Consumer medicine information

Instillagel Lido

Lidocaine (lignocaine) hydrochloride

BRAND INFORMATION

Brand name

Instillagel Lido

Active ingredient

Lidocaine (lignocaine) hydrochloride

Schedule

SUMMARY CMI

INSTILLAGEL LIDO

Consumer Medicine Information (CMI) summary

The full CMI on the next page has more details. If you are worried about using this medicine, speak to your doctor or pharmacist.

1. Why am I using INSTILLAGEL LIDO?

INSTILLAGEL LIDO contains the active ingredient lidocaine hydrochloride(as monohydrate). INSTILLAGEL LIDO is used for local anaesthesia.

For more information, see Section 1. Why am I using INSTILLAGEL LIDO? in the full CMI.

2. What should I know before I use INSTILLAGEL LIDO?

Do not use if you have ever had an allergic reaction to lidocaine hydrochloride or any of the ingredients listed at the end of the CMI.

Talk to your doctor if you have any other medical conditions, take any other medicines, or are pregnant or plan to become pregnant or are breastfeeding.

For more information, see Section 2. What should I know before I use INSTILLAGEL LIDO? in the full CMI.

3. What if I am taking other medicines?

Some medicines may interfere with INSTILLAGEL LIDO and affect how it works.

A list of these medicines is in Section 3. What if I am taking other medicines? in the full CMI.

4. How do I use INSTILLAGEL LIDO?

INSTILLAGEL LIDO is a sterile gel available in 6mL and 11mL pre filled syringes.

More instructions can be found in Section 4. How do I use INSTILLAGEL LIDO? in the full CMI.

5. What should I know while using INSTILLAGEL LIDO?

Things you should do	Remind any doctor, dentist or pharmacist you visit that you are using INSTILLAGEL LIDO. Use INSTILLAGEL LIDO as instructed by your doctor.
Things you should not do	Do not use more of this medicine than instructed by your doctor. Do not use if you are allergic to any of the ingredients or to local anaesthetics
Looking after your medicine	Store INSTILLAGEL LIDO at room temperature (below 25°C) away from direct heat, Do not refrigerate or freeze. INSTILLAGEL LIDO is for single use only. Use immediately after opening the blister. The syringe and any gel not used in a single application must be discarded.

For more information, see Section 5. What should I know while using INSTILLAGEL LIDO? in the full CMI.

6. Are there any side effects?

Some side effects that may occur include allergic reaction which may result in swelling of hands, feet, face, lips, mouth, tongue or throat, difficulties in breathing, skin rash or hives or a drop in blood pressure and shock. For more information, including what to do if you have any side effects, see Section 6. Are there any side effects? in the full CMI.

FULL CMI

INSTILLAGEL LIDO

Active ingredient(s): Lidocaine hydrochloride (as monohydrate) 2%w/w

Consumer Medicine Information (CMI)

This leaflet provides important information about using INSTILLAGEL LIDO. You should also speak to your doctor or pharmacist if you would like further information or if you have any concerns or questions about using INSTILLAGEL LIDO.

Where to find information in this leaflet:

1. Why am I using INSTILLAGEL LIDO?
2. What should I know before I use INSTILLAGEL LIDO?
3. What if I am taking other medicines?
4. How do I use INSTILLAGEL LIDO?
5. What should I know while using INSTILLAGEL LIDO?
6. Are there any side effects?
7. Product details

1. Why am I using INSTILLAGEL LIDO?

INSTILLAGEL LIDO contains the active ingredient lidocaine hydrochloride(as monohydrate) 2%w/w which has a local anaesthetic effect and is used to numb the parts of the body the gel is applied to. It stops the nerves from being able to pass pain messages to the brain and so stops you feeling pain.

INSTILLAGEL LIDO is used to relieve discomfort and ease the process during certain types of examinations or procedures.

for instillation (insertion) into the urethra before a catheter is inserted or replaced and for a cystoscopy, when a doctor inserts a tube through the urethra to visualise your bladder.
for proctoscopy/rectoscopy (medical procedures in which an instrument called an endoscope is used to examine the anal cavity or rectum). During this procedure, INSTILLAGEL LIDO is instilled into the anal cavity/rectum and/or the instrument used is lubricated with INSTILLAGEL LIDO before insertion

2. What should I know before I use INSTILLAGEL LIDO?

Warnings

Do not use INSTILLAGEL LIDO if:

you are allergic to lidocaine hydrochloride or any of the ingredients listed at the end of this leaflet.
if you are allergic to certain other local anaesthetics (of the amide type).
in children below 2 years of age.
Always check the ingredients to make sure you can use this medicine.

Check with your doctor if you:

if you have any wounds, injury to the mucous membranes or an ulcer/inflammation in or around the proposed application site.
if your liver or kidney function is impaired, if you are acutely ill, in a weak condition or have sepsis (“blood poisoning”). Your doctor may reduce your dose of Instillagel Lido
if you have a slow heartbeat, a heart or respiratory tract dysfunction (problems with your airways).
if you have a weak heart (heart failure) or heart conduction disturbances (atrioventricular block).
if you suffer from a medical shock.
if you are prone to convulsions (seizures) or if you have epilepsy.
if you are suffering from a certain muscle disease (myasthenia gravis).
if you have a rare inherited illness that affects the blood called ”glucose-6-phosphate dehydrogenase deficiency”.
if you have a problem with blood pigment levels called “methaemoglobinaemia”.
if you suffer from porphyria (a blood formation disorder).
if you are on treatment with certain medications to treat heart rhythm disorders, known as class III antiarrhythmics (e.g. amiodarone), as the effects on the heart may be increased. See also section 3. What if I am taking other medicines

Please also notify your doctor if you use other medicines containing lidocaine hydrochloride frequently and/or at high doses, as this may lead to serious side effects.

If a lot of INSTILLAGEL LIDO is instilled into the urethra and a large amount of gel gets into the bladder or if the urethra is ulcerous/inflamed, this may generally lead to increased absorption of lidocaine hydrochloride through the mucous membranes, particularly in children and elderly patients, resulting in serious side effects (see also section If you use too much INSTILLAGEL LIDO).

During treatment, you may be at risk of developing certain side effects. It is important you understand these risks and how to monitor for them. See additional information under Section 6. Are there any side effects?

Pregnancy and breastfeeding

Check with your doctor if you are pregnant or intend to become pregnant.

Talk to your doctor if you are breastfeeding or intend to breastfeed.

During pregnancy and breast-feeding INSTILLAGEL LIDO should only be used after your doctor has carefully considered the benefits and risks.

3. What if I am taking other medicines?

Tell your doctor or pharmacist if you are taking any other medicines, including any medicines, vitamins or supplements that you buy without a prescription from your pharmacy, supermarket or health food shop.

In particular, tell your doctor if you are taking/using any of the following:

antiarrhythmics - medicines to treat irregular heart beat (e.g. mexiletine, amiodarone).
calcium channel blockers - medicines taken for heart conditions or high blood pressure (e.g. diltiazem, verapamil).
beta-blockers (e.g. propranolol, metoprolol) - for the treatment of high blood pressure or angina (chest pain).
These medicines may have an enhanced effect on the heart.
other medicines containing lidocaine hydrochloride or certain other local anaesthetics (of the amide type), as this may enhance their respective effects in an unpredictable manner.
cimetidine to treat hyperacidity, stomach and duodenal ulcers. Using this medicine at the same time can increase the risk of side effects.
fluvoxamine to treat depression.
erythromycin (antibiotic).
protease inhibitors used to treat HIV (e.g ritonavir).
medicines used to treat infections, called sulphonamides and nitrofurantoin.
medicines used to treat epilepsy, called phenytoin and phenobarbital.

Check with your doctor or pharmacist if you are not sure about what medicines, vitamins or supplements you are taking and if these affect INSTILLAGEL LIDO.

4. How do I use INSTILLAGEL LIDO?

The administration will usually be performed by a doctor with appropriate training and relevant experience.

If you are treating yourself, such as for self-catheterisation (inserting a small plastic tube (catheter) into one's own urethra), always use this medicine exactly as your doctor has told you and follow the instructions below for how to apply the gel. Check with your doctor if you are not sure.

INSTILLAGEL LIDO starts to work within 5 - 15 minutes after the application. The effect usually lasts 20 to 30 minutes.

How much to use

Your doctor will decide on the most suitable dosage for your particular case according to your age and medical condition as well as for the site of application, the method used and your response.

The recommended dose is:

Adults

For instillation (insertion) into the urethra

Male patients

For adequate pain relief, 20 mL gel is usually required.

When anaesthesia is especially important, e.g., during sounding or cystoscopy, your doctor may instill a larger quantity of gel (up to 40 mL).

If you are treating yourself, such as for self-catheterisation, your doctor will tell you how much to use. Ask if you are not sure.

Female patients

The doctor will adapt the amount of gel to be inserted to the individual anatomical conditions of the urethra. Usually 5-10 mL of gel are instilled in small portions to fill the whole urethra.

For pain relief from inflammation of the urinary bladder
The doctor decides on the most suitable dose, frequency and duration based on your condition and symptoms.

Proctoscopy/rectoscopy
For adequate pain relief, your doctor will usually instill 10-20 mL gel into the anal cavity/rectum and will apply a small amount to lubricate the endoscope.

Special population

Your doctor may decide to reduce the dose if you are elderly, acutely ill, in a weak condition, if you have liver or kidney problems or if you have sepsis (“blood poisoning”).

Use in children and adolescents

Children < 2 years of age

INSTILLAGEL LIDO must not be used in children below 2 years of age.

Children (2 - 12 years) and adolescents (above 12 years of age)

The doctor will determine the dose depending on the child's age, weight and physical condition.

When to use INSTILLAGEL LIDO

The administration will usually be performed by a doctor with appropriate training and relevant experience.

For examinations/procedures INSTILLAGEL LIDO is usually only used for one or two doses or for a short course of treatment.

If you have been prescribed INSTILLAGEL LIDO for self-administration, your doctor will decide how long you should continue to use this medicine depending on your condition.

How to administer INSTILLAGEL LIDO

The pre-filled graduated syringes are available with 6 mL or 11 mL gel. Your doctor will choose the appropriate size depending on the amount you need.

Each graduation on the syringe is equivalent to approximately 1 mL of gel (20.1 mg lidocaine hydrochloride)

For (self-)catheterisation (urethral use)

Follow these directions carefully:

Wash your hands. Clean and disinfect the genital area.
When ready to use, open the blister.
Before removing the tip cap from the end of the syringe, press in the plunger to remove any resistance that may be present. This helps ensure that the syringe will empty easily and uniformly.[Picture 1]
Remove the tip cap from the syringe. The syringe is now ready for use. [Picture 2]
Insert the nozzle into the opening of the urethra and press the plunger slowly and evenly to push out the gel into the urethra. [Picture 3]
Wait for a few minutes after instillation of the gel for the anaesthetic to take full effect. Full anaesthetic effect will occur within 5 to 15 minutes after complete instillation.

For cystoscopy

Your doctor will administer this medicine in the urethra and/or apply it to the endoscope.

For proctoscopy/rectoscopy

Your doctor will administer this medicine in the anal cavity/rectum and/or apply it to the endoscope.

The syringe is for single use only. Use immediately after opening the blister.

The syringe and any gel not used in a single application must be discarded.

If you use too much INSTILLAGEL LIDO

Administration of INSTILLAGEL LIDO by a doctor

Since this medicine is usually administered to you by a trained doctor, it is unlikely that you will be given too much of INSTILLAGEL LIDO Nevertheless, if you think you have been given too much medicine or you begin to experience the overdose symptoms listed below, you must tell the person giving you INSTILLAGEL LIDO immediately. Your doctor will know how to manage these symptoms and give you any necessary treatment.

Administration of INSTILLAGEL LIDO by yourself or a caregiver for self-catheterisation

Whether you develop symptoms of an overdose or not depends on the level of this medicine present in your blood. The more lidocaine hydrochloride is in your blood, the more severely you might experience symptoms of an overdose. Normally only small amounts of the active ingredient lidocaine hydrochloride are absorbed into the blood INSTILLAGEL LIDO. Too much lidocaine hydrochloride can be absorbed if the surface being treated is damaged.

The first symptoms of overdose are for example:

problems with hearing, seeing, speaking and/or coordination of movements, yawning, restlessness, dizziness, nausea and vomiting.

If you think that you have used too much INSTILLAGEL LIDO you may need urgent medical attention.

You should immediately:

phone the Poisons Information Centre
(by calling 13 11 26), or
contact your doctor, or
go to the Emergency Department at your nearest hospital.

You should do this even if there are no signs of discomfort or poisoning.

5. What should I know while using INSTILLAGEL LIDO?

Things you should do

Remind any doctor, dentist or pharmacist you visit that you are using INSTILLAGEL LIDO

Driving or using machines

Be careful before you drive or use any machines or tools until you know how INSTILLAGEL LIDO affects you.

Effects on the ability to drive and use machines are unlikely, but cannot be completely ruled out in cases of increased individual sensitivity. If you feel drowsy, dizzy or if you have vision disturbances, do not drive or use any tools or machinery.

Looking after your medicine

Follow the instructions on the carton on how to take care of your medicine properly.

Store it in a cool dry place away from moisture, heat or sunlight; for example, do not store it:

in the bathroom or near a sink, or
in the car or on window sills.

Keep it where young children cannot reach it.

When to discard your medicine (as relevant)

INSTILLAGEL LIDO syringes are intended for single use. The syringe and any gel not used in a single application must be discarded.

Getting rid of any unwanted medicine

If you no longer need to use this medicine or it is out of date, take it to any pharmacy for safe disposal.

Do not use this medicine after the expiry date.

6. Are there any side effects?

Lidocaine hydrochloride is generally well tolerated provided the medicine is used as directed. All medicines can have side effects. If you do experience any side effects, most of them are minor and temporary. However, some side effects may need medical attention.

See the information below and, if you need to, ask your doctor or pharmacist if you have any further questions about side effects.

Less serious side effects

Less serious side effects	What to do
Administration Site irritation	Speak to your doctor if you have any of these less serious side effects and they worry you.

Serious side effects

Serious side effects	What to do
Allergic reaction - symptoms may include:- swelling of the hands, feet, face, lips, mouth, tongue or throat difficulties in breathing shortness of breath due to narrowing of the airways (bronchospasm) skin problems such as itchy skin or rash hives drop in blood pressure and shock	Call your doctor straight away, or go straight to the Emergency Department at your nearest hospital if you notice any of these serious side effects.

Tell your doctor or pharmacist if you notice anything else that may be making you feel unwell.

Other side effects not listed here may occur in some people.

Reporting side effects

After you have received medical advice for any side effects you experience, you can report side effects to the Therapeutic Goods Administration online at www.tga.gov.au/reporting-problems. By reporting side effects, you can help provide more information on the safety of this medicine.

Always make sure you speak to your doctor or pharmacist before you decide to stop taking any of your medicines.

7. Product details

This medicine is available only from a pharmacist.

What INSTILLAGEL LIDO contains

Active ingredient (main ingredient)	Lidocaine hydrochloride (as monohydrate)
Other ingredients (inactive ingredients)	Hypromellose Sodium hydroxide Purified water

Do not use this medicine if you are allergic to any of these ingredients.

What INSTILLAGEL LIDO looks like

INSTILLAGEL LIDO is a nearly colourless, clear sterile gel. INSTILAGEL LIDO is available as a gel in 6mL and 11mL (AUST R 468186) polypropylene disposable plastic syringes in packs of 10 pre-filled syringes per carton.

Each graduation on the syringe is equivalent to approximately 1 mL of gel (20.1 mg lidocaine hydrochloride).

An applicator nozzle is available for separate purchase.

Who distributes INSTILLAGEL LIDO

InterPharma Pty Ltd
Suite 103, 39 East Esplanade
MANLY NSW 2095 AUSTRALIA
Ph.: 029976 6876

This leaflet was prepared in Nov 2024

Published by MIMS March 2025

BRAND INFORMATION

Brand name

Instillagel Lido

Active ingredient

Lidocaine (lignocaine) hydrochloride

Schedule

1 Name of Medicine

Lidocaine hydrochloride monohydrate.

2 Qualitative and Quantitative Composition

Instillagel Lido contains the active ingredient lidocaine hydrochloride (as monohydrate) 2% w/w.
Instillagel Lido 6 mL prefilled syringe contains 120.84 mg lidocaine hydrochloride.
Instillagel Lido 11 mL gel contains 221.54 mg lidocaine hydrochloride.
For the full list of excipients, see Section 6.1 List of Excipients.

3 Pharmaceutical Form

Clear colourless sterile gel.

4 Clinical Particulars

4.1 Therapeutic Indications

For local anaesthesia and lubrication of the urethra prior to catheterization and endourethral procedures. Cystoscopy, proctoscopy and rectoscopy. Symptomatic treatment of painful cystitis and urethritis.

4.2 Dose and Method of Administration

This product is for single use in one patient only. Discard unused portion.
As with any local anaesthetic, reactions and complications are best averted by employing the minimum effective dosage. Debilitated or elderly patients and children should be given doses according to their age and physical condition.
The dose of topical lidocaine hydrochloride should be taken into consideration in estimating the total dose of lidocaine hydrochloride if parenteral lidocaine hydrochloride is to be administered concomitantly.
The following dosage recommendations should be regarded as a guide. The clinician's experience and knowledge of the patient's physical status are of importance in calculating the required dose. 1 mL of Instillagel Lido is approximately equal to 1 g of Instillagel Lido.

Males.

The usual dose required for adequate analgesia is 20 mL (equiv. lidocaine hydrochloride 400 mg).
The gel is instilled slowly into the urethra until it reaches the external sphincter, proximal to the prostate, where a certain resistance is felt. Compression is then applied for several minutes at the corona. The remaining gel is administered, filling the length of the urethra.
For procedures such as sounding or cystoscopy, a larger quantity of gel (up to 40 mL) may be required. This amount should be instilled in three to four portions and anaesthesia allowed to take effect for five to ten minutes before insertion of the instrument.

Females.

Instill 5 to 10 mL in small portions to fill the whole urethra. In order to obtain adequate anaesthesia, three to five minutes should be allowed prior to performing urological procedures.

Proctoscopy/rectoscopy.

Instill 10-20 mL gel into the anal cavity/rectum and a small amount to lubricate the endoscope.

Children.

In children under the age of 12 years, up to 6 mg/kg can be used.

4.3 Contraindications

Known hypersensitivity to amide type local anaesthetics or to any of the excipients.

4.4 Special Warnings and Precautions for Use

Not for injection.

Warning.

Excessive dosage, or short intervals between doses, can result in high serum levels of lidocaine hydrochloride or its metabolites and serious adverse effects, therefore the recommended dosage and administration guidelines should be strictly followed. Where possible the lowest dose that results in effective anaesthesia should be used to avoid high plasma levels and serious adverse effects.

Dose reduction.

Care is required with debilitated, elderly, acutely ill patients and children who should be given reduced doses relative to their age and physical status.

Excessive absorption.

As absorption from wound surfaces and mucous membranes is relatively high and tolerance to elevated blood levels varies with the status of the patient, use with caution in patients with severely traumatised mucosa and/or sepsis in the region of proposed application. If the dose or site of administration is likely to result in high blood levels, lidocaine hydrochloride, in common with other local anaesthetics, should be used with caution in patients with epilepsy, impaired cardiac conduction, bradycardia, impaired hepatic function, severe shock and patients with severe renal dysfunction.

Antiarrhythmic drugs class III.

Patients treated with antiarrhythmic drugs class III (e.g. amiodarone) should be kept under close surveillance and electrocardiogram (ECG) monitoring considered, since cardiac effects may be additive.

Porphyric patients.

Instillagel Lido is probably porphyrogenic and should only be used on patients with acute porphyria where there are strong or urgent indications. Appropriate precautions should be taken for all porphyric patients.

Use in the elderly.

Care is required with the elderly who should be given reduced doses relative to their age and physical status.

Paediatric use.

Care is required with children who should be given reduced doses relative to their age and physical status.

Effects on laboratory tests.

No data available.

4.5 Interactions with Other Medicines and Other Forms of Interactions

Antiarrhythmic drugs.

Lidocaine hydrochloride should be used with caution in patients receiving antiarrhythmic drugs such as mexiletine, since the toxic effects are additive. Specific interaction studies with lidocaine hydrochloride and antiarrhythmic drugs class III (e.g. amiodarone) have not been performed, but caution is advised.

Enzyme-inducing drugs.

Drugs that reduce the clearance of lidocaine hydrochloride (e.g. cimetidine or beta-blockers) may cause potentially toxic plasma concentrations when lidocaine hydrochloride is given in repeated high doses over a long time period. Caution should be taken if administered concurrently with lidocaine hydrochloride. However, such interactions should be of no clinical importance following short-term treatment with Instillagel Lido at the recommended dosage. Phenytoin and other antiepileptic drugs such as phenobarbitone, primidone and carbamazepine appear to enhance the metabolism of lidocaine hydrochloride but the significance of this effect is not known. Phenytoin and lidocaine hydrochloride have additive cardiac depressant effects.

4.6 Fertility, Pregnancy and Lactation

Effects on fertility.

No data available.
(Category A)
Lidocaine hydrochloride crosses the placental barrier and may be taken up by fetal tissues. When used for surface anaesthesia, lidocaine hydrochloride blood levels following normal administration are low thus minimal drug is available for placental transfer. No specific disturbances to the reproductive process have so far been reported.
Lidocaine hydrochloride enters the breast milk, but in such small quantities at therapeutic dose levels that there is generally no risk when breastfeeding.

4.7 Effects on Ability to Drive and Use Machines

Depending on the dose administered, local anaesthetics may have a very mild effect on mental function and may temporarily impair locomotion and coordination.

4.8 Adverse Effects (Undesirable Effects)

Systemic adverse reactions are rare and may result from high plasma levels due to excessive dosage or rapid absorption, or from hypersensitivity, idiosyncrasy or reduced tolerance on the part of the patient. Such reactions are systemic in nature and involve the central nervous and/or cardiovascular systems.

Central nervous system.

CNS reactions are excitatory and/or depressant and may be characterised by lightheadedness, nervousness, apprehension, euphoria, confusion, dizziness, drowsiness, tinnitus, blurred vision, vomiting, sensation of heat, cold or numbness, twitching, tremors, convulsions, unconsciousness and possibly respiratory arrest. The excitatory reactions may be very brief or may not occur at all, in which case the first manifestations of toxicity may be drowsiness, progressing to unconsciousness and respiratory arrest. Drowsiness following administration of lidocaine hydrochloride is usually an early sign of a high blood level of the drug and may occur as a result of rapid absorption.

Cardiovascular.

Cardiovascular reactions are depressant and may be characterised by hypotension, myocardial depression, bradycardia and possibly cardiac arrest.

Allergic reactions.

Allergic reactions may occur as a result of sensitivity either to the local anaesthetic agent or to other ingredients in the formulation. Allergic reactions as a result of sensitivity to lidocaine hydrochloride are rare. The detection of sensitivity by skin testing is of doubtful value. The extremely rare cases of allergy to local anaesthetic preparations have included bronchospasm, chest pain, dyspnoea, pruritus, rash, oedema, rhinitis, increased sweating, urticaria, sleepiness, dizziness, paraesthesia and, in the most severe instances, anaphylactic shock.

Effects on the blood.

Methaemoglobinaemia may occur, probably due to the metabolism of lidocaine hydrochloride to an aniline-like structure. Infants (during the first 3 months of life) are particularly susceptible to induced methaemoglobinaemia, probably due to their limited enzyme capacity.

Reporting suspected adverse effects.

Reporting suspected adverse reactions after registration 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 at www.tga.gov.au/reporting-problems.

4.9 Overdose

Lidocaine hydrochloride is absorbed from mucous membranes and serious toxicity has been reported following the use of lidocaine hydrochloride preparations for urethral anaesthesia.
Lidocaine hydrochloride intoxication affects the CNS and cardiovascular system. Overdose symptoms include: severe hypotension, asystole, bradycardia, apnoea, cardiac arrest, respiratory arrest, seizures, coma and possibly death.

Management of local anaesthetic emergencies.

The first consideration is prevention, which is best accomplished by careful and constant monitoring of cardiovascular and respiratory vital signs and the patient's state of consciousness after each local anaesthetic administration. At the first sign of change, oxygen should be administered.

Treatment.

If convulsions occur, immediate attention is required for the maintenance of a patent airway and assisted or controlled ventilation with oxygen. Adequacy of the circulation should then be evaluated, bearing in mind that drugs used to treat convulsions depress the circulation when administered intravenously.
Should convulsions persist despite adequate respiratory support, and if the status of the circulation permits, appropriate anticonvulsant medication such as an ultrashort acting barbiturate (e.g. thiopentone) or a benzodiazepine (e.g. diazepam) may be administered intravenously.
Hypotension may be initially managed by the use of intravenous fluids and by vasopressors if the problem persists.
Dialysis is of negligible value in the treatment of acute overdosage with lidocaine hydrochloride.
For information on the management of overdose, contact the Poisons Information Centre on 13 11 26 (Australia).

5 Pharmacological Properties

5.1 Pharmacodynamic Properties

Mechanism of action.

Local anaesthetic/antiarrhythmic.
Lidocaine hydrochloride is a local anaesthetic of the amide type. It produces a reversible loss of sensation by preventing or diminishing the conduction of sensory nerve impulses near the site of application.

Clinical trials.

No data available.

5.2 Pharmacokinetic Properties

Absorption.

Lidocaine hydrochloride is readily absorbed from mucous membranes and damaged skin producing rapid, local anaesthesia in these areas. Absorption from intact skin is poor. The rate of absorption and amount of dose absorbed is dependent upon concentration, the total dose administered, the specific site of application and the duration of exposure.

Metabolism.

Lidocaine hydrochloride is metabolised rapidly by the liver, with both metabolites and unchanged drug excreted by the kidney. Approximately 90% of lidocaine hydrochloride is excreted as metabolites and less than 10% is excreted as unchanged drug. Excessive blood levels of lidocaine hydrochloride may cause changes in cardiac output, total peripheral resistance and mean arterial pressure. These changes may be attributed to a direct depressant effect of the anaesthetic agent on various components of the cardiovascular system. The pharmacological/toxicological actions of the metabolites are similar to, but less potent than those of lidocaine hydrochloride.

Distribution.

The plasma binding of lidocaine hydrochloride is dependent on drug concentration, and the fraction bound decreases with increasing concentration. At concentrations of 1 to 4 microgram free base/mL, 60 to 80% of lidocaine hydrochloride is protein-bound. Binding is also dependent on the plasma concentrations of the alpha₁-acid glycoprotein. Lidocaine hydrochloride crosses the blood brain and placental barriers.

Excretion.

Studies of lidocaine hydrochloride metabolism following IV bolus injection have shown that the elimination half-life is usually 1.5 to 2 hours. The half-life may be doubled in patients with hepatic dysfunction. Renal dysfunction does not affect lidocaine hydrochloride kinetics, but may increase the accumulation of metabolites.
Acidosis and the use of CNS stimulants and depressants affect the CNS levels of lidocaine hydrochloride required to produce systemic effects. Adverse reactions become increasingly apparent with venous plasma levels above 6.0 microgram free base/mL.

5.3 Preclinical Safety Data

Genotoxicity.

Genotoxicity tests with lidocaine hydrochloride are inconclusive. In genotoxicity studies, a metabolite of lidocaine hydrochloride, 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.

Carcinogenicity.

No data available.

6 Pharmaceutical Particulars

6.1 List of Excipients

Hypromellose, sodium hydroxide and purified water.
Water for injections.

6.2 Incompatibilities

Incompatibilities were either not assessed or not identified as part of the registration of this medicine.

6.3 Shelf Life

In Australia, information on the shelf life can be found on the public summary of the Australian Register of Therapeutic Goods (ARTG). The expiry date can be found on the packaging.

6.4 Special Precautions for Storage

Store below 30°C.

6.5 Nature and Contents of Container

Instillagel Lido is supplied in a plastic syringe with an applicator nozzle for easy application. It is contained in an outer, sterile bag to allow assembly of syringe and nozzle under aseptic conditions.

Pack size.

10 x 6 mL and 10 x 11 mL syringes.

6.6 Special Precautions for Disposal

In Australia, any unused medicine or waste material should be disposed of in accordance with local requirements.

6.7 Physicochemical Properties

Chemical structure.

Molecular formula: C₁₄H₂₂N₂O. Molecular weight: 234.3.
Lidocaine hydrochloride is 2-(diethylamino)-N-(2,6-dimethylphenyl) acetamide. It is a white to almost white crystalline powder that is practically insoluble in water, very soluble in alcohol and in methylene chloride.

CAS number.

137-58-6.

7 Medicine Schedule (Poisons Standard)

S2 - Pharmacy Medicine.

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Consumer medicine information

Instillagel Lido

Lidocaine (lignocaine) hydrochloride

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BRAND INFORMATION