presynaptic a2 receptor PGE2 or degrade w/in terminals w/ MAO; reacumulate from synapse if cleaning

Adrenergics Flashcards by O lawformonde

Heart receptor?

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vessel receptor?

A1 = STRONGER = constrict

B2 = dilate (coronary/skeletal)

(a2=little effect)

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Kidney receptor?

B1 = release renin

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GI tract receptor?

a1 = stop secretion

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Sex organs receptor

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Uterus receptors?

contract = a1
Relax = b2

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Catecholamines

epi
NE
dopamine

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NE released at

postganglionic sympathetic

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Epi released from

adrenal medulla

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Isoproterenol

ISUPREL

selective B ag

Stim the heart

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Dopa

CNS transmitter

NE precursor

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NE synthesis

Transporter sucks in Tyrosine

Tyr->Dopa->DA->NE->Epi

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Inhibit NE release?

presynaptic a2 receptor
PGE2

*or degrade w/in terminals w/ MAO; reacumulate from synapse if cleaning

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Enhance NE release?

angiotensin II

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Most Cirulating Epi broken down by

MAO/COMT

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Most of NE removed by

recycled into terminal by NET

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receptors effects dependent on

g protein, kinases in target cell

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Guanethidine

Mech

enters via NET, depletes NE

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Reserpine

Mech

Enters terminal (lipid-solube), stops VMAT, NE can’t be recycled

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MAOI inhibitors

Mech

accumulate intracellular NE, increased NE synapse levels

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MAOI 8

Tranylcypromine (anti-depressant)

PARNATE

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Amphetamine

Mech

Increase NET activity
more NE release

Faster kinetics than guanethidine/reserpine = gradual NE depletion

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Large Tyramine load?

wine, cheese, beer, fava beans

MAO cleans tyramine, so MAO taken up
up NE = HTN
NO MAOIs w/ large tyramine load

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Block NET, Up synaptic NE

Cocaine
Imipramine TOFRANIL
Atomoxetine ASENDIN

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Alpha Ag

Phenylephrine

Beta Ag

Isoproterenol ISUPREL

Apha blocker

Phentolamine REGITINE

Beta blocker

Propanolol

Chronic ag treatment causes

desensitization | Downregulation

Chronic blocker treatment causes

supersensitization | Upregulation

NE likes

1s A1/B1

Isoproteranol likes

Betas used to stimulate heart

Epi likes

low dose = betas b1 b2 | High dose = everything

Dopamine likes

low: DA, b1 High: everything

Dobutamine likes

Low: b1 (UP contractility w/o effect HR) HUGE AMINE SUBSTITUTION High: may affect rate

B1 receptors like

Iso>epi=NE

B2 receptors like

iso> epi>>NE

A1 receptors like

epi>NE >> iso | Normally will see NE

Catecholamine structure

OH on 3+4 | amine side chain (LARGER = Up Beta receptor affinity)

Catecholamine Mech How to increase CNS penetration

remove hydroxyl groups (3+4)

COMT ONLY breaks down

catecholamines

What blocks MAO metabolism?

substitute A carbon

Contractility (SBP/CO) stimulated by

B1 Also up O2 use Down efficiency

Peripheral resistance (DBP) lowered by

Epi effects timeline

* B1+B2 = up contractility up HR, down peripheral resistance * then A1 = vasoconstriction * up HR then reflex lowers

Epi effects Blood pressure

B2 + A1 low: decrease (b2 dilation) High: increase (a1 constriction)

Epi effects Respiratory

B2 + A1 * Bronchioles dilated (B2) * Secretions decreased (A1)

Epi effects Metabolism

* glycogen breakdown (b2) * DOWN glycogen synth (a1) * DOWN insulin secretion (a2) * UP free fatty acids (b3) * Detruser muscle relax (b3)

Anaphylactic shock?

Epi * Open airways (b2) * Down histamines/leukotrienes (b2) * Up BP (a1)

Epi uses

* anaphylactic shock * Asthma (B2) * topical hemostasis (a1) * cardiac arrest (b1)

Epi S.E.

Arrythmia CVA emotional

NE Effects

* Heart (b1) * BP UP sys/dia/mean (a1) * CO same or down (a1) * DOWN Glyc synthase (a1)

Shock? Neurogenic w/ spinal anesthesia old-school Rx

NE (levophed)

Isoproterenol effects

* Heart (B1) * DOWN BP (B2) * Relax bronchi (B2)

Stimulate Heart in Heart block/pacemaker insertion?

Isoproterenol

Isoproterenol S.E.

* Fatal Arrythmia * Tachycardia * Palpitations * Anginal pain

Overactive bladder?

Mirabegron (b3) MIRBETRYQ

DA effects

DOSE-DEPENDENT * heart rate (b1) * BP = Low dose: DOWN (DA, B2) ;; High dose: UP (a1)

Shock? (cardiogenic)

DA S.E.

* Tachycardia * anginal pain * arrythmia * N/V (DA @ CTZ) NO CNS EFFECTS

Dobutamine Effects

* heart (B1) CONTRACTILITY ONLY | * BP= high dose: UP (a1)

Heart failure w/ open heart surgery/MI?

Dobutamine

Dobutamine S.E.

*arrythmia NO CNS EFFECTS

A1 ag uses

* decongest mucous membranes * Up BP * Dilate Pupil * Eye drops

A1 ag

A1 ag S.E.

UP BP

Non-catecholamine A1 ag Rx

* phenylephrine (replacing psuedoephedrine) - cold * Phenylpropanolamine PPA (CVA risk-gone) * Ephedrine (CNS, nasal decongest)

Non-catecholamine A1 ag broken down by

NOT COMT Substituted A carb = NO MAO = Longer t 1/2

B2 ags Uses

* Bronchial asthma * Anaphylactic shock (stops mast cells releasing) * Relaxation of uterus/delay labor = many S.E.

B2 ags Uses

B2 ags effects

Skeletal, heart (high dose

Delay premature labor?

``` Ritodrine YUTOPAR (b2 selective) Terbutaline BRETHINE ```

COPD?

Formeterol (B2 ag) PERFOROMIST

Asthma?

* Albuterol/levalbuteraol | * Terbutaline

Nasal decongestant, release NE, CNS stimulant, pressor? | b2 ag

Epehdrine

Narcolepsy

*Amphetamine/ methamphetamine CNS stim = Release NE

Weight reduction

Amphetamine CNS stim

ADHD

* Methylphenidate (Concerta) * Atomoxetine (Strattera) = NE reputake inhbitor NOT SCHEDULED *Lisdexamfetamine dimesylate VYVANSE (amphet prodrug)

CNS side effects

Abuse | Cardio/CNS stimulation

Xanthines

ADENOSINE RECEPTORS Resemble adrenergic stimulation but NOT binding adrenergic receptors (NO BETAS)

Xanthine effects

* CNS - all cortex * Cardio- HR + contractility up * Respiratory = relax bronchi

Xanthines Rx

Caffeine = CNS Theophylline = Heart, Bronchi

Theophylline uses

Aminophylline = asthma +B2 ag = chronic asthma

Adrenergics Flashcards

(83 cards)