Iclaprim

At Iclaprim it is a medical drug that is currently (as of 2017) still in the approval process. It is manufactured by the Swiss pharmaceutical and biopharmaceutical company ARPIDA, based in Reinach, and is intended to be used in the treatment of complicated skin and skin structure infections. From a pharmacological and medical point of view, it is an antibiotic whose mechanism of action originates from an inhibition of the bacterial dihydrofolate reductase.

What is Iclaprim?

Iclaprim is to be used in the near future to treat various skin infections and skin structure. The active ingredient is manufactured by the Swiss pharmaceutical company APRIDA, which also holds the patents on the substance. The antibiotic is still in the approval phase in the European Union (EU) and the United States of America (USA).

The US Food and Drug Administration (FDA) refused fast-track approval in an urgent procedure in 2009 and referred to the regular approval that APRIDA is currently striving for. Iclaprim is therefore not yet available on the drug markets. If approval is granted, the drug may only be given to patients after a doctor's prescription. It is also common to order compulsory pharmacies for comparable drugs.

In chemistry and pharmacology, Iclaprim is described by the empirical formula C 19 - H 22 - N 4 - O 3. The empirical formula C 20 - H 26 - N 4 - O 6 - S is used for Iclaprim mesilate, which is also common. This corresponds to a moral mass of 354.4 g / mol or 450.51 g / mol. The mechanism of action of Iclaprim is based on an inhibition of the bacterial dihydrofolate reductase. The antibiotic is seen as a beacon of hope for the treatment of diseases caused by resistant strains of pathogens.

Pharmacological effect on the body and organs

Due to its pharmacological properties and the mechanism of action used, Iclaprim is an antibiotic. It is assigned to the active substance group of the diaminopyrimidines, which also includes the drugs pyrimethamine, copexil and aminopterin. Typical of this group is the presence of an organic compound consisting of a base and two amino groups on a pyrimidine ring. The empirical formula of the diaminopyrimidines therefore always shows carbon (C), hydrogen (H) and nitrogen (N).

Iclaprim is considered to be an effective inhibitor of dihydrofolate reductase in a bacteria. There are therefore similarities with trimethoprim, which also belongs to the group of diaminopyrimidines. The special feature of Iclaprim is that it is also active on numerous strains of pathogens on which trimethoprim is no longer effective.

In medical studies carried out outside the living organism (in vitro) it has been proven that Iclaprim can be used against a large number of gram-positive bacteria. Those pathogens that turn blue when a differential staining process (Gram staining) is carried out are gram-positive. Iclaprim is therefore regarded as a beacon of hope for the treatment of skin diseases that are triggered by resistant bacteria.

Medical application & use for treatment & prevention

Iclaprim is said to be used to fight infections of the skin and the structure of the skin. In the clinical studies carried out so far, the administration was either orally or intravenously, so that these forms of administration will probably also be indicated in practice.

When taken orally in the form of film-coated tablets, the bioavailability of the antibiotic is approx. 40%. A dose of 160 mg is recommended for average patients. A plasma level of up to 0.5 µg / ml can be achieved here.

If Iclaprim is administered intravenously, the recommended dose is between 0.4 and 0.8 mg per body weight. Plasma concentrations of up to 0.87 µg / ml are possible here. The plasma half-life is set at two hours.

Risks & side effects

As with all drugs, undesirable side effects can occur after taking Iclaprim. According to the current state of knowledge, numerous comparisons can be made with the drug linezolid. The most frequent side effects therefore include gastrointestinal complaints, which can manifest themselves as diarrhea, loose stools, vomiting, abdominal pain, constipation (constipation), nausea or nausea. Headache and loss of taste are also potential side effects.

Changes in blood values ​​are also possible. A decrease in white blood cells, a lack of neutrophils or platelets can also occur. Furthermore, fever and skin reactions are to be expected. The latter manifest themselves in particular through itching, redness and rashes.

In addition, Iclaprim must not be used if there is a medical contraindication (indication). In medicine, this refers to a circumstance that makes the use of a certain preparation appear unreasonable, because incalculable risks and side effects are likely. This is especially the case if an intolerance to the active ingredient is known. In the case of allergies to diaminopyrimidines, particular caution must be exercised so that a careful weighing of the opportunities and benefits must be carried out.

In addition, attention should be paid to interactions with other medicinal substances. The attending physician must therefore be informed at regular intervals about all preparations that have been taken. In this way, risks can be minimized and made more predictable.