Clinsol Plus Tube

Clinsol Plus Tube Uses, Dosage, Side Effects, Food Interaction and all others data.

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.

Isotretinoin is a synthetic retinoid which reduces sebaceous gland size and inhibits sebum production. It also regulates cell proliferation and differentiation and has dermal anti-inflammatory effect.

The pharmacodynamics of isotretinoin are poorly understood.

Clinsol Plus Tube
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	Clinsol Plus Tube
Generic	Clindamycin + Isotretinoin
Weight	1%w/w
Type	Gel
Therapeutic Class
Manufacturer	Leeford Healthcare Ltd
Available Country	India
Last Updated:	September 19, 2023 at 7:00 am

Uses

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.

Isotretinoin is used for the treatment of severe recalcitrant nodular acne. Nodules are inflammatory lesions with a diameter of 5 mm or greater. The nodules may become suppurative or hemorrhagic. Because of significant adverse effects associated with its use, Isotretinoin should be reserved for patients with severe nodular acne who are unresponsive to conventional therapy, including systemic antibiotics. In addition, Isotretinoin is used only for those female patients who are not pregnant, because Isotretinoin can cause severe birth defects.

A single course of therapy for 15 to 20 weeks has been shown to result in complete and prolonged remission of disease in many patients. If a second course of therapy is needed, it should not be initiated until at least 8 weeks after completion of the first course, because experience has shown that patients may continue to improve while off Isotretinoin . The optimal interval before re-treatment has not been defined for patients who have not completed skeletal growth

How Clinsol Plus Tube 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.

Isotretinoin produces its effects through altering progress through the cell cycle, cell differentiation, survival, and apoptosis. These actions reduce sebum production, preventing the blockage of pores, and growth of acne causing bacteria. Isotretinoin and 4-oxo-isotretinoin both significantly reduce the production of sebum. Isotretinoin has little to no affinity for retinol binding proteins (RBPs) and retinoic acid nuclear receptors (RARs). Tretinoin and 4-oxo-tretinion bind to the RAR-γ receptor, which is suspected to be part of the action of acne treatment by isotretinoin. Isotretinoin induces apoptosis in sebocytes, leading to a decrease in sebum production. Isotretinoin also reduces the formation of comedones by reducing hyperkeratinization through an unknown mechanism. Isotretinoin does not directly kill bacteria but it does reduce the size of sebum ducts and makes the microenvironment less hospitable to acne causing bacteria. It may also increase immune mechanisms and alter chemotaxis of monocytes to reduce inflammation.

There is preliminary evidence suggesting isotretinoin may interact with FoxO1, which may explain a substantial number of isotretinoin's unexplained actions.

Dosage

Clinsol Plus Tube dosage

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.

Oral-

Adult: Initially, 0.5 mg/kg daily in single or 2 divided doses, increased to 1 mg/kg daily if necessary. Usual duration of treatment: 16-24 wk. May repeat treatment course after at least 8 wk if relapse after first course.
Child: ≥12 yr Same as adult dose.

Topical:Apply Isotretinoin 0.05% gel cautiously over the affected area once or twice daily.Patients should be advised that 6-8 weeks of treatment may be required before a therapeuticeffect is observed. The safety and efficacy of Isotretinoin have not been established in children since acne vulgarisrarely present in this age group. There are no specific recommendations for use in the elderly.Acne vulgaris does not present in the elderly.

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.

Erythema, skin exfoliation, stinging sensation, pruritus, irritation, tenderness, dry skin, hirsutism, photosensitivity, skin pigmentation, paronychia, nail dystrophy, pyogenic granuloma, increased sweating, corneal opacities, visual disturbances, headache, nausea and vomiting, arthralgia, myalgia, back pain, intracranial HTN, hyperostosis and calcinosis. Elevation of serum triglycerides, LFTs, ESR and blood glucose. Mood changes, psychotic symptoms, depression and suicidal behaviour.

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.

Patients experiencing an overdose may present with vomiting, facial flushing, cheilosis, abdominal pain, headache, dizziness, and ataxia. These symptoms may rapidly resolve. Generally no treatment is required for these overdoses.

The oral lowest dose causing toxic effect (TDLO) for children is 30mg/kg/21W, oral TDLO for men is 24mg/kg/4W, oral TDLO for women is 56mg/kg/8W. The intraperitoneal LD₅₀ for rats is 901mg/kg, oral LD₅₀ for mice is 3389mg/kg, oral LD₅₀ for rats is >4000mg/kg.

Isotretinoin is associated with major congenital malformations, spontaneous abortion, and premature birth. It is unknown if isotretinoin is expressed in breast milk but due to the associated hazards a decision should be made to either stop nursing or stop taking isotretinoin.

In animal studies, isotretinoin was associated with an increased risk of pheochromocytoma and adrenal medullary hyperplasia at doses above the recommended clinical dose. Isotretinoin was negative for the Ames test of mutagenicity once and weakly positive a second time. It has not been shown to be clastogenic. A study in dogs noted testicular atrophy after doses of 10-30 times the recommended clinical dose for 30 weeks. In trials with men there were no effects seen on sperm count, motility, morphology, ejaculate volume, and seminal plasma fructose.

Precaution

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

Avoid exposure to sunlight and sunlamps. Wear sunscreen daily.

Women of childbearing potential; anorexia nervosa. History of photoallergy, psychiatric disorder (e.g. depression); pre-existing or predisposition to hypertriglyceridaemia (e.g. DM, obesity or increased alcohol intake). Genetic predisposition for age-related osteoporosis, history of childhood osteoporosis, osteomalacia or other bone metabolism disorders. Not intended for the treatment of prepubertal acne. Severe renal impairment.

Interaction

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.

Additive adverse effects with vit A or its derivatives. Decreased efficacy of microdosed progesterone (use 2 forms of contraception).Increased risk of local irritation with topical keratolytic or exfoliative anti-acne agents. Oxidising agents (e.g. benzoyl peroxide) may reduce the efficacy of topical isotretinoin.

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.

The volume of distribution in humans is unknown because there is no intravenous preparation. In a study of pediatric patients with neuroblastoma the volume of distribution was found to be 85L. The volume of distribution was also found to be 2432mL/kg in guinea pigs and 1716mL/kg in obese rats.

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.

Patients reach a maximum concentration of 74-511ng/mL after 1-4 hours following a 100mg oral dose. Isotretinoin is better absorbed with a high fat meal and bioavailability may change from one brand to another.

Following a 40mg oral dose, fasted subjects reached a maximum concentration of 314ng/mL in 2.9 hours with an area under the curve of 4055ng/mL*hr. Subjects given a high fat meal and a 40mg oral doses reached a maximum concentration of 395ng/mL in 6.4 hours with an area under the curve of 6095ng/mL*mL.

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.

The half life ranges from 7-39 hours with a mean elimination half life of 20 hours. The half life of 4-oxo-13-cis-retinoic acid ranges from 17-50 hours with a mean elimination half life of 25 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.

The clearance of isotretinoin is 15.9L/h in pediatric patients with neuroblastoma. Clearance is also 21.3mL/min/kg in guinea pigs and 7.2mL/min/kg in obese rats.

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.

Isotretinoin and its metabolites are conjugated and excreted in the urine and feces in similar amounts. 53-74% of an oral dose is eliminated as unchanged isotretinoin in the feces.

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 is excreted through breast milk following topical administration. However, Clindacin lotion can be used during lactation with caution.

Category X: Studies in animals or human beings have demonstrated foetal abnormalities or there is evidence of foetal risk based on human experience or both, and the risk of the use of the drug in pregnant women clearly outweighs any possible benefit. The drug is contraindicated in women who are or may become pregnant.

Contraindication

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

Hypervitaminosis A, hyperlipidaemia. Hepatic impairment. Pregnancy and lactation. Concomitant admin of tetracycylines.

Special Warning

Renal Impairment: Oral: Severe: Reduce initial dose (e.g. 10 mg daily), then gradually increase to 1 mg/kg as necessary.

Hepatic Impairment: Oral: Contraindicated.

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.