Penicillin preparation

Table 6. Modified Penicillins Prepared Using IPNS...

Serum potassium concentration Is Increased by the concurrent administration of Intravenous potassium penicillin 6. The penicillin preparation contains 1.7 mmol of potassium per million units. Thus, a patient receiving 10 million units of the antibiotic receives 17 mmol (m q.) of potassium. 

The freeze drying of antibiotics and blood serum have largely represented the beginning of industrial lyophilization. Neumann [3.34] wrote in 1952 The (freeze drying) temperature for the older, not well purified Penicillin preparations had to be kept surprisingly low. It could not exceed -25 °C or -40 °C and later on Today Peniciilin is manufactured as crystals without the need of freeze drying . 

A disadvantage of ampicillin and amoxicillin is that they are inactivated by penicillinase, and more strains of H. influenzae are becoming resistant through penicillinase (p-lactamase) production. The addition of a p-lactamase inhibitor such as clavulanate (clavulanic acid) or sulbactam to a penicillin preparation can protect the penicillin component because these chemicals irreversibly inactivate bacterial P-lactamases. 

Saputo V, Bruni G. La sindrome di Nicolau da preparati di penidUina anaUsi della letteratura aUa ricerca di potenziah fattori di rischio. [Nicolau syndrome caused by penicillin preparations review of the literature in search for potential risk factors.] Pediatr Med Chir 1998 20(2) 105-23. 

Hoigne R. Akute Nebemeaktionen auf Penicillinpraparate. [Acute side-reactions to penicillin preparations.] Acta Med Scand 1962 171 201-8. 

Crystalline penicillin prepared synthetically was obtained for the first time by Professor du Vigneaud and collaborators (6). One of the major problems in their work was that of isolating crystalline active material from a reaction mixture originally containing approximately 0.1% of active material. Previous to, their work, extensive attempts by several laboratories to isolate or even to increase the activity had been so discouraging that many workers considered the activity to be due to some closely related compound. However,... 

Iodometric methods for the assay of penicillins were first described by Alicino 9 in 1946. Penicillin is inert to iodine in neutral aqueous solution. But after hydrolysis with alkali or penicillinase, the resulting penicilloic acid (III) consumes from 6 to 9 equivalents per mole, depending on the conditions used. The difference in consumption of iodine by penicillin preparations before and after alkaline hydrolysis was found proportional to the quantity of the drug. Alicino found penicillin G consumed 8.97 equivalents of iodine per mole under the conditions used in his assay procedure. He later demonstrated 0 other deactivated penicillins, including phenoxymethyl penicillin, consume nine equivalents of iodine per mole while 6-amino-penicillanic acid consumes only eight equivalents of iodine per mole. 

Nitrofuran preparations Ointments Parenteral solutions Penicillin preparations Pharmaceuticals Pills, pharmaceutical Pituitary gland pharmaceutical preparations... 

Clavulanic acid is a chemical similar in structure to penicillin, which acts as a substrate for penicillinase, thus inhibiting its action on penicillin. This agent is added to penicillin preparations to decrease the manifestation of bacterial resistance. 

U. Forsman and A. Karlsson, Polarographic Determination of Penicilloic Acid in Penicillin Preparations with a Flow Injection System. Anal. Chim. Acta, 139 (1982) 133. 

This is a penicillin preparation, not a sulfa medication or iodine. 

In summary, it seems firmly established that penicillin polymers, and especially polymers formed from aminopenicillins, exhibit a strong penicilloyl-specific antigenicity and it is likely that they may play a part in the elicitation of some clinical allergic reactions to penicillin preparations. The question of immunogenicity of penicillin polymers is still to be fully resolved. 

Because of the immunologic effects of penicillin polymers which are strongly supposed to be of clinical importance, their presence in clinically used penicillin preparations should be controlled and kept at the lowest possible level. 

An additional source of preformed antigenic penicilloyl-specific substances in penicillin preparations may be penicilloyl-carbohydrate conjugates. 

Several therapeutically used penicillin preparations contain carbohydrates. Thus, penicillins are commonly infused in glucose or fructose solutions, sucrose is a common ingredient of penicillin syrups and benzylpenicillin procaine suspensions may contain carboxymethylcellulose as an additive. Because of the antigenic and potentially allergenic effect of penicilloyl-carbohydrate conjugates, their presence in penicillin preparations must be avoided. Information about the kinetics of reaction of penicillins with carbohydrate and factors affecting the reaction rate have recently been reported. 

Penicillenic acids are readily formed in aqueous solutions of penicillins by an intramolecular rearrangement, as described in Sect. C.I.l.a, and they are present in small amounts in almost all penicillin preparations (e.g., Meulenhoff 1965 Seitzinger 1973 Brandt et al. 1974). The rate of formation of penicillenic acid increases strongly with decreasing pH of the penicillin solutions and it shows a high dependence on the inductive effect of the side chain structure of the penicillins (Schwartz and Wu 1966). The compounds are highly reactive with proteins and... 

Munro AC, Dewdney JM, Smith H, Wheeler AW (1976) Antigenic properties of polymers formed by j9-lactam antibiotics. Int Arch Allergy Appl Immunol 50 192-205 Muranaka M, Igarashi H, Koizumi K, Okumura H, Takeda K, Suzuki S (1974) Elicitation of homologous passive cutaneous anaphylactic reactions by a penicillin preparation. J Allergy Clin Immunol 54 329-338... 

Kristofferson A, Ahlstedt A, Pettersson E, Svaerd PO (1977) Antigens in penicillin allergy. I. A radioimmunoassay for detection of penicilloylated protein contaminants in penicillin preparations. Int Arch Allergy Appl Immunol 55 13 Lee WY, Sehon AH (1975) Suppression of reaginic antibody formation II. The use of adoptive transfer system for the study of immunological unresponsiveness. J Immunol 114 837... 

The chemical routes to the formation of the penicilloyl determinant can be multiple and have been the subject of some controversies. It has been claimed that the main source of immunogenic penicilloyl antigens leading to penicillin sensitization in therapy is the presence of penicilloylated protein impurities in most penicillin preparations. This topic is discussed extensively in Sect. 1.9. 

The immunological behavior of penicillin preparations may be markedly influenced by the presence of dimers, oligomers, and polymers in the penicillin preparations. It should be distinguished whether we are dealing with polymerization by internal rearrangement of the molecule or interaction between penicillin molecules carrying a free amino group, such as ampicillin. 

Not to be forgotten as possibly involved are macromolecular constituents of some penicillin preparations, such as carboxymethylcellulose, which may function as multivalent carriers (Schneu)er et al. 1971) and have been implicated in reactions to penicillins in cattle. 

Knudsen ET, Dewdney JM, Trafford JAP (1970) Reduction in incidence of ampicillin rash by purification of ampicillin. Br Med J 1 469 Koizumi K, Suzuki S, Fukuba S, Tadokoro K, Hirai K, Muranaka K (1980) Antigenicity of semisynthetic penicillin preparations to evoke systemic anaphylactic reactions in animal models. Allergy 35 657... 

Procaine penicillin preparations may be determined by the spectro-photometric method described by Stock (see above) but because of its low solubility in w ater, methanol is used as the extracting solvent. Procaine absorbs strongly in the ultra-violet and exhibits a maximum at 292 m/. The absorption at 322 m// (the maximum for penicillenic acid) is still significant and for pure procaine penicillin the irrelevant absorption amounts to 23 per cent of the total. I low ever, if the absorption is measured at 322 m/ both before and after the heating period, then the increase is entirely due to the penicillin present. 

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