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Pharmacology and Medical Chemistry I > Exam 4 - Lecture 37-38, Pharmacology of Sympathomimetics > Flashcards

Exam 4 - Lecture 37-38, Pharmacology of Sympathomimetics Flashcards

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1
Q

Primary endogenous neurotransmitters in the SNS

A

NE, E, DA

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2
Q

Primary drug targets in the SNS

A

a and b adrenergic receptors

Dopamine receptors

Monoamine transporters biosynthetic pathways

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3
Q

What does SNS do

A

Releases E and NE

Increases Heart and Lung action

Constricts bodily blood vessels, but increase blood flow to muscle

Increase BP, HR, BS, and fats

Releases Glucagon (increase glucose)

Inhibit digestion, relax bladder and inhibit erection

Promote clotting

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4
Q

Neuronal Membrane Transporters

A

NET, DAT, SERT

transport monoamines, rely on Na gradient to passively transport monoamines

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5
Q

Vesicular monoamine transporter

A

responsible for pacing monoamines into vesicles preventing MAO degradation.

relies on trans-vesicular proton gradient for driving force

Vesicles contain ATP and chromogranin A

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6
Q

Extraneuronal monoamine transporter

A

Passive transport, no ATP

Bind 1 molecule or ion, changes conformation and releases cargo opposite side of membrane

Transports HA, 5HT, NE, DA, MPP+

Found on SM, Cardiac Muscle, Endothelium

inhibited by drugs of abuse; cocaine, MDMA, amphetamines

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7
Q

Selectivity

A

Describes the property of a ligand having greater affinity for one receptor over another

Can be “overcome” with high concentrations of ligand, when other receptors experience binding and activation

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8
Q

Receptor Activation

A

Depends on drug structure, dose, receptor number, receptor status, physiology, disease state, polymorphisms, species

Also mood, atmosphere, place, diet, will, spirituality

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9
Q

Histamine greatest affinity for…

A

Vmat2 over Vmat 1

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10
Q

EMT vs Neuronal MT

A

EMT as quick transport and has higher saturation than Neuronal MT

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11
Q

Alpha 1a,1b,1d distribution

A 
Bronchi
GI tract
GI sphincters
Uterus
Bladder sphincter
Seminal tract
Iris (radial muscle)
Liver (hepatocytes)
Salivary gland
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12
Q

Alpha 2a,2b,2c

A

GI tract
Directly on Pancreatic islet (beta cells) + Platelets
Brain stem
Nerve terminals

Predominantly presynaptic nerve terminals on brainstem causing presyanptic inhibitory effect

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13
Q

B1

A

HEART and salivary gland

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14
Q

B2

A

BRONCHI and uterus, heart, mast cells, liver

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15
Q

B3

A

Bladder detrusor
Skeletal muscle
Fat

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16
Q

Skeletal muscle contraction

A

Calcium binds troponin allowing for troponin to interact with actin/myosin allowing for muscle contraction

Fast and direct mechanism, little pharamcological activity

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17
Q

Cardiac muscle contraction

A

Still fast but has a plateau period (~100ms) after initial rapid depolarization. Cardiac specific RyR Ca channels release Ca2+ from sarcoplasmic reticulum.

contractile machinery of Troponin/Ca troponin resembles SKM

Ca2+ release from RyR Ca channels may cause arrhythmia. Of interest in adrenergic blockers

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18
Q

Smooth muscle contraction

A

Large organ variance in contraction.

** Not entirely dependent on depolarization as GPCR ligands by IP3 trigger Ca2+ release from the ER.

cAMP regulates myosin Lc kinase and myosin phosphatase to balance contraction/relaxation

several ways to have smooth muscle contraction

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19
Q

Alpha 1 receptor Signaling

A

Epinephrine> Norepinephrine affinity (but effect same)

a1 stimulates Gq coupled to PLC; PLC gets phosphorylated (activated)

PLC then hydrolyzes phosphoinositides, produces IP3 and DAG

DAG activates PKC and leads to cellular response

IP3 releases stored intracellular Ca and activates Ca channels

increased cytoplasmic Ca activates Ca dependent kinases leading to cellular response

Predominantly found in SM, all types of SM (except GI tract) contract in response to stimulation of a1-adrenoceptors

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20
Q

a1 effect on Bronchi

A

Contraction (narrowing)

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21
Q

a1 effect on GI tract + GI sphincter

A

relaxation(decrease motility) + contraction (decrease motility)

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22
Q

a1 effect on uterus

A

contraction (child birth/miscarriage)

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23
Q

a1 effect on Bladder sphincter

A

contraction (narrowing)

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24
Q

a1 effect on Seminal tract

A

contraction (ejaculation)

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25
a1 effect Iris
contraction (small pupils)
26
a1 effect Liver
Glycogenolysis (increase glucose synthesis)
27
a1 effect salivary gland
K+ release (profuse saliva)
28
Alpha 2 receptor signaling
receptor found in blood vessels, presynaptic GI NMJ, pancreatic Bcells, platelets, brain stem and nerve terminals Common effects due to negative feedback on presynaptic nerves to inhibit further release of NE from presynaptic nerve terminal Gai, inhibit Adenylate Cyclase, decrease cAMP + PKA
29
a2 effect on Blood vessels
constriction (a2b) or dilation (a2A)
30
a2 effect on GI tract
Presynaptic relaxation (decrease motility)
31
a2 effect on Pancreatic B cells
Decreased insulin release
32
a2 effect on platelets
Aggregation
33
a2 effect on brain stem
inhibit sympathetic flow
34
a2 effect on Nerve terminals
Adrenergic: Decrease NE release Cholingeric: Decrease ACH release Locus ceruleus: Sedative Dorsal horn: Analgesic effects
35
Beta receptor Signaling
receptor all signal by increase cAMP/PKA B1 Primarily in heart (also salivary glands) B2 receptors in SM, Heart, SKm, mast cells, nerve terminal B3 small pharmacopeia, found in bladder SKm and fat
36
B1 activation
Increase HR, Force of contraction | Increase amylase secretion salivary gland
37
B2 activation
Increase HR, force of contraction Bronchi Dilation Relax Gi tract, uterus, bladder, seminal tract, ciliary muscle Mast cell: inhibit histamine release (stop allergic reaction) SKm: tremor, increase mass, speed of contraction and glycogenolysis Adrenergic nerve terminal: increase Ne release
38
B3 activation
**** Bladder detrusor: relax (increase flow) **** SKm: thermogenesis ("burn rate") Fat: increase lipolysis and thermogenesis
39
Dopamine Receptor signaling
D5R and D1R = Gs ( up cAMP) D4R, D3R, D2R = Gi (down cAMP
40
D1 receptor activation
Increase HR and cardiac output Improved renal perfusion and urine output in kidney Can cause arterial vasodilation
41
Dopamine
Equal affinity for D1 and D2 receptor Used for heart failure, shock and unstable bradycardia
42
Fendolpam
Hypertensive crisis/hypertension
43
methyldopa
increase inhibitory effect of a2
44
Epinephrine (Adrenaline)
released from adrenal medulla during excitement/stress Potent alpha and beta agonist, highest affinity at a2, medium b1, b2 lowest...potent bronchodilator Releases sugar stored in liver increase strength of HR muscle contractions, increase HR and BP due to constrictions of blood vessels at higher doses Lower eye pressure
45
Effect of epinephrine on vascular smooth muscle
number of a1> b2 receptors At low doses, epinephrine selectively stimulates B2 leading to vasodilation (muscle relaxation and decrease in peripheral resistance) At higher doses, epinephrine can activate a1 leading to vasoconstriction as conc increase, predominate effect will vasoconstriction
46
Norepinephrine
released presynaptically used to increase BP in hypotensive states Good to use with anesthetics Can be given IV,IM or SC but orally ineffective due to GI MAO
47
Dopamine usage
activates Dopamine receptors and B1 receptors, at high doses also a1 receptors positive iontropic and chrontropic effects At low doses, dilates renal (kidney) and mesenteric (intestinal) arteries via D1 receptors Vasodilation - vascular D1 receptors respond at low concentration
48
Direct Acting drugs
at postsynaptic receptors Mimic E, NE, DA
49
Indirect Acting drugs
blocking the breakdown or reuptake of neurotransmitters, or stimulating production and release of catecholamines Increase levels of E,NE, DA
50
Fenoldopam (Dopamine receptor analog)
D1 partial agonist, no B receptor activity May have a1 and a2 antagonist activity Side effect: Tachycardia, arrhythmias headache and flushing Contraindications: patients with asthma may have adverse effect to metabolites; avoid use in glaucoma and in patients on beta-blockers Indications: Antihypertensive, decreases cardiac after load FDA pregnancy/lactation: Class B
51
Dopamine as drug
B1 receptor agonist used in sever congestive heart failure in low doses, vasodilation, increase sodium secretion
52
Direct-acting a-receptor agonist
``` Phenylephrine Oxymetazoline Methoxamine Midodrine Clonidine Brimonidine Guanfacine ```
53
Direct-acting b-receptor agonist
``` Dobutamine Terbutaline Albuterol/levalbuterol Brimonidine Salbutamol Salmeterol Clenbuterol Mirabegron ```
54
Phenylephrine (OTC)
Highly selective a1 agonist Pregnancy class X 1st trimester, C 2nd trimester Oral decongestant Can be used in some hemorrhoid treatments
55
Oxymetazoline (OTC)
Selective a1 agonist Intranasal admin, nasal decongestant by vasoconstriction t1/2 ~ 8hr Pregnancy class C, potentially B due to low systemic absorption
56
Midodrine
Prodrug, forms desglymidodrine (a1 receptor agonist) ** Only FDA approved to treat orthostatic hypotension ** Side effects: Headache, flushing face (vasodilation), confusion/abnormal thoughts Pregnancy class X: risk of fetal resorption, decrease fetal weight and increase risk of miscarriage
57
Methoxamine
Alpha 1 receptor agonist Used for BP maintenance during surgery (no b activity) Contraindicated: patients with hypertension side effects: Acute nausea/vomiting, headache, anxiety
58
Droxidopa
Alpha 1 receptor agonist Prodrug, converted into NE...it is orally viably available Orphan drug designation: treat neurogenic orthostatic hypotension (DbH deficiency) Blackbox warning: monitor supine BP before and during treatment, keep head elevated to prevent risk of hypertension
59
Clonidine
** For exam, specific a2 receptor agonist ** Prototypic and classical a2 receptor agonist FDA approval: Hypertension Off label use: ADHD, Migraine, Nicotine dependence + withdrawal Side effects: Drowsiness, orthostatic hypotension, edema and weight gain, rebound hypertension Abrupt discontinuation can result in withdrawal agitation, headache, tremor, rapid HR Pregnancy class C
60
Tizanidine
a2 receptor agonist muscle relaxant Contraindications: benzo, alcohol, buprenorphine Metabolized via CYP1A2, avoid fluoroquinolone (not cipro), antiarrhythmics, cimetidine, famotidine, acyclovir, oral birth control Pregnancy class C ** Clinically significant differences may occur when switching between tablets or capsules; once a formulation has been selected, do not alter regimen **
61
Brimonidine
A2 agonist Used for ocular hypertension, open angle glaucoma, red eye Remove contacts before admin Side effects: hypertension, contact dermatitis, dry out (xerostomia), allergic conjunctivitis, fainting (syncope) Alphagan P has a purite preservative, may be better tolerated by those with allergic reactions to other preservatives
62
Apraclonidine
Alpha 2 agonist Prophylatcis postoperative ocular hypertension for cataract and laser eye surgery, adjunct to intraocular pressure No concomitant use of MAOIs Side effects: allergic conjunctivitis, blurred vision, edema of eye lid, reduced visual acuity*
63
Dobutamine
B1 selective, prototype B1 agonist Chronotropic (HR) and inotropic (CO) actions without vasodilation Used to treat hear failure and cardiogenic shock (ventricles stop working) Off label: toxic shock syndrome, septic shock, pulmonary embolism shock only given IV Side effects: cardiac dysrhythmia, coronary arteriosclerosis, syncope, dyspnea
64
Albuterol (salbutamol) ProAir/Ventolin
Prototypic B2 agonist Fast-acting bronchodilator Used for asthma, exercise asthma, COPD, premature infant respiratory distress syndrome Pregnancy class: assume C Caution in patients with Cardiovascular disorders, arrhythmias, hypertension, lactose intolerance
65
Salmeterol
B2 agonist Used in Asthma, COPD, Nocturnal asthma Contraindicated for use in patients with cardiac disorders Causes prolonged QT interval, can cause headache and musculoskeletal pain FDA black box warning: long acting B agonist increase risk of asthma related death when used as monotherapy; pediatric population is at increased risk for hospitalization
66
Terbutaline
IV B2 agonist, used to delay preterm labor in serious situations, PO should not be used to delay preterm labor Contraindicated for use in patients with cardiac disorders and pulmonary edema
67
Clenbuterol
b2 agonist Used in sports due to "anabolic" attempt to increase muscle strength, those with asthma shouldn't use this med
68
Mirabegron
B3 agonist, prototypic Used for Bladder muscle dysfunction, overactive contraindicated patients with hypertension side effects: nasopharyngitis, urinary tract infection, headache, constipation, diarrhea, and tachycardia Inhibits CYP2D6, avoid drugs metabolized by this pathway
69
Drugs that release NE
Tyramine Amphetamine Methylphenidate
70
Drugs that inhibit release NE
Reserpine | Guanethidine
71
Drugs affecting NE uptake
Duloxetine (NET blocker) Lisdexamfetamine (NET blocker) Imipramine (NET blocker) Cocaine (DAT/NET Blocker)
72
Amphetamine
Prototype NE release, MAO inhibitor, NET inhibitor, CNS stimulant Usage: narcolepsy, paradoxical benefits in children with ADHD Abused as appetite suppression, drug of abuse Side effects: tachycardia, hypertension, insomnia, acute psychosis with OD, can cause dependence Well absorbed GI and cross BBB Pregnancy Class: C
73
Methylphenidate
Amphetamine variants Used as ADHD med with similar mechanism as amphetamine
74
Tyramine
product of tyrosine metabolism cannot cross BBB releases catecholamines Found in cheese, cured meats, beer, fermented foods, critical interaction with MAOI
75
Duloxetine
SSNRI Clinical uses: Major depression disorder, fibromyalgia, neuropathic pain, generalized anxiety disorder (off label: appetite suppressant**) Side effects: Nausea, dry mouth, constipation, fatigue, decreased appetite
76
Imipramine
Pro drug, into desmethylimipramine Blocks neuronal NET, also classified as TCA Clinical use: Depression, IBS Side effects: Atropine like effects (anti-slud), cardiac dysrhythmias in OD
77
Lisdexamfetamine
Prodrug of dextroamphetamine Mechanism and side effects: similar to amphetamine Clinical uses: ADHD Inhibition of CYP2D6, CYP1A2, CYP3A4, considerations for drug interactions
78
Cocaine
inhibits NET by acting as substrate Rarely used local anesthetic, maybe during ophthalmic procedures Commonly abused
79
Methyldopa
Treatment of hypertension during pregnancy (a2 action), orphan drug in Type 1 diabetes (off label pediatric use); hot sweats during menopause Do not use with MAOI or populations with liver disorders Common side effects: 20% patients ED, disordered ejaculations, dizziness Serious side effects: colitis, Congestive Heart Failure, jaundice or Parkinsonism
80
Reserpine
At v low conc blocks NE transport and VMAT, causing accumulation and degradation by MAO Used to be used as antihypertensive, currently used only experimentally..still used in combo with hydrochlorothiazide DO NOT prescribe to patients with active peptic ulcers, history of depression Side effects: GI, Neurolgoic, psychiatric and congestion Serious side effects: atrial fibrillation, cardiac dysrhythmia, GI hemorrhage
81
Guanethidine
inhibit release of NE from nerve terminals, and accumulates in VMAT displacing adrenaline and preventing release Abolish response of nerves to sympathetic nerve activation Previously used as hypertensive Severe Side effects: lost of sympathetic nerve reflexes, postural hypotension, diarrhea, nasal congestion and inhibition of ejaculation
82
Ephedrine
Mixed sympathomimetics used as decongestant, appetite suppressant, and treat hypotension associated wit anesthesia (hypothermia due to anesthetic with caesarean and spinal injury) side effects: hypertension, palpitations, tachycardia, nausea, vomiting, dizziness and reslessness Monitor renal function in at risk populations (elderly, renal impairment) Commonly abused athletics
83
Pseudoephedrine
1/4 potent as ephedrine counsel patients purchasing to monitor blood pressure commonly used as decongestion No concurrent admin with MAOI side effect: anxiety, restlessness, atrial fibrillation, myocardial infarction, insomnia

Pharmacology and Medical Chemistry I (30 decks)

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