Xyloproct: Indications, Dosage, Precautions, Adverse Effects
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Xyloproct - Product Information

Manufacture: AstraZeneca
Country: Australia
Condition: Pain, Piles (Hemorrhoids)
Class: Anorectal preparations
Form: Cream, gel, liniment or balm, lotion, ointment, etc, Rectal
Ingredients: lignocaine base, hydrocortisone acetate, aluminium acetate, zinc, oxide, cetyl alcohol, stearyl alcohol, macrogol 400, macrogol 335 , purified water

(Lignocaine and hydrocortisone acetate)

Name of the Medicine

Xyloproct Ointment Contains lignocaine, a local anaesthetic and hydrocortisone acetate, a corticosteroid as active ingredients.

Chemical Structure:


Chemical Name: 2-(Diethylamino)-N-(2,6- dimethylphenyl)acetamide 11в,17-Dihydroxy-3,20- dioxopregn-4-en-21-yl acetate
Molecular Formula: C14H22N2O C23H32O6
Molecular Weight: 234.3 404.5
CAS: 137-58-6 50-03-3

Description

Lignocaine is a white or almost white, crystalline powder. Practically insoluble in water, very soluble in ethanol (96%) and in methylene chloride.

Hydrocortisone acetate is a white to almost white crystalline powder. Practically insoluble in water, slightly soluble in anhydrous ethanol and in methylene chloride.

Xyloproct Ointment is a white to slightly yellow, homogeneous ointment. Each gram contains lignocaine 50mg and hydrocortisone acetate 2.5mg as active ingredients. It also contains aluminium acetate, zinc oxide, cetyl alcohol, macrogols (3350 & 400), stearyl alcohol and purified water.

Pharmacology

Actions

Anti-inflammatory, anaesthetic, astringent. Hydrocortisone acetate is a corticosteroid.

Indications

Symptomatic relief of pain and irritation associated with haemorrhoids, anal fissure, pruritus ani, proctitis and for palliative use postoperatively. XYLOPROCT is intended for short-term palliative use only.

Contraindications

Children under 12 years; allergy to local anaesthetics of the amide type or to other components of the product; tuberculous, fungal or viral infections; traumatised mucosa and/or sepsis in anorectal region; concurrent oral or intravenous corticosteroid therapy. XYLOPROCT should not be used on atrophic skin.

Precautions

Preparations containing hydrocortisone should only be used in patients not responding to other forms of topical symptomatic treatment and in whom surgery is not feasible.

Prolonged and excessive use of topical corticosteroid preparations may lead to skin atrophy; this risk is reduced somewhat by including the minimal effective concentration of hydrocortisone in the formulation of XYLOPROCT.

If the condition for which XYLOPROCT is used persists, or if rash, irritation or rectal bleeding occurs, discontinue use. Although sensitivity to lignocaine is extremely rare, the possibility should not be overlooked and appropriate precautions observed. Not intended for prolonged use.

Excessive dosage of lignocaine or short intervals between doses, may result in high plasma levels of lignocaine and serious adverse effects. Patients should be instructed to strictly adhere to recommended dosage.

When applying XYLOPROCT ointment to the rectum by means of the special applicator, care should be taken to avoid the introduction of an excessive amount. Following rectal application the systemic availability is relatively high and large doses may result in central nervous system reactions.

XYLOPROCT should not be used until an adequate proctologic examination is completed to exclude malignant process.

XYLOPROCT is possibly porphyrinogenic and should only be prescribed to patients with acute porphyria when no safer alternative is available. Precautions are to be taken when XYLOPROCT is used in vulnerable patients.

Carcinogenic and Mutagenic Potential

Genotoxicity tests with lignocaine are inconclusive. In genotoxicity studies, a metabolite of lignocaine, 2,6-xylidine, showed evidence of activity in some tests but not in other tests. This metabolite has been shown to have carcinogenic potential (nasal and subcutaneous tumours) in preclinical toxicological studies evaluating chronic exposure.

Use in pregnancy

XYLOPROCT should be used with caution during the first trimester of pregnancy.

Use in lactation

Lignocaine and hydrocortisone acetate are excreted into breast milk in small amounts. Any effect on the nursing infant seems unlikely at therapeutic doses of XYLOPROCT.

Effects on ability to drive and operate machines

Depending on the dose local anaesthetics may have a very mild effect on mental function and co-ordination even in the absence of overt CNS toxicity and may temporarily impair locomotion and alertness. With recommended doses of XYLOPROCT adverse effects on the CNS are unlikely.

Interactions with other Medicines

With large doses of lignocaine, consideration should be given to the risk of additional systemic toxicity in patients receiving other local anaethetics or agents structurally related to local anaesthetics.

Adverse Effects

XYLOPROCT is well tolerated. It may be used in patients with a previous history of allergy to procaine and other para-aminobenzoic acid derivatives.

Contact sensitivity to lignocaine has been reported after perianal use and may also occur after the use of topical hydrocortisone.

The following local reactions after treatment with corticosteroids have been reported:

  • atrophy of the skin, often irreversible, with thinning of the skin, telangiectasia, purpura and striae
  • rosacea-like and perioral dermatitis, with or without atrophy of the skin
  • rebound-effect, which may cause dependency on steroids
  • slowing of the healing process

Dosage and Administration

Apply as directed by physician. Not more than 6 g to be used in a 24 hour period and not more than 7 days.

Overdosage

Symptoms

Overdosage may result in CNS excitation and/or depression, characterised by nervousness, dizziness, blurred vision and tremor and in cases of extreme toxicity, convulsions, coma, respiratory arrest and cardiovascular depression.

Treatment

Symptomatic treatment should be instituted.

Contact the Poisons Information Centre on 13 11 26 for advice on management.

Presentation and Storage Conditions

Xyloproct Ointment is packed in an aluminium tube with an outer carton in pack sizes of 15g, 20g & 35g.

Store at 2-8єC (Refrigerate – do not freeze).

Name and Address of the Sponsor

AstraZeneca Pty Ltd

ABN 54 009 682 311

Alma Road

NORTH RYDE NSW 2113

Poison Schedule of the Medicine

S2 – Pharmacy Medicine

Date of First Inclusion in the Australian Register of Therapeutic Goods

13 August 1991

Date of Most Recent Amendment

11 December 2013

XYLOPROCT® is a trade mark of the AstraZeneca group of companies.