|Place of Origin:||CHINA|
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|Product Name:||Phentolamine Mesilate||Purity:||99%|
|Appearance:||White To Off-white Powder|
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Product Name: Phentolamine mesilate
Synonym: REGITIN;REGITIN MESYLATE;PHENTOLAMINE MESILATE;PHENTOLAMINE MESYLATE;PHENTOLAMINE METHANESULFONATE;PHENTOLAMINE METHANESULFONATE SALT;VASOMAX;m-(n-(2-imidazolin-2-ylmethyl)-p-toluidino)-phenomonomethanesulfonate(sal
Related categories: Raw material medicine; medicine treatment of vasospasm disease; cell biology; biologically active small molecule; plant extract; chemical intermediate; pharmaceutical raw material; small molecule inhibitor; sulfur compound; male drug; cell signal and neurobiology; PHARMACEUTICAL INGREDIENTS;Erectile Dysfunction;Diagnostic;API;Pharmaceutical raw material;Regitine;pharmaceutical;Intermediates & Fine Chemicals;Pharmaceuticals;Adrenoceptor
Melting Point: 180-182 °C(lit.)
Density: 1.2256 (rough estimate)
Refractive index: 1.6320 (estimate)
Solubility: ethanol: 26 mg/mL
Water solubility: 50 mg/mL
Stability: Aq. Solutions Cannot be Stored
Appearance: white to off-white powder
Erectile dysfunction (ED) is a common and important sexual dysfunction, which is a urological disease. Epidemiological data suggest that male ED is more common and has a close relationship with age and dyslipidemia, hypertension, coronary artery disease and diabetes. About 152 million men worldwide suffer from ED. With the aging of human society, it is predicted that 322 million men worldwide will suffer from this sexual dysfunction by 2025. Phentolamine is a non-selective adrenergic receptor blocker that reduces peripheral vascular resistance and increases peripheral blood flow. In the treatment of male erectile dysfunction, the drug acts on the a receptors on the erectile tissue, relaxes the arterioles and capillaries, increases the blood supply to the corpus cavernosum, and promotes and enhances erectile function. Vasomax (Phenolamine Mesylate), developed by Schering AG, has been marketed in some South American countries for the treatment of male erectile dysfunction. In addition to oral administration, phentolamine is currently the usual mode of administration of injections. Due to the pain and inconvenience of administration by injection, the compliance of the patient's medication is extremely poor, and side effects such as cavernous fibrosis at the injection site may occur, which is not suitable for repeated medications. After years of clinical verification, phentolamine mesylate is mainly used for sexual dysfunction, especially for the treatment of erectile dysfunction, the effect is remarkable. Capsules and tablets as oral preparations are more popular among consumers because of their convenience in taking and carrying. At the same time, phentolamine mesylate is a commonly used α-adrenergic blocker in clinical practice, which can antagonize the effects of adrenaline and norepinephrine in the blood circulation, so that blood vessels dilate and reduce peripheral vascular resistance. Diagnosis of pheochromocytoma and treatment of hypertensive seizures, left ventricular failure and prevention of skin necrosis. Phentolamine mesylate (PM) is an adrenergic receptor blocker which acts on both α1 and α2 receptors, and preparations such as tablets, capsules and injections have been developed. The phentolamine mesylate tablet is a potential competitive blocker of α-receptors, which blocks the α1 receptor of vascular smooth muscle and possibly the α 2 receptor, resulting in decreased peripheral resistance and vasodilation. The corpus cavernosum smooth muscle relaxes, allowing more blood to flow into the cavernous tissue, while inhibiting blood flow out of the cavernous body, leading to erection. Phentolamine has low oral bioavailability and its oral preparations are clinically used for the treatment of erectile dysfunction. Phentolamine mesylate is a commonly used α-adrenergic blocker in clinical practice. It can antagonize the effects of adrenaline and norepinephrine in the blood circulation, dilate blood vessels and reduce peripheral vascular resistance. Chromoblastoma and treatment of hypertensive seizures, left ventricular failure and prevention of skin necrosis. This medicine is a variety contained in the 2005 edition of the Chinese Pharmacopoeia.
Mainly used for cardiovascular diseases, as well as diabetes, kidney disease, toxic intestinal paralysis, acute respiratory distress syndrome, bronchiolitis, severe asthma.
1. Phentolamine mesylate is a short-acting, non-selective a-receptor (a1, a2) blocker that antagonizes the action of adrenaline and norepinephrine in the blood circulation, expanding blood vessels and reducing peripheral vascular resistance . 2. Antagonizes the catecholamine effect for the diagnosis and treatment of pheochromocytoma, but has little effect on the blood pressure of normal or essential hypertension patients. 3. It can reduce peripheral vascular resistance, reduce post-cardiac load, decrease left ventricular end-diastolic pressure and pulmonary artery pressure, increase cardiac output, and can be used to treat heart failure. Carcinogenic, mutagenic and reproductive toxicity. 4. Long-term experiments have shown that phentolamine mesylate has no obvious carcinogenic, mutagenic and reproductive toxicity. In tests on rats, mice and rabbits, phentolamine mesylate was not found to be teratogenic or embryonic.
Tablets and Capsules:
1. This product is combined with guanethidine, and the incidence of orthostatic hypotension or bradycardia is increased.
2. Sedative and hypnotic drugs such as phenobarbital and glutidine, antihypertensive drugs such as reserpine and antihypertensive drugs can enhance the antihypertensive effect of the drug.
3. When combined with cardiac glycoside, it can enhance its toxicity.
4. Avoid use with iron.
5. Forbidden use with nitroglycerin drugs.
1. Use with sympathomimetic drugs to offset or attenuate the peripheral vasoconstriction of the latter.
2. With the use of guanethidine, the incidence of orthostatic hypotension or bradycardia increased.
3. Used together with diazoxide, the effect of diazoxide inhibiting insulin release is inhibited.
4. Phenobarbital, sleep-inducing energy, etc. strengthen the antihypertensive effect of this product.
5. Avoid compatibility with iron.
Tablets and Capsules:
For the treatment of erectile dysfunction.
This product is a short-acting α-blocker with no selectivity to α1 and α2 receptors; it can antagonize the catecholamine effect in blood, directly relax small arteries and capillaries, reduce peripheral resistance and cardiac load, and increase heart beat. the amount. For peripheral vasospasm diseases: such as acral arterial spasm (Renault disease), hand and foot cyanosis and thromboangiitis obliterans.
Capsule: 40mg*2 capsules
Injection: 1ml: 5mg, 1ml: 10mg
Tablets: Oral, 40mg each time (1 tablet), take 30 minutes before sex, take up to one time per day, according to need and tolerance, the dose can be adjusted to 60mg (1 tablet and a half), the maximum recommended dose is 80mg (2 tablets).
Capsules: Take one capsule at a time before oral activity and do not take more than one dose a day.
(1) phentolamine test: intravenous injection of 5mg, can also be injected 2.5mg first, if the reaction is negative, give 5mg, so the false positive results can be reduced, but also reduce the risk of blood pressure drop Sex.
(2) Prevention of skin necrosis: Inject 10 mg of this product into the norepinephrine solution per 1000 ml for prevention. Norepinephrine spillover has occurred, and 5-10 mg of this product plus 10 ml of sodium chloride injection is used for local infiltration. This method is effective within 12 hours after the overflow.
(3) pheochromocytoma surgery: intravenous injection of 5mg 1-2 hours before surgery, intravenous injection of 5mg or 0.5-1mg per minute to prevent a large amount of adrenaline release during tumor surgery.
(4) Reduce heart load during heart failure: intravenous infusion of 0.17-0.4 mg per minute.
The usual dose for children:
(1) phentolamine test: intravenous injection of 1mg, can also be 0.1mg / kg by weight or 3mg / m2 body surface area, or intramuscular injection of 3mg.
(2) pheochromocytoma surgery: intramuscular or intravenous injection of 1mg 1-2 hours before surgery, can also be based on body weight 0.1mg / kg or body surface area of 3mg / m2, if necessary, can be repeated; intravenous injection of 1mg, also It can be 0.1mg/kg by weight or 3mg/m2 by body surface area.
There are mainly orthostatic hypotension, tachycardia or arrhythmia, skin flushing, nasal congestion, nausea, vomiting, abdominal pain, angina pectoris, etc.; occasionally fainting, chest pain, ataxia, etc. These reactions may be manifestations of cerebral vasospasm or blockage . The pharmacological effects, pharmacokinetics, synthetic routes, indications, and precautions for phentolamine mesylate were compiled by Xu Yan, editor of Chemicalbook. (2016-03-25)
1. It has been reported that the use of this product can cause myocardial infarction, cerebral vasospasm and cerebrovascular disease, especially in low blood pressure.
2. When performing the phentolamine test, blood pressure is measured every minute for every 30 seconds and 7 minutes after the administration, or within 3 minutes after the intravenous administration, or within 30-45 minutes after the intramuscular injection. Blood pressure is measured every 5 minutes. During the test, it should be placed in a quiet and slightly dark room. The intravenous injection speed should be fast. Once the effect of venipuncture on blood pressure has passed, it will be injected. Patients with paroxysmal hypertension or pheochromocytoma that does not secrete too much catecholamine may have false negatives; uremia or antihypertensive drugs, barbiturates, opioid analgesics, sedatives may be used. The phentolamine test is false positive, so it should be stopped 24 hours before the test; those who use antihypertensive drugs must wait until the blood pressure rises back to the pre-treatment level before administration. When hypotension occurs during the overdue period, norepinephrine can be intravenously instilled, but epinephrine should not be used to prevent further lowering of blood pressure.
3. Patients with angina pectoris, myocardial infarction, and coronary artery insufficiency should be used with caution.
1. Low blood pressure, severe arteriosclerosis, angina pectoris, myocardial infarction, renal dysfunction, gastritis, stomach and duodenal ulcers are prohibited;
2. Treatment of toxic shock and severe pneumonia should supplement blood volume at the same time;
3. In the diagnosis of cell tumors, phenobarbital, glutamine, methaqualone, and reserpine can produce false positives;
4. Excessive adrenaline can be used;
5. Avoid compatibility with iron;
6. Dopamine or dobutamine can increase the heart rate significantly; combined with adenosine triphosphate, can antagonize the role of adenosine, so this product should not be combined with adenosine or adenosine to expand coronary artery drugs;
7. When used in combination with cardiac glycosides, the toxicity can be enhanced.
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