stimulants

anabolic def

build up

androgenic def

promotes male characteristics/development— testosterone

• smth endogenlous given exogenous

why can’t testosterone be given for performance

can;t be given PO

• high first pass metbaolism

where is testosterone synth stimulated from

hypothalamus— FSH/LH

box warnings for testosterone

virlization in kids exposed to gel

• keep out of reach, including clothes exposed to gel

aas ad eff muscoleskeletal

• Premature closing of epiphyseal— growth— plates

• Resulting short stature, growth in young children

aas ad eff lipid/CV

AMI— acute MI

• HF

• CVA— stroke

• HTN

• Sudden cardiac death due to arrhythmia

• Increase in LDL

• Decrease in HDL

ad eff aas endocrine/repro

Decreased LH, FSH

• Acne

• Gynecomastia

• Altered glucose tolerance

• Decreased spermatogenesis

ad eff aas

Personality disorders

• Aggression

• Mood changes, euphoria

• Slow intellectual performance

• Depression

• Paranoia

• Hallucinations

• Auditory

• Tactile

•Increased/decreased libido

• Opioid type drug dependence

• Violence/homicide

male reproductive ad eff of aas

Suppress gonadotropins

• Variable effects on sexual interest

• Breast enlargement

• Testicular/penile atrophy

• May be cocarcinogens for

prostate cancer

• Hypogonadism → depression → suicidality

female repro ad eff aas

Uterine bleeding in postmenopausal women

• Endometrial polyps

• Uterine fibroids

• Thickened endometrium

• Carcinoma

aas prevention for misuse

• education MOST effect

• focus off physical appearance/sports heroes

what is not helpful for aas prevention

drug screening

• water/diuretics can elminate traces

what are two big stimulants misused

ephedrine

caffeine

ephedrine why used?

Used for weight loss, increase energy and concentration

ephedrine what causes

Causes anxiety, panic attacks, HTN, tachycardia, CVA, MI

ephedrine banned by FDA why?

due to CV and CVA risk

caffiene why used

Used to increase energy, endurance and alertness, weight loss

caf ad eff

Causes agitation, HTN, potential for withdrawal

• Arrhythmia and CVA possible in combo with ephedrine

what are the prescription stimulatns

adderal, concerta, ritalin…

does human growth hormone given adogenic side effects

NO

why HGH prescribed?

dwarfism, decreased levels

HGH ad eff

insulin resistance, myopathy, acromegaly-like

effects, HTN, abnormal lipids, cardiomegaly

why HGH taken

increase muscle mass

• not clear if helps performance alone

erythropoietin MOA

Used to increase oxygen-carrying capacity of blood in endurance

athletes

ad eff of erythropoietin

more likely to have clotting

• PE

• MI

• Stroke

• Development of anti-EPO antibodies

beta-blockers why used

Reduce heart rate

• can be VERY STILL-archery

• Reduce signs of nervousness

• Reduces hand tremors

creatine what is it

Protein stored in skeletal muscle that binds phosphate

creatine what used for

increase production of ATP in skeletal muscle

creatine ad eff

Muscle cramps

• Weight gain

• Minor GI upset

• Compartment syndrome (SWOLLEN muscles)

• Muscle cramps

sildenafil brand

viagra

sildenafil MOA /why used

Causes vasodilation, increases oxygenation and exercise capacity

sildenafil ad eff

Headache

• Flushing

• Dyspepsia

• Blurring of vision

• Priapism

sildenafil is it thought to have benefit in sport esp at sea level?

nope no help

energy drinks how much caf contain

100-300 mg caf

what is FDA rec caf for adults

400 mg

max caf for preg

200 mg daily

ad eff of energy drinks

HTN, sleep disturbances, miscarriage, stillbirths, small-for-age infants

why energy drinks mixed with alcohol

Reduced sensation of intoxication

• Reduced sensation of intoxication impairs judgment relative to risky behaviors (e.g., driving)

• Reduced sensation of intoxication induces more alcohol consumption

• you are “drunker than you feel like you are”

are alcohol and energy drink dependance related

YES— usually increased with both

does caf affect OH metabolism

nopers

what does CDC say about mixing OH with caf

says not safe

why diuretics misued

counter fluid retention caused by AAS, decrease total weight, increase muscle defintion

• makes you more “ripped”

diuretics why increase risk of VTE

increase hematocrit bc less water concentration

diuretics what other ad eff from VTE

electrolyte abnormalitieds (hyper or hypokalemia)

why tamoixifen and clomiphene used

Agents taken by males to counteract the estrogenic effects of AAS → preventing gynecomastia

when if tamoxifen normally used

Used mainly in breast cancer— stop estrogen receptor to stop cell growth

Clomiphene why used

used mainly in female infertility due to anovulation

• Binds estrogen receptors, blocking effects

why finasteride used

prevents male pattern baldness, prevents acne from steroid use

what else used for acne

antibiotics, retinoids

HCG what used for

mimics LH

increase testosterone— reverse axis suppression that cause gynecomastia at end of steriod cycle

Levothyroxine and Liothyronine why used for aas

increase metabolism, increase aas ability to boost physical strength

• reduce body fat, higher energy

MOA of cocaine

block presynaptic reuptake in central/PNS

• NE and epi; DA (reward pathway), serotonin

block volt-gated membrane Na channels

• can cause arrhythmias

metabolism of catecholamines

90% metabolized by hydrolysis

• 10% n-demethylated

how long effects of cocaine

1-3 hours (nasal); onset of high 15-30min

how is crack cocaine dif

baking soda and ammonia

• immediate high— lasts 5-20 min

high of cocaine

Euphoria

Alertness

Excitement

Increased energy

Talkativeness/sociability

Decreased appetite/fatigue

Increased confidence, strength and

mental capacity

Emotional liability

Build tolerance easily!

crash after cocaine

Depression

Anxiety

Irritability

Difficulty concentrating

Anhedonia— reduced interest in other activities

Loss of appetite

Increased sleep/exhaustion

Drug cravings begin after crash

recovery

how are salt forms of cocaine used

snorted/iv, not smoked (high melting point)

base cocaine how ingested

easy to smoke bc low melting point

ad eff of chronic cocaine use

stroke risk

reduced attention

insatiable hunger

insmonia

lethargy

soreness, hoarseness

bronchospasm, dyspnea

chest pain

asthma

fever

eosinophilia

rhiorrhea

teeth grinding— bruxism

increased risk of infarction

itching

cardiovascular complications

htn/tachy

angina/MI

arrhthmias

thrombosis/cva

vasospasm

heart failure

accelerate arthrosclerosis risk

cocaine-induced angina/MI effects

Increased blood pressure, heart rate and contractility → 3 MVO2 determinants!

• Vasoconstriction

• Vasospasm of epicardial vessels

• Increased platelet aggregation

• Increased risk of coronary thrombosis

what is typical pt of cocaine-induced MI

white male, 30s, smoker

what is pref drug for cocaine-induced MI

n-dhp ccbs

what drug to AVOID for cocaine-induced MI

beta blockers

what is schedule for cocaine 4 or 10% solution

schedule 2

what is cocaine solution (Rx) used for

topical or local anesthetic

• reduce bleeding in mucous membranes

why cocaine cause heart problems

alpha vasoconstriction WITH increase in SNS tone

methamphetamine MOA

• indirect neurotransmitter— displaces epi, NE, DA, and serotonin

methamphetamine high

The Rush: initial response felt when

smoking or IV

The High or “The Shoulder”: feel

smarter, intensely focused and becomes argumentative

The Binge: urge to maintain the high

Tweaking: when meth no longer

provides a rush or a high

• Depression

• Hallucinations

methamphetamine crash

The Crash: body shuts down

Meth Hangover: starved, dehydrated

• Physical

• Mental

• Emotional

Withdrawal: may persist for up to

three weeks

• Insomnia, hypersomnia

• Appetite changes, depression

• Suicidal ideation

methamphetamine method of use

Smoking: seconds

IM/IV: seconds

Nasal: 5 minutes

Oral: 20 minutes

Rectal

Vaginal

methamphetamine ad eff

Paranoia, agitation, tactile delusions, visual/auditory hallucinations

Increased HR, HTN, hyperthermia

Stroke, cardiac arrhythmias, palpitations, MI

Metabolic acidosis

Seizures

Loss of appetite

Decreased need for sleep

Serious tooth decay/loss

Skin changes

name of Rx methamphetamine

desoxyn (schedule 2)

fda indications for desoxyn (Rx methamphetamine)

• Exogenous obesity

• ADHD

• Narcolepsy (off-label use)

what are the two big Rx stimulants

adderall and ritalin

Dextroamphetamine/amphetamine brand

adderall

Dextroamphetamine/amphetamine MOA

promote release of NE and DA

• block reuptake with catecholamines by competiitve inhibition

Methylphenidate brand

ritalin

Methylphenidate MOA

• Blocks the reuptake of NE and DA into presynaptic neurons

• Stimulate the cerebral cortex and subcortical structures similar to amphetamines

high of adderall/ritalin

• like cocaine but slower onset/longer duration

• Chronic use contributes to schizophrenia & paranoia,

  picking at skin, auditory/visual hallucinations,

  preoccupation with one’s own thoughts

method of consumption of adderall, ritalin

po or injection

• can smoke or snort for rush

ad eff of ritalin/adderall

increase blood pressure/HR

increase breathing rate

decrease blood flow

increased wakefulness

hyperactivity

state of euphoria

dangerous increase in body temp

seizures

heart fail

psychosis

acute management of stimulants: treating agitation s/s

Haloperidol

Benzodiazepines

Olanzapine or risperidone

Dexmedetomidine

Beta-blockers

management of stim HTN s/s

labetalol

ecg

stim management for seizures

benzos

management of stim airway s/s

ventiliation

how treat stim rhabdo s/s

iv fluids

Na Bicarb

long term treatment options for stimulants (rx)

Dexamphetamine: reduced severity of dependence and withdrawal symptoms

• Bupropion: reduced amphetamine use

• Methylphenidate: reduced craving

• Naltrexone: reduced use and craving

• Modafinil: reduced amphetamine use