Nitrates, Calcium Channel Blockers and Other Antianginal Drugs

Nitrates:

Glyceryl Trinitrate:

Indications: prophylaxis and treatment of angina; left ventricular failure; anal fissure; extravasation.

Contraindications: hypersensitivity to nitrates; hypotensive conditions and hypovolaemia; hypertrophic cardiomyopathy, aortic stenosis, cardiac tamponade, constrictive pericarditis, mitral stenosis; marked anaemia.

Dose and Administration:

Sublingually, 0.3–1 mg, repeated as required

By intravenous infusion, 10–200 micrograms/minute

By transdermal application, Prophylaxis of angina, apply one ‘5’ or one ‘10’ patch to lateral chest wall; replace every 24 hours, siting replacement patch on different area; max. two ‘10’ patches daily.

Isosorbide Dinitrate:

Indications: prophylaxis and treatment of angina; left ventricular failure. Contraindications: Allergic reactions to organic nitrates are extremely rare, but they do occur.

Dose and Administration: The usual starting dose is 5 mg to 20 mg, two or three times daily. For maintenance therapy, 10 mg to 40 mg, two or three times daily are recommended. Some patients may require higher doses.

Isosorbide Mononitrate:

Indications: prophylaxis of angina; adjunct in congestive heart failure. Contraindications: Allergic reactions to organic nitrates are extremely rare, but they do occur.

Dose and Administration: Initially 20 mg 2–3 times daily or 40 mg twice daily (10 mg twice daily in those who have not previously received nitrates); up to 120 mg daily in divided doses if required.

Calcium Channel Blockers:

Nifedipine:

Indications: prophylaxis of angina; hypertension; Raynaud’s phenomenon. Contraindications: cardiogenic shock; advanced aortic stenosis; within 1 month of myocardial infarction; unstable or acute attacks of angina; acute porphyria

Dose and Administration:

Hypertension, 20–30 mg once daily, increased if necessary to max. 90 mg once daily.

Angina prophylaxis, 30 mg once daily, increased if necessary to max. 90 mg once daily

Amlodipine:

Indications: treatment of hypertension. It may be used alone or in combination with other antihypertensive agents, symptomatic treatment of chronic stable angina alone or in combination with other antianginal agents.

Contraindications: cardiogenic shock, unstable angina, significant aortic stenosis; porphyria and breast-feeding.

Dose and Administration: Hypertension or angina, initially 5 mg once daily; max. 10 mg once daily.

Diltiazem:

Indications: treatment of hypertension. It may be used alone or in combination with other antihypertensive medications and management of chronic stable angina.

Contraindications: severe bradycardia, left ventricular failure with pulmonary congestion, second- or third-degree AV block (unless pacemaker fitted), sick sinus syndrome; acute porphyria; pregnancy and breast-feeding.

Dose and Administration: Angina and mild to moderate hypertension, 180– 300 mg once daily, increased if necessary to 360 mg once daily in hypertension and to 480 mg once daily in angina; elderly and in hepatic or renal impairment, initially 120 mg once daily

Nimodipine:

Indications: prevention and treatment of ischaemic neurological deficits following aneurysmal subarachnoid haemorrhage

Contraindications: within 1 month of myocardial infarction; unstable angina; porphyria.

Dose and Administration: Prevention, by mouth, 60 mg every 4 hours, starting within 4 days of aneurysmal subarachnoid haemorrhage and continued for 21 days. Treatment, by intravenous infusion via central catheter, initially 1 mg/hour (up to 500 micrograms/hour if body-weight less than 70 kg or if blood pressure unstable), increased after 2 hours to 2 mg/hour if no severe fall in blood pressure; continue for at least 5 days (max. 14 days); if surgical intervention during treatment, continue for at least 5 days after surgery; max. total duration of nimodipine use 21 days.

Verapamil:

See under treatment of Supraventricular arrhythmias.

Amlodipine and Valsartan:

Indications: treatment of hypertension also is used as initial therapy in patients who are likely to need multiple drugs to achieve their blood pressure goals

Contraindications: cardiogenic shock, unstable angina, significant aortic stenosis; porphyria, pregnency and breast-feeding.

Dose and Administration: In clinical trials with once daily (amlodipine and valsartan) using amlodipine doses of 5 mg to-10 mg and valsartan doses of 160 mg to -320 mg, the antihypertensive effects increased with increasing doses.

Other Antianginal Drugs:

Trimetazidine:

Indications: preventive treatment of episodes of angina pectoris and in ischaemia of neurosensorial tissues as in meniere`s disease.

Contraindications: pregnency and breast-feeding.

Dose and Administration: 70mg daily in two divided doses.

Ivabradine:

Indications: treatment of angina in patients in normal sinus rhythm.

Contraindications: severe bradycardia (not to be initiated if heart rate below 60 beats per minute); cardiogenic shock; acute myocardial infarction; immediately after cerebrovascular accident; sick-sinus syndrome; sino-atrial block; moderate to severe heart failure; patients with pacemaker; unstable angina; second- and third-degree heart block; congenital QT syndrome; pregnancy and breast-feeding.

Dose and Administration: Initially 5 mg twice daily, increased if necessary after 3–4 weeks to 7.5 mg twice daily (if not tolerated reduce dose to 2.5–5 mg twice daily); elderly initially 2.5 mg twice daily

Peripheral Vasodilators and Related Drugs:

Pentoxifylline:

Indications: treatment of patients with intermittent claudication on the basis of chronic occlusive arterial disease of the limbs. It may improve function and symptoms but is not intended to replace more definitive therapy, such as surgical bypass, or removal of arterial obstructions when treating peripheral vascular disease.

Contraindications: cerebral haemorrhage, extensive retinal haemorrhage, acute myocardial infarction; pregnancy and breast-feeding

Dose and Administration: 400 mg 2–3 times daily

Diosmin:

Indications: Treating hemorrhoids, Treating leg ulcers caused by poor circulation, when used in combination with hesperidin.

Contraindications: pregnancy and breast-feeding.

Dose and Administration: For the treatment of internal hemorrhoids: 1350 mg of diosmin plus 150 mg of hesperidin twice daily for 4 days followed by 900 mg of diosmin and 100 mg of hesperidin twice daily for 3 days. Some researchers also try 600 mg of diosmin three times daily for 4 days, followed by 300 mg twice daily for 10 days, in combination with 11 grams of psyllium daily. However, this lower diosmin dose does not seem to be as effective. For prevention of relapse internal hemorrhoids: 450 mg of diosmin plus 50 mg of hesperidin twice daily for 3 months of therapy. For the treatment of leg wounds due to bloodflow problems (venous stasis ulcers): the combination of 900 mg of diosmin and 100 mg of hesperidin daily has been used for up to 2 months

Beta Hydroxyethyl Rutosides:

Indications: indicated for oedema and symptoms (painful, tired, heavy, swollen legs with cramps and paraesthesia) associated with chronic venous insufficiency; postphlebitic syndrome, trophic disorders, varicose dermatitis and varicose ulcers. Also, it is indicated for symptoms of hemorrhoids (pain, exudation, pruritis and bleeding) and their complications.

Contraindications: pregnancy and breast-feeding.

Dose and Administration: 2 to 3 capsules of 300 a day with meals. After the disappearance of symptoms, usually in 2 to 4 weeks, it is advisable to continue treatment for some weeks to consolidate the results obtained.