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Cholesterol Lowering

What is cholesterol?

Cholesterol is an insoluble fatty substance that is needed by the body for many functions, such as building cell membranes, producing certain hormones and transporting fat soluble vitamins around the body. It is made in the liver and also obtained from the diet. Cholesterol is transported in the blood along with triglycerides, which is another type of fat. Since cholesterol is not soluble in blood it is carried to and from the liver by lipoproteins. These include low density lipoproteins (LDL) known as “bad” cholesterol because they carry cholesterol from the liver and deposit excess in the arteries. High density lipoproteins (HDL) carry cholesterol back to the liver and are therefore called “good” cholesterol.

High cholesterol and atherosclerosis

If there is more cholesterol in the blood than the body needs, it becomes deposited in the artery walls where it can build up, blocking the arteries and causing hardened areas called plaques, which increases risk of heart disease. This condition is known as atherosclerosis. High cholesterol in the blood and other fats (triglycerides) is known as hypercholesterolaemia and this condition is usually due to lifestyle, including high-fat diet, obesity and lack of exercise, but it can be inherited. The ratio of total cholesterol over HDL (good cholesterol) is also an important consideration.

Cholesterol lowering medications

Cholesterol lowering medications are available to treat hypercholesterolaemia in people who have not responded to a low-fat diet and lifestyle changes alone; also for those with an inherited condition and who cannot lower cholesterol levels by lifestyle changes alone. They include:
  • Statins that block the production of cholesterol by the liver, by inhibiting the action of the enzyme HMG-CoA reductase that plays an important role in cholesterol synthesis. Statins only block cholesterol produced in the liver but have no effect on cholesterol that comes from fat in the diet. Several statins are available including, atorvastatin, simvastatin, pravastatin and rosuvastatin.

  • Cholesterol absorption inhibitors, like ezetimibe act directly on the small intestine wall to block the action of the sterol transporter in the intestine wall. This action inhibits intestinal absorption of cholesterol from the diet and reduces cholesterol stores in the liver, which helps lower blood cholesterol levels.

  • Fibrates like fenofibrate activate the enzyme Peroxisome Proliferator Activated Receptor type alpha (PPARα) that regulates the production of another enzyme involved in the breakdown of lipids in the blood. It also reduces the production of proteins that transport LDL lipids but increases the production of proteins that transport HDL. The overall effect is to lower triglycerides, total cholesterol, and LDL (bad) cholesterol, and increase HDL (good) cholesterol.

Cholesterol Lowering
Erectile Dysfunction

What causes ED?

The natural process of sexual stimulation activates a series of biochemical reactions that relaxes blood vessels in the penis and allows blood flow into the corpus cavernosum, which is the spongy erectile tissue of the penis that fills with blood causing an erection. Loss of an erection is due to the activity of an enzyme called phosphodiesterase type 5 (PDE5) that breaks down the chemical responsible for relaxing blood vessels, cyclic guanosine monophosphate (cGMP), which results in contraction of the blood vessels, preventing blood flow. If the natural processes do not function properly due to physical or psychological problems, this can lead to erectile dysfunction or ED.

Medications for ED

The medications available for treating ED are used to increase blood flow into the penis, working by different mechanisms. These are:
  • Phosphodiesterase type 5 (PDE5) inhibitors
  • Prostaglandins

Phosphodiesterase type 5 (PDE5) inhibitors

Phosphodiesterase type 5 (PDE5) inhibitors block the action of the enzyme PDE5 that prevents blood flow into the penis and this action allows blood to remain in the penis, which maintains an erection. This resolves ED by allowing the natural process of sexual stimulation to activate the mechanism for achieving and maintaining an erection. However, PDE5 inhibitors only work when sexually aroused and do not work otherwise; their effect lasts for around four hours. These medications include sildenafil, tadalafil, vardenafil.

Prostaglandins

Prostaglandin E1, also known as alprostadil, is a naturally occurring chemical that has many functions including relaxation of smooth muscle in various tissues, including the corpus cavernosum and blood vessel walls. Prostaglandin E1 is used to treat ED by direct injection into the penis resulting in widening of the cavernosal arteries in the penis and relaxation of trabecular smooth muscle in the penis. This increases blood flow into the penis causing an erection.

Cold Sore Treatments

What are cold sores?

Herpes Simplex Virus (HSV) is a virus that infects mucous membrane cells and exists in two forms;HSV I that infects the lips, mouth and face, and HSV-II that infects the genitals. A cold sore is the result of an infection with HSV I and early warning signs of active virus include a tingling sensation on the lips or face. If untreated at an early stage the virus will multiply rapidly and within 24 hours a cold sore will form, starting as small blisters on the surface of the skin, which join up to form a weeping sore. This is when the virus is contagious and can spread to form more cold sores or can infect others by direct contact. Eventually the immune system kicks in to kill the virus and the cold sore crusts over to form a scab as it heals.

Once infected with HSV it is always possible that re-infection will occur, as the virus can persist undetected by travelling down a nerve fibre and lying dormant or inactive in a nerve cell, to be reactivated under certain conditions, such as by stress, illness, sunlight or a compromised immune system.

Treatments for cold sores

Acyclovir is an antiviral drug that can be used to treat infection with HSV-1. It is a nucleoside analogue, which means that it becomes incorporated into the viral DNA within the host cell and replaces building blocks needed for viral DNA synthesis. This inhibits the action of viral DNA polymerase and prevents normal viral DNA synthesis, without affecting normal processes of the host cells, which prevents the virus replicating and therefore stops the growth and spread of the virus. If applied to the skin within 24 hours of the first tingle, acyclovir can prevent a cold sore from developing. However, it can be used at any stage of infection, to prevent spread of infection, reduce and relieve painful symptoms, and speed up the heeling process to help heal blisters and sores caused by the infection. Acyclovir can also be taken orally to suppress recurrent infection of HSV and to prevent infection in people who are immunocompromised. Valacyclovir is a similar antiviral to acyclovir and is a prodrug of acyclovir that is more readily absorbed and is converted to acyclovir by the liver.
Anti Nausea/Vomiting

What is motion sickness?

Motion sickness is associated with various forms of travel including air, sea, train or car travel. It is also possible to experience motion sickness when watching a movie in which dramatic movements are shown, but the body is motionless. Movement is detected by the vestibular system of the ear, which comprise the fluid filled canals in the inner ear. These detect motion or changes in the body’s position and send the information to the brain. If visual messages sent by the eye suggest that the body is still, this conflict causes the brain to interpret this discrepancy as an hallucination due to an ingested toxin that needs to be cleared from the system. This stimulates the area postrema of the brain to induce the vomiting reflex. Motion sickness is a neurological condition that is based on perception rather than a physical disorder.

How do antiemetics help with motion sickness?

Antiemetics like the anticholinergic scopolamine work by blocking specific receptors for acetylcholine in the vestibular system of the ear and in the brain. Stimulation of acetylcholine receptors is involved in the transmission of information from the vestibular system of the ear to the vomiting center in brain and from the brain to the stomach. The anticholinergic action of antiemetics like scopolamine prevents the vomiting reflex from being induced, which eases symptoms of motion sickness.
 
 
 
 
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