Instillagel (Lidocaine and chlorhexidine) for Urethral Procedures

Instillagel (Lidocaine and chlorhexidine) is used as a lubricant and a local anesthetic before major and minor urological procedures such as urinary catheterization and cystoscopy. It also is helpful in the prevention of infection that may occur during the procedure owing to the chlorhexidine antiseptic properties.

Lidocaine and chlorhexidine Uses:

Note: Not approved in the US

  • Local anesthetic, lubricant, and antiseptic:

    • It is used inside the urethra before a urological procedure such as urinary catheterization, cystoscopy, ultrasound, and other procedures for lubrication, prevention of sepsis, and as a local anesthetic.

Instillagel (Lidocaine and chlorhexidine) dose in Adults:

Instillagel (Lidocaine and chlorhexidine) dose as an anesthetic, lubricant, and antiseptic prior to a urologic procedure:

Note: Total lidocaine dose should be considered with concomitant use of other lidocaine-containing agents.

  • Intraurethral:

    • Females:

      • Before the procedure, fill the urethra by instilling about 6 mL of the drug in small portions.
      • Some gel may also be deposited on the orifice and covered with a cotton swab if desired.
      • A maximum of 4 doses per 24- hour period should be used.
    • Males:

      • The dose may vary depending on the procedure.
      • Instill about 6 to 22 mL of the medicine before the procedure.
      • Up to 39 mL in 3 to 4 portions may be instilled into the urethra in patients when a greater anesthetic effect is desired as in patients undergoing cystoscopy or ultrasound prior to the procedure. A maximum of 4 doses per 24-hour period should be used.

Instillagel (Lidocaine and chlorhexidine) dose in Children:

Instillagel (Lidocaine and chlorhexidine) Dose as an anesthetic, lubricant, and antiseptic prior to a urologic procedure:

Note: The 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 for every 10 kgs. Avoid administering more than 4 doses per 24-hour period.
    • Children ≥12 years and Adolescents:

      • The manufacturer recommends using the drug according to the physical condition of the patient and body weight. The maximum recommended dose is four doses per 24 hours.

Dose in Pregnancy & lactation

For use of instillagel during breastfeeding and lactation, see individuals agents: Lidocaine and Chlorhexidine.


Dose in Kidney Disease:

No dosage adjustment is necessary.

Dose in Liver disease:

There are no dosage adjustments provided in the manufacturer's labeling. Since lidocaine is metabolized in the liver, use it with caution.


Side effects

See individual agents (Lidocaine and chlorhexidine) for side effects of Instillagel.


Contraindications to Instillagel (Lidocaine and chlorhexidine):

Allergies to local anesthetics, whether amide-type or chlorhexidine, can occur in any component of the formulation.

Warnings and precautions

  • Hypersensitivity: [Canadian boxed warning]

    • Chlorhexidine can cause serious allergic reactions, including hypotension, anaphylaxis and shortness of breath.
    • The intraurethral and topical application can cause allergic reactions.
    •  It is important to stop the treatment immediately and that patients be treated promptly if they develop symptoms or clinical signs of allergic reaction.
  • Malignant hyperthermia

    • It is possible to develop malignant hyperthermia from its use.
    •  It is important to have the protocol and treatment for malignant hyperthermia.
  • Systemic adverse reactions:

    • Systemic toxicities can occur when the drug has been used too often or is applied to inflamed skin.
    • Patients who are acutely ill, elderly or children, may be at greater risk for developing systemic toxicities.
    • Patients at high risk may need to be given the lowest possible dose.
  • Cardiovascular disease

    • The AV (atrioventricular conduction) may be prolonged by using an ide anesthetic. Patients with heart disease should not use it.
  • Hepatic impairment

    • Patients with hepatic impairment need to be cautious.
  • Renal impairment

    • Patients with impaired kidney function should be cautious.
  • Seizures:

    • Patients who have had seizures in the past should be cautious.
  • Sepsis:

    • Patients with sepsis should use it with caution, as systemic absorption can occur quickly. It may be necessary to reduce the dosage.
  • Surprise!

    • Patients in severe shock should not take the drug.

Lidocaine and chlorhexidine (United States: Not available): Drug Interaction

Risk Factor C (Monitor therapy)

Antiarrhythmic Agents (Class III)

Lidocaine (Topical) may enhance the arrhythmogenic effect of Antiarrhythmic Agents (Class III). Antiarrhythmic Agents (Class III) may increase the serum concentration of Lidocaine (Topical). This mechanism specifically applies to amiodarone and dronedarone.

Aprepitant

May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors).

Beta-Blockers

May increase the serum concentration of Lidocaine (Topical).

Clofazimine

May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors).

CYP3A4 Inhibitors (Moderate)

May decrease the metabolism of CYP3A4 Substrates (High risk with Inhibitors).

Dapsone (Topical)

May enhance the adverse/toxic effect of Methemoglobinemia Associated Agents.

Disopyramide

May enhance the arrhythmogenic effect of Lidocaine (Topical). Disopyramide may increase the serum concentration of Lidocaine (Topical). Specifically, the unbound/free fraction of lidocaine.

Duvelisib

May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors).

Erdafitinib

May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors).

Fosaprepitant

May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors).

Fosnetupitant

May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors).

Larotrectinib

May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors).

Local Anesthetics

Methemoglobinemia Associated Agents may enhance the adverse/toxic effect of Local Anesthetics. Specifically, the risk for methemoglobinemia may be increased.

Methemoglobinemia Associated Agents

May enhance the adverse/toxic effect of Local Anesthetics. Specifically, the risk for methemoglobinemia may be increased.

Netupitant

May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors).

Nitric Oxide

May enhance the adverse/toxic effect of Methemoglobinemia Associated Agents. Combinations of these agents may increase the likelihood of significant methemoglobinemia.

Palbociclib

May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors).

Prilocaine

Methemoglobinemia Associated Agents may enhance the adverse/toxic effect of Prilocaine. Combinations of these agents may increase the likelihood of significant methemoglobinemia. Management: Monitor patients for signs of methemoglobinemia (e.g., hypoxia, cyanosis) when prilocaine is used in combination with other agents associated with development of methemoglobinemia. Avoid lidocaine/prilocaine in infants receiving such agents.

Simeprevir

May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors).

Sodium Nitrite

Methemoglobinemia Associated Agents may enhance the adverse/toxic effect of Sodium Nitrite. Combinations of these agents may increase the likelihood of significant methemoglobinemia.

Risk Factor D (Consider therapy modification)

CYP3A4 Inhibitors (Strong)

May decrease the metabolism of CYP3A4 Substrates (High risk with Inhibitors).

MiFEPRIStone

May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Management: Minimize doses of CYP3A4 substrates, and monitor for increased concentrations/toxicity, during and 2 weeks following treatment with mifepristone. Avoid cyclosporine, dihydroergotamine, ergotamine, fentanyl, pimozide, quinidine, sirolimus, and tacrolimus.

Stiripentol

May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Management: Use of stiripentol with CYP3A4 substrates that are considered to have a narrow therapeutic index should be avoided due to the increased risk for adverse effects and toxicity. Any CYP3A4 substrate used with stiripentol requires closer monitoring.

Risk Factor X (Avoid combination)

Conivaptan

May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors).

Fusidic Acid (Systemic)

May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors).

Idelalisib

May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors).

 

Monitoring parameters:

None mentioned.


How to administer Instillagel (Lidocaine and chlorhexidine)?

  • A small amount of the gel is gradually instilled into your urethra approximately 5-10 minutes before any less invasive procedures such as urethral catheterization or 10-12 minutes before any invasive procedures such as cystoscopy.
  • For males, cover the whole urethral area, including the external sphincter.
  • Press the glans to produce a local anesthetic. Females should instill the gel in their urethra, then deposit some gel on the orifice.
  • Cover the area with a cotton swab. You should throw away any gel that is not used. Avoid eye contact.
"Do not administer parenterally"

Mechanism of action of Instillagel (Lidocaine and chlorhexidine):

Lidocaine:

  • Lidocaine inhibits nerve conduction by decreasing neuronal membrane permeability to sodiumions.
  • This results in inhibition of depolarization. It blocks both the conduction and initiation of nerve impulses.

Chlorhexidine:

  • It contains a cationic molecular that binds to negatively charged bacterial cell walls.
  • It acts as a bacteriostatic agent by altering the bacterial cell equilibrium and causing the release of potassium and phosphorus when administered at a low dose.
  • It can cause the precipitation and death of bacterial cells when taken in high doses.

See individual agents: Lidocaine and Chlorhexidine.


International Brand Names of Lidocaine and chlorhexidine:

  • Instillagel
  • Angiocine
  • Bonca
  • Buccoseptine
  • Cathejell
  • Cathejell mit lidocain
  • Cathejell with Lidocaine
  • Catherjell con Lidocaina
  • Collunosol-N
  • Endogel Esteril
  • Gardimax
  • Golaseptine-Lidocaine
  • Instillagel
  • Lidocaine C
  • Lidogel
  • Naticaine
  • Trachisan Sore Throat

Lidocaine and chlorhexidine Brand Names in Pakistan:

Brands Available in Pakistan will be posted later.