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138 Cards in this Set

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Isoproterenol
non-selective Beta agonist. Lowers peripheral vascular resistance. Parenteral administration
Isoproterenol
non-selective Beta agonist. Lowers peripheral vascular resistance. Parenteral administration
Dobutamine
(+ isomer) Beta 1 agonist, alpha1 antagonist. Parenteral administration. Treats shock (low blood volume, hypotension). Dopamine with same effects
Beta2 selective agonists
albuterol, metaproterenol, pirbuterol, terbutaline (short acting). salmeterol, fomoterol, arformoterol (long-acting) (all inhalation)
oral/parenteral beta2 selective agonist
terbutaline
nasal decongestants
phenylephrine, xylometazoline, oxymetazoline (alpha 1 agonists --> local action when applied topically. Sudafed PE = phenylephrine)
Dobutamine
(+ isomer) Beta 1 agonist, alpha1 antagonist. Parenteral administration. Treats shock (low blood volume, hypotension). Dopamine with same effects
long duration of action decongestants
xylometazoline, oxymetazoline
Beta2 selective agonists
albuterol, metaproterenol, pirbuterol, terbutaline (short acting). salmeterol, fomoterol, arformoterol (long-acting) (all inhalation)
epinephrine treats actute
anaphylaxis. Constricts capillary beds, decreasing edema. Binds beta 2 to reverse broncho constriction. Binds beta to suppress histamine, bradykinin, etc. released from mast cells. Raises low blood pressure by binding alpha1 and beta1
PSVT (paroxysmal supraventricular tachycardia)
Arrhythmia caused by Av nodal reentry. Blocking AV node (slowing down) will stop this arrhythmia.
Phenylephrine treats
PSVT. dilates pupil without cycloplegia, nasal decongestion. Also used topically to treat hemorrhoids
oral/parenteral beta2 selective agonist
terbutaline
terbutaline acts on ___ receptors to treat __
Beta 2 receptors, premature labor (stops uterine contractions by relaxing smooth muscle)
nasal decongestants
phenylephrine, xylometazoline, oxymetazoline (alpha 1 agonists --> local action when applied topically. Sudafed PE = phenylephrine)
cycloplegia
paralysis of the ciliary muscle
long duration of action decongestants
xylometazoline, oxymetazoline
epinephrine treats actute
anaphylaxis. Constricts capillary beds, decreasing edema. Binds beta 2 to reverse broncho constriction. Binds beta to suppress histamine, bradykinin, etc. released from mast cells. Raises low blood pressure by binding alpha1 and beta1
phenylephrine
alpha 1 agonist. Short duration of action
PSVT (paroxysmal supraventricular tachycardia)
Arrhythmia caused by Av nodal reentry. Blocking AV node (slowing down) will stop this arrhythmia.
Phenylephrine treats
PSVT. dilates pupil without cycloplegia, nasal decongestion. Also used topically to treat hemorrhoids
ephedrine
releases NE from nerve terminals (indirect NE mimetic). Adrenomimetic --> causes increased NE release from nerve terminals. Formerly used as a weightloss drugs, but too many side effects - e.g. increase HR
terbutaline acts on ___ receptors to treat __
Beta 2 receptors, premature labor (stops uterine contractions by relaxing smooth muscle)
pseudoephedrine
nasal decongestant. (Sudafed)
cycloplegia
paralysis of the ciliary muscle
alpha1 antagonsists (selective, reversible)
prazosin. terazosin, doxazosin, tamsulosin, alfuzosin, silodosin
phentolamine
non-selective alpha antagonist, reversible.
phenylephrine
alpha 1 agonist. Short duration of action
phenoxybenzamine
non-selective alpha antagonist, irreversible.
treats pheochromocytoma
tyramine
indirect action. NOT a drug, comes from a gut bacteria and fermented food. Metabolized by MAO (in liver). If not metabolized in liver, increases NE release. Increased levels can cause hypertension in people who are taking MAO inhibitors.
ephedrine
releases NE from nerve terminals (indirect NE mimetic). Adrenomimetic --> causes increased NE release from nerve terminals. Formerly used as a weightloss drugs, but too many side effects - e.g. increase HR
pheochromocytoma
tumor of adrenal medulla gland - releases a lot of EPI. Treat with phentolamine and phenoxybenzamine
Benign prostatic hyperplasia can be treated with
selective alpha 1 antagonists ( prazosin, terazosin, doxazosin, etc.) Terazosin particularly targets alpha1A receptor subtype on prostate.
pseudoephedrine
nasal decongestant. (Sudafed)
alpha1 antagonsists (selective, reversible)
prazosin. terazosin, doxazosin, tamsulosin, alfuzosin, silodosin
raynaud's disease
cold causes vasospasm in fingers and toes. Treat with prazosin (blocks alpha1 receptors)
phentolamine
non-selective alpha antagonist, reversible.
phenoxybenzamine
non-selective alpha antagonist, irreversible.
catecholamines
NE and EPI
pheochromocytoma
tumor of adrenal medulla gland - releases a lot of EPI. Treat with phentolamine and phenoxybenzamine
Gq results in
increased intracellular calcium, DAG activation of PKC --> phosphorylation of proteins
Benign prostatic hyperplasia can be treated with
selective alpha 1 antagonists ( prazosin, terazosin, doxazosin, etc.) Terazosin particularly targets alpha1A receptor subtype on prostate.
Gi
inhibitory G protein, coupled to alpha 2 receptors.
raynaud's disease
cold causes vasospasm in fingers and toes. Treat with prazosin (blocks alpha1 receptors)
catecholamines
NE and EPI
Mechanism of Gi activity
inhibits adenyl cyclase, increases K+ permeability in terminal bouton of presynaptic cell. Decreases neurotransmitter release
Gq
stimulatory G protein coupled to alpha 1.
Gs
coupled to Beta 1, 2, and 3 receptors. Stimulatory, activates AC to result in cAMP --> PKA --> phosphorylation of proteins
Antagonism of which receptors cause vision changes?
M receptor antagonsist. Allows dilation of the pupil, but prohibits near vision accomodation (ciliary muscle)
Gq results in
increased intracellular calcium, DAG activation of PKC --> phosphorylation of proteins
thermoregulatory sweating uses __ receptors, while sweat glands on palms of hands use ___ receptors
M. Alpha 1
Gi
inhibitory G protein, coupled to alpha 2 receptors.
Mechanism of Gi activity
inhibits adenyl cyclase, increases K+ permeability in terminal bouton of presynaptic cell. Decreases neurotransmitter release
dopamine
activates dopamine receptors (increase RAAS release) on kidney cells, alpha1 (increase CO), beta1 (increase HR)
Gs
coupled to Beta 1, 2, and 3 receptors. Stimulatory, activates AC to result in cAMP --> PKA --> phosphorylation of proteins
dipivefrin
prodrug that converts to EPI. Used as opthalmic agent
phenylephrine
alpha1 selective agonist. Sudafed PE
Antagonism of which receptors cause vision changes?
M receptor antagonsist. Allows dilation of the pupil, but prohibits near vision accomodation (ciliary muscle)
thermoregulatory sweating uses __ receptors, while sweat glands on palms of hands use ___ receptors
M. Alpha 1
xylometazoline
alpha1 selective agonist. Nasal decongestant
dopamine
activates dopamine receptors (increase RAAS release) on kidney cells, alpha1 (increase CO), beta1 (increase HR)
oxymetazoline
alpha1 agonist, alpha2 agonist. Nasal spray
midodrine
alpha1 agonist. Oral
dipivefrin
prodrug that converts to EPI. Used as opthalmic agent
phenylephrine
alpha1 selective agonist. Sudafed PE
alpha1 agonists
phenylephrine, xylometazoline, oxymetazoline, midodrine
alpha 2 selective agonists
brimonidine, apraclonidine (both topical, used for eye)
xylometazoline
alpha1 selective agonist. Nasa
these drugs treat shock
dopamine, dobutamine, NE
oxymetazoline
alpha1 agonist, alpha2 agonist. Nasal spray
ephedrine
mixed-acting - activates alpha and beta receptors. Crosses BBB
midodrine
alpha1 agonist. Oral
to treat hypertension, use
prazosin, terazosin, doxazosin. alpha blockers, selective, reversible.
alpha1 agonists
phenylephrine, xylometazoline, oxymetazoline, midodrine
EPI causes this effect on Beta 2 receptors of skeletal muscle
stimulates the Na+/K+ ATPase. Increases intracellular K+
alpha 2 selective agonists
brimonidine, apraclonidine (both topical, used for eye)
what is the consequence of blocking beta recpeotrs in a diabetic?
impair response to hypoglycemia
these drugs treat shock
dopamine, dobutamine, NE
why use albuterol instead of EPI/isoproterenol to treat asthma?
less side effects. Albuterol is a specific Beta2 agonist. EPI/isoprot are nonselective beta agonsists --> will increase HR
ephedrine
mixed-acting - activates alpha and beta receptors. Crosses BBB
atropine
muscarinic antagonist
ipratropium
muscarinic antagonist
EPI causes this effect on Beta 2 receptors of skeletal muscle
stimulates the Na+/K+ ATPase. Increases intracellular K+
what is the consequence of blocking beta recpeotrs in a diabetic?
impair response to hypoglycemia
Beta2 receptor activation on the liver causes
glycogenolysis --> more glucose in blood, hyperglycemia
scopolamine
M antagonist
why use albuterol instead of EPI/isoproterenol to treat asthma?
less side effects. Albuterol is a specific Beta2 agonist. EPI/isoprot are nonselective beta agonsists --> will increase HR
tropicamide
M antagonist
atropine
muscarinic antagonist
Nonselective Beta receptor antagonists
competitive, reversible. Propanolol, ndolol, timolol, pindolol, carteolol
ipratropium
muscarinic antagonist
Beta2 receptor activation on the liver causes
glycogenolysis --> more glucose in blood, hyperglycemia
Beta 1 selective antagonists
BEAM. Metoprolol, atenolol, acebutolol, betaxolol, bisoprolol, esmolol
scopolamine
M antagonist
raynaud's disease
vasoconstriction in extremities. Treat with alpha-1 blocker - prazosin.
tropicamide
M antagonist
alpha 1 antagonists are used to treat
Raynauds disease (prazosin), BPH (tamsulosin)
Treat BPH with
tamsulosin
Nonselective Beta receptor antagonists
competitive, reversible. Propanolol, ndolol, timolol, pindolol, carteolol
Bethanecol treats
post-operative abdominal distension and urinary retention
Beta 1 selective antagonists
BEAM. Metoprolol, atenolol, acebutolol, betaxolol, bisoprolol, esmolol
Neostigmine treats
myasthenia gravis
Neostigmine mechanism
blocks Acetylcholinesterase, results in more ACh in NMJ
alpha 1 antagonists are used to treat
Raynauds disease (prazosin), BPH (tamsulosin)
Treat BPH with
tamsulosin
Pyridostigmine
reversible AChE blocker. Does not cross BBB
Bethanecol treats
post-operative abdominal distension and urinary retention
Edrophonium
Neostigmine analog - lasts 3-4 min. Can be used to dianose myasthenia gravis (test muscle strength before and after administration)
depolarization blockade
no time for muscle cell to repolarize. Results from too much Neostigmine (too much ACh in NMJ)
Neostigmine treats
myasthenia gravis
Neostigmine mechanism
blocks Acetylcholinesterase, results in more ACh in NMJ
Physostigmine
can reverse effects of muscarinic blocker over dose. Lipid soluble
Pilocarpine treats
Sjogren's syndrome, treats open angle glaucoma, narrow angle glaucoma. Causes pupil constriction. Muscarinic agonist
sjogren's syndrome
autoimmune disorder that affects moistrue producing glands in body
depolarization blockade
no time for muscle cell to repolarize. Results from too much Neostigmine (too much ACh in NMJ)
-olol
Beta blocker. BEAM --> Beta 1 selective
Physostigmine
can reverse effects of muscarinic blocker over dose. Lipid soluble
essential tremor is caused by
activation of beta2 receptors on skeletal muscle. Treat with beta blockers
Pilocarpine treats
Sjogren's syndrome, treats open angle glaucoma, narrow angle glaucoma. Causes pupil constriction. Muscarinic agonist
-idine
alpha 2 agonists. Brimonidine, apraclonidine
sjogren's syndrome
autoimmune disorder that affects moistrue producing glands in body
- zoline
alpha 1 agonists. Xylometazoline, xocymatazoline, midodrine, phenylephrine.
-olol
Beta blocker. BEAM --> Beta 1 selective
what's the difference between physostigmine and neostigmine/pyridostigmine?
physostigmine is lipid soluble, crosses BBB to produces severe CNS side effects. Neostigmine and Pyridostigmine are NOT lipid soluble, reduced CNS effects. More selective at NMJ
2-PAM, Protopam
AChE reactivator. Used in response to irreversible AChE inhibitors.
essential tremor is caused by
activation of beta2 receptors on skeletal muscle. Treat with beta blockers
myasthenia gravis
autoimmune disorder. Antibodies to Nicotinic receptor in the NMJ cause muscle weakness.
-idine
alpha 2 agonists. Brimonidine, apraclonidine
what's the difference between physostigmine and neostigmine/pyridostigmine?
physostigmine is lipid soluble, crosses BBB to produces severe CNS side effects. Neostigmine and Pyridostigmine are NOT lipid soluble, reduced CNS effects. More selective at NMJ
what is the main cause of esophageal varices?
cirrhosis of liver and portal hypertension
2-PAM, Protopam
AChE reactivator. Used in response to irreversible AChE inhibitors.
myasthenia gravis
autoimmune disorder. Antibodies to Nicotinic receptor in the NMJ cause muscle weakness.
what treats postoperative abdominal distension and urinary retention?
bethanecol, neostigmine, pyridostigmine
bethanecol
muscarinic agonist. Direct acting.
dobutamine (-) isomer
alpha1 agonist
what is the main cause of esophageal varices?
cirrhosis of liver and portal hypertension
cevimeline treats
sjogren's syndrome. selective M agonist on salivary glands.
what treats postoperative abdominal distension and urinary retention?
bethanecol, neostigmine, pyridostigmine