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Chloramphenicol | apollo +9191 46 950 950
Chloramphenicol | apollo +9191 46 950 950
Chloramphenicol
CAS Number : 56-75-7
Molecular Formula : C11H12Cl2N2O5
Molecular Weight : 323.129 g/mol
Systematic (IUPAC) : 2,2-dichloro-N-[(1R,2R)-1,3-dihydroxy-1-(4-nitrophenyl)propan-2-yl]acetamide
Type : small molecule
Description : An antibiotic first isolated from cultures of Streptomyces venequelae in 1947 but now produced synthetically. It has a relatively simple structure and was the first broad-spectrum antibiotic to be discovered. It
acts by interfering with bacterial protein synthesis and is mainly bacteriostatic. (From Martindale, The Extra
Pharmacopoeia, 29th ed, p106)
Categories
Anti-Bacterial Agents
Protein Synthesis Inhibitors
Pharmacology
Indication : Used in treatment of cholera, as it destroys
the vibrios and decreases the diarrhea. It is effective against tetracycline-resistant vibrios. It is also used in eye drops or ointment to treat bacterial conjunctivitis.
Pharmacodynamics : Chloramphenicol is a broad-
spectrum antibiotic that was derived from the bacterium Streptomyces venezuelae and is now produced
synthetically. Chloramphenicol is effective against a wide variety of microorganisms, but due to serious side-
effects (e.g., damage to the bone marrow, including aplastic anemia) in humans, it is usually reserved for the treatment of serious and life-threatening infections (e.g., typhoid fever). Chloramphenicol is bacteriostatic but
may be bactericidal in high concentrations or when used against highly susceptible organisms. Chloramphenicol
stops bacterial growth by binding to the bacterial
ribosome (blocking peptidyl transferase) and inhibiting protein synthesis.
Mechanism of action : Chloramphenicol is lipid-
soluble, allowing it to diffuse through the bacterial cell membrane. It then reversibly binds to the L16 protein of the 50S subunit of bacterial ribosomes, where transfer of
amino acids to growing peptide chains is prevented (perhaps by suppression of peptidyl transferase activity), thus inhibiting peptide bond formation and subsequent
protein synthesis.
Absorption : Rapidly and completely absorbed from gastrointestinal tract following oral administration (bioavailability 80%). Well absorbed following
intramuscular administration (bioavailability 70%). Intraocular and some systemic absorption also occurs
after topical application to the eye.
Protein binding : Plasma protein binding is 50-60%
in adults and 32% is premature neonates.
Metabolism : Hepatic, with 90% conjugated to inactive
glucuronide.
Half life : Half-life in adults with normal hepatic and renal function is 1.5 - 3.5 hours. In patients with impaired renal function half-life is 3 - 4 hours. In
patients with severely impaired hepatic function half-life is 4.6 - 11.6 hours. Half-life in children 1 month to 16
years old is 3 - 6.5 hours, while half-life in infants 1 to 2 days old is 24 hours or longer and is highly variable,
especially in low birth-weight infants.
Toxicity : Oral, mouse: LD50 = 1500 mg/kg; Oral, rat: LD50 = 2500 mg/kg. Toxic reactions including fatalities have occurred in the premature and newborn; the signs and symptoms associated with these reactions have been referred to as the gray syndrome. Symptoms include (in
order of appearance) abdominal distension with or without emesis, progressive pallid cyanosis, vasomotor
collapse frequently accompanied by irregular respiration, and death within a few hours of onset of
these symptoms.
Affected organisms : Enteric bacteria and other
eubacteria
General Descriptions And Applications
Chloramphenicol is a relatively simple structure broad-spectrum antibiotic which is effective against rickettsiae, gram-positive and gram-negative bacteria, and certain
spirochetes by inhibiting translation on the 50S ribosomal subunit at the peptidyltransferase step
(elongation inhibition). It was originally isolated from a species of streptomyces bacteria and other spirochetes
later, but is produced synthetically. Because of its toxicity and side-effect, it should only be used for serious infections in which other medicines do not work; should not be used for colds, flu, other virus infections, sore
throats or other minor infections, or to prevent infections. It is used especially in the treatment of
typhus and other rickettsial infections and in typhoid, shigellosis, and related enteric diseases.
Chloramphenicol is used in biological research of protein synthesis. It is a greenish white or yellowish white needle-like solid; slightly soluble in water and
ether; soluble in alcohol; melting point 148-150 C. Its chemical designation is D(-)-threo-2,2-Dichloro-N-[beta-hydroxy-alpha-(hydroxymethyl)- beta-(4-nitrophenyl)ethyl] acetamide or D-(-)-threo-1-(p-
nitrophenyl)-2-dichloro acetamido-1,3-propanediol.
Chloramphenicol palmitate: the palmitic ester of chloramphenicol, administered orally.
Chloramphenicol sodium succinate: the sodium succinate derivative of chloramphenicol, administered
intravenously.
Thiamphenicol: a methylsulfonyl analog of chloramphenicol
Florfenicol: a fluorinated analog of thiamphenicol
Why is this medication prescribed?
Chloramphenicol injection is used to treat certain types of serious infections caused by bacteria when other
antibiotics cannot be used. Chloramphenicol injection is in a class of medications called antibiotics. It works by stopping the growth of bacteria. Antibiotics will not
work for colds, flu, or other viral infections.
How should this medicine be used?
Chloramphenicol injection comes as a liquid to be injected into a vein by a doctor or nurse in a hospital. It
is usually given every 6 hours. The length of your treatment depends on the type of infection being
treated. After your condition improves, your doctor may switch you to another antibiotic that you can take by
mouth to complete your treatment.
You should begin to feel better during the first few days of treatment with chloramphenicol injection. If your
symptoms do not improve or get worse, tell your doctor.
Use chloramphenicol injection for as long as your doctor tells you, even if you feel better. If you stop using
chloramphenicol injection too soon or skip doses, your infection may not be completely treated and the bacteria
may become resistant to antibiotics.
Other uses for this medicine
In the event of biological warfare, chloramphenicol injection may be used to treat and prevent dangerous illnesses that are deliberately spread such as plague, tularemia, and anthrax of the skin or mouth. Talk to
your doctor about the risks of using this medication for your condition.
This medication may be prescribed for other uses; ask your doctor or pharmacist for more information.
What special precautions should I follow?
Before receiving chloramphenicol injection,
tell your doctor and pharmacist if you are allergic to chloramphenicol injection or any other medications.
tell your doctor and pharmacist what other prescription and nonprescription medications, vitamins, nutritional supplements, and herbal products you are taking or plan
to take. Be sure to mention any of the following: anticoagulants (''blood thinners'') such as warfarin (Coumadin); aztreonam (Azactam); cephalosporin
antibiotics such as cefoperazone (Cefobid), cefotaxime (Claforan), ceftazidime (Fortaz, Tazicef), and ceftriaxone (Rocephin); cyanocobalamin (vitamin B12); folic acid; iron supplements; certain oral medications for diabetes such as chlorpropamide (Diabinese) and tolbutamide;
phenobarbital; phenytoin (Dilantin, Phenytek); rifampin (Rimactane, Rifadin); and medications that may cause a
decrease in the number of blood cells in the body. Ask your doctor or pharmacist if any of the medications that you are taking may cause a decrease in the number of
blood cells. Your doctor may need to change the doses of your medications or monitor you carefully for side effects. Other medications may also interact with
chloramphenicol injection, so be sure to tell your doctor about all the medications you are taking, even those that
do not appear on this list.
tell your doctor if you have ever been treated with chloramphenicol injection before, especially if you
experienced severe side effects. Your doctor may tell you not to use chloramphenicol injection.
tell your doctor if you have or have ever had kidney or liver disease.
tell your doctor if you are pregnant, plan to become pregnant, or are breast-feeding. If you become pregnant while receiving chloramphenicol injection, call your
doctor.
if you are having surgery, including dental surgery, tell the doctor or dentist that you are receiving
chloramphenicol injection.
What special dietary instructions should I
follow?
Unless your doctor tells you otherwise, continue your normal diet.
What side effects can this medication cause?
Chloramphenicol injection may cause side effects. Tell your doctor if any of these symptoms are severe or do
not go away:
nausea
vomiting
diarrhea
tongue or mouth sores
headache
depression
confusion
Some side effects can be serious. If you experience any of these symptoms or those listed in the IMPORTANT WARNING section, call your doctor immediately:
hives
rash
itching
swelling of the face, throat, tongue, lips, eyes, hands, feet, ankles, or lower legs
hoarseness
difficulty swallowing or breathing
watery or bloody stools (up to 2 months after your treatment)
stomach cramps
muscle aches or weakness
sweating
feelings of numbness, pain, or tingling in an arm or leg
sudden changes in vision
pain with eye movement
Chloramphenicol injection may cause a condition called gray syndrome in premature and newborn infants. There have also been reports of gray syndrome in children up to age 2 and in newborns whose mothers were treated
with chloramphenicol injection during labor. Symptoms, which usually occur after 3 to 4 days of treatment, may include: stomach bloating, vomiting, blue lips and skin due to lack of oxygen in the blood, low blood pressure,
difficulty breathing, and death. If treatment is stopped at the first sign of any symptoms, the symptoms may go
away, and the infant may recover completely. Talk to your doctor about the risks of using this medication during labor or to treat babies and young children.
Chloramphenicol injection may cause other side effects. Call your doctor if you have any unusual problems while
receiving this medication.
What other information should I know?
Ask your doctor any questions you have about chloramphenicol injection. If you still have symptoms of infection after you finish the chloramphenicol injection,
talk to your doctor.
It is important for you to keep a written list of all of the prescription and nonprescription (over-the-counter) medicines you are taking, as well as any products such
as vitamins, minerals, or other dietary supplements. You should bring this list with you each time you visit a doctor or if you are admitted to a hospital. It is also important information to carry with you in case of
emergencies.
Uses
Chloramphenicol is an antibiotic used to treat a variety of bacterial infections.
How To Use?
This medication is best taken on an empty stomach 1 hour before or 2 hours after meals. It may be taken with
food or milk if stomach upset occurs. The liquid suspension form of this medicine must be shaken well
before using. Store in the refrigerator. Check the expiration date and discard any unused portion after 14 days because the drug loses potency. Antibiotics work
best when the amount of medicine in your body is kept at a constant level. Do this by taking the medication at evenly spaced intervals throughout the day and night.
Continue to take this medication until the full prescribed amount is finished even if symptoms disappear after a few days. Stopping the medication too early may allow bacteria to continue to grow resulting in a relapse of the
infection.
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