Dapoxetine 30mg Tablet
Dapoxetine was created by dapoxetine 5mg Eli Lilly and in phase I clinical trial as an antidepressant. It never worked out well as a medication for the treatment of depression, though, and was shelved for a while before subsequently developed to treat PE. In December 2003, Eli Lilly sold the patent for dapoxetine to Pharmaceutical Product Development (PPD) for US$65 million. Eli Lilly may also receive royalties payment from PPD if the sale exceeds a certain amount. Research into the effectiveness of dapoxetine was revisited in 2020. ALZA is the current owner of dapoxetine, but PPD will receive milestone payments and drug royalties from ALZA. If approved, dapoxetine will be marketed in the US by Ortho McNeil pharmaceutical, Inc. Ortho McNeil and Janssen-Ortho Inc, or Janssen-Cilag are all units of Johnson & Johnson.
- Post-marketing surveillance continues for rare side effects.
- Priapism is a rare but serious urological emergency.
- Patients experiencing prolonged erection must seek help.
- Syncope can lead to falls and injury.
- Taking the first dose in a safe setting is advised.
- Blood pressure monitoring may be recommended.
- It can cause dose-dependent increases in heart rate.
- Patients with uncontrolled hypertension should avoid it.
- It is not studied in men with significant cardiovascular disease.
- Sexual activity itself poses cardiac risk for some.
- A pre-treatment cardiovascular assessment may be needed.
- The decision involves balancing cardiac and sexual health.
As at 2005, dapoxetine was in phase III clinical trials, pending review by the FDA.
| Step | Instructions | Timing Tips |
|---|---|---|
| Dose | 30 mg taken 1-3 hours before intercourse | Do not exceed once daily |
| Adjustment for elderly | Use lower doses if necessary | Under medical supervision |
| Missed dose | Skip if missed; do not double dose | Not relevant, as timing is pre-sex |
Dapoxetine has been marketed and approved in more than 50 countries.
Rights and permissions
Dapoxetine should not be used in men with moderate to severe hepatic impairment and in those receiving CYP3A4 inhibitors such as ketoconazole, ritonavir, and telithromycin. Dapoxetine also cannot be used in patients with heart failure, permanent pacemaker, or other significant ischemic heart disease. Caution is advised in men receiving thioridazine, monoamine oxidase inhibitors, SSRIs, serotonin-norepinephrine reuptake inhibitors, or tricyclic antidepressants. If a patient stops taking one of these drugs, he should wait for 14 days before taking dapoxetine. If a patient stops taking dapoxetine, he should wait for 7 days before receiving these drugs.
Chemical Names
The most common effects when taking dapoxetine are nausea, dizziness, dry mouth, headache, diarrhea, and insomnia. [16][17] Discontinuation rates due to adverse effects and costs are very high, as demonstrated in a study in Asia which showed that cumulative discontinuation rates within one year are as high as 87%. [18] Unlike other SSRIs used to treat depression, which have been associated with high incidences of sexual dysfunction,[19] dapoxetine is associated with low rates of sexual dysfunction. Taken as needed, dapoxetine has very mild adverse effects of decreased libido (<1%) and erectile dysfunction (<4%). No case of drug overdose has been reported during clinical trials.
Cardiovascular safety
Many men who have PE also suffer from erectile dysfunction (ED). Treatment for these patients should consider the drug–drug interaction between dapoxetine and PDE5 inhibitors such as tadalafil (Cialis) or sildenafil (Viagra). In Dresser study (2006), plasma concentration of 24 subjects was obtained. Half of the sample pool were treated with dapoxetine 60 mg plus tadalafil 20 mg; the other half were treated with dapoxetine 60 mg plus sildenafil 100 mg. These plasma samples were then analyzed using liquid chromatography-tandem mass spectrometry. [39] Dapoxetine has been approved in Italy, Spain, Mexico, South Korea, and New Zealand in 2009 and 2010; marketed in Sweden, Austria, Germany, Finland, Spain, Portugal, and Italy. It has also been approved in France, Russia, Malaysia, Philippines, Argentina, and Uruguay.
- Storage temperature is usually below 25°C or 77°F.
- The bottle should be kept tightly closed.
- Moisture protection is important for stability.
- It should be kept out of sight and reach of children.
- Accidental ingestion by a child requires immediate medical help.
- In case of overdose, symptoms may be severe.
- Overdose symptoms include serotonin syndrome, vertigo, and vomiting.
- There is no specific antidote; treatment is supportive.
- Contact a poison control center immediately.
- The prescriber should be informed of any overdose.
- The prescribed quantity is often limited to reduce overdose risk.
- Doctors may prescribe only a few tablets at first.
784 - Lists of Narcotic, Psychotropic, Precursor, and Other Substances under Special Control] (in Brazilian Portuguese).
| Product | Dosage | Quantity + Bonus | Price | |
|---|---|---|---|---|
| Levitra Generic | 60mg | 270 + 10 Pills | 714.53€ 680.50€ | |
| Priligy Generic Dapoxetine | 60mg | 90 + 10 Pills | 265.64€ 252.99€ | |
| Levitra Original | 20mg | 48 + 4 Pills | 235.14€ 223.94€ | |
| Priligy Generic Dapoxetine | 60mg | 60 + 8 Pills | 183.06€ 174.34€ | |
| Priligy Generic Dapoxetine | 60mg | 10 Pills | 47.63€ 45.36€ | |
| Priligy Generic Dapoxetine | 60mg | 20 + 4 Pills | 77.31€ 73.63€ | |
| Priligy Generic Dapoxetine | 60mg | 120 + 10 Pills | 341.26€ 325.01€ | |
| Viagra Soft Tabs | 100mg | 180 + 10 Pills | 314.95€ 299.95€ | |
| Cialis Professional | 20mg | 10 Pills | 48.29€ 45.99€ | |
| Priligy Generic Dapoxetine | 60mg | 30 + 6 Pills | 106.65€ 101.57€ | |
| Viagra Generic | 50mg | 30 + 4 Pills | 54.26€ 51.68€ | |
| Priligy Generic Dapoxetine | 60mg | 180 + 10 Pills | 494.76€ 471.20€ | |
| Kamagra Polo | 100mg | 84 + 4 Pills | 244.49€ 232.85€ | |
| Viagra Generic | 200mg | 10 Pills | 40.96€ 39.01€ | |
| Viagra Soft Tabs | 100mg | 60 + 6 Pills | 152.94€ 145.66€ | |
| Levitra Original | 20mg | 92 + 4 Pills | 406.22€ 386.88€ |
Archived from the original on 2023-08-03. "Dapoxetine, a novel treatment for premature ejaculation, does not have pharmacokinetic interactions with phosphodiesterase-5 inhibitors". "Dapoxetine: a new option in the medical management of premature ejaculation". ^ "Priligy is used to Treat Premature Ejaculation".
2. What should I know before I take PRILIGY?
The results showed that dapoxetine does not alter the pharmacokinetics of tadalafil or sildenafil. Alcohol does not affect the pharmacokinetics of dapoxetine when taking concurrently. The mechanism through which dapoxetine affects premature ejaculation is still unclear, but dapoxetine is presumed to work by inhibiting serotonin transporter (SERT) and subsequently increasing serotonin's action at pre- and postsynaptic receptors. [22] Human ejaculation is regulated by various areas in the central nervous system (CNS). These signals are passed on to the brain stem, which then is influenced by a number of nuclei in the brain such as medial preoptic and paraventricular nuclei.
Molecular Weight
[24] Clement's study performed on anaesthetized male rats showed that acute administration of dapoxetine inhibits ejaculatory expulsion reflex at supraspinal level by modulating activity of lateral paragigantocellular nucleus (LPGi) neurons. These effects cause an increase in pudendal motoneuron reflex discharge (PMRD) latency, though whether dapoxetine acts directly on LPGi or on the descending pathway in which LPGi located is unclear. Dapoxetine is a white, powdery, water-insoluble substance. Taken one to three hours before sexual activity, it is rapidly absorbed in the body. Its maximum plasma concentration (Cmax) is reached one to two hours after oral administration.
Neurocognitive safety
The Cmax and AUC (area under tadalafil with dapoxetine online the plasma vs. time curve) is dose dependent. The Cmax and Tm (time needed to obtain the maximum plasma concentration) after single doses of dapoxetine 30 mg and 60 mg are 297 and 498 ng/ml at 1.01 and 1.27 hours, respectively. A high-fat meal does reduce the Cmax slightly, but it is insignificant. It can be taken with or without food. ^ a b c "Australian Public Assessment Report for Dapoxetine" (PDF). "Pharmacokinetic and pharmacodynamic features of dapoxetine, a novel drug for 'on-demand' treatment of premature ejaculation". "Dapoxetine: an evidence-based review of its effectiveness in treatment of premature ejaculation". ^ "Furiex Pharma gets rights to Priligy, some of which it sells on to Menarini". "New agents in the treatment of premature ejaculation".
Precautions and Warnings
Currently, very few methods are used to synthesize (S)-dapoxetine. This novel approach consists of only six steps in which three main steps are shown above. The initial reactant is trans-cinnamyl alcohol, which is commercially available. Sharpless asymmetric epoxidation and Mitsunobu reaction have been used to produce expected (S)-dapoxetine. This method is considered a good choice compared to the known methods due to high yield and easily obtainable reactants. "Efficacy and tolerability of dapoxetine in treatment of premature ejaculation: an integrated analysis of two double-blind, randomised controlled trials". "Dapoxetine has long-term efficacy in the treatment of premature ejaculation". "AUA guideline on the pharmacologic management of premature ejaculation". "Dapoxetine: An Innovative Approach in the Therapeutic Management In Animal Model of Depression". "Antistress and antidepressant properties of dapoxetine and vortioxetine".
- The safety profile of dapoxetine 30mg shows most side effects are mild.
- Some men experience flushing or increased sweating after taking the pill.
- 30mg is considered an initial dose before evaluating effectiveness and tolerability.
- Combination with other drugs prolonging QT interval is discouraged.
- Inform the doctor if you have a history of seizures or epilepsy.
- Avoid seizure triggers such as excessive alcohol or sudden medication changes.
- Patients with severe depression should discuss risks before taking dapoxetine.
- In case of overdose, seek emergency medical attention immediately.
"Dapoxetine for the treatment of premature ejaculation: results from a randomized, double-blind, placebo-controlled phase 3 trial in dapoxetine sex 22 countries". "Discontinuation of Dapoxetine Treatment in Patients With Premature Ejaculation: A 2-Year Prospective Observational Study".
- The chemical is a derivative of naphthalene.
- Its synthesis involves multiple chemical steps.
- The hydrochloride salt form improves stability.
- Excipients in the tablet aid manufacturing and release.
- These may include microcrystalline cellulose and magnesium stearate.
- The film coat may contain hypromellose.
- The formulation is designed for rapid disintegration.
- This allows for quick release of the active ingredient.
- Bioequivalence studies ensure generics perform the same.
- Switching between brands is generally acceptable.
- However, patients should consult their pharmacist.
- Consistency in product may help some patients.
"Incidence of sexual dysfunction associated with antidepressant agents: a prospective multicenter study of 1022 outpatients. Spanish Working Group for the Study of Psychotropic-Related Sexual Dysfunction". "Dapoxetine-A Novel Drug for Premature Ejaculation".
7. Product details
Dapoxetine is absorbed and distributed rapidly in the body. The mean steady-state volume is 162 L. Its initial half-life is 1.31 hours (30 mg dose) and 1.42 hours (60 mg dose), and its terminal half life is 18.7 hours (30 mg dose) and 21.9 hours (60 mg dose). Dapoxetine is metabolized extensively in the liver and kidney by multiple enzymes such as CYP2D6, CYP3A4, and flavin monooxygenase 1. The major product at the end of the metabolic pathway is circulating dapoxetine N-oxide, which is a weak SSRI and contributes no clinical effect.
Do not take PRILIGY if:
The metabolites of dapoxetine are eliminated rapidly in the urine with a terminal half-life of 18.7 and 21.9 hours for a single dose of 30 mg and 60 mg, respectively. The cardiovascular safety profile of dapoxetine has been studied extensively during the drug development. Phase I trials showed that dapoxetine had neither clinically significant electrocardiographic effects nor delayed repolarization effects, with dosing up to four-fold greater than the maximum recommended dosage, which is 60 mg. Phase III studies in men with PE showed a safety and well tolerated profile of dapoxetine with dosing of 30 and 60 mg. No cardiovascular adverse had been found.
Cite this article
Studies of SSRIs in patients with major psychiatric disorders prove that SSRIs are potentially associated with certain neurocognitive adverse effects such as anxiety, akathisia, hypomania, changes in mood, or suicidal thought. [30][31] No study on the effects of SSRIs in men with PE has been done. McMahon's study in 2012 showed that dapoxetine has no effect on mood and is not associated with anxiety or suicidality. The incidence of antidepressant discontinuation syndrome symptoms in men using dapoxetine to treat PE has been described by reviewers as low or no different from the incidence of such symptoms in men withdrawn from placebo treatment. [33][34] The lack of chronic serotonergic stimulation with on-demand dapoxetine minimizes the potentiation action of serotonin at synaptic cleft, thus decreasing the risk of discontinuation symptoms. "Dapoxetine for the treatment of premature ejaculation: Lack of interaction with ethanol". "Monoaminergic transporter binding and inhibition profile of dapoxetine, a medication for the treatment of premature ejaculation". "Physiology of ejaculation: emphasis on serotonergic control". "Supraspinal site of action for the inhibition of ejaculatory reflex by dapoxetine". "Efficacy and safety of dapoxetine for the treatment of premature ejaculation: integrated analysis of results from five phase 3 trials". ^ "Dapoxetine: a guide to its use in premature ejaculation".
| Country | Legal Status | Prescription Requirement |
|---|---|---|
| USA | Prescription-only drug | Prescription required |
| UK | Prescription-only medication | Must be prescribed by healthcare provider |
| Australia | Schedule 4 (Prescription Only) | Prescription mandatory |
"Pharmacokinetics of single and multiple escalating doses of dapoxetine in healthy volunteers". "Cardiovascular safety profile of dapoxetine during the premarketing evaluation".
