Ahmed Lawind’s Post

Indoor agriculture to the next level. Here is an entire garden, without a single grain of soil, sand or compost Credit: O. Fawole #innovation #green #agritech #tech

“Can I consume X food while taking X medication? Or Is it safe to take atorvastatin with grapefruit juice or Isocarboxazid antidepressant with tofu? These are common questions asked by people who are managing their medical conditions with medication.   Were you aware that certain food and drug interactions can have lethal consequences?   Why does this happen? First, let's learn about grapefruit. Grapefruit or grapefruit juice contains compounds that inhibit certain enzymes in the liver, which can affect the way medications are metabolized. As a result, drugs can remain in the body for longer than usual, leading to higher concentrations and an increased risk of side effects. Some examples of medications that can interact with grapefruit juice include statins (used to lower cholesterol), certain blood pressure medications (such as nifedipine), some anti-anxiety medications (such as buspirone), and antihistamines (such as fexofenadine). There are many other food-drug interactions, such as: Dairy products can affect the absorption of certain antibiotics, such as tetracycline and ciprofloxacin. Leafy green vegetables, such as spinach, kale, and broccoli, contain vitamin K, which can interfere with the effectiveness of blood thinners like warfarin. Alcohol can interact with numerous medications, including pain relievers, antidepressants, and sedatives. Tyramine, a biogenic amine found in cheeses and other foods, can cause severe hypertensive reactions when consumed by patients treated with antidepressant monoamine oxidase inhibitors (MAOIs). Although the severity of the interaction can vary depending on the person, the drug, and the amount of grapefruit juice consumed, it's important to speak with your doctor or pharmacist about avoiding grapefruit juice or adjusting your medication dosage if you're taking any of these medications. By being aware of food-drug interactions, we can help ensure the safety and effectiveness of our medications. Stay informed and take care of your health!

The Fascinating Story Behind the Development of #Sitagliptin: From Weak Screening Hit to a #Blockbuster Drug   Introduction: Type 2 #diabetes is a growing epidemic worldwide, and scientists are continually searching for novel therapeutic approaches to treat this disease. One promising approach is to inhibit dipeptidyl peptidase-4 (DPP-4), an enzyme responsible for the rapid degradation of incretin hormones that regulate insulin secretion. This led to the discovery of sitagliptin, a potent and selective DPP-4 inhibitor developed by Merck & Co.   Discovery of #Sitagliptin: (see figure) The journey to develop sitagliptin started with a screening hit, β-Amino acid proline amide, which had weak DPP-4 inhibition (DPP-4 IC50 of 1900 nM). Scientists then optimized the compound, resulting in LEAD-1 with a DPP-4 IC50 of 119 nM. However, LEAD-1 had poor absorption, distribution, metabolism, and excretion (ADME) properties, so further modifications were necessary.   After several rounds of optimization, scientists developed LEAD-2, which had excellent potency but still had poor ADME properties. Researchers then conducted pharmacokinetic/pharmacodynamic studies in rats, which identified the metabolic breakdown products of LEAD-2 via oxidation of the piperazine ring.   Scientists eventually discovered that a bicyclic compound stabilized the metabolism of the piperazine ring in LEAD-2, leading to the development of sitagliptin. Sitagliptin has high potency (DPP-4, IC50 = 18 nM), ideal ADME properties, and has been approved for medical use in the United States since 2006.   Best Use of Biocatalysts in Sitagliptin Synthesis: Traditional methods for sitagliptin synthesis involve high-pressure hydrogenation with a rhodium-based chiral catalyst. However, a more sustainable biocatalytic route was developed that directly aminates prositagliptin ketone to provide enantiopure sitagliptin with a yield increase of 10 to 13%, a 53% increase in productivity, and a 19% reduction in total waste. This enzymatic reaction also avoids the need for specialized high-pressure hydrogenation equipment, reducing manufacturing costs and eliminating heavy metals. This is an amazing use of enzymes in the synthesis of bulk drugs.   Conclusion: In conclusion, the development of sitagliptin is a testament to the perseverance and dedication of the scientists involved in its discovery. It highlights the potential of medicinal chemistry and #biocatalysis in creating novel therapeutic approaches for the treatment of diseases.   Do you know some other interesting stories around drug discovery? References: 1. https://lnkd.in/d8gnh6CY 2. https://lnkd.in/d-G5WDhW 3. https://lnkd.in/d_Qnjj9f 4. DOI: 10.1126/science.118893 5. DOI: 10.1126/science.1188934 Note: This post does not promote the use of any drug or company...

Paracetamol could increase blood pressure. Regular use of paracetamol has been linked to higher blood pressure, according to research funded by the British Heart Foundation and published (2022) in the journal Circulation. The study found that long-term use of paracetamol could increase the risk of heart disease and strokes in people with high blood pressure. Those who had taken the medication for at least six months were found to have a 9% higher risk of developing high blood pressure compared to those who did not take the painkiller. Researchers from the University of Edinburgh advise that patients with a long-term prescription for the medication should use the lowest effective dose for the shortest possible time. While paracetamol is generally considered safe for short term use and when used appropriately, regular and long-term use of the medication can have adverse effects. These include higher blood pressure, liver damage. The findings highlight the importance of monitoring blood pressure in those taking paracetamol regularly and considering alternative and/or non-drug pain relief options where appropriate. Circulation. 2022;145:416–423 Stroke. 2016;47:1045–1052 #paracetamol #bloodpressure #hypertension #stroke #heartattack #painrelief