VTE/Men's health Pharmacology

Question 1

What are 3 key processes that thrombosis is regulated by?

Answer 1

1. Platelet activation and aggregation
2. The coagulation cascade
3. Fibrinolysis

Question 2

What are the 3 signalling molecules that platelets secrete to adjacent platelets to activate

Answer 2

1. ADP
2. TXA2 (thromboxane)
3. 5-HT (serotonin)

Question 3

Is calcium a coagulation factor?

Answer 3

Yes, Factor IV (4)

Question 4

Explain fibrinolysis

Answer 4

Fibrinogen to fibrin (insoluble)
- with the help of thrombin
- surrounds the platelet plug to be more stable and allow for clotting

Question 5

What occurs in the body in the presence of a clot

Answer 5

plasminogen is converted into plasmin
- targets fibrin clot and breaks it down into fibrin degradation products

Question 6

MOA of heparin

Answer 6

Binds to antithrombin III to increase its activity
- results in a conformational change to help its ability to break down factor II, Factor X, Factor VII, Factor 9
2,9,7,10

Question 7

How can heparin increase the risk of thrombosis?

Answer 7

Antibodies that are produced that target platelets, resulting in them clumping to microparticles that can activate the coagulation cascade and cause blood clotting

Question 8

ADRs of Heparin

Answer 8

• MAJOR BLEEDING
• thrombocytopenia
• osteoporosis
• Hyperkalemia, can impair aldosterone synthesis

Question 9

What is the MOA of the antidote protamine?

Answer 9

Binds to heparin and prevent it from activating antithrombin

Question 10

MOA of LWMH

Answer 10

Binding and activating of ATIII
- chemical or enzymatic cleavage of UFH to produce LWMH that are 1/3 the length

Question 11

MOA of Pentasaccharides (fondapurinux)

Answer 11

Only binds factor Xa
- does not bind thrombin IIa

Question 12

What is the MOA of apixiban?

Answer 12

Factor Xa inhibitors

Question 13

MOA of argatroban and dabigatran

Answer 13

Organic molecule direct thrombin inhibitors

Question 14

MOA of warfarin

Answer 14

• inhibits the 2nd carboxylation process to one of their glutamate amino acids
• warfarin inhibits vitamin K reductase
• Slows down the recycling of Vitamin K

Question 15

What is the first coagulation factor concentration to decrease after warfarin therapy? last?

Answer 15

First: Factor VII 7
Last: Factor II 2

Question 16

What is the MOA of warfarin and acetaminophen interaction? PD or PK?

Answer 16

Pharmacodynamic reaction
- One of acetaminophen’s metabolites NAPQI (N-acetyl-p-benzoquinone-imine) inhibits vitamin K carboxylase and vitamin K reductase by interaction with cysteine residues
- Metabolite acts like warfarin = inc INR

Question 17

In a patient with liver dysfunction, does INR inc or dec

Answer 17

inc

Question 18

What is the active form of testosterone

Answer 18

DHT

Question 19

Do anticholinergics and alpha 1 adrenergic inhibitors have effect on prostate size in BPH?

Answer 19

No

Question 20

MOA of mirabegron. Drug class?

Answer 20

Beta-3 receptor agonist

Relaxation of the detrusor muscle allowing for a longer storage phase for urine in the bladder

Question 21

MOA of desmopressin? drug class?

Answer 21

Vasopressin V2 receptor agonist

increases water excretion and is used for nocturnal dysuria

Question 22

What are the 2 types of 5-alpha receptors

Answer 22

Type 1: sebaceous glands in scalp, face, skin, and liver and regulated facial and body hair, acne

Type 2: genitourinary tract, PROSTATE gland and HAIR FOLLICLES

Question 23

What is the physiology of an erection? What are the Neurotransmitters and second messengers involved?

Answer 23

Ach promotes arterial vasodilation to increase sinusoidal filling of the corporal tissue

cGMP and cAMP promote smooth muscle relaxation and vasodilation through NO

Question 24

What terminates the erection?

Answer 24

Norepinephrine results in arterial smooth muscle contraction to decrease inflow and promote venous outflow

Question 25

PDE5 inhibitors MOA

Answer 25

Increase half-life of any cGMP produced, increasing the extent of smooth muscle relaxation, and promoting erection

Question 26

What other PDE receptors that sildenafil and tadalafil target that affect ADRs

Answer 26

Sildenafil = PDE6
- cause vision related ADRs

Tadalafil = PDE1
- striatal muscle to cause myalgia

Question 27

MOA of alprostadil

Answer 27

activates Gs-coupled PGE1 receptors to increase cAMP and increase blood flow to corpora cavernose
- can be injection or intra-urethral

Question 28

What other drugs can be used for ED?

Answer 28

Yohimbine
Trazadone

both block alpha1-adrenergic receptors

Question 29

Why isn’t oral minoxidil used?

Answer 29

Significatn adverse effects that such as hypotension
reflex sympathetic nervous system activation
fluid retention