Sumamed, 1000 mg, dispersible tablets, 1 pc.
Antacid drugs.
They do not affect the bioavailability of azithromycin, but reduce Cmax in the blood by 30%, so the drug should be taken at least 1 hour before or 2 hours after taking these drugs and food.
Cetirizine.
Concomitant use of azithromycin with cetirizine (20 mg) for 5 days in healthy volunteers did not lead to pharmacokinetic interaction or a significant change in the QT interval.
Didanosine (dideoxyinosine).
The simultaneous use of azithromycin (1200 mg/day) and didanosine (400 mg/day) in 6 HIV-infected patients did not reveal changes in the pharmacokinetic indications of didanosine compared to the placebo group.
Digoxin (P-glycoprotein substrates).
Simultaneous use of macrolide antibiotics, incl. azithromycin, with P-glycoprotein substrates such as digoxin, leads to increased concentrations of P-glycoprotein substrate in the blood serum. Thus, with the simultaneous use of azithromycin and digoxin, it is necessary to take into account the possibility of increasing the concentration of digoxin in the blood serum.
Zidovudine.
The simultaneous use of azithromycin (single dose of 1000 mg and multiple doses of 1200 or 600 mg) has a minor effect on pharmacokinetics, incl. renal excretion of zidovudine or its glucuronide metabolite. However, the use of azithromycin caused an increase in the concentration of phosphorylated zidovudine, a clinically active metabolite in peripheral blood mononuclear cells. The clinical significance of this fact is unclear. Azithromycin interacts weakly with isoenzymes of the cytochrome P450 system. Azithromycin has not been shown to participate in pharmacokinetic interactions similar to erythromycin and other macrolides. Azithromycin is not an inhibitor or inducer of cytochrome P450 isoenzymes.
Ergot alkaloids.
Given the theoretical possibility of ergotism, the simultaneous use of azithromycin with ergot alkaloid derivatives is not recommended. Pharmacokinetic studies were conducted on the simultaneous use of azithromycin and drugs whose metabolism occurs with the participation of isoenzymes of the cytochrome P450 system.
Atorvastatin.
Concomitant use of atorvastatin (10 mg daily) and azithromycin (500 mg daily) did not cause changes in atorvastatin plasma concentrations (based on an HMC-CoA reductase inhibition assay). However, in the post-marketing period, isolated case reports of rhabdomyolysis have been received in patients receiving concomitant azithromycin and statins.
Carbamazepine.
Pharmacokinetic studies involving healthy volunteers did not reveal a significant effect on the plasma concentrations of carbamazepine and its active metabolite in patients receiving concomitant azithromycin.
Cimetidine.
In pharmacokinetic studies of the effect of a single dose of cimetidine on the pharmacokinetics of azithromycin, no changes in the pharmacokinetics of azithromycin were detected when cimetidine was administered 2 hours before azithromycin.
Indirect anticoagulants (coumarin derivatives).
In pharmacokinetic studies, azithromycin did not affect the anticoagulant effect of a single 15 mg dose of warfarin administered to healthy volunteers. Potentiation of the anticoagulant effect has been reported after simultaneous use of azithromycin and indirect anticoagulants (coumarin derivatives). Although a causal relationship has not been established, the need for frequent monitoring of PT should be considered when using azithromycin in patients receiving indirect oral anticoagulants (coumarin derivatives).
Cyclosporine.
In a pharmacokinetic study involving healthy volunteers who took azithromycin (500 mg/day once) orally for 3 days, followed by cyclosporine (10 mg/kg/day once), a significant increase in plasma Cmax and AUC0–5 h was detected. cyclosporine. Caution is advised when using these drugs together. If simultaneous use of these drugs is necessary, it is necessary to monitor the concentration of cyclosporine in the blood plasma and adjust the dose accordingly.
Efavirenz.
Concomitant use of azithromycin (600 mg/day once) and efavirenz (400 mg/day) daily for 7 days did not cause any clinically significant pharmacokinetic interaction.
Fluconazole.
Concomitant use of azithromycin (1200 mg once) did not change the pharmacokinetics of fluconazole (800 mg once). The total exposure and T1/2 of azithromycin did not change with simultaneous use of fluconazole, however, a decrease in Cmax of azithromycin was observed (by 18%), which had no clinical significance.
Indinavir.
The simultaneous use of azithromycin (1200 mg once) did not cause a statistically significant effect on the pharmacokinetics of indinavir (800 mg 3 times a day for 5 days).
Methylprednisolone.
Azithromycin does not have a significant effect on the pharmacokinetics of methylprednisolone.
Nelfinavir.
The simultaneous use of azithromycin (1200 mg) and nelfinavir (750 mg 3 times a day) causes an increase in the Css of azithromycin in the blood serum. No clinically significant side effects were observed and no dose adjustment of azithromycin was required when used concomitantly with nelfinavir.
Rifabutin.
The simultaneous use of azithromycin and rifabutin does not affect the concentration of each drug in the blood serum. Neutropenia has sometimes been observed with simultaneous use of azithromycin and rifabutin. Although neutropenia has been associated with the use of rifabutin, a causal relationship between the use of the combination of azithromycin and rifabutin and neutropenia has not been established.
Sildenafil.
When used in healthy volunteers, there was no evidence of the effect of azithromycin (500 mg/day daily for 3 days) on the AUC and Cmax of sildenafil or its main circulating metabolite.
Terfenadine.
In pharmacokinetic studies, there was no evidence of interaction between azithromycin and terfenadine. There have been isolated cases reported where the possibility of such an interaction could not be completely excluded, but there was no concrete evidence that such an interaction occurred. It has been found that the simultaneous use of terfenadine and macrolides can cause arrhythmia and prolongation of the QT interval.
Theophylline.
No interaction has been detected between azithromycin and theophylline.
Triazolam/midazolam.
No significant changes in pharmacokinetic parameters were detected with simultaneous use of azithromycin with triazolam or midazolam in therapeutic doses.
Trimethoprim/sulfamethoxazole.
Concomitant use of trimethoprim/sulfamethoxazole with azithromycin did not show a significant effect on Cmax, total exposure or renal excretion of trimethoprim or sulfamethoxazole. Azithromycin serum concentrations were consistent with those found in other studies.
Sumamed Forte powder d/susp d/internal 200mg/5ml 16.74g 15ml banana
Compound
Active substance: azithromycin - 47.79 mg. Excipients: sucrose - 898.206 mg, sodium phosphate - 20 mg, hyprolose - 1.6 mg, xanthan gum - 1.6 mg, banana flavor - 12 mg, vanilla flavor - 4.5 mg, titanium dioxide - 5 mg, colloidal silicon dioxide - 7 mg.
Pharmacokinetics
Suction
Cmax in blood plasma is achieved after 2-3 hours. Bioavailability is 37%.
Distribution
Plasma protein binding is inversely proportional to blood concentration and ranges from 12 to 52%. Vd is 31.1 l/kg. Penetrates through cell membranes (effective against infections caused by intracellular pathogens). Transported by phagocytes, polymorphonuclear leukocytes and macrophages to the site of infection, where it is released in the presence of bacteria. Easily penetrates histohematic barriers and enters tissues. The concentration in tissues and cells is 50 times higher than in plasma, and at the site of infection it is 24-34% higher than in healthy tissues.
Metabolism
In the liver it is demethylated, losing activity.
Removal
It is slowly eliminated from tissues and has a long T1/2 - 2-4 days. The therapeutic concentration of azithromycin lasts up to 5-7 days after taking the last dose. Azithromycin is excreted mainly unchanged - 50% by the intestines, 12% by the kidneys.
Pharmacokinetics in special clinical situations
In patients with severe renal failure (creatinine clearance less than 10 ml/min), T1/2 increases by 33%.
Indications for use
Infectious and inflammatory diseases caused by microorganisms sensitive to the drug, including:
- upper respiratory tract infections, including pharyngitis/tonsillitis, sinusitis, otitis media;
- lower respiratory tract infections, including acute bronchitis, exacerbation of chronic bronchitis, community-acquired pneumonia;
- infections of the skin and soft tissues, including erysipelas, impetigo, secondary infected dermatoses;
- Lyme disease (initial stage of borreliosis) - erythema migrans.
Contraindications
- severe liver dysfunction;
- simultaneous use of ergotamine and dihydroergotamine;
- children up to 6 months;
- sucrase/isomaltase deficiency, fructose intolerance, glucose-galactose malabsorption;
- hypersensitivity to azithromycin, erythromycin, other macrolides or ketolides, or other components of the drug.
Carefully
the drug should be prescribed for myasthenia gravis, mild to moderate liver dysfunction, end-stage renal failure with GFR less than 10 ml/min, patients with the presence of proarrhythmogenic factors (especially elderly patients): with congenital or acquired prolongation of the QT interval, patients receiving antiarrhythmic therapy drugs of classes IA (quinidine, procainamide), III (dofetilide, amiodarone and sotalol), cisapride, terfenadine, antipsychotic drugs (pimozide), antidepressants (citalopram), fluoroquinolones (moxifloxacin and levofloxacin), with disturbances of water-electrolyte balance, especially in the case of hypokalemia or hypomagnesemia, clinically significant bradycardia, cardiac arrhythmia, or severe heart failure; with simultaneous use of digoxin, warfarin, cyclosporine; with diabetes mellitus.
Directions for use and doses
The drug is prescribed orally 1 time/day, 1 hour before or 2 hours after meals. After taking Sumamed® forte, the child must be offered to drink a few sips of water so that he can swallow the remainder of the suspension.
Before each use of the drug, the contents of the bottle are thoroughly shaken until a homogeneous suspension is obtained; if the required volume of the suspension is not taken from the bottle within 20 minutes after shaking, the suspension should be shaken again, the required volume is taken and given to the child.
The required dose is measured using a dosing syringe with a division value of 1 ml and a nominal suspension capacity of 5 ml (200 mg azithromycin) or a measuring spoon with a nominal suspension capacity of 2.5 ml (100 mg azithromycin) or 5 ml (200 mg azithromycin), placed in a cardboard packaging along with the bottle.
After use, the syringe (after disassembling it) and measuring spoon are washed with running water, dried and stored in a dry place until the next dose of Sumamed® forte.
For infectious and inflammatory diseases of the upper and lower respiratory tract, skin and soft tissues, the drug is prescribed at the rate of 10 mg/kg body weight 1 time/day for 3 days, the course dose is 30 mg/kg.
To accurately dose Sumamed® forte according to the child’s body weight, use the table below.
For pharyngitis/tonsillitis caused by Streptococcus pyogenes, Sumamed® forte is used at a dose of 20 mg/kg/day for 3 days (course dose 60 mg/kg). The maximum daily dose is 500 mg.
Children weighing up to 10 kg should be prescribed Sumamed® in powder form to prepare an oral suspension with a concentration of 100 mg/5 ml.
For Lyme disease (the initial stage of borreliosis) - erythema migrans - the drug is prescribed on the 1st day at a dose of 20 mg/kg/day, then from days 2 to 5 - at a dose of 10 mg/kg/day (course dose - 60 mg/kg).
When used in patients with impaired renal function with a GFR of 10-80 ml/min, no dose adjustment is required.
When used in patients with mild to moderate liver dysfunction, no dose adjustment is required.
Elderly patients do not require dose adjustment. In elderly patients, when using the drug Sumamed® forte, it is recommended to exercise special caution due to the possible presence of proarrhythmogenic factors that may increase the risk of developing cardiac arrhythmia and arrhythmias.
Rules for the preparation and storage of the suspension
To the contents of the bottle intended for the preparation of 15 ml of suspension (nominal volume), add 9.5 ml of water using a dosing syringe. Shake until a homogeneous suspension is obtained. The volume of the resulting suspension will be about 20 ml, which exceeds the nominal volume by approximately 5 ml. This is provided to compensate for the inevitable losses of suspension when dosing the drug. The prepared suspension can be stored at a temperature not exceeding 25°C for no more than 5 days.
To the contents of the bottle intended for the preparation of 30 ml of suspension (nominal volume), 16.5 ml of water is added using a dosing syringe. Shake until a homogeneous suspension is obtained. The volume of the resulting suspension will be about 35 ml, which exceeds the nominal volume by approximately 5 ml. This is provided to compensate for the inevitable losses of suspension when dosing the drug. The prepared suspension can be stored at a temperature not exceeding 25°C for no more than 10 days.
To the contents of the bottle intended for the preparation of 37.5 ml of suspension (nominal volume), add 20 ml of water using a dosing syringe. Shake until a homogeneous suspension is obtained. The volume of the resulting suspension will be approximately 42.5 ml, which exceeds the nominal volume by approximately 5 ml. This is provided to compensate for the inevitable losses of suspension when dosing the drug. The prepared suspension can be stored at a temperature not exceeding 25°C for no more than 10 days.
Storage conditions
The drug should be stored out of the reach of children at a temperature not exceeding 25°C.
Best before date
2 years. Do not use after the expiration date.
special instructions
When using the drug Sumamed® forte in patients with diabetes mellitus, as well as on a low-calorie diet, it is necessary to take into account that the suspension contains sucrose (0.32 XE/5 ml). If you miss taking one drug, Sumamed® forte, the missed dose should be taken as soon as possible, and subsequent doses should be taken at intervals of 24 hours.
Sumamed® forte should be taken at least 1 hour before or 2 hours after taking antacids.
The drug Sumamed® forte should be taken with caution in patients with mild to moderate liver dysfunction due to the possibility of developing fulminant hepatitis and severe liver failure.
If there are symptoms of liver dysfunction, such as rapidly increasing asthenia, jaundice, darkening of urine, tendency to bleeding, hepatic encephalopathy, therapy with Sumamed® forte should be stopped and a study of the functional state of the liver should be carried out.
If renal function is impaired in patients with GFR 10-80 ml/min, no dose adjustment is required; therapy with Sumamed® should be carried out with caution under monitoring the state of renal function.
As with the use of other antibacterial drugs, during therapy with Sumamed® forte, patients should be regularly examined for the presence of resistant microorganisms and signs of the development of superinfections, incl. fungal.
The drug Sumamed® forte should not be used for longer courses than indicated in the instructions, because The pharmacokinetic properties of azithromycin allow us to recommend a short and simple dosage regimen.
There is no data on a possible interaction between azithromycin and ergotamine and dihydroergotamine derivatives, but due to the development of ergotism with the simultaneous use of macrolides with ergotamine and dihydroergotamine derivatives, this combination is not recommended.
With long-term use of the drug Sumamed® forte, the development of pseudomembranous colitis caused by Clostridium difficile, both in the form of mild diarrhea and severe colitis, is possible. If antibiotic-associated diarrhea develops while taking Sumamed® forte, as well as 2 months after the end of therapy, clostridial pseudomembranous colitis should be excluded. You should not use drugs that inhibit intestinal motility.
When treated with macrolides, incl. azithromycin, prolongation of cardiac repolarization and QT interval was observed, increasing the risk of developing cardiac arrhythmias, incl. ari, which can lead to cardiac arrest.
Caution should be exercised when using the drug Sumamed® forte in patients with the presence of proarrhythmogenic factors (especially in elderly patients), incl. with congenital or acquired prolongation of the QT interval; in patients taking antiarrhythmic drugs of classes IA (quinidine, procainamide), III (dofetilide, amiodarone and sotalol), cisapride, terfenadine, antipsychotic drugs (pimozide), antidepressants (citalopram), fluoroquinolones (moxifloxacin and levofloxacin), with fluid and electrolyte disorders balance, especially in the case of hypokalemia or hypomagnesemia, clinically significant bradycardia, cardiac arrhythmia or severe heart failure.
The use of Sumamed® forte may provoke the development of myasthenic syndrome or cause an exacerbation of myasthenia.
Description
An antibiotic of the macrolide group - azalide.
Dosage form
Powder for the preparation of suspension for oral administration is white to yellowish-white in color, with a characteristic banana aroma; after dissolution in water - a homogeneous suspension from white to yellowish-white color, with a characteristic banana aroma.
Use in children
For children aged 6 months and older, it is recommended to prescribe the drug in the form of an oral suspension or 125 mg tablets.
Action
Bacteriostatic antibiotic of the macrolide-azalide group. Has a wide spectrum of antimicrobial action. The mechanism of action of azithromycin is associated with the suppression of protein synthesis in microbial cells. By binding to the 50S ribosomal subunit, it inhibits peptide translocase at the translation stage and suppresses protein synthesis, slowing down the growth and reproduction of bacteria. In high concentrations it has a bactericidal effect.
It is active against a number of gram-positive, gram-negative, anaerobes, intracellular and other microorganisms.
Sumamed® forte is active against aerobic gram-positive microorganisms: Staphylococcus aureus (methicillin-sensitive strains), Streptococcus pneumoniae (penicillin-sensitive strains), Streptococcus pyogenes; aerobic gram-negative microorganisms: Haemophilus influenzae, Haemophilus parainfluenzae, Legionella pneumophila, Moraxella catarrhalis, Pasteurella multocida, Neisseria gonorrhoeae; anaerobic microorganisms: Clostridium perfringens, Fusobacterium spp., Prevotella spp., Porphyriomonas spp.; other microorganisms: Chlamydia trachomatis, Chlamydia pneumoniae, Chlamydia psittaci, Mycoplasma pneumoniae, Mycoplasma hominis, Borrelia burgdorferi.
Microorganisms that can develop resistance to azithromycin: gram-positive aerobes - Streptococcus pneumoniae (penicillin-resistant strains and strains with intermediate sensitivity to penicillin).
Microorganisms with natural resistance: gram-positive aerobes - Enterococcus faecalis, Staphylococcus aureus (methicillin-resistant strains), Staphylococcus epidermidis (methicillin-resistant strains); anaerobes - Bacteroides fragilis.
Cases of cross-resistance between Streptococcus pneumoniae, Streptococcus pyogenes (group A beta-hemolytic streptococcus), Enterococcus faecalis and Staphylococcus aureus, including Staphylococcus aureus (methicillin-resistant strains) to erythromycin, azithromycin, other macrolides and lincosamides have been described.
Scale of sensitivity of microorganisms to azithromycin (MIC, mg/l)*
*Azithromycin has been used to treat infectious diseases caused by Salmonella typhi (MIC not more than 16 mg/l) and Shigella spp.
Side effects
The frequency of side effects is classified according to WHO recommendations: very common (≥10%), common (≥1%, <10%), uncommon (≥0.1%, <1%), rare (≥0.01%, <0.1%) , very rare (<0.01%), unknown frequency - cannot be estimated based on the available data.
Infectious diseases: uncommon - candidiasis, incl. mucous membrane of the oral cavity and genitals, pneumonia, pharyngitis, gastroenteritis, respiratory diseases, rhinitis; very rarely - pseudomembranous colitis.
From the blood and lymphatic system: infrequently leukopenia, neutropenia, eosinophilia; very rarely - thrombocytopenia, hemolytic anemia.
From the side of metabolism and nutrition: infrequently - anorexia.
Allergic reactions: uncommon - angioedema, hypersensitivity reaction; unknown frequency - anaphylactic reaction.
From the nervous system: often - headache; infrequently - dizziness, disturbance of taste, paresthesia, drowsiness, insomnia, nervousness; rarely - agitation; unknown frequency - hypoesthesia, anxiety, aggression, fainting, convulsions, psychomotor hyperactivity, loss of smell, perverted sense of smell, loss of taste, myasthenia gravis, delirium, hallucinations.
From the side of the organ of vision: infrequently - visual impairment.
From the organ of hearing and labyrinthine disorders: infrequently - hearing loss, vertigo; unknown frequency - hearing loss, incl. deafness and/or tinnitus.
From the cardiovascular system: infrequently - a feeling of palpitations, “flushes” of blood to the face; unknown frequency - decreased blood pressure, increased QT interval on ECG, ari, ventricular tachycardia.
From the respiratory system: infrequently - shortness of breath, nosebleeds.
From the gastrointestinal tract: very often - diarrhea; often - nausea, vomiting, abdominal pain: infrequently - flatulence, dyspepsia, constipation, gastritis, dysphagia, bloating, dry oral mucosa, belching, ulcers of the oral mucosa, increased secretion of the salivary glands; very rarely - change in tongue color, pancreatitis.
From the liver and biliary tract: infrequently - hepatitis; rarely - impaired liver function, cholestatic jaundice; unknown frequency - liver failure (in rare cases with death, mainly due to severe liver dysfunction), liver necrosis, fulminant hepatitis.
From the skin and subcutaneous tissues: uncommon - skin rash, itching, urticaria, dermatitis, dry skin, sweating; rarely - photosensitivity reaction; unknown frequency - Stevens-Johnson syndrome, toxic epidermal necrolysis, erythema multiforme.
From the musculoskeletal system: uncommon - osteoarthritis, myalgia, back pain, neck pain; unknown frequency - arthralgia.
From the kidneys and urinary tract: infrequently - dysuria, pain in the kidney area; unknown frequency - interstitial nephritis, acute renal failure.
From the genital organs and mammary gland: infrequently - metrorrhagia, dysfunction of the testicles.
Other: infrequently - asthenia, malaise, feeling of fatigue, facial swelling, chest pain, fever, peripheral edema.
Laboratory data: often - a decrease in the number of lymphocytes, an increase in the number of eosinophils, an increase in the number of basophils, an increase in the number of monocytes, an increase in the number of neutrophils, a decrease in the concentration of bicarbonates in the blood plasma; infrequently - increased activity of AST, ALT, increased concentration of bilirubin in the blood plasma, increased concentration of urea in the blood plasma, increased concentration of creatinine in the blood plasma, change in the potassium content in the blood plasma, increased activity of alkaline phosphatase in the blood plasma, increased chlorine content in the blood plasma, increased blood glucose concentration, increased platelet count, increased hematocrit, increased plasma bicarbonate concentration, change in plasma sodium content.
Use during pregnancy and breastfeeding
During pregnancy, the use of the drug is possible only if the potential benefit of therapy for the mother outweighs the possible risk to the fetus and child.
Breastfeeding should be suspended during treatment with azithromycin.
Interaction
- Antacids
Antacid drugs do not affect the bioavailability of azithromycin, but reduce Cmax in the blood by 30%, so Sumamed® forte should be taken at least 1 hour before or 2 hours after taking these drugs and food.
- Cetirizine
Concomitant use of azithromycin with cetirizine (20 mg) for 5 days in healthy volunteers did not lead to pharmacokinetic interaction or a significant change in the QT interval.
- Didanosine (dideoxyinosine)
The simultaneous use of azithromycin (1200 mg/day) and didanosine (400 mg/day) in 6 HIV-infected patients did not reveal changes in the pharmacokinetic indications of didanosine compared to the placebo group.
- Digoxin (P-glycoprotein substrates)
Simultaneous use of macrolide antibiotics, incl. azithromycin, with P-glycoprotein substrates such as digoxin, leads to increased concentrations of P-glycoprotein substrate in the blood serum. Thus, with the simultaneous use of azithromycin and digoxin, it is necessary to take into account the possibility of increasing the concentration of digoxin in the blood serum.
- Zidovudine
The simultaneous use of azithromycin (single dose of 1000 mg and multiple doses of 1200 mg or 600 mg) has a minor effect on pharmacokinetics, incl. renal excretion of zidovudine or its glucuronide metabolite. However, the use of azithromycin caused an increase in the concentration of phosphorylated zidovudine, a clinically active metabolite in peripheral blood mononuclear cells. The clinical significance of this fact is unclear. Azithromycin interacts weakly with isoenzymes of the cytochrome P450 system. Azithromycin has not been shown to participate in pharmacokinetic interactions similar to erythromycin and other macrolides. Azithromycin is not an inhibitor or inducer of cytochrome P450 isoenzymes.
- Ergot alkaloids
Given the theoretical possibility of ergotism, the simultaneous use of azithromycin with ergot alkaloid derivatives is not recommended.
Pharmacokinetic studies were conducted on the simultaneous use of azithromycin and drugs whose metabolism occurs with the participation of isoenzymes of the cytochrome P450 system.
- Atorvastatin
Concomitant use of atorvastatin (10 mg daily) and azithromycin (500 mg daily) did not cause changes in atorvastatin plasma concentrations (based on an HMC-CoA reductase inhibition assay). However, in the post-marketing period, isolated case reports of rhabdomyolysis have been received in patients receiving concomitant azithromycin and statins.
- Carbamazepine
Pharmacokinetic studies involving healthy volunteers did not reveal a significant effect on the plasma concentrations of carbamazepine and its active metabolite in patients receiving concomitant azithromycin.
- Cimetidine
In pharmacokinetic studies of the effect of a single dose of cimetidine on the pharmacokinetics of azithromycin, no changes in the pharmacokinetics of azithromycin were detected when cimetidine was administered 2 hours before azithromycin.
- Indirect anticoagulants (coumarin derivatives)
In pharmacokinetic studies, azithromycin did not affect the anticoagulant effect of a single 15 mg dose of warfarin administered to healthy volunteers. Potentiation of the anticoagulant effect has been reported after simultaneous use of azithromycin and indirect anticoagulants (coumarin derivatives). Although a causal relationship has not been established, the need for frequent monitoring of prothrombin time should be considered when using azithromycin in patients receiving indirect oral anticoagulants (coumarin derivatives).
- Cyclosporine
In a pharmacokinetic study involving healthy volunteers who took azithromycin (500 mg/day once) orally for 3 days, followed by cyclosporine (10 mg/kg/day once), a significant increase in plasma Cmax and AUC0-5 of cyclosporine was detected. . Caution is advised when using these drugs together. If simultaneous use of these drugs is necessary, it is necessary to monitor the concentration of cyclosporine in the blood plasma and adjust the dose accordingly.
- Efavirenz
Concomitant use of azithromycin (600 mg/day once) and efavirenz (400 mg/day) daily for 7 days did not cause any clinically significant pharmacokinetic interaction.
- Fluconazole
Concomitant use of azithromycin (1200 mg once) did not change the pharmacokinetics of fluconazole (800 mg once). The total exposure and half-life of azithromycin did not change with simultaneous use of fluconazole, however, a decrease in Cmax of azithromycin was observed (by 18%), which had no clinical significance.
- Indinavir
The simultaneous use of azithromycin (1200 mg once) did not cause a statistically significant effect on the pharmacokinetics of indinavir (800 mg 3 times a day for 5 days).
- Methylprednisolone
Azithromycin does not have a significant effect on the pharmacokinetics of methylprednisolone.
- Nelfinavir
The simultaneous use of azithromycin (1200 mg) and nelfinavir (750 mg 3 times / day) causes an increase in the equilibrium concentrations of azithromycin in the blood serum. No clinically significant side effects were observed and no dose adjustment of azithromycin was required when used concomitantly with nelfinavir.
- Rifabutin
The simultaneous use of azithromycin and rifabutin does not affect the concentration of each drug in the blood serum. Neutropenia has sometimes been observed with simultaneous use of azithromycin and rifabutin. Although neutropenia has been associated with the use of rifabutin, a causal relationship between the use of the combination of azithromycin and rifabutin and neutropenia has not been established.
- Sildenafil
When used in healthy volunteers, there was no evidence of the effect of azithromycin (500 mg/day daily for 3 days) on the AUC and Cmax of sildenafil or its main circulating metabolite.
- Terfenadine
In pharmacokinetic studies, there was no evidence of interaction between azithromycin and terfenadine. There have been isolated cases reported where the possibility of such an interaction could not be completely excluded, but there was no concrete evidence that such an interaction occurred.
It has been found that the simultaneous use of terfenadine and macrolides can cause arrhythmia and prolongation of the QT interval.
- Theophylline
No interaction has been detected between azithromycin and theophylline.
- Triazolam/midazolam
No significant changes in pharmacokinetic parameters were detected with simultaneous use of azithromycin with triazolam or midazolam in therapeutic doses.
- Trimethoprim/sulfamethoxazole
Concomitant use of trimethoprim/sulfamethoxazole with azithromycin did not show a significant effect on Cmax, total exposure or renal excretion of trimethoprim or sulfamethoxazole. Azithromycin serum concentrations were consistent with those found in other studies.
Overdose
Symptoms (similar to side effects that occur when taking the drug in recommended doses): severe nausea, temporary hearing loss, vomiting, diarrhea.
Treatment: taking activated carbon, conducting symptomatic therapy, monitoring vital functions.
Impact on the ability to drive vehicles and operate machinery
If undesirable effects on the nervous system and organ of vision develop, caution should be exercised when performing actions that require increased concentration and speed of psychomotor reactions.
Instructions for use SUMAMED® (SUMAMED)
- Atorvastatin
With simultaneous use of atorvastatin (10 mg per day) and azithromycin (500 mg per day), azithromycin did not affect the plasma concentration of atorvastatin. However, post-marketing cases of rhabdomyolysis have been observed in patients taking azithromycin with statins.
Carbamazepine
In pharmacokinetic studies conducted in healthy volunteers, azithromycin did not have a significant effect on plasma levels of carbamazepine or its active metabolite.
Oral coumarin anticoagulants
In a pharmacokinetic interaction study, azithromycin never altered the anticoagulant effect of warfarin when administered as a single 15 mg dose in healthy patients. In the post-marketing period, an increase in the anticoagulant effect of coumarin derivatives was observed when used in combination with azithromycin. Although a cause-and-effect relationship has not been established, more frequent monitoring of prothrombin time should be considered when azithromycin is used in patients taking coumarin anticoagulants.
While taking cimetidine
two hours before taking azithromycin, no changes in the pharmacokinetics of azithromycin were observed.
Cyclosporine
In a pharmacokinetic study in healthy volunteers who received a daily dose of azithromycin 500 mg orally for 3 days and who subsequently took a single dose of 10 mg/kg cyclosporine orally, the Cmax and AUC0-5 values of cyclosporine were significantly increased. Therefore, these drugs should be used simultaneously with caution. If concomitant use of these drugs is necessary, monitor cyclosporine levels and adjust the dose accordingly.
Efavirenz
Co-administration of a single dose of azithromycin 600 mg and efavirenz 400 mg per day for 7 days did not result in a clinically significant pharmacokinetic interaction.
Fluconazole
The simultaneous use of a single dose of 1200 mg of azithromycin does not change the pharmacokinetics of a single dose of 800 mg of fluconazole. The total concentration and half-life of azithromycin did not change with concomitant use of fluconazole. However, a clinically insignificant decrease in Cmax (18%) of azithromycin was noted.
Indinavir
Concomitant use of a single dose of 1200 mg of azithromycin does not have a significant effect on the pharmacokinetics of indinavir when administered at a dose of 800 mg three times daily for 5 days.
Methylprednisolone
In a pharmacokinetic study of drug interactions in healthy patients, azithromycin did not have a significant effect on the pharmacokinetics of methylprednisolone.
Midazolam
In healthy patients, simultaneous administration of azithromycin 500 mg daily for 3 days does not cause clinically significant changes in the pharmacokinetics and pharmacodynamics of midazolam when administered once 15 mg.
Eating reduces the absorption of azithromycin, so Sumamed should be taken 1 hour or 2 hours after meals.
Nelfinavir
The simultaneous use of azithromycin (1200 mg) and nelfinavir (750 mg three times a day) leads to an increase in the concentration of azithromycin at steady state. No clinically significant side effects were identified. There is no need to adjust the dose.
Rifabutin
Concomitant use of azithromycin and rifabutin did not affect the serum concentrations of either drug. With simultaneous use of azithromycin and rifabutin, neutropenia was observed in patients. Neutropenia is associated with the use of rifabutin; a causal relationship when taken in combination with azithromycin has not been established.
Sildenafil
There was no evidence of an effect of azithromycin (500 mg daily for 3 days) on the blood AUC and Cmax values of sildenafil or its major metabolites.
Terfenadine
There was no interaction between terfenandine and azithromycin. In some cases, such interaction cannot be completely eliminated. Yet there is no evidence of such a reaction. As with the use of other macrolides, azithromycin and terphenandine should be used simultaneously with caution.
Theophylline
Azithromycin did not affect the pharmacokinetics of theophylline in healthy volunteers. Concomitant use of theophylline and other macrolide antibiotics has sometimes resulted in increased serum theophylline concentrations.
Triazolam
Co-administration of azithromycin 500 mg on day 1 and 250 mg on day 2 and triazolam 0.125 mg on day 2 in 14 healthy patients did not have a significant effect on the pharmacokinetic parameters of triazolam compared with co-administration of triazolam and placebo.
Trimethoprim/sulfamethoxazole
Co-administration of trimethoprim/sulfamethoxazole DS (160 mg/800 mg) for 7 days and 1200 mg azithromycin on day 7 had no significant effect on peak concentrations and urinary excretion of trimethoprim/sulfamethoxazole. Azithromycin serum concentrations were similar to those in other studies.
