Tebipenem is a medicinal agent that belongs to the group of carbapenems. Tebipenem is thus a so-called beta-lactam antibiotic, which goes back to penicillin. It is used to fight infectious diseases caused by bacteria.
What is tebipenem?
Tebipenem is an antibiotic that is administered to treat infectious diseases. The chemical molecular formula of the substance (C 22 – H 31 – N 3 – O 6 – S 2) has a beta-lactam ring, which is why tebipenem belongs to the group of beta-lactam antibiotics and has a bactericidal effect. The moral mass of the white to whitish-yellow substance is 497.63 g/mol. Due to its chemical and pharmacological properties, tebipenem is also classified as a carbapenem. The closely related active ingredients ertapenem, imipenem, meropenem and doripenem are also part of this group of drugs. Tebipenem was developed specifically to counteract existing antibiotic resistance. Despite positive experience in a number of clinical trials, the active ingredient is currently only approved in Japan. In Europe and the USA, therefore, the active ingredient is not used in any preparations. In contrast, the related active ingredients ertapenem, imipenem, meropenem, and doripenem are widely used in the European Union and the United States.
Pharmacologic action
The pharmacologic action of tebipenem is largely similar to that of other carbapenems. Initial successes can therefore be recorded quite early. Bacteria are killed rapidly by the active ingredient by inhibiting the cell migration of the bacteria. Without the cell wall, bacteria are not viable, as water can penetrate the inside of the cell and inflate it. The cell subsequently bursts open, causing the bacterium to die. Tebipenem is largely insensitive to the bacteria’s own enzyme betalactasmase, which is typical for representatives of its active ingredient group. Bacteria need betalactasmase to prevent external attacks. The enzyme thus largely corresponds to the function of an antibody. Betalactasmase-sensitive substances are weakened in their effectiveness because they cannot attack the bacterium without loss. Because of its insensitivity to betalactasmase, tebipenem is therefore particularly effective. However, it is necessary to maintain a continuously high amount of the active substance in the body. A critical amount, above which efficacy reaches optimum, must always be exceeded (time-dependent killing genetics). However, eukaryotic cells, which do not possess a cell wall, are insensitive to tebipenem and other beta-lactam antibiotics. The drug is cleared primarily renally (via the kidneys).
Medicinal use and application
Tebipenem is administered to fight infectious diseases caused by infectious bacteria. The drug was specifically developed as a replacement medication to treat patients whose symptoms are caused by antibiotic-resistant bacteria. From a medical point of view, the field of application is therefore limited compared to other carbapenems, despite comparatively high efficacy. It should be used in particular when an infection has been acquired by resistant germs (e.g. in hospital). Tebipenem is thus the first-choice active ingredient only in exceptional cases. Clinical studies have shown particularly high efficacy in ear infections, making it particularly suitable as an alternative to carbapenems, which are mainly prescribed for infections of the ear, nose and throat (ENT) region. In principle, however, tebipenem is likely to have the same areas of application as other representatives of the beta-lactam antibiotics due to its pharmacological action. Furthermore, tebipenem is the first carbapenem whose prodrug form (pivalyl ester) is also suitable for oral use. A prodrug is a pharmacologic substance that is either low in activity or completely inactive on its own and acquires its full activity only through metabolization (metabolization) in the body.
Risks and side effects
Tebipenem must not be used if there is a contraindication from a medical point of view (contraindication). This is the case, among other things, if there is a known intolerance (allergy) to tebipenem or other representatives of the beta-lactam group (e.g., penicillin) or related carbapenems (e.g., imipenem, meropenem, and doripenem).Tebipenem should also not be used if complications or severe side effects have occurred during previous treatment with carbapenems. A contraindication is also given in the case of massive renal damage, since the degradation of the active substance occurs predominantly renally. The main undesirable side effects that may occur in connection with treatment include fungal infections, a general feeling of weakness and malaise, headache, fatigue, emotional upset, and gastrointestinal tract discomfort. Also conceivable are reactions of the skin, which may manifest as itching, redness, or the development of a rash. In order to avoid interactions with other medications, the attending physicians should always be informed about all preparations taken. Otherwise, there may be a reduction in efficacy or an immense increase in side effects, putting the goals of therapy in considerable jeopardy.
