Amlovas

Amlovas (amlodipine) is a calcium channel blocker drug used to treat high blood pressure (hypertension) and angina (chest pain caused by ischemic heart disease). Amlodipine works by widening blood vessels and improving blood flow, which helps lower blood pressure and reduce the workload on the heart.

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

It is important to use amlodipine only as directed by your doctor and to follow his or her recommendations regarding dosage and regimen to minimize the risk of possible side effects and ensure the best therapeutic effect.

Indications Amlovas

1. Hypertension (high blood pressure): Amlovas effectively lowers blood pressure by widening peripheral arteries and improving blood flow. This makes it one of the mainstays of hypertension treatment.
2. Angina (stable and unstable): Amlovas is also used to treat angina, a condition in which the heart muscle does not get enough oxygen, leading to attacks of chest pain. Amlovas helps to widen blood vessels and increase blood flow to the heart, reducing the frequency and severity of attacks.
3. Coronary artery disease: Amlovas may be used to treat coronary artery disease, which includes angina and myocardial infarction.
4. Vasospasms: Amlovas may sometimes be used to treat vasospasms (spasmodic narrowing of blood vessels), such as vasospasm in rhinos.
5. Other conditions as prescribed by your doctor: In some cases, Amlovas may be prescribed by your doctor to treat other conditions, such as some forms of heart failure or some types of arrhythmia.

Release form

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

Pharmacodynamics

1. Calcium channel blocking: Amlodipine blocks L-type calcium channels in vascular smooth muscle cells and myocardium, resulting in decreased intravascular calcium and decreased vascular tone.
2. Dilation of peripheral arteries: By blocking calcium channels in vascular smooth muscle, amlodipine causes 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 workload of the heart: Amlodipine reduces the late phase of diastolic pressure in the left ventricle of the heart, which reduces its workload and oxygen demand. This is especially useful in the treatment of stable and unstable angina.
4. Improved 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 adverse cardiac effects, especially in overdose.

Pharmacokinetics

1. Absorption: Amlodipine is generally well absorbed from the gastrointestinal tract after oral administration. Peak blood concentrations are usually reached 6-12 hours after administration.
2. Bioavailability: The oral bioavailability of amlodipine is approximately 60-65% due to a high degree of first-pass metabolism in the liver.
3. Metabolism: The major route of metabolism of amlodipine occurs in the liver with the participation of cytochrome P450, mainly CYP3A4 isoenzymes. The main metabolite, 2-pyrolidinecarboxylic acid, has no pharmacological activity.
4. Elimination: After metabolism, most of amlodipine and its metabolites are excreted via the kidneys as urea, within 10-12 hours. In elderly people and patients with liver failure, the elimination of amlodipine may be slower, which may require dosage adjustment.
5. Half-life: The half-life of amlodipine in 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 concomitantly.

Dosing and administration

Directions for use:

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

Recommended doses:

1. Arterial hypertension:

   • Initial 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 daily.

2. Angina pectoris (stable and vasospastic):

   • Initial 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 daily.

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 impaired liver function:

   • 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 required when increasing the dose.

3. Patients with impaired renal function:

   • Dose adjustment in patients with renal impairment is generally not required. Amlodipine is eliminated primarily via the liver, so renal function does not significantly affect 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 agents.

Notes:

• Missed Dose: If you miss a dose, take the missed dose as soon as possible. If it is near the time of your next dose, skip the missed dose and continue taking it at your regular schedule. Do not double the dose to make up for the missed dose.
• Withdrawal of the drug: Stopping the drug should be done under the supervision of a doctor. Abrupt withdrawal of amlodipine may lead to worsening of the condition.

Use Amlovas during pregnancy

1. Early pregnancy safety study: In a study of 231 women with chronic hypertension, the incidence of morphological abnormalities in neonates exposed to amlodipine in the first trimester was found to be no different from that in neonates whose mothers took other antihypertensive drugs or no antihypertensive drugs (Mito et al., 2019).
2. Pharmacokinetics of amlodipine during labor and lactation: A study showed that amlodipine crosses the placenta in measurable amounts but is not detectable in breast milk or infant plasma 24-48 hours postpartum, 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 case reports, women took amlodipine in the first trimester of pregnancy. Two of the three babies had no significant developmental abnormalities. One woman had a spontaneous abortion, but this was not directly related to amlodipine (Ahn et al., 2007).
4. Pilot clinical trial on the treatment of hypertension in pregnant women: The study showed that amlodipine in combination with magnesium sulfate effectively reduced blood pressure and improved pregnancy outcomes in women with gestational hypertension. It also showed a reduction in the incidence of postpartum complications and an improvement in the overall health of the newborns (Xiao-lon, 2015).
5. Effects on the fetus in mice: A study in mice showed that high doses of amlodipine can cause embryonic lethality and organ changes. However, normal therapeutic doses used in clinical practice are safe (Orish et al., 2000).

Contraindications

1. Hypersensitivity: People with known hypersensitivity to Amlovas or any other components of the drug should refrain from using it.
2. Severe aortic stenosis: The use of Amlovas may be contraindicated in patients with severe stenosis (narrowing) of the aortic valve due to the risk of worsening the condition.
3. Shock: The use of Amlovas is contraindicated in shock, as it may reduce cardiac contractility and worsen the decrease in blood pressure.
4. Unstable angina: In patients with unstable angina (eg, unstable angina), Amlovas may be contraindicated due to the possible risk of exacerbation of cardiac ischaemic symptoms.
5. Heart failure: In some cases, Amlovas may be contraindicated in patients with severe heart failure due to its potential negative effect 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, it may be necessary to adjust the dose of amlodipine due to possible decreased metabolism and elimination of the drug.

Side effects Amlovas

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 when changing position suddenly.
2. Swelling: In some people, amlodipine may cause swelling, usually in the legs or calves. This is due to dilation of peripheral blood vessels.
3. Headache: Some patients may experience headache or a feeling of heaviness in the head.
4. Abdominal pain and nausea: Some people may experience abdominal discomfort, nausea, or vomiting.
5. Skin redness and itching: Some patients may experience allergic reactions to amlodipine, which may include skin redness, 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 increasing arrhythmias.

Overdose

1. Severe drop in blood pressure: This is one of the main signs of amlodipine overdose. A severe drop in blood pressure can lead to fainting, dizziness, or even shock.
2. Tachycardia or bradycardia: Patients who overdose on amlodipine may experience a rapid or slow heartbeat.
3. Edema: 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 consciousness: This may include drowsiness, confusion, or even loss of consciousness.
6. Myocardial depression: This is a condition in which the heart muscle is unable to 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 levels of amlodipine, which may increase its effects. These drugs include antibiotics (eg, erythromycin, clarithromycin), antifungals (eg, ketoconazole, itraconazole), antivirals (eg, ritonavir), and some antifungals and other medications.
2. CYP3A4 inhibitors or inducers: Amlodipine may affect the metabolism of other drugs, especially those that are also metabolized via the CYP3A4 enzyme. This may result in either an increase or decrease in the effects of other drugs.
3. Blood pressure lowering drugs: When amlodipine is taken in combination with other blood pressure lowering drugs (eg, beta-blockers, angiotensin-converting enzyme inhibitors), an increased hypotensive effect may occur, which may lead to a severe drop in blood pressure.
4. Drugs that affect the cardiovascular system: These include antiarrhythmic drugs, drugs that increase cardiac conduction (eg, digoxin), and other calcium antagonists or drugs that affect vascular tone.
5. Medicines that increase blood potassium levels: Blood potassium levels may increase when amlodipine is taken concomitantly with potassium-sparing diuretics or potassium supplements, which may 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 excessive reduction in blood pressure.

7. Antianginal drugs:

   • Nitrates and other antianginal drugs:
     • Combined use may enhance the antianginal effect, which is the desired effect but requires monitoring to prevent excessive pressure reduction.

8. Statins:

   • Simvastatin:
     • Concomitant use with amlodipine may increase the blood concentration of simvastatin. 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 grapefruit juice while taking amlodipine.