Pindolol


Thông tin thuốc gốc
Chỉ định và Liều dùng
Oral
Angina pectoris
Adult: Usual dose: 2.5-5 mg tid according to patient's response. Treatment recommendations may vary among countries and individual products (refer to specific product guidelines).

Oral
Hypertension
Adult: Initially, 5 mg bid or tid, or 15 mg once daily; may increase according to patient's response. Usual maintenance: 15-30 mg once daily, may increase up to 45 mg daily given as a single dose or in divided doses. Max: 60 mg daily. Dosage recommendations may vary among countries and individual products (refer to specific product guidelines).
Suy thận
Severe: Contraindicated.
Cách dùng
May be taken with or without food. May be taken w/ meals to reduce GI discomfort.
Chống chỉ định
Cardiogenic shock, untreated cardiac failure; sick sinus syndrome, 2nd- and 3rd-degree heart block, Prinzmetal's angina, history of bronchospasm, bronchial asthma; untreated phaeochromocytoma; hypotension, pronounced bradycardia, peripheral circulatory disease, COPD, history of cor pulmonale; metabolic acidosis, prolonged fasting. Severe renal impairment.
Thận trọng
Patient with poor cardiac reserve, 1st-degree AV block, severe coronary or cerebral arteriosclerosis, history of a recent MI, history of well-compensated cardiac failure, non-allergic bronchospasm (e.g. emphysema, chronic bronchitis), spontaneous hypoglycaemia, diabetes mellitus, myasthenia gravis, psoriasis, history of severe anaphylaxis to allergens. Patient undergoing surgery. Avoid abrupt withdrawal, particularly in patients with ischaemic heart disease. May mask the signs and symptoms of hypoglycaemia and hyperthyroidism (particularly tachycardia). Hepatic and mild to moderate renal impairment. Elderly. Pregnancy and lactation.
Tác dụng không mong muốn
Significant: Cardiac failure; may exacerbate angina or precipitate MI and ventricular arrhythmias (after abrupt discontinuation); precipitation or exacerbation of psoriasis.
Blood and lymphatic system disorders: Agranulocytosis, thrombocytopenia (sometimes with purpura).
Cardiac disorders: Bradycardia, cardiac arrhythmia, complete AV block.
Eye disorders: Visual impairment or abnormalities, blurred vision, keratoconjunctivitis, dry eyes.
Gastrointestinal disorders: Diarrhoea, nausea, vomiting, dry mouth, constipation, flatulence, dyspepsia, abdominal discomfort.
General disorders and administration site conditions: Fatigue, hyperpyrexia.
Investigations: Decreased HDL and increased LDL (chronic treatment).
Metabolism and nutrition disorders: Diabetes mellitus, hypoglycaemia, hyperglycaemia.
Musculoskeletal and connective tissue disorders: Arthralgia, myalgia, myasthenia gravis, muscle spasms.
Nervous system disorders: Headache, tremor, dizziness, paraesthesia.
Psychiatric disorders: Hallucinations, nightmares, sleep disorder, depression, acute psychosis, confusional state.
Renal and urinary disorders: Glycosuria.
Reproductive system and breast disorders: Erectile dysfunction, libido disorder.
Respiratory, thoracic and mediastinal disorders: Dyspnoea; bronchospasm (particularly in patients with bronchial asthma or history of bronchial complaints).
Skin and subcutaneous tissue disorders: Rash, pruritus, hyperhidrosis, cutaneous lupus erythematosus, toxic epidermal necrolysis.
Vascular disorders: Hypotension, Raynaud's phenomenon, peripheral coldness, intermittent claudication, necrotising vasculitis.
Chỉ số theo dõi
Monitor blood pressure, heart rate, respiratory function; CrCl, urea, and electrolytes in patients with renal impairment.
Quá liều
Symptoms: Pronounced hypotension, bradycardia, hypoglycaemia, cardiogenic shock, heart failure, conduction abnormalities (e.g. 1st- or 2nd-degree block, complete heart block, asystole), dyspnoea, bronchospasm, vomiting, impairment of consciousness, generalised convulsions, cardiac arrest. Management: Supportive and symptomatic treatment. Perform gastric lavage and administer activated charcoal within 4 hours of ingestion. In case of marked bradycardia, administer atropine 1-2 mg IV. Use of a cardiac pacemaker may be required. If necessary, may administer isoprenaline starting with 25 mcg via slow IV inj (5 mcg/min) until the desired effect is achieved. Treat heart failure with digitalis glycosides and/or diuretics; glucagon may also be useful. Administer diazepam for seizures; bronchodilators (e.g. salbutamol, terbutaline, aminophylline) to reverse bronchospasm; vasopressors (e.g. epinephrine, norepinephrine) for hypotension.
Tương tác
May potentiate the negative inotropic and dromotropic effects of verapamil and diltiazem (lesser extent). May increase the serum concentration of thioridazine. May have an additive cardiodepressant effect with certain anaesthetics (e.g. halothane). May enhance the hypotensive effect with other antihypertensive agents (e.g. nifedipine), barbiturates, TCAs, rifampicin, and phenothiazines. May increase AV conduction time with digitalis glycosides. May enhance the rebound hypertension that can follow the withdrawal of clonidine. Amiodarone and class I antiarrhythmics (e.g. disopyramide) may enhance the bradycardic effect of pindolol. Concomitant use with reserpine may result in additive and potentially excessive β-adrenergic blockade. May potentiate the hypoglycaemic effects of insulin and other antidiabetic drugs. May enhance the vasoconstricting effect of ergot alkaloids. NSAIDs (e.g. indometacin) or sulfinpyrazone may decrease the hypotensive effect of pindolol. Concomitant use with xanthines and sympathomimetic agents with β-adrenergic stimulant activity (e.g. epinephrine, phenylephrine, ephedrine, isoprenaline, norepinephrine) may result in mutual inhibition of therapeutic effects. May decrease the clearance of theophylline. May increase plasma levels with cimetidine and fluoxetine.
Tương tác với thức ăn
Alcohol may increase the plasma levels of pindolol.
Ảnh hưởng đến kết quả xét nghiệm
May cause a false-positive aldosterone/renin ratio.
Tác dụng
Description:
Mechanism of Action: Pindolol is a nonselective β-adrenergic antagonist that inhibits both β1- and β2-adrenoreceptors and has mild intrinsic sympathomimetic activity. It has negative chronotropic and inotropic effects and can significantly slow AV nodal conduction.
Pharmacokinetics:
Absorption: Rapidly and almost completely absorbed from the gastrointestinal tract. Bioavailability: Approx 87%. Time to peak plasma concentration: Approx 1 hour.
Distribution: Crosses the placenta; enters breast milk (small amounts). Volume of distribution: Approx 2 L/kg. Plasma protein binding: Approx 40-60%.
Metabolism: Metabolised in the liver (60-65%) to conjugates.
Excretion: Via urine (30-40% as unchanged drug); faeces (6-9%). Elimination half-life: 3-4 hours.
Đặc tính

Chemical Structure Image
Pindolol

Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 4828, Pindolol. https://pubchem.ncbi.nlm.nih.gov/compound/Pindolol. Accessed Nov. 24, 2022.

Bảo quản
Store between 20-25°C. Protect from light.
Phân loại MIMS
Thuốc chống đau thắt ngực / Thuốc chẹn thụ thể bêta
Phân loại ATC
C07AA03 - pindolol ; Belongs to the class of non-selective beta-blocking agents. Used in the treatment of cardiovascular diseases.
Tài liệu tham khảo
Anon. Pindolol. AHFS Clinical Drug Information [online]. Bethesda, MD. American Society of Health-System Pharmacists, Inc. https://www.ahfscdi.com. Accessed 09/11/2022.

Anon. Pindolol. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 09/11/2022.

Buckingham R (ed). Pindolol. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 09/11/2022.

Joint Formulary Committee. Pindolol. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 09/11/2022.

Pindolol Tablet (Marlex Pharmaceuticals, Inc). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 09/11/2022.

Pindolol. Drugs and Lactation Database (LactMed) [Internet]. Bethesda, MD. U.S. National Library of Medicine. https://www.ncbi.nlm.nih.gov/books/NBK501922. Accessed 09/11/2022.

Pindolol. Gold Standard Drug Database in ClinicalKey [online]. Elsevier Inc. https://www.clinicalkey.com. Accessed 16/11/2022.

Visken 5 mg Tablets (Amdipharm UK Limited). MHRA. https://products.mhra.gov.uk. Accessed 09/11/2022.

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