Pharmacology basics

• define term pharmacology 


  the study of the effect of drugs on the function of living systems
• define term pharmacodynamics


  effect of drug on the body
• define pharmacokinetics


  effect of body on the drug
• molarity


  mass(g)= concentration(mol/l)xvolume(l)x formula weight(g/mol)
• define biological assays


  method of measuring effects of biological active substance using an intermediate in vivo or in vitro tissue or cell model under controlled conditions
• what 2 principles is homeopathy based on


  1. like cures like
  2. dilution and succession increase potency
• What is the main focus of PM2PY2 course?

  Design, synthesis, and development of lung medicines
• How can structure activity relationships influence medicine development?

  They can alter selectivity and duration of activity
• What is the purpose of studying structure activity relationships?

  To identify important atoms or functional groups
• What is a pharmacophore?

  Essential groups for biological activity
• What is the significance of identifying a pharmacophore in drug development?

  It helps create compound libraries for optimization
• What receptor is important for asthma treatment?

  β2-adrenoceptor
• What is the effect of activating the β2-adrenoceptor?

  It causes smooth muscle relaxation
• Which neurotransmitters were starting points for β2-agonists?

  Adrenaline and noradrenaline
• What role do mutagenic studies play in drug development?

  They identify important residues for binding
• Which residues are important for binding to adrenergic receptors?

  Asp-113, Phe-290, Ser-207, Ser-204
• How does the serine residue interact with catecholamines?

  Through hydrogen bonding with phenolic groups
• Why is selectivity important for β2-agonists in asthma treatment?

  To minimize side effects from other receptors
• What was the first compound used to dilate airways?

  Adrenaline
• What is a drawback of adrenaline as a treatment?

  It has a short duration of action
• How did isoprenaline improve upon adrenaline?

  It was more selective for β-receptors
• What modification increased selectivity for β2-receptors?

  Introducing alkyl substituents to the side chain
• What is isoetharine's limitation?

  It is short-lasting
• What causes the short duration of action of isoetharine?

  Metabolism by catechol-O-methyltransferase
• What modification was attempted to improve isoetharine's duration of action?

  Modifying the meta-phenol group
• What factors must be considered when replacing the phenol group?

  Hydrogen bonding, ionization, electronic influence
• How does salbutamol compare to isoprenaline?

  It is less active on the heart
• What modification made salbutamol successful against COMT metabolism?

  It was metabolized to a phenolic sulfate
• What is chiral switching in drug development?

  Switching to a pure enantiomer for patenting
• What is the advantage of the R-enantiomer of salbutamol?

  It is 68 times more active than S-enantiomer
• Why is it important to prove improvement in chiral switching?

  To justify a new patent for the enantiomer
• What happens when the N-alkyl substituent is increased in size?

  Potency at α-receptors decreases
• What is salmefamol's advantage over salbutamol?

  It has a longer duration of activity
• How does increased lipophilicity affect drug duration?

  It binds more strongly to tissue
• What is the desired characteristic of antiasthmatic drugs regarding metabolism?

  Stable in lungs but metabolized in blood
• What happens to the ester group in the blood?

  It produces an inactive carboxylic acid
• How can aspirin be used in salbutamol synthesis?

  As a starting material for reactions
• What are the important binding groups in catecholamines?

  Two phenolic groups, aromatic ring, secondary alcohol
• How does a bulky alkyl group affect β-receptor selectivity?

  It leads to selectivity for β-receptors
• What was a key finding in early β2-agonist metabolism?

  Replacing the phenol group prevented metabolism