Ультракаин

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Ультракаин

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Method of action: Local Anesthetic

Treatment option: Anesthesia

Medically reviewed

Marina Burgos

Last updated on 10/01/2026

This page provides general, reference-level information compiled from official medical sources. It is not a substitute for professional medical advice, diagnosis, or treatment. For decisions about your health, please consult a qualified healthcare professional.

Overview of Ультракаин

Quick Facts

Property Description
Active ingredient Articaine hydrochloride, Epinephrine
Form Injectable solution (Sterile, aqueous)
Pharmacological class Amide-type Local Anesthetic
Common use Inducing localized anesthesia
Origin Synthetic combination product

What Type of Medicine is Ультракаин?

Ультракаин is classified as a prescription-only pharmaceutical preparation that belongs to the amide-type local anesthetic class. The primary active component is Articaine hydrochloride, a potent synthetic substance specifically developed for inducing localized anesthesia. Articaine is structurally unique among this class due to the presence of both an amide and an ester group, a feature that contributes to its rapid metabolic breakdown. This rapid processing is a clinically recognized benefit, allowing the body to clear Articaine quickly following its targeted action. Ультракаин is supplied as a sterile injectable solution for targeted delivery, a presentation common for similar brands such as Septocaine and Articadent.

What are the Components of the Ультракаин Solution?

The injectable solution is defined as a combination product because it typically contains both the anesthetic agent and a vasoconstrictor. The active anesthetic is Articaine, which is combined with Epinephrine (Adrenaline) in an aqueous vehicle. The functional purpose of including Epinephrine is crucial: it causes a localized vasoconstriction, or narrowing of blood vessels, which slows the rate at which the body absorbs the Articaine, keeping the anesthetic concentrated at the intended site for an extended period. Combining a local anesthetic with Epinephrine is a standard practice to increase the depth and duration of the numbing effect compared to using the anesthetic alone.

What is the General Therapeutic Purpose of Articaine?

The general therapeutic purpose of Articaine is to provide reliable and effective targeted pain control by establishing a state of localized anesthesia. This preparation is used to temporarily block the electrical signals that nerves use to transmit sensation, specifically pain, from the area of administration to the central nervous system. A typical use scenario involves minimizing or eliminating sensation during localized procedures, such as minor surgical interventions. This action permits necessary procedures to be completed without discomfort for the patient, representing the core benefit of Articaine's fast-acting and precise nerve conduction blockade.

What side effects are possible with Ультракаин?

Official Adverse Reactions and Safety Profile

The safety profile of Articaine/Epinephrine (Ультракаин) is formally classified by government regulatory authorities, detailing potential adverse reactions and restrictions on use. Reactions are grouped by their frequency and the body system affected, consistent with official regulatory documentation (e.g., FDA, EMA).

Frequency-Classified Adverse Reactions

Classification Examples of Documented Effects
Common (≥1/100 to <1/10) Headache, Paresthesia (numbness/tingling), Pain at injection site
Uncommon (≥1/1,000 to <1/100) Tachycardia (increased heart rate), Dizziness, Nausea, Vomiting
Rare (≥1/10,000 to <1/1,000) Anaphylaxis, Severe Hypotension, Respiratory Depression

These effects primarily involve the Nervous System (e.g., paresthesia, dizziness), Cardiac System (e.g., tachycardia, hypotension), and Gastrointestinal System.

Serious Safety Considerations

The official labeling highlights the potential for serious, life-threatening events, which are generally associated with systemic toxicity from rapid absorption or overdosage. These serious adverse reactions include Convulsions, Cardiac Arrest, Methaemoglobinaemia, and Anaphylactic Shock.

Population-Specific Constraints

Regulatory documentation specifies that caution is required in certain populations. Use is generally contraindicated in children under four years of age. Particular caution is advised for elderly patients and individuals with severe hepatic or renal impairment due to the potential for increased drug levels. Furthermore, the Epinephrine component requires caution in patients with unmanaged severe cardiovascular conditions or uncontrolled thyrotoxicosis, as these are listed as contraindications.

Overdose and Emergency Response

Overdose and When to Seek Help

The overdose profile for Articaine and Epinephrine (Ультракаин) involves two documented forms of toxicity: systemic effects from the local anesthetic component and vasoconstrictor effects from Epinephrine.

Officially documented signs of systemic toxicity often follow a biphasic pattern. Initial manifestations, classified as CNS excitation, may include nervousness, dizziness, or tremors. If toxicity progresses, it can lead to CNS depression, characterized by somnolence, unconsciousness, seizures, and, ultimately, respiratory arrest.

Severe or life-threatening outcomes documented in regulatory labeling include critical cardiovascular events such as ventricular arrhythmias and cardiac arrest. The vasoconstrictor component can lead to severe hypertension, posing a risk of cerebrovascular hemorrhage.

The official guidance explicitly states that immediate medical attention must be sought for any systemic signs of toxicity, especially confusion, convulsions, or severe cardiovascular changes. Regulatory documents emphasize the necessity for immediate access to resuscitative equipment and providing symptomatic and supportive treatment to manage these acute manifestations.

Population-specific notes advise caution for patients with severe hepatic impairment or pre-existing cardiovascular disease. While no specific antidote is formally known for Articaine overdose, management focuses on supportive care for the documented symptoms.

Therapeutic Uses of Ультракаин

What Ультракаин Treats: Main Uses and Benefits

The therapeutic purpose of Ультракаин is to provide localized anesthesia by addressing the acute procedural pain and nociceptive sensation that may be present during necessary interventions. This medication is indicated for inducing localized anesthesia during dental procedures.

It is commonly used to manage the discomfort associated with a variety of treatments, including restorative dentistry, endodontic treatments, simple or complicated extractions, and minor oral surgery. The medication is particularly relevant in contexts marked by increased discomfort or tension, such as clinical scenarios demanding a dependable depth of anesthesia. This provides support that helps ease the overall symptom burden and contributes to improved comfort during the treatment. This offers symptomatic relief that helps patients cope more steadily with difficult episodes.

“This preparation is relevant when supportive symptom management is appropriate by addressing the pronounced symptoms of discomfort and sensitivity expected during localized interventions.”


Overview: Symptom Relief

Aspect Description
Primary Goal Reduction of sensation and acute pain in a localized area
Symptom Addressed Procedural pain, discomfort, and sensitivity
Context of Use Invasive dental and minor oral surgical procedures
Patient Benefit Supports general well-being during symptomatic phases

Regulatory References

  1. Articaine Hydrochloride and Epinephrine Injection DailyMed Overview

Eligibility and Restrictions for Use

The eligibility for using Ультракаин (Articaine hydrochloride with Epinephrine) is defined by regulatory agencies to ensure patient safety and is based on the drug's components.

Populations for Whom Use is Allowed

Adults and pediatric patients 4 years of age or older are generally approved for use in dental procedures, provided no contraindications exist. Safety and effectiveness have not been established in children under 4 years old.


Absolute Contraindications

Use is strictly prohibited in certain patient groups, including:

  • Patients with known allergy to articaine, epinephrine, or sulfites (due to the presence of a preservative).
  • Patients with uncontrolled severe hypertension, severe heart failure, unstable angina, recent myocardial infarction (within 3–6 months), or uncontrolled hyperthyroidism (due to the Epinephrine component).
  • Patients with hereditary or idiopathic methemoglobinemia.

Conditional Use and Restrictions

Caution is mandated for patients with severe hepatic or renal impairment, G-6-PD deficiency, or controlled cardiovascular conditions. For pregnancy, use is restricted to cases where the benefit justifies the potential risk to the fetus. Acutely ill or debilitated patients require a lower, commensurate dosage.

What should I know about interactions with other medicines?

Interactions with other medicines and products

The officially documented interaction profile for Articaine and Epinephrine (Ультракаин) is primarily structured by pharmacodynamic effects related to the Epinephrine vasoconstrictor component. Regulatory sources define specific classes of medicinal products that may lead to clinically significant interactions.


Documented Pharmacodynamic Interactions

Co-administration with certain drug classes may result in severe cardiovascular responses:

  • Monoamine Oxidase Inhibitors (MAOIs) and Tricyclic Antidepressants (TCAs) may produce severe, prolonged hypertension due to enhanced sympathomimetic effects.
  • Nonselective Beta-Adrenergic Antagonists (Nonselective Beta-Blockers) may lead to hypertension and bradycardia because of the unopposed alpha-adrenergic effects of Epinephrine.
  • Potent Inhalation Anesthetics or Ergot-type Oxytocic Drugs may increase the risk of serious ventricular rhythm disorders or severe, persistent hypertension, respectively.
  • Other Local Anesthetics or oxidizing agents may increase the risk of methemoglobinemia.

Other Interaction Considerations

The anesthetic component, Articaine, is primarily cleared by plasma carboxyesterase; major CYP-enzyme-mediated drug interactions are not typically highlighted in the regulatory interaction section. Caution is advised for patients with Severe Hepatic Disease due to the potential for slower clearance of Articaine, which could alter the overall drug exposure. The product is also restricted from use in patients with known sensitivity to sulfites (e.g., Sodium Metabisulfite), a component-driven restriction documented in official labeling.

Mechanism of Action

Molecular Interruption of Nerve Signal Transmission

The primary action of Articaine is a targeted, physical blockade of Voltage-Gated Sodium Channels (VGSCs) in peripheral sensory neurons. This molecular interaction prevents the crucial influx of Na^+ ions, which is necessary to generate an action potential. By halting this electrical event, the drug directly interrupts the peripheral nociceptive signaling pathway, leading to the physiological effect of interrupted sensory nerve conduction.


⏱️ Mechanistic Modulation of Local Hemodynamics

The combination product contains Epinephrine, which acts as an agonist on alpha1 -Adrenergic Receptors in the local vascular smooth muscle. This engagement initiates vasoconstriction, or the narrowing of nearby blood vessels. This effect is a mechanistic synergy that slows the rate of Articaine clearance from the site, which maintains a high concentration of the anesthetic around the nerve. This sustained concentration facilitates a mechanically prolonged and robust blockade of the VGSC function.


️ Physiological Constraints on Mechanism Effectiveness

The ability of Articaine to effectively block VGSCs is directly affected by the pH of the surrounding tissue. Under acidic conditions, such as those found in inflamed or infected areas, the molecule shifts predominantly to its ionized (charged) form. This charged state severely limits its ability to diffuse across the nerve cell membrane to reach its intracellular target, leading to a functionally incomplete or slowed intraneuronal drug concentration.

Dosage and Administration Information

How to Use Ультракаин: Administration Guidelines

This section describes the instructions for the use of Ультракаин (Articaine hydrochloride and Epinephrine).


Administration Scope

Feature Guideline
Route of administration Intraoral injection only, via submucosal infiltration or nerve block.
Dosing schedule Individualized dose must not exceed the maximum recommended dose of 7 mg/kg of Articaine (equivalent to 0.175 mL/kg) per appointment.
Preparation requirements (if applicable) Supplied as a sterile aqueous solution in single-use cartridges. No dilution is required.

Instruction Classifications (High-Level)

Classification Description
Administration method type Injection (Local/Regional Nerve Block)
Frequency pattern As-needed, single-event use (not for repeated daily or cyclic use).
Age-group administration rules The maximum dose limit of 7 mg/kg applies to pediatric patients 4 years and older. Doses must be reduced for older adults and patients with impaired liver function.

Resulting Procedural Structure

Standard step sequence:

  • Confirm the administration site via the intraoral route (infiltration or nerve block).
  • Aspiration is mandatory prior to injection to ensure the needle tip is not in a blood vessel.
  • Administer the lowest effective dose slowly (e.g., not exceeding 1 mL/minute), ensuring the total volume is within the required maximum limit.
  • Discard any remaining solution in the single-use cartridge immediately after the procedure is complete.

Connection to the overall use protocol

The protocol defines the use of Ультракаин as a sterile, non-repeated injection administered in a professional setting according to a precise dose proportional to the patient's body weight. This framework establishes the standardized, procedure-specific usage of the medicine, emphasizing controlled technique and strict adherence to maximum dose limits.

Recent Clinical Evidence

Research Evidence / Overview of Studies for Ультракаин (Articaine with Epinephrine)


Evidence for Use in General Dental and Oral Procedures

This section will summarize the findings from Randomized Controlled Trials (RCTs) and Meta-analyses that have evaluated Articaine was studied for localized anesthesia during routine and complex dental interventions. The summary will detail the outcomes measured, such as the assessed outcomes of anesthesia and the time to onset, as reported in the literature.

The research exploring Articaine with Epinephrine primarily consists of short-term RCTs, often double-blind, used in studies exploring patient-reported experiences during procedures like extractions, restorative work, and endodontic treatments. These trials mainly focused on outcomes related to pulpal anesthesia (numbness of the tooth nerve), measuring the time it took for the anesthetic effect to begin and the reported duration of the effect. Findings describe patterns observed in the studies related to measuring the attainment of a state of anesthesia for the procedure. Articaine was studied in trials including the traditional anesthetic, Lidocaine, as a reference agent, with research highlighting changes measured during the study period concerning the assessed outcomes of the nerve block.

Comparative Studies: Infiltration vs. Nerve Block Techniques

This subsection will specifically review the research comparing the anesthetic results achieved when Articaine is administered using the infiltration technique versus the Inferior Alveolar Nerve Block (IANB), highlighting the types of studies that have assessed these delivery methods.

The different methods of administration—infiltration (direct injection near the site) and nerve block (injection near the main nerve branch)—were evaluated in specific comparative trials. Research examined the assessed outcome rate for the anesthetic effect for each method. Findings describe patterns related to the assessed outcomes depending on whether Articaine was administered as an infiltration or as a nerve block, with some trials describing similar measurements between Articaine infiltration and traditional nerve block methods for some procedures.


Evidence for Procedures with Challenging Anesthesia

Articaine was evaluated in studies conducted during periods of increased symptom activity, specifically in patients with symptomatic irreversible pulpitis, a condition associated with acute or disruptive episodes of dental pain. Researchers monitored outcomes related to physical discomfort, using patient-reported outcomes describing perceived discomfort measured by pain scales during the procedure itself. Studies focused on episodes where symptoms become more noticeable, measuring the rate of assessed absence of reported pain during treatment access.

Findings indicate that Articaine was observed in some studies to have patterns related to successful anesthesia in this challenging setting. Research highlights that changes measured during the study period were associated with factors like the patient's existing level of inflammation and the precise injection technique.


Research Focus on Special Populations and Limitations

Articaine was evaluated in trials including pediatric patients (children) down to four years of age undergoing dental work. Research describes patterns related to the assessed anesthetic outcomes in the pediatric patients studied. Research describes patterns related to onset time, with some studies reporting differences in measured timing between pediatric patients and adults. However, data for other special groups, such as older adults with specific comorbidities, remain insufficient.

The research exploring Articaine with Epinephrine is primarily relevant in trials assessing short-term or episodic symptom patterns. The immediate onset and duration of localized anesthesia were the main clinical endpoints of interest; consequently, follow-up durations were limited. There is limited information for long-term outcomes, as the nature of the drug’s intended use does not necessitate extended observation periods.

Key Studies & References

  1. Articaine Hydrochloride and Epinephrine Injection, USP (DailyMed, NIH)
  2. Efficacy of articaine versus lidocaine in dental local anesthesia: a meta-analysis

Frequently Asked Questions (FAQ)

Common questions about Ультракаин (FAQ)


Q: How quickly does the numbing from Ультракаин usually begin after injection?

According to the official product information, the numbing effect on the dental pulp typically begins very quickly, usually within 1.4 to 5 minutes after the injection. The time to onset is a key characteristic described in regulatory documents.


Q: How long can the effects of Ультракаин be expected to last?

The duration of the anesthetic effect is determined by the tissue type. Official labeling states that pulpal (tooth) anesthesia generally lasts 60 to 75 minutes, while the numbness in the surrounding soft tissue may persist for 3 to 5 hours.


Q: What is the difference between Ультракаин and Lidocaine?

Regulatory documents describe Articaine (the active drug in Ультракаин) as having a unique chemical structure that combines both an amide group and an ester group. This specific structure is noted to contribute to its rapid breakdown in the body, distinguishing it from traditional amide-type local anesthetics like Lidocaine.


Q: Are there different versions of Ультракаин available?

Yes, official product documents show that Articaine is approved in different formulations. These typically include the anesthetic combined with varying concentrations of the vasoconstrictor epinephrine (e.g., 1:100,000 or 1:200,000). There are also formulations approved that contain articaine only, without epinephrine.


Q: What are the signs of a rare allergic reaction to Ультракаин?

Signs of a severe hypersensitivity reaction, as described in official safety information, can include generalized rash, itching, and swelling of the face, tongue, or throat. Official safety information notes that these events have been documented.


Q: Can older adults safely receive Ультракаин?

Official documentation advises that the dosage should be reduced in elderly patients compared to the maximum dose for younger adults. This is based on the potential for elderly patients to eliminate the drug more slowly and the consideration of associated health conditions.


Q: Is it normal to feel anxious or shaky after receiving the injection?

Feeling anxious, nervous, or experiencing palpitations (a fast heartbeat) can be signs related to the epinephrine component of the injection. Official labeling describes these effects as related to systemic toxicity or epinephrine excess, which are often dose-dependent.


Q: What should a patient tell their administering professional before getting Ультракаин?

Official guidelines recommend informing the professional about any known allergies, especially to Articaine, epinephrine, or sulfites. Additionally, any existing severe heart, liver, or thyroid conditions, as well as current medications, should be disclosed as they may affect the drug’s use or metabolism.


Q: What factors might make the numbing effect of Ультракаин last for a longer or shorter time?

Studies and official information indicate that the duration is influenced by the epinephrine component, which helps prolong the anesthetic's presence at the injection site. Official warnings also note that the drug's effectiveness may be reduced in inflamed or infected tissue due to the acidic environment in those areas.


Q: What happens to the active ingredient in Ультракаин after the numbing effect is over?

Once the numbing effect is complete, the articaine component is rapidly cleared by the body. Official documents describe that it is broken down in the bloodstream primarily by an enzyme called plasma carboxyesterase before being eliminated.


Q: Is the numbness from Ультракаин different than the numbness from Novocaine?

Regulatory classifications describe Articaine as having a unique chemical structure, a hybrid amide/ester type. This is chemically distinct from older local anesthetics like procaine (Novocaine), which belong to the ester class.


Q: Are there any reported cases of persistent numbness following Ультракаин use?

While temporary numbness (paresthesia) is a common and expected effect, official safety information indicates that very rare cases of prolonged or permanent nerve injury have been documented following the use of local anesthetics like Ультракаин.


Q: Why is the drug administered only by qualified healthcare professionals?

Official administration guidelines include mandatory steps like aspiration prior to injection and administering the drug according to a strict, calculated dose proportional to body weight. These requirements necessitate that the drug is administered by a trained healthcare professional.


Q: Are there special considerations for using Ультракаин while breastfeeding?

Regulatory information notes that Articaine is excreted into human breast milk. However, due to its rapid breakdown in the body, the amount is considered very small. Official guidance states that a decision regarding use is based on weighing the benefit against the potential risk.


Q: Is it possible to be allergic to all local anesthetics if I am allergic to Ультракаин?

Articaine belongs to the amide class of local anesthetics, although it has a unique chemical structure. Official documentation states that cross-sensitivity between different chemical classes of local anesthetics (such as between amide-type and ester-type) is rare.


Q: What is the purpose of the sulfite preservative in some anesthetic solutions?

The preservative Sodium Metabisulfite (a type of sulfite) is included in the formulations that contain epinephrine. Its purpose, as stated in regulatory documents, is to prevent the breakdown of the vasoconstrictor component, ensuring its stability and effectiveness.


Q: Is Ультракаин approved for use outside of dentistry?

Official labeling specifies that Ультракаин is indicated for use in local anesthesia during routine and complex dental procedures. Its formal approval is defined by this scope of dental use.


Q: Does the numbing effect wear off faster in certain parts of the body?

Yes, official data often report differences in the duration of effect depending on the tissue type. Specifically, the numbing effect on the dental pulp (the nerve within the tooth) is typically shorter than the duration of numbness felt in the surrounding soft tissue.


Q: Why does the injection sometimes cause a momentary burning or stinging sensation?

Pain or a reaction at the injection site is considered common. Official information suggests that this momentary burning sensation is often related to the injection technique or the slightly acidic nature of the anesthetic solution itself.


Q: Are there restrictions on consuming food or drink immediately after receiving Ультракаин?

Patient information advises that consuming food or hot beverages is typically avoided until the local anesthesia has completely worn off. This is a common precaution intended to prevent accidental biting of the numb tissue or potential burns from hot liquids.


Q: How long does it take for the adrenaline in the injection to leave the system?

Epinephrine (adrenaline) is rapidly cleared by the body. Regulatory documents describe that this component has a very short half-life, meaning it is quickly metabolized and eliminated from the body following its administration.

How should Ультракаин be stored and disposed of?

The Articaine/Epinephrine solution (Ультракаин) must be stored at room temperature, typically between 20 C and 25 C, and must not be frozen. To ensure product stability, the medication must be kept in its original carton to protect it from light.

Regulatory documents mandate that the product must not be used after the expiration date or if the solution is cloudy or discolored. The cartridges are for single use only; any remaining solution must be discarded immediately after the procedure.

For safety, the medication must be stored out of the sight and reach of children. Disposal of the unused product and containers must be performed in accordance with local, provincial, and federal regulations for pharmaceutical waste.

Attention! Always consult to a doctor or pharmacist before using pills or medicines.

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