Modern E.D.

Modern E.D.

In the last decades normal young guys became much more aware of all the drugs pro-bodybuilders use. Not only the steroids but especially the pain meds, the uppers – the downers. Something called cynically “substance abuse” or “poly-pharmacy.” I made a lot of blogposts about it. Its common knowledge, mostly due to the internet, how people combine meds to cure and improve performance. I’m not talking about athletic performance here, but sexual performance. Often they rely on orals like tadalafil (Cialis), vardenafil (Levitra), avanafil (Spedra or Stendra), yohimbine HCL, phentolamine, trazodone, apomorphine and neutraceuticals.

However, there is another good reason why Viagra and its derivatives sell so well, if you go to a dance event or to the beach, everywhere you see buff guys. Bodybuilding and hard-core fitness transferred from an obscure sub-culture to a mainstream phenomenon just like the use of anabolic steroids that accompanies it. As (almost) all of us know, the use of anabolics often causes problems with libido / erection. That added to the fact that many cosmetic bodybuilders are using the anabolic steroids and fat burners in tandem with many recreational drugs (X –speed – coke), which often cause erection problems by themselves, and combined with anabolics create an almost certain problem. Hence, the consumption of libido enhancers among young people is on the rise.

An increasing number of men in their 20s and 30s, not diagnosed with ED, are also using these drugs for, as one guy described it, “supercharged” sexual experiences, with stronger erections, longer endurance, and less downtime in between orgasms.

While ED drugs may not be physically addictive, men can certainly become psychologically dependent on them, where they fear lack of performance without the drug.

Which is ironic, because performance anxiety is one of the reasons that many young and healthy men have been turning to ED drugs in the first place.

It’s hard to imagine that men in their 20s are feeling insecure about their libidos, or pining for a past when their erections were somehow more mythical and epic. But many men seem to feel that way.

“Viagra gave me erections like when I was 13-years-old,” says Richie, 34. “I could go again in minutes.”

They don't suffer from diabetes, hypertension or any other medical cause of impotence.

Some complain about performance anxiety. Others say that their marriage is in need of a spark. Partygoers are looking for something to offset the effects of alcohol.

An erection involves the brain, nerves, hormones, muscles, and circulatory system. These systems work together to fill the erectile tissue in the penis with blood. A man with erectile dysfunction (ED) has trouble getting or maintaining an erection for sexual intercourse. Some men with ED are completely unable to get an erection, while others have trouble maintaining an erection for more than a short time.

A study in the July 2013 Journal of Sexual Medicine suggests that ED is more common among younger men than previously thought. Researchers found that ED affected 26 percent of adult men under 40. Almost half of these men suffered from severe ED.

That rate is similar to what is experienced by older men. Researchers also noted that younger ED patients were more likely than older men with ED to smoke or use drugs. Hormonal disorders, such as low testosterone, may contribute to ED. But other factors are more likely to be at work in young men with ED. Another hormonal cause of ED is increased production of prolactin, a hormone produced by the pituitary gland. An abnormally high or low thyroid hormone level can result in ED. Young men who use steroids to help build muscle mass are also at a higher risk for ED.

Combinations

Sildenafil (Viagra) is effective for all sorts of erectile dysfunction in 69% of people. Why is there a need for another pill? In some cases the erection is not hard enough, sometimes sildenafil (Viagra) just doesn’t work.

Structurally vardinafil (Levitra) is similar to sildenafil, while tadilafil (Cialis) is very different. That’s why this UG brand from India combines sildenafil with tadalafil. Personally I would have preferred tadalafil with vardenafil. Why?

Vardenafil (Levitra) is almost 10 times more biochemically potent than sildenafil, therefore a lower dose is needed to facilitate the penile erection, potentially resulting in less side effects. Selectivity is the ability of the drug to attach to the specific enzyme PDE 5 found in penile tissues. Vardenafil (Levitra) is more selective than sildenafil and tadalafil (Cialis) to PDE5, which again means a lower dose is needed with potentially less side effects.

Vardenafil has a slightly quicker time to onset than Viagra. It also has less interaction with food. For example, patients used to a meal with wine as a preamble to sex, can sometimes have a problem with Viagra. That’s why sildenafil to be effective should be taken on an empty stomach. Also diabetics do not respond well to sildenafil, just like older man with decreased testosterone blood levels. In fact vardenafil is an improved version of good old sildenafil.

Sildenafil (Viagra) has a half-life of 4 hours and vardenafil (Levitra) has a half-life of 4-6 hours while tadalafil (Cialis) has a half-life of 17.5 hours. This means that vardenafil (Levitra) should act longer than sildenafil (Viagra) but the clinical significance is not known. Tadalafil (Cialis) has the longest half-life and allows you to take the medication and not relate the sexual activity to the immediate use of the medication. The drawback is if you need nitrates after using tadalafil (Cialis), this medication lasts a long time in your blood stream and may place you at a higher risk. Younger people might do well treated with tadalafil, (Cialis) while older people with other health issues might be better off using sildenafil (Viagra) or vardenafil (Levitra) but more data are needed. The side effects of vardenafil (Levitra) are potentially less than sildenafil (Viagra), but more data are needed. In a recent study on men with erectile dysfunction and diabetes, vardenafil (Levitra) improved their erectile dysfunction.

But why all these new ED pills? Like recently the avanafil? Is “big Pharma” suddenly interested in improving the quality of life of men suffering from ED? Of course not, again its money, big money!! "Mr. Blue" - a slang term for the drug - has exploded into a multibillion-dollar industry, with nine Viagra tablets dispensed every second around the globe.

Men with ED aren't the only ones fueling the business. Curious men and others looking for that edge in the bedroom bought the pills by the millions. It’s not hard to understand that the pharmaceutical company that develops the perfect sex-pill hits the jackpot, and hits it hard. The same for the pharmaceutical that can develop and license a libido increasing compound for woman.

Older combinations

In the late 60’s early 70’s there was a product on the market called Aphrodex (from Bentex Pharmaceuticals). This contained 5mg of Methyltestosterone, 5mg of Yohimbine and 5mg of Nux Vumica

Nux vomica appears in many sexual stimulant mixes found in Asia and India. It's claimed to have aphrodisiac effects, it has been used as a stimulant and nootropic for hundreds of years. It has even been used in sports as a performance enhancer. They are very potent, somewhat toxic and therefore dangerous if not used properly. The active principle is strychnine. A very powerful stimulant active in dosage ranges of 0.2-5 mg. Nux Vomica was found to be effective after 2 to 3 weeks of use in most cases, various side effects were observed It had a success rate of 90%. It was pulled from the market in the mid 70’s more than likely due to puritan reasons.

Vigrol Forte (methyltestosterone 5 mg, Tocopherol Acetate 3 mg, Yohimbine HCL 3 mg, Caffeine 15 mg, Ephedrine HCL 1 mg)

Potentol (meprobamate/methyltestosterone/yohimbine hydrochloride)

Meprobamate was the first synthesized narcotic, in 1950, and  mistakenly thought to be non-addictive and was effective as an aphrodisiac.

Potensan Forte (methyl testosterone, yohimbine, pemoline and strychnine)

Prowess (methyltestosterone/pemoline/yohimbine HCL)

yohimbine hydrochloride/methyltestosterone/testes extracts

yohimbine hydrochloride/pemoline/methyltestosterone

Pemoline is a mild stimulant, although safer, more comfortable and less addictive than speed. Pemoline was used by American and British flyers during World War II to maintain alertness during long bombing missions.

yohimbine hydrochloride and methyltestosterone

Wari-Promocil (Yohimbine HCL 5mg， methyltestosterone 0.1mg) the spray also contains Lidocaine.

Creating the Absolute Sexual Beast

People have been trying for ages to stimulate their libido. They used herbs to create a potent aphrodisiac, or a stimulating cocktail of herbs.

In Africa, yohimbe bark has traditionally been used as an aphrodisiac but one with lots of side effects. Modern science has isolate the active ingredient Yohimbine HCL which is more potent and has fewer sides. Yohimbine is a MAOI (a weak one) with aphrodisiac and stimulant properties and like all MAO inhibitors should not be combined with any ssri’s (anti-depressant meds). Yohimbine works by blocking a2 receptors causing smooth muscle relaxation in the penis, the release of norephinephrine and increases in nitric oxide.

Unlike Cialis, Yohimbine not only strengthens your erections but it increases your sex drive as well. Sex and orgasm are amazing and your sexual energy is through the roof. The downside of the drug is that the side effects of nausea, chills, anxiety in my opinion are too great without something to take the edge off like Phenibut. Phenibut, Cialis and Yohimbine combined work synergistically and will make you an absolute sexual beast.

Uprima sneaked on to the market without the razzmatazz surrounding the launch of Viagra and Cialis. It is the brand name for apomorphine, a substance prescribed in high doses to treat Parkinson's disease. Now it is being marketed as an impotence remedy.

"I've been using it for some time," says Dean. "The attraction is that it works in a completely different way to the others. Uprima actively increases sexual stimulus in the brain. It reduces inhibitory signalling and increases positive signalling."

Uprima targets some of the brain receptors which are normally activated by dopamines. One disadvantage is that is it sub-lingual - it must be left to dissolve under the tongue; this is not so discrete as swallowing a tablet. Furthermore, a small minority of users experience nausea as a side effect.

More importantly, Uprima is not effective for many severely impotent patients. "It is suitable for mild to moderate erectile dysfunction - that is about 80% of GP patients," says Dean. "It is not very effective for chronic sufferers, for men who never ever get an erection."

Cabergoline is another curiosity. Hypersexuality (increased sexual desire) is a side effect of numerous medications used to treat Parkinson's disease. Unfortunately, it can co-exist with erectile dysfunction. None the less, clinical trials of Cabergoline in Germany indicate that this substance can increase male sexual stamina and frequency of orgasm. Yet Cabergoline is neither prescribed for anorgasmia (inability to orgasm) nor actively marketed on the net.

Melatonin is commonly known as anti-jet lag medication but its family of neural receptors has other functions that go beyond the body's internal clock. A medication called Pt 141 targeted at this receptor is likely to appear in the form of a nasal spray within a couple of years.

Apomorphine (Uprima) and Pt-141 (Bremelanotide or BMT) are both being touted as remedies for female sexual dysfunction. This is because they act upon brain receptors and not solely on biochemical processes in the genitalia. Women's sexuality is complex and you need more than a better clitoral erection to enhance their satisfaction.

User Report (from the net):

As soon as the bremelanotide (a.k.a. PT-141) arrived in the mail, I shook the white crystal onto a mirror and began to chop it into powder. I snorted some and a bitter taste began its steady descent down the back of my throat. But I wasn't about to complain. I finally had my hands on the most revolutionary sex drug ever created. This potion had undergone studies for almost a decade in a quest to make it the first-ever FDA-approved aphrodisiac to hit the U.S. market.

Sure, history and folk medicine are full of purported aphrodisiacs, like Spanish fly and rhinoceros horn. But bremelanotide isn't like those – neither is it simply an erectile dysfunction drug like Viagra or Cialis, so-called PDE-5 inhibitors that work by pushing blood around the body.

Bremelanotide belongs to a new class of drugs called melanocortins, which work in the mind, increasing sexual desire. Deep inside the brain, the substance stirs passion by activating hypothalamic and limbic emotional structures, the parts that naturally flare when you're turned on. Scientists aren't exactly sure how melanocortins do this, but the result is clear: Before you know it, you want to have sex. Or at least that's what the research has shown.

“After snorting 10 milligrams of the stuff, I felt nothing. Several hours later I still wasn't the slightest bit horny. So at midnight I went to bed, totally unaware of the flood of animalistic desire that was to take hold of me.”

A year earlier I was in the Montreal lab of Jim Pfaus, arguably the world's preeminent expert on bremelanotide.

A 50-year-old neuroscientist, Pfaus was in the last stages of preclinical trials aimed at getting FDA approval for bremelanotide. Originally developed as a self-tanning agent, the drug had been repurposed when male study subjects reported a surprising side effect: erections. A New Jersey pharmaceutical company called Palatin Technologies had bought the drug, then turned the pill into a powder that could be delivered nasally, hoping that sleek nasal-spray dispensers could blow away little blue pills – and earn profits that would dwarf the $150 million that Palatin had spent on research and clinical testing.

Pfaus showed me stunning testimonials from human test subjects. "On the five-point scale, I would rate the erection I had as a six," said one of the 1,300 anonymous testers. "You get this humming feeling," said another. "You're ready to take your pants off and go."

The drug worked equally well on women, who chronicled "an intense arousal" that lasted from six to 72 hours. "I was focused on sex," said one of the women.

But there were side effects, and in 2007, Palatin's sex drug hit a roadblock just before entering phase-three testing, the FDA's final clinical hurdle before the drug is released to the public. Some of the men who sniffed bremelanotide experienced an increase in blood pressure, and about one third of the women who took the drug reported nausea.

There were also those who doubted the drug would actually cause couples to want to jump into bed together. "It's baloney," says Leonore Tiefer, a professor of psychiatry at New York University's Langone School of Medicine. "You might increase genital itchiness, but you won't increase desire."

It appeared that bremelanotide would fall into the ash heap of failed aphrodisiacs, to rest in peace with tiger penis soup. But then something unexpected happened.

In 2008, Iranian urologist Mohammad Reza Safarinejad published findings he had gathered by testing bremelanotide that he purchased from a company in Dubai on men and women. "He got fantastic results," says Pfaus. "Palatin had published everything about the drug – including the exact sequence of the compound." Middle Eastern chemists used that sequence to create the drug themselves. Shortly thereafter, several companies began offering the drug online.

But was it safe? "Well," says Pfaus, "we never resolved that blood pressure thing. There's no guarantee of purity. The FDA won't regulate it."

“Clearly, the purity issue wasn't going to stop me. Several hours after taking the drug, I wasn't experiencing a headache, a palpitating heart, or nausea, but, sadly, I also hadn't enjoyed a spontaneous erection. Then, at four in the morning, it took hold. I felt a great surge of affection (greater than any regular level of arousal) for my lovely wife. My body tingled and, yes, I developed an erection that wouldn't quit. For two hours the drug wouldn't let me out of its grasp – nor my wife out of mine.”

What other users report on the forums:

“ If you’re looking for a herbal aphrodisiac yohimbine is very nice. It works very well, it can cut recovery time between orgasms down to minutes. It can be a bit jittery thought.”

“As far as synthetic aphrodisiacs meth is a no brainer and I have found 2C-B to be an excellent choice as well. “ “MDMA may work also for some people. Personally I’ve found it to have negative sexual side effects. The physical aspect is certainly there but I get to easily distracted on it :p”

“GHB (gamma hydroxybutyrate) is an aphrodisiac and is said to increase ones sex drive, sexual desire and sexual abilities. It has been reported that the relaxation of the psychosomatic constrain is the foremost pro-sexual property of GHB. GHB makes one feel relaxed and free from inhibition, which goes a long way in increasing libido.”

“…actually a combination of GHB + viagra + antiprolactin will make you super man!!”