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Three types of alkaloid. Isolysergic acid is optical isomer of lysergic acid. Clavine is
without 9-10 double bond and carboxyl.
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Vasoconstrictors! Dihydroergotamine is without 9-10 double bond and is intended for
nasal administration (rapid onset)
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Vasodilators!
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causes selective vasodilation in lungs
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weak αlpha2 antagonist as well – risk of reflexive tachycardia
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Prazosin is not in clinical use, other derivatives posses better safety profiles. Terazosin
and doxazosin has longer biological half-time (use 1x a day). Therapy of hypertension
and benign prostatic hyperplasia (BPH)
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Selective decrease of urethral and prostatic tonus. Therapy of BPH
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Urapidil is both alpha1 antagonist and central 5HT1A agonist – combined central and
peripheral antihypertensive effect
Tamsulosin selectively decreases urethral and prostatic tonus, improves bladder
function
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Alkaloid of Yohimbe tree
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R1 is substituted with lipophillic group – isopropyl, tert-butyl or arylalkyl – selectivity
towards beta receptors
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Same space orientation but different R/S name! Different groups priority!
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Non-cardioselective betablockers are contraindicated in cardiology (use only for
migrain and glaucoma therapy)
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Metipranolol – obsolent in cardiology; use for migraine prevention, stress urinary
incontinence
Cloranolol, Bufetolol – similar properties, less common
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Propranolol is used in migraine prevention
Indenalol less common, same use
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Carteolol – local application for glaucoma therapy
Nadolol – angina pectoris therapy
Bunolol / Levobunolol (pure S isomere) – local application in glaucoma therapy
Tertatolol – used for hypertension therapy
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Local application in glaucoma therapy
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Pindolol and Bopindolol (prodrug converted to dimethylpindolol) used for
hypertension therapy. Use limited to angina pectoris therapy now.
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Lipophillic compound passes through blood-brain barrier. Therapy of arrhythmias,
angina pectoris
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lipophillic compounds passes through blood-brain barrier – cerebral side-effects.
Alprenolol was used for hypertension, penbutolol for angina pectoris therapy.
Obsolent today.
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Atenolol is used for angina pectoris, myocardial infarction, arrhythmia and
hypertension therapy.
Metoprolol is widely used in same indications as atenolol, additionaly for migraine
prevention
Betaxolol posses some additional Ca2+ channel blocking effect – used for therapy of
glaucoma, angina pectoris and hypertension
Talinolol was used as antihypertensive agent.
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Celiprolol possess partial beta2 agonistic and alpha2 antagonistic effect. Used for
hypertension and angina pectoris therapy.
Acebutolol is used for angina pectoris and arrhythmia therapy
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Nebivolol possess direct vasodilating effect (nitrate-like effect). Therapy of angina
pectoris, heart insufficience.
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Used as antihypertensive and antiarrhythmic agent.
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Bisoprolol possess long biological half-time (allows 1x day administration). Used
against angina pectoris, arrhythmias, hypertension. Used in long term arrhythmia
profylaxion, after myocardium infarction.
Bevantolol posses additional alpha agonistic and Ca2+ channel blocking activity (due
to dimethoxy phenylethyl group). No renal side effects- suitable for patients with
renal insufficience. Used for treatment of angina pectoris, arrhythmias, hypertension.
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Short acting betablockers. Continual intravenous infusion application.
Esmolol – biological half-time 9min, end of effect up to 30 min. Use in acute medicine
for treating tachyarrhythmias and during myocardial infarction.
Flestolol – biological half-time 6min, not in clinical use.
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Labetalol – not selective beta and selective alpha1 blocker. Only intravenous
application. Hypertension crisis therapy, gravidity hypertension therapy.
Carvedilol – complex cardiovascular effect. non selective beta, but higher affinity for
blocking of beta1. Selective alpha1 blocker. Best mortality index, remedy of first
choice. Therapy of heart insufficience, angina pectoris, heart ischaemia and
hypertension.
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Non selective beta, selective alpha1 blocker. Used widely in Japan and South Korea.
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II. + III. class of antiarrhythmic agents (K+ channel blocker, non selective beta
blocker). Used for therapy of tachyarrhythmias.
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