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Labetalol

Generic Name: Labetalol
Brand Name: Trandate

Indications
Labetalol (trandate) tablets are indicated in the management of hypertension.

Dosage and Administration

Trandates are available for oral administration as 100mg, 200mg and 300mg tablets.

Normal Dosage: The recommended initial dosage is 100 mg twice daily whether used alone or added to a diuretic regimen. After 2 or 3 days, using standing blood pressure as an indicator, dosage may be titrated in increments of 100 mg b.i.d. every 2 or 3 days. The usual maintenance dosage of labetalol HCl is between 200 and 400 mg twice daily.

Overdose: Overdose symptoms include a slow heart beat, shortness of breath, fainting, dizziness, weakness, confusion, nausea, and vomiting.

Drug Description

Labetalol hydrochloride (HCl) is a racemate chemically designated as 2-hydroxy-5-[1- hydroxy-2-[(1-methyl-3-phenylpropyl)amino]ethyl]benzamide monohydrochloride, and it has the following structure:


TRANDATE (labetalol hydrochloride) structural formula illustration

Labetalol HCl has the empirical formula C19H24N2O3•HCl and a molecular weight of 364.9. It has two asymmetric centers and therefore exists as a molecular complex of two diastereoisomeric pairs. Dilevalol, the R,R stereoisomer, makes up 25% of racemic labetalol.
Labetalol HCl is a white or off-white crystalline powder, soluble in water.

Side Effects

The following are some of the side effects that are known to be associated with this medicine. Because a side effect is stated here, it does not mean that all people using this medicine will experience that or any side effect.

  • Headache
  • Slower than normal heart beat (bradycardia)
  • Tiredness
  • Disturbed sleep
  • A drop in blood pressure that occurs when going from lying down to sitting or standing, which results in dizziness and lightheadedness (postural hypotension)
  • Damage to the liver
  • Difficulty in passing urine (urinary retention)
  • Nausea and vomiting
  • Breathing difficulties due to a narrowing of the airways (bronchospasm)

Precautions

  • Use caution when driving, operating machinery, or performing other hazardous activities.
  • Use alcohol cautiously. Alcohol may reduce the effectiveness of this drug.
  • Tell your doctor and dentist that you are taking this medication before having surgery.
  • This drug belongs to the FDA pregnancy category C. This means that it is not known whether this medication will harm an unborn baby. Do not take this medication without first talking to your doctor if you are pregnant.

 

Drug Interactions

  • Before taking this medication, tell your doctor if you are taking:
    • a heart medication such as nifedipine (Procardia, Adalat), reserpine (Serpasil), verapamil (Calan, Verelan, Isoptin), diltiazem (Cardizem, Dilacor XR), clonidine (Catapres), digoxin (Lanoxin), doxazosin (Cardura), guanadrel (Hylorel), prazosin (Minipress), or terazosin (Hytrin)
    • a diabetes medication such as insulin, glyburide (Diabeta, Micronase, Glynase), glipizide (Glucotrol), chlorpropamide (Diabinese), or metformin (Glucophage)
    • a nonsteroidal anti-inflammatory drug (NSAID) such as ibuprofen (Motrin, Advil, others), naproxen (Aleve, Anaprox, Naprosyn, others), ketoprofen (Orudis, Orudis KT, Oruvail), and others
    • a respiratory medication such as albuterol (Ventolin, Proventil, Volmax, others), bitolterol (Tornalate), metaproterenol (Alupent, Metaprel), pirbuterol (Maxair), terbutaline (Brethaire, Brethine, Bricanyl), or theophylline (Theo-Dur, Theochron, Theolair, others), and others
    • the stomach medication cimetidine (Tagamet, Tagamet HB)
    • prescription or over-the-counter cough medicines, cold medicines, or diet pills
 

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