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Propranolol (a nonselective β antagonist) Propranolol is a beta-blocker…
Propranolol
(a nonselective β antagonist)
Propranolol is a beta-blocker medication.
Beta-blockers have an impact on the heart and circulation.
Actions
Cardiovascular
β1 and β2 receptors improves blood flow and lowers blood pressure by relaxing blood vessels and slowing heart rate.
Peripheral Vasoconstriction
It blocks the vasodilator (β1-receptor stimulating) effects of catecholamines without affecting the vasoconstrictor (α-receptor stimulating) property.
Bronchoconstriction
After the initial bronchospasm subsided, beta-adrenoceptor blockers and the isomer (+)-propranolol produced potentiation of the bronchoconstrictor effects of 5-hydroxytryptamine and histamine.
Disturbance In Glucose Metabolism
In hypertensive, non-diabetic subjects, it increased blood glucose concentrations, decreased plasma glucagon and FFA concentrations, but had no effect on serum insulin levels.
Therapeutic uses
Hypertension
It reduces your heart rate and makes it easier for your heart to pump blood throughout your body.
Angina pectoris
It failed to reduce the frequency of anginal attacks.
Migraine
Propranolol is a beta-blocker that is sometimes used to prevent migraines. It may work by preventing blood vessel dilation and stabilizing serotonin levels.
Hyperthyroidism
It prevents the peripheral conversion of inactive T4 to active T3.
Pharmacokinetics
Propranolol is rapidly and completely absorbed, with peak plasma levels achieved about 1–3 hours after ingestion.
In the blood, more than 90% of the drug is bound to plasma protein. It appears that co-administration with food improves bioavailability.
Hepatic impairment increases its bioavailability. 4-hydroxypropranolol, the main metabolite, has a longer half-life (5.2–7.5 hours) than the parent compound (3–4 hours) and is also pharmacologically active.
Adverse Effects
Drug Interactions
Alpha-blockers (such as prazosin), aluminum hydroxide, anticholinergics (such as atropine and scopolamine), chlorpromazine, and drugs that affect liver enzymes that remove propranolol from your body are all examples of such medications
Bronchoconstriction
Inhaled propranolol causes bronchoconstriction in asthmatic subjects via an unknown indirect mechanism.
Arrhythmias
Propranolol has been linked to heart failure in some patients. If you have chest pain, dilated neck veins, extreme fatigue, irregular breathing, swelling, fingers, legs, or weight gain.
Sexual Impairment
Propranolol may cause ED by increasing the latency to ex copula ejaculation, the latency to initial erection, and decreasing the number of erectile reflexes.
Metabolic Disturbance
Propranolol stimulated respiration and metabolism in heart slices when pyruvate or glucose was used as a substrate while inhibiting oxidative phosphorylation.
CNS Effects
Short- and long-term memory, psychomotor function, sleep quality, and mood have all been reported to be impaired with relatively low doses and treatment durations.
Brand Names
Inderal, Inderal LA, InnoPran XL, and Hemangeol.
Propranolol has variable bioavailability despite complete absorption due to extensive first-pass metabolism.