Clindamycin

Antibacterials (protein synthesis inhibitors)

30s • Aminoglycosides•Tetracycline Antibiotics

50s •Oxazolidinone•Peptidyl transferase•MLS(transpeptidation/translocation)

EF-G •steriods

Spectrum of activity

Lincosamide are narrow-spectrum antibiotics which act on staphylococci,streptococci,pneumococci,

Nonspore-forming anaerobic flora peptostreptococcus,peptococcus,fusobacterium,

bacteroides. Moderately active against

toxoplasama,P.falciparum,pneumocystis.

MOA

Lincosamide exert bacteriostatic action associated with inhibiting protien synthesis.

In high concentration lincosamides may exert bactericidal action.

Lincosamides prevent bacteria replicating by interfering with the synthesis of proteins. They bind to the 23s portion of the 50S subunit of bacterial ribosomes and cause premature dissociation of the peptidyl-tRNA from the ribosome.Lincosamides do not interfere with protein synthesis in human cells because our ribosomes are structurally different from those of bacteria.

Indications

Streptococcal tonsillopharyngitis Infection of lower respiratory tract Skin and soft tissue infections including diabetic foot Bone and joint infections Intra-abdominal infections Pelvic infections Toxoplasmosis Bacterial vaginosis Severe Acne

Clindamycin

Clindamycin is a lincosamide antibiotic Clindamycin is a semisynthetic antibiotic produced by a 7(S)-

chloro-substitution of 7(R)-hydroxyl group of the parent compound lincomycin.

It has primary bacteriostatic action against and a wide range of anaerobic bacteria

Spectrum of activity

Aerobic gram-positive cocci:staphylococcus aureus and s.epidermis both pencillin and nono-penicillinase producing

strains,streptococci except E.feacalis Anaerobic gram-negative: Bacteroides spacies Fusobacterium Anaerobic and microaerophillic gram-positive cocci. Clostridia

MOA

Clindamycin inhibit protein synthesis by revesibly binding to 50s subunits of the ribosomal thus blocking the transpeptidation or translocation reactions of susceptible organisms resulting to stunted cell growth.

CLINICAL PHARMACOLOGY

Biologically inactive clindamycin phosphate is rapidly converted to active clindamycin.

By the end of short-term intravenous infusion, peak serum levels of active clindamycin are reached.

Biologically inactive clindamycin phosphate disappears rapidly from the serum, the average elimination half-life is 6 minutes

CLINICAL PHARMACOLOGY

The serum elimination half-life of active clindamycin is about 3 hours in adults and 2½ hours in pediatric patients.

Serum levels of clindamycin can be maintained above the in vitro minimum inhibitory concentrations for most indicated organisms by administration of clindamycin phosphate every 8 to 12 hours in adults and every 6 to 8 hours in pediatric patients, or by continuous intravenous infusion.

CLINICAL PHARMACOLOGY

An equilibrium state is reached by the third dose. The elimination half-life of clindamycin is increased slightly in

patients with markedly reduced renal or hepatic function. Hemodialysis and peritoneal dialysis are not effective in

removing clindamycin from serum. Dosage schedules need not be modified in the presence of mild to moderate renal or hepatic disease.

IndicationsClindamycin is indicated in the treatment of serious

infections caused by susceptible anaerobic bacteria,streptococci,pneumococciandstaphylococci.

Clindamycin is used chiefly in the treatment of serious anaerobic infections.

Bacteroides flagilis or susceptible strains of gram positive bacteria:

Lower respiratory tract infections including bronchitis, pneumonia, emphysema and lung abscess.

UTI Septicemia caused by Staphylococcus aureus, Streptococci

(except Enterococcus faecalis), and susceptible anaerobes.

LRTI

LRTI : Lower respiratory tract infections including bronchitis, pneumonia, emphysema and lung abscess

Bronchitis is inflammation of the mucous membranes of the bronchiPneumonia is an inflammatory condition of the lung—especially affecting

the microscopic air sacs (alveoli)—associated with fever, chest symptoms Emphysema is a type of chronic obstructive pulmonary disease (COPD)

involving damage to the air sacs (alveoli) in the lungs. As a result, body does not get the oxygen it needs, hard to catch the breath ,chronic cough and trouble breathing.

Abscess is a collection of pus(dead neutrophils) that has accumulated in a cavity formed by the tissue in which the pus resides due to an infectious process

UTI

Urinary tract infection (UTI) is a bacterial infection that affects part of the urinary tract.

When it affects the lower urinary tract it is known as a simple cystitis (a bladder infection)

Symptoms from a lower urinary tract include painful urination and either frequent urination or urge to urinate (or both)

when it affects the upper urinary tract it is known as pyelonephritis(a kidney infection).

pyelonephritis include fever and flank pain in addition to the symptoms of a lower UTI.

The main causal agent of both types is Escherichia coli, however other bacteria, viruses or fungus may rarely be the cause.

Septicemia Septicemia caused by Staphylococcus aureus, Streptococci (except

Enterococcus faecalis), and susceptible anaerobes. Septicemia Septicemia is bacteria in the blood that often occurs with severe

infections.Causes Septicemia is a serious, life-threatening infection that gets worse

very quickly. It can arise from infections throughout the body, including infections in the lungs, abdomen, and urinary tract. It may come before or at the same time as infections of the:

Bone (osteomyelitis) Central nervous system (meningitis) Heart (endocarditis) Other tissues

Dose for childrens

The parenteral dose for clindamycin in children is 20 to 40 mg/kg/day divided and given IV or IM every 6 or 8 hours.

In neonates, the dose should be based on both weight and age, to allow for a slower elimination.

In preterm neonates less than 2 kg, a dose of 10 mg/kg/day should be divided and given every 12 hours.

In neonates over 2 kg and less than 1 week of age, a dose of 15 mg/kg/day should be divided and given every 8 hours.

In older neonates, a dose of 20-30 mg/kg/day may be divided and given every 6 to 8 hours

Adult dose

The recommended adult dose for parenteral clindamycin is 600 to 1,200 mg/day divided and given IV or IM every 12, 8, or 6 hours.

The maximum concentration for IV administration is 18 mg/mL, and the maximum rate of infusion is 30 mg/min

Dose

Clindamycin is diluted prior to IV administration.

Dose Diluent time

300mg 50ml 10min

600mg 50ml 20min

900mg 50ml-100ml 30min

1200mg 100ml 40min

Contraindications

The drug is contraindicated in individuals with a history of hypersensitivity to preparation containing clindamycin or lincomycin

Side Effects

Gastrointestinal: Abdominal pain, nausea, vomiting and diarrhea and esophagitis with oral preparations.

Hypersensitivity Reactions: Maculopapural rash and urticaria have been observed during drug therapy.

Liver: Jaundice and abnormalities in liver function tests have been observed during clindamycin therapy.

Side Effects

Skin and Mucous Membranes: Pruritus, vaginitis and rare instances of exfoliative dermatitis have been observed during clindamycin therapy.

Local Reactions: Pain and abscess have been reported after intramuscular injection and thrombophlebitis after intravenous infusion.

Reaction can be minimized or avoided by giving deep intramuscular injections and avoiding prolonged use of indwelling intravenous catheters.

Musculoskeletal: Rare instances of polyarthritis have been reported.

Precautions

The safety of use in pregnancy has not been established.

Clindamycin has been reported to appear in breast milk.

If therapy is prolonged, liver and renal function tests may be monitored periodically.

May enhance the action of neuromuscular blocking agents.

May counteract the effects of erythromycin.