TERBICIP Spray (Terbinafine hydrochloride)

Table of Content

Qualitative and Quantitative Composition

Terbinafine Hydrochloride IP (1.0 % W/W)

Excipient (- QS)

Dosage Form(S) And Strength(S)

Spray, 1%

Clinical Particulars

Therapeutic Indications

The treatment of tinea pedis (athelete’s foot), tinea corporis (ringworm) and tinea cruris (jock itch) caused by Trichophyton (e.g. T. rubrum, T. mentagrophytes, T. verrucosum, T. violaceum) and Epidermophyton floccosum.

Posology and Method of Administration

TERBICIP Spray, 1%, can be applied twice daily for one week for tinea pedis and once a day for one week for tinea cruris and tinea corporis.

Cleanse and dry the affected areas of the skin thoroughly before application of TERBICIP Spray, 1%. Hold the bottle upright, 4´´ to 6´´ away from the skin surface and spray a sufficient amount of TERBICIP Spray, 1%, to cover the affected area. Wash hands thoroughly after each use.

Contraindications

TERBICIP Spray, 1%, is contraindicated in patients with a history of hypersensitivity to terbinafine or any of the excipients contained in the spray solution.

Special Warnings and Precautions for Use

Keep out of the reach of children.

TERBICIP Spray, 1%, is for cutaneous use only. Contact with the eyes should be avoided. In case of accidental contact with the eyes, rinse the eyes thoroughly with running water.

Good general hygiene is necessary in conjunction with the use of TERBICIP Spray, 1%, in order to prevent re-infection (e.g. from underwear, socks, shoes, etc.).

Drug Interactions

There are no known drug interactions with terbinafine spray.

Use in Special Populations

Pregnant Women

Foetal toxicity and fertility studies in animals suggest no adverse effects. Since, clinical experience in pregnant women is very limited, TERBICIP Spray, 1%, should not be used during pregnancy unless the potential benefits outweigh any potential risks.

Lactating Women

Terbinafine is excreted in breast milk and, therefore, lactating mothers should not receive terbinafine spray. Infants should also not be allowed to come into contact with any treated skin, including the breasts.

Paediatric Patients

The experience with topical terbinafine in children is still limited and its use cannot, therefore, be recommended in children under 12 years of age.

Geriatric Patients

There is no evidence to suggest that elderly patients require different dosages or experience side effects different to those of younger patients.

Effects on Ability to Drive and Use Machines

TERBICIP Spray, 1%, has no influence on the ability to drive and use machines.

Undesirable Effects

Local symptoms such as pruritus, skin exfoliation, application site pain, application site irritation, pigmentation disorder, skin burning sensation, erythema and scab may occur at the site of application.

These minor symptoms must be distinguished from hypersensitivity reactions such as widespread pruritus, rash, bullous eruptions and hives, which are reported in sporadic cases but require discontinuation of the medication.

In rare cases, the underlying fungal infection may be aggravated.

Adverse reactions are listed below by frequency. Frequencies are defined as: very common (≥1/10); common (≥1/100 to <1/10); uncommon (≥1/1,000 to <1/100); rare (≥1/10,000 to <1/1,000); very rare (<1/10,000), or not known (can not to be estimated from available data). Within each frequency grouping, adverse reactions are presented in order of decreasing seriousness.

Common

Skin exfoliation, pruritus

Uncommon

Skin lesion, scab, skin disorder, pigmentation disorder, erythema, skin burning sensation

Application site pain, irritation

Rare

Eye irritation

Dry skin, dermatitis contact, eczema

Condition aggravated

Not known

Adverse drug reaction such as Acute Generalised Exanthematous Pustulosis (AGEP) has been observed with the use of terbinafine formulations.

Hypersensitivity

Rash

If you experience any side-effects, talk to your doctor or pharmacist or write to drugsafety@cipla.com. You can also report side effects directly via the national pharmacovigilance program of India by calling on 1800 180 3024 or you can report to Cipla Ltd on 18002677779. By reporting side-effects, you can help provide more information on the safety of this product.

Overdose

The low systemic absorption of topical terbinafine renders overdosage extremely unlikely.

Accidental ingestion of the contents of one 30 ml bottle of terbinafine spray, solution, which contains 300 mg terbinafine hydrochloride, is comparable to ingestion of one terbinafine 250 mg tablet (adult oral unit dose).

Should a larger amount of terbinafine spray be inadvertently ingested, adverse effects similar to those observed with an overdosage of terbinafine tablets are to be expected. These include headache, nausea, epigastric pain and dizziness.

If accidently ingested, the alcohol content should be considered. Terbinafine spray contains 25 % w/w alcohol.

The recommended treatment of overdosage consists of eliminating the drug, primarily by the administration of activated charcoal and giving symptomatic supportive therapy, if needed.

Pharmacology Properties

Mechanism of Action

Terbinafine interferes specifically with fungal sterol biosynthesis at an early stage. This leads to a deficiency in ergosterol and to an intracellular accumulation of squalene, resulting in fungal cell death.

Terbinafine acts by inhibition of squalene epoxidase in the fungal cell membrane. The enzyme, squalene epoxidase, is not linked to the cytochrome (CY) P450 system. Terbinafine does not influence the metabolism of hormones or other drugs.

Pharmacodynamic Properties

Terbinafine is an allylamine with a broad spectrum of activity against fungal pathogens of the skin, hair and nails, including dermatophytes such as Trichophyton (e.g. T. rubrum, T. mentagrophytes, T. verrucosum, T. tonsurans, T. violaceum), Microsporum (e.g. M. canis), Epidermophyton floccosum and yeasts of the genera Candida (e.g. C. albicans) and Pityrosporum. At low concentrations, terbinafine is fungicidal against dermatophytes, moulds and certain dimorphic fungi. Its activity against yeasts is fungicidal or fungistatic, depending on the species.

Pharmacokinetic Properties  

Less than 5% of the dose is absorbed after topical application in humans; systemic exposure is, thus, very less.

Nonclinical Properties

Animal Toxicology or Pharmacology

Carcinogenesis, Mutagenesis, Impairment of Fertility

In a 28-month oral carcinogenicity study in rats, a marginal increase in the incidence of liver tumors was observed in males at the highest dose level, 69 mg/kg/day (in terms of mg/m2/day equivalent to 34 times the maximum potential exposure at the recommended topical human dose*). There was no dose-related trend, and the mid-dose male rats, 20 mg/kg/day (in terms of mg/ m2/day equivalent to 10 times the maximum potential exposure at the recommended topical human dose*) did not have any tumors. No increased incidence in liver tumors was noted in female rats at dose levels up to 97 mg/kg/day (in terms of mg/m2/day equivalent to 47 times the maximum potential exposure at the recommended topical human dose*) or in male or female mice treated orally for 23 months at doses up to 156 mg/kg/day (in terms of mg/m2/day equivalent to 38 times the maximum potential exposure at the recommended topical human dose*).

A wide range of oral in vivo studies in mice, rats, dogs and monkeys, and in vitro studies using rat, monkey, and human hepatocytes suggest that the development of liver tumors in the high-dose male rats may be associated with peroxisome proliferation and support the conclusion that this is a rat-specific finding.

The results of a variety of in vitro (mutations in E. coli and Salmonella, DNA repair in rat hepatocytes, mutagenicity in Chinese hamster fibroblasts, chromosome aberration and sister chromatid exchanges in Chinese hamster lung cells) and in vivo (chromosome aberration in Chinese hamsters, micronucleus test in mice) genotoxicity tests gave no evidence of a mutagenic or clastogenic potential and demonstrated the absence of tumor-initiating or cell-proliferating activity.

Oral reproduction studies in rats at doses up to 300 mg/kg/day (in terms of mg/m2/day equivalent to 146 times the maximum potential exposure at the recommended topical human dose*) did not reveal any specific effects on fertility or other reproductive parameters. Intravaginal application of terbinafine hydrochloride at 150 mg/day (in terms of mg/m2/day equivalent to 165 times the maximum potential exposure at the recommended topical human dose*) in pregnant rabbits did not increase the incidence of abortions, premature deliveries or fetal abnormalities.

* The above comparisons between oral animal doses and maximum potential exposure at the recommended human topical dose are based upon the application to human skin of 0.1 mg of terbinafine/cm2 twice daily, the assumption of average human cutaneous exposure of 100 cm2 (assuming the use of 1 gram of Terbinafine Solution/dose), and the theoretical maximum human cutaneous absorption of 100%.

Description

TERBICIP Spray, 1% (terbinafine hydrochloride solution) contains the synthetic antifungal compound, terbinafine hydrochloride.

Pharmaceutical Particulars

Incompatibilities

Not applicable.

Shelf-Life

2 years

Packaging Information

TERBICIP Spray, 1%: HDPE bottle of 30 ml

Storage and Handling Instructions

Store below 25°C. Do not refrigerate.

Patient Counselling Information

What is TERBICIP Spray, 1%, and what is it used for?

TERBICIP Spray, 1%, contains the active ingredient terbinafine, which is an antifungal used to treat skin problems caused by fungi.

Precautions to note before you use TERBICIP Spray, 1%

DO NOT use TERBICIP Spray, 1%, if you have

  • an allergy (hypersensitivity) to any of the ingredients in the product.

The spray is NOT recommended for children under 12 years of age.

Take special care with TERBICIP Spray, 1%

The spray is for application on the skin only.

  • Avoid inhaling the product.
  • Eyes, mouth or face– avoid contact with the spray. In case of accidental contact with the eyes, rinse thoroughly with running water.
  • Damaged skin – avoid application of the spray to such areas because alcohol (one of the ingredients in this spray) could cause stinging or irritation.

Taking other medicines

Please tell your doctor if you are taking or have recently taken/used any other medicines, including medicines you have used on the areas you are treating with TERBICIP Spray, 1%.

Pregnancy and breastfeeding

If you are pregnant, ask your doctor before using this medicine. Do not use this spray if you are breastfeeding.

Driving and using machines

TERBICIP Spray, 1%, is not expected to affect your ability to drive or operate machinery.

How to use TERBICIP Spray, 1%

  • Always use this medicine exactly as described in this leaflet or as advised by your doctor.
  • Apply the spray once or twice a day for a week, but this will depend upon the type and area of infection. Infections usually appear to improve within a few days of starting to use TERBICIP Spray, 1%, but may reappear if the spray is not applied regularly or is stopped too early.
  • Cleanse and dry the affected areas of the skin thoroughly before application of TERBICIP Spray, 1%.
  • Hold the bottle upright, 4 to 6 inches away from the skin surface, and spray a sufficient amount of TERBICIP Spray, 1%, to cover the affected area.
  • Replace the cap on the spray bottle and wash your hands.

Children under 12 years of age

NOT recommended.

If you accidently swallow TERBICIP Spray, 1%

Contact your doctor or nearest hospital emergency department if you, or someone else, has accidently swallowed the spray. Take any remaining medicine and this leaflet with you if possible. Symptoms of accidental ingestion include headache, nausea (feeling sick), dizziness and stomach pain.

If you forget to use TERBICIP Spray, 1%

If you miss an application, apply the spray as soon as possible then carry on as before. If you only remember at the time of your next application, just apply the spray and carry on as normal. It is important to try to use the spray at the correct times as forgotten applications could risk the infection returning.

If you stop using TERBICIP Spray, 1%

You should not stop using the spray before the recommended time as this may reduce the effectiveness of treatment or the infection may return. If you have any further questions on the use of this product, ask your doctor.

Possible side effects

Like all medicines, TERBICIP Spray, 1%, can cause side effects, although not everybody gets them.

STOP using the spray and seek medical help immediately if you have any of the following allergic reactions:

Very rare (may affect less than 1 user in 10,000):

  • difficulty breathing or swallowing, swelling of the mouth, face, lips, tongue or throat (severe allergic reaction).
  • severe itching of the skin, with red rash or raised lumps, hives or blisters.

Common (may affect 1 to 10 users in 100): skin peeling, itching.

Uncommon (may affect 1 to 10 users in 1000): skin lesions, scab, skin colour changes, redness, burning, pain and irritation at the site of application. These common and uncommon side effects are usually harmless and you can carry on using the spray.

Rare (may affect 1 to 10 users in 10,000): eye irritation, dry skin, contact dermatitis, eczema, worsening of symptoms.

Not known (can not to be estimated from available data): acute generalised exanthematous pustulosis (AGEP), hypersensitivity, rash

Reporting of side effects

If you experience any side-effects, talk to your doctor or pharmacist or write to drugsafety@cipla.com. You can also report side effects directly via the national pharmacovigilance program of India by calling on 1800 180 3024 or you can report to Cipla Ltd on 18002677779. By reporting side-effects, you can help provide more information on the safety of this product.

How to store TERBICIP Spray, 1%

Keep out of the sight and reach of children.

Store below 25°C. Do not refrigerate.

Keep the bottle closed and in its carton.

Do not use or keep this medicine after the expiry date shown on the box and container.

What does TERBICIP Spray, 1%, contain?

The active ingredient is terbinafine hydrochloride 1% w/w.

What are the contents of the pack?

TERBICIP Spray, 1%, is available in a white 30 mL plastic bottle with a spray pump.

Details of Manufacturer

L-MISTAIR HEALTH & HYGIENE PVT. LTD. (KOL-KOLHAPUR) (706544)

PLOT NO.3, MIDC, SHIROLI, KOLHAPUR - 416122,

Tal: Hatkanangale, Dist: KOLHAPUR

Details of Permission or License Number with Date

1056551dated 01/11/2018

Date of Revision

19/11/2019