Pynastin
Pynastin Uses, Dosage, Side Effects, Food Interaction and all others data.
Pynastin is a first generation non-selective beta blocker used in the treatment of hypertension. Early research into the use of pindolol found it had chronotropic effects, and so further investigation focused on the treatment of arrhythmia. Research into pindolol's use in the treatment of hypertension began in the early 1970s.
Pynastin was granted FDA approval on 3 September 1982.
Pynastin is a nonselective beta blocker indicated in the management of hypertension and prophylaxis of angina. It has a short duration of action as it is given twice daily, and a wide therapeutic window as doses can range from 10-60 mg/day. Patients should be counselled regarding the risk of cardiac failure, exacerbating ischemic heart disease with sudden withdrawal, nonallergic bronchospasm, masking hypoglycemia in diabetics, and masking hyperthyroidism.
| Trade Name | Pynastin |
| Availability | Prescription only |
| Generic | Pindolol |
| Pindolol Other Names | Pindolol, Pindololum |
| Related Drugs | amlodipine, lisinopril, metoprolol, losartan, furosemide, hydrochlorothiazide |
| Type | |
| Formula | C14H20N2O2 |
| Weight | Average: 248.3208 Monoisotopic: 248.152477894 |
| Protein binding | Pindolol is 40% bound to proteins in plasma. Pindolol mainly binds more strongly to alpha-1-acid glycoprotein than it does to serum albumin. |
| Groups | Approved, Investigational |
| Therapeutic Class | |
| Manufacturer | |
| Available Country | |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Pynastin is a beta adrenoceptor antagonist used to treat hypertension, edema, ventricular tachycardias, and atrial fibrillation.
Pynastin is indicated in the management of hypertension. In Canada, it is also indicated in the prophylaxis of angina.
Pynastin is also used to associated treatment for these conditions: Angina Pectoris, Atrial Fibrillation, Depression, High Blood Pressure (Hypertension)
How Pynastin works
The beta-1 adrenoceptor is a G-protein-coupled receptor. Agonism of the beta-1 adrenoceptor allows the Gs subunit to upregulate adenylyl cyclase, converting ATP to cyclic AMP (cAMP). Increased concentrations of cAMP activate cAMP-dependant kinase A, phosphorylating calcium channels, raising intracellular calcium, increasing calcium exchange through the sarcoplasmic reticulum, and increasing cardiac inotropy. cAMP-dependant kinase A also phosphorylates myosin light chains, increasing smooth muscle contractility. Increased smooth muscle contractility in the kidney releases renin.
Pynastin is a non-selective beta blocker. Blocking beta-1 adrenergic receptors in the heart results in decreased heart rate and blood pressure. By blocking beta-1 receptors in the juxtaglomerular apparatus, pindolol inhibits the release of renin, which inhibits angiotensin II and aldosterone release. Reduced angiotensin II inhibits vasoconstriction and reduced aldosterone inhibits water retention.
Beta-2 adrenoceptors located in the kidneys and peripheral blood vessels use a similar mechanism to activate cAMP-dependant kinase A to increase smooth muscle contractility. Blocking of the beta-2 adrenoceptor relaxes smooth muscle, leading to vasodilation.
Toxicity
Patients experiencing an overdose may experience excessive bradycardia, cardiac failure, hypotension, and bronchospasm. Initiate treatment with symptomatic and supportive measures.
Food Interaction
- Avoid alcohol. Alcohol may aggravate signs and symptoms of overdose.
- Take with or without food. Food does not significantly affect absorption.
Pynastin Alcohol interaction
[Moderate]
Many psychotherapeutic and CNS-active agents (e.g., anxiolytics, sedatives, hypnotics, antidepressants, antipsychotics, opioids, alcohol, muscle relaxants) exhibit hypotensive effects, especially during initiation of therapy and dose escalation.
Coadministration with antihypertensives and other hypotensive agents, in particular vasodilators and alpha-blockers, may result in additive effects on blood pressure and orthostasis.
Caution and close monitoring for development of hypotension is advised during coadministration of these agents.
Some authorities recommend avoiding alcohol in patients receiving vasodilating antihypertensive drugs.
Patients should be advised to avoid rising abruptly from a sitting or recumbent position and to notify their physician if they experience dizziness, lightheadedness, syncope, orthostasis, or tachycardia.
Pynastin Cholesterol interaction
[Moderate] Beta-adrenergic receptor blocking agents (aka beta-blockers) may alter serum lipid profiles.
Increases in serum VLDL and LDL cholesterol and triglycerides, as well as decreases in HDL cholesterol, have been reported with some beta-blockers.
Patients with preexisting hyperlipidemia may require closer monitoring during beta-blocker therapy, and adjustments made accordingly in their lipid-lowering regimen.
Pynastin multivitamins interaction
[Moderate] ADJUST DOSING INTERVAL: Concurrent administration with calcium salts may decrease the oral bioavailability of atenolol and possibly other beta-blockers.
The exact mechanism of interaction is unknown.
In six healthy subjects, calcium 500 mg (as lactate, carbonate, and gluconate) reduced the mean peak plasma concentration (Cmax) and area under the concentration-time curve (AUC) of atenolol (100 mg) by 51% and 32%, respectively.
The elimination half-life increased by 44%.
Twelve hours after the combination, beta-blocking activity (as indicated by inhibition of exercise tachycardia) was reduced compared to that with atenolol alone.
However, during a 4-week treatment in six hypertensive patients, there was no difference in blood pressure values between treatments.
The investigators suggest that prolongation of the elimination half-life induced by calcium coadministration may have led to atenolol cumulation during long-term dosing, which compensated for the reduced bioavailability.
It may help to separate the administration times of beta-blockers and calcium products by at least 2 hours.
Patients should be monitored for potentially diminished beta-blocking effects following the addition of calcium therapy.
Pynastin Drug Interaction
Moderate: duloxetine, clonazepam, alprazolamMinor: levothyroxineUnknown: docusate, ubiquinone, venlafaxine, omega-3 polyunsaturated fatty acids, ferrous sulfate, escitalopram, atorvastatin, pregabalin, esomeprazole, omeprazole, bifidobacterium infantis / lactobacillus acidophilus, montelukast, topiramate, acetaminophen, cholecalciferol, sertraline
Pynastin Disease Interaction
Major: bradyarrhythmia/AV block, cardiogenic shock/hypotension, CHF, diabetes, hemodialysis, hypersensitivity, ischemic heart disease, PVD, asthma/COPD, liver diseaseModerate: cerebrovascular insufficiency, glaucoma, hyperlipidemia, hyperthyroidism, myasthenia gravis, pheochromocytoma, psoriasis, tachycardia, Prinzmetal's variant angina, renal dysfunction
Volume of Distribution
The volume of distribution of pindolol is approximately 2-3 L/kg.
Elimination Route
The mean oral bioavailability of pindolol is 87-92%. A 5 mg oral dose reaches a Cmax of 33.1 ± 5.2 ng/mL, with a Tmax of 1-2 hours.
Half Life
The half life of pindolol varies from 3-4 hours but can be as high as 30 hours in patients with cirrhosis of the liver.
Clearance
In otherwise healthy patients, the systemic clearance of pindolol is 400-500 mL/min. In patients with cirrhosis, the clearance of pindolol varies from 50-300 mL/min.
Elimination Route
80% of an oral dose is eliminated in the urine, with 25-40% of the dose as the unchanged parent compound. 6-9% of an intravenous dose is eliminated in the feces. Overall, 60-65% of a dose is eliminated as glucuronide and sulfate metabolites.
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