Medicinal chemistry

• Pharmaceutical Products and Drug Action involve ethics, side effects and safety, tolerance and addiction, drug action and development, clinical trials and placebo effect, bioavailability, and drug action & development.
• Drugs can be applied or administered in various ways such as ingestion by mouth, injection with a syringe, inhalation by mouth or nose, absorption through the skin, absorption in the rectum or vagina, or applied into the ear or eye.
• Drugs interact with binding sites of enzyme and cellular receptor(protein receiving signal) and when drugs bind to cellular receptors the cells responds by changing state to allow other molecules to pass.
• The efficiency of a drug depends on its chemical structure and binding sites.
• Drug development involves lead compound identification, either isolated from natural sources or synthesized and screened, and drug discovery is slow and expensive; drug design relies on computers.
• Clinical trials involve different phases, evaluating effectiveness, safety, dosage, and side effects.
• Post-clinical studies, or phase IV, continue to assess long-term effects, chronic toxicity, and carcinogenic potential.
• The placebo effect is the therapeutic action of placebo, a treatment with no active properties, and participants who take the placebo may experience an improvement in their condition, such as pain relief.
• Clinical trials involve laboratory animals or human volunteers being separated into two groups of equal size, one group receiving the drug, the other group receiving the placebo, and a double blind study ensures neither the participants nor the experimenters know who received the drug or placebo.
• Clinical trials for Remdesivir, a drug used for COVID-19, involved a small group of healthy individuals in phase I to determine the safety and dosage, a larger group of individuals diagnosed with COVID-19 in phase II to assess safety and effectiveness, and large-scale efficacy and safety trials in phase III.
• Common side effects of drugs include headache, constipation, and skin rash or dermatitis.
• Aspirin is synthesized from the first extraction from willow bark and is one of the most commonly used medicines around the world.
• Aspirin has multiple different ways of use and is a weak acid.
• The synthesis of aspirin involves the reaction of salicylic acid and acetic anhydride, which produces aspirin (acetylsalicylic acid) and acetic acid (ethanoic acid).
• The esterification reaction involves the splitting of the acetic anhydride molecule, where one part replaces the hydrogen atom of the –OH group on the salicylic acid and the other accepts the hydrogen atom to form acetic acid.
• The esterification reaction requires an acid catalyst and produces white odourless crystals (aspirin).
• Aspirin is primarily used as a pain reliever, fever reducer and anticoagulant.
• Opiates are a subset of drugs derived naturally from the opium poppies.
• Polar molecules with functional groups of hydroxyls, carboxyls, and amino acids are the most commonly used functional groups because of their solubility in water.
• The main steps in drug development include preclinical studies, clinical trials, and post-marketing surveillance
• Aspirin is an everyday pain reliever for many, as it relieves mild to moderate pain and inflammation.
• Aspirin interferes with the production of prostaglandins, which are involved in the transmission of pain impulses to the brain.
• The structure of drugs affects the drug receptor interaction.
• Diarrhea and dizziness are common side effects of many drugs.
• ED 50 is the minimum dose for desired effect in 50% of the population in a test subject.
• First-pass effect is the decrease in active drug concentration due to metabolism of drug at certain locations, especially oral.
• Side effects of morphine include hallucinations, drowsiness, and increased heart rate.
• Therapeutic Index (TI) is calculated after clinical trials and is used to express effectiveness and safety of a drug.
• Drugs use double blind tests and animal testing is used to determine lethal dose.
• Tolerance can be overcome by increasing dosage, but this can be dangerous.
• Therapeutic Window (TW) is the range of a drug dose that only causes positive effects.
• Addiction can be overcome by decreasing dopamine levels, but this can be dangerous.
• Heroin (diamorphine) has a higher pharmacological potency than morphine.
• High Therapeutic Index means the drug is relatively safe and difficult to overdose, while Low Therapeutic Index means the drug is dangerous and requires professional administration.
• Overdosing on any drug can lead to kidney, liver, and brain damage, which in severe cases can be fatal.
• Aspirin prevents blood clots and heart attacks as it has the ability to thin blood.
• Bioavailability is the fraction of drug dosage absorbed into the bloodstream.
• The main steps in drug development include preclinical studies, clinical trials, and post-marketing surveillance.
• Injections/intravenous have highest bioavailability (close to 100%) oral is very low (close to 20%).
• Low Therapeutic Index means that administration methods with high bioavailability must be monitored carefully to prevent overdose.