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Pharmacology > Adrenergic Drugs (Exam 1) > Flashcards

Adrenergic Drugs (Exam 1) Flashcards

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1
Q

Picture of Sympathetic (Adrenergic) and Parasympathetic (Cholinergic) Nervous System

A
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2
Q

Norepinephrine

A

Main adrenergic mediator (Sympathetic)

-Purpose is to maintain a constant internal environment

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3
Q

Epinephrine

A
  • Also known as adrenaline
  • Fight or flight

Synthesized and released from the adrenal medulla

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4
Q

Dopamine

A

Reward system contributes to survival

-Feel good, food, sex, drugs

*Abusive drugs release dopamine

Examples: amphetamine, opiates, nicotine, caffeine

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5
Q

Autonomic Nervous System breakdown

  • CNS Outflow
  • Ganglia
  • Pre/post-ganglionic fiber length
  • Postganglionic fiber distribution
  • Response to stimulation
  • Postganglionic neurotransmitter
A
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6
Q

Catecholamines (adrenergics)

A

Epinephrine, Norepinephrine, and dopamine

-Rapid onset of action/brief duration of action

Not orally active

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7
Q

Direct adrenergic agonist

A

Compounds that mimic the action of epinephrine

Ex. dopamine (binds to dopinergic, alpha, and beta receptors)

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8
Q

Indirect acting compounds

A

Release norepinephrine, which acts on the adrenergic receptors

Ex. amphetamine, tyramine (wine/cheese/sausage) or methylphenidate (Ritalin)

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9
Q

Mixed acting compounds

A

Have two actions:

1) Direct action to stimulate the receptors
2) Indirect action to release NE, which also acts on the receptors

Ex. pseudoephedrine (Sudafed)

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10
Q

What are the enzymes involved in adrenergic neurons? Cholinergic?

A

Adrenergic: MAO and COMT

Cholinergic: acetylecholinesterase

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11
Q

What is biosynthesis of catecholamines? (photo)

What is the rate limiting enzyme?

A

Tyrosine hydroxylase (Tyrosine to Dopa)

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12
Q

What can cause the accumulation of tyramine in humans?

A

MAO inhibitors

Consumption of food/beverages containing it (Wine/sausage/cheese)

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13
Q

When in the pre-synaptic neuron, what prevents MAO from breaking down all the adrenergic catecholamines (dopamine/NE)?

A

Dopamine and NE are stored in nerve vesicles, which prevent MAO from breaking them down

-Reserpine is an old drug that would prematurely release them from their vesicles, where they would be broken down and the neuron would be unable to release them upon arrival of an action potential (major side-effect: depression)

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14
Q

Catecholamine Release Sequence

A

Tyramine transported into a nerve ending by a Na+-dependent carrier

Converted to dopamine and transported into the vesicle by VMAT

Converted in the vesicle into NE by dopamine beta hydroxylase

NE physiologically released from nerve terminal (Dependent on Ca++ and an action potential)

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15
Q

What are some substances that can inhibit the recycling of NE back into the pre-synaptic neuron?

A

Cocaine and tricyclic anti-depressants (amitriptyline, nortriptyline, doxepin, etc.)

-Acts as an indirect agonist, inhibiting NET from bring NE back in and prolonging NE’s presence in synaptic cleft

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16
Q

Catecholamine Termination

A

Active reuptake (90%)

  1. NET carries NE back into the pre-synaptic neuron cell cytoplasm

Simple Diffusion (10%)

  1. NE diffuses into surrounding glial cells and smooth muscles, where it is eventually metabolized (plasma or liver)
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17
Q

What are examples of MAO inhibitors and what have they been used for?

A
  • Phenelzine, selegiline, tranylcypromine, isocarboxazid
  • Treat Parkinson’s disease (since NE/dopamine isn’t being metabolized by MAOs)
  • Old treatment for depression; not used anymore

*Tyramine can cause a hypertensive crisis while using these

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18
Q

What should be generally associated with a1 receptors? How about ß2 receptors?

A

a1: Vasoconstriction

ß2: Vasodilation

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19
Q

Alpha1 receptor

  • Location (2)
  • Function (6)
A

Adrenergic

Located on blood vessels and smooth muscle (GI, mucosa, skin)

Control vasomotor tone (BP), vasoconstriction, pupil dilation (mydriasis)

Increased: peripheral resistance, BP, and closure of internal sphincter of bladder

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20
Q

Alpha2 receptor

  • Location
  • Function
A

Adrenergic

-Located at terminal ending of NE-releasing neurons

Stimulation will inhibit release of:

1) NE (via negative feedback)
2) Insulin

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21
Q

ß1 receptor

  • Location (3)
  • Function (3)
A

Adrenergic

  • Located in Brain, heart and kidneys
    1) Tachycardia
  • Increased:
    2) Myocardial contractility
    3) Renin secretion (which ultimately increases BP)
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22
Q

ß2 receptors

  • Location (3)
  • Function (7)
A

-Located in the lung, pancreas and smooth muscle

Vasodilation, bronchodilation, relaxed uterine smooth muscle

Slight decrease in peripheral resistance (counters a1)

Increased:

1) muscle/liver glycogenolysis
2) glucagon release
3) insulin secretion

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23
Q

Affinity of NE and Epinephrine for receptors (tie in Local Anesthetics)

A

NE: 90% alpha

Epi: 50:50* (Prefer alpha at high concentrations)

*Problematic if ß1 receptor (heart concerns)

For local anesthetics we want:

1) Localized high dose: vasoconstricts to keep LA @ site
2) Systemic low dose: minimal vasodilation/heart concerns; therefore it is critical that we have negative aspiration

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24
Q

Dopamine receptors

  • Locations (4)
  • Type and function (2)
A

-Located in CNS, kidney, heart and vasculature

DA1-like: control movement, cognitive function

  • Positive inotropic effect (CV function; stronger contractions)
  • Decreased renin and Na+ reabsorption (Decr. BP)
  • Vasodilation (vasculature)

DA2-like: control movement, cognitive function, and prolactin secretion

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25
Ropinorole What receptor does it have affinity for? What is its function?
**Ropinirole (Requip)** **DA2** in brain (dopamine agonist) Treatment of **Parkinson's and restless-leg syndrome**
26
What is an example of a dopamine-antagonist? What is its function?
**haloperidol (Haldol)** and **chlorpromazine (Thorazine)** **Depleting DA in CNS**; anti-psychotics
27
What are the receptor types in the eye for the radial muscle (iris) and the ciliary muscle?
Radial muscle: alpha1 Ciliary muscle: ß2
28
What are the adrenergic responses for the radial muscle (iris) and ciliary muscle in the eye?
Radial muscle: Mydriasis pupil dilation Ciliary muscle: Relaxation for distant vision \*Note the sphincter muscle is the complement to the radial muscle, causing pupil constriction upon cholinergic impulse
29
What are the cholinergic responses for the sphincter and ciliary muscle in the eye?
Sphincter muscle: Miosis (pupil constriction) Ciliary muscle: contraction for near vision \*Note radial muscle is complementary to sphincter muscle during adrenergic stimulation
30
Heart Responses to Autonomic Nerve Impulses (chart) What receptor type is found for all heart receptors listed?
ß1 receptor
31
Blood Vessel Responses to Autonomic Nerve Impulses (chart) - Coronary BVs - Skin/mucosa BVs - Skeletal muscle BVs - Cerebral BVs - Pulmonary BVs - Abdominal viscera BVs - Veins - Salivary gland BVs
**Coronary: ß2 predominates** _Skin/mucosa: alpha1_ **Skeletal muscle BVs: ß2 predominates** _Cerebral: alpha_ **Pulmonary: Alpha predominates** *Abdominal: both alpha and ß2* **Veins: Alpha predominates** _Salivary glands: alpha_
32
Summarize adrenergic activity in blood vessels (based on receptor type)
**Alpha** recptors **constrict** (skin/kidney/abdomen) **Beta** receptors **dilate** (skeletal muscle/coronary artery)
33
Summarize CV effects of Catecholamines in therapeutic doses (Epi, NE, and Isoproterenol)
Epi: A1=A2; B1=B2 NE: All A, low ß Isoproterenol: All ß, low A
34
Lung, Stomach, Intestine, Gallbladder, and Kidney Responses to Autonomic Nerve Impulses (chart) - Bronchial muscle - Stomach motility/tone - Stomach sphincters - Intestinal motility/tone - Intestinal sphincters - Kidney
-Bronchial muscle: ß2 **-Stomach motility/tone: ß2 predominates** _-Stomach sphincters: Alpha_ **-Intestinal motility/tone: ß2 ​predominates** _-Intestinal sphincters: Alpha_ *-Kidney: ß1*
35
Summarize Adrenergic and Cholinergic activity in the GI Tract
Cholinergic: Rest and Digest= increased motility and secretion Adrenergic: Fight or Flight= reduced motility and sphincter contraction
36
Bladder, Sex Organs, Skin, and Adrenal Medulla Responses to Autonomic Nerve Impulses (chart) Bladder (detrusor) Bladder (trigone/sphincter) Sex organs Skin (piloerection) Sweat glands
Bladder (detrusor): ß Bladder (trigone/sphincter): alpha Sex organs: alpha Skin (piloerection): alpha Sweat gland: alpha \*Note Skin piloerection is solely adrenergic (no cholinergic impulses)
37
Liver, Pancrease, Fat Cells and Glands Responses to Autonomic Nerve Impulses (chart) - Liver - Pancreas (Acini) - Pancreas (Islets of langerhans) - Fat Cells - Salivary glands
- **Liver: ß2** * -Pancreas (Acini): Alpha* **-Pancreas (Islets of langerhans): ß2 predominates** _-Fat Cells: Both_ _-Salivary glands: Both_
38
Summarize Adrenergic activy on salivary glands
Cholinergic: thin secretions (more) Adrenergic: thick secretions (less) **\*Adrenergic agonists cause xerostomia**
39
What is critical in adrenergic activity in the CNS? What is the root cause? Where are side effects at toxic levels and what are they?
**The ability to cross the Blood Brain Barrier (BBB)** -Hydroxyl groups are the root cause At toxic levels, individuals experience severe **CNS** and _CV_ side effects: **nervousness/excitation/headache/tremor/cerebr. hemhorrage**; _hypertension/arrythmias/pulm. edema_
40
Alpha Agonists
Phenlyephrine: A1 \*Clonidine \*Dexmedetomidine \*Guanfacine \*Methyldopa \*=a2 predominates
41
What are the mixed alpha and beta agonists?
**NE** (*Levophed*): a1=a2; ß1\>\>ß2 **Epinephrine:** a1=a2; ß1=ß2
42
Beta agonists
**dobutamine:** **ß1** isoproteren**_ol_** **albuter**_ol_****/*metaproteren**_ol_***/levalbuter**_ol_**/pirbuterol/salmeter**_ol_**/formoter**_ol_**/arformeter**_ol_**/**terbutaline** **\*Note: ß2 agonists** all end in **-ol** (EXCEPT **terbutaline**)
43
Dopamine Agonists
dopamine: D1=D2>>ß\>\>alpha fenoldapam: D1 (vasodilator used in anti-hypertensive crisis)
44
Mixed Action Agonists
ephedrine (alpha, ß2) pseudoephedrine (alpha, ß2)
45
amphetamine & dextroamphetamine (Adderall) dextroamphetamine (Dexedrine) Controlled Substance classification for Adderall?
**alpha (CNS) & adrenergic agonists** - _Class 2_ controlled substance (Adderall) - Use for weight loss (NE depresses appetite) Off-label uses: Narcolepsy & ADHD
46
atomoxetine (Strattera) Controlled Class of drug?
**alpha (CNS) & adrenergic agonists** non-stimulant; selectively inhibits reuptake of NE with little or no activity at neuronal receptor sites _Class IV_
47
diethylpropion (Tenuate)
**alpha (CNS) & adrenergic agonists** Bath salts
48
methamphetamine (Desoxyn)
**Alpha (CNS) & adrenergic agonist**
49
methylphenidate (Ritalin; Concerta) dexmethylphenidate (Focalin) Controlled Substance classification?
**Alpha (CNS) & adrenergic agonists** -Blocks the reuptake of NE and dopamine and increases their release into extraneural space (_weight loss and better concentration; ADHD; narcolepsy; depression in elderly adults_) **Both Class 2 controlled substances** \*_Release more NE than dopamine_, therefore making them a lower probability for abuse
50
modafanil (Provigil) armodafinil (Nuvigil)
central **Alpha (CNS) & adrenergic agonist** * -Psychostimulants for nacrolepsy, shift work sleep disorder, obstructive sleep apnea, and off-label ADHD* - increases _NE, dopamine, seratonin, and glutamate_
51
phentermine (Adipex-P; Suprenza)
**Alpha (CNS) agonist** -Stimulates the hypothalamus to release NE and dopamine from neurons
52
sodium oxybate (Xyrem)
**GABA receptor** & adrenergic agonist -sodium salt of gamma-hydroxybutyrate
53
tyramine
**alpha, ß1**; adrenergic agonist
54
Therapeutic uses of the following drugs:
55
Therapeutic uses of the following drugs:
56
Therapeutic uses of the following drugs: albuterol arformoterol epinephrine formoterol levalbuterol metprolerenol pirbuterol salmeterol terbutaline
**Bronchial asthma, COPD** -oral ß2 agonists are less effective, produce more adverse effects and have slower onset of action than the same drugs given by aersol inhalation **-Stimulation of ß2 relaxes bronchial smooth muscle (bronchodilators)** **\*terbutaline** also **stops uterine contractions** and is used to prevent pre-term labor
57
-zoline
Alpha1 agonist (used as a decongestant) -Constricts arteriolar network, decreasing blood flow to edematous area and improving breathing
58
Therapeutic Uses of the following drugs:
Common Cold/Decongestion
59
Therapeutic use of the following drugs:
Opthalmic uses (to dilate the pupils through the **alpha1 receptor** in the iris)
60
Dexmedetomidine (Precedex) \*Important!\*
**selective Alpha 2 agonist** Used for anesthetic and sedative properties \*Inhibits NE release by binding to receptors in the brain stem \*High doses can result in vasoconstriction
61
clonidine (Catapres) guanfacine
Also stimulate **alpha 2 brain** receptors (in addition to controlling _hypertension_) **\*Both drugs cause sedation** Off Label uses: - ADHD - Hyperkinesis
62
Overdose of Adrenergic Agonists/CNS stimulants Signs
Dilated Pupils Shallow Respirations Increase in BP/HR Hyperactive tendon reflex Nervousness/Insomnia to excitation/hallucination Convulsion
63
Methylxanthines -What are they? What is their mechanism of action and function? -What are examples?
_Non-adrenergic stimulants_ -**Block adenosine (alpha 1 and 2b)** receptors in the brain Function: stimulates **respiratory center sensitivity** to CO2; **prevent apnea** (adenosine involved in constriction of airway smooth muscle/bronchoconstriction); **diuresis** (water/Na+ loss); _Increased lipolysis/glycogenolysis/gluconeogenesis_; **Induces release of epinephrine from adr. medulla** (**- side-effect**) **-Caffeine/theophylline**
64
What enzyme is inhibited by methylxanthines? What enzyme is inhibited by beta agonists?
Methylxanthines: **Phosphodiesterase** Beta agonists: **Adenylate cyclase**
65
Where does Caffeine have the highest impact? Theophylline? CNS Respiration Weak Diuretic Bronchial Relaxation (bronchodilation) Heart (positive inotropic/chronotropic effects)
Caffeine: **CNS Respiration** Theophylline: **Bronchodilation**
66
What is the #1 drug used in neonates?
Caffeine
67
What are some of the special considerations for methylxanthine therapeutic use?
- **Pregnancy**: may delay blood flow to the placenta, thus harming the fetus (decrease or eliminate consumption during this period) - Common side-effects are **benign breast lumps**, **GI reflux**, and **anxiety**
68
Why would you utilize another option than a methylxanthine for treatment of obstructive lung disorders (asthma, emphysema) or apnea?
Because it has a **tight therapeutic index** so other options are better Side effects: Cardiac/CNS stimulation; **nausea, vomiting, diarrhea, headache, insomnia, and irritability** (tachycardia and arrythmias can occur at higher levels than 35 mcg/mL)
69
What is aminophyline (IV) used for?
**Reversal agent for adenosine** (Adenoscan) and regadenoson (Lexiscan)

Pharmacology (7 decks)

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