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Showing posts with the label PHARMACOLGY

How Amoxicillin -Clavulanic Acid Overcomes Beta Lactamase Resistance

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                              AMOXICILLIN  Amoxicillin is a broad spectrum antibiotic beta lactam antibiotic, but its susceptible to degradation by beta lactamase enzymes produced by certain bacteria . Its susceptible to degradation by beta lactamase producing bacteria. They are resistant to broad spectrum beta lactam antibiotics  Amoxicillin is combined with clavulanic acid which is beta lactamase inhibitor  Clavulanic acid binds to beta lactamase -clavulanic acid get inactivated known as suicide inhibitor MECHANISM OF ACTION : Amoxillicin gets degraded easily by attack of bacteria thus resulting in its breakdown ,where as when amoxicillin gets combined with clavulanic acid ,it doesn't get degraded easily thereby aid in destroying the bacterial pathogens .

Beta lactam breakthroughs: From Penicillin to Superbugs

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                    BETA LACTUM ANTIBIOTICS PENICILLIN CATEGORY: Beta lactam antibiotics  FOUND BY: Alexander flaming  FOUND IN: Fungus penicillium notatum ,but commercially penicillium chrysogenum PROTOTYPE: Benzyl penicillin STRUCTURE: Beta lactam ,thiazolidine ring  PROPERTIES:  Highly water soluble More stable in salt form Stable in dry state Thermolabile Acid labile  MECHANISM OF ACTION : Bacterial action by inhibiting synthesis of cell wall In peptidoglycan :glycan chain consist of altering amino sugar  Penicillin-bind and inactivate penicillin binding protein Inhibit transpeptidase  Prevent peptidoglycan synthesis Cell wall deficient form develop autolysis and there by causing cell death 

CEPHALOSPORIN MECHANISM OF ACTION ( PART-2)

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                  CEPHALOSPORIN ANTIBACTERIAL SPECTRUM: GRAM POSITIVE BACTERIA : Streptococcus pyogens  Viridan streptococci Staphylococcus aureus  Streptococcus pneumonia  GRAM NEGATIVE BACTERIA: E.coli Klebsiella Pneumonia Proteus MECHANISM OF ACTION : IN GRAM POSITIVE BACTERIA - Cephalosporin penetrate peptidoglycan layer bind to penicillin binding protein blocking its activity there by causing damage to peptidoglycan synthesis  IN GRAM NEGATIVE BACTERIA- Enter through outer membrane bind to penicillin binding protein and damage peptidoglycan synthesis  some may release beta lactamase that bind to cephalosporin which inhibit its function but clavulanic acid and cephalosporin  thereby binds the bacteria and thus enabling bacterial action  SECOND GENERATION: CEFUROXIME- Resistant to gram negative beta lactamase Active against -ampicillin resistant H.Influenza Well tolerated in intramuscular action THIRD GEN...

CEPHALOSPORIN CLASSIFICATION (part-1)PHARMACOLOGY MADE EASY

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                  CEPHALOSPORIN: INTRODUCTION: Semi synthetic antibiotic  Derived :CEPHALOSPORIN -C Chemically related to penicillin Divided into four generation based on: Chronological sequence  Antibacterial spectrum It has bactericidal action MECHANISM OF ACTION: Inhibits cell wall synthesis CLASSIFICATION: FIRST GENERATION: CEFAZOLIN,CEPHALEXIN SECOND GENERATION: ORAL -CEFACLOR PARENTRAL-CEFUROXIME THIRD GENERATION: CEFOTAXIME,CEFTIZOXIME FOURTH GENERATION: CEFEPIME,CEFPIROME  CLASSIFICATION: FIRST GENERATION: CEFa zolin CEPHA loridine CEPHA lothin CEPHA radine CEPHA lexin CEPHA droxil SECOND GENERATION: CEF oxitin CEF aclor CEF uroxime THIRD GENERATION: CEF triaxone CEF otoxamine Cef tazidime FOURTH GENERATION: CEF ipime CEF ipirome FIFTH GENERATION  CEF taroline

ORAL REHYDRATION SOLUTION (ORS) old and new formulation along with its uses

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  ORAL REHYDRATION SOLUTION  Oral rehydration solution is given in oral rehydration therapy of mild to moderate diarrhea. Hydration must be maintained in all cases of diarrhea to prevent fluid depletion and shock . It contains sodium and  potassium chloride, trisodium citrate and glucose. Glucose help in absorption of sodium because glucose facilitated sodium reabsorption remains intact even in severe diarrhea Composition: Sodium chloride -3.5 grams Potassium chloride -1.5 grams Sodium citrate -2.9 grams Glucose-20 grams Above all compounds are dissolved in 1 liter of water Glucose-facilitate sodium reabsorption Sodium citrate correct acidosis, promote water and sodium retention NEW ORAL REHYDRATION SOLUTION FORMULA : Sodium chloride-2.6 grams Potassium chloride-1.5 grams Sodium citrate -2.9 grams Glucose-13.5 grams Water-1 liter In new formula WHO-ORS ,Concentration of sodium chloride and glucose as well as total osmolarity is decreased because : Use of standard formula ...

Carbamazepine -pharmacokinetics,uses,adverse effects

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  CARBAMAZIPINE Its pharmacological action similar to phenytoin Therapeutic effect in mood disorder and has anti diuretic action USE'S: Trigeminal neuralgia PHARMCOKINERTICS : ABSORPTON-Oral -slow DISTRIBUTION-75%plasma bound METABOLISM-liver EXCRETION-urine ADVERSE EFFECTS : Dizziness Sedation Vomiting  Rash INTERACTION: Decreased efficacy of oral contraceptive  Important note : Its important to recognize and manage phenytoin induced gum hypertrophy.

Prokinetic drug - METOCLOPRAMIDE /pharmacology notes

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                  PROKINETIC DRUGS Drug that promote gastrointestinal transit and hasten gastric emptying METACLOPRAMIDE: They act by blocking D2 dopamine receptor in CTZ -ANTIEMETIC ACTION Enhances acetylcholine release from cholinergic neuron in gut ACTION: GASTROINTESTINAL TRACT: Forward movement of content in upper gastrointestinal tract  Increased gastric emptying Prevent reflux esophagitis CENTRAL NERVOUS SYSTEM: Speeds up gastric emptying USES: Antiemetic Preanesthetic medication In endoscopy ADVERSE EFFECT: Sedation Gynecomastia Diarrhoea Note: Kindly do not consume medication without consulting a physician ,notes on our site is to provide notes for students only.

Paracetamol -mechanism of action,pharmacokinetics,uses,adverse effect

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                PARACETAMOL Analgesic ,anti-pyretic ,week anti inflammatory properties. Brain:Active cyclo-oxygenase -anti-pyretic action Gastric irritation mild STUDENT CORNER: HI!my dear stencildent family welcome back to our website ,if your knew to our site please do consider checking out our other posts to ,now moving on to our topic of discussion for today its about a very well and often used,and misused drug paracetamol it belongs to non -steroidal antiinflammatory drug click on this link to learn about  NSAID CLASSIFICATION  . PHARMACOKINETICS: Orally well absorbed Thirty percent protein bound Metabolised by microsomal enzyme  ADVERSE EFFECT: Nausea Rashes Large dose:  Acute paracetamol poisoning  Hepatotoxic Jaundice Nephrotoxicity - renal failure USES: Analgesic:tooth ache ,head ache  Antipyretic Chronic pulpitis,periodontal abscess,post extraction MECHANISM OF ACTION: Small portion: metabolised to -N-acetyl...

METRONIDAZOLE - ANTI AMEOBIC DRUG /PHARMACOLOGY NOTES

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                       METRONIDAZOLE INTRODUCTION: Antiameobic drug useful in infection caused by protozoa Entamoeba histolytica Its a tissue amoebicidal used for both extraintestinal and intra intestinal amoebiasis Metronidazole belongs to class nitroimidazole which is the first line drug for all forms of amoebiasis They are active against other protozoa ( TRICHONOMAS VAGINALIS, GIARDIA LAMBIA AND ANEROBIC INFECTION) MECHANISM OF ACTION: Metronidazole as a pro drug enter in the organism  Nitro group present in the drug accept electron from ferredoxin  Nitro group converted to highly reactive nitro radical Highly reactive nitro radical damage microbial DNA  Leads to death of organism produce cidal effects PHARMACOKINETICS: ABSORPTION: Orally ,Intravenous, Topical  DISTRIBUTION: Diffuse into tissue METABOLISM: liver EXCRETION: Urine  ADVERSE EFFECT : GASTROINTESTINAL :Nausea,vomiting ,abdominal cramps AL...

ODONSETRON- ANTI EMETIC DRUG/MECHANISM OF ACTION /PHARMACOKINETICS AND SIDE EFFECTS

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                              ODONSETRON  Pro type of anti-emetic drug Controls cancer chemotherapy /radiotherapy ,drug induced vomiting. MECHANISM OF ACTION: It blocks depolarization of 5 HT through 5-HT3 receptor on vagal  afferent in gastro intestinal tract. Cytotoxic drugs/chemotherapy causes cellular damage there by induce vomiting ,thereby release of mediator of 5-HT from intestinal mucosa,activation of vagal afferent in gut and sends emetogenic impulse to NTS. Odonsetron blocks emetogenic impulses both at peripheral and central relay  PHARMACOKINETICS: Oral bio availability :60-70% Eliminated in urine ,faceces SIDE EFFECTS : Headache Mild constipation Rashes  Allergic reaction  CONCLUSION: Hi stencildent family hope you all liked this short notes on odonsetron if it helped you learn then do let me know in the comment section below as this wou...

NSAID -PROPIONIC ACID DERIVATIVE DRUG (IBUPROFEN),ACETIC ACID DERIVATIVE (KETOROLAC),FENAMATE DRUG(MEPHENAMIC ACID) PHARMACOLOGY NOTES

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  NON -STEROIDAL INFLAMMTORY DRUG STUDENTS CORNER: Hello VANAKKAM!,my dear stencildent family members this is a continuation of previous blog on introduction to non-steroidal anti inflammatory drug where in we learnt classification, mechanism of action of NSAID in detail along with a short notes on ASPIRIN if we haven't learnt about it yet then do click on the link to  NSAID -PART 1 learn more. Now lets get inside our content on propionic acid derivative drug-ibuprofen ,acetic acid derivative drug -ketorolac and fenamate derivative mephenamic acid.  PROPIONIC ACID DERIVATIVE : IBUPROFEN Better tolerated alternative to aspirin ,safest NSAID  Antiplatelet  action is short lasting  Weaker anti-inflammatory drug USES: Analgesic ,anti-pyretic Rheumatoid arthritis Tooth extraction(aspirin +codeine) Soft tissue injury ADVERSE EFFECTS : Nausea Vomiting CENTRAL NERVOUS SYSTEM: Headache ,dizziness, blurring of vision ,rash ,itching  PHARMACOKINETICS AND INTERAC...

NON- STEROIDAL ANTI INFLAMMATORY DRUGS -PHARMACOLOGY CLASSSIFICATION ,ASPIRIN -USES AND ADVERSE EFFECTS

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  NON -STEROIDAL ANTI INFLAMMATORY DRUG  They are non-opioid analgesics  They have anti-pyretic ,uricosuria properties CLASSIFICATION  A)NON SELECTIVE COX-INHIBITOR : ACETIC ACID ACID :   KETOROLAC,INDOMETHACIN,NABUMETONE ENOLIC ACID : PIROXICAM PYRAZOLONE : PHENYLBUTAZONE OXYPHENBUTAZONE FENAMATE : MEPHENAMIC ACID PROPIONIC ACID : IBUPROFEN KETOPROFEN NAPROXEN FLURBIPROFEN SALICYLATE: ASPIRIN B)PREFERENTIAL COX-2 INHIBITORS  : DICLOFENAC ACECLOFENAC ETODOLAC NIMESULIDE MELOXICAM C)SELECTIVE COX - 2 INHIBITOR : PARECOXIB CELECOXIB ETORICOXIB D)ANALGESICS WITH ANTI-PYRETIC WITH POOR ANTI-INFLAMMATORY ACTION: PARA AMINOPHENOL DERIVATIVE :PARACETAMOL (ACETAMINOPHEN) PYRAZOLONE DERIVATIVES:METAMIZOL PROPIPHENAZONE BANZOXAZOCINE DERIVATIVE :NEFOPAM MECHANISM OF ACTION: When any infectious agent (stimuli)enters the  body it affect phospholipid bilayer ( important component of cell membrane)it stimulate enzyme phospholipase A2  ,it destroys phospholipids...

CIPROFLOXACIN- Mechanism of action ,pharmacokinetics,uses,adverse effect

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                         CIPROFLOXACIN Its a first generation fluoroquinolones anti microbial drug Active against gram negative bacilli especially Enterobacteriaceae and Neisseria Its highly susceptible to salmonella ,shigella, Enterobacter Rapid bactericidal activity activity by digesting DNA It has low frequency of resistance MECHANISM OF ACTION: Fluoroquinolone does 2 roles :  Inhibit topoisomerase in gram positive bacteria ,there by inhibit separation of DNA Strands  Inhibit DNA Gyrase enzyme in gram negative bacteria ,thereby resealing strands of DNA  Ultimately both block synthesis of bacterial DNA and produce bactericidal effect. PHARMACOKINETICS: ABSORPTION: Oral, Intravenous ,topical  DISTRIBUTION: Kidney ,lung ,bile METABOLISED: Liver  EXCRETION: Urine USE: Anthrax Bacterial diarrhea Chancroid Conjunctivitis Typhoid fever : first choice Tuberculosis: component for chemotherapy Urinary tra...

Anti-tubular action ,pharmacokinetics,adverse effects of Rifampicin

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  RIFAMPICIN : Its a semi-synthetic derivative of Rifamycin  1st line drug used in tuberculosis  Rifampicin is bactericidal to M.tuberculosis,M.leprae Inhibits most gram positive and gram negative bacteria like staphylococcus aureus,N.meningitidis,E.coli,klebsiella,pseudomonas,proteus and legionella ANTI-TUBULAR ACTION: Tuberculocidal :treatment for tuberculosis  Acts on intra and extracellular organism and drug resistant organism hence called - STERILISING AGENT  Inhibit DNA dependent RNA synthesis if used alone it develops drug resistance                                                    Rifampicin             Bind with beta subunit of DNA dependent RNA polymerase                                        ...