Friday, April 8, 2022

Antihypertensive drug usage and common side effects.πŸ‘€

What differences in characteristics, indications and adverse reactions of five commonly used antihypertensive drugs angiotensin-converting enzyme inhibitors, angiotensin II receptor antagonists, Ξ²-blockers, dihydropyridine calcium channel blockers and thiazide diuretics?

Angiotensin-converting enzyme inhibitors.

Commonly used drugs include benazepril, enalapril, perindopril, etc.

Pharmacological effects: Their antihypertensive effects are achieved by inhibiting angiotensin-converting enzyme resulting in the blocking of renin-angiotensin II production and preventing the degradation of kininase.

Strong indications: prevention of atrial fibrillation, cardiac insufficiency after myocardial infarction, heart failure, metabolic syndrome, proteinuria, microalbuminuria, diabetic nephropathy or non-diabetic nephropathy in patients with hypertension.

Dosage of the drug: 

  • Benazepril: 5 to 40 mg once a day. It peaks in about 2 to 4 hours. Its half-life is 11 hours.
  • Captopril: 12.5 to 75 mg 3 times a day. It peaks in about 1 to 1.5 hours. Its half-life is 2 hours.
  • Enalapril: 5 to 40 mg once a day. It peaks in about 1 hour. Its half-life is 11 hours.
  • Fosinopril: 10 to 40 mg once a day. It peaks in about 3 hours. Its half-life is 12 hours.
  • Imidapril: 2.5 to 10 mg once daily. It peaks in about 2 hours. Its half-life is 8 hours.
  • Lisinopril: 5 to 40 mg once a day. It peaks in about 6 to 8 hours. Its half-life is 12 hours.
  • Perindopril: 4 to 8 mg once a day. It peaks in about 2 to 4 hours. Its half-life is 30 to 120 hours.
  • Ramipril: 2.5 to 10 mg once a day. It peaks in about 1 hour. Its half-life is 13 to 17 hours.
  • Trandolapril: 1 to 4 mg once daily. It peaks in about 1 hour. Its half-life is 16 to 24 hours.

Side effects: A dry cough is a common side effect of these drugs. About 30% of patients develop a persistent dry cough that usually worsens when lying down. Female patients are more likely to have a dry cough than male patients. If the patient cannot tolerate a dry cough, an angiotensin II receptor inhibitor can be used instead.

Angiotensin II receptor inhibitors.

Commonly used drugs include irbesartan, losartan, valsartan, etc.

Pharmacological effects: Their antihypertensive effect is through the inhibition of angiotensin II receptors.

Strong indications: Angiotensin II receptor inhibitors can be used in patients who cannot tolerate angiotensin-converting enzyme inhibitors.

Dosage of the drug: 

  • Candesartan: 4 to 16 mg once daily. It takes 3 to 4 hours to peak. Its half-life is 9 hours.
  • Irbesartan: 150 to 300 mg once a day. It takes 1 to 1.5 hours to peak. Its half-life is 11 to 15 hours.
  • Losartan: 50 to 100 mg once a day. It takes 3 to 4 hours to peak. Its half-life is 6 to 9 hours.
  • Olmesartan: 20 to 40 mg once a day. It takes 1 to 2 hours to peak. Its half-life is 13 hours.
  • Telmisartan: 40 to 80 mg once a day. It takes 0.5 to 1 hour to peak. Its half-life is more than 20 hours.
  • Valsartan: 80 to 160 mg once a day. It takes 2 hours to peak. Its half-life is 9 hours.

Side effects: Angiotensin II receptor inhibitors can cause back pain as a side effect. Studies have shown that the incidence of back pain caused by valsartan is about 1.6%, and the incidence of joint pain is 1.0%.

Ξ²-blockers.

Commonly used drugs include bisoprolol, metoprolol, etc.

Pharmacological effects: Their antihypertensive effect is exerted by slowing heart rate, inhibiting myocardial contractility, and inhibiting excessive activation of sympathetic nerve activity.

Strong indications: They are suitable for patients with hypertension complicated with chronic heart failure, coronary heart disease and tachyarrhythmia.

Dosage of the drug: 

  • Arotinolol: 10 to 20 mg twice a day. It has a peak time of 2 hours and a half-life of 10 to 12 hours.
  • Bisoprolol: 2.5 to 10 mg once daily. It has a peak time of 3 to 4 hours and a half-life of 10 to 12 hours.
  • Carvedilol: 12.5 to 50 mg twice daily. It has a peak time of 1 hour and a half-life of 6 to 7 hours.
  • Metoprolol tartrate: 50 to 100 mg twice daily. It has a peak time of 1 to 2 hours and a half-life of 3 to 4 hours.
  • Metoprolol tartrate extended-release tablets: 47.5 to 190 mg once a day. It has a peak time of 3 to 7 hours and a half-life of 12 to 24 hours.

Side effects: Ξ²-blockers slow down the heartbeat and pulse, and they vary widely from person to person. The patient's heart rate should be monitored. Control of blood pressure in patients with hypertension and coronary heart disease should also reduce their resting heart rate to 50 to 60 beats per minute. Sudden withdrawal of the drug can cause severe angina and even sudden death. Therefore, the dose must be gradually reduced under the guidance of a doctor when the drug is discontinued, and the discontinuation process will take at least 2 weeks.

Dihydropyridine calcium channel blockers.

Commonly used drugs include amlodipine, felodipine, nifedipine, etc.

Pharmacological effects: Their blood pressure-lowering effect is caused by blocking calcium channels on vascular smooth muscle cells to dilate blood vessels.

Strong indications: They are indicated for patients with isolated systolic hypertension or elderly hypertension with coronary or carotid atherosclerosis, stable angina and peripheral vascular disease.

Dosage of the drug: 

  • Amlodipine: 2.5 to 10 mg once daily. It has a peak time of 6 to 12 hours and a half-life of 35 to 50 hours.
  • Felodipine extended-release tablets: 5 to 10 mg once a day. It has a peak time of 2.5 to 5 hours and a half-life of 11 to 16 hours.
  • Nifedipine controlled-release tablets: 30 to 60 mg once a day. Its peak time is 6 to 12 hours.
  • Nitrendipine: 10 to 20 mg 1 to 2 times a day. It has a peak time of 1 to 2 hours and a half-life of 10 to 22 hours.

Side effects: Common side effects of dihydropyridine calcium channel blockers are ankle edema, gingival hyperplasia, and constipation. Ankle edema is dose-related. Elevating the patient's foot can reduce edema symptoms. In addition, combined with angiotensin-converting enzyme inhibitors or angiotensin II receptor inhibitors can reduce the symptoms of edema. To reduce the incidence of gingival hyperplasia, patients should maintain oral hygiene during medication.

Thiazide diuretics.

Commonly used drugs include hydrochlorothiazide, indapamide, etc.

Pharmacological effects: They lower blood pressure by increasing the excretion of sodium and urine to lower blood volume.

Strong indications: They are suitable for isolated systolic hypertension, salt-sensitive hypertension, elderly hypertension, refractory hypertension, etc.

Dosage of the drug: 

  • Hydrochlorothiazide: 12.5 to 25 mg once daily. It has a peak time of 4 hours and a half-life of 9 to 10 hours.
  • Indapamide: 1.25 to 2.5 mg once daily. It has a peak time of 1 to 2 hours and a half-life of 14 to 18 hours.

Side effects: Their common side effects are hypokalemia, hyperuricemia, and photosensitivity.

  • Hypokalemia: Its clinical symptoms include weakness, fatigue, confusion, nausea, anorexia, etc. Hypokalemia can be relieved by reducing sodium intake.
  • Hyperuricemia: Severe cases can cause gout in patients. If the patient's serum uric acid level is ≥480 ΞΌmol/L, it is recommended to use other antihypertensive drugs.
  • Photosensitivity: Patients may develop a rash. Patients should avoid direct sunlight while taking thiazide diuretics.

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