Iclaprim is a medical drug that is currently (as of 2017) still in the approval process. It is manufactured by ARPIDA, a Swiss pharmaceutical and biopharmaceutical company based in Reinach, and is intended for the treatment of complicated skin and skin structure infections. From a pharmacological-medical point of view, it is an antibiotic whose mechanism of action stems from an inhibition of bacterial dihydrofolate reductase.
What is iclaprim?
Iclaprim is expected to be used in the near future to treat various infections of the skin as well as 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). In 2009, the U.S. Food and Drug Administration (FDA) denied fast-track approval and referred the case to the full approval currently being sought by APRIDA. Iclaprim is therefore not yet available on the drug markets. If approval is granted, the drug may only be dispensed to patients after a doctor’s prescription has been obtained. Mandatory pharmacy orders are also common for comparable drugs. In chemistry and pharmacology, Iclaprim is described by the molecular formula C 19 – H 22 – N 4 – O 3. For Iclaprim mesilate, which is also commonly used, the molecular formula C 20 – H 26 – N 4 – O 6 – S is used. This corresponds to a moral mass of 354.4 g/mol and 450.51 g/mol, respectively. The mechanism of action of Iclaprim is based on inhibition of bacterial dihydrofolate reductase. The antibiotic is considered a hopeful treatment for diseases caused by resistant strains of pathogens.
Pharmacologic effects on the body and organs
Due to its pharmacological properties as well as the mechanism of action applied, Iclaprim is an antibiotic. It is classified as belonging to the diaminopyrimidine group of drugs, which also includes the drugs pyrimethamine, copexil, and aminopterin. Typical for this group is the presence of an organic compound consisting of a base and two amino groups on a pyrimidine ring. Therefore, the molecular formula of diaminopyrimidines always has carbon (C), hydrogen (H) and nitrogen (N). Iclaprim is considered to be an effective inhibitor of the dihydrofolate reductase of a bacterium. 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. Medical studies conducted outside the living organism (in vitro) have demonstrated that Iclaprim can be used against a wide range of Gram-positive bacteria. Gram-positive bacteria are those pathogens that turn blue when a differential staining procedure (Gram stain) is performed. Iclaprim is thus considered a hopeful treatment for diseases of the skin caused by resistant bacteria.
Medical application and use for treatment and prevention.
Iclaprim is intended for use to combat infections of the skin and skin structure. In clinical trials conducted to date, administration has been either oral or intravenous, so these routes of administration are likely to be indicated in practice. When taken orally in the form of film-coated tablets, the bioavailability of the antibiotic is approximately 40%. A dose of 160 mg is recommended for average patients. In this case, a plasma level of up to 0.5 µg/ml can be achieved. If Iclaprim is administered intravenously, the recommended dosage is between 0.4 and 0.8 mg per body weight. Plasma concentrations of up to 0.87 µg/ml are possible. The plasma half-life is set at two hours.
Risks and side effects
As with all drugs, adverse side effects may occur after taking Iclaprim. According to current knowledge, numerous comparisons can be made to the drug linezolid. Therefore, the most common side effects include gastrointestinal symptoms, which may be diarrhea (diarrhea), soft stools, vomiting, abdominal pain, constipation (constipation), nausea, or nausea. Also, headaches and decreases in taste ability are potential side effects.In addition, changes in blood values are possible. A decrease in white blood cells, a lack of neutrophils or platelets may also occur. Furthermore, fever and skin reactions are to be expected. The latter are manifested in particular by 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 particular preparation appear unreasonable because of the likelihood of unmanageable risks and side effects. This is especially the case if an intolerance to the active ingredient is known. Special caution must be exercised in the case of allergies to diaminopyrimidines, so that a careful weighing of opportunities and benefits must be carried out. In addition, attention must be paid to interactions with other drugs. The attending physician must therefore be informed at regular intervals about all preparations taken. In this way, risks can be minimized and made more calculable.
