Slide 1

Chemistry in Everyday Life

Mode of action of Morphine

  • Morphine is an alkaloid drug derived from opioids.
  • It acts as a painkiller and is primarily used to treat severe pain.
  • Let’s dive into the mode of action of Morphine and understand how it affects our body.

Slide 2

Morphine and Opioid Receptors

  • Morphine interacts with our body’s opioid receptors.
  • Opioid receptors are found in the brain and spinal cord.
  • They play a crucial role in transmitting pain signals and regulating pain perception.

Slide 3

Binding to Opioid Receptors

  • Morphine binds to the opioid receptors, specifically the mu-opioid receptors.
  • This binding leads to the activation of certain intracellular signaling pathways.

Slide 4

Inhibition of Pain Signals

  • Activation of opioid receptors by morphine inhibits the transmission of pain signals.
  • It reduces the release of neurotransmitters responsible for transmitting pain signals.

Slide 5

Neurotransmitters and Pain Perception

  • Neurotransmitters like substance P and glutamate transmit pain signals in the brain.
  • Morphine suppresses the release of these neurotransmitters.
  • As a result, the pain signals are not effectively transmitted.

Slide 6

CNS Effects

  • Morphine has profound effects on the central nervous system (CNS).
  • It produces a sense of euphoria, promotes relaxation, and induces sleepiness.
  • These effects are due to its interaction with various neurotransmitter systems.

Slide 7

Side Effects

  • Morphine can cause various side effects when used for pain management.
  • Nausea, drowsiness, constipation, and respiratory depression are common side effects.
  • Long-term use can lead to tolerance, dependence, and addiction.

Slide 8

Tolerance and Dependence

  • Prolonged use of morphine can lead to tolerance.
  • Tolerance refers to the reduced effectiveness of the drug over time.
  • Dependence occurs when the body becomes reliant on morphine to function normally.

Slide 9

Addiction

  • Addiction is a severe consequence of long-term morphine use.
  • It is a compulsive drug-seeking behavior despite negative consequences.
  • Addiction is a complex disorder involving both physical and psychological dependence.

Slide 10

Conclusion

  • Morphine’s mode of action involves binding to opioid receptors.
  • It inhibits the transmission of pain signals and produces analgesic effects.
  • However, it can also cause side effects like respiratory depression and addiction.

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Modern Methods of Drug Design

  • Traditional methods of drug discovery involve trial and error processes.
  • Modern drug design incorporates computational techniques and rational drug design.
  • Examples include structure-based drug design and computer-aided drug design.

Structure-Based Drug Design (SBDD)

  • SBDD employs the knowledge of the target’s three-dimensional structure.
  • High-throughput screening and virtual screening are commonly used in SBDD.
  • Molecular docking and molecular dynamics simulations play a crucial role.

Computer-Aided Drug Design (CADD)

  • CADD involves computational tools for the design and optimization of drug candidates.
  • QSAR (Quantitative Structure-Activity Relationship) models predict drug activity.
  • Ligand-based and structure-based approaches are used in CADD.

QSAR (Quantitative Structure-Activity Relationship)

  • QSAR models correlate structural features to biological activities.
  • Molecular descriptors quantify the physicochemical properties of the drug.
  • Examples: Lipinski’s rule of five, Topological polar surface area (TPSA).

Ligand-Based Drug Design

  • Ligand-based approaches use the knowledge of already active ligands.
  • Similarity searching, pharmacophore modeling, and quantitative similarity analysis are employed.
  • These methods enable the synthesis of drug analogs with improved activity.

Structure-Based Drug Design

  • Structure-based approaches focus on the target’s structural information.
  • Molecular docking predicts the binding mode between the drug and target.
  • High-resolution structures obtained through X-ray crystallography or NMR spectroscopy are used.

Molecular Docking

  • Molecular docking predicts the binding affinity and binding site of the drug.
  • Algorithms like AutoDock, GOLD, and Glide are commonly used.
  • The docking score helps assess the binding strength of the drug with the target.

Molecular Dynamics Simulations

  • Molecular dynamics simulations study the motion of atoms and molecules.
  • They provide insights into the conformational changes and stability of drug-target complexes.
  • Examples: AMBER, GROMACS, NAMD.

Combination Therapies

  • Combination therapies involve using multiple drugs to treat a disease.
  • Synergistic effects can be achieved by targeting multiple pathways.
  • Examples: HAART for HIV, chemotherapy regimens for cancer.

Challenges in Drug Design

  • Drug design faces challenges like drug resistance and toxicity.
  • ADMET properties (absorption, distribution, metabolism, excretion, and toxicity) need to be considered.
  • Ethical concerns and high development costs are also factors to consider.

Chemistry in Everyday Life - Mode of action of Morphine

  • Morphine is an alkaloid drug derived from opioids.
  • It acts as a painkiller and is primarily used to treat severe pain.
  • Let’s dive into the mode of action of Morphine and understand how it affects our body.
  • Morphine and Opioid Receptors
  • Morphine interacts with our body’s opioid receptors.
  • Opioid receptors are found in the brain and spinal cord.
  • They play a crucial role in transmitting pain signals and regulating pain perception.
  • Binding to Opioid Receptors
  • Morphine binds to the opioid receptors, specifically the mu-opioid receptors.
  • This binding leads to the activation of certain intracellular signaling pathways.
  • Inhibition of Pain Signals
  • Activation of opioid receptors by morphine inhibits the transmission of pain signals.
  • It reduces the release of neurotransmitters responsible for transmitting pain signals.
  • Neurotransmitters and Pain Perception
  • Neurotransmitters like substance P and glutamate transmit pain signals in the brain.
  • Morphine suppresses the release of these neurotransmitters.
  • As a result, the pain signals are not effectively transmitted.
  • CNS Effects
  • Morphine has profound effects on the central nervous system (CNS).
  • It produces a sense of euphoria, promotes relaxation, and induces sleepiness.
  • These effects are due to its interaction with various neurotransmitter systems.
  • Side Effects
  • Morphine can cause various side effects when used for pain management.
  • Nausea, drowsiness, constipation, and respiratory depression are common side effects.
  • Long-term use can lead to tolerance, dependence, and addiction.
  • Tolerance and Dependence
  • Prolonged use of morphine can lead to tolerance.
  • Tolerance refers to the reduced effectiveness of the drug over time.
  • Dependence occurs when the body becomes reliant on morphine to function normally.
  • Addiction
  • Addiction is a severe consequence of long-term morphine use.
  • It is a compulsive drug-seeking behavior despite negative consequences.
  • Addiction is a complex disorder involving both physical and psychological dependence.
  • Conclusion
  • Morphine’s mode of action involves binding to opioid receptors.
  • It inhibits the transmission of pain signals and produces analgesic effects.
  • However, it can also cause side effects like respiratory depression and addiction.