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Adrenergic Pharmacology > drugs > Flashcards

drugs Flashcards

1
Q

selegiline

A

MAO inhibitor to treat depression

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2
Q

isocarboxazid

A

MAO inhibitor to treat depression

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3
Q

phenelzine

A

MAO inhibitor to treat depression

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4
Q

fenoldopam

A

an anti hypertensive agents (d1 agonist)

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5
Q

Isoproterenol

A

Highly selective for β-adrenergic receptors with little effect on the α receptors
Potent vasodilator with positive inotropic and chronotropic effects on the heart
Used for bradycardia and heart block

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6
Q

Midodrine

A

Direct-Acting Sympathomimetics
Pro-drug, metabolite (desglymidodrine) is selective alpha 1 agonist.
New, used for treatment of orthostatic hypotension”

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7
Q

Phenylephrine

A

Direct-Acting Sympathomimetics
Pure α1-selective agonist with plasma long t½ (resistance to COMT metabolism)
Nasal decongestant, mydriatic (dilation of the pupil), vasopressor and detumescent (often used to treat priapism (errection)

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8
Q

Methyldopa

A

Direct-Acting Sympathomimetics
Methyldopa is a pro-drug → alpha methyl norepinephrine
Selective agonist of (central) alpha 2 adrenergic receptors
For treatment of hypertension (methyldopa and clonidine), muscle relaxant and migraines (tizanidine)

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9
Q

Clonidine

A

Direct-Acting Sympathomimetics
Methyldopa is a pro-drug → alpha methyl norepinephrine
Selective agonist of (central) alpha 2 adrenergic receptors
For treatment of hypertension (methyldopa and clonidine), muscle relaxant and migraines (tizanidine)

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10
Q

Tizanidine

A

Direct-Acting Sympathomimetics
Methyldopa is a pro-drug → alpha methyl norepinephrine
Selective agonist of (central) alpha 2 adrenergic receptors
For treatment of hypertension (methyldopa and clonidine), muscle relaxant and migraines (tizanidine)

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11
Q

Dobutamine

A

Direct-Acting Sympathomimetics
Selective (overall) for β1 receptors but its effects are mediated by both α and β (differential effects between its two isomers)
More prominent inotropic than chronotropic effects, used in severe heart failure
In conjunction with imaging as a diagnostic agent for ischemic heart disease

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12
Q

Metaproterenol

A

Direct-Acting Sympathomimetics
Selective β2 agonists
all produce significant bronchodilation

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13
Q

Terbutaline

A

Direct-Acting Sympathomimetics
Selective β2 agonists
all produce significant bronchodilation

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14
Q

Albuterol

A

Direct-Acting Sympathomimetics
Selective β2 agonists
all produce significant bronchodilation

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15
Q

Ritodrine

A

Direct-Acting Sympathomimetics
Selective β2 agonists
all produce significant bronchodilation

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16
Q

Formoterol

A

Direct-Acting Sympathomimetics
Selective β2 agonists
all produce significant bronchodilation
Used mostly for the treatment of asthma and COPD (formoterol)
May cause hypoxia, arrhythmias and other side effects: formoterol and salmeterol are to be used only in combination with inhaled corticosteroids

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17
Q

salmeterol

A 
Direct-Acting Sympathomimetics
Selective β2 agonists
a partial agonist.
all produce significant bronchodilation
May cause hypoxia, arrhythmias and other side effects: formoterol and salmeterol are to be used only in combination with inhaled corticosteroids
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18
Q

Ephedrine

A

Mixed-Acting Sympathomimetics
Effective but non-specific adrenergic receptor agonist (activating α1, α2, β1 β2)
Occasionally used for treatment of refractory hypotension

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19
Q

Pseudoephedrine

A

Mixed-Acting Sympathomimetics
Widely used as an active ingredient in nasal decongestants
Sales of pseudoephedrine are restricted (illicit manufacture of amphetamine)

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20
Q

Amphetamine

A

Indirect-Acting Sympathomimetics
Amphetamine–like agents
Causes the release of norepinephrine and dopamine to a lesser extend. CNS stimulant and appetite suppressant

Its use and misuse are of clinical importance (military “go pill”)

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21
Q

Methamphetamine

A

Indirect-Acting Sympathomimetics
Amphetamine–like agents
Similar to amphetamine , stronger CNS effects

22
Q

Methylphenidate

A

Indirect-Acting Sympathomimetics
Amphetamine–like agents
Effective in some children with attention deficit hyperactivity

23
Q

Atomoxetine

A

Indirect-Acting Sympathomimetics

Catecholamine Reuptake Inhibitors

24
Q

Duloxetine

A

Indirect-Acting Sympathomimetics
Catecholamine Reuptake Inhibitors
Selective inhibitor of NE reuptake transporter used to treat attention deficit disorders
Causes orthostatic tachycardia and hypertension in some patients
Serotonin and norepinephrine uptake inhibitor widely used as an anti depressant
Along with milnacipran (also a serotonin and norepinephrine uptake inhibitor) approved for management of fibromyalgia

25
Q

Cocaine

A

Indirect-Acting Sympathomimetics

Catecholamine Reuptake Inhibitors

26
Q

Fenoldopam

A

Indirect-Acting Sympathomimetic
Dopamine Agonists
Treatment of severe hypertension
D1 selective (partial) agonist

27
Q

Bromocriptine

A

Indirect-Acting Sympathomimetic
Dopamine Agonists
Agonize all dopamine receptors and some serotonin receptors, but with strongest effect at D2 receptors
Mimics dopamine in the CNS, for management of Parkinson’s, pituitary adenomas with excess prolactin

28
Q

Ropinirole

A

Indirect-Acting Sympathomimetic
Dopamine Agonists
Nearly a pure D2 agonist, effective monotherapy mild Parkinson’s

29
Q

Pramipexole

A

Indirect-Acting Sympathomimetic
Dopamine Agonists
D3-selective agonist effective in conjunction with levodopa for advanced Parkinson’s
Neuroprotective effects, a plus

30
Q

Phenoxybenzamine

A

Alpha Receptor Antagonists
Irreversible blockade of alpha receptors, slightly selective for a1 than for α2
May increase cardiac output (peripheral a2 blockade, reflex tachycardia)
Treatment of pheochromocytoma (preoperative management of patients)
Side effects include: nasal stuffiness, orthostatic hypotension, tachycardia and inhibition of ejaculation

31
Q

Phentolamine

A

Alpha Receptor Antagonists
Potent alpha blocker (a1 = a2), occasionally used for treatment of pheochromocytoma, reversal of local anesthesia in soft tissues
Severe tachyarrhythmias, myocardial ischemia, erectile dysfunction

32
Q

Prazosin

A

Alpha Receptor Antagonist
Highly selective for a1 receptors, effective for management of hypertension
Dilate both arteries and veins, relative absence of tachycardia

33
Q

Terazosin

A

Alpha Receptor Antagonist
a1- selective antagonist, used for the treatment of hypertension, urinary complications associated with benign prosthetic hyperplasia (BPH)

34
Q

Doxazosin

A

Alpha Receptor Antagonist

For treatment of hypertension and BPH, long plasma t½

35
Q

Tamsulosin

A

Alpha Receptor Antagonists
More selectivea1A and a1D receptors, incline for prostate smooth muscle relax than vascular smooth muscles
Effective for treatment BPH, less orthostatic hypotension compared to others,

36
Q

Alfuzosin

A

Other Alpha Receptor Antagonist
a1-selective antagonist approved for the treatment of BPH
May cause QT prolongation in some patients

37
Q

Labetalol

A

Other Alpha Receptor Antagonist

a1-selective, and β-antagonist. Effective for control of blood pressure in patients with pre-eclampsia

38
Q

Chlorpromazine

A

Other Alpha Receptor Antagonist
Neuroleptic with significant dopamine antagonist effects
Have a antagonist effects (may contribute to their side effects)

39
Q

Haloperidol

A

Other Alpha Receptor Antagonist
Neuroleptic with significant dopamine antagonist effects
Have a antagonist effects (may contribute to their side effects)

40
Q

General Effects of Beta Receptor Antagonists
Eyes
Beta antagonists (down) intra ocular pressure , effects more prominent in glaucoma
(down) synthesis of aqueous humor

Metabolic system
(down) sympathetic-mediated lipolysis
(down) hepatic glycogenolysis (at least mediated by β2) → must be used with caution in patients with insulin-dependent diabetes mellitus
β agonists are  much safer in type 2 diabetes mellitus (less frequent episodes of hypoglycemia)
Prolonged use of β-blockers → plasma increase in VLDL and low HDL

Extra beta adrenergic effects
Metoprolol, labetalol, propranolol exhibit membrane stabilizing properties
Sotalol is an effective class 3 anti arrhythmic drug

A

just read front

41
Q

Propranolol

A

Beta Antagonists
(β1 = β2)
Prototype β-blocking drug, low and dose-dependent bioavailability
Available in sustained release preparations for long-term management of various cardiovascular diseases (hypertension, angina etc)
Timolol for glaucoma

42
Q

Nadolol

A

(β1 = β2)
Prototype β-blocking drug, low and dose-dependent bioavailability
Available in sustained release preparations for long-term management of various cardiovascular diseases (hypertension, angina etc)
Timolol for glaucoma

43
Q

Timolol

A

(β1 = β2)
Prototype β-blocking drug, low and dose-dependent bioavailability
Available in sustained release preparations for long-term management of various cardiovascular diseases (hypertension, angina etc)
Timolol for glaucoma

44
Q

Metoprolol

A

Beta Antagonists
(selective for β1)
Preferred (over non-selective blockers) in patients with diabetes mellitus
May be beneficial even in some patients with COPD, i.e. after myocardial infarction .
Nebivolol, highly selective for β1 and exhibits additional effects of vasodilation

45
Q

Atenolol

A

Beta Antagonists
(selective for β1)
Preferred (over non-selective blockers) in patients with diabetes mellitus
May be beneficial even in some patients with COPD, i.e. after myocardial infarction .
Nebivolol, highly selective for β1 and exhibits additional effects of vasodilation
Beta Antagonists
(selective for β1)
Preferred (over non-selective blockers) in patients with diabetes mellitus
May be beneficial even in some patients with COPD, i.e. after myocardial infarction .
Nebivolol, highly selective for β1 and exhibits additional effects of vasodilation

46
Q

Nebivolol

A

Beta Antagonists
(selective for β1)
Preferred (over non-selective blockers) in patients with diabetes mellitus
May be beneficial even in some patients with COPD, i.e. after myocardial infarction .
Nebivolol, highly selective for β1 and exhibits additional effects of vasodilation

47
Q

Pindolol

A

Beta Antagonists
a partial agonist at both β1 and β2 (β1 =
β2 with partial effects)
Advantages: less (decrease) in heart rate, blood pressure, abnormalities in plasma lipids etc, than with ordinary antagonists
Effective in treating hypertension and angina

48
Q

Acebutolol

A

Beta Antagonists
A partial agonist at β1 with no effect on β2, used for the management of hypertension.
May produce less bradycardia

49
Q

Carvedilol

A

Mixed Alpha-Beta Antagonists
More potent at β receptors than at a1
1 chiral center, two enantiomers with different metabolic kinetics, (R)-carvedilol is degraded by CYP2D6 → increased potential for drug interactions
Inhibits mitogenesis in vascular smooth muscles and the formation of injurious foam cells
Especially effective for treatment of chronic heart failure with decreased systolic function

50
Q

Labetalol

A

Mixed Alpha-Beta Antagonists
Two chiral centers, four enantiomers with different pharmacologic properties
Overall drug’s effect is a combination of the racemic mixture → a and β antagonist effects (slight selectivity for a1)
Treatment of hypertensive emergencies, pregnancy-induced high blood pressure
May induce hepatitis

Adrenergic Pharmacology (1 decks)

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