Exam 4: Drugs Flashcards

(86 cards)

1
Q

Resperine

A
  1. Blocks VMAT of NE and DA
  2. Used to deplete nerve ending of NE
  3. Allows fall in BP, but lots of ADRs

Hypertension, Insanity

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2
Q

Amphetamine

A

Indirect Acting Sympathomimetics
1. Non-catechol
2. a-methyl reduces MAO activity
3. Absorbs well, CNS stimulant, unchanged in urine

MOA
1. Ca2+ independent release of neurotransmitter
2. Competitive reuptake inhibitor, weak MAO inhibitor
3. Narcolepsy

SE
1. Hypertension
2. Tachycardia
3. Dependence
4. Psychosis

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3
Q

Tyramine

A

Indirect Acting Sympathomimetics
1. Displaces NE from synaptic vesicles to synapse
2. Ca2+ independent
3. Metabolized by MAO

SE
Hypertensive crisis in patients with MAO inhibitors

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4
Q

Ephedrine/Pseudophedrine

A

Indirect Acting Sympathomimetics
1. Nasal decongestion
2. Long-acting catechol with oral bioavailability
3. Can be both direct and indirect acting

MOA
1. CNS
2. Releases catecholamines from nerve terminals
2. Some direct stimulation of a and b receptors

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5
Q

Phenylpropanolamine

A

Indirect Acting Sympathomimetics
1. Non-cat
2. Less CNS than ephedrine
3. OTC diet prep and nasal decongenstion

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6
Q

Cocaine

A

Reuptake Inhibitor
1. Inhibits Uptake 1 inhibitor, slow uptake, high affinity
2. Block NE, DA, 5HT reuptake

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7
Q

What are the clinical uses for Indirect Acting Sympathomimetics?

A
  1. ADHD
  2. Narcolepsy
  3. Obesity
  4. Drug of abuse
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8
Q

Methylphenidate (Ritalin, Metadate, Daytrana, Concerta, Quillivan, others)

A

Reuptake inhibitor
1. CNS stimulant
2. Blocks 50% of DAT and increases extracellular DA and NE
3. ADHD by improving attention and decrease distractibility
4. Narcolepsy

SE
1. Insomnia
2. Anorexia
3. Weight loss

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9
Q

Concerta

A

Methylphenidate that has osmotic release using OROS

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10
Q

Atomoxetine (Strattera, NON stimulant)

A

Norepinephrine reuptuke inhibitor
1. Less abusive
2. Non-stimulant ADHD med

SE
1. Nausea dyspepsia
2. Sleep disturbances
3. Suicidal thought

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11
Q

Side effects for amphetamine and stimulant medication?

A
  1. Insomnia
  2. Anorexia
  3. Weight loss
  4. GI upset
  5. Precipitation or exacerbation of tics
  6. Abuse (hallucinations, panic, suicidal thoughts)
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12
Q

Methylamphetamine (Desoxyn)

A

ADHD CNS stimulant

Stimulant side effects

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13
Q

Dextroamphetamine (Dexedrine)

A

ADHD CNS stimulant

Stimulant side effects

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14
Q

Lisdexamfetamine (Vyvanse)

A

ADHD CNS stimulant
Prodrug of dextroamphetamine activated by liver after ingestion
Stimulant side effects

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15
Q

Mixed Salts (Adderall)

A

ADHD CNS stimulant
Stimulant side effects

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16
Q

Dexmethylphenidate (Focalin)

A

ADHD CNS stimulant
Stimulant side effects

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17
Q

Dextroamphetamine (Dexedrine)

A

Reuptake inhibitor
1. Increases release of NE and DA from nerve terminal and inhibits reuptake
2. Appetite suppression
3. Stimulant weight loss drug

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18
Q

Phentermine (Adipex-P)

A

Reuptake inhibitor
1. Increases release of NE and DA from nerve terminal and inhibits reuptake
2. Appetite suppression
3. Stimulant weight loss drug

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19
Q

Benzphetamine (Didrex)

A

Reuptake inhibitor
1. Increases release of NE and DA from nerve terminal and inhibits reuptake
2. Appetite suppression
3. Stimulant weight loss drug

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20
Q

Diethylpropion (Tenuate)

A

Reuptake inhibitor
1. Increases release of NE and DA from nerve terminal and inhibits reuptake
2. Appetite suppression
3. Stimulant weight loss drug

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21
Q

Phendimetrazine (Bontril)

A

Reuptake inhibitor
1. Increases release of NE and DA from nerve terminal and inhibits reuptake
2. Appetite suppression
3. Stimulant weight loss drug

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22
Q

Lorcaserin (Belviq)

A

Non-ampetamine appetite suppressant for long term use

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23
Q

Phentermine

A

New weight loss stimulant

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24
Q

Phenylephrine (Neo-Synephrine, Sudafed PE)

A

a-1 agonist
Non-catechol
Nasal decongestant
Mydriatic agent not cycloplegia
Increased BP causing reflex bradycardia from increased vagal response (PNS)

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25
Metaraminol (Aramine)
Mixed acting a1 agonist 1. a-1 direct agonist effect 2. Minor indirect agonist for some b1 responses 3. Increase BP IV Vasopressor
26
Mephentermine
Mixed acting a1 agonist 1. a-1 direct agonist effect 2. Minor indirect agonist for some b1 responses 3. Increase BP IV Vasopressor
27
Methoxamine
Mixed acting a1 agonist 1. a-1 direct agonist effect 2. Minor indirect agonist for some b1 responses 3. Increase BP IV Vasopressor
28
Midodrine (Orvaten)
a-1 agonist Prodrug converted to desglymidodrine Symptomatic orthostatic hypotension
29
Hydroxyamphetamine + tropicamide (Paremyd)
a-1 agonist Mydriatic agent
30
Droxidopa (Northera)
1. Prodrug of NE and E which metabolized in neurons by AADC to NE 2. Increases NE and E in PNS and CNS 3. Increases HR and BP Orthostatic hypotension (neurogenic)
31
Norepinephrine
Inotropic and vasopressor Shock Enhance CO and PVR
32
Tetrahydrozoline (Visine)
a-1 agonist imidazole derivative Ophthalmic and nasal
33
What are a-1 agonist therapeutical treat?
1. Hypotension 2. Shock
34
Clonidine (Catapres)
a-2 agonist Long duration of action (t1/2=12-16hr) ADHD Hypertension
35
Guanfacine (Tenex. Intuniv)
a-2 agonist 1. More slective than clonidine\ ADHD Sleepiness and dry mouth
36
Brimonidine (Alphagan P)
a-2 agonist Inhibit sympathetic tone, decreasing aqueous humor Increases uveoscleral outflow Chronic treatment for glaucoma
37
Apraclonidine (Iopidine)
a-2 agonist Short term treatment for reducing IOP Prevention and treatment of postsurgical intraocular pressure elevations
38
a-methyldopa (Aldomet)
a-2 agonist False neurotransmitter taken up by neurons Acculumates in synaptic vescicles Released by NE nerve terminals Hypertension in pregnancy
39
Oxymetazoline (Afrin)
a-1 agonist imidazole derivative Ophthalmic and nasal
40
Dexmedetomidine (Precedex)
a2 agonist ICU sedation Procedural sedation
41
Isoproterenol
Beta non-selective agonist Cardio-stimulatory Vasodilation
42
What ANS causes bronchodilation?
Sympathetic stimulation (E)
43
What ANS causes bronchoconstriction?
Cholinergic
44
Purpose of B2 selective agents?
1. Relaxes bronchial airways smooth muscle 2. Stabilizes mast cells
45
Albuterol (Proventil HFA)
b2 agonist Gold standard Racemic mixture SABA SE: tremors and tachycardia Oral and inhalationt (asthma)
46
Levalbuterol (Xopenex)
b2 agonist R-enantiomer of albuterol SABA SE: tremors and tachycardia Inhaler, nebulized solution
47
Terbutaline (Brethine)
b2-agonist SABA Tocolytic agent, relaxes uterine Phenyl ring modifications to decrease COMT metabolism Oral and parenteral preparationt for bronchospasms and status asmaticus
48
Salmeterol (Serevent Diskus)
B2 agonist LABA Onset: 15-30min Duration: 12 hr Combo with Fluticasone Inhalation (powder) therapy: not prn (rescue inhaler)
49
Vilanterol (+Umeclidinium, Anoro Ellipta)
b2-agonist Ultra-LABA Asmtha COPD agent
50
Indacaterol (Arcapta Neohaler)
b2-agonist Ultra-LABA COPD agent
51
Olodaterol (Striverdi Respimat)
b2-agonist Ultra-LABA COPD agent
52
B2-agonist therapeutic use
Asthma and COPD Bronchodilation
53
B2-agonist ADR
Tremors
54
Dobutamine (Dobutrex)
b1 agonist Cardiac decompensation (cardiogenic shock)
55
Mirabegron (Myrbetriq)
b3 agonist Moderate inhibitor of CYP2DP Increases bladder capacity relaxing detrusor smooth muscle Over active bladder SE: High BP, tachycardia (not recommended for those with hypertension)
56
Vibegron (Gemtesa)
b3 agonist Increases bladder capacity OAB (no BP effects)
57
Epinephrine
Nonselective, raises BP, bronchodilation Acute anaphylatic reactions
58
Phentolamine (Regitine, Oraverse)
Mixed a1 and a2 competitive antagonist Decreases PVR therefore decreasing BP Hypertension
59
Phenoxybenzamine (Dibenzyline)
Irreversible a antagonist 1. Covalently binds to receptors 2. Blocks ACh, histamine 3. Long acting oral med
60
Prazosin (Minipress)
Reversible a1 antagonist 1. Less cardiac stimulation by preserving a2 negative feedback 2. Less tachycardia 3. First dose may cause orthostatic hypotension 4. Relaxes prostate and reduces urethreal resistance to flow BPH
61
Terazosin (Hytrin)
a1 antagonist Oral 90% bioavailablity Relaxes prostate and reduces urethreal resistance to flow Hypertension, BPH
62
Doxazosin (Cardura)
a1 antagonist Oral 60% bioavalability Hypertension, BPH
63
Tamsulosin (Flomax)
a1-A (prostate) blocker over a1-B (vasculature) Relaxes prostate and reduces urethreal resistance to flow BPH
64
Silodosin (Rapaflo)
1. Highly selective a1-A blocker than B 2. High uroselectivity, and positive cardiovascular safety profile BPH
65
Alfuzosin (Uroxatral)
a1-blocker Some uroselectivity which leads to lower incidence of ejaculatory dysfunction (50% bioavailability) BPH
66
Pindolol (Visken)
b partial agonist 1. Low concentration: slight activation of receptors 2. High concentrations: antagonist and ISA function 3. MSA
67
Propranolol (Inderal)
Nonselective beta blocker (MSA) 1. High first pass metabolism 2. Highly lipid soluble (CNS) - causing migraines 3. Block Na+ channels in heart and neurons 1. Membrane stabilizing activity 2. Portal hypertension 3. Cirrhosis prevent visceral bleeding
68
Pindolol (Visken)
b partial agonist 1. Low concentration: slight activation of receptors 2. High concentrations: antagonist and ISA function 3. MSA
69
Nadolol (Corgard)
Nonselective beta blocker 1. Low lipid solubility 2. Long duration of action 3. Avoid abrupt cessation
70
Sotalol (Betapace)
Nonselective beta blocker 1. Low lipophilicity 2. Blocks potassium channels in heart HTN and ventricular arrythmia
71
Sotalol AF (Betapace AF)
Nonselective beta blocker 1. Low lipophilicity 2. Blocks potassium channels in heart Artrial fibrillation
72
Timolol (Blocadren, Timoptic, and Betimol)
Nonselective beta blocker 1. Decreases aqueous humor production 2. Excellent ocular hyportensive effect Glaucoma HTN post-MI angina Prophylaxis of migraine
73
Carteolol (Cartrol)
Nonselective b blocker 1. Low lipid solubility 2. ISA activity Glaucoma
74
Levobunolol (Betagan)
Nonselective b blocker Glaucoma
75
Carvedilol (Coreg)
Mixed a1 and nonselective b-blocker (no ISA) 1. a1: Decrease in PVR, preload, afterload 2. Increased ventricular function CHF and Antioxidant SE: orthostatic hypotension, fatigue, bradycardia
76
Labetalol (Trandate)
Mixed a1 and nonselective b-blocker, partial agonist at b2 (ISA) 1. MSA 2. May cause liver damage or hepatocellular injury Hypertension
77
Metoprolol (Toprol XL)
b1 antagonist 1. Lipid soluble 2. MSA 3. Avoid abrupt cessation
78
Atenolol (Tenormin)
b1 antagonist 1. Low lipid solubility 2. Prophylaxis of migraine 3. Avoid abrupt cessation
79
Esmolol (Brevibloc)
b1 antagonist 1. Rapid metabolism (8min) 2. IV Prep only
80
Esmolol (Brevibloc)
b1 antagonist 1. Rapid metabolism (8min) 2. IV Prep only Acute supraventricular tachycardia Hypertensive emergency
81
Acebutolol (Sectral)
b1 antagonist 1. Hydrolysis to active metabolite (diacetolol) 2. ISA 3. MSA
82
Betaxolol (Betoptic, Kerlone)
b1 antagonist Ophthalmic: glaucoma Oral: HTN
83
Bisoprolol (Zebeta)
b1 antagonist HTN once a day dosing
84
Nebivolol (Bystolic)
b1 antagonist 1. Nitric oxide potentiativng vasodilatory effect Antioxidants HTN once/day dosing
85
Dopamine
Inotropic and vasopressor 1. DA1 receptors enhance blood flow to renal 2. Inhibiton of Na+/K+ ATPase for tubule reabsoprtion (large infusions) 3. Increased cardia output 4. Increased PVR Shock CHF Cardiac life support
86
Fenoldopam (Corlopam)
Vasodilator dopamine agonist Decreased PVR in renal Emergency HTN