Background and History Spironolactone is a light cream colored stable powder that has a faint odor (6). Spironolactone was created by G.D. Searle and is currently the only product that directly treats hyperaldosteronism, the excess production of aldosterone in the body (9). Spironolactone is in the aldosterone-receptor blockers medication category. Spironolactone is a diuretic mostly used to treat hypertension and edemas (8). The discovery that led to the development of spironolactone was aldosterone being found to be the third hormone in the adrenal cortex (6). Aldosterone is created in the zona glomerulosa that is a region of the adrenal cortex. The information know aldosterone led to research into the creation of compounds and medications …show more content…
that could inhibit the activity of the aldosterone. One of these compounds that was created was a group of spirolactones (6). Some of the first work on adrenal compounds was done at Columbia University in 1935. The first major breakthrough came in 1953 from the work of Reichstein who discovered how to isolate aldosterone (7). After discovering that aldosterone caused edemas that could lead to other conditions, there was a research phase to develop an antagonist for the aldosterone receptor (9). Spironolactone was first given to rats and showed aldosterone-blocking activity. The lactone-carbonyl group has an important role in the receptor-blocking activity of spironolactone (6). Chemistry To prepare Spironolactone, 3beta-hydroxy-5-androsten-17-one is reacted with acetylene to form another compound that is then reacted with carbon dioxide and methyl magnesium bromide.
The compound that is formed is 17alpha-propiolic acid which is reduced to the lactone. Then the solution is oxidized and treated with thioacetic acid and chloranil that finally create spironolactone, also known as 17-hydroxy-7α-mercapto-3-oxo-17α-pregn-4-ene-21-carboxylic acid γ-lactone acetate (6). Spironolactone has a melting point of 198 degrees Celsius to 207 degrees Celsius. It is insoluble in water, but soluble in benzene, ethyl acetate, and alcohol. The solubility of Spironolactone increases with increasing polarity of the solvent. The IR spectrum of spironolactone shows a conjugate carbonyl group and a lactone carbonyl present in the structure …show more content…
(6). Pharmacology Spironolactone acts as a pharmacologic antagonist of aldosterone by acting as a competitive binder to aldosterone receptors (5). Aldosterone works in the kidney to absorb sodium and water and regulate the excretion of potassium (9). Spironolactone acts as a diuretic by excreting excess sodium and water, but potassium remains in the body. Spironolactone can be given with other diuretic medications to have an increased effect. Increased amounts of aldosterone, a mineral corticosteroid, and causes primary and secondary hyperaldosteronism. Primary hyperaldosteronism can lead to hypertension and secondary hyperaldosteronism can lead to heart conditions, such as heart failure, and edemas. Spironolactone is effective in treating hypertension from primary hyperaldosteronism. Spironolactone acts primarily at the collecting tubule in the kidneys, but can also act in the heart (9). Aldactone, one of the main components of spironolactone, is quickly absorbed into the body and along with the sulfur components is a main reason for the effectiveness of the drug. Food increases the absorption of the drug and is excreted many through urine and partially bile (5). Spironolactone is metabolized in to many metabolites, including the two most important in relation to pharmacology, canrenoate and canrenone. Side Effect, Adverse Effects, and Toxicology Therapeutic Application Spironolactone is used for treatment of primary hyperaldosteronism for use in patients that need short term treatment before possible surgery.
It can also be used for patients who need long term treatment for hyperaldosteronism and decline surgery. Spironolactone can also be used to treat congestive heart failure that are caused from edemas and can treat essential hypertension with other medications if it is appropriate for the patient (5). Spironolactone was also found to be the most effective treatment for resistant hypertension to add on to current therapy (1). Spironolactone has some minor uses in women treating hirsutism resulting from polycystic ovarian syndrome and treat acne occurring during puberty (8). The average dose for adults is twenty-five milligrams four times a day in tablet form and the usual pediatric dose is 3.3 milligrams per kilogram given throughout the day (8). Spironolactone is not commonly used during pregnancy because of the diuretic usage it can be unsafe for the mother and fetus
(5).
In a small reaction tube, the tetraphenylcyclopentadienone (0.110 g, 0.28 mmol) was added into the dimethyl acetylene dicarboxylate (0.1 mL) and nitrobenzene (1 mL) along with a boiling stick. The color of the mixed solution was purple. The solution was then heated to reflux until it turned into a tan color. After the color change has occurred, ethanol (3 mL) was stirred into the small reaction tube. After that, the small reaction tube was placed in an ice bath until the solid was formed at the bottom of the tube. Then, the solution with the precipitate was filtered through vacuum filtration and washed with ethanol. The precipitate then was dried and weighed. The final product was dimethyl tertraphenylpthalate (0.086 g, 0.172mmol, 61.42%).
The purpose of this experiment was to learn and preform an acid-base extraction technique to separate organic compounds successfully and obtaining amounts of each component in the mixture. In this experiment, the separation will be done by separatory funnel preforming on two liquids that are immiscible from two layers when added together. The individual components of Phensuprin (Acetylsalicylic acid, Acetanilide, and Sucrose as a filler) was separated based upon their solubility and reactivity, and the amount of each component in the mixture was obtained. Also, the purity of each component will be determined by the melting point of the component.
Ace Inhibitors are used to treat hypertension and congestive heart failure (CHF). Most of the drugs that are Ace Inhibitors have the common ending –pril. It inhibits an enzyme; that decreases the tension of blood vessels and the blood volume, thus lowering blood pressure. Lotensin (benzapril) comes in tablets and is used for oral administration. It is one of the ace inhibitors that are indicated for treating hypertension. There is warning while using Lotensin when pregnant, it indicates to stop using immediately when pregnancy is detected. Vasotec (enalpril) comes in tablets and injection. It is indicated for the treatment of hypertension and is effective alone or in combination with other Ace Inhibitors agents, especially thiazide-type diuretics. There is a warning for fetal toxicity; when pregnancy is detected; stop using.
The primary goal of this laboratory project was to identify an unknown compound and determine its chemical and physical properties. First the appearance, odor, solubility, and conductivity of the compound were observed and measured so that they could be compared to those of known compounds. Then the cation present in the compound was identified using the flame test. The identity of the anion present in the compound was deduced through a series of chemical tests (Cooper, 2009).
Results: Through a melting point reading, it was determined that the product obtained was 2,4-Dibromoanisol mp 55-58 C. The products obtained by my partners, were determined to be: (p-bromoacetanilide mp 160-165 C) and (2,4,6 tribromoaniline, mp of 108-110 C) respectively.
The solvent should be easily removed from the purified product, not react with the target substances, and should only dissolve the target substance near it’s boiling point, but none at freezing. A successful recrystallization uses minimum amount of solvent, and cools the solution slowly, if done to fast, many impurities will be left in the crystals. Using the correct solvent, in this case ice water and ethyl acetate, the impurities in the compound can be dissolved to obtain just the pure compound. A mixed solvent was used to control the solubility of the product. The product is soluble in ethanol an insoluble in water. Adding water reduced solubility and saturates the solution and then the crystals
Ropivacaine is homologous to Bupivacaine . If local anaesthetics are administered into the vein or artery it results to very high systemic levels possibly causing CNS and CV toxicity due to rapid penetration into these regions. Both bupivacaine and ropivacaine are amide linked esters. They are extensively bound in the plasma. Amides extensively bind to the alpha-1 acid glycoprotein (AAG) with ~94% ropivacaine bound to it; it has a higher affinity even though albumin binds to greater amount due to its relative abundance in the human plasma. AAG concentration increases after operative surgery. Ropivacaine is metabolised by the cytochrome P450 isoenzymes CYP1A2 and CYP3A4 to four metabolites, 3-OH-2’6’-pipecoloxylidide, 4-OH-ropivacaine, 3-OH-ropivacaine, and N-dealkylated PPX. Reduced protein binding means that there is higher fraction of the unbound drug circulating in the plasma. Furthermore, amides are hepatically metabolised by amidases. Amidase metabolism is much slower than plasma hydrolysis in which ester linked local anaesthetics undergo. This means that amides are prone to accumulation when administered by continuous infusion. Drug accumulation is also influenced by reduced hepatic perfusion and hepatic dysfunction. It has been reported that high concentrations of unbound bupivacaine are linked with higher rates of early symptoms of CNS toxicity.
The purified unknown had a melting point range, as seen in Table 1, of 135-137ºC. When the unknown was combined with acetanilide, the melting point range of the mixture was much lower, at only 97-106ºC. The literature melting point of acetanilide is 114ºC where the literature melting point of phenacetin is 135ºC. When the unknown was combined with phenacetin, as seen in Table 1, the melting point range of the mixture was very close to that of the purified unknown, 134-138ºC, and the literature value of phenacetin. It could therefore be concluded that, based on the solubility and melting point of the unknown component, the unknown could be identified as
Aldosterone is in a class of hormones called mineralocorticoids which is also produced by the adrenal glands. The main functions of aldosterone are to help to maintain blood pressure and helping the kidneys retain needed sodium and excrete unwanted potassium to maintain the balance of water and salt in the body.
The recommended dose is 200 mg daily, taken as two separate 100 mg doses, one tablet in the morning and one in the evening.
WILLIAMS, P and POULTER NR et al (2004) Guidelines for management of hypertension: report of the fourth working party of the British Hypertension Society. British Hypertension Society, pp. 139-85
Patient takes captopril orally 12.5-50 mg 2-3 times daily. It lowers blood pressure by vasodilating blood vessels, and decreasing excessive water and salt in tissue. Side effects of captopril are hypotension, protein in urine, taste disturbances, hyperkalemia, headache, dry cough. Adverse effects are fever, chills, swelling in the face, hands, or feet, trouble swallowing, and chest pain. More serious adverse effects are allergic reaction and kidney failure. Patient teaching includes to take medication at the same time every day, and take it 1 hour before eating. Patient should report side effect to the doctor
Menopause naturally occurs in women at a median age of 51 years old due to deficiencies in hormones from ovarian loss of function.1 Some of the most common symptoms of menopause are vasomotor hot flashes and night sweats. The goal of therapy is symptom and quality of life improvement while minimizing side effects. As long as no contraindications are present, the recommended treatment for menopausal vasomotor hot flashes is hormone replacement therapy (HRT).1,2,3 Customized to patient’s symptoms, history of risk factors, and preferences, HRT may increase quality of life.2 However, there are some serious contraindications, possible increased risk for venous thromboembolism and breast cancer, and unclear risk areas concerning HRT along with public skepticism.1,3 Escitalopram(Lexapro ®) is another option studied for
Hypertension is an illness that affect elderly across the world, and it most affect women more than man, this is because women are mostly affected because of pregnancy, birth controls and menopause. Hypertension is “the silent killer” because in most cases it does not cause symptoms for many years until a vital organ in the body is damaged, furthermore it can be controlled by reducing salt intake, and increase physical activity and eating fruits and vegetables.
Becoming pregnant is something that is a struggle for many women, especially when certain infections and diseases are involved. These infections can make it harder to conceive because they can affect the health of the woman and her reproductive system.