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209 Cards in this Set

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Bethanecol
(MOA)
Muscarinic agonist w/ selective GI & GU effects
Bethanecol
(Pharm Effects)
Increase acid secretion, motility & tone, relax sphincters, stim secretion in GI tract, contract detrusor muscle & relax ext sphincter
Bethanecol
(Therapeutic Uses)
*bowel stasis
*post op paralytic ileus
*urinary retention (post op or neurological)
Bethanecol
(Adverse Effects)
Contraindications:
*asthma
*COPD
*peptic ulcer
*CHF
*hyperthryroidism
Succinylcholine
(MOA)
Exhibits specificity for N2 cholinergic receptors in NMJs of sk muscle.
Succinylcholine
(Pharm Effects)
1. NM blocking drug
- IV bolus causes initial contraction followed by a flaccid paralysis lasting 3-5 min.
- Plasma cholinesterase determines quantity of drug to reach NMJ
- Termination of action is determined by diffusion
Pilocarpine
(MOA)
- Muscarinic receptor agonist
- Not metabolized by AChase or pseudocholinesterase
Pilocarpine
(Pharm Effects)
Contraction of meridional fibers of ciliary muscles > Increases iridiocorneal angle > Increasing outflow of aqueous humor
Pilocarpine
(Therapeutic Uses)
Glaucoma
Dry Mouth (Sjogren's syndrome)
Pilocarpine
(Adverse Reactions)
In trmt of glaucoma:
*lens fixation impairs far vision
*persistent miosis causes poor night vision

Contraindications:
*asthma & COPD (bronchoconstriction)
*peptic ulcer (increased production of gastric acid)
*hyperthyroidism (atrial flutter or fib)
*dilated heart (atrial flutter or fib)
Betaxolol
(MOA)
Beta-adrenoreceptor antagonist
Betaxolol
(Pharm Effects)
- Decreases aqueous humor
- Decreases IOP 20-30%
Betaxolol
(Therapeutic Uses)
Open Angle Glaucoma
Betaxolol
(Adverse Reactions)
Systemic absorb-bradycardia
(Selective for B1-little effect on bronch smooth muscle)
Timolol
(MOA)
Beta-adrenoreceptor antagonist
Timolol
(Pharm Effects)
Decrease production of aqueous humor
Lower IOP by 20-30%
Timolol
(Therapeutic Uses)
Glaucoma
Timolol
(Adverse reactions)
Systemic absorption can cause bronchoconstriction & bradycardia
Lantanoprost
(MOA)
Stable analog of PGF 2alpha
(prsostaglandin analog)
Lantanoprost
(Pharm Effects)
-Increase uveoscleral outflow
(Only drug that enhances this)
- Lower IOP by 20-25%
Lantanoprost
(Therapeutic Uses)
Open Angle Glaucoma
Epinephrine
(MOA)
Alpha1-adrenoreceptor agonist
Epinephrine
(Pharm Effects)
-Enhance outflow of aqueous humor via nl press dep path.
-Decreases IOP
Epinephrine
(Therapeutic Uses)
Open Angle Glaucoma
Epinephrine
(Adverse Reactions)
Causes mydriasis via stimulation of alpha1 adrenoreceptors in the radial muscle of the iris
Dipivefrin
(MOA)
Alpha-adrenoreceptor agonist
Dipivefrin
(Pharm Effects)
-Lipid soluble cmpd that penetrates into the ant chamber before being hydrolyzed to epinephrine
-enhance outflow of aqueous humor via nl press dep path
Dipivefrin
(Therapeutic Uses)
Open Angle Glaucoma
Dipivefrin
(Adverse Reactions)
Causes mydriasis via stimulation of alpha1 adrenoreceptors in the radial muscle of the iris
Dorzolamide
(MOA)
Carbonic anhydrase inhibitor
Dorzolamide
(Pharm Effects)
-Topical decrease production of aqueous humor
-Decrease IOP by 10-20%
Dorzolamide
(Therapeutic Uses)
Glaucoma
Donepezil
(MOA)
Carbamate cmpd that is a Reversible inhibitor of AChase
Donepezil
(Pharm Effects)
Inhibits the action of acetyl cholinesterase so that acetylcholine will stay around longer
Donepezil
(Therapeutic Uses)
DOC for Alzheimer’s dz- it is more selective for the CNS
Decreases apathy, hallucinations, anxiety & behavioral problems
Donepezil
(Adverse Reactions)
S/E:
Diarrhea
Muscle cramps
Fatigue
Insomnia
Anorexia
N/V
Neostigmine Quarternary
(MOA)
4º amine
Direct agonist at cholinergic N2 receptor, inhibits AChase (by carbamoylation) at all peripheral sites
Neostigmine Quarternary
(Pharm Effects)
Increases the conc of acetylcholine at N2 receptor of NMJ by blocking AChase, inhibition of AChase increases the conc of ACh at muscarinic sites (eg heart, salivary glands, etc)
Neostigmine Quarternary
(Therapeutic Uses)
*post op paralytic ileus
*atony of the GI & GU tracts
*Myasthenia gravis
*reversal of the muscle paralysis caused by competitive neuromuscular blocking agents
Pyridostigmine
(MOA)
4º amine
Direct agonist at cholinergic N2 receptor, inhibits AChase (by carbamoylation) at all peripheral sites.
Pyridostigmine
(Pharm Effects)
Inhibits the action of acetyl cholinesterase so that acetylcholine will stay around longer
Pyridostigmine
(Therapeutic Uses)
Long-term p.o. dosing used to treat Myasthenia gravis:
*mild ocular symptoms- pyridostigmine + corticosteroids
*mild/mod general symptoms- pyridostigmine + thymectomy
*mod/severe general symptoms- pyridostigmine + azathioprine (an immunosuppressant drug)
Edrophonium
(MOA)
Even though it does inhibit AChase at all peripheral cholinergic nerve junc (carbamoylation of active site), the majority of its action at the NMJ results from direct stim of cholinergic N2 receptors
Edrophonium
(Pharm Effects)
*must be given im or iv b/c of extremely short half life
Edrophonium
(Thearpeutic Uses)
diagnosis of & titrate adequacy of trmt of myasthenia gravis
*distinguish between “myasthenic” & “cholinergic” crisis in pts treated p.o. w/ pyridostigmine
*reversal of muscle paralysis caused by competitive neuromuscular blocking agents such as d-tubocurarine
Carbaryl
(MOA)
Carbamate (insecticide used around the house).
Carbaryl
(Thearapeutic Uses)
Treat carbaryl poisoning w/ atropine (only drug) & supportive care
Carbaryl
(Adverse Reactions)
CNS-Loss of concentration, irritability, forgetfulness, depression, insomnia, slurred speech.
PNS-Miosis, blurred vision, bradycardia, cough
Nicotinic-Cramping, tachycardia
Malathion [Insecticide]
(MOA)
Insecticide that is much safer than parathion, mammals & birds have plasma carboxyesterases which destroy malathion
Malathion [Insecticide]
(Therapeutic Uses)
Spray for mosquitos and in dermatological preparations used to kill head lice
Pralidoxime
(MOA)
-Accelerates the rate of hydrolysis of phosphorylated enzyme, at NMJ.
-Less effective if aging of phosphorylation has occurred
Pralidoxime
(Therapeutic Uses)
Treatment for organophosphate poisoning with Atropine!
DOC for relieving priaprism
Epi (adrenalin) mixed alpha,beta
DOC for mydriasis
Fundoscopic exam
tropicamide
DOC for
uveitis, keratitis, choroiditis
atropine or scopolamine
relaxation of sphincter
DOC for HTN in pregnant woman
alpha methyldopa
DOC for alzheimers disease
donepezil
aricept
DOC for treatment of anaphylactic reactions
epinephrine
cholinergic agonist
succinylcholine
bethanechol
pilocarpine
tertiary muscarinic blockers
diphenhydramine
cyclopenate - receptor
scopolamine - receptor
tropicamide
atropine
benzotropine
carbonic anhydrase inhibitor
dorzolamide
treatment for organophosphate poisoning
pralidoxime
quartenary muscarinic blocker
ipratropiam
glycopyriolate
adrenergic agonist
ephederine
citrodrine
oxymetazoline
albuterol
epi-alpha
isoproterenol
nor-epi
dopamine
phenylephrine
dipivefrin
tertiary carbmate achase inhibitor
carbaryl
dicylamine
donepezil
tertiary muscarinic agonist
tolterodine
alpha blockers
labetalol
tamsulosin
phentolamine
beta blockers
betaxolol
propanolol
esmolol
metoprolol
atenolol
timolol
tertiary amines
vs
quartenary amines
tertiary: Enter CNS-Placenta, eye, breast milk, semen
Quartenary: do not
Quartenary carbamate achase inhibitor
pyridostigmine
neostigmine
edrophonium
sympathetic drug
alpha-methyldopa
why dobutamine over dopamine in tx of MI
dobutamine does not increase DBP (afterload)
dobutamine is less likely to cause tachycardia
dobutamine causes venodilation which decreases venous return (preload), so cardiac filling pressure is decreased.
Pralidoxime
MOA
Quaternary:
Greatly accel the rate of hydrolysis of the phosphorylated enzyme, particularly at NMJ, less effective if “aging” of phosphorylation has occurred, does not enter CNS
Atropine
MOA
1. muscarinic receptor antagonist (Belladonna alkaloids)
2. Tertiary amines enter CNS, cross plancental barrier, penetrate into eye, and pass into breast milk and semen.
3. Blocks central/peripheral muscarinic receptors
Atropine
Pharm Effects
Muscarinic antagonists:
Iris: sphincter relaxation (no miosis) Ciliary relaxation (no near vision)
Cardiac: ↑ atrial & ventricle contraction
♥ conduction: ↑ HR, atrial conduction velocity, AV conduction velocity and automaticity, ↓ APD/ERP
Bronchi relaxation
GI tract ↓ motility and tone
GU detrusor relaxes & sphincter contract
↓ secretion of saliva, lacrimal, sweat, gastric juice, bronchial
Atropine
Therapuetic Uses
1. Treats organophosphate poison
2. Treats carbamate poisoning along with pralidoxime
3. Perioperative use:
-Used to decrease production of saliva/pulmonary secretions
-Counteracts the bradycardia caused by ocular pressure, visceral traction, carotid sinus stimulation or injection of multiple doses of succinylcholine
-reverse competitive neuromuscular blockade caused by drugs like d-turbocurarine
-prevents unwanted muscarinic stimulation which result in the inhibition of AChase at sites innervated by the PNS
4. Ophthalmology:
-Use for determination of refractive error
-DOC for Tx of anterior uveitis, keratitis , & choroiditis; Relaxation of sphincter & ciliary muscles decrease pain
-Used in cataract surgery which req mydriasis for access to lens sac via the pupil
5. CV disease:
-Reversal of digoxin induced AVB
-Reversal of bradycardia in kids
-Tx of hyperactive carotid sinus syndrome
6. GI disease
-Diphenoxylate+atropine (Limotil) for diarrhea: very small atropine dose req to prevent abuse of diphenoxylate opiate (↓ GI motility)
7.Prevents indirect adverse S/E’s of neostigmine & pyridostigmine
8. Blocks central muscarinic receptors: (Parkinson’s Ds)
Atropine
Adverse Effects
1. Parkinson’s Ds.: Cycloplegia, constipation, urinary retention, and dry mouth

Toxicity of atropine-like drugs:
CNS: nervousness, excitation, confusion, hallucinations, weakness, giddiness, muscular incoordination, hypertension, maniacal tendencies.
PNS: dry mouth, thirst, dysphagia, hot/dry/flushed skin, dilated pupils, photophobia, blurred vision, tachycardia, urinary retention, absence of bowel sounds.

Overdose: red as a beet (cutaneous dilation), hot as pistol (hot skin), mad as a hatter (hallucinations/delirium), and dry as a desert (inhibition of salivation/difficulty swallowing)
Scopolamine
MOA
Muscarinic antagonist (Belladonna alkaloids
Scopolamine
Pharm Effects
Relaxes ciliary (no near vision) &/or sphincter muscle (no miosis
Scopolamine
Therapeutic Uses
1. Ophthalmology:
-Used in determination of refractive error
-DOC: Tx of anterior uveitis, keratitis, & choroiditis; Relaxation of sphincter & ciliary muscles dec pain
-Used in cataract surgery which req mydriasis for access to lens sac via the pupil.
2. Motion sickness (prophylactically)
Scopolamine
Adverse Effects
Therapeutic doses can cause somnolence, euphoria, amnesia, and dreamless sleep (reduced REM sleep); Little effect on heart rate.
Cyclopentolate
MOA
Muscarinic antagonist
Cyclopentolate
Pharm Effects
Relaxes ciliary (no near vision) &/or sphincter muscle (no miosis)
Cyclopentolate
Therapeutic Uses
Ophthalmology:
-Used in determination of refractive error
-Used in cataract surgery which req mydriasis for access to lens sac via the pupil.
Tropicamide
MOA
Muscarinic antagonist
Tropicamide
Pharm Effects
1. Mydriasis
2. Short duration of action
3. Cannot penetrate into the ciliary muscle
Tropicamide
Therapeutic effects
Opthalmology:
-DOC for fundoscopic exam requiring mydriasis in thorough exam of retina & optic disc
Benztropine
MOA
Central muscarinic antagonist
Benztropine
Therapeutic Uses
Parkinson’s dz: most effective in tremor, some effect on rigidity, little effect on akinesia/ dyskinesia
Benztropine
Adverse Reaction
Cycloplegia, constipation, urinary retention, and dry mouth (therefore, limited in Parkinson’s dz).
Dicyclomine
MOA
Muscarinic antagonist
Dicyclomine
Therapeutic Uses
GI dz: prevent bowel spasm & dec the pain associated with irritable bowel syndrome
Tolterodine
MOA
Selective M3-muscarinic receptor antagonist effective in tx of urge intcontinence
Tolterodine
Therapeutic Effects
OAB/Urinary incontinence
Prevent post-prostatectomy bladder spasms
Tolterodine
Adverse Reaction
Somnolence, dry mouth, blurred vision, constipation
Solifenacin
MOA
Selective M3-muscarinic receptor antagonist
Solifenacin
Pharm Effects
Fewer CNS effects
Solifenacin
Therapeutic Uses
DOC for OAB/urinary incontinence
Prevent post-prostatectomy bladder
Solifenacin
Adverse Reaction
Less dry mouth
Darifenacin
MOA
Selective M3-muscarinic receptor antagonist
Darifenacin
Pharm Effects
No CNS or CV effects
Darifenacin
Therapeutic Uses
DOC for OAB/urinary incontinence
Prevent post-prostatectomy bladder spasms
Darifenacin
Adverse Reaction
Less dry mouth
Diphenhydramine
(benadryl)
MOA
Muscarinic antagonist
Diphenhydramine
(benadryl)
Pharm Effects
Antihistamine that blocks central muscarinic receceptor
Diphenhydramine
(benadryl)
Therapeutic Uses
Parkinson’s dz: most effective in tremor, some effect on rigidity, little effect on akinesia/ dyskinesia
Diphenhydramine
(benadryl)
Adverse Reaction
Cycloplegia, constipation, urinary retention, and dry mouth (therefore, limited in Parkinson’s dz)
Ipratropium
MOA
Muscarinic antagonist
Ipratropium
Pharm Effects
Relaxes bronchial smooth muscle
Ipratropium
Therapeutic Effects
COPD (bronchitis+emphysema) Imporves ventilation by relaxing bronchial smooth muscle
Glycopyrrolate
MOA
Muscarinic antagonist
Glycopyrrolate
Therapeutic Uses
Perioperative use:
-Used to decrease production of saliva/pulmonary secretions
-Counteracts the bradycardia caused by ocular pressure, visceral traction, carotid sinus stimulation or injection of multiple doses of succinylcholine
-Prevents unwanted muscarinic stimulation which result in the inh of AChase at sites innervated by the PNS.
Varenicline
MOA
1. Partial agonist at central α4 β2 – nicotinic receptors
2. 50% of the intrinsic activity of nicotine
Varenicline
Pharm Effects
1. causes the release of dopamine from the nucleus accumbens
2. blocks the binding of nicotine to α4 β2 – nicotinic receptors
Varenicline
Therapeutic Effects
Smoking cessation
Varenicline
Adverse Reaction
Nausea, insomnia, headache, abnormal dreams, constipation, abdominal pain
Dopamine
MOA
D1>β1>α1
Dopamine
Pharm Effects
Know the doses
Low i.v. dose: 0.5-2.0 μg/kg/min stimulates D1 dopamine receptors = dilates renal afferent arterioles
Intermediate iv dose: 2-10 μg/kg/min stimulates D1 and B1 receptors = ↑ dp/dt
Large dose: >10 μg/kg/min
stimulate a-receptors in resistance arterioles = ↑ TPR & DBP/afterload
Dopamine
Therapeutic Effects
Used to increase BP in hemorrhagic & septic shock and increase CO after MI
Used to increase CO in CHF which is refractory to digoxin plus diuretic drugs
Used to increase urine flow in the tx of barbiturate and salicylate poisoning (inc in RBF results from inc CO and direct renal vasodilation). Small doses used to maintain urine flow in ICU.
Dopamine
Adverse Reaction
1. Cerebrovascular hemorrhage
2. Pulmonary edema
3. B-agonist action: cardiac arrhythmias, angina in CAD patients
4. a-agonist: renal and mesenteric ischemia / mesenteric arterioles rapidly “escape” from the vasoconstrictor effects of
a-adrenoceptor agonist
Dobutamine
MOA
B1≥B2
Dobutamine
Pharm Effects
1. (+) inotropic effects via B1 stimulation ↑SV
2. Arteriolar dilation via B2 stimulation lowers TPR so DBP may fall slightly.
3. Venodilation via B2 stimulation decreases venous return & thus decreases venous filling pressure in pts with MI.
4. Unlike dopamine, dobutamine has little effect on HR at most clinical doses. Excessive doses can cause tachycardia & cardiac dysrhythmias.
5. increase in GFR results solely form the increase in CI, i.e., no effect at renal D1 receptors.
Dobutamine
Therapeutic Uses
Used to increase CO after MI, septic, and Cardiogenic shock

Advantages over dopamine in MI tx:
1. does not inc DBP
2. less likely to cause tachycardia
3. causes venodilation which dec venous return (preload), so cardiac filling pressure is decreased.
Dobutamine
Adverse Reaction
1. Tremor with B2 action

2. B-agonist action: cardiac arrhythmias, angina in CAD patients
Norepinephrine
MOA
α>β1>β2

Pure α-receptor stimulation
Norepinephrine
Pharm Effects
-Direct CV effects: ↑ TPR, DBP
-Indirect CV effects: bradycardia
Norepinephrine
Therapeutic Effects
Used as vasopressor agent when CO & tissue perfusion are relatively normal (spinal shock)
Vasoconstrictor agent with local anesthetic drugs
Norepinephrine
Adverse Reaction
B-agonist action: cardiac arrhythmias, angina in CAD patients
a-agonist: renal and mesenteric ischemia / mesenteric arterioles rapidly “escape” from the vasoconstrictor effects of a-adrenoceptor agonist esp NE

Cerebrovascular hemorrhage
Pulmonary edema
Epinephrine
(adrenalin)
MOA
β2>β1>α
Epinephrine
(adrenalin)
Therapeutic Effects
1. Bronchodilator in patients with asthma & COPD
2. Local application lowers intraocular pressure by increasing outflow of aqueous humor (a1)
3. Vasoconstrictor agent with local anesthetic drugs
4. DOC for the tx of anaphylactic reactions (reverses bronchodilation and laryngeal edema)
4. DOC for relieving priapism (persistent painful erection)
5. Uses as a positive inotropic & chronotropic agent in cardiac arrest (1/3 saved)
Epinephrine
(adrenalin)
Adverse Reactions
Anxiety
B-agonist action: cardiac arrhythmias, angina in CAD patients
a-agonist: renal and mesenteric ischemia
Cerebrovascular hemorrhage
Pulm edema from prolonged TPR increases.
Tremor with B2 action
Isoprotenerol
MOA
B1=B2
Isoprotenerol
Therapeutic Effects
Increases AV conduction in AV block.
Used as a positive inotropic & chronotropic agent in cardiac arrest.
Isoprotenerol
Adverse Reactions
B-agonist action: cardiac arrhythmias, angina in CAD patients
Cerebrovascular hemorrhage
Tremor with B2 action
Albuterol
MOA
B2>>B1
Albuterol
Therapeutic Effects
Used to relieve the bronchoconstriction associated w/ asthma, COPD, & bronchitis with less tachycardia
Albuterol
Adverse Reactions
B-agonist action: cardiac arrhythmias, angina in CAD patients
Tremor with B2 action
Ritodrine
MOA
B2>>B1
Ritodrine
Therapeutic Uses
1. Used to relax uterine smooth muscle in order to delay parturition.
2. Used to relax uterine smooth muscle in order to achieve external version of a fetus from breech position to a vetex position prior to birth.
3. Used to relieve the bronchoconstriction associated w/ asthma, COPD, & bronchitis with less tachycardia
Ritodrine
Adverse Reaction
B-agonist action: cardiac arrhythmias, angina in CAD patients
Tremor with B2 action
Phenylephrine
MOA
α1 only
Phenylephrine
Therapeutic Uses
Systemic vasoconstrictor agent (increase B/P)
Local application:
1. relieves nasal congestion by constricting the blood vessels of the nasal mucosa.
2. produces mydriasis by contraction of the radial muscle of the iris / Used for fundoscopic exams and ocular surgery
Phenylephrine
Adverse Reaction
a-agonist: renal and mesenteric ischemia
Cerebrovascular hemorrhage
Oxymetazoline
(Afrin)
MOA
α only
Oxymetazoline
(Afrin)
Therapeutic Uses
Used as a nasal decongestant.
Longer duration of action than phenylephrine
Oxymetazoline
(Afrin)
Adverse Reaction
a-agonist: renal and mesenteric ischemia
d-amphetamine
MOA
Indirect acting agonist
no direct agonist effect at adrenoreceptor
d-amphetamine
Pharm Effects
1. Cause the release of endogenous NE stored in noradrenergic fibers.
2. Inc B/P to some extent b/c they release NE from the sympathetic nerves which innervate the blood vessels
d-amphetamine
Therapeutic Effects
Used to treat ADHD and ADD
d-amphetamine
Adverse Reaction
Insomnia
Psychiatric disturbance
a-agonist: renal and mesenteric ischemia / mesenteric arterioles rapidly “escape” from the vasoconstrictor effects of a-adrenoceptor agonist esp NE
Cerebrovascular hemorrhage
Ephedrine
MOA
Mixed agonist
1. Direct B1 & B2 adrenoreceptor
2. indirect: releases endogeous NE which acts at a- & B-adrenoceptors
Ephedrine
Pharm Effects
Direct B-adrenoceptor mediated actions cause bronchodilation in asthma & increased HR, CO, &, AV conduction in AV block.
Indirect a-adrenoceptor mediated actions produce mydriasis, increased B/P, and nasal decongestion.

-Central excitation d/t release of NE in the brain (milder than amphetamine
-Lipid soluble: enters CNS
Ephedrine
Therapeutic Uses
Used as nasal decongestant
Used as a pressor agent to reverse hypotension during anesthesia
Ephedrine
Adverse Reaction
Insomnia
B-agonist action: cardiac arrhythmias, angina in CAD patients
a-agonist: renal and mesenteric ischemia
Cerebrovascular hemorrhage
Tremor with B2 action.
Rebound nasal congestion
Pseudoephedrine
(Sudafed)
MOA
Mixed agonist

Stereoisomer of ephedrine

Lipid Soluble: enters CNS
Pseudoephedrine
(Sudafed)
Pharm Effects
Causes less CNS excitation and less of an increased BP & HR as compared to ephedrine
Pseudoephedrine
(Sudafed)
Therapeutic Uses
Used as nasal and sinus decongestant
Pseudoephedrine
(Sudafed)
Adverse Reactions
Insomnia
B-agonist action: cardiac arrhythmias, angina in CAD patients
a-agonist: renal and mesenteric ischemia
Cerebrovascular hemorrhage
Tremor with B2 action.
Rebound nasal congestion
Tamsulosin
MOA
a-antagonist
a-blockers

selective for α1a:
abundant in smooth muscle of prostate, prostatic capsule, prostatic urethra, and bladder neck / 70% of receptors are a1A-subtype
Tamsulosin
Therapeutic Uses
Prostatic hypertrophy: relieve urinary obstruction to increase urine flow rate
Tamsulosin
Adverse Reaction
Same as phentolamine, except for angina
Phentolamine
MOA
a-antagonist
a-blockers (α1=α2)
Phentolamine
Pharm Effects
CV effects in HTN w/ normal cardiac fxn: ↓ TPR & BP, ↑ HR, dp/dt, & venous capacitance; no effect on CO
Phentolamine
Therapeutic Uses
Epinephrine reversal
HTN
Reversal of the ischemia and tissue necrosis c/b extravasation of dopamine
Pheochromocytoma
Erectile dysfunction
Phentolamine
Adverse Reaction
1. Orthostatic hypotension
2. Angina
4. Failure to ejaculate/retrograde ejaculatin
5. Miosis (unopposed PNS)
6. Nasal congestion (unopposed PNS)
7. Abdominal cramping (unopposed PNS)
Doxazosin
MOA
a-antagonist
a-blockers
Doxazosin
Pharm Effects
CV effects in HTN w/ normal cardiac fxn: ↓ TPR & BP, ↑ venous capacitance; no effect on HR, dt/dt, or CO
Doxazosin
Therapeutic Uses
HTN
Doxazosin
Adverse Reaction
Same as phentolamine, except angina
Labetalol
MOA
a-antagonist
a-blockers

also blocks B1
Labetalol
Pharm Effects
CV effects in hypertensive pts with normal cardiac fxn: ↓ TPR, BP, dp/dt; ↑ venous capacitance; 0/↓ HR; has
no effect on CO
Labetalol
Therapeutic Uses
Hypertension; especially HTN emergency

Not effective in Pheochromocytoma preoperative BP control
Labetalol
Adverse Reaction
Same as phentolamine, except for angina
Ergotamine
MOA
a-antagonist
a-blockers

partial a-agonist
Ergotamine
Pharm Effects
Believed to reduce pain by partial constriction of “dilated” cerebral blood vessels
Ergotamine
Therapeutic Uses
Migraine headache
Ergotamine
Adverse Reaction
Migraine tx S/E’s: spontaneous abortion, muscle pain, paresthesias, digital vasospasm, and gangrene


Same as phentolamine, except for angina
Betaxolol

“BAM”
MOA
B-blockers

Selective for β1
Betaxolol

“BAM”
Pharm Effects
Cardioselectivity ++
Heart: blocks all B1 on left side of charts starting pg. 22 last section
-↓ myocardial oxygen demand and coronary blood flow
BP: the net effect is slow-developing decline in BP, even in pts who were normotensive prior to therapy
Kidney: ↓ (JG cells) renin release 30-50% so plasma renin activity (PRA) & plasma Angiotensin II fall; in hypertensive pts, the 8-10 mmHg decline in BP caused by these drugs may cause salt & H2O retention & ECF volume expansion if filtration fraction is increased.
Lungs: Increased airway resistance
↓ FEV1.
Eye: local application to ↓ IOP by ↓ aqueous humor production via unknown mechanism (exception: propanolol)
Metabolic effects: blocks lipolysis c/b sympathetic stimulation of adipocytes
Betaxolol

“BAM”
Therapeutics Uses
Cardiac dysrhythmias: most effective esp supraventricular arrhythmias, may also prevent the PVC’s c/ b the psychological stress; initiation of therapy soon after MI decreases the probability of subsequent sudden death by 25-40% probably by preventing fatal catecholamine-induced ventricular dysrhythmias.
Angina pectoris: reduces myocardial O2 demand & decreases the frequency of attacks, increases exercise tolerance, and reduces the need for nitroglycerin.
Hypertension
Hyperthyroidsim (Grave’s disease)
Pheochromocytoma
Glaucoma
Migraine headache: fewer episodes; no beneficial effect after headache has begun.
Betaxolol

“BAM”
Adverse Reaction
Heart: depression of myocardial contractility (neg inotropic effect)
Bradycardia: contraindicated in AV block
Up-regulation of B-blockers: sudden cessation of therapy can precipitate cardiac palpitations & tremor
Lungs: large daily doses of the cardioselective B-blockers may also dec FEV1.
Glucose metabolism in type 2 (non-insulin dep) DM: B-blockers do not prevent the insulin release elicited by the orally-acting hypoglycemic drugs like glipizide; despite this fact, the B-adrenoceptors are relatively contraindicated in Type 2 DM.
Impotence: reversible/ mechanism unknown
Atenolol

“BAM”
MOA
B-blockers

Selective for β1
Atenolol

“BAM”
Pharm Effects
Cardioselectivity ++
See Betaxolol
Least decrease in FEV1
Atenolol

“BAM”
Therapeutic Uses
Same as betaxolol
Atenolol

“BAM”
Adverse Effects
Same as betaxolol
Metoprolol

“BAM”
MOA
B-blockers

Selective for β1
Metoprolol

“BAM”
Pharm Effects
Cardioselectivity +
See Betaxolol
Least decrease in FEV1
Metoprolol

“BAM”
Therapeutic Uses
Same as betaxolol
Metoprolol

“BAM”
Adverse Effects
Same as betaxolol
Esmolol
i.v.
MOA
B-blockers
Esmolol
i.v.
Pharm Effects
Cardioselectivity +
t1/2 = 9 min
Esmolol
Therapeutic Uses
Same as betaxolol
Esmolol
Adverse Reaction
Same as betaxolol
Propranolol
MOA
B-blockers

Non-selective (B1 & B2)
Propranolol
Pharm Effect
1. No cardioselectivity
Lung: Most decrease in FEV1
Digits: Digital blood flow may be reduced significantly by non-selective antagonist
Eye: Not used to reduce IOP b/c of its anesthetic effects which may reduce sensation of foreign bodies in the eye
Metabolic: lypolysis, blocks glycogenolyis in liver and skeletal musc.
Propranolol
Therapeutic Uses
Pheochromocytoma: used before and during surgery in combo with a-antagonist
Essential tremor: non-selective drugs are most effective (a portion of the tremor derives from peripheral B2 stimulation)
Portal HTN: ↓ in CO c/b propranolol ↓ hepatic portal pressure and hemorrhage from esophageal varices
Propranolol
Adverse Reaction
Up-regulation of B adrenoceptors: “propranolol withdrawal syndrome”
Lungs: contraindicated in COPD and chronic bronchitis b/c ↓FEV1
Glucose metabolism:
Type 1: mask warning s/s of hypoglycemia, slows rate of recover of plasma glucose, produces severe HTN (d/t high plasma [ ] of epi)
Digital blood flow may be reduced significantly by non-selective antagonist & pts complain of cold hands so they are contraindicated in Raynaud’s syndrome and Buerger’s dz; Smoking accentuates fall in digital blood flow.
Exercise intolerance in nonanginal pts: non-selective agents block the increased FEV1, CO, & muscle blood flow caused by vigorous exercise
Timolol
MOA
B-blockers

Non-selective (B1-B2)
Timolol
Pharm Effects
No cardioselectivity
Most decrease in FEV1
Timolol
Therapeutic Uses
Pheochromocytoma: non selective B-blockers used before and during surgery in combo with a-antagonist
Essential tremor: an accentuation of the normal physiological tremor of 8-12 Hz that occurs in the absence of other neuro dysfunction; excess caffeine, lack of sleep, alcohol hangover, & strenuous can induce short bouts of tremor, but essential tremor is more persistent & impairs the ability of the pt to perform simple tasks such as writing, eating, & drinking; non-selective drugs are most effective (a portion of the tremor derives from peripheral B2 stimulation
Timolol
Adverse Reaction
Digital blood flow may be reduced significantly by non-selective antagonist & pts complain of cold hands; they are contraindicated in Raynaud’s syndrome and Buerger’s dz; Smoking accentuates fall in digital blood flow.
Exercise intolerance in nonanginal pts: non-selective agents block the increased FEV1, CO, & muscle blood flow cuased by vigorous exercise
Alpha-methyldopa
MOA
-Sympatholytic drug

-a-methyl-NE: stimulates α2-adrenoceptors= ↓ preganglionic sympathetic nerve activity

-↓ SNS reduces the amount of NE and a-methyl-NE released from peripheral sympathetic fibers which innervate the ♥ & blood vessels.

- Symp reflexes are attenuated but not blocked
Alpha-methyldopa
Pharm Effects
Blood vessels dilate passively b/c SNS activity is decreased:
-dilation of arterioles = ↓ TPR & DBP -dilation of venules ↑ venous capacitance & thus lowers venous return = net effect is balanced vasodilation.
Heart: the inc HR which occurs when moving from supine to standing position is attenuated, CO is unchanged or dec slightly, myocardial O2 demand is decresed
Kidney: the dec in renal perfusion pressure may result in increased filtration fraction which slowly causes salt/H2O retention.
Pituitary gland: Prolactin secretion increases.
Alpha-methyldopa
Therapeutic Uses
Used to treat hypertension in kids and pregnant women (b/c it has less teratogenic effects on the fetus)
Alpha-methyldopa
Adverse Effects
Sedation and somnolence, dry mouth and nasal congestion, edema, flu-like syndrome, hepatitis and hyperprolactinemia (males may develop gynecomastia, oligospermia & impotence or dec libido; females can develop amenorrhea and galactorrhea)
Cocaine
Alkaloid of botanical origin
MOA
-Local anesthesia: blocks Na channels in neuronal membranes of sensory pain fibers
-noncompetitive blockade of monoamine uptake1 transporter in central/periph neurons amplifies the postjunctional/ postsynaptic effects of NE, DA, Epi, & serotonin (5HT)
-centrally increases peripheral sympathetic outflow
-euphoria & addictive properties result from inc DA release in nucleus accumbens
Cocaine
Alkaloid of botanical origin
Pharm Effects
Local anesthesia
CNS: Euphoria. Very addicting
Dose-related increase in BP & HR
Vasoconstriction:
-local application of cocaine produces intense vasoconstriction.
-produces noncompetitive blockade of the uptake1 transporter, so NE released by normal symp nerve activity accumulates in the nerve junction. The increased NE concentration in the nerve junction causes persistent stimulation of postjunctional a-adrenoceptors in vascular smooth muscle: persistent vasoconstriction ensues.
Local hemostasis: the intense vasoconstriction accounts for the hemostasis which occurs when cocaine is used as a topical anesthetic agent
Cocaine
Alkaloid of botanical origin
Therapeutic Uses
Local anesthesia in ocular and nasal surgery
Cocaine
Alkaloid of botanical origin
Adverse Reaction
Cardiac dysrhythmias: blockade of Na channels impairs ventricular impulse conduction providing a substrate for re-entrant ventricular dysrhythmias; increases NE release (central effect) and potentiates the cardiac actions of NE (blockade fo uptake1)
MI
Chest pain mimicking MI
Pulmonary edema: results from a direct depressant effect on cardiac contractility and inc afterload
CVA:
Respiratory dz: barotrauma, pulmonary hemorrhage, & hypersensitivity pneumonitis
Seizures
Sudden death
“Crack” burns of the larynx
Necrosis of the nasal septum