Blueshell Procaine Benzylpenicillin
Blueshell Procaine Benzylpenicillin Uses, Dosage, Side Effects, Food Interaction and all others data.
Benzylpenicillin (Penicillin G) is narrow spectrum antibiotic used to treat infections caused by susceptible bacteria. It is a natural penicillin antibiotic that is administered intravenously or intramuscularly due to poor oral absorption. Penicillin G may also be used in some cases as prophylaxis against susceptible organisms.
Natural penicillins are considered the drugs of choice for several infections caused by susceptible gram positive aerobic organisms, such as Streptococcus pneumoniae, groups A, B, C and G streptococci, nonenterococcal group D streptococci, viridans group streptococci, and non-penicillinase producing staphylococcus. Aminoglycosides may be added for synergy against group B streptococcus (S. agalactiae), S. viridans, and Enterococcus faecalis. The natural penicillins may also be used as first or second line agents against susceptible gram positive aerobic bacilli such as Bacillus anthracis, Corynebacterium diphtheriae, and Erysipelothrix rhusiopathiae. Natural penicillins have limited activity against gram negative organisms; however, they may be used in some cases to treat infections caused by Neisseria meningitidis and Pasteurella. They are not generally used to treat anaerobic infections. Resistance patterns, susceptibility and treatment guidelines vary across regions.
Penicillin G is a penicillin beta-lactam antibiotic used in the treatment of bacterial infections caused by susceptible, usually gram-positive, organisms. The name "penicillin" can either refer to several variants of penicillin available, or to the group of antibiotics derived from the penicillins. Penicillin G has in vitro activity against gram-positive and gram-negative aerobic and anaerobic bacteria. The bactericidal activity of penicillin G results from the inhibition of cell wall synthesis and is mediated through penicillin G binding to penicillin binding proteins (PBPs). Penicillin G is stable against hydrolysis by a variety of beta-lactamases, including penicillinases, and cephalosporinases and extended spectrum beta-lactamases.
Procaine benzylpenicillin (INN), also known as procaine G penicillin, is an injectable antiobiotic. It is a poorly soluble salt form of penicillin which is a combination of naturally occuring benzylpenicillin (penicillin G) and the local anaesthetic agent procaine in equimolar amounts. Procaine benzylpenicillin is administered by deep intramuscular injection. It is slowly absorbed and hydrolyzed to benzylpenicillin. This drug is used where prolonged exposure to benzylpenicillin at a low concentration is required. This combination is aimed at reducing the pain and discomfort associated with a large intramuscular injection of penicillin. It is widely used in veterinary settings. Benzylpenicillin is active against a wide range of organisms and is the drug of first choice for many infections.
It is an antibiotic against penicillin-susceptible microorganisms with bactericidal effect. Like all penicillins, procaine benzylpenicillin interferes with the synthesis of the bacterial cell wall peptidoglycan. It acts through the inhibition of biosynthesis of cell-wall peptidoglycan, rendering the cell wall osmotically unstable. It is part of the penicillin and beta lactam family of antibacterial drugs.
| Trade Name | Blueshell Procaine Benzylpenicillin |
| Generic | Procaine Benzylpenicillin + Benzylpenicillin |
| Weight | Mega |
| Type | Injection |
| Therapeutic Class | |
| Manufacturer | Shandong Xier Kangtai Pharm Co Ltd |
| Available Country | China, Nigeria |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Benzylpenicillin is a penicillin used for the treatment of infections caused by gram-positive cocci, in particular streptococcal infections. This form of penicillin is typically used in intravenous or long-acting injectable formulations due to poor oral absorption.
For use in the treatment of severe infections caused by penicillin G-susceptible microorganisms when rapid and high penicillin levels are required such as in the treatment of septicemia, meningitis, pericarditis, endocarditis and severe pneumonia.
Procaine benzylpenicillin is a local anesthetic and antibiotic combination for intramuscular injection to treat a variety of bacterial infections while reducing pain from a deep intramuscular injection.
For the treatment of a number of bacterial infections such as syphilis, anthrax, mouth infections, pneumonia and diphtheria.
Blueshell Procaine Benzylpenicillin is also used to associated treatment for these conditions: Actinomycosis, Acute Rheumatic Fever, Anthrax, Bloodstream Infections, Botulism, Diphtheria, Empyema, Endocarditis, Endocarditis caused by Erysipelothrix infections, Fusospirochetosis, Gas Gangrene, Gonococcal infections, Gram-Negative Bacterial Infections, Haverhill fever, Listeria infection, Meningitis, Meningococcal Meningitis, Pasteurella infections, Pericarditis, Pneumonia, Rat-bite fever, Syphilis, TetanusAnthrax, Bacterial Infections, Diphtheria, Endocarditis, Subacute Bacterial, Erysipelas, Erysipelas caused by susceptible streptococci, Erysipeloid, Necrotizing ulcerative gingivostomatitis, Non-venereal endemic syphilis, Otitis Media caused by susceptible pneumococci, Pinta, Pneumonia caused by susceptible pneumococci, Primary Syphilis, Rat-bite fever, Respiratory Tract Infections (RTI), Scarlet Fever, Scarlet Fever caused by susceptible streptococci, Secondary Syphilis, Skin Structures and Soft Tissue Infections caused by susceptible streptococci, Skin and Subcutaneous Tissue Bacterial Infections, Tertiary syphilis, Upper Respiratory Tract Infection caused by susceptible streptococci, Yaws
How Blueshell Procaine Benzylpenicillin works
By binding to specific penicillin-binding proteins (PBPs) located inside the bacterial cell wall, penicillin G inhibits the third and last stage of bacterial cell wall synthesis. Cell lysis is then mediated by bacterial cell wall autolytic enzymes such as autolysins; it is possible that penicillin G interferes with an autolysin inhibitor.
Procaine benzylpenicillin is hydrolyzed into penicillin G once it is released from the injection site. Penicillin G attaches to the penicillin-binding proteins on bacterial cell wall and inhibit the transpeptidation enzyme that crosslinks the peptide chains attached to the backbone of the peptidoglycan. The final bactericidal event involves the inactivation of an inhibitor of autolytic enzymes in the cell wall, leading to lysis of the bacterium .
Toxicity
Oral LD50 in rat is 8900 mg/kg . Neurological adverse reactions, including convulsions, may occur with the attainment of high CSF levels of beta-lactams. Neutropenia can occur if high doses are administered consistently for over 2 weeks.
Procaine benzylpenicillin is associated with the pain at the injection site, blood clotting problems, and seizures. Treatment targeted against syphilis is often associated with Jarisch-Herxheimer reaction. The main unwanted effects are hypersensitivity reactions caused by the degradation products of penicillin, which combine with host protein and become antigenic. Other common adverse effects include skin rashes, fever and delayed serum sickness. Rare but fatal anaphylactic shock may occur. Oral LD50 values in mouse and rat are > 2000 mg/kg. Overdosage can cause convulsions, paralysis and even death. Emesis and gastric lavage may be of value if begun within a few hours of injection. Excessive blood concentrations can be lowered by haemodialysis .
Volume of Distribution
0.53–0.67 L/kg in adults with normal renal function
The drug is distributed throughout the body tissues in widely varying amounts and spinal fluid to a lesser degree. Highest levels are found in the kidneys with lesser amounts in the liver, skin, and intestines. It displays low solubility thus results in blood serum levels much lower but more prolonged than other parenteral penicillins.
Elimination Route
Rapidly absorbed following both intramuscular and subcutaneous injection. Initial blood levels following parenteral administration are high but transient. Oral absorption in fasting, healthy humans is only about 15-30% as it is very susceptible to acid-catalyzed hydrolysis.
After intramuscular injection, it dissolves slowly at the site of injection, giving a plateau type of blood level at about 4 hours which falls slowly over a period of the next 15 to 20 hours.
Half Life
In adults with normal renal function is reportedly 0.4–0.9 hours
Intramuscular injection of benzylpenicillin has a plasma half-life of 30 minutes .
Clearance
560ml/min in healthy humans
Elimination Route
Penicillin G is eliminated by the kidneys. Nonrenal clearance includes hepatic metabolism and, to a lesser extent, biliary excretion.
The drug is rapidly and predominantly cleared via renal elimination, with 90% being through tubular secretion. Approximately 60 -90 % of a dose of parenteral penicillin G is excreted in the urine within 24 to 36 hours.
Innovators Monograph
You find simplified version here Blueshell Procaine Benzylpenicillin
