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Pindolol

Prescription

商品名: Pindolol

剤形
Tablet
投与経路
ORAL

About This Medication

DESCRIPTION Pindolol, a synthetic beta-adrenergic receptor blocking agent with intrinsic sympathomimetic activity is 1-(Indol-4-yloxy)-3-(isopropylamino)-2-propanol. Pindolol, USP is a white to off-white, crystalline powder having a faint odor which is practically insoluble in water; slightly soluble in methanol; and very slightly soluble in chloroform. Each tablet for oral administration contains pindolol and the following inactive ingredients: crospovidone, lactose, magnesium stearate, microcrystalline cellulose, and pregelatinized starch. Structure

有効成分

成分 含有量
Pindolol -

適応症と用法

INDICATIONS AND USAGE Pindolol tablets are indicated in the management of hypertension. It may be used alone or concomitantly with other antihypertensive agents, particularly with a thiazide-type diuretic.

用量と投与方法

DOSAGE AND ADMINISTRATION The dosage of pindolol tablets should be individualized. The recommended initial dose of pindolol tablets is 5 mg b.i.d. alone or in combination with other antihypertensive agents. An antihypertensive response usually occurs within the first week of treatment. Maximal response, however, may take as long as or occasionally longer than 2 weeks. If a satisfactory reduction in blood pressure does not occur within 3 to 4 weeks, the dose may be adjusted in increments of 10 mg/day at these intervals up to a maximum of 60 mg/day.

Side Effects Overview

ADVERSE REACTIONS Most adverse reactions have been mild. The incidences listed in the following table are derived from 12-week comparative double-blind, parallel design trials in hypertensive patients given pindolol as monotherapy, given various active control drugs as monotherapy, or given placebo. Data for pindolol and the positive controls were pooled from several trials because no striking differences were seen in the individual studies, with one exception. When considering all adverse reactions reported, the frequency of edema was noticeably higher in positive control trials (16% pindolol vs. 9% positive control) than in placebo controlled trials (6% pindolol vs. 3% placebo). The table includes adverse reactions either volunteered or elicited, and at least possibly drug-related, which were reported in greater than 2% of pindolol patients and other selected important reactions. ADVERSE REACTIONS WHICH WERE VOLUNTEERED OR ELICITED (and at least possibly drug-related) Body System/ Adverse Reactions Pindolol (N = 322) % Central Nervous System Bizarre or Many Dreams 5 Dizziness 9 Fatigue 8 Hallucinations < 1 Insomnia 10 Nervousness 7 Weakness 4 Autonomic Nervous System Paresthesia 3 Cardiovascular Dyspnea 5 Edema 6 Heart Failure < 1 Palpitations < 1 Musculoskeletal Chest Pain 3 Joint Pain 7 Muscle Cramps 3 Muscle Pain 10 Gastrointestinal Abdominal Discomfort 4 Nausea 5 Skin Pruritus 1 Rash < 1 Body System/ Adverse Reactions Active Controls Active Controls: Patients received either propranolol, α-methyldopa or a diuretic (hydrochlorothiazide or chlorthalidone). (N = 188) % Central Nervous System Bizarre or Many Dreams 0 Dizziness 11 Fatigue 4 Hallucinations 0 Insomnia 3 Nervousness 3 Weakness 2 Autonomic Nervous System Paresthesia 1 Cardiovascular Dyspnea 4 Edema 3 Heart Failure < 1 Palpitations 1 Musculoskeletal Chest Pain 1 Joint Pain 4 Muscle Cramps 1 Muscle Pain 9 Gastrointestinal Abdominal Discomfort 4 Nausea 2 Skin Pruritus < 1 Rash < 1 Body System/ Adverse Reactions Placebo (N = 78) % Central Nervous System Bizarre or Many Dreams 6 Dizziness 1 Fatigue 4 Hallucinations 0 Insomnia 10 Nervousness 5 Weakness 1 Autonomic Nervous System Paresthesia 6 Cardiovascular Dyspnea 6 Edema 1 Heart Failure 0 Palpitations 0 Musculoskeletal Chest Pain 3 Joint Pain 4 Muscle Cramps 0 Muscle Pain 8 Gastrointestinal Abdominal Discomfort 5 Nausea 1 Skin Pruritus 0 Rash 1 The following selected (potentially important) adverse reactions were seen in 2% or fewer patients and their relationship to pindolol is uncertain. CENTRAL NERVOUS SYSTEM: anxiety, lethargy; AUTONOMIC NERVOUS SYSTEM: visual disturbances, hyperhidrosis; CARDIOVASCULAR: bradycardia, claudication, cold extremities, heart block, hypotension, syncope, tachycardia, weight gain; GASTROINTESTINAL: diarrhea, vomiting; RESPIRATORY: wheezing; UROGENITAL: impotence, pollakiuria; MISCELLANEOUS: eye discomfort or burning eyes.

警告と注意事項

禁忌

薬物動態

PHARMACOKINETICS AND METABOLISM Pindolol is rapidly and reproducibly absorbed (greater than 95%), achieving peak plasma concentrations within 1 hour of drug administration. Pindolol has no significant first-pass effect. The blood concentrations are proportional in a linear manner to the administered dose in the range of 5 mg to 20 mg. Upon repeated administration to the same subject, variation is minimal. After a single dose, intersubject variation for peak plasma concentrations was about 4-fold (e.g., 45 to 167 ng/mL for a 20 mg dose). Upon multiple dosing, intersubject variation decreased to 2- to 2.5-fold. Pindolol is only 40% bound to plasma proteins and is evenly distributed between plasma and red cells. The volume of distribution in healthy subjects is about 2 L/kg. Pindolol undergoes extensive metabolism in animals and man. In man, 35% to 40% is excreted unchanged in the urine and 60% to 65% is metabolized primarily to hydroxy-metabolites which are excreted as glucuronides and ethereal sulfates. The polar metabolites are excreted with a half-life of approximately 8 hours and thus multiple dosing therapy (q.8H) results in a less than 50% accumulation in plasma. About 6% to 9% of an administered intravenous dose is excreted by the bile into the feces. The disposition of pindolol after oral administration is monophasic with a half-life in healthy subjects or hypertensive patients with normal renal function of approximately 3 to 4 hours. Following t.i.d. administration (q.8H), no significant accumulation of pindolol is observed. In elderly hypertensive patients with normal renal function, the half-life of pindolol is more variable, averaging about 7 hours, but with values as high as 15 hours. In hypertensive patients with renal diseases, the half-life is within the range expected for healthy subjects. However, a significant decrease (50%) in volume of distribution (V D ) is observed in uremic patients and V D appears to be directly correlated to creatinine clearance. Therefore, renal drug clearance is significantly reduced in uremic patients, resulting in a significant decrease in urinary excretion of unchanged drug. Uremic patients with a creatinine clearance of less than 20 mL/min generally excreted less than 15% of the administered dose unchanged in the urine. In patients with histologically diagnosed cirrhosis of the liver, the elimination of pindolol was more variable in rate and generally significantly slower than in healthy subjects. The total body clearance of pindolol in cirrhotic patients ranged from about 50 to 300 mL/min and was directly correlated to antipyrine clearance. The half-life ranges from 2.5 hours to greater than 30 hours. These findings strongly suggest that caution should be exercised in dosage adjustments of pindolol in such patients. The bioavailability of pindolol is not significantly affected by coadministration of food, hydralazine, hydrochlorothiazide or aspirin. Pindolol has no effect on warfarin activity or the clinical effectiveness of digoxin, although small transient decreases in plasma digoxin concentrations were noted.

Frequently Asked Questions

INDICATIONS AND USAGE Pindolol tablets are indicated in the management of hypertension. It may be used alone or concomitantly with other antihypertensive agents, particularly with a thiazide-type diuretic.

DOSAGE AND ADMINISTRATION The dosage of pindolol tablets should be individualized. The recommended initial dose of pindolol tablets is 5 mg b.i.d. alone or in combination with other antihypertensive agents. An antihypertensive response usually occurs within the first week of treatment. Maximal response, however, may take as long as or occasionally longer than 2 weeks. If a satisfactory reduction in blood pressure does not occur within 3 to 4 weeks, the dose may be adjusted in increments of 10 mg/day …

WARNINGS Cardiac Failure Sympathetic stimulation may be a vital component supporting circulatory function in patients with congestive heart failure, and its inhibition by beta-blockade may precipitate more severe failure. Although beta-blockers should be avoided in overt congestive heart failure, if necessary, pindolol can be used with caution in patients with a history of failure who are well-compensated, usually with digitalis and diuretics. Both digitalis glycosides and beta-blockers slow atrioventricular conduction and decrease heart rate. Concomitant use can increase risk of …

CONTRAINDICATIONS Pindolol tablets are contraindicated in: 1) bronchial asthma; 2) overt cardiac failure; 3) cardiogenic shock; 4) second and third degree heart block; 5) severe bradycardia. (See WARNINGS. )

Pindolol is a prescription medication. You will need a valid prescription from a licensed healthcare provider.

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References & Data Sources

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データソース: DailyMed (NLM), openFDA, MFDS

Medical Disclaimer

This content is for educational and informational purposes only. It is not a substitute for professional medical advice, diagnosis, or treatment. Always consult a qualified healthcare provider before making medication decisions.

Data sources: ChEMBL, PubChem, DailyMed.