Bezclin

Bezclin Uses, Dosage, Side Effects, Food Interaction and all others data.

Benzoyl peroxide has mild keratolytic effect and antimicrobial activity due to release of free-radical oxygen which oxidizes bacterial protein. It is active against Staphylococcus epidermidis and Propionibacterium acnes.

Benzoyl peroxide is a topical treatment for acne that generates free radicals to break down comedones and increase the rate of epithelial cell turnover. It has a short duration of action as its active free radical metabolites quickly react to form inactive metabolites. The therapeutic index is wide, as overdoses are rare, however patients may still experience skin peeling. Patients should be counselled regarding increased risks of skin irritation, dryness, and sunburn.

Clindamycin is a lincosamide antibiotic used in the treatment of infections caused by susceptible microorganisms. Clindamycin is a semisynthetic antibiotic derived from lincomycin. It has antiacne and antibacterial activity. It binds with the 50s subunit of the bacterial ribosome and inhibits the early stage of protein synthesis. It is highly potent against gram positive and anaerobic bacteria.

Microbiology: Aerobic gram-positive cocci, including: Staphylococcus aureus, Staphylococcus epidermidis (penicillinase and non-penicillinase producing strains), Streptococci, Pneumococci. Anaerobic gram-negative bacilli, including: Bacteroides species, Fusobacterium species. Anaerobic gram-positive non-spore forming bacilli, including: Propionibacterium species, Eubacterium species, Actinomyces species. Anaerobic and microaerophilic gram-positive cocci, including: Peptococcus species, Peptostreptococcus species, Microaerophilic streptococci, C. perfringes

Clindamycin exerts its bacteriostatic effect via inhibition of microbial protein synthesis. Clindamycin has a relatively short Tmax and half-life necessitating administration every six hours to ensure adequate antibiotic concentrations.

Clostridium difficile associated diarrhea (CDAD) has been observed in patients using clindamycin, ranging in severity from mild diarrhea to fatal colitis and occasionally occurring over two months following cessation of antibiotic therapy. Overgrowth of C. difficile resulting from antibiotic use, along with its production of A and B toxins, contributes to morbidity and mortality in these patients. Because of the associated risks, clindamycin should be reserved for serious infections for which the use of less toxic antimicrobial agents are inappropriate.

Clindamycin is active against a number of gram-positive aerobic bacteria, as well as both gram-positive and gram-negative anaerobes. Resistance to clindamycin may develop, and is generally the result of base modification within the 23S ribosomal RNA. Cross-resistance between clindamycin and lincomycin is complete, and may also occur between clindamycin and macrolide antibiotics (e.g. erythromycin) due to similarities in their binding sites.

Bezclin
Uses
Dosage
Side Effect
Precautions
Interactions
Uses during Pregnancy
Uses during Breastfeeding
Accute Overdose
Food Interaction
Half Life
Volume of Distribution
Clearance
Interaction With other Medicine
Contradiction
Storage

Trade Name	Bezclin
Generic	Benzoyl Peroxide + Clindamycin
Weight	5%w/w, 1%w/w
Type	Gel
Therapeutic Class
Manufacturer	Derma Techno Pakistan
Available Country	Pakistan
Last Updated:	September 19, 2023 at 7:00 am

Uses

Topical therapy for the treatment of acne vulgaris.

Clindacin lotion is used for the treatment of acne vulgaris.

Other uses of topical Clindamycin lotion are:

• Skin infections such as erythrasma caused by Corynebacterium minutissimum; rosacea, periorificial dermatitis, folliculitis, stasis, chronic lymphaedema and familial pemphigus.

• Dermal ulcers.

How Bezclin works

Acne vulgaris is caused by inflammation in the pilosebaceous gland. Acne is generally caused by increased excretion of sebum from pilosebaceous glands, endocrine factors such as androgenic hormones, keratin developing around follicles, bacterial growth, and inflammation. These factors contribute to the formation of comedones (whiteheads and blackheads).

The peroxide bond of benzoyl peroxide is cleaved to form 2 benzoyloxy radicals. These radicals interact nonspecifically with bacterial proteins, interfering with their function, and survival of the bacteria. Over time, free radical interactions with bacterial proteins lead to decreased keratin and sebum around follicles.

Benzoyl peroxide can also increase the turnover rate of epithelial cells, leading to skin peeling, and breaking down comedones.

Clindamycin inhibits bacterial protein synthesis by binding to 23S RNA of the 50S subunit of the bacterial ribosome. It impedes both the assembly of the ribosome and the translation process. The molecular mechanism through which this occurs is thought to be due to clindamycin's three-dimensional structure, which closely resembles the 3'-ends of L-Pro-Met-tRNA and deacylated-tRNA during the peptide elongation cycle - in acting as a structural analog of these tRNA molecules, clindamycin impairs peptide chain initiation and may stimulate dissociation of peptidyl-tRNA from bacterial ribosomes.

The mechanism through which topical clindamycin treats acne vulgaris is unclear, but may be related to its activity against Propionibacterium acnes, a bacteria that has been associated with acne.

Dosage

Bezclin dosage

Adult: As 2.5-10% preparation: Apply 1-2 times daily after cleansing, may gradually increase to tid if needed. Start with lower strength preparations.

As cleanser: Wash 1-2 times daily.

Child: ≥12 yr Same as adult dose.

At first wash the face or affected area gently with warm water or soap.

Clindacin lotion: When the skin is completely dried (about 30 minutes later) apply a thin film of Clindacin lotion to the entire affected area twice daily. Applied area should not be washed within 3 hours. Noticeable improvement is usually seen after about 6 weeks . However, 8 to 12 weeks of treatment may be required for maximum benefit. Eye, lip or nose contact should be avoided while applying Clindacin lotion.

Clindamycin Lotion 1%: Clean the face or affected area gently with warm water or soap as recommended by the physician. After the skin is dried, apply a thin film of lotion to the affected areas twice daily, in the morning and in the evening.

Do not wash within three hours after using lotion. The treatment period is usually 6 weeks or as advised by the physician.

However, 8 to 12 weeks of treatment may be required for maximum benefit.

Clindamycin 2% Vaginal preparation: One applicator full (approximately 5 gm) intravaginally at bedtime for 7 consecutive days. In patients in whom a shorter treatment course is desirable, a 3 day regimen has been shown to be effective.

Side Effects

The major adverse reaction reported to date with Benzoyl Peroxide cutaneous therapy is irritation of the skin including erythema, burning, peeling, dryness, itching, stinging, feeling of skin tension locally at the site of application. This is reversible when treatment is reduced in frequency or discontinued. Allergic contact dermatitis, including face oedema, may occur.

Side effects are usually rare. Possible side-effects may includes skin rash, itching, oily skin, dryness, erythema, burning, change in skin color, diarrhea, colitis, GI disturbance etc.

Toxicity

Data regarding overdoses of benzoyl peroxide are not readily available. During an overdose patients may experience and increased risk or severity of adverse effects such as skin itching, burning, peeling, inflammation, and erythema.

The oral LD₅₀ in rats is 490 mg/kg.

The oral LD₅₀ in mice and rats is 2540 mg/kg and 2190 mg/kg, respectively.

While no cases of overdose have been reported, symptoms are expected to be consistent with the adverse effect profile of clindamycin and may therefore include abdominal pain, nausea, vomiting, and diarrhea. During clinical trials, one 3-year-old child was given a dose of 100 mg/kg daily for 5 days and showed only mild abdominal pain and diarrhea. Activated charcoal may be of value to remove unabsorbed drug, but hemodialysis and peritoneal dialysis are ineffective. General supportive measures are recommended in cases of clindamycin overdose.

Precaution

Children, Pregnancy and lactation.

Clindacin lotion is not for oral, ophthalmic, or Intravaginal use.

Avoid exposure to sunlight and sunlamps. Wear sunscreen daily.

Interaction

There is no known interaction with other medications which might be used cutaneously and concurrently with Benzoyl Peroxide; however, drugs with desquamative, irritant and drying effects should not be used concurrently with Benzoyl Peroxide gel.

Clindamycin enhance the action of other neuromuscular blocking agents. Therefore, it should be used with caution in patients receiving such agents. Antagonism has been demonstrated between clindamycin and erythromycin in vitro. Because of possible clinical significance, these two drugs should not be administered concurrently.

Volume of Distribution

Clindamycin is widely distributed in the body, including into bone, but does not distribute into cerebrospinal fluid. The volume of distribution has been variably estimated between 43-74 L.

Elimination Route

In a sample of excised skin, 1.9% of a radiolabelled topical dose fully penetrates the skin, and 2.6% remains in the skin. The radiolabelled dose that fully penetrates the skin is recovered as benzoic acid, while the dose in the skin is approximately half benzoic acid and half benzoyl peroxide. 95.5% of a radiolabelled dose is not absorbed or metabolized after 8 hours.

Oral bioavailability is nearly complete, at approximately 90%, and peak serum concentrations (C_max) of, on average, 2.50 µg/mL are reached at 0.75 hours (T_max). The AUC following an orally administered dose of 300mg was found to be approximately 11 µg•hr/mL. Systemic exposure from the administration of vaginal suppository formulations is 40-fold to 50-fold lower than that observed following parenteral administration and the C_max observed following administration of vaginal cream formulations was 0.1% of that observed following parenteral administration.

Half Life

The elimination half-life of clindamycin is about 3 hours in adults and 2.5 hours in children. Half-life is increased to approximately 4 hours in the elderly.

Clearance

The plasma clearance of clindamycin is estimated to be 12.3-17.4 L/h, and is reduced in patients with cirrhosis and altered in those with anemia.

Elimination Route

Benzoyl peroxide's metabolite benzoic acid, is eliminated in the urine. Data regarding fecal elimination is not readily available.

Approximately 10% of clindamycin bioactivity is excreted in the urine and 3.6% in the feces, with the remainder excreted as inactive metabolites.

Pregnancy & Breastfeeding use

Pregnancy Category C. Either studies in animals have revealed adverse effects on the fetus (teratogenic or embryocidal or other) and there are no controlled studies in women or studies in women and animals are not available. Drugs should be given only if the potential benefit justifies the potential risk to the fetus.

Pregnancy: There is no adequate data for safe use in pregnancy. Animal studies showed no adverse effects on the fetus.

Lactation: It is not known that whether Clindamycin is excreted through breast milk following topical administration. However, Clindacin lotion can be used during lactation with caution.

Contraindication

Benzoyl Peroxide gel is contra-indicated in patients with known hypersensitivity to Benzoyl Peroxide.

Clindamycin is contraindicated in patients previously found to be sensitive to clindamycin or any of the ingredients of this medicine.

Acute Overdose

Benzoyl Peroxide gel is a preparation indicated for topical treatment only. If the medication is applied excessively, no more rapid or better results will be obtained and severe irritation might develop. In this event, treatment must be discontinued and appropriate symptomatic therapy should be instituted.

Overdosage with orally administered clindamycin has been rare. Adverse reactions similar to those seen with normal doses can be expected, however, unexpected reactions could occur. Haemodialysis and peritoneal dialysis are not effective in removing clindamycin from the serum. Overdosage should be treated with simple gastric lavage. No specific antidote is known.