Chloramphenicol

Drug #158

Chloramphenicol was first isolated in 1947 from the cultures of Streptomyces venezuelae. Chloramphenicol was synthesized in 1949, becoming the first completely synthetic antibiotic of importance to be produced commercially. Chloramphenicol is a broad spectrum antibiotic. Chloramphenicol is a nitrobenzene derivative. Chloramphenicol is primarily bacteriostatic and may be bacteriocidal to some strains. Chloramphenicol is active against both aerobic and anaerobic gram positive and gram negative organisms, rickettsiae and certain spirochetes. Adminitered orally or applied topically. Antibiotics require constant drug level in body for therapeutic effect. This is achieved by taking the drug at regular interval of time throughout the day and night as prescribed. Chloramphenicol is important to take the drug for the full time period as prescribed. If you discontinue the drug Chloramphenicol may result in ineffective treatment.

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Primary Characteristics

Chloramphenicol is also known as Chloramphenicol Palmitat.

It is of Semi Synthetic origin and belongs to Nitrophyenyl acetamide.

It belongs to Peptidyl transferase inhibitor pharmacological group on the basis of mechanism of action and also classified in Antibiotics pharmacological group.

Molecular Weight: 323.1 · pK_a: 5.5 · Solubility in Water: 1 in 400 · Solubility in Alcohol: 1 in 2.5 · Non-proprietary name: Chloramphenicol · pH: 6.1 · Isotonic value: 6.83.

Pharmacokinetics

Absorption: Chloramphenicol has an oral bioavailability is 85% (±5%), pre-systemic (first-pass) metabolism accounts for 25% (±5%).

Distribution: Chloramphenicol has a volume of distribution is 0.25-1.99 l/kg. plasma protein binding is ~53%.

Elimination: it is metabolised via Hepatic, plasma half-life is 1.7-12 hr, renal excretion is 5-15% (unchanged) , less than 3% in bile.

Indications

Chloramphenicol is primarily indicated in conditions like Acromegaly, Acute epiglottitis, Anaerobic infections, Bacterial infections, Blepharitis, Brain abscesses, Brucellosis, Cellulitis, Corneal ulcers, Intraocular infections, Iron deficiency anaemia, Keratoconjuctivitis sicca, Life threatning infections, Meningitis, Peritonitis, Plague, Psittacosis, Q Fever, Septicaemia, Spotted fever, Tularemia, Typhoid.

Chloramphenicol is also indicated for secondary conditions like Enteritis, Gangrene, Haemophilia, Influenza, Whipple's disease.

Contraindications

Chloramphenicol is contraindicated in conditions like Hypersensitivity.

Dosage

Chloramphenicol's dosage details are as follows:

Dose	Single Dose	Frequency	Route	Instructions
Adult Dosage
0.5 %w/v	0.5 %w/v	Every 12h	Ophthalmic	1-2 drops 4-6 times a day for first 72 hours.Treatment should be continued for approx 7days.
1 %w/w	1 %w/w	Every 6h	Ophthalmic	Frequency may be increased to 8 times if needed.
5 – 10 %	—	Every 6h	Otic	1-2 drops.
50 – 100 mg/kg	—	Every 6h	PO,IV	Maximum dose: 4 g/day.
Paediatric Dosage (20kg)
18.75 mg/kg	18.75 mg/kg	Every 6h	Intra Venous	-
18.75 mg/kg	18.75 mg/kg	Every 6h	Oral	-
Neonatal Dosage (3kg)
18.75 mg/kg	18.75 mg/kg	Every 6h	Intravenous
18.75 mg/kg	18.75 mg/kg	Every 6h	oral

Drug Interactions

Unknown35 interactions

8 interactions

Major1 interaction

Moderate5 interactions

Always consult your physician for the change of dose regimen or an alternative drug of choice that may strictly be required.

Side Effects

Chloramphenicol in overdosage may give rise to further complications which include Encephalopathy , Pseudomembranous colitis , Urticaria , Thrombocytopenia , Hepatitis , Aplastic anemia , Hemolytic anemia , Aplastic anemia , Hemolytic anemia , Ototoxicity , Peripheral neuropathy , Optic neuritis , Hemolytic reactions , Interstitial nephritis , Hemolytic anemia, Aplastic anemia, Hair growth depression, Physical growth depression.

Chloramphenicol produces potentially life-threatening effects which include Bone marrow suppression, Grey baby syndrome, Anaphylaxis . Careful monitoring is needed with proper medical management.

The signs and symptoms that are produced after acute overdosage of Chloramphenicol are Grey baby syndrome.

Chloramphenicol is known to cause more or less tolerable side effects which are usually transient. These include Confusion, Delirium , Depression, Diarrhea, Glossitis, Headache, Maculopapular rash, Nausea, Pruritus , Salmonella infection, Stomatitis, Transient stinging, Typhoid, Vision disturbances, Vomiting .

Warnings / Precautions

Evaluate blood count after every 2 days during therapy of chloramphenicol. Avoid concurrent therapy with other drugs that may cause bone marrow depression. It should be used with caution in case of liver or kidney disease. Discontinue therapy if secondry infection occurs.

Interference in Pathology

Chloramphenicol may interfere in the diagnosis of Interferes with the determination of total protein & blood urea nitrogen. , Effects the determination of urine sugar, 17-ketosteroids & 17-OH corticosteroids. .

Available Brands

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Single Ingredient

Caps

250 mg 500 mg

Drops

0.3 %w/v 0.5 %w/v 1 %w/v

E and E Drops

0.5 %w/v

Ear Drops

0.5 %w/v 1 %w/v

Eye Drops

0.5 %v/v 0.5 %w/v 1 %w/v

Eye Oint

1 %w/w

Inj

1 g

Oint

0.3 %w/w 0.5 %w/w 1 %w/w

Susp

125 mg/5ml 25 mg/5ml

Tabs

250 mg

Multi-Ingredient Combinations

Drops

Eye Drops

Eye Drops

Eye Oint

Oint

Syrup

Syrup

Storage Conditions

Chloramphenicol should be stored Caps, Oral Susp, Dry Powder for Inj. Cream, Syrup, Eye Ointment, Eye Drops, Ear Soln. Inj (reconstituted soln).

Drug Classification

1.6.2.2.1 — Chloramphenicol
2.21.1.1 — Antibacterials
3.28 — Otic drugs

Manufacturers

Manufacturers of Chloramphenicol in Pakistan: