Isotrexin

Erythromycin:

• Pharmacological action
• Pharmacokinetics
• Why is Isotrexin prescribed?
• Dosage and administration
• Isotrexin (Erythromycin) side effects, adverse reactions
• Isotrexin contraindications
• Using during pregnancy and breastfeeding
• Special instructions
• Precautionary measures
• Isotrexin (Erythromycin) drug interactions
• Isotrexin in case of emergency / overdose
• Isotrexin (Erythromycin) reviews

Pharmacological action

Isotrexin is a macrolide antibiotic. Has bacteriostatic action. However at higher doses against susceptible organisms has a bactericidal effect. Isotrexin (Erythromycin) is reversibly bound to the ribosome of bacteria, thereby inhibiting protein synthesis. Isotrexin (Erythromycin) is active against gram-positive bacteria: Staphylococcus spp. (strains producing and not producing penicillinase), Streptococcus spp. (including Streptococcus pneumoniae); gram-negative bacteria: Neisseria gonorrhoeae, Haemophilus influenzae, Bordetella pertussis, Brucella spp., Legionella spp., Bacillus anthracis, Corynebacterium diphtheriae; anaerobic bacteria: Clostridium spp. Isotrexin (Erythromycin) is also active against Mycoplasma spp., Chlamydia spp., Spirochaetaceae, Rickettsia spp. To Isotrexin (Erythromycin) resistant gram-negative bacilli, including Escherichia coli, Pseudomonas aeruginosa, Shigella spp., Salmonella spp.

Pharmacokinetics

Isotrexin (Erythromycin) bioavailability is 30-65%. Distributed in most tissues and body fluids. Plasma protein binding is 70-90%. Metabolised in the liver, partly with the formation of inactive metabolites. T1/2 is 1.4-2 hours. It is derived from bile and urine.

Why is Isotrexin prescribed?

Infectious-inflammatory diseases caused by microorganisms sensitive to Isotrexin (Erythromycin), including diphtheria, pertussis, trachoma, brucellosis, a disease Legionnaires, sore throat, scarlet fever, otitis media, sinusitis, cholecystitis, pneumonia, gonorrhea, syphilis. Also Isotrexin (Erythromycin) used for the treatment of infectious-inflammatory diseases caused by pathogens (eg staphylococci) are resistant to penicillin, tetracycline, chloramphenicol, streptomycin.

For external use: acne vulgaris.

For local use: the infectious-inflammatory diseases of eyes.

Dosage and administration

Isotrexin prescribed individually depending on the location and severity of infection, the sensitivity of the parasite. In adults use a daily dose of 1-4 g. Children under the age of 3 months - 20-40 mg / kg / day, aged from 4 months to 18 years - 30-50 mg / kg / day. Multiplicity is 4 times / day. The treatment course - 5-14 days after the disappearance of symptoms treatment should be continued for a further 2 days. Accepts up to 1 hour before eating or 2-3 hours after eating.

Solution for external applications lubricate the affected skin.

The ointment is applied to the affected area and in diseases of the eye lay behind the lower eyelid. The dose, frequency and duration of application is determined individually.

Isotrexin (Erythromycin) side effects, adverse reactions

Digestive system: nausea, vomiting, epigastric pain, cholestatic jaundice, tenesmus, diarrhea, dysbacteriosis; rarely - pseudomembranous enterocolitis, abnormal liver function, increase in liver transaminases, pancreatitis.

Allergic reactions: skin rash, urticaria, eosinophilia, rarely - anaphylactic shock.

Effects due to the influence of chemotherapy: oral candidiasis, vaginal candidiasis.

From the senses: the reversible ototoxicity - hearing loss and / or tinnitus (in the application of high doses - more than 4 g / day).

Since the cardiovascular system: rarely - tachycardia, prolongation of the QT interval on ECG, flickering and / or atrial flutter (patients with long QT interval on the ECG).

Local reactions: phlebitis at the site of / in the introduction.

Isotrexin contraindications

Jaundice in history, marked disturbances of liver function, hypersensitivity to macrolides.

Using during pregnancy and breastfeeding

Isotrexin crosses the placental barrier, excreted in breast milk.

In the application of Isotrexin (Erythromycin) in pregnancy should assess the intended benefits to the mother and the potential risk to the fetus. If necessary, use during lactation should decide on the termination of breastfeeding.

Special instructions

With careful use Isotrexin (Erythromycin) when disorders of liver function and / or kidneys. Medications that increase the acidity of gastric juice and acidic drinks inactivate Isotrexin (Erythromycin). Isotrexin (Erythromycin) can not drink milk and dairy products.

Precautionary measures

The use of Isotrexin containing benzene for IV injection sometimes accompanied by the development of a fatal syndrome Gaspinga in children, as well as acute hepatitis drug in adults and children.

Isotrexin (Erythromycin) drug interactions

With simultaneous use of Isotrexin (Erythromycin) with theophylline, aminophylline, caffeine, there is an increase in their concentration in blood plasma and thus increases the risk of toxic effects.

Isotrexin (Erythromycin) increases the concentrations of cyclosporine in the blood plasma and may increase the risk of nephrotoxicity.

Drugs that block tubular secretion prolongs T1/2 of Isotrexin (Erythromycin).

Incompatible with lincomycin, clindamycin and chloramphenicol (antagonism).

Isotrexin (Erythromycin) reduces the bactericidal action of beta-lactam antibiotics (penicillins, cephalosporins, carbapenems).

With simultaneous use of Isotrexin (Erythromycin) increases the concentration of theophylline.

At the same time receiving chemotherapy, which is carried metabolism in the liver (carbamazepine, valproic acid, hexobarbital, phenytoin, alfentanil, dizopiramid, lovastatin, bromocriptine), may increase the concentration of these drugs in plasma (an inhibitor of microsomal liver enzymes).

IV injection of Isotrexin (Erythromycin) increases the effects of ethanol (accelerating gastric emptying and decrease the duration of alcohol dehydrogenase in the gastric mucosa).

Isotrexin (Erythromycin) reduces the clearance of triazolam and midazolam and therefore may increase the pharmacological effects of benzodiazepines.

At the same time taking with terfenadine or astemizole may develop arrhythmias (fibrillation and ventricular flutter, ventricular tachycardia, until death); with dihydroergotamine or non hydrated ergot alkaloids may vasoconstriction to spasm, dysesthesia.

With simultaneous application Isotrexin (Erythromycin) slows elimination (increases the effect) of methylprednisolone, felodipine and anticoagulants of cumarine series.

In a joint appointment with lovastatin increased rhabdomyolysis.

Isotrexin (Erythromycin) increases the bioavailability of digoxin.

Isotrexin (Erythromycin) reduces the effectiveness of hormonal contraceptives.

Isotrexin in case of emergency / overdose

Symptoms: disruption of the liver until the acute liver failure, and hearing loss.

Treatment: gastric lavage, forced diuresis, hemo-and peritoneal dialysis. Produced a constant monitoring of vital functions (ECG, electrolyte composition of blood).

Isotretinoin:

• Pharmacological action
• Pharmacokinetics
• Why is Isotrexin prescribed?
• Dosage and administration
• Isotrexin (Isotretinoin) side effects, adverse reactions
• Isotrexin contraindications
• Using Isotrexin during pregnancy and lactation
• Special instructions
• Isotrexin (Isotretinoin) drug interactions
• Isotrexin (Isotretinoin) reviews

Pharmacological action

Isotrexin is a pharmaceutical agent for the treatment of acne. Contributes to the normalization of terminal cell differentiation, inhibits the hyperproliferation of the epithelium of excretory ducts of the sebaceous glands, the formation of detritus and makes it easier to evacuate. Due to this reduced production of sebum and facilitates its isolation, normal structure, decreasing the inflammatory reaction around the glands. For external and systemic application Isotrexin (Isotretinoin) has antiseborrhea, sebostatic, anti-inflammatory, keratitis and immunomodulatory actions, strengthens the processes of regeneration in the skin.

Pharmacokinetics

When Isotrexin (Isotretinoin) administered orally Isotrexin (Isotretinoin) is absorbed from the gastrointestinal tract, absorption may increase when taken with food. C_max plasma levels reached after 1-4 hours after ingestion.

Oral bioavailability of Isotrexin (Isotretinoin) is low which may be caused by parietal metabolism in the intestinal wall and the effect of "first passage" through the liver.

Isotrexin (Isotretinoin) is highly bound to plasma proteins. Metabolized in the liver with the formation of the main metabolite 4-oxo-isotretinoin, also there is some isomerization of Isotrexin (Isotretinoin) in tretinoin.

Isotrexin (Isotretinoin), tretinoin and its metabolites are enterohepatic recycling.

The end of T1/2 of tretinoin is 10-20 hours. An equivalent amount is determined in the feces, mostly unchanged, and urine in the form of metabolites.

Why is Isotrexin prescribed?

For Isotrexin (Isotretinoin) oral administration: severe nodular-cystic acne especially with the localization on the body.

For rectal administration: severe relapsing forms of acne, rashes associated with seborrheic process.

For external use: papule-pustular acne, seborrhea, rosacea, perioral dermatitis.

Dosage and administration

For oral administration initial dose of Isotrexin is 500 mcg / kg / day; the maximum daily dose used for a limited time and is 1 mg / kg; the maintenance dose is 0.1-1 mg / kg / day; duration of treatment is 16 weeks, a second course conducted at intervals of 8 days. Isotrexin (Isotretinoin) is taken with meals in one or more receptions.

Rectal - 0.5-1 mg / kg / day, one time at night (in the supine position); course of treatment - 8-12 weeks, the intervals between courses - 1-2 months.

Ointment applied thinly to the affected areas of skin 2 times / day. Duration of treatment - 4-6 weeks.

Isotrexin (Isotretinoin) side effects, adverse reactions

Dermatological reactions: dry mucous membranes, skin rashes, dermatitis, pruritus, cheilitis, erythema (especially on the face), sweating, palmar-plantar desquamation and paronychia, nail dystrophy, increased proliferation of granulation tissue in the affected area, rarely - thinning hair, vasculitis, photosensitivity.

Senses: conjunctivitis, photophobia, decreased night vision, corneal opacity, weakening of the hearing.

CNS and peripheral nervous system: headache, rarely - depression, seizures, suicide, and in rare cases - intracranial hypertension.

Digestive system: nausea, rarely - colitis, bleeding from the gastrointestinal tract, transient elevation of liver transaminases and in rare cases - hepatitis.

Hematopoietic system: anemia, neutropenia, changes in platelet count, increased erythrocyte sedimentation rate.

Metabolism: increased concentrations of TG and glucose.

Musculoskeletal system: pain in muscles and joints, rarely - hyperostosis.

Other: nasal bleeding.

Rectal and topical using: 1-2 weeks of treatment may cause new eruptions, itching, swelling and redness.

Isotrexin contraindications

Pregnancy, established and planned lactation, hypersensitivity to Isotrexin (Isotretinoin), the simultaneous use of tetracycline antibiotics.

For oral administration: severe liver and / or kidney damage, hypervitaminosis A, significantly elevated levels of lipids in blood plasma, neoplasms.

For rectal use - diseases of the rectum.

Using Isotrexin during pregnancy and lactation

Isotrexin (Isotretinoin) has a pronounced teratogenic and embryotoxic action.

Isotrexin (Isotretinoin) is contraindicated in established and planned pregnancy.

Also Isotrexin (Isotretinoin) is contraindicated during lactation.

Special instructions

Rectally and topically applied with caution in liver disease, kidney disease, chronic pancreatitis, decompensation of heart function, chronic intoxication.

Rectal and external use in a pronounced exacerbation of the reaction (on 1-2-week treatment) is recommended to cancel the medication for a few days before its decline, then therapy can be resumed.

For oral administration requires regular monitoring of liver function and lipid levels in blood plasma before treatment, 1 month after initiation of therapy and then every 3 months.

In diabetes, obesity, alcoholism or lipid metabolism violations recommended more frequent monitoring of laboratory parameters. In diabetes mellitus or suspected it is necessary to strictly control glucose levels in plasma.

With prolonged use may develop symptoms of chronic hypervitaminosis A.

During treatment or within a certain time after its completion can not be donors for women of childbearing age.

During the treatment, patients should not be given UV treatment, patients should avoid direct exposure to sunlight.

In the course of treatment with Isotrexin (Isotretinoin) may occur intolerance of contact lenses.

Safety of children and prepubertal patients has not been established.

Should avoid the simultaneous use of Isotrexin (Isotretinoin) and 19-nortestosterone derivatives, particularly in patients with gynecological / endocrine diseases.

Not recommended for concurrent use of other drugs with keratolytic or exfoliative properties (including other retinoids), and progesterone in the microdose (including drugs "mini-pilly").

Isotrexin (Isotretinoin) drug interactions

The action of Isotrexin (Isotretinoin) is weakened by the simultaneous application of progesterone in the microdose.

With the simultaneous application of Isotrexin (Isotretinoin) and vitamin A may increase toxic effects.

With the simultaneous application of Isotrexin (Isotretinoin) and aminoglycoside antibiotics is at risk of developing intracranial hypertension.