Durapil 30 S.P.M medicine for premature ejaculation in men (1 blister x 10 tablets)

Dosage form Box of 1 blister x 10 tablets
Specifications Dapoxetine
Ingredient SPM Joint Stock Company - Vietnam

Ingredient

Composition information	Content
Dapoxetine	30mg

Uses

indications

Durapil drugs are indicated in the following cases:

Used in cases of premature ejaculation in men aged 18 - 64 with the following symptoms:

persistent ejaculation and relapse when there is a minimum sexual stimulation, before, during or after penetration, before the patient is intended.

dapoxetin is a selective reabsorption inhibitor Serotonin (SSRI) with IC50 at 1.12 nm, while the metabolic product of dapoxetin, is Desmethyl dapoxetin (IC50 Ejaculation activities in people are mainly active through the intermediaries of the sympathetic nervous system. The path of signaling for ejaculation is derived from the center of the spinal cord, to the intermediate of the brain body, which is first influenced by some of the background in the brain.

The mechanism of effects of dapoxetin in the treatment of premature ejaculation is thought to be related to the inhibition of Serotonin reabsorption in nerve cells and inhibit the nerve transmission voltage in the cash receptor and the synap. In the mouse, dapoxetin inhibits premature ejaculation by impacting the brain hemisphere, namely the location of specialized base areas (LPGI). The sympathetic lymph nodes that distribute the nerves that dominate the vermato bags, the vas deferens, the prostate, the sphincter and the bladder neck make them shrink in a combination way to achieve ejaculation. Dapoxetin coordinates this ejaculation reflex in mice.

Effective and safety

Research on the effectiveness of dapoxetin in the treatment of premature ejaculation has been carried out, clinical trials of placebo, double blindness, including a total of 6081 randomly selected objects. The object is 18 years old and has a history of premature ejaculation in most of the intercourse within 6 months before participating in the study. Premature ejaculation is defined according to the DSM-IV diagnostic criteria: Short intercourse time (IELT: The time from the time of penetration into the vagina to the time of ejaculation in the vagina) ≤ 2 minutes, measured of stopwatch in four studies), weak ejaculation control, acknowledging difficulties with the maintenance of intercourse of love couples in specific conditions.

Object with other forms of sexual dysfunction, including erectile dysfunction, or those who use other pharmaceuticals to treat premature ejaculation are all eliminated from research.

The results of all random studies have been agreed. The effect has been proven after 12 weeks of treatment. A study collected patients who undergo 24 -week treatment. In the study, 1162 subjects were randomly selected, 385 placebo users, 388 dapoxetin users 30mg when necessary. The average value and average medium value IELT (intercourse time) at the end of the study are presented below. Other studies and analysis of data combined at week 12 have given appropriate results.

Table 2: Statistics of the end of the study He

1.05 minutes 1.72 minutes

[0.37, 0.72]

The smallest average area 1.7 minutes 2.9 minutes

[0.59, 1.72]

Pharmaceutical 14.3 26.0 6 5.0 11.7 have the previous background value. Clinical associated effectively dapoxetin treatment is continued to prove when patients report the differences between before and after the drug and the results of analysis of the level of treatment.

Meeting the treatment is defined as a patient with at least one increase in 2 - items in controlling the pure, besides at least 1 decrease - the premature ejaculation item. The significant higher rate of statistics of the objects responded in each dapoxetin group compared to the placebo on the weekend of the 12th or 24th research week. The percentage of the high response in the group using Dapoxetin 30 mg (11.1% - 95% CI [7.24; 14.87]) compared to the placebo group in week 12.

The association between the effect of Dapoxetin clinical treatment is represented by the Clinical Global Impression of Change (CGIC), in which patients are required to compare their premature ejaculation from the start of research, with different reaction items options, from much better to worse. At the end of the study (Week 24), 28.4% (group 30 mg) of subjects reporting their status is "good" or "much better", compared to 14% in the placebo group, while 53.4% of the subjects are treated with Dapoxetin 30 mg, corresponding to the status report "a little better", compared to 28.8% in the placebo group.

pharmacokinetics

absorption:

dapoxetin is quickly absorbed at maximum dose in plasma (CMAX) reaching approximately 1-2 hours after taking the drug. Birth completely is 42% (about 15 - 76%). After taking a 30mg oral dose of hunger, the peak concentration of dapoxetin plasma is 297 mg/ml, after 1.01 hours. When eating a lot of fat will reduce CMAX (about 10%) and increase the area under the curve (AUC concentration of about 12%) of dapoxetin and slow down a little time to reach the peak concentration of dapoxetin. However, when consuming more fat will not affect the absorption process. These changes have no clinical significance. So you can take medicine when hungry or when full.

distribution: There are more than 99% dapoxetin is connected to people's plasma proteins in in vitro studies. The active metabolites are desmethindapoxetin associated with 98.5% with protein. Dapoxetin is quickly distributed with an average volume of 162L. After intravenous injection for humans, the initial average disposal time is 0.10 hours, the intermediate selling time is 2.19 hours, the last waste sale time is 19.3 hours.

metabolism:

In vitro studies suggest that dapoxetin is metabolized by an enzyme system in the liver and kidneys, mainly CYP2D6, CYP3A4 and Flavin Monooxygenase (FMO1). Dapoxetin is converted mainly into many different types of metabolites, mainly through the path of biological conversion: N-Oxidatio, N-Demethylation, Naphthyl Hydroxylation, Glucoronidation and Sulfation. Dapoxetin is not metabolized and dapoxetin - N - oxide are two main substances circulated in plasma. The auxiliary metabolites include desmethyldapoxetin that meets the equivalent of dapoxetin and didesmethyldapoxetin, accounting for about 50% of dapoxetin effect. In metabolites, only desmethyldapoxetin can contribute to the effect of dapoxetin in in vivo. The half -life of desmethyldapoxetin is equivalent to dapoxetin.

excretion: Dapoxetin metabolites are mainly eliminated in the urine in the form of the next form. The non -metabolic drug is not determined in the urine. Dapoxetin is quickly eliminated, based on evidence that the remaining concentration is very low after 24 hours (less than 5% of the peak concentration). There is a small amount of dapoxetin accumulated after daily dose. The final half -life is approximately 19 hours after taking the medicine.

Special subjects:

Ded metabolic active ingredients contribute to the pharmacological effects of dapoxetin, especially when the contact is up. In some populations, the active substance metabolizes increases normally.

It is a total of free and dapoxetin molecules. Ded and dapoxetin are equal. Studies assume that Ded's distribution is equal in the central nervous system but it is not known whether this is accurate.

race:

Analysis of clinical pharmacological studies using dapoxetin 60 mg single dose shows that there is no statistical significance difference between white, black, Spanish and Asian people.

A clinical study conducted to compare the pharmacokinetics of dapoxetin on subjects in Japan and whiten races showed that the plasma concentration of dapoxetin is 10% to 20% higher (AUC and the peak concentration) in the Japanese due to lower body weight. This higher job does not make sense in terms of clinical.

Elderly:

Analysis of clinical pharmacological studies using dapoxetin 60 mg single dose shows that there is no significant difference in pharmacokinetic parameters (CMAX, Aucinf, Tmax) between healthy elderly men and healthy young men. Efficiency and safety have not been established in this population.

Patients with renal failure:

A clinical pharmacological study used the only 60 mg dapoxetin dose has been conducted in people with mild renal failure (CRC1 50-80 ml/minute), average (CrCl 30 to 80 mL/minute). There is no clear relevance to the increase in the AUC of dapoxetin with the reduced renal function. AUC in severe kidney failure is approximately twice in subjects with normal renal function, although there are limitations of collecting data in patients with severe renal failure. Dapoxetin's pharmacobi has not been studied in patients with dialysis.

Patients with liver failure: In patients with mild liver failure, the free cmax of dapoxetin is reduced by 28% and the free AUC does not change. Free cmax and AUCs of the active ingredients (all dapoxetin and desmethyl dapoxetin) are 30% and 5% sequentially. In patients with moderate liver failure, free cmax of dapoxetin does not change (down 3%) and free AUC increases 66%. The free cmax and AUCs of the active ingredient are basically unchanged and double, respectively. In patients with severe liver failure, dapoxetin's cmax decreased by 42% but AUC increased by about 223%. CMAX and AUC of the active ingredient have changed the same.

polymorphic genotype CYP2D6:

In clinical pharmacological research using the only dose Dapoxetin 60 mg, found that people with poor metabolic CYP2D6 have a higher plasma drug concentration than a group of people with good metabolic CYP2D6 (CMAX is about 31% higher for and 36% higher for dapoxetin and CMAX higher than 98% for and AUCINF 161% higher for desmethyl dapoxetin). CMAX and AUC of the active ingredient of dapoxetin can increase by about 46% and about 90%. This increase can lead to higher risks and the severity of the side effects of the drug depends on the dose. The safety of dapoxetin in groups of people with poor metabolic CYP2D6 should pay special attention when using other drugs that can inhibit metabolism of dapoxetin as medium and strong CYP3A4 inhibitors.

Before taking Durapil 30 S.P.M medicine for premature ejaculation in men (1 blister x 10 tablets)

How to use

oral tablets. Take the tablet with a glass of water.

Dosage

Men from 18 - 64 years old:

The starting dose is 30mg in all cases, taking before sex from 1-3 hours. If the 30mg dose is ineffective and an acceptable side effect, it may increase the dose to a maximum dose of 60 mg. The maximum dose when used regularly is once in 24 hours. The drug can be used with food or not.

Doctors who prescribe Durapil 30 need the risk of risks with the effects that bring patients after the first 4 weeks of use or after 6 doses of Durapil 30 to assess the balance between benefits and risks to consider whether to continue treatment with Durapil 30.

Older people over 65 years old:

The dosage has not been determined to be safe and effective when using dapoxetin in groups of people over 65 years old.

Children and teenagers:

Do not take medicine for people under 18 years old.

Persons impaired kidney and liver function:

No need to adjust the dose on patients with moderate renal impairment, mild liver failure. Do not use dapoxetin for patients with severe renal impairment, medium and severe liver failure.

Patients with poor metabolic CYP2D6 or patients treated with strong CYP2D6 inhibitors: Be careful when increasing the dose to 60 mg in patients is known to have weak metabolic CYP2D6 genotype or in patients who use simultaneously treated with strong CYP2D6 inhibitors.

Patients are treated with moderate or strong inhibitors or CYP3A4: Concomitance of strong CYP3A4 inhibitors is contraindicated. The dose should be limited to 30mg when patients use simultaneously treated with medium CYP3A4 inhibitors and need to be cautious.

Note: The above dose is for reference only. Specific dosage depends on the condition and level of progression of the disease. For a suitable dose, you need to consult a doctor or medical specialist.

What to do when overdose?

There are no unexpected adverse effects with daily doses of up to 240 mg (two doses of 120 mg for 3 hours apart). In general, overdose symptoms include side effects such as drowsiness, gastrointestinal disorders such as nausea and vomiting, tachycardia, tremor, agitation and dizziness.

In case of overdose, should take supportive treatments.

Due to the high protein cohesion and the distribution of dapoxetin hydrochloride wide throughout the body, so diuretics, dialysis, blood transfusion and dialysis seem to be ineffective. There is currently no effective antidote for dapoxetin hydrochloride.

What to do when you forget 1 dose? However, if the time to relax with the next dose is too short, skip the dose and continue the calendar of the drug. Do not use double doses to compensate for missed dose.

Side Effects

When using the drug, there are common unwanted effects (ADR) such as:

Table 1: Frequency of Adverse Reactions (Meddra) 1/10)

Uncommon (≥ 1/1000 to 1

rare (≥ 1/10000 to 1 Abnormal, reducing sexual desire depression, depression, manic, stress, apathy, indifference, confusion state, loss of orientation, sensitivity, sleep disorders, initial insomnia, nightmares, grinding teeth, loss of sexual desire, pleasure disorders In the beginning
drowsy, disordered in concentration, trembling, abnormal fainting, fainting due to vague nerve reflexes, dizziness posture, restlessness, bitter mouth, drowsiness, sleep, sedation, reduction of awareness dizzy when energetic, sleeping chicken blurred vision dilated pupils, eye pain, vision Circuit
sinus sinus stops, sinus pace, tachycardia Respiratory, chest, thymus disorders nasal septum, yawning

Abdominal, epigastric pain, digestive disorders, flatulence, uncomfortable stomach, abdominal distention, dry mouth discomfort abdominal area, uncomfortable epigastric region Definition many times Genital disorders Tired, uncomfortable weakness, hot feeling, restlessness, abnormal feeling, drunkenness
Notify the physician with unwanted effects when using the drug.

Warnings

Before using the drug you need to read the instructions carefully and refer to the information below.

contraindicated

Durapil drugs contraindicated in the following cases:

Hypersensitivity to dapoxetin or any ingredients of the drug. Dapoxetin period with Monoamid oxydase inhibitors, or within 14 days of stopping IMAO. Similarly, Imao is not used within 7 days after stopping dapoxetin treatment. Similarly, Thioridazin is not used within 7 days after stopping dapoxetin treatment. Similarly, do not use these drugs within 7 days after stopping using dapoxetin.

Caution when using

General warning:

Only use dapoxetin for patients with premature ejaculation.

The safety of the drug has not been proven and there is no data on the effectiveness of the drug for late ejaculation cases.

faint:

Money symptoms such as nausea, dizziness, mild headache, sweating are common symptoms that are reported among patients using dapoxetin compared to the placebo group. Cases of fainting are characterized by the loss of consciousness recorded in clinical studies that manifest blood vessels and most occur in the first 3 hours when using the drug, after the first dose or related to clinical tricks. Million symptoms such as nausea, dizziness, chest drum, headache, fatigue, confusion and sweat often occur in the first 3 hours after taking the drug and often leads to fainting.

Fainting may occur whenever there is or no symptoms in advance during dapoxetin treatment. Doctors need to explain to patients about the importance of maintaining water balance and how to perceive millions signs to reduce the risk of falling injuries due to loss of consciousness.

Hypotenary pressure:

Hypotension has been reported in clinical trials. Dapoxetin caution should be used with patients using vasodilators (Anpha adrenergic, nitrate, pdes inhibitors).

Excessive (crazy): Do not use dapoxetin for patients with a history of emotional disorders such as excitement, depression or bipolar disorder or should stop the drug immediately if these symptoms.

epilepsy:

Stop using dapoxetin when symptoms of convulsions appear and do not indicate dapoxetin for patients with a history of unstable epilepsy.

Children and teenagers under 18 years old:

Do not use dapoxetin for children and teenagers under 18 years old.

Depression has mental disorders:

Not used simultaneously dapoxetin with antidepressants.

Bleeding:

Be careful when using dapoxetin when used simultaneously with drugs that affect the function of platelets or anticoagulic drugs, as well as for patients with a history of bleeding or coagulation disorders.

Renal failure:

Do not use dapoxetin for patients with severe renal function. Caution should be used for patients with medium and mild renal function.

suicide tendency:

Antidepressants, including SSRIs, increases risk (compared to placebo) on the formation of suicide and suicide in short -term studies in children and young people with depression and other mental disorders.

In the group of people greater than 24 years old, it does not show an increase in the risk of suicide when taking antidepressants compared to placebo. In clinical trials with dapoxetin to treat premature ejaculation, there is no clear sign of emergency care cases according to the assessment of side effects that may be related to suicidal, in the classification of suicide cases such as Columbia Class Beck Depression Inventory-II.

Patients with cardiovascular risk factors:

Subjects with cardiovascular disease have been recommended not to be used. The risk of cardiovascular bad complications from fainting (fainting due to heart and fainting due to other causes) is increased in patients with cardiovascular disease (for example, obstruction flow, heart valve, carotid stenosis and coronary artery disease). Not enough data to determine if there is an increase in prolonged risk, resulting in fainting due to the vague neurological reaction in patients with hidden cardiovascular disease

Sharing other stimulants:

Do not use dapoxetin in combination with other addictive drugs.

addictive drugs with serotonin activity such as ketamine, methylenedioxy methamphetamine (MDMA) and diethylamide Lysergic acid (LSD) can lead to serious reactions if combined with dapoxetin. These reactions include: arrhythmia, hyperthermia, and serotonin syndrome. Using dapoxetin with drug drugs with sedative properties such as addictive painkillers and benzodiazepin may increase drowsiness and dizziness.

alcohol:

Patients should be advised not to use dapoxetin with alcohol.

A combination of alcohol with dapoxetin can increase the nerve cognitive effects related to alcohol and can also enhance cardiovascular -nervous side effects, thus increasing the risk of an accident. Therefore, patients should be advised to avoid drinking while using dapoxetin.

Sharing CYP3A44 inhibitors Average:

Must be cautious and not exceed the dose of 30mg.

Sharing strong CYP2D6 inhibitors:

Be careful when increasing the dose to 60 mg in patients with strong CYP2D6 inhibitors or in patients known as a weak metabolic CYP2D6 genotype, as this may increase the concentration of blood drugs leading to increased risk and severity of the dose side effects.

Blood disorders:

There have been reports on abnormal bleeding when taking SSRIs. Caution should be careful in patients using dapoxetin, especially in simultaneous use with drugs that affect platelet function (for example, not typical anti -psychotic drugs and phenothiazine, acetylsalicylic acid, nonsteroidal anti -inflammatory drugs [NSAID), anti -platelet drugs) or anticoagulic drugs (eg, warfarin), as well as patients with bleeding or blood coagulation.

kidney failure:

dapoxetin is not recommended for patients with severe renal impairment and need to be cautious in patients with mild or medium renal failure.

Eye disorders:

The use of dapoxetin has been reported to be associated with eye symptoms such as pupils and eyeballs. Dapoxetin should be used carefully in patients with increased intraocular pressure or those at risk of closing angle glaucoma (closed angle glaucom).

Lactose intolerance:

Patients with rare genetic problems of galactose intolerance, lactase deficiency, or malposure of glucose-galactose should not use this drug.

Reaction when stopping treatment suddenly:

Causes insomnia and dizziness.

The effect of the drug on the ability to drive and operate machinery

because the drug causes dizziness and drowsiness should not be used for drivers and machinery.

Using drugs for women during pregnancy and lactation

Using drugs for pregnant women:

Do not use this drug for pregnant women.

Use drugs for breastfeeding women:

Do not use this medication for breastfeeding women.

Drug interaction

alcohol:

Concomitant use of dapoxetin with alcohol can increase the effects of alcohol related to cognitive ability and can also increase foreign effects. Patients should not drink alcohol when using dapoxetin.

Simultaneous use of sympathetic effects:

Do not simultaneously use dapoxetin with excitement drugs or excitement drugs that have sympathetic effects such as ketamine, methylenedioxymethampininin (MDMA) and lysergic acid diethylamid (LSD) can cause serious adverse reactions when used simultaneously dapoxetin (fast -paced, hyperthermage, sympathetic syndrome). Simultaneous use of dapoxetin with excited drugs that have a sedative effect like addictive drugs and benzodiazepine groups can cause chicken sleep and dizziness.

With medication CYP3A4 at an average level:

Need to be cautious and do not take the dose exceeding 30 mg when used simultaneously with CYP3A4 inhibitors at an average level such as erythromycin, fluconazole, amprenavir, fosamprenavir, aprepitant, verapamil and diltiazem.

With strong CYP2D6 inhibitors:

Be careful when increasing the dose to 60 mg when used simultaneously with strong inhibitors CYP2D6 or when increasing the dose up to 60 mg in difficult rings to metabolize CYP2D6 because this can increase the severity of the adverse reactions of the drug.

The drugs have an impact on the central nervous system:

Should be cautious when using Durapil 30 with drugs that work on the central nervous system.

Enzyme inhibitors:

can reduce the clearance of dapoxetin.

PDE5 inhibitors:

Be cautious when prescribing dapoxetin for patients with PDE5 drugs because it can lower vertical blood pressure.

wafarin:

Should be cautious when using dapoxetin for patients with long -term wafarin.

Interaction with thioridazin:

thioridazine-has the effect of extending the QTC range, closely related to serious ventricular arrhythmia. Dapoxetin inhibits isoenzyme CYP2D6, thus inhibiting the metabolism of thioridazine and as a result, Thioridazine concentration will increase, increasing the risk of QTC. Dapoxetin should not be used in combination with

thioridazine or within 14 days from the date of discontinuation of treatment with thioridazine. Similarly, Thioridazine should not be indicated within 7 days after dapoxetin.

Effect of dapoxetin when sharing tamsulosin:

Single or multi -therapy with dapoxetin 30 mg or 60 mg for patients being treated long -term with Tamsulosin does not change the pharmacokinetics of Tamsulosin. Simultaneous use of dapoxetin and tamsulosin does not increase the risk of lowering vertical voltage and there is no difference in the risk of the appearance of vertical voltage when using tamsulosin in combination with all 30 or 60 mg dapoxetin compared to Tamsulosin alone; However, dapoxetin should be carefully indicated in patients using alpha adrenergic receptor drugs due to the ability to increase the appearance of vertical pressure.

Storage

Leave a cool place, avoid light, temperatures below 30⁰C.

To be out of reach of children, read the instructions carefully before use.

Other drugs

Disclaimer

Every effort has been made to ensure that the information provided by Drugslib.com is accurate, up-to-date, and complete, but no guarantee is made to that effect. Drug information contained herein may be time sensitive. Drugslib.com information has been compiled for use by healthcare practitioners and consumers in the United States and therefore Drugslib.com does not warrant that uses outside of the United States are appropriate, unless specifically indicated otherwise. Drugslib.com's drug information does not endorse drugs, diagnose patients or recommend therapy. Drugslib.com's drug information is an informational resource designed to assist licensed healthcare practitioners in caring for their patients and/or to serve consumers viewing this service as a supplement to, and not a substitute for, the expertise, skill, knowledge and judgment of healthcare practitioners.

The absence of a warning for a given drug or drug combination in no way should be construed to indicate that the drug or drug combination is safe, effective or appropriate for any given patient. Drugslib.com does not assume any responsibility for any aspect of healthcare administered with the aid of information Drugslib.com provides. The information contained herein is not intended to cover all possible uses, directions, precautions, warnings, drug interactions, allergic reactions, or adverse effects. If you have questions about the drugs you are taking, check with your doctor, nurse or pharmacist.