Verapamil

$ 109.42$ 245.26

Category: Blood Pressure
Commercial name: Verapamil
Active ingredient: Verapamil
Production form: Pills
Available dosage: 20 mg, 80 mg, 120 mg, 240 mg

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Description

Verapamil. Dosage, Side Effects, Interactions

Verapamil belongs to the active substance group of selective calcium channel blockers or calcium antagonists of the phenylalkylamine type, which can be used to treat cardiac arrhythmia, coronary artery disease and high blood pressure.

The calcium channel antagonist verapamil is mainly used in coronary heart disease and various forms of angina pectoris to improve the oxygen supply to the heart. Other indications for verapamil are hypertension and hypertrophic obstructive cardiomyopathy (HOCM).

As an antiarrhythmic , verapamil is used primarily in supraventricular tachyarrhythmias, as well as atrial fibrillation and atrial flutter with rapid AV conduction (with the exception of WPW syndrome or Lown.Ganong-Levine syndrome).

Rare areas of application for verapamil are also the prophylaxis of cluster headaches and the therapy of plaque deposits in the case of hardening in the erectile tissue of the penis (induratio penis plastica).

Application type

Verapamil is available as a salt (verapamil hydrochloride) in tablets, prolonged-release tablets and in injection solutions. The tablets should be taken three to four times a day and the prolonged-release tablets should be taken once or twice a day. It is taken without chewing with sufficient liquid (no grapefruit juice!), preferably with or shortly after meals.

The duration of use is not limited. If verapamil is to be discontinued again after prolonged therapy, the dose should be gradually reduced and then discontinued.

The intravenous injection should be carried out slowly (injection time at least 2 minutes) under observation of the patient, if possible with ECG and blood pressure monitoring. Continuous drip infusion can be done in isotonic sodium chloride, 5% glucose, or other suitable solutions (pH < 6.5).

How Verapamil works

The active ingredient blocks the influx of calcium into the heart muscle cells. This leads to a reduction in the heart’s ability to beat and a reduced beat rate. As a result, the heart is relieved.

In addition, verapamil has a dilating effect, particularly in the coronary arteries. This improves the oxygen supply to the myocardium and alleviates the symptoms typical of angina pectoris. In addition, peripheral resistance decreases, cardiac output increases and blood pressure decreases.

The antiarrhythmogenic effect is based on a prolonged conduction time at the AV node.

Pharmacokinetics

Verapamil hydrochloride is a racemate of equal proportions of the R and S enantiomers.

Absorption

After oral administration, more than 90% of verapamil is rapidly absorbed from the small intestine. The bioavailability after a single dose of verapamil tablets is 22%, with prolonged-release verapamil it is about 32%. Verapamil undergoes extensive first-pass metabolism. After administration of verapamil tablets, the maximum plasma levels are reached after one to two hours, after administration of prolonged-release verapamil after four to five hours. After several daily doses, the steady state is reached after three to four days.

Distribution

Verapamil is 90% bound to plasma proteins. The volume of distribution is 1.8 to 6.8 l/kg.

Biotransformation

Verapamil is extensively metabolised in the liver by CYP3A4 , CYP1A2 , CYP2C8 , CYP2C9 and CYP2C18. About 12 metabolites have been identified, of which only norverapamil has an appreciable pharmacological effect (about 20% of verapamil).

Elimination

The terminal elimination half-life after intravenous infusion is two to five hours. After oral administration, the elimination half-life is three to seven hours. About 50% of the administered dose is eliminated renally within 24 hours, 70% within five days. Up to 16% is excreted in the faeces.

Dosage of Verapamil

Hypertension in adults and adolescents weighing more than 50 kg

Oral: The recommended dosage is 240 mg – 360 mg verapamil per day.

Coronary heart disease in adults and adolescents weighing more than 50 kg

Oral: The recommended dosage is 240 mg – 480 mg verapamil per day. In patients with angina pectoris after myocardial infarction, verapamil may only be used 7 days after the acute infarction event.

Paroxysmal, supraventricular tachycardia, atrial fibrillation/atrial flutter

The recommended oral dosage for adults is 240 mg – 480 mg verapamil per day. For older preschool children up to 6 years of age, the recommended dosage is 80 mg – 120 mg verapamil per day. School children between the ages of 6 and 14 receive between 80 mg and 360 mg of verapamil hydrochloride per day.

Paroxysmal, supraventricular tachycardia, atrial fibrillation/flutter and initial treatment of unstable angina pectoris

  • Adults and adolescents over 50 kg body weight: initial dose 5 mg verapamil iv, if necessary after 5-10 minutes another 5 mg verapamil.
  • A continuous drip infusion of 5-10 mg verapamil/hour, on average up to a total dose of 100 mg verapamil/day, can then be administered.
  • If therapy for unstable angina pectoris is started with intravenous verapamil, the switch to oral therapy should be made as soon as possible.
  • Children : If there are signs of tachycardia-related cardiac insufficiency, the administration of cardiac glycosides is required before the intravenous administration of verapamil .

The injection should only be given until the onset of action.

  • 6-14 years: 2.5-5.0 mg IV
  • 1-5 years: 2.0-3.0 mg IV
  • Infants: 0.75-2.0 mg IV
  • Newborns: 0.75-1.0 mg IV
  • 0-1 year: Only if there is a compelling indication if no alternative is available.

Impaired kidney function:

Verapamil should be used with caution and under close observation in patients with impaired renal function.

Impaired liver function:

In patients with impaired liver function, the metabolism of verapamil is slowed down, as a result of which the bioavailability of verapamil can increase significantly and the effect can be enhanced or prolonged. Therefore, initially low starting doses of 80 to 120 mg verapamil per day are recommended.

side effects

The very common side effects of verapamil include gastrointestinal symptoms such as nausea, constipation and bloating. Serious common undesirable effects include cardiac arrhythmia and blood pressure regulation disorders as well as worsening of existing cardiac insufficiency . Allergic reactions with skin redness, itching, or hives , as well as fatigue, headache, ankle edema, and dizziness are some of the other common side effects of verapamil.

interactions

Serious consequences likely – contraindicated in certain cases (verapamil as CYP3A4 inhibitor):

  • Eliglustat : Increased effect of eliglustat possible

Serious consequences possible – contraindicated as a precaution (verapamil as CYP3A4 inhibitor):

  • Cariprazine : Enhanced effects of cariprazine
  • Ivabradine : Enhanced Effects of Ivabradine (Bradycardia)
  • Lomitapid : Enhanced effects of lomitapid possible
  • Neratinib : Enhanced effects of neratinib cannot be ruled out
  • Sertindole : Increased effects of sertindole ► Risk of life-threatening cardiac arrhythmia

Simultaneous use not recommended:

  • Amiodarone : Additive cardiodepressive effect possible
  • Enzyme inducers (CYP3A4): Decreased effects of calcium channel blockers
  • Rifampicin : Decreased effects of nifedipine and derivatives
  • Colchicine :Danger of colchicine intoxication

Further interactions can be found in the relevant prescribing information.

contraindication

  • Hypersensitivity to verapamil
  • cardiovascular shock
  • Pronounced conduction disturbances (e.g. SA or AV block of the second and third degree; except in patients with pacemakers)
  • Sinus node syndrome (except in patients with pacemakers)
  • Heart failure with a reduced ejection fraction of less than 35% and/or an occlusion pressure greater than 20 mmHg (unless secondary to verapamil-responsive supraventricular tachycardia)
  • Atrial fibrillation/flutter and the simultaneous presence of accessory pathways (e.g. WPW or Lown-Ganong-Levine syndrome). These patients are at increased risk of developing ventricular tachycardia, including ventricular fibrillation, with verapamil
  • Concomitant administration of ivabradine
  • The simultaneous intravenous administration of beta-receptor blockers must not take place in patients during treatment with verapamil (exception: intensive care medicine)
  • Solution for injection: Pregnancy and lactation

pregnancy

Verapamil crosses the placenta and animal studies have also shown reproductive toxicity. Therefore, verapamil should not be taken orally during the first and second trimester of pregnancy. It may only be taken in the third trimester of pregnancy if there is a compelling indication and after a strict benefit/risk assessment.

Intravenous administration of verapamil in pregnancy is contraindicated. There is a risk of hypotension and thus a decrease in uteroplacental perfusion with the risk of fetal hypoxia.

lactation

Verapamil passes into breast milk in small amounts after oral administration, which is why verapamil should only be used orally during breastfeeding after a strict benefit/risk assessment. Intravenous administration of verapamil is contraindicated during lactation. If there is a compelling indication, breastfeeding must be interrupted for the duration of the treatment. There is also evidence that hyperprolactinemia and galactorrhea can be caused.

driving ability

Treatment with verapamil requires regular medical supervision. Due to the different reactions that occur individually, the ability to react can be changed to such an extent that the ability to actively participate in road traffic or to operate machines is impaired. This applies to a greater extent at the start of treatment and when the dose is increased.

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Additional information

Dosage

40 mg, 80 mg, 120 mg, 240 mg

Quantity

30, 60, 90, 120, 180

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