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Question 2

Aliskerin

First?

Synthetic compound having _______

Indicated for the treatment of? Either ____ or ___

___ absorbed, but ____ is low, high ___ decreases absorption

Half-life?

90% eliminated? Other part?

Adverse effects?

Answer 2

• First and only renin inhibitor, directly inhibits renin and prevents formation of Ang I
• Chiral centers
• HTN, as monotherapy or in combination
• Orally absorbed, but absolute bioavailability is low, high fat meals decrease absorption
• Half life is 44 hours
• 90% unchanged in feces, rest metabolized by CYP3A4
• AEs
  
  • Diarrhea and other GI, Hyperkalemia, headache, Dizziness, rash
  • ARBs are contraindicated during pregnancy. Co-administration with Ibesartan reduces the plasma levels and efficacy of Aliskiren, might require dose-adjustment

Question 3

Thromboxanes and Aspirin?

Answer 3

Question 4

COX-1 and COX-2 Structurally similar enzymes

Answer 4

Question 5

Properties of selected Prostanoids

Answer 5

Question 7

Other prostaglandin analogues in therapeutics?

Answer 7

• Misoprostol:
  
  • Prevention/treatment of NSAID-induced gastric ulcers
  • Orally active
  • Methyl ester increases antisecretory effect, increases duration of action, conversion to acid (active)
  • Increase GI mucosal and bicarb formation: Decreasing acid secretion, blocks NSAID induced GI bleeding
  • SE:Diarrhea
  • Contraindication in pregnant women
  • Labor induction, also used vaginal in combination with methotrexate for termination of early stage pregnancy
• Latanaprost
  
  • Structurally modified PDF analog
  • Reduces intraocular pressure by increasing the outflow of aqueous humor
  • Available as ophthalmic solution for glaucoma treatment
  • Causes growth and darkening of existing eyelashes!

Question 11

Prostaglandin analogues in therapeutics?

Answer 11

• Dinoprostone PGE2- Induction of labor
  
  • Onset 10 minutes
  • Increase Uterine contraction
    
    • Frequency, amplitude, Cervical ripening
    • SEs- fever, nausea, allergic rxn, Cramping
• Alprostadil (PGE1)
  
  • Vasodilator, Increases blood flow
  • Maintaining an open ductus arteriosus in newborns with congenital defects that restrict pulmonary or systemic blood flow until surgery can be performed
  • Male erectile dysfunction: Penile suppository, or, injected directly into penis
  • Onset 2-25 minutes lasts for an hour

Question 12

Aliskerin

First?

Synthetic compound having _______

Indicated for the treatment of? Either ____ or ___

___ absorbed, but ____ is low, high ___ decreases absorption

Half-life?

90% eliminated? Other part?

Adverse effects?

Answer 12

• First and only renin inhibitor, directly inhibits renin and prevents formation of Ang I
• Chiral centers
• HTN, as monotherapy or in combination
• Orally absorbed, but absolute bioavailability is low, high fat meals decrease absorption
• Half life is 44 hours
• 90% unchanged in feces, rest metabolized by CYP3A4
• AEs
  
  • Diarrhea and other GI, Hyperkalemia, headache, Dizziness, rash
  • ARBs are contraindicated during pregnancy. Co-administration with Ibesartan reduces the plasma levels and efficacy of Aliskiren, might require dose-adjustment

Question 13

Thromboxanes and Aspirin?

Answer 13

Question 14

COX-1 and COX-2 Structurally similar enzymes

Answer 14

Question 15

Properties of selected Prostanoids

Answer 15

Question 17

Other prostaglandin analogues in therapeutics?

Answer 17

• Misoprostol:
  
  • Prevention/treatment of NSAID-induced gastric ulcers
  • Orally active
  • Methyl ester increases antisecretory effect, increases duration of action, conversion to acid (active)
  • Increase GI mucosal and bicarb formation: Decreasing acid secretion, blocks NSAID induced GI bleeding
  • SE:Diarrhea
  • Contraindication in pregnant women
  • Labor induction, also used vaginal in combination with methotrexate for termination of early stage pregnancy
• Latanaprost
  
  • Structurally modified PDF analog
  • Reduces intraocular pressure by increasing the outflow of aqueous humor
  • Available as ophthalmic solution for glaucoma treatment
  • Causes growth and darkening of existing eyelashes!

Question 21

Prostaglandin analogues in therapeutics?

Answer 21

• Dinoprostone PGE2- Induction of labor
  
  • Onset 10 minutes
  • Increase Uterine contraction
    
    • Frequency, amplitude, Cervical ripening
    • SEs- fever, nausea, allergic rxn, Cramping
• Alprostadil (PGE1)
  
  • Vasodilator, Increases blood flow
  • Maintaining an open ductus arteriosus in newborns with congenital defects that restrict pulmonary or systemic blood flow until surgery can be performed
  • Male erectile dysfunction: Penile suppository, or, injected directly into penis
  • Onset 2-25 minutes lasts for an hour