Sumaclide 1000,1000 mg 3 pcs

Pharmacotherapeutic group

Azalid antibiotic

ATC code

J01FA10

Pharmacodynamics:

The broad-spectrum antibacterial agent azalide acts bacteriostatically. Binding to 50S-subunit of ribosomes inhibits peptide translocation stage inhibits protein synthesis inhibits bacterial growth and multiplication in high concentrations and produces bactericidal effect. It acts on extra- and intracellular pathogens.

Active against Gram-positive aerobic microorganisms: Streptococcus pneumoniae (penicillin-sensitive) Streptococcus pyogenes Staphylococcus aureus (methicillin-sensitive); Gram-negative aerobic organisms: Haemophilus influenzae Haemophilus parainfluenzae Moraxella catarrhalis Legionella pneumophila Neisseria gonorrhoeae Pasteurella multocida; some anaerobic microorganisms: Prevotella spp. Clostridium perlringens Fusobacterium spp. Porphyriomonas spp.; and Chlamydia trachomatis Chlamydia pneumoniae Chlamydia psittaci Mycoplasma pneumoniae Mycoplasma hominis Borrelia burgdorferi.

Microorganisms capable of developing resistance to azithromycin: Gram-positive aerobes (Streptococcus pneumoniae (penicillin-resistant). Initially resistant microorganisms: gram-positive aerobes (Enterococcus faecalis Staphylococcus spp. (methicillin-resistant staphylococci show very high resistance to macrolides) gram-positive bacteria resistant to erythromycin); anaerobes (Bacteroides lragilis).

It is inactive against erythromycin-resistant Gram-positive bacteria. Pharmacokinetics:

Azithromycin is quickly absorbed from the gastrointestinal tract due to its stability in acidic environment and lipophilicity. Bioavailability after single use of 05 g – 37% (effect of “first passage” through the liver) maximum drug concentration in plasma after peroral use of 05 g is 04 mg/l time of reaching maximum drug concentration in plasma – 25-29 h; in tissues and cells concentration is 10-50 times higher than in blood serum volume of distribution – 311 l/kg. It easily passes through histohematic barriers. It penetrates well into the respiratory tract, urogenital organs and tissues in the prostate, skin and soft tissues; it accumulates in lysosomes in low pH environment (which is especially important for eradication of intracellularly located pathogens). It is also transported by phagocytes by polymorphonuclear leukocytes and macrophages. It penetrates through cell membranes and generates high concentrations in cells.

The concentration in the foci of infection is significantly higher (by 24-34%) than in healthy tissues and correlates with the severity of inflammatory edema. In the focus of inflammation it is maintained in effective concentrations for 5-7 days after the last dose. Binding with plasma proteins is 7-50 % (inversely proportional to the concentration in blood).

It is demethylated in the liver and the resulting metabolites are not active. Plasma clearance is 630 ml/min: half-life of the preparation between 8 and 24 hours after drug intake – 14-20 hours half-life of the preparation from 24 to 72 hours – 41 hours. 50% is excreted with bile unchanged 6 % – by kidneys.

Eating significantly changes pharmacokinetics: maximum drug concentration in plasma is increased (by 31 %) the area under “concentration-time” curve does not change. In elderly men (65-85 years old) pharmacokinetic parameters did not change in women maximum drug concentration in plasma increased (by 30-50 %).

Indications

Active ingredient

Composition

Composition per tablet.

The active ingredient:

Azithromycin dihydrate – 1.048 g

(in terms of azithromycin 1 g)

The excipients of the core:

Hypromellose (hydroxypropyl methylcellulose) – 0.0126 g

sodium lauryl sulfate – 0.0018 g
calcium stearate – 0,0144 g

sodium stearyl fumarate – 0,0144 g

Sodium croscarmellose – 0,0432 g

calcium phosphate divalent (calcium hydrophosphate dihydrate) to receive 1.2 g of kernel mass

Excipients in coating:

Hypromellose (hydroxypropyl methylcellulose) – 0.029535 g

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Polysorbate-80 (tween-80) – 0,0029 g

Colorant Ponceau 4R, E 124 – 0,000065 g

How to take, the dosage

Orally, without chewing 1 hour before or 2 hours after a meal, once a day.

In case of urogenital tract infections caused by Chlamydia trachomatis (urethritis-cervicitis): uncomplicated urethritis/cervicitis – 1 g (1 tablet of 1000 mI) once.

When used in patients with mild to moderate renal dysfunction, no dose adjustment is required.

Dose adjustment is not required when used in patients with mild to moderate hepatic impairment in elderly patients.

Interaction

Antacids (A13+ and Mg2+-containing) ethanol and food slow down and decrease absorption of azithromycin (for oral forms) so the interval between their intake should be 1 h before or 2 h after taking food and the above medicines.

When co-administering warfarin and azithromycin (in usual doses) no change in prothrombin time was found, but since macrolides and warfarin may increase anticoagulation, patients should carefully monitor prothrombin time.

Asithromycin interacts poorly with cytochrome P450 isoenzymes ns has not been found to be involved in pharmacokinetic interactions similar to those of erythromycin and other macrolides and azithromycin is neither inducer nor inhibitor of cytochrome P450 isoenzymes.

In contrast to macrolides, no interaction with theophylline terfenadine carbamazepine triazolam digoxin has been noted.

We should use caution when using terfenadine and azithromycin concomitantly as terfenadine and different types of antibiotics have been found to cause arrhythmias and prolongation of ventricular complex duration reflecting the duration of electrical ventricular systole. Therefore, the above complications cannot be excluded when terfenadine and azithromycin are used together.

Ergotamine and dihydroergotamine: aggravation of toxic effects (vasospasm dysesthesia). Macrolides delay excretion increases plasma concentration and toxicity of cycloserine indirect anticoagulants methylprednisolone felodipine as well as drugs subject to microsomal oxidation (carbamazepine terfenadine cyclosporine hexobarbital ergot alkaloids valproic acid disopyramide bromocriptine phenytoin oral hypoglycemic drugs).This type of interaction has not been observed with azalides (including azithromycin).

Lincosamides weaken and tetracycline and chloramphenicol enhance the effectiveness of azithromycin.

With cetirizine: Simultaneous use of azithromycin with cetirizine (20 mg) for 5 days in healthy volunteers did not result in pharmacokinetic interaction and significant QT interval changes.

With didanosine: Concomitant use of azithromycin (1200 mg/day) and didanosine (400 mg/day) in 6 HIV-infected patients showed no change in the pharmacokinetic readings of didanosine compared with the placebo group.

With zidovudine: Concomitant use of azithromycin (single administration of 1000 mg and multiple administration of 1200 mg or 600 mg) has little effect on pharmacokinetics including renal excretion of zidovudine or its glucuronide metabolite. However, azithromycin administration caused an increase in the concentration of phosphorylated zidovudine clinically active metabolite in peripheral blood mononuclear cells. The clinical significance of this fact is unclear.

With atorvastatin: concomitant use of atorvastatin (10 mg daily) and azithromycin (500 mg daily) did not cause changes in plasma concentrations of atorvastatin (based on HMK-CoA reductase inhibition assay). However, there have been isolated reports of cases of rhabdomyolysis in patients taking azithromycin and statins concomitantly.

With cimetidine: according to the results of the study aimed at determining the effect of a single dose of cimetidine taken 2 hours before taking azithromycin on its pharmacokinetics no changes were found.

With efavirenz: Concomitant use of azithromycin (600 mg/day once daily) and efavirenz (400 mg/day) daily for 7 days did not cause any clinically significant pharmacokinetic interaction.

With fluconazole: concomitant use of azithromycin (1200 mg once daily) did not alter the pharmacokinetics of fluconazole (800 mg once daily). Total exposure and half-life of azithromycin were not altered by concomitant use of fluconazole, but there was an 18% decrease in maximum azithromycin concentration, which had no clinical significance.

With indinavir: concomitant use of azithromycin (1200 mg once daily) had no statistically significant effect on the pharmacokinetics of indinavir (800 mg three times daily for 5 days).

With nelfinavir: concomitant use of azithromycin (1200 mg) and nelfinavir (750 mg 3 times daily) causes increase of equilibrium plasma concentration of azithromycin no clinically significant adverse effects were observed and no dose adjustments of azithromycin in concomitant use with nelfinavir are required.

With rifabutin: Neutropenia has occasionally been observed with concomitant use of azithromycin and rifabutin, although neutropenia has been associated with rifabutin use, a causal relationship between azithromycin and rifabutin combination use and neutropenia has not been established.

With sildenafil: when used in healthy volunteers there is no evidence of the effect of azithromycin (500 mg/day for 3 days) when used in combination has no effect on the area under the pharmacokinetic curve “concentration-time” (AUC) maximum concentration (Cmax) time to maximum concentration (Cmax) elimination rate constant and elimination half-life of sildenafil or its main circulating metabolite.

With trimethoprim/sulfamethoxazole: Concomitant use of trimethoprim/sulfamethoxazole with azithromycin showed no significant effect on the maximum concentration of total exposure or renal excretion of trimethoprim or sulfamethoxazole. Serum azithromycin concentrations were consistent with those found in other studies.

In case of concomitant use of azithromycin and cyclosporine, correction of the dose of cyclosporine is necessary.

Special Instructions

If a dose is missed, the missed dose should be taken as soon as possible and subsequent doses should be taken 24 hours apart.

A 2-hour break should be observed with concomitant use of antacids. Azithromycin should be used with caution in patients with mild to moderate hepatic impairment due to possible fulminant hepatitis and hepatic failure; in patients with mild to moderate renal impairment (under control of renal function).

In the presence of symptoms of hepatic impairment (rapidly increasing asthenia jaundice darkening of urine bleeding tendency hepatic encephalopathy) azithromycin therapy should be discontinued and liver function tests should be performed.

The concomitant use of azithromycin with ergotamine and dihydroergotamine derivatives is contraindicated because of the possible development of ergotism.

As with other antibacterial agents, patients should be regularly monitored during therapy with azithromycin for the presence of non-susceptible microorganisms and for signs of superinfections, including fungal infections.

Pseudomembranous colitis caused by Clostridium difficile is possible when taking azithromycin in the form of both mild diarrhea and severe colitis. If antibiotic-associated diarrhea develops during azithromycin therapy and 2 months after the end of therapy, clostridial pseudomembranous colitis should be excluded. During azithromycin therapy the use of drugs inhibiting intestinal peristalsis is contraindicated.

Attention should be avoided to activities requiring high concentration and quick psychomotor reactions (including driving a car) during treatment with the drug.

Contraindications

Hypersensitivity to azithromycin other macrolides other components of the drug hypersensitivity to erythromycin; ketolides; simultaneous use with ergotamine and dihydroergotamine severe liver function impairment (Child-Pugh class C); severe lobe function impairment (creatinine clearance less than 40 ml/min); breastfeeding children under 18 years (for this dosage).

Mild to moderate myasthenia gravis impaired liver function (creatinine clearance greater than 40 mL/min) in patients with proarrhythmogenic factors (especially in elderly patients): with congenital or acquired prolongation of the QT interval in patients receiving therapy with antiarrhythmic drugs of class IA(quinidine procainamide) III(dofetilide amiodarone and sotalol) cisapride terfenadine antipsychotic drugs (pimozide) antidepressants (citalopram) fluoroquinolones (moxifloxacin and levofloxacin) with disorders of water andelectrolyte balance disorders especially in case of hypokalemia or hypomagnesemia with clinically significant bradycardia, cardiac arrhythmia or severe heart failure; concomitant use of digoxin warfarin cyclosporine.

Side effects

– Digestive system disorders: anorexia nausea vomiting color change of tongue dry mouth mucosa belching oral mucosa ulcers increased salivary gland secretion abdominal pain flatulence constipation dyspepsia dysphagia abdominal bloating diarrhea pseudomembranous colitis melena pancreatitis increased activity of “liver” transaminases bilirubin level hepatitis cholestatic jaundice fulminant hepatitis liver failure (possibly fatal) liver necrosis In addition, decreased appetite gastritis.

– Cardiovascular system: palpitations pain in the chest decrease blood pressure increase QT interval in electrocardiogram pirouette arrhythmia ventricular tachycardia flushing blood to the face.

– Blood system: leukopenia neutropenia eosinophilia thrombocytopenia hemolytic anemia.

– Nervous system: dizziness headache vertigo sleepiness paresthesia agitation increased fatigue tinnitus hyperkinesia anxiety neurosis sleep disorders sweating insomnia hypoesthesia aggression fainting convulsions psychomotor hyperactivity nervousness agitation delirium hallucinations.

– Sensory organs: visual impairment conjunctivitis reversible hearing impairment to deafness hearing impairment loss of taste loss perversion of sense of smell loss of sense of smell.

– Urinary system: vaginal candidiasis dysuria kidney pain interstitial nephritis acute renal failure metrorrhagia testicular dysfunction.

– Allergic reactions: rash urticaria pruritus skin angioedema anaphylactic reaction Stevens-Johnson syndrome necrolysis erythema multiforme.

– Skin disorders: dermatitis dry skin photosensitization.

– Musculoskeletal system: myasthenia myalgia back pain neck pain arthralgia osteoarthritis.

– Respiratory system: dyspnea nasal bleeding.

– Infectious diseases: rhinitis pharyngitis respiratory diseases pneumonia gastroenteritis candida mucosa.

– Other: asthenia facial edema fever peripheral edema.

– Laboratory data: in plasma: increased number of basophils monocytes neutrophils decreased or increased concentration of bicarbonates increased activity of alkaline phosphatase increased concentration of chlorine increased concentration of glucose increased number of platelets increased hematocrit changed sodium increased concentration of urea creatinine changed potassium content.

Overdose

Symptoms: severe nausea temporary hearing loss vomiting diarrhea.

Treatment: gastric lavage symptomatic therapy.

Pregnancy use

Pregnant use is possible only if the estimated benefit to the mother exceeds the potential risk to the fetus.

Breast-feeding should be stopped during treatment (data on penetration into breast milk are not available).

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