Simvastatin + Ezetimibe Pharmacology

Simvastatin + Ezetimibe

About Simvastatin + Ezetimibe
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Mechanism of Action of Simvastatin + Ezetimibe
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Pharmacokinets of Simvastatin + Ezetimibe
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Onset of Action for Simvastatin + Ezetimibe
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Duration of Action for Simvastatin + Ezetimibe
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Half Life of Simvastatin + Ezetimibe
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Side Effects of Simvastatin + Ezetimibe
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Contra-indications of Simvastatin + Ezetimibe
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Special Precautions while taking Simvastatin + Ezetimibe
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Pregnancy Related Information
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Old Age Related Information
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Breast Feeding Related Information
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Children Related Information
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Indications for Simvastatin + Ezetimibe
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Interactions for Simvastatin + Ezetimibe
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Typical Dosage for Simvastatin + Ezetimibe
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Schedule of Simvastatin + Ezetimibe
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Storage Requirements for Simvastatin + Ezetimibe
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Effects of Missed Dosage of Simvastatin + Ezetimibe
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Effects of Overdose of Simvastatin + Ezetimibe
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Simvastatin

About Simvastatin
Statins, HMG-CoA reductase inhibitor, A hypolipidemic agent.
Mechanism of Action of Simvastatin
It is a precursor lactone converted in to active form in the body which competitively inhibits the conversion of 3-hydroxy-3-methyl glutaryl coenzyme A (HMG CoA) to mevalonate. The drug exerts it`s action by specific inhibition of enzyme; 3-hydroxy-3-methyl glutaryl coenzyme A reductase (HMG CoA reductase) and reduces cholesterol synthesis up to 50% at therapeutic doses. This results in compensatory increase in low density lipoprotein (LDL) receptor expression in liver which ultimately leads to increased receptor mediated uptake and catabolism of intermediate density lipoprotein(IDL) and low density lipoprotein (LDL). It causes dose dependent lowering of LDL cholesterol and reduces hepatic synthesis of very low density lipoprotein (VLDL) and lowers plasma triglyceride levels. It increases high density lipoprotein (HDL) levels than other statins.
Pharmacokinets of Simvastatin
Absorption: Readily absorbed orally but extensive fist pass hepatic metabolism limits bioavailability, Distribution: Distributed mainly to liver in a highly protein bound form and less than 5%of an oral dose reaches systemic circulation, Metabolism: Metabolized in liver in to active metabolite, Excretion: Excreted mainly through bile.
Onset of Action for Simvastatin
Significant response seen after 1 to 2 weeks maximum therapeutic response seen after 4 to 6 weeks.
Duration of Action for Simvastatin
N/A
Half Life of Simvastatin
3 hours
Side Effects of Simvastatin
1.Headache
2.Dizziness
3.Abdominal discomfort
4.Heart burn
5.Abdominal pain
6.Nausea
7.Dyspepsia
8.Flatulence
9.Constipation
10.Blurred vision
11.Abnormal liver function tests
12.Rash
13.Pruritus
14.Fatigue
15.Myopathy
16. Upper respiratory tract infections


Contra-indications of Simvastatin
1.Hypersensitivity to the drug
2.Active liver diseases
3.Persistent elevation of serum transaminase levels
Special Precautions while taking Simvastatin
1.Renal impairment
2.History of liver diseases
3.Alcoholics
Pregnancy Related Information
Contraindicated
Old Age Related Information
Use with caution
Breast Feeding Related Information
Contraindicated
Children Related Information
Contraindicated
Indications for Simvastatin
1.Hypercholesterolemia(types IIa, IIb)
2.Hypercholesterolemia along with hypertriglyceridemia)
Interactions for Simvastatin
Cyclosporine, erythromycin, niacin, gemfibrozil: Severe myopathy or rhabdomyolysis.
Propranolol: Decrease in antihyperlipidaemic activity.
Itraconazole: Plasma levels of lovastatin increased 20-fold.
Warfarin: Anticoagulant effect increased, chances of bleeding.
Typical Dosage for Simvastatin
Oral:
Starts with 5 to 10mg once daily; with evening meals. Increased if required based on patients response at every four weeks.
Maximum dose: 40mg

Schedule of Simvastatin
H
Storage Requirements for Simvastatin
Store at room temperature at a range of 15 to 25 degree C.
Effects of Missed Dosage of Simvastatin
Take the missed dose as soon as noticed and if it is the time for next dose then skip the missed dose. Continue the regular schedule. Do not double the dose.



Effects of Overdose of Simvastatin
Provide supportive care and symptomatic treatment.

Ezetimibe

About Ezetimibe
Cholesterol Absorption Inhibitor, 2-Azetidinone derivative, Hypolipidemic agent.
Mechanism of Action of Ezetimibe
It reduces the absorption of cholesterol from the intestine by localising at the brush border of the small intestine, where it inhibits the absorption of cholesterol from the diet. Specifically, it appears to bind to the Niemann-Pick C1-Like 1 (NPC1L1) protein on the gastrointestinal tract epithelium, a critical mediator of cholesterol absorption. This decreased cholesterol absorption leads to an increase in LDL-cholesterol uptake into cells, thus decreasing levels in the blood plasma.
Pharmacokinets of Ezetimibe
Absorption- Poorly absorbed after oral administration
Distribution- Widely distributed in the body as plasma protein binding form (>90%)
Metabolism- Metabolized in the liver and intestinal wall
Excretion- Excreted through urine and feces

Onset of Action for Ezetimibe
N/A
Duration of Action for Ezetimibe
N/A
Half Life of Ezetimibe
19-30 hours
Side Effects of Ezetimibe
1. Difficulty breathing
2. Closing of the throat
3. Swelling of the lips, tongue, or face
4. Abdominal pain
5. Diarrhea
6. Tiredness
7. Headache
8. Dizziness
9. Sore throat
10. Runny nose
11. Sneezing
12. Joint pain
13. Rash
14. Itching.
15. Hoarseness
16. Upset stomach
17. Unusual bleeding or bruising
18. Loss of appetite
19. Pain in the upper right part of the stomach
20. Yellowing of the skin or eyes
21. flu-like symptoms
22. Muscle pain or weakness
23. Fever
24. Chills
25. Pale or fatty stools
26. Chest pain
Contra-indications of Ezetimibe
Contraindicated in patients with hypersensitivity to the drug or any components of it
Special Precautions while taking Ezetimibe
1. Liver disease
2. Liver enzymes, persistently high levels
3. Major surgery or serious illness
4. Diabetes mellitus
5. Kidney disease
Pregnancy Related Information
Use with caution
Old Age Related Information
Use with caution
Breast Feeding Related Information
Contraindicated
Children Related Information
Use with caution
Indications for Ezetimibe
1. Adjunct to dietary measures and statin in primary and homozygous familial hypercholesterolaemia
2. Adjunct to dietary measures in homozygous familial sitosterolaemia
Interactions for Ezetimibe
Cyclosporin: Plasma concentraction of ezetimibe increased. Lipid-regulating drugs: Avoid concomitant use with fibrates.
Typical Dosage for Ezetimibe
Oral-
Adult -10 mg/day
Schedule of Ezetimibe
N/A
Storage Requirements for Ezetimibe
Stored at room temperature (15-30 degree C).
Effects of Missed Dosage of Ezetimibe
Take the missed dose as soon as noticed and if it is the time for next dose then skip the missed dose. Continue the regular schedule. Do not double the dose.
Effects of Overdose of Ezetimibe
Give symptomatic and supportive treatment

Home Delivery for Simvastatin + Ezetimibe in Your City

Medicine India is just a publishing medium for medicine related information and does not provide services or sales of medicines including simvastatin + ezetimibe.

However, we do publish a comprehensive directory of Pharmacies, Chemists and Druggists in cities all over India. You can use this directory to find the medicine stores in your city (or area) that provide home delivery services for simvastatin + ezetimibe and other medicines and health products. Home delivery services for simvastatin + ezetimibe may be free or they may cost you depending on the pharmacy and the minimum order requirements. It would be best to get this clarified while placing the order.

Please be aware that you should take simvastatin + ezetimibe only if a doctor has recommended or prescribed it. Some or all pharmacies who provide a home delivery service for medicines might insist on a prescription for simvastatin + ezetimibe before they complete the sale. You can get this information while placing the order for simvastatin + ezetimibe with the pharmacy.

Simvastatin + Ezetimibe is a generic medicine name and there are several brands available for it. Some of the brands for simvastatin + ezetimibe might be better known than simvastatin + ezetimibe itself. If the pharmacy that's willing to deliver medicines to your home doesn't have simvastatin + ezetimibe in stock, you can ask for one of the branded alternatives for simvastatin + ezetimibe.