Efasol

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

Erythromycin Lotion is a bacteriostatic macrolide antibiotic, but may be bactericidal in high concentrations. Although the mechanism by which topical erythromycin acts in reducing inflammatory lessions of Acne vulgaris is unknown, it is presummable due to its antibiotic action.

Erythromycin tablet inhibits microsomal protein synthesis in susceptible organisms by inhibiting the translocation process. Specific binding to the 50S subunit or 70S ribosome occurs in these organisms but there is no binding to the stable 80S mammalian ribosome. Erythromycin is active against many Grampositive bacteria, some Gram-negative bacteria and against mycoplasmas and chlamydia.

Macrolides, such as erythromycin, stop bacterial growth by inhibiting protein synthesis and translation, treating bacterial infections. Erythromycin does not exert effects on nucleic acid synthesis. This drug has been shown to be active against most strains of the following microorganisms, effectively treating both in vitro and clinical infections. Despite this, it is important to perform bacterial susceptibility testing before administering this antibiotic, as resistance is a common issue that may affect treatment.

A note on antimicrobial resistance, pseudomembranous colitis, and hepatotoxicity

Tretinoin is structurally and pharmacologically related to vitamin A. Current evidence suggests that topical Tretinoin decreases cohesiveness of follicular epithelial cells with decreased microcomedone formation. Additionally, Tretinoin stimulates mitotic activity and increases turnover of follicular epithelial cells, causing extrusion of the comedones

Tretinoin, also known as all-trans-retinoic acid (ATRA), is a naturally occurring derivative of vitamin A (retinol). Retinoids such as tretinoin are important regulators of cell reproduction, proliferation, and differentiation and are used to treat acne and photodamaged skin and to manage keratinization disorders such as ichthyosis and keratosis follicularis. Tretinoin also represents the class of anticancer drugs called differentiating agents and is used in the treatment of acute promyelocytic leukemia (APL).

Trade Name Efasol
Generic erythromycin + tretinoin
Type
Therapeutic Class
Manufacturer
Available Country Malaysia
Last Updated: September 19, 2023 at 7:00 am
Efasol
Efasol

Uses

Erythromycin tablet is highly effective in the treatment of a wide variety of clinical infections, such as

  • Upper respiratory tract infections: Tonsillitis, peritonsillar abscess, pharyngitis, laryngitis, sinusitis, and secondary infections in cold and influenza.
  • Lower respiratory tract infections: Tracheitis, acute and chronic bronchitis. Mycoplasma pneumoniae (lobar pneumonia, broncho pneumonia, primary atypical pneumoniae), bronchiectasis.
  • Skin and soft tissue infections: Boils and carbuncles, paronychia, abscesses, pustular acne, impetigo, cellulitis, furuncolosis, erythrasma.
  • Veneral infections: Non-specific urethritis, syphilis (if the patient is allergic to penicillin).
  • Gastro-intestinal infections: Cholecystitis, Staphylococcal enterocolitis, infectious diarrhoea, & cholera.
  • Ear and oral infections: 0titis media and otitis externa, gingivitis, dental abscesses.
  • Prophylaxis: Pre-operative and post-operative, trauma, burns, rheumatic fever.
  • Other infections: Diphtheria, whooping cough.

For topical treatment of acne, pimples & bacterial skin infections susceptible to Erythromycin

  • For the treatment of acne vulgaris in which comedones, papules and pustules predominate.
  • For the treatment of hyperpigmentation, roughness and fine wrinkling of photodamaged skin due to chronic sun exposure.
  • For the treatment of Acute promyelocytic leukaemia

Efasol is also used to associated treatment for these conditions: Acne, Acne Vulgaris, Acute Otitis Media caused by Haemophilus Influenzae, Acute pelvic inflammatory disease caused by Neisseria Gonorrheae Infection, Bacterial Infections, Chancroid, Chlamydia Trachomatis, Chlamydial ophthalmia neonatorum, Community Acquired Pneumonia (CAP), Diphtheria, Erythrasma, Gastroparesis, Granuloma Inguinale, Intestinal amebiasis caused by entamoeba histolytica, Legionella Pneumophila Infections, Listeria infection, Lower Respiratory Tract Infection (LRTI), Lymphogranuloma Venereum, Nongonococcal urethritis, Ophthalmia neonatorum (gonococcal), Pertussis, Postoperative Infections, Primary Syphilis, Respiratory Tract Infections (RTI), Staphylococcal Skin Infections, Syphilis, Upper Respiratory Tract Infection, Ureaplasma urethritis, Whooping Cough, Inflammatory papular lesions, Mild Acne vulgaris, Moderate Acne vulgaris, Predominant skin comedones, papules and pustules, Prophylaxis of Rheumatic fever, Pustular lesions, Skin and skin-structure infections, Skin and subcutaneous tissue bacterial infections caused by streptococcus pyogenes, Superficial ocular infectionsAcne 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 Efasol works

In order to replicate, bacteria require a specific process of protein synthesis, enabled by ribosomal proteins. Erythromycin acts by inhibition of protein synthesis by binding to the 23S ribosomal RNA molecule in the 50S subunit of ribosomes in susceptible bacterial organisms. It stops bacterial protein synthesis by inhibiting the transpeptidation/translocation step of protein synthesis and by inhibiting the assembly of the 50S ribosomal subunit. This results in the control of various bacterial infections. The strong affinity of macrolides, including erythromycin, for bacterial ribosomes, supports their broad‐spectrum antibacterial activities.

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

Efasol dosage

Adult and Child over 8 years: 250-500 mg every 6 hours or 0.5-1 gm every 12 hours. This may be increased up to 4 gm daily according to severity of infections.

Child of 2-8 years: 250 mg every 6 hours, doses doubled for severe infections.

Child up to 2 years: 125 mg every 6 hours.

Neonates: 30 to 45 mg/kg daily in 3 divided doses.

Elderly: Same as for adults.If administration on a twice daily schedule is desirable, one half of the total daily dose may be given every 12 hours, one hour before meal.

Amoebic dysentery:

  • Adult: 250 - 500 mg four times daily for 10 - 14 days.
  • Children: 30 - 50 mg/kg/day in divided doses for 10 - 14 days.

Pertussis: 30 - 50 mg/kg/day in divided doses for 5-14 days depending upon eradication of a positive culture.Streptococcal infections: In the treatment of group A beta haemolytic streptococcal infections, therapeutic dosage of Erythromycin should be administered for at least 10 days.

Acne: The usual dosage regimen of erythromycin in the treatment of acne is 500 mg twice daily for 3 months. Then the dose is to be reduced to 250 mg twice daily for another 3 months.

Early Syphilis: 500 mg 4 times daily for 14 days.Uncomplicated genital Chlamydia nongonococcal Urethritis: 500 mg twice daily for 14 days.

Prophylaxis: In continuous prophylaxis of streptococcal infections in person with a rheumatic heart disease, the dosage is 250 mg twice daily.

When Erythromycin is used prior to surgery to prevent endocarditis caused by alpha haemolytic streptococci, a recommended schedule:

  • For children: 20 mg/Kg 1.5 - 2 hours pre-operatively and 10 mg/kg every 6 hours for 8 doses post-operatively.
  • For adults:The dose is 1 g, 1.5 - 2 hours pre-operatively and 500 mg every 6 hours for 8 doses post-operatively.

Topical: Apply to the affected areas in the morning and evening. Before applying thoroughly wash with warm water and soap, rinse and pat dry all areas to be treated. Apply with applicator. Wash hands after use.

Tretinoin cream: Tretinoin cream should be applied sparingly to the whole affected area once or twice daily. The skin should be thoroughly cleaned and dried before application. Patient should be advised that 6 to 8 weeks of treatment may be required before a therapeutic effect is observed. Moisturisers and cosmetics may be used during treatment with Cosmotrin cream but should not be applied to the skin at the same time. Astringent toiletries should be avoided.

Tretinoin gel: Tretinoin gel should be applied once or twice a day, before retiring, to the skin where lesions appear, using enough to cover the entire affected area lightly. The frequency of application can be adjusted to obtain maximum clinical efficacy with minimal erythema and scaling.

If Tretinoin gel is applied excessively, no more rapid or better results will be obtained and marked redness, peeling or discomfort may occur. Should this occur accidentally or through over-enthusiastic use, application should be discontinued for few days.

Patience is needed in this treatment, since the therapeutic effects will not usually be observed until after 6-8 weeks of treatment. During the early weeks of treatment, an apparent exacerbation of inflammatory lesions may occur. This is due to the action of the medication on deep, previously unseen comedones and papules. Once the acne lesions have responded satisfactorily, it should be possible to maintain the improvement with less frequent applications.

Moisturizers and cosmetics may be used during treatment with Tretinoin gel but should not be applied to the skin at the same time. The skin should be thoroughly washed before application of Tretinoin gel. Astringent toiletries should be avoided.

Capsule: The recommended dose is 45 mg/m2/day administered as two evenly divided doses until complete remission is documented. Therapy should be discontinued 30 days after achievement of complete remission or after 90 days of treatment, whichever occurs first.

If after initiation of treatment of Tretinoin the presence of the translocation is not confirmed by cytogenetics and/or by polymerase chain reaction studies and the patient has not responded to Tretinoin, alternative therapy appropriate for acute myelogenous leukemia should be considered.

Direction for reconstitution of suspension: Shake the bottle to loosen powder. Add 60 ml (12 measuring spoonful) of boiled and cooled water to the dry powder of the bottle. For ease of preparation, add water to the bottle in two proportions. Shake well after each addition until all the powder is in suspension.

Note: Shake the suspension well before each use. Keep the bottle tightly closed. The reconstituted suspension should be stored in a cool and dry place, preferably in refrigerator and unused portion should be discarded after 7 days.

Side Effects

Generally erythromycin is well tolerated and serious adverse effects are rare. Side-effects are gastrointestinal and are dose-related. They include nausea, vomiting, abdominal pain, diarrhea and anorexia. Mild allergic reactions, such as urticaria and skin rashes have occurred. Serious allergic reactions, including anaphylaxis may occur.

True allergic contact dermatitis is rare but a primary irritant dermatitis, manifesting itself as irritation, erythema, peeling and sensation of warmth, is common. Slight stinging is common as a mild reaction in many people but usually settles with continuous use and/or reduction in the frequency of application of the drug.

Toxicity

LD50

The oral LD50 of erythromycin in rats is 9272 mg/kg.

Overdose information

Symptoms of overdose may include diarrhea, nausea, stomach cramps, and vomiting. Erythromycin should immediately be discontinued in cases of overdose. Rapid elimination of unabsorbed drug should be attempted. Supportive measures should be initiated. Erythromycin is not adequately removed by peritoneal dialysis or hemodialysis.

Precaution

Lotion/Cream: For external use only. Keep away from eyes, nose, mouth and other mucous membrane.

Use of antibiotics (especially prolonged or repeated therapy) may result in bacterial or fungal overgrowth of non-susceptible organisms. Such overgrowth may lead to a secondary infection. Take appropriate measures if superinfections occur.

Tablet: Since Erythromycin is metabolized principally by the liver, caution should be exercised when erythromycin is administered to patients with impaired hepatic function. There have been reports of hepatic dysfunction with or without jaundice occurring in patients taking oral Erythromycin.

Interaction

Theophylline: The use of Erythromycin in patients who are receiving concomitant high doses of theophylline may be associated with an increase in serum theophylline and potential theophylline toxicity. If symptoms of toxicity develop, the dose of theophylline should be reduced.

Digoxin: Concomitant administration of Erythromycin and Digoxin has been reported to result in elevated digoxin serum levels.

Clindamycin interacts with Erythromycin

Particular caution should be exercised in using preparations containing peeling agents (i.e. sulfur, resorcinol, benzoyl peroxide or salicylic acid). Use of topical preparations with high concentrations of alcohol, menthol, spices or lime- such as shaving lotions, astringents and perfume- should be avoided, especially during initial therapy.

Volume of Distribution

Erythromycin is found in most body fluids and accumulates in leucocytes and inflammatory liquid. Spinal fluid concentrations of erythromycin are low, however, the diffusion of erythromycin through the blood-brain barrier increases in meningitis, likely due to the presence of inflamed tissues which are easily penetrated. Erythromycin crosses the placenta.

Elimination Route

Orally administered erythromycin is readily absorbed. Food intake does not appear to exert effects on serum concentrations of erythromycin. Some interindividual variation exists in terms of erythromycin absorption, which may impact absorption to varying degrees. The Cmax of erythromycin is 1.8 mcg/L and the Tmax is 1.2 hours. The serum AUC of erythromycin after the administration of a 500mg oral dose was 7.3±3.9 mg.h/l in one pharmacokinetic study. Erythromycin is well known for a bioavailability that is variable (18-45%) after oral administration and its susceptibility to broken down under acidic conditions.

1-31% (topical)

Half Life

The elimination half-life of oral erythromycin was 3.5 hours according to one study and ranged between 2.4-3.1 hours in another study. Repetitive dosing of erythromycin leads to increased elimination half-life.

0.5-2 hours

Clearance

The clearance of erythromycin in healthy subjects was 0.53 ± 0.13 l/h/kg after a 125mg intravenous dose. In a clinical study of healthy patients and patients with liver cirrhosis, clearance of erythromycin was significantly reduced in those with severe liver cirrhosis. The clearance in cirrhotic patients was 42.2 ± 10.1 l h–1 versus 113.2 ± 44.2 l h-1 in healthy patients.

Elimination Route

In patients with normal liver function, erythromycin concentrates in the liver and is then excreted in the bile.Under 5% of the orally administered dose of erythromycin is found excreted in the urine. A high percentage of absorbed erythromycin is not accounted for, but is likely metabolized.

Pregnancy & Breastfeeding use

Safety for use during pregnancy has not been established. Use only when the potential benefits outweigh potential hazards to the fetus.

Erythromycin is excreted in breast milk. Exercise caution when administering to a nursing mother.

Tretinoin is contraindicated in pregnancy or suspected pregnancy. The drug should be avoided by breast feeding mothers.

Contraindication

Erythomycin is contraindicated in patients with a known hypersensitivity to this drug.

Tretinoin is contraindicated in patients who are allergic to this drug. It is contraindicated in pregnancy or suspected pregnancy. It is also contraindicated in personal or familial history of cutaneous epithelioma.

Local irritation: The presence of cutaneous irritative signs (e.g. erythema, peeling, pruritus, sunburn, etc.) should prohibit initiation or recommencement of treatment with Tretinoin until the symptoms resolve. Tretinoin has been reported to cause severe irritation on eczematous skin and should be used with caution in patients with this condition.

Exposure to sunlight: Exposure to sunlight, including ultraviolet sun-lamps, should be avoided or minimised during the use of Tretinoin.

General precaution: Before application of Tretinoin, areas to be treated should be cleansed thoroughly. Abstain from washing the treated area frequently; twice daily is sufficient. Use of mild soap is recommended. Dry the skin without rubbing.

Avoid contact with eyes, eyelids, nostrils, mouth and mucous membranes. If contact in these areas occurs, careful washing with water is recommended.

Special Warning

Safety and effectiveness in children less than 12 years have not been established.

Acute Overdose

In case of overdosage, Erythromycin should be discontinued. Overdosage should be handled with the prompt elimination of unabsorbed drug and all other appropriate measures should be instituted. Erythromycin is not removed by peritoneal dialysis or haemodialysis.

Storage Condition

Keep at room temperature and away from light.

Store in a cool and dry place, away from light. Keep out of reach of children.

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