Bupivacaine is a pharmacologically active substance that is included in the category of anesthetics. The drug bupivacaine is a local anesthetic and is part of the so-called amide type. The active ingredient is used, inter alia, as a racemate. Bupivacaine is characterized by a comparatively slow onset of action. In addition, the effect of the drug lasting up to twelve hours is relatively long.

What is bupivacaine?

The drug bupivacaine is primarily used in the context of local anesthesia and anesthesia of entire body areas. It is used in the line anesthesia and infiltration anesthesia. Nerve cords are anesthetized during conduction anesthesia, while the agent bupivacaine is injected into the tissue during infiltration anesthesia to quench pain locally.

Also in the context of pain therapy, the drug bupivacaine is used. In addition, the active substance is used to turn off the sympathetic nerve, as it can reduce pain associated with this nerve.

Unlike the active ingredients mepivacaine and lidocaine, the drug bupivacaine is lipophilic. If it enters the blood, the active substance binds to 96 percent of certain plasma proteins. Basically, the effect of the drug is relatively slow. The so-called plasma half-life is on average about five and a half hours. Because of this, bupivacaine is able to work for up to twelve hours. Following this, the active ingredient is eliminated via the kidneys.

Pharmacological action

The drug bupivacaine is characterized by a characteristic mode of action in the human organism. First, the drug causes a change in the permeability of cell membranes. This change is especially relevant for sodium ions. As a result, they are no longer able to enter the cell, which means that no action potential can form. Thus, no pain can be felt in the corresponding area.

First and foremost, the drug bupivacaine is a drug for local anesthesia dar. The substance blocks nerve fibers in the autonomic nervous system over a longer period of time, the blockade is not permanent, but reversible.

In addition, the active ingredient is able to temporarily switch off special sensory nerves and those for controlling movements. Even those nerve fibers that control the action of the heart can numb the drug bupivacaine.

The action of the drug bupivacaine is believed to be achieved by blocking the channels of sodium ions within the nerve cell walls. Because the influx of these ions plays an important role in the electrical Umpolung in the nerves, which only the conduction of stimuli is possible. Dense sodium channels do not allow corresponding ions in the nerve cell, so that no build-up of electrical voltage can occur.

In the majority of cases, the active ingredient bupivacaine is in the form of bupivacaine hydrochloride, a salt. In this state, the drug first reaches the nerve cell and unfolds its effect there. If it is a very acidic environment, such as in inflamed areas, bupivacaine hydrochloride does not cleave into its two basic constituents. For this reason, no analgesic effect is possible in such a case.

Medical application & use

The drug bupivacaine is used primarily in the context of anesthesia. It is mainly used for those anesthesia procedures that are located near the spinal cord. These include, for example, peridural or spinal anesthesia.

Due to the relatively long-lasting effect, the drug bupivacaine is a very frequently used local anesthetic. On the other hand, it tends to be used less frequently in dentistry. Here it is primarily used for very long treatments.

In addition, bupivacaine is used in the context of conduction and infiltration anesthesia. In principle, the active substance is suitable for the temporary elimination of severe to very severe pain in different areas of the body.

Risks & Side Effects

The drug bupivacaine has undesirable side effects that need to be considered before using the drug. Basically, it should be noted that bupivacaine is a very toxic local anesthetic. This toxicity is particularly problematic in uncontrolled intravenous injection.

Possible side effects and symptoms of the drug bupivacaine include, for example, dizziness and hypotension or hypertension. The affected patients may experience nausea and vomiting. More serious side effects include cardiac arrhythmia or bradycardia.

In addition, so-called palpitations are possible while taking the drug. In some cases, convulsions appear in the patients. In addition, disorders of hearing and vision as well as speech disorders are possible. Occasionally, hypersensitivity reactions to bupivacaine, which manifest themselves, for example, in diarrhea or asthma attacks.

In certain cases, administration of the active substance bupivacaine is contraindicated. This includes, for example, an existing hypersensitivity to so-called acid amides. Even with low blood pressure (hypotension) or a decompensated heart failure, the use of the drug should be avoided if possible.

Other contraindications include, for example, disorders of blood clotting, hypovolemia and increased intracranial pressure in epidural anesthesia. Tags: 

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