LIGNOZOL EAR DROPS
CLOTRIMAZOLE AND LIGNOCAINE HYDROCHLORIDE EAR DROPS IP (1% & 2% w/v)
COMPOSITION
Each ml contains:
Clotrimazole IP 1.0% w/v
Lignocaine Hydrochloride IP 2.0% w/v
Propylene Glycol IP q.s.
DESCRIPTION
A clear, colorless to slightly viscous solution.
PHARMACODYNAMIC
Clotrimazole
Pharmacotherapeutic group: Antifungals for topical use – imidazole and triazole
derivatives
ATC Code: D01A C01
Mechanism of Action
Clotrimazole acts against fungi by inhibiting ergosterol synthesis. Inhibition of ergosterol
synthesis leads to structural and functional impairment of the fungal cytoplasmic membrane.
Clotrimazole has a broad antimycotic spectrum of action in vitro and in vivo, which includes
dermatophytes, yeasts, moulds, etc.
Under appropriate test conditions, the MIC values for these types of fungi are in the region of
less than 0.062-8.0 µ g/ml substrate. The mode of action of clotrimazole is primarily
fungistatic or fungicidal depending on the concentration of clotrimazole at the site of
infection. In vitro activity is limited to proliferating fungal elements; fungal spores are only
slightly sensitive.
In addition to its antimycotic action, clotrimazole also acts on gram-positive microorganisms
(Streptococci / Staphylococci / Gardnerella vaginalis), and gram-negative microorganisms
(Bacteroides).
In vitro clotrimazole inhibits the multiplication of Corynebacteria and gram-positive cocci –
with the exception of Enterococci – in concentrations of 0.5-10 µ g/ml substrate.
Primarily resistant variants of sensitive fungal species are very rare; the development of
secondary resistance by sensitive fungi has so far only been observed in very isolated cases
under therapeutic conditions.
Lignocaine
Pharmacotherapeutic group: Analgesics and anesthetics- Amide Group
ATC Code: S02DA01
Mechanism of Action
Lidocaine is classified as a voltage-gated sodium channel blocker, and that's exactly how it
performs its desired action. Lidocaine prohibits the activation of nerve channels (sodium
channels) that rely on electromagnetic currents (voltage). Nerve cells fire repeatedly to pass
on signals of pain or stimulation, but to do this they must polarize and repolarize. Lidocaine
blocks this process.
PHARMACOKINETICS
Clotrimazole: Pharmacokinetic investigations after dermal application have shown that
clotrimazole is minimally absorbed from the intact or inflamed skin into the human blood
circulation. The resulting peak serum concentrations of clotrimazole were below the detection
limit of 0.001 µ g/ml, suggesting that clotrimazole applied topically is unlikely to lead to
measurable systemic effects or side effects.
Lignocaine: Due to the external administration and application of the active substances at
low doses, systemic absorption is unlikely (in case of intact tympanic membrane), and for
that reason no pharmacokinetic studies have been performed.
THERAPEUTIC INDICATION
It is used for the treatment of fungal infections in the ear. This medicine also relieves the ear
pain caused due to the fungal infection. It works by reducing the growth of the fungi
responsible for the infection.
DOSAGE AND ADMINISTRATION
Instill 2-3 drops two or three times daily into the external auditory canal of the affected ear,
slightly pressing the elastic part of the dropper.
INSTRUCTION FOR USE
Warm the bottle in your hand.
Lie down with the affected ear facing up toward the ceiling.
Hold the outer part of your ear (just above your ear lobe) and gently pull back. This helps
straighten your ear canal.
Place the recommended number of drops into your ear canal.
Massage your tragus (the little piece of tissue that sits just in front of your ear canal). This
encourages the drops down your ear canal.
Lie on your side for a few minutes. This allows the ear drops to reach your eardrum.
Sit up and allow any excess drops to drain out of your ear.
Don’t stick objects in your ear canal, such as a cotton swab or hairpins.
OVERDOSE
Clotrimazole: No risk of acute intoxication is seen as it is unlikely to occur following a
single dermal application of an overdose (application over a large area under conditions
favorable to absorption) or inadvertent oral ingestion. There is no specific antidote.
However, in the event of accidental oral ingestion, routine measures such as gastric lavage
should be performed only if clinical symptoms of overdose become apparent (e.g. dizziness,
nausea or vomiting). Gastric lavage should be carried out only if the airway can be protected
adequately.
Lignocaine: No cases of overdose have been reported for Lignocaine.
CONTRAINDICATION
Hypersensitivity to Clotrimazole and Lidocaine or any of its excipients.
WARNING AND PRECAUTIONS
Before the beginning of treatment with the medicinal product, it is recommended to check if
there is perforation of the tympanic membrane. If the tympanic membrane is perforated,
intra-auricular administration may lead to contact of the product with middle ear structures
and cause undesirable effects in these tissues.
PREGNANCY, LACTATION AND FERTILITY
Clotrimazole
Pregnancy:
There is a limited amount of data from the use of clotrimazole in pregnant women. Animal
studies with clotrimazole have shown reproductive toxicity at high oral doses. At the low
systemic exposures of clotrimazole following topical treatment, harmful effects with respect
to reproductive toxicity are not predicted.
Clotrimazole can be used during pregnancy, but only under the supervision of a physician or
midwife.
Lactation:
There are no data on the excretion of clotrimazole into human milk. However, systemic
absorption is minimal after administration and is unlikely to lead to systemic effects.
Clotrimazole may be used during lactation. If used topically on the nipple area, wash breasts
before feeding child.
Fertility:
No human studies of the effects of clotrimazole on fertility have been performed; however,
animal studies have not demonstrated any effects of the drug on fertility.
Lignocaine
In case of intact tympanic membrane, systemic absorption is unlikely.
If the recommended dosage (4 drops two or three times daily) and therapy duration (should
not exceed 7 days) are observed, the product can be administered during pregnancy and
breast-feeding, if necessary. However, women during pregnancy or during breast-feeding
should consult their doctor or pharmacist before using Lignocaine. There is limited
pharmacokinetic information available. It is not known if Lignocaine active substances pass
into breast milk or/and crosses the placenta.
DRUG INTERACTION
No interaction studies have been performed.
ADVERSE EFFECTS
Clotrimazole
As the listed undesirable effects are based on spontaneous reports, assigning accurate
frequency of occurrence for each is not possible.
Immune system disorders: anaphylactic reaction, angioedema, hypersensitivity.
Vascular disorders: syncope, hypotension.
Respiratory, thoracic and mediastinal disorders: dyspnoea.
Skin and subcutaneous tissue disorders: blister, dermatitis contact, erythema, paraesthesia,
skin exfoliation, pruritus, rash, urticaria, stinging skin/burning sensation skin.
General disorders and administration site conditions: application site irritation,
application site reaction, oedema, pain.
Lignocaine
Ear and labyrinth disorders: local allergic reactions (itching, maculopapular rash), auditory
canal hyperaemia.
PRESENTATION
LIGNOZOL Ear Drops are supplied in 10 ml sterilized opaque plastic container with nozzle
and cap.
STORAGE AND OTHER INFORMATION
Store at temperature below 30 °C. Keep this medicine out of the sight and reach of children.
Do not touch the dropper tip or other dispensing tip to any surface since this may contaminate
the solution. Use the solution within one month after opening the container.