Amlovas

Amlovas (amlodipine) is a calcium channel antagonist drug used to treat high blood pressure (hypertension) and angina (chest pain caused by ischemia of the heart). Amlodipine acts by dilating blood vessels and improving blood flow, which helps lower blood pressure and reduce stress on the heart.

It is often used as monotherapy or in combination with other drugs to effectively control blood pressure. In some cases, amlodipine may be used to treat other conditions as recommended by your doctor.

It is important to use amlodipine only as prescribed by your doctor and follow your doctor's recommendations regarding dosage and administration to minimize the risk of possible side effects and ensure the best therapeutic effect.

Indications Amlovasa

1. Hypertension (high blood pressure): Amlovas effectively lowers blood pressure by dilating peripheral arteries and improving blood flow. This makes it one of the main drugs for the treatment of hypertension.
2. Angina (stable and unstable): Amlovas is also used to treat angina, a condition in which the heart muscle does not receive enough oxygen, leading to attacks of chest pain. Amlovas helps dilate blood vessels and increase blood flow to the heart, reducing the frequency and severity of attacks.
3. Ischemic heart disease: Amlovas can be used in the treatment of ischemic heart disease, which includes angina and myocardial infarction.
4. Vasospasms: Sometimes Amlovas can be used to treat vasospasms (convulsive contraction of blood vessels), such as vascular spasm in rhinoplasty.
5. Other conditions prescribed by a doctor: In some cases, Amlovas may be prescribed by a doctor to treat other conditions, such as some forms of heart failure or some types of arrhythmias.

Release form

Tablets: This is the most common form of release of Amlovas. The tablets may have different dosages, such as 5 mg or 10 mg, depending on the medical needs of the patient.

Pharmacodynamics

1. Blocking calcium channels: Amlodipine blocks L-type calcium channels in vascular smooth muscle cells and the myocardium, which leads to a decrease in intravascular calcium and a decrease in vascular tone.
2. Dilation of peripheral arteries: By blocking calcium channels in vascular smooth muscle, amlodipine promotes dilation of peripheral arteries and arterioles, which leads to a decrease in vascular resistance and, as a result, a decrease in blood pressure.
3. Reducing the load on the heart: Amlodipine reduces the late phase of diastolic pressure in the left ventricle of the heart, which reduces its load and oxygen demand. It is especially useful in the treatment of stable and unstable angina.
4. Improving myocardial perfusion: By dilating peripheral arteries, amlodipine increases blood flow to the myocardium, which improves its oxygen perfusion and nutrition.
5. Moderate effect on myocardial conduction and contractility: Unlike some other calcium channel antagonists, amlodipine has predominantly vasodilatory properties, with limited effects on cardiac conduction and contractility. However, this does not exclude the possibility of undesirable effects on the heart, especially in case of overdose.

Pharmacokinetics

1. Absorption: Amlodipine is usually well absorbed from the gastrointestinal tract after oral administration. Peak blood concentrations are usually achieved 6-12 hours after administration.
2. Bioavailability: The oral bioavailability of amlodipine is about 60-65% due to the high degree of first-pass metabolism in the liver.
3. Metabolism: The main pathway of amlodipine metabolism occurs in the liver with the participation of cytochrome P450, predominantly CYP3A4 isoenzymes. The main metabolite, 2-pyrrolidinecarboxylic acid, has no pharmacological activity.
4. Elimination: After metabolism, most of amlodipine and its metabolites are excreted through the kidneys in the form of urea within 10-12 hours. In elderly people and patients with liver failure, the elimination of amlodipine may be delayed, which may require dosage adjustment.
5. Half-life: The half-life of amlodipine from the blood is about 30-50 hours, which determines its long-lasting effect after a single dose.
6. Interactions with other drugs: Amlodipine may interact with other drugs, in particular with inhibitors or inducers of the CYP3A4 isoenzyme, which may change its pharmacokinetics and require dosage adjustment when used simultaneously.

Dosing and administration

Method of application:

• The drug is taken orally, regardless of meals, with a sufficient amount of water.
• Tablets should be swallowed whole, without chewing or crushing.

Recommended doses:

1. Arterial hypertension:

   • Starting dose: The recommended starting dose for adults is 5 mg once daily.
   • Maintenance Dose: Depending on the patient's clinical response, the dose may be increased to 10 mg once daily.
   • Maximum daily dose: 10 mg once a day.

2. Angina (stable and vasospastic):

   • Starting dose: The recommended starting dose for adults is 5 mg once daily.
   • Maintenance Dose: Depending on the patient's clinical response, the dose may be increased to 10 mg once daily.
   • Maximum daily dose: 10 mg once a day.

Special patient groups:

1. Elderly patients:

   • The starting dose for elderly patients is usually 2.5 mg once daily, which helps minimize the risk of hypotension and other side effects. The dose may be gradually increased depending on the clinical response and tolerability of the drug.

2. Patients with liver dysfunction:

   • In patients with impaired liver function, the initial dose is also 2.5 mg once daily. Caution and regular monitoring of the patient's condition are necessary when increasing the dose.

3. Patients with impaired renal function:

   • Dose adjustment is usually not required in patients with impaired renal function. Amlodipine is excreted primarily through the liver, so renal function does not have a significant effect on its pharmacokinetics.

Duration of treatment:

• Treatment with amlodipine is usually long-term and depends on the patient's condition and response to therapy.
• The drug can be used as monotherapy or in combination with other antihypertensive and antianginal drugs.

Notes:

• Missing a dose: If you miss a dose, take the missed dose as soon as possible. If it is near your next dose, skip the missed dose and continue on your regular schedule. Do not double the dose to make up for a missed dose.
• Discontinuation of the drug: Discontinuation of the drug should be carried out under the supervision of a physician. Abrupt withdrawal of amlodipine may lead to worsening of the condition.

Use Amlovasa during pregnancy

1. Early Pregnancy Safety Study: In a study of 231 women with chronic hypertension, the incidence of morphological abnormalities in infants exposed to amlodipine in the first trimester was found to be no different from that in infants whose mothers were taking other antihypertensive drugs. Or did not take them at all (Mito et al., 2019).
2. Pharmacokinetics of amlodipine during labor and lactation: The study showed that amlodipine crosses the placenta in measurable amounts, but was not detected in breast milk or infant plasma 24-48 hours after delivery, indicating its safety for use in the peripartum period ( Morgan et al., 2019).
3. Case study of amlodipine use in the first trimester: In three clinical cases, women took amlodipine in the first trimester of pregnancy. Two out of three children had no significant developmental abnormalities. One woman had a spontaneous miscarriage, but this was not directly related to amlodipine (Ahn et al., 2007).
4. Pilot clinical trial for the treatment of hypertension in pregnancy: The study showed that amlodipine in combination with magnesium sulfate was effective in lowering blood pressure and improving pregnancy outcomes in women with gestational hypertension. There was also a decrease in the incidence of postpartum complications and an improvement in the general condition of newborns (Xiao-lon, 2015).
5. Fetal effects in mice: A study in mice showed that high doses of amlodipine can cause fetal lethality and organ changes. However, normal therapeutic doses used in clinical practice are safe (Orish et al., 2000).

Contraindications

1. Hypersensitivity: People with a known hypersensitivity to Amlovas or other components of the drug should avoid using it.
2. Severe aortic stenosis: The use of Amlovas may be contraindicated in patients with severe stenosis (narrowness) of the aortic valve due to the risk of worsening the condition.
3. Shock: The use of Amlovas is contraindicated in a state of shock, as it can reduce cardiac contractility and aggravate the decrease in blood pressure.
4. Unsustainable angina: In patients with unstable angina (eg, unstable angina), Amlovas may be contraindicated due to the possible risk of increased cardiac ischemic symptoms.
5. Heart failure: In some cases, Amlovas may be contraindicated in patients with severe heart failure due to its potential negative effects on cardiac function.
6. Pregnancy and breastfeeding: There is insufficient data on the safety of Amlovas during pregnancy and breastfeeding, so its use may be contraindicated during these periods.
7. Hepatic Impairment: In patients with severe hepatic impairment, amlodipine dosage adjustments may be necessary due to the potential for decreased metabolism and elimination of the drug.

Side effects Amlovasa

1. Dizziness and weakness: This is one of the most common side effects of Amlovas. Patients may experience dizziness or a feeling of weakness, especially if there is a sudden change in body position.
2. Swelling: Amlodipine may cause swelling in some people, usually in the legs or lower legs. This occurs due to dilation of peripheral blood vessels.
3. Headache: Some patients may experience a headache or a feeling of heaviness in the head.
4. Stomach pain and nausea: Some people may experience abdominal discomfort, nausea, or vomiting.
5. Redness of the skin and itching: Some patients may experience allergic reactions to amlodipine, manifested by redness of the skin, itching or rash.
6. Drowsiness: Some people may feel drowsy or tired.
7. Runny nose and difficulty breathing: Rarely, amlodipine may cause a runny nose or difficulty breathing in some patients.
8. Cardiac side effects: In some cases, amlodipine may cause cardiac side effects such as worsening heart failure or worsening arrhythmias.

Overdose

1. Severe decrease in blood pressure: This is one of the main signs of an amlodipine overdose. A severe decrease in blood pressure can lead to fainting, dizziness, or even shock.
2. Tachycardia or bradycardia: Patients with an overdose of amlodipine may experience a rapid or slow heartbeat.
3. Swelling: An overdose of amlodipine may cause swelling, especially in the lower extremities.
4. Cardiac arrhythmias: Cardiac arrhythmias, such as atrial fibrillation or atrial fibrillation, may occur.
5. Changes in state of consciousness: This may include drowsiness, confusion, or even loss of consciousness.
6. Myocardial depression: This is a condition in which the heart muscle cannot contract effectively due to decreased calcium flow into the cells.

Interactions with other drugs

1. CYP3A4 inhibitors: Drugs that inhibit the CYP3A4 enzyme may increase the blood concentration of amlodipine, which may result in increased effects. These drugs include antibiotics (eg, erythromycin, clarithromycin), antifungals (eg, ketoconazole, itraconazole), antivirals (eg, ritonavir), and some antifungals and other drugs.
2. CYP3A4 inhibitors or inducers: Amlodipine may affect the metabolism of other drugs, mainly those that are also metabolized through the CYP3A4 enzyme. This can either increase or decrease the effect of other drugs.
3. Medicines that lower blood pressure: When amlodipine is taken in combination with other drugs that lower blood pressure (eg, beta blockers, angiotensin-converting enzyme inhibitors), an enhanced hypotensive effect may occur, which can lead to a severe decrease in blood pressure.
4. Medicines that affect the cardiovascular system: These include antiarrhythmics, drugs that increase cardiac conduction (eg, digoxin), and other calcium antagonists or drugs that affect vascular tone.
5. Medicines that increase the concentration of potassium in the blood: The concentration of potassium in the blood may increase when amlodipine is taken concomitantly with potassium-sparing diuretics or drugs containing potassium supplements, which can lead to hyperkalemia.

6. Antihypertensive drugs:

   • Other calcium channel blockers, beta blockers, diuretics and ACE inhibitors:
     • Concomitant use may enhance the hypotensive effect of amlodipine, which may lead to an excessive decrease in blood pressure.

7. Antianginal drugs:

   • Nitrates and other antianginal agents:
     • Combination use may enhance the antianginal effect, which is a desirable effect but requires monitoring to prevent excessive decrease in blood pressure.

8. Statins:

   • Simvastatin:
     • Concomitant use with amlodipine may increase the concentration of simvastatin in the blood. It is recommended to limit the dose of simvastatin to 20 mg per day when taken concomitantly with amlodipine.

9. Immunosuppressants:

   • Cyclosporine and tacrolimus:
     • Amlodipine may increase the concentration of these drugs in the blood, which requires monitoring and possible dosage adjustment.

10. Grapefruit juice:

    • Grapefruit juice may increase blood concentrations of amlodipine by inhibiting metabolism via CYP3A4 enzymes. It is recommended to avoid drinking grapefruit juice while taking amlodipine.