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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
Cocaine
Indirect-Acting Sympathomimetics | Catecholamine Reuptake Inhibitors
26
Fenoldopam
Indirect-Acting Sympathomimetic Dopamine Agonists Treatment of severe hypertension D1 selective (partial) agonist
27
Bromocriptine
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
Ropinirole
Indirect-Acting Sympathomimetic Dopamine Agonists Nearly a pure D2 agonist, effective monotherapy mild Parkinson’s
29
Pramipexole
Indirect-Acting Sympathomimetic Dopamine Agonists D3-selective agonist effective in conjunction with levodopa for advanced Parkinson's Neuroprotective effects, a plus
30
Phenoxybenzamine
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
Phentolamine
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
Prazosin
Alpha Receptor Antagonist Highly selective for a1 receptors, effective for management of hypertension Dilate both arteries and veins, relative absence of tachycardia
33
Terazosin
Alpha Receptor Antagonist a1- selective antagonist, used for the treatment of hypertension, urinary complications associated with benign prosthetic hyperplasia (BPH)
34
Doxazosin
Alpha Receptor Antagonist | For treatment of hypertension and BPH, long plasma t½
35
Tamsulosin
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
Alfuzosin
Other Alpha Receptor Antagonist a1-selective antagonist approved for the treatment of BPH May cause QT prolongation in some patients
37
Labetalol
Other Alpha Receptor Antagonist | a1-selective, and β-antagonist. Effective for control of blood pressure in patients with pre-eclampsia
38
Chlorpromazine
Other Alpha Receptor Antagonist Neuroleptic with significant dopamine antagonist effects Have a antagonist effects (may contribute to their side effects)
39
Haloperidol
Other Alpha Receptor Antagonist Neuroleptic with significant dopamine antagonist effects Have a antagonist effects (may contribute to their side effects)
40
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
just read front
41
Propranolol
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
Nadolol
(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
Timolol
(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
Metoprolol
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
Atenolol
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
Nebivolol
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
Pindolol
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
Acebutolol
Beta Antagonists A partial agonist at β1 with no effect on β2, used for the management of hypertension. May produce less bradycardia
49
Carvedilol
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
Labetalol
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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