Pharmacological properties Altabax Ointment.
Pharmacodynamics.
Retapamulin is a synthetic derivative of substance plevromutilinu, which was isolated by fermentation of Clitopilus passeckerianus.
Altabax Ointment Retapamulin selectively inhibits bacterial protein synthesis by interfering with bacterial 50S ribosomal subodineyu, which is, in some respects different from that of other antibiotics that interact with the ribosome. These data suggest that the site of ribosomal protein compounds include L3, ribosomal P-site and peptidyl center. By binding to this site inhibits plevromutilin peptidiltransferazu, partially blocks the interaction with P-site and interferes with the normal formation of active 50S ribosomal subunits of bacteria, ie, inhibits bacterial protein variety of mechanisms. Because of this specific method of in vitro cross-sensitivity with other antibiotics and retapamulinom is rare.
Retapamulin active against most strains of common pathogens of skin and subcutaneous tissue, as Staphylococcus aureus and Staphylococcus pyogenes as in vitro, and clinical studies. However, clinical studies retapamulin was less effective against some strains metitsillinrezistentnye Staphylococcus aureus.
The drug is also active in vitro against certain Gram positive, Gram-negative and anaerobic microorganisms.
Retapamulin mainly bacteriostatic effect against Staphylococcus aureus and Staphylococcus pyogenes. The minimum bactericidal concentration (MBC) against S. aureus and S. pyogenes in the 512 and 1024 times the minimum inhibitory concentration (MIC).
According to in vitro retapamulin active against strains of Staphylococcus epidermidis, Streptococcus agalactiae, Streptococci viridans, Propionibacterium acnes, Peptostreptococcus, Prevotella, Fusobacterium, Porphyromonas, but the clinical significance of this is unknown.
Resistance decrease in vitro activity retapamulinu mediated through a mutation in ribosomal protein L3. The presence of ABC transporter vgaAv reduces in vitro activity retapamulinu. The sensitivity to plevromutilinu may affect CfrrRNA methyltransferase, which provides cross-resistance to fenikoliv, linkosamindiv and streptogramins A in staphylococci.
Retapamulin prodemonstriroval low potential for resistance development in vitro.
The highest level of the IPC in a series of retapamulinu passages S. aureus and S. pyogenes in the presence of inhibitory activity subminimalnoi retapamulinu was 2 mg / ml. Pharmacokinetics.
Absorption. Systemic effects of 1% retapamulinu studied when applied to intact skin and wounds abrasive for 7 days. Systemic effects when applied to intact skin was very low. Geometric mean maximum concentration of drug in plasma after application to 200 cm2 of damaged skin was 9.75 ng / ml at day 1 and 8.79 ng / ml – on day 7 with a maximum individual value of 22.1 ng / ml .
Were carried out one-time determination of the concentration of the drug in the blood plasma of 516 adults and children with secondarily infected wounds that were treated with 1% retapamulinom 2 times a day for 5 days. Determination was carried out before applying ointment to the 3rd or 4th day in adults and between 0 and 12 hours after the last application of ointment on the 3rd or 4th day in children. In most samples (89%) concentration was below the level of measurability (0.5 ng / ml). Among the samples, which were measured in 90% of cases, the concentration was less than retapamulinu 2.5 ng / ml. The maximum measured concentration retapamulinu 10.7 ng / ml in adults and 18.5 ng / ml – for children (ages 2 to 17 years).
Children under 2 years of the study of the pharmacokinetics of topical retapamulinu in children, plasma samples were obtained from patients aged 2 months to 2 years. In 46% of the samples was measured by the concentration of retapamulinu (0.52 to 177.3 ng / ml), where most of the samples (75%) had a concentration
Children from 2 to 9 months
Retapamulinu concentration in plasma was measured at 69% of patients (n = 20). In this age group recorded four cases in which the concentration in plasma repatamulinu (26 .. 9, 80.3, 174.3 and 177.3 ng / ml) was higher than the highest concentration in plasma retapamulinu, recorded in patients older than 2 to 17 (18.5 ng / ml). Application retapamulinu is not recommended for children under 9 months (see “Application”).
Children from 9 months to 2 years retapamulinu concentration in plasma was measured at 32% of patients (n = 16). In this age group recorded one case in which the concentration of repatamulinu in plasma (95.1 ng / ml) was higher than the highest concentration in plasma retapamulinu, recorded in patients aged 2 to 17 years (18.5 ng / ml). (See “Interaction with other medicinal products and other forms of interaction”).
Distribution. Due to the very low systemic action of the drug, the drug distribution in human tissues has not been studied. In in vitro studies retapamulin is a substrate and inhibitor of P-glycoprotein. However, systemic effects after topical application retapamulinu to 660 times lower concentration retapamulinu (IS50) which is required for inhibition of P-glycoprotein. Retapamulin approximately 94% bound to plasma proteins.
Metabolism. In vitro metabolism retapamulinu in human liver microsomes mainly mediyuetsya by CYP3A4, a much lesser extent – CYP2C8 and CYP2D6.
Output. Withdrawal from the human body has not been studied.
How to use Altabax Ointment:
The use of this drug on the skin only. Clean and dry the affected area first. Then apply a small amount of ointment to the affected area, usually 2 times a day for 5 days or as directed by your doctor. Wash hands after use, if you do not treat the area on his hands. Do not use this medication around the eyes, nose, mouth or vaginal area, or on large areas of skin unless otherwise directed by your doctor. You can cover the treated area with a bandage / gauze. This can help prevent your child from accidentally getting medication in their eyes, nose or mouth. Use this medication regularly in order to get the most benefit from it. Continue to use it on all the time prescribed. Stopping the medication too early may allow bacteria to continue to grow, which may lead to the return of the infection. You should see some improvement (cured / dry ulcers, decreased redness) in 3 to 4 days. Tell your doctor if your condition does not improve in 3 to 4 days.
Application Altabax Ointment:
Retapamulin is used to treat certain skin infections (impetigo) caused by bacteria. It is an antibiotic that works by stopping the growth of some bacteria (staphylococci and streptococci) in the skin.
Side effects Altabax Ointment:
Mild burning, tingling, itching, or can occur. If any of these effects persist or worsen, tell your doctor or pharmacist promptly. Remember that your doctor has prescribed this medication because he determines that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects. Tell your doctor immediately if any of these unlikely but serious side effects, blistering / swelling / oozing skin. Use of this medication for prolonged or repeated periods may lead to new infections (eg fungal infection). Consult your doctor if you notice signs of new infection (eg, new / worsening ulcers, fever). A very serious allergic reaction to this drug is rare. However, seek immediate medical attention if you notice any symptoms of a serious allergic reaction, including: rash, itching / swelling (especially the face / tongue / throat), severe dizziness, trouble breathing. This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist. In the United States – See your doctor for medical advice about side effects. You may report side effects FDA at 1-800-FDA-1088. In Canada – Call your doctor for medical advice about side effects. You may report side effects to the health of Canada 1-866-234-2345.
Precautions Altabax Ointment:
Before using retapamulin, tell your doctor if you are allergic to it, or if you have any other allergies. This product may contain inactive ingredients that may cause allergic reactions or other problems. Talk to your pharmacist for more information. Before using this medication, tell your doctor or pharmacist your medical history. During pregnancy, this medication should be used only when really necessary. Discuss the risks and benefits with your doctor. It is unknown whether this drug passes into breast milk. Consult your doctor before breast-feeding.
Drug Interactions Altabax Ointment:
Your doctor or pharmacist may already be aware of any possible drug interactions and may be monitoring them. Do not start, stop or change the dosage of any medicine before checking with them first. Before using this medication, tell your doctor or pharmacist of all prescription and nonprescription / herbal products you may use. Keep a list of all your medications with you, and share the list with your doctor and pharmacist.
Overdosage Altabax Ointment
This medication may be harmful if swallowed. If swallowing or overdose is suspected, contact your local poison control center or emergency room immediately. U.S. residents can call the U.S. National Poison Hotline at 1-800-222-1222. Canada residents can call the provincial poison control center.
Notes:
Do not share this medication with others. This medication was prescribed for your current condition only. Do not use it later for another infection unless told to do so by your doctor. Various medications may be necessary in those cases.
Missed dose:
If you miss a dose, use it as soon as you remember. If it is near the time of the next dose, skip the missed dose and resume your usual dosing. Do not double the dose to catch up.
Storage:
Store at room temperature to 77 degrees Fahrenheit (25 degrees C) away from light and moisture. Brief storage between 59-86 degrees F (15-30 degrees C) is not allowed. Do not store in the bathroom. Keep medicines away from children and pets. Do not flush medications down the toilet or pour them into the drainage, if instructed to do so. Properly discard this product when it is expired or no longer needed. Consult your pharmacist or local waste disposal company for more information about how to safely abandon your product.
