Pindolol is an aryloxypropanolamine derivative with the antihypertensive property. Pindolol competitively binds to beta-adrenergic receptors, resulting in a decrease in beta-adrenergic activities, i.e., vasodilation, and negative chronotropic and inotropic effects. In addition, this agent blocks serotonin (5-HT) 1A receptors, thereby increasing the available serotonin in the brain. Increased serotonin levels augment the antidepressant action of selective serotonin reuptake inhibitors and monoamine oxidase inhibitors.
Pindolol is a nonselective beta-adrenergic receptor blocker that is widely used for the therapy of hypertension and angina pectoris. Pindolol has yet to be convincingly associated with clinically apparent liver injury.
Mechanism of Action of Pindolol
Pindolol non-selectively blocks beta-1 adrenergic receptors mainly in the heart, inhibiting the effects of epinephrine and norepinephrine resulting in a decrease in heart rate and blood pressure. By binding beta-2 receptors in the juxtaglomerular apparatus, Pindolol inhibits the production of renin, thereby inhibiting angiotensin II and aldosterone production and therefore inhibits the vasoconstriction and water retention due to angiotensin II and aldosterone, respectively.
A moderately lipophilic beta blocker (adrenergic beta-antagonists). It is non-cardioselective and has intrinsic sympathomimetic actions, but little membrane-stabilizing activity. It is also an antagonist of the serotonin 5-HT1A receptor, preferentially blocking inhibitory 5-HT1A autoreceptors, and has been researched as an add-on therapy to selective serotonin reuptake inhibitors (SSRIs) in the treatment of depression, though with little or no effectiveness ultimately seen.
Indications of Pindolol
- High Blood Pressure
- Angina Pectoris
- Depression
- Ventricular tachycardias, and atrial fibrillation.
- Nonvalvular atrial fibrillation
- Hypertension, edema,
Contra-Indications of Pindolol
- Diabetes
- Depression
- Myasthenia Gravis
- Complete heart block
- Partial heart block
- Sinus bradycardia
- Suddenly serious symptoms of heart failure
- Occasional Numbness
- Tingling of Fingers and Toes
- Emphysema
- Asthma
- Severe Chronic Obstructed Lung Disease
- Liver problems
- Blood Circulation Failure due to Serious Heart Condition
- Anaphylactic Shock due to Allergy Shots
- Right-sided Heart Failure
- Kidney disease with likely reduction in kidney function
- Allergies to beta-Blockers (Beta-Adrenergic Blocking Agents)
Dosage of Pindolol
Strengths: 5 mg; 10 mg;
Hypertension
- Initial dose: 5 mg orally 2 times a day
- Titration: The dose may be adjusted in increments of 10 mg per day every 3 to 4 weeks
- Maximum dose: 60 mg per day
Side Effects of Pindolol
The most common
- Swelling of the face, fingers, feet, or lower legs
- Burning, crawling, itching, numbness, prickling, “pins and needles”, or tingling feelings
- Fever, chills, or a sore throat
- Shortness of breath
- Chest pain or discomfort
- Slow or irregular heartbeat
- Dry mouth/ a cough
- muscle trembling, jerking, or stiffness
- anxiety
- changes in vision, including blurred vision
- dizziness, faintness, or lightheadedness when getting up suddenly from a lying or sitting position
- stomach pain or cramping
- diarrhea
- a headache
- stomach pain;
- back pain, joint or muscle pain.
- problems with your vision (including color vision);
- sudden chest pain or trouble breathing;
- pain or swelling in one or both legs;
- a migraine headache;
- pale skin, feeling light-headed or short of breath, rapid heart rate, trouble concentrating; or
More common
- Abdominal or stomach pain, discomfort, or tenderness
- chills or fever
- difficulty with moving
- a headache, severe and throbbing
- joint or back pain
- muscle aching or cramping
- muscle pains or stiffness
- chest pressure or squeezing pain in the chest
- discomfort in arms, shoulders, neck or upper back
- excessive sweating
- feeling of heaviness, pain, warmth and/or swelling in a leg or in the pelvis
- sudden tingling or coldness in an arm or leg
- sudden slow or difficult speech
- sudden drowsiness or need to sleep
- fast breathing
- sharp pain when taking a deep breath
- fast or slow heartbeat
- coughing up blood
- rust colored urine
- decreased amount of urine
Rare
- Anxiety
- change in vision
- chest pain or tightness
- confusion
- a cough
- Agitation
- arm, back, or jaw pain
- blurred vision
- chest pain or discomfort
- convulsions
- extra heartbeats
- fainting
- hallucinations
- a headache
- irritability
- lightheadedness
- mood or mental changes
- muscle pain or cramps
- muscle spasm or jerking of all extremities
- nervousness
Drug Interactions of
Pindolol may interact with the the following drug, supplements, & may change the efficacy of the drug
- alpha-1 blockers (e.g., doxazosin, prazosin, tamsulosin)
- alpha-2 blockers (e.g., clonidine, dexmedetomidine, methyldopa)
- angiotensin-converting enzyme inhibitors (ACEIs; e.g., captopril, ramipril)
- angiotensin II receptor blockers (i.e., irbesartan, losartan, valsartan)
- anti-psychotics (e.g., clozapine, olanzapine, quetiapine, risperidone)
- atorvastatin
- azole antifungals (e.g., itraconazole, ketoconazole, posaconazole)
- barbiturates (e.g., phenobarbital)
- benzodiazepines (e.g., alprazolam, diazepam, lorazepam)
- beta-agonists (e.g., formoterol, salbutamol, salmeterol)
- other beta-blockers (e.g., propanolol, metoprolol)
- calcium channel blockers (e.g., amlodipine, diltiazem, nifedipine, verapamil)
- carbamazepine
- cyclosporine
- dexamethasone
- diuretics (water pills; e.g., furosemide, hydrochlorothiazide)
- duloxetine
- levodopa
- lidocaine
- MAO inhibitors (e.g., phenelzine, moclobemide, selegiline)
- macrolide antibiotics (e.g., azithromycin, clarithromycin, erythromycin)
- nilotinib
- nonsteroidal anti-inflammatory drugs (NSAIDs; e.g., ibuprofen, naproxen)
- other beta-blockers (e.g., atenolol, metoprolol, propranolol)
- pentoxifylline
- phosphodiesterase-5-inhibitors (e.g., sildenafil, tadalafil)
- selective serotonin reuptake inhibitors (SSRI; e.g., fluoxetine, paroxetine, sertraline)
- sunitinib
- theophyllines (e.g., aminophylline, oxtriphylline, theophylline)
Pregnancy Catagory of Pindolol
FDA Pregnancy Category C
Pregnancy
The safety of this medication for use by pregnant women has not been established. It should not be taken by pregnant women unless the benefits outweigh the risks. If you become pregnant while taking this medication, contact your doctor immediately.
Lactation
Pindolol passes into breast milk. If you are a breastfeeding mother and are taking this medication, it may affect your baby. Talk to your doctor about whether you should continue breastfeeding. The safety and effectiveness of using this medication have not been established for children.
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