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96 Cards in this Set

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Ciliary Muscle Receptors
Muscarinic(M;contract muscle- for near focus)and Beta 2 adrenergic (Beta 2; relax muscle- for far focus) receptors
parasympathetic and sympathetic
Vascular Smooth Muscle Receptors
Alpha1 (contract)and Beta2 (relax) adrenergic receptors
just sympathetic
Sinoatrial Node Receptors
Muscarinic (decreased HR; bradycardia) and Beta1 (and some Beta2) adrenergic (increased HR; tachycardia) Receptors
parasympathetic and sympathetic
Gastrointestinal Smooth Muscle receptors
Muscarinic (contraction) and Beta2 adrenergic (relaxation) receptors
parasympathetic and sympathetic
Bronchial Smooth Muscle Receptors
Muscarinic (contraction) and Beta2 adrenergic (relaxation) receptors
parasympathetic and sympathetic
Sphincter (colonic, esophageal and urinary bladder) Muscle Receptors
Muscarinic (relaxation) and Alpha1 adrenergic (contraction) receptors
parasympathetic and sympathetic
Urinary Bladder Detrusor Muscle Receptors
Muscarinic (contraction) and Beta2 adrenergic (relaxation)
parasympathetic and sympathetic
Urethral Receptors
Muscarinic (relaxation) and Alpha 1 adrenergic (contraction) receptors
parasympathetic and sympathetic
Salivary Gland Receptors
Muscarinic (increased thin watery secretion, copious) and Alpha1 adrenergic (increased mucous secretion, thick)
parasympathetic and sympathetic
Pupil Smooth Muscle Receptors
Muscarinic (contraction circular muscle; constricts pupil; miosis) and Alpha1 adrenergic (contraction radial muscle; dilates pupil; mydriasis)
parasympathetic and sympathetic
Norepinephrine Degrading Enzymes (name, location and inhibitors)
Monoamine Oxidase (MAO, mitochondrial outer membrane, phenelzine) and Catechol-O-methyltransferase (COMT, cytoplasm, tolcapone)
2
Acetylcholine Degrading Enzyme (name, location and inhibitors)
Acetylcholinesterase (AChE, postsynaptic membrane, organophosphates)
Alpha Adrenergic Receptor agonist potency
E >,= NE >> isoproterenol
Beta1 Adrenergic Receptor agonist potency
isoproterenol > E = NE
Beta2 Adrenergic Receptor agonist potency
isoproterenol > E >> NE
Alpha1 Adrenergic Receptor
Signal Transduction
Increases IP3 and DAG
Increase Phospholipase C
Beta Adrenergic Receptors Signal Trasduction
Increase cAMP
activates Gs
Alpha2 Adrenergic Receptor Signal Transduction
Decrease cAMP
activates Gi
adrenergic drugs that pass through the BBB
Reserpine and alpha-methyltyrosine
2
alpha2 selective agonists
clonidine and alpha-methylnorepinephrine (both CNS action)
2
Nonselective (alpha, beta) adrenergic agonists
epinephrine
1
Alpha1 selective agonists
phenlyephrine
1
Beta selective agonists
isoproterenol
1
Beta1 selective agonists
dobutamine
1
Beta2 selective agonists
albuterol
1
Nonselective (alpha1, beta1,2) antagonists
carvedilol
1
Alpha selective antagonists
phentolamine (competitive antagonist; shorter acting-hours) and phenoxybenzamine (irreversible antagonist; longer acting-days)
2
Alpha1 selective antagonists
prazosin
1
Beta selective antagonists
propranolol
1
Beta1 selective antagonist
metoprolol
1
Ganglionic blocker
mecamylamine
1
TH inhibitor
alpha-methyltyrosine
1
DA analog
alpha-methyldopa
1
Adrenergic vesicular uptake inhibitor
reserpine
1
Adrenergic reuptake inhibitors
cocaine and imipramine
2
Indirectly acting sympathomimetics
D-amphetamine (and tyramine)
1 (and 1)
mixed-acting sympathomimetics
ephedrine
1
Choline Esters
bethanechol and carbechol
2
Reversible Acetylcholinesterase Inhibitors
edrophonium, neostigmine, physostigmine, and pyridostigmine
4
Irreversible Acetylcholinesterase Inhibitors
echothiophate(organophosphate)
1
reverses acetylcholinesterase inhibition by an 'irreversible' AChE inhibitor
pralidoxime
1
Cholinergic nerve blocker
botulinum toxin
1
Muscarinic Receptor Antagonists
atropine, ipratropium, scopolamine
3
Beta1 adrenergic receptor agonists -action
increase heart output
Where are the receptors concentrated?
Beta1 adrenergic receptor antagonists- action
prevent increase in heart output by Beta1 agonists
Where are the receptors concentrated?
Beta2 adrenergic receptor agonists- action
open (dilate) airways
Where are the receptors concentrated?
Beta2 adrenergic receptor antagonists- action
constrict airways
Where are the receptors concentrated?
Alpha1 adrenergic receptor agonists- action
constrict vessels, increase BP
Where are the receptors concentrated and usually dominant?
Alpha1 adrenergic receptor antagonists- action
dilate vessels, decrease BP
Where are the receptors concentrated and usually dominant?
ganglionic blockers- example, uses, side effects and contraindications
example: mecamylamine
uses: rapid pressure reduction in acute dissecting aortic aneurysm and clinical management of hyperreflexia
side effects: paralytic ileus, urinary retention, respiratory arrest and syncope.
contraindications: coronary insufficiency and glaucoma
blocks both parasympathetic and sympathetic outflow- effect on organ will be the blockade of the predominat tone of that organ.
alpha-methyltyrosine- action, uses
action: competitive inhibitor of TH
uses: in treatment of pheochromocytoma prior to surgery or when surgery is not feasible
alpha-methyldopa- action, uses
action: crosses BBB, DOPA analog- prodrug converted to alpha-methylnorepinephrine- agonist at Alpha2 adrenergic receptors in CNS
uses: treat hypertension
reserpine- action, uses, side effects
action: irreversible blocking vesicular uptake of catecholamines
uses: original use as an antihypertensive- but side effects too great!!!
side effects: cardiac arrhythmia; crosses BBB- so CNS side effects too
Imipramine- action, uses
action: Reuptake inhibitor
uses: to treat enuresis- by increasing sympathetic tone of bladder sphincter and relaxation of bladder wall.
amphetamine- action, uses, side effects and contraindications
action: indirect acting sympathomimetic
use: treatment of ADHD, narcolepsy and appetite suppression
side effects: tachycardia and hypertension
contraindications: severe hypertension, glaucoma, hyperthyroidism and MAOI therapy- also do not take during pregnancy- adverse effects on fetal development.
ephedrine- action, uses and contraindications
action: mixed acting sympathomimetic
uses: asthma (bronchodilator) and nasal decongestant, also used as a pressor agent during epidural or intra-anesthesia
side effects: tachycardia and hypertension
contraindications: severe hypertension, glaucoma, hyperthyroidism and MAOI therapy.
clonidine and alpha-methylnorepinephrine- action, uses, side effects
action: alpha-2 adrenergic receptor agonists
uses: centrally acting antihypertensives
peripheral side effects: bradycardia, heart failure.
epinephrine- action, uses, contraindications
action: adrenergic receptor agonist
uses: relieve respiratory distress due to bronchospasm, to ease hypersensitivity reactions (anaphylactic shock), used in cardiac arrest (increase heart rate (Beta1), and systolic pressure (Alpha2) and decreases some peripheral vascular resistance (Beta2), also used to prolong action of local anesthetics by local restriction of blood flow (Alpha1)
contraindications: don't give in presence of Beta adrenergic receptor blockade (would lead to severe hypertension and cerebral hemorrhage), also contraindicated in narrow angle glaucoma.
phenylephrine-action, uses, side effects and contraindications
action: alpha1 selective agonist
uses: treatment of shock, hypotension (inc BP by contricting BV) and as a nasal decongestant(decrease blood flow to nasal mucosa decreases mucous production)
side effects: bradycardia and hypertension
contraindications: glaucoma, hypertension
hyperthyroidism, difficulty urinating (enlarged prostate gland)
albuterol- action, uses, side effects, contraindications
action: Beta2 selective adrenergic receptor agonist
uses: treatment of asthma (dilation of airways), COPD
side effects: tachycardia
contraindications: cardiac disease (preexisting arrhythmias), hyperthyroidism
dopamine- peripheral uses
uses: DOC for treatment of shock
used in the treatment of conditions characterized by compromised renal function- like shock- it dilates renal blood vessels.
prazocin- action, uses, side effects
action: Alpha1 selective adrenergic receptor antagonist
uses: treatment of hypertension
side effects: orthostatic hypotension
phentolamine and phenoxybenzamine- action, uses, side effects, and contraindications
action: alpha selective adrenergic receptor antagonists (competitive and irreversible, respectively)
uses: in the treatment of pheochromocytoma, sometimes useful in the treatment of Raynaud disease.
side effects: postural hypotension
contraindications: don't use in patients with decreased coronary perfusion
propranolol-action, uses, side effects and contraindications
action: Beta adrenergic receptor antagonist
uses: treatment of hypertension, angina, performance anxiety, hyperthyroidism, glaucoma (dec secretion of aqueous humor)
side effects: bronchospasm, AV-block and bradycardia
contraindications: bronchial asthma, COPD and bradycardia
metoprolol-action, uses, side effects and contraindications
action: Beta1 selective adrenergic receptor antagonist
uses: angina, heart failure(decrease heart output), hypertension
side effects: bronchospasm, atrioventricular block
contraindications: asthma, sinus bradycardia
carvedilol
action: nonslective adrenergic receptor antagonsist (alpha1, Beta1 and Beta2)
uses: treatment for congestive heart failure, hypertension
What is the rate limiting step in acetylcholine synthesis?
Choline uptake
LUSHPADS BBB
Lacrimation
Urination
Salivation
Hypotension
Pinpoint pupils
Accomodation
Defecation
Sweating

Bronchial contriction
Bonchial secretion
Bradycardia
muscarinic effects of acetylcholine
DUMBELS
Diarhea
Urination
Miosis
Bronchial constriction/secretion
Excitation (skeletal muscle and CNS)
Lacrimation
Sweating/salivation
acetylcholine effects
Direct Cholinomimetics
Choline esters: bethanocol and carbachol
2
Indirect Cholinomimetics
Acetylcholinesterase inhibitors
Reversible: edrophonium, neostigmine, physiostigmine, pyridostigmine
Irreversible (organophosphate): echothiophate
Acetylcholinesterase inhibitors
4 reversible
1 irreversible
Reverses 'irreversible' acetylcholinesterase inhibition
pralidoxime
1
Cholinergic Nerve Blocker
(blocks Ach release)
Botulinum toxin
1
Muscarinic Receptor Anatagonists
atropine, ipatropium, scopolamine
3
Carbachol- action, uses, side effects
action: Direct cholinomimetic-choline ester - resistant to hydrolysis by acetylcholinesterase.
uses: wide angle glaucoma, narrow angle glaucoma- treatment immediately prior to surgical iridotomy, cause pupil constriction (miosis) for eye surgery.
side effects - are reduced due to local application and poor absorption profile (quaternary amine)
Bethanechol-action, uses, side effects and contraindications
action: Direct cholinomimetic-choline ester- highly resistant to acetylcholinesterase and highly selective for muscarinic receptors-
uses: for treatment of urinary retention
side effects: LUSHPADS BBB
contraindications: peptic ulcer, asthma, coronary insufficiency, hyperthyroidism, gastrointestinal/urinary tract obstruction
Edrophonium-action, uses
action: Indirect cholinomimetic- reversible acetylcholinesterase inhibitor short half-life of inhibition (10-20 min)
uses: diagnosis of Myesthenia Gravis, reversal of pharmacologically induced neuromuscular block from competitive blockade (tuboburarine) not depolarization blockade (succinylcholine)
Neostigmine- action, uses, side effects, contraindications,
action: Indirect cholinomimetic- reversible acetylcholinesterase inhibitor- intermediate half-life of inhibition (30min-2hrs)
uses: treatment of Myasthenia Gravis, reversal of pharmacologically induced neuromuscular block from competitive blockade (tuboburarine) not depolarization blockade (succinylcholine), alleviate smooth muscle atony of gastrointestinal and urinary tract.
side effects: LUSHPADS BBB
contraindications: peptic ulcer, asthma, coronary insufficiency, hyperthyroidism, gastrointestinal/urinary tract obstruction, don't use when using succinylcholine for depolarization blockade during surgery
Pyridostigmine-action, uses
action: Indirect cholinomimetic- reversible acetylcholinesterase inhibitor- intermediate half-life of inhibition (3 to 6 hrs)
uses: treatment of Myasthenia Gravis, reversal of pharmacologically induced neuromuscular block from competitive blockade (tuboburarine) not depolarization blockade (succinylcholine), alleviate smooth muscle atony of gastrointestinal and urinary tract.
Physiostigmine- action, uses, side effects, contraindications
action: Indirect cholinomimetic- reversible acetylcholinesterase inhibitor-intermediate half-life of inhibition.
(Can gain access to CNS since not a quaternary amine)
uses: wide angle glaucoma (local application), treat GI or urinary atony (increases motility), also to treat antimuscarinic toxicity and other drugs that have antimuscarinic effects
side effects: LUSHPADS BBB
contraindications: peptic ulcer, asthma, coronary insufficiency, hyperthyroidism, gastrointestinal/urinary tract obstruction, don't use when using succinylcholine for depolarization blockade during surgery
Echothiophate-action, uses
action: Indirect Cholinomimetic- organophosphate-irreversible acetylcholinesterase inhibitor -long half-life of inhibition.
uses: treatment of wide angle glaucoma, treatment of strabismus
Pralidoxime- action, uses
action: reverses 'irreversible' acetylcholinesterase inhibitor
note: also has some action as an inhibitor of acetylcholinesterase- so don't use with a non-organophosphate acetylcholinesterase inhibitor- would potentiate effect.
uses: in the treatment of organophosphate toxicity
Side effects of cholinomimetics:
LUSHPADS BBB
Contraindications of cholinomimetics:
peptic ulcer, asthma, coronary insufficiency, hyperthyroidism, gastrointestinal/urinary tract obstruction
Acetylcholinesterase inhibitors are contraindicated when-
using succinylcholine for depolarization blockade during surgery
Botulinum Toxin-action, uses
action: Cholinergic nerve blocker- blocks release of acetylcholine from nerve terminal
uses: treament of spasm of the eyelid, larynx, used for facial paralysis, cosmetics, and to prevent profuse sweating
Atropine-action, uses, side effects,
action: muscarinic receptor antagonist
uses: preoperative medication to reduce salivation and respiratory secretions, to reverse bradycardia, treat spastic disorders of the GI and urinary tracts, in the treatment of organophosphate poisoning, to treat muscarine poisoning
side effects: reverse of LUSHPADS BBB
Scopolamine-action, uses, side effects, contraindications
action: muscarinic receptor antagonist
uses: motion sickness (CNS action)
side effects: reverse of LUSHPADS BBB
contraindications: narrow angle glaucoma, prostatic hypertrophy, cardiac disease,
Ipatropium-action, uses,
action: muscarinic receptor antagonist
uses: asthma- decreases both watery and mucous secretions, COPD
side effects reduced due to the fact that its a qauternary amine that given directly to lungs by inhalation-
Non-depolarizing Neuromuscular Blockers-names and uses
names:tubocurarine, pancuronium, vecuronium, rocuronium
uses: relax muscles during surgery
4
Depolarizing Neuromuscular Blockers-names and uses
name:succinylcholine
uses: when rapid endotracheal intubation is required, also used during elctroconvulsive shock treatment
1
Neuromuscular Blocker- block Ach release from terminal
botulinum toxin
1
Stimulate release of Ach from neuromuscular junction
4-aminopyridine
1
Spasmolytic drugs
baclofen, diazepam, cyclobenzaprene, dantrolene
4
Isoproterenol-action, uses
action: beta selective adrenergic receptor agonist
uses: rarely used as a bronchodilator in asthma, can be used to stimulate the heart in emergency situations
dobutamine-action, uses, contraindications
action: Beta1 selective adrenergic receptor agonist
uses: increase cardiac output in congestive heart failure
contraindications- should be used with caution with atrial fibrillation