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Endocrine Pharm > Androgen Pharm > Flashcards

Androgen Pharm Flashcards

1
Q

What cells produce Testosterone in men and women?

A

Leydig Cells

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2
Q

How often is GnRH secreted?

A

every 30-120 minutes

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3
Q

Where does negative feedback for Testosterone take place?

A

Anterior Pituitary and Hypothalamus

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4
Q

What is the enzyme int the Leydig cells that converts androstendione testosterone?

A

17B hydroxysteroid dehydrogenase (17B-HSD)

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5
Q

What proteins is Test. normally bound to?

A

Albumin (bioavailable)

SHBG sex hormone binding globulin (unavailable)

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6
Q

What are the 2 functions of Testosterone?

A 
Anabolic 
Androgenic (sexual repro and 2ndry male sex char.)
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7
Q

What are the anabolic Effects of Androgens?

A 
Inc. RMR
Lower Blood Glucose
Inh. Lipid acc. in adipocytes
Skel- Enhances bone formation
closure of  epi Gr Plate
RBCs- Inc production of EPO
Muscle- Inc. Protein synth and Inh. Protein Breakdown
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8
Q

What are the Theraputic uses of androgens?

A 
Endometriosis
Delayed puberty
Hypogonadism
Aging
Anabolic Effects
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9
Q

What is Hypogonadism?

A

Androgen deficiency

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10
Q

What is Primary Androgen Def?

A

Testicular dysfunction. Dec. T

Loss of Neg. FB

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11
Q

What is Secondary Androgen Def?

A

Hypothalamus
Morbid obesity
Dec in circulating gonadotropins
Low T with low LH andFSH

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12
Q

What are the theraputic androgen preparations?

A

Methyltestosterone (Oral or SL)
Test. Enanthate (IM)
Testosterone (TD or topical)

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13
Q

What are the adverse effects of Androgen therapy?

A 
Premature epiphyseal closure
Inc Musc/tend injuries
Hepatic Dysfunction
Lipid metabolism
Edema, Fluid retention
Polycythemia
Mental Disturbances
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14
Q

Waht are the theraputic uses of Antiangrogens?

A 
F- Hirsuitism
M-Precocious Puberty
-BPH
-Prostate Cancer
-Alopecia
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15
Q

What are the different types of anti-androgens?

A

Androgen Receptor inhibitors
GnRH Agonists
GnRH Antagonists
Steroid Synthesis Inhibitors

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16
Q

Waht are the drugs included in the And. Rec. Antagonists?

A

Flutamide

Bicalutamide

17
Q

What is the Use of And. Rec. Antagonists?

A

Tx for Prostate cancer

18
Q

What is are the SA of And. Rec. Antagonists?

A

Gynecomastia
Rev. Liver Tox
Limited effects when used alone
Admin prior to GnRH analog Tx

19
Q

What is the purpose of GnRH Receptor agonists?

A

Prostate Cancer Tx

20
Q

What drugs are GnRH Receptor agonists?

A

Leuprolide

Goserelin

21
Q

What are the SAs of GnRH agonists?

A 
Sexual Dys
Bone mineral density loss
Anemia 
Fatigue
Initial Surge in T levels that can cause growth of Pros. Cancer
22
Q

What are the defferences between Degarelix and other GnRH receptor agonists?

A

Faster
No LH (test) surge
Red LH/FSH prod
Dec Test Production. More effective T supression

23
Q

What is the drug in the Androgen Biosynth Inhibitors?

A

Abiraterone

24
Q

What is the use of Abiraterone?

A

Mets prostate cancer

Used with prednisone

25
Q

SA ofAbiraterone

A

Hepatic Tox

HTN, Hyper K and fluid retention

26
Q

What are the 5a reductase inhibitors?

A

Finasteride and dutasteride

27
Q

What is the use of 5a-reductase inhibitors?

A

BPH

Male pattern baldness

28
Q

What is the Mechanism of Tx of Androgenic Alopecia?

A

Balding people have increased androgen receptor and 5a-reductase (DHT)levels

DHT cause baldness by inducing apoptosis in dermal papilla

29
Q

What are the SA of 5a reductase inhibitors.

A

Impotence and Gynecomastia
Lower PSA levels
-False neg in PC screening
-PSA values should be doubled for comparison.

30
Q

What is the Mechanism of Penile Erection?

A 
Nitric Oxide
Act. Guanylyl cyclase
cGMP
Relaxation ofSM of corpus cavernosum
Inc. BF
erection
31
Q

Waht is the MOA of ED Tx Drugs?

A

Increase in cGMP

32
Q

What are the PDE5 inhibitor drugs?

A

Sildenafil
Vardenafil
Tadalafil

33
Q

Which Pts respond the least well to PDE5 inhibitors?

A

Cavernous nerve dysfunction

Diabetics and Prostatectomies

34
Q

What are the SA of PDE5 inhibitors?

A

Serious crdiac events
Dangerous combo with nitrates/nitrites. Dangerously Low BP
Priapism
Sudden vision loss

35
Q

How are Testosterone esters made and used?

A 
FA conjugated to Test. (C17 w/ ester bond)
Increases lipophilicity
Dissolved in oil, given IM
Slow Release
Ester hydrolysed in vivo
Slower metabilism(liver)
Longer duration
36
Q

What are the properties and risks of 17 alkylated derivatives of Test?

A

Slower Liver Cat.
Oral
Liver and Hepatic Tox can occur (higher risk than with unmod T or Test Esters)

37
Q

What is the MOA of the Androgen receptor Antagonists?

A

Inhibits nuclear translocation of AR
Blocks DNA binding
Blocks coactivator recruitment

38
Q

What is the MOA of the GnRH receptor agonists?

A

Increased receptor affinity and decreased proteolysis compared to GnRH
Increases LH and test. production
Desensitization and Dn Reg of GnRH receptors on pituitary gonadotropes

39
Q

What must be added to the GnRH agonists in Tx of prostate cancer?

A

AR Receptor antagonist

prevents initial Test. Surge that can inc. cancer growth

Endocrine Pharm (11 decks)

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