M.SARIM SHAFIQUEBPD01093173

7th CUNIVERSITY OF LHR.

Macrolides are one of the most commonly used families of antibiotics.

Currently available macrolides are:1.Erythromycin2.Clarithromycin3.Azithromycin4.Telithromycin

First macrolide that is Erythromycin:

In 1952 from products produced

by Streptomyceserythreus.

In 1991 , two semisyntheticderivative of erythromycin were brought into market.

Pharmacology Class:

Protien-Synthesis Inhibitor.

Therapeutic Class:

Anti-Biotic/Anti-Bacterial , Anti-Infective.

Chemical Class:Macrolide

Macrocyclic lactone ring

Lactone

Chemical Structure:

Chemical Formula: C38H69NO13

Chemical Name: 6-O-methyl erythromycin.

Colour Colourless

Form Crystalline solid

Odor Odorless

Taste Bitter Taste

pH 8.0-10.0

Solubility Insoluble in water and slightly soluble in ethanol , methanol.

Molecular weight

748 [g/mole]

Gram-positive aerobic bacteria (Staphylococcus aureus,S. pneumoniae, and S.pyogenes,Listeriamonocytogens)

Gram-negative aerobic bacteria (Haemophilus influenzae, H. parainfluenzae, and Moraxellacatarrhalis,Neisseriagonorrhea)

Some Anaerobic bacteria

Some Mycobacteria(Mycobacterium avium and others)

Some other microrganismsincluding : Mycoplasma, Ureaplasma, Chlamydia and Toxoplasma.

Halicobacter(H.pylori)

Has spectrum of activity against:

Clarithromycin is usually bacteriostatic, but may be bactericidal depending on the organism and the drug concentration.

Steps for Bacterial Protien Synthesis:

1. Activation of Amino Acids:The amino acid AMP enzyme

complex is called an activated amino acid.

2. Charging of tRNA:Amino acid AMP Enzyme complex + tRNA

3. Activatin Of Ribosomes. The smaller and the larger subunits of

ribosome are joined together.

4. Assembly of Amino Acids.

5. Initiation of Polypeptide Chain.

6. Elongation of Polypeptide Chain.

7. Termination & Release of Polypeptide Chain.

Oral , I.V .....

Almost complete Oral absorption occurs.

Clarithromycin is widely distributed through out the body (volume of distribution approximately 250L after a 250mg oral dose).

2.9-9.2 Hours.

80%

The absolute bioavailability of clarithromucin in itself after

oral administration is approximately 55%.

As renal function declines , half life increase to 7.7 hr.At a CrCl of 30 to 80 ml/minHalf ife increase upto 14hr .. And at less than 30ml/min increases upto 32hrs.

A significant fraction dose of clarithromycin is metabolized through liver.

14-hydroxy-6-O-methylerythromycin (half-

life 5.8h).

Eliminated both by renal excretion(37%) and

hepatic metabolism(60%).

1.Upper Respiratory tract Infection

2.Lower Respiratory tract Infection

3.Skin and soft tissue Infections

4.Mycobacterium avium infections.

5.Gastric and Doudenal Ulcers.

6.Eradication of H.pylori.

Causative Agent: S.pyogenes

Causative Agent: S.pyogenes

CausativeAgents:

Streptococcus pneumoniae , Haemophilus influenzaeand Moraxella catarrhalis .

Causative Agents:In Children-S.pneumoniae and P.aeruginosa.In older adolescents and young adults-H.Influenza,

.

Bacteria are uncommon pathoges but may inlude:Mycoplasma pneumoniae , Chlamydophila pneumoniae, Streptococcus pneumoniae and H.influenzae.

Causative Agents:

50% Streptococcus pnemoniae

20% H.influenza

13% Chlamydophilapneumoniae.

Causative Agents: Normal skin floraor exogenous bateria.Skin Flora i.e . S.pyogens & S.aureus.

Causative Agent: S.pyogens

Occuring in AIDS and immunocompromised patients .

Causative Agents:70-90% linked with the H.pylori.

Inhibition of CYP3A4 by the use of Clarithromycin:Alprazolam , Carbamazepine , Cyclosporin , Ergot alkaloids , Lovastatin , Methylprednisolone , Midazolam , Omeprazole , Oral Anticoagulants(e.g Warfarrin) , Quinidine , Sildenafil , Simvastatin , Terfinadine , Vinblastine.

Inhibition of Pgp:Digoxin , Colchicine.

Inducers of CYP3A4 :Rifabutin , Rifampicin , Rifapentine , Nevirapine.

Bi-Directional Drug Interactions:Itrconazole , Atazanavir , Saquanivir.

QT prolongation:Concomitant use of Clarithromycin with Cimetidine , Fluxotine , Foods like grapefruit.

Phenytoin And Valporate:

Grape fruit juice may delay the GIT absorption of clarithromycin.

COLITISRENAL IMPAIRMENTMYASTHENIA GRAVIS

Renal ImpairmentHepatic ImpairmentPregnancyLactation

Phlebitis at injection site.

A: Pyschiatric Disorder: Insomnia B:Nervous system Disorder: Dysgeusia , Headache , Taste Perversion.C: Vascular Disorder: Vasodilation.D: GIT Disorders: Diarrhea , Vomiting , Dyspepsia , Nausea , Abdominal pain.E:Hepatobiliary Disorders: Lft’s Abnormal.F:Skin and Subcutaneous tissue Disorders: Rash , Hyperhidrosis.G:Administration site Condition:Injection site pain , Injection site Inflammation.

Is Contraindiacated in patients who have known hypersenstivity to macrolides antibiotics.Certain Heart problems like Qt prolongation.Electrolyte Imbalance e.g low potassium or sodium level.

In renal impaired patient in which CrCl level is less than 30ml/min, the dosage of clarithromycin should reduce by one-half i.e250 mg once daily or 250mg twice daily in severe infections.

Pregnancy category C .

Klaricid

Generic Name:Clarithromycin

Manufacturer:Abbott

Dosage form:Granules,IVinfusion,Tablets.

Clacin

Generic Name:Clarithromycin

Manufecturer:Werrick

Dosage Form:Susp, Tablets.

Claritek

Generic Name: Clarithromycin

Manufecturer : Getz Pharma

Dosage form: Granules,Drops,

Tablets.

Clatz

Generic Name :Clarithromycin

Manufecturer: Glitz Pharma

Dosage form : Suspension,

Tablets.

1.For Classification and

Spectrum & Mechanism:

2.For Bacterial Protien

Synthesis:

3.For Clinical Indications:

4.For Dosages:

Also Leaflet of Klaricid prepared by AbottLabortaries.