WHAT IS ATORVASTATIN
A synthetic HMG-CoA reductase inhibitor atorvastatin reduces the level of plasma cholesterol by suppressing endogenous cholesterol synthesis. Atorvastatin 10 mg is lipid-lowering used in the treatment of primary, secondary and tertiary protection of coronary heart disease. 3-hydroxy-3-methylglutaryl-coenzyme reductase is completely inhibited with the assistance of statins. Statins mitigate the cholesterol production in the liver by protecting the transformation of HMG-CoA to mevalonate. Atorvastatin also accelerates the proportion of LDL receptors on the surface of hepatic cells. One study was performed which depicted that reduction based on dose in total cholesterol level, low density lipoprotein (LDL)-cholesterol and triglyceride levels have been reflected with atorvastatin in person who is suffering from hypercholesterolemia as well as hypertriglyceridemia.
ENLIST THE PHYSICAL CHARACTERISTICS OF ATORVASTATIN
Physical Profile | Descriptions |
Molecular Formula | C33H34FN2O5 |
IUPAC Name | 7-[2-(4-fluorophenyl)-3-phenyl-4-(phenylcarbamoyl)-5-(propan-2-yl)-1H-pyrrol-1-yl]-3,5-dihydroxyheptanoate |
Molecular Mass | 557.632 g/mol |
Density | 1.03 g/ml g/cm3 |
Boiling point | 722ºC at 760 mmHg |
Melting point | 176°C |
State | Solid |
Solubility | Practically Insoluble in water |
EXPLICATE FEW PHARMACODYNAMIC ASPECTS OF ATORVASTATIN
Like other members of its class, Atorvastatin inhibits the action of HMG-CoA reductase which prevents the formation of mevalonic acid, the same as members of its group.
Reduced concentration of intracellular cholesterol causes an elevation in the number of low-density lipoprotein (LDL) receptors and an increase in the removal of LDL cholesterol from plasma.
With the reduction of LDL and VLDL cholesterol in the liver, HMG-CoA reductase inhibitors have the potential to reduce plasma cholesterol levels as well. At 73 nmoI/L, atorvastatin suppresses the production of cholesterol in the human liver-derived cell line Hep-G2 by 50%.
Patients with heterozygous familial hypercholesterolemia experience the 59% reduction in fasting plasma mevalonic acid levels after taking atorvastatin 80 mg per day.
Hypertriglyceridemia patients taking atorvastatin either 10 or 80 mg/day for 4 weeks benefit from considerable reductions in plasma levels of total triglycerides, cholesterol and apolipoprotein B, C-II, C-III and E.
HOW ATORVASTATIN WORK IN RECTIFYING THE DISEASE IN HUMAN BODY
3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase exclusively inhibits Atorvastatin. A group of Statins drugs decrease the production of cholesterol in the liver by inhibiting HMG-CoA conversion to mevalonate. Atorvastatin also increases the number of LDL receptors on the surface of hepatic cells with the help of this drug. In various researches the effects of atorvastatin on patients have been demonstrated with heterozygous or homozygous familial hypercholesterolemia, mixed dyslipidemia, isolated hypertriglyceridemia, and nonfamilial hypercholesterolemia. This has been shown that to lower intermediate-density lipoprotein (IDL-C) in individuals with dysbetalipoproteinemia statins are widely used.
SHEDDING LITTLE LIGHT TOWARDS THE ADME OF ATORSTATIN
Absorption
This is instantly absorbed after p.o. administration with a peak plasma concentration at 1 to 2 hours additionally its bioavailability is low at 14% due to high first-pass metabolism.
Distribution
It has a volume of distribution of about 380 liters and is highly bound towards plasma proteins.
Metabolism
It is metabolized with the aid of cytochrome P450 3A4 (CYP3A4) to activate the ortho- and para-hydroxylated metabolites.
Excretion
Elimination of Atorvastatin and its metabolites occur in bile and this is not entering in the enterohepatic circulation because this has a time span of 14 hours whereas its active metabolites have a half-life of about 20 to 30 hours.
EXPLICATE ABOUT THE DOSE DISTRIBUTION OF ATORVASTATIN IN DIFFERENT AGE GROUPS
Atorvastatin calcium tablet is available in different doses like 10, 20, 40 and 80 mg. This drug can be swallowed with or without a meal and should be taken at the same time every day. It is always prescribed to administer statins during bedtime because cholesterol production is rotating with the extreme production levels during fast as at night. Whereas, the longer time span of atorvastatin in the body in comparison with other shorter half-life statins (e.g., lovastatin, Fluvastatin and simvastatin) provide more flexibility regarding dosing times.
Adult Dosing
The intensity to decrease LDL-C can be utilized to evaluate the dosage or this can be altered to fulfill given lipid objectives. Depending on the benefit of statin, the American College of Cardiology/American Heart Association Guidelines prescribe either mild intensity (atorvastatin 10 to 20 mg) or high intensity (atorvastatin 40 to 80 mg) drug. More than 50% of High-intensity statins reduce LDL-C whereas moderate-intensity statins reduce LDL-C by around 30% to 50%.
Pediatrics
In case of heterozygous familial hypercholesterolemia dosage form of 20 mg do not have any clinical data while in the case of familial hypercholesterolemia dose upto 80 mg have been used in few ratio of juvenile patients.
Geriatrics
Plasma concentrations of atorvastatin may be high in patients older than 65 as compared to the young adults because older patients may be at high risk of statin-induced myopathies.
Renal Impairment
These metabolites do not experience renal elimination, therefore dose adjustments are required with reduced renal function.
Hepatic Impairment
In patients with chronic alcoholic liver disease the plasma concentration of the drug increased while in patients suffering with active liver disease the use of Atorvastatin is contraindicated.
DISCUSS FEW LINES ABOUT DRUG INTERACTIONS
CYP3A4 inhibitors collaborating with the atorvastatin may elevate the plasma concentrations as well worsen side effects including myopathy. OATP1B1 inhibitors have the ability to increase the bioavailability of drug additionally decreased plasma concentrations resulting from CYP3A4 inducers. The concentration of Digoxin, Norethindrone and ethinyl estradiol may proliferate in persons taking atorvastatin as a result, they should be closely watched.
STATE SOME COMPLICATIONS OCCUR WITH REGULAR USE OF ATORVASTATIN
Rthralgia
Dyspepsia
Diarrhea
Nausea
Nasopharyngitis
Insomnia
Urinary tract infection
Pain in the extremities
Muscle aches
Muscle tenderness
Muscle weakness
Developing diabetes mellitus
DECODING THE CONTRAINDICATION OF ATORVASTATIN
Patients with active liver illness are contraindicated for atorvastatin in the case of chronic liver conditions such as non-alcoholic fatty liver disease and hepatitis, the advantages of lipid-lowering treatment definitely exceed the potential dangers. It is inadvisable to use atorvastatin when pregnant or in female patients who may become pregnant. Since this risk is greatest during the first trimester, it is now advised to stop taking statin medication at least three months before getting pregnant. If the patient becomes pregnant, they should stop using this drug right away. If a female patient is breastfeeding, she should also refrain from taking atorvastatin. Patients should be instructed to stop nursing if they need to start statin treatment.
WHAT ARE SOME SAFETY MEASURES WHILE TAKING A DOSE OF ATORVASTATIN
Swallow as suggested by your doctor and take this medicine by oral route once a day. It should always be taken one hour before or two hours after a meal
The dose should be decided on the basis of age, age-related side effects, and medical condition other than response to therapy.
Make sure your pharmacist and doctor are aware of everything you use, including over-the-counter, prescription and herbal medications.
Before each dosage, provide the bottle a good shake. Use a specific measuring spoon to accurately measure the dosage carefully.
This medication's adverse effects may be increased by grapefruit. To learn more, speak with your pharmacist or physician and If your doctor or pharmacist thinks it's safe for you to eat or drink grapefruit juice while taking this medicine, then avoid doing so.
IMPROVING THE RESULTS OF HEALTHCARE TEAMS WITH RESPECT TO ATORVASTATIN
Adherence to the treatment is pivotal for statins to effectively reduce the level of cholesterol or protect from heart related events in patients. Adverse effects such as the dearth of comprehension about the immense benefits of statin therapy along with the price are some obstacles to successful statin treatment therefore these issues may keep patients from taking these drugs as directed. The interprofessional team must also stress more towards how critical lifestyle adjustment is the key in the management of hyperlipidemia. This includes maintaining a balanced, healthful diet, doing regular exercise and controlling weight. The inclusion of a dietician or nutritionist to the medical team might be beneficial in assisting patients with the required dietary modifications.
Improved health may be attainable with more patient education and counseling on pharmaceutical advantages and patient concerns. To boom in the therapy, healthcare teams must interact across different boundaries. Person should get the first evaluation and recommendation about statin medication from the doctor's side. In addition to reporting to the prescriber or nurse, pharmacists can advise patients on the best way to take their medications (such as taking them before sleep) and look for drug interactions.
FREQUENTLY ASKED QUESTIONS ON ATORVASTATIN
Question1: Can I drink alcohol while taking this drug?
Yes, you can but in low quantities because drinking too much alcohol regularly elevates the chance of you having side effects and liver problems.
Question 2: What food does one person avoid while taking Atorvastatin?
It is recommended from the site that too much grapefruit juice when taking atorvastatin increases severe side effects. Additionally this also alters the mode of action of the drug and lastly the amount of drug in blood increases automatically which proves to be more hazardous in spite of curing.
Question 3 : Can lifestyle alteration affect the level of cholesterol?
Yes definitely, if you are able to change your lifestyle then no need to take or engulf statins. For Example: Maintenance of body weight, stop doing smoking, avoid junk food, doing exercise and avoid alcohol.
Question 4: Are statins safe?
Most people who use statins won't experience any adverse effects, and they are successful at decreasing cholesterol. If you have questions concerning the safety of statins, see your physician or pharmacist.
Question 5: What will happen if I stop taking it?
If you suspect negative effects from atorvastatin, you might wish to discontinue taking it. Consult your physician to determine whether the issue is a side effect of atorvastatin or something else entirely. It's possible that your doctor will advise you to change medications or reduce your dosage. However, your cholesterol may increase if you stop taking atorvastatin.
Question 6: Will taking Atorvastatin increase my risk of diabetes?
If you are obese, have high blood pressure and high blood sugar you are definitely more prone towards developing diabetes. There is evidence that atorvastatin may cause some individuals' blood sugar levels to rise. See your doctor if you have any concerns. They will be able to clarify how this slightly elevated risk is likely to be outweighed by the advantages of taking statins.