What is the mechanism of action of simvastatin?

Simvastatin is in a class of medications called HMG-CoA reductase inhibitors (statins). It works by slowing the production of cholesterol in the body to decrease the amount of cholesterol that may build up on the walls of the arteries and block blood flow to the heart, brain, and other parts of the body.

Where is simvastatin metabolised?

liver
Relative to the liver, OATP1B1 moves simvastatin to its site of action where inhibition of HMG CoA reductase results in decreased cholesterol production, thus exerting its pharmacologic and therapeutic effects. Additionally, the liver is the main site of statin metabolism.

How do statins work pharmacology?

By inhibiting HMG-CoA reductase, statins block the pathway for synthesizing cholesterol in the liver. This is significant because most circulating cholesterol comes from internal manufacture rather than the diet. When the liver can no longer produce cholesterol, levels of cholesterol in the blood will fall.

How long does simvastatin stay in your system?

Short-acting statins work better at night because the liver enzyme that produces cholesterol is more active at this time. Most short-acting statins have a half-life of 6 hours. A medication’s half-life is the time that it takes for the body to process and remove half of the medication.

What are the bad side effects of simvastatin?

The most common statin side effects include:

• Headache.
• Difficulty sleeping.
• Flushing of the skin.
• Muscle aches, tenderness, or weakness (myalgia)
• Drowsiness.
• Dizziness.
• Nausea or vomiting.
• Abdominal cramping or pain.

What is the contraindications for simvastatin?

Patients with contraindications to simvastatin pharmacotherapy include those with active liver disease, including those who have elevated hepatic enzymes, pregnancy, and women who may become pregnant or who are breastfeeding.

What are the side effects of simvastatin?

This medication may rarely cause liver problems. If you notice any of the following rare but serious side effects, tell your doctor right away: yellowing eyes/skin, dark urine, severe stomach/abdominal pain, persistent nausea/vomiting. A very serious allergic reaction to this drug is rare.

How do I activate simvastatin?

Activation of simvastatin Simvastatin needs to be activated by opening of the lactone ring before use in cell culture. We used the protocol provided by Merck. Briefly, eight milligrams of simvastatin (0.019 mM) were dissolved in 0.2 ml of 100% ethanol, with subsequent addition of 0.3 ml of 0.1 N NaOH.

What are the side effects of simvastatin 40 mg?

Common side effects of simvastatin include:

• CPK elevation (greater than 3x ULN)
• Constipation.
• Upper respiratory infection.
• Gas (flatulence)
• Transaminases increased (greater than 3x ULN)
• Headache.
• Muscle pain, muscle damage, or muscle weakness.
• Eczema.

What happens when you stop taking simvastatin?

Statins (atorvastatin, simvastatin, Crestor) decrease mortality rates in patients with high cholesterol. They will help you live longer. Stopping your statin has been linked to increased risk for cardiovascular events (like heart attack) and death in patients with coronary artery disease.

What should you avoid while taking simvastatin?

Drinking large amounts of grapefruit juice (more than 1 quart each day) while taking this medicine may increase your risk of muscle injury and could result in kidney problems. Do not drink large amounts of alcohol with simvastatin. This could cause unwanted effects on the liver.

How many mg of simvastatin are in a tablet?

Simvastatin is a white to off-white, nonhygroscopic, crystalline powder that is practically insoluble in water, and freely soluble in chloroform, methanol and ethanol. Simvastatin orally disintegrating tablets for oral administration contain either 10 mg, 20 mg, 40 mg or 80 mg of simvastatin.

What are the inactive ingredients in simvastatin tablets?

Simvastatin tablets for oral administration contain either 10 mg, 20 mg, 40 mg or 80 mg of simvastatin and the following inactive ingredients: ascorbic acid, citric acid, hydroxy propyl cellulose, hypromellose, iron oxides, lactose monohydrate, magnesium stearate, microcrystalline cellulose, pregelatinised starch, talc and titanium dioxide.

How much simvastatin is in a film coated tablet?

Each film-coated tablet contains 10 mg simvastatin. One film-coated tablet contains 70 mg lactose monohydrate. For the full list of excipients, see section 6.1. 3. Pharmaceutical form Film-coated tablet. Light pink, round [diameter 6.1 mm] and biconvex film-coated tablets with “A” debossed on one side and “01” on the other side. 4.

Can you drink 240 ml of water after taking simvastatin?

The pharmacokinetics of simvastatin and simvastatin acid, following administration of the 80 mg Simvastatin orally disintegrating tablet and 240 mL water at 1 minute post-dosing, were comparable to those following administration of the simvastatin immediate release 80 mg tablet taken with 240 mL water.