Product Information: Ixense (previously Uprima)

Product Information
Apomorphine: The Development Of Ixense (previously Uprima®)

Our Uprima product has recently changed it's name to Ixense.

Ixense is a potent agonist of dopamine, specifically it acts upon D1 receptor sites, and this makes it different to the majority of ergot derived drugs for dopamine improvement, such as, bromocriptine, which normally target D2 receptors. Accordingly, Ixense doesn’t act directly upon the penis like Viagra® or Befar®, but instead exerts its influence in the brain for arousal, pleasure and climax. Ixense is known to act upon receptors in the hypothalamus, and that this can enhance erection by increasing the signals from the brain to begin the process. Specifically, it induces selective activation in the nucleus paraventricularis, leading to erectogenic signals.

It is this brain action that makes Uprima® a unique new approach to the treatment of ED. As Dr. Dula stated after being involved with a trial of 1472 patients using Ixense; “From a urologist’s perspective, it is important to understand that this is an entirely novel agent and works totally differently to Sildenafil (Ed.- Viagra®). It is a centrally-acting agent. What’s more, apomorphine works fairly quickly, in 15-25 minutes. The main side effect is nausea, but over time and repeated dosages it rapidly dissipates. We think that it is a safe and efficacious treatment for erectile dysfunction.”

In a multi-center, double blind study, 520 patients (of an average median age of 54) took either 2mg, 4mg, 5mg, 6mg of apomorphine or a placebo. The number of attempts resulting in an erection firm enough for intercourse was recorded, along with the actual attempts resulting in intercourse.

The most significant improvements over placebo are at dosages of 4mg to 6mg. However it was clear in this same trial and others, that increased dosages also increase the likelihood of the most common side effect of nausea. These side effects are reported to diminish with continued dosing.

In fact, the most favorable risk/ benefit ratio is seen with a dose optimization regimen of 3mg, with the 3mg dose providing efficacy comparable to that of 4mg, but with fewer side effects.

Other side effects with Ixense include headache, dizziness, and flushing.

Contraindications with apomorphine include heart medications, (particularly those for hypertension) and because of potential synergy any other dopamine agonists such as bromocriptine, hydergine, deprenyl and L-dopa etc. Should you be taking such drugs, then always consult with your physician before embarking upon a concurrent use of apomorphine.

As stated earlier, the average dosages of Ixense are 2mg or 3mg taken sublingual (dissolved under the tongue) about 15 minutes before sex. (Note that the advent of the sublingual tablet is the only way that apomorphine should be used to treat ED). The drug insert clearly states, that (like most ED drugs), a 3mg dose should not be repeated again within any 8-hour period.

Conclusion:
Ixense represents a radical new departure in the treatment of ED. Rather than just stimulation to the penis for enhanced blood flow etc., for the first time brain receptor sites are being targeted for enhanced sexual performance.

We are confident that we are going to see other drugs being developed along similar lines in the coming months and years. I am also confident that similar (and even some of the same drugs), are eventually also going to be approved for sexual enhancement in females too.

Manufacturers Insert

UPRIMA®

What Uprima is and what it is used for?
Uprima tablets are sub-lingual tablets each containing 3mg of apomorphine (as hydrochloride). The 3mg tablet is available is packs of 2 and 4 sublingual tablets. Uprima 3mg tablets are brick red in colour and are triangle shaped embossed with 3 on one side and the Abbott logo on the other side. Uprima is a medicine known as a dopaminergic agonist which helps men achieve an erection by stimulating the region of the brain, called the hypothalamus, thereby helping to produce the natural signals which start the erection process in the penis. Sexual stimulation is necessary for Uprima to work. Uprima is different to morphine and has no morphine-like properties. Uprima is a therapy for the treatment of men with erectile dysfunction (sometimes called ED or impotence). This is a condition in which a man cannot get, or keep, a hard penis (erection) sufficient for satisfactory sexual performance.

Before you take Uprima:

Do not take Uprima if:
You have ever had allergic reaction to apomorphine or any of the ingredients in Uprima. Possible signs of an allergic reaction include rash, itching, swollen face or lips and shortness of breath. Tell your doctor if you get any of these.
You have severe unstable angina, recent myocardial infarction, severe heart failure or hypotension, and other medical conditions, which could make sexual activity dangerous. Always consult your Doctor about your medical history.
Your partner is pregnant or breastfeeding.

You should tell your doctor if:
You have a deformity of disease of the penis as these may require special care when using medicines such as Uprima.
You experience severe dizziness/light headedness or feel faint after taking Uprima, especially if you also have severe nausea or vomiting, sweating, become pale or become unusually hot. In these cases you should not attempt to stand up. If you experience these symptoms or feel faint for any reason you should like down and raise your legs. The feeling of faintness should go away.
You are taking nitrates (often used for relief of angina or chest pains) or any medicines for hypertension (high blood pressure).
You have liver or kidney problems. Your suitability for Uprima and/or the appropriate dose may need to be considered by your doctor.
You have abnormally high or low blood pressure or are prone to dizzy spells or fainting.
You are taking any other treatment for erectile dysfunction. Uprima should not be used with any other treatment for erectile dysfunction.
Uprima should not be given to children under the age of 18. No dose adjustment is required for the elderly. Taking alcohol with Uprima can increase undesirable effects, in particular low blood pressure. In addition, Taking alcohol can make it more difficult to obtain an erection. Not for use in women.

Driving and using machinery:
Because some patients can experience dizziness, light headedness and, uncommonly fainting, it is recommended that you do not drive or operate machinery for at least 2 hours after taking Uprima or until any such symptoms are fully resolved.

Taking other medicines:
Please inform your doctor if:
You are taking nitrates (often used for the relief of angina or chest pains) or any medicines for hypertension (high blood pressure).
You are taking drugs that affect the dopamine systems (often used to treat Parkinson’s disease, disturbance of the mind or to prevent vomiting.
You should also inform your doctor or pharmacist if you are taking or have recently taken any other medicines, even those not prescribed.

How to take Uprima
Your doctor will decide the dose of Uprima which is suitable for you. Do not take more tablets than your doctor has prescribed. All patients should begin with the 2mg tablet. If your erection is not sufficient for satisfactory sexual activity at this dose and you have not experienced side effects, you may increase the dose to the 3mg tablet following consultation with your doctor. You should not take more than 3mg in any 8-hour period.

When taking Uprima:
Swallow a small amount of water to help moisten your mouth.
Place one tablet of Uprima under your tongue. The tablet will not work if you swallow it.
Let the tablet dissolve under your tongue – this usually takes about 10 minutes (if any tablet residue is left after 20 minutes it may be swallowed).
Sexual activity may begin as soon as the Uprima is placed under the tongue and you may proceed with intercourse when you and your partner are ready.
Typically erections may be achieved in less than 20 minutes, although this varies from person to person.
You should not take more than 3mg Uprima in any 8-hour period.

If Uprima does not help you get a satisfactory erection tell your doctor, as your dose may need adjustment.

You should only take Uprima as directed. If you take too many tablets or the wrong dose, contact your doctor.

Possible side effects
Like all medicines, Uprima can have side effects. These are generally mild and transient in nature. Common undesirable effects are nausea, headache, dizziness, yawning, sleepiness, infection, sore throat, pain, increased cough, rhinitis, flushing, taste disorder and sweating. Uncommonly, fainting has occurred. If you feel faint, follow the instructions given under 'Do not take Uprima'.

If you have chest pains during intercourse, you should stop immediately and contact your doctor. If you have any undesirable effect, which is severe or prolonged, you should tell your doctor. If you notice any side effects not mentioned in this leaflet, please inform your doctor or pharmacist.

Storing Uprima
Keep out of the reach and sight of children. Store your Uprima in the original package. Do not use this medicine after the expiry date shown on the pack or if the pack has been damaged or tampered with.