Citanest Dental Octapressin
Prilocaine hydrochloride 30 mg/ml + Felypressin 0.54 micrograms/ml — Local Dental Anesthetic
Citanest Dental Octapressin is a local anesthetic solution used exclusively in dental procedures. It contains prilocaine hydrochloride combined with felypressin, a synthetic vasopressin analogue that prolongs the anesthetic effect without using epinephrine. This makes it a valuable option in dental practice, particularly for patients who may need to avoid catecholamine-based vasoconstrictors.
Quick Facts
Key Takeaways
- Citanest Dental Octapressin is a local anesthetic specifically designed for dental use, combining prilocaine with the non-catecholamine vasoconstrictor felypressin.
- Felypressin provides local vasoconstriction without the cardiac stimulatory effects of epinephrine, making it potentially suitable for patients with certain cardiovascular conditions.
- At higher doses, prilocaine can cause methemoglobinemia — a condition where hemoglobin cannot carry oxygen effectively. Standard dental doses rarely cause this.
- The maximum recommended dose for healthy adults is 400 mg of prilocaine (approximately 6 mg/kg body weight), which corresponds to about 7 standard cartridges (1.8 ml each).
- Use with caution in pregnancy as felypressin has structural similarity to oxytocin and may theoretically stimulate uterine contractions.
What Is Citanest Dental Octapressin and What Is It Used For?
Citanest Dental Octapressin belongs to the amide class of local anesthetics and is manufactured specifically for dental applications. The formulation combines two active pharmaceutical ingredients: prilocaine hydrochloride, which provides the anesthetic effect, and felypressin (also known as Octapressin), which serves as a vasoconstrictor to prolong the duration of anesthesia and reduce bleeding at the injection site.
Prilocaine works by blocking sodium ion channels in the membranes of nerve fibers. When a local anesthetic is injected near a nerve, it penetrates the nerve cell membrane and blocks the voltage-gated sodium channels from the inside. This prevents the initiation and propagation of nerve impulses, resulting in a reversible loss of sensation in the affected area. The patient experiences numbness in the teeth, gums, and surrounding soft tissues, allowing the dentist to perform procedures without pain.
Felypressin is a synthetic analogue of the naturally occurring hormone vasopressin (antidiuretic hormone). Unlike epinephrine (adrenaline), which is the more commonly used vasoconstrictor in dental local anesthetics, felypressin acts primarily on V1 receptors in vascular smooth muscle to cause local vasoconstriction. This constriction of blood vessels at the injection site serves two important purposes: it slows the absorption of prilocaine into the systemic circulation (thereby prolonging the local anesthetic effect) and it reduces bleeding in the surgical field.
One of the key pharmacological distinctions of felypressin is that it is not a catecholamine. This means it does not stimulate adrenergic receptors and therefore lacks the cardiac stimulatory effects (increased heart rate and blood pressure) that can occur with epinephrine. This pharmacological property has historically made Citanest Dental Octapressin a preferred choice for patients in whom catecholamines may be undesirable, though current evidence has nuanced this clinical decision.
This combination product is indicated for a wide range of dental procedures, including but not limited to:
- Restorative dentistry — fillings, crown preparations, and inlays
- Endodontic procedures — root canal treatments and pulp capping
- Oral surgery — simple and surgical tooth extractions
- Periodontal procedures — deep cleaning, scaling, and root planing
- Prosthodontic procedures — preparations for bridges and dentures
- Pediatric dentistry — dental procedures in children (with appropriate dose adjustment)
Citanest Dental Octapressin is supplied in dental cartridges (typically 1.8 ml or 2.2 ml) designed for use with standard dental aspirating syringes. Each cartridge contains a pre-measured dose of the anesthetic solution, allowing for precise and consistent administration by the dental practitioner. The product is intended for professional use only and should be administered by qualified dental professionals trained in local anesthetic techniques.
What Should You Know Before Receiving Citanest Dental Octapressin?
Contraindications
Citanest Dental Octapressin must not be used in the following situations:
- Known hypersensitivity to prilocaine, felypressin, or any other amide-type local anesthetic (such as lidocaine, articaine, mepivacaine, or bupivacaine)
- Congenital or idiopathic methemoglobinemia — patients with this condition are at significantly increased risk of dangerous methemoglobin levels
- Severe anemia — reduced hemoglobin levels increase vulnerability to the effects of methemoglobinemia
- Severe cardiac conduction disorders without a functioning pacemaker, as local anesthetics may affect cardiac conduction
- Hypersensitivity to any of the excipients in the formulation
Warnings and Precautions
Special care and close monitoring are required when Citanest Dental Octapressin is used in patients with the following conditions:
- Cardiovascular disease — including heart failure, coronary artery disease, and arrhythmias. While felypressin has minimal cardiac effects compared to epinephrine, prilocaine itself can affect cardiac conduction at high plasma levels.
- Hepatic impairment — prilocaine is primarily metabolized by the liver. Patients with significant liver disease may have reduced clearance, leading to higher plasma levels and increased risk of systemic toxicity.
- Renal impairment — the kidneys play a role in prilocaine metabolism and excretion of metabolites. Impaired renal function may lead to accumulation of the methemoglobin-inducing metabolite o-toluidine.
- Epilepsy — local anesthetics may lower the seizure threshold. Patients with epilepsy should be closely monitored, and the lowest effective dose should be used.
- Porphyria — amide-type local anesthetics are potentially porphyrinogenic and should be used with caution in patients with acute porphyria.
- Glucose-6-phosphate dehydrogenase (G6PD) deficiency — patients with G6PD deficiency may be more susceptible to oxidative stress from o-toluidine, increasing the risk of methemoglobinemia at lower doses.
- Elderly patients — may have reduced hepatic blood flow and enzyme activity, potentially increasing the risk of toxicity. Dose reduction may be appropriate.
- Debilitated or acutely ill patients — may be more susceptible to the systemic effects of local anesthetics.
Accidental intravascular injection can lead to serious cardiovascular and central nervous system toxicity. Dental practitioners must always aspirate before injecting to check that the needle is not positioned within a blood vessel. Equipment and medications for resuscitation must be immediately available whenever local anesthetics are administered.
Pregnancy and Breastfeeding
The use of Citanest Dental Octapressin during pregnancy requires careful consideration of the benefits and risks. Prilocaine crosses the placental barrier, and while no definitive evidence of teratogenicity has been established in humans, animal studies warrant caution.
Of particular concern is the felypressin component, which is structurally related to oxytocin. Felypressin may theoretically stimulate uterine smooth muscle contractions, which could be problematic during pregnancy, especially in the third trimester. For this reason, many dental practitioners prefer to use local anesthetic formulations containing epinephrine rather than felypressin for pregnant patients when a vasoconstrictor is needed.
Regarding breastfeeding, small amounts of prilocaine may be excreted in breast milk. However, given the low doses used in dental procedures and the rapid metabolism of the drug, a single dental procedure is generally considered compatible with continued breastfeeding. The American Academy of Pediatrics and most international guidelines consider short dental anesthetic exposure safe during lactation. Patients may wish to express and discard milk for 4–6 hours after the procedure as an additional precaution, though this is generally not considered necessary.
How Does Citanest Dental Octapressin Interact with Other Drugs?
Drug interactions with Citanest Dental Octapressin can be broadly categorized into those related to the prilocaine component and those related to the felypressin component. Understanding these interactions is essential for safe dental practice, as many patients presenting for dental treatment will be taking concurrent medications for various medical conditions.
Major Interactions
| Interacting Drug | Effect | Clinical Significance |
|---|---|---|
| Other local anesthetics | Additive systemic toxicity; combined doses must not exceed maximum safe limits | High — reduce doses when multiple local anesthetics are used |
| Methemoglobin inducers (sulfonamides, dapsone, nitrates, nitrites, phenazopyridine) | Increased risk of methemoglobinemia due to additive effects on hemoglobin oxidation | High — use lowest effective dose; monitor for cyanosis |
| Oxytocin | Felypressin may potentiate the effects of oxytocin on uterine muscle | High — avoid concurrent use, especially in pregnancy |
| Class III antiarrhythmics (amiodarone) | Additive cardiac depressant effects; risk of prolonged conduction | High — use with caution; monitor cardiac function |
Minor Interactions
| Interacting Drug | Effect | Clinical Significance |
|---|---|---|
| Beta-blockers | May reduce hepatic blood flow, slowing prilocaine metabolism and increasing plasma levels | Moderate — consider dose reduction |
| Cimetidine | Inhibits hepatic enzymes, potentially reducing prilocaine clearance | Low to Moderate — monitor for signs of toxicity |
| Tricyclic antidepressants | May enhance the vasopressor effects of felypressin | Low — felypressin effects are minimal at dental doses |
| Sedatives and CNS depressants | Additive central nervous system depression if prilocaine reaches systemic circulation | Low — relevant only at high doses or accidental intravascular injection |
It is important to note that felypressin has a significantly different drug interaction profile compared to epinephrine-containing local anesthetics. Because felypressin is not a catecholamine, it does not interact with monoamine oxidase inhibitors (MAOIs) or non-selective beta-blockers in the same clinically significant way that epinephrine does. This has historically been one of the reasons for choosing Citanest Dental Octapressin in patients taking these medications, although current evidence suggests that the small amounts of epinephrine in dental cartridges are generally safe even in patients on MAOIs when used with careful aspiration technique.
What Is the Correct Dosage of Citanest Dental Octapressin?
Citanest Dental Octapressin is administered by dental professionals using standard dental aspirating syringes with dental cartridges. The dose must be individualized based on the specific dental procedure, the area to be anesthetized, the vascularity of the tissue, the patient's physical status, body weight, and the injection technique employed. The fundamental principle of local anesthetic administration is to use the minimum dose necessary to achieve adequate anesthesia.
Adults
Standard Adult Dosing
For healthy adults weighing 70 kg or more:
- Infiltration anesthesia: 0.5–2.0 ml (15–60 mg prilocaine) per injection site
- Inferior alveolar nerve block: 1.0–2.0 ml (30–60 mg prilocaine) per side
- Maximum single session dose: 400 mg prilocaine (approximately 13.3 ml of 30 mg/ml solution)
- Maximum dose by body weight: 6 mg/kg of prilocaine
In a standard 1.8 ml dental cartridge, the prilocaine content is 54 mg. Therefore, the maximum number of cartridges for a 70 kg adult is approximately 7 cartridges per session. However, most routine dental procedures require only 1–3 cartridges.
Children
Pediatric Dosing
Dosing in children must be carefully calculated based on body weight:
- Children over 6 months of age: The dose should be calculated on the basis of body weight
- Maximum dose: 6 mg/kg body weight of prilocaine
- Not recommended for infants under 6 months of age
For example, a child weighing 20 kg should receive no more than 120 mg of prilocaine (approximately 4 ml or 2.2 cartridges of 1.8 ml). Children may be more susceptible to methemoglobinemia, so particular care should be taken to use the lowest effective dose. Practitioners should also be aware that children may inadvertently bite or chew on numbed lip and tongue tissues, causing self-inflicted injury — parents and caregivers should be warned about this risk.
Elderly Patients
Geriatric Dosing
Elderly patients may require dose adjustments due to physiological changes associated with aging:
- Reduced hepatic function: Slower metabolism may lead to higher plasma levels of prilocaine
- Reduced cardiac output: May affect the distribution and elimination of local anesthetics
- Recommended approach: Use the lower end of the dosage range and titrate carefully
- Maximum dose: Consider reducing the maximum dose by 20–30% in patients over 70 years
Missed Dose
The concept of a missed dose does not apply to Citanest Dental Octapressin, as it is administered as a single dose by a dental professional immediately before or during a dental procedure. It is not a medication that patients take on a schedule. If the anesthetic effect wears off before the procedure is complete, the dentist may administer an additional dose, provided the total dose does not exceed the maximum recommended limits.
Overdose
Overdose of prilocaine can result in two distinct types of toxicity: systemic local anesthetic toxicity and methemoglobinemia. Both require immediate medical intervention.
Central nervous system and cardiovascular toxicity: Symptoms of systemic local anesthetic toxicity typically appear in a progressive fashion. Initial signs include circumoral numbness, tongue paresthesia, light-headedness, tinnitus, visual disturbances, and metallic taste. As plasma levels rise, muscle twitching, tremors, and generalized tonic-clonic seizures may occur. At very high levels, cardiovascular depression ensues with hypotension, bradycardia, arrhythmias, and potentially cardiac arrest.
Methemoglobinemia: This is a unique risk associated with prilocaine among local anesthetics. Prilocaine is metabolized to o-toluidine, which oxidizes hemoglobin to methemoglobin. Clinically significant methemoglobinemia (methemoglobin levels above 20%) is unlikely at doses below 600 mg in healthy adults but can occur at lower doses in susceptible individuals. Symptoms include cyanosis (blue-grey discoloration of the skin, lips, and nail beds), headache, dyspnea, fatigue, and tachycardia. In severe cases (methemoglobin levels above 70%), it can be fatal.
Treatment of overdose: Management is supportive and may include the following:
- Discontinue the injection immediately
- Ensure adequate oxygenation and ventilation
- For seizures: administer intravenous benzodiazepines (e.g., midazolam or diazepam)
- For cardiovascular collapse: initiate advanced cardiac life support; consider lipid emulsion therapy (Intralipid 20%)
- For methemoglobinemia: administer methylene blue 1–2 mg/kg intravenously over 5 minutes; may be repeated once after 30–60 minutes if necessary
What Are the Side Effects of Citanest Dental Octapressin?
Like all medications, Citanest Dental Octapressin can cause side effects, although not everybody gets them. Most adverse effects associated with local dental anesthetics are related to the injection procedure itself rather than the pharmacological action of the drug. It is important to distinguish between true adverse drug reactions and effects that are a natural consequence of nerve blockade (such as numbness of the lip or tongue).
The following frequency classification is based on post-marketing surveillance data and clinical trial reports:
Common
Affects 1 to 10 in every 100 patients
- Pain, swelling, or bruising at the injection site
- Prolonged numbness of the lip, tongue, or cheek beyond the intended duration
- Headache
- Dizziness or light-headedness
- Transient taste disturbance (metallic taste)
Uncommon
Affects 1 to 10 in every 1,000 patients
- Nausea
- Paresthesia (tingling or altered sensation) persisting beyond 24 hours
- Trismus (difficulty opening the mouth) following inferior alveolar nerve block
- Facial nerve palsy (temporary drooping of the eyelid or lip on the injected side)
- Tachycardia (rapid heartbeat) due to anxiety or vasovagal response
Rare
Affects fewer than 1 in 1,000 patients
- Methemoglobinemia (blue-grey skin discoloration, shortness of breath) — dose-dependent risk, primarily at doses exceeding 400 mg
- Allergic reactions (true allergy to amide-type local anesthetics is extremely rare, estimated at less than 1 in 100,000)
- Persistent nerve injury causing prolonged numbness, tingling, or pain lasting weeks to months
- Systemic toxicity with CNS excitation (seizures) followed by CNS depression — typically only after accidental intravascular injection or significant overdose
- Cardiovascular depression (hypotension, bradycardia) — typically only at high systemic levels
- Syncope (fainting) related to vasovagal response
True allergic reactions to amide-type local anesthetics such as prilocaine are exceptionally rare. Most reported “allergic reactions” to dental local anesthetics are actually vasovagal syncope (fainting), anxiety-related hyperventilation, or reactions to other components such as preservatives (sodium metabisulfite) or latex in the cartridge stopper. Allergic reactions are more commonly associated with ester-type local anesthetics (such as procaine or benzocaine). If a patient has a documented allergy to one amide-type local anesthetic, cross-sensitivity to other amides is possible but uncommon.
If you experience any concerning symptoms after receiving a dental local anesthetic — such as persistent numbness lasting more than 8 hours, blue discoloration of the lips or fingertips, difficulty breathing, or widespread skin rash — you should contact your dentist or seek medical attention promptly.
How Should Citanest Dental Octapressin Be Stored?
Proper storage of Citanest Dental Octapressin is essential to maintain the stability, sterility, and efficacy of the product. As this is a prescription medication administered exclusively in dental settings, storage is managed by the dental practice rather than by patients. However, understanding storage requirements helps ensure that the product you receive has been properly maintained.
The following storage conditions apply:
- Temperature: Store below 25°C (77°F). Do not refrigerate or freeze, as freezing can damage the cartridge and alter the solution's properties.
- Light protection: Store in the original packaging to protect from light. Exposure to light can degrade the active ingredients over time.
- Sterility: Dental cartridges are sterile and should not be used if the packaging is damaged or if the solution appears discolored, cloudy, or contains particulate matter.
- Expiration date: Do not use after the expiration date printed on the cartridge and packaging. Expired local anesthetics may have reduced potency and an altered pH, potentially causing increased pain on injection.
- Single use only: Each cartridge is intended for single patient use. Partially used cartridges must not be saved or reused due to the risk of cross-contamination.
Patients do not typically need to store this medication at home, as it is administered in the dental office. If you have any concerns about the condition of a dental local anesthetic being used for your procedure, you are within your rights to ask your dental professional about the product's expiration date and storage conditions.
What Does Citanest Dental Octapressin Contain?
Understanding the composition of Citanest Dental Octapressin can help patients and healthcare professionals identify potential allergens or substances of concern. The formulation contains both active and inactive ingredients carefully selected to ensure the product's stability, efficacy, and safety profile.
Active Ingredients
- Prilocaine hydrochloride 30 mg/ml — An amide-type local anesthetic. Prilocaine (chemical name: 2-(propylamino)-o-propionotoluidide hydrochloride) is the primary active ingredient responsible for the numbing effect. The 3% concentration (30 mg/ml) provides effective local anesthesia for the majority of dental procedures.
- Felypressin 0.54 micrograms/ml (0.03 IU/ml) — Also known as Octapressin or 2-phenylalanine-8-lysine-vasopressin, this is a synthetic analogue of the natural hormone vasopressin. It acts as a local vasoconstrictor, reducing blood flow at the injection site to prolong the anesthetic effect and reduce systemic absorption of prilocaine.
Inactive Ingredients (Excipients)
- Sodium chloride — Used to adjust the tonicity of the solution to make it isotonic with body fluids, reducing pain on injection
- Sodium hydroxide and/or hydrochloric acid — Used for pH adjustment to maintain solution stability and reduce pain on injection
- Water for injections — The solvent vehicle for the active ingredients
Citanest Dental Octapressin cartridges do not contain sodium metabisulfite or other sulfite preservatives, unlike many epinephrine-containing dental local anesthetic formulations. This can be an advantage for patients with known sulfite sensitivity. The formulation also does not contain methylparaben or other parabens, which were historically associated with allergic reactions in some ester-type local anesthetic preparations.
The dental cartridges are made of glass with rubber plunger stoppers. Patients with known latex allergy should inform their dental practitioner, as some older cartridge designs may contain natural rubber latex in the stopper. Modern cartridges from most manufacturers now use synthetic rubber, but it is worth verifying with your dental practice if you have a severe latex allergy.
Frequently Asked Questions
Medical References
This article is based on the following peer-reviewed sources and international medical guidelines:
- European Medicines Agency (EMA). Summary of Product Characteristics — Citanest Dental Octapressin. Updated 2024. Available from: www.ema.europa.eu
- Becker DE, Reed KL. Local anesthetics: review of pharmacological considerations. Anesthesia Progress. 2012;59(2):90-102. doi:10.2344/0003-3006-59.2.90
- Malamed SF. Handbook of Local Anesthesia. 7th ed. Elsevier; 2020.
- World Health Organization (WHO). WHO Model List of Essential Medicines — 23rd List, 2023. Geneva: WHO; 2023.
- Ogle OE, Mahjoubi G. Local anesthesia: agents, techniques, and complications. Dental Clinics of North America. 2012;56(1):133-148. doi:10.1016/j.cden.2011.08.003
- Guay J. Methemoglobinemia related to local anesthetics: a summary of 242 episodes. Anesthesia & Analgesia. 2009;108(3):837-845. doi:10.1213/ane.0b013e318187c4b1
- Scottish Dental Clinical Effectiveness Programme (SDCEP). Drug Prescribing for Dentistry. 3rd ed. Dundee: SDCEP; 2016.
- American Dental Association (ADA). ADA/PDR Guide to Dental Therapeutics. 6th ed. Chicago: ADA; 2021.
- British National Formulary (BNF). Local anaesthesia — Dental anaesthesia. London: BMJ Group and Pharmaceutical Press; 2024. Available from: bnf.nice.org.uk
- Haas DA. An update on local anesthetics in dentistry. Journal of the Canadian Dental Association. 2002;68(9):546-551.
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