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
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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 helpful in nocturnal GERD symptoms due to its
irreversible binding to ????????
Pantoprazole
PPI enzyme
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6. Drug interaction…..
– Pantoprazole is Less interacting drug when compared with other PPI's
– More compared to panto ex warfarin (anticoagulant), cyclosporine
(immunosuppressant)
7. Drug combination
– Clopidogrel-PPI interaction 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…..
– Research studies 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….
– Nausea and 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.
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-positive aerobes, 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 is hydrolysed by renal dehydropeptidase-1 enzymes
– Meropenem Stable to renal dehydropeptidase
Stability….
16. During Pregnancy…..
"Category C for 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….
– A notable 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 treatment of serious infections, imipenem is
more economical than meropenem based on acquisition
cost
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Binding site….
– Ceftrixone: Carboxypeptidases, endopeptidases and transpeptidases (PBP 2B)
– Cefixime: PBP 2
– Cefepime: PBP 2
21. Efficacy
– Ceftriaxone has a 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: Highly resistance 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 all belongs 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.
27. Sources….
– Whey is left 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….
Protein Type
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 Efficiency Ratio
– 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
32. Health….
– The use of 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…..
– Soy phytoestrogens (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