PRELIM 07 - Adrenergic Agonists and Antagonists Flashcards
Parent compound found in sympathomimetics
β-phenylethylamine
Bind to and activate alpha and/or beta receptors (Types of sympathomimetics)
Direct-acting sympathomimetics
3 examples of endogenous catecholamines (END)
Epinephrine, Norepinephrine, Dopamine
A nonselective α1α2 and β1β2 agonist; is a major hormone secreted by the adrenal medulla (Examples of endogenous catecholamines)
Epinephrine
Serves as the DOC for anaphylactic shock (Examples of endogenous catecholamines)
Epinephrine
2 other names of norepinephrine (LN)
Levarterenol, Noradrenaline
A nonselective α1α2 and β1 agonist; is the major neurotransmitter in postganglionic sympathetic nerves (Examples of endogenous catecholamines)
Norepinephrine
A compensatory vagal reflex that slows down heart rate and blood pressure in response to increased blood pressure; involves norepinephrine
Baroreceptor reflex
Used to raise or support blood pressure under certain intensive care conditions and is the vasopressor of choice in cardiogenic and septic shock (Examples of endogenous catecholamines)
Norepinephrine
A nonselective D1 = D2 > β1 > α1 agonist; is the major neurotransmitter in the CNS and is involved in the reward stimulus relevant to addiction (Examples of endogenous catecholamines)
Dopamine
Is used for congestive heart failure, and cardiogenic and septic shock (Examples of endogenous catecholamines)
Dopamine
Dopamine overdose can lead to __________
Excessive sympathomimetic activity
Used as a topical nasal decongestant (Examples of nonselective α1α2 agonists) (ONX)
Oxymetazoline, Naphazoline, Xylometazoline
Used as a nasal decongestant and mydriatic (Examples of selective α1 agonists) (PM)
Phenylephrine, Methoxamine (discontinued)
Used for the treatment of hypotension (Examples of selective α1 agonists) (MM)
Metaraminol, Mephentermine
A prodrug of desglymidodrine; used for the treatment of postural (orthostatic) hypotension (Examples of selective α1 agonists)
Midodrine
A 2-imidazoline derivative used for the treatment of hypertension; its adverse effects include xerostomia, sedation, and withdrawal syndrome (Examples of selective α2 agonists)
Clonidine
A prodrug of α-methylnorepinephrine; used as an antihypertensive (Examples of selective α2 agonists)
Methyldopa
More selective for α2 than Clonidine; used as an antihypertensive; its SR form is used for ADHD (Examples of selective α2 agonists)
Guanfacine
Used as an antihypertensive (Examples of selective α2 agonists)
Guanabenz
Used as an antihypertensive and analgesic (Examples of selective α2 agonists)
Moxonidine
Used as a sedative before anesthesia (Examples of selective α2 agonists)
Dexmedetomidine
Used as a muscle relaxant (Examples of selective α2 agonists)
Tizanidine
Used for bradycardia or heart block (Examples of nonselective β1β2 agonists)
Isoproterenol (Isoprenaline)
Used for short-term treatment of cardiac decompensation and is the inotropic of choice in cardiogenic shock (Examples of selective β1 agonists)
Dobutamine
Metaproterenol, albuterol, and levalbuterol are examples of __________ selective β2 agonists
Short-acting (SABA)
Salmeterol, forrmoterol, and arformoterol are examples of __________ selective β2 agonists
Long-acting (LABA)
Indacaterol, olodaterol, and vilanterol are examples of __________ selective β2 agonists
Very long-acting (VLABA)
__________ agonists are used as the DOC for acute asthmatic bronchoconstriction, COPD, and used as a tocolytic
Selective β2
Used for incontinence; induces detrusor muscle relaxation and increased bladder capacity (Examples of selective β3 agonists)
Mirabegron
3 examples of mixed-acting sympathomimetics (EPP)
Ephedrine, Pseudoephedrine, Phenylpropanolamine
Has been used in China; used for asthma, promote urinary incontinence, and hypotension in spinal anesthesia (Examples of mixed-acting sympathomimetics)
Ephedrine
One of the 4 ephedrine enantiomers; used as a nasal decongestant (OTC); can be used as a precursor for meth (Examples of mixed-acting sympathomimetics)
Pseudoephedrine
Used as a nasal decongestant and appetite suppressant; withdrawn in the US due to risk of hemorrhagic stroke (Examples of mixed-acting sympathomimetics)
Phenylpropanolamine
A racemic mixture of β-phenylisopropylamine; used for narcolepsy and ADHD (Examples of indirect-acting sympathomimetics: releasing agents)
Amphetamine
Widely abused as a cheap, accessible recreational drug (Examples of indirect-acting sympathomimetics: releasing agents)
Methamphetamine/N-methylamphetamine/Crystal meth/Shabu
An amphetamine variant; used for narcolepsy and is a first-line drug for ADHD in children (Examples of indirect-acting sympathomimetics: releasing agents)
Methylphenidate
A normal byproduct of tyrosine metabolism; produced in high concentrations in protein-rich foods (Examples of indirect-acting sympathomimetics: releasing agents)
Tyramine
Inhibits norepinephrine transporter (NET) and dopamine transporter (DAT); used as a first-line agent for narcolepsy (Examples of indirect-acting sympathomimetics: reuptake inhibitors)
Modafinil
Has a shorter but more intense effect than amphetamine; used as a local anesthetic (Examples of indirect-acting sympathomimetics: reuptake inhibitors)
Cocaine (coke)
Used for pheochromocytoma and reversal of soft tissue anesthesia; its adverse effects include orthostatic hypotension and inhibition of ejaculation (Examples of α1α2 antagonists) (PP)
Phentolamine, Phenoxybenzamine
Ergot alkaloids, which are examples of α1α2 antagonists, are sourced from the fungi __________ and __________ (CP, CP)
Claviceps purpurea, Claviceps paspali
2 examples of ergot alkaloids (ED)
Ergotamine, Dyhydroergotamine
__________ are the first adrenergic receptor antagonists to be discovered
Ergot alkaloids
Used for hypertension, CHF, and for urinary retention in benign prostatic hyperplasia (BPH); its adverse effects include the first-dose effect (Examples of α1 antagonists) (PTIU)
Prazosin, Tamsulosin, Idoramin, Urapidil
An indolealkylamine alkaloid from Pausinystalia yohimba bark and in Rauwolfia serpentina root; formerly used for erectile dysfunction (Examples of α2 antagonists)
Yohimbine
Propanolol, nadolol, penbutolol, pindolol, and timolol are examples of __________ β antagonists
1st generation (Nonselective)
Metoprolol, acebutolol, atenolol, bisoprolol, and esmolol are examples of __________ β antagonists
2nd generation (β1 selective)
Carteolol, carvedilol, and labetalol are examples of __________ β antagonists
3rd generation (Nonselective w/ additional CV actions)
Betaxolol, celiprolol and nebivolol are examples of __________ β antagonists
3rd generation (β1 selective with additional CV actions)
Epinephrine results to positive inotropic and chronotropic effect via __________ receptor
β1
Epinephrine results to vasoconstriction in most blood vessels via __________ receptor
α1
Epinephrine results to vasodilation in some blood vessels (ex: skeletal muscle blood vessels) via __________ receptor
β2
Epinephrine results to inhibition of insulin secretion via __________ receptor
α2
Epinephrine results to promotion of insulin secretion via __________ receptor
β2
Epinephrine results to promotion of glucagon secretion via __________ receptor
β2
Epinephrine results to glycogenolysis via __________ and __________ receptor
α1, β2
Epinephrine results to lipolysis via __________ receptor (activates hormone-sensitive lipase)
β3
Epinephrine administered orally is inactivated by __________ and __________ (MC)
MAO, COMP