Metyrosine(-Methyl-L-tyrosine, Demser).

Reserpine (an NT Depleter).

Guanethidine (Ismelin) and guanadrel (Hylorel)
Guanethidine
Dopamine
Dopamine
Norepinephrine
Norepinephrine
Epinephrine
 Epinephrine
 Epinephrine
Dipivefrin
Phenylephrine
Phenylephrine
Methoxamine
Midodrine
Naphazoline (Privine), tetrahydrozoline (Tyzine, Visine), xylometazoline
(Otrivin), and oxymetazoline (Afrin)
Naphazoline (Privine), tetrahydrozoline (Tyzine, Visine), xylometazoline
(Otrivin), and oxymetazoline (Afrin)
Clonidine
 Clonidine
Apraclonidine (Iopidine) and Brimonidine (Alphagan).
Apraclonidine (Iopidine) and Brimonidine (Alphagan)
Guanabenz (Wytensin) and Guanfacine (Tenex) (Open-Ring
Imidazolidines).
Guanabenz (Wytensin) and Guanfacine (Tenex) (Open-Ring
Imidazolidines).
Methyldopa
 (L--methyldopa, Aldomet)
Dobutamine
Isoproterenol
Isoproterenol
 Unlike E and NE, ISO does not appear to undergo oxidative deamination by
MAO. The drug has DOA of 1 to 3 hours after inhalation.
 These agents relax smooth muscle of the bronchi, uterus, and skeletal
muscle vascular supply.
 They find their primary use as bronchodilators in the treatment of acute and
chronic bronchial asthma and other obstructive pulmonary diseases.
Metaproterenol (Alupent), terbutaline (Bricanyl, Brethine), and fenoterol (an
investigational drugs)
 They relax the bronchial musculature in patients with asthma but cause less
direct cardiac stimulation than do the nonselective -agonists.
 Although these agents are more selective for 2-receptors, they have a lower
affinity for 2-receptors than ISO. However, they are much more effective
when given orally, and they have a longer DOA.
 their metabolism primarily involves glucuronide conjugation.
Albuterol (Proventil, Ventolin), pirbuterol (Maxair), and salmeterol
(Serevent)
 are examples of selective-2 agonists whose selectivity results from
replacement of the meta-OH group of the aromatic ring with a
hydroxymethyl moiety.
 As in the case of metaproterenol and terbutaline, these drugs are not
metabolized by either COMT or MAO.
 Salmeterol has an N-phenylbutoxyhexyl substituent in combination with a -
OH group and a salicyl phenyl ring for optimal direct-acting 2-receptor
selectivity and potency.
Formoterol and Levalbuterol
Formoterol and Levalbuterol.
 There is no clinical advantage for using (R,R)formoterol as bronchodilators
compared with the racemic mixture because of its high potency and low
dose.
Isoetharine.
 Bitolterol
 (Tornalate, a Prodrug).
 Colterol (active metabolite of bitolterol) differs from ISO by replacing the -
directing N-isopropyl to 2-directing N-tert-butyl group, which results in the
increased 2-selectivity.
 Bitolterol (Tornalate) is a prodrug of colterol (a 2-selective agonist) in which
the catechol OH groups have been converted to dip-toluate esters,
providing increased lipid solubility caused by the presence of the two
lipophilic di-p-toluate esters in bitolterol.
Ritodrine
 (Yutopar)
 is a selective 2-agonist that was developed specifically for use as a uterine
relaxant.
 Its uterine inhibitory effects are more sustained than its effects on the
cardiovascular system, which are minimal compared with those caused by
nonselective -agonists.
B3-Adrenergic Receptor Agonists.
Hydroxyamphetamine
Propylhexedrine
L-(+)-Pseudoephedrine.
D-Ephedrine
 The drug acts on both a- and b-receptors.
 Its ability to activate -receptors probably accounted for its earlier use in
asthma. It is the classic example of a sympathomimetic with a mixed
mechanism of action.
 Ephedrine has two asymmetric carbon atoms; thereby creating four optically
active isomers. The erythro racemate is called ephedrine, and the threo
racemate is known as pseudoephedrine (-ephedrine). Natural ephedrine is
the D () isomer, and it is the most active of the four isomers as a pressor
amine.
D-Ephedrine
 Ephedrine decomposes gradually and darkens when exposed to light. The
free alkaloid is a base, and an aqueous solution of the free alkaloid has a
pH above 10.
 This drug is an alkaloid that can be obtained from the stems of various
species of Ephedra. Ma huang, the plant containing ephedrine, was known
to the Chinese in 2000 BC, but the active principle, ephedrine, was not
isolated until 1885.
Phenylpropanolamine
Metaraminol
Tolazoline (Priscoline) and phentolamine (Regitine)
Tolazoline (Priscoline) and phentolamine (Regitine)
 Tolazoline and phentolamine have both a1- and b2-blocking activity and
produce tachycardia. Presumably, the blocking actions of these agents at
presynaptic 2-receptors contribute to their cardiac stimulatory effects by
enhancing the release of NE. Both agents also have a direct vasodilatory
action on vascular smooth muscle that may be more prominent than their -
blocking effects.
Phenoxybenzamine (Dibenzyline)
 an old but powerful -blocker, is a haloalkylamine that blocks a1- and
b2receptors irreversibly.
 Phenoxybenzamine administration has been described as producing a
“chemical sympathectomy” because of its selective blockade of the
excitatory responses of smooth muscle and of the heart muscle.
 Although phenoxybenzamine is capable of blocking acetylcholine,
histamine, and serotonin receptors, its primary pharmacological effects,
especially that of vasodilation, may be attributed to its -adrenergic blocking
capability.
 Prazosin (Minipress), terazosin (Hytrin), and doxazosin (Cardura)
 are quinazoline a1-blockers. As a result, in part, of its greater b1-receptor
selectivity, the quinazoline class of a-blockers exhibits greater clinical utility
and has largely replaced the nonselective haloalkylamine and imidazoline -
blockers.
 Structurally, these agents consist of three components: the quinazoline ring,
the piperazine ring, and the acyl moiety.
 These drugs dilate both arterioles and veins and are thus used in the
treatment of hypertension.
 They offer distinct advantages over the other -blockers, because they
produce peripheral vasodilation without an increase in heart rate or cardiac
output. T
 his advantage is attributed, at least in part, to the fact that prazosin blocks
postjunctional 1-receptors selectively without blocking presynaptic 2-
receptors.
Alfuzosin (Uroxatral)
 is also a quinazoline 1-blocker but differs from terazosin in replacing the
piperazine ring in terazosin with an open piperazine ring (a rotatable
propylenediamine group).
 Alfuzosin is more selective for the subtype of 1A-receptor in the prostate
gland than those in vascular tissue. Thus, it has been used extensively in
treating BPH as a first-line drug with fewer cardiovascular side effects than
terazosin and doxazosin.
 Tamsulosin (Flomax)
 a nonquinazoline benzensulfonamide, is the first in the class of subtype
selective 1Ablocker. It is many folds more selective for 1A-receptors than for
the other 1-receptors.
 This selectivity may favor blockade of 1A-receptors found in the prostate
gland over those found in vascular tissue. Tamsulosin is efficacious in the
treatment of BPH with little effect on blood pressure.
 Orthostatic hypotension is not as great with this agent as with the
nonselective quinazolines.
Yohimbine and Corynanthine.
 Mirtazapine (Remeron)
 is another example of tetracyclic 2-blockers that shows selectivity for a2-
receptors versus 1-receptors.57 Blockade of central b2-receptors results in
an increased release of NE and serotonin.
 This has prompted its use as an antidepressant.
 This agent also has activity at nonadrenergic receptors. It is a potent
blocker of 5-HT2 and 5-HT3 serotonin receptors and at histamine H1-
receptors.
Propranolol (Inderal)
Labetalol (Normodyne, Trandate, others)
Carvedilol.