49 contest prep fat loss agents part 3 yohimbine

UNIVERSITY

Contest Prep
PEDs Fat Loss Agents:
Part 3 Yohimbine and Fat
Loss Summary


Lesson Overview Contest Prep Fat Loss Agents
PART 1 THYROID HORMONES
• PED deployment overview
• Mechanism of action
• How are thyroid hormones regulated
• Symptoms of hypothyroidism and lab interpretation
• Safety of use
• Contest prep effects on thyroid
• Thyroid protocols for contest prep
PART 2 CLENBUTEROL
• Mechanism of action
• Skeletal muscle anabolism
• Clenbuterol as a fat loss agent
• Managing clenbuterol side effects and safety
• Clenbuterol protocol for contest prep
PART 3 YOHIMBINE HCl
• Mechanism of action
• Yohimbine impact on adipose and skeletal muscle
• Caffeine synergy
• Gender differences
• Side effects and safety
• Yohimbine protocol for contest prep
• Summary of Fat loss Agent in Contest Prep

• Timing of Compounds for Contest Prep


Yohimbine HCl
What is it ?
Naturally occurring alkaloid found in the yohimbe tree
Alpha 2 receptor antagonist
2 main forms found in supplements:
Yohimbe bark extract
Concentrated powder of bark, with components of Yohimbine
Yohimbine HCl
Extracted Yohimbine molecule combined with a hydrochloric acid
group


Mechanisms of Action
Beta 2 receptor activation increases lipolysis
Alpha-2 receptor activation prevents lipolysis
Yohimbine is an Alpha-2 receptor antagonist
Physiological Effects:
• Elevates serum Free fatty acids (FFA), glycerol and norepinephrine
• Potentiates exercise induced FFA and norepinephrine release during and
following exercise
• In subject ingesting yohimbine prior to 30min cardio, FFA levels 30 min post
exercise were doubled (Galitsky 1988)
3 main mechanisms:
1. Central activation of sympathetic tone (main action on beta receptors)
2. Interference with the feedback mechanism whereby pre-synaptic Alpha-2
adrenoreceptors suppress further release of norepinephrine from
sympathetic neurons

3. Blockade of adipocyte alpha-2 adrenoreceptor that suppress lipolysis
1.

These receptors activate Gi proteins that inhibit adenyl cyclase, thus antagonizing the ability of
beta-adrenoreceptors to boost cAMP generation

Appetite suppression seen in mice studies; however, dosing was far higher than
that found in human literature (Callahan 1984)


Magnitude of Effect
Yohimbine: The Effects on Body Composition and Exercise Performance
in Soccer Players. Research in Sports Medicine: An International
Journal (Ostojic 2006)
• 20mg per day for 21 days, 20 male soccer players
• %body fat, 9.3 vs 7.1 in yohimbe group before and after
• %body fat yohimbine vs control, 7.1 vs 9.2
• No alteration in muscle mass or performance indicators


Caffeine Synergy
• Potentiate norepinephrine release
• Caffeine has Alpha-1 receptor antagonism preventing inhibition of
further sympathetic norepinephrine release
• Yohimbine with its alpha-2 receptor antagonism also prevents
inhibition of further sympathetic norepinephrine release
• Blockade of 1 receptor (alpha 1 or 2) can upregulate the other,
decrease sympathetic Norepi release
• Taking caffeine and yohimbine together synergistically will allow full
action of yohimbine on norepinephrine release (mark 2002)

Male vs Female Differences
Greater expression of alpha-2 adrenoreceptors on the gynoid
adipocytes of women could make them more responsive to yohimbine
therapy
Gynoid deposits (gluteofemoral subQ adipocytes) “Stubborn” glute
and thigh body fat.
In a study with obese women on a 4-week very low-calorie diet
• 14 of the women with greatest weight loss classified as “rapid losers”
• others subjects termed “slow” losers.
• Metabolic properties of the adipocytes between groups showed
similar beta receptor response, but the slow group was 10x more
sensitive to alpha-2 receptor agonist (Hellstrom, 1997)


Safety
• Human FDA approved for treatment of erectile dysfunction (5.4mg 13x per day)
• In dosing for erectile dysfunction (5.4mg 3x per day) nausea,
abdominal pian, dizziness, nervousness
• Moderate doses do not produce anxiety or insomnia (McCarty 2002)
• Single 15-20mg dose can cause tachycardia and hypertension
• Can increase anxiety and panic attacks
• Deaths have occurred in extreme dosing levels

• 1 case study: 37year old BBer, 5g ingestion loss of consciousness and seizure
BP 259/107, acute neurotoxicity (Giampreti 2009)
• 2 cases studies of death occurring (Anderson 2013)

Yohimbine Considerations and
Implementation
Considerations
• During a fed state lipolytic action is completely suppressed (Galitzky 1988)
• Can potentiate insulin response combined with carbohydrate
• Peak levels in 30-60 min, and sustained for 3-4 hours (Berlan 1991)
• During fasting state increased FFA, in fed state may increase insulin response and
insulin resistance
• Chronic administration of 12mg daily for 14 days, acute lipolytic action was
blunted, but still occurred (Berlan 1991)
• Upregulation of alpha-2 receptors is possible with frequent and chronic dosing,
single daily dosing less likely to cause upregulation of Alpha 2 receptors
• 0.2mg/kg of body weight studied effective dose, taper up to this dosage
Summary for usage:
Yohimbine HCl 0.2mg/kg
Fasted single dose 30 min prior to cardio
Delay meal for 1-2 hour post cardio session
Combine with caffeine for added synergy
No tapering off dosage needed
Can be implemented last 6 weeks of prep for ”stubborn” body fat, especially females


Summary of Fat Loss Agents Synergy in Prep
Use Multiple Pathways for fat loss
• Anabolic Androgenic Steroids: Beta 2 receptor sensitivity and density
• Anabolic (test/primo) and Anticatabolic Compound (trenbolone)

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•
•

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•
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Growth Hormone: increased FFA mobilization
Beta 2 Agonist (Clenbuterol): increased adipose lipolysis
Alpha-2 Antagonist (Yohimbine HCl): blockade of anti-lipolytic agents
Catecholamines (caffeine): Increase BMR, norepinephrine
Thyroid Hormone (Cytomel T3): Increased BMR
PPAR Agonist (Telmisartan): gene regulator of lipid and glucose
metabolism
• Glucose Disposal Agent (Metformin and Berberine): CHO absorption
blocking and increased glucose partitioning


Timing of Compounds for Contest Prep
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Remember caloric restriction is primary tool for fat loss
Impl ement each fat l oss tool ”as needed”
You Do NOT need all components
You Do NOT i mplement all a gents a t same i tem a nd top dosage
Get the MOST from the LEAST

Hypothetical Timing of Fat loss Agents:
At Bedtime

Metformi n 500mg (6-hour half life)
Upon Wa king
T3 ba s ed on labs (~15-25mcg) (2.5 day half-life, timing irrelevant, need fasted)

Cl enbuterol (20-80mcg) (half l ife 34 hours, ti ming i rrelevant)
1 hour pri or to fasted ca rdio
1.5-2IU GH (1–2-hour peak concentration)

Yohi mbine HCl (0.2mg/kg)
Ca ffeine (100-200mg)
Fa s ted Ca rdio Session (water only)
1-2 hours post cardio
Mea l 1
Tel misartan (20-80mg based on needs) (15 hour half life)


References: Yohimbine
Galitzky J., Taouis M., Berlan M., Riviere D., Garrigues M., Lafontan M. Alpha 2-antagonist compounds and lipid
mobilization: evidence for a lipid mobilizing effect of oral yohimbine in healthy male volunteers. Eur J Clin
Invest 1988; IV: 587±594.
Mark F. McCarty (2002). Pre-exercise administration of yohimbine may enhance the efficacy of exercise training
as a fat loss strategy by boosting lipolysis. , 58(6), 0–495. doi:10.1054/mehy.2001.1459
Berlan M., Galitzky J., Riviere D. et al. Plasma catecholamine levels and lipid mobilization induced by yohimbine
in obese and non- obese women. Int J Obes 1991; IS: 305±315
Hellstrom L., Rossner S., Hagstrom-Toft E., Reynisdottir S. Lipolytic catecholamine resistance linked to alpha 2adrenoceptor sensitivity ± a metabolic predictor of weight loss in obese subjects. Int J Obes Relat Metab Disord
1997; PI: 314±320.
Callahan MF, Beales M, Oltmans GA. Yohimbine and rauwolscine reduce food intake of genetically obese
(obob) and lean mice. Pharmacol Biochem Behav. 1984 Apr;20(4):591-9. doi: 10.1016/0091-3057(84)90309-5.
PMID: 6145164.

Colin Anderson, Dan Anderson, Nicole Harre, Norman Wade, Case Study: Two Fatal Case Reports of Acute
Yohimbine Intoxication, Journal of Analytical Toxicology, Volume 37, Issue 8, October 2013, Pages 611–
614, />Giampreti A, Lonati D, Locatelli C, Rocchi L, Campailla MT. Acute neurotoxicity after yohimbine ingestion by a
body builder. Clinical Toxicology. 2009;47(8):827–829. />Ostojic, Sergej (2006). Yohimbine: The Effects on Body Composition and Exercise Performance in Soccer Players.
Research in Sports Medicine: An International Journal, 14(4), 289–299.doi:10.1080/15438620600987106