Autonomic Drugs Flashcards
A1 Receptor (location, action, preferred substrate)
location: smooth muscle
action: vasoconstriction
preferred substrate: Epi> NE
A2 Receptor (location, action, preferred substrate)
location: nerve terminals
action: inhibits release of neurotransmitters
preferred substrate: Epi> NE
B1 Receptor (location, action, preferred substrate)
location: heart
action: increase rate and contractility
preferred substrate: isoproterenol>Epi>NE
B2 Receptor (location, action, preferred substrate)
location: respiratory smooth muscles; uterus
action: broncho/vasodilation, uterine relaxation
preferred substrate: isoproterenol>Epi>NE
B3 Receptor (location)
location: brown fat
D1 Receptor (location, action, preferred substrate)
location: splanchnic and renal vessels
action: vasodilation of renal blood vessels
preferred substrate: dopamine
D2 Receptor (location, action, preferred substrate)
location: nerve terminals of CNS
action: regulates neurotransmitters
preferred substrate: dopamine
M1 Receptor (location, action, preferred substrate)
location: CNS
action: stimulation
preferred substrate: ACH
M2 Receptor (location, action, preferred substrate)
location: heart
action: decrease HR
preferred substrate: ACH
M3 Receptor (location, action, preferred substrate)
location: smooth muscle: GI, GU, Pulmo, Eye
action: gut peristalsis, bladder contraction, bronchoconstriction, pupil constriction
preferred substrate: isoproterenol>Epi>NE
Cholinergic inhibitors steps: synthesis
hemicholinium
Cholinergic inhibitors steps: storage
vesamicol
Cholinergic inhibitors steps: release
botulinum
Cholinergic inhibitors steps: termination (metabolism)
neostigmine
Cholinergic inhibitors steps: termination (reuptake)
none
Adrenergic inhibitors steps: synthesis
metyrosine
Adrenergic inhibitors steps: storage
reserpine
Adrenergic inhibitors steps: release
guanethidine
Adrenergic inhibitors steps: termination (metabolism)
MAOIs, COMTIs
Adrenergic inhibitors steps: termination (reuptake)
Cocaine, TCAs
[Cholinergic drugs]
bowel and bladder atony
MOA: direct acting M agonist, M2-M3
Bethanecol
“B= Bethanecol = bowel and bladder atony”
(carbacol for glaucoma)
[Cholinergic drugs]
Sjorgen syndrome (xerostomia, xerophthalmia and rheumatoid arthritis)
MOA: direct acting M agonist, M1 M2 M3
“cry, drool, sweat on your pillow”
Pilocarpine
[Cholinergic drugs]
diagnosis of myasthenia gravis, differentiation of myastenic and cholinergic crisis (indirect acting cholinomimetic)
“tensilon test”
Edrophonium
[Cholinergic drugs]
treatment of myasthenia gravis
Pyridostigmine
“-stigmine”
[Cholinergic drugs]
Reversal of nondepolarizing neuromuscular block
Neostigmine
[Cholinergic drugs]
treatment of glaucoma
[PLE-TSU]
Physostigmine, Pilocarpine - trabecular meshwork
Latanoprost - schlemm
Epinephrine - uveoscleral vein
[Cholinergic drugs]
diagnosis of bronchial hyperreactivity (direct acting M agonist, M3)
methacoline
[Cholinergic drugs]
treatment of Alzheimer disease (Acetylcholinesterase inhibitor)
Donepezil
Rivastigmine (patch)
How does EDROPHONIUM differentiate myasthenic crisis from cholinergic crisis?
EDROPHONIUM
IMPROVES muscle strength in myasthenic crisis
WEAKENS muscle strength in cholinergic crisis
Small cell cancer may present with a myasthenia-like paraneoplastic syndrome. What is this condition called?
Lambert-Eaton Syndrome
What are the signs and symptoms of organophosphate poisoning?
DUMBBELSS diarrhea urination miosis bronchospasm bradycardia excitation (skeletal muscle and CNS) & Emesis lacrimation sweating salivation
[Cholinergic Antagonists]
induction of mydriasis(innervation of radial muscles) and cycloplegia (loss of accommodation)
tropicamide
[Cholinergic Antagonists]
Parkinsons disease
Biperiden
[Cholinergic Antagonists]
Sinus bradycardia
atropine
[Cholinergic Antagonists]
Chronic obstructive pulmonary disease(COPD)
Ipratropium
[Cholinergic Antagonists]
Motion sickness, sea sickness
Scopolamine
[Cholinergic Antagonists]
Gastrointestinal spasms
hyoscyamine, HNBB (Hyoscine N-butylbromide)
“glycopyrrolate”
[Cholinergic Antagonists]
treatment for organophosphate poisoning/ nerve gas poisoning
Pralidoxime + Atropine
Muscarinic Antagonists for Parkinson Disease
“Try to Park your Benz, beep here.”
TRIhexyphenidyl
BENZtropine
BIPeriden
Why is Ipratropium the preferred bronchodilator in patients with comorbid COPD and heart disease?
Ipratropium is less likely to cause tachycardia and cardiac arrhythmia
What are the signs of atropine toxicity?
HOT as a hare DRY as a bone RED as a beet BLIND as a bat MAD as a hatter
Contraindications to muscarinic blockers
cautious use in infants,
acute angle-closure glaucoma,
benign prostatic hyperplasia
[Adrenergic Agonists]
drug of choice for anaphylactic shock, adjunct to local anesthesia, cardiac arrest, croup
epinephrine
[Adrenergic Agonists]
acute CHF, cardiac stress testing
dobutamine
[Adrenergic Agonists]
acute CHF, shock (cardiogenic, septic)
dopamine
[Adrenergic Agonists]
Alpha> Beta receptor affinity
uses: neurogenic shock
SE: reflex bradycardia (baroreceptor mechanism to achieve hemostasis)
norepinephrine
[Adrenergic Agonists]
nasal congestion, mydriasis without cycloplegia
phenylephrine
antidote: phentolamine
[Adrenergic Agonists]
SE: rebound hypertension on discontinuation
clonidine
antidote: phentolamine
[Adrenergic Agonists]
SE: hemolytic anemia (positive Coombs test)
methyldopa
[Adrenergic Agonists]
bronchial asthma, COPD
acute asthma attack DOC
salbutamol
[Adrenergic Agonists]
tocolysis for preterm labor
terbutaline
ritodrine
isoxuprine
Direct NON-SELECTIVE Adrenergics/Sympathomimetics
"DINE" Dopamine Isoproterenol Norepinephrine Epinephrine
Epinephrine MOA
Epinephrine MOA
A1: vasoconstriction, increase BP
B1: increase HR, conduction and contractility
B2: bronchodilation
- can cross placenta (may cause fetal anoxia)
Norepinephrine MOA
Norepinephrine MOA
A1: vasoconstriction, increase BP
B1: increase HR, conduction and contractility
Dopamine MOA
Dopamine MOA
A1: vasoconstriction, increase BP
B1: increase HR, conduction and contractility
D1: vasoDilation in splanchnic and renal blood vessels
Isoproterenol MOA
non selective beta adrenergic receptors activator
B1: increase HR, conduction and contractility
B2: bronchodilation
uses: asthma
Direct ALPHA 1 Adrenergics/Sympathomimetics drugs
Phenylephrine pseudophedrine oxymetazoline tetrahydrozoline midrodine naphazoline xylometazoline
Direct ALPHA 1 Adrenergics/Sympathomimetics MOA
Phenylephrine pseudophedrine oxymetazoline tetrahydrozoline midrodine naphazoline xylometazoline
MOA:
A1: vasoconstriction, increase BP
SE: rebound nasal congestion (rhinitis medicamentosa)
- avoid PSEUDOEPHEDRINE in 1st term, may cause gastroschisis
- Phentolamine - DOC for A1 agonist overdose
Direct ALPHA 2 Adrenergics/Sympathomimetics drugs
“CAM”
Clonidine
Apraclonidine (+ brimonidine)
Methyldopa (+guanfacine, guanabenz, dexmedetomidine, tizanidine)
Direct ALPHA 2 Adrenergics/Sympathomimetics:
CLONIDINE
MOA
Direct ALPHA 2 Adrenergics/Sympathomimetics:
CLONIDINE
MOA:
A2: decrease central sympathetic outlfow
*treat rebound HPN with phentolamine
Direct ALPHA 2 Adrenergics/Sympathomimetics:
METHYLDOPA, guanfacine, guanabenz, dexmedetomidine, tizanidine
MOA
Direct ALPHA 2 Adrenergics/Sympathomimetics:
METHYLDOPA, guanfacine, guanabenz, dexmedetomidine, tizanidine
MOA:
A2: decrease central sympathetic outlfow
uses: preeclampsia, GHPN,
dexmedetomidine- used for conscious sedation
tizanidine- used for muscle relaxant
SE: sedation, hemolytic anemia, (+) coomb’s test
Direct ALPHA 2 Adrenergics/Sympathomimetics:
APRACLONIDINE, Brimonidine
MOA
Direct ALPHA 2 Adrenergics/Sympathomimetics:
APRACLONIDINE, Brimonidine
MOA: decrease secretion of aqueous humor
uses: glaucoma
Direct BETA 1 Adrenergics/Sympathomimetics drug
Direct BETA 1 Adrenergics/Sympathomimetics drug
dobutamine
Direct BETA 2 Adrenergics/Sympathomimetics drug
Direct BETA 2 Adrenergics/Sympathomimetics drug
salbutamol albuterol terbutaline isoxuprine ritodrine
Direct BETA 2 Adrenergics/Sympathomimetics
salbutamol, albuterol, terbutaline, isoxuprine, ritodrine
MOA
Direct BETA 2 Adrenergics/Sympathomimetics
salbutamol, albuterol, terbutaline, isoxuprine, ritodrine
MOA:
B2: bronchodilation
uses:
salbutamol- acute asthma attack DOC
used as vasodilator in Reynaud’s phenomenon; may cause maternal pulmonary edema
isoxuprine
most common SE of B2 agonists
muscle tremor, palpitations
Indirect adrenergics/sympathomimetics (releasers)
Phenylpropanolamine
Indirect adrenergics/sympathomimetics (releasers): Phenylpropanolamine MOA
Indirect adrenergics/sympathomimetics (releasers): Phenylpropanolamine
MOA: act mainly by causing release of NE, but also has direct agonist activity at some adrenergic receptors; activates A and B adrenergic receptors in respi mucosa
uses: nasal vasoconstrictor, appetite suppressant
* may precipitate hemorrhagic stroke especially in women
[Dose dependent action of dopamine]
vasodilation in the splanchnic and renal vascular beds via D1 receptors
low dose (1-5 mcg/kg/min)
[Dose dependent action of dopamine]
increased renal blood flow and urine output
low dose (1-5 mcg/kg/min)
[Dose dependent action of dopamine]
increased renal blood flow, heart rate, cardiac contractility, and cardiac output via B1 receptors
medium dose (5-15 mcg/kg/min)
[Dose dependent action of dopamine]
vasoconstriction and increased blood pressure via alpha receptors
high dose (>15 mcg/kg/min)
[Adrenergic Antagonist]
preoperative treatment if pheochromocytoma
phenoxybenzamine (non-selective, irreversible)
[Adrenergic Antagonist]
treatment of rebound hypertension
phentolamine
tolazoline
(non-selective, reversible)
[Adrenergic Antagonist]
benign prostatic hyperplasia
SE: first dose orthostatic hypotension
"-osin" prazosin doxazosin terazosin tamsulosin silodosin alfuzosin
[Adrenergic Antagonist]
most selective for prostatic smooth muscle
tamsulosin
[Adrenergic Antagonist]
not indicated in females for treatment of hypertension
Alpha 1 selective adrenergic antagonists "-osin" doxazosin tamsulosin silodosin alduzosin
[Adrenergic Antagonist]
- used for angina prophylaxis, hyperthyroidism
- masks hypOglycemia in diabetics
SE: bronchospasm, erectile dysfunction
nonselective beta adrenergic antagonists (L-Z except Carvedilol and Carteolol) propranolol pindolol timolol labetalol carvedilol nadolol levobunolol metipranolol carteolol
[Adrenergic Antagonist]
combined alpha and beta blockade (may be used in pheochromocytoma)
“CL”
carvedilol
labetalol
[Adrenergic Antagonist]
adverse effects: IUGR, small placenta and congenital abnormalities have been reported with use, but no adequate and well-contracted studies conducted
Propranolol
[Adrenergic Antagonist]
used as ophthalmic drops for glaucoma
metipranolol
[Adrenergic Antagonist]
has longest half-life
“NAsa DOLO”
Nadolol
Beta blockers with intrinsic sympathomimetic (partial agonist) activity
“ISA PA! isa pa! isa pang chicken joy”
Intrinsic sympathomimetic activity = Pindolol, Acebutolol
[Adrenergic Antagonist]
Beta 1 selectivity
beta 1 selectivity: (A-K except Metoprolol and Nebivolol) atenolol betaxolol esmolol acebutol metoprolol alprenolol nebivolol bisoprolol "NBEAM"
Beta 1 adrenergic antagonist (beta 1 blocker) with shortest half-life
“Esmall-LOL”
esmolol
Beta 1 adrenergic antagonist (beta 1 blocker) that may also be used as ophthalmic solution for glaucoma
betaxolol
use of this cardioselective beta blocker during pregnancy has been shown to lower birthweights and impair fetal growth
atenolol
nonselective beta blocker used to treat glaucoma
timolol
-lack local anesthetic effect
What drugs are used to control blood pressure in pheochromocytoma?
phenoxybenzamine
phentolamine
labetalol
what is the pharmacologic advantage of alpha 1 selectivity?
reflex tachycardia is less common and less severe
non selective adrenergic antagonist
propranolol, timolol
beta1 selective adrenergic antagonist
acebutolol, betaxolol, esmolol, atenolol, metoprolol
[adrenergic antagonist]
partial agonist
pindolol, acebutolol
[adrenergic antagonist]
lacking local anesthetic
timolol
[adrenergic antagonist]
low lipid solubility
atenolol
[adrenergic antagonist]
shortest-acting
esmolol
[adrenergic antagonist]
longest-acting
nadolol
[adrenergic antagonist]
combined alpha and beta blockade
carvedilol, labetalol
a nonselective beta AGONIST
isoproterenol
