Penicillins (see table: penicillins) are ?-lactam antibiotics, which are bactericidal and whose exact mechanism of action is unknown. Presumably, there is an activation of autolytic enzymes that leads to destruction of the bacterial cell wall of certain pathogens. Penicillins drug administration route penicillin G-like drugs penicillin G oral or parenteral penicillin G benzathine penicillin G procaine administration Parenteral administration Parenteral penicillin V Oral Ampicillin similar medicines ampicillin oral or parenteral ampicillin plus sulbactam Parenteral administration Amoxicillin Oral amoxicillin and clavulanate oral penicillinase-resistant penicillins dicloxacillin Oral nafcillin oral or parenteral oxacillin oral or parenteral broad-spectrum penicillins (Pseudomonas effective) Carbenicillin Oral Parenteral administration Piperacillin Tazobactam Piperacillin plus Parenteral administration Ticarcillin Parenteral administration ticarcillin and clavulanate Parenteral administration resistance Some pathogens form ?-lactamases that inactivate ?-lactam antibiotics; However, this effect can be blocked by addition of a ?-lactamase inhibitor (clavulanic acid, sulbactam or tazobactam). Nevertheless, the available ?-lactamase inhibitors do not inhibit amp C-?-lactamases, which are often of Enterobacter, Serratia, P. aeruginosa, Citrobacter, Providencia and Morganella spp. or are formed by Pseudomonas aeruginosa, and these drugs can only partially extended spectrum ?-lactamase (ESBL), which is formed by some Klebsiella pneumoniae, Escherichia coli and other Enterobacteriaceae, inhibit. Carbapenemases that can inactivate all ?-lactam antibiotics in Klebsiella sp, other Enterobacteriaceae, P. aeruginosa, and Acinetobacter sp become increasingly common. Currently no carbapenemase inhibitors are available, although some are being developed. Pharmacology The absorption of amoxicillin not interfere with the intake of food, but should penicillin G 1 hour before or 2 hours after a meal are added. Amoxicillin has largely replaced ampicillin following oral administration due to its better absorption and less frequent gastrointestinal side effects, although it can be given less frequently. Penicillins are rapidly distributed in the extracellular fluid of most tissues, especially in inflammation. All penicillins except nafcillin are excreted in the urine and reach high levels in the urine. Parenteral penicillin G is rapidly excreted (serum half-life 0.5 h), except for depot forms (benzathine or procaine penicillin salts), these embodiments are only for deep i.m. Injection provided and create a tissue depot, takes its absorption many hours to days. Benzathine penicillin reaches its peak levels more slowly and the effect lasts longer than with procaine penicillin. Indications penicillin G-like drugs penicillin G-like drugs (including penicillin V) are primarily used against gram positive bacteria Some Gram negative cocci (eg. B. meningococcal) A minority of gram-negative bacteria are also prone to large parenteral doses of penicillin G. most staphylococci, the most gonorrhoeae Neisseria and many anaerobic gram-negative rods and about 30% of Haemophilus influenzae are resistant. Penicillin G is the antibiotic of choice in syphilis, in certain Clostridial infections and, together with gentamicin at a endocarditis, which is caused by sensitive enterococci. Benzathine penicillin G is available as a pure benzathine penicillin, a mixture of equal amounts of benzathine and procaine penicillin G and a mixture of 0.9 million units of benzathine and 0.3 million units of procaine penicillin G. Of the three products is recommended only pure benzathine penicillin for treatment of syphilis and for the prevention of rheumatic fever. Whether the mixture of equal amounts is effective in treating syphilis is unknown. Bicillin L-A and bicillin C-R are indicated for the treatment of urinary tract infections and skin and soft tissue infections caused by susceptible werden.Amoxicillin streptococci and ampicillin Arzeniemittel These are particularly effective against enterococci Certain gram-negative rods such. B. non-?-lactamase-producing H. influenzae, E. coli and Proteus mirabilis; Salmonella sp and Shigella sp. The addition of a ?-lactamase inhibitor allows use against methicillin-sensitive staphylococcus, H. influenzae, Moraxella catarrhalis, Bacteroides sp, E. coli and K. pneumoniae. Ampicillin is especially indicated for infections that are typically caused by gram-negative bacteria. HWI meningococcal meningitis Biliary sepsis respiratory infections Listeria meningitis enterococcal infections Some types of typhus and typhoid carriers penicillinase-resistant penicillins These drugs are used primarily in Penicillinasebildendem methicillin-sensitive Staphylococcus aureus, these drugs also act in some infections caused by Streptococcus pneumoniae, Group A streptococci and methicillin -sensitive coagulase Staphylokokken.Breitspektrumpenicillin (Pseudomonas effective) These drugs act to ampicillin-susceptible bacteria, some strains of Enterobacter and Serratia spp. Many strains of P. aeruginosa ticarcillin is less effective against enterococci as piperacillin. The addition of a ?-lactamase inhibitor enhanced efficacy against ?-lactamase-producing methicillin-sensitive S. aureus, E. coli, K. pneumoniae, H. influenzae and gram-negative anaerobic rods, but not against gram-negative rods, a ? ampC lactamase form, and they can only partially inhibit ESBL produced by some K. pneumoniae, E. coli and other enteric bacteria. Broad-spectrum penicillins have a synergistic effect on with aminoglycosides and are usually used together with them to treat P. aeruginosa infections Contraindications penicillins are common in patients who have had severe allergic reactions to these contraindicated. Use during pregnancy and lactation penicillins are in pregnancy category B (animal studies show no risk, human experience is incomplete or animal studies show risk, but human studies do not). Penicillins go about in small amounts in breast milk. Their use during lactation is possible. Side effects Side effects include hypersensitivity reactions with skin rashes (most common) Other side effects that occur less frequently. Hypersensitivity The most common side effects are hypersensitivity reactions: Immediate reactions: anaphylaxis (which can lead within minutes of death), urticaria and angioedema (10,000 injections at about 1 to 5), death (about 0.3 / 10,000 injections) , Delayed reactions (up to 8% of patients): serum sickness, rashes (. For example, macular, papulär, morbilliform) and a Exfoliativdermatitis, (usually after 7 to 10 days of therapy). Most patients who report of an allergic reaction to penicillin, but do not respond to subsequent exposure to penicillin. Despite the overall low risk occurs in patients with a previous allergic reaction about 10 times more likely to cause an allergic reaction. Many patients report adverse reactions to penicillin, which is not really based on allergic reactions (eg., Gastrointestinal side effects, non-specific symptoms). If patients have a vague or contradictory history in relation to a penicillin allergy and alternative antibiotics are not effective or can not be given for other reasons, skin tests can be performed (drug hypersensitivity: skin test). In patients with a positive skin test, desensitization may be attempted if there is no alternative to a penicillin-like drug. However, no ?-lactam antibiotic in patients with previous anaphylactic reactions to penicillin may (including with skin tests) be given except in very rare cases when no substitute is available. In such cases, precautions and desensitization are required (drug hypersensitivity: desensitization) .Hautausschläge rashes are common in ampicillin and amoxicillin before with other penicillins. Patients with infectious mononucleosis often develop a non-allergic rash, typically maculopapular, which can penicillins usually between the 4th and the 7th day of treatment side effects beginnt.Andere also a cause toxic central nervous system symptoms (eg. As seizures), at high doses, especially in patients with renal insufficiency. Nephritis C. difficile-induced diarrhea (pseudomembranous Kolitis- Clostridium difficile-induced diarrhea) Coombs-positive hemolytic anemia leukopenia thrombocytopenia leukopenia A seems to occur at nafcillin most often. Each penicillin can at very high i.v. interfere with doses of platelet function and cause bleeding, but Ticarcillin is the most common cause, particularly in patients with renal insufficiency. Other side effects include. a. Pain at the i.m. Injection site, thrombophlebitis (if the same position is repeatedly used for i.v. injection), and gastrointestinal side effects in oral applications. Rarely can occur because of irritation of the tongue surface and keratinization of the superficial layers of a black hairy tongue, usually this happens when administered orally. Ticarcillin may lead to sodium overload in high doses, because it is a disodium salt. Ticarcillin can also cause hypokalemic metabolic alkalosis because the large amounts of nonabsorbable anions that are prevalent in the distal tubules that change H + ion excretion, which secondarily leads to a K + loss. except Nafcilllin all penicillins achieve considerations for dosing Because high urine levels, must be a dose reduction in patients with severe renal impairment. Probenecid inhibits the renal tubular secretion of many penicillins and thereby increases their serum levels. Sometimes it is administered simultaneously to achieve high blood levels.