Fortified Procaine Benzylpenicillin Injection 4 Mega
Fortified Procaine Benzylpenicillin Injection 4 Mega 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.
A local anesthetic of the ester type that has a slow onset and a short duration of action. It is mainly used for infiltration anesthesia, peripheral nerve block, and spinal block. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1016). Procaine has also been investigated as an oral entry inhibitor in treatment-experienced HIV patients .
Procaine is an anesthetic agent indicated for production of local or regional anesthesia, particularly for oral surgery. Procaine (like cocaine) has the advantage of constricting blood vessels which reduces bleeding, unlike other local anesthetics like lidocaine. Procaine is an ester anesthetic. It is metabolized in the plasma by the enzyme pseudocholinesterase through hydrolysis into para-aminobenzoic acid (PABA), which is then excreted by the kidneys into the urine.
| Trade Name | Fortified Procaine Benzylpenicillin Injection 4 Mega |
| Generic | Procaine + Benzylpenicillin |
| Weight | 3,000,000iu, 100,000iu |
| Type | Powder For Injection |
| Therapeutic Class | |
| Manufacturer | North China 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 is a local anesthetic used for anesthesia, peripheral nerve block, and spinal nerve block.
Used as a local anesthetic primarily in oral surgery
Fortified Procaine Benzylpenicillin Injection 4 Mega 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, TetanusOtalgia
How Fortified Procaine Benzylpenicillin Injection 4 Mega 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 acts mainly by inhibiting sodium influx through voltage gated sodium channels in the neuronal cell membrane of peripheral nerves. When the influx of sodium is interrupted, an action potential cannot arise and signal conduction is thus inhibited. The receptor site is thought to be located at the cytoplasmic (inner) portion of the sodium channel. Procaine has also been shown to bind or antagonize the function of N-methyl-D-aspartate (NMDA) receptors as well as nicotinic acetylcholine receptors and the serotonin receptor-ion channel complex.
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.
Volume of Distribution
0.53–0.67 L/kg in adults with normal renal function
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.
Half Life
In adults with normal renal function is reportedly 0.4–0.9 hours
7.7 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.
With normal kidney function, the drug is excreted rapidly by tubular excretion.
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