BS2014: Drugs & Sport

Anabolic agents

substances that promote metabolism & synthesis of complex molecules

Endogenous anabolic steroid example

testosterone

The broad effects of testosterone?

• androgenic

• anabolic

Anabolic effect of testosterone

protein building in skeletal muscle and bone

Aims of changing testosterone chemistry

• slow inactivation/metabolism

• increase lipid solubility

• decrease androgenic effects

Exogenous anabolic steroid examples

• nandrolone

• stanozolol

Anabolic:androgenic ratio of different anabolic steroids

• testosterone — 1:1

• nandrolone — 10:1

• stanozolol — 30:1

Which region of the testosterone molecule is changed to increase anabolic activity in derivative drugs?

cyclohexane rings

Morphometric effects of testosterone administration on muscle

• increased muscle volume

• increased cross-sectional area of type I and type II muscle fibres

• increased myonuclear number

What are morphometric changes associated with

• increased protein synthesis

• reduced amino acid export

• increased androgen receptor expression

• fibre hypertrophy → increased strength

• enhanced Ca²⁺ release from SR/increased Ca²⁺ sensitivity of contractile proteins

• increased muscle pennation

Side effects of anabolic steroids

• testicular atrophy

• acne

• oedema

• insomnia

• injection site pain

• stretch marks

• mood alterations

• sexual dysfunction

• gynecomastia

Life-threatening side effects of anabolic steroids

• cardiovascular disease

• liver dysfunction

• cancer

Properties of amphetamines

• CNS stimulant

• psychomotor stimulant

• sympathomimetic

Possible benefits of amphetamines in sport

• increased alertness, self-confidence & concentration

• feeling of increased energy

• reduced fatigue
  

What endogenous substances is amphetamine structurally related to?

monoamine neurotransmitters (e.g. noradrenaline, dopamine)

Metabolic difference between monoamines and amphetamine

• amphetamine is resistant to monoamine oxidase (MAO)

• amphetamine is orally active, unlike monoamines

• amphetamine is not metabolised, but excreted via urine

TAARs

trace amine associated receptors

TAAR agonists

• trace amines

• monoamines

• amphetamines

Acute side effects of amphetamines

• increased heart rate and blood pressure

• insomnia

• agitation

• nausea

• headaches

• hallucinations & paranoia

• distortion of reality & time perception

• death

Chronic side effects of amphetamines

• dyskinesias

• compulsive & repetitive behaviour

• paranoia

• blood vessel and nerve damage/death

Effects of recreational use of amphetamine

• euphoria

• increased confidence

• hyperactivity

• reduces physical and mental fatigue

Side effects of recreational use of amphetamine

• hypertension

• insomnia

• tremors

• psychosis

• reduced GI motility

• anorexia

Clinical uses of amphetamine

• ocular actions

• nasal decongestants

• narcolepsy

• ADHD

• chronic fatigue syndrome

How may amphetamines reduce neurotransmitter reuptake

• inhibition of transporter

• internalisation of transporter