Amlin Injection – Lincomycin 

Amlin Injection – Lincomycin 

Amlin Injection – Lincomycin 

AMLIN (Lincomycin) is a lincosamide antibiotic that comes from the actinomycete Streptomycin lincolnesis. Chemically, lincomycin is described as Lincomycin hydrochloride consists mainly of the monohydrate of methyl  6,8-dideoxy-6-[(2S,4R)-1-methyl-4-propylpyrrolidine-2-carboxamido]-1-thio-D-erythro--D-galacto-octopyranoside hydrochloride. The molecular formula is C18H34N2O6S and the structural formula is:

DESCRIPTION

AMLIN (Lincomycin) is a lincosamide antibiotic that comes from the actinomycete Streptomycin lincolnesis. Chemically, lincomycin is described as Lincomycin hydrochloride consists mainly of the monohydrate of methyl  6,8-dideoxy-6-[(2S,4R)-1-methyl-4-propylpyrrolidine-2-carboxamido]-1-thio-D-erythro--D-galacto-octopyranoside hydrochloride. The molecular formula is C18H34N2O6S and the structural formula is:

QUALITATIVE & QUANTITATIVE COMPOSITION

AMLIN (Lincomycin) is available for oral/IM/IV administration as:

AMLIN Capsules 500mg   

Each capsule contains:

Lincomycin Hydrochloride equivalent to Lincomycin.………500mg

AMLIN INJETION 600 mg

Each ml contains:

Lincomycin Hydrochloride equivalent to Lincomycin.………300mg

CLINICAL PHARMACOLOGY

Mechanism of Action

Lincomycin is an antibiotic produced by fermentation of Streptomyces lincolnensis. Lincomycin inhibits bacterial protein synthesis by binding to the 50S subunit of the bacterial ribosome. Lincomycin is predominantly bacteriostatic in vitro. The antibacterial activity of Lincomycin appears to best correlate with the length of time the concentration of active ingredient remains above the minimum inhibitory concentration (MIC) of the infecting organism.

Pharmacokinetics

Absorption/Distribution

Lincomycin is absorbed rapidly after a 500 mg oral dose in the fasting state, producing an average peak serum level of 5.3 micrograms/mL at 2 hours post dose, . Doubling the dose increases but does not double the peak serum levels. Food in the stomach reduces total absorption as well as peak serum levels.

Distribution

Significant levels have been demonstrated in the majority of body tissues. Although lincomycin appears to diffuse into cerebrospinal fluid (CSF), levels of lincomycin in the CSF appear inadequate for the treatment of meningitis.

Metabolism

Tissue level studies indicate that bile is an important route of excretion. The excretion of lincomycin in urine and bile does not account for all of the administered dose and a substantial proportion of the drug appears to be inactivated in the body, presumably in the liver.

Excretion

Urinary recovery of drug in a 24-hour period ranges from 1.0% to 31% (mean: 4.0%) after a single oral dose of 500 mg. Bile is an important route of excretion.

Intramuscular administration of a single dose of 600 mg of lincomycin produces an average peak serum level of 11.6 micrograms/mL at 60 minutes and maintains therapeutic levels for 17 to 20 hours for most susceptible gram-positive organisms. Urinary excretion after this dose ranges from 1.8% to 24.8% (mean: 10.3%).

The intravenous infusion over a 2-hour interval of 600 mg of lincomycin achieves average peak serum levels of 15.9 μg/mL and yields therapeutic levels for 14 hours for most susceptible gram-positive organisms. Urinary excretion ranges from 4.9% to 23.3% (mean: 15.1%).

Haemodialysis and peritoneal dialysis do not effectively remove lincomycin from the blood.

Special Populations

Patients with Renal Impairment

The serum half-life of LINCOCIN may be prolonged in patients with severe impairment of renal function compared to patients with normal renal function.

Patients with Hepatic Impairment In patients with abnormal hepatic function, serum half-life may be two-fold longer than in patients with normal hepatic function.

THERAPEUTIC INDICATIONS

AMLIN is indicated in the treatment of serious infections due to susceptible strains of  gram-positive aerobes such as streptococci, pneumococci and staphylococci.

AMLIN (Lincomycin) is effective in the treatment of the following infections.

* Upper respiratory infections including tonsillitis, pharyngitis, otitis media, sinusitis, scarlet fever and as

  adjuvant therapy for diphtheria. Effectiveness in the treatment of mastoiditis would be anticipated.

* Lower respiratory infections including acute and chronic bronchitis and pneumonia.

* Skin and skin structure infections including cellulitis, furuncles, abscesses, impetigo, acne and wound

  infections. Conditions such as erysipelas, lymphadenitis, paronychia (panaritium), mastitis and cutaneous

  gangrene should, if caused by susceptible organisms, respond to lincomycin therapy.

* Bone and joint infections including osteomyelitis and septic arthritis.

* Septicemia and endocarditis. Selected cases of septicaemia and/or endocarditis due to susceptible

organisms have responded well to lincomycin. However, bactericidal drugs are often preferred for these  infections. * Bacillary Dysentery. Although Shigella is resistant to lincomycin in vitro (MIC approximately 200-400 micrograms/mL), lincomycin has been effective in its treatment due to the very high levels of lincomycin attained in the bowel (approximately 3000-7000 micrograms/gram of stool). Amlin has been demonstrated to be effective in an  Aerobic wound, Soft tissue, Pulmonary and bacteraemic infections.

The anaerobic spectrum of activity includes Clostridium tetani, Clostridium perfringens, Corynebacterium diptheriae, Corynebacterium acnes, Bacteroides, Fusobacterium, Peptococcus Peptostreptococcus and Antinomies.

DOSAGE AND ADMINISTRATION 

CONTRAINDICATIONS

Lincomycin is contraindicated in patients previously found to be hypersensitive to lincomycin or clindamycin. It is not indicated in the treatment of minor bacterial infections or viral infections. Lincomycin is not indicated in the newborn.

SIDE EFFECT

  • Potential side effects with AMLIN include:
  • Diarrhea, nausea, stomach cramps and vomiting.
  • Vaginal itching or discharge.
  • Skin rash or itching
  • Pain or swelling in the area where the drug was injected.

PRECAUTIONS

AMLIN has to be given cautionally to patient with gastrointestinal disorders, especially in colitis, to asthametic patients and those with severe allergies in their history. It has not been confirmed that administration of AMLIN to newborn and pregnancy is harmless. In case of long administration of AMLIN renal tests have to be carried out as well as blood followed up.

STORAGE

AMLIN Injection:

Store below 300C. Protect from sunlight.

The expiration date refers to the product correctly stored at the required conditions

AMLIN Capsules

Do not store above 30°C.

Store in the original package in order to protect from light and moisture.

 PRESENTATION     

– AMLIN (Lincomycin) Capsules 500mg are available in blister packs of 4×3 capsules.

– AMLIN (Lincomycin) Injection in 2ml x10 Ampoules.

Amlin Injection by Amros Pharmaceutical