INDICATIONS     CONTRA-INDICATIONS     DOSAGE     SIDE-EFFECTS     PREGNANCY     OVERDOSE     IDENTIFICATION     PATIENT INFORMATION

Logo LAMISPOR 250 (Tablets).

SCHEDULING STATUS:
S4

PROPRIETARY NAME
(and dosage form):

LAMISPOR 250 (Tablets).

COMPOSITION:
Each tablet contains 250 mg
terbinafine as terbinafine hydrochloride.

PHARMACOLOGICAL CLASSIFICATION:
A20.2.2. Antimicrobial (chemotherapeutic) agents. Fungicides.

PHARMACOLOGICAL ACTION:
Pharmacodynamics:
Terbinafine, an allylamine antifungal, has a broad spectrum of activity. Terbinafine is fungicidal against dermatophytes, moulds and certain fungi at low concentrations, whereas the activity against yeasts is either fungicidal or fungistatic, depending on the species.
Terbinafine exerts its fungicidal activity by specifically interfering with fungal sterol biosynthesis at an early stage. Fungal cell death is caused by a deficiency in ergosterol and an intracellular accumulation of squalene. Terbinafine inhibits squalene epoxidase in the fungal cell membrane. This enzyme squalene epoxidase is not related to the cytochrome P450 system. When administered orally, terbinafine concentrates in skin at levels associated with fungicidal activity.
Pharmacokinetics:
A mean peak plasma concentration of 0.97 mg/mL is reached within 2 hours of administration of a single oral dose of 250 mg terbinafine. Terbinafine has an absorption half-life of 0.8 hours and a distribution half-life of 4.6 hours. It binds strongly to plasma proteins. Diffusion through the dermis occurs rapidly following which terbinafine concentrates in the lipophilic stratum corneum.
Terbinafine is also secreted in sebum and therefore high concentrations are reached in hair follicles, hair and sebum-rich skins. Evidence indicates that terbinafine is distributed into the nail plate within the first few weeks of initiation of treatment. Biotransformation leads to the formation of metabolites with no antifungal activity and with predominantly renal excretion. The elimination half-life is 17 hours and there is no evidence of accumulation.
Although no age-dependent changes in pharmacokinetics have been observed with terbinafine, the elimination rate may be reduced in patients with impaired renal or hepatic function, thus resulting in higher blood concentrations of terbinafine.
Food does not affect the bioavailability of terbinafine.

INDICATIONS:
LAMISPOR 250
is indicated for the treatment of fungal infections of the skin caused by Trichophyton (e.g. T. rubrum, T. mentagrophytes, T. verrucosum, T. violaceum), Microsporum canis and Epidermophyton floccosum.
LAMISPOR 250 is indicated in the treatment of:
Ringworm (tinea corporis, tinea cruris and tinea pedis) where oral therapy is considered appropriate due to the site, severity or extent of the infection.
Onychomycosis.

CONTRA-INDICATIONS:
LAMISPOR 250
is contra-indicated in patients:
With hypersensitivity to terbinafine hydrochloride or any of the excipients.
With impaired liver function.
Who are pregnant or breastfeeding, as safety has not been demonstrated.

INTERACTIONS:
Medicines that induce metabolism (such as rifampicin) may result in accelerated plasma clearance of LAMISPOR 250, whereas plasma clearance may be reduced by medicines that inhibit cytochrome P450 (such as cimetidine). Adjustments in the dosage of LAMISPOR 250 may be required where co-administration of such agents is necessary.
It has been reported that LAMISPOR 250 inhibits the CYP2D6-mediated metabolism. Although this was an in vitro finding, it may become clinically relevant in patients who receive compounds that are predominantly metabolised by this enzyme, e.g. tricyclic antidepressants (TCA’s), beta-blockers, selective serotonin reuptake inhibitors (SSRI’s), and monoamine oxidase inhibitors (MAOI’s) type B. Other in vitro studies as well as studies in healthy volunteers suggested that LAMISPOR 250 has negligible potential to inhibit or induce the clearance of medicines that are metabolised via other cytochrome P450 enzymes (e.g. ciclosporin, tolbutamide, terfenadine, triazolam, oral contraceptives). However, some cases of menstrual disturbance (breakthrough bleeding and irregular cycle) have been reported in patients who took LAMISPOR 250 concomitantly with oral contraceptives.

PREGNANCY AND LACTATION:
There is no clinical experience with LAMISPOR 250 in pregnancy. Since terbinafine is excreted in breast milk, mothers should not receive treatment with LAMISPOR 250 whilst breast-feeding.

DOSAGE AND DIRECTIONS FOR USE:
The duration of treatment with LAMISPOR 250 is dependent on the indication and the severity of the infection.
The usual recommended dosage in adults is 250 mg once daily.

Skin infections:
Likely durations of treatment are as follows:
Tinea pedis (interdigital, plantar/ moccasin type): 2 to 6 weeks.
Tinea corporis: 4 weeks
Tinea cruris: 2 to 4 weeks

Onychomycosis: The duration of treatment for the majority of patients is between 6 weeks and 3 months. Treatment periods of less than 3 months may be sufficient in younger patients or in patients with fingernail infection or toenail infection other than of the big toe. Although a 3-month treatment period is usually sufficient in the treatment of toenail infections, a few patients may require treatment for 6 months or more. Poor nail outgrowth during the first weeks of therapy may help to identify the need for prolonged therapy.
Signs and symptoms of infection may persist after mycological cure and it may take several weeks for complete resolution to occur.

Children:
Due to limited data, use of LAMISPOR 250 in children is not recommended.

Elderly:
There is no evidence to suggest that elderly patients require different dosages or experience side-effects different to those of younger patients. The possibility of impairment of liver or kidney function should be considered in this age group.

Impaired renal function:
Patients with impaired renal function (creatinine clearance less than 50 mL/minute or serum creatinine of more than 300 mmol/L) should receive half the normal dose.

SIDE-EFFECTS AND SPECIAL PRECAUTIONS:
Side-effects:
Haematological system disorders
:
Less frequent: Neutropenia, thrombocytopenia and agranulocytosis.
Nervous system disorders:
Less frequent: Psychiatric disturbances such as depression and anxiety, headache, paraesthesia, hypoaesthesia, dizziness, vertigo, malaise and fatigue.
Gastrointestinal system disorders:
Frequent: Dyspepsia, fullness, loss of appetite, nausea, mild abdominal pain, diarrhoea.
Taste loss and taste disturbance have been reported in approximately 0.6 % of patients treated with LAMISPOR 250. This usually resolves slowly on medicine discontinuation.
Hepatobiliary system disorders:
Frequent: Jaundice, cholestasis and hepatitis. If hepatic dysfunction develops, treatment with LAMISPOR 250 should be discontinued (see also “Special Precautions”).
Skin and subcutaneous disorders:
Less frequent: Stevens-Johnson syndrome, toxic epidermal necrolysis, rash, urticaria, photosensitivity and angioneurotic oedema, psoriasis. If progressive skin rash occurs, treatment with LAMISPOR 250 should be discontinued.
Other side-effects reported include:
Musculoskeletal disorders including arthralgia and myalgia. These may occur as part of a hypersensitivity reaction in association with allergic skin reactions.

Special Precautions:
Rarely, cases of cholestasis and hepatitis have been reported, these usually occur within two months of starting treatment.
Signs and symptoms suggestive of liver dysfunction include pruritus, unexplained persistent nausea, anorexia, tiredness, jaundice, vomiting, fatigue, abdominal pain, and dark urine or pale stools. If a patient presents with these signs or symptoms, hepatic origin should be confirmed and therapy with LAMISPOR 250 should be discontinued. Pharmacokinetic studies in patients with pre-existing liver disease who received single doses have shown that the clearance of LAMISPOR 250 may be reduced by approximately 50%. Since the therapeutic use of LAMISPOR 250 in patients with chronic or active liver disease has not been studied in prospective clinical trials, its use in these circumstances is not recommended.
Due to reports of very rare cases of exacerbation of psoriasis, LAMISPOR 250 should be used with caution in patients with psoriasis.

KNOWN SYMPTOMS OF OVERDOSAGE AND PARTICULARS OF ITS TREATMENT:
There have been a few reports of overdose (up to 5 g) with the following symptoms: headache, nausea, epigastric pain and dizziness. In such instances the recommended treatment consists of the administration of activated charcoal to eliminate further absorption of the medicine. Supportive therapy should be provided as needed.

IDENTIFICATION:
White, circular, biconvex tablets with deep score on one side and TF embossed on the other side.

PRESENTATION:
Supplied in white opaque PVC and aluminium foil blister strips of 14 tablets.

STORAGE CONDITIONS:
Store below 25°C. Protect from light.
STORE THIS MEDICINE OUT OF REACH OF CHILDREN.
Keep the blisters in the outer carton until required for use.

REGISTRATION NUMBER:
A40/20.2.2/0614

NAME AND BUSINESS ADDRESS OF THE HOLDER OF THE CERTIFICATE OF REGISTRATION:
CIPLA MEDPRO (PTY) LTD
Rosen Heights, Pasita Street,
Rosen Park, Bellville, 7530 RSA

DATE OF PUBLICATION OF THIS PACKAGE INSERT:
January 2009

© CIPLA MEDPRO (PTY) LTD

DP49 A

New addition to this site: December 2016.
Source: http://www.cipla.co.za/wp-content/uploads/2013/10/sep_lamispor.pdf

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