
- Adults with acute or chronic renal insufficiency should not use intravenous drip of this product, because excessively rapid drip can cause renal failure.
- The highest daily dose for adults is 30mg / kg for body weight, or 1.5g / m2 for body area.
- Pediatric:
- For the first treatment of severe genital herpes, infants and children under 12 years of age will have a body surface area of 250 mg / m 2 every 8 hours for 5 days.
- Herpes simplex of skin and mucous membrane of immunodeficiency patients, infants and children under 12 years old, according to the body surface area of 250mg / m2 every 8 hours, a total of 7 days, 12 years old or more as an adult.
- Herpes simplex encephalitis, 10mg / kg body weight every 8 hours for a total of 10 days.
- The highest dose for children is 500mg / m2 according to body surface area every 8 hours.
- Topical
- Acyclovir
- (1) Once herpes symptoms and signs appear, they should be administered as soon as possible.
- (2) Oral capsules can be eaten at the same time and have no significant effect on absorption. Recurrent genital herpes infection is effective with intermittent short course therapy. As animal experiments have found that this product has an effect on fertility and mutagenesis, the oral dose and course of treatment should not exceed the recommended standards. Long-term therapy for genital recurrent herpes should also not exceed 6 months.
- (3) intravenous administration:
- Acyclovir sodium is provided for intravenous infusion, and the drug solution is dripped at a uniform rate for at least 1 hour to avoid rapid drip or intravenous bolus injection, because drug deposition in the renal tubules may occur in this way, and cases of renal function damage may Up to 10%
- The urine concentration is highest 2 hours after the intravenous drip. At this time, the patient should be given sufficient water to prevent the drug from depositing in the renal tubules;
- Hemodialysis can reduce the blood drug concentration by 60%, so the dose should be repeated once every 6 hours of hemodialysis;
- Dispensing method: After adding 1ml of water for injection to dissolve, add an appropriate amount of solution (such as glucose injection), so that the concentration is not higher than 7mg / ml. If the concentration is too high (10mg / ml), it can cause phlebitis and overflow. Inflammation occurs at the injection site. Infants should not use benzyl alcohol-containing dilutions to prepare intravenous infusions, or they may cause fatal syndromes, including acidosis, central depression, dyspnea, renal failure, hypotension, epilepsy, and intracranial hemorrhage.
- (4) The ointment is used only on the skin and not on the eyes. Wear finger gloves or gloves when applying medicine.
- (5) Carcinogenic and mutagenic: Tumors have been reported in in vitro cell transformation assays, but no carcinogenic evidence was found in animal experiments. Some animal experiments show that high concentrations of drugs can cause mutations, but there is no basis for chromosomal changes. The carcinogenicity and mutagenicity of this product are not clear.
- (6) Fertility and pregnant women: high-dose oral administration can reduce the number of sperm in animals, but humans take oral 400mg and 1000mg daily for 6 consecutive months without similar situations. The drug can pass through the placenta, and animal experiments have confirmed that it has no effect on the embryo.
- (7) Nursing mother: The concentration of the drug in the milk is 0.6-4.1 times the blood concentration, but no abnormalities were found in the infants.
- (8) Follow-up inspection: Because most patients with genital herpes are prone to cause cervical cancer, patients should be checked at least once a year to detect early. Renal toxicity may be caused by intravenous administration, and renal function should be checked before or during administration. Occasionally a slight irritation was seen after eye drops, but it quickly adapted. This product has poor water solubility, and it is easy to precipitate crystals in cold climates. It needs to be dissolved when used. Intravenous injection needs to be diluted with a large amount of glucose and sodium chloride injection, the pH is alkaline, and the intravenous drip should be slow. Do not let it leak out of the blood vessel, so as not to cause pain and phlebitis. Because the sodium salt of this product is alkaline, it should not be used in combination with other drugs. This product is easy to cause resistance to herpes virus. In severe cases, resistance needs to be replaced with other drugs. Drink more water during medication; creatinine clearance rate of> 0.835ml / 1.73 square meters · seconds in patients with renal insufficiency, 5mg / kg every 8h; creatinine clearance rate of 0.167 0835ml / 1.73 square meters · seconds, 5mg / kg Once every 12 to 24 hours; those whose creatinine clearance is <0.167ml / 1.73 square meters · second, the dose is reduced to 2.5mg / kg, administered every 24h; the dose should be replenished after hemodialysis. Apply to the eyes, an appropriate amount, 5 times a day, while applying antibacterial drugs.
- Eye drops: 1 to 2 drops each time, 3 to 5 times a day, and then use it for 3 days. A total of 5 days [5] .
Acyclovir adverse reactions
- 2. Rare adverse reactions: oral itching of the skin, occasional menstrual disorders in long-term administration. Acute renal insufficiency, hematuria, and hypotension are rare when given by injection, especially intravenously.
- 3. Rare adverse reactions: coma, blurred consciousness, hallucinations, epilepsy and other central nervous system symptoms.
- 4. Local medication adverse reactions: mild pain, burning and stinging accounted for 28%, pruritus accounted for 4%, and rash 0.3%.
- 5. If the following symptoms persist or are noticeable, long-term oral administration of this product will cause joint pain, diarrhea, headache, nausea, vomiting, and dizziness (most of the short-term medications). Long-term medications rarely include acne and insomnia; short-term medications rarely cause loss of appetite. Mild headaches are common for injections, and sweating is rare. The product has low toxicity to cells and a large safety range. Topical eye drops and creams have no significant adverse effects. Intravenous administration requires slow infusion for more than 1 hour or continuous slow infusion, and generally no response. Sometimes rashes, nettles
- Acyclovir
- Except for occasional dizziness, vomiting, and headache, oral acyclovir is almost non-toxic, and intravenous injection is well tolerated. Encephalopathy occurs in only 1% of patients. High-dose intravenous injection can cause neurological disorders. A large number of sudden injections can cause acute tubular necrosis [5] .
Acyclovir precautions
- 1. People who are allergic to acyclovir may also be allergic to this product.
- 2. Genital recurrent herpes infection is effective when administered with short rest therapy. As animal experiments have found that this product has an effect on fertility and mutagenesis, the oral dose and course of treatment should not exceed the recommended standards. Long-term therapy for genital recurrent herpes should also not exceed 6 months.
- 3. Fertility and pregnant women: High-dose injections can cause testicular atrophy and decrease sperm counts in animals, however, humans have taken 400mg and 1000mg daily for 6 consecutive months without similar conditions. The drug can pass through the placenta, and animal experiments have confirmed that it has no effect on the embryo.
- 4. Nursing mother: The concentration of the drug in the milk is 0.6 to 4.1 times the blood concentration, but no abnormalities were found in the infant. No special adverse reactions were found in children.
- 5. Adults with acute or chronic renal insufficiency should not use this product intravenously, because the drip rate may cause renal failure.
- Acyclovir tablets
- 6. Elderly: Due to the decline of physiological renal function, the dose of this product needs to be adjusted.
- 7. The pros and cons of medication need to be considered in the following cases: those who are dehydrated or have renal insufficiency, the dose of this product should be reduced. Patients with severe liver dysfunction, those who cannot tolerate the product, mental abnormalities, or those who have previously had a psychiatric reaction to cytotoxic drugs, intravenous application of this product is prone to produce mental symptoms and should be used with caution.
- 8. Patients with severe immune dysfunction may cause herpes simplex virus and shingles virus resistance to this product after long-term or repeated application of this product. If herpes simplex patients do not improve the skin lesions after applying acyclovir, the sensitivity of herpes simplex virus to this product should be tested.
- 9. Interference to diagnosis: Intravenous administration can cause renal tubular obstruction, which increases blood creatinine and urea nitrogen. If the dose is appropriate, sufficient water will not cause it.
- 10. Follow-up inspection: Most female genital herpes patients are susceptible to cervical cancer, so patients should be checked at least once a year for early detection. Renal toxicity may be caused by intravenous administration, and renal function should be checked before or during administration.
- 11. Overdose: There is no special antidote for this product. Symptomatic treatment and supportive therapy are mainly used: sufficient water is provided to prevent the drug from being deposited in the renal tubules; hemodialysis helps excrete drugs in the blood, which is especially important for patients with acute renal failure and hematuria [6] .
Acyclovir storage
- Keep tightly closed.
Acyclovir Taboo
- Elderly: Due to the decline of physiological renal function, the dose and interval of this product need to be adjusted. The following situations need to consider the pros and cons of medication: dehydration or renal insufficiency, the dose of this product should be reduced. Patients with severe liver dysfunction, those who cannot tolerate the product, mental abnormalities, or those who have previously had a psychiatric reaction to cytotoxic drugs, intravenous application of this product is prone to produce mental symptoms and should be used with caution.
- 1. Those with a history of allergies to this product are prohibited.
- 2. Patients with abnormal liver and kidney function should be used with caution.
- 3. Do not use orally or intravenously for pregnant women. Disable pregnant women; intravenous drip time is not less than 1h.
Acyclovir drug interactions
- 1. Intravenous administration with interferon or methotrexate (intrathecally) may cause mental disorders and should be used with caution. 2. Combined with nephrotoxic drugs during intravenous administration can aggravate nephrotoxicity, especially for those with renal insufficiency.
- 3. Probenecid can reduce the secretion of the drug from the renal tubules during intravenous administration of the product, increase the blood concentration, eliminate the prolonged half-life, and increase the toxicity.
- 4. Combination with Zidovudine can cause renal toxicity, manifested as deep lethargy and fatigue. Probenecid and -lactams can increase the blood concentration of this product. This product is used in combination with aminoglycosides to increase renal toxicity. This product and probenecid competitively inhibit the secretion of organic acids, and probenecid can slow the excretion of this product, prolong the half-life, and accumulate the amount of drug in the body.