Articaine: Effects, Uses & Risks

Articaine is an active medical ingredient. It is classified in the group of local anesthetics.

What is articaine?

Articaine is an active medical ingredient. It is assigned to the group of local anesthetics. The most common field of application of the substance is dentistry. The agent articaine belongs to the local anesthetics. Until 1984, the active ingredient was called carticaine. Another name is Articainum. The drug was developed between 1969 and 1974 by the former Farbwerke Hoechst. The most common application of the substance is in dentistry. There, articaine is used to inhibit the transmission of stimuli, cause a blockade of the sodium channels of the nerves and eliminate the perception of pain.

Pharmacologic action

The action of articaine is due to a change in membrane permeability. When a stimulus is received and transmitted, tiny electrical currents occur in the nerve fiber. Various minerals such as potassium and sodium are discharged from the nerve cell through channels during this process. However, they can also flow into the cell. By administering articaine, it is possible to block the channels responsible for transporting sodium. In this way, the transmission of the stimulus is stopped. This, in turn, leads to the temporary elimination of pain. In the case of superficial application, articaine can provide only a very small anesthetic effect. Therefore, injection of the local anesthetic is performed. This procedure allows to anesthetize the adjacent tissue at the injection site. However, it is also possible to anesthetize an entire nerve cord, provided that the injection is performed in its vicinity. One of the greatest advantages of articaine is its rapid anesthetic effect. This sets in at intervals of 1 to 11 minutes, regardless of which application technique is used. In addition, articaine works reliably. The duration of action of the anesthetic lasts between 60 and 225 minutes. The intervention-ready duration of action is between 20 and 75 minutes. If the physician additionally uses blood circulation-inhibiting preparations, the positive effect is prolonged, because this counteracts a washout of the local anesthetic. Another advantage of articaine is its good penetration ability into the tissue of a bone. In addition, the anesthetic can be rapidly eliminated from the body. Thus, its inactivation occurs via hydrolysis as well as the exposure of a hydrophilic acid group.

Medical application and use

Articaine is administered to anesthetize nerves in specific areas of the body. Likewise, entire areas of the body can be treated with the anesthetic. Since the patient does not feel pain, this makes the treatment process much easier. In most cases, articaine is used in routine dental procedures to prevent pain during treatment. Since local anesthetics are mostly used in dentistry, the drug is particularly suitable for this purpose. Articaine can be administered into the skin, into a muscle, into the connective tissue or into the intestinal area. Intravenous injection is also possible. Metabolization of the anesthetic occurs both in the blood plasma and in the liver. This involves cleavage of the articaine in esterases. The plasma half-life averages 30 minutes. Articaine is generally considered to be well tolerated. Thus, it is also suitable for the treatment of pregnant women.

Risks and side effects

Despite the good tolerability of articaine, troublesome side effects are sometimes within the realm of possibility. For example, in some cases, numbness, sensory disturbances, and nausea and vomiting may occur. However, these complaints do not manifest themselves in every case, as the reaction to medication varies from person to person. Rather rarely, dizziness, allergic reactions such as inflammation and swelling, slowed heartbeat and low blood pressure occur after taking articaine. In the worst case, even life-threatening shock or heart failure is conceivable. A strict indication of articaine is necessary in patients suffering from cholinesterase deficiency. In such cases, the effect of the anesthetic may be prolonged or increased. Also, if severe liver or kidney dysfunction, blood clotting disorders, or epilepsy are present, special caution is required during treatment.It is not appropriate to use articaine in cases of severe low blood pressure, hypersensitivity to articaine, severe disorders of the cardiac conduction system, and acute myocardial insufficiency.