qu Flashcards
1
Q
A
2
Q
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?
A
- 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
3
Q
Thromboxanes and Aspirin?
A
4
Q
COX-1 and COX-2 Structurally similar enzymes
A
5
Q
Properties of selected Prostanoids
A
7
Q
Other prostaglandin analogues in therapeutics?
A
- 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!
11
Q
Prostaglandin analogues in therapeutics?
A
- 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
12
Q
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?
A
- 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
13
Q
Thromboxanes and Aspirin?
A
14
Q
COX-1 and COX-2 Structurally similar enzymes
A
15
Q
Properties of selected Prostanoids
A
17
Q
Other prostaglandin analogues in therapeutics?
A
- 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!
21
Q
Prostaglandin analogues in therapeutics?
A
- 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
