Xyloproct (Lidocaine and Hydrocortisone) Cream

Xyloproct (Lidocaine and hydrocortisone) cream is a combination of a local anesthetic - lidocaine (lignocaine) - and a topical corticosteroid (hydrocortisone). It is used to relieve inflammation, itching, redness, and local signs of inflammation as may occur in patients with hemorrhoids.

Lidocaine and hydrocortisone Uses:

As an anti-inflammatory and anesthetic:
- It is indicated topically for the symptomatic relief of pruritus, pruritic eczema, insect bites, and burns.
- It is also used inside the rectum to relieve pain, itching, soreness, and discomfort due to hemorrhoids, anal fissure, anal pruritus, vulval pruritus, and other similar conditions of the mucous membranes.

Xyloproct (Lidocaine and hydrocortisone) Dose in Adults:

Xyloproct (Lidocaine and hydrocortisone) Dose as an anti-inflammatory/ anesthetic agent:

Topical: Apply two times a day
Rectal: One applicatorful two times a day.

Use in Children:

Refer to adult dosing.

Pregnancy Risk Factor C

In pregnant animals and humans, the combination of hydrocortisone/lidocaine was not studied.
Hydrocortisone or Lidocaine?

Use of hydrocortisone and lidocaine during lactation

It is unknown if the drug will be excreted into breastmilk.
It is recommended that you use it with caution if you are breastfeeding.
Hydrocortisone or Lidocaine are available from individual agents.

Dose in Kidney Disease:

There are no dosage adjustments provided in the manufacturer's labeling.

Dose in Liver disease:

There are no dosage adjustments provided in the manufacturer's labeling.

Side effects of Xyloproct (Lidocaine and hydrocortisone):

See individual agents: Hydrocortisone and Lidocaine

Contraindications to Xyloproct (Lidocaine and hydrocortisone):

Allergies to hydrocortisone, lidocaine, hydrocortisone and local anesthetics (amide type), corticosteroids or any component of formulation
Fungal lesions
Tuberculosis
Varicella infection, skin vaccinia and acute herpes sox infections are all possible.

Warnings and precautions

Contact dermatitis:
- It is possible for patients to develop allergic contact dermatitis.
- This condition can be difficult to diagnose. If the lesions don't heal, it is a sign that allergic contact dermatitis has occurred.
Hypersensitivity
- Some patients may experience allergic reactions to the drug.
- There may be fatal anaphylactic reactions.
- Patients who are allergic to the derivatives of para-aminobenzoic acids have not been observed to experience any cross-reactions when using lidocaine (eg, procaine or tetracaine)
Kaposi Sarcoma:
- Literature has reported cases of Kaposi's Sarcoma after prolonged topical corticosteroids use.
- Patients who suspect that they have lesions should be stopped from receiving topical corticosteroids and investigated.
Local effects
- At the application site, local responses like skin sensitivity, irritation, and infection are possible.
- Local reactions should be stopped immediately and the appropriate treatment instituted.
Methemoglobinemia:
- Methemoglobinemia can be caused by the use of local anaesthetics.
- This may lead to severe reactions that require treatment discontinuation and/or other oxidizing agents. It is important to immediately start the appropriate treatment.
- Methemoglobinemia can occur immediately or after several hours of prolonged exposure to anesthetics.
- Patients who are at high risk should be regularly watched for methemoglobinemia-related signs and symptoms including cyanosis (tachycardia), headaches, shortness of breath, lethargy, and lightheadedness.
- Patients with methemoglobinemia are at high risk for:
  - Infants younger than six months
  - Individuals with a G6PD deficiency
  - Pulmonary and cardiac compromise
  - Methemoglobinemia is idiopathic and congenital
  - Patients with oxidising agent exposure, their metabolites
Systemic effects
- When corticosteroids are applied topically, they may be absorbed into your systemic circulation.
- Topical corticosteroid use for an extended period of time may cause reversible suppression of the hypothalamic-pituitary-adrenal axis, Cushing syndrome, hyperglycemia, or glycosuria. Suppression of HPA may lead to an adrenal crisis.
- If:
  - Occlusive dressings can be used.
  - Apply the cream/ointment to irritated, fissured or abraded skin.
  - The ointment can be used for a long time or is disposable.
  - The medicine can be applied to large or extensive areas.
- Patients who are debilitated or acutely ill have a higher risk of developing systemic toxicities.
Hepatic impairment
- Hepatic impairment patients should use it cautiously.

Lidocaine and hydrocortisone: 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).
Calcipotriene	Calcipotriene's medicinal effects may be diminished by topical hydrocortisone. Management: If using hydrocortisone valerate in combination with calcipotriene, watch for diminished potency. To reduce the danger of this potential interaction, think about administering these drugs 10 to 12 hours apart.
Clofazimine	May elevate CYP3A4 substrates' serum concentration (High risk with Inhibitors).
Corticorelin	The therapeutic benefit of corticorelin may be reduced by corticosteroids. In particular, recent or ongoing corticosteroid medication may reduce the plasma ACTH response to corticorelin.
CYP3A4 Inhibitors (Moderate)	May slow down CYP3A4 substrate metabolism (High risk with Inhibitors).
Dapsone (Topical)	May intensify the harmful/toxic effects of agents associated with methemoglobinemia.
Deferasirox	Corticosteroids may intensify Deferasirox's negative/toxic effects. Particularly, there may be a higher risk of GI bleeding or ulcers.
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.
Ritodrine	Corticosteroids may enhance the adverse/toxic effect of Ritodrine.
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).
Hyaluronidase	The therapeutic benefit of hyaluronidase may be reduced by corticosteroids. Treatment: Standard doses of hyaluronidase may not produce the desired clinical response in patients using corticosteroids (especially at higher doses). Hyaluronidase may be needed at higher doses.
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: The 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)
Aldesleukin	Corticosteroids may diminish the antineoplastic effect of Aldesleukin.
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:

Monitor oxygenation and haemoglobin in patients who develop methemoglobinemia
Monitor the patient for opportunistic infections including fungal infections.
If the medication is taken for an extended period of time, keep an eye on the patients for the onset of Cushing's syndrome or hypothalamic pituitary adrenal axis suppression.

How to administer Xyloproct (Lidocaine and hydrocortisone)?

It is indicated for external use only. Avoid using inside the oral cavity, eyes, nose, or ears.

Topical Application:

Over the affected area, apply a thin coating.

Rectal:

Apply to the affected area gently (cleansing wipes may be used if provided). Attach the applicator to the tube and squeeze it until a small amount of the cream comes out of it.
Insert the applicator tip gently into the anal area and squeeze the tube until it is empty. Avoid inserting the tube deep into the anal canal or rectum.

Mechanism of action of Xyloproct (Lidocaine and hydrocortisone):

Lidocaine:

It blocks nerve conduction by preventing the initiation or conduction of neuronal impulses.
It reduces the permeability of the membrane to sodium ions, resulting in nerve conduction being blocked.

Hydrocortisone