Citanest Plain Dental (Prilocaine Hydrochloride Injection): Uses, Dosage, Side Effects, Interactions, Warning (2023)

drug description

What is Citanest Plain Dental and how is it used?

Citanest Plain Dental is a prescription medication used as aAnesthesiaduring dental procedures. Citanest Plain Dental can be used alone or with other medications.

Citanest Plain Dental is in a class of drugs called local anesthetics, amides; Dental Local Anesthetics.

What are the possible side effects of Citanest Plain Dental?

Citanest Plain Dental can cause serious side effects, including:

• urticaria,
• difficult breathing,
• swelling of the face, lips, tongue or throat,
• skin irritation,
• Itch,
• red, swollen, blistered, or peeling skin with or without fever
• wheezing,
• tightness in the chest or throat
• difficulty swallowing or speaking
• unusualhoarseness,
• blue or gray color of lips, nails or skin,
• fluttering in your chest,
• seizures,
• severe dizziness,
• fainting,
• severe headache,
• somnolence,
• weakness,
• fatigue,
• difficulty breathing,
• fast breathing,
• fast or slow heart rate
• stomachache,
• bellyache,
• vomit,
• burning, numbness, or tingling around the mouth
• stun,
• confusion,
• blurred vision,
• perspiration,
• ringing in the ears,
• depression,
• nervousness,
• anxiety,
• instability,
• spasms,
• bad coordination,
• interest,
• emotion, and
• feeling hot or cold

Get medical help right away if you have any of the symptoms listed above.

The most common side effects of Citanest Plain Dental include:

• swelling around the lips and
• numbness or tingling in the lips or mouth

Tell your doctor if you experience any side effects that bother you or that do not go away.

These are not all possible side effects of Citanest Plain Dental. For more information, consult your doctor or pharmacist.

Call your doctor for medical advice about side effects. You can report side effects to the FDA at 1-800-FDA-1088.

DESCRIPTION

Citanest Plain Dental 4% (HCI Prilocaine Injection, USP), is aisotonic solutioncontaining a locationanestheticand is administered parenterally by injection. To seeINDICATIONS AND USEfor specific uses. Thequantitythe composition is shown in Table 1.

Citanest Plain Dental 4% contains prilocaine HCl, which is chemically designated as propanamide, N-(2-methyl-phenyl)-2-(propylamino)-, monohydrochloride and has the following structural formula:

Parenteral pharmaceuticals should be visually inspected for particulate matter and discoloration prior to administration.

The specific quantitative composition is shown in Table 1.

TABLE 1: COMPOSITION

Note: Sodium hydroxide or hydrochloric acid can be used to adjust the pH of Citanest 4% Single Dental Injection.

Secundary effects

SECUNDARY EFFECTS

Edema and persistent paresthesia of the lips and oral tissues may occur. Persistent paresthesias lasting weeks to months and, rarely, lasting more than a year have been reported.

Adverse experiences following prilocaine administration are similar in nature to those seen with other amide-type local anesthetic agents. These adverse experiences are usually dose-related and may result from elevated plasma levels caused by excessive doses, rapid absorption, or unintended intravascular injection, or may result from hypersensitivity, idiosyncrasy, or decreased tolerance on the part of the patient. Serious adverse experiences are usually systemic in nature. The following types are most commonly reported:

Central nervous system

CNS manifestations are excitatory and/or depressive and may be characterized by dizziness, nervousness, apprehension, euphoria, confusion, dizziness, drowsiness, tinnitus, blurred or double vision, vomiting, feeling hot, cold or numb, spasms, tremors, seizures , loss of consciousness. , respiratory depression and arrest. Excitatory manifestations may be very brief or may not occur at all, in which case the first manifestation of toxicity may be drowsiness mixed with unconsciousness and respiratory arrest.

Drowsiness after prilocaine administration is usually an early sign of an elevated blood level of the drug and may occur as a result of rapid absorption.

sistema cardiovascular

Cardiovascular manifestations are usually depressive and characterized by bradycardia, hypotension and cardiovascular collapse, which can lead to cardiac arrest.

Signs and symptoms of depressed cardiovascular function are often the result of a vasovagal reaction, especially if the patient is upright. Less often, they can result from a direct effect of the drug. Failure to recognize premonitory signs such as sweating, fainting, pulse or sensory changes can lead to progressive cerebral hypoxia and seizures or severe cardiovascular catastrophe. Management consists of placing the patient in a supine position and ventilation with oxygen. Supportive treatment of circulatory depression may require administration of intravenous fluids and, where appropriate, a vasopressor (eg, ephedrine), as indicated by the clinical situation.

Allergic

Allergic reactions are characterized by skin lesions, hives, edema or anaphylactoid reactions. Allergic reactions resulting from sensitivity to prilocaine are extremely rare and, if they occur, must be treated by conventional means. Sensitivity detection by skin testing is of questionable value.

neurological

The incidences of adverse reactions (eg, persistent neurological deficits) associated with the use of local anesthetics may be related to the technique used, the total dose of local anesthetic administered, the specific drug used, the route of administration and physical condition. of the patient

Drug interactions

DRUG INTERACTIONS

Clinically significant drug interactions

Patients receiving local anesthetics are at increased risk of developing methemoglobinemia when concurrently exposed to the following medications, which may include other local anesthetics:

Examples of Medications Associated with Methemoglobinemia

Concomitant administration of vasopressor drugs and ergot-type oxytocic drugs may cause severe and persistent hypertension or cerebrovascular accidents.

Interactions between drugs and laboratory tests

Intramuscular injection of prilocaine may result in an increase in creatine kinase levels. Therefore, the use of this enzymatic determination, without separation of isoenzymes, as a diagnostic test for the presence of acute myocardial infarction may be compromised by the intramuscular injection of prilocaine.

Notices

NOTICES

DENTAL PROFESSIONALS WHO USE LOCAL ANESTHETICS MUST BE QUALIFIED IN THE DIAGNOSIS AND TREATMENT OF EMERGENCIES THAT MAY RESULT FROM THEIR USE. RESUSCITATION EQUIPMENT, OXYGEN AND OTHER RESUSCITATION MEDICINES MUST BE AVAILABLE FOR IMMEDIATE USE.

Metahemoglobinemia

Cases of methemoglobinemia have been reported in association with the use of local anesthetics. Although all patients are at risk for methemoglobinemia, patients with glucose-6-phosphate dehydrogenase deficiency, congenital or idiopathic methemoglobinemia, cardiac or pulmonary involvement, children younger than 6 months of age, and concomitant exposure to oxidizing agents or their metabolites are more susceptible. . develop clinical manifestations of the disease. 🇧🇷 If local anesthetics are to be used in these patients, close monitoring for signs and symptoms of methemoglobinemia is recommended.

Signs of methemoglobinemia may occur immediately or take several hours after exposure and are characterized by cyanotic discoloration of the skin and/or abnormal blood coloration. Methemoglobin levels may continue to rise; therefore, immediate treatment is required to avoid more serious cardiovascular and central nervous system adverse effects, including seizures, coma, arrhythmias, and death. Discontinue CITANEST and any other oxidizing agents. Depending on the severity of signs and symptoms, patients may respond to supportive care, i.e. oxygen therapy, hydration. A more severe clinical presentation may require treatment with methylene blue, exchange transfusion, or hyperbaric oxygen.

To minimize the likelihood of an intravascular injection, aspiration should be performed prior to injecting the local anesthetic solution. If blood is aspirated, the needle should be repositioned until aspiration does not produce blood return. Note, however, that the absence of blood in the syringe does not guarantee that intravascular injection will be avoided.

Precautions

PRECAUTIONS

Generally

The safety and effectiveness of prilocaine depend on proper dosage, correct technique, proper precautions and emergency preparedness. Standard textbooks should be consulted for specific techniques and precautions for various regional anesthetic procedures. Resuscitation equipment, oxygen and other resuscitation drugs must be available for immediate use. (To seeNOTICESyADVERSE REACTIONS.) The lowest dose that results in effective anesthesia should be used to avoid high plasma levels and serious adverse effects. Repeated doses of prilocaine can cause significant increases in blood levels with each repeated dose due to the slow accumulation of the drug or its metabolites. Tolerance to elevated blood levels varies depending on the patient's condition. Debilitated, elderly, acutely ill patients and children should receive reduced doses according to their age and physical condition. Prilocaine should also be used with caution in patients with severe shock or heart block.

Cardiovascular and respiratory vital signs (adequacy of ventilation) and the patient's state of consciousness should be monitored after each local anesthetic injection. Restlessness, anxiety, tinnitus, dizziness, blurred vision, tremors, depression, or drowsiness should alert the physician to the possibility of central nervous system toxicity. Signs and symptoms of depressed cardiovascular function are often the result of a vasovagal reaction, particularly if the patient is upright. (To seeADVERSE REACTIONS,sistema cardiovascular).

As amide-type local anesthetics are metabolized by the liver, prilocaine should be used with caution in patients with liver disease.

Patients with severe liver disease, due to their inability to metabolize local anesthetics normally, are at increased risk of developing toxic plasma concentrations. Prilocaine should also be used with caution in patients with impaired cardiovascular function, as they may not be able to compensate for the functional changes associated with prolonged A-V conduction produced by these drugs.

Many drugs used during conduction anesthesia are considered potential triggers for familial malignant hyperthermia. As it is not known whether amide-type local anesthetics can trigger this reaction and as the need for additional general anesthesia cannot be predicted in advance, it is suggested that a standard be used. the protocol for the management of malignant hyperthermia must be available. The first unexplained signs of tachycardia, tachypnea, unstable blood pressure, and metabolic acidosis may precede the temperature rise. Successful outcome depends on early diagnosis, prompt discontinuation of suspected precipitating agents, and institution of treatment, including oxygen therapy, indicated supportive measures, and dantrolene (see IV dantrolene sodium package insert before use).

Prilocaine should be used with caution in people with known drug sensitivity. Patients allergic to para-aminobenzoic acid derivatives (procaine, tetracaine, benzocaine, etc.) did not show cross-sensitivity to prilocaine.

Use on the head and neck area.

Small doses of local anesthetics injected into the head and neck area, including retrobulbar, dental, and stellate ganglion blocks, can produce adverse reactions similar to the systemic toxicity seen with unintentional intravascular injections of higher doses. Confusion, seizures, respiratory depression and/or respiratory arrest, and cardiovascular stimulation or depression have been reported. These reactions may be due to intra-arterial injection of the local anesthetic with retrograde flow into the cerebral circulation. Patients receiving these blocks must monitor their circulation and breathing and be constantly observed. Resuscitation equipment and personnel to manage adverse reactions should be immediately available. Dosage recommendations should not be exceeded. (To seeDOSAGE AND ADMINISTRATION.)

information for patients

Inform patients that the use of local anesthetics can cause methemoglobinemia, a serious condition that must be treated immediately. Advise patients or caregivers to seek immediate medical attention if they or someone under their care has the following signs or symptoms: pale, gray, or bluish skin (cyanosis); headache; elevated heart rate; difficulty breathing; stun; or fatigue.

The patient should be informed about the possibility of temporary loss of sensitivity and muscle function after infiltration injections or nerve blocks.

The patient should be advised to consult a dentist if anesthesia persists or if a rash develops.

Carcinogenesis, Mutagenesis, Impairment of Fertility

Animal studies of prilocaine have not been performed to evaluate carcinogenic and mutagenic potential or effect on fertility.

Chronic oral toxicity studies of orthotoluidine, a metabolite of prilocaine, in mice (150 to 4800 mg/kg) and rats (150 to 800 mg/kg) have shown that orthotoluidine is a carcinogen in both species. The lowest dose corresponds to approximately 50 times the maximum amount of orthotoluidine that a 50 kg individual would be expected to be exposed to after a single injection (8 mg/kg) of prilocaine.

Orthotoluidine (0.5 mg/mL) showed positive results inEscherichia coli DNA repairyI do- induction tests. Urine concentrates from rats treated withHorta-toluidina(300 mg/kg, orally) were mutagenic toSalmonella typhimuriumwith metabolic activation. Various other tests, including reverse mutations in five differentSalmonella typhimuriumstrains with or without metabolic activation and single-strand breaks in the DNA of Chinese hamster V79 cells were negative.

use in pregnancy

teratogenic effects

Pregnancy Category B. Reproduction studies have been performed in rats at doses up to 30 times the human dose and have revealed no evidence of impaired fertility or harm to the fetus due to prilocaine. However, there are no adequate and well-controlled studies in pregnant women. Animal reproduction studies do not always predict human response. This fact should be taken into account before administering prilocaine to women of childbearing potential, especially during the early stages of pregnancy when maximum organogenesis occurs.

lactating mothers

It is not known whether this drug is excreted in human milk. As many drugs are excreted in human milk, care should be taken when administering prilocaine to lactating women.

pediatric use

Doses in children should be reduced according to age, body weight and physical condition. (To seeDOSAGE AND ADMINISTRATION.)

clinical pharmacology

CLINICAL PHARMACOLOGY

Mechanism of action

Prilocaine stabilizes the neuronal membrane by inhibiting the ionic fluxes necessary for the initiation and conduction of impulses, thus exerting a local anesthetic action.

Start and duration of action

When used for infiltration injection in dental patients, the onset time of anesthesia averages less than 2 minutes, with an average duration of soft tissue anesthesia of approximately 2 hours.

Based on electrical stimulation studies, CitanestPlain 4% Dental Injection provides a duration of pulpal anesthesia of approximately 10 minutes in maxillary infiltration injections. In clinical studies, it has been found to provide complete anesthesia for procedures lasting an average of 20 minutes.

when used toinferior alveolar nerve block, The time to onset of a single dental injection of Citanest 4% is on average less than three minutes, with an average duration of soft tissue anesthesia of approximately 2.5 hours.

hemodynamics

Excessive blood levels can cause changes in cardiac output, total peripheral resistance, and mean arterial pressure. These changes can be attributed to a direct depressant effect of the local anesthetic agent on various components of thesistema cardiovascular.

Pharmacokinetics and Metabolism

Information derived from various formulations, concentrations and uses reveals that prilocaine is completely absorbed afterparenteraladministration depending on its rate of absorption, for example, on factors such as the site of administration and the presence or absence of a vasoconstrictor agent. Prilocaine is metabolized in the liver and kidneys and is excreted by the kidneys. It is not metabolized by plasmaesterases. Hydrolysis of prilocaine by amidases produces ortho-toluidine and N-propylalanine. Both compounds can undergo ring hydroxylation.

It has been found that O-toluidine producesmetahemoglobina, both in vitro and in vivo (verADVERSE REACTIONS).

As prilocaine is metabolized in both the liver and the kidneys, hepatic and renal dysfunction may impair prilocaine administration.kinetics.

As with other local anesthetic agents, plasma binding of prilocaine may depend on drug concentration. At 0.5 to 1.0 mg/mL, it is 55% protein bound.

Prilocaine crosses the blood-brain and placental barriers, presumably by passive diffusion.

factors likeacidosisand the use of CNS stimulants and depressants affects the CNS levels of prilocaine required to produce systemic effects. In the rhesus monkey, arterial blood levels of 20 mg/mL have been shown to be the threshold for seizure activity.

medication guide

PATIENT INFORMATION

No information provided. please consultNOTICESyPRECAUTIONSSections.