Hi my name is isa valente and i am a current 30 year animal science transfer and in this video i will be discussing the pharmacological properties of pseudoephedrine from the television show make-it-or-break-it on the last episode of make-it-or-break-it the morning of the 2012 olympic trials a young female gymnast tested positive for the presence of the banned
Substance pseudoephedrine in her urine a jealous team a days leading up to the trials had been secretly giving this gymnast fruit smoothies mixed with pseudoephedrine every morning in hopes of securing a spot on the olympic team the gymnast was prohibited from competing at the olympic trials pseudoephedrine is known to be used by athletes as a performance aid in
This presentation the physicochemical properties pharmacokinetics and pharmacodynamics of pseudoephedrine will be discussed to support or oppose the effect pseudoephedrine can elicit on an elite level athlete training for the olympics pseudoephedrine naturally occurs any feature appliance and has been used in traditional eastern medicine since 1889 pseudoephedrine
Is a sim pathogenetic amine used for its nasal and sinus decongestant activity it has the capability to improve airflow and relieve nasal blockage in viral upper respiratory tract infections pseudoephedrine has many physical chemical properties for example pseudoephedrine is a weak base with the pka of 10.25 it has a molecular weight of a hundred and sixty-five
Point twenty three grams per mole it is six point six plus three minus 0.4 percent bound to human serum albumin and has a lipid water partition coefficient of zero point eighty nine indicating pseudoephedrine to be more soluble in octanol than water due to its lipophilic character it has a half-life of six hours at urinary ph of five and a half-life of 16 hours at
Urinary ph of eight lastly it has a volume of distribution of 2.6 to 3.3 liters per kilogram indicating that it is largely confined to plasma pseudoephedrine is primarily administered orally in tablet form the average adult may take a sixty milligram tablet every four to six hours a hundred and twenty milligram tablet every 12 hours or 240 milligrams tablet once
Daily pseudoephedrine is mainly absorbed in the gastrointestinal tract following oral and administration we will now discuss the pharmacokinetics and pharmacodynamics of pseudoephedrine once pseudoephedrine is ingested orally it’ll pass through various organs in the body before it is metabolized it will pass through the stomach small intestine veins of mesentery
Portal vein and then the liver in the liver pseudoephedrine will undergo first pass metabolism where air will begin to be metabolized pseudoephedrine is incompletely metabolized in the liver less than 1% will be nd methylated to an inactive metabolite via phase one metabolism the majority of pseudoephedrine is eliminated unmetabolized by the kidney in the urine
Typically 55 to 75 percent of an oral dose is detected in the urine as unaltered pseudoephedrine pseudoephedrine acts as an agonist that mainly binds to alpha adrenergic receptors and beta adrenergic receptors in the mucosa of the respiratory tract and stimulates the sympathetic nervous system the alpha adrenergic receptor is a gq g-protein coupled receptor that
Naturally binds to nor per nephron and epinephrine that are typically produced by the body the binding of pseudoephedrine to the alpha adrenergic receptor activates the gq alpha subunit and allows you to move and activate phospholipase c the activated phospholipase c cleaves pip to causing an increase in ip3 and dag ip3 binds to its respective binding site our
Calcium ion channels of the endoplasmic reticulum and sarcoplasmic reticulum increasing cytoplasmic calcium the cytoplasmic calcium ions triggers the contraction of smooth muscle causing vascular constriction of the blood vessels which aid as a decongestant the sympathomimetic effects of pseudoephedrine promotes vascular constriction of cutaneous blood vessels
Vasodilation of the skeletal muscles and a redistribution of blood from the skin and portions of the splink neck bed to the skeletal muscles and brain the oral ld50 of pseudoephedrine is 2206 milligrams per kilogram in rats and 726 milligrams per kilograms and mice patients who experience pseudoephedrine overdose may show signs of giddiness nausea vomiting sweating
And muscle weakness four times the single therapeutic dose of about 240 milligrams is required to cause an increase in diastolic blood pressure above 90 millimeters of mercury in normotensive human subjects pseudoephedrine has been on the international olympic committee’s list of banned substances for many years and is assumed to be because of how easily it is
Converted into mithya and feta mien and its ability to mimic the sympathetic nervous system findings from a randomized double-blind crossover study indicated that 22 healthy males ingested a hundred and eighty milligrams of pseudoephedrine 45 minutes prior to exercising and showed greater torque in the extension higher heart rate following a 30 second cycle sprint
And the expiration of more air per rath in an anaerobic setting there were no significant differences detected and strength endurance or upper-body benchpress tasks an increased heart rate and vascular tone may increase cardiac output which can send more supply to contracting muscles findings from a placebo control study indicated no significant effect on the times
Of an 800-meter run for female college athletes pseudoephedrine can improve lung function and lower body strength and power however the small increase in performance is outweighed by the risks an individual is most likely to encounter when ingesting high dosages of pseudoephedrine in the show the total amount of pseudoephedrine consumed was not mentioned however
The gymnast did consume pseudoephedrine for a couple of days so the effects of the drug could have been sustained therefore i strongly believe that the 16 year old gymnast could have potentially enhanced her short-term maximal exercise performance but would have most likely negatively experienced dizziness headache nervousness and cardiovascular effects simultaneously
In conclusion pseudoephedrine has stimulatory properties in the central nervous system bronchodilation and vascular constrictive properties when taking in doses of 60 milligrams three to four times per day it’s similar chemical nature to n feta means allows it to cause an increase in systolic and diastolic blood pressure heart rate peripheral vascular tone and
Respiratory stimulation the adverse side effects are greater than the enhancements therefore this drug may be banned not for its benefits but to discourage this type of drug doping if you found this video interesting and wants to learn more i have provided the references down below and encourage you to take some time to read through them thank you for watching
And a big thank you to professor kucera and the tas for a wonderful quarter
Transcribed from video
VMB 101Y Spring 2020 Isai Valente, Pharmacological Effects of Pseudoephedrine in Olympic Athletes By Isai Valente
