Version July 2025
Anesthetic, lubricant, and antiseptic prior to urologic procedure: Note: Total lidocaine dose should be considered with concomitant use of other lidocaine-containing agents.
Females: Intraurethral: Instill 6 mL in small portions to fill whole urethra 5 to 10 minutes prior to procedure; may deposit some gel on the orifice and cover with cotton swab if desired. Maximum: 4 doses per 24-hour period.
Males:
Introduction of instruments into the urethra: Intraurethral: Instill 11 mL and some patients may require an additional 6 to 11 mL; when greater anesthetic effects are desired (eg, for ultrasound or cystoscopy), may instill up to 39 mL in 3 to 4 portions 10 to 12 minutes prior to procedure; maximum: 4 doses per 24-hour period.
Anterior urethra: Intraurethral: Instill 6 to 11 mL prior to procedure.
Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.
No dosage adjustment necessary.
There are no dosage adjustments provided in the manufacturer's labeling. Lidocaine undergoes hepatic metabolism; use with caution.
Refer to adult dosing; use with caution. Repeated doses may lead to increased systemic exposure and dose reductions may be necessary.
Anesthetic, lubricant, and antiseptic prior to urologic procedure: Note: Total lidocaine dose should be considered with concomitant use of other lidocaine-containing agents.
Intraurethral:
Children <12 years: Maximum lidocaine dose: 6 mg/kg or 3 mL per 10 kg. Do not administer more than 4 doses per 24-hour period.
Children ≥12 years and Adolescents: The manufacturer labeling recommends that the dose should correspond with the patient's weight and physical condition; maximum: 4 doses per 24-hour period
Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.
No dosage adjustment necessary.
There are no dosage adjustments provided in the manufacturer's labeling. Lidocaine undergoes hepatic metabolism; use with caution.
The following adverse drug reactions are derived from product labeling unless otherwise specified. Also see individual agents.
Postmarketing:
Hypersensitivity: Hypersensitivity reaction (including anaphylaxis) (Totty 2017)
Local: Local discomfort
Hypersensitivity to local anesthetics of the amide type, chlorhexidine, or any component of the formulation
Concerns related to adverse effects:
• Hypersensitivity: [Canadian Boxed Warning]: Serious hypersensitivity reactions including anaphylaxis, hypotension, tachycardia, shortness of breath, and erythema have been reported with use of chlorhexidine gluconate, including topical and/or intraurethral use. Discontinue use immediately in patients who develop hypersensitivity reactions.
• Malignant hyperthermia: Use may trigger familial malignant hyperthermia; a protocol for managing malignant hyperthermia should be available during use.
• Methemoglobinemia: Has been reported with local anesthetics; clinically significant methemoglobinemia requires immediate treatment along with discontinuation of the anesthetic and other oxidizing agents. Onset may be immediate or delayed (hours) after anesthetic exposure. Patients with glucose-6-phosphate dehydrogenase deficiency, congenital or idiopathic methemoglobinemia, cardiac or pulmonary compromise, exposure to oxidizing agents or their metabolites, or infants <6 months of age are more susceptible and should be closely monitored for signs and symptoms of methemoglobinemia (eg, cyanosis, headache, rapid pulse, shortness of breath, lightheadedness, fatigue).
• Systemic adverse effects: Application to broken or inflamed skin, excessive dosing, or short dosing intervals may lead to increased absorption and systemic toxicity; lowest effective dose should be administered. Children, individuals who are acutely ill, debilitated, and/or elderly patients may be at increased risk of systemic toxicity; dose reductions may be necessary.
Disease-related concerns:
• Cardiovascular disease: Use with caution in patients with cardiovascular disease due to the propensity of amide anesthetics to prolong A-V conduction.
• Hepatic impairment: Use with caution in patients with hepatic impairment.
• Renal impairment: Use with caution in patients with renal impairment.
• Seizures: Use with caution in patients with a history of seizures.
• Sepsis: Use with caution in septic patients due to potential for rapid systemic absorption; dose reduction may be necessary.
• Shock: Use with caution in patients with severe shock.
Other warnings/precautions:
• Appropriate use: [Canadian Boxed Warning]: For topical use only. Do not use parenterally. Avoid contact with eyes.
Not available in the US
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Gel, topical:
Instillagel: Lidocaine hydrochloride 2% and chlorhexidine gluconate 0.05% (6 mL, 11 mL)
Instill small portions of gel slowly into the urethra 5 to 10 minutes prior to less invasive procedure (eg, catheterization) and 10 to 12 minutes prior to more invasive procedures (eg, cystoscopy). In males, the entire urethral area including the external sphincter should be covered with gel and the glans compressed until a local anesthetic effect is achieved. In females, some gel may be deposited onto the orifice and covered with a cotton swab. Discard unused portion of gel. Do not administer parenterally. Avoid contact with eyes.
Intraurethral: Instill small portions of gel slowly into the urethra 5 to 10 minutes prior to less invasive procedure (eg, catheterization) and 10 to 12 minutes prior to more invasive procedures (eg, cystoscopy). In males, the entire urethral area including the external sphincter should be covered with gel and the glans compressed until a local anesthetic effect is achieved. In females, some gel may be deposited onto the orifice and covered with a cotton swab. Discard unused portion of gel. Do not administer parenterally. Avoid contact with eyes.
Note: Not approved in the US
Local anesthetic/lubricant/antiseptic: To provide local anesthesia, lubrication, and antisepsis during urologic procedures including catheterization, cystoscopy, ultrasound, or other intraurethral procedures.
ALERT: Canadian Boxed Warning: Health Canada-approved labeling includes a boxed warning. See Warnings/Precautions section for a concise summary of this information. For verbatim wording of the boxed warning, consult the product labeling.
Refer to individual components.
Note: Interacting drugs may not be individually listed below if they are part of a group interaction (eg, individual drugs within “CYP3A4 Inducers [Strong]” are NOT listed). For a complete list of drug interactions by individual drug name and detailed management recommendations, use the drug interactions program by clicking on the “Launch drug interactions program” link above.
Antiarrhythmic Agents (Class IB): Lidocaine (Topical) may increase adverse/toxic effects of Antiarrhythmic Agents (Class IB). Risk C: Monitor
Articaine: May increase adverse/toxic effects of Local Anesthetics. Risk C: Monitor
Cimetidine: May increase serum concentration of Lidocaine (Topical). Risk C: Monitor
Dapsone (Topical): May increase adverse/toxic effects of Methemoglobinemia Associated Agents. Risk C: Monitor
Local Anesthetics: Methemoglobinemia Associated Agents may increase adverse/toxic effects of Local Anesthetics. Specifically, the risk for methemoglobinemia may be increased. Risk C: Monitor
Methemoglobinemia Associated Agents: May increase adverse/toxic effects of Local Anesthetics. Specifically, the risk for methemoglobinemia may be increased. Risk C: Monitor
Nitric Oxide: May increase adverse/toxic effects of Methemoglobinemia Associated Agents. Combinations of these agents may increase the likelihood of significant methemoglobinemia. Risk C: Monitor
Prilocaine: Methemoglobinemia Associated Agents may increase adverse/toxic effects of Prilocaine. Combinations of these agents may increase the likelihood of significant methemoglobinemia. Management: Monitor for signs of methemoglobinemia when prilocaine is used in combination with other agents associated with development of methemoglobinemia. Avoid use of these agents with prilocaine/lidocaine cream in infants less than 12 months of age. Risk C: Monitor
Primaquine: Methemoglobinemia Associated Agents may increase adverse/toxic effects of Primaquine. Specifically, the risk for methemoglobinemia may be increased. Management: Avoid concomitant use of primaquine and other drugs that are associated with methemoglobinemia when possible. If combined, monitor methemoglobin levels closely. Risk D: Consider Therapy Modification
ROPivacaine: May increase adverse/toxic effects of Local Anesthetics. Risk C: Monitor
Sodium Nitrite: Methemoglobinemia Associated Agents may increase adverse/toxic effects of Sodium Nitrite. Combinations of these agents may increase the likelihood of significant methemoglobinemia. Risk C: Monitor
See individual agents.
See individual agents.
Lidocaine: Lidocaine blocks both the initiation and conduction of nerve impulses by decreasing the neuronal membrane's permeability to sodium ions, which results in inhibition of depolarization with resultant blockade of conduction.
Chlorhexidine: The bactericidal effect of chlorhexidine is a result of the binding of this cationic molecule to negatively charged bacterial cell walls and extramicrobial complexes. At low concentrations, this causes an alteration of bacterial cell osmotic equilibrium and leakage of potassium and phosphorous resulting in a bacteriostatic effect. At high concentrations of chlorhexidine, the cytoplasmic contents of the bacterial cell precipitate and result in cell death.
See individual agents.
