Types and Forms

The module seeks to give a broad-brush introduction into the subject area, as a result, the types and formulations of different substances are not exhaustive.   This is an area where there is increasing changes as availability grows.

AAS (Anabolic-Androgenic Steroids)

Examples: Testosterone Enanthate, Testosterone Proprionate, Stanazolol, Trenbolone, Boldenone

The most commonplace IPED at our clinic.  Use spans from a minor increase above a normal baseline testosterone for “health and wellbeing/sexual function purposes” all the way to doses that are over ten times the normal recommended dose.

Research was undertaken on AAS during the 80’s and 90’s and whilst short term health consequences are typically understood by users, the long term health consequences in abuse doses are still emerging.

AAS can be injectable or oral.  Oral formulations tend to place a heavy burden on the liver due to their metabolism.  Whilst use of oral anabolic steroids have declined in service users accessing our clinics, use remains high, especially amongst women who perceive them to have fewer masculinising features.

Anabolic-Androgenic Steroids are purported to be used for a variety of intended benefits, the table below explains how this is believed to occur⁽¹⁾: 

1. Effect on muscle tissue	Increase in lean muscle mass and muscle synthesis
2. Effect on Receptors	Upregulation of androgen receptors
3. Anti-catabolic effects	Suspected to be from androgen binding to glucocorticoid receptors
4. Growth Hormone secretion	Androgen-induced stimulation of GH secretion is believed to be augment the anabolic effect of testosterone
5. Complimentary effects with training	Exercise plus testosterone supplementation showed clearly that effects of testosterone and resistance exercise were additive, compared to exercise or testosterone in isolation.
6. CNS effects	Studies showed that respondents expressed improved euphoria, energy, and sexual arousal with AAS usage

Human Growth Hormone

Whilst evidence supporting usage is somewhat mixed, Human Growth Hormone has received widespread popularity in sport.  In recent years, becoming widely more available through recombinant technology.   HGH is prescribed outside of the UK for the purposes of longevity or injury recovery, but again, evidence supporting this use is limited.

Studies have shown increased whole body protein and muscle protein synthesis, reduction in muscle degradation via IGF-1 mediation and also lipolysis 2-3 hours following injection. ⁽²⁾

One of the higher price items in an IPED cycle.  Outlay for recombinant Human Growth Hormone can stretch to several hundred pounds per month.

Aromatase Inhibitors

Anastrozole (Arimidex) / Exemestane (Aromasin) / Letrozole (Femara)

Aromatase inhibitors (AI’s), traditionally used in conditions such as breast cancer, reduce the conversion of testosterone to oestrogen.  Often used as an IPED as supplementary item when taking anabolic steroids, they are intended to reduce high concentrations of oestrogen resulting from aromatisation of endogenous testosterone. 

Aromatase inhibitors are often taken with the intention to prevent gynaecomastia (breast tissue development) in male IPED users.  Evidence for their use is limited.  Development of gynaecomastia appears to be more complex than simple increased oestrogen concentrations, as some users never develop gynaecomastia, despite heavy use of injectable testosterone.  Two individual case studies have shown that following cessation of testosterone replacement therapy, patients commenced on a aromatase inhibitor for several weeks prior to resuming testosterone replacement therapy⁽³⁾ have a reduced incidence of developing gynaecomastia, however, larger studies have shown that aromatase inhibitors, solely, does not prevent gynaecomastia, especially in younger males who may have a pubertal predisposition to development of gynaecomastia.⁽⁴⁾

It should be noted that AI’s vary in strength and Letrozole being significantly more potent than Anastrazole. Such intense suppression of aromatisation could lead to very low level of oestrogens, which can affect bone quality, have consequences for cardiovascular health and sexual function.⁽⁵⁾

Triiodothyronine (T3)

Used historically as a weight loss medication, this thyroid hormone increases basal metabolic rate in part by increasing heart rate and force of contraction, amongst other biochemical processes.⁽⁶⁾  Used by IPED users to metabolise fat.  Side-effects are similar to thyrotoxicosis: tremor, heat intolerance, thinning hair, anxiety, palpitations. 

Clenbuterol

An increasingly popular veterinary medicine, still licensed for human use outside of the UK.  A potent beta-agonist, in the same family as salbutamol.  This drug has gained widespread popularity as it has both purported anabolic and lipolytic properties.  That is, it builds muscle and burns fat.  In addition to this, it may have a role in improving sporting performance.⁽⁷⁾

Fat loss is likely a result of increased basal metabolic action from increased cardiac and respiratory rate, however the mechanism for muscle hypertrophy is not clear.  Studies suggest that rapid, perhaps direct, inhibitory effect on protein degradation. Therefore the growth-promoting effect of clenbuterol may be specific to muscle and act in a novel manner, therefore it is anti-catabolic, rather than anabolic in nature.⁽⁸⁾

Side-effects include tachypnoea, hypokalaemia, hyperglycaemia, ST changes on ECG, elevated troponin, elevated creatine kinase (CK), palpitations, chest pain, and tremor. Recorded cases of myocardial injury have been documented with this drug. ⁽⁷⁾

Human Growth Hormone Secretagogues (GHS) or “Peptides”

HGH fragment 176-191, 191aa (many)

These are biologically active synthetic peptides which are structurally related to a region within human growth hormone.  Some studies show the role of these compounds in raising Growth Hormone levels.⁽⁹⁾  Although due to the relatively emerging use, long term data is needed on safety and efficacy, including mortality and cancer incidence. ⁽¹⁰⁾

Insulin

A potent anabolic for both muscle tissue and fat.  It decreases the rate of lipolysis in adipose tissue, stimulates fatty acid synthesis in tissues, it increases the uptake of triglycerides from the blood into adipose tissue.  In addition to this, increases transport of amino acids into tissues and it decreases the rate of protein degradation in muscle. ⁽¹¹⁾

In sport, especially powerlifting and bodybuilding, regular administration of short acting insulin with short acting carbohydrates is intended to increase muscle bulk by reducing protein degradation and increase glycogen storage for performance.   It has been established that insulin-treated patients with diabetes have an increase in lean body mass when compared with matched controls.  ⁽¹²⁾

Associated Drugs  

Isotretinoin/Differin/Adapalene

Oral or topical use – used to combat dermatological side effects of acne from Anabolic Steroids.

Sildenafil/Tadalafil

Oral use – Used to combat erectile dysfunction during or following a cycle

Modafinil

Oral use – Used as a stimulant to encourage improvements in workout performance, combat fatigue as a nootropic or to combat sleep apnoea in individuals with a very high muscle bulk

Di-nitro-phenol (DNP)

Oral use – Used as a “fat burner”.  Substance is highly toxic (as per Toxbase)

Incretin Mimetics (E.g. Semaglutide/Liraglutide)

Injectable - Used to suppress appetite for the purposes of fat loss

EPO (erythropoietin)

Injectable

First developed for patients with anaemia and chronic kidney disease. It exists physiologically to upregulate the number of red blood cells (RBCs) produced by the bone marrow when oxygen concentration in tissues is decreasing⁽¹³⁾. This decrease in oxygen concentration is recognised by Hypoxic Induced Factors (HIFs) which bind to EPO to activate it ⁽¹⁴⁾. The use of EPO in a sporting context is most famous for its role in cycling scandals. EPO is favoured more commonly in sports with a higher aerobic content (e.g. long distance running, cycling, cross-country skiing, etc.)⁽¹⁵⁾.

Risks associated with EPO use are twofold; the effects of supraphysiological doses of EPO and the risks associated with needle use and injections.

Common risks⁽¹⁶⁾ include:

• Hypertension
• Pulmonary embolism
• Myocardial infarction
• Stroke

Stimulants

Stimulants make up some of the oldest of the techniques used to gain a competitive advantage in sport. Whilst the category is fairly broad for what is considered a stimulant, common drugs used in a doping context include

Amphetamine/Dexamphetamine/Methamphetamine/Cocaine/Ephedrine

These drugs can have multiple effects, but they stimulate the central nervous system in three main ways⁽¹⁷⁾

1. To increase the release of certain neurotransmitters e.g. dopamine, noradrenaline and serotonin
2. Directly stimulating post-synaptic neurons
3. Inhibiting neurotransmitter reuptake

The theory behind taking stimulants is to increase aggression, alertness and competitiveness, and have been used both in competition and training to maximise effort and intensity. They can also increase muscular strength and endurance⁽¹⁸⁾. The table below explains possible side-effects of these stimulants, if unfamiliar. 

Amphetamines	Cocaine	Ephedrine
Confusion/Delirium	Agitation/Irritability	Headache
Sweating	Sudden Cardiac Death	Dizziness
Palpitations	Seizures	Irritability
Hypertension	Respiratory arrest	Anxiety
Tachycardia	Cardiac arrest	Tremor
Tremors		Respiratory Difficulties
Muscle/Joint Pain		Convulsions
Cardiac Arrest		Arrhythmias

 

Post-Cycle Therapy (PCT)

A post cycle therapy is usually a drug or series of drugs used in the belief it will restore normal function of the HPA (or speed recovery) following HPA suppression from endogenous testosterone use.

Human Chorionic Gonadatrophin (hCG)

Studies have demonstrated increase in testicular volume and testosterone production in pre-pubertal males.^(19,20)  Other studies have shown efficacy of hCG use in anabolic steroid induced hypogonadism in recovery of Leydig cell function, even from chronic use of anabolic steroids ^{(21, 22, 23)}.  Evidence also shows it has use for improving subfertility following prolonged suppression with anabolic steroids.⁽²⁴⁾

Therefore its use in recovery following extensive AAS usage is promising, however, whilst this practice may be being undertaken by IPED users, as a clinic, we are currently not aware of a clinical setting where this is being offered to IPED users.

Tamoxifen

Used during a cycle or during PCT, traditionally to prevent gynaecomastia⁽²⁵⁾ which may be seen with aromatisation of testosterone and reciprocal rises in oestrogen.  However evidence is limited, some cases studies do demonstrate its effectiveness is in reducing gynecomastia⁽²⁶⁾, however some studies suggest inferiority compared to aromatase inhibitors for this action.

It should be noted that usage can cause liver damage⁽²⁷⁾ in longer term use and patients should be counselled on this accordingly.

Clomiphene

Widely used for the purposes of restoring function of normal testosterone production. Studies demonstrate elevation in LH, FSH, and total and free testosterone levels in response to clomiphene citrate⁽²⁸⁾ which explains the rationale as to why many IPED users take this in recovery phase.  Users of AAS for greater than one year may benefit from short term treatment with Clomiphene ⁽²⁹⁾.

Evidence for effective and safe withdrawal of AAS and the management of this withdrawal remains poor and at the time of publishing, we are not aware of any consensus guidelines or a framework with which to approach medical, i.e, non-psychological, rehabilitation.

 

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