Tramadol for Premature Ejaculation

Premature ejaculation is a condition in which a man ejaculates sooner than normal ejaculation time, or too fast for couples sexual relationship, with the IELT (intravaginal ejaculation latency time) = 2 min at 80% sexual relationship. Premature ejaculation is the most common sexual dysfunction, affecting approximately 23% of men aged 18-75 years.

Tramadol, an opioid class of drugs known efficacious as an analgesic, is shown to have relatively good safety profile during the 30 years of its use in humans. In addition, as an analgesic, tramadol mechanism of action was also useful to delay ejaculation. Tramadol is known to work as an agonist at µ-opioid receptor, serotonin release, and inhibit re-uptake (reuptake) of norepinephrine. Efficacy as a cure premature ejaculation appears to be associated with the last two mechanisms.

Phase II clinical trial showed that tramadol is an effective drug, with minimal side effects, for men with premature ejaculation. Men who ate tramadol had significantly longer IELT, improved ejaculation control, increased sexual satisfaction, as well as domestic relations problems are much less compared to placebo. Comparison of clinical data by a pharmaceutical company suggests that tramadol has a better efficacy than dapoxetine, an SSRI class of antidepressants (selective serotonin reuptake inhibitors) which is the first oral drug approved for the indication of premature ejaculation. In addition, the SSRI class of drugs considered to have more serious side effects. However, dapoxetine should be used only if needed when going on a sexual relationship, and need not be consumed regularly.

Another study conducted by EA Salem et al. in 2008 showed that 25 mg tramadol is useful for cases of premature ejaculation. Tramadol HCl 25 mg administered in the first group (n = 30) before sexual intercourse, while the second group was given placebo (n = 30). Therapy administered for 8 weeks. Drugs taken 1-2 hours before sexual activity, and patients were asked to have sex at least once a week. The average initial value of IELT before treatment was 1.17 + / - 0.39 minutes. At the time the patients received tramadol, an average IELT increased significantly to 7.37 + / - 2.53 minutes. When given a placebo, the mean IELT of only 2.01 + / - 0.71 minutes. All patients also reported that they were satisfied with their ejaculatory control.

Conclusion, tramadol HCl at a dose of 25-50 mg can be used as a cure for premature ejaculation.

Tramadol VS Meperidine

• Shivering is one of the post-anesthetic complications.
• How to prevent chills are not always effective.
• Meperidine is the analgesic drug that can be used to prevent post-anesthetic shivering, but these drugs have a constraint between others are not always effective, causing nausea and vomiting, sedation, euphoria and the incidence of pruritus and respiratory depression which is quite high.
• Tramadol is an analgesic drug that can be used to prevent post-anesthesia shivering, cause less respiratory depression and sedation compared with meperidine.
• From the statement above, can be prepared a formulation of the problem is provision of tramadol 2 mg / kg intravenously before the end of the operation is more effective than meperidine 0.5 mg / kg intravenously before the end of the operation to prevent incidence of post-anesthetic shivering.

What Is Tramadol ???

Tramadol hydrochloride (tramadol) is an opioid analgesic drug which The central work. Tramadol inhibits re-uptake (re-uptake) norepinephrine and 5-hydroxytryptamine threshold of nerve fibers, facilitating the release f 5-hydroxytryptamine and activates µ-opioid receptors, and little influenced or ? receptors. 

All these mechanisms would affect the central regulation temperature. Therefore, these drugs can be used to prevent post-anesthetic shivering.The advantage gained by using tramadol in addition to the influence of hemodynamic bermaknan not they cause respiratory depression and less sedation compared with meperidine. So it can be said to use more secure, especially in patients with cardiorespiratory conditions who not good. Besides, the incidence of nausea and vomiting are relatively smaller than meperidine.

Bhatnagar et al. using a dose of 1 mg / kg intravenously to treat the incidence of post-anesthetic shivering and get the 80% patients stopped shivering in a span of 10 minutes after the drug is administered. S. Mathews et al. who conducted the study using a dose of tramadol mg / kg and 2 mg / kg given at the start of wound closure in patients who underwent general anesthesia conclude that tramadol effectively and secure to prevent the occurrence of post-anesthetic shivering. The same is shown by the results of the study De Witte et al., but with a dose of 3 mg / kg.

Tsai YC et al. conduct research using tramadol dose of 0.5 mg / kg body weight intravenously to prevent shivering after epidural anesthesia. The results obtained tramadol apparently have the same effectiveness with meperidine dose of 0.5 mg / kg iv in preventing shivering after epidural anesthesia. While AMH Chan et al. conclude tramadol dose of 0.25 mg / kg intravenously effective overcome shivering in cesarean patients who performed regional anesthesia Cesarea with minimal side effects.

Tramadol HCl made

Tramadol HCl is a synthetic opioid and is included in group aminosikloheksan is efficacious as an analgesic or antinyeri. tramadol HCl characteristics that support for slow-release preparations made ??15 among other things that do not use too large a dose of 100 mg, absorbed well in the stomach, the half-life of 5.5 hours and have good stability in water and ethanol (Anonymous, 2004).

One reason for tramadol HCl made ??in the slow-release preparations are association as an analgesic medication for chronic diseases. patients with Chronic diseases tend to use drugs on a regular basis with frequency of more than 2 times a day and in the long term. In order to enhance patient comfort, the tramadol HCl made ??in slow-release preparations.

One method is the simplest and often used in manufacture of slow-release preparation is a matrix system, where the active substance is mixed homogeneously in the matrix (solid carrier). Metolose 90SH ®(cellulose derivative) which is hydrophilic. matrix form a hydrophilic gel is widely used to inhibit the release extended drug because it is like water (hydrophilic), although stable is hygroscopic after drying, is stable in old water, and reduce the risk of dose dumping (Huang, et al., 2004; Harwood, 2005).

The results Kurniawati (2005) proved that the increase concentration of methocel K4M Premium EP matrix used influence of granular flow properties. The more the number of methocel K4M Premium EP to used lower speeds. Use of methocel K4M Premium EP with levels of 30% has the ability to inhibit The best drug release.

Formulation Tablet Tramadol HCl Off Late The Matrix 90SH® Metolose

Tramadol HCl is one type of analgesic drugs, which are used to cope with severe pain either acute or chronic pain after surgery.Tramadol HCl has some characteristics such as the use of doses which is not too large, namely 100 mg, 5.5 hour half-life, absorbed with either in the stomach, has a price of 9.14 pKa, log P of 1.35 at pH 7 and  have good stability in water and ethanol (Anonymous, 2004).

One reason for tramadol HCl made ??in the slow-release preparations are association as an analgesic medication for chronic diseases. patients with Chronic diseases tend to use drugs on a regular basis with frequency of more than 2 times a day and in the long term. In order to enhance patient comfort, the tramadol HCl made ??in slow-release preparations. One method used in the manufacture of slow-release preparations is a matrix system where the drug is mixed homogeneously with the matrix material. One advantage of the matrix system is its use of  elatively simple and inexpensive compared to other systems. 

The research was conducted with the addition of matrix to slow release of active substances. Matrix used in this study is metolose 90SH®. Metolose 90SH® a hydrophilic matrix which can form a hydrogel layer is thick all around on the slow-release preparations after contact with gastrointestinal fluids. Hydrogel layer is capable of blocking the release of active substance in the preparation so that the rate of drug release can be controlled (Kavanagh and Corrigan, 2004). The advantage of this matrix is a character who likes water (hydrophilic), although it is hygroscopic stable after drying, and is stable in cold water (Harwood, 2005; Huang, et al., 2004).

TRAMADOL

Indications:

TRAMADOL is indicated for treating and preventing moderate to severe pain, such as those below:

• Acute and chronic pain is severe.
• Pain after surgery.

Contra Indications:

• Acute poisoning by alcohol, hypnotics, analgesics or medications that affect other CNS.
• Patients receiving monoamine oxidase inhibitor treatment (MAO).
• Patients who are hypersensitive to tramadol.

Composition:

• Each capsule contains:
• Tramadol Hydrochloride 50 mg .....................................

How Drugs Work:

• TRAMADOL is a powerful analgesic that works on opiate receptors.
• Stereospsifik tramadol binds to receptors in the central nervous system to stop the sensation of pain and response to pain. In addition tramadol inhibits the release of neutrotransmiter of afferent nerves that are sensitive to stimuli, resulting in stunted pain impulses.

Side Effects:

• Same as generally centrally acting analgesics, side effects may occur: nausea, vomiting, dyspepsia, obstipasi, fatigue, sedation, dizziness, pruritus, sweating, flushed skin, dry mouth and headache.
• Although tramadol interact with receptors apiat until now proven incidence after the use of tramadol addiction, lightweight.

Attention:

• Be careful when used in patients with head trauma, increased intracranial pressure, impaired kidney and liver function are severe or bronchial hypersecretion; because it can increase the risk of seizures or shock.
• Can a decline in lung function when the use of tramadol in combination with drugs or other CNS depression when exceeding the recommended dosage.
• Tramadol should not be used in patients with drug dependence. Although including opiate agonist, tramadol can not suppress withdrawal symptoms, due to administration of morphine.
• Tramadol should not be given to pregnant women unless absolutely necessary.
• 0.1% of tramadol is excreted through breast milk (breast milk).
• TRAMADOL sufferers can reduce the rate of reaction, such as the ability to drive or operate machinery.
• Duration of treatment
• In the long-term treatment, the possibility of dependence, therefore the doctor must set the length of treatment. Should not be given for longer than is necessary.

Drug Interactions:

• Use of tramadol together with medicines that work on the CNS (such as tranquillizer, hypnotic), can enhance the effect sedasinya.
• Use of tramadol with tranquillizer can also increase the analgesic effect.

Dose:

• As with analgesic drugs, the dose should be adjusted according to the severity of pain and clinical response of patients.
• Dose for adults and children over the age of 14 years:
• A single dose: 1 capsule.
• Daily dose: up to 8 capsules.
• If the pain is still felt, you can add a second single dose of 1 capsule tramadol more, After an interval of 30-60 minutes.
• In patients with impaired renal and hepatic function, dosage adjustments should be done.

Packaging:

• Thus the content of 5 strips @ 10 capsules.

Storage:

• Store in a cool, dry, protected from light.