Hormonal Drugs Flashcards
Lecture Outcomes
Describe the basic structure of steroid hormones
Outline how endogenous steroid hormone levels are kept within a
normal range by feedback mechanisms
List other steroid hormones and therapeutic drugs related to them
Describe what male sex hormones, i.e. androgens, do in the body
Outline when androgen replacement therapy should be prescribed
Describe the difference between androgen misuse and abuse, i.e. one is
legal while the other is illegal but neither are appropriate
List the problems caused by androgen abuse
What are Steroids?
Organic compounds with 4 carbon rings
Cholesterol
Rings are named A to D & carbons are numbered
Cholesterol side chain is cleaved off - SCC
To produce other endogenous steroids - steroid hormones
What are
Hormones?
Endocrine glands such as:
thyroid
pancreas
adrenal glands
ovaries & testes
…secrete hormones that:
travel in the blood
to distant targets
(not all hormones are steroids, e.g. growth hormone)
Blood borne chemical messengers
Hormone levels are actively kept
within limits - ‘normal range’
Steroid Hormones
Many functions… - many drugs:
Androgens Inhaled glucocorticoids Oral contraceptives
Steroid Hormones Include:
- Corticosteroids -
Glucocorticoids - cortisol/hydrocortisone etc.
(Mineralocorticoids) - Female sex hormones -
Oestrogens/estrogens
Progesterone - Male sex hormones - Androgens incl. testosterone
Corticosteroid
Side Effects
Severe, especially with:
high dose
systemic (oral)
CUSHINGOID:
fat deposition - moon face,
buffalo hump, central obesity
thin skin - bruising & stretch
marks
many other problems
Endogenous Androgens
Testosterone
DHEA
Androstenedione
Produced mostly by the testes but a little by the
adrenal cortex
Testosterone is the primary natural androgen
Synthesis of endogenous testosterone is tightly controlled
- Corticosteroids - widely used
in clinical practice
ANTI-INFLAMMATORY DRUGS
asthma
allergic rhinitis/hay fever
arthritis & joint injuries
dermatitis/eczema
inflammatory bowel disease
premature infants
eye disease
many more.
- Estrogens/Progestogens
Also very widely prescribed in clinical practice:
birth control
menstrual irregularities
hormone replacement therapy
Control of Testosterone Synthesis
Legal Clinical (Prescribed)
Uses of AAS
Appropriate AAS use = Androgen Deficiency:
congenital (born with) or acquired (disease or trauma)
life expectancy is normal
but significant effects - ↓ vigour, ↓ bone & muscle mass,
↓ red blood cells
treated by androgen replacement therapy (ART) wikipedia
AAS misuse - prescribed clinically by doctor - still legal but inappropriate:
prescribed with no acceptable medical indication - infertility or erectile dysfunction
Illegal Use of AAS = Steroid Abuse
Involves using androgens obtained without a legal prescription
(i.e. no medical indication):
sporting - competitive, usually power sports
professional - bouncers, security, wrestling
recreational - bodybuilders, “body beautiful”
The evolution of steroid abuse
Brown-Séquard - 19th century doctor/experimentalist
Injected himself with testicular extracts from guinea
pigs & dogs
“Restored vitality”
Recent study → testicular extract [testosterone] too
low for any effect!
1935 - testosterone first isolated & synthesized by Butenandt &
Ruzicka → Nobel Prize (1939)
Then used for medical purposes only but soon enough…
When AAS must not be used
Legal aspects
Anabolic steroids (performance & image enhancing drugs -
PIEDs) are controlled drugs in Australia
Therefore, it is illegal to possess, use, supply, manufacture,
import or trade PIEDs without a prescription or a licence
People convicted of importing PIEDs face maximum fines of
$110,000 &/or 5 years gaol!
“Supplements” are untested and often contain unlabelled
steroids → athletes beware
The problems begin
WWII - testosterone apparently used by Nazi
soldiers to ↑ strength & aggression
1954 - USSR weightlifters dominate world championships
1950s - other power based sports - elite athletes only
1970s - competitive bodybuilders catch on
1975 - IOC bans anabolic steroids
1976 - East German ♀ - 11/13 golds at Montreal Olympics
1988 - Ben Johnson → out of competition testing
It’s been going on for
many years…
Olympic marathon winner in 1904 - Thomas Hicks
Given strychnine & brandy during the race -
needed treatment by 4 physicians after!
Heroin, morphine & cocaine also used in early
Olympic Games
Performance Enhancing Drugs in Sport
WHY do athletes TAKE AAS?
supra-physiological AAS doses → users moderately ↑ muscle
mass & strength
swifter recovery
steroid abusers stack (40-100x) → increases»_space; normal limits
testosterone levels in ♀<♂/10 → ♀ benefit more from steroid
abuse
♀ - 0.4 sec, ♂ - 0.2 s over 100m (Victor Conte)
Use of synthetic androgens
Endogenous anabolic androgenic steroids have 2 problems:
strong androgenic effects (+ oestrogen effects)
cannot be taken orally
AND anabolic steroid abusers tend
to use very high doses (stacking)
Synthetic androgens developed to:
maximise anabolic effects
↓↓ oestrogen effects and ↓
androgen effects
oral rather than injected
BUT no synthetic androgens are
purely anabolic
Adverse effects of AAS