Beepen-VK (Penicillin V Potassium) - Description and Clinical Pharmacology

DESCRIPTION

Beepen-VK (penicillin V potassium) is the potassium salt of penicillin V. Chemically it is 4-Thia-1-azabicyclo[3.2.0]-heptane-2-carboxylic acid, 3,3-dimethyl-7-oxo-6-[(phenoxy-acetyl)aminol-, monopotassium salt, [2S-(2α,5α,6β)]-, and can be represented structurally as:

The oral solutions contain in each 5 mL (teaspoonful) 125 mg or 250 mg of penicillin V activity, respectively. The tablets contain penicillin V potassium equivalent to 250 mg or 500 mg (400,000 or 800,000 units) penicillin V, respectively. The oral solution, 125 mg/5 mL, contains 0.33 mEq of sodium, and the oral solution, 250 mg/5 mL, contains 0.63 mEq of sodium.

Inactive ingredients: Oral solutions: Citric acid, flavorings, saccharin sodium, sodium benzoate, sodium chloride, sodium citrate, sucrose and xanthan. 125 mg contains FD&C Yellow No. 10 and FD&C Red No. 40. 250 mg contains FD&C Blue No. 1 and FD&C Red No. 3. Tablets: Colloidal silicon dioxide, lactose, magnesium stearate, microcrystalline cellulose and stearic acid.

CLINICAL PHARMACOLOGY

Penicillin V has the distinct advantage over penicillin G in resistance to inactivation by gastric acid. It may be given with meals; however, blood levels are slightly higher when the drug is given on an empty stomach. Average blood levels are 2 to 5 times higher than the levels following the same dose of oral penicillin G and also show much less individual variation. Once absorbed, penicillin V is about 80% bound to serum protein. Tissue levels are highest in the kidney, with lesser amounts in the liver, skin and intestines. Small amounts are found in all other body tissues and the cerebrospinal fluid. The drug is excreted as rapidly as it is absorbed in individuals with normal renal function; however, recovery of the drug from the urine indicates that only about 24% of the dose is absorbed. In neonates, young infants and individuals with impaired renal function, excretion is considerably delayed.

MICROBIOLOGY

Penicillin V exerts a bactericidal action against penicillin-susceptible microorganisms during the stage of active multiplication. It acts through the inhibition of biosynthesis of cell wall mucopeptide. Penicillin V is not active against the penicillinase-producing bacteria, which include many strains of staphylococci. While in vitro studies have demonstrated the susceptibility of most strains of the following organisms, clinical efficacy for infections other than those included in the INDICATIONS AND USAGE section has not been documented. This drug exerts in vitro activity against staphylococci (except penicillinase-producing strains), streptococci (Groups A, C, G, H, L and M) and pneumococci. Other organisms susceptible in vitro to penicillin V are Corynebacterium diphtheriae, Bacillus anthracis, Clostridia, Actinomyces bovis, Streptobacilus moniloformis, Listeria monocytogenes, Leptospira and Neisseria gonorrhoeae. Treponema pallidum is extremely susceptible.