Penicillin G Procaine King Actions
Description: Penicillin G Procaine King has a bactericidal action against gm+ve bacteria, gm-ve cocci, some other gm-ve bacteria, spirochetes and actinomycetes. It inhibits final cross-linking stage of peptidoglycan production through binding and inactivation of transpeptidases on the inner surface of the bacterial cell membrane thus inhibiting bacterial cell wall synthesis. It is inhibited by penicillinase and other β-lactamases.
Absorption: Rapidly appears in blood after IM inj. Inactivated fairly rapidly by gastric acid and up to approx 30% is absorbed. Absorption is reduced by the presence of food. Time to peak plasma concentration: 15-30 min (IM); approx 1 hr (oral/IV).
Distribution: Widely distributed. Crosses the placenta and enters breast milk (small amounts). Volume of distribution: 0.53-0.67 L/kg. Plasma protein binding: Approx 60%.
Metabolism: Undergoes limited hepatic metabolism to penicilloic acid.
Excretion: Via urine (58-85% as unchanged drug) and bile (small amounts). Plasma half-life: Approx 30 min.
Should be taken on an empty stomach. Take w/ a full glass of water on an empty stomach 1 hr before or 2 hr after meals. Do not take acidic beverages w/in 1 hr of a dose.
Penicillin G Procaine King binds to penicillin-binding protein 1A (PBP-1A) located inside the bacterial cell well. Penicillins acylate the penicillin-sensitive transpeptidase C-terminal domain by opening the lactam ring. This inactivation of the enzyme prevents the formation of a cross-link of two linear peptidoglycan strands, inhibiting 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 amoxicllin interferes with an autolysin inhibitor.
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Information checked by Dr. Sachin Kumar, MD Pharmacology