Topical Anesthetics for Delaying Ejaculation

[13] Mean maximal plasma concentrations of dapoxetine decreased slightly after a cenforce professional 100 high-fat meal, from 443 ng/mL (fasted) to 398 ng/mL (fed), and were delayed by approximately 0.5 hours following a high-fat meal (1.3 hours fasted, 1.63 hours fed).

• Dapoxetine used before sex provides quick relief from PE.
• Topical anesthetic applications should be tailored to individual needs.
• SSRIs may cause delayed orgasm or decreased sexual desire.
• Tramadol is an alternative but carries substantial risks.
• Training with behavioral techniques can lead to lasting improvements.
• Fatigue and stress reduction support sexual performance.
• Pelvic floor strengthening is a natural method to control ejaculation.
• Psychological support addresses underlying emotional issues.
• Mechanical aids are an option for some men.
• Combining medications with psychotherapy enhances efficacy.
• Avoid self-medicating without professional advice.
• Consistent follow-up optimizes long-term management.

There was no effect of food on elimination of this agent, with < 5% of peak plasma concentration being present 24 hours after oral administration. Interestingly, the most frequent AE with dapoxetine is nausea, which was decreased after a high-fat meal (24% of fasted and 14% of fed subjects). Perhaps a complete steak dinner will be required with this medication for the patients who complain of nausea. The question of daily dosing and accumulation was reported in a study of 42 healthy males.

• Dapoxetine is specifically designed for on-demand use in PE.
• Topical anesthetics require minimal use to avoid excessive numbness.
• SSRIs impact neurotransmitters involved in ejaculation control.
• Tramadol's side effects limit its routine use for PE.
• Non-drug approaches include psychological counseling and exercises.
• Pelvic strengthening exercises aid in delay of ejaculation.
• Partner education enhances understanding and support.
• Managing stress and anxiety can significantly improve PE.
• Some therapies combine medication with sex therapy sessions.
• Medical evaluation is essential before initiating treatment.
• Lifestyle factors like smoking can influence sexual performance.
• Patient adherence to treatment plans improves outcomes.

[14] Dapoxetine was rapidly absorbed with mean maximal plasma concentrations achieved at 1.01 and 1.27 hours after single doses of dapoxetine 30 and 60 mg. With repeated daily dosing, steady-state plasma concentrations were reached within 4 days, with modest accumulation (1.5-fold).

How Do You Treat Premature Ejaculation?

The only objective criterion for PE that has been globally accepted is a nonexistent or severely shortened intravaginal ejaculatory latency time (IELT). This translates simply into ejaculation that occurs after intromission and "too soon." Subjective criteria have focused on 3 parameters: (1) reduced control over ejaculation; (2) decreased patient and/or partner satisfaction with intercourse, and (3) patient and/or partner distress or bother about the condition. Few men and/or their partners can define a "normal" time to ejaculation. In one 4-week, multicenter, US observational study in males at least 18 years of age with and without PE, data was collected from both men and their partners, including IELT, using a stopwatch and subjective patient-reported outcome measures. [3] This study included 207 men with PE diagnosed using the DSM-IV TR criteria and 1380 men without PE.

Sex therapy

Stepwise logistic regression analysis was used to determine the significant factors associated with the diagnosis of PE and were identified as: control over ejaculation, personal distress, and IELT less than 2 minutes. While IELT does discriminate between men with and without PE, substantial overlap between these groups exists when IELT is used alone. Discrimination between men with and without PE is enhanced substantially when the 2 subject-reported measures (control of ejaculation and personal distress) are used in combination with IELT in a clinical evaluation. While stopwatch IELT is mandated for use in clinical trials, estimated IELT is more commonly used in clinical practice. A study was performed to determine the how closely objective measurement of IELT matches estimated IELT.

Information to gather in advance

[4] From observations of 207 men with PE and 1380 men without PE, each subject was asked to estimate his IELT at the first study visit. Following this visit, subjects and partners were provided with a stopwatch and event log. The IELT of each episode of sexual intercourse during the ensuing 2-week study interval was measured and recorded by the female partner. The results showed both PE and non-PE subjects slightly overestimated their IELT compared with the stopwatch-recorded IELT. For subjects with PE, the mean measured value of IELT was 1.8 minutes and the mean estimated value was 2.0 minutes. Elimination of dapoxetine was rapid and biphasic, with initial and terminal half-lives of 1.4 and 20 hours.

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The authors concluded that the pharmacokinetic profile of dapoxetine is ideally suited to an on-demand oral therapy for PE.

What causes premature ejaculation?

For subjects without PE mean measured value was 7.3 minutes and estimated value was 9.0 minutes. Hence, patient-estimated IELT is generally reliable (although slightly high) and for clinical purposes a stopwatch-assessment is not mandatory. According to a number of academic and pharmaceutical-company-sponsored epidemiologic studies, PE affects an estimated 25% to 35% of men aged 18 to 59 years. In a corresponding community practice-based study, 614 men were asked to complete 13 demographic questions and the 32-question Male sex tablet 100mg Sexual Health Questionnaire (MSHQ). [5] PE was the most common sexual dysfunction (32.7% of men), with ED (10.6%) and decreased libido (10.3%) ranked second and third.

More Information

Men with PE were found to be significantly less likely to be satisfied with their overall sexual relationship, quality of sex life, and their overall partner relationship. Besides the behavioral approaches mentioned previously, clinicians have focused on topical and medical treatments of PE. Topical treatments (anesthetics and SS-cream) appear to increase IELT, but are associated with mild local adverse effects (AEs), may be messy, can be indiscreet, and require partner cooperation. Frequent use can lead to anorgasmia, anejaculation, and genital numbness in the female. PDE5 inhibitors are effective in the treatment of secondary PE when caused by mild ED.

Clomipramine (Anafranil)

[2] By improving a man's failing erections, it is hypothesized that his anxiety is reduced, thereby alleviating his secondary PE. Selective serotonin reuptake inhibitors (SSRIs), which were found to delay ejaculation, have been used off-label for the treatment of PE for the last 1 to 2 decades. The optimal dose and regimens for these agents for the treatment of PE have not been established; however, data show greater success with chronic vs on-demand (PRN) dosing. However, chronic use of SSRIs is associated with a variety of AEs, including dry mouth, nervousness, gastrointestinal upset, diarrhea, headache, drowsiness, and restlessness. These AEs make current SSRIs less than ideal for the treatment of PE. Even though PE is the most common male sexual dysfunction, it seems to be under-reported by patients and underestimated by physicians.

• Dapoxetine has a rapid onset, typically within 1-3 hours.
• Topical anesthetics should be applied in small amounts to avoid overdose.
• SSRI side effects may include sleep disturbances or gastrointestinal upset.
• Tramadol can cause dizziness, dry mouth, and nausea as side effects.
• Behavioral techniques teach men to recognize early signs of ejaculation.
• Pelvic floor training can enhance ejaculatory control.
• Counseling sessions help address performance anxiety and stress.
• Medications should be used as prescribed to minimize risks.
• Some men respond better to combination therapies.
• Abstaining from excessive masturbation may help in some cases.
• Lifestyle changes and psychological support are important adjuncts.
• Any medication or supplement should be discussed with a healthcare professional.

There have been 2 large surveys conducted -- one that looked at the prevalence and attitudes regarding PE among 11,543 men from the United States, Germany, and Italy, and another querying 271 physicians (primary care physicians, urologists, and psychiatrists) from the United States, Germany, Italy, and Mexico..[15] Seventy-two percent of men with self-reported PE claimed significant worry about their ability to last during intercourse, with 59% reporting frustration at climaxing too soon. In contrast, > 90% of physicians thought that PE caused only minor or no distress to their patients. Approximately 12% of men stated that they had consulted a physician for this condition, with 80% claiming to have initiated the conversation and 85% reporting little or no improvement from this medical interaction.

Treatment Options for Premature or Rapid Ejaculation at UCLA

The ideal drug for PE should have a number of characteristics: (1) its use should be discreet, preferably oral; (2) it would have a rapid onset of action (< 1 hour), rapid elimination, and minimal accumulation; (3) it should have good tolerability with few AEs; (4) it should be effective on demand, without requiring chronic use or a loading dose; and (5) it should have demonstrated efficacy on IELT and patient-related outcomes in large-scale, long-term, placebo-controlled trials. None of the current off-label medications fulfill all these criteria. In a community-based practice study 32.7% (201/614) of men reported PE. [6] None of the men with self-declared PE in this study were currently seeking a treatment, but most (80%) reported that if they sought treatment for PE, their primary goal would be sexual satisfaction for both themselves and their partner. Eighty-one percent reported that a pill to prolong IELT would be their treatment of choice.

How can I prevent premature ejaculation?

Dapoxetine hydrochloride is the first oral compound developed specifically for the treatment of PE. In preclinical studies, dapoxetine was found to be a potent inhibitor of serotonin reuptake and is considered by authorities in the field to be a serotonin transporter inhibitor. In experimental animal studies, researchers from Paris, France, evaluated the emission and expulsion phases of ejaculation using p-chloroamphetamine-induced ejaculation in anesthetized rats. [7] Different doses of intravenous dapoxetine reduced both the emission and expulsion phases in a dose-dependent manner. Similar experiments in the same anesthetized-rat model were conducted to elucidate the drug's mechanism of action.

Ejaculation Problems: Too Fast, Too Slow or Not at All

These studies revealed that dapoxetine worked by increasing the pudendal motor neuron reflex latency period. Dapoxetine has previously demonstrated its efficacy in the treatment of PE in 2 identically designed, double-blind, randomized, placebo-controlled, 12-week phase III trials. [9] An open-label, long-term (1 year) on-demand study of dapoxetine efficacy was presented. [10] Of the 1774 men enrolled in the 3-month studies (placebo, dapoxetine 30 mg and 60 mg) all were provided with dapoxetine 60 mg to be taken as needed 1 to 3 hours before sexual intercourse. Patients were evaluated at 1, 2, 3, 6, and 9 months in this extension study. Clearly, PE is a common and distressing condition for a sizeable segment of the male population.

Therapy Type	Description	Typical Duration	Success Rate	Noted Benefits	Noted Drawbacks
SSRI Medications	Selective serotonin reuptake inhibitors, delay ejaculation	4-12 weeks	70%	Long-term control	Possible side effects
Behavioral Therapy	Techniques like start-stop and squeeze method	Several sessions	60-80%	No medication needed	Requires patient commitment
Topical Anesthetics	Numbing creams or sprays applied to glans penis	As needed	65-75%	Fast onset	Reduced sensation, partner sensitivity
Pelvic Floor Exercises	Exercises to strengthen pubococcygeus muscles	6-12 weeks	50-65%	Improves control	Time-consuming

Patients and couples often seek expensive and ineffective off-label therapies.

Drug Name	Approval Year	Primary Use	Recommended Dosage	Prescription Needed	Monitor Required	Typical Side Effects
Dapoxetine	2009	Premature ejaculation	30 mg before sex	Yes	Yes	Nausea, dizziness
Paroxetine	Approved for other uses, off-label for PE	20 mg/day	Yes	Yes	Yes	Fatigue, sexual dysfunction
Sertraline	Approved for depression, off-label for PE	50 mg/day	Yes	Yes	Yes	Insomnia, digestive issues

Education about PE, its prevalence, and beneficial therapies for both consumers and physicians is urgently needed.

Side Effect	Medication Type	Incidence Rate	Severity Level	Management Strategies	Notes
Nausea	SSRIs, topical anesthetics	10-15%	Mild to Moderate	Dose adjustment, timing	Usually transient
Dizziness	SSRIs, topical anesthetics	8-12%	Mild	Standing slowly, hydration	Common with beginning treatment
Headache	SSRIs, topical anesthetics	5-10%	Mild	Analgesics, time to adjust	Typically diminishes over time
Reduced Sensation	Topical anesthetics	10-20%	Mild	Reduced dose, application timing	Can affect partner satisfaction

Althof S, Rowland D, McNulty P, Rothman M. Evaluation of the impact of premature ejaculation on a man's self esteem, confidence, and overall relationship.

Find your care

The final results showed that the improvements in satisfaction with sexual intercourse, control of ejaculation, symptom severity, and benefit from the medication were maintained through the duration of the study. Further analysis of the data sets from different groups of researchers revealed that dapoxetine equally improved IELT in men with both acquired and lifelong PE. [11] Additionally, men with PE who had the lowest IELTs appeared to benefit most. Men with a baseline IELT < 30 seconds had a 6.8-fold increase; those with a baseline IELT > 30 seconds and < 1 minute had a 4.4-fold increase; and those with baseline IELT > 1 minute and ≤ 2 minutes had a 3.2-fold increase. Additional studies involving dapoxetine showed minimal food effects.