PRESIN

COMPOSITION:

Presin-2.5:

Each film coated tablet contains: Amlodipine Besylate IP equivalent to Amlodipine 2.5 mg

Presin-5:

Each film coated tablet contains: Amlodipine Besylate IP equivalent to Amlodipine 5 mg

Presin-10:

Each film coated tablet contains: Amlodipine Besylate IP equivalent to Amlodipine 10 mg

CLINICAL PHARMACOLOGY:

Mechanism of Action: 

Amlodipine is a calcium channel blocker that primarily inhibits calcium influx into vascular smooth muscle, with a lesser effect on cardiac muscle.Amlodipine does not affect serum calcium levels and has minimal negative inotropic effects at therapeutic doses.

Pharmacokinetics 

Absorption: Amlodipine has 64%-90% bioavailability, 

Distribution: It reaches peak plasma concentration in 6-12 hours, is 93% plasma protein bound, 

Metabolism: It is metabolized in the liver,

Elimination: 30-50 hour half-life; renal impairment has no significant effect, while hepatic insufficiency and age may require dose adjustments

INDICATIONS AND USAGE: 

Amlodipine is used alone or in combination with other antihypertensive and antianginal agents to treat hypertension and coronary artery disease. It is indicated for chronic stable angina, vasospastic angina, and angiographically documented coronary artery disease in patients without heart failure or an ejection fraction < 40%

DOSAGE AND ADMINISTRATION:

Adults: The usual initial dose of Amlodipine Besylate is 5 mg once daily, with a maximum dose of 10 mg once daily. For elderly or patients with hepatic insufficiency, start with 2.5 mg once daily. The recommended dose for angina and coronary artery disease is 5–10 mg, with lower doses in elderly or those with hepatic insufficiency.

Children: The effective antihypertensive dose for children aged 6–17 years is 2.5 mg to 5 mg once daily, with no studies on doses exceeding 5 mg daily.

WARNINGS AND PRECAUTIONS: 

Warnings: 

Symptomatic hypotension may occur, especially in patients with severe aortic stenosis, but acute hypotension is unlikely due to the gradual onset of action. 

Precautions:

Caution is needed when increasing the dose in patients with severe obstructive coronary artery disease or hepatic impairment, as worsening angina, acute myocardial infarction, and the need for slow titration may arise.

ADVERSE REACTIONS:

Most common adverse reactions are headache and edema which occurred in a dose related manner. Other adverse experiences not dose related but reported with an incidence >1.0% are headache, fatigue, nausea, abdominal pain, and somnolence. 

DRUG INTERACTIONS:

Amlodipine may interact with other antihypertensive agents, leading to an enhanced blood pressure-lowering effect, and with medications like simvastatin, increasing the risk of muscle toxicity. Co-administration with CYP3A4 inhibitors (e.g., ketoconazole) can increase amlodipine levels, potentially enhancing side effects

USE IN SPECIFIC POPULATIONS:

Pregnancy: Category C. Amlodipine should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.

Nursing Mothers: It is not known whether Amlodipine is excreted in human milk. In the absence of this information, it is recommended that nursing be discontinued while Amlodipine Besylate tablet is administered.

Pediatric Use: Effect of Amlodipine on blood pressure in patients less than 6 years of age is not known.

Geriatric Use: Dosing at the low end of the dose range should be started, due to the greater frequency of decreased hepatic, renal, or cardiac function and of concomitant disease or other drug therapy. 

CONTRAINDICATIONS: 

Amlodipine Besylate tablets are contraindicated in patients with known sensitivity to Amlodipine 

OVERDOSAGE: 

Overdosage of amlodipine can lead to excessive peripheral vasodilation, marked hypotension, and possibly reflex tachycardia. Treatment involves cardiovascular support, including fluid administration, vasopressors if needed, and careful monitoring of cardiac and respiratory function 

STORAGE: 

Store below 30°C protected from light and moisture. 

PRESENTATION: 

Box containing 3 strips of 10 tablets for Presin 2.5 & Presin 10. 

Box containing 5 strips of 30 tablets for Presin 5.