Acnelak Ret

Uses

Clindamycin + Tretinoi is used for the treatment of acne vulgaris.

Acnelak Ret is also used to associated treatment for these conditions: Abscess, Intra-Abdominal caused by Anaerobic Bacterial Infection, Acne Vulgaris, Babesiosis, Bacterial Endocarditis, Bacterial Vaginosis (BV), Bloodstream Infections caused by Anaerobic Bacterial Infection, Bone and Joint Infections caused by susceptible Staphylococcus, Empyema caused by Anaerobic Bacterial Infection, Endometritis caused by Anaerobic Bacterial Infection, Lung Abscess caused by Anaerobic Bacterial Infection, Malaria caused by Plasmodium falciparum, Mixed Vaginal Infections, Pelvic cellulitis caused by Anaerobic Bacterial Infection, Peritonitis caused by Anaerobic Bacterial Infection, Pneumocystis Jirovecii Pneumonia, Pneumonitis caused by Anaerobic Bacterial Infection, Respiratory Tract Infections (RTI) caused by susceptible Staphylococcus, Respiratory Tract Infections (RTI) caused by susceptible pneumococci, Respiratory Tract Infections (RTI) caused by susceptible streptococci, Skin Structures and Soft Tissue Infections caused by Anaerobic Bacterial Infection, Skin Structures and Soft Tissue Infections caused by susceptible Staphylococcus, Skin Structures and Soft Tissue Infections caused by susceptible streptococci, Toxoplasmosis, Tubo-ovarian abscess caused by Anaerobic Bacterial Infection, Vaginal Candidiasis, Vaginal Mycosis, Chronic Bone and Joint Infections caused by Susceptible infections, Moderate Acne vulgaris, Post-surgical vaginal cuff infection caused by Anaerobic Bacterial Infection, Viridans group streptococciAcne Vulgaris, Alopecia, Cornification and dystrophic skin disorders, FAB classification M3 Acute promyelocytic leukemia, Skin hyperpigmentation, Solar Lentigines, Facial fine wrinkling, Keratinization disorders of the feet, Keratinization disorders of the hand, Moderate Melasma, Mottled hyperpigmentation, Severe Melasma, Severe, recalcitrant Cystic acne, Tactile roughness of facial skin

How Acnelak Ret works

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.

Tretinoin binds to alpha, beta, and gamma retinoic acid receptors (RARs). RAR-alpha and RAR-beta have been associated with the development of acute promyelocytic leukemia and squamous cell cancers, respectively. RAR-gamma is associated with retinoid effects on mucocutaneous tissues and bone. Although the exact mechanism of action of tretinoin is unknown, current evidence suggests that the effectiveness of tretinoin in acne is due primarily to its ability to modify abnormal follicular keratinization. Comedones form in follicles with an excess of keratinized epithelial cells. Tretinoin promotes detachment of cornified cells and the enhanced shedding of corneocytes from the follicle. By increasing the mitotic activity of follicular epithelia, tretinoin also increases the turnover rate of thin, loosely-adherent corneocytes. Through these actions, the comedo contents are extruded and the formation of the microcomedo, the precursor lesion of acne vulgaris, is reduced. Tretinoin is not a cytolytic agent but instead induces cytodifferentiation and decreased proliferation of APL cells in culture and in vivo. When Tretinoin is given systemically to APL patients, tretinoin treatment produces an initial maturation of the primitive promyelocytes derived from the leukemic clone, followed by a repopulation of the bone marrow and peripheral blood by normal, polyclonal hematopoietic cells in patients achieving complete remission (CR). The exact mechanism of action of tretinoin in APL is unknown.

Dosage

Acnelak Ret dosage

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

Clindacin plus gel: When the skin is completely dried (about 30 minutes later) apply a pea-size amount of Clindacin plus gel to your fingertip and spread it over your face once daily preferably at bed time. Treatment should be continued for 12 weeks or as directed by the physician.

Eye, lip or nose contact should be avoided while applying Clindacin plus gel.

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

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

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

Clindacin plus gel is not for oral, ophthalmic, or Intravaginal use.

Avoid exposure to sunlight and sunlamps. Wear sunscreen daily.

Interaction

Clindamycin & Tretinoin should be used with caution in patients receiving neuromuscular agents, erythromycin, tetracyclines, quinolone and other topical products (eg. Alcohol, drying agent).

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

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.

1-31% (topical)

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.

0.5-2 hours

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

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: 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 or tretinoin excreted through breast milk following topical administration. However, Clindacin plus gel can be used during lactation with caution.

Contraindication

Contraindicated in patients with hypersensitivity to clindamycin or tretinoin or any of the ingredients of these medicine.

Special Warning

Pediatric Uses: Safety and effectiveness in children below 12 years of age have not been established.

Acute Overdose

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.

Interaction with other Medicine

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.

Storage Condition

Store in a cool (below 25° C) and dry place away from light. Do not freeze.

Innovators Monograph

You find simplified version here Acnelak Ret