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Verapamil

 

Verapamil is used to treat high blood pressure and to control angina.

It is a class of medications called calcium-channel blockers.

It increases the supply of blood and oxygen to the heart and slows electrical activity in the heart to control the heart rate.

Verapamil controls arrhythmias, high blood pressure, and angina but does not cure these conditions.

Verapamil

Verapamil is a calcium channel blocker medication used for the treatment of high blood pressure, angina, and supraventricular tachycardia.

It is in the non–dihydropyridine calcium channel blocker family of medications.

It may also be used for the prevention of migraines and cluster headaches.

It is given by mouth or by intravenously.

Pregnancy category AU: 

Calcium channel blocker.

Bioavailability 35.1%.

Metabolism liver.

Elimination half-life 2.8–7.4 hours.

Excretion kidney: 11%

Common side effects include headache, low blood pressure, nausea, and constipation, other side effects include allergic reactions and muscle pains.

It is not recommended in people with a slow heart rate or heart failure.

Can cause problems for the fetus if used during pregnancy.

It is in the non–dihydropyridine calcium channel blocker family of medications.

is used for controlling ventricular rate in supraventricular tachycardia and migraine headache prevention.   

It is a class-IV antiarrhythmic and more effective than digoxin in controlling ventricular rate.

It may be used to treat hypertension if patient has co-morbid atrial fibrillation or other types of arrhythmia.

Verapamil is also used intra-arterially to treat cerebral vasospasm.

It is used to treat the condition cluster headache.

Evidence supports the use of verapamil topically to treat plantar fibromatosis.

Use of verapamil is generally avoided in people with severe left ventricular dysfunction, hypotension , cardiogenic shock, and hypersensitivity to verapamil.

It is also contraindicated in people with atrial flutter or fibrillation and an existing accessory tract such as in Wolff-Parkinson-White syndrome.

The most common side effect of verapamil is constipation (7.3%). 

Other side effects include dizziness (3.3%), nausea (2.7%), low blood pressure (2.5%), and headache 2.2%. 

Other side effects seen in less than 2% of the population include: edema, congestive heart failure, pulmonary edema, fatigue, elevated liver enzymes, shortness of breath, low heart rate, atrioventricular block, rash and flushing.

Verapamil is known to induce gingival enlargement.

Acute overdose associated with nausea, weakness, slow heart rate, dizziness, low blood pressure, and abnormal heart rhythms. 

Plasma, serum, or blood concentrations of verapamil and its major active metabolite, may be measured to confirm a diagnosis of poisoning in hospitalized patients or to aid in the medicolegal investigation of fatalities. 

Blood or plasma verapamil concentrations are usually in a range of 50–500 μg/L in persons on therapy.

This agents blocks voltage-dependent calcium channels.

Calcium channel blockers are considered class-IV antiarrhythmic agents. 

Calcium channels are especially concentrated in the sinoatrial and atrioventricular nodes, these agents can be used to decrease impulse conduction through the AV node, thus protecting the ventricles from atrial tachyarrhythmias. 

Verapamil is also a Kv voltage gated potassium channel blocker.

Calcium channels are present in the smooth muscle lining blood vessels. 

By relaxing the tone of this smooth muscle, calcium channel blockers dilate the blood vessels, leading to their use in treating high blood pressure and angina pectoris. 

Calcium channel blockers dilate blood vessels, which increases the supply of blood and oxygen to the heart.

Preventive therapy for migraines with verapamil works on the circadian rhythm and on   Calcitonin gene-related peptide (CGRP).

As CGRP-release is controlled by voltage-gated calcium channels.

More than 90% of verapamil is absorbed when given orally.

It has a high first-pass metabolism, so it’s bioavailability is much lower at 10–35%.

It is 90% bound to plasma proteins and has a volume of distribution of 3–5 L/kg. 

Peak plasma concentration are reached after oral administration at 1 to 2 hours.

It is metabolized in the liver to at least 12 inactive metabolite.

The metabolite, norverapamil, retains 20% of the vasodilatory activity of the parent drug.

Excretion: 70% of metabolites are excreted in the urine and 16% in feces, 

while 3–4% is excreted unchanged in urine. 

Onset of action with verapamil is 1–2 hours after oral dosage. 

Half-life is 5–12 hours.

Verapamil is not cleared by hemodialysis. 

It is excreted in human milk, and nursing infants should be discontinued while verapamil is administered.

It is effective in both short-term and long-term treatment of mania and hypomania.

Magnesium oxide added to the verapamil treatment protocol enhances its antimanic effect.

Verapamil in patients with recent onset type one diabetes, modestly preserves endogenous insulin secretion.

Verapamil treatment resulted in a 30% increase in C-peptide secretion compared with placebo and delayed the expected decline of C-peptide production from 3 to 6 months after diagnosis early onset of type one diabetes.

 

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