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#Post#: 1207--------------------------------------------------
Tadalafil Not Just for Erections
By: Road2HardCoreIron Date: October 20, 2022, 4:45 am
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HTML https://themenshealthclinic.co.uk/trt-tadalafil-its-not-just-about-erections/
TRT & Tadalafil – It’s Not Just About Erections!
Tadalafil is a drug commonly discussed in the world of
Testosterone Replacement Therapy (TRT). It is a medication
that’s primary use is within the realms of erectile dysfunction,
which you’ve probably have heard of before by it’s more commonly
known brand name ‘Cialis’. In the context of TRT however, our
primary use of this drug is not really for erectile dysfunction,
but that is not to say that this is not a positive benefit that
is observed when using it. Let’s take a deeper look at
Tadalafil and its role in TRT.
What Exactly is Tadalafil?
Tadalafil is a medication which comes under the class of
selective PDE 5 inhibitors. It is in the same class of drug as a
much more commonly known drug used for erectile dysfunction
named ‘Sildenafil’, more commonly known as ‘Viagra’, which most
people have heard of.
How Does it Work?
To understand that we need to dig into biochemistry to
understand the physiology.
PDE 5 stands for Phosphodiesterase 5. What is PDE5? PDE5 is an
enzyme that is found within the walls of blood vessels and its
role is to affect blood flow and cell signalling. It inhibits
Cyclic Guanosine Monophosphate or cGMP. cGMP is a very common
cell signalling substance that regulates ion channel conductance
[1]. This inhibition causes a relaxation of blood vessels which
increases blood flow, we call that in medical terms
vasodilation.
Now whilst we are on the subject of the pharmacology of
tadalafil we need to talk about its safe use. Tadalafil is a
prescription only medication that should only ever be taken when
provided by a qualified prescribing clinician. One of the main
reasons for this is that nearly all medications are subjected to
metabolism via what is known as the P450 Cytochrome system. This
is a group of enzymes that play a role on the breakdown of
medications through the liver [2]. Tadalafil specifically
interacts with CYP3A4 a specific enzyme within the P450
cytochrome. Now this system can be inhibited and induced by
certain medications. So Tadalafil must be prescribed with
caution alongside any other medication that may cause inhibition
or inducement of the P450 cytochrome. For example, Tadalafil
should be administered with caution alongside Nitrate
medications, however these are not as commonly used nowadays
outside of specialist cardiac care. Its concurrent
administration with more common medications such as the
antibiotics erythromycin and clarithromycin which are both
CYP3A4 inhibitors as are grapefruit juice and Naringenin
supplements and these will increase the plasma concentration
levels of tadalafil up to 2-4 fold.
Equally, certain epilepsy medications such as phenytoin,
phenobarbital and carbamazepine should be avoided as these are
CYP3A4 inducers and may reduce plasma concentration levels of
tadalafil by up to 88% and therefore reduce the efficacy [3].
What Are the Benefits of Using Tadalafil as Part of Your TRT
Protocol?
The first and most obvious benefit would be the alleviation of
erectile dysfunction which is commonly seen in those with
testosterone deficiency. However, if we think back to the
mechanism of action, the vasodilation is not restricted to the
corpus cavernosum, which is the erectile tissue found within the
penis. The vasodilatory effect can be found in other tissues
such as the smooth muscle of the prostate and bladder which is
beneficial to those suffering with benign prostatic hyperplasia
or more simply an enlarged prostate not secondary to a sinister
pathology [4]. This vasodilatory effect also effects skeletal
muscle, visceral smooth muscle and also to a lesser degree
cardiac muscle, kidneys and the liver. Although, these
aforementioned organs primarily utilise PDE1, 2 and 4 for their
particular cell signalling purposes [5].
Another benefit of its use is reduction in blood pressure. This
is interesting as the studies that have been conducted in a
controlled environment do not seem to replicate this effect [6].
However, it is something that a lot of our patients have
reported and commensurately has been observed in the clinic’s
patients.
Interestingly there is evidence in the literature that supports
one of the main benefits that we here at TMHC utilise this
medication for, and that is a reduction of serum oestradiol
levels [7]. Again, this is something THMC have observed in
clinical practice and the limited studies around this topic do
demonstrate this effect. The caveat from the evidence base
around this particular effect is that in one 2016 study by
Aversa et al [8] the reduction in oestradiol levels was
primarily observed in those without excess central adiposity,
i.e.. men with a healthy lean muscle mass. This particular
application of Tadalafil can sometimes mean the difference
between requirement for aromatase inhibitor medication and not.
So, that’s further motivation to moderate your diet and
exercise.
On the subject of weight management, those patients on TRT who
do regular resistance training may also see an additional
benefit in reduced muscle soreness and reduced recovery time due
to the increased blood flow to the muscle groups being stressed
during training [9].
Finally, another useful benefit that Tadalafil confers is
demonstrated in a 2010 study by Foresta et al [10] that showed
that Tadalafil has a positive effect on vascular endothelial
cell regeneration by increasing the amount of endothelial
progenitor cells and CXCR4 expression which is linked to the
cGMP cellular messenger system resulting in improved repair of
vascular damage. Put more simply it helps to improve the repair
and recovery of the lining of blood vessel walls thus improving
cardiovascular health and longevity.
Dosing?
Tadalafil has a half-life of between 17-21 hours and a peak
plasma concentration time or cMax of approximately 2 hours. So
stable serum concentration levels can be achieved quite quickly
on a daily dosing regimen. Now, if we were to use Tadalafil for
its primary clinical indication of erectile dysfunction you
would look to utilise a dose of 10 to 20mg. As many will know,
at the men’s health clinic we focus on balance and stability, so
we are advocates of microdosing to give stable serum
concentration levels. As has been mentioned before we subscribe
to daily microdosing of testosterone cypionate and HCG and when
it comes to Tadalafil we are no different. We use a dose of
between 2.5 to 5mg daily via oral administration and will
titrate that dose to the desired effect.
Are There Any Side Effects?
As with all medications there will always be a list of side
effects. The most common reported side effects when using
Tadalafil are:
Headache
Back pain
Dyspepsia (so acid reflux/indigestion)
Facial flushing
Nasal congestion
Anecdotally in our clinical experience, these side effects tend
to settle between weeks 2-6 on a daily microdosing regimen. If
the dyspepsia or acid reflux does not settle, you can first look
to moderate your diet and if there is still no relief, you can
approach your GP about medications that can help with this.
Summary
To summarise, the benefits of using tadalafil in a microdosing
manner alongside TRT are:
Relief of erectile dysfunction symptoms
Relief of symptoms associated with benign prostatic hyperplasia
Blood pressure modulation
Oestradiol modulation
Increased cardiovascular health through endothelial cell
regeneration
The potential for reduced muscle soreness and reduced recovery
time post resistance training.
In conclusion, Tadalafil is not all about erections. It has
many other befits alongside a well-balanced TRT protocol.
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