Articaine

Articaine hydrochloride is an amide local anesthetic. Local anesthetics block the generation and conduction of nerve impulses, presumably by increasing the threshold for electrical excitation in the nerve, by slowing the propagation of the nerve impulse, and by reducing the rate of rise of the action potential.

• CYKLX is indicated for ocular surface anesthesia prior to ocular procedures and/or intraocular injections in adults and pediatric patients. CYKLX is an amide local anesthetic indicated for ocular surface anesthesia prior to ocular procedures and/or intraocular injections in adults and pediatric patients.

• CYKLX is contraindicated in patients with known hypersensitivity to any component of this preparation. CYKLX is contraindicated in patients with a hypersensitivity to any component of this preparation.contraindicated

The recommended dose of CYKLX is 2 drops applied 30 seconds apart to the ocular surface. The recommended dose of CYKLX is 2 drops applied 30 seconds apart to the ocular surface. ( 2 )

CYKLX is not for injection or intraocular administration ( 5.1 ) Patients should not touch the eye for at least 10 to 20 minutes after using anesthetic as accidental injuries can occur due to insensitivity of the eye ( 5.2 ) Corneal Opacification : Prolonged use of topical ocular anesthetics may produce permanent corneal opacification and ulceration with accompanying visual loss. ( 5.3 ) Do not touch the dropper tip to the eye, eyelids, or any other surface as this may contaminate the solution ( 5.4 ) For Administration by Healthcare Provider : CYKLX is not intended for patient self-administration ( 5.5 ) 5.1 For Topical Ophthalmic Use CYKLX is not for injection or intraocular administration. 5.2 Corneal Injury Due to Insensitivity Patients should not touch the eye for at least 10 to 20 minutes after using CYKLX as accidental injuries can occur due to insensitivity of the eye. 5.3 Corneal Opacification Prolonged use of topical ocular anesthetics may produce permanent corneal opacification and ulceration with accompanying visual loss. 5.4 Risk of Contamination Do not touch the dropper tip to the eye, eyelids, or any other surface as this may contaminate the solution. 5.5 For Administration by Healthcare Provider CYKLX is indicated for administration under the direct supervision of a healthcare provider. CYKLX is not intended for patient self-administration.

The most common adverse reaction was instillation site pain (incidence 24.5%). ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact American Genomics at 855-242-9559 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch 6.1 Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice. In controlled trials, the most common adverse reaction with CYKLX was instillation site pain reported in 24.5% (70/286) of subjects, compared to 6.9% (14/203) of subjects in the placebo group.

8.1 Pregnancy Risk Summary There are no adequate and well-controlled studies in pregnant women with CYKLX to inform a drug associated risk. In animal reproduction studies, subcutaneous administration of articaine hydrochloride and epinephrine (1:100,000) to rabbits throughout organogenesis resulted in maternal toxicity, embryofetal death and increased fetal skeletal variations at doses approximately 160 times the maximum recommended human ophthalmic dose (MRHOD) of CYKLX (see Data ) . The background risk of major birth defects and miscarriage for the indicated population is unknown. However, the background risk in the U.S. general population of major birth defects is 2 to 4%, and of miscarriage is 15 to 20%, of clinically recognized pregnancies. Data Human Data No adequate and well-controlled trials of CYKLX have been conducted in pregnant women. Animal Data In embryo-fetal toxicity studies, subcutaneous administration of articaine hydrochloride and epinephrine (1:100,000) to pregnant rabbits throughout organogenesis produced maternal toxicity, including seizures, at doses of 80 mg/kg/day (approximately 160-fold higher than the bilateral maximum recommended human ophthalmic dose [MRHOD] of 9.6 mg, based on body surface area).

Metabolism

Following ocular administration of CYKLX (2 drops), the geometric mean (geometric CV%) maximum plasma concentration (C max ) is 5.4 ng/mL and total systemic exposure (AUC) is 5.1 ng*hr/mL. Absorption Articaine median (min, max) time to maximum plasma concentration (T max ) is 0.25 hour (0.25 – 1.03 hour) Distribution Approximately 60 to 80% of articaine HCl is bound to human serum albumin and γ-globulins at 37°C in vitro.

Acute emergencies from local anesthetics are generally related to high plasma levels encountered during therapeutic use of local anesthetics or to unintended subarachnoid injection of local anesthetic solution.

• Apr 3, 2000NDANDA020971Deproco
• Feb 26, 2010NDANDA022466Pierrel
• Aug 15, 2025NDANDA218643Thea Pharma

1. 1Drug Ineffective31941%
2. 2Hypoaesthesia435.6%
3. 3Hypoaesthesia Oral415.3%
4. 4Dyspnoea344.4%
5. 5Nausea293.8%
6. 6Paraesthesia283.6%
7. 7Hypersensitivity263.4%
8. 8Anaphylactic Reaction253.2%
9. 9Dizziness253.2%
10. 10Pain243.1%
11. 11Erythema212.7%
12. 12Hypertension212.7%
13. 13Injection Site Pain212.7%
14. 14Pruritus212.7%
15. 15Condition Aggravated202.6%

Recent PubMed references pinned to Articaine as a MeSH major topic. Citations link to pubmed.ncbi.nlm.nih.gov.

• Comparative efficacy and safety of bupivacaine versus articaine in third molar surgery: a systematic review and meta-analysis of randomized controlled trials.
  Acta odontologica Scandinavica · 2026 · Zeng Z, Wang L, Ding G, et al.
  PMID 42233242DOI 10.2340/aos.v85.45787
• Modified Mylohyoid Nerve Anesthesia/Block With 4% Articaine and Dexamethasone Versus Halstead's IANB With 2% Lidocaine in Mandibular Molar Surgery: A Comparative Analysis of Efficacy and Safety Outcomes.
  Medical science monitor : international medical journal of experimental and clinical research · 2026 · Burić K, Stojanović S, Tijanic M, et al.
  PMID 42231550DOI 10.12659/MSM.951821
• Role of articaine and perineural dexamethasone in prolonging postoperative analgesia in mandibular third molar surgery: A comparative analysis.
  Medicina oral, patologia oral y cirugia bucal · 2026 · Şitilci AT, Atalay B, Kuşlu T, et al.
  PMID 41578897DOI 10.4317/medoral.27891
• [Analysis of 101 new adverse drug reactions caused by articaine and epinephrine injection].
  Zhonghua kou qiang yi xue za zhi = Zhonghua kouqiang yixue zazhi = Chinese journal of stomatology · 2026 · Song XY, Zheng LG, Zhao SH, et al.
  PMID 41469011DOI 10.3760/cma.j.cn112144-20250811-00312
• Articaine provides a faster onset and longer duration of analgesia at lower supplemental injections compared to mepivacaine in third molar extractions.
  Oral and maxillofacial surgery · 2025 · Santos SS, Bonatto MDS, Mendes PGJ, et al.
  PMID 41068533DOI 10.1007/s10006-025-01476-7
• Evaluation of Articaine Infiltration Location on the Success Rate of Mandibular Lateral Incisor Anesthesia: A Prospective Crossover Randomized Clinical Trial Study.
  Journal of endodontics · 2026 · Adl A, Alimardani F, Sobhnamayan F, et al.
  PMID 41067376DOI 10.1016/j.joen.2025.09.018
• Self-reported pain after buccal infiltration of articaine vs buccal and palatal infiltration of lidocaine for maxillary primary molar extractions: A noninferiority randomized clinical trial.
  Journal of the American Dental Association (1939) · 2025 · Rigo DCA, Santos PS, Moccelini BS, et al.
  PMID 40932429DOI 10.1016/j.adaj.2025.07.014
• Assessing whether breastfeeding is safe after an intraoral injection of 68 mg of articaine.
  Journal of the American Dental Association (1939) · 2025 · Liu SP, Wu XF, Li XQ, et al.
  PMID 40467122DOI 10.1016/j.adaj.2025.03.008

The 10 most recently updated of 237 ClinicalTrials.gov registrations naming Articaine as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

• Pre-emptive Local Anesthesia and Emergence Behavior After Pediatric Dental General Anesthesia
  Not yet recruiting · Interventional · 80 enrolled · seher orbay yasli
  NCT07604337updated 2026-06-09
• Comparison of the Efficacy of Inferior Alveolar Nerve Block and Digital Anesthesia in Pulpectomy of Mandibular Permanent Molars in Children
  Recruiting · Interventional · 128 enrolled · Inonu University
  NCT07634900updated 2026-06-09
• Comparative Clinical Study Between Virtual Reality Hypnosis and Nitrous Oxide Inhalation for Dental Anxie
  Terminated · Interventional · 30 enrolled · University Hospital, Strasbourg, France
  NCT05167331updated 2026-06-08
• Pre-emptive Local Anesthesia and Sevoflurane Consumption in Pediatric Dental Anesthesia
  Not yet recruiting · Interventional · 80 enrolled · TC Erciyes University
  NCT07608900updated 2026-05-27
• Effect of Immediate Placement and Loading of Compressive Versus Conventional Implants
  Recruiting · Interventional · 30 enrolled · Ahmed Nagi Alghandour
  NCT07601347updated 2026-05-22
• Comparison of Anesthetic Efficacy and Safety Between Inferior Alveolar Nerve Block and the Infiltrative Technique for the Treatment of Peri-implant Diseases in Posterior Mandibular Implants
  Not yet recruiting · Interventional · 30 enrolled · University of Barcelona
  NCT07590037updated 2026-05-22
• A Comparsion Between Articaine Hydrochloride and Buffered Lidocaine Hydrochloride in the Context of Maxillary Permanent Teeth Extraction Using the Buccal Infiltration Technique Only(Clinical Study).
  Active not recruiting · Interventional · 50 enrolled · Tishreen University
  NCT07597408updated 2026-05-19
• Horizontal Ridge Augmentation in Maxillary Esthetic Zone Using Bovine Bone Graft Versus Extended Sticky Bone With Simultaneous Implant Placement
  Completed · Interventional · 16 enrolled · Mansoura University
  NCT07589426updated 2026-05-15
• Comfort-in Needle-Free Injection System in Pediatric Dental Anesthesia
  Completed · Interventional · 60 enrolled · Ondokuz Mayıs University
  NCT07585812updated 2026-05-14
• EFFECT OF SUPER PEN COMPUTER-CONTROLLED INTRALIGAMENTARY INJECTION ON PAIN PERCEPTION IN PEDIATRIC PATIENTS UNDERGOING EXTRACTION OF PRIMARY MOLARS
  Not yet recruiting · Interventional · 30 enrolled · Shatha Musaad Alharthi
  NCT07575035updated 2026-05-08

Frequently asked questions

How does Articaine work?

Articaine hydrochloride is an amide local anesthetic. Local anesthetics block the generation and conduction of nerve impulses, presumably by increasing the threshold for electrical excitation in the nerve, by slowing the propagation of the nerve impulse, and by reducing the rate of rise of the action potential.

What is Articaine used for?

According to FDA labeling, Articaine carries indications including: CYKLX is indicated for ocular surface anesthesia prior to ocular procedures and/or intraocular injections in adults and pediatric patients. CYKLX is an amide local anesthetic indicated for ocular surface anesthesia prior to ocular procedures and/or intraocular injections in adults and pediatric patients.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.

What class of drug is Articaine?

Articaine is classified as Amides, Amide Local Anesthetic, Sodium Channel Interactions, Decreased Sensory-Somatic Nervous System Organized Electrical Activity, Local Anesthesia.

What are the brand names for Articaine?

Articaine is marketed under brand names including Articadent, Cyklx, Orabloc, Septocaine, Ultacan, Zorcaine.

What are the contraindications for Articaine?

Articaine labeling lists contraindications including: CYKLX is contraindicated in patients with known hypersensitivity to any component of this preparation. CYKLX is contraindicated in patients with a hypersensitivity to any component of this preparation.. Always consult the full prescribing information and a clinician.