Clinzol ZD (Gel) Instructions for Use

Marketing Authorization Holder

Zelenaya Dubrava, CJSC (Russia)

ATC Code

D10AF01 (Clindamycin)

Active Substance

Clindamycin (Rec.INN registered by WHO)

Dosage Form

Clinzol ZD

Gel for external use 1%: tubes 15 g, 30 g, 40 g, or 50 g

Dosage Form, Packaging, and Composition

Gel for external use 1% colorless, almost transparent, homogeneous with a characteristic odor; the presence of opalescence is allowed.

Excipients : allantoin – 2 mg, carbomer – 8 mg, methylparahydroxybenzoate – 3 mg, macrogol 400 (polyethylene glycol) – 100 mg, propylene glycol – 50 mg, sodium hydroxide solution 30% – to pH 4.5-6.5, purified water – to 1 g.

15 g – aluminum tubes (1) – cardboard packs.
30 g – aluminum tubes (1) – cardboard packs.
40 g – aluminum tubes (1) – cardboard packs.
50 g – aluminum tubes (1) – cardboard packs.

Clinical-Pharmacological Group

A drug with antibacterial action for the treatment of acne

Pharmacotherapeutic Group

Drugs for the treatment of acne; drugs for the treatment of acne for topical use; antimicrobial agents for the treatment of acne

Pharmacological Action

An antibiotic of the lincosamide group. In therapeutic doses, it has a bacteriostatic effect; in high doses, it has a bactericidal effect on susceptible strains. It disrupts intracellular protein synthesis at early stages by binding to the 50S subunit of bacterial ribosomes.

Clindamycin is active against most aerobic gram-positive bacteria, including Staphylococcus spp. (including strains producing penicillinase); Streptococcus spp., Bacillus anthracis, Corynebacterium diphtheriae.

Clindamycin is also active against anaerobic gram-positive bacteria, including Eubacterium, Propionibacterium, Peptococcus, Peptostreptococcus spp., many strains of Clostridium perfringens and Clostridium tetani.

Among gram-negative anaerobes, Fusobacterium spp. (excluding F. varium, which is usually resistant), Veillonella, Bacteroides spp. (including B. fragilis) are susceptible to clindamycin.

Against Mycoplasma spp., Clindamycin is usually less active than erythromycin.

Some strains of Actinomyces spp. and Nocardia asteroides are susceptible to clindamycin.

Some antiprotozoal activity against Toxoplasma gondii and Plasmodium spp. has been reported.

Enterococcus spp., methicillin-resistant strains of Staphylococcus aureus, most gram-negative aerobic bacteria (including Enterobacteriaceae spp.), Neisseria gonorrhoeae, Neisseria meningitidis and Haemophilus influenzae, as well as fungi (including yeasts) and viruses are resistant to clindamycin.

Pharmacokinetics

After oral administration, about 90% of the clindamycin dose is absorbed from the gastrointestinal tract. After a dose of 150 mg, the plasma concentration of clindamycin is 2-3 µg/ml after 1 hour, and about 0.7 µg/ml after 6 hours. After doses of 300 mg and 600 mg, the C_max in plasma is 4 µg/ml and 8 µg/ml, respectively. When taken simultaneously with food, the absorption rate decreases, while the extent of absorption changes insignificantly.

After intramuscular injection of a 300 mg dose, the average C_max in plasma is 6 µg/ml and is reached within 3 hours; with a 600 µg dose – 9 µg/ml.

In children, C_max in plasma is reached within 1 hour. When the same doses are administered intravenously, the C_max in plasma is 7-10 µg/ml and is reached at the end of the infusion.

Clindamycin is absorbed in small amounts from the skin surface.

With intravaginal administration, systemic absorption can be about 5%.

Clindamycin is widely distributed in body tissues and fluids, including bones, but does not reach significant concentrations in the CNS. High concentrations of clindamycin are found in bile. Clindamycin accumulates in leukocytes and macrophages.

About 90% of clindamycin is bound to plasma proteins.

Clindamycin is metabolized, mainly in the liver, to form N-demethylated and sulfoxide metabolites, as well as inactive metabolites.

T_1/2 is 2-3 hours, increased in patients with severe kidney disease and in premature newborns.

About 10% of the dose is excreted in the urine as unchanged drug and metabolites and about 4% in feces. The remainder is excreted as inactive metabolites. Excretion is slow, over 7 days.

Not removed from the blood by dialysis.

Indications

For systemic use: severe infectious and inflammatory diseases caused by microorganisms susceptible to clindamycin: pneumonia, lung abscess, pleural empyema, osteomyelitis, endometritis, adnexitis, purulent skin infections, soft tissues, wounds, peritonitis. Prevention of peritonitis and intra-abdominal abscesses after intestinal perforation or injury (in combination with aminoglycosides). As a reserve antibiotic for infections caused by strains of staphylococcus and other gram-positive microorganisms resistant to penicillin. As a prophylactic agent for tooth extraction.

For external use: acne vulgaris.

For topical use: vaginosis caused by susceptible microorganisms.

ICD codes

Dosage Regimen

Orally for adults – 150-450 mg every 6 hours. For tooth extraction for prophylaxis, a single dose is 600 mg in 1-2 doses according to the scheme.

Orally for children – 3-6 mg/kg every 6 hours.

For intramuscular or intravenous administration to adults – 0.6-2.7 g/day in divided doses. For very severe infections, up to 4.8 g/day can be administered intravenously. Maximum doses for intramuscular administration single dose – 600 mg, for intravenous infusion lasting 1 hour – 1.2 g.

For intramuscular or intravenous administration to children over 1 month of age – 15-40 mg/kg/day in divided doses. For severe infections, a total dose of at least 300 mg/day should be administered.

Externally – apply to the affected area 2-3 times/day.

Intravaginally – 100 mg at night for 3-7 days.

Adverse Reactions

From the digestive system nausea, vomiting, abdominal pain, diarrhea, after intravenous administration in high doses – unpleasant metallic taste; after oral administration – symptoms of esophagitis; transient increase in the activity of hepatic transaminases and bilirubin in blood plasma; in isolated cases – jaundice and liver disease.

From the hematopoietic system rarely – reversible leukopenia, neutropenia, thrombocytopenia, agranulocytosis.

Allergic reactions urticaria; rarely – erythema multiforme; in some cases – angioedema, fever, anaphylactic shock.

From the cardiovascular system with rapid intravenous administration – decreased blood pressure, dizziness, weakness.

Local reactions with intravenous administration in high doses – phlebitis; with intramuscular administration rarely – irritation at the injection site, development of infiltrate, abscess.

With external use irritation at the application site, contact dermatitis. Due to slight systemic absorption, there is a possibility of systemic side effects.

With topical use cervicitis, vaginitis or vulvovaginal irritation.

Effects due to chemotherapeutic action pseudomembranous colitis, candidiasis.

Contraindications

Hypersensitivity to clindamycin or lincomycin.

For systemic use: severe impairment of liver or kidney function, myasthenia gravis, bronchial asthma, ulcerative colitis (in history), pregnancy, lactation, children under 1 month of age, old age.

Use in Pregnancy and Lactation

Clindamycin crosses the placental barrier into the fetal bloodstream. It is excreted in breast milk.

Clindamycin for oral and parenteral administration is contraindicated during pregnancy and lactation.

Intravaginal use of clindamycin during pregnancy is possible if the intended benefit to the mother outweighs the potential risk to the fetus; during lactation – only for strict indications.

Use in Hepatic Impairment

Systemic use is contraindicated in severe liver impairment.

Use in Renal Impairment

Systemic use is contraindicated in severe renal impairment.

Pediatric Use

Systemic use is contraindicated in children under 1 month of age.

Geriatric Use

Systemic use is contraindicated in old age.

Special Precautions

Use with caution in patients with a history of gastrointestinal diseases.

If diarrhea or symptoms of colitis appear, Clindamycin should be discontinued.

Pseudomembranous colitis can appear both during clindamycin administration and 2-3 weeks after treatment cessation. Drugs that inhibit intestinal peristalsis should not be used.

It is not recommended to use Clindamycin simultaneously with drugs that slow down neuromuscular transmission.

Intravaginally, it is not recommended to use simultaneously with other intravaginal agents.

Drug Interactions

Clindamycin enhances the effect of drugs that block neuromuscular transmission.

With simultaneous use with opioids, an increase in the depressant effect on respiration is possible. Clindamycin may exhibit antagonism towards the activity of sympathomimetics.

Synergism regarding the antibacterial action on some anaerobes between clindamycin and ceftazidime, metronidazole, ciprofloxacin has been noted.

There is evidence that Clindamycin inhibits the bacterial activity of aminoglycosides. Due to the similarity of binding sites on ribosomes, Clindamycin may competitively inhibit the action of macrolides and chloramphenicol.

Storage Conditions

Store at 2°C (36°F) to 25°C (77°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Over-the-Counter

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.