Amoxicillin Dispersible Tablets

Amoxicillin Dispersible Tablets
Generic name: Amoxicillin Dispersible Tablets
Brand name: Zailin
Composition: (2S,5,R,6,R)-6-[(,R)-(-)-2-amino-2-(p-hydroxyphenyl)acetamido]-3,3-dimethyl-7-oxo-4-thia-
1-azabicyclo[3.2.0]heptane-2-carboxylic acid trihydrate
Chemical structure:
Molecular formula: C16H19N3O5S•3H2O
Molecular weight:419.45
Description:Zailin is a white or almost white tablet.
Strength:0.25gIndications:
Amoxicillin is indicated for the treatment of following infections caused by sensitive bacteria (strains that donot produce β-lactamase):
1 Upper Respiratory Tract Infections, such as otitis media, sinusitis, pharyngitis, tonsillitis, caused by Hemolytic streptococcus, Streptococcus pneumoniae, Staphylococcus, Haemophilus influenzae.
2 Urogenital Tract Infections caused by Escherichia coli, Proteus mirabilis and Enterococcus faecalis.
3 Skin and Soft Tissue Infections caused by Streptococcus hemolyticus, Staphylococcus and Escherichia coli.
4 Lower Respiratory Tract Infection such as acute bronchitis and pneumonia etc. caused by Streptococcushemolyticus, Streptococcus pneumoniae,Staphylococcus aureus, or Haemophilus influenza.
5 Acute simple gonorrhea.
6 The product can be used for the treatment of typhoid fever, carrier of typhoid and leptospirosis. Tripletherapy of amoxicillin, clarithromycin and lansoprazole can eradicate H. pylori in the stomach and duodenumand lower the recurrence rate of peptic ulcer.
Dosage and Administration:This product can be given orally directly, or adding proper amount of water , shake well and then take it.
Foradult:0.5g each time, every 6 to 8 hours, the daily dose shall not exceed 4g For children:the daily dose is20~40mg/kg based on patient weight, 1 time every 8 hours;
Forinfants less than three months:the dailydose is 30mg/kg based on patient weight, 1 time every 12 hours.
Dose adjustment is required in patients with severe renal impairment, for patients with endogenous creatinineclearance rate at 10 ~ 30ml/ minutes, the dose is 25 ~ 0.5g every 12 hours,and for patients with endogenouscreatinine clearance rate less than 10ml/ minutes, the dose is 0.25 ~ 0.5g every 24 hours.Precautions:
Caution is needed when administering amoxycillin to patients with syphilis, as the Jarisch-Herxheimer reaction may occur in these patients.When high doses are administered, adequate fluid intake andurinary output must be maintained.The sodium content must be taken into account in patients on a sodium-restricted diet if the administration of high doses is necessary.Periodic assessment of organ system function,including renal, hepatic and haematopoietic function, isadvisable during prolonged therapy. Since it containsamoxycillin, an aminopenicillin, it is not the treatment of choice in patients presenting with sore throat orpharyngitis because of the possibility that the underlying cause is infectious mononucleosis, in the presenceof which there is a high incidence of rash if amoxycillin is used. It should be given with caution to patients with
lymphatic leukaemia since they are especially susceptible to amoxycillin induced skin rashes.The possibilityof superinfections with mycotic or bacterial pathogens should be kept in mind during therapy. If superinfectionoccur, the agent should be discontinued and/or appropriate therapy instituted.
Impaired hepatic function:
Changes in liver function tests have been observed in some patients receiving 250mg. It should be used withcare in patients with evidence of severe hepatic dysfunction.
Impaired renal function:
In patients with moderate or severe renal impairment 250mg dosage should be adjusted.
(See Dosage and Directions for use).
Use in lactation:
Amoxycillin is excreted in the milk. Therefore, caution should be exercised when it is administered to anursing woman.
The use of may lead to the selection of resistant strains of organisms andsensitivity testing should, thereforebe carried out whenever possible, to demonstrate the appropriateness of therapy.
Pharmacology and toxicology
Pharmacotherapeutic group: penicillins with extended spectrum;Mechanism of action Amoxicillin is a semisynthetic penicillin (beta-lactam antibiotic) thatinhibits one or moreenzymes (often referred to as penicillin-binding proteins, PBPs) in the biosynthetic pathway of bacterialpeptidoglycan, which is an integral structural component of the bacterial cell wall. Inhibition of peptidoglycansynthesis leads to weakening of the cell wall, which is usually followed by cell lysis and death.Amoxicillin issusceptible to degradation by beta-lactamases produced by resistant bacteria and therefore the spectrumof activity of amoxicillin alone does not include organisms which produce these enzymes.
The time above the minimum inhibitory concentration (T>MIC) is considered to be the major determinant ofefficacy for amoxicillin.
Mechanisms of resistance The main mechanisms of resistance to amoxicillin are:
Inactivation by bacterial beta-lactamases.
Alteration of PBPs, which reduce the affinity of the antibacterial agent for the target.
Impermeability of bacteria or efflux pump mechanisms may cause or contribute to bacterial resistance,particularly in Gram-negative bacteria.
Pharmacokinetics:
Absorption:
Amoxycillin is stable in the presence of acidic gastric secretions. Peak blood levels are achieved 1-2hr afteradministration. There is a linear dose response in peak serum levels.
Food does not interfere with the absorption of amoxycillin.
Distribution:
Approximately 18% of the total plasma amoxycillin content is protein bound. Amoxycillin diffuses readily intomost body tissues with the exception of the brain and spinal fluid. Inflammation generally increases thepermeability of themeninges to penicillins and this may apply to amoxycillin.
Excretion:
The elimination half-life is approximately 1hour. Amoxycillin is primarily excreted via the kidneys.
Small amounts of the drug are also excreted in the faeces and bile.
Amoxycillin crosses the placenta and is distributed into breast milk.
SIDE EFFECTS AND SPECIAL PRECAUTIONS:
Skin rashes are the most common side effects and vary from maculopapular to urticarial.
Urticarial reactions are typical of penicillin hypersensitivity reactions.
If serious anaphylactic reaction occurs, Amoxicillin Hexal500 should be discontinued and the patient treatedwith adrenalin, corticosteriods and antihistamines.
Most patients with infectious mononucleosis develop a maculopapular rash, and patients with other lymphoiddisorders seem to be more at risk. Avoid using in these instances.
Gastro-intestinal side effects including diahrroea, nausea and vomiting may occur quite frequently.
Pseudomembranous colitis has also been reported.
Super-infection is relatively common.
Doses should be reduced in severe renal failure.
Use in pregnancy : animal reproduction studies have failed to demonstrate a risk to the foetus. However,there are no adequate and well controlled studies in pregnant women.
Storage:Protect from light, and keep air-tightly.
Packs:Package material: 6Tablet/Blist,2Blists/Box
Shelf-life:36 months