Adrenergic Antagonists

Front 1

non-selective α blockers

Back 1

Phentolamine (competitive reversible), phenoxybenzamine (potent irreversible, 1-2 days)

Front 2

Phentolamine

Back 2

non-selective α antagonist (reversible)
Use: Frostbite, BPH, Impotence (↑ Vasodilation), periph vascular disease, Epinephrine REVERSAL, Miosis, Nasal congestion, PHEOCHROMOCYTOMA (Adrenal tumor, drug blocks alpha1 -> lowers Ca2+)
SE: Reflex TACHYcardia (pre-synaptic α2 blockade), Postural hypotension, arrythmias, anginal pain, excacerbates peptic ulcer

Front 3

Phenoxybenzamine

Back 3

non-selective α antagonist (Irreversible, 1-2 days)
Use: Frostbite, Impotence (↑ Vasodilation), periph vascular disease, BPH
SE: Epinephrine Reversal, Postural Hypotension, reflex tachycardia, NVD, INHIBITS EJACULATION

Front 4

Tx for BPH (Benign Prostatic Hypertrophy)

Back 4

Phentolamine (non-selective reversible α antag) + Papaverine
Terazosin, Tamsulosin (Flomax) ↓ Smooth mm of prostate -> ↑Urine flow

Front 5

α1 Antagonists

Back 5

Prazosin, Terazosin, Tamsulosin (Flomax)
"At 1 Tammy, & Tera Prayed"
use: BPH, moderate hypertension

Front 6

Prazosin

Back 6

α1 antagonist, relax arterioles & veins -> ↓ TPR & BP W/ NO REFLEX TACHYCARDIA
Use: BPH, Moderate Hypertension
1st Dose phenomena (fainting w/ 1st dose)

Front 7

Terazosin

Back 7

α1 antagonist, relax arterioles & veins -> ↓ TPR & BP W/ NO REFLEX TACHYCARDIA
Use: BPH, Moderate Hypertension

Front 8

Tamsulosin

Back 8

α1 antagonist, relax arterioles & veins -> ↓ TPR & BP W/ NO REFLEX TACHYCARDIA
Use: BPH, Moderate Hypertension

Front 9

Yohimbine

Back 9

α2 antagonist
Use: IMPOTENCE

Front 10

Non-selective β antagonists

Back 10

Propanolol, Nadolol (14-24 hrs), Timolol, Pindolol
"The B-Boys Pinned (pain = ISA) Tim's (who can't see well) Nads (for a long time) against the Propane tank"

Front 11

Propanolol

Back 11

Nonselective β Antagonist
Use: Angina, MIGRAINE, CARDIOMYOPATHY, Tremor, Hyperthyroidism, "My doc told me to huff Propane for my HTN & Headaches, and pain"
SE: Bradycardia (β1), CHF, Hypotension, A-V block, Bronchiole constriction (β2) (Tx: Metroprolol)
WITHDRAWAL SYNDROME in angina/MI c/o ↑ # β-R (supersensitivity)
Lipid soluble, High 1st pass effect, metab in liver

Front 12

Nadolol

Back 12

Nonselective β antagonist, LONG ACTING (14-24 hrs), NO CNS (low lipid solubility)
use: ANGINA PECTORIS
SE: Bradycardia (β1), CHF, Hypotension, A-V block, Bronchiole constriction (β2) (Tx: Metroprolol)
WITHDRAWAL SYNDROME in angina/MI c/o ↑ # β-R (supersensitivity)

Front 13

Timolol

Back 13

Nonselective β antagonist
USE: GLAUCOMA, MI prevention
SE: Bradycardia (β1), CHF, Hypotension, A-V block, Bronchiole constriction (β2) (Tx: Metroprolol)
WITHDRAWAL SYNDROME in angina/MI c/o ↑ # β-R (supersensitivity)

Front 14

Pindolol

Back 14

Nonselective β antagonist, Some ISA (Intrinsic Sympathomimetic Activity)
use: Bradycardia, CHF, Elderly w/ HT & Diabetes
SE: Bradycardia (β1), CHF, Hypotension, A-V block, Bronchiole constriction (β2) (Tx: Metroprolol)
WITHDRAWAL SYNDROME in angina/MI c/o ↑ # β-R (supersensitivity)

Front 15

Selective β1 antagonists

Back 15

METOPROLOL, ATENOLOL, acebutolol (has ISA), Esmolol
Use: HTN patients w/ asthma
Cardioselectivity lost at high doses
"My 1st Brother's Heart was Aced by little Esmol who I Met Atending outside CNS (well tolerated)"

Front 16

Metoprolol

Back 16

Selective β1 antagonist (at low doses)
Use: HTN patients w/ asthma
Cardioselectivity lost at high doses

Front 17

Acebutolol

Back 17

Selective β1 antagonist, some ISA (Intrinsic Sympathomimetic Activity)
Use: Arrhythmia, Bradycardia, CHF, Elderly HT pt w/ diabetes
Less ↓HR & CO, less sugar/lipid metabolism disturbances

Front 18

Atenolol

Back 18

Selective β1 antagonist
Use: HTN, does NOT enter CNS, Well-tolerated
Long-acting

Front 19

Esmolol

Back 19

Selective β1 antagonist
Use: Arrhythmia
SHORTEST acting (10 min), RBC esterases metabolize

Front 20

Labetalol

Back 20

mixed α & β antagonist (Racemic mixture (one = α, other = β blocker)), some ISA
Use: Elderly, Black, Preganant w/ HTN
↓ BP w/ periph vasodilation & LESS TACHYCARDIA than phentolamine
"Old Black Pregnant women Labeled (Stereotyped) - which angers them (HTN) & flex Carved ABs"

Front 21

Carvedilol

Back 21

mixed α & β antagonist
Use: HTN & CONGESTIVE HEART FAILURE

Front 22

Guanethidine

Back 22

inhibits release of Norepinephrine -> CHEMICAL SYMPATHECTOMY
use: Severe HTN
SE: General Symp Nervous depression, ↓Ejaculation, Orthostatic Hypotension, supersensitivity to Catecholamines (upreg Receptors)
"Guano - can't poop out your NE"

Front 23

Reserpine

Back 23

Blocks Vesicle uptake/storage of NE
use: Mild HTN, ENTERS CNS
SE: Chronic -> deplete amines (NE, DOPA, 5-HT -> sedation, Depression - suicide)
"NE has to stay in Reserves - sad"

Front 24

Methyldopa

Back 24

PRODRUG -> convert α-methyl-dopamine & α-methyl-NE
FALSE ADRENERGIC TRANSMITTER Stim central (presynaptic) α2-R ↓Sympathetic outflow -> ↓CO, TPR, BP

Front 25

Clonidine

Back 25

α2 agonist
↓Sympathetic outflow -> ↓HR/CO, periph: ↓NE release (block α2-autoreceptor)
↓↓HR & CO more than MethylDOPA (POTENT)
SE: Sedation - fatigue, lassitude, depression
WORSE SIDE EFFECTS!!!

Front 26

Trimethaphan

Back 26

COMPLETELY block N & ACH receptors on Postganglionic neurons (Symp & PS)
Use: HTN (lots of side effects though)

Front 27

Apraclonidine

Back 27

Use: GLAUCOMA
Centrally Acting Sympathomimetic Drug
(alpha2 wants to be CENTER of attention)