LLCOL Cream
( Luliconazole Cream IP )
Composition :
Luliconazole IP 1.0% w/w
preservatives :
Benzyl Alcohol IP 1.0% w/w
Cream Base q.s.
DESCRIPTION :
Luliconazole cream 1% w/w contains luliconazole, an azole anti-fungal agent in a cream formulation for topical application. Luliconazole is (2E)-2-[(4R)-4-(2,4-dichlorophenyl)-1 ,3-dithiolan-2-ylidene]2-imidazol-1ylacetonitrile.
The molecular formula is C14 H9 CL2 N2 S2 with a molecular weight of 354.28 g/mol
CLINICAl PHARMACOLOGY
PHARMACODYNAMICS:
Luliconazole is an antifungal that belongs to the azole class, Luliconazole appears to inhibit ergosterol synthesis by inhibiting the enzyme lanosterol demethylase. Inhibition of this enzyme's activity of azoles results in decreased amounts of ergosterol, a constituent of fungal cell membranes, and a corresponding accumulation of lanosterol.
PHARMACOKINETICS:
Luliconazole is the R-enantiomer of a chiral molecule. The potential for enter-conversion between R and S-enantiomer in humans has not been assessed, Information on the pharmacokinetics of luliconazole presented below refers to both R-enantiomer and S-enantiomer. Luliconazole is >99% protein bound in plasma.
In a pharmacokinetic trial, 12 subjects with moderate to severe tinea pedis and 8 subjects with moderate to severe tinea cruris applied a mean daily amount of approximately 3.5 grams of luliconazole cream, 1% to the affected and surrounding areas once daily for 15 days, Plasma concentration of luliconazole on day 15 were measurable in all subjects and fluctuated little during the 24 hour interval.
In subjects with tinea pedis, the mean +- SD of the maximum concentration (Cmax) was 0.40 +- 0.76ng/mL after the first dose and 0.93 +- 1.23ng/mL after the final dose, The mean time to reach Cmax (Tmax) was 16.9 +- 9.39hours after the first dose and 5.8 +- 7.61 hours after the final dose, Exposure to luliconazole, as expressed by urea under the concentration time curve (AUC 0-24) was 6.88 +- 14.50 ng*hr/mL after the first dose and 18.74 +- 27.05 ng*hr/mL after the final dose.
In subjects with tinea cruris, the mean +- SD Cmax was 4.91 +- 2.51 ng/mL after the first dose and 7.36 +- 2.66 ng/mL after the final dose. The mean Tmax was 21.0 +- 5.55 hour after the first dose and 6.5 +- 8.25 hours after the final dose. Exposure to luliconazole, as expressed by AUC 0.24 was 85.1 +- 43.69 ng*hr/mL after the first dose and 121.74 +- 53.36 ng*hr/mL after the final dose.
SPECIAL PRECAUTIONS:
PREGNANCY:
Pregnancy Category:C
There are no adequate and well-controlled studies of luliconazole cream 1% w/w in pregnant women, It should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.
NURSING MOTHERS:
It is not known whether luliconazole is excreted in human milk, Because many drugs are excreted in human milk, caution should be exercised when luliconazole cream 1% w/w is administered to women who are breastfeeding.
PEDIATRIC USE:
The safety and effectiveness of luliconazole cream 1% w/w in pediatric patients have not been established. The number of pediatric patient's >12 year of age were too small to adequately assess safety and efficacy.
GERIATRIC USE:
No overall differences in safety or effectiveness were observed between these subjects and younger subjects, and other reported clinic al experience has not identified difference in responses between the elderly and younger patients, but greater sensitivity of some older individual cannot be ruled out.
INDICATIONS (S):
Luliconazole cream 1% w/w is indicated for the treatment of cutaneous mycosis viz. Tinea pedis, tinea corporis, tinea cruris.
DOSAGE AND ADMINISTRATION:
For topical use only.
Luliconazole cream 1% is not for ophthalmic, oral or intravaginal use.
When treating inter-digital tinea pedis, a thin layer of luliconazole cream 1% w/w should be applied to the affected area and approximately 1 inch of the immediate surrounding area (s) once daily for two (2) weeks.
When treating tinea, cruris or tinea corporis, luliconazole cream 1% w/w should be applied to the affected area and approximately 1 inch of the immediate surrounding area (s) once daily for (1) week.
CONTRAINDICATIONS:
Know hypersensitivity to luliconazole or any of the excipients contained in the cream.
ADVERSE EFFECTS:
During clinical trials with luliconazole cream 1% w/w, the most common adverse reactions were application site reactions which occurred in less than 1% of subjects. Most adverse reactions were mild in severity.
During the Post-Marketing Experience (PME), the following adverse reactions have been identified during use of luliconazole cream 1% w/w: Contact dermatitis and cellulitis.
Because these reactions are reported voluntarily from a population of uncertain size, it is not always possible to reliable estimate their frequency or establish a causal relationship to drug exposure.
DRUG INTERACTIONS:
The potential of luliconazole to inhibit cytochrome P-450 (CYP) enzymes 1A2, 2C9, 2C19, 2D6, and 3A4 was evaluated in vitro. Based on in vitro assessment, luliconazole at therapeutic doses, particularly when applied to patients with moderate to severe tinea cruris, may inhibit the activity of CYP2C19 and CPY3A4. However, no in vivo drug interaction trial have been conducted evaluate the effect of luliconazole on other drugs that are substrates of CYP2C19 and CYP3A4.
Luliconazole is not expected to inhibit CYPs 1A2, 2C9 and 2DC based on in vitro assessment. The induction potential of luliconazole on CYP enzymes has not been evaluated.
STORAGE:
Store at a temperature not exceeding 30℃. Do not freeze.
Keep out of reach of children
Avoid contact with eyes
PRESENTATION:
- 5 gm
- 20 gm
- 50 gm
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