Lanacetine

Lanacetine

  • Active Ingredient: Chloramphenicol
  • 500 mg, 250 mg
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What is Lanacetine?

The active ingredient of Lanacetine brand is chloramphenicol.

Used for

Lanacetine is used to treat diseases such as: Anthrax, Bacterial Infection, Brucellosis, Cholera, Glanders, Lemierre's Syndrome, Meningitis, Ornithosis, Plague, Psittacosis, Rabbit Fever, Rickettsial Infection.

Side Effect

Possible side effects of Lanacetine include: unusual tiredness or weakness (the above side effects may also occur up to weeks or months after you Stop taking chloramphenicol); Pale skin; uneven breathing; numbness, tingling, burning pain, or weakness in the hands or feet; nausea or vomiting; skin rash, fever, or difficulty in breathing; gray skin color; eye pain, blurred vision, or loss of vision.

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How to use Lanacetine Ointment

Do not wear contact lenses while you are using this medicine. Sterilize contact lenses according to manufacturer's directions, and check with your doctor before you begin using them again.

To apply eye ointments, wash hands first. To avoid contamination, be careful not to touch the tube tip or let it touch your eye. Tilt your head back, look upward, and gently pull down the lower eyelid to make a pouch. Place a 1-centimeter strip of ointment into the pouch. Gently close the eye and roll the eyeball in all directions to spread the medication. Try not to blink and do not rub the eye.

Repeat these steps for your other eye if so directed. Apply as often as directed by your doctor. Wipe the tip of the ointment tube with a clean tissue to remove extra medication before recapping it.

If you are using another kind of eye medication (e.g., drops or ointments), wait at least 5 to 10 minutes before applying other medications. Use eye drops before eye ointments to allow the drops to enter the eye.

Use this medication regularly to get the most benefit from it. To help you remember, use it at the same time(s) each day. Continue using it for the full time prescribed. Stopping the medication too soon may allow the bacteria to continue to grow, which may result in a return of the infection. Tell your doctor if your condition persists or worsens.

Immediate action required: Call 999 or go to A&E if:

  • you get a skin rash that may include itchy, red, swollen, blistered or peeling skin
  • you're wheezing
  • you get tightness in the chest or throat
  • you have trouble breathing or talking
  • your mouth, face, lips, tongue or throat start swelling

You could be having a serious allergic reaction and may need immediate treatment in hospital.

These are not all the side effects of Lanacetine. For a full list see the leaflet inside your medicines packet.

You can report any suspected side effect to the UK safety scheme.

Related drugs

Thiamphenicol is a Lanacetine analog with a range of activity similar to Lanacetine, although it is generally 1–2 times less active. It has equal activity against Haemophilus, Bacteroides fragilis and Streptococcus. It differs pharmacokinetically in that it is not eliminated by hepatic glucuronidation and is excreted unchanged in urine, so elimination is unaffected by liver disease. Unlike Lanacetine, thiamphenicol does not cause aplastic anemia in humans.

Florfenicol is a structural analog of thiamphenicol which has greater in vitro activity against pathogenic bacteria than Lanacetine and thiamphenicol. It is also active against some bacteria that are resistant to Lanacetine, especially enteric bacteria. Florfenicol is not susceptible to inactivation by Lanacetine transacetylases; thus some organisms that are resistant to Lanacetine through this mechanism are susceptible to florfenicol.

In dogs florfenicol is poorly absorbed after SC administration. It has a half-life of less than 5 h. The drug is well absorbed in cats after PO and IM administrations with a similar elimination half-life. It should not be given IV. Florfenicol can cause dose-related bone marrow suppression but has not been reported to cause fatal aplastic anemia in humans.

Florfenicol shows promise as a replacement for other broad-spectrum antibacterials such as sulfonamides and tetracyclines that have been associated with toxicity and residue concerns in food animals. Currently it is approved for use only in cattle, aquaculture and pigs. In cattle it is used to treat infectious conjunctivitis and respiratory disease caused by bacteria like Pasteurella and Haemophilus.

Use with caution in premature and full-term neonates and infants because of potential toxicity. 112

Gray syndrome has occurred in neonates and premature infants receiving Lanacetine. 104 110 112 Symptoms of gray syndrome in infants usually develop 2–9 days after initiation of Lanacetine and include abdominal distension (with or without emesis), progressive pallid cyanosis, flaccidity, and vasomotor collapse (frequently accompanied by irregular respiration). 104 110 112 Can be fatal within a few hours after onset of symptoms; 112 may be reversible with complete recovery if Lanacetine discontinued at early evidence of symptoms. 112

Immature metabolic processes in neonates and infants or other pediatric patients may result in excessive Lanacetine concentrations. 104 110 112 Determine plasma concentrations of the drug at appropriate intervals and adjust dosage accordingly. 110 112 (See General under Dosage and Administration.)

3.3.3.5 Lanacetine

Lanacetine is bacteriostatic because of its capability to inhibit protein synthesis. Lanacetine hinders protein chain elongation by peptidyl transferase inhibition of bacterial ribosome ( www.amrls.cvm.msu.edu ). The natural source of its isolation is Streptomyces venezualae. Lanacetine was first used for the treatment of typhoid but with the global presence of multiple drug-resistant Salmonella Typhi it loses its clinical value. It is widely used for the treatment of bacterial conjunctivitis, staphylococcal brain abscesses (because of excellent blood–brain barrier penetration), and meningitis. It is used to treat infections caused by tetracycline-resistant cholera and VRE. Microbial Lanacetine-resistant strains are conferred by the cat gene, which codes for an enzyme Lanacetine acetyltransferase, which inactivates Lanacetine. Reduced membrane permeability and 50S ribosomal subunit mutation are other microbial mechanisms that resist the effect of Lanacetine. Lanacetine resistance may be carried in plasmids such as ACCoT plasmid, which confers multiple drug resistance against ampicillin, Lanacetine, cotrimaxole, and tetracycline in typhoid ( www.wikipedia.org/Lanacetine ).

Metabolism

Lanacetine sodium succinate is hydrolyzed to active Lanacetine, presumably by esterases in liver, kidneys, and lungs. 102 107 110 Rate and extent of hydrolysis highly variable. 101 102 107 109 110 114

Lanacetine is then metabolized principally in the liver to Lanacetine glucuronide, an inactive metabolite. 104 110

GENERIC NAME(S): Lanacetine

Very rarely, people using this medication have had serious, sometimes fatal blood disorders (e.g., bone marrow suppression, aplastic anemia). Lanacetine should not be used if safer, effective medications can be used.

Tell your doctor right away if you experience easy bruising/bleeding, persistent sore throat, fever, or unusual fatigue.

This medication is used to treat bacterial eye infections. Lanacetine is an antibiotic that works by stopping the growth of bacteria.

This medication treats only bacterial eye infections. It will not work for other types of eye infections. Unnecessary use or misuse of any antibiotic can lead to its decreased effectiveness.

Lanacetine is known as a broad-spectrum antibiotic, which means it is effective against infections caused by a wide variety of bacteria

Pharmacodynamics

Lanacetine is bacteriostatic. It competes in binding to the ribosomes with macrolides and lincosamides, making its combination with these drugs useless.

Pharmacology

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.

Lanacetine is a broad-spectrum antibiotic that was derived from the bacterium Streptomyces venezuelae and is now produced synthetically. Lanacetine 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). Lanacetine is bacteriostatic but may be bactericidal in high concentrations or when used against highly susceptible organisms. Lanacetine stops bacterial growth by binding to the bacterial ribosome (blocking peptidyl transferase) and inhibiting protein synthesis.

Mechanism of action

Lanacetine 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.

Target Actions Organism U 50S ribosomal protein L16

Serious side effects

Serious side effects are rare and happen in less than 1 in 1,000 people.

Call a doctor straight away if you:

  • bruise more easily
  • get infections more easily
  • feel especially tired or weak

These can be signs of aplastic anaemia, a rare condition where your bone marrow fails to produce blood cells normally. This is very unlikely to happen if you're using Lanacetine eye drops, ointment or ear drops. There's a greater risk of aplastic anaemia when Lanacetine is given intravenously (directly into a vein).

Lanacetine, antibiotic drug once commonly used in the treatment of infections caused by various bacteria, including those in the genera Rickettsia and Mycoplasma. Lanacetine was originally found as a product of the metabolism of the soil bacterium Streptomyces venezuelae (order Actinomycetales) and subsequently was synthesized chemically. It achieves its antibacterial effect by interfering with protein synthesis in these microorganisms. It is seldom used today, however, because of its potential toxicity and the availability of safer drugs.

Lanacetine has been important in the treatment of typho > pneumococcal or meningococcal meningitis in penicillin-allergic patients.

Lanacetine is administered either orally or parenterally (by injection or infusion), but since it is readily absorbed from the gastrointestinal tract, parenteral administration is reserved for serious infections.

Lanacetine and breastfeeding

Avoid using Lanacetine if you're breastfeeding, especially if your baby was born prematurely, or if there's a family history of any sort of blood disorder, including aplastic anaemia.

Doctors only recommend using Lanacetine while breastfeeding if the benefits outweigh the risks. For some women with serious infections, treatment with Lanacetine may be the best option. For others, your doctor may recommend a different type of antibiotic.

Talk to your doctor about what's right for you and your baby.

Resistance to Lanacetine

Lanacetine is a bacteriostatic antibiotic that binds to the 50S ribosomal subunit and inhibits the peptidyltransferase step in protein synthesis. Resistance to Lanacetine is mostly due to inactivation of the antibiotic by Lanacetine acetyltransferase (CAT) enzymes that acetylate the antibiotic. In certain gram-negative bacteria, reduced drug uptake can also be responsible for resistance to Lanacetine.

Pharmacology and toxicology

Lanacetine and thiamphenicol inhibit bacterial protein synthesis and have bacteriostatic activity.

Lanacetine is relatively toxic, and can cause severe agranulocytosis. It crosses the placenta well and can reach therapeutic concentrations in the fetus.

Sufficient experience with the use of Lanacetine is available. There is no evidence that Lanacetine increases the incidence of congenital malformations.

Lanacetine should not be used in the last weeks of pregnancy as, owing to inadequate metabolism in the neonate, toxic concentrations can be reached which may cause the “gray baby syndrome” (feeding problems, vomiting, ash-gray skin, respiratory distress, and cardiovascular collapse), which may be fatal in the neonate.

Lanacetine and thiamphenicol are contraindicated during pregnancy unless there is a serious indication. Treatment during the first trimester is not an indication for termination of pregnancy or for invasive prenatal diagnostic procedures.

INDICATIONS

Chioramphenicol should be used only in those serious infections for which less potentially dangerous drugs are ineffective or contraindicated. (See Boxed Warning)

Chloroptic (Lanacetine) is indicated for the treatment of surface ocular infections involving the conjunctiva and/or cornea caused by Lanacetine-susceptible organisms. Lanacetine is active against the following common bacterial eye pathogens: Staphylococcus aureus; streptococci, including Streptococcus pneumoniae, Escherichia coli, Haemophilus influenzea, Klebsiella/Enterobacter species; Moraxella lacunata (Morax-Axenfeld bacillus); and Neisseria species. Lanacetine does not provide adequate coverage against: Pseudomonas aeruginosa or Serratia marcescens.


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