Exam 4: Drugs Flashcards by Hannah Lapos | Brainscape

Q

Resperine

A

Blocks VMAT of NE and DA
Used to deplete nerve ending of NE
Allows fall in BP, but lots of ADRs

Hypertension, Insanity

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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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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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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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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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Q

Cocaine

A

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

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Q

What are the clinical uses for Indirect Acting Sympathomimetics?

A

ADHD
Narcolepsy
Obesity
Drug of abuse

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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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Q

Concerta

A

Methylphenidate that has osmotic release using OROS

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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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Q

Side effects for amphetamine and stimulant medication?

A

Insomnia
Anorexia
Weight loss
GI upset
Precipitation or exacerbation of tics
Abuse (hallucinations, panic, suicidal thoughts)

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Q

Methylamphetamine (Desoxyn)

A

ADHD CNS stimulant

Stimulant side effects

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Q

Dextroamphetamine (Dexedrine)

A

ADHD CNS stimulant

Stimulant side effects

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Q

Lisdexamfetamine (Vyvanse)

A

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

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Q

Mixed Salts (Adderall)

A

ADHD CNS stimulant
Stimulant side effects

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Q

Dexmethylphenidate (Focalin)

A

ADHD CNS stimulant
Stimulant side effects

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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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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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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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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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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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Q

Lorcaserin (Belviq)

A

Non-ampetamine appetite suppressant for long term use

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Q

Phentermine

A

New weight loss stimulant

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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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Q

Metaraminol (Aramine)

A

Mixed acting a1 agonist
1. a-1 direct agonist effect
2. Minor indirect agonist for some b1 responses
3. Increase BP
IV Vasopressor

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Q

Mephentermine

A

Mixed acting a1 agonist
1. a-1 direct agonist effect
2. Minor indirect agonist for some b1 responses
3. Increase BP
IV Vasopressor

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Q

Methoxamine

A

Mixed acting a1 agonist
1. a-1 direct agonist effect
2. Minor indirect agonist for some b1 responses
3. Increase BP
IV Vasopressor

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Q

Midodrine (Orvaten)

A

a-1 agonist
Prodrug converted to desglymidodrine
Symptomatic orthostatic hypotension

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Q

Hydroxyamphetamine + tropicamide (Paremyd)

A

a-1 agonist
Mydriatic agent

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Q

Droxidopa (Northera)

A

Prodrug of NE and E which metabolized in neurons by AADC to NE
Increases NE and E in PNS and CNS
Increases HR and BP
Orthostatic hypotension (neurogenic)

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Q

Norepinephrine

A

Inotropic and vasopressor
Shock
Enhance CO and PVR

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Q

Tetrahydrozoline (Visine)

A

a-1 agonist imidazole derivative
Ophthalmic and nasal

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Q

What are a-1 agonist therapeutical treat?

A

Hypotension
Shock

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Q

Clonidine (Catapres)

A

a-2 agonist
Long duration of action (t1/2=12-16hr)
ADHD
Hypertension

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Q

Guanfacine (Tenex. Intuniv)

A

a-2 agonist
1. More slective than clonidine\
ADHD
Sleepiness and dry mouth

Q

Brimonidine (Alphagan P)

A

a-2 agonist
Inhibit sympathetic tone, decreasing aqueous humor
Increases uveoscleral outflow
Chronic treatment for glaucoma

Q

Apraclonidine (Iopidine)

A

a-2 agonist
Short term treatment for reducing IOP
Prevention and treatment of postsurgical intraocular pressure elevations

Q

a-methyldopa (Aldomet)

A

a-2 agonist
False neurotransmitter taken up by neurons
Acculumates in synaptic vescicles
Released by NE nerve terminals
Hypertension in pregnancy

Q

Oxymetazoline (Afrin)

A

a-1 agonist imidazole derivative
Ophthalmic and nasal

Q

Dexmedetomidine (Precedex)

A

a2 agonist
ICU sedation
Procedural sedation

Q

Isoproterenol

A

Beta non-selective agonist
Cardio-stimulatory
Vasodilation

Q

What ANS causes bronchodilation?

A

Sympathetic stimulation (E)

Q

What ANS causes bronchoconstriction?

A

Cholinergic

Q

Purpose of B2 selective agents?

A

Relaxes bronchial airways smooth muscle
Stabilizes mast cells

Q

Albuterol (Proventil HFA)

A

b2 agonist
Gold standard
Racemic mixture
SABA

SE: tremors and tachycardia

Oral and inhalationt (asthma)

Q

Levalbuterol (Xopenex)

A

b2 agonist
R-enantiomer of albuterol
SABA

SE: tremors and tachycardia

Inhaler, nebulized solution

Q

Terbutaline (Brethine)

A

b2-agonist
SABA
Tocolytic agent, relaxes uterine
Phenyl ring modifications to decrease COMT metabolism

Oral and parenteral preparationt for bronchospasms and status asmaticus

Q

Salmeterol (Serevent Diskus)

A

B2 agonist
LABA
Onset: 15-30min
Duration: 12 hr
Combo with Fluticasone

Inhalation (powder) therapy: not prn (rescue inhaler)

Q

Vilanterol (+Umeclidinium, Anoro Ellipta)

A

b2-agonist
Ultra-LABA
Asmtha
COPD agent

Q

Indacaterol (Arcapta Neohaler)

A

b2-agonist
Ultra-LABA

COPD agent

Q

Olodaterol (Striverdi Respimat)

A

b2-agonist
Ultra-LABA

COPD agent

Q

B2-agonist therapeutic use

A

Asthma and COPD
Bronchodilation

Q

B2-agonist ADR

A

Tremors

Q

Dobutamine (Dobutrex)

A

b1 agonist

Cardiac decompensation (cardiogenic shock)

Q

Mirabegron (Myrbetriq)

A

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)

Q

Vibegron (Gemtesa)

A

b3 agonist
Increases bladder capacity

OAB (no BP effects)

Q

Epinephrine

A

Nonselective, raises BP, bronchodilation

Acute anaphylatic reactions

Q

Phentolamine (Regitine, Oraverse)

A

Mixed a1 and a2 competitive antagonist
Decreases PVR therefore decreasing BP
Hypertension

Q

Phenoxybenzamine (Dibenzyline)

A

Irreversible a antagonist

Covalently binds to receptors
Blocks ACh, histamine
Long acting oral med

Q

Prazosin (Minipress)

A

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

Q

Terazosin (Hytrin)

A

a1 antagonist
Oral 90% bioavailablity
Relaxes prostate and reduces urethreal resistance to flow
Hypertension, BPH

Q

Doxazosin (Cardura)

A

a1 antagonist
Oral 60% bioavalability
Hypertension, BPH

Q

Tamsulosin (Flomax)

A

a1-A (prostate) blocker over a1-B (vasculature)
Relaxes prostate and reduces urethreal resistance to flow
BPH

Q

Silodosin (Rapaflo)

A

Highly selective a1-A blocker than B
High uroselectivity, and positive cardiovascular safety profile

BPH

Q

Alfuzosin (Uroxatral)

A

a1-blocker
Some uroselectivity which leads to lower incidence of ejaculatory dysfunction (50% bioavailability)
BPH

Q

Pindolol (Visken)

A

b partial agonist
1. Low concentration: slight activation of receptors
2. High concentrations: antagonist and ISA function
3. MSA

Q

Propranolol (Inderal)

A

Nonselective beta blocker (MSA)
1. High first pass metabolism
2. Highly lipid soluble (CNS) - causing migraines
3. Block Na+ channels in heart and neurons

Membrane stabilizing activity
Portal hypertension
Cirrhosis prevent visceral bleeding

Q

Pindolol (Visken)

A

b partial agonist
1. Low concentration: slight activation of receptors
2. High concentrations: antagonist and ISA function
3. MSA

Q

Nadolol (Corgard)

A

Nonselective beta blocker
1. Low lipid solubility
2. Long duration of action
3. Avoid abrupt cessation

Q

Sotalol (Betapace)

A

Nonselective beta blocker
1. Low lipophilicity
2. Blocks potassium channels in heart
HTN and ventricular arrythmia

Q

Sotalol AF (Betapace AF)

A

Nonselective beta blocker
1. Low lipophilicity
2. Blocks potassium channels in heart
Artrial fibrillation

Q

Timolol (Blocadren, Timoptic, and Betimol)

A

Nonselective beta blocker
1. Decreases aqueous humor production
2. Excellent ocular hyportensive effect

Glaucoma
HTN
post-MI angina
Prophylaxis of migraine

Q

Carteolol (Cartrol)

A

Nonselective b blocker
1. Low lipid solubility
2. ISA activity
Glaucoma

Q

Levobunolol (Betagan)

A

Nonselective b blocker
Glaucoma

Q

Carvedilol (Coreg)

A

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

Q

Labetalol (Trandate)

A

Mixed a1 and nonselective b-blocker, partial agonist at b2 (ISA)
1. MSA
2. May cause liver damage or hepatocellular injury
Hypertension

Q

Metoprolol (Toprol XL)

A

b1 antagonist
1. Lipid soluble
2. MSA
3. Avoid abrupt cessation

Q

Atenolol (Tenormin)

A

b1 antagonist
1. Low lipid solubility
2. Prophylaxis of migraine
3. Avoid abrupt cessation

Q

Esmolol (Brevibloc)

A

b1 antagonist
1. Rapid metabolism (8min)
2. IV Prep only

Q

Esmolol (Brevibloc)

A

b1 antagonist
1. Rapid metabolism (8min)
2. IV Prep only

Acute supraventricular tachycardia
Hypertensive emergency

Q

Acebutolol (Sectral)

A

b1 antagonist
1. Hydrolysis to active metabolite (diacetolol)
2. ISA
3. MSA

Q

Betaxolol (Betoptic, Kerlone)

A

b1 antagonist
Ophthalmic: glaucoma
Oral: HTN

Q

Bisoprolol (Zebeta)

A

b1 antagonist
HTN once a day dosing

Q

Nebivolol (Bystolic)

A

b1 antagonist
1. Nitric oxide potentiativng vasodilatory effect
Antioxidants
HTN once/day dosing

Q

Dopamine

A

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

Q

Fenoldopam (Corlopam)

A

Vasodilator dopamine agonist
Decreased PVR in renal
Emergency HTN