Consists of adapalene, clindamycin
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Klenzit-C Actions |
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Consists of adapalene, clindamycin
Adapalene acts on retinoid receptors. Biochemical and pharmacological profile studies have demonstrated that adapalene is a modulator of cellular differentiation, keratinization, and inflammatory processes all of which represent important features in the pathology of acne vulgaris.
Mechanistically, adapalene binds to specific retinoic acid nuclear receptors but does not bind to the cytosolic receptor protein. Although the exact mode of action of adapalene is unknown, it is suggested that topical adapalene normalizes the differentiation of follicular epithelial cells resulting in decreased microcomedone formation.
It is very important that you use adapalene only as directed. Do not use more of it, do not use it more often, and do not use it for a longer time than your doctor ordered. To do so may cause irritation of the skin.
Do not apply adapalene to windburned or sunburned skin or on open wounds.
Do not use adapalene in or around the eyes, lips, or inside of the nose. Spread the medicine away from these areas when applying. If the medicine accidently gets on these areas, wash with water at once.
Apply the medicine to clean, dry areas of the skin affected by acne. Rub in gently and well. Wash your hands afterwards to remove any medicine that may remain on them.
To help clear up your acne completely, it is very important that you keep using adapalene for the full time of treatment, even if your symptoms begin to clear up after a short time. If you stop using adapalene too soon, your acne may return or get worse.
The dose of adapalene will be different for different patients. Follow your doctor's orders or the directions on the label. The following information includes only the average doses of adapalene. If your dose is different, do not change it unless your doctor tells you to do so.
The amount of medicine that you take depends on the strength of the medicine. Also, the number of doses you take each day, the time allowed between doses, and the length of time you take the medicine depend on the medical problem for which you are using the medicine.
If you miss a dose of adapalene, skip the missed dose and go back to your regular dosing schedule. Do not double doses.
Store the medicine in a closed container at room temperature, away from heat, moisture, and direct light. Keep from freezing.
Keep out of the reach of children.
Do not keep outdated medicine or medicine no longer needed.
Use adapalene topical exactly as your doctor has prescribed it for you. Using more medicine or applying it more often than prescribed will not make it work any faster, and may increase side effects. Do not use this medication for longer than your doctor has prescribed.
Adapalene topical is usually applied once daily in the evening.
Wash your hands before applying adapalene topical.
Clean your skin with a mild cleanser (not soap) before applying the medication. Pat the skin dry with a clean towel.
Apply the medication in a thin layer to the entire face or other affected skin areas. Do not apply any other skin products unless your doctor has told you to.
Use this medication for as many days as it has been prescribed for you even if you think it is not working. It may take weeks or months of use before you notice improvement in your skin. Your acne may get slightly worse for a short time when you first start using the medication. Call your doctor if skin irritation becomes severe or if your acne does not improve within 8 to 12 weeks.
Store adapalene topical at room temperature away from moisture and heat.
Adapalene binds to specific retinoic acid nuclear receptors but does not bind to cytosolic receptor protein. Biochemical and pharmacological profile studies have demonstrated that adapalene is a modulator of cellular differentiation, keratinization and inflammatory processes. However, the significance of these findings with regard to the mechanism of action of adapalene for the treatment of acne is unknown.
Pharmacodynamics of Adapalene (Klenzit-C) is unknown.
Systemic exposure of adapalene following a topical application of Adapalene (Klenzit-C) was studied in two pharmacokinetic (PK) clinical trials.
The first trial was conducted in 14 adult subjects 18 to 29 years of age with severe acne and the second trial was conducted in 13 adolescent subjects 12 to 17 years of age with moderate to severe acne.
In each trial, subjects were treated with 2 g of Adapalene (Klenzit-C) applied once daily applied to approximately 1000 cm2 of acne involved skin for 28 days (adolescent subjects) or 30 days (adult subjects). Serial plasma samples were collected at 24 or 72 hours following application on days 1, 15 and 28/30. Daily topical application of Adapalene (Klenzit-C) resulted in low systemic exposure to adapalene in the two populations (adult and adolescent subjects). In the adult population, all plasma concentrations in 12 out of 14 subjects were below the limit of quantification (LOQ=0.1 ng/mL). One subject had one sample above LOQ at day 30 and the other subject had four plasma samples above LOQ on both days 1 and 15, which ranged from 0.102 and 0.131 ng/mL. In the adolescent population, plasma concentrations were quantifiable (>0.1 ng/mL) in five subjects. On Day 28, the mean Cmax was 0.128± 0.049 ng/mL (range: <0.100 to 0.244 ng/mL) and the mean of AUC0-24hr was 3.07 ± 1.21 ng.hr/mL (range: 1.86 to 4.93 ng.hr/mL). Adapalene plasma concentrations in all subjects were below the limit of quantification (<0.1 ng/mL) 48 hours after the last application on Day 28.
Pharmacology: Pharmacodynamics: Although clindamycin phosphate is inactive in vitro, rapid in vivo hydrolysis converts this compound to the antibacterially active clindamycin. Clindamycin has been shown to have in vitro activity against isolates of Propionibacterium acnes cultures tested [minimum inhibitory concentration (MICs) 0.4 mcg/mL]. This may account for its usefulness in acne. Free fatty acids on the skin surface have been decreased from approximately 14-2% following application of clindamycin.
Cross-resistance has been demonstrated between clindamycin and lincomycin. Antagonism has been demonstrated between clindamycin and erythromycin.
Clindamycin has no fungicidal activity.
The in vitro inactive clindamycin phosphate is hydrolysed by phosphatases of the skin to active clindamycin base.
Pharmacokinetics: Following multiple topical applications of clindamycin phosphate at a concentration equivalent to clindamycin 10 mg/mL in an isopropyl alcohol and water solution, very low levels of clindamycin are present in the serum (0-3 ng/mL) and <0.2% of the dose is recovered in urine as clindamycin.
Following multiple topical applications of clindamycin phosphate at a concentration equivalent to clindamycin 10 mg/g in the gel formulation, 0.053% (morning) and 0.07% (evening) of the administered dose was recovered in the urine as clindamycin. Average absolute bioavailability was 1.6% and 2.2% after morning and evening doses, respectively.
Clindamycin activity has been demonstrated in comedones from acne patients. The mean concentration of antibiotic activity in extracted comedones after application of clindamycin (10 mg/mL) in an isopropyl alcohol and water solution for 4 weeks was 597 mcg/g of comedonal material (range 0-1,490 mcg/g).
Geriatric Use: Clinical studies for topical clindamycin did not include sufficient numbers of subjects ≥65 years to determine whether they respond differently from younger subjects.
Toxicology: Preclinical Safety Data: Carcinogenesis: Long-term studies in animals have not been performed with clindamycin to evaluate carcinogenic potential.
Mutagenesis: Genotoxicity tests performed included a rat micronucleus test and an Ames Salmonella reversion test. Both tests were negative.
Impairment of Fertility: Fertility studies in rats treated orally with up to 300 mg/kg/day (approximately 1.1 times the highest recommended adult human dose based on mg/m2) revealed no effects on fertility or mating ability.
In oral embryofetal development studies in rats and SC embryofetal development studies in rats and rabbits, no developmental toxicity was observed except at doses that produced maternal toxicity.
Before applying clindamycin, thoroughly wash the affected areas with warm water and soap, rinse well, and pat dry.
When applying the medicine, use enough to cover the affected area lightly. You should apply the medicine to the whole area usually affected by acne, not just to the pimples themselves. This will help keep new pimples from breaking out.
You should avoid washing the acne-affected areas too often. This may dry your skin and make your acne worse. Washing with a mild, bland soap 2 or 3 times a day should be enough, unless you have oily skin. If you have any questions about this, check with your doctor.
Topical clindamycin will not cure your acne. However, to help keep your acne under control, keep using clindamycin for the full time of treatment, even if your symptoms begin to clear up after a few days. You may have to continue using clindamycin every day for months or even longer in some cases. If you stop using clindamycin too soon, your symptoms may return. It is important that you do not miss any doses.
For patients using the topical foam form of clindamycin:
For patients using the topical solution form of clindamycin:
For patients using the topical suspension form of clindamycin:
The dose of clindamycin will be different for different patients. Follow your doctor's orders or the directions on the label. The following information includes only the average doses of clindamycin. If your dose is different, do not change it unless your doctor tells you to do so.
The amount of medicine that you take depends on the strength of the medicine. Also, the number of doses you take each day, the time allowed between doses, and the length of time you take the medicine depend on the medical problem for which you are using the medicine.
If you miss a dose of clindamycin, apply it as soon as possible. However, if it is almost time for your next dose, skip the missed dose and go back to your regular dosing schedule.
Store the medicine in a closed container at room temperature, away from heat, moisture, and direct light. Keep from freezing.
Keep out of the reach of children.
Do not keep outdated medicine or medicine no longer needed.
Take exactly as prescribed by your doctor. Do not take in larger or smaller amounts or for longer than recommended. Follow the directions on your prescription label.
Take this medicine with a full glass of water to keep it from irritating your throat.
Measure liquid medicine with a special dose-measuring spoon or medicine cup, not with a regular table spoon. If you do not have a dose-measuring device, ask your pharmacist for one.
Take this medicine for the full prescribed length of time. Your symptoms may improve before the infection is completely cleared. Skipping doses may also increase your risk of further infection that is resistant to antibiotics. Clindamycin will not treat a viral infection such as the common cold or flu.
To be sure this medication is not causing harmful effects, your blood may need to be tested often. Your kidney or liver function may also need to be tested. Visit your doctor regularly.
If you need surgery, tell the surgeon ahead of time that you are using clindamycin. You may need to stop using the medicine for a short time.
Store at room temperature away from moisture and heat. Do not store clindamycin liquid in the refrigerator.
Mechanism of action in acne vulgaris is unknown.
Pharmacodynamics of Clindamycin (Klenzit-C) Foam is unknown.
In an open label, parallel group study in 24 subjects with acne vulgaris, 12 subjects (3 male and 9 female) applied 4 grams of Clindamycin (Klenzit-C) Foam once-daily for five days, and 12 subjects (7 male and 5 female) applied 4 grams of a clindamycin gel, 1%, once daily for five days. On Day 5, the mean Cmax and AUC(0-12) were 23% and 9% lower, respectively, for Clindamycin (Klenzit-C) Foam than for the clindamycin gel, 1%.
Following multiple applications of Clindamycin (Klenzit-C) Foam, less than 0.024% of the total dose was excreted unchanged in the urine over 12 hours on Day 5.
No microbiology studies were conducted in the clinical trials with this product.
Clindamycin binds to the 50S ribosomal subunits of susceptible bacteria and prevents elongation of peptide chains by interfering with peptidyl transfer, thereby suppressing protein synthesis. Clindamycin has been shown to have in vitro activity against Propionibacterium acnes (P. acnes), an organism that has been associated with acne vulgaris; however, the clinical significance of this activity against P. acnes was not examined in clinical studies with Clindamycin (Klenzit-C) Foam. P. acnes resistance to clindamycin has been documented.
Inducible Clindamycin Resistance
The treatment of acne with antimicrobials is associated with the development of antimicrobial resistance in P. acnes as well as other bacteria (e.g. Staphylococcus aureus, Streptococcus pyogenes). The use of clindamycin may result in developing inducible resistance in these organisms. This resistance is not detected by routine susceptibility testing.
Cross Resistance
Resistance to clindamycin is often associated with resistance to erythromycin.
I'm a nursing mother and I've been having acne breakouts every now and then. This time round it got worse so i went to see a dermatologist who prescribed Klenzit gel yesterday. So I've only used it once, precisely yesternight and already i can see something positive. I woke up with most pimples dried out. I can't wait to see how i'll look like in two weeks..... |
Information checked by Dr. Sachin Kumar, MD Pharmacology
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