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Tadalafil Citrate Explored ~ a closer look at Cialis
by Mike Arnold
With drug-based performance enhancement now being utilized for a multitude of purposes in nearly every sector of society, the idea that one can gain an advantage through pharmaceutical assistance is no longer looked down upon like it once was. With this growing social acceptance, the stigma attached to the use of ED drugs has diminished significantly. No longer viewed solely as a treatment for ED, they are now being used with ever greater frequency to improve sexual potency in otherwise healthy men. While frowned upon by the medical establishment, the truth is that these drugs are equally safe in both populations, helping the impotent to restore their sexual prowess and the adequate to achieve a degree of performance beyond the norm.
In the BB’ing community, both are valid concerns, as AAS can act as either sexual superchargers or as impotence promoting drugs, depending on the steroid employed and the user’s personal response. Both trenbolone and nandrolone are known to decrease libido and impair sexual functioning with extended use, most often as a result of elevated prolactin levels. Although this problem can generally be rectified with anti-prolactin drugs, they can sometimes take weeks to reach full effectiveness, while PDE-5 inhibitors (ED drugs) provide a rapid-acting alternative capable of producing near immediate results.
Regardless of the intended application, the addition of a PED-5 inhibitor confers benefits that cannot be obtained elsewhere. Whether you are trying to overcome the negative effects of AAS on sexual performance or morph into a virtual sexual dynamo, PED-5 inhibitors can assist you with your goal.
What is Cialis and how does it Work?
The invention of PED-5 inhibitors for the treatment of erectile dysfunction came about more as an accident rather than a planned attempt to cure the ailment. The story goes back to 1994, when GlaxoSmithKline discovered that their prospective heart medication, sildenafil (most commonly known as Viagra), demonstrated strong erection promoting effects in test subjects. This revelation led the company to terminate all further testing of sildenafil as a heart medication and to initiate a new round of clinical trials designed to evaluate the drug as a treatment for erectile dysfunction. By 1998 Viagra had gained FDA approval and was released onto the market with no small amount of fanfare. After netting sales exceeding 1 billion dollars and with GlaxoSmithKline holding a virtual monopoly on the treatment of this condition, other companies took notice and quickly began testing their own versions of PED-5 inhibitors.
Following the massive success of Viagra in 1998, Eli Lilly began clinical testing for tadalafil that same year and by 2003, FDA approval was granted. Marketed under the brand name Cialis, it held distinct advantages over the competition (which now included both Viagra and Levitra), that helped differentiate it from its peers and gain market share.
In 2008, Eli Lilly sold the exclusive rights to commercialize tadalafil for pulmonary arterial hypertension to United Therapeutics. Gaining FDA approval in 2009 for this purpose and sold under the brand name Adcirca, it is the first and so far only PED-5 inhibitor to be sold as a heart medication—the original reason PED-5 research began. A couple years later, in 2011, tadalafil was granted FDA approval for a third use—to treat the signs and symptoms of benign prostatic hyperplasia.
Although many of these drugs are now household names, only a small percentage of people understand how PDE-5 (phosphodiesterase type 5 enzyme) inhibitors actually work. However, before we can answer this question in a way that is easy to comprehend, we must first understand how the body produces an erection. During arousal, nitric oxide is released from the synapses of neurons in the corpus cavernosum of the penis. This results in an accumulation of cGMP (cyclic guanosine monophosphate) and the subsequent relaxation of smooth muscle, allowing an erection to take place.
The mechanism by which these drugs work is fairly simple. Post-ingestion, tadalafil enters the bloodstream and makes its way to the penis, where it prevents the breakdown of cGMP, allowing for an enhanced and sustained erection. Regardless of which PED-5 inhibitor we are referring to, all work through this same basic mechanism of action. For many, the resultant effect is so powerful that even those with severe ED issues are often able to achieve a normal level of functioning, while those with normal function frequently experience the ability to engage in long-lasting, repeated bouts of sexual intercourse in a single session.
Additional Benefits of Cialis
Although all PDE-5 inhibitors do the same basic job, each one is different in its pharmacodynamics (i.e. how a drug affects the body). Depending on the individual’s needs and circumstances, these differences often determine which treatment option is preferred. Compared to the other two candidates (Viagra & Levitra), which are similar in action and effect, tadalafil is somewhat unique; possessing characteristics which set it apart from the competition.
The first of these is its duration of action. Unlike the other PDE-5 inhibitors, which are only effective for about 4-6 hours, tadalafil continues to maintain its effectiveness for an extended period of time. With an active life approaching 36 hours, it has come to be known as the “weekender”. Aside from not needing to administer the drug as frequently, there are other benefits attached to this defining characteristic, particularly in the area of spontaneity. Nothing can kill the mood faster (at least for a woman) than putting things on hold for 30-60 minutes while you pop a pill and wait for it to take effect. With tadalafil, one can take the medication earlier in the day, long before sexual activity is anticipated, and ensure that you are at the top of your game should luck go your way. This is especially important for the non-married—or for those looking for prospective mates at bars or other social gatherings. Even for married couples, the loss of spontaneity can be an issue, so regardless of which situation you find yourself in, tadalafil’s long duration of action is a significant benefit.
Another characteristic associated with tadalafil, which is appreciated by many users, is its greater degree of tolerability. Quite simply, tadalafil is more pleasant to take than drugs like Viagra and Levitra, which are well known to cause side effects such as headache, pressure behind the eyes, a stuffy nose, and even ringing in the ears or vision problems. I am not trying to knock these medications, as they work extremely well for most users, but the accompanying side effects can real old, real fast. Try kissing someone when you can’t breathe through your nose—doesn’t work to well. It can be just as much of a hassle when your eyes begin to water and feel like they are going to pop out of your head. Both of these scenarios are undesirable. While tadalafil can cause these side effects (usually at higher dosages) in some people, they are rarely so intense that they become problematic and many don’t notice them at all.
One of the reasons tadalafil is so much milder in these areas, particularly in regards to vision problems, is because of its increased selectivity. Poor selectivity is common with many drugs—they often affect areas of the body that have nothing to do with the issue one is trying to treat. For example, cancer patients often employ chemotherapy, but rather than targeting cancer cells specifically, it adversely affects the entire body, damaging literally every cell in the process. While this is an extreme example, it perfectly illustrates how a lack of specificity can lead to negative, unintended side effects. In the same way, PDE-5 inhibitors affect more than just the PDE-5 enzyme—they also affect the PDE-6 enzyme, but to varying degrees.
The problem here is that the PDE-6 enzyme is intimately involved in vision, playing a vital role in the transfer of light impulses into nerve impulses. When this enzyme is inhibited through the use of PDE-5 inhibitors, color perception problems can result. However, while drugs like Levitra and Viagra are 3X and 7X more selective for the PDE-5 enzyme, respectively, tadalafil is 700X more selective. Basically, this means that tadalafil affects the PED-5 and PDE-6 enzyme at a ratio of 700:1, making it far less likely to interfere with one’s vision.
Lastly, tadalafil’s efficacy is not dependent on one’s diet, as is the case with Viagra and Levitra. Food, specifically dietary fat, hinders both the rate and extent of absorption when using Viagra and Levitra, but has no affect on tadalafil. In other words, food consumption will not only reduce the effectiveness of the other PED-5 inhibitors, but it will also make them take longer to work. Although this problem can be eliminated through proper timing, it would be better if we didn’t need to worry about it at all. With tadalafil, you don’t have to, as it can be taken with or without food, regardless of type or quantity, without affecting its efficacy or onset of action.
Administering Cialis
When administering tadalafil for improved sexual performance on an as needed basis, 20 mg is the most common dose, although some users will go as low as 10 mg or as high as 40 mg. Tadalafil will begin to take effect within 30-60 minutes of ingestion and will reach peak plasma concentrations in roughly 2 hours. With adequate dosing, there is no need to take this medication more than once daily. Another option is to take tadalafil every day, but at a reduced dosage. Some users report that this method produces more pronounced effects with extended use, while simultaneously minimizing the potential side effects associated with higher dosages. When administered in this fashion, 5 mg daily is the most commonly recommended dose, although some will elect to go as high as 10 mg daily.
Lastly, PDE-5 inhibitors should not be consumed with grapefruit juice, as it will hinder absorption. I realize this is in contrast to the common claim that grapefruit increases the absorption rate and duration of action of certain drugs, but in some cases it can have the opposite effect. In this case, the increase in P-glycoprotein that accompanies grapefruit consumption can actually decrease the absorption of PDE-5 inhibitors into the bloodstream, thereby reducing their overall effectiveness.
While the individual profiles of the various PEDE-5 inhibitors are useful for helping one make an informed decision, one should also keep in mind that personal response can vary significantly in terms of both effectiveness and side effects. So, just because one may not meet your initial expectations, it does not mean that another one won’t. Over the last 10 years, tadalafil has increased in popularity tremendously. With a longer active life than the competition, increased tolerability, and greater specificity in its effects, many have chosen tadalafil as their go-to PED-5 inhibitor of choice.
by Mike Arnold
With drug-based performance enhancement now being utilized for a multitude of purposes in nearly every sector of society, the idea that one can gain an advantage through pharmaceutical assistance is no longer looked down upon like it once was. With this growing social acceptance, the stigma attached to the use of ED drugs has diminished significantly. No longer viewed solely as a treatment for ED, they are now being used with ever greater frequency to improve sexual potency in otherwise healthy men. While frowned upon by the medical establishment, the truth is that these drugs are equally safe in both populations, helping the impotent to restore their sexual prowess and the adequate to achieve a degree of performance beyond the norm.
In the BB’ing community, both are valid concerns, as AAS can act as either sexual superchargers or as impotence promoting drugs, depending on the steroid employed and the user’s personal response. Both trenbolone and nandrolone are known to decrease libido and impair sexual functioning with extended use, most often as a result of elevated prolactin levels. Although this problem can generally be rectified with anti-prolactin drugs, they can sometimes take weeks to reach full effectiveness, while PDE-5 inhibitors (ED drugs) provide a rapid-acting alternative capable of producing near immediate results.
Regardless of the intended application, the addition of a PED-5 inhibitor confers benefits that cannot be obtained elsewhere. Whether you are trying to overcome the negative effects of AAS on sexual performance or morph into a virtual sexual dynamo, PED-5 inhibitors can assist you with your goal.
What is Cialis and how does it Work?
The invention of PED-5 inhibitors for the treatment of erectile dysfunction came about more as an accident rather than a planned attempt to cure the ailment. The story goes back to 1994, when GlaxoSmithKline discovered that their prospective heart medication, sildenafil (most commonly known as Viagra), demonstrated strong erection promoting effects in test subjects. This revelation led the company to terminate all further testing of sildenafil as a heart medication and to initiate a new round of clinical trials designed to evaluate the drug as a treatment for erectile dysfunction. By 1998 Viagra had gained FDA approval and was released onto the market with no small amount of fanfare. After netting sales exceeding 1 billion dollars and with GlaxoSmithKline holding a virtual monopoly on the treatment of this condition, other companies took notice and quickly began testing their own versions of PED-5 inhibitors.
Following the massive success of Viagra in 1998, Eli Lilly began clinical testing for tadalafil that same year and by 2003, FDA approval was granted. Marketed under the brand name Cialis, it held distinct advantages over the competition (which now included both Viagra and Levitra), that helped differentiate it from its peers and gain market share.
In 2008, Eli Lilly sold the exclusive rights to commercialize tadalafil for pulmonary arterial hypertension to United Therapeutics. Gaining FDA approval in 2009 for this purpose and sold under the brand name Adcirca, it is the first and so far only PED-5 inhibitor to be sold as a heart medication—the original reason PED-5 research began. A couple years later, in 2011, tadalafil was granted FDA approval for a third use—to treat the signs and symptoms of benign prostatic hyperplasia.
Although many of these drugs are now household names, only a small percentage of people understand how PDE-5 (phosphodiesterase type 5 enzyme) inhibitors actually work. However, before we can answer this question in a way that is easy to comprehend, we must first understand how the body produces an erection. During arousal, nitric oxide is released from the synapses of neurons in the corpus cavernosum of the penis. This results in an accumulation of cGMP (cyclic guanosine monophosphate) and the subsequent relaxation of smooth muscle, allowing an erection to take place.
The mechanism by which these drugs work is fairly simple. Post-ingestion, tadalafil enters the bloodstream and makes its way to the penis, where it prevents the breakdown of cGMP, allowing for an enhanced and sustained erection. Regardless of which PED-5 inhibitor we are referring to, all work through this same basic mechanism of action. For many, the resultant effect is so powerful that even those with severe ED issues are often able to achieve a normal level of functioning, while those with normal function frequently experience the ability to engage in long-lasting, repeated bouts of sexual intercourse in a single session.
Additional Benefits of Cialis
Although all PDE-5 inhibitors do the same basic job, each one is different in its pharmacodynamics (i.e. how a drug affects the body). Depending on the individual’s needs and circumstances, these differences often determine which treatment option is preferred. Compared to the other two candidates (Viagra & Levitra), which are similar in action and effect, tadalafil is somewhat unique; possessing characteristics which set it apart from the competition.
The first of these is its duration of action. Unlike the other PDE-5 inhibitors, which are only effective for about 4-6 hours, tadalafil continues to maintain its effectiveness for an extended period of time. With an active life approaching 36 hours, it has come to be known as the “weekender”. Aside from not needing to administer the drug as frequently, there are other benefits attached to this defining characteristic, particularly in the area of spontaneity. Nothing can kill the mood faster (at least for a woman) than putting things on hold for 30-60 minutes while you pop a pill and wait for it to take effect. With tadalafil, one can take the medication earlier in the day, long before sexual activity is anticipated, and ensure that you are at the top of your game should luck go your way. This is especially important for the non-married—or for those looking for prospective mates at bars or other social gatherings. Even for married couples, the loss of spontaneity can be an issue, so regardless of which situation you find yourself in, tadalafil’s long duration of action is a significant benefit.
Another characteristic associated with tadalafil, which is appreciated by many users, is its greater degree of tolerability. Quite simply, tadalafil is more pleasant to take than drugs like Viagra and Levitra, which are well known to cause side effects such as headache, pressure behind the eyes, a stuffy nose, and even ringing in the ears or vision problems. I am not trying to knock these medications, as they work extremely well for most users, but the accompanying side effects can real old, real fast. Try kissing someone when you can’t breathe through your nose—doesn’t work to well. It can be just as much of a hassle when your eyes begin to water and feel like they are going to pop out of your head. Both of these scenarios are undesirable. While tadalafil can cause these side effects (usually at higher dosages) in some people, they are rarely so intense that they become problematic and many don’t notice them at all.
One of the reasons tadalafil is so much milder in these areas, particularly in regards to vision problems, is because of its increased selectivity. Poor selectivity is common with many drugs—they often affect areas of the body that have nothing to do with the issue one is trying to treat. For example, cancer patients often employ chemotherapy, but rather than targeting cancer cells specifically, it adversely affects the entire body, damaging literally every cell in the process. While this is an extreme example, it perfectly illustrates how a lack of specificity can lead to negative, unintended side effects. In the same way, PDE-5 inhibitors affect more than just the PDE-5 enzyme—they also affect the PDE-6 enzyme, but to varying degrees.
The problem here is that the PDE-6 enzyme is intimately involved in vision, playing a vital role in the transfer of light impulses into nerve impulses. When this enzyme is inhibited through the use of PDE-5 inhibitors, color perception problems can result. However, while drugs like Levitra and Viagra are 3X and 7X more selective for the PDE-5 enzyme, respectively, tadalafil is 700X more selective. Basically, this means that tadalafil affects the PED-5 and PDE-6 enzyme at a ratio of 700:1, making it far less likely to interfere with one’s vision.
Lastly, tadalafil’s efficacy is not dependent on one’s diet, as is the case with Viagra and Levitra. Food, specifically dietary fat, hinders both the rate and extent of absorption when using Viagra and Levitra, but has no affect on tadalafil. In other words, food consumption will not only reduce the effectiveness of the other PED-5 inhibitors, but it will also make them take longer to work. Although this problem can be eliminated through proper timing, it would be better if we didn’t need to worry about it at all. With tadalafil, you don’t have to, as it can be taken with or without food, regardless of type or quantity, without affecting its efficacy or onset of action.
Administering Cialis
When administering tadalafil for improved sexual performance on an as needed basis, 20 mg is the most common dose, although some users will go as low as 10 mg or as high as 40 mg. Tadalafil will begin to take effect within 30-60 minutes of ingestion and will reach peak plasma concentrations in roughly 2 hours. With adequate dosing, there is no need to take this medication more than once daily. Another option is to take tadalafil every day, but at a reduced dosage. Some users report that this method produces more pronounced effects with extended use, while simultaneously minimizing the potential side effects associated with higher dosages. When administered in this fashion, 5 mg daily is the most commonly recommended dose, although some will elect to go as high as 10 mg daily.
Lastly, PDE-5 inhibitors should not be consumed with grapefruit juice, as it will hinder absorption. I realize this is in contrast to the common claim that grapefruit increases the absorption rate and duration of action of certain drugs, but in some cases it can have the opposite effect. In this case, the increase in P-glycoprotein that accompanies grapefruit consumption can actually decrease the absorption of PDE-5 inhibitors into the bloodstream, thereby reducing their overall effectiveness.
While the individual profiles of the various PEDE-5 inhibitors are useful for helping one make an informed decision, one should also keep in mind that personal response can vary significantly in terms of both effectiveness and side effects. So, just because one may not meet your initial expectations, it does not mean that another one won’t. Over the last 10 years, tadalafil has increased in popularity tremendously. With a longer active life than the competition, increased tolerability, and greater specificity in its effects, many have chosen tadalafil as their go-to PED-5 inhibitor of choice.
