دوشنبه 29 مهر 1398  08:07 ب.ظ

Alupent (Orciprenaline Sulfate)

Orciprenaline powder is a bronchodilating agent. The bronchospasm associated with various pulmonary diseases – chronic bronchitis, pulmonary emphysema, bronchial asthma, silicosis, tuberculosis, sarcoidosis and carcinoma of the lung, has been successfully reversed by therapy with orciprenaline.

Orciprenaline has the following major characteristics: The action of orciprenaline is one of beta stimulation. Receptor sites in the bronchi and bronchioles are more sensitive to the drug than those in the heart and blood vessels, so that the ratio of bronchodilating to cardiovascular effects is favorable. Consequently, it is usually possible clinically to produce good bronchodilation at dosage levels which are unlikely to cause cardiovascular side effects.

The efficacy of the bronchodilator after both oral and inhalation administration has been demonstrated by pulmonary function studies (spirometry, and by measurements of airways resistance by body plethysmography).Rapid onset of action follows administration of orciprenaline inhalants, and the effect is usually noted immediately. Following oral administration, the effect is usually noted within 30 minutes.The peak effect of bronchodilator activity following orciprenaline generally occurs within 60 to 90 minutes, and this activity lasts for 3 to 6 hours.Orciprenaline taken orally potentiates the action of a bronchodilator inhalant administered 90 minutes later, whereas no additive effect occurs when the drugs are given in reverse order.

Patients have not developed tolerance to the drug during prolonged therapy.No toxic effects on the liver, kidneys or hematologic system have been reported in the long-term use of orciprenaline in man.Indications And Clinical Uses: Orciprenaline has been found useful in the following conditions: bronchial asthma, chronic bronchitis, pulmonary emphysema.Orciprenaline is also useful in sarcoidosis, silicosis, carcinoma of the lung and tuberculosis when bronchospasm contributes to the disability.

Patients with chronic airways obstructive disease require long-term therapy with bronchodilators as an essential part of overall management aimed at lowering airways resistance and facilitating bronchial drainage. Orciprenaline has been shown to fulfill the basic requirements of such continued therapy in that it is effective both orally and as an inhalant, has a rapid and prolonged action, and has a low incidence of side effects.

Inhalation Aerosol: The efficacy of orciprenaline administered as an aerosol has been demonstrated by increased flow rates (FEV1, MMFR, MEFR, MBC) decreased airways resistance (body plethysmography), and decreased functional residual capacity (body plethysmography).

In one study the effect of 4.5 mg of orciprenaline has been compared with the effect of 0.45 mg of isoproterenol each drug being given as an aerosol over a period of 8 minutes. Although the improvement in pulmonary function was consistently better with orciprenaline, 1 hour, 3 hours, and 6 hours following inhalation, changes in pulse rate and blood pressure were less pronounced with orciprenaline. This indicated a more favorable ratio of bronchodilating to cardiovascular effects for orciprenaline.

In another study, orciprenaline 2% solution, racemic epinephrine 2.25% and isoproterenol 1% were each administered as aerosols on separate days. The aerosols were administered by hand nebulizer for 30 minutes or until cardiovascular side effects appeared.

The immediate effect of orciprenaline on airways resistance in this study was similar to that produced by isoproterenol and by racemic epinephrine. However, the reduction in airways resistance after orciprenaline was significantly greater than that seen with isoproterenol in 30 minutes after inhalation, and after 90 minutes the effect of orciprenaline was superior to both isoproterenol and racemic epinephrine.

Whereas isoproterenol aerosol and epinephrine aerosol produced only transient reductions in the functional residual capacity of less than 30 minutes duration, the effect of orciprenaline on this parameter remained significant up to 90 minutes after inhalation.

Syrup: The efficacy of orciprenaline has been demonstrated by improvement of flow rates (FEV1, MMFR, MEFR) and airways resistance measurements (body plethysmography). Repeated measurements of pulmonary function made over a 4-hour period show that orciprenaline 20 mg orally gives a generally better result regarding duration of action and magnitude of response than placebo, 100 mg methoxyphenamine, 30 mg ephedrine by mouth, or 10 mg isoproterenol sublingually.

The effect of an inhalant bronchodilator may be potentiated by oral administration of 20 mg of orciprenaline 90 minutes prior to use of the inhalant. No additive effect occurs when the drugs are given in reverse order. The probable reason for this is that a bronchodilator delivered to the lungs via the vascular system (i.v. or oral medication) acts upon bronchioles whether or not they are occluded. Such an effect causes a wider distribution in the lungs of a subsequently given drug, and consequently the bronchodilation is more intense. Knowledge of this interaction is of value when instructing patients in the combined use of oral and inhalant forms of orciprenaline.

Orciprenaline may be given orally in dosages ranging from 60 to 120 mg daily. An effective clinical response in adults and children above 12 years can be achieved by 20 mg orciprenaline 3 times daily, and at this dosage side effects are not significantly different from those following placebo. Orciprenaline at a dosage of 20 mg 4 times daily is well tolerated and side effects are usually mild. Only at dosages of 100 mg daily and above, do palpitations and tremulousness become troublesome. If high doses of orciprenaline are necessary, it may be possible to eliminate the side effects whilst continuing the same total daily dose, by administering 10 mg single doses at more frequent intervals.

General: The low incidence of side effects together with effective bronchodilation make orciprenaline acceptable to patients with chronic bronchial asthma for continuous use either alone or concurrently with corticosteroids. Some of these patients may be controlled with orciprenaline as the sole medication, and it may be possible to avoid the use of steroid therapy. In a proportion of individuals who are already taking corticosteroids, it may be possible to withdraw this medication and continue with orciprenaline alone. However, caution should be observed in this regard as many patients, particularly those with severe bronchial asthma, can be managed satisfactorily only if steroids and bronchodilators are given together.

Prolonged studies have shown that patients with bronchitis and emphysema respond to continuous therapy with orciprenaline. The frequency and severity of acute attacks decrease, and patients experience relief of wheezing, chest congestion and shortness of breath. A close association is apparent between objective measurements of pulmonary function and the subjective response.

Contra-Indications: Known sensitivity to the drug or other sympathomimetic amines. The use of orciprenaline and other beta stimulators is generally considered to be contraindicated in patients with cardiac arrhythmias associated with tachycardia.Beta blocking agents, (e.g. propranolol) effectively antagonize the action of orciprenaline. Their concomitant use, except in the treatment of accidental overdosage, is therefore contraindicated.


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دوشنبه 29 مهر 1398  08:01 ب.ظ

The global market size of Tulobuterol hydrochloride is $XX million in 2018 with XX CAGR from 2014 to 2018, and it is expected to reach $XX million by the end of 2024 with a CAGR of XX% from 2019 to 2024.

Global Tulobuterol Hydrochloride Market Report 2019 – Market Size, Share, Price, Trend and Forecast is a professional and in-depth study on the current state of the global Tulobuterol Hydrochloride industry. The key insights of the report:

1.The report provides key statistics on the market status of the Tulobuterol Hydrochloride manufacturers and is a valuable source of guidance and direction for companies and individuals interested in the industry.

2.The report provides a basic overview of the industry including its definition, applications and manufacturing technology.

3.The report presents the company profile, product specifications, capacity, production value, and 2013-2018 market shares for key vendors.

4.The total market is further divided by company, by country, and by application/type for the competitive landscape analysis.

5.The report estimates 2019-2024 market development trends of Tulobuterol Hydrochloride industry.

6.Analysis of upstream raw materials, downstream demand, and current market dynamics is also carried out

7.The report makes some important proposals for a new project of Tulobuterol Hydrochloride Industry before evaluating its feasibility.

There are 4 key segments covered in this report: competitor segment, product type segment, end use/application segment and geography segment.

For competitor segment, the report includes global key players of Tulobuterol Hydrochloride as well as some small players.


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دوشنبه 29 مهر 1398  07:55 ب.ظ

Raloxifene Hydrochloride Tablets

Raloxifene Hydrochloride Tablets, USP is indicated for the reduction in risk of invasive breast cancer in postmenopausal women at high risk of invasive breast cancer [see Clinical Studies (14.4)].

The effect in the reduction in the incidence of breast cancer was shown in a study of postmenopausal women at high risk for breast cancer with a 5-year planned duration with a median follow-up of 4.3 years [see Clinical Studies (14.4)]. Twenty-seven percent of the participants received drug for 5 years. The long-term effects and the recommended length of treatment are not known.

High risk of breast cancer is defined as at least one breast biopsy showing lobular carcinoma in situ (LCIS) or atypical hyperplasia, one or more first-degree relatives with breast cancer, or a 5-year predicted risk of breast cancer ≥1.66% (based on the modified Gail model). Among the factors included in the modified Gail model are the following: current age, number of first-degree relatives with breast cancer, number of breast biopsies, age at menarche, nulliparity or age of first live birth. Currently, no single clinical finding or test result can quantify risk of breast cancer with certainty.

After an assessment of the risk of developing breast cancer, the decision regarding therapy with Raloxifene Hydrochloride Tablets, USP should be based upon an individual assessment of the benefits and risks.

Raloxifene Hydrochloride Tablets, USP does not eliminate the risk of breast cancer. Patients should have breast exams and mammograms before starting Raloxifene Hydrochloride Tablets, USP and should continue regular breast exams and mammograms in keeping with good medical practice after beginning treatment with Raloxifene Hydrochloride Tablets, USP.
For either osteoporosis treatment or prevention, supplemental calcium and/or vitamin D should be added to the diet if daily intake is inadequate. Postmenopausal women require an average of 1500 mg/day of elemental calcium. Total daily intake of calcium above 1500 mg has not demonstrated additional bone benefits while daily intake above 2000 mg has been associated with increased risk of adverse effects, including hypercalcemia and kidney stones. The recommended intake of vitamin D is 400 to 800 IU daily. Patients at increased risk for vitamin D insufficiency (e.g., over the age of 70 years, nursing home bound, or chronically ill) may need additional vitamin D supplements. Patients with gastrointestinal malabsorption syndromes may require higher doses of vitamin D supplementation and measurement of 25-hydroxyvitamin D should be considered.

In clinical trials, raloxifene-treated women had an increased risk of venous thromboembolism (deep vein thrombosis and pulmonary embolism). Other venous thromboembolic events also could occur. A less serious event, superficial thrombophlebitis, also has been reported more frequently with raloxifene than with placebo. The greatest risk for deep vein thrombosis and pulmonary embolism occurs during the first 4 months of treatment, and the magnitude of risk appears to be similar to the reported risk associated with use of hormone therapy. Because immobilization increases the risk for venous thromboembolic events independent of therapy, raloxifene should be discontinued at least 72 hours prior to and during prolonged immobilization (e.g., post-surgical recovery, prolonged bed rest), and raloxifene therapy should be resumed only after the patient is fully ambulatory. In addition, women taking raloxifene should be advised to move about periodically during prolonged travel. The risk-benefit balance should be considered in women at risk of thromboembolic disease for other reasons, such as congestive heart failure, superficial thrombophlebitis, and active malignancy [see Contraindications (4.1) and Adverse Reactions (6.1)].


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Raloxifene hydrochloride is an estrogen agonist/antagonist, referred to as a selective estrogen receptor modulator (SERM) and belongs to the benzothiophene class of compounds. The biological actions of raloxifene Hcl are largely mediated through binding to estrogen receptors.β-agonist Powder

This binding results in activation of estrogenic pathways in some tissues (agonism) and and the blockade of estrogenic pathways in other tissues (antagonism). The agonistic or antagonistic activity of raloxiffene depends on the extent of recruitment of coactivators and corepressors to estrogen receptor (ER) target gene promotors.

Raloxifene Hcl appears to act as an estrogen agonist in bone. It decreases bone resorption and bone turnover, increases bone mineral density and decreases fracture incidence.

Raloxifene Hydrochloride Application:
1) Raloxifene Hcl used to prevent & treat osteoporosis in women who have undergone menopause.

2) Raloxifene Hcl used to decrease the risk of developing invasive breast cancer in women who are at high risk of developing this type of cancer or who have osteoporosis. Raloxifene Hcl cannot be used to treat invasive breast cancer or to prevent invasive breast cancer from coming back in women who have already had the condition.

3) Raloxifene Hcl prevents and treats osteoporosis by mimicking the effects of estrogen to increase the density (thickness) of bone.

4) Raloxifene Hcl decreases the risk of developing invasive breast cancer by blocking the effects of estrogen on breast tissue, which may stop the development of tumors that need estrogen to grow.


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High Purity Anastrozole Acetate Arimidex with Safety Shipping

Anastrozole powder
Alias: Arimidex
CAS No: 120511-73-1
MF: C17H19N5
MW: 293.37
Purity: 99%min
Appearance: White crystalline powder.
If you have any questions,welcome to your consult

Usage: An aromatase inhibitor. Used as an antineoplastic raw materials.
Potent selective triazole aromatase inhibitors, can inhibit the cytochrome P-450 aromatase enzyme which depends blocking the biosynthesis of estrogen, and estrogen to stimulate breast cancer cell growth factors. Treatment of breast cancer, especially for those with hormone relapse after adjuvant therapy after menopause for women with advanced breast cancer.

Arimidex (anastrozoles) is the aromatase inhibitor of choice. Arimidex’s mechanism of action – blocking conversion of aromatizable steroids to estrogen – is in contrast to the mechanism of action of anti-estrogens such as clomiphene (Clomid) (Nolvadex), which block estrogen receptors in some tissues, and activate estrogen receptors in others.

Applications:
High Purity Anastrozoles/Arimidex/CAS No: 120511-73-1
The drug is appropriately used when using substantial amounts of aromatizing steroids, or when one is prone to gynecomastia and using moderate amounts of such steroids. Arimidex does not have the side effects of aminoglutethimide (Cytadren) and can achieve a high degree of estrogen blockade, much moreso than Cytadren. It is possible to reduce estrogen too much with Arimidex, and for this reason blood tests, or less preferably salivary tests, should be taken after the first week of use to determine if the dosing is correct.


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دوشنبه 29 مهر 1398  07:36 ب.ظ

Hypergranulation is a frequent complication of dermatologic surgery, especially when surgical defects are left to heal by secondary intention (eg, after electrodesiccation and curettage). Although management of postoperative hypergranulation with routine wound care, superpotent topical corticosteroids, and/or topical silver nitrate often is effective, refractory cases pose a difficult challenge given the paucity of treatment options. Effective management of these cases is important because hypergranulation can delay wound healing, cause patient discomfort, and lead to poor wound cosmesis.Timolol powder
If refractory hypergranulation fails to respond to treatment with routine wound care and topical silver nitrate, we prescribe twice-daily application of timolol maleate ophthalmic gel forming solution 0.5% for up to 14 days or until complete resolution of the hypergranulation is achieved. We counsel patients to continue routine wound care with daily dressing changes in conjunction with topical timolol application.
We initiated treatment with topical timolol in a patient who developed hypergranulation at 2 separate electrodesiccation and curettage sites that was refractory to 6 weeks of routine wound care with white petrolatum under nonadherent sterile gauze dressings and 2 subsequent topical silver nitrate applications (Figure 1). After 2 weeks of treatment with topical timolol, resolution of the hypergranulation and re-epithelialization of the surgical sites was observed (Figure 2). Another patient presented with hypergranulation that developed following a traumatic injury on the left upper arm and had been treated unsuccessfully for several months at a wound care clinic with daily nonadherent sterile gauze dressings and both topical and oral antibiotics (Figure 3A). After treatment for 9 days with topical timolol, resolution of the hypergranulation and re-epithelialization of the surgical sites was observed (Figure 3B).
Beta-blockers are increasingly being used for management of chronic nonhealing wounds since the 1990s when oral administration of propranolol initially was reported to be an effective adjuvant therapy for managing severe burns.1 Since then, topical beta-blockers have been reported to be effective for management of ulcerated hemangiomas, venous stasis ulcers, chronic diabetic ulcers, and chronic nonhealing surgical wounds; however, there are no known reports of using topical beta-blockers for management of hypergranulation.2-5 We found timolol ophthalmic gel to be an excellent second-line therapy for management of postoperative hypergranulation if prior treatment with routine wound care and superpotent topical corticosteroids has failed. To date, we have found no reported adverse effects from the use of topical timolol for this indication that have required discontinuation of the medication. Use of this simple and safe intervention can be effective as a solution to a common postoperative condition.


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Sensitive and fast analysis of terbutaline sulfate in food

Terbutaline sulfate (TBS) is a β2-adrenoceptor agonist, overdoses of which can cause serious harm and even be life-threatening to humans. Herein, we demonstrate a simple and facile method for the preparation of a molybdenum disulfide–gold nanoparticle composite (MoS2/AuNPs). The obtained MoS2 and MoS2/AuNPs were characterized and investigated by X-ray powder diffraction, scanning electron microscopy, and transmission electron microscopy.
An MoS2/AuNPs-modified glassy carbon electrode (MoS2/AuNPs/GCE) was constructed using the dropping method and used to study the electrochemical behavior of TBS. The results indicated that the sensor had excellent electrocatalytic activity for TBS, with detection sensitivity for TBS more than 100 times higher compared with the bare GCE. With the successive addition of TBS, the peak current of the differential pulse stripping voltammogram (DPSV) of TBS was proportional to its concentration within a certain range, with a linear range of 1–85 nmol L−1 and limit of detection (LOD) of up to 0.47 nmol L−1. Furthermore, the modified electrode showed good stability, reproducibility, and anti-interference ability, meaning that it could be used to detect TBS in real samples.


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دوشنبه 29 مهر 1398  07:21 ب.ظ

Bricanyl® Turbohaler® 0.5 mg/dose inhalation powder /
Terbutaline sulfate 0.5 mg dry powder inhaler
(terbutaline sulfate)
This product is available as any of the above names but will be referred to as Bricanyl Turbohaler throughout this leaflet.
Read all of this leaflet carefully before you start using this medicine because it contains important information for you.

Keep this leaflet. You may need to read it again.

If you have any further questions, ask your doctor or pharmacist.

This medicine has been prescribed for you only. Do not pass it on to others. It may harm them, even if their signs of illness are the same as yours.β-agonist Powder

If you get any side effects, talk to your doctor or pharmacist. This includes any possible side effects not listed in this leaflet. See section 4. What is in this leaflet
1. What Bricanyl Turbohaler is and what it is used for
2. What you need to know before you use Bricanyl Turbohaler
3. How to use Bricanyl Turbohaler
4. Possible side effects
5. How to store Bricanyl Turbohaler
6. Contents of the pack and other information
1. WHAT BRICANYL TURBOHALER IS AND WHAT IT IS USED FOR
Bricanyl Turbohaler is an inhaler. It contains a medicine called terbutaline. This belongs to a group of medicines called ‘beta-agonists’. These work by relaxing certain muscles and opening up the airways in the lungs.
Bricanyl Turbohaler is used for asthma and other breathing problems where you have a tight chest and difficulty breathing.
2. WHAT YOU NEED TO KNOW BEFORE YOU USE BRICANYL TURBOHALER Do not use Bricanyl Turbohaler:
• If you are allergic to terbutaline.
Warnings and precautions
Talk to your doctor or pharmacist before using Bricanyl Turbohaler if:
• You have diabetes. If so, you may need some extra blood sugar tests when you start using Bricanyl Turbohaler.
• You have a history of heart disease, irregular heart rhythm or angina.
• You have an overactive thyroid gland.
If you are not sure if any of the above apply to you, talk to your doctor or pharmacist before using Bricanyl
Turbohaler.
Other medicines and Bricanyl Turbohaler
Tell your doctor or pharmacist if you are taking, have recently taken or might take any other medicines. This includes medicines that you buy without a prescription and herbal medicines. Bricanyl can affect the way that some medicines work and some medicines can have an effect on Bricanyl.In particular, tell your doctor or pharmacist if you are taking any of the following medicines:
• Steroid medicines (such as prednisolone).
• Medicines called ‘xanthines’ (such as theophylline).
• Medicines called ‘beta-blockers’ (such as atenolol or propranolol) including eye drops (such as timolol).
• Water tablets (diuretics) such as furosemide (also known as frusemide).
If you are to undergo surgery with general anaesthetics it is important that you inform your doctor about all medicines you use, including Bricanyl to protect you from adverse effects (e.g. irregular heart beat).Pregnancy, breast-feeding and fertility
• If you are pregnant or breast-feeding, think you may be pregnant or are planning to have a baby, ask your doctor or pharmacist for advice before using this medicine.
• If you become pregnant while you are using Bricanyl Turbohaler, talk to your doctor straight away.Driving and using machines Bricanyl is not likely to affect you being able to drive or use any machines.
3. HOW TO USE BRICANYL TURBOHALER
Always use this medicine exactly as your doctor or pharmacist has told you. Check with your doctor or pharmacist if you are not sure. If Bricanyl Turbohaler is to be used by a child, make sure that they use it correctly.
How much to take
• The recommended dose is one inhalation as required.
• Do not take more than four inhalations in any 24 hour period.
• One inhalation from your Bricanyl Turbohaler should last for up to six hours.
Talk to your doctor straight away if:
• Your breathing is getting worse.
• You often wake at night with asthma.
• You start getting a tight chest.
• You are not getting relief from your current dose.
These are signs that your asthma is not being controlled. You may need a different or additional treatment straight away.
Please read the complete instructions carefully before you start to take your medication Turbohaler is a multidose inhaler from which very small amounts of powder are
administered (Figure 1). When you breathe in through Turbohaler the powder is delivered to your lungs. It is therefore important that you inhale forcefully and deeply through the mouthpiece.
How to prepare a new Turbohaler for use Before using Turbohaler for the first time you need to prepare the inhaler for use.


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دوشنبه 29 مهر 1398  07:15 ب.ظ

Molecular Formula: C26H29NO.C6H8O7
Molecular weight: 563.64
CAS NO.: 54965-24-1
Appearance: white crystalline powder
MP: 140-144 ºC
How It Works
is the most commonly used hormone therapy for the treatment of breast cancer.
to know more about Antiestrogen,powder,liquid,peptide,prohormone)

Description:
Many women have breast cancer that tests positive for estrogen receptors (ER+). This means that estrogen promotes the growth of the breast cancer cells. T`amoxifen blocks the effects of estrogen on these cells. It is often called an “anti-estrogen. “Tamoxifen powder

Application:
Tamoxifen Citrate is agent that demonstrates potent anti-estrogenic properties. The drug is technically an estrogen agonist/antagonist, which competitively binds to estrogen receptors in various target tissues. With the t`amoxifen molecule bound to this receptor, estrogen is blocked from exerting any action, and an anti-estrogenic effect is achieved. Since many forms of breast cancer are responsive to estrogen, the ability of t`amoxifen citrate to block its action in such cells has proven to be a very effective treatment. It is also utilized successfully as a preventative measure, taken by people with an extremely high familial tendency for breast cancer.


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دوشنبه 29 مهر 1398  07:08 ب.ظ

Sotalol (3930-20-9) Mechanism Of Action

Sotalol powder is indicated to treat life threatening ventricular arrhytmias and maintain normal sinus rhythm in patients with atrial fibrillation or flutter.Label There are also oral solutions and intravenous injections indicated for patients requiring sotalol, but for whom a tablet would not be appropriate.

Sotalol powder is a competitive inhibitor of the rapid potassium channel. This inhibition lengthens the duration of action potentials and the refractory period in the atria and ventricles. The inhibition of rapid potassium channels is increases as heart rate decreases, which is why adverse effects like torsades de points is more likely to be seen at lower heart rates.6 L-sotalol also has beta adrenergic receptor blocking activity seen above plasma concentrations of 800ng/L. The beta blocking ability of sotalol further prolongs action potentials. D-sotalol does not have beta blocking activity but also reduces a patient’s heart rate while standing or exercising. These actions combine to produce a negative inotropic effect that reduces the strength of contractility of muscle cells in the heart. Extension of the QT interval is also adversely associated with the induction of arrhythmia in patients.
Sotalol powder was first synthesized in 1960 by A. A. Larsen of Mead-Johnson Pharmaceutical. It was originally recognized for its blood pressure lowering effects and its ability to reduce the symptoms of angina. It was made available in the United Kingdom and France in 1974, Germany in 1975, and Sweden in 1979. It became widely used in the 1980s. In the 1980s, its antiarrhythmic properties were discovered. The United States approved the drug in 1992.
06 Sotalol (3930-20-9) Mechanism Of Action

Beta-blocker action

Sotalol non-selectively binds to both β1- and β2-adrenergic receptors preventing activation of the receptors by their stimulatory ligand (catecholamines). Without the binding of this ligand to the receptor, the G-protein complex associated with the receptor cannot activate production of cyclic AMP, which is responsible for turning on calcium inflow channels. A decrease in activation of calcium channels will therefore result in a decrease in intracellular calcium. In heart cells, calcium is important in generating electrical signals for heart muscle contraction, as well as generating force for this contraction. In consideration of these important properties of calcium, two conclusions can Beta-blocker action

Sotalol non-selectively binds to both β1- and β2-adrenergic receptors preventing activation of the receptors by their stimulatory ligand (catecholamines). Without the binding of this ligand to the receptor, the G-protein complex associated with the receptor cannot activate production of cyclic AMP, which is responsible for turning on calcium inflow channels. A decrease in activation of calcium channels will therefore result in a decrease in intracellular calcium. In heart cells, calcium is important in generating electrical signals for heart muscle contraction, as well as generating force for this contraction. In consideration of these important properties of calcium, two conclusions can be drawn. First, with less calcium in the cell, there is a decrease in electrical signals for contraction, thus allowing time for the heart’s natural pacemaker to rectify arrhythmic contractions. Secondly, lower calcium means a decrease in strength and rate of the contractions, which can be helpful in treatment of abnormally fast heart rates.

Type III antiarrhythmic action

Sotalol also acts on potassium channels and causes a delay in relaxation of the ventricles. By blocking these potassium channels, sotalol inhibits efflux of K+ ions, which results in an increase in the time before another electrical signal can be generated in ventricular myocytes. This increase in the period before a new signal for contraction is generated, helps to correct arrhythmias by reducing the potential for premature or abnormal contraction of the ventricles but also prolongs the frequency of ventricular contraction to help treat tachycardia.


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Steroids Hormone Albuterol Sulfateis usually given by the inhaled route for direct effect on bronchial smooth muscle. This is usually achieved through a metered dose inhaler (MDI), nebulizer or other proprietary delivery devices (e.g. Rotahaler or Autohaler). In these forms of delivery, the maximal effect of salbutamol can take place within five to 20 minutes of dosing, though some relief is immediately seen. It can also be given intravenously.Used in the treatment of bronchial asthma, asthmatic bronchitis, emphysema, patients bronchospasm.Salbutamol powder

Albuterol is a bronchodilator that relaxes muscles in the airways and increases air flow to the lungs.Albuterol inhalation is used to treat or prevent bronchospasm in people with reversible obstructive airway disease. It is also used to prevent exercise-induced bronchospasm.

Albuterol sulfate is a prescription medication indicated to treat or prevent airway constriction in people with asthma. This medication is a bronchodilator, which works by relaxing the bronchial muscles within a patient’s airways to allow oxygen to reach the lungs. In certain instances, patients can develop allergic reaction symptoms after taking albuterol sulfate for the first time. Affected patients require immediate, emergency medical attention to avoid developing potentially life-threatening medical complications.
Albuterol Sulfate Usage:

Albuterol is used to treat wheezing and shortness of breath caused by breathing problems such as asthma. It is a quick-relief medication. Albuterol belongs to a class of medicine known as bronchodilators. It works in the airways by opening breathing passages and relaxing muscles. Controlling symptoms of breathing problems can decrease time lost from work or schoo


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دوشنبه 29 مهر 1398  06:51 ب.ظ

A haemangioma is a collection of small immature blood vessels. They are sometimes called ‘strawberry marks’ because the surface of some haemangiomas look a bit like a strawberry.Propanolol

Haemangiomas can be superficial or deep in the skin. Some haemangiomas are a combination of the two, seen as a raised red area on the surface of the skin, and as a bluish swelling of abnormal blood vessels deeper in the skin. Very occasionally haemangiomas may occur internally.
Haemangiomas are not usually obvious at birth but become apparent within a few days or weeks. They grow rapidly in the first three months, increasing in size and sometimes in redness.It is unusual for haemangiomas to grow after six to 10 months of age, when most haemangiomas tend to have a ‘rest period’ and then begin to shrink.

What is propranolol?
Propranolol is a beta-blocker. Some nerves release a chemical called noradrenaline when they are stimulated, which in turn stimulates ‘beta adrenergic receptors’. These can cause a variety of effects. For instance, if the beta adrenergic receptors in the heart are stimulated, the heart pumps harder and faster than before, so more blood is pumped around the body. Betablocker medicines block the beta adrenergic receptors and stop them being stimulated.

How does propranolol help with haemangiomas?
By blocking the beta adrenergic receptors, propranolol can make blood vessels narrower, reducing the amount of blood flowing through them. This is particularly effective in haemangiomas, by reducing the colour and making them softer. Growth of the haemangioma cells is also limited by propranolol so that the haemangioma starts to reduce in size. More research is needed to fully understand how propranolol works. The beneficial effects are usually seen very quickly.

Are there side effects with propranolol treatment?
Propranolol is associated with the following side effects, which happen very rarely. However, you should report any of the following to your doctor as the dose of propranolol may need to be altered or on very rare occasions, stopped.
Bradycardia (slow heart rate).
Hypotension (low blood pressure).
Bronchspasm (temporary narrowing of the airway, leading to wheezing and coughing).
Peripheral vasoconstriction (reduced blood flow to the extremities, such as fingers and toes, making them feel cold and turn a blue colour).
Weakness and fatigue, showing as floppiness and disinterest in surroundings.
Sleep disturbance.
Hypoglycaemia (low blood sugar).
Gastrointestinal disturbances such as constipation or diarrhoea.
If you have any concerns about these side effects, please discuss them with your doctor, nurse or pharmacist.
Are any tests needed before starting propranolol treatment?
Occasionally we will suggest some tests to check that your child can safely take the medicine. These may include blood and urine tests, an electrocardiogram (ECG) and echocardiogram (echo). If your child has multiple haemangiomas visible on the skin, we may also carry out an abdominal ultrasound scan to look for any haemangiomas in the liver.

What happens when my child starts treatment?
Some infants will be monitored for two hours after the first dose. This monitoring allows the doctors to be absolutely sure your child can tolerate the prescribed dose. The procedure is occasionally repeated after one week when the dose is increased, although the dose is normally increased at home.


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دوشنبه 29 مهر 1398  06:45 ب.ظ

Propranolol Hydrochloride is a synthetic beta-adrenergic receptor blocking agent chemically described as 2-Propanol, 1-[(1-methylethyl)amino]-3-(1-naphthalenyloxy)-, hydrochloride,(±)-. Its molecular and structural formula:β-agonist Powder

Propranolol Hydrochloride Oral Solution is available for oral administration containing either 20 mg per 5 mL or 40 mg per 5 mL of propranolol hydrochloride USP. The oral solution contains the following inactive ingredients: citric acid anhydrous, crème de menthe flavor, disodium edetate, methyl paraben, propylene glycol, propylparaben, purified water, saccharin sodium, sorbitol solution and strawberry flavor.

Propranolol is a nonselective beta-adrenergic receptor blocking agent possessing no other autonomic nervous system activity. It specifically competes with beta-adrenergic receptor agonist agents for available receptor sites. When access to beta-receptor sites is blocked by propranolol, the chronotropic, inotropic, and vasodilator responses to beta-adrenergic stimulation are decreased proportionately. At dosages greater than required for beta-blockade, propranolol also exerts a quinidine-like or anesthetic-like membrane action, which affects the cardiac action potential. The significance of the membrane action in the treatment of arrhythmias is uncertain.

Mechanism of Action

The mechanism of the antihypertensive effect of propranolol has not been established. Factors that may contribute to the antihypertensive action include: (1) decreased cardiac output, (2) inhibition of renin release by the kidneys, and (3) diminution of tonic sympathetic nerve outflow from vasomotor centers in the brain. Although total peripheral resistance may increase initially, it readjusts to or below the pretreatment level with chronic use of propranolol. Effects of propranolol on plasma volume appear to be minor and somewhat variable.

In angina pectoris, propranolol generally reduces the oxygen requirement of the heart at any given level of effort by blocking the catecholamine-induced increases in the heart rate, systolic blood pressure, and the velocity and extent of myocardial contraction. Propranolol may increase oxygen requirements by increasing left ventricular fiber length, end diastolic pressure, and systolic ejection period. The net physiologic effect of beta-adrenergic blockade is usually advantageous and is manifested during exercise by delayed onset of pain and increased work capacity.

Propranolol exerts its antiarrhythmic effects in concentrations associated with beta-adrenergic blockade, and this appears to be its principal antiarrhythmic mechanism of action. In dosages greater than required for beta-blockade, propranolol also exerts a quinidine-like or anesthetic-like membrane action, which affects the cardiac action potential. The significance of the membrane action in the treatment of arrhythmias is uncertain.

The mechanism of the antimigraine effect of propranolol has not been established. Beta-adrenergic receptors have been demonstrated in the pial vessels of the brain.

The specific mechanism of propranolol’s antitremor effects has not been established, but beta-2 (noncardiac) receptors may be involved. A central effect is also possible. Clinical studies have demonstrated that propranolol is of benefit in exaggerated physiological and essential (familial) tremor
Propranolol is highly lipophilic and almost completely absorbed after oral administration. However, it undergoes high first-pass metabolism by the liver and on average, only about 25% of propranolol reaches the systemic circulation. Peak plasma concentrations occur about 1 to 4 hours after an oral dose.

Administration of protein-rich foods increase the bioavailability of propranolol by about 50% with no change in time to peak concentration, plasma binding, half-life, or the amount of unchanged drug in the urine.

Distribution

Approximately 90% of circulating propranolol is bound to plasma proteins (albumin and alpha1 acid glycoprotein). The binding is enantiomer-selective. The S(-)-enantiomer is preferentially bound to alpha1 glycoprotein and the R(+)- enantiomer preferentially bound to albumin. The volume of distribution of propranolol is approximately 4 liters/kg.


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Factory Supply Pharmaceutical Raw Material High Quality Indapamide 99%

1. Indapamide is a thiazide-like diuretic drug marketed by Servier, generally used in the treatment of hypertension, as well as decompensated heart failure. Combination preparations with perindopril (an ACE inhibitor antihypertensive) are also available.Indapamide powder

2. White needle crystal or crystalline powder, odorless, tasteless. It is almost insoluble in water or dilute hydrochloric acid, while it can be dissolved in ethanol or ethyl acetate, and it is soluble in acetone, acetic acid, slightly soluble in chloroform or ether.

3. Indapamide is currently the most popular non-prescription diuretic antihypertensive drug with good efficacy, stable blood pressure, fewer side effects, etc.
1. Indapamide have diuretic and calcium antagonist dual effect by inhibiting the proximal end of the distal convoluted tubule Na+ reabsorption, resulting in diuresis, while by blocking Ca2+ influx especially a higher selectivity for vascular smooth muscle to dilate the small blood vessels of the outer periphery, resulting in antihypertensive effect. But the effect to vascular smooth muscle is stronger than the diuretic effect.

2. It can lower blood pressure with lower dose compared to diuretic effect. Higher dose will display diuretic effect. But there is no disadvantage compared to thiazide diuretics, that it does not cause orthostatic hypotension, flushing and reflex tachycardia, nor blood lipids, glucose metabolism and renal function.

Indapamide Application
1. This medication is used to treat high blood pressure. Indapamide is also used to reduce extra salt and fluid in the body (edema) caused by a certain heart problem (congestive heart failure). Lowering high blood pressure helps prevent strokes, heart attacks, and kidney problems. Decreasing extra salt and fluid in the body helps to decrease swelling and breathing problems from congestive heart failure and increases your ability to exercise.

2. Indapamide is a “water pill” (diuretic) that increases the amount of urine you make. Getting rid of extra water and salt may help to relax the blood vessels so that bloodcan flow more easily. These effects help to lower blood pressure and decrease the amount of work the heart must do to pump blood.


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دوشنبه 29 مهر 1398  06:32 ب.ظ

White needle crystal or crystalline powder, odorless and tasteless. Almost insoluble in water or dilute hydrochloric acid, soluble in ethanol or ethyl acetate, soluble in acetone, acetic acid, slightly soluble in chloroform or ether.β-agonist Powder

Indapamide is an over-the-counter diuretic antihypertensive drug commonly used in China, which has the advantages of good efficacy, stable antihypertensive and less side effects.

Indapamide has dual effects of diuresis and calcium antagonism. By inhibiting Na+ reabsorption at the proximal end of the distal convoluted tubule, it can produce diuretic effect and block Ca2+ internal flow. It is highly selective to vascular smooth muscle, so as to dilate peripheral small blood vessels and generate antihypertensive effect. But the effect on vascular smooth muscle stronger diuretic effect, below the diuretic doses can step-down, higher doses showed diuretic effect, but no thiazide diuretic shortcomings, namely not cause orthostatic hypotension, flush and reflective tachycardia, on blood picture, metabolism of blood fat, sugar and renal function also had no obvious effect, therapeutic doses of heart rate, cardiac output, no significant changes in electrocardiogram (ecg) were on the central nervous system and plant nerve has no obvious effect. The antihypertensive effect was produced by oral administration for 2 ~ 3h and maintained for 24h. The diuretic effect appeared for 3h and reached the maximum effect for 4 ~ 6h. Different from other diuretics, this product has high lipid solubility. After oral absorption, the plasma concentration of liver and kidney is the highest, while the concentration of heart, lung, muscle and fat is lower. This product is mainly excreted from the kidney by metabolites and 5% prototype. Indapamide is suitable for mild and moderate primary hypertension, can also be used for congestive heart failure caused by water sodium retention, with renal failure are also applicable to the patients with high blood pressure, diabetes, hyperlipidemia, use antihypertensive effect is remarkable, and beta blockers used curative effect is better, because this drug has diuretic effect, can cause hypokalemia, can complement potassium at the same time.


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