Topical gel TRADE NAME: Ultracaine gel COMPOSITION: Each 1 gm gel contains : Active ingredient: Lidocaine (base) 0.05 gm Excipients: Propylene glycol, oleic acid, Carbopol 934, Triethanolamine, Deionized water. PHARMACEUTICAL FORM: Topical Gel. Colorless transparent smooth homogenous gel free from lumps & foreign matter. INDICATIONS: Topical anaesthetic for the temporary relief of pain and itching due to anorectal disorders. DOSAGE AND ADMINISTRATION: ● When practical, clean area with mild soap and warm water and rinse thoroughly ● Gently dry by patting or blotting with toilet tissue or soft cloth before applying ● Adults and children 12 years old and older: Apply externally to the affected area up to 6 times a day ● Children under 12 years of age: consult a doctor. CONTRAINDICATIONS: Known history of hypersensitivity to local anaesthetics of the amide type, or other components of the gel. WARNINGS AND PRECAUTIONS: For external use only Flammable Keep away from sparks, heat and fire. Cap tube tightly when not in use. When using this product ● avoid contact with eyes ● do not use in large quantities, particularly over raw surfaces or blistered areas ● do not put in rectum ● do not exceed recommended dosage unless directed by a doctor Stop use and ask a doctor if: ● allergic reaction occurs ● rectal bleeding occurs ● condition worsens or does not improve within 7 days ● symptoms clear up and return within a few days ● redness, irritation, swelling, pain or other symptoms begin or increase. Ultracaine gel contains 500mg Propylene glycol per 1g of the gel, which may cause skin irritation. Do not use this medicine in babies less than 4 weeks old with open wounds or large areas of broken or damaged skin (such as burns) without talking to your doctor or pharmacist. Keep out of the reach of children INTERACTIONS WITH OTHER MEDICINES AND OTHER FORMS OF INTERACTION Lidocaine should be used with caution in patients receiving agents structurally related to local anaesthetics, since the toxic effects are additive. Specific interaction studies with Lidocaine and anti-arrhythmic drugs class III (e.g. amiodarone) have not been performed, but caution when treating patients is advised. Medicines that reduce the clearance of Lidocaine (e.g. cimetidine or betablockers) may cause potentially toxic plasma concentrations when Lidocaine is given in repeated high doses over a long period of time. Such interactions should be of no clinical importance following short term treatment with Lidocaine at recommended doses. FERTILITY, PREGNANCY AND LACTATION It is reasonable to assume that a large number of pregnant women and women of child-bearing age have been given Lidocaine. No specific disturbances to the Xylocaine Jelly - Data Sheet Page 4 of 7 reproductive process have so far been reported, e.g. no increased incidence of malformations. Like other local anaesthetics, Lidocaine may enter the mother's milk, but in such small amounts that there is generally no risk of this affecting the neonate. EFFECTS ON ABILITY TO DRIVE AND USE MACHINES Depending on the dose, local anaesthetics may have a very mild effect on mental function and may temporarily impair locomotion and co-ordination. UNDESIRABLE EFFECTS: Allergic Reactions Allergic reactions (in most severe instances anaphylactic shock) to local anaesthetics of the amide type are rare (<1/1000). Acute Systemic Toxicity Lidocaine may have acute toxic effects if high systemic levels occur due to fast absorption or overdosage. If swallowed, get medical help or contact a Poison Control Center right away. Reporting of suspected adverse reactions: • Reporting suspected adverse reactions after authorisation of the medicinal product is important. It allows continued monitoring of the benefit/risk balance of the medicinal product. Healthcare professionals are asked to report any suspected adverse reactions via: • e-mail for reporting: pv.followup@edaegypt.gov.eg • Website for reporting: www.edaegypt.gov.eg • Hotline: 15301 • Scan QR code: PHARMCOLOGICAL PROPERTIES Pharmacodynamic properties Lidocaine provides prompt and profound anaesthesia of mucous membranes and lubrication which reduces friction. Its water-miscible base, characterised by high viscosity and low surface tension, brings the anaesthetic into intimate and prolonged contact with the tissue, giving effective anaesthesia of long duration (approximately 20-30 minutes). Anaesthesia usually occurs rapidly (within 5 minutes, depending upon the area of application). Lidocaine , like other local anaesthetics, causes a reversible blockade of impulse propagation along nerve fibres by preventing the inward movement of sodium ions through the nerve membrane. Local anaesthetics of the amide type are thought to act within the sodium channels of the nerve membrane. Local anaesthetic drugs may also have similar effects on excitable membranes in the brain and myocardium. If excessive amounts of drug reach the systemic circulation rapidly, symptoms and signs of toxicity will appear, emanating from the central nervous and cardiovascular systems. Central nervous system toxicity usually precedes the cardiovascular effects as it occurs at lower plasma concentrations. Direct effects of local anaesthetics on the heart include slow conduction, negative inotropism and possibly cardiac arrest. 5.2 Pharmacokinetic properties Lidocaine is absorbed following topical administration to mucous membranes, its rate and extent of absorption being dependent upon concentration and the total dose administered, the specific site of application, and the duration of exposure. In general, the rate of absorption of local anaesthetic agents following topical application is most rapid after intratracheal and bronchial administration. Lidocaine is also well-absorbed from the gastrointestinal tract, although little intact drug appears in the circulation because of biotransformation in the liver. Normally about 65% of the lidocaine is bound to plasma proteins. Amide local anaesthetics are mainly bound to alpha-1-acid glycoprotein but also to albumin. Lidocaine crosses the blood-brain and placental barriers, presumably by passive diffusion. The main elimination pathway of lidocaine is by liver metabolism. The primary route of lidocaine in human is N-dealkylation to monoethylglycine xylidine EGX), followed by hydrolysis to 2,6-xylidine and hydroxylation to 4-hydroxy-2,6-xylidine. MEGX can also be further dealkylated to glycine xylidine (GX). The pharmacological/toxicological actions of MEGX and GX are similar to, but less potent than, those of lidocaine . GX has a longer half-life (about 10 hours) than lidocaine and may accumulate during long-term administration. Approximately 90% of the lidocaine administrated intravenously is excreted in the form of various metabolites, and less than 10 % is excreted unchanged in the urine. The primary metabolite in urine is a conjugate of 4-hydroxy-2,6-xylidine, accounting for about 70-80% of the dose excreted in the urine. The elimination half-life of lidocaine following an intravenous bolus injection is typically 1.5 to 2.0 hours. Because of the rapid rate at which lidocaine is metabolised, any condition that affects liver function may alter lidocaine kinetics. The half-life may be prolonged two-fold or more in patients with liver dysfunction. Renal dysfunction does not affect lidocaine kinetics but may increase the accumulation of metabolites. Factors such as acidosis and the use of CNS stimulants and depressants affect the CNS levels of lidocaine required to produce overt systemic effects. Objective adverse manifestations become increasingly apparent with increasing venous plasma levels above 6.0 µg free base per mL. STORAGE : Store in a temperature not exceeding 30°C, in a dry place. Shelf-life: 36 months. PACKAGE : Carton box containing aluminum metallic tube of 20 gm or 30 gm gel with white opaque (HDPE) plastic screw cap with aluminum membrane + inner leaflet.
