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91 Cards in this Set

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EPI
-alpha 1, alpha 2, beta 1, beta 2
-Rapid- alpha-1, only small ↑ in HR b/c of vagal reflex, ↑BP, ↑PP, ↑ TPR
-Slow- beta-2, large ↑ in HR, small ↓ in BP, ↓ TPR, ino=chrono
-prolongs effects of local anesthetics, interacts w/halogenated (↑cardiac effects of CAs)
-anaphylactic/cardiac arrest, redistribution of blood flow
NE
- alpha1, alpha 2, beta1 NO beta 2 agonist
no axn at beta-2 receptors, large reflex ↓ in HR, ↑ BP, ↑ TPR (NO redistribution of blood)
Isoproterenol
- beta 1= beta 2 agonist
large ↑ in HR, small ↑ in BP, ↓ TPR
Dobutamine
Beta 1 agonist
I.V, ino>chrono, cardiac decompensation, ↑ CO w/o ↑ TPR
Beta-2 Agonists
Albuterol
Terbuterol
Metaproterenol
all are more resistant to MAO/COMT, ↓leukotrienes/histamine
Albuterol
Beta 2 agonist
asthma, more selective for beta 2 than other beta 2's
Terbuterol
Beta 2 agonist
status asmaticus (IV)
Metaproterenol
Beta 2 agonist
bronchospasm (less selective)
Alpha 1 agonists
Phenylephrine
Methoxamine
Phenylephrine
Alpha 1 agonist
mydriatic and nasal decongestant, dx of horner’s
Methoxamine
Alpha 1 agonist
I.V. for hypotension, or to indirectly ↓HR in PAT
Alpha 2 agonists
Clonidine
Apraclonidine
Methyldopa
Guanfacine
Side Effects: dry mouth & sedation (50%)
Clonidine
Alpha 2 agonist
hypertension, ADHD/Tourette’s (+Ritalin), withdrawal htn
Apraclonidine
Alpha 2 agonist
Glaucoma ↓ production of aqueous humor
Methyldopa
Alpha 2 agonist
metabolized centrally to α-methylnorepinephrine, activates α2 receptors to ↓
sympathetic outflow
Guanfacine
Alpha 2 agonist
similar to clonidine
Indirect Acting Sympathomimetics
1) Methamphetamine
2) Methylphenidate
3) Atomoxetine
4) Ephedrine
5) Tyramine
6) Cocaine
Side Effects: restlessness, tremor, irritability, headache, “psychosis”, psychological dependence
Uses: obesity, narcolepsy, enuresis, ADHD
Methamphetamine
Indirect Acting Sympathomimetic
-more pronounced CNS effects, less prominent peripheral effects
–Block reuptake of monoamines
–Induces euphoria, increase alertness, decrease fatigue
–Effects last 6-8 hours, initial “rush” assoc. with smoking or injection
Methylphenidate
Indirect Acting Sympathomimetic
more prominent effects on mental activities than motor activities
–Used for ADHD--ADHD etiology is unknown, may be assoc. with DA transmission dysfunction in striatum and prefrontal ctx and an increase in DAT activity
– methylphenidate may decrease/block DAT binding sites--improves focus and inhibitory control
Atomoxetine
Indirect Acting Sympathomimetic
selective NE reuptake inhibitor in prefrontal ctx--non-stimulant, for ADHD (no effect on DA in striatum or nucleus accumbens)
Ephedrine
Indirect Acting Sympathomimetic
•Has direct actions on α and β receptors and acts indirectly to increase NE release--amphetamine-like actions
•Similar effects to EPI and NE, with longer duration. Increases HR, CO, TPR (variably) and usually increases BP. Orally effective. Associated with tachyphylaxis
•CNS stimulant, used for bronchodilation, nasal decongestant. Also used to enhance athletic performance, as an energy enhancer, and for weight loss
Tyramine
Indirect Acting Sympathomimetic
taken up into presynaptic nerve terminals and causes release of catecholamines
•Normal by-product of tyrosine metabolism, and found in many fermented foods (red wine, pickled herring, nuts, aged cheeses, soy and teriyaki sauce)
•Normally metabolized by MAO in the liver without reaching significant blood concentration
•Can ppt. a hypertensive crisis when patients on MAO inhibitors (particularly MAO-A inhibitors) ingest tyramine-containing foods
Cocaine
Indirect Acting Sympathomimetic
block DAT reuptake mechanism--less potent at NE and 5HT reuptake. Also has local anesthetic action, by blocking sodium channels
Alpha Adrenergic Receptor Blockers
Yohimbine
Prazosin
Phentolamine
Phenoxybenzamine
Phenoxybenzamine
Nonselective Alpha Blocker-irreversible
–Decreases PVR, increases CO (symp. reflex)
–α2 blockade increases NE release--reflex tachycardia
–Decreases BP in upright position (dep. on existing tone)
–Uses: pheochromocytoma
–Side Effects: orthostatic hypotension, reflex tachycardia
• Uses: treatment of pheochromocytoma
Phentolamine
Nonselective Alpha Blocker-reversible
Similar actions to phenoxybenzamine
–Uses:
•short term control of BP in patients with pheochromocytoma
•Treatment of hypertensive crisis following clonidine withdrawal or tyramine-MAOI interaction
–Toxicity: hypotension, reflex tachycardia, myocardial ischemia
Prazosin
Alpha1 Selective Blocker
•Major action: arteriolar and venous dilation
•No significant change in HR or reflex tachycardia (no α2 autoreceptor block)
–Also no significant increase in CO
May be beneficial in patients with benign prostatic hyperplasia that are not good surgical candidates
•Adverse effects: first dose phenomenon--marked postural hypotension and syncope, also dizziness, headache, drowsiness
•Uses: hypertension, refractory CHF
Yohimbine
Alpha2 Receptor Blocker
competitive selective α2 receptor antagonist
–Can increase sympathetic outflow centrally and increase release of NE peripherally by blocking autoreceptors
–Increase α1 and β1 activities, increase BP
•Nonselective alpha blockers do not increase BP
–Limited use for treatment of male sexual dysfunction (limited clinical evidence to support this)
Ergot Alkaloids
•Have a variety of effects at α-adrenergic, 5HT and DA receptors
•CNS active
•Used for the treatment of migraine (probably other receptor systems are responsible) and to prevent postpartum hemorrhage
Nonselective Beta Blockers
Propranolol:
Nadolol
Timolol
Pindolol
Inhibit the chronotropic, inotropic, and vasodilating response to β-adrenergic stimulation--have little effect on normal heart at rest (effects depends on existing tone)
Metabolic Effects: block glucose utilization in response to hypoglycemia
–Block peripheral signals of hypoglycemia
–Use with caution in patients with labile diabetes
Propranolol
Nonselective Beta Blocker
highly lipophilic, extensive first pass metabolism, highly protein bound, also used for migraine, stage fright
Nadolol
Nonselective Beta Blocker
long duration of action
Timolol
Nonselective Beta Blocker
short-acting, used for glaucoma
Pindolol
Nonselective Beta Blocker
prototype for ISA
best for patients with obstructive airway disorders
Non-selective beta+alpha 1 blockers
Carvedilol
Labetolol
Carvedilol
Non-selective beta+alpha 1 blocker
nonselective beta blocker, also blocks α1 receptors. Higher β1 : α1 blocking ratio, longer duration of β1 blocking activity

all patients with CHF respond favorably to beta blockers
Labetolol
Non-selective beta+alpha 1 blocker
also blocks α1 receptors, can inhibit Uptake-1, decreases BP with no reflex tachycardia
Sotalol
Nonselective Beta Blocker
antiarrhythmic agent
β1-Selective Antagonists
Atenolol
Esmolol
Acebutolol
Metoprolol
Atenolol
β1-Selective Antagonists
limited CNS penetration, no ISA
Esmolol
β1-Selective Antagonists
short duration, given IV, no ISA or membrane stabilization
Acebutolol
β1-Selective Antagonists
actions similar to metoprolol, has ISA, membrane stabilizing activity
Metoprolol
β1-Selective Antagonists
no ISA, do not use in patients with acute MI associated with bradycardia or heart block
Sympatholytic Agents
Metyrosine
Reserpine
Guanethidine
Bretylium
Metyrosine
Sympatholytic Agents
inhibits catecholamine synthesis. Decreases biosynthesis by inhibitng tyrosine hydroxylase. Used for treatment of pheochromocytoma. Not effective for treatment of hypertension.
Reserpine
Sympatholytic Agents
Reduces cardiac output and PVR. Side effects include sedation, psychotic depression. Irreversibly blocks VMAT, making catecholamines stuck in the nerve terminal where they're eaten up. Depletes the catecholamines.
Guanethidine
Sympatholytic Agents
Interferes with excitation-release coupling to inhibit NE release in peripheral adrenergic nerve terminals. Can also interfere with vesicular storage and act as a false transmitter. Uses: hypertension
Competes for Norepinephrine transporter (NET)
Bretylium
Sympatholytic Agents
prevents invasion of action potentials into nerve terminals—interferes with normal excitation-release coupling. Used for treatment of arrhythmias
Choline Esters
Carbachol
Bethanechol
Indications
•CV (ACh infusion)--to test patency of the endothelium of coronary vessels
•GI disorders (postoperative abdominal distension, gastric atony, adynamic ileus)
•UR bladder disorders (urinary retention, hypotonic, myogenic or neurogenic bladder)
•Ophthalmology: cataract extractions (ACh), wide angle glaucoma (local application--contraction of the ciliary body facilitates outflow of aqueous humor to decrease intraocular pressure)
Adverse Effects of Cholinomimetics
DUMBELS: Diarrhea, Urination, Miosis, Bronchoconstriction, Excitation (of skeletal muscle and in CNS-convulsions), Lacrimation, Salivation and Sweating
Tissue Sensitivity to ACh
Cardiovascular effects >
Smooth Muscle and Glands>
Autonomic Ganglia>
Neuromuscular Junction
Carbachol
Mixed nicotinic and muscarinic agonist
May be used locally in eye to produce miosis
Bethanechol
Mostly muscarinic agonist
GI/Urinary retention
Pilocarpine
Alkaloid muscarinic agonist
-predominantly muscarinic actions; sweat glands very sensitive.
-used as a miotic agent in the treatment of glaucoma (open angle).
-better tolerated than anticholinesterases.
Alcohol Anticholinesterases
edrophonium
donepezil
reversible, non-covalent, short duration
Carbamate Anticholinesterases
Neostigmine
Physostigmine
reversible, covalent, moderate duration
Organophosphates
echothiophate
Malathion
Soman
Sarin
DFP
Irreversible covalent long duration
Edrophonium
Alcohol anitcholinesterase
diagnostic test and to assess the adequacy of dosing of anti-ChE agents in the treatment of myasthenia gravis.
Donepezil
Alcohol anitcholinesterase
Mild to moderate Alzheimer's Disease
Neostigmine
Carbamate anitcholinesterase
Myasthenia Gravis:
Postoperative ileus, atony of smooth muscle of the GI or urinary bladder
Termination of the effects of neuromuscular blockers
physostigmine
Carbamate anitcholinesterase
short acting glaucoma
pyridostigmine
Carbamate anitcholinesterase
intermediate myasthenia gravis
ambenonium
carbamate anticholinesterase
intermediate-long acting myasthenia gravis
Echothiophate
organophosphate
long acting glaucoma, NOT lipid soluble tho
Malathion
organophosphate
insecticide, metabolized well by humans tho
Sarin, Soman, DFP
Organophosphates
lipophilic with excessive muscarinic action
pralidoxime
aka 2-pam
Treatment of organophosphate posioning:
Within 1-2 days: Atropine + 2-PAM
–2-PAM (pralidoxime) exerts a nucleophilic attack on phosporylated enzyme, causing a splitting off of the oxime-phosphonate to regenerate the AChE enzyme
•Primarily affects skeletal muscle; no effect in CNS
•Most effective if given before the “aging” process
Glaucoma Treatment with Anticholinesterases
physostigmine (short-acting), demarcarium (intermediate), echothiophate (long-lasting).
Myasthenia Gravis Treatment with Anticholinesterases
neostigmine (short-acting), pyridostigmine (intermediate), ambenonium (intermediate-long acting).
More lipid soluble agents (e.g., physostigmine) are well absorbed orally and have effects at both peripheral and central sites.
Termination of the effects of neuromuscular blockers
neostigmine, edrophonium
Agents containing quaternary ammonium groups (i.e. edrophonium, neostigmine,) do not penetrate cell membranes easily, they are poorly absorbed from the GI tract or across the skin or into the CNS. These compounds seem to work more selectively at the neuromuscular junction.
Antimuscarinic Agent
Atropine
Scopolamine
Cyclopentolate
Pirenzepine
Tolterodine
Ipratropium
COMPETITIVE blockade
Sensitivity of different effector organs to Atropine
↓salivation > ↓ bronchial secretions, sweating >
pupillary dilation, spasm of lens accommodation > tachycardia > ↓ micturition, ↓ gut tone/motility > ↓ gastric secretion and motility > CNS excitation, delirium, coma
Contraindications for anticholinergics
Contraindications:
–Narrow angle glaucoma (may ppt. closure)
–Prostatic hypertrophy
–Gastric ulcer (slows emptying)
Atropine
Antimuscarinic Agent
Produce mydriasis and
cycloplegia
minimal CNS effects at clinical doses
Atropine is usually the preferred drug unless depressant action is wanted (i.e. preanesthetic medication)
Antitremor activity, useful in treatment of Parkinson's Disease
Scopolamine
Antimuscarinic Agent
motion sickness
Ipratropium
Muscarinic Anticholinergic
Quaternary ammonium.
blocks M2 and M3 receptors
-used as an inhalational drug for treatment of asthma.
-poorly absorbed.
-produces bronchodilation.
-effects limited to mouth and airways—blocks M2 and M, receptors in airways.
Cyclopentolate
Muscarinic Anticholinergic
-Mydriatic.
-shorter duration.
-preferred over atropine or scopolamine
Pirenzepine
Muscarinic Anticholinergic
-selective M1 receptor antagonist.
-used for peptic ulcer; greater GI selectivity, no CNS effects.
Tolterodine
Muscarinic Anticholinergic
Selective for M2 and M3 receptors
-Targets the bladder, fewer side effects
-Urinary incontinence
Nondepolarizing (Competitive) Neuromuscular Blocks
Tubocurarine, Pancuronium, Vecuronium
Depolarizing-Desensitizing Blocks
Succinylcholine
Tubocurarine
Prototype nondepolarizing (competitive, stabilizing) neuromuscular block
-competitively blocks ACh transmitter action
-does not interfere with the contractile capabilities of the muscle
-muscle does not respond to motor-nerve impulses or applied ACh
-histamine release
Succinylcholine
Prototype depolarizing (depolarizing-desensitizing) neuromuscular blocker
-Characteristics of Paralysis: transient muscle fasciculations all over chest and abdomen.
-Neck, arms and legs before facial, lingual, laryngeal and pharyngeal.
-I.V. administration.
-Very short duration; rapidly hydrolyzed by butyrylcholinesterases.
-No significant effect at autonomic ganglia.
-Malignant Hyperthermia
dantrolene
depresses excitation-contraction coupling in skeletal muscle by binding to the ryanodine receptor
treatment for malignant hyperthermia
Anticholinesterases + competitive neuromuscular blockers
reverse or decrease neuromuscular block.
Anticholinesterases + depolarizing blockers
do not reverse, and can enhance the neuromuscular block.
Inhalation anesthetics + competitive neuromuscular blockers
can act synergistically with competitive blockers.
Aminoglycosides + competitive neuromuscular blockers
can act synergistically with competitive blockers.
Ganglionic Blocking Agents
Hexamethonium, Trimethaphan.
-still used for initial control of blood pressure in patients with acute dissecting aortic aneurysm.
-also used in the production of controlled hypotension to minimize hemorrhage in the operative field.
Site
Arterioles
Veins
Heart
Iris
Ciliary Muscle
GI Tract
Urinary Bladder
Salivary Glands
Sweat Glands
PREDOMINANT TONE AT VARIOUS AUTONOMIC EFFECTOR SITES
Site Predominant Tone
Arterioles Sympathetic
Veins Sympathetic
Heart Parasympathetic
Iris Parasympathetic
Ciliary Muscle Parasympathetic
GI Tract Parasympathetic
Urinary Bladder Parasympathetic
Salivary Glands Parasympathetic
Sweat Glands Sympathetic (cholinergic)
PREDOMINANT TONE AT VARIOUS AUTONOMIC EFFECTOR SITES
Site Predominant Tone Effect of Ganglionic Blockade
Arterioles Sympathetic Vasodilation
Veins Sympathetic Vasodilation
Heart Parasympathetic Tachycardia
Iris Parasympathetic Mydriasis
Ciliary Muscle Parasympathetic Cycloplegia
GI Tract Parasympathetic Depressed tone and motility
Urinary Bladder Parasympathetic Urinary retention
Salivary Glands Parasympathetic Xerostomia
Sweat Glands Sympathetic (cholinergic) Anhidrosis