Performance enhancer drugs Flashcards
what are the major performance enhancing drugs
anabolic steroids
what are anabolic steroids based on
testosterone but mostly synthetic derivatives
why were anabolic steroids originally used
to allow malnourished patients to gain weight and buscle
what are the 2 main roles of naturally occurring steroids
growth and maintenance of body
what are the 2 main effects of steroids
androgenic and anabolic
what are the androgenic effects of steroids
promotion of male sexual characteristics, like muscle and facial hair
what are the 4 anabolic effects of steroids
increase muscle mass, increase protein synthesis, redistribution of body fat, increase calcium deposits in bone
do users want the androgenic or anabolic of steroids
the anabolic effects, especially females
how many anabolic steroid classes are there?
3
what are type 1 anabolic steroids
testosterone esters
what are 3 things that testosterone esters do (type 1)
slows down metabolism for longer effect
hydrolyzed in body to free T
aromatized into estrogens
what do testosterone esters (type 1) do to metabolism
slow it down
what is testosterone esters (type 1) metabolized into
free T
what is testosterone esters (type 1) aromatized into
estrogens
which type of anabolic steroid is bad for males and why
testosterone esters (type 1) because they are aromatized into estrogens`
what are type 2 anabolic steroids
19-nor testosterone derivatives
what is the structure of 19-nor testosterone derivatives like
methyl group at C19 is removed
what is the half life of 19-nor testosterone derivatives
extended
what is the androgenic activity of 19-nor testosterone derivatives (type 2)
reduced
is 19-nor testosterone derivatives (type 2) aromatized like type 1
yes but 20% as efficiently (so much less)
what are type 3 anabolic steroids
17α-alkyl derivative
what does alkylation on type 3 anabolic steroids do
reduces liver metabolism so they can be taken orally
are type 3 converted into 17β-estradiol
no
what does the extra ring in type 3 cause
increased anabolic effect
what are 2 structural things added to type 3 anabolic steroids
alkyl group and an extra ring
what is 1 structural difference with T and type 2
removed methyl at C19
which of the anabolic steroid classes cant be taken orally
2
are many old steroids easily detectable and why
yes because they were/are commonly used
are many new steroids easily detectable and why
no because they dont know what to look for
what are 2 big issues with designer steroids
- drug labs dont know what to identify(cant detect what you dont know)
- they havent been tested for safetly like the origional ones
how are designer steroids made
modifications of existing steroids by illicit drug labs
which receptor do anabolic steroids bind
to the androgen receptor
what happens to receptor binding with high concentrations of androgens
anabolic steroids will start binding to other receptors, like estrogen
what happens once steroids bind to its receptor (4 steps)
- complex enters nucleus
- Binds to region of DNA to activate certain genes
- makes mRNA
- mRNA used to make new proteins (like muscle mass)
what do steroids do to stem cells
steer them into muscle cells and prevent them forming fat cells
are the proteins made by steroid just those involved in muscle
no - steroid receptors are found in many different tissue (even brain)
are there steroid receptors in the brain
yes
do we know all the genes that are activated by steroids
no, huge gap in knowledge
what are some of the genes other than those for muscle growth responsible for
unwanted and dangerous side effects
what is hypogonadism
testes reacting to steroids by making less T, shrink testicles, lower sperm count, can be irreversible
what can happen to fertility with steroids
some people become permanently infertile
what are effects of steroids in women
masculinization
facial hair
decreased breast size
loss of period
what happens to breast size in women with steroids
decrease
what happens to breast size in men with steroids
increase because testosterone is the precursor to estradiol - mediated by aromatase enzyme
what is gynecomastia
breast enlargement in men
why do some bros take aromatase inhibitors
to block conversion of testosterone into estrogen
how do androgens cause severe acne
- steroids enlarge sebaceous glands
- increase sebum production
- increase cell growth in hair follicles
- increase bacteria population
what is acne fulminans
severe type of acne with a bone lesion and arthritis component
what causes acne fulminans (likely)
reaction to P. acne bacterium
can acne fulminans happen without steroids
yes but very rare
where are steroids metabolized
in the liver
what does steroids do to the liver
increase risk of tumors
what kind of liver tumors happen with steroids
benign blood filled cysts that can cause liver failure or bleeding out
are the liver tumors reversible
yes upon cessation usually
what are 3 effects of steroids on the cardiovascular system
increase BP, increase cholesterol, heart abnormalities
how do steroids increase cholesterol
increase LDL:HDL ratio
how do many steroid abusers die
cardiac issues - heart attack and stroke
why are steroid users more prone to heart attack and stroke (3)
- more platelet aggregation
- immune cells stick to vessel walls (increase inflammation)
- inhibit synthesis of nitric oxide (vasodilator)
what does steroids do to platelet aggregation
increase
what does steroids do to immune cells
increase inflammation
what does steroids do to nitric oxide
inhibits synthesis
what does steroids do to heart muscle mass
increase
what is the issue with steroids increase to heart muscle mass
it doesnt increase the amount of blood vessels so therefore less oxygen can be delivered
what is roid rage
aggression and anger and rage in users
is roid rage a myth
no
what are other common mental issues associated with roid rage
psychosis and depression and suicide
which users are more prone to aggression and roid rage and stuff
dependent users (63% in dependent and 16% in non dependent)
what is the mechanism of action of steroid cause aggression
modulate GABA-a NMDA and 5HT receptors
how are GABA-a NMDA and 5HT receptors activated by receptors
because there are steroid binding sites on them (normally modulated by “neurosteroids” produced in the brain
what part of the brain is the centre of aggression
anterior hypothalamus
what receptor stimulation in the anterior hypothalamus will result in aggression and violence in animal models
D2 receptor
what does D2 stimulation in the anterior hypothalamus cause
aggression and violence in animal models
what does moderate doses of anabolic steroids in adolescence do to D2 in anterior hypothalamus
increase
where are D2 receptors that are linked to aggression
anterior hypothalamus
what is arginine vasopression (AVP) (excitatory or inhibitory, what does it do to aggression)
excitatory, potentiates aggression
what is serotonin (excitatory or inhibitory, what does it do to aggression)
inhibitory, decreases aggression
what does anabolic steroid exposure do to AVP (arginine vasopression) effects
increase
what does anabolic steroid exposure do to serotonin effects
decrease
what is nandrolone
a steroid
what does chronic nandrolone exposure do to mice
increases aggression
how does nandrolone increase expression
decreases mRNA levels for 5HT receptors in many brain regions (PFC, hypothalamus, hippocampus, amygdala)
what was the most commonly reported effect in steroid users
depression
how do steroids cause depression
decrease BDNF (in rats)
what does DBNF do normally
stimulates neuronal growth in hippocampus
what is cholimipramine
TCA antidepressant
what can reverse depression from steroids
cholimipramine, a TCA antidepressant
what does a decrease in BDNF correlate to
depressed behaviour
do steroids actually increase muscle mass
yes
what is the % increase in baseline strength with steroids
5-20% depending on dose
what do recent animal studies suggest about how steroids increase muscle mass
increase in the number of myonuclei and increased muscle fibre cross-sectional area
what can further increase the muscle mass increase with steroids
muscle overload (working out)
what does acute anabolic steroid exposure do to long lasting muscle
it can lead to long-lasting increase in myonuclei that helps muscles to grow in absense of drug
what are the effects of steroids after 3 weeks
number of myosteroids stay significantly higher
what are the effects of steroids after many weeks of not using and not exercising
cross sectional area fell back to control levels
what are the effects of steroids after many weeks of not using and then 2 weeks of exercise (compared to control)
increase myonuclei and cross sectional area compared to control (maintained advantage in steroid animals despite not taking steroids in weeks)
what % of steroid users become dependent
30%
what is a possible reward symptom of using steroids
euphoria
what is the mechanism of reward in steroids (2)
- increase beta-endorphin levels which can decrease GABA release onto DA neurons in VTA
- modulate GABA-A R that increases DA firing in mesolimbic pathway
what do steroids do to beta endorphins and what is the result with you
increase which decreases GABA release onto dopaminergic neurons in the VTA
what happens when steroids modulate GABA-A receptors
there is an increased firing rate of dopaminergic neurons in the mesolimbic pathway
what do steroids do to GABA release onto DA neurons in VTA
decrease
what do steroids DA neuron firing in mesolimbic pathway
increase