Lidocaine Hydrochloride/ Phenylephrine Hydrochloride

Registered South African indications:

• Preparation of nasal mucosa for surgery (e.g. Cautery to Little’s area) or endoscopy
• Aid the treatment of acute nose bleeds and removal of foreign bodies from the nose
• Topical anaesthesia of the pharynx prior to direct or indirect laryngoscopy
• Topical anaesthesia and local vasoconstriction prior to endoscopy of the upper airways

Registered South African contraindications

• Hypersensitivity to the active ingredient or any of the excipients in this combination product
• Hypersensitivity to other local anaesthetics of the amide type and to other sympathomimetic medicines
• Pregnancy
• Breastfeeding
• Hypovolaemia
• Hypertension
• Acute ischaemic heart disease
• Complete heart block
• Thyrotoxicosis
• Glaucoma
• Urinary retention
• Children under 12 years of age

South African recommendations

Caution in the following patient groups

• Renal impairment
• Hepatic impairment
• Angina pectoris (sympathomimetic-containing products should be used with great care in patients suffering from angina pectoris)
• Epilepsy
• Impaired cardiac conduction
• Bradycardia
• Severe shock

Elderly and debilitated patients

• Elderly and debilitated patients should be given reduced dosages

Eating and drinking

• The use of topical anaesthetic medicines in the oral cavity and upper airway tissues may interfere with swallowing and enhance the danger of aspiration of food or drink
• Food or drink should not be ingested within 2 hours of using local anaesthetics in the mouth area
• Numbness of the tongue or buccal mucosa may increase the risk of trauma from hot drinks or biting

Patients with cardiovascular diseases

• Lidocaine/ phenylephrine should be given with caution to patients with cardiovascular disease, especially those suffering from hypertension, severe bradycardia, conduction disturbances or severe digoxin intoxication
• There is a small but transient increase in pulse rate and blood pressure after the administration of lidocaine/ phenylephrine to healthy individuals; this must be taken into account in hypertensive patients

Patients taking β-adrenoceptor blocking medicines

• Lidocaine/ phenylephrine should be administered with caution to patients taking β-adrenoceptor blocking medicines and those with cardiovascular disease, diabetes mellitus, hypertension, hyperthyroidism, hypoxia, hypercapnia, and porphyria

Asthmatic patients

• This preparation contains sodium metabisulfite, which may cause allergic-type reactions including anaphylactic symptoms and life-threatening or less severe asthmatic episodes in susceptible individuals
• Sulphite sensitivity is seen more frequently in asthmatic patients than in non-asthmatic people

General precautions

• Genetic predisposition to malignant hyperthermia and pre-existing abnormal neurological conditions should be considered

Use in patients with traumatised mucosa and/or sepsis

• Lidocaine/ phenylephrine should be used with caution in patients with traumatised mucosa and/or sepsis in the region of the proposed application

Sympathomimetic-containing preparations

• The medical practitioner or pharmacist should check that sympathomimetic-containing preparations are not administered simultaneously by several routes (oral and topical such as nasal, aural, and eye preparations)

Mydriasis

• Mydriasis (prolonged dilation of the pupils) has been reported with phenylephrine
• Patients should be advised to notify their medical practitioner if they have a history of glaucoma or increased intraocular pressure

Use of benzalkonium chloride

• Lidocaine/ phenylephrine contains benzalkonium chloride, which may cause oedema of the nasal mucosa with long-term use
• Benzalkonium chloride may cause wheezing and breathing difficulties (bronchospasm), especially in asthmatic patients
• Benzalkonium chloride may cause local irritation

Effects on ability to drive and use machines

• Lidocaine/ phenylephrine spray has no or negligible influence on the ability to drive and use machines

Forms avail. in SA and covered in this monograph: spr

South African registered indications and dosages

Preparation of nasal mucosa for surgery (e.g. Cautery to Little’s area) or endoscopy
Aid the treatment of acute nose bleeds and removal of foreign bodies from the nose
Topical anaesthesia of the pharynx prior to direct or indirect laryngoscopy
Topical anaesthesia and local vasoconstriction prior to endoscopy of the upper airways

Lidocaine Hydrochloride/ Phenylephrine Hydrochloride
5/0.5 (mg/spray)

• Nasal/Pharyngeal (spr): 5 sprays per nostril, or 5 sprays to the throat; Doses are to be admin. once only

---

Do not exceed the recommended dosage regimes

---

Each spray measures 100 microlitres. A new spray nozzle must be used for each patient

Paed. forms avail. in SA and covered in this monograph: spr

South African registered indications and dosages

Preparation of nasal mucosa for surgery (e.g. Cautery to Little’s area) or endoscopy
Aid the treatment of acute nose bleeds and removal of foreign bodies from the nose
Topical anaesthesia of the pharynx prior to direct or indirect laryngoscopy
Topical anaesthesia and local vasoconstriction prior to endoscopy of the upper airways

Lidocaine Hydrochloride/ Phenylephrine Hydrochloride
5/0.5 (mg/spray)

Younger than 12 years

• Contraindicated

Older than 12 years

• See adult dosages

---

Do not exceed the recommended dosage regimes

---

Each spray measures 100 microlitres. A new spray nozzle must be used for each patient

---

Do not administer to children under 12 years of age

Pregnancy

South African recommendations

• Contraindicated
• Lidocaine/ phenylephrine spray should not be used during pregnancy

Breastfeeding

South African recommendations

• Contraindicated
• Lidocaine/ phenylephrine spray should not be used by breastfeeding mothers

South African recommendations

• Caution; no dose adjustment recommended
  Metabolites of lidocaine may accumulate in patients with renal impairment

South African recommendations

• Caution; no dose adjustment recommended
  Lidoocaine is metabolised in the liver and must be given with caution to patients with hepatic insufficiency

South African recommendations

• Caution; dose adjustment recommended
  Elderly and debilitated patients should be given reduced dosages

Lidocaine Hydrochloride/ Phenylephrine Hydrochloride

Cardiac Disorders

Less frequent

• Palpitations

Nervous System Disorders

Less frequent

• Tremor
• Nervousness
• Dizziness
• Numbness
• Disorientation

Vascular Disorders

Frequency unknown

• Hypertension

Gastrointestinal Disorders

Frequent

• Transient bitter taste in the mouth lasting one to two minutes before disappearing

Less frequent

• Nausea
• Vomiting

Eye Disorders

Frequency unknown

• Mydriasis

Ear and Labyrinth Disorders

Less frequent

• Tinnitus

Possible Systemic Side Effects Due to Lidocaine

Central Nervous System

• Excitation of the central nervous system
  • Restlessness
  • Excitement
  • Nervousness
  • Dizziness
  • Tinnitus
  • Blurred vision
  • Nausea
  • Vomiting
  • Muscle twitching and tremors
  • Convulsions
  • Numbness of the tongue and perioral region
  • Drowsiness (follows transient excitation)
  • Respiratory failure (follows transient excitation)
  • Coma (follows transient excitation)

Cardiovascular System

• Myocardial depression and peripheral vasodilation resulting in
  • Hypotension
  • Bradycardia
  • Dysrhythmias
  • Cardiac arrest

Other

• Methaemoglobinaemia

Possible Systemic Side Effects Due to Phenylephrine

Central Nervous System

• Fear
• Anxiety
• Nervousness
• Restlessness
• Tremors
• Insomnia
• Confusion
• Irritability
• Psychotic states
• Epileptiform convulsions
• Reduced appetite
• Nausea
• Vomiting

Cardiovascular System

• Vasoconstriction with resultant hypertension
• Severe vasoconstriction leading to gangrene (if infiltrated into digits)
• Cerebral haemorrhage
• Pulmonary oedema
• Reflex bradycardia
• Tachycardia
• Cardiac dysrhythmias
• Angina pectoris
• Palpitations
• Cardiac arrest
• Hypotension with dizziness and fainting
• Flushing
• Increased incidence of sudden death (with excessive use)

Other

• Difficulty in micturition (especially in prostatic hypertrophy)
• Urinary retention
• Dyspnoea
• Weakness
• Altered metabolism
• Sweating
• Hyperpyrexia
• Hypersalivation
• Headache

Lidocaine Hydrochloride/ Phenylephrine Hydrochloride

• Halogenated anaesthetic medicines
• Chloroform
• Cyclopropane
• Halothane
• Enflurane
• Isoflurane

Lidocaine (Lignocaine) Hydrochloride

• Propranolol
• Anti-dysrhythmic medicines
• Tocainide
• Diuretics
• Acetazolamide
• Loop diuretics
• Thiazide diuretics
• Cimetidine
• Suxamethonium
• Phenytoin

Phenylephrine Hydrochloride

• Monoamine oxidase inhibitors (MAOIs)
• Debrisoquine
• Reserpine
• Guanethidine
• Cardiac glycosides
• Digoxin
• Methyldopa
• β-adrenoceptor blocking medicines
• Propranolol
• Hydrochlorothiazide
• Antihypertensive medicines
• Anti-dysrhythmic medicines
• Doxapram
• Oxytocin
• Ergot alkaloids
• Phenothiazines
• Tricyclic antidepressants

None routine

Lidocaine (lignocaine) Hydrochloride
Lidocaine is a local anaesthetic. It stabilises the neuronal membrane and blocks the initiation and transmission of nerve impulses in sensory nerves by slowing sodium permeability (depolarisation), reducing height and rate of rise of the action potential, increasing excitation threshold, and slowing conduction velocity.

Phenylephrine Hydrochloride
This is a postsynaptic alpha-adrenoceptor stimulant that causes local vasoconstriction. The phenylephrine in lidocaine/ phenylephrine spray constricts the blood vessels locally, which can decrease the systemic absorption of lignocaine and restrict bleeding. It also decreases the onset of action and increases the duration of action of lignocaine. Its nasal decongestant action can assist in easier passage of endoscopes.