Pharmacology Of Atorvastatin Calcium Lipitor Biology Essay

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It is a cholesterol lowering medication that blocks the production of cholesterol a type of fat in the body. It reduces low density lipo-protein (LDL) cholesterol and total cholesterol in the blood lowering the cholesterol can help to prevent heart disease. Atorvastatin is used to treat high cholesterol is used to treat high cholesterol lower the risk of stroke heart attack are other heart complications in people with coronary heart disease or type 2 diabetes.

Atorvastatin calcium is absorbed from the gastro intestinal track it has low bio availability of 12% due to pre systemic clearance in the gastrointestinal mucosa and first pass metabolism in the liver. it is metabolized by the cytochrome p450 iso enzyme cyp3A4 to a number of active metabolites it is 98% bound to plasma. The mean plasma elimination half life of Atorvastatin is about 14 hrs although the half life of inhibitory activity for HMG-COA reductase is about 20 to30 hrs due to active metabolites Atorvastatin is excreted as metabolites primarily on the bile

Initial dosage: 10 mg to 80 mg orally once a day. The initial dosage of Atorvastatin recommended for the patient in the prevention of cardiovascular disease is 10 mg to 80 mg orally once a day Atorvastatin may be administered at any time of the day without regards for meals. Studies have demonstrated that treatment with Atorvastatin is associated with significant reduction in the risk of cardiovascular end points and stroke in various patient populations for both primary and secondary prevention. For primary prevention Atorvastatin treatment was effective in hypertensive patients with normal or mildly elevated cholesterol level as well as in patients with type 2 diabetes. Treatment with Atorvastatin still resulted in significant reductions in cardiovascular outcomes and stroke. For secondary prevention intensive lipid lowering therapy with Atorvastatin 80 mg/day was associated significant incremental clinical Benefit beyond therapy with 10 mg/day in patients with stable coronary heart disease it was also shown to significantly reduce the risk of clinical outcomes in coronary heart disease patients versus usual medical care.

Action and use:

HMG-COA Reductase inhibitor

Reduce the risk of myocardial infarction

Reduce the risk of stroke

Reduce the risk of revascularization procedures and Angina

Reduce the risk of fatal and non-fatal stroke

Drug Interaction:

The risk of myopathy during treatment with statins is increased with concurrent administration of fibric acid derivatives, lipid modifying doses of niacin cyclosporine or strong CYP3A4 inhibitors, (e.g.: claritromycin HIV protease inhibitors and itraconozole).The most serious consequence of drug interactions with Atorvastatin and other statins is the development of myopathy or Rhabdomylysis. The risk of myopathy is also increased by drugs that increase the plasma levels of statins by inhibiting their metabolism.

Side effects

Mild nausea or stomach pain, stomach upset,


Blotting gas

Stuffy noise

Itching, skin rashes,

Head ache

Fever with flu symptoms. Loss appetite, dark urine, clay colored stools, jaundice

4.1.7 Dosage and Administration:

-Maintenance dose: 10 to 80 mg orally once a day. Usual pediatric Dose for heterozygous familial Hypercholesterolemia 10 to17 years.10mg per day (max dose is20mg per day) Adjustments should be made at intervals of 4 weeks.


4.2.1 Pharmacology:

Telmisartan is an Angiotensin Receptor Blocker (ARB) that shows high affinity for the Angiotensin 2 type 1 (AT1) receptors, has a long duration of action. Telmisartan acts as selective modulator of peroxisome. Proliferators. Activated receptor gamma, a central regulator of insulin and glucose metabolism. Telmisartan has dual mode of action that may provide protective benefits against the vascular and renal damage caused by diabetes and cardiovascular disease. Telmisartan has binding affinity 3000 times greater for AT1 than AT2 receptors. Telmisartan also having the longest half-life (24hrs) of all angiotensin 2type1 receptor antagonists. Telmisartan has largest volume of distribution.

4.2.2 Pharmacokinetics:

Telmisartan is rapidly absorbed from the gastro intestinal tract. The absolute bioavailability is dose dependent and is about 42% after a 40mg dose and 58% after a 160 mg dose. Peak plasma concentration of Telmisartan is reached about 0.5 to 1 hour after an oral dose. Telmisartan is over 99% bound to plasma proteins it is excreted almost entirely in the faeces via bile mainly as unchanged drug .The terminal elimination half life telmisartan is about 24 hours.

4.2.3 Pharmacodynamics:

Temlisartan is an Angiotensin 2 receptor Antagonist.It is used in the Management of Hypertension. Telmisartan is given by mouth after an oral dose after an oral dose the hypotensive effect peaks with in 3 hrs persist for at least for 24 hrs the maximum hypotensive effect occurs within 4 to 8 weeks after starting therapy. In Hypertension telmisartan is given in an initial dose of 40mg once daily. This may be increased if necessary to a maximum dose of 80mg once daily. Lower doses should be considered in patients with hepatic or renal impairment.

4.2.4 Drug Interaction:

Telmisartan can increase blood concentrations of digoxin (lanoxin).Medications which interfere with the Angiotensin converting enzyme system such as Telmisartan have been found to cause fetal and neonatal toxicity and death when taken by pregnant women. In the case of pregnancy they should discontinue use of Telmisartan.

-In Nursing Mothers should discontinue.

4.2.5 Side Effects:

Head Ache


Back pain



4.2.6 Dosage and Administration:

Administered Orally

20-80 mg daily in hypertension

80 mg daily for cardiovascular reduction