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PRESENTED BY-SURAIYA AHMEDID# 132 0916 046

A PRESENTATION ON

CEFALOTIN

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INTRODUCTIONSTRUCTURAL CHEMISTRYCHEMICAL & PHYSICAL PROPERTIESDOSE & FREQUENCYDOSAGE FORMINDICATIONSPHARMACOKINETICSM/APHARMACODYNAMICSPHARMACOECONOMICSINTERACTIONSSIDE EFFECTSPRECAUTIONCONTRAINDICATIONINCOMPATIBILITYPACKAGING & STORAGE

OBJECTIVES

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Cefalotin, also called cephalothin, is a semisynthetic first generation cephalosporin antibiotic.

It is administered parenterally (mainly intravenously).

Active against gram-positive organisms but limited activity against gram-negative bacteria.

INTRODUCTION

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IUPAC Name: (6R,7R)-3-(acetyloxymethyl)-8-oxo-7-[(2-thiophen-2-ylacetyl)amino]-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid.

Chemical Names: Cephalothin; Cefalotin; Cefalothin; Cephalotin; Cefalotine; Keflin.

Brand Names: Averon-1® Cemastin® Coaxin® Keflin® Seffin®

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The presence of a beta-lactam moiety makes it susceptible to degradation by some bacterial strains.

The structure of cefalotin has a six-membered ring attached to the four-membered ring.

A β-lactam (beta-lactam) ring is a four-membered lactam. (A lactam is a cyclic amide).

STRUCTURAL CHEMISTRY

β-lactam ring

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o Molecular formula: C16H16N2O6S2

o Molar mass: 396.43804 g/molo Hydrogen Bond Donor Count: 2o Hydrogen Bond Acceptor Count: 8o Melting Point: 160-160.5 °Co Water solubility: 158 mg/Lo pKa: 3.8

Chemical and Physical Properties

StabilitySolutions of cefalotin may darken, especially if stored at room temperature. A slight discoloration does not affect potency. Solutions stored under refrigeration may precipitate, but the precipitate can be redissolved by warming to room temperature with constant agitation.

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Cefalotin is available in the following forms:Injectable Solution ROUTE: IV injection, IM injection

Forms of Medication

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Dose Single Dose Frequency Route Instructions

Adult Dosage

7.142 mg/kg 7.1 (7.142) 6 hourly Slow IV -

Pediatric Dosage ( 20 Kg. )

80 to 160 mg/kg 120 (120) 4 hourly Intra Venous

Up to 12g daily in serve infection.

Neonatal Dosage ( 3 Kg. )

20 mg/kg 20 (20) 8 hourly Intravenous

DOSE & FREQUENCY

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First-generation cephalosporins are mainly active predominantly against Gram-positive bacteria.

Cephalothin is used in the treatment of infections caused by Gram positive organisms like pneumococci, Streptococcus Viridians, Staphylococcus Aureus.

Also active against gram negative organisms like E.coli, Klebsiella pneumoniae and Proteus mirabilis.

INDICATIONS

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• Bone and joint infection• Surgical infections• CVS infections• Genitourinary tract infections• Respiratory tract infections• Soft tissue and skin infections• Cellulitis• Endocarditis• Alternative drug of choice in Peritonitis, Septic

abortion, Surgical prophylaxis.

Cefalotin is used to prevent-

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Absorption: Cefalotin is not well absorbed from GI tract, but it is rapidly absorbed from the site of injection.

Volume of distribution: 0.26 l/kgPlasma protien binding: 65-80%Metabolism: Hepatic.Renal Excretion: >65%Plasma half life: 35 minutes.Toxicity: Rat intravenous LD50 is 4000 mg/kg.

Pharmacokinetics

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The bactericidal activity of cefalotin results from the inhibition of cell wall synthesis via affinity for penicillin-binding proteins (PBPs).

Like penicillin and other cephalosporins, cefalotin works by disrupting the last stage of bacterial cell wall synthesis, leading to autolysis of the bacteria cells by autolytic enzymes such as the autolysins.

Some bacteria gain the ability to produce beta-lactamases, which can degrade the beta-lactam moiety present in penicillins and cephalosporins, and can thus be resistant to those drugs.

M/A OF CEFALOTIN

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Cefalotin or cephalothin is a semisynthetic first generation cephalosporin having a broad spectrum of antibiotic activity that is administered parenterally.

PHARMACODYNAMICS

PHARMACOECONOMICS

•Abraxis pharmaceutical products•Bristol laboratories•Baxter healthcare corporation•Eli lilly and co•Glaxosmithkline

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Drug InteractionsCalcium GluconateDiphenhydramineFrusemide or FurosemidePenicillamineProbenecid (increases the blood level of Cefalotin)Amikacin (Increases the risk of nephrotoxicity)

INTERACTIONS

•Renal Dysfunction•Colitis•Dialysis•Sodium restriction

Disease Interactions

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Local reactions: Swelling, redness, or pain at the injection site may occur.

Hypersensitivity: Hypersensitivity reactions occur in up to 15% of patients with a history of penicillin allergy. Manifestations may include-• Urticarial or maculopapular rash• Bronchospasm• Fever• Anaphylaxis, including severe hypotension and cardiac

arrest

Renal: Nephrotoxicity & Renal insufficiency

SIDE EFFECTS

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Hematologic:thrombocytopenia, hemolytic anemia, and rare cases of pancytopenia.

Gastrointestinal: Diarrhea, nausea and vomiting.

Warning / Precautions

Cephalothin should be used with caution in patients with impaired kidney or liver function, patients with aspirin hypersensitivity, because it may cause allergic reactions (including bronchial asthma).Precaution to be taken during renal disease and in Gastro-intestinal diseases (especially colitis, enteritis)

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Cephalothin is contraindicated in pregnancy, lactation, hypersensitivity and in pseudomembranous colitis.

Drug should not be given to Pediatrics and patients suffering from Kidney dysfunction.

CONTRAINDICATION

Cefalotin and Pregnancy

The FDA categorizes medications based on safety for use during pregnancy. Five categories - A, B, C, D, and X, are used to classify the possible risks to an unborn baby when a medication is taken during pregnancy.

Cefalotin falls into category B

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Adrenaline,amikacin,aminophylline,calcium chloride,calcium gluconate,chlorpromazine,diphenhydramine,erythromycin,gentamicin,hyaluronidase,kanamycin,

INCOMPATIBILITY lignocaine, metoclopramide, oxytocin, penicillin G, phenobarbitone, phenytoin, phytomenadione, prochlorperazine, ranitidine, ticarciliin.

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Sterile cephalothin is available in 10-mL rubber-stoppered vials containing either 1, 2, or 4 g.

Storage ConditionsStore in a well closed container, at room temperature. Protect from Sunlight.

PACKAGING & STORAGE

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http://www.rxwiki.com/cefalotinhttp://www.drugbank.ca/drugs/DB00456http://

www.webmd.com/drugs/2/drug-19324/cephalothin-injection/details#interactions

https://pubchem.ncbi.nlm.nih.gov/compound/cephalothin#section=Formulations-Preparations

http://druginfosys.com/Drug.aspx?drugCode=150&drugName=Cephalothin%20(Na)&type=1

http://www.webhealthcentre.com/drugix/Cephalothin_DI0033.aspx#Interactions

http://en.wikipedia.org/wiki/Cefalotin

RRFERENCES

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THANK YOU!