WHAT IT’S USED FOR

Penicillin (UK: Penicillin or PCN) refers to a group of β-lactam antibiotic used in the treatment of bacterial infections caused by susceptible, usually Gram positif.Madigan, MT. Brock Biology of Microorganisms (edition 12th Edition). San Francisco: Pearson Benjamin Cummings. p. p. 795. ISBN 9780321536150. Penicillin works by inhibiting bacterial cell wall formation, by inhibiting acid N-asetilmuramat Combined non-essential to the structure Mukopeptida usually makes cells become rigid and strong. This way of working also means that penicillin would only actively working on the unit pathogen growing actively. The name "penicillin" can also be used to refer to a specific member of the penicillin group. All have basic Penam penicillin, which has the molecular formula R-C9H11N2O4S, where R is a variable side chain.

The discovery penislin always associated with Scottish scientist, Alexander Fleming in 1929, even though many other scientists have noted the antibacterial effects before Fleming.

Fleming, in his laboratory at St. Mary's Hospital (now the one teaching hospital in London), noticed a halo of inhibition (clear zone) on the growth of the bacteria Staphylococcus plate culture. Fleming concluded that the resistance is due to a substance inhibiting bacterial growth and destroy. He grew a pure culture and discovered what became known as Penicillium Penicillium chrysogenum. Fleming coined the term "penicillin" to describe the filtrate of a culture of the Penicillium mold.

Although in these early stages, penicillin was found to be effective against Gram-positive and Gram-negative ineffective and fungi. Fleming optimism that penicillin would be a useful disinfectant, high potential with a low level of toxicity compared to antiseptics period.

In subsequent experiments, Fleming was convinced that penicillin could not last long in the human body to kill pathogenic bacteria. He stopped studying penicillin after 1931, but trying to start it again in 1934.

In 1939, Australian scientist Howard Walter Florey and a team of researchers at the University of Oxford made a significant progress in showing the in vivo bactericidal action of penicillin. They failed in the experiment due to insufficient penicillin, but they proved harmless penislin and work in mice. Several experiments carried out in Oxford penicillin. In 1942, John Bumstead and Orvan Hess became the first expert successfully cure patients with penicillin.

When World War II, penicillin was instrumental in suppressing the number of deaths due to infection caused by an open wound that did not receive treatment, which is in a similar situation can lead to gangrene and even death, 12-15% saving lives. Availability of penicillin is still very limited because of the difficulty to produce them en masse, and rapid renal residual penicillin was not used by the body. At that time, the collection returned from the urine of patients penicillin is the usual procedure. Penicillin will be used again.

Reuse of penicillin is not the end of the road is good. This led researchers to look for a way to slow penicillin secretion. They hoped to find a molecule that could compete with penicillin for the organic acid transporter. Transportter's function in the secretion of penicillin, it is estimated that transporter will carry penicillin molecule inhibitors that will last longer in the body. An agent probenecid eventually proven to prevent. Probenecid will compete and inhibit the secretion of penicillin. Penislin finally able to work longer in the body. Techniques in mass production of penicillin was finally able to overcome.

Chemical structure of penicillin by Dorothy Crowfoot Hodgkin known in the early 1940s. This discovery makes penicillin can be made synthetically. A team from Oxford discovered a method of mass production of penicillin. The team, led by Howard Walter Florey, received the Nobel Prize in Medicine or Physiology in 1945. Penicillin has since become the banayak antibiotics used and is still used for some Gram-positive bacterial infections.

The development of penicillin

The narrow scope of activity of penicillin made the researcher looking for derivatives of penicillin that could treat more infections.

The first major development was ampicillin, which has a broader scope of activities than the original penicillin. The next development that can withstand produce penicillin beta-lactamase enzymes, including flucloxacillin, dicloxacillin and methicillin. This discovery is very important to fight bacterial species that have beta-lactamase, but can not resist strain methicillin-resistant Staphylococcus aureus.

Penicillin Piperacillin antipseudomal like Tisarsilin and useless against Gram-negative bacteria.

Mechanism of action

Β-lactam antibiotics work by inhibiting the formation of peptidoglycan in the cell wall. Beta-lactam be bound transpeptidase enzymes associated with bacterial peptidoglycan molecules, and this will weaken the bacterial cell wall as dividing. In other words, these antibiotics can cause cell rupture (cytolysis) when the bacteria tries to divide.

In Gram-positive bacterial cell wall that loss will be protoplasts, a Gram-negative sedangkam sferoplas. Protoplasts and sferoplas then be broken or lysis.

Clinical Function

The term "penicillin" is often used primarily to indicate benzylpenicillin.

Benzathine benzylpenicillin

Benzathine benzylpenicillin or benzathine penicillin, is slowly absorbed into the circulation, intramuscularly or injected in the muscles, and hydrolysed to benzylpenicillin in vivo. The drug is selected when low concentrations of benzylpenicillin are required, allowing prolonged antibiotic action over 2-4 weeks after a single IM dose.

Specific indications for benzathine penicillin:

• Prophylaxis of rheumatic fever

• Early or latent syphilis

Benzylpenicillin (penicillin G)

Benzylpenicillin or penicillin G is the gold standard penicillin. Penicillin G is typically given by mouth because it is unstable with hydrochloric acid in the stomach. Penicillin G is the first effective antibiotic clinically, discovered by Howard Florey and his colleagues in 1939

Specific indications for benzylpenicillin:

• Cellulite

• bacterial endocarditis

• Meningitis

• aspiration pneumonia, lung abscess

• Syphilis

• Septicaemia in children

Phenoxymethylpenicillin (penicillin V)

Phenoxymethylpenicillin, also known as penicillin V, is the active penicillin oral (taken by mouth). The drug is less active than benzylpenicillin. The drug is only appropriate in conditions of high tissue concentrations are not required.

Specific indications for phenoxymethylpenicillin:

• Infections due to Streptococcus pyogenes

ü  Tonsillitis

ü  Pharyngitis

ü  Skin Infections

• Prophylaxis of rheumatic fever

• moderate-to-severe gingivitis (with metronidazole)

Procaine benzylpenicillin

Procaine penicillin, procaine penicillin, is a combination of benzylpenicillin with the local anesthetic agent procaine. Intramuscular injection, it is slowly absorbed into the circulation and dihdrolisa to benzylpenicillin.

This combination is aimed at reducing the pain and discomfort associated with injections of penicillin that much into muscle. Perlakuakn is often used in veterinary medicine.

Specific indications for procaine penicillin:

• Syphilis

• respiratory tract infections

• Cellulitis

The drug is also used in anthrax.

Penicillin semi-sintetetik

Structural modifications to the side chain of the penicillin nucleus to enhance the ability of the drug, stabilizing beta-lactamase activity, and increase the scope of work.

Penicillin narrow scope

This group was developed to be effective against beta-lactamase produced by Staphylococcus aureus, and is known as an anti-staphylococcal penicillin.

Penicillin scope is being

This group was developed to improve llingkup work, such as amoxicillin.

• Amoxicillin

• Ampicillin

Spectrum Penicillins

This group was developed to increase efficacy against Gram-negative bacteria.

• Piperacillin

• Tisarsilin

• Azlosillin

• carbenicillin

Penicillin with β-lactamase inhibitors

Penicillin can be combined with beta-lactamase inhibitors to help fight the enzyme beta-lactamase.

Side effects

Adverse reaction

Adverse reactions are frequently (≥ 1% of patients) diarrhea, urticaria, nausea, and superinfection dri Candidiasis. Securities that are rare (0.1-1% of patients) were fever, vomiting, dermatitis, angioedema or pseudomembarnosus colitis. [5]

Allergy

Allergy to beta-lactam antibiotic may occur in 10% of patients. 0.01% may suffer from anaphylaxis.