DRUGS & SUPPLEMENTS

Atorvastatin

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Atorvastatin uses


Pharmacological action

Atorvastatin is a lipid-lowering drugs of the statin group. An inhibition of HMG-CoA reductase leads to a series of sequential reactions that result in reduced intracellular cholesterol content and it is a compensatory increase in activity of LDL receptors and thus accelerate the catabolism of LDL cholesterol.

The lipid-lowering effect of statins is associated with lower levels of total cholesterol by LDL-C. The reduction in LDL cholesterol is dose-dependent and is not linear, but exponential. The inhibitory effect of atorvastatin on HMG-CoA reductase by about 70% determined by the activity of its circulating metabolites.

Statins do not affect the activity of lipoprotein lipase and hepatic, no significant effect on the synthesis and catabolism of free fatty acids, so their effect on triglycerides and again vicariously through their main effects on reducing LDL-C.

In addition to lipid-lowering actions, statins have beneficial effects in endothelial dysfunction in the vascular wall, the state of atheroma, improves blood rheology, have antioxidant, antiproliferative properties.

Atorvastatin lowers cholesterol levels in patients with homozygous familial hypercholesterolemia, which is usually not amenable to therapy with lipid-lowering agents.

Pharmacokinetics

Atorvastatin is rapidly absorbed from the gastrointestinal tract. The absolute bioavailability is low (about 12%) due to first-pass clearance in gastrointestinal mucosa and / or due to the "first pass" through the liver, predominantly in the scene. Atorvastatin is metabolized with the participation of isoenzyme CYP3A4 to form a number of substances which are inhibitors of HMG-CoA reductase inhibitors.

T1/2 from plasma is about 14 hours, although the T1/2 inhibitor activity of HMG-CoA reductase is approximately 20-30 hours, due to the involvement of active metabolites.

The plasma protein binding is 98%.

Atorvastatin is excreted in the form of metabolites mainly in the bile.

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Why is Atorvastatin prescribed?

Primary hypercholesterolemia in ineffectiveness of diet, combined hypercholesterolemia and hypertriglyceridemia, heterozygous and homozygous familial hypercholesterolemia with the ineffectiveness of diet.

Dosage and administration

The treatment by Atorvastatin is with a standard diet for patients with hypercholesterolemia. The dose is determined individually, depending on the initial cholesterol levels. This medication is taken orally. The initial dose is usually 10 mg 1 time / day. The effect is manifested within 2 weeks, and the maximum effect is for 4 weeks. If necessary, the dose can be gradually increased every 4 weeks or more. The maximum daily dose is 80 mg.

Atorvastatin side effects, adverse reactions

Digestive system: constipation, flatulence, dyspepsia, abdominal pain, nausea, diarrhea.

CNS and peripheral nervous system: headache, insomnia.

Other: asthenia, myalgia.

Atorvastatin contraindications

Liver disease in the active phase, increasing the serum transaminase activity more than 3 times of unknown origin, pregnancy, lactation, hypersensitivity to atorvastatin. Women of reproductive age not using reliable contraception.

Using during pregnancy and breastfeeding

Atorvastatin is contraindicated during pregnancy and lactation (breastfeeding).

It is not known whether atorvastatin is allocated in breast milk. Given the potential for adverse effects in infants, if necessary to use this drug during lactation it should decide on the termination of breastfeeding.

Women of reproductive age during treatment should use adequate contraceptive methods. Atorvastatin may be used in women of childbearing age only if the probability of pregnancy is very low, and the patient informed about the possible risk of treatment for the fetus.

Category of the fetus by FDA - X.

Special instructions

Prior to and during treatment with atorvastatin, especially if symptoms of liver damage, it is necessary to monitor liver function tests. With an increase in transaminase levels it should be monitored their activity up to normalization. If AST or ALT more than 3 times the norm persists, we recommend reducing the dose or withdrawal of atorvastatin.

When prompted during the treatment of symptoms of myopathy it should determine the activity of creatine kinase. If a significant increase in CK levels is preserved, it is recommended to reduce the dose of Atorvastatin or to cancel taking it.

The risk of myopathy during the treatment with atorvastatin increased, while the use of cyclosporine, fibrates, erythromycin, antifungal agents belonging to azoles, and niacin.

There is a likelihood of the following side effects, but not in all cases, a clear link with taking atorvastatin: muscle cramps, myositis, myopathy, paresthesia, peripheral neuropathy, pancreatitis, hepatitis, cholestatic jaundice, anorexia, vomiting, alopecia, pruritus, rash, impotence, hyperglycemia and hypoglycemia.

The children experience of atorvastatin using at a dose of 80 mg / day is restricted.

With careful use Atorvastatin in patients with chronic alcoholism.

Atorvastatin drug interactions

When this drug applied simultaneously with:

- digoxin slightly increased concentration of digoxin in plasma.

- itraconazole greatly increases the concentration of atorvastatin in plasma, apparently due to inhibition of itraconazole its metabolism in the liver that occurs with the participation of isoenzyme CYP3A4; increased risk of myopathy.

- colestipol may decrease the concentration of atorvastatin in plasma, with lipid-lowering effect is enhanced.

- antacids containing magnesium hydroxide and aluminum hydroxide, reduce the concentration of atorvastatin by approximately 35%.

- cyclosporine, fibrates, azole antifungals derivatives, nicotinic acid increases the risk of myopathy.

- erythromycin, clarithromycin moderately increased concentrations of atorvastatin in plasma, increases the risk of myopathy.

- ethinyl estradiol, norethisterone (norethindrone) slightly increases the concentration of ethinyl estradiol, norethisterone and (norethindrone) in blood plasma.

- protease inhibitors increases the concentration of Atorvastatin in plasma, as protease inhibitors are inhibitors of the CYP3A4 isoenzyme.

Diltiazem, verapamil, isradipine inhibit isoenzyme CYP3A4, which participates in the metabolism of Atorvastatin, so that while the use of these calcium channel blockers may increase the concentration of atorvastatin in plasma and increased risk of myopathy.

Atorvastatin in case of emergency / overdose

Treatment: symptomatic and supportive therapy. There is no specific antidote. Hemodialysis is ineffective.

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Atorvastatin pharmaceutical active ingredients containing related brand and generic drugs:

infoActive ingredient is the part of the drug or medicine which is biologically active. This portion of the drug is responsible for the main action of the drug which is intended to cure or reduce the symptom or disease. The other portions of the drug which are inactive are called excipients; there role is to act as vehicle or binder. In contrast to active ingredient, the inactive ingredient's role is not significant in the cure or treatment of the disease. There can be one or more active ingredients in a drug.


Atorvastatin available forms, composition, doses:

infoForm of the medicine is the form in which the medicine is marketed in the market, for example, a medicine X can be in the form of capsule or the form of chewable tablet or the form of tablet. Sometimes same medicine can be available as injection form. Each medicine cannot be in all forms but can be marketed in 1, 2, or 3 forms which the pharmaceutical company decided based on various background research results.
Composition is the list of ingredients which combinedly form a medicine. Both active ingredients and inactive ingredients form the composition. The active ingredient gives the desired therapeutic effect whereas the inactive ingredient helps in making the medicine stable.
Doses are various strengths of the medicine like 10mg, 20mg, 30mg and so on. Each medicine comes in various doses which is decided by the manufacturer, that is, pharmaceutical company. The dose is decided on the severity of the symptom or disease.

Price
Lipitor 10 mg tablet1.87 USD
Lipitor 20 mg tablet2.34 USD
Lipitor 40 mg tablet2.52 USD
Lipitor 80 mg tablet2.52 USD
Tablets, Film-Coated; Oral; Atorvastatin Calcium 10 mg
Tablets, Film-Coated; Oral; Atorvastatin Calcium 20 mg
Tablets, Film-Coated; Oral; Atorvastatin Calcium 40 mg
Tablets; Oral; Atorvastatin Calcium 10 mg
Tablets; Oral; Atorvastatin Calcium 20 mg
Tablets; Oral; Atorvastatin Calcium 40 mg
Tablets; Oral; Atorvastatin Calcium 80 mg

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Atorvastatin destination | category:

infoDestination is defined as the organism to which the drug or medicine is targeted. For most of the drugs what we discuss, human is the drug destination.
Drug category can be defined as major classification of the drug. For example, an antihistaminic or an antipyretic or anti anginal or pain killer, anti-inflammatory or so.


Atorvastatin Anatomical Therapeutic Chemical codes:

infoA medicine is classified depending on the organ or system it acts [Anatomical], based on what result it gives on what disease, symptom [Therapeutical], based on chemical composition [Chemical]. It is called as ATC code. The code is based on Active ingredients of the medicine. A medicine can have different codes as sometimes it acts on different organs for different indications. Same way, different brands with same active ingredients and same indications can have same ATC code.


Atorvastatin pharmaceutical companies:

infoPharmaceutical companies are drug manufacturing companies that help in complete development of the drug from the background research to formation, clinical trials, release of the drug into the market and marketing of the drug.
Researchers are the persons who are responsible for the scientific research and is responsible for all the background clinical trials that resulted in the development of the drug.


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References

  1. Dailymed."LIPITOR (ATORVASTATIN CALCIUM) TABLET, FILM COATED [LAKE ERIE MEDICAL & SURGICAL SUPPLY DBA QUALITY CARE PRODUCTS LLC]". https://dailymed.nlm.nih.gov/dailym... (accessed August 28, 2018).
  2. Dailymed."AMLODIPINE BESYLATE; ATORVASTATIN CALCIUM: DailyMed provides trustworthy information about marketed drugs in the United States. DailyMed is the official provider of FDA label information (package inserts).". https://dailymed.nlm.nih.gov/dailym... (accessed August 28, 2018).
  3. "atorvastatin". https://pubchem.ncbi.nlm.nih.gov/co... (accessed August 28, 2018).

Frequently asked Questions

Can i drive or operate heavy machine after consuming Atorvastatin?

Depending on the reaction of the Atorvastatin after taken, if you are feeling dizziness, drowsiness or any weakness as a reaction on your body, Then consider Atorvastatin not safe to drive or operate heavy machine after consumption. Meaning that, do not drive or operate heavy duty machines after taking the capsule if the capsule has a strange reaction on your body like dizziness, drowsiness. As prescribed by a pharmacist, it is dangerous to take alcohol while taking medicines as it exposed patients to drowsiness and health risk. Please take note of such effect most especially when taking Primosa capsule. It's advisable to consult your doctor on time for a proper recommendation and medical consultations.

Is Atorvastatin addictive or habit forming?

Medicines are not designed with the mind of creating an addiction or abuse on the health of the users. Addictive Medicine is categorically called Controlled substances by the government. For instance, Schedule H or X in India and schedule II-V in the US are controlled substances.

Please consult the medicine instruction manual on how to use and ensure it is not a controlled substance.In conclusion, self medication is a killer to your health. Consult your doctor for a proper prescription, recommendation, and guidiance.

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Review

sDrugs.com conducted a study on Atorvastatin, and the result of the survey is set out below. It is noteworthy that the product of the survey is based on the perception and impressions of the visitors of the website as well as the views of Atorvastatin consumers. We, as a result of this, advice that you do not base your therapeutic or medical decisions on this result, but rather consult your certified medical experts for their recommendations.

Visitor reports

One visitor reported useful

How is the drug Atorvastatin useful in reducing or relieving the symptoms? How useful is it?
According to the survey conducted by the website sDrugs.com, there are variable results and below are the percentages of the users that say the medicine is useful to them and that say it is not helping them much. It is not ideal to continue taking the medication if you feel it is not helping you much. Contact your healthcare provider to check if there is a need to change the medicine or if there is a need to re-evaluate your condition. The usefulness of the medicine may vary from patient to patient, depending on the other diseases he is suffering from and slightly depends on the brand name.
Visitors%
Useful1
100.0%

One visitor reported price estimates

What is your opinion about drug cost? Did you feel the cost is apt, or did you feel it is expensive?
The report given by the sDrugs.com website users shows the following figures about several people who felt the medicine Atorvastatin is expensive, and the medicine is not expensive. The results are mixed. The perception of the cost of the medicine to be expensive or not depends on the brand name of the medicine, country, and place where it is sold, and the affordability of the patient. You can choose a generic drug in the place of the branded drug to save the cost. The efficiency of the medicine will not vary if it is generic or a branded one.
Visitors%
Not expensive1
100.0%

One visitor reported frequency of use

How often in a day do you take the medicine?
Are you taking the Atorvastatin drug as prescribed by the doctor?

Few medications can be taken Twice in a day more than prescribed when the doctor's advice mentions the medicine can be taken according to frequency or severity of symptoms. Most times, be very careful and clear about the number of times you are taking the medication. The report of sDrugs.com website users about the frequency of taking the drug Atorvastatin is mentioned below.
Visitors%
Twice in a day1
100.0%

Three visitors reported doses

What is the dose of Atorvastatin drug you are taking?
According to the survey conducted among sDrugs.com website users, the maximum number of people are using the following dose 51-100mg. Few medications come in only one or two doses. Few are specific for adult dose and child dose. The dose of the medicine given to the patient depends on the severity of the symptom/disease. There can be dose adjustments made by the doctor, based on the progression of the disease. Follow-up is important.
Visitors%
51-100mg2
66.7%
11-50mg1
33.3%

Four visitors reported age

Visitors%
> 602
50.0%
46-601
25.0%
30-451
25.0%

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The information was verified by Dr. Arunabha Ray, MD Pharmacology

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