Cimetidine was the first H2 antagonist in anti-ulcer therapy in the 1960s. The development of cimetidine was inspired by the fact that histamine stimulates gastric acid release in vitro. Which drug design strategy was used in the development of cimetidine: O Fragment based screening O X-ray crystallography O Rational drug design O Molecular modelling
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- In the design of H2 antagonists, the polar guanidine group of compound A was proposed to interact with the antagonist binding region by two hydrogen bonds. This compelled researchers to derivatize compound B from compound A. HN EN Chain Extension Rigidification ZI compound A What drug design strategy has been used here? Simplification H₂N NH Substituent variation HN NH₂ HN NH N compound BBiotransformation is an important concept in pharmacology, which amongst others, enables the effective administration of prodrugs. Provide a detailed description of factors influencing the biotransformation of drugs.In the discovery of new drugs, the chemical and physical properties of a molecule are very important to be determined. All of the following are physical and chemical properties that are important in drug discovery EXCEPT….A. route of administrationB. fat/water partitionC. molecular steric hindranceD. pHE. pKa Secretion of acid ions from gastric acid, is one of the drug distribution processes by...A. Passive diffusion with facilitiesB. passive diffusionC. dissolves in lipids that make up the membraneD. pinocytosisE. active diffusion
- Which of the following statements concerning drug delivery system is INCORRECT?* A.Drugs with good aqueous solubility are good for controlled release formulation. B.The delay-released form is also called extended release form. C.Absorption rate is higher in compressed tablets than that in capsules. D.Drug core with polymer membrane coating belongs to diffusion sustained system. E.Disintegration and dissolution can occur at the same time.What is the mechanism of action of the drug LIDOCAINE? pls. dont plagiarizeWhat properties of drug are relevant for developing modified release drug delivery formulation. Please briefly explain this at your own words.
- Which of the following drugs inhibits protein synthesis through binding to ribosomal 30S subunit: O a. Linezolid O b. Amikacin O c. Ciprofloxacin O d. AzithromycinBiDil® is indicated for the treatment of heart failure as an adjunct to standard therapy in self-identified black patients to improve survival, to prolong time to hospitalization for heart failure, and to improve patient-reported functional status Question: The results of BiDil® clinical trials were compelling…Expound on the results. Question : What role did FDA’s approval resulted in BiDil® being a great example of pharmacogenomics/pharmacogenetics in the U.S.?Please Write the Drug Discovery Process of Diltiazem? Please write at your own words.
- A patient is receiving morphine sulfate intravenously via a patient controlled analgesia (PCA) pump. The concentration of the solution is 11 mg/mL and is being infused continuously around the clock at a rate of 0.1 mL/hr. The patient may also access a 2-mg bolus dose every hour for breakthrough pain if needed and they are currently using an average of 5 additional bolus doses per day. The patient is to be converted to fentanyl using the table below. But before using the table we must determine their morphine usage, so what is this patient's total daily dosage of IV morphine? TABLE 10.3 FENTANYL TRANSDERMAL DOSAGE CONVERSION GUIDELINES", b Current Analgesic Oral morphine IM/IV morphine Oral oxycodone Oral codeine Oral hydromorphone IV hydromorphone IM meperidine Oral methadone 60-134 10-22 30-67 150-447 8-17 1.5-3.4 75-165 20-44 Recommended fentanyl transdermal system dose Fentanyl transdermal system 25 mcg/h Daily Dosage (mg/day) 135-224 23-37 67.5-112 17.1-28 3.5-5.6 166-278 45-74…Read this article and answer the following question There are 3 different Metformin ER products available: Glucophage XR Glumetza ER Fortamet ER All 3 formulations are available generically but they are not interchangeable as they all use different release mechanisms. Glucophage XR uses a dual hydrophilic polymer system. The drug is slowly released by diffusing through a gel matrix, also known as GelShield diffusion system. Once the tablet is swallowed, the outer layer of the tablet forms a gel layer and the metformin contained within is slowly released. Due to this release mechanism, Glucophage XR can not be cut or split. Glumetza ER uses a mechanism known as gastro-retentive technology (also known as 'Modified Release'). The tablets are designed to remain in the stomach and deliver metformin to the upper GI tract over an extended period of time. Like Glucophage XR, Glumetza ER can not be cut or split. Fortamet ER uses single-composition osmotic technology (SCOT). After…Here’s the fractional binding data for 2 different proteins (1 and 2) binding to a Drug D. Which of the following statements is/are true? 1 of 5: Each Protein 1 must only bind 1 molecule of D. 2 of 5: Each Protein 2 must bind 2 or more molecules of D. 3 of 5: Protein 2 binds significantly more D than Protein 1. 4 of 5: Protein 1 and 2 have roughly similar binding affinities for D. 5 of 5: Protein 1 binds faster to D than protein 2 does at low concentrations of D.