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- Pharmacology For Lercanidipine + Atenolol
Lercanidipine + Atenolol Pharmacology
Lercanidipine + AtenololAbout Lercanidipine + AtenololN/AMechanism of Action of Lercanidipine + AtenololN/APharmacokinets of Lercanidipine + AtenololN/AOnset of Action for Lercanidipine + AtenololN/ADuration of Action for Lercanidipine + AtenololN/AHalf Life of Lercanidipine + AtenololN/ASide Effects of Lercanidipine + AtenololN/AContra-indications of Lercanidipine + AtenololN/ASpecial Precautions while taking Lercanidipine + AtenololN/APregnancy Related InformationContraindicatedOld Age Related InformationUse with cautionBreast Feeding Related InformationContraindicatedChildren Related InformationContraindicatedIndications for Lercanidipine + AtenololHypertensionInteractions for Lercanidipine + AtenololN/ATypical Dosage for Lercanidipine + AtenololN/ASchedule of Lercanidipine + AtenololN/AStorage Requirements for Lercanidipine + AtenololN/AEffects of Missed Dosage of Lercanidipine + AtenololN/AEffects of Overdose of Lercanidipine + AtenololN/A
LercanidipineAbout LercanidipineA selective calcium channel blocker, dihydropyridine derivative, Antihypertensive.Mechanism of Action of LercanidipineLercanidipine is a vasoselective long acting dihydropyridine Ca2+ channel blocker. It exerts antihypertensive actions through blocking the influx of Ca ions through voltage gated L-type Ca channels to the vascular smooth muscle cells, Coronary smooth muscle cells and to the myocardial cells. It has greater effects on vascular smooth muscles than cardiac muscles. Thus causes dilatation of vascular endothelium, decrease total peripheral resistance, and decreases both systolic and diastolic BP. It possesses anti atherosclerogenic action. As a coronary vasodilator it improves coronary blood flow.Pharmacokinets of LercanidipineAbsorption: Well absorbed orally, bioavailability is reduced due to first pass metabolism.
Distribution: Widely distributed in a protein bound form.
Metabolism: Metabolized in liver in to inactive metabolites.
Excretion: Excreted through urine and faeces.
Onset of Action for LercanidipineN/ADuration of Action for LercanidipineN/AHalf Life of LercanidipineN/ASide Effects of Lercanidipine1. Flushing
12. Gastrointestinal disturbances
15. Abdominal pain
Contra-indications of Lercanidipine1. Acute myocardial infarction
2. Heart failure
3. Aortic stenosis
4. Hypersensitivity to the drug
5. Severe hepatic and renal impairment
Special Precautions while taking Lercanidipine1.Cardiovascular disorders: Use cautiously in cardiovascular disorders such as congestive heart failure, cardiovascular insufficiency, hypotension, Ischaemic heart diseases, Left ventricular outflow obstruction, Sick sinus syndrome, Unstable angina etc.
2. Hepatic impairment
3. Renal impairment
1. Slowly withdraw the drug with caution
2. Avoid alcohol use during therapy
3. Use cautiously along with other antihypertensive drugs
Pregnancy Related InformationContraindicatedOld Age Related InformationContraindicatedBreast Feeding Related InformationContraindicatedChildren Related InformationContraindicatedIndications for Lercanidipine1. HypertensionInteractions for LercanidipineAvoid grapefruit juice as it may affect metabolism.
Histamine H2 antagonists: Cimetidine and ranitidine enhance the bioavailability of lercanidipine.
Beta blockers: Though advantageous in some, concomitant use results in increased adverse effects like bradycardia and conduction disturbances.
Digitalis Glycosides: Increased serum digoxin levels with possible toxicity.
Magnesium Sulphate: With parenteral magnesium suplhate neuromuscular blockade and hypotension may occur.
Theophyllines: Increased pharmacological effects of theophylline, resulting in toxicity.
Quinidine: Hypotension, bradycardia, ventricular tachycardia, AV block and pulmonary oedema may occur. Serum quinidine levels may also be decreased by lercanidipine.
Anticoagulants: Increased prothrombin time.
Fentanyl: Severe hypotension or increased fluid requirements.
Typical Dosage for Lercanidipine10mg once daily; 15minutes before meals. Gradually increased at 2week intervals up to 20mg if required depending up on the patient`s response..Schedule of LercanidipineHStorage Requirements for LercanidipineStore at room temperature below 30 degree C. Protect from moisture and light.Effects of Missed Dosage of LercanidipineTake the missed dose as soon as remember and If it is the time for next dose then skip the missed dose and take the regular dose.Effects of Overdose of LercanidipineMonitor &support cardiac and respiratory functions. Measure the BP. Give cardiovascular support by elevating the limbs and maintaining fluid balance. Administer vasopressers like nor epinephrine if required.
AtenololAbout AtenololCardioselective Beta(Beta1 )-adrenergic blocking agent, Antihypertensive,anti anginal.Mechanism of Action of AtenololAtenolol is a cardio selective beta-1 adrenergic antagonist. It has negative chronotropic and negative inotropic effects on heart. It decreases oxygen consumption; cardiac work and aortic pressure. It decreases nor adrenaline and renin releases. It decreases central sympathetic out flow In sympathetic over activity, it prolongs systole by retarding conduction. It increases oxygen supply and exercise tolerance in angina patients. The drug decreases BP in hypertensive individuals; both systolic and diastolic BP is reduced.
Antimigraine action: Atenolol is useful in migraine due to its beta blockade action. Through beta blockade action it inhibits vasodilation and relieves migraine.
Pharmacokinets of AtenololAbsorption: Absorbed orally up to 60%, Distribution: Widely distributed but no CSF penetration Metabolism: A small portion is metabolized in liver. Excretion: Excreted mainly through urine. Remaining portion is excreted through faeces.Onset of Action for Atenolol1hourDuration of Action for AtenololBelow 1dayHalf Life of Atenolol6 - 7 hoursSide Effects of Atenolol1.Heart failure
15.Changes in kidney function tests
16.Changes in liver function tests.
Contra-indications of Atenolol1.Hypersensitivity to the drug
2.Second or third degree heart block
Special Precautions while taking Atenolol1.Congestive heart failure
4.The drug should be gradually withdraw with caution
Pregnancy Related InformationContraindicatedOld Age Related InformationUse with cautionBreast Feeding Related InformationContraindicatedChildren Related InformationUse with cautionIndications for Atenolol1.Hypertension
4.Migraine prophylaxisInteractions for AtenololAlcohol, Anaesthetics, Antidepressants, Anxiolytics, Hypnotics, Cimetidine, Diuretics: Enhanced hypotensive effect.
Analgesics: NSAIDs antagonise hypotensive effect.
Antibacterials (Rifampicin): Reduce plasma concentration of atenolol.
Antidiabetics: Enhanced hypoglycemic effect.
Antihypertensives: Enhanced hypotensive effect, with clonidine there is increased severity of rebound hypertension.
Calcium channel Blockers: increased risk of bradycardia and AV block with diltiazem, severe hypotension and heart failure with verapamil, nifedipine
Cardiac glycosides: Increased AV block and bradycardia.
Cholinergics: Effects antagonised by atenolol.
Corticosteroids: Antagonism of hypotensive effect.
Ergotamine: Increased peripheral vasoconstriction
Sympathomimetics: Severe hypertension with adrenaline and noradrenaline.
Lab. Tests: Interferes with Glucose or insulin tolerence tests.Typical Dosage for AtenololHypertension: Starts with 50mg single dose then gradually increases at weekly intervals to 100mg/day once daily based on patient`s response.
Children: 1 to 1.3 mg/kg/day once daily or as two divided doses
Angina: Starts with 50mg single dose orally, and then gradually increases to 100mg/day based on patient`s response at one week intervals
Maximum dose: 200mg/day
Myocardial infarction: 5mg I.V. over 5minuts twice daily at 10minuts intervals. Then after 10minuts starts oral therapy with 50mg dose. Then 50mg at 12th hour. And increases to 100mg/day once daily or in two divided doses up to 9days
Migraine prophylaxis: 50 - 150mg / day in divided doses
Schedule of AtenololHStorage Requirements for AtenololStore at room temperature and protect from heat, moisture, and direct sunlightEffects of Missed Dosage of AtenololTake 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 AtenololTreatment is supportive and symptomatic. After ingestion empty the stomach by induced emesis or gastric lavage. Administer activated charcoal to reduce absorption
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