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Difference between drugs
The document compares several drugs and proteins. It discusses how pantoprazole binds deeper in proton pumps than rabeprazole, making it more effective for nocturnal GERD. It also notes that pantoprazole has fewer drug interactions than other PPIs but can decrease the anti-aggregation effects of clopidogrel, though this is not seen with pantoprazole. The document further compares meropenem and imipenem in their binding sites and spectra, stability to dehydropeptidase, and costs. Whey and soy proteins are also compared in their amino acid profiles and health effects, with whey noted to be higher in BCAAs and cysteine while soy isoflavones
Difference between drugs
- 1. Difference that can change yourtarget to achieve Lakshmi Narayan M
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- 3. I won Binding site…. –Pantoprazole binds to cysteine 822 (covalently inhibit enzyme), which is deeper in the membrane domain of the proton pump. Due to this AUC, half life and Cmax, is more. – Rabeprazole binds to cysteine 813 and both 892 and 321 in the enzyme
- 4. Efficacy Pentprazole is helpfulin nocturnal GERD symptoms due to its irreversible binding to ???????? Pantoprazole PPI enzyme Who am I???
- 5. Stability…. Pantoprazole is morestable to gastric acid….. Who am I
- 6. Drug interaction….. – Pantoprazoleis Less interacting drug when compared with other PPI's – More compared to panto ex warfarin (anticoagulant), cyclosporine (immunosuppressant)
- 7. Drug combination – Clopidogrel-PPIinteraction found a significant decrease of the clopidogrel platelet antiaggregation effect for other PPI, but not for pantoprazole – Decreases the anti aggregation activity of clopidogrel Because of this property panto is very helpful in cardiac disorder patient when given with clopidogrel
- 8. During Pregnancy….. – Researchstudies with animals found harmful effects on unborn babies. It hasn’t been properly studied in humans. The benefits might outweigh the risks even if you’re pregnant – Research studies with animals haven’t found a risk to unborn babies, but it hasn’t been properly studied in humans.
- 9. Side effects…. – Nauseaand vomiting for pantoprazole – Diarrhoea , flatulence (formation of gas), frequent bowel movements. – Rabeprazole in high doses or for longer than 1 year can increase the risk for bone fractures, especially in osteoporosis (weak bones) patients.
- 10. Cost….. Rabiprazol when comparedto pantoprazole is little more expensive
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- 12. Binding site….. – Imipenem:PBP1, PBP 2 and PBP 4 – Meropenem: PBP1, PBP 2, PBP 3 and PBP 4 (PBP 3 which may account for its enhanced activity against Gram-negative bacilli compared with imipenem)
- 13. – Against Gram-positiveaerobes, imipenem is in general two to fourfold more active than meropenem ex:S.auerus (penicillinase-producing strains), Acinetobacter sp., Enterobacter sp., E.coli, H. influenzae, H. parainfluenzae, Klebsiella sp., or Serratia marcescens – Meropenem is two to 16 fold more active than imipenem against Gram- negative aerobes, Meropenem is approved for the treatment of bacterial meningitis. Ex S. aureus (methicillin susceptible strains only), Streptococcus pyogenes, Group B streptococci, viridans streptococci, E. coli, Pseudomonas aeruginosa, Proteus mirabilis, Peptostreptococcus sp., B.fragilis6 Efficacy
- 14. – Imipenem ishydrolysed by renal dehydropeptidase-1 enzymes – Meropenem Stable to renal dehydropeptidase Stability….
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- 16. During Pregnancy….. "Category Cfor imipenum – Animal reproduction studies have shown an adverse effect on the fetus and there are no adequate and well-controlled studies in humans, but potential benefits may warrant use in pregnant women despite potential risks" "Category B for meropenum – Animal reproduction studies have failed to demonstrate a risk to the foetus and there are no adequate and well-controlled studies in pregnant women."
- 17. Side effects…. – Anotable adverse effect associated with imipenem is the development of seizures, phlebitis or thrombophlebitis at the injection site – Renal adjustment is required – Redness and swelling at the injection site – Renal adjustment is required
- 18. Cost….. For the treatmentof serious infections, imipenem is more economical than meropenem based on acquisition cost
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- 20. I won Binding site…. –Ceftrixone: Carboxypeptidases, endopeptidases and transpeptidases (PBP 2B) – Cefixime: PBP 2 – Cefepime: PBP 2
- 21. Efficacy – Ceftriaxone hasa broad spectrum of activity against Gram-positive and Gram- negative aerobic, and some anaerobic, bacteria. Effective against multidrug- resistant Enterobacteriaceae, meningitis, urethral, cervical, rectal or pharyngeal gonorrhoea (Standard therapy) – Cefixime: It is an orally active third generation cephalosporin. used to treat bacterial infections of the ear, urinary tract, and upper respiratory caused by many Enterobacteriaceae, Haemophilus influenzae, Moraxella catarrhalis and Streptococcus pyogenes. – Cefepime is usually reserved to treat severe nosocomial pneumonia, infections caused by multi-resistant microorganisms (e.g. Pseudomonas aeruginosa) and empirical treatment of febrile neutropenia.
- 22. Stability…. – Ceftriaxone: Highlyresistance to penicillinases, cephalosporinases and extended spectrum beta-lactamases – Cefixime: resistant to hydrolysis by many beta-lactamases – Cefepime: Stable to TEM-1, TEM-2 and SHV-1 beta lactamases
- 23. Drug interaction….. – Ceftriaxone:Aminoglycosides (ex, gentamicin), anticoagulants (eg, warfarin), cyclosporine, or heparin because the risk of their side effects may be increased by ceftriaxone, Certain live vaccines (BCG, oral typhoid) because ceftriaxone may decrease their effectiveness – Cefexime: Anti coagulants increased and BCG – Cefepime: should be taken care with drugs which produces nephrotoxicity
- 24. During Pregnancy….. We allbelongs to same category Animal reproduction studies have failed to demonstrate a risk to the foetus and there are no adequate and well-controlled studies in pregnant women."
- 25. Side effects…. – Ceftrixone:Hypoprothrombinaemia and bleeding are specific adverse effects. Haemolysis is reported, Allergic neutropenia. – Cefexime: Stool changes and diarrhoea are the most prominent side effects. Renal adjustment required – Cefepime: Symptoms of overdose include seizures, encephalopathy, and neuromuscular excitability, Renal adjustment required.
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- 27. Sources…. – Whey isleft over when milk is coagulated during the process of cheese production, and contains everything that is soluble from milk – Soy protein is a protein that is isolated from soybean. It is made from soybean meal that has been dehulled and defatted
- 28. Protein Rating Scales…. ProteinType Protein Efficiency Ratio Biological Value Net Protein Utilization Protein Digestibility Corrected Amino Acid Score Beef 2.90 80.00 73.00 0.92 Black Beans 0.00 0.00 0.75 Casein 2.50 77.00 76.00 1.00 Egg 3.90 100.00 94.00 1.00 Milk 2.50 91.00 82.00 1.00 Peanuts 1.80 0.52 Soy protein 2.20 74.00 61.00 1.00 Wheat gluten 0.80 64.00 67.00 0.25 Whey protein 3.20 104.00 92.00 1.00
- 29. Some definitions… Protein EfficiencyRatio – The protein efficiency ratio (PER) determines the effectiveness of a protein through the measurement of animal growth. Standard value is 2.7 Biological Value – Biological value measures protein quality by calculating the nitrogen used for tissue formation divided by the nitrogen absorbed from food. Net Protein Utilization – Net protein utilization is similar to the biological value except that it involves a direct measure of retention of absorbed nitrogen
- 30. Complete protein…. ESSNTIAL AMINOACIDS MILLIGRAMS PER 26 GRAMS AMINO ACID SOY WHEY LEUCINE (BCAA) 1546.00 2609.00 ISOLEUCINE (BCAA) 921.00 1333.00 VALINE (BCAA) 940.00 942.00 METHIONINE 245.00 443.00 ARGININE 1428.00 480.00 HISTIDINE 489.00 425.00 LYSINE 1184.00 2222.00 PHENYLALANINE 977.00 831.00 TRYPTOPHAN 595.00 244.00 TOTALS 9039.00 10491.00
- 31. Continue…. AMINO ACIDS MILLIGRAMSPER 26 GRAMS AMINO ACID SOY WHEY CYSTEINE 244.00 869.00 ASPARTIC ACID 2180.00 2039.00 ALANINE 808.00 230.00 GLUTAMIC ACID 3589.00 2683.00 GLYCINE 789.00 78.00 PROLINE 940.00 179.00 SERINE 977.00 180.00 TYROSINE 714.00 172.00 TOTALS 10241.00 6430.00
- 32. Health…. – The useof whey which contains an ample supply of the amino acid cysteine. Cysteine appears to enhance glutathione levels, which has been shown to have strong antioxidant properties that can reduces the risks of diseases such as heart disease, cancer and diabetes – Whey is an abundant source of branched-chain amino acids (BCAAs), which are used to stimulate protein synthesis. – consumption of whey protein shortly after vigorous exercise can boost muscle hypertrophy – Scientific evidence has shown that proteins high in essential amino acids (EAA), branched chain amino acids (BCAA), and particularly leucine (Leu) are associated with increased muscle protein synthesis, weight loss, body fat loss, and triglyceride profile
- 33. Health Soyaaa….. – Soyphytoestrogens (isoflavones: genistein and daidzein) adsorbed onto the soy protein were suggested as the agent reducing serum cholesterol levels and the risk of heart disease – The health benefits associated with soy protein are related to the physiologically active components that are part of soy, such as protease inhibitors, phytosterols, saponins, and isoflavones – Some nutritional counselors have begun to suspect that soy may be to blame for the low energy, digestive disturbances, hypothyroidism, infertility, and other ailments they see in clients. – It may cause male breast enlargement and ever lead to male breast cancer