UPRIMA
Indications and Usage
UPRIMA is indicated for the treatment of erectile dysfunction (ED).
Contraindications
UPRIMA is contraindicated in patients with known hypersensitivity to the active substance or any of the excipients in the tablet formulation. In addition, UPRIMA is contraindicated in patients with severe unstable angina, recent myocardial infraction, severe heart failure or hypotension, and other conditions where sexual activity is inadvisable.
Precautions
The efficacy of UPRIMA is patients with spinal cord injuries, or multiple sclerosis, and in patients who have undergone prostatectomy or pelvic surgery is not known. Furthermore, the efficacy of UPRIMA at the recommended doses of 2 and 3 mg has not been established in diabetic patients.
Cardiovascular status. The cardiovascular status of the patients should be considered before initiating any treatment for ED. Patients with preexisting cardiovascular disease have potentially increased cardiac risk during sexual activity. Treatments for ED, including UPRIMA, should not be used in men for whom sexual activity is inadvisable because of underlying cardiovascular status.
UPRIMA should be used with caution in patients with uncontrolled hypertension, known hypotension, or those with a history of postural hypotension. Acute decreases in blood pressure have been noted after UPRIMA administration. Elderly patients may be more prone to such occurrences and are more susceptible to any deleterious consequences.
UPRIMA should be used with caution in patients taking antihypertensives or nitrate medications, owing to the potential for hypotension.
Alcohol. Interaction studies in volunteers where alcohol was given with UPRIMA at higher than recommended doses indicated that consurrent alcohol intake might cause an increase in the incidence and extent of hypotension. Additionally, intake of alcohol can diminish sexual performance. Patients are recommended to avoid excess alcohol consumption prior to taking UPRIMA.
Renal and Hepatic Dysfunction. In patients with renal insufficiency, an increase in apomorphine AUC∞ values and prolongation of the elimination half-life was observed; however, C
max was not significantly altered. The maximum dosage should therefore be limited to 2 mg in patients with severely impaired renal function.
In patients with hepatic insufficiency, significant increases were observed in the AUC∞ values, C
max, and elimination half-life of UPRIMA. Owing to the potential for a higher risk of adverse events in this population, patients with significantly impaired hepatic function should only be given UPRIMA if the benefits outweigh the risks. Such patients may be initiated at the 2-mg dosage level, with care exercised in any dose increase.
Additional Precautions
Interaction studies and/or clinical experience with ondansetron hydrochloride, prochlorperazine maleate, and domperidone indicate that these agents may be given safely with UPRIMA. No studies have been performed with UPRIMA in combinations are not recommended.
UPRIMA should not be given in combination with other centrally acting dopamine agonists or antagonists because of the potential for pharmacodynamic interactions.
No formal drug interaction studies have been performed with antidepressants, anticonvulsants, or other CNS-active agents; however, clinical experience has not indicated the presence of interactions.
The safety and efficacy of UPRIMA use with other treatments for ED have not been studied. Therefore, the use of combinations is not recommended.
No studies on the effects of UPRIMA on the ability to drive and use machines have been performed. Because some patients can eperience dizziness, light-headedness, and, uncommonly, syncope, they should not engage in activities such as driving or operating machinery for at least 2 hours after administration of UPRIMA or until any such symptoms are fully resolved.
All agents for the treatment of ED should be used with caution in patients with anatomical penile deformity (such as angulation, cavernosal fibrosis, or peyronie's disease) or in patients who have conditions (such as sickle cell anemia, multiple myeloma, or leukemia) that may predispose them to priapism. UPRIMA has not been studied sufficiently in these populations.
UPRIMA may uncommonly produce a transient vasovagal syndrome that may manifest as a self-limiting fainting/syncope (incidence <0.20% at the recommended doses). Nearly all (>90%) syncopal episodes were preceded by a prodrome of symptoms that included mild to severe nausea, vomiting, pallor, sweating/hot flushes, and dizziness or light-headedness. If patients experience prodromal symptoms, they shoulf not attempt to stand up, but should lie down and raise their legs until their symptoms resolve.
UPRIMA is not indicated for use in women. Animal reproduction studies have not been conducted with UPRMA. It is not known whether UPRIMA can cause foetal harm in pregnant women or whether it can affect female reproduction capacity. Also, it is not known whether apomorphine passes into breast milk.
UPRIMA is available as a sublingual tablet in 2 dosage strengths: 2 and 3 mg. One tablet of UPRIMA should be administered to achieve an erection. The onset of the effect of 1 tablet typically occures within 18-19 minutes after administration, although the actual onset of the erection may vary from patient to patient. The tablets dissolve under moist conditions, so the patient should be adivsed to drink a small amount of water before taking UPRIMA. Patients dhould allow a minimum of at least 8 hours between doses.
The recommended starting dose of UPRIMA is 2 mg for all patients. If required, the dose can be increased to 3 mf to achieve a therapeutic response. No dose adjustment is necessary for the elderly. Patients with impaired hepatic function may initiate dosing with UPRIMA at 2 mg, and care should be exercised in any dose increase. Patients with significant hepatic impairment should be administered UPRIMA only when the benefit outweights the risk. If patients with renal impairment receive UPRIMA, dosing should be limited to 2 mg.
