Brainscape's Knowledge GenomeTM

Browse over 1 million classes created by top students, professors, publishers, and experts.


See full index

Drug Action II > Block 5: BPH, ED, UI Med Chem > Flashcards

Block 5: BPH, ED, UI Med Chem Flashcards

1
Q

Drugs used for BPH?

A

Reversal of urethral constriction via smooth muscle action: a1a-Adrenergic antagonist (sx tx)
Inhibitors of conversion of testosterone to DHT: 5a-reductase inhibitors (dx tx)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

What drugs are for ED?

A

PDE-5 Inhibitors
Prostaglandin E1 (PGE1)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

What drugs are used for urinary incontinence?

A
  1. Anticholinergics
    * Darifenacin (Enablex)
    * Oxybutynin (Ditropan)
    * Tolterodine (Detrol)
  2. b3-Adrenergic agonists
    * Mirabegron (Myrbetriq)
  3. Anti-diuretic hormone (ADH)
    * Desmopressin (DDAVP)
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

MOA of selective a1 adrenergic antagonists?

A

Decrease smooth muscle contraction in prostate (a1a) and vasculature (a1b)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

What are the selective a1 adrenergic antagonists?

A
  1. Prazosin
  2. Terazosin
  3. Doxazosin
  4. Tamsulosin
  5. Alfuzosin
  6. Silodosin (Rapaflo): exclusive for BPH
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

MOA of Inhibitors of 5a-reductase?

A
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

What are the isoforms of 5a reductase?

A

Type 1: skin and liver
Type 2: Reproductive tissues

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

What cause BPH?

A

DHT is a potent androgen that can cause prostate enlargement

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

How do the 5a reductase inhibitors differ from one another?

A

Finasteride (Proscar): 30X>selective for Type 2 5a-reductase
Dutasteride (Avodart): 10X> inhibitor of Type 2 5a-reductase

Both finasteride and dutasteride inhibit only Type 2 – thus DHT synthesis may continues to occur elsewhere and potential for continued prostate enlargement exists

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

What is the benefits of combo therapy for BPH?

A

Synergistic effect and lowering of dx progression

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

Describe the MOA of smooth muscle constration/relaxation?

A

cAMP and cGMP and relax muscle

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

What isoform is the focus in ED tx?

A

PDE5 inhibition

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

What was modified from Zaprinast to produce Sildenafil?

A
  1. Reduce lipophilicity and incr H2O solubility
  2. Add sulfonamide
  3. Mimic cGMP structure with the guanine structure
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

What is the endogenous substrate of PDE5?

A

cGMP

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

What is the first PO anti-impotence drug?

A

Sildenafil (Viagra)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

What are the ADRs of Sildenafil?

A

Only >10-fold for PDE5 vs PDE6:
* PDE6 is in the retina altering color vision: bluish vision, making green and blue indistinguishable or vision loss
* Potentiates the action of nitrates used for angina -> hypotension, MI

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
17
Q

What are the PDE5 inhibitors indicated for ED?

A
  1. Sildenafil (Viagra)
  2. Tadalafil (Cialis)
  3. Vardenafil (Levitra)
18
Q

Advantages of vardenafill and tadalafil than sildenafil?

A

Vardenafil (Levitra):
* 30X more selective for PDE5 than sildenafil
* 10X more potent at PDE5 than sildenafil/tadalafil

Tadalafil (Cialis):
* 85X more selective for PDE5 than sildenafil
* Equipotent at PDE5 with sildenafil

Overall lower dosing = lower risk of ADRs

19
Q
A
19
Q

What does a lower IC50 number mean?

A

More potent, requiring less drug to reach action

20
Q

What is the difference between selectivity and potency?

A

Selectivity: 1 drug, 2 targets
Potency: 2 drugs, 1 target

21
Q

What is the function of PGE1?

A

Endogenous vasodilator: Used mainly in maintaining patent ductus arteriosis in peds until surgical fix can occur

22
Q

Forms of PGE1 products?

A

CaverJet: injectable in corpus cavernosum of the penis
Muse: urethral suppositpory
PGE1 topical cream: Vitaros

23
Q

What drug class is this?

A

Anti-muscarinic: acetylcholine and bulk

24
Q

Selectivity of Oxybutynin?

A

M1-M3

25
Q

Selectvity of Tolterodine?

A

M2-M3

26
Q

Darifenacin

Brand

A

Enablex

27
Q

Solifenacin

Brand

A

Vesicare

28
Q

Oxybutynin

Brand

A

Ditropan

29
Q

Tolterodine

Brand

A

Detrol

30
Q

Mirabegron

Brand, Structure

A

Myrbetriq
b3-receptor: mimics epinephrine

31
Q

Identify

A

Epinephrine

32
Q

Identify

A

Ach

33
Q

Identify

A

guanine

34
Q

Where are Vasopressin receptors found? MOA?

A

V1 (peripheral)
V2 (renal)

35
Q

Indications for vasopressin?

A
  1. central diabetes insipidus (desmopressin)
  2. vWb dx due to its ability to increase factor
36
Q

What is DDAVP?

A

Analogue of vasopressin by altering Arg and deaminated Cys to form a more acidic and stable product (more PO F)

37
Q

ADR of vasopressin?

A

HTN, fluid retention

38
Q

5a reductase inhibitors mimics what endogenous substrate?

A

Testosterone

39
Q

Anti muscarinics must mimic what endogenous substrate?

A

Ach

Drug Action II (28 decks)

Brainscape helps you reach your goals faster, through stronger study habits.
© 2024 Bold Learning Solutions. Terms and Conditions