Experimental Oral Agents - Erectile dysfunction treatment

Oral Phentolamine. Phentolamine is an agent that has been in injections for achieving erection. The drug blocks adrenaline (epinephrine), which dilates blood vessels. An oral form of phentolamine (Vasomax) has been developed that may be of some benefit for men with mild impotence. The drug is not as effective as sildenafil .

(Viagra), but it does not interact with nitrates. In some studies, it was effective in producing erections within 20 to 40 minutes in 40% to 50% of men with mild to moderate erectile dysfunction. Side effects include nasal congestion, headache, light-headedness, low blood pressure, Tachycardia (increased heart rate), and nausea.

Apomorphine. Apomorphine (Uprima) causes a sexual signal in the brain to trigger an erection, although it is not an aphrodisiac. Studies report improved erectile function in 40% to 60% of men, with the better results occurring at the higher doses. High doses, however, also cause more severe side effects, including nausea (in about a third of patients), yawning, fatigue, dizziness, sweating, excitability, and aggression. Apomorphine appears to be safe for men with diabetes, stable heart disease, and is well tolerated by men with High Blood Pressure.

Melanotan II. Researchers are investigating drugs that are derived from a natural substance released in the brain called alpha-MSH, which increases sexual behavior. One such agent called Melanotan II is showing promise in investigative studies. In one study, 60% of men achieved erections after injections of Melanotan II, but about 20% of men experience severe nausea. It appears to increase sexual desire and takes over an hour to take effect.

Other Areas of Investigation. Investigators are also looking at agents that might target very specific elements in the erectile process.

• Genetically Designed Agents. Genetically designed agents for erectile dysfunction are being investigated. One agent uses a gene that enhances specific channels that carry potassium to the smooth muscle cells of the penis, which may relax these muscles and achieve erection.

• Immunophilins. Research is being done on proteins called immunophilins, which may play a positive role in regenerating nerves in the penis after an injury.

• Arginase Inhibitors. The amino acid arginine is a key ingredient in erectile function. It is converted into nitric oxide, which relaxes smooth muscles. Research indicates that the enzyme arginase can disrupt this chemical process and prevent sexual arousal in both men and women. Researchers have identified arginase inhibitors, an amino acid derivative called S-(2-boronoethyl)-L-cysteine (BEC) and (S)-2-amino-6-boronohexanoic acid, which may prove to be the basis for therapies.

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