Apomorphine-containing dosage form for ameliorating male erectile dysfunction

• US 20030073715A1
• Filed: 10/23/2001
• Published: 04/17/2003
• Est. Priority Date: 04/22/1994
• Status: Active Grant

• Current Assignee: Pentech Pharmaceuticals Incorporated
• Original Assignee: Pentech Pharmaceuticals Incorporated
• Inventors: El-Rashidy, Ragab, Ronsen, Bruce
• Granted Patent: US 6,566,368 B2
• Time in Patent Office: Days
• US Class Current: 514/289
• CPC Class Codes: A61K 31/00 Medicinal preparations containing organic active ingredients
• CPC Class Codes: A61K 31/4045 Indole-alkylamines; Amides thereof, e.g. serotonin, melatonin
• CPC Class Codes: A61K 31/44 Non condensed pyridines; Hydrogenated derivatives thereof
• CPC Class Codes: A61K 31/472 Non-condensed isoquinolines, e.g. papaverine
• CPC Class Codes: A61K 31/473 ortho- or peri-condensed with carbocyclic ring systems, e.g. acridines, phenanthridines
• CPC Class Codes: A61K 31/485 Morphinan derivatives, e.g. morphine, codeine
• CPC Class Codes: A61K 31/506 not condensed and containing further heterocyclic rings
• CPC Class Codes: A61K 49/0004 Screening or testing of compounds for diagnosis of disorders, assessment of conditions, e.g. renal clearance, gastric emptying, testing for diabetes, allergy, rheuma, pancreas functions
• CPC Class Codes: A61K 9/0056 Mouth soluble or dispersible forms; Suckable, eatable, chewable coherent forms; Forms rapidly disintegrating in the mouth; Lozenges; Lollipops; Bite capsules; Baked products; Baits or other oral forms for animals
• CPC Class Codes: A61P 1/08 for nausea, cinetosis or vertigo; Antiemetics
• CPC Class Codes: A61P 15/10 for impotence
• CPC Class Codes: A61P 43/00 Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
• CPC Class Codes: A61P 9/02 Non-specific cardiovascular stimulants, e.g. drugs for syncope, antihypotensives

Abstract

Impotence can be ameliorated without substantial undesirable side effects by nasal administration of apomorphine, optionally with an antiemetic agent present in an amount sufficient to substantially reduce nausea symptoms that may be associated with the use of apomorphine.

Claims

1. A method of ameliorating erectile dysfunction in a psychogenic male patient which comprises administering to said patient apomorphine or a pharmaceutically acceptable acid addition salt thereof intranasally and in an amount sufficient to induce an erection adequate for vaginal penetration but less than the amount that induces substantial nausea.

2. The method in accordance with claim 1 wherein the amount of apomorphine administered is in the range of about 1 milligram to about 3.75 milligrams.

3. The method in accordance with claim 1 wherein apomorphine is administered as a nasal spray containing hydrochloride salt of apomorphine.

4. The method in accordance with claim 1 wherein the apomorphine is administered together with an anti-emetic agent.

5. A method for diagnosing a male human patient suffering from erectile dysfunction which method comprises the steps of

administering intranasally to the patient at least about 1 milligram of apomorphine;

and thereafter, in response to a visual erotic stimulus,

determining the patient'"'"'s maximum increase in penile circumference;

determining the patient'"'"'s maximum penile rigidity; and

comprising the determined maximum increase and maximum rigidity values against a predetermined base value for erectile dysfunction.

6. The diagnostic method in accordance with claim 5 wherein said maximum increase in penile circumference is determined by measuring penile tip circumference and penile basal circumference, and wherein said maximum rigidity is determined by measuring penile tip rigidity and penile basal rigidity.

7. A method of stimulating dopamine receptors in the mid-brain region of a patient to cause an erection which comprises administering to the patient apomorphine in an intranasal dose containing about 1 to about 3.75 milligrams of apomorphine.

8. The method in accordance with claim 7 wherein the intranasal dose contains about 1.25 to about 2.5 milligrams of apomorphine.

9. The method in accordance with claim 7 wherein the apomorphine is administered together with an anti-emetic agent.

10. The method in accordance with claim 9 wherein the anti-emetic agent is domperidone.