Jan 18, 2023 Viewed: 23

Prilocaine/Amide Local Anesthetics

Prilocaine/Amide Local Anesthetics


Indications for Prilocaine

Prilocaine is an amide local anesthetic. The anesthetic intensity and speed are similar to lidocaine, but the duration is longer and the vasodilation effect is weaker. Toxicity is lower than lidocaine. It is clinically used for local anesthesia, especially for patients who are forbidden to use epinephrine.


Dosage of Prilocaine

Infiltration anesthesia: use 0.5% to 1% solution, and the duration of action is 1 to 1.5 hours.

Nerve block anesthesia: use 1% to 2% solution, and the duration of action is 2 to 3 hours.

Epidural anesthesia: use 10-30ml of 1%-1.5% solution, and the duration of action is 2.5-3.5 hours. A maximum dose of 600mg.



1. For dental infiltration anesthesia, 4% solution can be used, the initial dosage is 1-2ml (40-80mg), and the total dosage should not exceed 600mg.

2. Generally, 1%-2% solution can be used for infiltration anesthesia, and the total amount should be less than 600mg.

3. Children under 10 years old can also use it when necessary, but the dosage should not exceed 40mg.


Adverse Reactions


Excessive dosage (>600mg) can easily cause methemoglobinemia, tachycardia, headache, dizziness and weakness. Available methylene blue 1mg/kg rescue.



1. It is contraindicated for those with anemia or a history of methemoglobinemia.

2. It is contraindicated for children under 1 year old, and used with caution for children under 10 years old.

3. This product is contraindicated for paracervical block in obstetrics.



1. This product does not need to add epinephrine, so it is suitable for those who are allergic to epinephrine.

2. It is not commonly used clinically at present, and it is mainly limited to local infiltration anesthesia and local intravenous anesthesia.

3. The maximum dose at one time is 600mg.

4. Patients with anemia, congenital or acquired methaemoglobinemia, heart failure and respiratory failure or hypoxia are prohibited. Avoid for obstetric anesthesia.


Medicine Interactions

If sulfa drugs are used at the same time, even low doses of this product can cause methemoglobinemia.


Pharmacological Effect

Similar to lidocaine, but the duration of action is slightly longer, the accumulation is less, and the toxicity is lower.

The local anesthetic effect of its 3% solution is equivalent to that of 2% lidocaine plus epinephrine, the onset of effect is slow, about 6-7 minutes, and the maintenance time is about 1.5-2 hours, and it has strong penetration to the mucosa. Epinephrine prolongs its action slightly. PPB is 55%, T1/2 is about 1.5h. Metabolized in the liver, its metabolite nitrosotoluidine can oxidize hemoglobin to form methemoglobin. Can be transferred to the fetus through the placenta.



1. When used in dentistry, it starts to take effect within 2 minutes and has a pulp anesthesia effect lasting 10-15 minutes.

2. For inferior alveolar nerve block, it starts to work within 3 minutes, and the average duration of soft tissue anesthesia is 2.5 hours.

3. When the blood drug concentration of this product reaches 0.5-1μg/ml, nearly 55% can be combined with protein. This product can pass through the blood-brain barrier and placental barrier.

4. This product is mainly metabolized in the liver and also in the kidney. Most of the metabolites are excreted with the urine, and only 1% of the original drug is excreted with the urine. The main metabolite that appears in the urine is called o-toluidine. This metabolite is thought to cause methemoglobinemia. This product can also enter breast milk.


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