Atorvastatin + Clopidogrel + Aspirin Pharmacology

Atorvastatin + Clopidogrel + Aspirin

About Atorvastatin + Clopidogrel + Aspirin
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Mechanism of Action of Atorvastatin + Clopidogrel + Aspirin
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Pharmacokinets of Atorvastatin + Clopidogrel + Aspirin
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Onset of Action for Atorvastatin + Clopidogrel + Aspirin
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Duration of Action for Atorvastatin + Clopidogrel + Aspirin
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Half Life of Atorvastatin + Clopidogrel + Aspirin
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Side Effects of Atorvastatin + Clopidogrel + Aspirin
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Contra-indications of Atorvastatin + Clopidogrel + Aspirin
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Special Precautions while taking Atorvastatin + Clopidogrel + Aspirin
N/A
Pregnancy Related Information
Contraindicated
Old Age Related Information
Use with caution
Breast Feeding Related Information
Contraindicated
Children Related Information
N/A
Indications for Atorvastatin + Clopidogrel + Aspirin
1.Prophylaxis of ischaemic events.
2.Acute coronary syndrome.
3.Hypertention
Interactions for Atorvastatin + Clopidogrel + Aspirin
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Typical Dosage for Atorvastatin + Clopidogrel + Aspirin
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Schedule of Atorvastatin + Clopidogrel + Aspirin
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Storage Requirements for Atorvastatin + Clopidogrel + Aspirin
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Effects of Missed Dosage of Atorvastatin + Clopidogrel + Aspirin
N/A
Effects of Overdose of Atorvastatin + Clopidogrel + Aspirin
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Atorvastatin

About Atorvastatin
HMG-CoA Reductase Inhibitor, statins, Antilipemic agent.
Mechanism of Action of Atorvastatin
It is a more potent statin 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 also increases high density lipoprotein (HDL) levels. It also exerts antioxidant property.
Pharmacokinets of Atorvastatin
Absorption: Readily absorbed orally, Distribution: Widely distributed in a highly protein bound form, Metabolism: Metabolized in liver in to active metabolite, Excretion: Excreted mainly through bile.
Onset of Action for Atorvastatin
N/A
Duration of Action for Atorvastatin
N/A
Half Life of Atorvastatin
18 to 24 hours
Side Effects of Atorvastatin
1.Headache
2.Dizziness
3.Insomnia
4.Alopecia
5.Anorexia
6.Abdominal discomfort
7.Heart burn
8.Abdominal pain
9.Nausea
10.Dyspepsia
11.Flatulence
12.Constipation
13.Abnormal liver function tests
14.Rash
15.Pruritus
16.Fatigue
17.Myositis
18.Chest pain
19.Impotence
20.Myopathy
21.Upper respiratory tract infections

Contra-indications of Atorvastatin
1.Hypersensitivity to the drug
2.Active liver diseases
3.Persistent elevation of serum transaminase levels
Special Precautions while taking Atorvastatin

1.Monitor hepatic function tests and lipid levels before and periodically during therapy and stop drug if there is marked elevation of creatinine phosphokinase level
2.History of liver diseases
3.Alcoholics
4.In severe adverse effects and fever


Pregnancy Related Information
Contraindicated
Old Age Related Information
May be used
Breast Feeding Related Information
Contraindicated
Children Related Information
Use with caution
Below 9years: Contraindicated
Indications for Atorvastatin
1.Hypercholesterolemia
2.Combined hyperlipidaemia
Interactions for Atorvastatin
N/A
Typical Dosage for Atorvastatin
Oral:
Starts with 10mg once daily; Increased if required based on patients response.
Maximum dose: 80mg
Schedule of Atorvastatin
H
Storage Requirements for Atorvastatin
Store at room temperature at a range of 15 to 25 degree C.
Effects of Missed Dosage of Atorvastatin
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 Atorvastatin
Provide supportive care and symptomatic treatment.

Clopidogrel

About Clopidogrel
Thienopyridine class, Platelet Aggregation Inhibitor, Antithrombic, Anti platelet agent.
Mechanism of Action of Clopidogrel
The drug exerts it`s antithrombotic action by interfering with platelet aggregation. It alters surface receptors in platelets and inhibits ADP induced platelet-fibrinogen and platelet-platelet binding and prevents platelet aggregation. It blocks G-protein coupled P2YAC type of inhibitory purinergic receptors which mediates adenylyl cyclase inhibition by ADP. It prolongs bleeding time.
Pharmacokinets of Clopidogrel
Absorption: About 50% of drug is absorbed orally.Distribution: Widely distributed in the body in a protein bound form.Metabolism: Metabolized in liver. Excretion: About 50% is excreted through urine and 46% is excreted through faeces as metabolites.
Onset of Action for Clopidogrel
2hours
Duration of Action for Clopidogrel
5days
Half Life of Clopidogrel
8 hours
Side Effects of Clopidogrel
1.Diarrhoea
2.Vomiting
3.Nausea
4.Abdominal pain
5.Headache
6.Tinnitus
7.Rash
8.Pruritus
9.Haemorrhage
10.Neutropenia (rare)
11.Thrombocytopenia (are)
Contra-indications of Clopidogrel
1. Hypersensitivity to the drug
2. Haemorrhagic disorders
3. Intracranial haemorrhage
4. Gastrointestinal tract ulcer
Special Precautions while taking Clopidogrel
1.Haemopoetic disorders
2.Renal impairment
3.Hepatic impairment
4.Trauma
5. Recent surgery
Pregnancy Related Information
Contraindicated
Old Age Related Information
Use with caution
Breast Feeding Related Information
Contraindicated.
Children Related Information
Contraindicated
Indications for Clopidogrel
1. To reduce atherosclerotic events
2. Thrombotic disorders
3. Prevention of stroke
4. Prophylaxis of myocardial infarction
5. Peripheral vascular diseases
6. Coronary artery diseases.
Interactions for Clopidogrel
Asprin: Potentiates the effect of aspirin on collagen-induced platelet aggregation.
NSAIDs: Risk of increased occult gastrontestinal blood loss.
Phenytoin, tamoxifen, tolbutamide, warfarin, torsemide, fluvastatin: Since clopidogrel inhibits CYP4502C9 it may interfere with the metabolism of these drugs.
Typical Dosage for Clopidogrel
Oral: 75mg/day as single dose.
Schedule of Clopidogrel
N/A
Storage Requirements for Clopidogrel
Store at room temperature at a range of 15 to 30 degree C. Protect from excess heat and moisture
Effects of Missed Dosage of Clopidogrel
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 Clopidogrel
Provide supportive treatment. Platelet transfusion reverses the effects of the drug.

Aspirin

About Aspirin
Salicylate, Non narcotic analgesic, anti pyretic ,anti inflammatory.
Mechanism of Action of Aspirin
Aspirin has analgesic, anti-inflammatory and antipyretic action. Analgesic action: Central action: Aspirin acts on the Hypothalamus and inhibits the generation of pain impulses.
Peripheral action: It acts by inhibition of Prostaglandin (PGs) synthesis by blocking the activity of the precursor enzyme cyclo-oxygenase.
Anti-inflammatory action: It acts by inhibiting Prostaglandin (PGs) synthesis and their release at the site of injury. Prostaglandins cause tenderness and amplify the action of other algesics. Aspirin inhibits cyclo-oxygenase enzyme and antagonizes prostaglandin actions. It also inhibits other inflammatory mediators.
Antipyretic action: Aspirin lowers fever by affecting thermoregulation in the CNS and by inhibiting the action of prostaglandins peripherally. Aspirin inhibits the production of prostaglandin E1 which is the powerful pyretic agent.
Anticoagulant action: Aspirin inhibits the synthesis of Thromboxane A2 and Prostacyclin (PGI2). This leads to inhibition of platelet aggregation.
Pharmacokinets of Aspirin
Absorption: Aspirin is rapidly and completely absorbed after oral administration. Distribution: It is widely distributed in the body in protein bound form. Metabolism: It is completely metabolised in the liver. Excretion: Excreted in the urine.
Onset of Action for Aspirin
5-30 minutes
Duration of Action for Aspirin
1 - 4 hours
Half Life of Aspirin
15 - 20 minutes
Side Effects of Aspirin
1.Nausea,
2.Vomiting,
3.Diarrhoea,
4.Gastrointestinal bleeding,
5.Abdominal distress,
6.Dyspepsia,
7.Dizziness,
8.Blurred vision,
9.Tinnitus,
10.Rash,
11.Pruritis
12.Ototoxicity
Contra-indications of Aspirin
1.Hypersensitivity to Aspirin and other NSAIDs,
2.Peptic ulcer,
3.Bleeding disorders- Haemophilia, von Willebrand`s disease
4.Chicken pox and flu like syndrome in children
Special Precautions while taking Aspirin
1.Hepatic impairment
2.Renal impairment
3.Cardiovascular diseases- hypertension
4.Gastrointestinal diseases
5.Hypoprothrombinemia
6.Pre existing asthma
7.Patient on anticoagulant therapy
8.Diabetes


Pregnancy Related Information
Use with caution
3rd trimester: Contraindicated
Old Age Related Information
Use with caution
Breast Feeding Related Information
Use with caution.
Children Related Information
Use with caution
NEONATES: contraindicated
Indications for Aspirin
1.Rheumatoid arthritis,
2.Ankylosing spondylitis,
3.Acute gout,
4.Joint disorders e.g. inflammatory disease in joints, crystal deposition in the joints,
5.Osteoarthritis,
6.For the relief of fever, pain and inflammation in dental, minor surgery and orthopedic
7.Dysmenorrhoea,
8.Rheumatic fever
9. Juvenile arthritis
10.Migraine

Interactions for Aspirin
Drugs Affecting Aspirin:
Activated charcoal: Decreases absorption of aspirin.
Antacids Urinary alkalizers and Cortiosteroids: Decrease efficacy of aspirin.
Drugs affected by aspirin:
Alcohol: Risk of G.I. ulceration increases; may also prolong bleeding time.
ACE inhibitors: Antihypertensive action decreased.
Oral Anticoagulants : May potentiate effect.
Methotrexate: Effect potentiated.
Tetracycline: Efficacy decreased.
Tricyclic Antidepressants - Effect potentiated.
Nitroglycerin: May result in unexpected hypotension.
Beta-adrenergic Blockers - Antihypertensive effect blunted.
NSAIDs: May decrease serum concentration.
Sulfonylureas and Exogenous Insulin: In high doses may potentiate these drugs.
Valproic Acid: Potentiates effect.
Spironolactone: May inhibit diuretic effect.
Probenecid & Sulfinpyrazone : Antagonise uricosuric effect (In doses > 3gm/day - uricosuric effect)
Lab Tests:
Thyroid Function Tests: Increase in PBI
Serum Uric Acid Levels: Increased by levels less than 10 mg/dl and decreased by levels> 10 mg/dl.
Urine Glucose: False negative by glucose oxidase method. False positive results by reduction method.
Urinary Ketones: Produce reddish colour.
Typical Dosage for Aspirin
Adult:
Analgesic, antipyretic: 325 - 650mg 3 -4 times daily.
Anti-inflammatory, Arthritis: 3 g / day in divided doses increases the dose if needed.
Maintenance: 3.6 - 5.4 g / day in divided doses.
Rheumatic fever: 4.9 - 7.8 g / day in 3 - 4 divided doses for 1- 2 weeks
For prophylaxis of venous thromboembolism after total hip replacement: 650 mg twice a day started 1 day before surgery and continued for 2 weeks.
For other platelet aggregation inhibitory uses: 325 to 1300 mg daily according to individual needs.
For migraine: 300 - 600 mg to be taken at the first sign of migraine attack and repeated 4 - 6 hourly until suppress mild attacks.

Children:
Arthritis: 60 - 130 mg / kg body weight /day in divided doses
Anti-inflammatory: 60 - 125 mg / kg daily in 4 - 6 hours
Analgesic and Antipyretic: Adults: 1 to 2 tablets (325 to 650 mg) orally every 4 hours.
Children under 12: 10 to 15 mg/kg every 6 hours, not to exceed total daily dose of 2.4 g.
Schedule of Aspirin
N/A
Storage Requirements for Aspirin
N/A
Effects of Missed Dosage of Aspirin
N/A
Effects of Overdose of Aspirin
N/A

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