Sympatholytic drugs

Question 1

Sympatholytic drugs used hypertension

Answer 1

α-adrenoceptor antagonists
β-adrenoceptor antagonists
Centrally acting α2-adrenoceptor agonists

Question 2

α-adrenoceptor antagonists - cardiovascular effects

Answer 2

PVR: Decrease
Activate RAA
Left ventricular hypertrophy: Decrease

Question 3

β-adrenoceptor antagonists - cardiovascular effects

Answer 3

Cardiac output: decrease
Plasma renin activity: decrease
Left ventricular hypertrophy: decrease

Question 4

Centrally acting α2-adrenoceptor agonists - cardiovascular effects

Answer 4

PVR: Decrease
Blood volume: increase (except guanfacine)
Plasma renin activity: decrease
Left ventricular hypertrophy: decrease

Question 5

α-adrenoceptor antagonists - effect on potassium and cholesterol

Answer 5

Total cholesterol: Decrease
LDLs: Decrease
HDLs: Increase
TGs: Decrease

Question 6

α-adrenoceptor antagonists - adverse effects

Answer 6

Dizziness, first-dose syncope, fluid retention, orthostatic hypotension.
Selective α1-blockers: Reflex activation of sympathetic nervous system (increased HR, contractile force, NE levels, oxygen demand).

Question 7

β-adrenoceptor antagonists - adverse effects

Answer 7

Bradycardia, bronchoconstriction, depression, fatigue, impaired glycogenolysis, vivid dreams, orthostatic hypotension, hepatic, renal and hematopoietic toxicity. Reduced exercise capacity.

Question 8

α- and β-adrenoceptor antagonists - interactions

Answer 8

β-adrenoceptor antagonists: Cardiac depression is increased by diltiazem and verapamil. Hypotensive effect decreased by NSAIDs.
α-adrenoceptor antagonists: Hypotensive effect is increased by β-adrenoceptor antagonists and diuretics.

Question 9

Selective α1-blockers - indications and contraindication in hypertension

Answer 9

NOT initial treatment. Added to other drugs if not properly cotrolled.

Question 10

Selective α1-blockers used for HT

Answer 10

Doxazosin
Prazosin
Terazosin

Question 11

β-blockers - MOA and indications HT

Answer 11

MOA: Decrease HR and contractility, inhibit renin secretion.
Indications: HT with cardiovascular diseases (e.g. coronary heart disease)

Question 12

Carvedilol - indications in HT and reason for this indication

Answer 12

Diabetes - may improve insulin sensitivity.

Question 13

Selective β1-blockers used in HT

Answer 13

Atenolol, bisoprolol, metoprolol

Question 14

Atenolol - advantages

Answer 14

Fewer nervous system side effects

Question 15

Labetalol - indications and adverse effects

Answer 15

Indications: Chronic hypertension, hypertensive emergencies

Adverse effects: Orthostatic hypotension

Question 16

Esmolol - indication - adm - reason for indication

Answer 16

Adm IV. HT in surgery and hypertensive emergencies. Is a ultrashort-acting β1-blocker.

Question 17

Third-generation α and β-blockers

Answer 17

Carvedilol.

Nebivolol.

Question 18

Nebivolol - indications

Answer 18

HT in heart failure, diabetes, cardiac arrhythmias.

Question 19

Nebivolol - effects

Answer 19

Selective β1-blocker.
Antioxidant properties.
Increases NO from endothelial cells.

Question 20

Centrally acting sympatholytics

Answer 20

Clonidine
Guanfacine
Methyldopa

Question 21

Clonidine, guanfacine, methyldopa - adverse effects

Answer 21

Dry mouth, fatigue, rebound hypertension, sedation, decreased mental acuity. These adverse effects are milder in guanfacine than clonidine.
Methyldopa: Autoimmune hemolytic anemia, hepatitis, lupus-like syndrome.

Question 22

Clonidine, guanfacine, methyldopa - interactions

Answer 22

Tricyclic antidepressants - decrease hypotensive effect.
CNS depressants - increased sedative effect.
Methyldopa: Levodopa cause increased hypotensive effect.

Question 23

Centrally acting sympatholytics - MOA

Answer 23

Reduce sympathetic outflow by activation of central α2-adrenoceptors in medulla. This reduces vascular resistance, little effect on HR and cardiac output.

Question 24

Centrally acting sympetholytics - contra and why

Answer 24

Abrupt discontinuation - severe rebound hypertension.
Tricyclic antidepressants - block effect of these sympatholytics.
Clonidine - Not used for chronic treatment because of more side effects.

Question 25

Clonidine and methyldopa- indications

Answer 25

Hypertensive emergencies. Symptoms of alcohol, opioid or nicotine withdrawal.
Methyldopa: HT in pregnancy