Amlodipine

BRAND NAMES:

This dosage is available as an oral suspension. It was given orally. This oral solution contains amlodipine at a concentration of 1mg/mL. This katerzia is used once a day at a dose of 5mg, with a maximum of 10mg. 

Norliqva – For the treatment of hypertension and coronary artery disease, the FDA has authorized this liquid amlodipine solution. The usual oral dosage for norliqva as an antihypertensive is 5 mg once daily, up to a maximum of 10 mg daily. 

•    Norvasc is available in oral tablets in doses of 2.5 mg, 5 mg, and 10 mg.

•    Amlodipine is also available in various combinations. 

•    Azor contains Amlodipine and Olmesartan.

•   Caduet contains Amlodipine and Atorvastatin.

•   Consensi contains Amlodipine and Celecoxib.

•   Exforge contains Amlodipine and Valsartan as the main active components.

•   Exforge HCT contains Amlodipine, Hydrochlorothiazide, and Valsartan. 

•   Lotrel has Amlodipine and Benzapril.

MECHANISM OF ACTION:

Amlodipine, a dihydropyridine calcium antagonist, blocks calcium ions from entering vascular smooth muscle and cardiac muscle. Experimental results show that amlodipine interacts with dihydropyridine and nondihydropyridine binding sites on cell membranes. Extracellular calcium ions enter cardiac and vascular smooth muscle via specific channels, causing contraction. Amlodipine specifically inhibits calcium ion influx through cell membranes. Amlodipine is more effectively excreted by vascular smooth muscle cells than cardiac muscle cells. Amlodipine's direct action on vascular smooth muscle lowers blood pressure. 

PHARMACOKINETICS:

Absorption: Amlodipine's absolute bioavailability ranges from 64% to 90%. Amlodipine's bioavailability is not altered by meals. Peak plasma concentrations are achieved within 6 to 12 hours. After 7 to 8 days of consistent amlodipine medication, plasma levels reverted to normal. Patients with liver dysfunction showed reduced amlodipine clearance rates. As a result, patients with liver illness have an increased area under the curve of 40% to 60%.

Distribution: The distribution volume of amlodipine is 21L/kg.

Metabolism: The liver extensively metabolizes amlodipine, producing inactive metabolites. Cytochrome P-450, CYP3A4, and CYP3A5 are all crucial in the metabolism of amlodipine.

Excretion: The terminal elimination half-life of amlodipine, which ranges from 30 to 50 hours, is biphasic and rises with hepatic impairment. 10% of the parent drug and 60% of its metabolites are excreted in urine, with the kidneys handling the bulk capacity of the drug's removal.

PHARMACODYNAMICS:

In clinical trials, chronic oral administration of amlodipine did not cause clinically meaningful changes in heart rate or blood pressure in patients with angina and normal blood pressure levels. Long-term, daily oral dosing maintains antihypertensive efficacy for at least 24 hours—patients who received amlodipine with beta-blockers achieved similar results. In clinical trials in which amlodipine was given in combination with beta-blockers to patients with hypertension or angina, no detrimental effects on electrocardiographic parameters were seen. Amlodipine did not affect electrocardiographic intervals or cause significant AV block in clinical investigations including only angina patients.

DOSAGE AND ADMINISTRATION:

Amlodipine is available as Katerzia, Norliqva, Norvasc, and generic amlodipine in the following dosage forms that are taken by mouth

Amlodipine 5mg, 10 mg, and 2.5 mg tablets –Norvasac

                     1mg/ml solution-Norliqva

                     1 mg/ml oral suspension- Katerzia

Amlodipine is generally taken orally and comes in 2.5, 5, and 10 mg tablets. Suspensions created from oral pills are offered to youngsters and the elderly who have difficulty swallowing. Compared to nifedipine and other dihydropyridine medications, amlodipine has the longest half-life, lasting 30 to 50 hours. The benefit of having a long half-life is that it only needs to be taken periodically.

CONTRAINDICATIONS:

Amlodipine is contraindicated in patients who have a known hypersensitivity to the drug or any of its components. Lymphocyte transformation tests can be performed to determine medication allergy.

DRUG INTERACTIONS:

Amlodipine can interact with a variety of other drugs. Different combinations can have a variety of consequences. For example, some can impair a drug's effectiveness, while others can exacerbate negative effects. 

•   Diltiazem is used to treat heart conditions. 

•   Antifungal: ketoconazole, itraconazole, voriconazole 

•   Simvastatin is a medication often used to treat excessive cholesterol levels in the blood and minimize the risk of heart disease. 

•   Cyclosporine works to suppress the immunological system. 

SIDE EFFECTS:

In addition to its necessary effects, a drug may cause certain undesired effects. 

• swelling of the ankles or feet 

• Chest tightness. 

• Having trouble breathing 

• Dizziness 

• Fast heartbeat or pulse. 

• Redness on the face, neck, and arms

OVERDOSE:

A high level of peripheral vasodilation and the potential for reflux tachycardia could arise from an overdose of amlodipine. Significant and protracted hypotension resulting in shock and death has been documented. When a patient overdoses on amlodipine, activated charcoal should be provided. Intravenous fluid resuscitation, IV calcium gluconate, and vasopressor treatment with norepinephrine or dopamine are usually sufficient to treat hypotension. High-dose insulin is also occasionally given, as research has shown that it reduces mortality and improves hemodynamics. 

During an overdose, electrocardiographic data, vital signs, kidney function, urine output, and electrolytes must all be monitored continuously. As amlodipine has a strong plasma protein binding, hemodialysis is unlikely useful. A recent case report reports a successful resin hemadosrption treatment for amlodipine overdose, demonstrating its efficacy in treating severe toxicity and hemodynamic instability. 

•  Dizziness 

•  Fainting 

•  A rapid heartbeat 

TOXICITY:

Amlodipine overdose and toxicity can cause extensive vasodilation, hypotension, and reflex tachycardia as compensatory strategies. Prolonged systemic hypotension can lead to shock and death. 

STORAGE:

 Keep amlodipine in suspension between 36°F and 46°F (2°C and 8°C).68°F to 77°F (20°C to 25°C) is the recommended temperature range for storing oral medications and solutions. Keep dry and cold, sealed in an airtight container. Stay out of the sun as much as possible. The recommended temperature range for amlodipine in suspension storage is 36°F to 46°F (2°C and 8°C).