Antihypertensive drugs, pharmacology

1. Antihypertensive
drugs for primary
care physician
DOMINA PETRIC, MD

2. 1.) Centrally acting antiadrenergic agents
Imidazole receptors
selective agonists:
•moxonidinum
•guanfacine (for ADHD)

3. Moxonidinum 0,2 mg or 0,4 mg tbl.
▪ For treatment of arterial hypertension.
▪ Start dose is 0,2 mg per os a day.
▪ Maximum dose is 0,6 mg per os a day divided in two doses.
▪ It can be taken with or without food.
▪ Contraindications are hypersensitivity, sick sinus syndrome,
bradycardia (<50 bmp), AV block of II. and III. degree, heart
insufficiency.
▪ It is not recommended to use it with tricyclic antidepressants and
benzodiazepines. It is not recommended during pregnancy and
lactation.

4. 2.) Peripherally acting antiadrenergic agents
Alfa adrenergic
receptors blocators:
•doxazosinum
•urapidilum

5. Doxazosinum 2 mg or 4 mg tbl.
▪ Indicated for arterial hypertension as monotherapy or in
combination with tiazide diuretics, beta-blockers, calcium
antagonists or ACE-i.
▪ It is also indicated for treatment of symptoms in benign prostatic
hyperplasia.
▪ Start dose for arterial hypertension treatment is 1 mg.
▪ Maintenance dose is 2-4 mg per os a day.
▪ Maximum daily dose is 16 mg.
▪ Contraindicated in hypotension and lactation.

6. Urapidilum
Ebrantil 25 mg/50 mg ampulla
▪ for iv. application
▪ hypertensive crisis
▪ refractory hypertension
▪ 10-50 mg iv. slowly
▪ arterial blood pressure
monitoring is obligatory
Ebrantil 60 mg/90 mg tbl.
▪ for treatment of arterial
hypertension in adults
▪ 30 mg per os twice a day for
slowly lowering blood pressure
▪ 60 mg per os twice a day for
more rapidly lowering RR
▪ 60-180 mg per os a day is
maintenance dose

7. Urapidilum
▪Contraindicated in pregnancy and
lactation.
▪Not recommended (caution is
mandatory) for children and patients
with heart, kidney or liver failure.
▪Caution also with older patients and
patients taking cimetidine.

8. DIURETICS
3.)

9. A) Low threshold diuretics, sulphonamides

10. Chlortalidonum (Hygroton 25 mg tbl.)
Indications are:
▪ arterial hypertension (esential, nephrogenic,
systolic)
▪ chronic heart failure (NYHA II or III)
▪ ascites (liver cyrosis in stable patients)
▪ oedemas in nephrotic sydrome
▪ diabetes insipidus

11. Chlortalidonum (Hygroton 25 mg tbl.)
▪ For arterial hypertension daily dose is 25 mg per os.
▪ Dose can be increased up to 50 mg per os a day.
▪ For heart failure dose is 25-50 mg per os a day, but the
dose can be increased up to 100-200 mg per os a day.
▪ For diabetes insipidus start dose is 100 mg twice a day and
then maintenance dose should be 50 mg a day.
▪ Contraindications are hypersensitivity, anuria, severe
kidney failure (ClCr <30 mL/min), hypokalemia,
hyponatremia, hypercalcemia, gout, hypertension during
pregnancy.

12. Indapamidum (1,5 mg tbl.)
▪Indicated for treatment of esential
hypertension in adults.
▪Dose is 1,5 mg per os a day taken with glass
of water in the morning.
▪Contraindications are hypersensitivity,
severe kidney failure, hepatic
encephalopathy or severe liver damage,
hypokalemia.

13. B) High treshold diuretics, sulphonamides

14. Furosemidum
(40 mg tbl., 500 mg tbl., 40 mg/4 mL ampulla for iv.
application)
▪ Indicated for treatment of oedemas caused with heart or liver
failure, oedemas in kidney diseases and arterial hypertension.
▪ Start dose is usually 40 mg and can be increased on 80 mg or
even on 160 mg per os a day depending on the severity of the
heart/liver/kidney failure.
▪ Diuresis (with furosemid) should not be more than 1 kg a day.
▪ High treshold diuretics better act when the daily dose is divided
into two or three doses taken every 12 hours (or 8 hours if three
doses, or 6 hours if four doses needed).
▪ For arterial hypertension dose is 40 mg a day.

15. Furosemidum
▪ Tablet should be taken on the empty stomach
with lots of water.
▪ Contraindications are hypersensitivity, kidney
insufficiency with anuria not responding on this
medication, hepatic coma, severe hypokalemia or
hyponatremia, hypovolemia or dehydration,
during lactation.

16. Furosemidum 500 mg tbl. (Edemid forte)
▪ prevention of acute kidney insufficiency in patients with
GF<20 mL/min
▪ chronic kidney insufficiency before dialysis
▪ patent with fluid retention and very high blood pressure
▪ nephrotic syndrome (together with albumins infusion)
▪ resistent congestive heart failure
Dose varies from 250 mg a day up to 2000 mg per os a
day!

17. C) Potassium sparing diuretics, aldosterone
antagonists

18. Spironolactonum 25 mg, 50 mg and 100 mg tbl.
▪Indications are primary hyperaldosteronism,
oedemas and ascites in conditions with
secondary hyperaldosteronism.
▪Dose is 50-100 mg per os a day.
▪Contraindications are anuria, acute kidney
failure, hyperkalemia, hyponatremia,
pregnancy and lactation.

19. Eplerenonum 25 mg and 50 mg tbl.

20. Beta adrenergic
receptors blockers
4.)

21. A) Non-selective beta adrenergic blocators

22. Propranololum 40 mg tbl.
▪ after acute myocardial infarction
▪ prophylaxis of stenocardic pain in patients with chronic stable
angina pectoris
▪ arterial hypertension (alone or in combination, usually with tiazide
diuretics)
▪ prevention of bleeding in portal hypertension
▪ pheochromocytoma
▪ esential tremor
▪ migraine

23. Propranololum 40 mg tbl.
▪For arterial hypertension start dose is 80 mg
per os twice a day.
▪ Overall daily dose can vary from 160 mg up to 320 mg.
▪ Contraindications are hypersensitivity, bronchial spasm
(asthma, COPD), severe sinus bradycardia (heart rate
<50 bmp), Prinzmetal´s angina, cardiogenic shock, right
heart failure caused with pulmonary hypertension,
severe heart failure, severe hypotension, risk of
hypoglicemia...

24. B) Selective beta adrenergic blockers
▪ atenololum
▪ metoprololum
▪ bisoprololum
▪ esmololum
▪ nebivololum

25. Bisoprololum 2,5 mg, 5 mg, 10 mg tbl.
▪ Treatment of arterial hypertension, angina pectoris, stable chronic
heart failure with left ventricular systolic dysfunction.
▪ Start dose for arterial hypertension is 5 mg per os a day.
▪ Maintenance dose is 10 mg a day, maximum dose is 20 mg a day.
Dose in stable chronic heart failure should be titrated:
▪ 1,25 mg a day for a week
▪ 2,5 mg a day for a week
▪ 3,75 mg a day for a week
▪ 5 mg a day during next four weeks
▪ 7,5 mg a day during next four weeks
▪ 10 mg a day is maintenance dose

26. Contraindications:
▪ acute heart failure
▪ cardiogenic shock
▪ AV block of II. and III. degree without pacemaker
▪ sick sinus syndrome
▪ symptomatic bradycardia, symptomatic hypotension
▪ severe bronchial asthma or COPD
▪ metabolic acidosis
All beta adrenergic blockers should be taken carefully if patient is
diabetic!

27. Calcium inhibitors
V.)

28. Dihydropyridine derivatives
▪ amplodipinum
▪ lercanidipinum
▪ nifedipinum
▪ lacidipinum
▪ felodipinum

29. Lercanidipinum 10 mg or 20 mg tbl.
▪Indication is mild to moderate esential
arterial hypertension.
▪Daily dose is 10 mg per os 15 minutes
before meal with glass of water.
▪Dose can be increased up to 20 mg.
▪Lercanidipinum causes less peripheral
oedemas than other dihydropyridine
derivatives.

30. Renin angiotensin system
agents
VI.)

31. A) ACE-inhibitors
▪ quinaprilum
▪ lisinoprilum
▪ ramiprilum
▪ perindoprilum
▪ cilazaprilum
▪ trandolaprilum
▪ ...

32. Ramiprilum 1,25 mg, 2,5 mg, 5 mg, 10 mg tbl.

33. Contraindications:
▪ hypersensitivity
▪ angioedema in family anamnesis
▪ bilateral renal artery stenosis
▪ second and third trimester of pregnancy
▪ severe hypotension
▪ haemodinamic instability

34. B) Angiotensin II antagonists
▪ irbesartan
▪ candesartanum
▪ losartanum
▪ valsartanum
▪ azilsartan medoximil
▪ ...

35. Literature:
Mediately
HALMED