Apomorphine for sexual enhancement

Jason Mcfaddinn
Version 4.0, December 2004

When Uprima (apomorphine by generic name) was launched in Europe as the first medical treatment for sexual dysfunction after Viagra, it was suspected that it could repeat the success of Viagra. It did not. Which doesn't mean that it would be a useless drug.

Apomorphine is a dopaminergic drug. It stimulates dopamine receptors. And dopaminergics are a blessing. If you know how to take them, and what to suspect. And if you can purchase dopaminergics at a lower price than the 10 dollars per milligram charged by official Uprima selling sites, or at US pharmacies for other dopaminergics such as Dostinex.

Unlike sildenafil (Viagra), apomorphine and other dopaminergics exert their pro-sexual effect not upon the erectile organ but upon the brain. Apomorphine provokes erections not by interfering with the plumbing of male sexual function (speak: blood supply to the penis), but the wiring necessary for arousal.

That Viagra only effects the plumbing, puts clear limits to its potential as a lifestyle drug. Viagra will do little for men whose plumbing doesn't leak. On the other hand, a good shot of additional desire can be a welcome life enhancement for many people with whom there is nothing wrong physically but who just feel bored with their everyday life. For them, apomorphine can be a real enrichment, and even a medication that saves their marriages.

Provided, they can afford it.

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What is a chemical peel

A body treatment technique used to improve and smooth the texture of the facial skin using a chemical solution that causes the skin to blister and eventually peel off. The regenerated skin is usually smoother and less wrinkled than the old skin. Thus the term chemical peel is derived. Some types of chemical peels can be purchased and administered without a medical license, however people are advised to seek professional help from a plastic surgeon or dermatologist on a specific type of chemical peel before a procedure is performed.

Alpha hydroxy acids (AHAs) are naturally occurring organic carboxylic acids such as glycolic acid, a natural constituent of sugar cane juice and lactic acid, found in sour milk and tomato juice. This is the mildest of the peel formulas and produces light peels for treatment of fine wrinkles, areas of dryness, uneven pigmentation and acne. Alpha hydroxy acids can also be mixed with a facial wash or cream in lesser concentrations as part of a daily skin-care regimen to improve the skin's texture.

It is becoming common for the use of beta hydroxy acid (BHA) peels to be used instead of the stronger Alpha Hyroxy (AHA) peels due to BHA's albility to get deeper into the pore than AHA. Studies show that BHA peels control oil, acne as well as remove dead skin cells to a certain extent better than AHA's, due to AHA's only working on the surface of the skin.

Jessner's peel is a combination of salicylic and lactic acids, and resorcinol. It is thought to break intracellular bridges between keratinocytes.

Trichloroacetic acid (TCA) is used as an intermediate to deep peeling agent in concentrations ranging from 20-50%. Depth of penetration is increased as concentration increases, with 50% TCA penetrating into the reticular dermis. Concentrations higher than 35% are not recommended because of the high risk of scarring.

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How apomorphine works

Version 2.0, April 2003

Strictly speaking, Uprima is not a new drug. The active ingredient of Uprima is apomorphine, which has been around for decades, and is used in the treatment of Parkinson's disease and as an emetic in dogs and other domestic animals. (An emetic is a drug that induces vomiting.)

While apomorphine has a definite potential as a pleasure drug, this is about all it has in common with its more famous colleague in name, morphine. Sure, apomorphine is produced from morphine. But its pharmacological effects are completely different. Morphine is a sedative agent, while apomorphine is a stimulant.

Apomorphine primarily works as a dopamine agonist, which accounts for its usefulness in the management of Parkinson's Disease, a condition characterized by the loss of dopamine-producing neurons, leading to severe motor function disturbance. Apomorphine is a D1 receptor-specific dopamine agonist that makes it different from mostly ergot-derived dopamine agonists, which usually target D2 dopamine receptors, e.g. pergolide and bromocriptine. D3 and D4 dopamine receptors are less often targeted in the management of Parkinson's Disease.

It has long been documented that most Parkinson's medications have sexuality-enhancing side effects. I was personally using Parkinson's medications for sexual enhancement long before Uprima was launched. I gained the most experience with Parlodel (bromocriptine), but I have also tested Dopergine (lisuride), Cabergoline (brand name: Dostinex), Mirapex (pramipexole), L-dopa, and deprenyl.

It has to be noted that the sexuality-enhancing side effects hold true for many but not all dopamine-enhancing Parkinson's medications. Whether or not a dopamine agonist enhances sexual functions seems to depend primarily on the dopamine receptor and sub-receptor sites it targets.

Unlike sildenafil (Viagra), dopamine agonists, whether Uprima or cabergoline (brand name: Dostinex), exert their pro-sexual effect not upon the erectile organ but upon the brain. They provoke erections not by messing with the plumbing of male sexual function (i.e. blood supply to the penis), but by interfering with the wiring necessary for arousal, pleasure, and climax.

That Viagra only affects the plumbing, puts limits to its potential as a lifestyle drug. Viagra will add little for men whose plumbing doesn't leak. On the other hand, a good shot of additional desire would be a welcome life enhancement for many people with whom there is nothing wrong physically but who just feel bored with their everyday life. For them, dopamine agonists could be a real enrichment, and even a medication that saves their marriages.

Dosage for a pro-sexual effect is difficult to determine for all dopamine agonists. This is the case because a dosage that is too high will inevitably result in nausea. This nausea can be so bad that the last thing one fancies is sex. This particularly is a problem with apomorphine, which indeed is commonly used to induce nausea. One of the advantages of cabergoline is that it has far fewer side effects.

Uprima has so far not been approved for marketing in the US. If a FDA endorsement is to be obtained for its marketing in the US as treatment for erectile dysfunction, the primary concern has to be to keep the nausea side effect at bay.

With apomorphine, nausea can be reduced if it gets into the bloodstream quick enough. Parkinson's patients use injected apomorphine. Parkinson's is a serious condition, a matter of life and death, and in such a case, patients can be expected to tolerate injections. But as treatment for non-life-threatening conditions like lack of libido or erectile dysfunction, injection medications have always been a flop.

Tap Pharmaceuticals, the makers of Uprima, try to get around the problem in two ways: by packaging the drug as sublingual, and by keeping the dosage per tablet rather low (2 or 3 mg per sublingual.

The point is: with small doses of apomorphine, the likelihood of nausea will be negligible. But so will the pro-sexual effect.

When I myself use Uprima, I go for 6 mg, which for me is a borderline nausea dosage. With 6 mg of sublingual apomorphine, I'm not really nauseated, but I do have a definite preference for a horizontal position. And at that dosage, I do get a sexual kick out of the medication.

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Otoplasty

A cosmetic surgery to change the appearance of a person's external ears. Otoplasty can take many forms, such as bringing the ears closer to the head (often called ear pinning), reducing the size of very big ears, or reshaping various bends in the cartilage. Other reconstructive procedures deal with the deformed, or abscent-microtic ears.

Otoplasty surgery can involve a combination of moving, reshaping, adding, or removing structural ear elements. This procedure is usually performed by either an oral and maxillofacial surgeon, plastic surgeon, or ENT surgeon.

The pinna, or external ear, is made of a thin structural cartilage cover over with thin skin. Each of the various folds and structures of the pinna is named. Ear deformity results from distorted, damaged, or missing ear elements. Many otoplasties are performed not because of actual deformity, but because the individual is displeased with the shape of their ears.

Anesthetic options depend on the problem to be treated and ability of the patient to cooperate and can include local anesthesia alone, local anesthesia with sedation, and under general anesthesia (which is generally the case for children). Most otoplasty surgery is performed as a outpatient surgery, some requires a hospital stay. The procedure can take from two to five hours depending on the problem.

Incising one side of a flat cartilage piece leaves unopposed elastic forces on the other side and permits the shape to evolve over time. Thus, incising one side of the lop-ear cartilage along the new anti-helical fold may be one element of the surgery. This can be done through a small incision, or without an incision: an "Incisionless

Otoplasty," where a needle is placed through the skin to model the cartilage and also to place the retention sutures.

For many ear operations, one or more incisions give access to the structures to be sculpted. The main, and often only incision, is behind the ear. Other possible incisions depend on what needs to be done. Through the incision behind the ear, the concha bowl can be moved closer to the head, a small tunnel created along the front of a poorly folded antihelix to weaken this cartilage, sutures placed to reshape the anti-helix fold, and to balance the ear lobe with the rest of the ear.

Ear reduction otoplasty may involve reducing one or more components of the ear. Incisions are typically hidden near folds in the front when a part of this surgery.

Addressing Microtia (small ear deformity) or Anotia (missing ear deformity) involve augmentation or adding elements to replace deformed or missing structures. Cartilage from the ear or rib are the most common for these more extensive reconstructions. Other ear shapes may be changed through moving, adding, and weakening ear structures. Internal sutures often are permanent. The wound(s) are then closed with either dissolvable sutures or ones that are removed by a doctor after the wounds have healed. A bulky ear dressing protects the ear after surgery.

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Intermittent apomorphine injections as rescue therapy for advanced Parkinson's disease : Consensus statement.

Trenkwalder C, Boesch S, Ceballos-Baumann A, Dressler D, Eggert K, Gasser T, Honig H, Müller T, Reichmann H, Sieb JP, Storch A, Odin P, Poewe W

Zentrum für Parkinson-Syndrome und Bewegungsstörungen, Paracelsus-Elena-Klinik, Klinikstraße 16, 34128, Kassel, Deutschland, CTrenkwalder@gmx.de.

Intermittent subcutaneous apomorphine therapy should be considered in patients with advanced Parkinson's disease who experience recurrent off periods despite optimised oral treatment (according to guidelines), for reliable and quick reversal of these otherwise refractory periods. Such treatment is also called rescue therapy. At present, apomorphine injections with the apomorphine pen are underutilised, considering its current indications and contraindications. In the present consensus statement, concepts for the use of apomorphine are presented and discussed based on existing study results, indications, and contraindications. Recommendations for a practical approach are also provided.

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Behavioral responses to methylphenidate and apomorphine in rats exposed neonatally to bisphenol-A.

Kiguchi M, Fujita S, Lee J, Shimizu N, Koshikawa N

Department of Orthodontics, Nihon University School of Dentistry.

Neonatal exposure of rats to bisphenol-A, an endocrine disruptor, has recently been proposed as a possible animal model of attention-deficit hyperactivity disorder, because such rats exhibit motor hyperactivity and impaired habituation to a novel environment 4-5 weeks after bisphenol-A pretreatment. To extend the original experiments, the present study additionally analyzed the effects of neonatal exposure to bisphenol-A (20 and 40 mug) on rat habituation to a novel environment and drug-induced behavior particularly at a later stage after bisphenol-A pretreatment. Single intracisternal administration of bisphenol-A (20 mug) into 5-day-old male Wistar rats did not cause any significant changes in habituation, as assessed in terms of locomotor activity, rearing, sniffing and grooming in rats at 8 weeks of age. Methylphenidate (1 and 3 mg/kg, i.p.), a psychostimulant, dose-dependently enhanced locomotor activity in both vehicle- and bisphenol-A (20 mug)-pretreated rats at 8 weeks of age, whereas other behaviors, i.e. rearing, sniffing and grooming, were not significantly affected. Additional challenge with apomorphine (1 mg/kg, i.v.), a dopamine receptor agonist, in vehicle- and bisphenol-A (20 and 40 mug)-pretreated rats at 10 weeks of age elicited a similar level of repetitive jaw movements measured by a magnet-sensing system under freely moving conditions during both the dark and the light phases. Thus, the effects of apomorphine did not differ between bisphenol-A-pretreated and vehicle-pretreated rats. It is concluded that, though some behavioral changes are evident in rats at an early stage (4-5 weeks) after neonatal treatment with bisphenol-A, the pretreatment does not induce any behavioral changes in habituation to a novel environment or in response to methylphenidate and to apomorphine at a later stage (8-10 weeks). (J. Oral Sci. 49, 311-318, 2007).

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Rheum officinale

A rhubarb from the family Polygonaceae originating in Asia.

The root and stem of R. officinale are used to treat constipation, as well as to aid in the dissolution of blood clots and pus eruptions. Is used in traditional Chinese medicine, where it is called yào yòng dà huáng (????), and is also a component in the North American herbal remedy called Essiac tea.

In modern medicine, R. officinale has been found to be useful in treatment of Hepatitis B


Copyright © Jason Mcfaddinn