Generic name: Penicillin potassium for injection
English name:
Benzylpenicillin Potassium For Injection Hanyu Pinyin: Zhusheyong Qingmeisujia
[Main ingredients] Potassium penicillin
[Properties] This product is white crystalline powder.
[Pharmacological action] Pharmacodynamics Penicillin is a bactericidal antibiotic with strong antibacterial activity, and its antibacterial mechanism of action is mainly to inhibit the synthesis of bacterial cell wall mucin. In the growth period of sensitive bacteria, the cell wall is in the biosynthesis stage, under the action of penicillin, the synthesis of mucopeptide is blocked and cannot form the cell wall, which leads to the cell membrane rupture and death under the action of osmotic pressure. If the bacteria in the non-growing and reproducing period do not need to synthesize cell wall, penicillin will not have bactericidal effect. The latter puts the bacteria in a state of growth inhibition. The latter puts the bacteria in a state of growth inhibition, resulting in the inability of penicillin to work.
Penicillin is a narrow-spectrum antibiotic, mainly against a variety of gram-positive bacteria and a few gram-negative bacteria. The main sensitive bacteria are Staphylococcus, Streptococcus, Bacillus porcineus, Corynebacterium, Clostridium tetani, Actinomyces, Bacillus anthracis, Spirochete, etc. It is not sensitive to Mycobacterium, Mycoplasma, Chlamydia, Rickettsia, Nocardia, fungi and viruses.
Pharmacokinetics Penicillin potassium salt is rapidly absorbed after intra-muscular injection, reaching peak blood concentration in 15-30 minutes, and the time to maintain blood concentration above 0.5μg/ml after intra-muscular injection is 6-7 hours. Penicillin can be widely distributed to all tissues of the body, and can enter the fetal circulation, with higher concentrations in kidney, liver, lung, muscle, small intestine and spleen; the content of bone, saliva and milk is lower. It is difficult to enter the cerebrospinal fluid, its concentration in the normal cerebrospinal fluid is only 1%~3% of the blood drug concentration, and the concentration in the cerebrospinal fluid can reach 5%~30% of the blood drug concentration when inflammation. The concentration of penicillin in breast milk can be 5%-20% of the blood concentration. Penicillin injected into the milk chamber can be absorbed in large quantities in the first few hours. However, the antibacterial concentration in milk can be maintained for a considerable period of time. It has been reported that 100,000 units of penicillin aqueous solution injected into the milk chamber can be retained in milk for 4.26 units/ml up to 2 4 hours.
A small proportion of penicillin is metabolized in the liver and most of it is excreted in its original form. Under normal renal function, 50%-75% is excreted from the kidneys, 90% of which is secreted through the renal tubules and is eliminated in vivo more rapidly because of rapid excretion. The plasma protein binding rate of penicillin is about 50%. The half-life of penicillin is short and the difference between species is small, with a half-life of 0.5 to 1.2 hours in all domestic animals. The apparent volume of distribution is also small, generally 0.2 to 0.3 L/kg. plasma concentration is high, tissue concentration is low.
[Drug Interaction] (1) Penicillin combined with aminoglycosides can increase the concentration of the latter in the body of bacteria, showing synergistic effect.
(2) Macrolides, tetracyclines and amidol and other fast-acting antibacterial agents interfere with the bactericidal activity of penicillin and should not be used together.
(3) Heavy metal ions (especially copper, zinc, mercury), alcohols, acids, iodine, oxidizing agents, reducing agents, hydroxyl compounds, acidic glucose injection or tetracycline hydrochloride injection, etc. can destroy the activity of penicillin and are prohibited to be used together.
(4) Amines and penicillin can form insoluble salts, which can delay the absorption of penicillin, such as procaine penicillin.
(5) Potassium penicillin water-soluble and some drug solutions (such as chlorpromazine hydrochloride, lincomycin hydrochloride, norepinephrine tartrate, oxytetracycline hydrochloride, tetracycline hydrochloride, B vitamins and vitamin C) should not be mixed, otherwise it may produce turbidity, flocculence or precipitation.
[Indications] It is mainly used for Gram-positive bacterial infections, but also for infections of actinomycetes and leptospirosis, such as porcine dysentery, emphysema, malignant edema, actinomycosis, equine glandular disease, necrobiosis, leptospirosis and mastitis, skin soft tissue infections, arthritis, uterine inflammation, pyelonephritis, pneumonia, septicemia and tetanus. It should be used in combination with tetanus antitoxin in the treatment of tetanus.
[Dosage and Administration] Intramuscular injection: once per 1kg body weight, 10,000～20,000 units for horses and cattle; 20,000～30,000 units for sheep, pigs, foals and calves; 30,000～40,000 units for dogs and cats; 50,000 units for birds. 2~3 times a day for 2~3 days.
Before use, add sterilized water for injection to dissolve.
[Adverse reactions] (1) Mainly allergic reactions, which can occur in most domestic animals, but the incidence is low. Local reactions include edema and pain at the injection site, and systemic reactions include urticaria and rash, which may cause shock or death in serious cases.
(2) In some animals, penicillin can induce secondary infection of the gastrointestinal tract.
(1) Penicillin potassium is easily soluble in water, the aqueous solution is unstable and easily hydrolyzed, the rate of hydrolysis is accelerated with the increase of temperature, so the injection should be prepared before use. When necessary, it should be kept in the refrigerator (2-8℃) for 7 days, and only 24 hours at room temperature.
(2) Interaction with other drugs and contraindications should be understood to avoid affecting the efficacy of penicillin.
(3) Penicillin potassium 1,000,000 units (0.625g) contains 0.065g of potassium ion, and hyperkalemia may occur with high dose injection. It will have adverse effects on animals with reduced renal function or cardiac insufficiency, and the adverse effects of potassium ion on the heart are more serious.
[Rest period] Cattle, sheep, pigs and poultry: 0 days; cattle and sheep: 72 hours during milk abandonment.
[Specification] 1.0g (1.6 million units) in C16H17KN2O4S
[Storage] Airtight, kept in a cool, dark and dry place.
Execution standard] "Chinese Veterinary Pharmacopoeia" 2010 edition a
GMP Mark] (2015) Veterinary Drug GMP Certificate No. 22016
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