Drug List 5: Moa [Pharmacology I]

Front 1

Mechanism of Action for alpha-Methyltyrosine (al fa meth ill tie’ ro seen)

Back 1

Inhibits tyrosine hydroxylase, which is the rate-limiting enzyme in the catecholamine biosynthesis pathway.

Front 2

Mechanism of Action for Reserpine (re ser’ peen)

Back 2

Irreversibly damages vesicular monoamine transporters (VMAT-1 & VMAT-2) that concentrate NE, serotonin, & dopamine in vesicles, thus leading to their depletion in adrenergic terminals via intraneuronal, mitochondrial MAO metabolism.

Front 3

Mechanism of Action for Guanethidine (gwahn eth’ i deen)

Back 3

Guanethidine, like guanadrel, is actively transported into neurons by NET, where it concentrates in transmitter vesicles, displacing NE, leading to a gradual depletion of NE.

Front 4

Mechanism of Action for Guanadrel (gwhan’ a drel)

Back 4

Guanadrel, like guanethidine, is actively transported into neurons by NET, where it concentrates in transmitter vesicles, displacing NE, leading to a gradual depletion of NE.

Front 5

Mechanism of Action for Amphetamine (am fet’ a meen)

Back 5

Amphetamine displaces endogenous catecholamines from storage vesicles, weakly inhibits MAO, and blocks catecholamine reuptake mediated by NET and DAT.

Front 6

Mechanism of Action for Methylphenidate (meth il fen’ i date)

Back 6

Like amphetamine, methylphenidate is said to displace endogenous catecholamines from storage vesicles, to weakly inhibit MAO, and to block catecholamine reuptake mediated by NET and DAT.

Front 7

Mechanism of Action for Pseudoephedrine (soo doe e fed’ rin)

Back 7

Pseudoephedrine displaces NE from pre-synaptic vesicles, causing NE release into the neuronal synapse where it activates postsynaptic alpha-receptors located on the muscles lining the walls of blood vessels, causing vasoconstriction, which allows less fluid to leave the blood vessels and enter the nose, throat, & sinus linings, thereby decreasing the inflammation of nasal membranes and the production of mucus.

Front 8

Mechanism of Action for Cocaine (koe kane’)

Back 8

Cocaine inhibits norepinephrine transporter (NET) allowing NE to remain in the synaptic cleft longer, thus potentiating neurotransmission at adrenergic synapses.

Front 9

Mechanism of Action for Amitriptyline (a mee trip’ ti leen)

Back 9

Amitriptyline, like imipramine, inhibits reuptake of serotonin and norepinephrine by blocking serotonin transporter (SERT) and norepinephrine transporter (NET), thus facilitating their accumulation in the synaptic cleft.

Front 10

Mechanism of Action for Imipramine (im ip’ ra meen)

Back 10

Imipramine, like amitriptyline, inhibits reuptake of serotonin and norepinephrine by blocking serotonin transporter (SERT) and norepinephrine transporter (NET), thus facilitating their accumulation in the synaptic cleft.

Front 11

Mechanism of Action for Iproniazid (eye pro neye’ ah zid)

Back 11

Iproniazid, like phenelzine & tranylcypromine, nonselectively and irreversibly inhibits both MAO-A & MAO-B, thereby increasing catecholamine levels by blocking catecholamine degradation.

Front 12

Mechanism of Action for Phenelzine (fen’ el zeen)

Back 12

Phenelzine, like iproniazid & tranylcypromine, nonselectively and irreversibly inhibits both MAO-A & MAO-B, thereby increasing catecholamine levels by blocking catecholamine degradation.

Front 13

Mechanism of Action for Tranylcypromine (tran il sip’ roe meen)

Back 13

Tranylcypromine, like iproniazid & phenelzine, nonselectively and irreversibly inhibits both MAO-A & MAO-B, thereby increasing catecholamine levels by blocking catecholamine degradation.

Front 14

Mechanism of Action for Moclobemide (moe kloe’ be mide)

Back 14

Moclobemide, like befloxatone & brofaromine, is a Reversible Inhibitor of Monoamine Oxidase A (a medication class referred by the acronym RIMA).

Front 15

Mechanism of Action for Befloxatone (be flocks’ a tone)

Back 15

Befloxatone, like moclobemide & brofaromine, is a Reversible Inhibitor of Monoamine Oxidase A (a medication class referred by the acronym RIMA).

Front 16

Mechanism of Action for Brofaromine (bro fare’ o meen)

Back 16

Brofaromine, like moclobemide & befloxatone, is a Reversible Inhibitor of Monoamine Oxidase A (a medication class referred by the acronym RIMA).

Front 17

Mechanism of Action for Selegiline (se le’ ji leen)

Back 17

Selective, irreversible MAO-B inhibitor.

Front 18

Mechanism of Action for Methoxamine (meth ox’ a meen)

Back 18

Methoxamine is a systemically-administered, selective, alpha1-receptors agonist used to increase peripheral vascular resistance.

Front 19

Mechanism of Action for Phenylephrine (fen il ef’ rin)

Back 19

Phenylephrine, like oxymetazoline & tetrahydrazoline, is a selective alpha1-receptor agonist.

Front 20

Mechanism of Action for Oxymetazoline (ok” see met az’ oh leen)

Back 20

Oxymetazoline, like phenylephrine & tetrahydrazoline, is a selective alpha1-receptor agonist.

Front 21

Mechanism of Action for Tetrahydrazoline (teh truh hi droze' oh leen)

Back 21

Tetrahydrazoline, like phenylephrine & oxymetazoline, is a selective alpha1-receptor agonist.

Front 22

Mechanism of Action for Clonidine (kloe’ ni deen)

Back 22

Clonidine, like guanabenz & glunfacine, selectively activates central alpha2-autoreceptors, thereby inhibiting sympathetic outflow from the CNS.

Front 23

Mechanism of Action for Guanabenz (gwahn’ a benz)

Back 23

Guanabenz, like clonidine & guanfacine, selectively activates central alpha2-autoreceptors, thereby inhibiting sympathetic outflow from the CNS.

Front 24

Mechanism of Action for Guanfacine (gwahn’ fa seen)

Back 24

Guanfacine, like clonidine & guanabenz, selectively activates central alpha2-autoreceptors, thereby inhibiting sympathetic outflow from the CNS.

Front 25

Mechanism of Action for Methyldopa (meth ill doe’ pa)

Back 25

Inhibits aromatic L-amino acid decarboxylase, which is the enzyme responsible for converting DOPA to Dopamine. Its metabolite, methylnorepinephrine, selectively activates central alpha2-autoreceptors, thereby inhibiting sympathetic outflow from the CNS.

Front 26

Mechanism of Action for Isoproterenol (eye soe proe ter’ e nol)

Back 26

Isoproterenol is a nonselective beta-receptor agonist having a higher potency for these receptors than epinephrine (which is has a higher potency than norepinephrine).

Front 27

Mechanism of Action for Dobutamine (doe byoo’ ta meen)

Back 27

Dobutamine is a selective, beta1-receptor agonist.

Front 28

Mechanism of Action for Metaproterenol (met a proe ter’ e nole)

Back 28

Metaproterenol is a selective, beta2-receptor agonist.

Front 29

Mechanism of Action for Terbutaline (ter byoo’ ta leen)

Back 29

Terbutaline, as well as albuterol, selectively activates beta2-receptors, and thus causes fewer cardiac effects than less selective adrenergic agonists.

Front 30

Mechanism of Action for Albuterol (al byoo’ ter ole)

Back 30

Albuterol, as well as terbutaline, selectively activates beta2-receptors, and thus cause fewer cardiac effects than less selective adrenergic agonists.

Front 31

Mechanism of Action for Salmeterol (sal me’ te role)

Back 31

Salmeterol is a long-acting, beta2-receptor agonist (LABA) with a duration of action lasting 12 to 24 hrs.

Front 32

Mechanism of Action for Phenoxybenzamine (fen ox ee ben’ za meen)

Back 32

Phenoxybenzamine irreversibly blocks both alpha1- & alpha2-receptors (alpha1 > alpha2).

Front 33

Mechanism of Action for Phentolamine (fen tole’ a meen)

Back 33

Phentolamine is a reversible, nonselective alpha-receptor antagonist

Front 34

Mechanism of Action for Prazosin (pra’ zoe sin)

Back 34

Prazosin, like terazosin & doxazosin, is a selective antagonist of alpha1-receptors in arterioles and veins (1000-fold greater affinity for alpha1 than alpha2)

Front 35

Mechanism of Action for Terazosin (ter ay’ zoe sin)

Back 35

Terazosin, like prazosin & doxazosin, is a selective antagonist of alpha1-receptors in arterioles and veins. Like doxazosin, it has a longer half-life than prazosin, allowing less frequent dosing.

Front 36

Mechanism of Action for Doxazosin (dox ay’ zoe sin)

Back 36

Doxazosin, like prazosin & terazosin, is a selective antagonist of alpha1-receptors in arterioles and veins. Like terazosin, it has a longer half-life than prazosin, allowing less frequent dosing.

Front 37

Mechanism of Action for Tamsulosin (tam soo’ loe sin)

Back 37

Tamsulosin is a subtype-selective alpha1A-receptor antagonist that has more specificity towards smooth muscle in the genitourinary tract. Hence it has a lower incident of orthostatic hypotension than prazosin, terazosin, or doxazosin.

Front 38

Mechanism of Action for Yohimbine (yo him’ bean)

Back 38

Yohimbine blockades alpha2-autoreceptors, which leads to increased release of NE (stimulating cardiac beta1-receptors and peripheral vasculature alpha1-receptors) and causes increased insulin release through blockade of suppressive alpha2-receptors in the pancreatic islets.

Front 39

Mechanism of Action for Propranolol (proe pran’ oh lole)

Back 39

Propranolol is a lipophilic, nonselective beta blocker having relatively equal affinity for beta1- & beta2-receptors.

Front 40

Mechanism of Action for Nadolol (nay doe’ lole)

Back 40

Nadolol is a nonselective beta blocker having a relatively long half-life and a relatively equal affinity for beta1- & beta2-receptors.

Front 41

Mechanism of Action for Timolol (tye’ moe lole)

Back 41

Timolol is a nonselective beta blocker having a relatively short half-life and a relatively equal affinity for beta1- & beta2-receptors.

Front 42

Mechanism of Action for Labetalol (la bet’ a lole)

Back 42

Labetalol blocks alpha1-, beta1-, & beta2-receptors. Although it also acts as a weak, partial agonist of beta2, it has a 5- to 10-fold greater effect as a beta-blocker.

Front 43

Mechanism of Action for Carvedilol (kar’ ve dil ol)

Back 43

Carvedilol blocks alpha1-, beta1-, & beta2-receptors.

Front 44

Mechanism of Action for Pindolol (pin’ doe lole)

Back 44

Pindolol is a nonselective beta-receptor antagonist having partial agonist activity at both beta1- & beta2-receptors, which attenuates its antagonistic effect, making it useful for treating hypertensive patients who have bradycardia or decreased cardiac reserve.

Front 45

Mechanism of Action for Acebutolol (a se byoo’ toe lole)

Back 45

Acebutolol is a selective beta1-receptor antagonist having partial agonist activity, which makes it more suitable than noncardioselective beta blockers for the treatment of hypertensive patients who also have asthma or COPD.

Front 46

Mechanism of Action for Esmolol (es’ moe lol)

Back 46

Esmolol is a selective, beta1-receptor antagonist having a rapid onset of action and a very short duration of action, which makes it useful for emergency beta-blockade in the treatment in thyroid storm or in suspected aortic dissection, as examples.

Front 47

Mechanism of Action for Metoprolol (me toe’ proe lole)

Back 47

Metoprolol is a selective, beta1-receptor antagonist having an intermediate half-life (4 to 9 hrs).

Front 48

Mechanism of Action for Atenolol (a ten’ oh lole)

Back 48

Atenolol is a selective beta1-receptor antagonist have an intermediate half-life (4 to 9 hrs).

Front 49

Mechanism of Action for Celiprolol (see’ li proe lole)

Back 49

Celiprolol is a selective beta1-receptor antagonist and a selective beta2-receptor agonist.